IL201239A

(s)-2-{[(2r,3r,4r,5r)-5-(2,4-dioxo-3,4-dihydro-2h-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyl-tetrahydrofuran-2-ylmethoxy]-phenoxy-phosphorylamino}-propionic acid isopropyl ester or a stereoisomer thereof, (s)-isopropyl 2-(((s)-((2r,3r,4r,5r)-5-(2,4-dioxo-3,4-dihydropyrimidin-yl)methoxy)(phenoxy)phosphoryl)amino)propanoate, a method of synthesizing the nucleotides and uses thereof

Abstract

This record has no abstract on file.

Term

No projected expiry on record.

13 claims: 1 independent, 12 dependent

1
201239/4 CLAIMS 1. (S)-2-{[(2R,3R,4R,5R)-5-(2,4-Dioxo-3,4-dihydro-2H-pyrimidin-l-yl)-4-fluoro-3-hydroxy-4-methyl-tetrahydrofuran-2-ylmethoxy] -phenoxy-phosphorylamino } -propionic acid isopropyl ester or a stereoisomer thereof.
8
9. A composition comprising the compound as claimed in claim 8 and a pharmaceutically acceptable medium.

Independent claims2

3,745 paragraphs in 40 sections, as filed

201239/2 -l-pTZrTD-2H-nT7r>4,3-'iop>iKn-4,2)-5-(5R ,4R ,3R ,2R)]}-2-(S) -·Όρΐ3θ-[·Όριηΰι?·’χ-2-τηοΐΊΤ’ΠΊϋα-’7·’ηΏ-4-·’ορπ7,π-3-ΐ“ηχιί?ο-4-(^ιχ

-(S) "lairxiinoo in ίώον >οηοΐΡΝ γτ’πτόπο n^n-fTraN'rmooiD

3-10^7-4,2)-5-(5R,4R,3R,2R)))-(S)))-2 ’rDWir’N -2-1“Π01“Ι7,ΠΊϋϋ’7ιηΏ-4-1θρτηιΠ-3-1Ί1ΝΊϊ70-4-(’71Ν-(2Η)1 □Η’ϋΊΝ^ρΏΠ “Π2Σ1ι57 ΓΚΡΙΖΖ ,DN13NDTlD(l3,’»N(l7,’“nOD1D(,Dp133X,,Dpina(l7,’N an’w cmzru/i (S)-2-{ [(2R,3R,4R,5R)-5-(2,4-Dioxo-3,4-dihydro-2H-pyrimidin-1 -yl)-4-fluoro-3 -hy droxy-4-methyl-tetrahy drofuran-2-y lmethoxy ] -phenoxy-phosphorylamino}-propionic acid isopropyl ester or a stereoisomer thereof, (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-l(2H)-yl)-4-fhioro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoate, a method of synthesizing the nucleotides and uses thereof

Agent Ref: 003638IL

Agent: Borochov Korakh &amp; Co.

Applicant: PHARMASSET,INC. 201239/2 WO 2008/121634 PCT/US2008/058183

This application is being filed on March 25,2008, as a PCT International Patent application in the name of Pharmasset, Inc., a U.S. national corporation, 5 applicant for the designation of all countries except the US, and Michael Joseph Sofia, a citizen of the U.S.; Jinfa Du, a citizen of the U.S.; Peiyuan Wang, a citizen of the People’s Republic of China; and Dhanapalan Nagarathnam, a citizen of the U.S.; applicants for the designation of the US only, and claims priority to U.S. Provisional Application Nos. 60/909,315, filed March 30, 2007; 10 60/982,309, filed October 24,2007; and U.S. Non-Provisional Application No. 12/053,015, filed March 21,2008.

Field of Invention ' 15 The present invention pertains to nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals. The invention provides novel chemical 20 compounds, and the use of these compounds alone or in combination with other antiviral agents for treating HCV infection.

Background

Hepatitis C virus (HCV) infection is a major health problem that leads to chronic liver disease, such as cirrhosis and hepatocellular carcinoma, in a .-1- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 substantial number of infected individuals, estimated to be 2-15% of the world's population. There are an estimated 4.5 million infected people in the United States alone, according to the U.S. Center for Disease Control. According to the World Health Organization, there are more than 200 million infected individuals 5 worldwide, with at least 3 to 4 million people being infected each year. Once infected, about 20% of people clear the virus, but the rest can harbor HCV the rest of their lives. Ten to twenty percent of chronically infected individuals eventually develop liver-destroying cirrhosis or cancer. The viral disease is transmitted parenterally by contaminated blood and blood products, 10 contaminated needles, or sexually and vertically from infected mothers or carrier mothers to their offspring. Current treatments for HCV infection, which are restricted to immunotherapy with recombinant interferon-α alone or in combination with the nucleoside analog ribavirin, are of limited clinical benefit. Moreover, there is no established vaccine for HCV. Consequently, there is an 15 urgent need for improved therapeutic agents that effectively combat chronic HCV infection.

The HCV virion is an enveloped positive-strand RNA virus with a single oligoribonucleotide genomic sequence of about 9600 bases which encodes a polyprotein of about 3,010 amino acids. The protein products of the HCV gene 20 consist of the structural proteins C, El, and E2, and the non-structural proteins NS2, NS3, NS4A and NS4B, and NS5A and NS5B. The nonstructural (NS) proteins are believed to provide the catalytic machinery for viral replication.

The NS3 protease releases NS5B, the RNA-dependent RNA polymerase from the polyprotein chain. HCV NS5B polymerase is required for the synthesis of a 25 double-stranded RNA from a single-stranded viral RNA that serves as a template 2983472-1 -2- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 in the replication cycle of HCV. Therefore, NS5B polymerase is considered to be an essential component in the HCV replication complex (K. Ishi, et al,

Heptology, 1999, 29: 1227-1235; V. Lohmann, et al., Virology, 1998,249: 108-118). Inhibition of HCV NS5B polymerase prevents formation of the double- 5 stranded HCV RNA and therefore constitutes an attractive approach to the development of HCV-specific antiviral therapies. HCV belongs to a much larger family of viruses that share many common features.

Flaviviridae Viruses 10 The Flaviviridae family of viruses comprises at least three distinct genera: pestiviruses, which cause disease in cattle and pigsiyfov/vmy&amp;y, which are the primary cause of diseases such as dengue fever and yellow fever; and hepaciviruses, whose sole member is HCV. The flavivirus genus includes more than 68 members separated into groups on the basis of serological relatedness 15 (Calisher et al., J. Gen. Virol, 1993,70,37-43). Clinical symptoms vary and include fever, encephalitis and hemorrhagic fever (Fields Virology, Editors:

Fields, B. N., Knipe, D. M., and Howley, P. M., Lippincott-Raven Publishers, Philadelphia, PA, 1996, Chapter 31,931-959). Flaviviruses of global concern that are associated with human disease include the Dengue Hemorrhagic Fever 20 viruses (DHF), yellow fever virus, shock syndrome and Japanese encephalitis virus (Halstead, S. B., Rev. Infect. Dis., 1984,6,251-264; Halstead, S. B.,

Science, 239:476-481,1988; Monath, T. P., New Eng. J. Med, 1988,319,64 1-643). 2983472-1 -3- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

The pestivirus genus includes bovine viral diarrhea virus (BVDV), classical swine fever virus (CSFV, also called hog cholera virus) and border disease virus (BDV) of sheep (Moennig, V. et al. Adv. Vir. Res. 1992,41, 53-98). Pestivirus infections of domesticated livestock (cattle, pigs and sheep) cause 5 significant economic losses worldwide. BVDV causes mucosal disease in cattle and is of significant economic importance to the livestock industry (Meyers, G. and Thiel, H.J., Advances in Virus Research, 1996,47, 53-118; Moennig V., et al, Adv. Vir. Res. 1992,41,53-98). Human pestiviruses have not been as extensively characterized as the animal pestiviruses. However, serological 10 surveys indicate considerable pestivirus exposure in humans.

Pestiviruses and hepaciviruses are closely related virus groups within the Flaviviridae family. Other closely related viruses in this family include the GB l virus A, GB virus A-like agents, GB virus-B and GB virus-C (also called hepatitis G virus, HGV). The hepacivirus group (hepatitis C virus; HCV) 15 consists of a number of closely related but genotypically distinguishable viruses that infect humans. There are at least 6 HCV genotypes and more than 50 subtypes. Due to the similarities between pestiviruses and hepaciviruses, combined with the poor ability of hepaciviruses to grow efficiently in cell culture, bovine viral diarrhea virus (BVDV) is often used as a surrogate to study 20 the HCV virus.

The genetic organization of pestiviruses and hepaciviruses is very similar. These positive stranded RNA viruses possess a single large open reading frame (ORF) encoding all the viral proteins necessary for virus replication.

These proteins are expressed as a polyprotein that is co- and post-translationally 2983472-1 -4- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 processed by both cellular and virus-encoded proteinases to yield the mature viral proteins. The viral proteins responsible for the replication of the viral genome RNA are located within approximately the carboxy-terminal. Two-thirds of the ORF are termed nonstructural (NS) proteins. The genetic 5 organization and polyprotein processing of the nonstructural protein portion of the ORF for pestiviruses and hepaciviruses is very similar. For both the pestiviruses and hepaciviruses, the mature nonstructural (NS) proteins, in sequential order from the amino-terminus of the nonstructural protein coding region to the carboxy-terminus of the ORF, consist of p7, NS2, NS3, NS4A, 10 NS4B,NS5A, andNS5B.

The NS proteins of pestiviruses and hepaciviruses share sequence domains that are characteristic of specific protein functions. For example, the NS3 proteins of viruses in both groups possess amino acid sequence motifs characteristic of serine proteinases and of helicases (Gorbalenya et al., Nature, 15 1988, 333, 22; Bazan and Fletterick Virology, 1989,171,637-639; Gorbalenya et al., Nucleic Acid Res.,1989, 17, 3889-3897). Similarly, theNSSB proteins of pestiviruses and hepaciviruses have the motifs characteristic of RNA-directed RNA polymerases (Koonin, E.V. and Dolja, V.V., Crir. Rev. Biochem. Molec.

Biol· 1993,28, 375-430). 20 The actual roles and functions of the NS proteins of pestiviruses and hepaciviruses in the lifecycle of the viruses are directly analogous. In both cases, the NS3 serine proteinase is responsible for all proteolytic processing of polyprotein precursors downstream of its position in the ORF (Wiskerchen and Collett, Virology, 1991, 184,341-350; BartenschlageretaL, J. Virol. 1993,67, 2983472-1 -5- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 3835-3844; Eckart et al. Biochem. Biophys. Res. Comm. 1993,192, 399-406;

Grakoui et al., J. Virol. 1993, 67,2832-2843; Grakoui et at, Proc. Natl. Acad Sci. USA 1993, 90,10583-10587; Hijikata et al., J. Virol. 1993, 67, 4665-4675;

Tome et al., J. Virol., 1993, 67,4017-4026). The NS4A protein, in both cases, 5 acts as a co factor with the NS3 serine protease (Bartenschlager et al., J. Virol. 1994, 68, 5045-5055; Failla et al., J. Virol. 1994,68, 3753-3760; Xu et al., J.

Virol., 1997, 71:53 12-5322). The NS3 protein of both viruses also functions as a helicase (Kim et al., Biochem. Biophys. Res. Comm., 1995,215,160-166; Jin and Peterson, Arch. Biochem. Biophys., 1995, 323,47-53; Warrener and Collett, 10 J. Virol. 1995,69,1720-1726). Finally, the NS5B proteins of pestiviruses and hepaciviruses have the predicted RNA-di reeled RNA polymerases activity (Behrens et al., EMBO, 1996, 15, 12-22; Lechmann et al., J. Virol., 1997,71, 8416-8428; Yuan et Biochem, Biophys. Res. Comm. 1997,232,231-235; Hagedorn, PCT WO 97/12033; Zhong et al, J. Virol., 1998, 72, 9365-9369). 15 Currently, there are limited treatment options for individuals infected with hepatitis C virus. The current approved therapeutic.option is the use of immunotherapy with recombinant interferon-α alone or in combination with the nucleoside analog ribavirin. This therapy is limited in its clinical effectiveness and only 50% of treated patients respond to therapy. Therefore, there is 20 significant need for more effective and novel therapies to address the unmet medical need posed by HCV infection. A number of potential molecular targets for drug development of direct acting antivirals as anti -HCV therapeutics have now been identified including, but not limited to, the NS2-NS3 autoprotease, the N3 protease, the N3 helicase 2983472-1 -6- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 and the NS5B polymerase. The RNA-dependent RNA polymerase is absolutely essential for replication of the single-stranded, positive sense, RNA genome and this enzyme has elicited significant interest among medicinal chemists.

Inhibitors of HCV NS5B as potential therapies for HCV infection have 5 been reviewed: Tan, S.-L., et al., Nature Rev. Drug Discov., 2002,1, 867-881; Walker, M.P. et al., Exp. Opin. Investigational Drugs, 2003, 12, 1269-1280; Ni, Z-J., et at, Current Opinion in Drug Discovery and Development, 2004,7,446-459; Beaulieu, P. L., et al., Current Opinion in Investigational Drugs, 2004, 5, 838-850; Wu, J., et at, Current Drug Targets-Infectious Disorders, 2003,3, 10 207-219; Griffith, R.C., et al, Annual Reports in Medicinal Chemistry, 2004,39, 223-237; Carrol, S., et al., Infectious Disorders-Drug Targets, 2006, 6, 17-29.

The potential for the emergence of resistant HCV strains and the need to identify agents with broad genotype coverage supports the need for continuing efforts to identify novel and more effective nucleosides as HCV NS5B inhibitors. 15 Nucleoside inhibitors of NS5B polymerase can act either as a non-natural substrate that results in chain termination or as a competitive inhibitor which competes with nucleotide binding to the polymerase. To function as a chain terminator the nucleoside analog must be taken up by the cell and converted in vivo to a triphosphate to compete for the polymerase nucleotide binding site. 20 This conversion to the triphosphate is commonly mediated by cellular kinases which imparts additional structural requirements on a potential nucleoside polymerase inhibitor. Unfortunately, this limits the direct evaluation of nucleosides as inhibitors of HCV replication to cell-based assays capable of in situ phosphorylation. 2983472-1 -7- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

In some cases, the biological activity of a nucleoside is hampered by its poor substrate characteristics for one or more of the kinases needed to convert it to the active triphosphate form. Formation of the monophosphate by a nucleoside kinase is generally viewed as the rate limiting step of the three 5 phosphorylation events. To circumvent the need for the initial phosphorylation step in the metabolism of a nucleoside to the active triphosphate analog, the preparation of stable phosphate prodrugs has been reported. Nucleoside phosphoramidate prodrugs have been shown to be precursors of the active nucleoside triphosphate and to inhibit viral replication when administered to 10 viral infected whole cells (McGuigan, C., etak, J. Med, Chem., 1996,39,1748-1753; Valette, G., et ak, J. Med. Chem., 1996,39, 1981-1990; Balzarini, J., et ak, Proc. National AcadSci USA, 1996,93,7295-7299; Siddiqui, A. Q., et ak, J.

Med. Chem., 1999,42,4122-4128; Eisenberg, E. J., etak, Nucleosides,

Nucleotides and Nucleic Acids, 2001,20,1091-1098; Lee, W.A., et ak, 15 Antimicrobial Agents and Chemotherapy, 2005,49, 1898); US 2006/0241064; and WO 2007/095269.

Also limiting the utility of nucleosides as viable therapeutic agents is their sometimes poor physicochemical and pharmacokinetic properties. These poor properties can limit the intestinal absorption of an agent and limit uptake 20 into the target tissue or cell. To improve on their properties prodrugs of nucleosides have been employed. It has been demonstrated that preparation of nucleoside phosphoramidates improves the systemic absorption of a nucleoside and furthermore, the phosphoramidate moiety of these "pronucleotides" is masked with neutral lipophilic groups to obtain a suitable partition coefficient to 25 optimize uptake and transport into the cell dramatically enhancing the 2983472-1 -8- 201239/2 WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 intracellular concentration of the nucleoside monophosphate analog relative to administering the parent nucleoside alone. Enzyme-mediated hydrolysis of the phosphate ester moiety produces a nucleoside monophosphate wherein the rate limiting initial phosphorylation is unnecessary.

5 SUMMARY OF THE INVENTION

The present invention describes . novel phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof, represented by the 10 following structure:

I wherein (a) Rl is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which 15 includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of Ci_6 alkyl, C2^ alkenyl, C2-6 alkynyl,

Ci-6 alkoxy, F, Cl, Br, I, nitro, cyano, Cu haloalkyl, -N(R! )2, C|.6 acyiamino, -NHSO2Ci.6 alkyl, -SO2N(Rr)2, COR? , and -SO2Cj.6 alkyl; (R? is independently hydrogen or alkyl, which includes, but is not limited to, Cj.2o alkyl, C^o alkyl, 20 or Ci^ alkyl, R1 is -OR' or -N(R’ )2); (b) R2 is hydrogen, C mo alkyl, R3a or R3b and R2 together are (CH2)„ so as to form a cyclic ring that includes the adjoining N and C atoms, C(O)CR3aR3bNHRl, where n is 2 to 4 and R1, R3a, and R3b; 2983472-1 -9- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 (c) R3a and R3b are (i) independently selected from hydrogen, Cmo alkyl, cycloalkyl, -(CH2)c(NR3j2, Ci^ hydroxyalkyl, -CH2SH, -(CII2)2S(O)dMe, -(CH2)3NHC(=NH)NH2, (lH-indol-3-yl)methyl, (lH-imidazol-4-yl)methyl, -(CH2)cCORr, aryl and aryl C).3 alkyl, said aryl groups optionally substituted 5 with a group selected from hydroxyl, Cmo alkyl, Ci.6 alkoxy, halogen, nitro and cyano; (ii) R3a and R3b both are Cj.6 alkyl; (iii) R3a and R3b together are(CH2)f so as to form a spiro ring; (iv) R3a is hydrogen and R3b and R2 together are (CH2)„ so as to form a cyclic ring that includes the adjoining N and C atoms (v) R3b is hydrogen and R3a and R2 together are (CH2)n so as to form a cyclic ring that 10 includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3' is independently hydrogen or Ci-e alkyl and R3' is -OR' or-N(R3')2); (vi) R3a is H and R3b is H, CH3, CH2CH3, CH(CH3)2s CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, 15 CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3a is CH3, -CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, ch2- 20 imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloaikyl and R3b is H, where R3 is independently hydrogen or alkyl, which includes, but is not limited to, Ci.2o alkyl, Cmo alkyl, or alkyl, R3" is -OR' or -N(R3)2); (d) R4 is hydrogen, Cmo alkyl, Cmo alkyl optionally substituted with 25 a lower alkyl, alkoxy, di(lower alkyl)-amino, or halogen, Cmo haloalkyl, C^io cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroatyl; (e) R5 is H, a lower alkyl, CN, vinyl, 0-(lower alkyl), hydroxyl lower alkyl, i.e., -(CH2)POH, where p is 1 -6, including hydroxyl methyl (CH2OH),

30 CH2F, N3, CH2CN, CH2NH2, CH2NHCH3, CH2N(CH3)2, alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X 2983472-1 -io- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 is OH, base is cytosine and R6 is H, R5 cannot be N3 and when X is OH, R6 is CH3 or CH2F and B is a purine base, R5 cannot be H; (f) R6 is H, CH3, CH2F, CHF2j CF3, F, or CN; (g) X is H, OH, F, OMe, halogen, NH2, or N3; 5 (h) Y is OH, H, C1-4 alkyl, C24 alkenyl, Cw alkynyl, vinyl, N3, CN,

Cl, Br, F, I, NO2, OC(O)O(CM alkyl), OC(O)O(CM alkyl), 0C(0)0(C24 alkynyl), OC(O)O(C2^ alkenyl), OCmo haloalkyl, O(aminoacyl), 0(Cmo acyl), O(CM alkyl), 0(C24 alkenyl), S(CM acyl), S(CM alkyl), S(C24 alkynyl), S(C2^ alkenyl), SO(CM acyl), SO(CM alkyl), SO(C2Jl alkynyl), S0(C2^ alkenyl), 10 SO2(Cm acyl), SO2(CM alkyl), SO2(C2^ alkynyl), SO2(C2^ alkenyl), OS(O)2(C|. 4 acyl), OS(O)2(Ci-4 alkyl), OS(O)2(CW alkenyl), NH2, NH(CM alkyl), NH(C2-4 alkenyl), NH(Cm alkynyl), NH(Ci-4 acyl), N(Cu alkyl)2, N(Cms acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F, I), NO2, C(O)0(CM alkyl), C(O)O(CM alkyl), 15 C(O)O(CM alkynyl), C(O)O(CW alkenyl), O(CM acyl), O(CM alkyl), O(C24 alkenyl), S(Cm acyl), S(Cm alkyl), S(C2_4 alkynyl), S(Cm alkenyl), S0(Cm acyl), SO(CM alkyl), SO(CW alkynyl), SO(C24 alkenyl), SO2(CM acyl), SO2(CM alkyl), SO2(C24 alkynyl), SO2(C2^ alkenyl), OS(O)2(Cu acyl), 0S(0)2(CM alkyl), OS(O)2(CW alkenyl), NH2, NH(CM alkyl), NH(C2„ 20 alkenyl), NH(C24 alkynyl), NH(Cm acyl), N(Cm alkyl)2, N(Cm acyl)2; the base is a naturally occurring or modified purine or pyrimidine base represented by the following structures: 2983472-1 -11- PCT/US2008/058183 WO 2008/121634 . Docket No. 60137.0034WOU1

wherein Z is Nor CR12; 5 R7, R8,R9, Ri0, and R1 ‘are independently H, F, Cl, Br, 1, OH, OR', SH, SR', NH2, NHR', NR'2, lower alkyl of Ci-Ce, halogenated (F, Cl, Br, I) lower alkyl of Ci-Cs, lower alkenyl of CrCe, halogenated (F, Cl, Br, I) lower alkenyl of C2-Ce, lower alkynyl of C2-Ce such as C^CH, halogenated (F, Cl, Br, I) lower alkynyl of C2-C6, lower alkoxy of Ci-Ce, halogenated (F, Cl, Br, I) lower alkoxy 10 of Cj-Cfi, CO2H, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CHCHCChR', wherein R' is an optionally substituted alkyl, which includes, but is not limited to, an optionally substituted C].2o alkyl, an optionally substituted Cmo alkyl, an optionally substituted lower alkyl; an optionally substituted cycloalkyl; 15 an optionally substituted alkynyl of C2-Ce, an optionally substituted lower alkenyl of C2-Ce, or optionally substituted acyl, which includes but is not limited to C(O) alkyl, C(O)(C|.20 alkyl), C(O)(Cm0 alkyl), or C(O)(lower alkyl) or alternatively, in the instance of NR’2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 20 R12 is H, halogen (including F, Cl, Br, I), OH, OR’, SH, SR’, NH2, NHR’, NR'2, NO2 lower alkyl of Ci-Cg, halogenated (F, Cl, Br, I) lower alkyl of Ci-C6, lower alkenyl of C^-Ce, halogenated (F, Cl, Br, I) lower alkenyl of Cj-Ce, lower alkynyl of C2-C6, halogenated (F, Cl, Br, I) lower alkynyl of C2-Cfi, lower alkoxy of C)-Ce, halogenated (F, Cl, Br, I) lower alkoxy of Ci-C6, CO2H, CChR', 25 CONH2, CONHR', CONR'2, CHCHCChH, or CH=CHCO2R'; with the proviso 298M72-1 -12- 201239/1 that when base is represented by the structure c with Rn being hydrogen, R12 is not a: (i) -OC-H, (ii) -C=CH2, or (iii) -NO2.

The present invention is directed to (S)-2-{[(2R,3R,4R,5R)-5-(2,4-Dioxo-3,4-dihydro-2H-pyrimidin-l-yl)-4-fluoro-3-hydroxy-4-methyl-tetrahydro-furan-2-ylmethoxy]-phenoxy-phosphorylamino}-propionic acid isopropyl ester or a stereoisomer thereof. The present invention is also directed to (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5 -(2,4-d ioxo-3,4-dihydropyrim idin-1 (2H)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl) methoxy) (phenoxy) phosphoryl) amino) propanoate.

The invention further provides compositions comprising any one of these compounds or a stereoisomer thereof and a pharmaceutically acceptable medium.

In addition, the present invention further provides a process for preparing any one of the compounds or a stereoisomer thereof comprising reacting a compound 4" with a nucleoside analog 5'

wherein X' is a leaving group. -12a- 201239/2 WO 2008/121634

Docket No. 60137.003.4WOU1 PCT/US2008/Q58183

DEFINITIONS 5 The phrase "a” or "an" entity as used herein refers to one or more of that entity; for example, a compound refers to one or more compounds or at least one compound. As such, the terms "a" (or "an"), "one or more", and "at least one" can be used interchangeably herein.

The phrase "as defined herein above" refers to the first definition 10 provided in the Summary of the Invention.

The terms "optional" or "optionally" as used herein means that a subsequently described event or circumstance may but need not occur, and that the description includes instances where the event or circumstance occurs and instances in which it does not. For example, "optional bond" means that the 15 bond may or may not be present, and that the description includes single, double, or triple bonds.

The term "independently’1 is used herein to indicate that a variable is applied in any one instance without regard to the presence or absence of a variable having that same or a different definition within the same compound. 20 Thus, in a compound in which R appears twice and is defined as "independently carbon or nitrogen", both R's can be carbon, both R's can be nitrogen, or one R’ can be carbon and the other nitrogen.

The term "alkenyl" refers to an unsubstituted hydrocarbon chain radical having from 2 to 10 carbon atoms having one or two olefinic double bonds, 25 preferably one olefinic double bond. The term "C2-N alkenyl" refers to an alkenyl comprising 2 to N carbon atoms, where N is an integer having the following values: 3, 4, 5, 6, 7, 8, 9, or 10. The term "C2-10 alkenyl" refers to an alkenyl comprising 2 to 10 carbon atoms. The term ’'C2-4 alkenyl" refers to an alkenyl comprising 2 to 4 carbon atoms. Examples include, but are not limited 30 to, vinyl, 1-propenyl, 2-propenyl (allyl) or 2-butenyl (crotyl).

2983472-J -13- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

The term "halogenated alkenyl" refers to an alkenyl comprising at least one of F, Cl, Br, and I.

The term "alkyl" refers to an unbranched or branched chain, saturated, monovalent hydrocarbon residue containing 1 to 30 carbon atoms. The term "Ci. 5 m alkyl" refers to an alkyl comprising 1 to M carbon atoms, where M is an integer having the following values: 2, 3, 4, 5, 6, 7, 8, 9,10, 11, 12,13, 14, 15, 16, 17, 18, 19,20,21, 22,23, 24,25,26,27,28,29, or 30. The term "CM alkyl" refers to an alkyl containing 1 to 4 carbon atoms. The term "lower alkyl" denotes a straight or branched chain hydrocarbon residue comprising 1 to 6 10 carbon atoms. "Ci.2o alkyl" as used herein refers to an alkyl comprising 1 to 20 carbon atoms. "Cno alkyl" as used herein refers to an alkyl comprising 1 to 10 carbons. Examples of alkyl groups include, but are not limited to, lower alkyl groups include methyl, ethyl, propyl, /-propyl, «-butyl, /-butyl, /-butyl or pentyl, isopentyl, neopentyl, hexyl, heptyl, and octyl. The term (ar)alkyl or 15 (heteroaryl)alkyl indicate the alkyl group is optionally substituted by an aryl or a heteroaryl group respectively.

The term "cycloalkyl" refers to an unsubstituted or substituted carbocycle, in which the carbocycle contains 3 to 10 carbon atoms; preferably 3 to 8 carbon atoms; more preferably 3 to 6 carbon atoms (i.e., lower cycloalkyls). 20 Examples of cycloalkyl groups include, but are not limited to, cyclopropyl, 2-methyl-cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl.

The term "cycloalkyl alkyl" refers to an additionally unsubstituted or substituted alkyl substituted by a lower cycloalkyl. Examples of cycloalkyl alkyls include, but are not limited to, any one of methyl, ethyl, propyl, i-propyl, 25 n-butyl, i-butyl, t-butyl or pentyl, isopentyl, neopentyl, hexyl, heptyl, and octyl that is substituted with cyclopropyl, 2-methyl-cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl.

The term "cycloheteroalkyl" refers to an unsubstituted or substituted heterocycle, in which the heterocycle contains 2 to 9 carbon atoms; preferably 2 30 to 7 carbon atoms; more preferably 2 to 5 carbon atoms. Examples of cycloheteroalkyls include, but are not limited to, aziridin-2-yl, jV-Ci_3-alkyl- 2983472-1 -14- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 aziridin-2-yl, azetidinyl, 7V-C j.3-a Iky I-azetid in-m'-yl, pyrrol id in-m'-yl, /V-C1.3-alkyl-pyrrolidin-m'-yl, piperidin-m'-yl, and ?Z-Ci.3-alkyl-piperidin-m'-yl, where m' is 2, 3, or 4 depending on the cycloheteroalkyl. Specific examples of N-C1.3-alkyl-cycloheteroalkyls include, but are not limited to, N-methyl-aziridin-2-yl, 5 N-methyl-azetidin-3-yl, N-methyl-pyrroIidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-2-yl, N-methyl-piperidin-3-yl, and N-methyl-piperidin-4-yl. In the instance of R4, the point of attachment between the eye Ioheteroalkyl ring carbon and the oxygen occurs at any one of m'

The term "heterocycle" refers to an unsubstituted or substituted 10 heterocycle containing carbon, hydrogen, and at least one of N, 0, and S, where the C and N can be trivalent or tetravalent, i.e., sp2- or sp3-hybridized. Examples of heterocycles include, but are not limited to, aziridine, azetidine, pyrrolidine, piperidine, imidazole, oxazole, piperazine, etc. In the instance of piperazine, as related to R10 for NR'2, the corresponding opposite nitrogen atom of the 15 piperazinyl is substituted by a lower alkyl represented by the following structure: lower alkyl-

Preferably, the opposite nitrogen of the piperazinyl is substituted by a methyl group.

The term "halogenated alkyl" (or "haloalkyl") refers to an unbranched or 20 branched chain alkyl comprising at least one of F, Cl, Br, and I. The term "Ci.M haloalkyl" refers to an alkyl comprising 1 to M carbon atoms that comprises at least one of F, Cl, Br, and I, where M is an integer having the following values: 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20,21, 22,23, 24, 25, 26, 27, 28, 29, or 30. "C1-3 haloalkyl" refers to a haloalkyl comprising 1 to 3 25 carbons and at least one of F, Cl, Br, and I. The term "halogenated lower alkyl" (or "lower haloalkyl") refers to a haloalkyl comprising 1 to 6 carbon atoms and at least one of F, Cl, Br, and I. Examples include, but are not limited to, fluoromethyl, chloromethyl, bromomethyl, iodomethyl, difluoromethyl, dichloromethyl, dibromomethyl, diiodomethyl, tri fluoromethyl, trichloromethyl, 30 tribromomethyl, triiodomethyl, 1-fluoroethyl, 1-chloroethyl, 1-bromoethyl, 1- 2983472-1 -15- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 iodoethyl, 2-fluoroethyl, 2-chloroethyl, 2-bromoethyl, 2-iodoethyl, 2,2- difluoroethyl, 2,2-dichloroethyl, 2,2-di bromomethyl, 2-2-di iodomethyl, 3- fluoropropyl, 3-chloropropyl, 3-bromopropyl, 2,2,2-trifluoroethyl or 1,1,2,2,2- pentafluoroethyl. 5 The term "alkynyl" refers to an unbranched or branched hydrocarbon chain radical having from 2 to 10 carbon atoms, preferably 2 to 5 carbon atoms, and having one triple bond. The term "C2.N alkynyl" refers to an alkynyl comprising 2 to N carbon atoms, where N is an integer having the following values: 3, 4, 5, 6, 7, 8, 9, or 10. The term "C C2-4 alkynyl” refers to an alkynyl 10 comprising 2 to 4 carbon atoms. The term "C2-10 alkynyl” refers to an alkynyl comprising 2 to 10 carbons. Examples include, but are limited to, ethynyl, 1-propynyl, 2-propynyl, 1-butynyl, 2-butynyl or 3-butynyl.

The term "halogenated alkynyl" refers to an unbranched or branched hydrocarbon chain radical having from 2 to 10 carbon atoms, preferably 2 to 5 15 carbon atoms, and having one triple bond and at least one of F, Cl, Br, and I.

The term "cycloalkyl” refers to a saturated carbocyclic ring comprising 3 to 8 carbon atoms, i.e. cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl. The term "C3-7 cycloalkyl” as used herein refers to a cycloalkyl comprising 3 to 7 carbons in the carbocyclic ring. 20 The term "alkoxy" refers to an -O-alkyl group or an -O-cycloalkyl group, wherein alkyl and cycloalkyl are as defined above. Examples of -O-alkyl groups include, but are not limited to, methoxy, ethoxy, n-propyloxy, /-propyloxy, n-butyloxy, /-butyloxy, ί-butyloxy. "Lower alkoxy" as used herein denotes an alkoxy group with a "lower alkyl" group as previously defined. "Ci-10 25 alkoxy" refers to an-O-alkyl wherein alkyl is Cho. Examples of-O-cycloalkyl groups include, but are not limited to, -O-c-propyl, -O-c-butyl, -O-c-pentyl, and -O-c-hexyl.

The term "halogenated alkoxy" refers to an -O-alkyl group in which the alkyl group comprises at least one of F, Cl, Br, and I. 2983472-1 -16- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

The term "halogenated lower alkoxy" refers to an -O-(lower alkyl) group in which the lower alkyl group comprises at least one of F, Cl, Br, and I.

The term "amino acid" includes naturally occurring and synthetic α, β γ or δ amino acids, and includes but is not limited to, amino acids found in 5 proteins, i.e. glycine, alanine, valine, leucine, isoleucine, methionine, phenylalanine, tryptophan, proline, serine, threonine, cysteine, tyrosine, asparagine, glutamine, aspartate, glutamate, lysine, arginine and histidine. In a preferred embodiment, the amino acid is in the L-configuration. Alternatively, the amino acid can be a derivative of alanyl, valinyl, leucinyl, isoleucinyl, 10 prolinyl, phenylalaninyl, tryptophanyl, methioninyl, glycinyl, serinyl, threoninyl, cysteinyl, tyrosinyl, asparaginyl, glutaminyl, aspartoyl, glutaroyl, lysinyl, argininyl, histidinyl, β-alanyl, p-valinyl, β-leucinyl, β-isoleucinyl, β-prolinyl, β-phenylalaninyl, β-tryptophanyl, β-methioninyl, β-glycinyl, β-serinyl, β-threoninyl, β-cysteinyl, β-tyrosinyl, β-asparaginyl, β-glutaminyl, β-aspartoyl, β- 15 glutaroyl, β-lysinyl, β-argininyl or β-histidinyl. When the term amino acid is used, it is considered to be a specific and independent disclosure of each of the esters of α, β γ or δ glycine, alanine, valine, leucine, isoleucine, methionine, phenylalanine, tryptophan, proline, serine, threonine, cysteine, tyrosine, asparagine, glutamine, aspartate, glutamate, lysine, arginine and histidine in the 20 D and L-configurations.

The term "aminoacyl" includes N,N-un substituted, N,N-monosubstituted, and Ν,Ν-disubstituted derivatives of naturally occurring and synthetic α, β γ or δ amino acyls, where the amino acyls are derived from amino acids. The aminonitrogen can be substituted or unsubstituted. When the amino-nitrogen is 25 substituted, the nitrogen is either mono- or di-substituted, where the substituent bound to the amino-nitrogen is a lower alkyl or an alkaryl. In the instance of its use for Y, the expression "O(aminoacyl)" is used. It is understood that the C3' carbon of the ribose is bound to the oxygen "0", which is then bound to the carbonyl carbon of the aminoacyl. 30 The terms "alkylamino" or "arylamino" refer to an amino group that has one or two alkyl or aryl substituents, respectively. 2983472-1 -17- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

The term "protected," as used herein and unless otherwise defined, refers to a group that is added to an oxygen, nitrogen, or phosphorus atom to prevent its further reaction or for other purposes. A wide variety of oxygen and nitrogen protecting groups are known to those skilled in the art of organic synthesis. Non- 5 limiting examples include: C(O)-alkyl, C(O)Ph, C(O)aryl, CH3, CH2-alkyl, CH2-alkenyl, CH2Ph, CH2-aryl, CH2O-aikyl, CH2O-aryl, SO2-alkyl, SO2-aryl, tert-butyldimethylsilyl, /ert-butyldiphenylsilyl, and 1,3-(1,1,3,3- tetraisopropyldisiloxanylidene).

The term "aryl," as used herein, and unless otherwise specified, refers to 10 substituted or unsubstituted phenyl (Ph), biphenyl, or naphthyl, preferably the term aryl refers to substituted or unsubstituted phenyl. The aryl group can be substituted with one or more moieties selected from among hydroxyl, F, Cl, Br, I, amino, alkylamino, arylamino, alkoxy, aryloxy, nitro, cyano, sulfonic acid, sulfate, phosphonic acid, phosphate, and phosphonate, either unprotected, or 15 protected as necessary, as known to those skilled in the art, for example, as taught in T.W. Greene and P.G. M. Wuts, "Protective Groups in Organic Synthesis," 3rd ed., John Wiley &amp; Sons, 1999.

The terms "alkaryl" or "alkylaryl" refer to an alkyl group with an aryl substituent, such as benzyl. The terms "aralkyl" or "arylalkyl" refer to an aryl 20 group with an alkyl substituent.

The term "di(lower alkyl)amino-lower alkyl" refers to a lower alkyl substituted by an amino group that is itself substituted by two lower alkyl groups. Examples include, but are not limited to, (CH3)2NCH2, (CH3)2NCH2CH2, (CH3)2NCH2CH2CH2, etc. The examples above show lower 25 alkyls substituted at the terminus carbon atom with an N,N-dimethyl-amino substituent. These are intended as examples only and are not intended to limit the meaning of the term "di(lower alkyl)amino-lower alkyl" so as to require the same. It is contemplated that the lower alkyl chain can be substituted with an N,N-di(lower alkyl)-amino at any point along the chain, e.g., CH3CH(N-(lower 30 aikyl^CHjCHi.

The term "halo," as used herein, includes chloro, bromo, iodo and fluoro. 2983472-1 -18- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

The term "acyl" refers to a substituent containing a carbonyl moiety and a non-carbonyl moiety. The carbonyl moiety contains a double-bond between the carbonyl carbon and a heteroatom, where the heteroatom is selected from among Ο, N and S. When the heteroatom is N, the N is substituted by a lower 5 alkyl. The non-carbonyl moiety is selected from straight, branched, and cyclic alkyl, which includes, but is not limited to, a straight, branched, or cyclic C1.20 alkyl, Cho alkyl, or lower alkyl; alkoxyalkyl, including methoxymethyl; aralkyl, including benzyl; aryloxyalkyl, such as phenoxymethyl; or aryl, including phenyl optionally substituted with halogen (F, Cl, Br, I), hydroxy], Ci to C4 10 alkyl, or Ci to C4 alkoxy, sulfonate esters, such as alkyl or aralkyl sulphonyl, including methanesulfonyl, the mono, di or triphosphate ester, trityl or monomethoxytrityl, substituted benzyl, trialkylsilyl (e.g. dimethyl-t-butylsilyl) or diphenylmethylsilyl. When at least one aryl group is present in the non-carbonyl moiety, it is preferred that the aryl group comprises a phenyl group. 15 The term "lower acyl" refers to an acyl group in which the non-carbonyl moiety is lower alkyl.

The term "purine" or "pyrimidine" base includes, but is not limited to, adenine, N^-alkylpurines, N6-acylpurines (wherein acyl is C(O)(alkyl, aryl, alkylaryl, or arylalkyl), N^-benzylpurine, N6-halopurine, N6-vinylpurine, N6- 20 acetylenic purine, N6-acyl purine, N6-hydroxyalkyl purine, N6- allcylaminopurine, N6-thioallcyl purine, N2-alkylpurines, N2-alkyl-6-thiopurines, thymine, cytosine, 5-fluorocytosine, 5-methylcytosine, 6-azapyrimidine, including 6-azacytosine, 2- and/or 4-mercaptopyrmidine, uracil, 5-halouracil, including 5-fluorouracil, C5-alkylpyrimidines, C5-benzylpyrimidines, C5- 25 halopyrimidines, Cs-vinyipyrimidine, C5-acetylenic pyrimidine, C5-acyl pyrimidine, C5-hydroxyalkyl purine, C5-amidopyrimidine, C5-cyanopyrimidine, ,C5-iodopyrimidine, C6-lodo-pyrimidine, C5-Br-vinyl pyrimidine, C6-Br-vinyl pyrimidine, C5-nitropyrimidine, C5-amino-pyrimidine, N2-alkyIpurines, N2-alkyl-6-thiopurines, 5-azacytidinyl, 5-azauracilyl, triazolopyridinyl, 30 imidazolopyridinyl, pyrrolopyrimidinyl, and pyrazolopyrimidinyl. Purine bases include, but are not limited to, guanine, adenine, hypoxanthine, 2,6-diaminopurine, and 6-chloropurine. Functional oxygen and nitrogen groups on 2983472-1 -19- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 the base can be protected as necessary or desired. Suitable protecting groups are well known to those skilled in the art, and include trimethylsilyl, dimethylhexylsilyl, Z-butyldimethyIsilyl, and /-butyIdiphenylsilyl, trityl, alkyl groups, and acyl groups such as acetyl and propionyl, rnethanesulfonyl, and p- 5 toluenesulfonyl.

The term "tautomerism" and "tautomers" have their accepted plain meanings.

The term "P*" means that the phosphorous atom is chiral and that it has a corresponding Cahn-Ingold-Prelog designation of "R" or "S" which have their 10 accepted plain meanings. It is contemplated that compounds of the formula I are racemic because the chirality at phosphorous. Applicants contemplate use of the racemate and/or the resolved enantiomers. In some instances, an asterisk does not appear next to the phosphoroamidate phosphorous atom. In these instances, it is understood that the phosphorous atom is chiral and that one of ordinary skill 15 understands this to be so unless the substituents bound to the phosphorous exclude the possibility of chirality at phosphorous, such as in P(O)Cb.

DETAILED DESCRIPTION OF THE INVENTION

An aspect of the invention is directed to a compound, its salts, hydrates, solvates, crystalline forms, and the like represented by formula I:

wherein (a) R1 is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of Ci^ alkyl, C2-6 alkenyl, C2-6 alkynyl, 25 C1.6 alkoxy, F, Cl, Br, I, nitro, cyano, Cu haloalkyl, -N(R’ )2, Ci^ acylamino, - 2983472-1 -20- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 NHSO2Ci-6 alkyl, -SO^R3’^, COR1', and -SO2C)^ alkyl; (Rl'is independently hydrogen or alkyl, which includes, but is not limited to, Ci.2o alkyl, Cmo alkyl, or C|.6 alkyl, R1" is -OR' or -N(Rl’)2); (b) R2 is hydrogen, C mo alkyl, R3a or R3b and R2 together are (CH2)„ 5 so as to form a cyclic ring that includes the adjoining N and C atoms, C(O)CR3aR3bNHR3, where n is 2 to 4 and R1, R3a, and R3b; (c) R3a and R3b are (i) independently selected from hydrogen, Cmo alkyl, cycloalkyl, -(CH2)c(NR3‘)2, CM hydroxyalky], -CH2SH, -(CH2)2S(O)dMe, -(CH2)3NHC(=NH)NH2, (lH-indol-3-yl)methyl, (lH-imidazol-4-yl)methyl, - 10 (CH2)eCOR3", aryl and aryl Ci.3 alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Cmo alkyl, Ci-e alkoxy, halogen, nitro and cyano; (ii) R3a and R3b both are C1-0 alkyl; (iii) R3a and R3b together are(CH2)r so as to form a spiro ring; (iv) R3a is hydrogen and R3b and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms (v) R3b is 15 hydrogen and R3a and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3 is independently hydrogen or Ci_<s alkyl and R3’ is -OR' or-N(R3)2); (vi) R3a is H and R3b is H, CH3, CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, 20 CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH20H, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3a is CH3, -CH2CH3j CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, 25 CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, ch2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H, where R3 is independently hydrogen or alkyl, which includes, but is not limited to, Ci.2o alkyl, Cmo alkyl, or C^ alkyl, R3" is -OR’ or -N(R3'W; 30 (d) R4 is hydrogen, Cmo alkyl, Ci.,o alkyl optionally substituted with a lower alkyl, alkoxy, di(lower alkyl)-amino, or halogen, Cmo haloalkyl, C3.io 2983472-1 -21- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; (e) R5 is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., -(CH2)POH, where p is 1 -6, including hydroxyl methyl (CH2OH), 5 CH2F, N3j CH2CN, CH2NH2, CH2NHCH3, CH2N(CH3)2, alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R6 is H, R5 cannot be N3 and when X is OH, R6 is CH3 or CH2F and B is a purine base, R5 cannot be H; 10 (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OMe, halogen, NH2, or N3; (h) Y is OH, H, Cm alkyl, C2m alkenyl, C2m alkynyl, vinyl, N3, CN, Cl, Br, F, I, NO2, OC(O)O(CM alkyl), OC(O)O(CM alkyl), 0C(0)0(C24 alkynyl), OC(O)O(C2_4 alkenyl), OCmo haloalkyl, O(aminoacyl), 0(Cmo acyl), O(CM alkyl), O(C2m alkenyl), S(CM acyl), S(Cm alkyl), S(C2.4 alkynyl), S(C2m 15 alkenyl), SO(Cm acyl), SO(Cm alkyl), SO(C2m alkynyl), SO(C2-4 alkenyl), SO2(Cm acyl), SO2(Cm alkyl), S02(C2m alkynyl), SO2(CW alkenyl), OS(O)2(Cj-4 acyl), OS(O)2(Cm alkyl), OS(O)2(CW alkenyl), NH2, NH(CM alkyl), NH(CW alkenyl), NH(C2m alkynyl), NH(CM acyl), N(Cm alkyl)2, N(Cm8 acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, 20 one to three halogen (CI, Br, F, I), NO2, C(O)O(Cm alkyl), C(O)0(Cm alkyl), C(O)O(C2m alkynyl), C(O)O(C2m alkenyl), 0(Cm acyl), O(CM alkyl), O(C2m alkenyl), S(CM acyl), S(CM alkyl), S(C2„ alkynyl), S(CW alkenyl), SO(CM acyl), SO(Cm alkyl), SO(C2m alkynyl), SO(C2m alkenyl), SO2(Cm acyl), SO2(Cm alkyl), SO2(CW alkynyl), SO2(C2m alkenyl), 0S(0)2(Cm acyl), 25 OS(O)2(CM alkyl), OS(O)2(CM alkenyl), NH2, NH(CM alkyl), NH(C24 alkenyl), NH(CW alkynyl), NH(CM acyl), N(CM alkyl)2, N(CM acyl)2; the base is a naturally occurring or modified purine or pyrimidine base represented by the following structures: 2983472-1 -22- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

a b c d wherein Z is Nor CR12; 5 R7, R8,R9, R10, and Rnare independently H, F, Cl, Br, I, OH, OR', SH, SR', NH2, NHR', NR'2, lower alkyl of Ct-Ce, halogenated (F, Cl, Br, I) lower alkyl of Cj-Ce, lower alkenyl of C2-C6, halogenated (F, Cl, Br, I) lower alkenyl of C2-Ce, lower alkynyl of C2-Ce such as C=CH, halogenated (F, Cl, Br, I) lower alkynyl of C2-C6, lower alkoxy of Ci -Ce, halogenated (F, Cl, Br, I) lower alkoxy 10 of Cj-C6, CO2H, CO2R’, CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R', wherein R' is an optionally substituted alkyl, which includes, but is not limited to, an optionally substituted C1-20 alkyl, an optionally substituted Cmo alkyl, an optionally substituted lower alkyl; an optionally substituted cycloalkyl; 15 an optionally substituted alkynyl of C2-C0, an optionally substituted lower alkenyl of C2-Ce, or optionally substituted acyl, which includes but is not limited to C(O) alkyl, C(0)(C(.2o alkyl), C(0)(Cj.io alkyl), or C(0)(lower alkyl) or alternatively, in the instance of NR'2, each R’ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 20 RIJ is H, halogen (including F, Cl, Br, 1), OH, OR', SH, SR', NHj, NHR', NR'2, NO2 lower alkyl of Cj-Ce, halogenated (F, Cl, Br, I) lower alkyl of CpCe, lower alkenyl of C2-Ce, halogenated (F, Cl, Br, 1) lower alkenyl of C2-C6, lower alkynyl of C2-Ce, halogenated (F, Cl, Br, 1) lower alkynyl of C2-C6, lower alkoxy of Ci-Cg, halogenated (F, Cl, Br, I) lower alkoxy of Ci-Ce, CO2H, CO2R', 25 CONH2, CONHR', CONR'2) CH=CHCO2H, or CH=CHCO2R'; with the proviso 2983472-1 -23- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 that when base is represented by the structure c with R11 being hydrogen, R12 is not a: (i) -OC-H, (ii) -0=01¼ or (iii) -NO2.

As can be appreciated from the structure represented by formula I above, there are myriad ways to express the several embodiments and aspects of each 5 embodiment of the present invention. As seen below, the inventors have disclosed certain embodiments directed to the compound of formula I, each having several aspects, based on the identity of the modified purine or pyrimidine base. This is not intended to be an explicit or implicit admission that the three embodiments are independent or distinct nor should it be interpreted as 10 such. Rather, it is intended to convey information so that the full breadth of the present invention can be understood. Furthermore, the following embodiments, and aspects thereof, are not meant to be limiting on the full breadth of the invention as recited by the structure of formula I. A first embodiment of the invention is directed to a compound 15 represented by formula 1-1:

wherein (a) R1 is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which 20 includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are 2983472-1 -24- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 optionally substituted with at least one of Cm alkyl, C2-6 alkenyl, C2~6 alkynyl,

Cm alkoxy, F, Cl, Br, I, nitro, cyano, Cj.6 haloalkyl, -N(R* )2, Cm acylamino, -NHSO2Cm alkyl, -SO2N(R1')2, COR1", and -SO2Ci.6 alkyl; (Rris independently hydrogen or alkyl, which includes, but is not limited to, C|.2o alkyl, Cmo alkyl, 5 or Cm alkyl, Rr is -OR' or -N(Rr)2); · (b) R2 is hydrogen, C mo alkyl, R3fl or R3b and R2 together are (CHjJn so as to form a cyclic ring that includes the adjoining N and C atoms, C(O)CR3flR3bNHR', where n is 2 to 4 and R1, R3a, and R3b; (c) R3a and R3b are (i) independently selected from hydrogen, Cmo 10 alkyl, cycloalkyl, -(CH2)c(NR3')2, Cm hydroxyalkyl, -CH2SH, -(CH2)2S(O)dMe, - (CH2)3NHC(=NH)NH2, (lH-indol-3-yl)methyl, (lH-imidazol-4-yl)methyl, -(CH2)eCOR3', aryl and aryl C1.3 alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, C1-10 alkyl, C].6 alkoxy, halogen, nitro and cyano; (ii) R3b and R3b both are Cm alkyl; (iii) R3a and R3b together are(CH2)f so 15 as to form a spiro ring; (iv) R3n is hydrogen and R3b and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms (v) R3b is hydrogen and R3“ and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3 is independently hydrogen or Cm alkyl and 20 R3’ is -OR* or -N(R3)2); (vi) R3a is H and R3b is H, CH3, CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3j CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) 25 R3a is CH3, -CH2CH3, CH(CH3)2> CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, ch2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H, where R3 is independently hydrogen or alkyl, which 30 includes, but is not limited to, Ci.2q alkyl, Cmo alkyl, or Cm alkyl, R3' is -OR* or -N(R3h); 2983472-1 -25- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 (d) R4 is hydrogen, C|.io alkyl, Cmo alkyl optionally substituted with a lower alkyl, alkoxy, di(lower alkyl)-amino, or halogen, Cmo haloalkyl, C3-io cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)-amino, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or 5 substituted heteroaryl;

(e) R5 is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., -(CH2)POH, where p is 1 -6, including hydroxyl methyl (CH2OH), CH2F, N3, CH2CN, CH2NH2, CH2NHCH3, CH2N(CH3)2, alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X 10 is OH, base is cytosine and R6 is H, R5 cannot be N3 and when X is OH, R6 is CH3 or CH2F and B is a purine base, R5 cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OMe, Cl, Br, I, NH2, orN3; (h) Y is OH, H, Cm alkyl, C2m alkenyl, C2m alkynyl, vinyl, N3, CN, 15 Cl, Br, F, I, NO2, OC(O)O(CM alkyl), OC(O)O(CM alkyl), 0C(0)0(C24 alkynyl), OC(O)O(C2m alkenyl), OCmo haloalkyl, O(aminoacyl), 0(Cmo acyl), O(Cm alkyl), O(C2m alkenyl), S(Cm acyl), S(Cm alkyl), S(C2-4 alkynyl), S(C2m alkenyl), SO(CM acyl), SO(Cm alkyl), SO(C2m alkynyl), SO(C2.4 alkenyl), SO2(CM acyl), S02(Cm alkyl), SO2(C2m alkynyl), SO2(CW alkenyl), OS(Oh(Ci. 20 4 acyl), OS(O)2(CM alkyl), OS(O)2(C2-4 alkenyl), NH2, NH(Ct-4 alkyl), NH(C2m alkenyl), NH(C2-4 alkynyl), NH(CM acyl), N(CM alkyl)2, N(Cm8 acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F, I), NO2, C(O)O(Cm alkyl), C(O)O(Cm alkyl), C(O)O(C2m alkynyl), C(O)O(C2m alkenyl), O(CM acyl), O(Cm alkyl), O(C2m 25 alkenyl), S(Cm acyl), S(CM alkyl), S(C2m alkynyl), S(C2m alkenyl), SO(CM acyl), SO(Cm alkyl), SO(C2m alkynyl), SO(C2m alkenyl), SO2(Cm acyl), SO2(CM alkyl), SO2(C24 alkynyl), S02(C2-4 alkenyl), OS(O)2(Cm acyl), OS(O)2(CM alkyl), 08(0^(0^ alkenyl), NH2, NH(CU alkyl), NH(C24 alkenyl), NH(C2m alkynyl), NH(CM acyl), N(Cm alkyl)2, N(CM acyl)2; 30 (i) R7, R’,R9 are independently H, F, Cl, Br, I, OH, OR', SH, SR', NH2, NHR', NR'2j lower alkyl, halogenated (F, Cl, Br, I) lower alkyl, lower 2983472-1 -26- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 alkenyl of C2-C6, CO2H, CO2R', CONH2, CONHR', CONR'2, wherein R' is a Ci. 20 alkyl; a Ci.2o cycloalkyl; a C2-C6 alkenyl, a C2-C6 alkynyl. A first aspect of the first embodiment is directed to a compound represented by formula 1-1 5 wherein (a) R1 is hydrogen, n-alkyl or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of Ci.6 alkyl, Cm alkoxy, F, Cl, Br, I, nitro, cyano, Cm haloalkyl; (b) R2 is hydrogen or CH3; 10 (c) R3a and R3b are independently (i) R3a is hydrogen and R3b and R2 together are (CH2)„ so as to form a cyclic ring that includes the adjoining N and C atoms (v) R3b is hydrogen and R3a and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 3 to 5, n is 2 to 4, and where R3' is independently hydrogen or 15 alkyl and R3" is -OR* or-N(R3')2); (vi) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) 20 R3" is CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3- yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, ch2-imidazol-4-yI, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), or CH2SH and R3b is H; (d) R" is hydrogen, Cmo alkyl, Cmo alkyl optionally substituted with 25 a lower alkyl, alkoxy, di(lower alkyl)-amino, or halogen, Cmo haloalkyl, C3-io cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; (e) R5 is H, CN, CH3, vinyl, OCH3) OCH2CH3, CH2OH, CH2(halo), such as CH2F, N3i CH2CN, CH2N3> CH2NH2> CH2NHCH3, CH2N(CH3)2, 3983472-1 -27- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 halogen, including F, Cl, Br, or I, with the provisos that when X is OH , base is cytosine and R6 is H, R5 cannot be N3; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; 10 15 (g) X is H, OH, F, OMe, Cl, Br, I, NH2, or N3; (h) Y is OH, H, CM alkyl, vinyl, N3, CN, Cl, Br, F, I, O(C,.6 acyl), 0(Cu alkyl), NH2, NH(CM alkyl), NH(CM alkenyl), NH(C24 alkynyl), NH(CM acyl), N(Cm alkyl)2, N(C|.ig acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F, I), NO2, OC(O)O(CM alkyl), OC(O)O(CM alkyl), 0C(0)0(C24 alkynyl), OC(O)O(C2m alkenyl), OCM haloalkyl, O(aminoacyl), 0(Cm acyl), O(CM alkyl), O(C2m alkenyl), S(CM acyl), S(CM alkyl), S(C2m alkynyl), S(C2m alkenyl), SO(CM acyl), SO(Cim alkyl), SO(C2m alkynyl), SO(C2m alkenyl), SO2(Cm acyl), SO2(Cim alkyl), SO2(C2m alkynyl), SO2(C2m alkenyl), OS(O)2(Cim acyl), OS(O)2(CM alkyl), OS(O)2(C2m alkenyl), NH2, NH(CM alkyl), NH(CM alkenyl), NH(C2m alkynyl), NH(Cm acyl), N(Cm alkyl)2, or N(Cm acyl)2; (i) R7, R8,R9 are independently H, F, Cl, Br, I, OH, OR', SH, SR', NH2, NHR', NR'2j lower alkyl, halogenated (F, Cl, Br, I) lower alkyl, lower alkenyl of C2-C$, CO2H, CO2R', CONH2, CONHR', CONR'2> wherein R' is a Ci. 2o alkyl; a Ci-2o cycloalkyl; a C2-Ce alkenyl, a C2-Cg alkynyl. 20 A second aspect of the first embodiment is directed to a compound represented by formula 1-1 wherein (a) Rl is hydrogen, n-alkyl or a substituted or unsubstituted phenyl, where the substitutent of the substituted phenyl is at least one of a Ci_3 alkyl, a 25 C).3 alkoxy, F, Cl, Br, 1, nitro, cyano, and a Ci.3 haloalkyl; (b) R2 is hydrogen or CH3; (c) R3a and R3b are independently (i) R3a is hydrogen and R3b and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and 2983472-1 -28- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 C atoms (v) R3b is hydrogen and R3a and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 3 to 5, n is 2 to 4, and where R3' is independently hydrogen or C]^ alkyl and R3 is -OR1 or-N(R3')2); (vi) R3a is H and R3b is H, CH3, 5 CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, - CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3a is CH3, CH(CH3h, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3- 10 yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, ch2ch2cooh, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, ch2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4’-OH)-Ph), or CH2SH and R3b is H; (d) R4 is hydrogen, CH3, Εζ zPr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N- 15 methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haioalkyl, di(lower alkyl)amino-lower alkyl, or aminoacyl; (e) R5 is H, CN, CH3, OCH3, CH2OH, CH2(halo), such as CH2F, N3, CH2CN, CH2N3, CH2NH2i CH2NHCH3, CH2N(CH3)2, halogen, including F, Cl, 20 Br, or I, with the provisos that when X is OH, base is cytosine and R6 is H, R5 cannot be N3; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OCH3, NH2, or N3; (h) Y is OH, H, CH3, vinyl, N3, CN, Cl, Br, F, 1, OC(O)CH3, OCH3, 25 NH2, NHCH3, NH(vinyl), NH(acetyl), NH(C(O)CH3), N(CH3)2, N(C(O)CH3)2, or O(aminoacyl); (i) R7 and R8 are independently H, F, Cl, Br, I, OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, CH3, CH3^Xq, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, COiH, CO2CH3, CONH2, CONHCH3, or CON(CH3)2; and 2983472-1 -29- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 0) R9 is selected from among OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, OC(O)(Cl-20 alkyl), which include but are not limited to OC(O)(CH2)sCH3, NHC(O)(Cl-20 alkyl), which include but are not limited to NHC(O)(CH2)SCH3, and N(C(O)(CH2)SCH3)2, which include but is not limited to 5 N(C(O)(CH2)SCH3)2, where s is an integer selected from 0,1,2, 3,4, 5, 6,7, 8, 9,10, 11,12, 13,14, 15, 16, 17,18, and 19. A third aspect of the first embodiment is directed to a compound represented by formula 1-1 wherein 10 (a) R1 is hydrogen, n-alkyl or a substituted or unsubstituted phenyl, where the substitutent of the substituted phenyl is at least one of a CH3, OCH3, F, Cl, Br, I, nitro, cyano, and a CH3^Xq, where X is F, Cl, Br, or I, and q is 1-3; (b) R2 is hydrogen or CH3; (c) R3a is H and R3b is H, CH3, CH(CH3)2) CH2CH(CH3)2, 15 CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl or R3a is CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, 20 CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, - CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4’-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H; (d) R4 is hydrogen, CH3, Et, *Pr, "Pr, "Bu, 2-butyl, fBu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N- 25 methyl-azetidin-3-yI, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yI, lower haloalkyl, di(lower alkyl)amino-lower alkyl, or aminoacyl; (e) R5 is H, CN, CH3, OCH3, CH2OH, CH2(halo), such as CH2F, N3, CH2CN, CH2N3, CH2NH2, CH2NHCH3, CH2N(CH3)2, halogen, including F, Cl, 2983472-1 -30- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Br, or I, with the provisos that when X is OH, base is cytosine and R6 is H, R5 cannot be N3; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OCH3, NH2j or N3; 5 (h) Y is OH, H, CH3, vinyl, N3, CN, Cl, Br, F, I, OC(O)CH3, OCH3,. NH2, NHCH3, NH(vinyl), NH(acetyl), NH(C(O)CH3), N(CH3)2, N(C(O)CH3)2, or O(aminoacyl); (i) R7 and R8 are independently H, F, CI, Br, I, OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, CH3, CH3^Xq, where X is F, Cl, Br, or I and q is 10 1 to 3, vinyl, CO2H, CO2CH3, CONH2, CONHCH3, or CON(CH3)2, wherein R' is a Ci-2o alkyl; a Ci.2o cycloaikyl; a C2-C6 alkenyl, a C2-C6 alkynyl'; and (j) R9 is selected from among OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, OC(O)(Cl-20 alkyl), which include but are not limited to OC(O)(CH2)SCH3, NHC(O)(Cl-20 alkyl), which include but are not limited to 15 NHC(O)(CH2)SCH3, and N(C(O)(CH2)SCH3)2, which include but is not limited to N(C(O)(CH2)8CH3)2, where s is an integer selected from 0, 1,2, 3,4, 5,6,7, 8, 9, 10,11,12,13, 14,15,16,17,18, and 19. A fourth aspect of the first embodiment is directed to a compound represented by formula 1-2 2983472-1 -31 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 R9

1-2 wherein (a) R1 is hydrogen, methyl, ethyl, «-propyl, /-propyl, or a substituted 5 or unsubstituted phenyl, where the substitutent of the substituted phenyl is at least one of a CH3, OCH3, F, Cl, Br, I, nitro, cyano, and a CHa^Xq, where X is F, Cl, Br, or I, and q is 1-3; (b) R2 is hydrogen or CH3; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, 10 CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4’-OH)-Ph), CH2SH, or lower cycloalkyl or R3a is CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3) CH2CO2H, 15 CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, - CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4’-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H; (d) R4 is hydrogen, Cmo alkyl, Cmo alkyl optionally substituted with a lower alkyl, alkoxy or halogen, Cmo haloalkyl, C3^o cycloalkyl, cycloalkyl 20 alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such 2983472-1 -32- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; (e) R5 is H, CN, CH3, OCH3, CH2OH, CH2F, N3, CH2CN, CH2N3, CH2NH2, CH2NHCH3, CH2N(CH3)2, halogen, including F, Cl, Br, or I, with the 5 provisos that when X is OH, base is cytosine and R6 is H, R5 cannot be N3; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OCH3, Cl, Br, I, NH2, or N3; (h) Y is OH, H, CH3, vinyl, N3, CN, Cl, Br, F, I, OC(O)CH3, OCH3, NH2, NHCH3j NH(vinyl), NH(acetyl), NH(C(O)CH3), N(CH3)2, N(C(O)CH3)2, 10 or O(aminoacyl); (i) R7 and R8 are independently H, F, Cl, Br, I, OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, CH3, CH3.qXq, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2H, CO2CH3, CONH2, CONHCHj, or CON(CH3)2, wherein R' is a C|.2o alkyl; a Ci.2o cycloalkyl; a C2-C$ alkenyl, a C2-C6 alkynyl; and 15 (j) R9 is selected from among OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, OC(O)(Cl-20 alkyl), which include but are not limited to OC(O)(CH2)SCH3, NHC(O)(Cl-20 alkyl), which include but are not limited to NHC(O)(CH2)SCH3, and and N(C(O)(CH2)SCH3, which include but is not limited to N(C(O)(CH2)3CH3)2, where s is an integer selected from 0, 1,2, 3,4, 5, 6, 7, 20 8,9, 10, 11, 12, 13,14, 15,16, 17,18, and 19. A fifth aspect of the first embodiment is directed to a compound represented by formula 1-2 wherein (a) R1 is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, 25 p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; 2983472-1 -33- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 (c) R3· is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3h, CH(CH3)CH2CH3> CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CHjCHjCHjCHjNHj, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'- 5 OH)-Ph), CH2SH, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, MPr, "Bu, 2-butyl, fBu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyI-pyrrolidin-4-yl, lower haloalkyl, di(lower atkyl)amino-lower alkyl, or aminoacyl; 10 (e) R5 is H, CN, CH3, OCH3, CH2OH, CH2F, halogen, including F,

Cl, Br, or I; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OCH3, NH2, or N3; (h) Y is OH, H, CH3, vinyl, N3, CN, Cl, Br, F, I, OC(O)CH3, OCH3, 15 or O(aminoacyl); (i) R7 and R8 are independently H, F, Cl, Br, I, OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, CH3, CH3^Xq, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2H, CO2CH3, CONH2, CONHCH3, or CON(CH3)2, wherein R’ is a Ci-2o alkyl; a Ci.2o cycloalkyl; a C2-C6 alkenyl, a C2-Ce alkynyl; and 20 (j) R9 is selected from among OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, OC(0)(Ci-2o alkyl), which include but are not limited to OC(O)(CH2)SCH3, NHC(0)(Ci.2o alkyl), which include but are not limited to NHC(O)(CH2)SCH3, and N(C(O)(CH2)sCH3)2, which include but is not limited to N(C(0)(CH2)#CH3)2, where s is an integer selected from 0,1,2,3,4, 5,6,7, 8, 25 9,10,11,12,13, 14, 15,16,17, 18, and 19. A sixth aspect of the first embodiment is directed to a compound represented by formula 1-2 wherein 2983472-1 -34- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOUI (a) R1 is hydrogen, methyl, ethyl, n-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, 5 CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, Cmo alkyl, Cmo alkyl optionally substituted with a lower alkyl, alkoxy or halogen, Cmo haloalkyl, C3.10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted 10 heteroaryl; (e) Rs is H, OMe, CN, CH2F, F, Cl, Br, or I; (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, F, OCH3, F, Cl, Br, I, or N3; (h) Y is H, OH, CH3, F, Cl, Br, I, or N3, OCH3, OC(O)CH3, or 15 O(aminoacyl); (i) R7 and R8 are independently H, F, Br, SCH3, CH3, CHj^Xq, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2CH3, CONH2, CONHCH3, or CON(CH3)2; and (j) R9 is selected from among OH, OCH3, SH, SCH3, NH2, NHCH3, 20 N(CH3)2, OC(0)(Ci.2o alkyl), which include but are not limited to OC(O)(CH2)SCH3, NHC(0)(Ci.2o alkyl), which include but are not limited to NHC(O)(CH2)SCH3, and N(C(O)(CH2)5CH3)2, which include but is not limited to N(C(O)(CH2)SCH3)2, where s is an integer selected from 0, 1,2, 3, 4, 5, 6,7, 8, 9,10,11,12,13, 14,15,16,17,18, and 19. 25 A seventh aspect of the first embodiment is directed to a compound represented by formula 1-2 wherein 2983472-1 -35- WO 2008/121634

Docket No. 60137.0034WOU1 (a) R1 is hydrogen, methyl, ethyl, «-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-ch loro-phenyl, p-fluorophenyl; PCT/US2008/0S8183 (b) R2 is hydrogen; (c) R3" is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, 5 CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yI, N-methyl-pyrrolidin-3-yi, N-methyl-pyrrolidin-4-yl, N-methyI-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 10 (e) Rs is H; (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, OCH3, F, or N3; (h) Y is OH, OCH3, OC(O)CH3, or O(aminoacyl); (i) R7 and R8 are independently H, F, Br, SCH3, CH3, CH3^Xq, 15 where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2CH3, CONH2, CONHCH3, or CON(CH3)2; and (j) R9 is selected from among OH, OCH3, NH2, NHCH3, N(CH3)2, OC(O)(Ci_20 alkyl), which include but are not limited to OC(O)(CH2)SCH3, NHC(0)(Ci.2o alkyl), which include but are not limited to NHC(O)(CH2),CH3, 20 and N(C(O)(CH2)SCH3)2, which include but is not limited to N(C(O)(CH2)SCH3)2, where s is an integer selected from among 0,1,2, 3,4, 5, 6, 7, 8, 9,10,11,12,13,14, 15, 16,17,18, and 19.

An eighth aspect of the first embodiment is directed to a compound represented by formula 1-2 25 wherein (a) R1 is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro- phenyl, p-fluorophenyl; 2983472-1 -36- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 (b) R2 is hydrogen; (c) R3a is H and R3b is Η, CH3, CfI(CH3)2, CH2CH(CH3)2) CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, nPr, "Bu, 2-butyl, 'Bu, benzyl, 5 cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N- methyl-azetidin-3-yl, N-methyI-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; (e) R5isH; (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; 10 (g) X is H, OH, OCH3, F, orN3; (h) Y is OH, OCH3, OC(O)CH3, or O(aminoacyl); (i) R7 and R8 are independently H, F, Br, SCH3, CH3, CH^Xq, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2CH3, CONH2, CONHCH3, or CON(CH3)2; 15 (j) R9 is selected from among OH, OCH3, NH2, NHCH3, N(CH3)2, OC(O)(C|.20 alkyl), which include but are not limited to OC(O)(CH2)sCH3, NHC(0)(Ci-2o alkyl), which include but are not limited to NHC(O)(CH2)SCH3, and N(C(O)(CH2),CH3)2, which include but is not limited to N(C(0)(CH2)jCH3)2, where s is an integer selected from among 0,1,2, 3,4, 5, 6, 20 7, 8,9, 10, 11, 12, 13,14,15,16, 17, 18, and 19. A second embodiment of the invention is directed to a compound represented by formula I in which the base is a structure represented by formula b above, wherein R1, R2, R3a, R3b, R4, Rs, R6, X, Y, R7, and R8are defined in the Summary of the Invention section above. 25 A first aspect of the second embodiment is directed to a compound represented by formula 1-3 2983472-1 -37-

1-3 wherein (a) R1 is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which 5 includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of Cj.6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C].6 alkoxy, F, Cl, Br, I, nitro, cyano, Cm haloalkyl, -N(R* )2, Cm acylamino, -NHSO2Ci-6 alkyl, -SChNiR1'^ COR1", and -SO2Ci-6 alkyl; (Rr is independently hydrogen or alkyl, which includes, but is not limited to, C1.20 alkyl, Cmo alkyl, 10 or Cm alkyl, R1" is -OR' or -N(R* )2); (b) R2 is hydrogen or CH3; (c) R3a and R3b are (i) independently selected from hydrogen, Cmo alkyl, cycloalkyl, -(CH2)c(NR3)2, Cm hydroxyalkyl, -CH2SH, -(CH2)2S(O)dMe, -(CH2)3NHC(=NH)NH2, (lH-indol-3-yl)methyl, (lH-imidazol-4-yl)methyl, - 15 (CH2)eCOR3", aryl and aryl Cm alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Cm0 alkyl, Cm alkoxy, halogen, nitro and cyano; (ii) R3a and R3b both are Cm alkyl; (iii) R3a and R3b together are(CH2)f so as to form a spiro ring; (iv) R3a is hydrogen and R3b and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms (v) R is 20 hydrogen and R3a and R2 together are (CFhjn so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3' is independently hydrogen or Cm alkyl and R3" is -OR’ or -N(R3’)2); (vi) R3a is H and R3b is H, CH3, CH2CH3, CH(CH3)2, 2983472-1 -38- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2808/058183 CH2CH(CH3)2> CH(CH3)CH2CH3j CHjPh, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CHjCH2NH2, -CH2CH2CH2NHC(NH)NH2> CH2-imidazol-4-yl, CHjOH, CH(OH)CH3j CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) 5 R3° is CH3, -CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CHj-indol-3-yl, -CH2CH2SCH3) CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, ch2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b Is H, where R3' is independently hydrogen or alkyl, which 10 includes, but is not limited to, Cuo alkyl, Cmo alkyl, or alkyl, R3 is -OR' or -n(R3')2); (d) R" is hydrogen, Cmo alkyl, Cmo alkyl optionally substituted with a lower alkyl, alkoxy or halogen, Cmo haloalkyl, C3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such 15 as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; (e) R5 is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., -(CFDpOH, where p is 1 -6, including hydroxyl methyl (CH2OH), CH2F, N3, CH2CN, CH2NH2, CH2NHCH3, CH2N(CH3)2, alkyne (optionally 20 substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R6 is H, R5 cannot be N3 and when X is OH, R6 is CH3 or CH2F and B is a purine base, R5 cannot be H; (f) R6 is H, CH3, CH2F, CHFj, CF3, F, or CN; (g) X is H, OH, F, OMe, Cl, Br, I, NH2, or N3; 25 (h) Y is OH, H, Cm alkyl, C2-4 alkenyl, C24 alkynyl, vinyl, N3, CN,

Cl, Br, F, I,NO2, OC(O)O(Cm alkyl), OC(O)O(CM alkyl), OC(O)O(C24 alkynyl), 0C(0)0(C24 alkenyl), OCmo haloalkyl, O(aminoacyl), 0(Cmo acyl), O(CM alkyl), 0(C24 alkenyl), S(Cj4 acyl), S(Cm alkyl), S(C24 alkynyl), S(C24 alkenyl), SO(CM acyl), SO(CM alkyl), SO(C2m alkynyl), S0(C24 alkenyl), 30 S02(Ci4 acyl), SO2(Ci4 alkyl), S02(C2m alkynyl), SO2(C24 alkenyl), OS(O)2(Ci. 4 acyl), 0S(0)2(C,4 alkyl), OS(OHC24 alkenyl), NH2, NH(CM alkyl), NH(C24 2983472*1 -39- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 alkenyl), NH(C24 alkynyl), NH(Ct.4 acyl), N(Cm alkyl)2, or N(Cm8 acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (CI, Br, F, I), NO2, C(0)0(Ci4 alkyl), C(O)O(Ct_4 alkyl), C(O)O(C24 alkynyl), C(0)0(C24 alkenyl), O(CM acyl), O(CM alkyl), 0(C24 5 alkenyl), S(CM acyl), S(CM alkyl), S(C24 alkynyl), S(C24 alkenyl), SO(CM acyl), SO(CM alkyl), SO(C24 alkynyl), SO(C24 alkenyl), SO2(CM acyl), SO2(Cm alkyl), SO2(C24 alkynyl), SO2(C24 alkenyl), 0S(0)2(Ci4 acyl), 0S(0)2(C,4 alkyl), OS(O)2(C24 alkenyl), NH2, NH(CM alkyl), NH(C24 alkenyl), NH(C24 alkynyl), NH(Ci4 acyl), N(C]4 alkyl)2, or N(CM acyl)2; 10 (i) R7 and R8 are independently H, F, Cl, Br, I, OH, OR', SH, SR', NH2, NHR', NR2, lower alkyl, halogenated (F, Cl, Br, Ϊ) lower alkyl, lower alkenyl of C2-Cs, CO2H, CO2R’, CONH2, CONHR', CONR'2, wherein R* is a Ci. 20 alkyl; a Ci.2o cycloalkyl; a C2-C6 alkenyl, a C2-C6 alkynyl.

The second aspect of the second embodiment is directed to a compound 15 represented by formula 1-3 wherein (a) R1 is hydrogen, n-alkyl or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of Cj.6 alkyl, C].6 alkoxy, F, Cl, Br, I, nitro, cyano, Cm haloalkyl; 20 (b) R2 is hydrogen or CH3; (c) R3a and R3b are independently (i) R3“ is hydrogen and R3b and R2 together are (CH2)„ so as to form a cyclic ring that includes the adjoining N and C atoms (v) R3b is hydrogen and R3a and R2 together are (CH2)„ so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 25 2, e is 0 to 3, f is 3 to 5, n is 2 to 4, and where R3 is independently hydrogen or CM alkyl and R3" is -OR’ or -N(R3‘)2); (vi) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3h, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, 30 CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) 2983472-1 -40- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOUI R3a is CHj, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3> CH2CO2H, CH2C(O)NH2j ch2ch2cooh, CH2CH2C(O)NH2j CH2CH2CH2CH2NH2j -CH2CH2CH2NHC(NH)NH2, ch2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4’-OH)-Ph), or CH2SH and R3b is H; 5 (d) R4 is hydrogen, Cmo alkyl, Cmo alkyl optionally substituted with a lower alkyl, alkoxy or halogen, Cmo haloalkyl, €3.10 cycloalkyl, cycloalkyt alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; 10 (e) R5 is H, CN, CH3, vinyl, OCH3, OCH2CH3, CH2OH, CH2(halo), such as CH2F, N3, CH2CN, CH2N3, CH2NH2, CH2NHCH3, CH2N(CH3)2, halogen, including F, Cl, Br, or I; (f) R6 is H, CH3> CH2F, CHF2, CF3) F, or CN; (g) X is H, OH, F, OMe, halogen, NH2, or N3; 15 (h) Y is OH, H, Cm alkyl, vinyl, N3, CN, Cl, Br, F, I, 0(Cm acyl), O(CM alkyl), NH2, NH(CM alkyl), NH(C24 alkenyl), NH(CW alkynyl), NH(CM acyl), N(Cm alkyl^, N(Cm8 acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F, I), NO2, OC(O)O(CM alkyl), OC(O)O(CM alkyl), OC(O)O(C2^ alkynyl), OC(O)O(C2-4 20 alkenyl), OCmo haloalkyl, O(aminoacyl), O(Ci-4 acyl), 0(Cm alkyl), O(C2-4 alkenyl), S(Ci^ acyl), S(CM alkyl), S(C24 alkynyl), S(C2-4 alkenyl), SO(CM acyl), SO(Cm alkyl), SO(C2^ alkynyl), SO(C24 alkenyl), SO2(CM acyl), SO2(CM alkyl), SO2(C24 alkynyl), SO2(C24 alkenyl), OS(O>2(Cm acyl), OS(O)2(Cm alkyl), OS(O)2(C24 alkenyl), NH2, NH(CM alkyl), NH(C2-4 25 alkenyl), NH(C2^ alkynyl), NH(CM acyl), N(CM alkyl)2, N(CM acyl^; (i) R7 and R8 are independently H, F, Cl, Br, I, OH, OR', SH, SR', NH2, NHR*, NR'2, lower alkyl, halogenated (F, Cl, Br, I) lower alkyl, lower alkenyl of C2-Cfi, CO2H, CO2R', CONH2, CONHR', CONRr2, wherein R' is a Ci. 20 alkyl; a C1-20 cycloalkyl; a C2-Q alkenyl, a C2-C6 alkynyl. 2983472-1 -41 - PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOUI

The third aspect of the second embodiment is directed to a compound represented by formula 1-3 wherein (a) R1 is hydrogen, n-alkyl or a substituted or unsubstituted phenyl, 5 where the substitutent of the substituted phenyl is at least one of a C].3 alkyl, a

Ci.3 alkoxy, F, Cl, Br, I, nitro, cyano, and a C).3 haloalkyl; (b) R2 is hydrogen, CH3, R3a or R3b and R2 together are (CH2)3 so as to form a cyclic ring that includes the adjoining N and C atoms, C(O)CR3aR3bNHR1, where n is 2 to 4 and R1, R3a, and R3b are as defined herein; 10 (c) R3a and R3b are independently (i) R3a is hydrogen and R3b and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms (v) R3b is hydrogen and R3a and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 3 to .5, n is 2 to 4, and where R3' is independently hydrogen or 15 .Ci.6 alkyl and R3" is -OR' or -N(R3’)2); (vi) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4’-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) 20 R3a is CH3, CH(CH3)2, CHiCH^h, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, ch2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H; 25 (d) R4 is hydrogen, CH3, Et, 'Pr, flPr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 2983472-1 -42- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 (e) R5 is H, CN, CH3, OCH3, CH2OH, CH2(halo), such as CH2F, N3, CH2CN, CH2N3, CH2NH2, CH2NHCH3, CH2N(CH3)2, halogen, including F, Cl, Br, or I; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OCH3, halogen, NH2, or N3 (h) Y is OH, H, CH3, vinyl, N3, CN, Cl, Br, F, I, OC(O)CH3, OCH3, NH2, NHCH3, NH(vinyl), NH(acetyl), NH(C(O)CH3), N(CH3)2, N(C(O)CH3)2; (i) R7 and R8 are independently H, F, Cl, Br, I, OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, CH3, CH3^Xq, where X is F, Cl, Br, or 1 and q is 10 1 to 3, vinyl, CO2H, CO2CH3, CONH2, CONHCH3, or CON(CH3)2.

The fourth aspect of the second embodiment is directed to a compound represented by formula 1-3 wherein (a) R1 is hydrogen, n-alkyl or a substituted or unsubstituted phenyl, 15 where the substitutent of the substituted phenyl is at least one of a CH3, OCH3, F, Cl, Br, I, nitro, cyano, and a CH3.qX<„ where X is F, Cl, Br, or I, and q is 1-3; (b) R2 is hydrogen or CH3; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, 20 CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, - CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4’-OH)-Ph), CH2SH, or lower cycloalkyl or R3a is CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, - 25 CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H; (d) R4 is hydrogen, CH3, Et, *Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N- 2983472-1 -43- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WODl methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N- methyi-piperidin-4-yl, lower haloalkyI, or di(lower alkyi)amino-lower alkyl; (e) R5 is H, CN, CH3, OCH3, CH2OH, CH2(halo), such as CH2F, N3, CH2CN, CH2N3, CH2NH2, CH2NHCH3j CH2N(CH3)2, halogen, including F, Cl, 5 Br, or I; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OCH3, NH2, or N3; (h) Y is OH, H, CH3, vinyl, N3, CN, Cl, Br, F, I, OC(O)CH3, OCH3, NH2, NHCH3, NH(vinyl), NH(acetyl), NH(C(O)CH3), N(CH3)2, N(C(O)CH3)2; 10 (i) R7 and R8 are independently H, F, Cl, Br, I, OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, CH3, CHa-qXq, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2H, CO2CH3, CONH2, CONHCH3, or CON(CH3)2, wherein R' is a Ci-20 alkyl; a Ci.2o cycloalkyl; a C2-Ce alkenyl, a C2-C6 alkynyl.

The fifth aspect of the second embodiment is directed to a compound 15 represented by formula 1-4

1-4 wherein (a) R1 is hydrogen, methyl, ethyl, n-propyl, /-propyl, or a substituted 20 or unsubstituted phenyl, where the substitutent of the substituted phenyl is at 2983472-1 -44- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 least one of a CH3, OCH3, F, Cl, Br, I, nitro, cyano, and a CH3.qXq, where X is F,

Cl, Br, or I, and q is 1-3; (b) R2 is hydrogen or CH3; (c) R3fl is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, 5 CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl or R3a is CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yI, -CH2CH2SCH3, CH2CO2H, 10 CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, - CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H; (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, iBu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N- 15 methyl-azetidin-3-yl, N-methyi-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; (e) R5 is H, CN, CH3, OCH3, CH2OH, CH2F, N3, CH2CN, CH2N3, CH2NH2, CH2NHCH3, CH2N(CH3)2, halogen, including F, CI, Br, or I; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; 20 (g) X is H, OH, F, OCH3j Cl, Br, I, NH2, or N3; (h) Y is OH, H, CH3, vinyl, N3, CN, Cl, Br, F, I, OC(O)CH3, OCH3, NH2, NHCH3, NH(vinyl), NH(acetyl), NH(C(O)CH3), N(CH3)2, N(C(O)CH3)2; (i) R7 and R8 are independently H, F, Cl, Br, 1, OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, CH3, CH^Xq, where X is F, Cl, Br, or I and q is 25 1 to 3, vinyl, CO2H, CCbCTB, CONH2, CONHCH3, or CON(CH3)2, wherein R' is a Ci-2o alkyl; a Cj.2o cycloalkyl; a C2-C6 alkenyl, a C2-Cfi alkynyl,

The sixth aspect of the second embodiment is directed to a compound represented by formula 1-4 2983472-1 -45- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 wherein (a) R1 is hydrogen, methyl, ethyl, «-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; 5 (c) R3' is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2> CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2i CH2CH2CH2CH2NH2i -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH20H, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; 10 (d) R4 is hydrogen, CH3, Et, jPr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; (e) R5 is H, CN, CH3, OCH3, CH2OH, CH2F, halogen, including F, 15 Cl, Br, or I; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OCH3, NH2, or N3; (h) OCH3; Y is OH, H, CH3, vinyl, NH2, N3, CN, Cl, Br, F, I, OC(O)CH3, 20 (i) R7 and R8 are independently H, F, Cl, Br, I, OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, CH3, CHa-qXq, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2H, CO2CH3, CONH2, CONHCH3, or CON(CH3)2, wherein R’ is a C1.20 alkyl; a Ci_2o cycloalkyl; a C2-C6 alkenyl, a C2-C6 alkynyl.

The seventh aspect of the second embodiment is directed to a compound 25 represented by formula 1-4 wherein 2983472-1 -46- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 (a) R1 is hydrogen, methyl, ethyl, η-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) RJ is hydrogen or CH3; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, 5 CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyI, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yI, lower haloalkyl, or di(Jower alkyl)amino-lower alkyl; 10 (e) R5 is H, OMe, CN, CH2F, F, Cl, Br, or I; (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, F, OCH3, F, Cl, Br, I, NH2 or N3; (h) Y is H, OH, CH3, F, Cl, Br, I, NH2 or N3, OCH3, or OC(O)CH3; (i) R7 and R* are independently H, F, Br, SCH3, CH3, CH^Xq, 15 where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2CH3, CONH2, CONHCH3, or CON(CH3)2;

The eighth aspect of the second embodiment is directed to a compound represented by formula 1-4 wherein 20 (a) R1 is hydrogen, methyl, ethyl, n-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; 2983472-1 -47- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 (d) R4 is hydrogen, 0¾. Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 5 (e) R5isH; (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, OCH3, F, NH2 or N3; (h) Y is OH, NH2, OCH3, or OC(O)CH3; (i) R7 and R8 are independently H, F, Br, SCH3, CH3, CH3^Xq, 10 where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2CH3, CONH2, CONHCH3, or CON(CH3)2.

The ninth aspect of the second embodiment is directed to a compound represented by formula 1-4 wherein 15 (a) R1 is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro- phenyl, p-fluorophenyl; (b) R2 is hydrogen; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; 20 (d) R4 is hydrogen, CH3, Et, ’Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yI, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; (e) R5isH; 25 (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; 2983472-1 -48- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 (g) X is H, OH, OCH3, F, or N3; (h) Y is OH, OCH3, or OC(O)CH3; (i) R7 and R8 are independently H, F, Br, SCH3, CH3, CH3.qXq, where X is F, Cl, Br, or 1 and q is 1 to 3, vinyl, CO2CH3, CONH2, CONHCH3, or 5 CON(CH3)2. A third embodiment of the invention is directed to a compound represented by formula I in which the base is a structure represented by formula c above, wherein Rl, R2, R3a, R3b, R4, R5, R6, X, Y, Z, R10, Rn, and R12 are defined in the Summary of the Invention section above; with the proviso that R11 10 is not H. A first aspect of the third embodiment is directed to a compound represented by formula 1-5

1-5 15 wherein (a) R1 is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of Ci^ alkyl, C2^ alkenyl, €2^ alkynyl, Ci_6 alkoxy, F, Cl, Br, I, nitro, cyano, C^ haloalkyl, -N(Rr)2, C^ acylamino, - 20 NHSOjCi^ alkyl, -SO2N(R* )2, COR1', and -SOjCj-e alkyl; (R1 is independently hydrogen or alkyl, which includes, but is not limited to, C1-20 alkyl, Cmo alkyl, or Cj_6 alkyl, R1" is -OR' or -N(R’ h); 2983472-1 -49- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 (b) R2 is hydrogen or CH3; (c) R3a and R3b are (i) independently selected from hydrogen, Ci.10 alkyl, cycloalkyl, -(CH2)c(NR3')2, Ci^ hydroxyalkyl, -CH2SH, -(CH2)2S(O)dMe, -(CH2)3NHC(-NH)NH2, (lH-indol-3-yl)methyl, (lH-imidazol-4-yI)methyl, - 5 (CH2)eCOR3\ aryl and aryl Ci.3 alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Cmo alkyl, Ci-e alkoxy, halogen, nitro and cyano; (ii) R3a and R3b both are Ct^ alkyl; (iii) R3a and R3b together are(CH2)rso as to form a spiro ring; (iv) R3a is hydrogen and R3b and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms (v) R3b is 10 hydrogen and R3a and R2 together are (CH2)„ so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3' is independently hydrogen or Ci^ alkyl and R3" is -OR' or -N(R3’)2); (vi) R3a is H and R3b is from H, CH3, CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, - 15 CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4’-OH)-Ph), CH2SH, or lower cycloalkyl; or(viii) R3a is CH3, -CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indoI-3-yl,-CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, 20 CH2CH2C(O)NH2, CH2CH2CH2CH2NH2j -CH2CH2CH2NHC(NH)NH2, ch2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H, where R3' is independently hydrogen or alkyl, which includes, but is not limited to, C].2o alkyl, Cmo alkyl, or Ci^ alkyl, R3" is -OR' or -N(R3)2); 25 (d) R4 is hydrogen, Cmo alkyl, Cmo alkyl optionally substituted with a lower alkyl, alkoxy or halogen, Cmo haloalkyl, C3.i0 cycioalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; 30 (e) R5 is H, a lower alkyl, CN, vinyl, 0-(lower alkyl), hydroxyl lower alkyl, i.e., -(CH2)POH, where p is 1 -6, including hydroxyl methyl (CH2OH), CH2F, N3, CH2CN, CH2NH2, CH2NHCH3, CH2N(CH3)2, alkyne (optionally 2983472-1 -50- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R6 is H, R5 cannot be N3 and when X is OH, R6 is CH3 or CH2F and B is a purine base, R5 cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OMe, halogen, NH2, or N3; (h) Y is OH, H, Cm alkyl, Cm alkenyl, Cm alkynyl, vinyl, N3, CN, Cl, Br, F, I, NO2, OC(0)0(Cm alkyl), OC(O)O(CM alkyl), OC(O)O(C24 alkynyl), OC(O)O(Cm alkenyl), OCi.10 haloalkyl, O(aminoacyl), O(Cm0 acyl), 0(Cm alkyl), 0(Cm alkenyl), S(Cm acyl), S(Cm alkyl), S(C24 alkynyl), S(Cm 10 alkenyl), SO(Cm acyl), SO(CM alkyl), SO(Cm alkynyl), SO(Cm alkenyl), SO^Cm acyl), SO2(CM alkyl), SO2(Cm alkynyl), SO2(Cm alkenyl), OS(O)2(Ci. 4 acyl), OS(O)2(Cm alkyl), OS(O)2(Cm alkenyl), NH2, NH(CM alkyl), NH(C24 alkenyl), NH(Cm alkynyl), NH(Cm acyl), N(Cm alkyl)2, N(Cm8 acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, 15 one to three halogen (Cl, Br, F, I), NO2, C(O)O(Cm alkyl), C(0)0(Cm alkyl), C(0)0(Cm alkynyl), C(0)0(Cm alkenyl), O(C|4 acyl), O(CM alkyl), O(Cm alkenyl), S(Cm acyl), S(Cm alkyl), S(Cm alkynyl), S(Cm alkenyl), SO(Cm acyl), SO(Cm alkyl), SO(Cm alkynyl), SO(Cm alkenyl), SO2(Cm acyl), SO2(Cm alkyl), S02(Cm alkynyl), SO2(Cm alkenyl), OS(O)2(Cm acyl), 20 OS(O)2(CM alkyl), OS(O)2(Cm alkenyl), NH2, NH(Cm alkyl), NH(C24 alkenyl), NH(C24 alkynyl), NH(Cm acyl), N(Cm alkyl)2, N(Cm acyl)2; (i) R10 and R11 are independently H, F, Cl, Br, I, OH, OR', SH, SR', NH2, NHR', NR'2, lower alkyl of Ci-Ce, halogenated (F, Cl, Br, I) lower alkyl of Cj-Ce, lower alkenyl of C2-C6, halogenated (F, Cl, Br, I) lower alkenyl of C2-Cfi, 25 lower alkynyl of C2-Ci such as OCH, halogenated (F, Cl, Br, 1) lower alkynyl of C2-C6, lower alkoxy of Ci-Ce, halogenated (F, Cl, Br, I) lower alkoxy of Ci-C6, COaH, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R', with the proviso that when R10 is OH and Rn is not NH2; wherein R' is an optionally substituted alkyl, which includes, but is not 30 limited to, an optionally substituted Cj.2o alkyl, an optionally substituted Cmo alkyl, an optionally substituted lower alkyl; an optionally substituted cycloalkyl; 2983472-1 -51- PCT/US2008/058183 WO 2008/121634

Docket No· 60137.0034WOU1 an optionally substituted alkynyl of C2-C6, an optionally substituted lower alkenyl of C2-Cg, or optionally substituted acyl, which includes but is not limited . to C(O) alkyl, C(0)(Ci.2o alkyl), C(0)(Cuo alkyl), or C(O)(lower alkyl) or alternatively, in the instance of NR2, each R' comprise at least one C atom that 5 are joined to form a heterocycle comprising at least two carbon atoms; and (J) Z isN or CR12; and R12 is an H, halogen (including F, Cl, Br, I), OH, OR*, SH, SR', NH2, NHR', NR*2, NO2 lower alkyl of Ci-Cfi, halogenated (F, CI, Br, I) lower alkyl of Ci-Ce, lower alkenyl of C2-Ce, halogenated (F, Cl, Br, I) lower alkenyl of C2-C6, 10 lower alkynyl of C2-C6, halogenated (F, Cl, Br, I) lower alkynyl of C2-C6, lower alkoxy of Ci-C$, halogenated (F, Cl, Br, I) lower alkoxy of C1 -Cg, CO2H, CO2R', CONH2, CONHR’, CONR'2, CH=CHCO2H, or CH=CHCO2R'.

A second aspect of the third embodiment is directed to a compound represented by formula I-S 15 wherein (a) R1 is hydrogen, methyl, ethyl, «-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, 20 CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yI,-CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CHa((4'-OH)-Ph), CH2SH, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, wBu, 2-butyl, 'Bu, benzyl, 25 cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N- methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 2983472-] -52- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 (e) R5 is H, CN, CH3, OCH3, CH2OH, CH2F, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H. (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OCH3, Cl, Br, I, NH2, or N3; (h) Y is OH, H, CH3, vinyl, NH2, N3, CN, Cl, Br, F, I, OC(O)CH3, OCH3; (i) R10 and R11 are independently H, F, Br, I, OH, OR’, NH2, NHR', NR’2, CO2R', CONH2, CONHR’, CONR'2, CH=CHCO2H, or CH=CHCO2R', 10 with the proviso that when R10 is OH and Rn is not NH2; wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 0) Z is N or CR12; and 15 R12 is an H, halogen (including F, Cl, Br, I), OR1, NH2, NHR*, NR2, NO2, lower alkyl of Ci-C6, CO2R', CONH2, CONHR', CONR’2, CH=CHCO2H, or CH=CHCO2R’. A third aspect of the third embodiment is directed to a compound 20 represented by formula 1-5 wherein (a) R1 is hydrogen, methyl, ethyl, n-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; 25 (c) R38 is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; 2983472-1 -53- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N- methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N- methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 5 (e) R5 is H, CN, CH2F, F, Cl, Br, or I; with the proviso that X is OH, R6 is CH3 or CH2F, R5 cannot be H; (0 R6 is H, CH3, CH2F, CHF2, CF3j or F; (g) X is H, OH, F, OCH3, F, Cl, Br, I, NH2 or N3; (h) Y is H, OH, CH3, F, Cl, Br, I, NH2 or N3, OCH3, or OC(O)CH3; 10 (i) R10 and R11 are independently H, F, Br, I, OH, OR', NH2, NHR', NR'2, CO2R\ CONH2, CONHR', CONR’2, CH=CHCO2H, or CH=CHCO2R', with the proviso that when R10 is OH and R11 is not NH2; wherein R’ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R' comprise at least one C atom that 15 are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z is N or CR12; and R’2 is an H, halogen (including F, Cl, Br, I), OR', NH2, NHR’, NR'2, NO2, lower alkyl of C|-C6, CO2R', CONH2, CONHR', CONR’2, CH=CHCO2H, or CH=CHCO2R'. 20 A fourth aspect of the third embodiment is directed to a compound represented by formula 1-5 wherein (a) R* is hydrogen, methyl, ethyl, «-propyl, /-propyl, phenyl, p-tolyl, 25 p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen; 2983472-1 -54- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N- 5 methyl-azetid in-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; (e) R5 is H, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; 10 (g) X is H, OH, OCH3, F, NH2 or N3; (h) Y is OH, NH2, OCH3, or OC(O)CH3; (i) R10 and R11 are independently H, F, Br, I, OH, OR’, NH2, NHR', NR'2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R', with the proviso that when R10 is OH and R11 is not NH2; 15 wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR’2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z is N or CR12; and R12 is an H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, NO2, 20 lower alkyl of CrC6, CO^’, CONH2, CONHR', CONR'2, CHCHCOiH, or CH=CHCO2R’. A fifth aspect of the third embodiment is directed to a compound represented by formula 1-5 25 wherein (a) R1 is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro- phenyl, p-fluorophenyl; 2983472-1 -55- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 (b) R2 is hydrogen; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, 5 cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyI-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower hatoalkyl, or di(lower atkyl)amino-lower alkyl; (e) R5 is H, with the provisos that when X is OH, R6 is CH3 or CH2F, Rs cannot be H; 10 (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, OCH3, F, NH2 or N3; (h) Y is OH, NH2, OCH3, or OC(O)CH3; (i) R10 and R11 are independently H, F, Br, I, OH, OR', NH2, NHR', NR*2, CO2R', CONH2, CONHR', CONR'z, CH=CIICO2H, or CH=CHCO2R', 15 with the proviso that when R10 is OH and R11 is notNH2; wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 0) Z is N or CR12; and 20 R12 is an H, halogen (including F, Cl, Br, 1), OR’, NH2l NHR', NR',, NO2, lower alkyl of Ci-C6, COjR', CONHj, CONHR', CONR'z, CH=CHCOzH, or CH=CHCO2R'. A sixth aspect of the third embodiment is directed to a compound represented by formula 1-5 25 wherein 2983472-1 -56- WO 2008/121634

Docket No. 60137.0034WOUI PCT/US2008/058183 (a) R1 is hydrogen, methyl, ethyl, η-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, 5 CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, ch2ch2ch2ch2nh2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CHaOH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Εζ 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, 10 cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; (e) R5 is H, CN, CH3, OCH3, CH2OH, CH2F, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot 15 beH. (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OCH3, Cl, Br, I, NH2, or N3; (h) Y is OH, H, CH3, vinyl, NH2, N3, CN, Cl, Br, F, I, OC(O)CH3, OCH3; 20 (i) R*° is NH2 and Rn is H, F, Br, I, OH, OR', NH2, NHR', NR’2, CO2R\ CONH2, CONHR*, CONR’z, CH=CHCO2H, or CH=CHCO2R'; wherein R' is a lower alkyl, a lower cycloalkyl, or C(0)(lower alkyl) or alternatively, in the instance of NR'2, each Rr comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 25 G) Z is N or CR12; and 2983472-1 -57- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 R*2 is an H, halogen (including F, Cl, Br, I), OR', NH2, NHR’, NR'2, NO2, lower alkyl of C,-C6, CO2R', CONH2, CONHR', CONR’2, CH=CHCO2H, or CH=CHCO2R'. A seventh aspect of the third embodiment is directed to a compound 5 represented by formula 1-5 wherein (a) R1 is hydrogen, methyl, ethyl, η-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; 10 (c) R3* is H and R3b is H, CHj, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3> Et, 'Pr, "Pr, ”Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-y), N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N- 15 methyl-piperidin-4-yl, lower haloalkyl, or di(lower atkyl)amino-lower alkyl; (e) R5 is H, CN, CH2F, F, Cl, Br, or I; with the proviso that X is OH, R6 is CH3 or CH2F, R5 cannot be H; 20 (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, F, OCH3, F, Cl, Br, I, NH2 or N3; (h) Y is H, OH, CH3, F, Cl, Br, I,NH2orN3, OCH3, or OC(O)CH3; (i) R10 is NH2 and R11 is H, F, Br, I, OH, OR’, NH2, NHR’, NR'a, CO2R’, CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'; wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR2, each R' comprise at least one C atom that 25 are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z is N or CR12; and 2983472-1 -58- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 R12 is an H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, NO2, lower alkyl of CrC6, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R’.

An eighth aspect of the third embodiment is directed to a compound 5 represented by formula 1-5 wherein (a) R1 is hydrogen, methyl, ethyl, «-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-ch loro-phenyl, p-fluorophenyl; (b) RJ is hydrogen; 10 (c) R3" is H and R3b is H, CH3> CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2PI1, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyI, zBu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N- 15 methyl-piperidin-4-yl, lower haloalkyl; (e) R5 is H, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H; (1) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, OCH3, F, NH2 or N3; 20 (h) Y is OH, NH2, OCH3, or OC(O)CH3; (i) R10 is NH2 and R11 is H, F, Br, I, OH, OR’, NH2, NHR’, NR’2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'; wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R' comprise at least one C atom that 25 are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z is N or CR12; and 2983472-1 -59- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 R12 is an H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, NO2, lower alkyl of Ct-C6, CO2R', CONH2, CONHR', CONR’2, CH=CHCO2H, or CH=CHCO2R'. A ninth aspect of the third embodiment is directed to a compound 5 represented by formula 1-5 wherein (a) R1 is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen; 10 (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, nPr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, or N-methyl-pyrrolidin-4-yl, 15 lower haloalkyl, or di(lower alkyl)amino-lower alkyl; (e) R5 is H, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, OCH3, F, NH2 or N3; 20 (h) Y is OH, NH2, OCH3, or OC(O)CH3; (i) R10 is NH2 and R’1 is H, F, Br, I, OH, OR’, NH2, NHR’, NR’2, CO2R1, CONH2, CONHR’, CONR'2, CH-CHCO2H, or CH=CHCO2R’; wherein R’ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R* comprise at least one C atom that 25 are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z is N or CR12; and 2983472-1 -60- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 R12 is an H, halogen (including F, Cl, Br, I), OR’, NH2, NHR', NR'2) NO2, lower alkyl of C,-C6, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R’. 5 A tenth aspect of the third embodiment is directed to a compound represented by formula 1-6

wherein 10 (a) R’ is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of Cm alkyl, C2-0 alkenyl, C2^ alkynyl, Cm alkoxy, F, Cl, Br, I, nitro, cyano, Cm haloalkyl, -N(R' )2, Cm acylamino, -NHS02Cm alkyl, -SO2N(Rr)2, COR1’, and -SC^Cm alkyl; (Rr is independently 15 hydrogen or alkyl, which includes, but is not limited to, Cj.2o alkyl, Ci.jo alkyl, or Cm alkyl, R1" is-OR1 or-N(Rl)2); (b) R2 is hydrogen or CH3; (c) R3a and R3b are (i) independently selected from hydrogen, Ci_io alkyl, cycloalkyl, -(CH2)c(NR3)2, Cm hydroxyalkyl, -CH2SH, -(CH2)2S(O)dMe, - 20 (CH2)3NHC(~NH)NH2, (1 H-indol-3-y l)methy 1, (1 H-imidazol-4-yl)methyl, -(CH2)eCOR3", aryl and aryl Cj.3 alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Ci-io alkyl, Cm alkoxy, halogen, nitro and cyano; (ii) R3a and R3b both are Cm alkyl; (iii) R3a and R3b together are(CH2)f so 2983472-1 -61- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 as to form a spiro ring; (iv) R3fl is hydrogen and R3b and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms (v) R3b is hydrogen and R3a and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f 5 is 2 to 5, n is 2 to 4, and where R3 is independently hydrogen or Cj.6 alkyl and R3" is -OR’ or -N(R3’)2); (vi) R3a is H and R3b is H, CH3, CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yI, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, 10 CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R38 is CH3, -CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, ch2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower 15 cycloalkyl and R3b is H, where R3 is independently hydrogen or alkyl, which includes, but is not limited to, C1.2o alkyl, Cmo alkyl, or Cms alkyl, R3 is -OR1 or -N(R3')2); (d) R4 is hydrogen, Cmo alkyl, C1-10 alkyl optionally substituted with a lower alkyl, alkoxy or halogen, Cmo haloalkyl, C3.io cycloalkyl, cycloalkyl 20 alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; (e) R5 is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e,, -(CH2)POH, where p is 1 -6, including hydroxyl methyl (CH2OH), 25 CH2F, N3, CH2CN, CH2NH2, CH2NHCH3, CH2N(CH3)2, alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R6 is H, Rs cannot be N3 and when X is OH, R6 is CH3 or CH2F and B is a purine base, R3 cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; 30 (g) X is H, OH, F, OMe, Cl, Br, I, NH2, or N3; 2983472-i -62- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 (h) Y is OH, H, Cm alkyl, Cm alkenyl, Cm alkynyl, vinyl, N3, CN, Cl, Br, F, I, NO2, OC(O)O(Cm alkyl), OC(O)O(Cm alkyl), 0C(0)0(C24 alkynyl), OC(O)O(Cm alkenyl), OCuo haloalkyl, O(aminoacyl), O(Cu0 acyl), O(Cm alkyl), O(Cm alkenyl), S(Cm acyl), S(Cm alkyl), S(CM alkynyl), S(Cm 5 alkenyl), SO(Cm acyl), SO(Cm alkyl), SO (Cm alkynyl), SO(C2-4 alkenyl), SO2(Cm acyl), SO2(Cm alkyl), SO2(Cm alkynyl), SO2(Cm alkenyl), OS(O)2(C]. 4 acyl), OS(O)2(Cm alkyl), OS(O)2(C2.4 alkenyl), NH2, NH(Cm alkyl), NH(Cm alkenyl), NH(Cm alkynyl), NH(Cm acyl), N(Cm alkyt)2, N(Cue acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, 10 one to three halogen (Cl, Br, F, I), NO2, C(O)O(Cm alkyl), C(O)O(Cm alkyl), C(O)O(Cm alkynyl), C(O)O(Cm alkenyl), O(CM acyl), O(CM alkyl), O(C2^ alkenyl), S(Cm acyl), S(CM alkyl), S(Cm alkynyl), S(Cm alkenyl), SO(Cm acyl), SO(Cm alkyl), SO(Cm alkynyl), SO(Cm alkenyl), SO2(CM acyl), SO^Cm alkyl), SO2(C2-4 alkynyl), SO2(Cm alkenyl), OS(O)2(CM acyl), 15 OS(O)2(Cm alkyl), OS(O)2(Cm alkenyl), NH2, NH(CM alkyl), NH(Cm alkenyl), NH(Cm alkynyl), NH(Cm acyl), N(CM alkyl)2, N(CM acyl)2; (i) R10 and R11 are independently H, F, Br, I, OH, OR1, NH2, NHR', NR’2, CO2R\ CONH2, CONHR', CONR'i, CH-CHCChH, or CH^HCOaR', with the proviso that when R10 is OH and R11 is notNH2; 20 wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R’ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z is N or CR12; and R12 is an H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, NO2, 25 lower alkyl of Ci-Ce, COaR’, CONH2, CONHR’, CONR‘2, CH=CHCO2H, or CH=CHCO2R'.

An eleventh aspect of the third embodiment is directed to a compound represented by formula 1-6 wherein 2983472-1 -63- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 (a) Rl is hydrogen, methyl, ethyl, «-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-ch loro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; (c) R3a is H and R3b is H, CH3) CH(CH3)2, CH2CH(CH3)2, 5 CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, 10 cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yI, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; (e) R5 is H, CN, CH3, OCH3, CH2OH, CH2F, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot 15 beH; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OCH3, Cl, Br, I, NH2, or N3; (h) Y is OH, H, CH3, vinyl, NH2, N3, CN, Cl, Br, F, I, OC(O)CH3, OCH3; 20 (i) R10 and R11 are independently H, F, Br, I, OH, OR', NH2,NHR', NR'2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH^HCCfeR’, with the proviso that when R10 is OH and R11 is not NH2; wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R* comprise at least one C atom that 25 are joined to form a heterocycle comprising at least two carbon atoms; and 0) Z is N or CR12; and 2983472-1 -64- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 R12 is an H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, NO2, lower alkyl of Ci-C6, CO2R', CONH2, CONHR', CONR’2> CH=CHCO2H, or CH=CHCO2R'. 5 A twelvth aspect of the third embodiment is directed to a compound represented by formula 1-6 . wherein (a) R1 is hydrogen, methyl, ethyl, Λ-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 10 (b) R2 is hydrogen or CH3; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N- 15 methyl-azetidin-3-yI, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; (e) R5 is H, CN, CH2F, F, Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, R3 cannot be H; 20 (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, F, OCH3, F, Cl, Br, I, NH2 or N3; (h) Y is H, OH, CH3, F, Cl, Br, I, NH2 or N3, OCH3, or OC(O)CH3; (i) R10 and R11 are independently H, F, Br, 1, OH, OR', NH2, NHR', NR’2, CO2R', C0NH2, CONHR', CONR'2, CHCHCOiH, or CH-CHCO2R', with the proviso that when R10 is OH and R11 is not NH2; 25 wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 2983472-1 -65- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 0) Z isN orCR12; and R12 is a H, halogen (including F, Cl, Br, 1), OR', NH2, NHR', NR'2) NO2, lower alkyl of Ci-Q, CO2R', CONH2) CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'. 5 A thirteenth aspect of the third embodiment is directed to a compound represented by formula 1-6 wherein (a) R1 is hydrogen, methyl, ethyl, «-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 10 (b) R2 is hydrogen; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, fPr, MPr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N- 15 methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyi)amino-lower alkyl; (e) R5 is H, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; 20 (g) X is H, OH, OCH3, F, NH2 or N3; (h) Y is OH, NH2, OCH3, or 0C(O)CH3; (i) Rt0 and R11 are independently H, F, Br, I, OH, OR', NH2, NHR', NR'2> CO2R’, CONH2, CONHR’, CONR'2, CHCHCChH, or CHCHCChR’, with the proviso that when R10 is OH and Ru is not NH2; 2983472-1 -66- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R’ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z is N or CR12; and 5 R*2 is an H, halogen (including F, Cl, Br, I), OR*, NH2, NHR', NR'2, NO2, lower alkyl of CrC6, CO2R’, CONH2, CONHR', CONR’2) CH=CHCO2H, or CH=CHCO2R'. A fourteenth aspect of the third embodiment is directed to a compound represented by formula 1-6 10 wherein (a) R1 is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, 15 CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, yPr, nPr, ftBu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azeti din-3-yl, N-methyI-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 20 (e) R5 is H, with the provisos that when X is OH, R6 is CH3 or CH2F,

Rs cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, OCH3, F, NH2 or N3; (h) Y is OH, NH2, OCH3, or OC(0)CH3; 2983472-1 -67- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 (i) R10 and R11 are independently H, F, Br, 1, OH, OR', NH2, NHR', NR’2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R', with the proviso that when R10 is OH and R11 is not NH2; wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or 5 alternatively, in the instance of NR’2, each R* comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z is N or CR12; and R12 is an H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, NO2, lower alkyl of CrC6, CO2R', CONH2, CONHR', CONR’2, CH=CHCO2H, or 10 CH=CHCO2R'. A fifteenth aspect of the third embodiment is directed to a compound represented by formula 1-6 wherein (a) R1 is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which 15 includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of C^ alkyl, C2.e alkenyl, C2-e alkynyl, Ci_6 alkoxy, F, Cl, Br, I, nitro, cyano, Cw haloalkyl, -N(Rr)2, C|^ acylamino, -NHSO2Ci_6 alkyl, -SO2N(R‘')2, COR1’, and -SO2C^ alkyl; (R1' is independently hydrogen or alkyl, which includes, but is not limited to, C|.2o alkyl, Cmo alkyl, 20 or C,^ alkyl, Rr is -OR' or -N(Rl')2); (b) R2 is hydrogen or CH3; (c) R3a and R3b are (i) independently selected from hydrogen, Cmo alkyl, cycloalkyl, -(CH2)c(NR3')2, C].6 hydroxyalkyl, -CH2SH, -(CH2)2S(O)aMe, -(CH2)3NHC(=NH)NH2, (lH-indol-3-yl)methyl, (lH-imidazol-4-yl)methyl, - 25 (CH2)cCOR3', aryl and aryl Cj-3 alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Cmo alkyl, C1-0 alkoxy, halogen, nitro and cyano; (ii) R3a and R3b both are Cj^ alkyl; (iii) R3a and R3b together are(CH2)f so as to form a spiro ring; (iv) R3a is hydrogen and R3b and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms (v) R3b is 2983472-1 -68- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 hydrogen and R30 and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3’ is independently hydrogen or Cm alkyl and R3’ is -OR’ or -N(R3’)2); (vi) R3a is H and R3b is H, CH3, CH2CFI3, CH(CH3)2, 5 CH2CH(CH3)2, CH(CH3)CH2CH3i CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2j CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2) -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH20H, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3a is CH3, -CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, 10 CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, ch2-itnidazol-4-yl, CH2OH, CH(0H)CH3, CH2((4’-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H, where R3’ is independently hydrogen or alkyl, which includes, but is not limited to, C].2o alkyl, Cmo alkyl, or Cm alkyl, R3 is -OR' or 15 -N(R3’)2); (d) R4 is hydrogen, Cmo alkyl, Cmo alkyl optionally substituted with a lower alkyl, alkoxy or halogen, Cmo haloalkyl, C3.io cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted 20 heteroaryl;

(e) R5 is H, a lower alkyl, CN, vinyl, 0-(lower alkyl), hydroxyl lower alkyl, i.e., -(CH2)POH, where p is 1 -6, including hydroxyl methyl (CH2OH), CH2F, N3, CH2CN, CH2NH2, CH2NHCH3, CH2N(CH3)2j alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X 25 is OH, base is cytosine and R6 is H, R5 cannot be N3 and when X is OH, R6 is CH3 or CH2F and B is a purine base, R5 cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OMe, halogen, NH2, or N3; (h) Y is OH, H, CM alkyl, C24 alkenyl, C2^ alkynyl, vinyl, N3, CN, 30 Cl, Br, F, 1, NO2, OC(O)O(CM alkyl), 0C(0)0(Cm alkyl), 0C(0)0(C24 alkynyl), 0C(0)0(Qm alkenyl), OCmo haloalkyl, O(aminoacyl), 0(Cmo acyl), 2983472-1 -69- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 O(CM alkyl), O(C24 alkenyl), S(Cm acyl), S(Cm alkyl), S(C24 alkynyl), S(C24 alkenyl), SO(CM acyl), SO(CM alkyl), S0(C24 alkynyl), S0(C24 alkenyl), SO2(CM acyl), SO2(CM alkyl), SO2(C24 alkynyl), SO2(C24 alkenyl), OS(O)2(Cj. 4 acyl), OS(O)2(Cm alkyl), OS(O)2(C24 alkenyl), NH2, NH(Cm alkyl), NH(C24 5 alkenyl), NH(C24 alkynyl), NH(Cj4 acyl), N(Cm alkyl)2, N(Ct.ig acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F, I), NO2, C(O)O(Cm alkyl), C(O)O(Ci4 alkyl), C(0)0(C24 alkynyl), C(0)0(C24 alkenyl), O(CM acyl), O(CM alkyl), 0(C24 alkenyl), S(Cj4 acyl), S(CM alkyl), S(C2-4 alkynyl), S(C24 alkenyl), SO(Cm 10 acyl), SO(C14 alkyl), S0(C24 alkynyl), SO(C24 alkenyl), S02(C14 acyl), SO2(Cm alkyl), SO2(C24 alkynyl), SO2(C24 alkenyl), OS(O)2(C!4 acyl), OS(O)2(CM alkyl), OS(O)2(C24 alkenyl), NH2, NH(Cm alkyl), NH(C24 alkenyl), NH(C24 alkynyl), NH(Ci4 acyl), N(Cr alkyl^, N(C)4 acyl)2; (i) R10 is NH2 and R11 is H, F, Br, I, OH, OR*, NH2, NHR’, NR’2, 15 CO2R', CONH2, CONHR’, CONR’2, CH=CHCO2H, or CH=CHCO2R’; wherein R* is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR’2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and (j) ZisNorCRl2;and 20 R12 is an H, halogen (including F, Cl, Br, I), OR', NH2. NHR', NR'2, NO2, lower alkyl of C,-C6> CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R’.

An sixteenth aspect of the third embodiment is directed to a compound represented by formula 1-6 25 wherein (a) R1 is hydrogen, methyl, ethyl, n-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; 2983472-1 -70- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/OS8183 (c) R3’ is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2> CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2> CH2CH2COOH, CH2CH2C(O)NH2> ch2ch2ch2ch2nh2) -CHjCHjCHaNHCfNHJNH* CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'- 5 OH)-Ph), CH2SH, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, (Pr, ”Pr, rtBu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 10 (e) R5 is H, CN, CH3, OCH3, CH2OH, CH2F, halogen, including F,

Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, R3 cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; 15 (g) X is H, OH, F, OCH3, Cl, Br, I, NH2, or N3; (h) Y is OH, H, CH3, vinyl, NH2, N3, CN, Cl, Br, F, I, OC(O)CH3, OCH3; (i) R10 is NH2 and R11 is H, F, Br, 1, OH, OR', NH2, NHR', NR’2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'; wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or 20 alternatively, in the instance of NR'2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z is N or CR12; and R12 is an H, halogen (including F, Cl, Br, I), OR’, NH2, NHR’, NR’2, NO2, lower alkyl of Cj-Ce, CO2R', CONH2, CONHR', CONR’2, CH-CHCO2H, or 25 CH=CHCO2R'. A seventeenth aspect of the third embodiment is directed to a compound represented by formula 1-6 2983472-1 -71 - PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 wherein (a) R1 is hydrogen, methyl, ethyl, «-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; 5 (c) R5,isHandR3bisH,CH3,CH(CH3)2,CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, zBu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yI, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N- 10 methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; (e) R5 is H, CN, CH2F, F, Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H; ω R6 is H, CH3, CH2F, CHF2, CF3i or F; (g) X is H, OH, F, OCH3l F, CI, Br, I, NH2 orN3; 15 (h) Y is H, OH, CH3, F, Cl, Br, I, NH2 or N3, OCH3, or OC(O)CH3; (i) R10 is NH2 and R1' is H, F, Br, I, OH, OR', NH2, NHR', NR'2, CO2R’, CONH2, CONHR’, CONR’2, CHCHCOzH, or CH=CHCO2R'; wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R' comprise at least one C atom that 20 are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z isN or CR12; and R12 is an H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2) NO2, lower alkyl of CrC6, CO2R', CONH2, CONHR’, CONR'2, CH=CHCO2H, or CH=CHCO2R'. 25 An eighteenth aspect of the third embodiment is directed to a compound represented by formula 1-6 2983472-1 -72- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 wherein (a) R1 is hydrogen, methyl, ethyl, η-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen; 5 (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, ”Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N- 10 methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; (e) Rs is H, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; 15 (g) X is H, OH, OCH3, F, NH2 or N3; (h) Y is OH, NH2, OCH3, or OC(O)CH3; (i) R10 is NH2 and R11 is H, F, Br, I, OH, OR’, NH2, NHR’, NR’2, CO2R’, CONH2, CONHR’, CONR’2, CH=CHCO2H, or CH=CHCO2R’; wherein R* is a lower alkyl, a lower cycloalkyl, or C(0)(lower alkyl) or alternatively, in the instance of NR’2, each R’ comprise at least one C atom that 20 are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z is N or CR12; and R12 is an H, halogen (including F, Cl, Br, 1), OR’, NH2, NHR’, NR’2, NO2, lower alkyl of C,-C6, CO2R’, CONH2, CONHR’, CONR’i, CH=CHCO2H, or CH=CHCO2R’. 25 A ninteenth aspect of the third embodiment is directed to a compound represented by formula 1-6 2983472-1 t73- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 wherein (a) R1 is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen; 5 (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, zPr, "Pr, ΛΒυ, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N- 10 methyl-piperidin-4-yl, lower haloalky 1, or di(lower alkyl)ami no-lower alkyl; (e) R5 is H, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H; 15 (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, OCH3, F, NH2 or N3; (h) Y is OH, NH2, OCH3, or OC(O)CH3; (i) R10 is NH2 and R11 are independently H, F, Br, I, OH, OR1, NH2, NHR', NR'2, CO2R*, CONH2, CONHR’, CONR’2, CH=CHCO2H, or CH=CHCO2R'; wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or 20 alternatively, in the instance of NR’2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z is N or CR12; and R12 is an H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR’2, NO2, lower alkyl of CrC6, CO2R*. CONH2, CONHR’, CONR’2, CH-CHCO2H, or 25 CH-CHCO2R'. 2983472-1 -74- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 A fourth embodiment of the invention is directed to a compound represented by formula I in which the base is a structure represented by formula c above, where R11 is H and R2, R3a, R3b, R4, R5, R6, X, and Y are defined in the

Summary of the Invention section above. 5 A first aspect of the fourth embodiment is directed to a compound represented by formula 1-7

1-7 10 wherein (a) R1 is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of Ci-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, Cm alkoxy, F, Cl, Br, I, nitro, cyano, Cm haloalkyl, -N(Rr)2, Cm acylamino, - 15 NHSO2Cm alkyl, -SO2N(Rr)2» COR1’, and -SO2Cm alkyl; (R* is independently hydrogen or alkyl, which includes, but is not limited to, C^o alkyl, Cwo alkyl, or Cm alkyl, R1" is -OR' or -N(Rr)2); (b) R2 is hydrogen or CH3; (c) R3® and R3b are (i) independently selected from hydrogen, Cwo 20 alkyl, cycloalkyl, -(CH2)c(NR3')2, Cm hydroxyalkyl, -CH2SH, -(CH2)2S(O)dMe, - (CH2)3NHC(=NH)NH2, (lH-indol-3-yl)methyl, (lH-imidazol-4-yl)methyl, -(CH2)eCOR3", aryl and aryl C1-3 alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Cwo alkyl, Cm alkoxy, halogen, nitro and 2983472-1 -75- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 cyano; (ii) R3’ and R3b both are C|^ alkyl; (iii) R3a and R3b together are(CH2)f so as to form a spiro ring; (iv) R3a is hydrogen and R3b and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms (v) R3b is hydrogen and R3a and R2 together are (CH2)n so as to form a cyclic ring that 5 includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3 is independently hydrogen or C]^ alkyl and R3" is -OR’ or -N(R3')2); (vi) R3a is H and R3b is H, CH3, CH2CH3> CH(CH3)2, - CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, 10 CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3a is CH3, -CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3i CH2Ph, CH2-indol-3-yl,-CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, ch2- 15 imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4’-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H, where R3’ is independently hydrogen or alkyl, which includes, but is not limited to, Ci.2o alkyl, Cmo alkyl, or Ci^ alkyl, R3 is -OR* or -N(R3)a); (d) R4 is hydrogen, Cmo alkyl, Cmo alkyl optionally substituted with 20 a lower alkyl, alkoxy or halogen, Cmo haloalkyl, C3.i0 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyI)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; (e) R5 is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower 25 alkyl, i.e., -(CH2)pOH, where p is 1 -6, including hydroxyl methyl (CH2OH), CH2F, N3, CH2CN, CHiNHa, CH2NHCH3, CH2N(CH3)2, alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R6 is H, R5 cannot be N3 and when X is OH, R6is CH2 or CH2F and B is a purine base, Rs cannot be H; 30 (f) R6isH,CH3,CH2F, CHF2,CF3,F,orCN; (g) X is H, OH, F, OMe, halogen, NH2, or N3; 2983472-1 -76- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.003 4WOU1 (h) Y is OH, H, CM alkyl, C2-4 alkenyl, C2^ alkynyl, vinyl, N3, CN, Cl, Br, F, I, NO2, OC(O)O(CM alkyl), 0C(O)0(CM alkyl), OC(O)O(CM alkynyl), OC(O)O(C2m alkenyl), OCmo haloalkyl, O(aminoacyl), O(Ci.)0 acyl), O(CM alkyl), O(C2.4 alkenyl), S(CM acyl), S(CM alkyl), S(C2-4 alkynyl), S(C2m 5 alkenyl), SO(CM acyl), SO(CM alkyl), SO(C2m alkynyl), SO(C2m alkenyl), SO2(CH acyl), SO2(CM alkyl), SO2(C2m alkynyl), SO2(C2m alkenyl), OS(O)2(Ci. 4 acyl), OS(O)2(CM alkyl), OS(O)2(C2-4 alkenyl), NH2, NH(CM alkyl), NH(C2-4 alkenyl), NH(C2m alkynyl), NH(Cm acyl), N(Cm alkyl)2, N(Ci.ie acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, 10 one to three halogen (Cl, Br, F, 1), NO2, C(O)O(Cm alkyl), C(O)O(Cm alkyl), C(O)O(C2-< alkynyl), C(O)O(C2.4 alkenyl), 0(Cm acyl), O(C)4 alkyl), O(C2m alkenyl), S(CM acyl), S(CM alkyl), S(C2.4 alkynyl), S(C2m alkenyl), SO(Cm acyl), SO(CM alkyl), S0(C24 alkynyl), SO(C2m alkenyl), S02(CM acyl), SOiCCm alkyl), SO2(C24 alkynyl), SO2(CW alkenyl), 0S(O)2(Ci4 acyl), 15 OS(O)2(CM alkyl), OS(O)2(CW alkenyl), NH2, NH(CM alkyl), NH(C24 alkenyl), NH(C2m alkynyl), NH(Cm acyl), N(CM alkyl)2, N(C).4 acyl)2; (i) R10 is H, F, Cl, Br, I, OH, OR', SH, SR’, NH2, NHR’, NR'2, lower alkyl of Cj-C*, halogenated (F, Cl, Br, I) lower alkyl of Ci-C6, lower alkenyl of C2-Cfi, halogenated (F, Cl, Br, I) lower alkenyl of C2-Ce, lower alkynyl of C2-C6 20 such as OCH, halogenated (F, Cl, Br, 1) lower alkynyl of C2-C6, lower alkoxy of C)-C6, halogenated (F, CI, Br, I) lower alkoxy of Ci-Cg, CO2H, COiR', CONH2, CONHR', CONR’2, CH-CHCO2H, or CH=CHCO2R(, wherein R‘ is an optionally substituted alkyl, which includes, but is not limited to, an optionally substituted C).2o alkyl, an optionally substituted Cmo 25 alkyl, an optionally substituted lower alkyl; an optionally substituted cycloalkyl; an optionally substituted alkynyl of C2-Ce, an optionally substituted lower alkenyl of C2-Ce, or optionally substituted acyl, which includes but is not limited to C(O) alkyl, C(O)(Ci.20 alkyl), C(0)(Cmo alkyl), or C(O)(lower alkyl) or alternatively, in the instance of NR’2, each R' comprise at least one C atom that 30 are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z is N or CR12; and 2983472-1 -77- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 R12 is H, halogen (including F, Cl, Br, I), OH, OR', SH, SR', NH2, NHR', NR'2, NO2 lower alkyl of CpCe, halogenated (F, Cl, Br, Ϊ) lower alkyl of Ci-C6, lower alkenyl of C2-Cfi, halogenated (F, Cl, Br, I) lower alkenyl of C2-C6, lower alkynyl of C2-C6, halogenated (F, Cl, Br, I) lower alkynyl of C2-C6, lower alkoxy 5 of CrCfi, halogenated (F, Cl, Br, I) lower alkoxy of Ci-Ce, CO2H, CChR', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'; with the proviso that R12 is not a: (i) -C=C-H, (ii) -C=CH2, or (iii) -NO2. A second aspect of the fourth embodiment is directed to a compound represented by formula 1-7 10 wherein (a) Rl is hydrogen, methyl, ethyl, «-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; (c) R3tt is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, 15 CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-y 1, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, rtPr, nBu, 2-butyl, *Bu, benzyl, 20 cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N- methyl-azetidin-3-yl, N-methyl-pyrrol idin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; (e) R5 is H, CN, CH3, OCH3, CH2OH, CH2F, halogen, including F,

Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot 25 be H. (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OCH3, halogen, NH2, or N3; 2983472-1 -78- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 (h) Y is OH, H, CH3, vinyl, NH2> N3, CN, Cl, Br, F, 1, OC(O)CH3, OCH3; (i) R10 is H, F, Br, I, OH, OR', NH2, NHR’, NR’2, CO2R', CONH2, CONHR’, CONR'2) CH=CHCO2H, or CH=CHCO2R’, 5 wherein R' is a lower alkyl, a lower cycloalkyl, or C(0)(lower alkyl) or alternatively, in the instance of NR’2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z is N or CR12; and R12 is H, halogen (including F, Cl, Br, I), OR', NH2, NHR1, NR'2, NO2, 10 lower alkyl of CpC6, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH-CHCO2R'; with the proviso that R12 is not a: (i) -C=C-H, (ii) -C=CH2, or (iii) -NO2. A third aspect of the third embodiment is directed to a compound represented by formula 1-7 15 wherein (a) R* is hydrogen, methyl, ethyl, n-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, 20 CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, (Pr, "Pr, ”Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yi, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrroIidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)ami no-lower alkyl; 25 (e) R5 is H, CN, CH2F, F, Cl, Br, or I; with the proviso that X is OH, R6 is CH3 or CH2F, R5 cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; 2983472-1 -79- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1. (g) X is H, OH, F, OCHj, F, Cl, Br, I, NH2 or N3; (h) Y is H, OH, CH3, F, Cl, Br, I, NH2 or N3, OCH3, or OC(O)CH3; (i) R10 is H, F, Br, I, OH, OR’, NH2, NHR', NR'2, CO2R', CONH2, CONHR’, CONR'2, CH-CHCO2H, or CH=CHCO2R't 5 wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 0) Z is N or CR12; and R12 is H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, NO2, 10 lower alkyl of CrC6, CO2R', CONH2, CONHR', CONR'2, CHCHCOaH, or CH=CHCO2R'; with the proviso that R12 is not a: (i) -C-C-H, (ii) -C=CH2, or (iii) -NO2. A fourth aspect of the fourth embodiment is directed to a compound represented by formula 1-7 15 wherein (a) R1 is hydrogen, methyl, ethyl, n-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen; (c) R34 is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, 20 CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, ”Bu, 2-butyl, *Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 25 (e) R5 is H, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H; 2983472-1 -80- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, OCH3, F, NH2 or N3; (h) Y is OH, NH2, OCH3, or OC(O)CH3; (i) R10 and R11 H, F, Br, I, OH, OR’, NH2, NHR', NR'2, CO2R', 5 CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R', wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and (j) ZisNorCR12;and 10 R12 is an H, halogen (including F, Cl, Br, I), OR’, NH2, NHR', NR'2, NO2, lower alkyl of CrC6, CO2R', CONH2, CONHR’, CONR'2, CH=CHCO2H, or CH=CHCO2R’; with the proviso that R12 is not a: (i) -C=C-H, (ii) -C=CH2, or (iii) -NO2. A fifth aspect of the fourth embodiment is directed to a compound 15 represented by formula 1-7 wherein (a) R1 is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen; 20 (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Εζ 'Pr, ”Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N- 25 methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-Iower alkyl; 2983472-1 -81- WO 2008/121634 ‘ Docket No. 60137.0034WOU1 PCT/US2008/058183 (e) R5 is H, with the provisos that when X is OH, R° is CH3 or CH2F, R5 cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, OCH3) F, NH2 or N3; (h) Y is OH, NH2, OCH3, or OC(O)CH3; (i) Ru is H, F, Br, I, OH, OR’, NH2, NHR', NR’2, CO2R', CONH2, CONHR', CONR’2, CH=CHCO2H, or CH=CHCO2R’, wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R' comprise at least one C atom that 10 are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z is N or CR12; and R12 is H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, NO2, lower alkyl of Ci-C6, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R’. 15 A sixth aspect of the fourth embodiment is directed to a compound represented by formula 1-8

1-8 wherein 2983472-1 -82- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.003 4WOU1 (a) R1 is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of Ci-g alkyl, C2.e alkenyl, C2-6 alkynyi,

Cm alkoxy, F, Cl, Br, I, nitro, cyano, Cm haloalkyl, -N(Rr)2, Cw acylamino, - 5 NHSO2C1.6 alkyl, -SO2N(Rr)2, COR1", and -SO2Cm alkyl; (R1 is independently hydrogen or alkyl, which includes, but is not limited to, C1.20 alkyl, Cmg alkyl, or Ci-6 alkyl, R1’ is -OR’ or -N(Rl )2); (b) R2 is hydrogen or CH3; (c) R3fl and R3b are (i) independently selected from hydrogen, Cmo 10 alkyl, cycloalkyl, -(CH2)c(NR3')2, Cm hydroxyalkyl, -CH2SH, -(CH2)2S(O)dMe, -(CH2)3NHC(=NH)NH2, (lH-indol-3-yl)methyl, (lH-imidazol-4-yl)methyl, -(CH2)eCOR3", aryl and aryl Ci-3 alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Cmo alkyl, Ci^ alkoxy, halogen, nitro and cyano; (ii) R3a and R3b both are Cu alkyl; (iii) R3a and R3b together are(CH2)r so 15 as to form a spiro ring; (iv) R3a is hydrogen and R3b and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms (v) R3b is hydrogen and R3a and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3’ is independently hydrogen or Cj.6 alkyl and 20 R3’ is -OR* or -N(R3 j2); (vi) R3a is H and R3b is H, CH3, CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4’-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) 25 R3a is CH3, -CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, ch2-itnidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H, where R3 is independently hydrogen or alkyl, which 30 includes, but is not limited to, Cj.2o alkyl, Cmo alkyl, or C1-6 alkyl, R3" is -OR* or -N(R3’)2); 2983472-1 -83- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 (d) R4 is hydrogen, Cmo alkyl, Cmo alkyl optionally substituted with a lower alkyl, alkoxy or halogen, Cmo haloalkyl, ¢3.10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-tower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted 5 heteroaryl; (e) R5 is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., -(CH2)POH, where p is 1 -6, including hydroxyl methyl (CH2OH),

CH2F, N3, CH2CN, CH2NH2, CH2NHCH3, CH2N(CH3)2, alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X 10 is OH, base is cytosine and R6 is H, R5 cannot be N3 and when X is OH, R6 is CH3 or CH2F and B is a purine base, R5 cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OMe, halogen, NH2, or N3; (h) Y is OH, H, CM alkyl, C2Jt alkenyl, Cm alkynyl, vinyl, N3, CN,

15 Cl, Br, F, I, NO2, OC(O)O(CM alkyl), OC(O)O(Cm alkynyl), OC(O)O(C2M alkenyl), OCmo haloalkyl, O(aminoacyl), 0(Cmo acyl), 0(Cm alkyl), O(C2-4 alkenyl), S(Cm acyl), S(Cm alkyl), S(Cm alkynyl), S(C2m alkenyl), SO(CM acyl), SO(CM alkyl), SO(Cm alkynyl), SO(Cm alkenyl), SO2(Cm acyl), SO2(CM alkyl), SO2(CW alkynyl), S02(Cm alkenyl), OS(O)2(CM acyl), 20 OS(O)2(Cm alkyl), 0S(0)2(Cm alkenyl), NH2, NH(CM alkyl), NH(C2-4 alkenyl), NH(Cm alkynyl), NH(CM acyl), N(Cm alkyl)2, N(Cms acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F, I), NO2, C(O)O(Cm alkyl), C(O)O(Cm alkyl), C(0)0(C2-4 alkynyl), C(O)O(Cm alkenyl), 0(Cm acyl), 0(Cm alkyl), 0(Cm 25 alkenyl), S(Cm acyl), S(Cm alkyl), S(Cm alkynyl), S(Cm alkenyl), SO(CM acyl), S0(Cm alkyl), S0(Cm alkynyl), S0(Cm alkenyl), S02(Cm acyl), SO2(CM alkyl), SO2(C2-4 alkynyl), SO2(Cm alkenyl), 0S(0)2(Cm acyl), OS(O)2(CM alkyl), OS^MCm alkenyl), NH2, NH(CM alkyl), NH(Cm alkenyl), NH(Cm alkynyl), NH(CM acyl), N(Cm alkyl)2, N(CM acyl)2; 30 (i) R10 is H, F, Br, I, OH, OR', NH,, NHR', NR'2, COjR'. CONHa, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R', 2983472-1 -84- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 wherein R' is a lower alkyl, a lower cycloalkyl, or C(0)(lower alkyl) or alternatively, in the instance of NR'2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z isNorCR12; and 5 R12 is H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, NO2, lower alkyl of CrC6, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'; with the proviso that when base is represented by the structure c with R11 being hydrogen, R12 is not a: (i) -C=C-H, (ii) -O=CH2, or (Hi) -NO2. A seventh aspect of the fourth embodiment is directed to a compound 10 represented by formula 1-8 wherein (a) R1 is hydrogen, methyl, ethyl, «-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; 15 (c) R38 is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indoi-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazoi-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; 20 (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; (e) R5 is H, CN, CH3, OCH3, CH2OH, CH2F, halogen, including F, 25 Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot beH; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; 2983472-1 -85- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.003 4WOU1 (g) X is H, OH, F, OCH3, halogen, NH2, or N3; (h) Y is OH, H, CH3, vinyl, NH2, N3, CN, Cl, Br, F, I, OC(O)CH3, OCH3; (i) R'° is H, F, Br, I, OH, OR', NH2, NHR', NR'2, CO2R’, CONH2, 5 CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R’, wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z is N or CR12; and 10 R12 is an H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, NO2, lower alkyl of CrC6, CO2R’, CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R’; with the proviso that R12 is not a: (i) -C=C-H, (ii) -C=CH2, or (iii) -NO2.

An eighth aspect of the fourth embodiment is directed to a compound 15 represented by formula 1-8 wherein (a) R* is hydrogen, methyl, ethyl, n-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; 20 (c) R38 is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyI, 'flu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N- 25 methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; (e) R5 is H, CN, CH2F, F, Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, Rs cannot be H; 2983472-1 -86- PCT/US2008/058I83 WO 2008/121634

Docket No. 60137.0034WOU I (f) R6 is H, CH3> CH2F, CHF2, CF3, or F; (g) X is H, OH, F, OCHj, F, Cl, Br, I, NH2 or N3; (h) Y is H, OH, CH3, F, Cl, Br, 1, NH2 or N3, OCH3, or OC(O)CH3; (i) R'° is H, F, Br, I, OH, OR’, NH2, NHR’, NR’j, CO2R’, CONH2, 5 CONHR’, CONR’2, CH=CHCO2H, or CH=CHCO2R’, wherein R’ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR*2, each R’ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z is N or CR12; and 10 R12 is an H, halogen (including F, Cl, Br, 1), OR', NH2, NHR', NR'i, NO2, lower alkyl ofCi-Ce, CChR', CONH2, CONHR’, CONR'2, CH-CHCO2H, or CH=CHCO2R’; with the proviso that RJ2 is not a: (i) -C=C-H, (ii) -C=CH2, or (iii)-NOz. A ninth aspect of the fourth embodiment is directed to a compound 15 represented by formula 1-8 wherein (a) R1 is hydrogen, methyl, ethyl, «-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen; 20 (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CHaPh, or lower cycloalkyt; (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N- 25 methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-Iower alkyl; 2983472-1 -87- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 (e) R5 is H, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H; (i) R6 is H, CH3, CH2F} CHF2, CF3, or F; (g) X is H, OH, OCH3, F, NH2 or N3; (h) Y is OH, NH2, OCH3, or OC(O)CH3; (i) R10 is H, F, Br, I, OH, OR’, NH2, NHR', NR’2, CO2R’, CONH2, CONHR’, CONR’2, CH=CHCO2H, or CH=CHCO2R’, wherein R’ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR’2, each R’ comprise at least one C atom that 10 are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z is N or CR12; and R12 is an H, halogen (including F, Cl, Br, I), OR’, NH2, NHR’, NR’2, NO2, lower alkyl of Ci-Ce, CO2R’, CONH2, CONHR’, CONR’z, CH=CHCO2H, or CH=CHCO2R’; with the proviso that R12 is not a: (i) -C=C-H, (ii) -C~CH2, or 15 (iii)-NO2. A tenth aspect of the fourth embodiment is directed to a compound represented by formula 1-8 wherein (a) R1 is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-20 phenyl, p-fluorophenyl; (b) R2 is hydrogen; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, 25 cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N- 2983472-1 -88- PCT/US2008/058183 WO 2008/121634

Docket No. 6O137.0O34WOU1 methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N- methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; (e) R5 is H, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H; 5 (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, OCH3, F, NH2 or N3; (h) Y is OH, NH2, OCH3, or OC(O)CH3; (i) R10 is H, F, Br, 1, OH, OR', NH2, NHR', NR'2> CO2R\ CONH2, CONHR', CONR'i, CH=CHCO2H, or CH=CHCO2R', 10 wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and (j) Z isN or CR12; and R12 is an H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, NO2, 15 lower alkyl of CrC6, CO2R\ CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'; with the proviso that R12 is not a: (i) -OC-H, (ii) -C-CH2, or (iii) -NO2. A fifth embodiment of the invention is directed to a compound represented by formula I in which the base is a structure represented by formula 20 d above, wherein R1, R2, R3n, R3b, R4, R5, R6, X, and Y are defined in the Summary of the Invention section above.

The first aspect of the fifth embodiment is directed to a compound represented by formula 1-9 2983472-1 -89- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WQU1

1-9 wherein (a) R* is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which 5 includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of Cm alkyl, C2.6 alkenyl, C2.6 alkynyl,

Ci-6 alkoxy, F, Cl, Br, I, nitro, cyano, Ci-6 haloalkyl, -N(Rr)2, Cm acylamino, -NHSO2Ci-6 alkyl, -SO2N(Rll)2, COR1", and -SO2Cm alkyl; (Rris independently hydrogen or alkyl, which includes, but is not limited to, C1-20 alkyl, Cmo alkyl, 10 or Cm alkyl, R1" is -OR' or -N(Rl >2); (b) R2 is hydrogen or CH3; (c) R3a and R3b are (i) independently selected from hydrogen, Cmo alkyl, cycloalkyl, -(CH2)c(NR3)2, C).6 hydroxyalkyl, -CH2SH, -(CH2)2S(O)dMe, -(CH2)3NHC(=NH)NH2, (lH-indol-3-yl)methyl, (lH-imidazoM-yl)methyl, - 15 (CH2)cCOR3", aryl and aryl Cm alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Cmo alkyl, Cm alkoxy, halogen, nitro and cyano; (ii) R3a and R3b both are Cm alkyl; (iii) R38 and R3b together are(CH2)f so as to form a spiro ring; (iv) R3a is hydrogen and R3b and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms (v) R3b is 20 hydrogen and R3a and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3' is independently hydrogen or Cm alkyl and R3" is -OR1 or -N(R3)2); (vi) R3a is H and R3b is H, CH3, CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, 2983472-1 -90- WO 2008/121634 PCT/US2008/058183

Docket No. 6013 7.0034WOU1 CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3a is CH3, -CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, 5 CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, ch2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4’-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H, where R3 is independently hydrogen or alkyl, which includes, but is not limited to, Ci-2o alkyl, Cmo alkyl, or Ci-g alkyl, R3 is -OR' or 10 -N(R3)2); (d) R4 is hydrogen, Cmo alkyl, Cmo alkyl optionally substituted with a lower alkyl, alkoxy or halogen, Cmo haloalkyl, C3.io cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted 15 heteroaryl; (e) R5 is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., -(CH2)POH, where p is 1 -6, including hydroxyl methyl (CH2OH),

CH2F, N3, CH2CN, CH2NH2, CH2NHCH3, CH2N(CH3)2, alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X 20 is OH, base is cytosine and R6 is H, R5 cannot be N3 and when X is OH, R6 is CH3 or CH2F and B is a purine base, R5 cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OMe, halogen, NH2, or N3; (h) Y is OH, H, Cm alkyl, C24 alkenyl, C24 alkynyl, vinyl, N3, CN, 25 Cl, Br, F, I, NOa, OC(O)O(CM alkyl), 0C(O)0(CM alkyl), 0C(0)0(C24 alkynyl), 0C(0)0(C24 alkenyl), OCmo haloalkyl, O(aminoacyl), 0(Cmo acyl), O(Cm alkyl), O(C24 alkenyl), S(Cm acyl), S(Cm alkyl), S(C24 alkynyl), S(C24 alkenyl), S0(Cj4 acyl), SO(Cj4 alkyl), SO(C24 alkynyl), S0(C24 alkenyl), SO2(Cm acyl), S02(CM alkyl), SO^Cm alkynyl), S02(C2-4 alkenyl), 0S(0)2(Cj. 30 4 acyl), OS(O)2(Cm alkyl), OS(O)2(C24 alkenyl), NH2,NH(Cm alkyl), NH(C24 alkenyl), NH(C24 alkynyl), NH(C14 acyl), N(Cm alkyl)2, N(Cms acyl)2, 2983472-1 -91- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F, I), NO2, C(O)O(Cm alkyl), C(O)O(Cu alkyl), C(O)O(C2-4 alkynyl), C(O)O(C2-4 alkenyl), O(Ci.4 acyl), O(CM alkyl), O(C2u»

alkenyl), S(CM acyl), S(CM alkyl), S(C2-4 alkynyl), S(C2-4 alkenyl), SO(CM 5 acyl), SO(CM alkyl), SO(CW alkynyl), SO(C2-4 alkenyl), SO2(CM acyl), SO/Cm alkyl), SO2(C2^ alkynyl), SO2(C2^ alkenyl), OS(O)2(Cw acyl), OS(0)2(CM alkyl), OS(O)2(CW alkenyl), NH2, NH(CM alkyl), NH(C2-4 alkenyl), NH(C2^ alkynyl), NH(C|^ acyl), N(Cm alkyl)2, N(Cm acyl)2. A second aspect of the fifth embodiment is directed to a compound 10 represented by formula 1-9 wherein (a) Rl is hydrogen, methyl, ethyl, «-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; 15 (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CHrindol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4’-OH)-Ph), CH2SH, or lower cycloalkyl; 20 (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, ”Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(Iower alkyl)amino-lower alkyl; (e) R5 is H, CN, CH3, OCH3, CH2OH, CH2F, halogen, including F, 25 Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot beH. (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) . X is H, OH, F,OCH3, halogen, NH2, or N3; 2983472-1 -92- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 (h) Y is OH, H, CH3, vinyl, NH2> N3, CN, CI, Br, F, I, OC(O)CH3, OCH3; A third aspect of the fifth embodiment is directed to a compound represented by formula 1-9 5 wherein (a) R1 is hydrogen, methyl, ethyl, n-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, 10 CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyI-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 15 (e) R5 is H, CN, CH2F, F, Cl, Br, or I; with the proviso that X is OH, R6 is CH3 or CH2F, R5 cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, F, OCH3, F, Cl, Br, I, NH2orN3; (h) Y is H, OH, CH3, F, Cl, Br, I, NH2 N3, OCH3, or OC(O)CH3; 20 A fourth aspect of the fifth embodiment is directed to a compound represented by formula 1-9 wherein (a) R1 is hydrogen, methyl, ethyl, Λ-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 25 (b) R2 is hydrogen; 2983472-1 -93- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 (c) R3fl is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, flPr, rtBu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N- 5 methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; (e) R5 is H, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H; 10 (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, OCH3, F, NH2 or N3; (h) Y is OH, NH2, OCH3, or OC(O)CH3; A fifth aspect of the fifth embodiment is directed to a compound represented by formula 1-9 wherein 15 (a) R1 is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro- . phenyl, p-fluorophenyl; (b) R2 is hydrogen; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; 20 (d) R4 is hydrogen, CH3, Et, 'Pr, nPr, "Bu, 2-butyl, fBu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; (e) R5 is H, with the provisos that when X is OH, R6 is CH3 or CH2F, 25 R5 cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; 2983472-1 -94- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU 1 (g) X is H, OH, OCH3, F, NH2 or N3; (h) Y is OH, NH2, OCH3, or OC(O)CH3; A sixth aspect of the fifth embodiment is directed to a compound represented by formula 1-10

HO wherein (a) R1 is hydrogen, methyl, ethyl, n-propyl, /-propyl, or a substituted or unsubstituted phenyl, where the substitutent of the substituted phenyl is at 10 least one of a CH3, OCH3, F, Cl, Br, 1, nitro, cyano, and a CH3^Xq, where X is F,

Cl, Br, or I, and q is 1-3; (b) R2 is hydrogen or CH3; (c) R3b is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, 15 CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, - CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl or R3a is CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, - 20 CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H; 2983472-1 -95- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, fBu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-y I, N- methyl-azetidin-3-yI, N-methyl-pyrrol i di n-3-yl, N-methyl-pyrrolidin-4-yl, N- methyl-piperidin-4-yl, lower haloalky 1, or di(lower alkyl)amino-lower alkyl; 5 (e) R5 is H, CN, CH3, OCH3, CH2OH, CH2F, N3, CH2CN, CH2N3, CH2NH2, CH2NHCH3, CH2N(CH3)2, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OCH3, Cl, Br, I, NH2, or N3; 10 (h) Y is OH, H, CH3, vinyl, N3, CN, Cl, Br, F, I, OC(O)CH3, OCH3, NH2, NHCH3, NH(vinyl), NH(acetyl), NH(C(O)CH3), N(CH3)2, N(C(O)CH3)2; A seventh aspect of the fifth embodiment is directed to a compound represented by formula 1-10 wherein 15 (a) R1 is hydrogen, methyl, ethyl, n-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-ch loro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, 20 CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, - CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4*-OH)-Ph), CH2SH, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Εζ zPr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N- 25 methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N- methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl;

29S3472-I -96- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 (e) R5 is H, CN, CH3, OCH3, CH2OH, CH2F, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, Rs cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, F, or CN; (g) X is H, OH, F, OCH3, CI, Br, I, NH2, or N3; and (h) Y is OH, H, CH3, vinyl, NH2, N3, CN, Cl, Br, F, I, OC(O)CH3, OCH3.

An eighth aspect of the fifth embodiment is directed to a compound represented by formula 1-10 10 wherein (a) R1 is hydrogen, methyl, ethyl, «-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; (b) R2 is hydrogen or CH3; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, 15 CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, ”Pr, ”Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yI, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-Iower alkyl;

20 (e) R5 is H, CN, CH2F, F, Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, Rs cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, F, OCH3, F, Cl, Br, 1, NH2 or N3; (h) Y is H, OH, CH3, F, Cl, Br, I, NH2 or N3, OCH3, or OC(O)CH3; 25 A ninth aspect of the fifth embodiment is directed to a compound 2983472-1 -97- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 represented by formula 1-10 wherein (a) R1 is hydrogen, methyl, ethyl, «-propyl, /-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 5 (b) R2 is hydrogen; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, rtBu, 2-butyl, fBu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N- 10 methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(loweralkyl)amino-lower alkyl; (e) R5 is H, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H; 15 (f) Rfi is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, OCH3, F, NH2 or N3; (h) Y is OH, NH2, OCH3s or OC(O)CH3; A tenth aspect of the fifth embodiment is directed to a compound represented by formula Ϊ-10 wherein 20 (a) R1 is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro- phenyl, p-fluorophenyl; (b) R2 is hydrogen; (c) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; .2983472-1 -98- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 (d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 5 (e) R5 is H, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H; (f) R6 is H, CH3, CH2F, CHF2, CF3, or F; (g) X is H, OH, OCH3, F, NH2 or N3; (h) Y is OH, NH2, OCH3, or OC(O)CH3. 10 The following tables contain numeric identifiers associated with various substituent designators that should be viewed in light of the accompanying structure. These structures are contemplated species of the various aspects of the disclosed embodiments and are not intended to be limiting on full breadth of the contemplated compound represented by the structure of formula I. However, it 15 is contemplated that any one of the exemplified nucleoside bases can be used in combination with any one of contemplated species that specify a particular combination of R1, R2, R3a, R3b, R4, R5, R6, X, and Y. In each of the presented tables, the phosphoramidate substituent containing the substituents R3a and R3b are depicted without reference to stereochemical structure (cf. structures 1-1,1-3, 20 1-5,1-7, and 1-9 above). It is contemplated that the compounds recited below embody compounds in which R3a projects toward the viewer while R3b projects away from the viewer (cf. structures 1-2,1-4,1-6,1-8, and 1-10). Moreover, it is contemplated that the compounds recited below also embody compounds in which R3a projects away from the viewer while R3b projects towards the viewer. 25 Not meant to be limiting, however, it is contemplated that preferred compounds are those in which R3a projects towards the viewer and R3b projects away from the viewer such that the natural L-amino acid (S)-configuration is presented. Additionally, the inventors recognize that the phosphorus atom of the phosphoramidate moiety is another source of chirality. Although the structures 30 below do not specifically depict chirality at phosphorus, the inventors recognize that stereochemical configurations are possible such that in a staggered (or zig- 2983472-1 -99- WO 2008/121634

Docket No. 60137.0034WOU 1 PCT/US2008/058183

Ns R1 R3 r3« R5 R6 X Y Ί< R8 R* II-11-3 ch3 H H CH(CH3)2 Et H ch3 OH OH H H nh2 II-11-4 ch3 H H CH2CH(CH3)2 Et H ch3 OH OH H H nh2 II-11-5 ch3 H H CH2Ph Et H ch3 OH OH H H nh2 II-11-6 ch3 H H CH2-indot-3-yl Et H ch3 OH OH H H nh2 Π-11-7 ch3 H H CH2CH2SCH3 Et H ch3 OH OH' H H nh2 II-11-8 ch3 T73bTZ * H 4 Et H ch3 OH OH H H nh2 *Rzand Rejoined together by (Ctbbt0 fonn five-membered ring.

Table 11-12. R* R2 "R36 ir RJ R6 X Y R7 R8 r’ Π-12-1 Et H H H Et H ch3 OH OH H H nh2 II-12-2 Et H H ch3 Et H ch3 OH OH H H nh2 II-12-3 Et H H CHCCH^ Et H ch3 OH OH H H nh2 II-12-4 Et H H CH2CH(CH3)2 Et H ch3 OH OH H H nh2 II-12-5 Et H H CH2Ph Et H ch3 OH OH H H nh2 Π-12-6 Et H H CH2-indol-3-yl Et H ch3 OH OH H H nh2 II-12-7 Et H H CH2CH2SCH3 Et H ch3 OH OH H H nh2 U-12-8 Et * H * Et H ch3 OH OH H H nh2 *R7 and RJb joined together by (CH2)3 to form five-membered ring.

Table II-13. R1 R3 R* R4 R5 R6 X Y r" R8 Π-13-1 'W H Η Η Et H CH3 OH OH H H νη2 II-13-2 fPr H Η CH3 Et H ch3 OH OH H H νη2 II-13-3 fPr H Η CH(CH3)2 Et H ch3 OH OH H Η νη2 II-13-4 'Pr H Η CH2CH(CH3)2 Et H ch3 OH OH H H νη2 II-13-5 'Pr Η Η CH2Ph Et H ch3 OH OH H Η νη2 ΪΙ-13-6 Ψγ H Η CH2-indol-3-yl Et H ch3 OH OH H Η νη2 II-13-7 'Pr H Η ch2ch2sch3 Et H ch3 OH OH H Η νη2 II-13-8 ipr * Η * Et H ch3 OH OH H Η νη2 *R2andRJ0 joined together by (CH2)3 to form five-membered ring.

Table II-14.

Xs R ΊΓ R 3» R3t> R4 R3 Rfc X Y R7 R8 Rs ΙΙ-14-1 'Bu Η Η Η Et Η ch3 OH OH H H nh2 Π-14-2 zBu Η Η ch3 Et Η ch3 OH OH H H nh2 2983472-1 -105- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 zag) line structure the oxo-substitutent projects towards the viewer while the OR1 substituted projects away from the viewer, and vice versa, i.e., where the

Cahn-Ingold-Prelog stereochemical designation of phosphorous is either R or S.

Therefore, the structures below include all possible stereochemical 5 configurations possible for phosphorus.

II

Table Π-1.

Ks RJ R2 R3· R3b R4 Rs R4 X Y R’ R" Π-1-1 ch3 H H H ch3 H ch3 OH OH H H NH2 H-l-2 ch3 H H ch3 ch3 H ch3 OH OH H H nh2 H-l-3 ch3 H H CH(CH3)2 ch3 H ch3 OH OH H H nh2 II-1-4 ch3 H H CH2CH(CH3)2 ch3 H. ch3 OH OH H H nh2 H-l-5 ch3 H H CH2Ph ch3 H ch3 OH OH H H nh2 H-l-6 ch3 H H CH2-indol-3-yl ch3 H ch3 OH OH H H nh2 II-1-7 ch3 H H CH2CH2SCH3 ch3 H ch3 OH OH H H nh2 Π-1-8 ch3 ♦ H * ch3 H ch3 OH OH H H nh2 *R2 and RJb joined together by (CH2)3 to form five-membered ring. 10 Table II-2. — ——, . > ......- i· .w i — j- — *> — ·»τγ u" n "

Xs R R2 r3. R3b R4 R5 R6 X Y R' R“ Π-2-1 Et H H H ch3 H CH3 OH OH H H NH2 11-2-2 Et H H CH3 ch3 H ch3 OH OH H H nh2 II-2-3 Et H H CH(CH3)2 ch3 H ch3 OH OH H H nh2 H-2-4 Et H H CH2CH(CH3)2 ch3 H ch3 OH OH H H nh2 H-2-5 Et H H CH2Ph ch3 H ch3 OH OH H H nh2 Π-2-6 Et H H CH2-indol-3-yl ch3 H ch3 OH OH H H nh2 2983472-1 -100- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.003 4WOU1 "jfc R‘ R2 Rio R36 R4 R* R6 X Y R7 RB R9 11-2-7 Et Η H CH2CH2SCH3 CH3 H CH3 OH OH Η H NH2 II-2-8 Et * H * CH3 H CH3 OH OH Η H NH2 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table II-3.

Ns R1 R2 R3’ R3b R4 IF R6 X Y R7 Ru R9 II-3-1 'Pr H H H CH3 H ch3 OH OH H Η νη2 II-3-2 Tr H H ch3 ch3 H ch3 oh oh H Η νη2 11-3-3 'Pr H H CH(CH3)2 ch3 H ch3 oh oh H Η νη2 II-3-4 'Pr H H CH2CH(CH3)2 ch3 H ch3 oh oh Η Η νη2 ΪΙ-3-5 'Pr H H CH2Ph ch3 H ch3 oh oh Η Η νη2 11-3-6 'Pr H H CH2-indol-3-yl ch3 H ch3 oh oh Η Η νη2 11-3-7 'Pr H H CH2CH2SCH3 ch3 H ch3 oh oh Η Η νη2 II-3-8 'Pr * H * ch3 H ch3 oh oh Η Η νη2 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table II-4.

Ns R R5 R3’ R3” R4 ΊΓ R6 X Y R7 R“ R9 11-4-1 fBu H H Η CH3 H CH3 OH OH H H nh2 ΙΙ-4-2 'Bu Η H ch3 ch3 Η ch3 OH OH H H nh2 ΙΙ-4-3 *Bu H H CH(CH3)2 ch3 H ch3 OH OH H H nh2 ΙΙ-4-4 *Bu H H CH2CH(CH3)2 ch3 H ch3 OH OH H H nh2 ΙΙ-4-5 *Bu H H CH2Ph ch3 H ch3 OH OH H H nh2 11-4-6 *Bu H H CH2-indol-3-yI ch3 Η ch3 OH OH H H nh2 ΙΙ-4-7 'Bu H H CH2CH2SCH3 ch3 H ch3 OH OH H H nh2 ΙΙ-4-8 'Bu ♦ H * ch3 H ch3 OH OH H H nh2 5 *R2 and R30 joined together by (CH2)3 to form five-membered ring.

Table 11-5.

Ns R1 RJ R3b r! R6 X ' Y R R“ Rs II-5-1 Ph H H H CH3 H CH3 OH OH H H nh2 II-5-2 Ph Η H CH3 ch3 H ch3 OH OH H H nh2 ΙΪ-5-3 Ph H H CH(CH3}i ch3 Η ch3 OH OH H H nh2 ΪΙ-5-4 Ph H H CH2CH(CH3)2 ch3 H ch3 OH OH H H nh2 ΙΪ-5-5 Ph H H CH2Ph ch3 H ch3 OH OH H H nh2 II-5-6 Ph H H CHrindol-3-yl ch3 H ch3 OH OH H H nh2 II-5-7 Ph H H CH2CH2SCH3 ch3 H ch3 OH OH H H nh2 2983472-1 -101- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ns Rl R2 r3« R35 R4 RJ R6 X γ r R« R’ II-S-8 Ph * H * ch3 H ch3 OH OH H H nh2 ♦r2 and RJb joined together by (CH2)3 to form five-membered ring. Table II-6. Ns R1R3 ‘ R3b R4 RJ R6 X Y R7 r“ Ry II- p-Me- H H H ch3 H ch3 OH OH H H nh2 6-1 Ph II- p-Me- H H ch3 ch3 H ch3 OH OH H H nh2 6-2 Ph II- p-Me- H H CH(CH3)2 ch3 H ch3 OH OH H H nh2 6-3 Ph II- p-Me- H H CH2CH(CH3)2 ch3 H ch3 OH OH H H nh2 6-4 Ph II- p-Me- H H CH2Ph ch3 H ch3 OH OH H H nh2 6-5 Ph II- p-Me- H H CH2-indol-3- ch3 H ch3 OH OH H H nh2 6-6 Ph yi II- p-Me- H H ch2ch2sch3 ch3 H ch3 OH OH H H nh2 6-7 Ph II- p-Me- * H * ch3 H ch3 OH OH H H nh2 *R2 and R30 joined together by (CKfeb to form five-membered ring. .Table 11-7.

Ns R1 R4 r3. R3b R4 Rs R* X Y R’ R“ R5 II-7- p-F-1 Ph H H H ch3 H CH3 OH OH H H nh2 Π-7- p-F-2 Ph H Η ch3 ch3 H ch3 OH OH Η H nh2 II-7- p-F-3 Ph H H CH(CH3)2 ch3 H CH3 OH OH H H nh2 Π-7- p-F-4 Ph H H CH2CH(CH3)2 ch3 H ch3 OH OH H H nh2 II-7- p-F- H H CH2Ph . ch3 H ch3 OH OH H H NH2 6 Ph 2983472-1 -102- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Xs R1 R2 R3a "r35 r5- R6 X Y r“ R5* II-7- p-F- H H CH2-indol-3- ch3 H ch3 OH OH H H nh2 7 Ph yi Π-7- p-F- H H ch2ch2sch3 ch3 H ch3 OH OH H H nh2 8 Ph II-7- p-F- * H * ch3 H ch3 OH OH H H nh2 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table II-8.

Xfi "R1- R2 Ί?β “R36 ~R*“ Rs R6 X Y R’ R* II- p-Cl- Η Η Η CH3 H ch3 OH oh H H NH2 8-1 Ph II- p-Ct- Η Η ch3 ch3 Η ch3 oh OH H H nh2 8-2 Ph II- p-CI- Η Η CH(CH3)2 ch3 Η ch3 OH OH H H nh2 8-3 Ph II- p-Cl- Η Η CH2CH(CH3)2 ch3 Η ch3 OH OH H H nh2 8-4 Ph II- p-Cl- Η Η CH2Ph ch3 Η ch3 OH OH H H nh2 8-5 Ph II- p-Cl- Η Η CH2-indol-3- ch3 Η ch3 oh OH H H nh2 8-6 Ph yi II- p-Cl- Η Η CH2CH2SCH3 ch3 Η ch3 oh OH H H nh2 8-7 Ph II- p-Cl- * Η * ch3 Η ch3 oh OH H H nh2 *R2 and R3t> joined together by (CH2)3 to form five-membered ring.

Table II-9.

Xs Rl R2 R3b ΊΓ R6 X Y R7 R“ R9 II-9- p-Br- Η Η Η ch3 H ch3 OH OH Η Η νη2 1 Ph Π-9- p-Br- Η Η ch3 ch3 Η ch3 OH OH Η Η νη2 2 Ph II-9- p-Br- Η Η CH(CH3)2 ch3 H ch3 OH OH Η Η νη2 3 2983472-1 -103- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Ks R1 R2 R3a R% R3 R5" R6 X Ϋ R7 R8 Ry H-9- p-Br- H 4 Ph H CH2CH(CH3)2 ch3 H ch3 OH OH H H nh2 II-9- p-Br- H 6 Ph H CH2Ph ch3 H ch3 OH OH H H nh2 II-9- p-Br- H H CH2-indol-3- ch3 H ch3 OH OH H H nh2 7 Ph yi II-9- p-Br- H 8 Ph H ch2ch2sch3 ch3 H ch3 OH OH H H nh2 ΪΙ-9- p-Br- * 20 Ph H * ch3 H ch3 OH OH H H nh2 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table Π-10.

Ka R1 R3 Rjs "1F R4 Rs R6 X Y R’ r“ R9 II- 10-1 p-I- Ph H H Η CH3 Η ch3 OH OH H H NH2 II- 10-2 p-I- Ph Η Η ch3 ch3 H ch3 OH OH H H nh2 II- 10-3 p-I- Ph H Η CHiCH,), ch3 H ch3 OH OH H H nh2 II- 10-4 p-I- Ph H Η CH2CH(CH3)2 ch3 Η ch3 OH OH H H nh2 II- 10-5 p-I- Ph H Η CH2Ph ch3 Η ch3 OH OH H H nh2 II- 10-6 p-I- Ph H Η CH2-indol-3- yi ch3 Η ch3 OH OH H H nh2 II- 10-7 p-I- Ph Η Η CH2CH2SCH3 ch3 Η ch3 OH OH H H nh2 II- 10-8 p-I- Ph * Η * ch3 Η ch3 OH OH H H nh2 *R2 and Rejoined together by (CH2)3 to form Five-membered ring.

Table 11-11. Ka R R3 RJa R3b r4 R5 R6 X Y R’ R* Ry ΙΙ-Π-1 ch3 H H H Et H ch3 OH OH H H nh2 II-11-2 ch3 Η H ch3 Et H ch3 OH OH H H nh2 2983472*1 -104- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ns R1 R2 R 3« R4 R6 X Y R' R8 II-14-3 'Bu H H CH(CH3)2 Et H ch3 OH OH H H NH2 II-14-4 'Bu H H CH2CH(CH3)2 Et H ch3 OH OH H H nh2 II-14-5 'Bu H H CH2Ph Et H ch3 OH OH H H nh2 II-14-6 'Bu H H CH2-indol-3-yl Et H ch3 OH OH H H nh2 II-14-7 'Bu H H CH2CH2SCH3 Et H ch3 OH OH H H nh2 II-14-8 'Bu * H * Et H ch3 OH OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table 11-15.

Ns nr R2 R3a R---- R4 T R6 X Y r' R8 R5^ II-15-1 Ph H H H Et H CH3 OH OH H Η nh2 11-15-2 Ph H H ch3 Et H ch3 OH OH H H nh2 II-15-3 Ph H H CH(CH3)2 Et H ch3 OH OH H H nh2 II-15-4 Ph H H CH2CH(CH3)2 Et H ch3 OH OH H H nh2 II-15-5 Ph H H CH2Ph Et H ch3 OH OH H H nh2 II-15-6 Ph H H CH2-indol-3-yl Et H ch3 OH OH Η H nh2 II-15-7 Ph H H CH2CH2SCH3 Et H ch3 OH OH H H nh2 H-15-8 Ph * H * Et H ch3 OH OH H H nh2 *R2 and RJ0 joined together by (CH2)3 to form five-membered ring. Table 11-16. Ns R R2 R 3a R 4 R3 R6 X Y R7 R8 R9 II- p-Me- H H H Et H ch3 OH OH H H nh2 16-1 Ph II- p-Me- H H CH3 Et H ch3 OH OH H H nh2 16-2 Ph II- p-Me- Jtl H chcch,). Et H ch3 OH OH H H nh2 16-3 Ph II- p-Me- Η Η CH2CH(CH3)2 Et H ch3 OH OH H H nh2 16-4 Ph II- p-Me- H H CHjPh Et H ch3 OH OH H H nh2 16-5 Ph II- p-Me- H H CH2-indoi-3- Et H ch3 OH OH H H nh2 16-6 Ph y· II- p-Me- H H CH2CH2SCH3 Et H ch3 OH OH H H nh2

Ph 2983472-1 -106- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Xs R1 "R1" r38 R5b"~ R4 RJ R4 X Y R7 R8 R’ 16-7 II- 16-8 p-Me- Ph ♦ H * Et H ch3 OH OH H H nh2 *R2 and RJbjoined together by (CHib to form five-membered ring. Table 11-17. Xs Rl R2 'R3a“ R4 R3 R6 X Y R7 R- R9 Π-17- 1 p-F- Ph H H H Et H ch3 OH OH H H nh2 11-17- 2 p-F- Ph H H ch3 Et H ch3 OH OH H H nh2 11-17- 3 p-F- Ph H H CH(CH3)j Et H ch3 OH OH H H nh2 11-17- 4 p-F- Ph H H CH2CH(CH3)2 Et H ch3 OH OH H H nh2 11-17- 5 p-F- Ph H H CH2Ph Et H ch3 OH OH H H nh2 11-17- 6 p-F- Ph H H CH2-indol-3- yi Et H ch3 OH OH H H nh2 11-17- 7 p-F- Ph H H ch2ch2sch3 Et H ch3 OH OH H H nh2 II-17- 8 p-F- Ph * H * Et H ch3 OH OH H H nh2 *RJ and Rejoined together by (CHaji to form five-membered ring.

Table 11-18. X° R1 R2 R3’ R3b R4 R5 R6 X Y R' R’ Ry II- 18-1 p-Cl- Ph Η Η Η Et H CH3 OH OH H H nh2 II- 18-2 p-Cl- Ph Η Η ch3 Et H ch3 OH OH H H nh2 II- 18-3 p-CI- Ph Η Η CH(CH3)2 Et H ch3 OH OH H H nh2 II- 18-4 p-Cl- Ph Η Η ΟΗ2ΟΗ(ΟΗ3)2 Et H ch3 OH OH H H nh2 II- p-Cl- Η Η CH2Ph Et H ch3 OH OH H H nh2

Ph 2983472-1 -107- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Ns R1 R2 r3« R” R4 R3 R6 X Y R7 R8 R9^ 18-5 II- p-Cl- H H CH2-indol-3- Et H ch3 OH OH H H nh2 18-6 Ph yi 11- p-Cl- H H ch2ch2sch3 Et H ch3 OH OH H H nh2 18-7 Ph II- p-Cl- 4 H ♦ Et H ch3 OH OH H H NH2 *R2 and Re joined together by (CHab to form five-membered ring.

Table 11-19.

Ns r‘ R2 R3a "r35 R4 R3 R6 X Y R7" R8 R9 II- 19-1 p-Br- Ph H H H Et H ch3 OH OH H H nh2 II- 19-2 p-Br- Ph H H ch3 Et H ch3 OH OH Η H nh2 II- 19-3 p-Br- Ph H H CH(CH3)2 Et H ch3 OH OH H H nh2 II- 19-4 p-Br- Ph H H CH2CH(CH3)2 Et H ch3 OH OH H H nh2 II- 19-5 p-Br- Ph H H CH2Ph Et H ch3 OH OH H H nh2 11- 19-6 p-Br- Ph H H CH2-indol-3- y] Et H ch3 OH OH H H nh2 II- 19-7 p-Br- Ph H H CH2CH2SCH3 Et H ch3 OH OH H H nh2 II- 19-8 p-Br- Ph * H 4 Et H ch3 OH OH H H nh2 ♦R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table 11-20. Ns R R2 R3a R3b R4 R3 R6 X Y R' R1 R9 Π-20- 1 p-I- Ph H H H Et H ch3 OH OH H H nh2 H-20- 2 p-I- Ph H H CH3 Et H ch3 OH OH H H NHa Π-20- p-I- H Η CH(CH3)2 Et H ch3 OH OH H H NH2

Ph 2983472-1 -108- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Xa R1 R2 R3® —35 TT "r3" Ra X Y R7 R5 R5 3 11-20- p-I- H H CH2CH(CH3)2 Et H ch3 OH OH H H nh2 4 Ph 11-20- p-I- H H CH2Ph Et H ch3 OH OH H H nh2 5 Ph 11-20- p-1- H H CH2-indol-3- Et H ch3 OH OH H H nh2 6 Ph yi 11-20- p-I- H H ch2ch2sch3 Et H ch3 OH OH H H nh2 7 Ph 11-20- p-I- * H * Et H ch3 OH OH H H nh2

Ph *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table 11-21.

Xa R RJ Ri. R3b R4 R5 R6 X Y R' R“ R9 11-21-1 ch3 H H H jPr H ch3 OH OH H H NH2 II-21-2 ch3 H H CH3 'Pr H ch3 OH OH H H nh2 11-21-3 ch3 H H CH(CH3)2 'Pr H ch3 OH OH H H nh2 II-21-4 ch3 H H CH2CH(CH3)2 'Pr H ch3 OH OH H H nh2 U-21-5 ch3 H H CH2Ph 'Pr H ch3 OH OH H H nh2 II-21-6 ch3 H H CH2-indol-3-yl 'Pr H ch3 OH OH H H nh2 II-21-7 ch3 H H CH2CH2SCH3 'Pr H ch3 OH OH H H nh2 ΙΪ-21-8 d.n'2 _ J ch3 * H * 'Pr H ch3 OH OH H H NH2 ♦R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table 11-22.

Xa R1 R2 R3fl R3b R4 Rs R6 X Y R7 R* r^ II-22-1 Et H H H 'pr H ch3 OH OH H H nh2 11-22-2 Et H H CH3 'Pr H ch3 OH OH H H nh2 II-22-3 Et H H CH(CH3)j 'Pr H ch3 OH OH H H nh2 II-22-4 Et H H CH2CH(CH3)2 'Pr H ch3 OH OH H H nh2 H-22-5 Et H H CH2Ph *Pr H ch3 OH OH H H nh2 II-22-6 Et H H CH2-indol-3-yl 'Pr H ch3 OH OH H H nh2 II-22-7 Et H H CH2CH2SCH3 Tr H ch3 OH OH H H nh2 11-22-8 Et * H * 'Pr H ch3 OH OH H H NHi 5 *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -109- WO 2008/121634

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Table 11-23. X2 R* R2 r3“~ R3b R4 R5 R6 X Y r’ R8 H-23-1 'Pr H H H -Ip7 H ch3 OH OH H H NH2 II-23-2 'Pr H H ch3 'Pr H ch3 OH OH H H nh2 H-23-3 'Pr H H CH(CH3)2 'Pr H ch3 OH OH H H nh2 II-23-4 'Pr H H CH2CH(CH3)2 'Pr H ch3 OH OH H H nh2 II-23-5 'Pr H H CH2Ph 'Pr H ch3 OH OH H H nh2 Π-23-6 'Pr H H CH2-indol-3-yl 'Pr H ch3 OH OH H H nh2 H-23-7 'Pr H H CH2CH2SCH3 'Pr H ch3 OH OH H H nh2 ΪΙ-23-8 j 'Pr * H * 'Pr H ch3 OH OH H H nh2 *R2 and Rejoined together by (ΟΗ2)3 to form five-membered ring.

Table Π-24.

Ns IF RJa R4 R5 R6 X Y r r“ r^ ΙΪ-24-1 'Bu Η Η Η 'Pr H ch3 OH OH H H nh2 Π-24-2 'Bu H Η ch3 'Pr H ch3 OH OH H H nh2 H-24-3 *Bu Η Η CHCCH,), 'Pr H ch3 OH OH H H nh2 II-24-4 'Bu Η Η CH2CH(CH3)2 'Pr H ch3 OH OH H H nh2 II-24-5 ^Bu Η Η CH2Ph 'Pr H ch3 OH OH H H nh2 II-24-6 Έυ Η Η CH2-indol-3-yl 'Pr H ch3 OH OH H H nh2 II-24-7 'Bu Η Η CH2CH2SCH3 'Pr H ch3 OH OH H H nh2 II-24-8 4 Η * 'Pr H ch3 OH OH H H nh2 5 *R2 and R30 joined together by (CH2)3 to form five-membered ring.

Table II-25.

Xa R1 R2 IF “r* R4 RJ R$ X Y IV R8 R^ Π-25-1 Ph Η H H ""'pT H CH3 OH OH H H NH2 II-25-2 Ph H H CH3 'Pr H ch3 OH OH H H nh2 II-25-3 Ph H H CH(CH3)2 'Pr H ch3 OH OH H H nh2 II-25-4 Ph H H CH2CH(CH3)2 'Pr H ch3 OH OH H H nh2 Π-25-5 Ph H H CH2Ph Tr H ch3 OH OH H H nh2 II-25-6 Ph H H CH2-indol-3-yl 'Pr H ch3 OH OH H H nh2 ΙΪ-25-7 Ph H H CH2CH2SCH3 'Pr H ch3 OH OH H H nh2 II-25-8 “ZR2—5 Ph * H * 'Pr H ch3 OH OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -110- WO 2008/121634

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Table 11-26. "R1-; R2 r3. -r3E R5 R6 X Y ir R8 R9 II- 26-1 p-Me- Ph H H H JPr H ch3 OH OH H H nh2 II- 26-2 p-Me- Ph H H CH3 'Pr H ch3 OH OH H H nh2 II- 26-3 p-Me- Ph H H CH(CH3)2 'Pr H ch3 OH OH H H nh2 II- 26-4 p-Me- Ph H H CH2CH(CH3)2 'Pr H ch3 OH OH H H nh2 II- 26-5 p-Me- Ph H H CH2Ph 'Pr H ch3 OH OH H H nh2 II- 26-6 p-Me- Ph H H CH2-indol-3- yt Tr H ch3 OH OH H H nh2 II- 26-7 p-Me- Ph H H ch2ch2sch3 'Pr H ch3 OH OH H H nh2 II- p-Me- * H * 'Pr H ch3 OH OH H H nh2 26-8 Ρ1ΐ *R2 and Rejoined together by (0¾¼ to form five-membered ring.

Table II-27.

Rl R2 R3a’ R3b R4 R5 R* X Y R7 R8 Ry 11-27- p-F-1 Ph H H H ipr H CH3 OH OH H H NH2 11-27- p-F-2 Ph H H CH3 'Pr H ch3 OH OH H H nh2 11-27- p-F-3 Ph H H CHiCHah 'Pr H ch3 OH OH H H nh2 11-27- p-F-4 ph H H CH2CH(CH3)2 'Pr H ch3 OH OH H H nh2 11-27- p-F-5 Ph H H CH2Ph 'Pr H ch3 OH OH H, H nh2 11-27- p-F- H H CH2-indol-3- 'Pr H ch3 OH OH H H nh2 6 Ph yi Π-27- p-F-7 Ph H H CHaCH2SCH3 'Pr H ch3 OH OH H H nh2 2983472-1 -111- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Jfe R1 R2 R3· R3b R4 R5 R6 X Y R? R8 R9 H-27- p-F- * H ♦ 'Pr H CH3 OH OH Η H NH2 8 Ph ♦R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table ΪΙ-28. R1 R2 RJa R* RJ R6 X Y R7 R8 R9^ II- 28-1 p-Cl- Ph H H H H ch3 OH OH H H nh2 II- 28-2 p-Cl- Ph H H ch3 'Pr H ch3 OH OH H H nh2 II- 28-3 p-Cl- Ph H H CH(CH3h 'Pr H ch3 OH OH H H nh2 II- 28-4 p-Cl- Ph H H CH2CH(CH3)2 'Pr H ch3 OH OH H H nh2 II- 28-5 p-Cl- Ph H H CII2Ph 'Pr H ch3 OH OH H H nh2 II- 28-6 p-CI- Ph H H CH2-indol-3- yi 'Pr H ch3 OH OH H H nh2 II- 28-7 p-Cl- Ph H H ch2ch2sch3 'Pr H ch3 OH OH H H nh2 II- p-Cl- 4 H 4 'Pr H ch3 OH OH H H nh2 28-8 Ph *R2 and R3t) joined together by (CFhbto form five-membered ring.

Table II-29.

Xs R1 R2 R3a Ίτ R3 R5 X Y R’ R8 F II- p-Br- H H H Ipr H ch3 OH OH Η H nh2 29-1 Ph II- p-Br- H H ch3 Tr H ch3 oh oh H Η nh2 29-2 Ph II- p-Br- H H CHiCH^ 'Pr H ch3 OH oh H H nh2 29-3 Ph II- p-Br- H H CH2CH(CH3)2 'Pr H ch3 OH OH H H nh2 29-4 Ph II- p-Br- H H CH2Ph 'Pr H ch3 oh OH H H nh2 29-5 Ph 2983472-] -112- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Jfe R2 ' R5* nr R5 R6 X Y R R8 R9 II- p-Br- H H CH2-indol-3- ;Pr H ch3 OH OH H H nh2 29-6 Ph yi II- p-Br- H H CHjCHjSCB, 'Pr H ch3 OH OH H H nh2 29-7 Ph II- p-Br- * H * 'Pr H ch3 OH OH H H nh2 29-8 Ph *R2 and R3b joined together by (QUb to form five-membered ring.

Table ΪΙ-30. R* R2 R3* R35 R4 R5 Rb X Y R7 R8 R3 Π-30- 1 p-I- Ph H H H 'Pr H CH3 OH OH H H NH2 11-30- 2 p-I- Ph H H ch3 'Pr H ch3 OH OH H H nh2 11-30- 3 p-I- Ph H H CH(CH3)2 'Pr H ch3 OH OH H H nh2 11-30- 4 p-I- Ph H H CH2CH(CH3)2 'Pr H ch3 OH OH H H nh2 11-30- 5 p-I- Ph H H CH2Ph 'Pr H ch3 OH OH H H nh2 11-30- 6 p-I- Ph H H CH2-indol-3- yi Tr H ch3 OH OH H H nh2 II-30- 7 p-I- Ph H H CH2CH2SCH3 'Pr H ch3 OH OH H H nh2 H-30- 8 p-I- Ph * H ♦ 'Pr H ch3 OH OH H H nh2 *R" and RJt) joined together by (CH2)3 to form five-membered ring. Table 11-31. Xs R R2 R3"- R3® R4 RJ R6 X Y R1 Ru R9 11-31- 1 11-31- "i CH3 H H H "Bu H CH3 OH OH H H NH2 ch3 H H CH3 "Bu H ch3 OH OH H H nh2 i, 11-31- ch3 H H CHfCHab "Bu H ch3 OH OH H H nh2 3 2983472-1 113- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Xs R1 R1 R3a "r* R4 RJ R6 X Y r’ r“ R9 11-31- ch3 H H CH2CH(CH3)2 "Bu H ch3 OH OH H H NH2 4 Π-31- ch3 H H CH2Ph "Bu H ch3 OH OH H H nh2 5 Π-31- ch3 H H CH2-indol-3- "Bu H ch3 OH OH H H nh2 6 yi H-31- ch3 H H ch2ch2sch3 "Bu H ch3 OH OH H H nh2 7 11-31- ch3 * H ♦ "Bu H ch3 OH OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table II-32. Ίΰλ o'

Ns R* RJ r3> R3b R4 R5 R6 X Y R' Ra R9 Π-32-1 Et H Η Η "Bu H ch3 OH OH H H NH2 II-32-2 Et H Η ch3 "Bu H ch3 OH OH H H nh2 II-32-3 Et Η Η CH(CH3)2 "Bu H ch3 OH OH H H nh2 H-32-4 Et Η Η CH2CH(CH3)2 "Bu H ch3 OH OH H H nh2 H-32-5 Et Η Η CH2Ph "Bu H ch3 OH OH H H nh2 II-32-6 Et Η Η CH2-indol-3-yl "Bu H ch3 OH OH H H nh2 11-32-7 Et Η Η CH2CH2SCH3 "Bu H ch3 OH OH H H nh2 II-32-8 Et ♦ Η ♦ "Bu H ch3 OH OH H H nh2 ♦R2 and R3b joined together by (CH^ to form five-membered ring.

Table Π-33.

Ns R R3 R3b R4 Rs R6 X Y ΊΓ R“ R9 H-33-1 'Pr H H H "Bu H CH3 OH OH H H NH2 H-33-2 'Pr ,H H CH3 "Bu H ch3 OH OH H H nh2 Π-33-3 'Pr H H CH(CH3)2 "Bu H ch3 OH OH H H nh2 H-33-4 'Pr H H CH2CH(CH3)2 "Bu H ch3 OH OH H H nh2 11-33-5 'Pr H H CH2Ph "Bu H ch3 OH OH H H nh2 11-33-6 'Pr H H CH2-indol-3-yl "Bu H ch3 OH OH H H nh2 H-33-7 'Pr H H CH2CH2SCH3 "Bu H ch3 OH OH H H nh2 Π-33-8 'Pr * H * "Bu H ch3 OH OH H H nh2 5 *R2 and R3b joined together by (01¾ to form five-membered ring. 2983472-1 -114- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table II-34.

Ns R1 R3 R3’ —35 TT“ r! R6 X Y IT R9 11-34-1 'Bu H H H "Bu H ch3 OH OH H H nh2 II-34-2 'Bu H H ch3 "Bu H ch3 OH OH H H nh2 II-34-3 'Bu H H CH(CH3)2 "Bu H ch3 OH OH H H NHi II-34-4 'Bu H H CH2CH(CH3)2 "Bu H ch3 OH OH H H nh2 II-34-5 'Bu H H CH2Ph "Bu H ch3 OH OH H H nh2 II-34-6 'Bu H H CHrindol-3-yl "Bu H ch3 OH OH H H nh2 II-34-7 'Bu H H ch2ch2sch3 "Bu H ch3 OH OH H H nh2 II-34-8 'Bu * H * "Bu H ch3 OH OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table 11-35.

Ns R R3 RJ« R3b R4 Rs R6 X Y R' R8 R9 II-35-1 Ph H H H "Bu H CH3 OH OH H H NH2 II-35-2 Ph H H CH3 "Bu H ch3 OH OH H H nh2 II-35-3 Ph H H CH(CH3)2 "Bu H ch3 OH OH H H nh2 II-35-4 Ph H H CHjCHCCH^ "Bu H · ch3 OH OH H H nh2 H-35-5 Ph H H CH2Ph "Bu H ch3 OH OH H H nh2 II-35-6 Ph H H CH2-indol-3-yl "Bu H ch3 OH OH H H nh2 11-35-7 Ph H H CH2CH2SCH3 "Bu H ch3 OH OH H H nh2 II-35-8 Ph * H * "Bu H ch3 OH OH H H nh2 *R2andR30 joined together by (CHjfe to form five-membered ring Table 11-36. Ns R 1 R2 R3· R3b R4 Rs Rfc X Y r’ r“ R9 II- p- Η Η Η "Bu H ch3 OH OH H H NH2 36-1 Me- Ph II- p- Η Η ch3 "Bu H ch3 OH OH H H nh2 36-2 Me- Ph II- p- Η Η CH(CH3)2 "Bu H ch3 OH OH H H nh2 36-3 Me- Ph II- p- Η Η CHjCH(CH3)2 "Bu H ch3 OH OH H H nh2 36-4 Me- Ph II- p- Η Η CH2Ph "Bu H ch3 OH OH H H nh2 36-5 Me- Ph II- p- Η Η CH2-indoI-3- "Bu H CHj OH OH H H nh2 2983472-1 1.15 - WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Xs R1 R2 R3a R3b R4 R5 R6 X Y R5* 36-6 II- Me- Ph p- H H yi ch2ch2sch3 "Bu H ch3 OH OH H H nh2 36-7 II- Me- Ph p- * H * "Bu H ch3 OH OH H H nh2 *R2 and RJb joined together by (CH^ to form five-membered ring.

Table 11-37.

Xa R' R2 r3. "R36- ΊΤ~ R3" R* X Y ΊΓ r“ Ry II- 37-1 p-F- Ph H H H "Bu H ch3 OH OH H H NH2 II- 37-2 p-F- Ph H H ch3 "Bu H ch3 OH OH H H nh2 II- 37-3 p-F- Ph H H CH(CH3)2 "Bu H ch3 OH OH H H nh2 II- 37-4 p-F- Ph H H CH2CH(CH3)2 "Bu H ch3 OH OH H H nh2 II- 37-5 p-F- Ph H H CH2Ph "Bu H ch3 OH OH H H nh2 II- 37-6 p-F- Ph H H CH2-indol-3- yi "Bu H ch3 OH OH H H nh2 II- 37-7 p-F- Ph H H CH2CH2SCH3 "Bu H ch3 OH OH H H nh2 II- p-F- ♦ H ♦ "Bu H ch3 OH OH H H nh2 37-8 Ph *R2 and Rejoined together by (Cthhto fonn five-membered ring.

Table 11-38.

Xa R1 R2 r3b R3b R* ΊΓ R6 X Y R7 R“ II- p-Cl- H H Η "Bu Η ch3 OH OH Η Η nh2 38-1 Ph II- p-Cl- H H ch3 "Bu Η ch3 OH OH H Η nh2 38-2 Ph II- p-Cl- H H CHCCH^ "Bu Η ch3 OH OH H Η nh2 38-3 Ph 2983472-1 -116- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ns R‘ R5 R3’ R3b R4 R5 R4 X Y "R7" r8 R5- II- p-Cl- H H CH2CH(CH3)2 "Bu H CH3 OH OH H H NH2 38-4 Ph II- p-Cl- H H CH2Ph "Bu H ch3 OH OH H H nh2 38-5 Ph II- p-Cl- H H CH2-indol-3- "Bu H ch3 OH OH H H nh2 38-6 Ph yi II- p-Cl- H H CH2CH2SCH3 "Bu H ch3 OH OH H H nh2 38-7 Ph II- p-Cl- * H * "Bu H ch3 OH OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table 11-39.

Ns "r1 R2" T5" Έ5 R4 R5 R4 X Y r’ R8 Ry II- p-Br- Η H H "Bu H ch3 OH OH H H nh2 39-1 Ph II- p-Br- Η H ch3 "Bu H ch3 OH OH H H nh2 39-2 Ph 11- p-Br- Η H CHCCHa), "Bu H ch3 OH OH H H nh2 39-3 Ph II- p-Br- Η H CHjCHCCHj), "Bu H ch3 OH OH H H nh2 39-4 Ph II- p-Br- H H CH2Ph "Bu H ch3 OH OH H H nh2 39-5 Ph II- p-Br- H H CH2-indoI-3- "Bu H ch3 OH OH H H nh2 39-6 Ph yi II- p-Br- H H CH2CH2SCH3 "Bu H ch3 OH OH H H nh2 39-7 Ph II- p-Br- * H * "Bu H ch3 OH OH H H nh2 39-8 Ph *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table 11-40. Ns Rl RJ R3‘ R3b R4 R5 R4 X Y R7 R" R9 II- p-I- H Η H "Bu H CH3 OH OH H H NH2 40-1 Ph 2983472-1 -117- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 T” Rih "r3E R4 Rs R4 X Y R7" r“ R9 II- p-I- H H ch3 "Bu H ch3 OH OH H H NH2 40-2 Ph II- p-I- H H CH(CHj)2 "Bu H CH3 OH OH H H nh2 40-3 Ph II- p-I- H H CH2CH(CH3)2 "Bu H ch3 OH OH H H nh2 40-4 Ph II- p-I- H H CH2Ph "Bu H ch3 OH OH H H nh2 40-5 Ph II- p-I- H H CH2-indol-3- "Bu H ch3 OH OH H H nh2 40-6 Ph yi II- p-I- H H ch2ch2sch3 "Bu H ch3 OH OH H H nh2 40-7 Ph II- p-I- * H * "Bu H ch3 OH OH H H nh2 *R? and RJb joined together by (0¾^ to form five-membered ring.

Table 11-41.

Ji2 ΊΓ” R2 R38 R3b R4 Rs X Y R7 R8 R3"^ II-41-1 ch3 Η Η Η Bz H ch3 OH OH H H nh2 H-41-2 ch3 Η Η ch3 Bz H ch3 OH OH H H nh2 II-41-3 ch3 Η Η CH(CH3)2 Bz H ch3 OH OH H H nh2 II-41-4 ch3 Η Η CH2CH(CH3)2 Bz H ch3 OH OH H H nh2 II-41-5 ch3 Η Η CH2Ph Bz H ch3 OH OH H H nh2 Π-41-6 ch3 Η Η CH2-indol-3-yl Bz H ch3 OH OH H H nh2 II-41-7 ch3 Η Η CH2CH2SCH3 Bz H ch3 OH OH H H nh2 II-41-8 ch3 * Η * Bz H ch3 OH OH H H nh2 *R2 and Rejoined together by (CHj)3 to form five-membered ring.

Table II-42. R1 R2 R3" R3" R4 RJ R4 X Y R7" R# R9 II-42-1 Et H H H Bz H CH3 OH OH H H NH2 II-42-2 Et H H ch3 Bz H ch3 OH OH H H nh2 U-42-3 Et H H CH(CH3)2 Bz H ch3 OH OH H H nh2 U-42-4 Et H H CH2CH(CH3)2 Bz H ch3 OH OH H H nh2 U-42-5 Et H H CH2Ph Bz H ch3 OH OH H H nh2 II-42-6 Et H H CH2-indol-3-yl Bz H ch3 OH OH H H nh2 29SM72-1 -118- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Xa R1 RJ R3“ R4 R5 R6 X Y ΊΓ Ra R5 11-42-7 Et H H CH3CH2SCH3 Bz H ch3 OH OH H H NH2 11-42-8 “*772-3 Et * H * Bz H ch3 OH OH H H nh2 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table II-43.

Xa R1 R1 "r3s R4 R5 R6 X Y R7 Rs 1? II-43-1 JPr H H H Bz H CH3 OH OH H H nh2 11-43-2 'Pr H H CH3 Bz H ch3 OH OH H H nh2 II-43-3 'Pr H H CH(CH3)2 Bz H ch3 • OH OH H H nh2 11-43-4 'Pr H H CH2CH(CH3)2 Bz H ch3 OH OH H H nh2 Π-43-5 'Pr H H CH2Ph Bz H ch3 OH OH H H nh2 II-43-6 'Pr H H CH2-indoI-3-yl Bz H ch3 OH OH H H nh2 ΪΙ-43-7 'Pr H H CH2CH2SCH3 Bz H ch3 OH OH H H nh2 II-43-8 'Pr * H * Bz H ch3 OH OH H H nh2 *R2 and R3b joined together by to form five-membered ring.

Table 11-44.

Xa R R3 R3. Rib R4 Rs R6 X Y R7 Rb R/ Π-44-1 'Bu H H H Bz H CH3 OH OH H H nh2 II-44-2 'Bu H H CH3 Bz H ch3 OH OH H H nh2 II-44-3 *Bu H H CH(CH3)2 Bz H ch3 OH OH H H nh2 H-44-4 'Bu H H CHiCHCCHa), Bz H ch3 OH OH H H nh2 H-44-5 'Bu H H CH2Ph Bz H ch3 OH OH H H nh2 II-44-6 H H CH2-indol-3-yl Bz H ch3 OH OH H H nh2 H-44-7 *Bu H H ch2ch2sch3 Bz H ch3 OH OH H H nh2 11-44-8 'Bu * H 4 Bz H ch3 OH OH H H nh2 5 *R2 and R3” joined together by (CH2)3 to form five-membered ring.

Table Π-45.

Xa R1" R2 R3‘ "r3S R4 R5 R* X Y r“ Ry 11-45-1 Ph Η Η Η Bz Η ch3 OH OH H H NH2 II-45-2 Ph Η Η ch3 Bz Η ch3 OH OH H H NH3 H-45-3 Ph Η Η CH(CH3)2 Bz Η ch3 OH OH H H nh2 H-45-4 Ph Η Η CH2CH(CH3)2 Bz Η ch3 OH OH H H nh2 II-45-5 Ph Η Η CH2Ph Bz Η ch3 OH OH H H nh2 II-45-6 Ph Η Η CH2-indol-3-yl Bz Η ch3 OH OH H H nh2 11-45-7 Ph Η Η ch2ch2sch3 Bz Η ch3 OH OH H H nh2 2983472-1 119- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ms R‘ R2 R3fl R3b R4 RJ R6 X Y R7 R“ R9 II-45-8 Ph ♦ H * Bz H CH3 OH OH H H NH2 *RJ and R" joined together by (CH2)3 to form five-membered ring. Table 11-46. Ms R1 R2 R3* R3b R4 Rs R6 X Y R' RK R9 II- 46-1 p-Me- Ph H H H Bz H ch3 oh OH H H NH2 II- 46-2 p-Me- Ph H H ch3 Bz H ch3 OH OH H H nh2 II- 46-3 p-Me- Ph H H CH(CH3)2 Bz H ch3 OH OH H H nh2 II- 46-4 p-Me- Ph H H ch2ch(ch3)2 Bz H ch3 OH OH H H nh2 II- 46-5 p-Me- Ph H H CH2Ph Bz H ch3 OH OH H H nh2 II- 46-6 p-Me- Ph H H CH2-indol-3- yi Bz H ch3 OH OH H H nh2 II- 46-7 p-Me- Ph H H CH2CH2SCH3 Bz H ch3 OH OH H H nh2 II- p-Me- * H * Bz H ch3 OH OH H H nh2 46-8 Ph *R2 and R36 joined together by (CH2)i to form five-membered ring.

Table Π-47. “jfe R1 R2 Ί?·’ “R35- "Τ' r! R6 X Y r’ R“ R3^ 11-47- p-F- i Η Η Η Bz H CH3 OH OH H H nh2 11-47- p-F-.2 Ph Η Η ch3 Bz H ch3 oh OH H H nh2 11-47- p-F-3 Ph Η Η ΟΗ(ΟΗ3)2 Bz H ch3 OH OH H H nh2 H-47- p-F-4 Ph Η Η CH2CH(CH3)2 Bz H ch3 OH OH H H nh2 11-47- p-F- 5 Η Η CH2Ph Bz H ch3 OH OH H H nh2 II-47- p-F- Η Η CH2-indoI-3- Bz H ch3 OH OH H H nh2

Ph 2983472-1 -120- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Na R’ “R2" “R^ “R* R4 RJ R* X Y r’ R8 R9 6 yi 11-47- p-F- H H ch2ch2sch3 Bz H ch3 OH OH H H NH2 7 Ph 11-47- p-F- 4 H * Bz H ch3 OH OH H H nh2

Ph *R7 and Rejoined together by (CH2)3 to form five-membered ring.

Table 11-48.

Na “r1— R^ R3’ R3b R4 r! R6 X Y r’ r II- 48-1 p-CI- Ph H H H Bz H ch3 OH oh H H NH2 II- 48-2 p-Cl- Ph H H CH3 Bz H ch3 oh oh Η H nh2 II- 48-3 p-CI- Ph H H CHCCH^ Bz H ch3 OH oh H H nh2 II- 48-4 p-CI- Ph H H CH2CH(CH3)2 Bz H ch3 OH OH H H nh2 II- 48-5 p-Cl- Ph H H CH2Ph Bz H ch3 oh OH H H nh2 II- 48-6 p-Cl- Ph H H CH2-indol-3- yi Bz H ch3 oh OH H H nh2 II- 48-7 p-Cl- Ph H H CH2CH2SCH3 Bz H ch3 oh OH H H nh2 II- 48-8 p-Cl- Ph 4 H * Bz H ch3 oh OH H H nh2 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table 11-49. Xa R1 Rz Rj. r30 R4 R5 R6 X Y R7 R8 R^ II- 49-1 p-Br- Ph H Η Η Bz H ch3 OH OH H H nh2 II- 49-2 p-Br- Ph Η Η ch3 Bz H ch3 OH OH H H nh2 II- 49-3 p-Br- Ph Η Η CH(CH3)2 Bz H ch3 OH OH H H nh2 II- p-Br- Η Η CH2CH(CH3)2 Bz H ch3 OH OH H H nh2

Ph 2983472-1 -121 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Na R1 "eF ’r35 ΊΓ“ RJ R6 X Y V R8 iV 49-4 II- p-Br- H H CH2Ph Bz H ch3 OH OH H H nh2 49-5 Ph II- p-Br- H H CH2-indol-3- Bz H ch3 OH OH H H nh2 49-6 Ph yt II- p-Br- H H ch2ch2sch3 Bz H ch3 OH OH H H nh2 49-7 Ph II- p-Br- ♦ H * Bz H ch3 OH OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table II-50.

Trk dT of

Ns R1 R2 RJ" Rib R* R5 R6 X Y R R9 11-50- p-I- Η H H Bz H CH3 OH OH H H NH2 1 Ph 11-50- p-I- H H ch3 Bz H ch3 OH OH H H nh2 2 Ph 11-50- p-1- H H CH(CH3)2 Bz H ch3 OH OH H H nh2 3 Ph 11-50- p-I- H H CH2CH(CH3)2 Bz H ch3 OH OH H H nh2 4 Ph II-50- p-I- H H CH2Ph Bz H ch3 OH OH H H nh2 5 Ph Π-50- p-I- H H CH2-indoI-3- Bz H ch3 OH OH H H nh2 6 Ph yt 11-50- p-I- H H CH2CH2SCH3 Bz H ch3 OH OH H H nh2 7 Ph 11-50- p-I- ♦ H * Bz H ch3 OH OH H H nh2 8 Ph 2983472-1 -122- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 *R2 and R3b joined together by (CHj)] to form five-membered ring. R9

Table III-l.

Xs R1 R2 R3b “r* RJ R6 X Y IV RT r” III-l-l ch3 H H H ch3 H ch3 F OH H H nh2 IB-l-2 ch3 H H ch3 ch3 H ch3 F OH H H nh2 ΠΙ-1-3 ch3 H H CH(CH3)2 ch3 H ch3 F OH H H nh2 ΠΙ-1-4 ch3 H H CH2CH(CH3)2 ch3 H ch3 F OH H H nh2 ΪΙΙ-1-5 CHj H H CH2Ph ch3 H ch3 F OH H H nh2 ΠΙ-1-6 ch3 H H CH2-indol-3-yl ch3 H ch3 F OH H H nh2 ΠΙ-1-7 ch3 H H ch2ch2sch3 ch3 H ch3 F OH H H nh2 ΙΠ-1-8 ch3 * H • ch3 H ch3 F OH H H nh2 5 *R2 and Rejoined together by (Cl·^ to form five-membered ring.

Table ΠΙ-2.

Xs R R2 r3> R3b R4 Rs R6 X Y R' R* Rs 1II-2-1 Et H Η Η ch3 Η ch3 F OH Η Η ΝΗ2 ΙΠ-2-2 Et Η Η ch3 ch3 Η ch3 F OH Η Η νη2 IH-2-3 Et Η Η CHiCH,), ch3 Η ch3. F OH Η Η νη2 III-2-4 Et Η Η CH2CH(CH3)2 ch3 Η ch3 F OH Η Η νη2 ΙΠ-2-5 Et Η Η CH2Ph ch3 Η ch3 F OH Η Η νη2 ΙΠ-2-6 Et Η Η CH2-indol-3-yl ch3 Η ch3 F OH Η Η νη2 ΠΙ-2-7 Et Η Η CH2CH2SCH3 ch3 Η ch3 F OH Η Η νη2 HI-2-8 Et * Η * ch3 Η ch3 F OH Η Η νη2 *R2 and Rdb joined together by (CH2)3 to form five-membered ring. 2983472-1 -123 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table III-3.

Xa R1 ΊΓ -£33- RJb R4 RJ R6 X Y iC R8 R5 III-3-1 'Pr H H H ch3 H gh3 F OH H H NH2 ΠΙ-3-2 'Pr H H ch3 ch3 H ch3 F OH H H nh2 HI-3-3 'Pr H H CH(CH3)2 ch3 H ch3 F OH H H nh2 III-3-4 'Pr H H CH2CH(CH3)2 ch3 H ch3 F OH H H nh2 III-3-5 'Pr H H CH2Ph ch3 H ch3 F OH H H nh2 HI-3-6 fPr H H CH2-lndol-3-yl ch3 H ch3 F OH H H nh2 III-3-7 ipr H H CH2CH2SCH3 ch3 H ch3 F OH H H nh2 HI-3-8 'pr « H 4 ch3 H ch3 F OH H H nh2 •R2 and Rejoined together by (Chkh to form five-membered ring.

Table III-4.

Xa Rr RJ RJa R3b R4 R3 R6 X Y R7 R8 R9 III-4-1 'Bu H H H ch3 H ch3 F OH Η Η ΝΗ2 ΙΠ-4-2 'Bu H H ch3 ch3 H ch3 F OH H Η νη2 III-4-3 'Bu H H CH(CH3)2 ch3 Η ch3 F OH H Η νη2 IH-4-4 'Bu H H CH2CH(CH3)2 ch3 Η ch3 F OH Η Η νη2 IH-4-5 'Bu H H CH2Ph ch3 Η ch3 F OH Η Η νη2 IH-4-6 'Bu H H CH2-indol-3-yl ch3 Η ch3 F OH Η Η νη2 IH-4-7 'Bu H H CH2CH2SCH3 ch3 Η ch3 F OH Η Η νη2 III-4-8 'Bu 4 H * ch3 Η ch3 F OH Η Η νη2 *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table III-5. 1 1' 1 m j '.'t j a

Xa R R2 r3« R3b R4 Rs R6 X Y R7 R8 R9^ ΠΙ-5-1 Ph Η H H ch3 H ch3 F OH H H NH2 ΗΙ-5-2 Ph H H CH3 ch3 Η ch3 F OH H H nh2 ΠΙ-5-3 Ph H H CHCCH^ ch3 H ch3 F OH H H nh2 ΙΠ-5-4 Ph Η H CH2CH(CH3)2 ch3 H ch3 F OH H H nh2 ΗΙ-5-5 Ph H H CH2Ph ch3 H ch3 F OH H H nh2 ΙΙΙ-5-6 Ph Η H CH2-lndol-3-yl ch3 H ch3 F OH H H nh2 ΠΙ-5-7 Ph H H CH2CH2SCH3 ch3 H ch3 F OH H H nh2 ΙΗ-5-8 Ph * H * ch3 H ch3 F OH H H nh2 *R2 and Rejoined together by (CH^ to form five-membered ring. 2983472-1 -124- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table II1-6.

Ns R1 R2 R3b Rs R6 X Y R7 r“ Hl- p-Me- H H H ch3 H ch3 F OH H H NH2 6-1 Ph HI- p-Me- H H ch3 ch3 H ch3 F OH H H nh2 6-2 Ph III- p-Me- H H CH(CH3)2 ch3 H ch3 F OH H H nh2 6-3 Ph III- p-Me- H H CH2CH(CH3)2 ch3 H ch3 F OH H H nh2 6-4 Ph III- p-Me- H H CH2Ph ch3 H ch3 F OH H H nh2 6-5 Ph III- p-Me- H H CHrindol-3- ch3 H ch3 F OH H H nh2 6-6 Ph yi III- p-Me- H H ch2ch2sch3 ch3 H ch3 F OH H H nh2 6-7 Ph III- p-Me- * H * ch3 H ch3 F OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table HI-7. D*

Ns R* R2 RJa Rib R* ic R6 X Y R7 R8 Jc ΙΠ-7- 1 p-F- Ph H H H ch3 H CH3 F OH H H NH2 ΙΠ-7- 2 p-F- Ph H H CH3 ch3 H ch3 F OH H H nh2 ΙΠ-7- 3 p-F- Ph H H CHCCH·,), ch3 H ch3 F OH H H nh2 IH-7- 4 p-F- Ph H H CH2CH(CH3)2 ch3 H ch3 F OH H H nh2 HI-7- 6 p-F- Ph Η H CH2Ph ch3 H ch3 F OH H H nh2 III-7- 7 p-F- Ph H H CH2-indol-3- yi ch3 H ch3 F OH H H nh2 IH-7- 8 p-F- Ph Η H CH2CH2SCH3 ch3 H ch3 F OH H H nh2 HI-7- p-F- * H ch3 H ch3 F OH H H nh2 2983472-1 -125- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Ns R1 R2 R3* R3b R4 R5 R6 X Y R7 R8 R’ 20 Ph *R2 and R·*6 joined together by (CH2)3 to form five-membered ring.

Table III-8. Ns R' R2 R3" R3b R4 R3 R6 X Y R7 R8 R* ΪΗ-8- 1 p-Cl- Ph H H H ch3 H ch3 F OH H H NH2 III-8- 2 p-Cl- Ph H H ch3 ch3 H ch3 F OH H H nh2 HI-8- 3 p-Cl- Ph H H CH(CH3)2 ch3 H ch3 F OH H H nh2 IH-8- 4 p-Cl- Ph H H CH2CH(CH3)2 ch3 H ch3 F OH H H nh2 III-8- 5 p-Cl- Ph H H CH2Ph ch3 H ch3 F OH H H nh2 HI-8- 6 p-Cl- Ph H H CH2-indol-3- y! ch3 H ch3 F OH H H nh2 HI-8- 7 p-Cl- Ph H H ch2ch2sch3 ch3 H ch3 F OH H H nh2 HI-8- p-Cl- * H * ch3 H ch3 F OH H H nh2

Ph *R2 and R36 joined together by (CFhb to form five-membered ring.

Table ΠΙ-9.

Ns R’ ΊΓ r3. r35 R4 R5 R6 X Y r’ ΊΓ Ry II1-9- 1 p-Br- Ph H H H ch3 Η ch3 F OH H H nh2 I1I-9- 2 p-Br- Ph H H CH3 ch3 H ch3 F OH H H nh2 IH-9- 3 p-Br- Ph H H CHCCHah ch3 Η ch3 F OH H H nh2 HI-9- 4 p-Br- Ph H H CH2CH(CH3)2 ch3 H ch3 F OH H H nh2 ΠΙ-9- 6 p-Br- Ph H H CH2Ph ch3 H ch3 F OH H H nh2 HI-9- p-Br- H H CH2-indol-3- ch3 H ch3 F OH H H nh2

Ph 2983472-1 -126- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Na R1 R1 R3n R4 R* R6 X Y R7 R8 R5” 7 yi III-9- p-Br- H H ch2ch2sch3 ch3 H ch3 F OH H H NH2 8 Ph III-9- p-Br- * H ♦ ch3 H ch3 F OH H H nh2 *R^ and Rejoined together by (CH2)3 to form five-membered ring.

Table III-10. X2 R' RJ Rj« R3b R4 R’ Rb X Y R' R“ R9 III- p-I- H H H ch3 Η CH3 F OH H H nh2 10-1 Ph in- p-I- H H CH3 ch3 H ch3 F OH H H nh2 10-2 Ph in- p-I- H H CH(CH3)2 ch3 H ch3 F OH H H nh2 10-3 Ph in- p-I- H H CH2CH(CH3)2 ch3 H ch3 F OH H H nh2 10-4 Ph III- p-I- H H CH2Ph ch3 H ch3 F OH H H nh2 10-5 Ph ΠΙ- p-I- H H CH2-indol-3- ch3 H ch3 F OH H H nh2 10-6 Ph yi in- p-I- H H CH2CH2SCH3 ch3 H ch3 F OH H H nh2 10-7 Ph in- p-I- * H ♦ ch3 H ch3 F OH H H nh2 10-8 Ph »Ra! andR36 joined together by (CH2)3 to form five ;-meml bered ring. Tabl e HI-11. Ka R* R2 r3·" R30 R4 R5 R6 X Y R7 R8 Ry ΠΙ-11-1 ΠΙ-11-2 HI-11-3 ch3 ch3 ch3 Η H Η H H H H CH3 CH(CH3)2 Et Et Et H H H ch3 ch3 ch3 F F F OH H H H H NH2 nh2 nh2 OH OH H H HI-11-4 ch3 H H CH2CH(CH3)2 Et H ch3 F OH H H nh2 ΙΠ-11-5 ch3 H H CH2Ph Et H ch3 F OH H H nh2 HI-11-6 ch3 H H CH2-indol-3-yl Et H ch3 F OH H H nh2 IH-11-7 ch3 H H CH2CH2SCH3 Et H ch3 F OH H H nh2 2981472- .- 127 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Nb R1 R2 R3a R3b R4 R3 R* X Y R7 R8 R9 HI-11-8 CH3 * H * Et H CH3 F OH Η H NH2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table 111-12.

Ne R1 R2 “ft® R4 RJ R6 X Y r’ Ra R5 IH-12-1 Et H H H Et H ch3 F OH H H nh2 ΠΙ-12-2 Et H H ch3 Et H ch3 F OH H H nh2 ΙΠ-12-3 Et H H CH(CH3)2 Et H ch3 F OH H H nh2 HI-12-4 Et H H CH2CH(CH3)2 Et H CH3 F OH H H nh2 ΙΠ-12-5 Et H H CH2Ph Et H ch3 F OH H H nh2 HI-12-6 Et H H CH2-indol-3-yl Et H ch3 F OH H H nh2 IH-12-7 Et H H CH2CH2SCH3 Et H ch3 F OH H H nh2 IH-12-8 Et ♦ H * Et H ch3 F OH H H nh2 *R2andRJb joined together by (CH2)3 to form five-membered ring.

Table III-13.

No R R2 R3’ R3b R4 Rs R6 X Y R7 R" R9 HI-13-1 'Pr H H H Et H ch3 F OH Η Η ΝΗ2 IH-13-2 'Pr H H CH3 Et H ch3 F OH Η Η νη2 ΠΙ-13-3 'Pr H H CH(CH3)2 Et H ch3 F OH Η Η νη2 IH-13-4 (pr H H CH2CH(CH3)2 Et H ch3 F OH Η Η νη2 IH-13-5 'Pr H H CH2Ph Et H ch3 F OH Η Η νη2 ΙΠ-13-6 'Pr H H CH2-indol-3-yl Et H ch3 F OH Η Η νη2 HI-13-7 'Pr H H CH2CH2SCH3 Et H ch3 F OH Η Η νη2 HI-13-8 'Pr ♦ H * Et H ch3 F OH Η Η νη2 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table III-14.

Ns R R2 R 3a R3b R4 R5 R6 X Y R7 R’ R9 ΙΗ-14- 1 'Bu Η Η Η Et H CH3 F OH H H NH2 1 ΙΙΙ-14- Έυ Η Η ch3 Et H ch3 F OH H H nh2 2 ΙΠ-14- 'Bu Η Η CH(CH3)2 Et H ch3 F OH H H nh2 3 UI-14- 'Bu Η Η CH2CH(CH3)2 Et H ch3 F OH H H nh2 2983472-1 -128 WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Xa R1 R2 R 3a ΊΤ R4 R! R6 X Y Ί?’ R# Rs 4 ΙΠ-14- 'Bu H H CH2Ph Et H ch3 F OH H H NH2 5 ΙΠ-14- 'Bu H H CHi-indol-3-yl Et H ch3 F OH H H NH2 6 ΙΙΙ-14- 'Bu H H CH2CH2SCH3 Et H ch3 F OH H H nh2 7 ΠΙ-14- 'Bu * H ♦ Et H ch3 F OH H H nh2 8 *R2 and R30 joined together by (CH2)3 to form five-membered ring.

Table 111-15. "ΪΛ Dl

Xa R1 R2 R3“ R4 Rs R6 X Y R7 IV IH-15-1 Ph H H H Et H ch3 F OH H H nh2 ΙΠ-15-2 Ph H H ch3 Et H ch3 F OH H H nh2 HI-15-3 Ph H H CH(CH3)2 Et H ch3 F OH H H nh2 III-15-4 Ph H H CH2CH(CH3)2 Et H ch3 F OH H H nh2 HI-15-5 Ph H H CH2Ph Et H ch3 F OH H H nh2 HI-15-6 Ph H H CH2-indol-3-yl Et’ H ch3 F OH H H nh2 ΠΙ-15-7 Ph H H CH2CH2SCH3 Et H ch3 F OH H H nh2 ΙΠ-15-8 Ph ♦ H * Et H ch3 F OH H H nh2 *R2 and Rejoined together by (CHah to form five-membered ring.

Table IU-16.

Xa R1 nr ΊΤ~ "IT R4 ΊΤ R6 X Y k' R8 Ry III- p-Me- H H H Et H ch3 F OH H Η nh2 16-1 Ph III- p-Me- Η H CH3 Et H ch3 F OH H H nh2 16-2 Ph III- p-Me- H Η CHiCHah Et H ch3 F OH H H nh2 16-3 Ph III- p-Me- H H ΟΗ2ΟΗ(ΟΗ3)2 Et H ch3 F OH H H nh2 16-4 Ph in- p-Me- H Η CH2Ph Et H ch3 F OH Η H NH2 2983472-1 -129- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Xs R] R2 "R35" R3b R4 R5 R6 X Y r’ Rtt R9^ III- p-Me- H H CH2-indoI-3- Et H ch3 F OH H H nh2 16-6 Ph yi III- p-Me- H H ch2ch2sch3 Et H ch3 F OH H H nh2 16-7 Ph III- p-Me- * H * Et H ch3 F OH H H nh2 16-8 “ΪΤΤ2— Ph 1-.. /ru \ J *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table III-17.

Xs Rl R1 "r31" R3b R4 R5 R* X Y R7 R# R9 III-17- 1 p-F- Ph H H H Et H ch3 F OH H H NH2 III-17- 2 p-F- Ph H H CH3 Et H ch3 F OH H H nh2 ΠΙ-17- 3 p-F- Ph H H CH(CH3)2 Et H ch3 F OH H H nh2 III-17- 4 p-F- Ph H H CH2CH(CH3)3 Et H ch3 F OH H H nh2 III-17- 5 p-F- Ph H H CH2Ph Et H ch3 F OH H H nh2 111-17- 6 p-F- Ph H H CH2-indol-3- yi Et H ch3 F OH H H nh2 III-17- 7 p-F- Ph H H CH2CH2SCH3 Et H ch3 F OH H H nh2 ΙΠ-17- 8 p-F- Ph * H * Et H ch3 F OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table III-18. Xs R1 R2 R3. R3b R4 R5 R6 X Y R7 R8 R9 IH-18- 1 p-Cl- Ph Η H H Et H ch3 F OH H H nh2 ΙΗ-18- 2 p-CI- Ph H H ch3 Et H ch3 F OH H Η nh2 ΠΙ-18- p-Cl- H H CHCCHah Et H ch3 F OH H H nh2 3 Ph 2983472-1 -130- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Ns Rl R2 R3* R3b R4 Rs R6 X Y R7 R8 I? ΠΙ-18- 4 p-Ci- Ph H H CH2CH(CH3)2 Et H ch3 F OH H H nh2 ΙΠ-18- 5 p-Cl- Ph H H CH2Ph Et H ch3 F OH H H nh2 ΙΠ-18- 6 p-Cl- Ph H H CH2-indol-3- yt Et H ch3 F OH H H nh2 III-18- 7 p-Cl- Ph H H ch2ch2sch3 Et H ch3 F OH H H nh2 ΠΙ-18- 8 p-Cl- Ph * H * Et H ch3 F OH H H nh2 *RZ and R3b joined together by (Cthh to form five-membered ring.

Table ΠΙ-19. Xs R' R2 R3’ R3b IV R5 R X Y R' R Ry HI-19- p-Br-1 Ph H H H Et H CH3 F OH H H NH2 HI-19- p-Br-2 Ph H H CH3 Et H ch3 F OH H H nh2 111-19- p-Br-3 Ph H H CHCCHah Et H ch3 F OH H H nh2 HI-19- p-Br-4 Ph H H CH2CH(CH3)2 Et H ch3 F OH H H nh2 IH-19- p-Br-5 Ph H H CH2Ph Et H ch3 F OH H H nh2 UI-19- p-Br-6 Ph H H CHrindol-3- yi Et H ch3 F OH H H nh2 ΠΙ-19- p-Br-7 Ph H H CH2CH2SCH3 Et H ch3 F OH H H nh2 HI-19- p-Br-8 Ph * H * Et H ch3 F OH H H nh2 *R2 and R3t> joined together by (CFbb to form five-membered ring.

Table III-20. Xa Rl R2 R3' RJb R4 R5 R6 X Y R7 R8 R9 IH-20- p-I- Η Η H Et H CH3 F OH Η H NH2 2983472-1 -131 - WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ns R1 R2 R3’ R3b R4 R3 R6 X Y r’ R8 V ΠΙ-20- p-I- H H ch3 Et H ch3 F OH H H nh2 2 Ph ΠΙ-20- p-I- H H CH(CH3)2 Et H ch3 F OH H H nh2 3 Ph HI-20- p-I- H H CH2CH(CH3)2 Et H ch3 F OH H H nh2 4 Ph HI-20- p-I- H H CH2Ph Et H ch3 F OH H H nh2 5 Ph III-20- p-I- H H CH2-indol-3- Et H ch3 F OH H H nh2 6 Ph yi III-20- p-I- H H ch2ch2sch3 Et H ch3 F OH H H nh2 7 Ph HI-20- p-I- * H * Et H ch3 F OH H H nh2

Ph *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table HI-21.

Jf2 R’ RJ RJ‘ R3b R4 R5 R6 X Y R7 R8 R9 III-21-1 ch3 H H H H ch3 F OH H H NH2 III-21-2 ch3 H H CH3 Pr H ch3 F OH H H nh2 UI-21-3 ch3 H H CH(CH3)2 Pr H ch3 F OH H H nh2 IH-21-4 ch3 H H CH2CH(CH3)2 Pr H ch3 F OH H H nh2 HI-21-5 ch3 H H CH2Ph 'Pr H ch3 F OH H H nh2 HI-21-6 ch3 H H CH2-indol-3-yl 'Pr H ch3 F OH H H nh2 III-21-7 ch3 H H CH2CH2SCH3 'Pr H ch3 F OH H H nh2 HI-21-8 ch3 * H ♦ 'Pr H ch3 F OH H H nh2 ♦R2 and RJb joined together by (0¾¼ to form five-membered ring.

Table III-22.

Xa R1 R2 r3b R3b Ίτ R3 R* X Y R7 R“ R4* HI-22-1 Et H H H Pr H CH3 F OH H H NH2 ΙΠ-22-2 Et H H ch3 Pr H ch3 F OH H H nh2 HI-22-3 Et H H CH(CH3)2 Pr H ch3 F OH H H nh2 IH-22-4 Et H H CH2CH(CH3)2 Pr H ch3 F OH H H nh2 IH-22-5 Et H H CH2Ph Pr H ch3 F OH H H nh2 ΠΙ-22-6 Et H H CH2-indol-3-yl Pr H ch3 F OH H H nh2 2983472-1 -132- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ns Rl ΊΓ R3a R3b R4 RJ R6 X Y R7 R8 R5 HI-22-7 Et H H CH2CH2SCH3 Jpr H ch3 F OH H H NH2 HI-22-8 j Et nib ' * H * 'Pr H ch3 F OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table ΠΙ-23.

Ns R1 R2 R3" IF R4 v R6 X Y R7 r“ R9 III-23-1 'Pr H H H 'Pr H ch3 F OH H H nh2 ΠΙ-23-2 'Pr H H ch3 'Pr H ch3 F OH Η H nh2 ΠΙ-23-3 'Pr H H CH(CH3)2 'Pr H ch3 F OH H H nh2 HI-23-4 'Pr H H CH2CH(CH3)2 'Pr H ch3 F OH H H nh2 ΙΠ-23-5 'Pr H H CH2Ph *Pr H ch3 F OH H H nh2 IU-23-6 'Pr H H CH2-indol-3-yl 'Pr H ch3 F OH Η Η nh2 HI-23-7 'Pr H H ch2ch2sch3 'Pr H ch3 F OH H H nh2 ΠΙ-23-8 J 'Pr * H * 'Pr H ch3 F OH H H nh2 ♦R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table III-24.

Ns Rl R2 R3‘ IF r4" R1 R6 X Y R7 R8 "ΪΤ IH-24-1 'Bu Η H H 'Pr Η ch3 F OH H H nh2 ΙΠ-24-2 <Bu H H ch3 Tr Η ch3 F OH H H nh2 HI-24-3 'Bu H H CHCCHah 'Pr Η ch3 F OH H H nh2 HI-24-4 'Bu H H CH2CH(CH3)2 Tr Η ch3 F OH H H nh2 HI-24-5 <Bu H H CH2Ph Tr Η ch3 F OH H H nh2 IH-24-6 'Bu H H CH2-indoI-3-yl 'Pr Η ch3 F OH H H nh2 HI-24-7 "Bu H H ch2ch2sch3 'Pr Η ch3 F OH H H nh2 IU-24-8 'Bu ♦ H * 'Pr Η ch3 F OH H H nh2 5 *R2 and RJb joined together by (GH2)3 to form five-membered ring.

Table ΠΙ-25.

Ns R1 R2 RJa 1F R4 R5 "R^ X Y R7 R8 Ry IH-25-1 Ph Η Η Η H ch3 F OH H H nh2 ΠΙ-25-2 Ph Η Η ch3 Tr H ch3 F OH H H nh2 ΙΠ-25-3 Ph Η Η ΟΗ(ΟΗ3)2 'Pr H ch3 F OH H H nh2 ΙΠ-25-4 Ph Η Η CH2CH(CH3)2 'Pr H ch3 F OH H H nh2 ΙΠ-25-5 Ph Η Η CH2Ph Tr H ch3 F OH H H nh2 IH-25-6 Ph Η Η CHa-indol-3-yl Tr H ch3 F OH H H nh2 III-25-7 Ph Η Η CH2CH2SCH3 Tr H ch3 F OH H H nh2 2983472-1 -133- WO 2008/121634 PCT/US2008/058183

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Rl R2 R3* R3b R4 R5 RA Χ^Ϋ R? R1* R9’ HI-25-8 Ph * H * 'Pr H CH3 F OH Η H NH2 *R2 and Rejoined together by (CH2)a to form five-membered ring.

Table III-26.

Ns T R2 ηρΓ- R4 R5 R6 X Y R7 Rs R9 III- 26-1 p-Me- Ph H H H H ch3 F OH H H NH2 III- 26-2 p-Me- Ph H H ch3 'Pr H ch3 F OH H H nh2 III- 26-3 p-Me- Ph H H CHCCHah 'Pr H ch3 F OH H H NH2 III- 26-4 p-Me- Ph H H CH2CH(CH3)2 'Pr H ch3 F OH H H nh2 III- 26-5 p-Me- Ph H H CH2Ph *Pr H ch3 F OH H H nh2 III- 26-6 p-Me- Ph H H CHi-indol-3- yi Pr H ch3 F OH H H nh2 III- 26-7 p-Me- Ph H H ch2ch2sch3 'Pr H ch3 F OH H H nh2 ΙΠ- 26-8 p-Me- Ph * H * 'Pr H ch3 F OH H H nh2 ♦R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table ΠΙ-27. Ns R1 r2 R3a R3b R4 RJ R6 X Y R7 R8 R9 IH-27- p-F-1 Ph H H H Pr H ch3 F OH H H nh2 HI-27- p-F-2 Ph H H ch3 'Pr H ch3 F OH H H nh2 HI-27- p-F-3 Ph H H CH(CH3)2 'Pr H ch3 F OH H H nh2 IH-27- p-F-4 Ph H H CH2CH(CH3)2 'Pr H ch3 F OH H H nh2 IH-27- p-F-S Ph H H CH2Ph 'Pr H ch3 F OH H H nh2 HI-27- p-F-Ph H H CH2-indol-3- 'Pr H ch3 F OH H H nh2 2983472-1 -134- WO 2008/121634 PCT/US2008/058183

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Ko ΊΤ”· R2 R3b R4 RJ R6 X Y R8 R9 6 yi III-27- 7 p-F- Ph H H ch2ch2sch3 'Pr H ch3 F OH H H nh2 ΙΠ-27- 8 p-F- Ph + H * 'Pr H ch3 F OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring

Table III-28. N° R* ϊΓ RJa R3b R4 RJ R6 X Y R' R R IH-28- p-Cl-1 Ph H H H 'Pr H ch3 F OH H H nh2 HI-28- p-Cl-2 Ph H H CH3 'Pr H ch3 F OH H H nh2 III-28- p-CI-3 Ph H H CH(CH3)2 'Pr H ch3 F OH H H nh2 III-28- p-CI-4 ph H H CH2CH(CH3)2 'Pr H ch3 F OH H H nh2 III-28- p-CI-5 Ph H H CH2Ph 'Pr H ch3 F OH H H nh2 HI-28- p-Cl-i Ph H H CH2-indol-3- yi 'Pr H ch3 F OH H H nh2 III-28- p-CI-7 Ph H H ch2ch2sch3 'Pr H ch3 F OH H H nh2 IU-28- p-Cl- 8 Ph ♦ H * /pr H ch3 F OH H H nh2 *R^ and RJb joined together by (CH2)3 to form five-membered ring.

Table 111-29. Ka R1 R2 Rj« RJb R4 R6 X Y R' R8 Ry HI-29- p-Br- 1 Ph H H Η *Pr H ch3 F OH H H NH2 HI-29- p-Br-2 Ph H H CH3 'Pr H ch3 F OH H H nh2 HI-29- p-Br-3 Ph H H CH(CH3)2 'Pr H ch3 F OH H H nh2 ΠΙ-29- p-Br- H H CH2CH(CH3)2 'Pr H ch3 F OH H H nh2

Ph 2983472-1 -135- WO 2008/121634 PCT/US2008/058183

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Ife R1 R2 R3’ "r36 - “ R'i R5 R^ X Y R7 Rs R^ 4 UI-29- p-Br-5 Ph H H CH2Ph 'Pr H ch3 F OH H H nh2 IH-29- p-Br- H H CH2-indol-3- 'Pr H ch3 F OH H H nh2 6 Ph yi IH-29- p-Br-7 Ph H H ch2ch2sch3 'Pr H ch3 F OH H H nh2 IH-29- p-Br- * H 4 ‘Pr H ch3 F OH H H nh2

Ph *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table IH-30.

Xs R1 R2 RJ< R3b R4 R5 R4 X Y r' r“ R9 ΠΙ-30- 1 p-I- Ph H H H "W Η ch3 F OH H H nh2 ΙΙΪ-30- 2 p-I- Ph Η H ch3 'pr H CHj F OH H H nh2 III-30- 3 p-I- Ph H H CH(CH3)2 'Pr H ch3 F OH H H nh2 HI-30- 4 p-I- Ph H H CH2CH(CH3)2 Tr H ch3 F OH H H nh2 III-30- 5 p-I- Ph H H CH2Ph 'Pr H ch3 F OH H H nh2 HI-30- 6 p-I- Ph H H CH2-indol-3- yi 'Pr H ch3 F OH H H nh2 III-30- 7 p-I- Ph H H ch2ch2sch3 fpr Η ch3 F OH H H nh2 HI-30- 8 p-I- Ph 4 H 4 Tr Η ch3 F OH H H nh2 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table HI -31. Xs R1 R2 R3‘ ""ή3® R4 R5 R6 X Y r’ R8 Ry iii-31-i ch3 H H H "Bu Η ch3 F OH Η H nh2 III-31-2 ch3 H H CH3 "Bu Η ch3 F OH H H nh2 IH-31-3 ch3 H H CH(CH3)2 "Bu Η ch3 F OH H H nh2 2983472-1 -136- WO 2008/121634 PCT/US2008/058183

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Ns R1 R2 Rjl TF " R4 Rs R6 X Y r" R8 R^ 1U-31-4 ch3 H H CH2CH(CH3)2 "Bu H ch3 F OH H H NH2 HI-31-5 ch3 H H CH2Ph "Bu H ch3 F OH H H nh2 ΙΠ-31-6 ch3 H H CH2-indol-3-yl "Bu H ch3 F OH H H nh2 HI-31-7 ch3 H H CH2CH2SCH3 "Bu H ch3 F OH H H nh2 ΙΠ-31-8 ch3 * H ♦ "Bu H ch3 F OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table ΠΙ-32.

Ns R R1 R3e R3b R4 R5 Rb X Y ΊΓ R8 R^ HI-32-1 Et H H H "Bu H CH3 F OH H H nh2 III-32-2 Et H H ch3 "Bu H ch3 F OH H H nh2 ΠΙ-32-3 Et H H CH(CH3)2 "Bu H ch3 F OH H H nh2 ΠΙ-32-4 Et H H CH2CH(CH3)2 "Bu H ch3 F OH H H nh2 HI-32-5 Et H H CH2Ph "Bu H ch3 F OH H H nh2 ΠΙ-32-6 Et H H CH2-indol-3-yl "Bu H ch3 F OH H H nh2 ΙΠ-32-7 Et H H CH2CH2SCH3 "Bu H ch3 F OH H H nh2 IH-32-8 Et * H * "Bu H ch3 F OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table III-33.

Ns R ΪΤ RJe R3b R4 R5 R6 X Y R7 R“ R9 IH-33-1 "ΤΓ H Η H "Bu H CH3 F OH H H NH2 III-33-2 'Pr Η H CH3 "Bu H ch3 F OH H H nh2 ΙΠ-33-3 'Pr H H CH(CH3)2 "Bu H ch3 F OH H H nh2 IH-33-4 'Pr H H CH2CH(CH3)2 "Bu H ch3 F OH H H nh2 ΠΙ-33-5 'Pr Η H CH2Ph "Bu H ch3 F OH H H nh2 ΙΠ-33-6 'Pr H H CH2-indol-3-yl "Bu H ch3 F OH H H nh2 ΠΙ-33-7 'Pr H H CH2CH2SCH3 "Bu H ch3 F OH H H nh2 ΠΙ-33-8 'Pr * H * "Bu H ch3 F OH H H NH2 5 *R'i and RJb joined together by to form five-membered ring. 2983472-1 -137- WO 2008/121634 PCT/US2008/058183

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Table III-34. X9 T” R2 R3a I?b R4 R5 R6 X Y R7 Ra R9 ΙΠ-34-1 ‘Bu H H H "Bu H ch3 F OH H H nh2 ΠΙ-34-2 'Bu H H ch3 "Bu H ch3 F OH H H nh2 ΠΙ-34-3 'Bu H H CH(CH3)2 "Bu H ch3 F OH H H nh2 ΙΠ-34-4 *Bu H H CH2CH(CH3)2 "Bu H ch3 F OH H H nh2 ΙΠ-34-5 'Bu H H CH2Ph "Bu H ch3 F OH H H nh2 III-34-6 T8u H H CH2-indol-3-yl "Bu H ch3 F OH H H nh2 III-34-7 'Bu H H CH2CH2SCH3 "Bu H ch3 F OH H H nh2 ΠΙ-34-8 'Bu ♦ H * "Bu H ch3 F OH H H nh2 *RZ and R3b joined together by (CH2)3 to form five-membered ring.

Table III-35. M Ί?~ R2 r’· R3b R4 Rs R* X Y ΤΓ R^ ΙΠ-35-1 Ph H H H "Bu H ch3 F OH H H nh2 ΙΠ-35-2 Ph H H ch3 "Bu H ch3 F OH H H nh2 III-35-3 Ph H H CH(CH3)2 "Bu H ch3 F OH H H nh2 III-35-4 Ph H H CH2CH(CH3)2 "Bu H ch3 F OH H H nh2 UI-35-5 Ph H H CHaPh "Bu H ch3 F OH H H nh2 ΠΙ-35-6 Ph H H CH2-indol-3-yl "Bu H ch3 F OH H H nh2 1II-35-7 Ph H H CH2CH2SCH3 "Bu H ch3 F OH H H nh2 ΙΠ-35-8 Ph * H * "Bu H ch3 F OH H H nh2 *RZ and R3b joined together by (CH2)3 to form five-membered ring. 5 Table III-36.

— 'Γ — H ' " " '"»1 — J------- J .T” . R

Ks R‘ R2 R3. R3b R R5 Rfi X Y RJ R" R^ III- 36-1 p-Me- H Ph H H "Bu H CH3 F OH H H nh2 III- 36-2 p-Me- H Ph H CH3 "Bu H ch3 F OH H H nh2 ΙΠ- 36-3 p-Me- H Ph H CH(CH3)2 "Bu H ch3 F OH H H nh2 III- 36-4 p-Me- H Ph H CH2CH(CH3)2 "Bu H ch3 F OH H H nh2 ΠΙ- 36-5 p-Me- H Ph H CH2Ph "Bu H ch3 F OH H H nh2 in- p-Me- H H CH2-indol-3- "Bu H ch3 F OH H H nh2

Ph 2983472-1 -138 - WO 2008/121634 PCT/US2008/058183

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Xs R* R2 R3a R3b R^ R6 X Y R R1 R^ 36-6 yl in- p-Me- H H ch2ch2sch3 "Bu H ch3 F OH H H NH2 36-7 Ph III- p-Me- * H * "Bu H ch3 F OH H H nh2 36-8 Ph . r,3b · ; *RZ and R3b joined together by (CH2)3 to form five-membered ring.

Table III-37.

Xa R1 “R2- "r35" "R36 R4 R5 ΊΤ" X Y R7 R8 R^ III- 37-1 p-F- Ph H H H "Bu H ch3 F OH H H NH2 III- 37-2 p-F- Ph H H ch3 "Bu H ch3 F OH H H nh2 III- 37-3 p-F- Ph H H CH(CH3)2 "Bu H ch3 F OH H H nh2 III- 37-4 p-F- Ph H H CH2CH(CH3)2 "Bu H ch3 F OH H H nh2 III- 37-5 p-F- Ph H H CH2Ph "Bu H ch3 F OH H H nh2 III- 37-6 p-F- Ph H H CH2-indol-3- yi "Bu H ch3 F OH H H nh2 III- 37-7 p-F- Ph H H CH2CH2SCH3 "Bu H ch3 F OH H H NH2 III- 37-8 p-F- Ph « H * "Bu H ch3 F OH H H nh2 *RZ and R3b joined together by (0¾^ to form five-membered ring.

Table III-38. Xa Rl R2 RJa Rjt, R5 R6 X Y ΊΓ R' III- 38-1 p-Cl- Ph Η H Η "Bu H CH3 F OH H H nh2 ΙΠ- 38-2 p-Cl- Ph H H ch3 "Bu H ch3 F OH H H nh2 III- 38-3 p-Cl- Ph Η H CHiCH^ "Bu H ch3 F OH H H nh2 III- p-Cl- Η H CH2CH(CH3)2 "Bu H ch3 F OH H H nh2

Ph 2983472-1 -139- WO 2008/121634 PCT/US2008/058183

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Na R* “ΊΓ -pr R4 Rs Ί? '' X Y “R7· R* R9 38-4 III- p-Cl- H H CH2Ph "Bu H ch3 F OH H H nh2 38-5 Ph III- p-CI- H H CH2-indol-3- "Bu H ch3 F OH H H nh2 38-6 Ph yi III- p-Cl- H H ch2ch2sch3 "Bu H ch3 F OH H H nh2 38-7 Ph in- p-Cl- * H * "Bu H ch3 F OH H H nh2 38-8 Ph *R2 and R3b joined together by (CH^a to form five-membered ring.

Table III-39.

Ns R1 R2 RjB R3” R4 R5 R® X Y R’ R“ R9 III- 39-1 p-Br- Ph H H H "Bu H ch3 F OH H H NH2 III- 39-2 p-Br- Ph H H ch3 "Bu H ch3 F OH H H nh2 III- 39-3 p-Br- Ph H H CHCCH^ "Bu H ch3 F OH H H nh2 III- 39-4 p-Br- Ph H H CH2CH(CH3)2 "Bu H ch3 F OH H H nh2 III- 39-5 p-Br- Ph H H CH2Ph "Bu H ch3 F OH H H nh2 III- 39-6 p-Br- Ph H H CH2-indol-3- yi "Bu H ch3 F OH H H nh2 III- 39-7 p-Br- Ph H H ch2ch2sch3 "Bu H ch3 F OH H H nh2 III- 39-8 p-Br- Ph * H * "Bu H ch3 F OH H H nh2 *R and R joined together by (CHfe^ to form five-membered ring.

Table III-40. Ns R1 R1 RJa R3b R4 R5 R6 X Y R7 R” R* HI-40- 1 p-I- Ph Η Η Η "Bu Η ch3 F OH H H NH2 111-40- p-I- Ph Η Η ch3 "Bu Η ch3 F OH H H nh2 2983472-1 -140- WO 2008/121634 PCT/US2008/058183

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Rs R1 R2 R3a "R35 R4 Rs R6 X Y r’ r“ iv 2 III-40- p-I- H H CH(CH3)2 "Bu H ch3 F OH H H nh2 3 Ph HI-40- p-I- H H CH2CH(CH3)2 "Bu H ch3 F OH H H nh2 4 Ph IH-40- p-I- H H CH2Ph "Bu H ch3 F OH H H nh2 5 Ph III-40- p-I- H H CH2-indol-3- "Bu H ch3 F OH H H nh2 6 Ph yi ΙΠ-40- p-I- H H ch2ch2sch3 "Bu H ch3 F OH H H nh2 7 Ph III-40- p-I- * H * "Bu H ch3 F OH H H nh2 8 Ph *R2 and Rejoined together by (0¾^ to form, five-membered ring.

Table III-41.

Rs R1 R2 R3® R3b "R4” ΊΓ R6 X Y R2 R* R* III-41-1 ch3 H H H Bz H ch3 F OH H H nh2 HI-41-2 ch3 H H ch3 Bz H ch3 F OH H H nh2 ΙΠ-41-3 ch3 H H CHCCH,), Bz H ch3 F OH H H nh2 IH-41-4 ch3 H H ΟΗ,ΟΗζΟΗ,Η Bz H ch3 F OH H H nh2 ΙΠ-41-5 ch3 H H CH2Ph Bz H ch3 F OH H H nh2 ΙΠ-41-6 ch3 H H CH2-indol-3-yl Bz H ch3 F OH H H nh2 ΙΠ-41-7 ch3 H H CH2CH2SCH3 Bz H ch3 F OH H H nh2 IU-41-8 ch3 ♦ H * Bz H ch3 F OH H H nh2 *R2 and Rejoined together by (CH2)3 to form Five-membered ring.

Table ΙΠ-42.

Rs R R2 rJb R36 R5 R6 X Y Ic RB R^ ΙΠ-42-1 Et Η Η Η Bz H CH3 F OH H H nh2 HI-42-2 Et H Η ch3 Bz H ch3 F OH H H nh2 HI-42-3 Et Η Η CHiCH,), Bz H ch3 F OH H H nh2 HI-42-4 Et Η Η CH2CH(CH3)2 Bz H ch3 F OH H H nh2 ΠΙ-42-5 Et Η Η CH2Ph Bz H ch3 F OH H H nh2 UI-42-6 Et Η Η CH2-indol-3-yl Bz H ch3 F OH H H nh2 ΙΠ-42-7 Et Η Η ch2ch2sch3 Bz H ch3 F OH H H nh2 2983472-1 141- WO 2008/121634

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Ns Rl R2 R3" Έ5 r’™ R5 I?-· X Y I? Ic R^ III-42-8 Et * H * Bz H ch3 F OH H H NH2 *R2 and RJb joined together by (CH2)3 to form five-membered ring. Table III-43. Xa R R2 R3· R3b R4 R5 R6 X Y R7 R11 Ry III-43-1 'Pr H H H Bz H ch3 F OH H H nh2 IH-43-2 'Pr H H ch3 Bz H ch3 F OH H H nh2 III-43-3 'Pr H H CH(CH3)2 Bz H ch3 F OH H H nh2 ΙΠ-43-4 'Pr H H CH2CH(CH3)2 Bz H ch3 F OH H H nh2 ΠΙ-43-5 'Pr H H CH2Ph Bz H ch3 F OH H H nh2 I1I-43-6 'Pr H H CH2-indol-3-yl Bz H ch3 F OH H H nh2 III-43-7 'Pr H H ch2ch2sch3 Bz H ch3 F OH H H nh2 HI-43-8 'pr * H * Bz H ch3 F OH H H nh2 *R2 and RJb joined together by (CHah to form five-membered ring.

Table III-44. Xa R R2 r3. R3b III-44-1 'Bu H H H ΙΙΪ-44-2 'Bu. H H ch3 ΙΠ-44-3 H H CH(CH3)2 III-44-4 'Bu H H CH2CH(CH3)2 111-44-5 'Bu H H CH2Ph ΪΙΙ-44-6 'Bu H H CH2-indol-3-yl IH-44-7 'Bu H H CH2CH2SCH3 HI-44-8 'Bu * H * R4 r! R6 X Y R7 r“ "R7” Bz H CH3 F OH H H nh2 Bz H ch3 F OH H H nh2 Bz H ch3 F OH H H nh2 Bz H ch3 F OH H H nh2 Bz H ch3 F OH H H nh2 Bz H ch3 F OH H H nh2 Bz H ch3 F OH H H nh2

Bz H CH3 F OH Η H NH2 *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2933472-1 -142- PCT/US2008/058183 WO 2008/121634

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Table III-45.

Ns R1 R3 -jpr- T?” R5 IF” X Y R7 r“ R9 III-45-1 Ph H H H Bz H ch3 F OH H H nh2 ΙΠ-45-2 Ph H H ch3 Bz H ch3 F OH H H nh2 III-45-3 Ph H H CH(CH3)2 Bz H ch3 F OH H H nh2 III-45-4 Ph H H CH2CH(CH3)2 Bz H ch3 F OH H H nh2 ΙΠ-45-5 Ph H H CH2Ph Bz H ch3 F OH H H nh2 ΙΠ-45-6 Ph H H CH2-indol-3-yl Bz H ch3 F OH H H nh2 ΙΠ-45-7 Ph H H CH2CH2SCH3 Bz H ch3 F OH H H nh2 III-45-8 Ph * H * Bz H ch3 F OH H H nh2 *RZ and Rejoined together by (CH2)3 to form five-membered ring.

Table III-46.

Na R1 R3 RJl R3b R4 R* R6 X Y R' R“ R^ III- p-Me- Η H H Bz H CH3 F OH H H NH2 46-1 Ph III- p-Me- H H ch3 Bz H ch3 F OH H H nh2 46-2 Ph III- p-Me- H H CH(CH3)2 Bz H ch3 F OH H H nh2 46-3 Ph III- p-Me- H H CH2CH(CH3)2 Bz H ch3 F OH H H NH2 46-4 Ph III- p-Me- H H CH2Ph Bz H ch3 F OH H H NH2 46-5 Ph in- p-Me- H H CH2-indol-3- Bz H ch3 F OH H H nh2 46-6 Ph yi III- p-Me- H H CH2CH2SCH3 Bz H ch3 F OH H H nh2 46-7 Ph ΠΙ- p-Me- 4 H Bz H ch3 F OH H H nh2 46-8 Ph *R< and RJb joined togeth er by (0¾^ to form five- memfc lered ring. Tabl e IU-47. Ns R1 R* r35" “r35 R4 R3 R6 X Y R7 Ru R9 ΙΠ-47- 1 p-F- Ph Η Η H Bz H ch3 F OH H H NH2 ΙΠ-47- p-F- Ph H H ch3 Bz Η ch3 F OH H H nh2 2983472-1 -143- WO 2008/121634 PCT/US2008/058183

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Xa R1 R2 k3i R3b Rs X Y R7 R! R9 2 HI-47- p-F- H H CH(CH3)2 Bz H CH3 F OH H H NH2 3 Ph HI-47- p-F- H H CH2CH(CH3)2 Bz H ch3 F OH H H nh2 4 Ph HI-47- p-F- H H CHjPh Bz H ch3 F OH H H nh2 5 Ph IH-47- p-F- H H CH2-indol-3- Bz H ch3 F OH H H nh2 6 Ph yi HI-47- p-F- H H ch2ch2sch3 Bz H ch3 F OH H H nh2 7 Ph IH-47- p-F- * H * Bz H ch3 F OH H H nh2

Ph *R2 and RJb joined together by (0¾^ to form five-membered ring.

Table 111-48.

Xa R1 R2 R’· R3b R1* RJ R6 X Y ΊΓ Ra R5^ HI- 48-1 p-Cl- Ph H H H Bz H CH3 F OH H H NH2 III- 48-2 p-Cl- Ph H H ch3 Bz H ch3 F OH H H nh2 IH- 48-3 p-Cl- Ph H H CH(CH3)2 Bz H ch3 F OH H H nh2 IU- 48-4 p-CI- Ph H H CH2CH(CH3)2 Bz H ch3 F OH H H nh2 III- 48-5 p-Cl- Ph H H CH2Ph Bz H ch3 F OH H H nh2 ΙΠ- 48-6 p-Cl- Ph H H CH2-indol-3- yt Bz H ch3 F OH H H nh2 III- 48-7 p-CI- Ph H H CH2CH2SCH3 Bz H ch3 F OH H H nh2 III- 48-8 p-Cl- Ph .□nJb·'·' * H ♦ Bz H ch3 F OH H H nh2 ♦I? and Rejoined together by (Cthk to form five-membered ring. 2983472-1 -144- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table III-49.

Ks R1 R2 RJa R3b R3 R6 X Y R7 R“ R5^ III- 49-1 p-Br- Ph H H H Bz H ch3 F OH H H nh2 III- 49-2 p-Br- Ph H H ch3 Bz H ch3 F OH H H nh2 III- 49-3 p-Br- Ph H H CHCCHah Bz H ch3 F OH H H nh2 III- 49-4 p-Br- Ph H H CH2CH(CH3)2 Bz H ch3 F OH H H nh2 III- 49-5 p-Br- Ph H H CH2Ph Bz H ch3 F OH H H nh2 III- 49-6 p-Br- Ph H H CH2-indol-3- yi Bz H ch3 F OH H H nh2 III- 49-7 p-Br- Ph H H ch2ch2sch3 Bz H ch3 F OH H H nh2 III- p-Br- ♦ H * Bz H ch3 F OH H H nh2 *R2 and R36 joined together by (CH2)3 to form five-membered ring.

Table III-50.

Ka R1 R2 Rj« R3b R4 R3 R6 X Y R7 R8 iC ΠΙ-50- 1 p-I- Ph Η Η Η Bz H ch3 F OH H H NH2 III-50- 2 p-I- Ph H Η ch3 Bz H ch3 F OH H H nh2 ΠΙ-50- 3 p-I- Ph Η Η ΟΗ(ΟΗ3)2 Bz H ch3 F OH H H nh2 ΠΙ-50- 4 p-I- Ph Η Η CH2CH(CH3)2 Bz H ch3 F OH H H nh2 ΠΙ-50- 5 p-I- Ph Η Η CH2Ph Bz H ch3 F OH H H nh2 ΙΠ-50- 6 p-I- Ph Η Η CH2-indol-3- yi Bz H ch3 F OH H H nh2 ΙΠ-50- 7 p-I- Ph Η Η ch2ch2sch3 Bz H ch3 F OH H H nh2 ΙΠ-50- p-I- * Η * Bz H ch3 F OH H H nh2 2983472-1 -145- WO 2008/121634

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Nb R1 R2 R30 R3b S’ R5 R6 X Y R7 R“ R9 8 Ph *R2 and R3b joined together by (0¾¼ to form five-membered ring. R9

Table IV-1.

Ns R1 R31 -jpE R4 RJ R6 X Y r’ R8 R9 IV-1-1 ch3 H H H ch3 H F F OH H H NH2 IV-1-2 ch3 H H ch3 ch3 H F F OH H H nh2 IV-1-3 ch3 H H CH(CH3)2 ch3 H F F OH H H nh2 IV-1-4 ch3 H H CH2CH(CH3)2 ch3 H F F OH H H nh2 1V-1-5 ch3 H H CH2Ph ch3 H F F OH H H nh2 IV-1-6 ch3 H H CH2-indol-3-yl ch3 H F F OH H H nh2 IV-1-7 ch3 H H ch2ch2sch3 ch3 H F F OH H H nh2 IV-1-8 _ ch3 . r»3b: * H * ch3 H F F OH H H nh2 *R2 and RJt> joined together by (CH2)3 to form five-membered ring.

Table IV-2.

Ns R R2 R3’ R3b R4 Rs R4 X Υ R7 ΊΓ "S’” IV-2-1 Et H H H ch3 Η F F ΟΗ Η Η νη2 IV-2-2 Et H H ch3 ch3 Η F F ΟΗ Η Η νη2 IV-2-3 Et H H CH(CH3)2 ch3 Η F F ΟΗ Η Η νη2 IV-2-4 Et H H CH2CH(CH3)2 ch3 Η F F ΟΗ Η Η νη2 IV-2-5 Et H H CH2Ph ch3 Η F F ΟΗ Η Η νη2 IV-2-6 Et H H CH2-indol-3-yI ch3 Η F F ΟΗ Η Η νη2 IV-2-7 Et H H CH2CH2SCH3 ch3 Η F F ΟΗ Η Η νη2 2983472-1 -146- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 x° R1 R2 "r5- 1F~ R4 v X Y IV R*" 1V-2-8 Et * H ♦ ch3 H F F OH H H nh2 *R2 and R3b joined together by (CH2)3 to form five-membered ring. Table IV-3. Ns R R2 R3* "r36 R4 RJ R* X Y R7 Ra Ry IV-3-1 'Pr H H H ch3 H F F OH H H nh2 IV-3-2 'Pr H H ch3 ch3 H F F OH H H nh2 1V-3-3 'Pr H H CH(CH3)2 ch3 H F F OH H H nh2 IV-3-4 ipr H H CH2CH(CH3)2 ch3 H F F OH H H nh2 IV-3-5 'Pr H H CH2Ph ch3 H F F OH H H nh2 IV-3-6 ’Pr H H CH2-indol-3-yl ch3 H F F OH H H nh2 IV-3-7 'Pr H H CH2CH2SCH3 ch3 H F F OH H H nh2 1V-3-8 'pr * H * ch3 H F F OH H H nh2 *R2 and R3b joined together by ((¾^ to form five-membered ring.

Table IV-4. N° Rl R2 rU. R3b R4 r! R6 X Y R7 RB ΊΤ" IV-4-1 'Bu H H H ch3 Η ch3 F OH H H NH2 IV-4-2 'Bu H H ch3 ch3 Η ch3 F OH H H nh2 IV-4-3 H H CH(CH3)2 ch3 Η ch3 F OH H H nh2 IV-4-4 'Bu H H CH2CH(CH3)2 ch3 Η ch3 F OH H H nh2 IV-4-5 'Bu H H CH2Ph ch3 Η ch3 F OH H H nh2 IV-4-6 'Bu H H CH2-indol-3-yl ch3 Η ch3 F OH H H nh2 IV-4-7 'Bu H H CH2CH2SCH3 ch3 Η ch3 F OH H H nh2 IV-4-8 'Bu · * H * ch3 Η ch3 F OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -147- WO 2008/121634 PCT/US2008/058183

Docket No. 6013 7.0034WOU1

Table IV-5.

Ns R1 R12 "r35" R3b r5" R6 X Y r" Ra R9 IV-5-1 Ph H H H ch3 H F F OH H H nh2 IV-5-2 Ph H H ch3 ch3 H F F OH H H nh2 IV-5-3 Ph H H CH(CH3)2 ch3 H F F OH H H nh2 IV-5-4 Ph H H CH2CH(CH3)2 ch3 H F F OH H H nh2 IV-5-5 Ph H H CH2Ph ch3 H F F OH H H nh2 IV-5-6 Ph H H CH2-indol-3-yl ch3 H F F OH H H nh2 IV-5-7 Ph H H CH2CH2SCH3 ch3 H F F OH H H nh2 IV-5-8 Ph * H. ♦ ch3 H F F OH H H nh2 *R3 and Rejoined together by (CH2)3 to form five-membered ring.

Table IV-6.

Ns Rl R3 r3‘ R3b R^ Rs R6 X Y R7 R“ R5 IV-6- 1 p-Me- Ph H H H CH3 H F F OH H H NH2 IV-6- 2 p-Me- Ph H H ch3 ch3 H F F OH H H nh2 IV-6- 3 p-Me- Ph H H CHiCHjh ch3 H F F OH H H nh2 IV-6- 4 p-Me- Ph H H CH2CH(CH3)2 ch3 H F F OH H H nh2 IV-6- 5 p-Me- Ph H H CH2Ph ch3 H F F OH H H nh2 IV-6- 6 p-Me- Ph H H CH2-indol-3- yi ch3 H F F OH H H nh2 IV-6- 7 p-Me- Ph H H CH2CH2SCH3 ch3 H F F OH H H nh2 IV-6- 8 p-Me- Ph ♦ H * ch3 H F F OH H H nh2 ♦R2 and R3b joined together by (0¾^ to fotm five-membered ring.

Table IV-7. Ns Rl R3 R3* R3b R4 R5 R6 X Y R7 R" R9 IV-7-1 p-F- Ph H H H ch3 H F F OH H H nh2 IV-7-2 p-F- Ph H H ch3 ch3 H F F OH H H nh2 IV-7-3 p-F- H H CH(CH3)z ch3 H F F OH H H nh2 2983472-1 -148- WO 2008/121634 PCT/US2008/058183

Docket No, 60137.0034WOU1 to R1 lc r3. Rib r! R6 X Y R“ R^ IV-7-4 Ph p-F- H H CH2CH(CH3)2 ch3 H F F OH H H NH2 IV-7-6 Ph p-F- H H CH2Ph ch3 H F F OH H H nh2 IV-7-7 Ph p-F- H H CH2-indol-3- ch3 H F F OH H H nh2 IV-7-8 Ph p-F- H H yi ch2ch2sch3 ch3 H F F OH H H nh2 IV-7- Ph p-F- * H * ch3 H F F OH H H nh2 *R2 and RJb joined together by (0¾¼ to form five-membered ring.

Table IV-8.

Xs Rl ir R3a Rib R4 Rs R6 X Y r" R# IV-8- 1 p-CI- Ph H H H ch3 Η F F OH H H NH2 IV-8- 2 p-Cl- Ph H H CH3 ch3 H F F OH H H nh2 IV-8- 3 p-Cl- Ph H H CH(CH3)2 ch3 H F F OH H H nh2 IV-8- 4 p-Cl- Ph H H CH2CH(CH3)2 ch3 H F F OH H H nh2 IV-8- 5 p-Cl- Ph H H CH2Ph ch3 H F F OH H H nh2 IV-8- 6 p-Cl- Ph H H CH2-indol-3- yi ch3 H F F OH H H nh2 rv-8- 7 p-Cl- Ph H H CH3CH2SCH3 ch3 H F F OH H H nh2 IV-8- 8 p-Cl- Ph * H * ch3 H F F OH H H nh2 ♦R2 and R30 joined together by (0¾¼ to form five-membered ring.

Table IV-9. Xs R R2 R3b R3b R4 Rs R° X Y R7 R” R9 IV-9-1 p-Br- Ph H H H ch3 H F F OH H H NH2 IV-9-2 p-Br- Ph Η H ch3 ch3 H F F OH H H nh2 , 2983472-1 -149- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 "R1 R2 r3. R35 R4 Rs R6 X Y R7 R8 R’"" IV-9-3 p-Br- Ph H H CH(CH3)2 ch3 H F F OH H H nh2 IV-9-4 p-Br- Ph H H CH2CH(CH3)2 ch3 H F F OH H H nh2 IV-9-6 p-Br- Ph H H CH2Ph ch3 H F F OH H H nh2 IV-9-7 p-Br- Ph H H CH2-indol-3- yi ch3 H F F OH H H nh2 IV-9-8 p-Br- Ph H H ch2ch2sch3 ch3 H F F OH H H nh2 IV-9- 20 p-Br- Ph * H * ch3 H F F OH H H nh2 *R2 and Rejoined together by (CHjb to form five-membered ring.

Table IV-10.

Wa R' R2 r3. R3b ΊΤ- RJ R6 X Y R7 R8 1^“ IV-10- p-I- H H Η ch3 H F F OH H H nh2 1 Ph IV-10- p-I- H H ch3 ch3 H F F OH H H nh2 2 Ph IV-10- p-I- H Η CHCCHa), ch3 H F F OH H. H nh2 3 Ph IV-10- p-I- Η Η CH2CH(CH3)2 ch3 H F F OH H H nh2 , 4 Ph IV-10- p-I- H Η CH2Ph ch3 H F F OH H H nh2 5 Ph IV-10- p-I- H Η CH2-indol-3- ch3 H F F OH H H nh2 6 Ph yi IV-10- p-I- H Η ch2ch2sch3 ch3 H F F OH H H nh2 7 Ph IV-10- p-I- * Η * ch3 H F F OH H H nh2 8 Ph *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table IV-11. R R2 R3· R3b R4 R5 R6 X Y R7 R8 R5 IV-11-1 ch3 H Η H Et H F F OH H H NH2 IV-11-2 ch3 H Η ch3 Et Η F F OH H H nh2 2983472-1 -150- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ns R1 R2 "r35" "R* R4 RJ R6 X Y ΊΓ Rb IV-11-3 ch3 H H CH(CH3)2 Et H F F OH H H nh2 IV-11-4 ch3 H H CH2CH(CH3)2 Et H F F OH H H nh2 IV-11-5 ch3 H H CH2Ph Et H F F OH H H nh2 IV-11-6 ch3 H H CH2-indol-3-yl Et H F F OH H H nh2 IV-11-7 ch3 H H CH2CH2SCH3 Et H F F OH H H nh2 IV-11-8 ♦ _ , ch3 ,RJb· * H * Et H F F OH H H nh2 IJ UL· *R and R joined together by (CH2)3 to form five-membered ring.

Table IV-12. Ns R1 R2 Rj. R3’ R4 R5 R4 X Y R7 Rb R5 IV-12-1 Et H H H Et H F F OH H H nh2 IV-12-2 Et H H CH3 Et H F F OH H H nh2 IV-12-3 Et H H CHfCHah Et H F F OH H H nh2 IV-12-4 Et H H CH2CH(CH3)2 Et H F F OH H H nh2 IV-12-5 Et H H CH2Ph Et H F F OH H H nh2 IV-12-6 Et H H CH2-indol-3-yl Et H F F OH H H nh2 IV-12-7 Et H H CH2CH2SCH3 Et H F F OH H H nh2 IV-12-8 Et * H * Et H F F OH H H nh2 *R2 and Rejoined together by (CHjfe to form five-membered ring.

Table IV-13.

Ns R1 R2 RJ. R3b R4 Rs R4 X Y R/ Rb R5 IV-13-1 'Pr H H H Et H F F OH H H nh2 IV-13-2 'Pr H H ch3 Et H F F OH H H nh2 JV-13-3 'Pr H H CHfCH^ Et H F F OH H H nh2 IV-13-4 'Pr H H CH2CH(CH3)2 Et H F F OH H H nh2 IV-13-5 'Pr H H CH2Ph Et H F F OH H H nh2 IV-13-6 'Pr H H CH2-indol-3-yl Et H F F OH H H nh2 IV-13-7 Ψγ H H CH2CH2SCH3 Et H F F OH H H nh2 IV-13-8 ipr * H ♦ Et H F F OH H H nh2 5 *R4 and Rejoined together by (CH2)3 to form five-membered ring.

Table IV-14.

Ns R1 R2 R Rdb 3a R4 R3 R6 X Y R7 R8 Ry IV-14- Η Η H Et H F F OH Η Η NH2 1 »83472-1 -151- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 R1 R2 R 3o ηρε R4 Rs R6 X Y "R7- R8 R9 IV-14- 2 'Bu H H ch3 Et H F F OH H H NH2 IV-14- 3 'Bu H H CH(CH3)2 Et H F F OH H H nh2 IV-14- 4 'Bu H H CH2CH(CH3)2 Et H F F OH H H nh2 IV-14- 5 'Bu H H CH2Ph Et H F F OH H H nh2 1V-14- 6 'Bu H H CH2-indol-3-yl Et H F F OH H H nh2 IV-14- 7 'Bu H H CH2CH2SCH3 Et H F F OH H H nh2 IV-14- 8 'Bu * H * Et H F F OH H H nh2 *R* and RJb joined together by (CH2)3 to form five-membered ring.

Table IV-15.

Ks R R2 R3· R4 Rs R6 X Y R7 R8 ~r5 IV-15-1 Ph Η Η Η Et H F F OH H H nh2 IV-15-2 Ph Η Η ch3 Et H F F OH H H nh2 IV-15-3 Ph Η Η CH(CH3)2 Et H F F OH H H nh2 IV-15-4 Ph Η Η CH2CH(CH3)2 Et H F F OH H H nh2 IV-15-5 Ph Η Η CH2Ph Et H F F OH H H nh2 IV-15-6 Ph Η Η CH2-indol-3-yl Et H F F OH H H nh2 IV-15-7 Ph Η Η CH2CH2SCH3 Et H F F OH H H nh2 IV-15-8 Ph * Η * Et H F F OH H H nh2 *R2 and RJb joined together by to form five-membered ring.

Table IV-16.

Ks R1 R2 RJa R3t. R4 R5 Rs X Y ΊΓ r^ r5^ IV-16- 1 p-Me- Ph H Η H Et H F F OH H H nh2 IV-16- 2 p-Me- Ph H H ch3 Et H F F OH H H nh2 IV-16- p-Me- Η H ΟΗ(ΟΗ3)2 Et H F F OH H H nh2

Ph 2983472-1 -152- WO 2008/121634

Docket No. 60137.0034WOU I PCT/US2008/058183 R1 R2 R3a R3b R4 RJ R4 X Y R7 ΊΓ 3 IV-16- p-Me- H H CH2CH(CH3)2 Et H F F OH H H nh2 4 Ph IV-16- p-Me- H H CH2Ph Et H F F OH H H nh2 5 Ph IV-16- p-Me- H H CHrindol-3- Et H F F OH H H nh2 6 Ph yi IV-16- p-Me- H H ch2ch2sch3 Et H F F OH H H nh2 7 Ph IV-16- p-Me- ♦ H * Et H F F OH H H nh2 8 Ph 1 n3O : : *R^ and Rejoined together by (CH2)a to form five-membered ring.

Table IV-17.

Ns Rl R2 jpr "r35 R4 i? R6 X Y R7 R8 r9" 1V-17-1 p-F-Ph H H H Et H F F OH H H nh2 IV-17-2 p-F-Ph H H ch3 Et H F F OH H H nh2 IV-17-3 p-F-Ph H H CH(CH3)i Et H F F OH H H nh2 IV-17-4 p-F-Ph H H CH2CH(CH3)2 Et H F F OH H H nh2 IV-17-5 p-F-Ph H H CH2Ph Et H F F OH H H nh2 IV-17-6 p-F-Ph H H CH2-indol-3-yl Et H F F OH H H nh2 IV-17-7 p-F-Ph H H CH2CH2SCH3 Et H F F OH H H nh2 IV-17-8 p-F-Ph * H * Et H F F OH H H nh2 *R2 and R^^joined together by (CH2)3 to form fivermembered ring.

TableIV-18.

Rl R: R R3b R4 Ic R6 X Y R7 RV IV-18- 1 p-Cl- Ph Η Η Η Et H F F OH H H nh2 IV-18- 2 p-Cl- Ph Η Η ch3 Et H F F OH H H nh2 IV-18- 3 p-Cl- Ph Η Η ΟΗ(ΟΗ3)2 Et H F F OH H H nh2 IV-18- 4 p-Cl- Ph Η Η CH2CH(CH3)2 Et H F F OH H H nh2 1V-18- p-Cl- Η Η CH2Ph Et H F F OH H H nh2

Ph 2983472-1 -153- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Ns r1 R2 r3‘ R3b R4 R5 R6 X Y R7 R1 I? 5 IV-18- p-Cl- H H CH2-indot-3- Et H F F OH H H NH2 6 Ph yi IV-18- p-Cl- H H ch2ch2sch3 Et H F F OH H H nh2 7 Ph IV-18- p-Cl- ♦ H * Et H F F OH H H nh2

Ph *R2 and RJb joined together by (CFI2)3 to form five-membered ring.

Table IV-19.

Ns Rl R2 R3“ R3b R4 r! R6 X Y R7 R9™ IV-19- 1 p-Br- Ph H H H Et H F F OH H H nh2 IV-19- 2 p-Br- Ph H H CH3 Et H F F OH H H nh2 IV-19- 3 p-Br- Ph H H CHfCHah Et H F F OH H H nh2 IV-19- 4 p-Br- Ph H H CH2CH(CH3)2 Et H F p OH H H nh2 IV-19- 5 p-Br- Ph H H CH2Ph Et H F F OH H H nh2 IV-19- 6 p-Br- Ph H H CH2-indol-3- y! Et H F F OH H H nh2 IV-19- 7 p-Br- Ph H H CH2CH2SCH3 Et H F F OH H H nh2 IV-19- 8 p-Br- Ph * H . * Et H F F OH H H nh2 *R2 and R3D joined together by (CHbb to form five-membered ring.

Table IV-20. Ns R‘ R1 RJ‘ R3b R4 R5 R6 X Y ΊΓ R1 R9^ IV-20-1 p-I-Ph H H H Et H F F OH H H NH2 IV-20-2 p-I-Ph H H CH3 Et H F F OH H H nh2 IV-20-3 p-I-Ph H H CH(CH3)2 Et H F F OH H H nh2 IV-20-4 p-I-Ph H H CH2CH(CH3)2 Et H F F OH H H nh2 IV-20-5 p-I-Ph H H CH2Ph Et H F F OH H H nh2 2983472-1 -154- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 K9 R1 R2 r3. R3b R4 RJ R6 X Y R7 R8 R5 IV-20-6 p-I-Ph H H CH2-indol-3-yl Et H F F OH H H nh2 IV-20-7 p-I-Ph H H CH2CH2SCH3 Et H F F OH H H nh2 IV-20-8 p-I-Ph * H * Et H F F OH H H nh2 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table IV-21.

Jfe R1 R2 R3a R3b r34" Rs R6 X Y R7 r“ R9 IV-21-1 CH3 H H H 'Pr H F F OH H H nh2 IV-21-2 ch3 H H ch3 'Pr H F F OH H H nh2 IV-21-3 ch3 H H CH(CH3)a 'Pr H F F OH H H nh2 IV-21-4 ch3 H H CH2CH(CH3)2 'Pr H F F OH H H nh2 IV-21-5 ch3 H H CH2Ph 'Pr H F F OH H H nh2 IV-21-6 ch3 H H CH2-indol-3-yl 'Pr H F F OH H H nh2 IV-21-7 ch3 H H CH2CH2SCH3 'Pr H F F OH H H nh2 IV-21-8 ch3 * H * 'Pr H F F OH H H nh2 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table IV-22. R1 R2 r35" ”r3B R4 R3 r6 X Y R7 R" R9 IV-22-1 Et H H H 'Pr H F F OH H H NH2 IV-22-2 Et H H CH3 'Pr H F F OH H H nh2 1V-22-3 Et Η H CH(CH3)2 'Pr H F F OH H H nh2 IV-22-4 Et H H CHjCHCCH^ 'Pr H F F OH H H nh2 IV-22-5 Et H H CH2Ph 'Pr H F F OH H H nh2 rv-22-6 Et H H CH2-indol-3-yl 'Pr H F F OH H H nh2 IV-22-7 Et H H CH2CH2SCH3 'Pr H F F OH H H nh2 IV-22-8 Et * H * 'Pr H F F OH H H nh2 5 *R2 and RJb joined together by (0¾^ to form five-membered ring.

Table IV-23. X2 R R2 RJl R3b R4 Rs R6 X Y R7 R8 R9 IV-23-1 'Pr H H H ίρΓ H F F OH H H nh2 IV-23-2 *Pr H H ch3 'Pr H F F OH H H nh2 IV-23-3 'Pr H H CH(CH3)2 'Pr H F F OH H H nh2 IV-23-4 *Pr H H CH2CH(CH3)2 'Pr H F F OH H H nh2 IV-23-5 'Pr H H CH2Ph 'Pr H F F OH H H nh2 IV-23-6 'Pr H H CH2-indoI-3-yI 'Pr H F F OH H H nh2

I 2983472-1 -155- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 R' R2 R36 R5 R6 X Y R7"" R*~ IV-23-7 'Pr H H ch2ch2sch3 'Pr H F F OH H H nh2 IV-23-8 'Pr * H * 'Pr H F F OH H H nh2 *R2 and Rejoined toge ther by (CH2)3t o form five-m lembered ring. Table 1V-24. R1” R2 R3i “TF5 R4 R1 R6 X Y r’ r“ Ry IV-24-1 'Bu H H H H F F OH H H NH2 IV-24-2 'Bu H H ch3 'Pr H F F OH H H nh2 IV-24-3 'Bu H H CH(CH3)2 'Pr H F F OH H H nh2 IV-24-4 'Bu H H CH2CH(CH3)2 'Pr H F F OH H H nh2 IV-24-5 'Bu H H CH2Ph 'Pr H F F OH H H nh2 IV-24-6 'Bu H H CH2-indol-3-yl 'Pr H F F OH H H nh2 IV-24-7 'Bu H H CH2CH2SCH3 'Pr H F F OH H H nh2 IV-24-8 'Bu * H « 'Pr H F F OH H H nh2 *R2 and RJD joined toge sther by (CH2)31 o form five-membered ring. Table IV-25. "jfe R7” R2. R3· "r35 R4 R5 R6 X Y R7 r“ Ry IV-25-1 Ph H H H 'Pr H F F OH H H NH2 IV-25-2 Ph H H ch3 'Pr H F F OH H H nh2 IV-25-3 Ph H H CH(CH3)2 'Pr H F F OH H H nh2 IV-25-4 Ph H H CH2CH(CH3)2 'Pr H F F OH H H nh2 IV-25-5 Ph H H CH2Ph 'Pr H F F OH H H nh2 IV-25-6 Ph H H CH2-indol-3-yl 'Pr H F F OH H H nh2 IV-25-7 Ph H H CH2CH2SCH3 'Pr H F F OH H H nh2 IV-25-8 Ph * H * 'Pr H F F OH H H nh2 *R^ and RJb joined together by (Ctfeb to form five-membered ring.

Table IV-26.

Na . R1 R2 r3b R3b R4 R5 R6 X Y Ic r“ R^ IV-26- 1 p-Me- Ph H H H ^r H F F OH H H nh2 IV-26- 2 p-Me- Ph H H CH3 'Pr H F F OH H H nh2 IV-26- 3 p-Me- Ph H H CHCCHah 'Pr H F F OH H H nh2 IV-26- p-Me- H H CH2CH(CH3)2 'Pr H F F OH H H nh2 2983472-1 -156- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ns Rl "F" F^ F5 R4 F" F~ X Y r" F F 4 Ph IV-26- 5 p-Me- Ph H H CHjPh 'Pr H F F OH H H nh2 IV-26- 6 p-Me- Ph H H CH2-indol-3- yi 'Pr H F F OH H H nh2 IV-26- 7 p-Me- Ph H H ch2ch2sch3 'Pr H F F OH H H nh2 IV-26- p-Me- * H * 'Pr H F F OH H H nh2

Ph *R2 and Rejoined together by (Cltk to form five-membered ring.

Table IV-27.

Ns R' F" F1- R3b R4 Rs R4 X Y F~ R8 "IT IV-27-1 p-F-Ph H H H FT H F F OH H H NH2 IV-27-2 p-F-Ph H H CH3 'Pr H F F OH H H nh2 IV-27-3 p-F-Ph H H CH(C%)2 'Pr H F F OH H H nh2 IV-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr H F F OH H H nh2 IV-27-5 p-F-Ph H H CH2Ph 'Pr H F F OH H H nh2 IV-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr H F F OH H H nh2 IV-27-7 p-F-Ph H H CH2CH2SCH3 'Pr H F F OH H H nh2 IV-27-8 p-F-Ph * H * 'Pr H F F OH H H nh2 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table IV-28.

Ns F- R2 R3a R3b r Rs R4 X Y F" F^ IV-28- 1 p-Cl- Ph H H H /Pr Η F F OH H H NH2 IV-28- 2 p-Cl- Ph H H ch3 'Pr H F F OH H H nh2 1V-28- 3 p-Cl- Ph H H CH(CH3)j 'Pr H F F OH H H nh2 IV-28- 4 p-Cl- Ph H H CH2CH(CH3)2 'Pr H F F OH H H nh2 IV-28- 5 p-Cl- Ph H H CH2Ph 'Pr H F F OH H H nh2 IV-28- p-Cl- H H CH2-indol-3- 'Pr H F F OH H H nh2

Ph 2983472-1 - 157- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Ns R1 “ΊΓ R3‘~ ~R* R5 "R®- X Y R7 Ra R9 6 yi IV-28- 7 p-Cl- Ph H H ch2ch2sch3 fPr H F F OH H H NH2 IV-28- 8 p-Cl- Ph * H * 'Pr H F F OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table IV-29.

Ns Rl "ΤΓ R3" "iV Rs R* X Y ΊΓ r“ R9 IV-29- 1 p-Br- Ph H H H H F F OH H H nh2 IV-29- 2 p-Br- Ph H H ch3 'Pr H F F OH H H nh2 IV-29- 3 p-Br- Ph H H CH(CH3)2 'Pr H F F OH H H nh2 IV-29- 4 p-Br- Ph H H CH2CH(CH3)2 'Pr H F F OH H H nh2 1V-29- S p-Br- Ph H H CH2Ph 'Pr H F F OH H H NHZ IV-29- 6 p-Br- Ph H H CH2-indol-3- yt 'Pr H F F OH H H nh2 IV-29- 7 p-Br- Ph H H CH2CH2SCH3 'Pr H F F OH H H nh2 IV-29- p-Br- ♦ H * 'Pr H F F OH H H nh2

Ph *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table IV-30.

Ns R1 R2 "r35" jps— RJ R6 X Y R7 Rtt R · IV-30-1 p-I-Ph H H Η Jpr H F F OH H H NHa IV-30-2 p-I-Ph Η H ch3 'Pr H F F OH H H nh2 IV-30-3 p-I-Ph H H ΟΗ(ΟΗ3)2 'Pr H F F OH H H nh2 IV-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr H F F OH H H nh2 IV-30-5 p-I-Ph H Η CH2Ph 'Pr H F F OH H H nh2 IV-30-6 p-I-Ph H Η CH2-indol-3-yl Tr H F F OH H H nh2 IV-30-7 p-I-Ph H Η CH2CH2SCH3 'Pr H F F OH H H nh2 2983472-1 -158- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Ns R1 R2 R3b R5b RJ R6 X Y r^ R8 1V-30-8 p-I-Ph * H * Ψ7 H F F OH H H nh2 *R2 and Rejoined together by (CHhb to form five-membered ring. Table IV-31. N° R Rz R3a R36 R4 R5 R6 X Y R7 R8 Ry IV-31-1 ch3 Η H H "Bu H F F OH H H NH2 IV-31-2 ch3 Η H ch3 "Bu H F F OH H H nh2 IV-31-3 ch3 Η H CH(CH3)2 "Bu H F F OH H H nh2 IV-31-4 ch3 Η H CH2CH(CH3)2 "Bu H F F OH H H nh2 IV-31-5 ch3 Η H CH2Ph "Bu H F F OH H H nh2 IV-31-6 ch3 Η H CH2-indol-3-yl "Bu H F F OH H H nh2 IV-31-7 ch3 Η H CH2CH2SCH3 "Bu H F F OH H H nh2 IV-31-8 —τ ch3 Ti3b"7~ * H * "Bu H F F OH H H nh2 *R2 and Rejoined together by (CF^b to form five-membered ring.

Table IV-32.

Ns R1 R2 “r33" R3b R4 p" R6 X Y ΤΓ R** R9 IV-32-1 Et H Η Η "Bu H F F OH H H NH2 IV-32-2 Et H Η ch3 "Bu H F F OH H H nh2 IV-32-3 Et H Η CHfCH,), "Bu H F F OH H H nh2 IV-32-4 Et Η Η CH2CH(CH3)2 "Bu H F F OH H H nh2 IV-32-5 Et Η Η CH2Ph "Bu H F F OH H H nh2 IV-32-6 Et Η Η CH2-indol-3-yl "Bu H F F OH H H nh2 IV-32-7 Et Η Η CH2CH2SCH3 "Bu H F F OH H H nh2 IV-32-8 Et * Η * "Bu H F F OH H H nh2 5 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table IV-33.

Ns R1 ΊΓ R3’ R3b R4 R5 R6 X Y R7 R8 R9 IV-33-1 ipr H H H "Bu H F F OH H H NH2 IV-33-2 'Pr Η Η CH3 "Bu H F F OH H H nh2 IV-33-3 /pr H H CH(CH3>2 "Bu H F F OH H H nh2 IV-33-4 'Pr H Η CH2CH(CH3)2 "Bu H F F OH H H nh2 IV-33-5 ’Pr H H CH2Ph "Bu H F F OH H H nh2 IV-33-6 'Pr H H CH2-indol-3-yl "Bu H F F OH H H nh2 IV-33-7 /Pr H H CH2CH2SCH3 "Bu H F F OH H H nh2 IV-33-8 'Pr * Η * "Bu H F F OH H H nh2 2983472-1 -159- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table IV-34.

Xs R1 R2 r^ R3b ΊΤ" RJ X Y R7 R5" ΊΓ" IV-34-1 'Bu H H H "Bu H F F OH H H nh2 IV-34-2 'Bu H H ch3 "Bu H F F OH H H nh2 IV-34-3 'Bu H H CH(CH3)2 "Bu H F F OH H H nh2 IV-34-4 'Bu H H CH2CH(CH3)2 "Bu H F F OH H H nh2 IV-34-5 'Bu H H CH2Ph "Bu H F F OH H H nh2 IV-34-6 'Bu H H CH2-indol-3-yl "Bu H F F OH H H nh2 IV-34-7 H H CH2CH2SCH3 "Bu H F F OH H H nh2 IV-34-8 'Bu * H * "Bu H F F OH H H nh2 *R2 and R3b joined together by (CHab to form five-membered ring.

Table IV-35.

Xs R1 R2 r3‘ R3b R4 "r5" R6 X Y R7 R“ IV-35-1 Ph Η H H "Bu H F F OH H H nh2 IV-35-2 Ph H H ch3 "Bu H F F OH H H nh2 IV-35-3 Ph H H CH(CH3)2 "Bu H F F OH H H nh2 IV-35-4 Ph H H CH2CH(CH3)2 "Bu H F F OH H H nh2 IV-35-5 Ph H H CH2Ph "Bu H F F OH H H nh2 IV-35-6 Ph H H CH2-indol-3-yl "Bu H F F OH H H nh2 IV-35-7 Ph H H CH2CH2SCH3 "Bu H F F OH H H nh2 IV-35-8 Ph * H ♦ "Bu H F F OH H H nh2 5 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table IV-36.

Xs R1 R2 R3b R4 RJ R6 X Y R7 R8 R^ IV- 36-1 p-Me- Ph H H H "Bu H F F OH H H nh2 IV- 36-2 p-Me- Ph Η H CH3 "Bu H F F OH H H nh2 IV- 36-3 p-Me- Ph H H CH(CH3)2 "Bu H F F OH H H nh2 IV- 36-4 p-Me- Ph H H CH2CH(CH3)2 "Bu Η F F OH H H nh2 IV- p-Me- H H CH2Ph "Bu Η F F OH H H nh2 2983472-1 -160- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Ns ΊΓ R2 "r^ r35 R4 RJ R6 X Y R9 IV- p-Me- H H CH2-indol-3- "Bu H F F OH H H NH2 36-6 Ph yi IV- p-Me- H H ch2ch2sch3 "Bu H F F OH H H nh2 36-7 Ph IV- p-Me- * H * "Bu H F F OH H H nh2 36-8 Ph *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table IV-37.

Ns R1 R2 R3’ r35- ΊΤ- R5 R6 X Y r" r“ R^ IV-37- 1 p-F- Ph Η Η Η "Bu H F F OH H H nh2 IV-37- 2 p-F- Ph Η Η ch3 "Bu H F F OH H H nh2 IV-37- 3 p-F- Ph Η Η CH(CH3)2 "Bu H F F OH H H nh2 IV-37- 4 p-F- Ph Η Η CH2CH(CH3)2 "Bu H F F OH H H nh2 IV-37- 5 p-F- Ph Η Η CH2Ph "Bu H F F OH H H hh2 IV-37- 6 p-F- Ph Η Η CH2-indol-3- yi "Bu H F F OH H H nh2 IV-37- 7 p-F- Ph Η Η CH2CH2SCH3 "Bu H F F OH H H nh2 IV-37- 8 p-F- Ph * Η * "Bu H F F OH H H nh2 ♦R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table IV-38. Ns R1 R2 RJa R3b R* RJ R6 X Y R7 R8 R9 IV-38- 1 p-Cl- Ph H Η H "Bu H F F OH H H nh2 1V-38- 2 p-Cl- Ph H H CH3 "Bu H F F OH H H nh2 IV-38- p-Cl- Η H CHiCHah "Bu H F F OH H H nh2 3 Ph 2983472-1 -161- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1 x° R1 R2 r3‘ R3b RJ R4 X Y r" r“ RJ IV-38- 4 p-Cl- Ph H H CH2CH(CH3)2 "Bu H F F OH H H nh2 IV-38- 5 p-Cl- Ph H H CH2Ph "Bu H F F OH H H nh2 IV-38- 6 p-Cl- Ph H H CH2-indol-3- yi "Bu H F F OH H H nh2 IV-38- 7 p-Cl- Ph H H ch2ch2sch3 "Bu H F F OH H H nh2 IV-38- p-Cl- * H * "Bu H F F OH H H nh2

Ph *R2 and RJb joined together by (Cl^b to form five-membered ring.

Table IV-39. R1 “ir R3b R4 RJ R4 X Y I? r“ Ic IV-39- 1 p-Br- Ph Η H H "Bu H F F OH H H nh2 IV-39- 2 p-Br- Ph H H ch3 "Bu Η F F OH H H nh2 IV-39- 3 p-Br- Ph H H CH(CH3)2 "Bu H F F OH H H nh2 IV-39- 4 p-Br- Ph H H CH2CH(CH3)2 "Bu H F F OH H H nh2 IV-39- 5 p-Br- Ph H H CH2Ph "Bu H F F OH H H nh2 IV-39- 6 p-Br- Ph H H CH2-indol-3- yi "Bu H F F OH H H nh2 IV-39- 7 p-Br- Ph H H ch2ch2sch3 "Bu H F F OH H H nh2 IV-39- 8 p-Br- Ph * H ♦ "Bu H F F OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table IV-40. Ka R1 R2 R3a R3b R4 Rs R4 X Y R' Re Ry IV-40- p-I- H H H "Bu H F F OH H H NH2 2983472-1 -162- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ms ΊΓ"”'" “IF R3a “Η35 R4 R5 Rb X Y ~r7 R8 If IV-40- p-I- H H ch3 flBu H F F OH H H NH2 2 Ph IV-40- p-I- H H CH(CH3)2 ”Bu H F F OH H H nh2 3 Ph IV-40- p-I- H H CH2CH(CH3)2 "Bu H F F OH H H nh2 4 Ph IV-40- p-I- H H CH2Ph "Bu H F F OH H H nh2 5 Ph IV-40- p-I- H H CH2-indoI-3- "Bu H F F OH H H nh2 6 Ph yi IV-40- p-I- H H CH2CH2SCH3 "Bu H F F OH H H nh2 7 Ph IV-40- p-I- * H ♦ "Bu H F F OH H H nh2 8 Ph *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table IV-41.

Ms R1 R2 "r35 "r4- R5 R6 X Y R7 p- Ff IV-41-1 ch3 H H H Bz H F F OH H H nh2 IV-41-2 ch3 H H ch3 Bz H F F OH H H nh2 IV-41-3 ch3 H H CHCCHa), Bz H F F OH H H nh2 IV-41-4 ch3 H H CH2CH(CH3)2 Bz H F F OH H H nh2 IV-41-5 ch3 H H CH2Ph Bz H F F OH H H nh2 IV-41-6 ch3 H H CH2-indol-3-yl Bz H F F OH H H nh2 IV-41-7 ch3 H H CH2CH2SCH3 Bz H F F OH H H nh2 IV-41-8 ch3 * H * Bz H F F OH H H nh2 *R2 and RJb joined together by (ΟΗ2)3 to form five-membered ring.

Table IV-42.

Ms R R2 RJa R3b R4 Rs R6 X Y If Rs R9 IV-42-1 Et Η Η Η Bz H F F OH H H NH2 IV-42-2 Et H Η ch3 Bz H F F OH H H nh2 IV-42-3 Et Η Η CHCCHah Bz H F F OH H H nh2 IV-42-4 Et Η Η CH2CH(CH3)2 Bz H F F OH H H nh2 IV-42-5 Et Η Η CH2Ph Bz H F F OH H H nh2 IV-42-6 Et Η Η CH2-indoI-3-yl Bz H F F OH H H nh2 2983472-1 -163- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Ns R1 R2 R3a R3b R4 r5- R5 X Y r’ r“ IV-42-7 Et H H ch2ch2sch3 Bz H F F OH H H NH2 IV-42-8 Et * H * Bz H F F OH H H nh2 *R2 and RJb joined together by (CFhb to form five-membered ring.

Table IV-43.

Xa R1 R2 R3a R3b R4 RJ R6 X Y r’ r“ R5 IV-43-1 'Pr H H H Bz H F F OH H H nh2 IV-43-2 'Pr H H ch3 Bz H F F OH H H nh2 IV-43-3 'Pr H H CH(CH3)2 Bz H F F OH H H nh2 IV-43-4 'Pr H H CH2CH(CH3)2 Bz H F F OH H H nh2 IV-43-5 'Pr H H CH2Ph Bz H F F OH H H nh2 IV-43-6 'Pr H H CH2-indol-3-yl Bz H F F OH H H nh2 IV-43-7 'Pr H H CH2CH2SCH3 Bz H F F OH H H nh2 IV-43-8 'Pr * H * Bz H F F OH H H nh2 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table 1V-44. X° Rl R3 -r3T "R36 R4 Rs R6 X Y R7 R# R^ IV-44-1 'Bu H H H Bz H F F OH H H nh2 IV-44-2 'Bu H H CH3 Bz H F F OH H H nh2 IV-44-3 'Bu H H CH(CH3)2 Bz H F F OH H H nh2 IV-44-4 'Bu H H CH2CH(CH3)2 Bz H F F OH H H nh2 IV-44-5 'Bu H H CH2Ph Bz H F F OH H H nh2 IV-44-6 'Bu H H CH2-indol-3-yl Bz H F F OH H H nh2 IV-44-7 'Bu H H CH2CH2SCH3 Bz H F F OH H H nh2 IV-44-8 'Bu * H * Bz H ’ F F OH H H nh2 5 *R2 and R3 6 joined together by (CH2)3 to form five-membered ring.

Table IV-45.

Xa R R3 rJ. R3b R4 RJ R6 X Y r' r“ R9 IV-45-1 Ph Η H H Bz H F F OH H H nh2 IV-45-2 Ph H H ch3 Bz H F F OH H H nh2 IV-45-3 Ph H H CHCCH,^ Bz H F F OH H H nh2 IV-45-4 Ph H H CH2CH(CH3)2 Bz H F F OH H H nh2 IV-45-5 Ph H H CH2Ph Bz H F F OH H H nh2 IV-45-6 Ph H H CH2-indol-3-yl Bz H F F OH H H nh2 IV-45-7 Ph H H CH2CH2SCH3 Bz H F F OH H H nh2 2983472-) -164- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Xa "r1- R2 R3b R3b R4 Rs R6 X Y R7 R8 Ry 1V-45-8 Ph * H * Bz H F F OH II H NH2 *R2 and Rejoined together by (C 1-12)3 to form five-membered ring.

Table IV-46. Xa R1 RJ RJa R3b R4 R5 R° X Y R7 R8 Ry IV-46- 1 p-Me- Ph H H H Bz H F F OH H H nh2 IV-46- 2 p-Me- Ph H H ch3 Bz H F F OH H H nh2 IV-46- 3 p-Me- Ph H H CH(CH3)2 Bz H F F OH H H nh2 IV-46- 4 p-Me- Ph H H CH2CH(CH3)2 Bz H F F OH H H nh2 IV-46- 5 p-Me- Ph H H CH2Ph Bz H F F OH H H nh2 IV-46- 6 p-Me- Ph H H CH2-indol-3- yi Bz H F F OH H H nh2 IV-46- 7 p-Me- Ph H H ch2ch2sch3 Bz H F F OH H H nh2 IV-46- p-Me- * H * Bz H F F OH H H nh2

Ph *R2 and Rejoined together by to form five-membered ring.

Table IV-47.

Xa R1 R3 r3« R3b R4 Rs R6 X Y R7 R“ R9 IV-47- 1 IV-47- 2 p-F-Ph H H H Bz H F F OH H H nh2 p-F-Ph H H ch3 Bz H F F OH H H nh2 IV-47- 3 p-F-Ph H H CHCCH,), Bz H F F OH H H nh2 IV-47- 4 p-F-Ph H H CH2CH(CH3)2 Bz H F F OH H H nh2 IV-47- c p-F-Ph H H CH2Ph Bz H F F OH H H nh2 3 IV-47- p-F-Ph H H CH2-indol-3-yl Bz H F F OH H H nh2 2983472-1 -165- PCT/US2008/058183 WO 2008/121634 ΛΛη ,„,ΛΤΤ,

Docket No. 60137.0034WOU1 X° R1 R2 -jpr- R4 Rs R5” X Y ΊΓ R’ R9 6 IV-47- p-F-Ph H H ch2ch2sch3 Bz H F F OH H H nh2 7 IV-47- p-F-Ph * H * Bz H F F OH H H nh2 8 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table IV-48.

Xs R1 R2 r3« "IP® R4 Rs IC X Y R7 R“ f? IV-48- 1 p-Cl- Ph H H H Bz H F F OH H H NH2 IV-48- 2 p-Cl- Ph H H CH3 Bz H F F OH H H nh2 IV-48- 3 p-Cl- Ph H H CH(CH3)2 Bz H F F OH H H nh2 IV-48- 4 p-Cl- Ph H H CH2CH(CH3)2 Bz H F F OH H H nh2 IV-48- 5 p-CI- Ph H H CH2Ph Bz H F F OH H H nh2 IV-48- 6 p-Cl- Ph H H CH2-indol-3- yi Bz H F F OH H H nh2 IV-48- 7 p-Cl- Ph H H CH2CH2SCH3 Bz H F F OH H H nh2 IV-48- 8 p-Cl- Ph * H * Bz H F F OH H H nh2 *R2 and RJb joined together by (CLtys to form five-membered ring.

Table IV-49. Xs R R2 Rj. R3b R* R3 R6 X Y R7 R* R9 IV-49- 1 p-Br- Ph Η Η Η Bz H F F OH H H nh2 IV-49- 2 p-Br- Ph H Η ch3 Bz H F F OH H H nh2 IV-49- 3 p-Br- Ph Η Η CHfCH^ Bz H F F OH H H nh2 IV-49- p-Br- H Η CH2CH(CH3)2 Bz H F F OH H H nh2

Ph 2983472-1 -166- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 K2 Rl R2 Ria -p; R4 Rs R6 X Y r’ r“ 4 IV-49- p-Br- H H CHiPh Bz H F F OH H H nh2 5 Ph IV-49- p-Br- H H CH2-indol-3- Bz H F F OH H H nh2 6 Ph yi IV-49- p-Br- H H ch2ch2sch3 Bz H F F OH H H nh2 7 Ph IV-49- p-Br- * H * Bz H F F OH H H nh2

Ph *R2 and Rejoined together by (CH2)3t0 form five-membered ring.

Table 1V-50. X2 R1 R4 RJa R3b R4 Rs R6 X Y R7 R8 R* IV-50-1 p-I-Ph Η Η Η Bz H F F OH H H NH2 IV-50-2 p-l-Ph Η Η ch3 Bz H F F OH H H NH2 IV-50-3 p-I-Ph Η Η CH(CH3)2 Bz H F F OH H H nh2 IV-50-4 p-l-Ph Η Η CH2CH(CH3)2 Bz H F F OH H H nh2 IV-50-5 p-I-Ph Η Η CH2Ph Bz H F F OH H H nh2 IV-50-6 p-I-Ph Η Η CH2-indol-3-yl Bz H F F OH H H nh2 IV-50-7 p-I-Ph Η Η CH2CH2SCH3 Bz H F F OH H H nh2 IV-50-8 *r»2 j p-I-Ph r»3b’· · * Η ♦ Bz H F F OH H H nh2 *R^ and Rejoined together by (CH2)3 to form five-membered ring.

V 2983472-1 -167- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Table V-l.

Ns R1 R2 "r37" -jpb R4 Rs R6 X Y r’ rb R9 V-l-1 ch3 H H H ch3 H H F OH H H nh2 V-l-2 ch3 H H ch3 ch3 H H F OH H H nh2 V-l-3 ch3 H H CH(CH3)2 ch3 H H F OH H H nh2 V-l-4 ch3 H H CH2CH(CH3)2 ch3 H H F OH H H nh2 V-l-5 ch3 H H CH2Ph ch3 H H F OH H H nh2 V-l-6 ch3 H H CH2-indol-3-yl ch3 H H F OH H H nh2 V-l-7 ch3 H H ch2ch2sch3 ch3 H H F OH H H nh2 V-l-8 __ ch3 . r.3b' * H ♦ ch3 H H F OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table V-2.

Ns Rl R2 r3b “P— R4 ΊΓ R6 X Υ R7 R* R9^ V-2-1 Et H H H ch3 H Η F ΟΗ Η Η ΝΗ2 V-2-2 Et H H CH3 ch3 Η Η F ΟΗ Η Η νη2 V-2-3 Et H H ORCH^ ch3 Η Η F ΟΗ Η Η νη2 V-2-4 Et H H CH2CH(CH3)2 ch3 Η Η F ΟΗ Η Η νη2 V-2-S Et Η H CH2Ph ch3 Η Η F ΟΗ Η Η νη2 V-2-6 Et H H CH2-indol-3-yl ch3 Η Η F ΟΗ Η Η νη2 V-2-7 Et H H CH2CH2SCH3 ch3 Η Η F ΟΗ Η Η νη2 V-2-8 Et * H * ch3 Η Η F ΟΗ Η Η νη2 *R2 and RJb joined together by (0-12)3 to form five-membered ring.

Ns R1 R2 -jpr "r35 R4 r3- R6 X Y R7 Ru R9 V-3-1 -ρΓ H H H ch3 H H F OH H H NH2 V-3-2 'Pr H H ch3 ch3 H H F OH H H nh2 V-3-3 'Pr H H CH(CH3)2 ch3 H H F OH H H nh2 V-3-4 'Pr H H CH2CH(CH3)2 ch3 H H F OH H H nh2 V-3-5 'Pr H H CH2Ph ch3 H H F OH H H nh2 V-3-6 'Pr H H CH2-indol-3-yl ch3 H H F OH H H nh2 V-3-7 'Pr H H CH2CH2SCH3 ch3 H H F OH H H nh2 V-3-8 — 'Pr * > ! · H * ch3 H H F OH H H nh2 *R2 and Re joined together by (CKbb to form five-membered ring. 2983472-1 -168- WO 2008/121634No^ 6θ137Λ034Μ)υι PCT/US2008/058183

Table V-4.

Xa R1 R2 r3« R^ R4 R5 R* X Y R7 R“ Ry V-4-1 'Bu H H H ch3 H H F OH H H NH2 V-4-2 'Bu H H ch3 ch3 H H F OH H H nh2 V-4-3 'Bu H H CHiCHs^ ch3 H H F OH H H nh2 V-4-4 'Bu H H CH2CH(CH3)2 ch3 H H F OH H H nh2 V-4-5 'Bu H H CH2Ph ch3 H H F OH H H nh2 V-4-6 'Bu H H CHrindol-3-yl ch3 H H F OH H H nh2 V-4-7 'Bu H H ch2ch2sch3 ch3 H H F OH H H nh2 V-4-8 'Bu ♦ H * ch3 H H F OH H H nh2 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table V-5.

Xs R1 R2 R3’ RJb R1 R3 R6 X Y R7 Rs R^ V-5-1 Ph H H H CH3 H H F OH H H nh2 V-5-2 Ph H H CH3 ch3 H H F OH H H nh2 V-5-3 Ph H H CH(CH3)2 ch3 H H F OH H H nh2 V-5-4 Ph H H CH2CH(CH3)2 ch3 H H F OH H H nh2 V-5-5 Ph H H CH2Ph ch3 H H F OH H H nh2 V-5-6 Ph H H CH2-indol-3-yl ch3 H H F OH H H nh2 V-5-7 Ph H H CH2CH2SCH3 ch3 H H F OH H H nh2 V-5-8 Ph * H * ch3 H H F OH H H nh2 *R2 and R3b joined together by (0¾)^ to form five-membered ring. 5 Table V-6. " 1 "Τ'" I- ' ""Ί-1 22^1....... J T.......... ............- a n

Xa R1 R2 RJ“ R3b R* R5 R6 X Y R7 R8 R^ V-6- 1 p-Me- Ph Η Η Η ch3 Η H F OH H H nh2 V-6- 2 p-Me- Ph Η Η ch3 ch3 H H F OH H H nh2 V-6- 3 p-Me- Ph Η Η CH(CH3)i ch3 H H F OH H H nh2 V-6- 4 p-Me- Ph Η Η CH2CH(CH3)2 ch3 H H F OH H H nh2 V-6- 5 p-Me- Ph Η Η CH2Ph ch3 H H F OH H H nh2 V-6- p-Me- Η Η CH2-indol-3- ch3 H H F OH H H nh2

Ph 2983472-1 -169- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Ns r’ R2 R3a R3b R4 RJ R6 X Y R7 R# Ry 6 yi V-6- p-Me- H H ch2ch2sch3 ch3 H H F OH H H nh2 7 Ph V-6- p-Me- * H * ch3 H H F OH H H nh2

Ph *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table V-7.

Ns R* IP" r^ R4 ψ" R* X Υ r7- ΊΓ R9 V-7-1 p-F- Ph H H H ch3 Η Η F ΟΗ Η Η νη2 V-7-2 p-F- Ph H H ch3 ch3 Η Η F ΟΗ Η Η νη2 V-7-3 p-F- Ph H H CH(CH3)2 ch3 Η Η F ΟΗ Η Η νη2 V-7-4 p-F- Ph H H CH2CH(CH3)2 ch3 Η Η F ΟΗ Η Η νη2 V-7-6 p-F- Ph H H CH2Ph ch3 Η Η F ΟΗ Η Η νη2 V-7-7 p-F- Ph H H CH2-indol-3- yi ch3 Η Η F ΟΗ Η Η νη2 V-7-8 p-F- Ph H H CH2CH2SCH3 ch3 Η Η F ΟΗ Η Η νη2 V-7- 20 p-F- Ph ♦ H * ch3 Η Η F ΟΗ Η Η νη2 *R2 and R3” joined together by (CH2)3 to form five-membered ring.

Table V-8. Ns Rl RJ RJa R3b R4 rs R* X Y R7 R* R^ V-8- 1 p-Cl- Ph H H H ch3 H H F OH H H NH2 V-8- 2 p-Cl- Ph H H ch3 ch3 H H F OH H H nh2 V-8- 3 p-Cl- Ph H H CH(CH3)2 ch3 H H F OH H H nh2 V-8- 4 p-Cl- Ph H H CH2CH(CH3)2 ch3 H H F OH H H nh2 V-8- p-Cl- H H CH2Ph ch3 H H F OH H H nh2 2983472-1 -170- WO 2008/121634 PCT/US2008/058183

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Ns R' R2 “r35" R3” Ί7- RJ R6 X Y R rb 7 V-8- 6 p-Cl- Ph H H CH2-indol-3- yi ch3 H H F OH H H nh2 V-8- 7 p-Cl- Ph H H ch2ch2sch3 ch3 H H F OH H H nh2 V-8- 8 *n'2 p-Cl- Ph . J t ! * H * ch3 H H F OH H H nh2 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table V-9.

Ns R1 R2 -£rr -p; R4 R5 R4 X Υ Ra Τ” V-9-1 p-Br- Ph Η H H ch3 Η Η F ΟΗ Η Η ΝΗ2 V-9-2 p-Br- Ph H H ch3 ch3 Η Η F ΟΗ Η Η νη2 V-9-3 p-Br- Ph H H CHCCHah ch3 Η Η F ΟΗ Η Η νη2 V-9-4 p-Br- Ph H H CH2CH(CH3)2 ch3 Η Η F ΟΗ Η Η νη2 V-9-6 p-Br- Ph H H CH2Ph ch3 Η Η F ΟΗ Η Η νη2 V-9-7 p-Br- Ph H H CH2-indol-3- yi ch3 Η Η F ΟΗ Η Η νη2 V-9-8 p-Br- Ph H H CH2CH2SCH3 ch3 Η Η F ΟΗ Η Η νη2 V-9- p-Br- * H * ch3 Η Η F ΟΗ Η Η νη2 *R2 and R30 joined together by (CH2)3 to form five-membered ring.

Table V-10.

Ns R1 R2 "R33" R3b R4 Rs R4 X Y R’ R8 R3 V-10-1 p-1-Ph Η Η Η ch3 H H F OH H H NH2 V-10-2 p-1-Ph Η Η ch3 ch3 H H F OH H H nh2 V-10-3 p-1-Ph Η Η CH(CH3)2 ch3 H H F OH H H nh2 V-10^4 p-1-Ph Η Η CH2CH(CH3)2 ch3 H H F OH H H nh2 V-10-5 p-1-Ph Η Η CH2Ph ch3 H H F OH H H nh2 V-10-6 p-1-Ph Η Η CH2-indol-3-yl ch3 H H F OH H H nh2 V-10-7 p-1-Ph Η Η CH2CH2SCH3 ch3 H H F OH H H nh2 V-10-8 , p-1-Ph . «3b· · « Η ♦ ch3 H H F OH H H nh2 *R2 and RJb joined together by (Ctbb to form five-membered ring. 2983472-1 -171- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table V-ll.

Xs Rl RJ "R35 R4 Rs R6 X Y r“ R^ V-ll-l CH3 H H H Et H H F OH H H NH2 V-ll-2 ch3 H H ch3 Et H H F OH H H nh2 V-1I-3 ch3 H H CH(CH3)2 Et H H F OH H H nh2 V-ll-4 ch3 H H CH2CH(CH3)2 Et H H F OH H H nh2 V-ll-5 ch3 H H CH2Ph Et H H F OH H H nh2 V-ll-6 ch3 H H CH2-indol-3-yl Et H H F OH H H nh2 V-ll-7 ch3 H H CH2CH2SCH3 Et H H F OH H H nh2 V-ll-8 ch3 * H * Et H H F OH H H nh2 *R2 and R3b joined together by to form five-membered ring

Table V-12.

Xs R R2 rJ. R3b R4 Rs R6 X Y R7 R“ R" V-12-1 Et H H H Et H H F OH H H nh2 V-12-2 Et H H CH3 Et H H F OH H H nh2 V-12-3 Et H H CH(CH3)2 Et H H F OH H H nh2 V-12-4 Et H H CH2CH(CH3)2 Et H H F OH H H nh2 V-12-5 Et H H CH2Ph Et H H F OH H H nh2 V-12-6 Et H H CH2-indol-3-yl Et H H F OH H H nh2 V-12-7 Et H H CH2CH2SCH3 Et H H F OH H H nh2 V-12-8 Et ♦ H * Et H H F OH H H nh2 *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table V-13. ' ' .......—-« < ......... J " ' .......

Xs R* R2 R3a R3b R4 R3 R6 X Υ R7 R8 R^ V-13-1 ipr H Η H Et H Η F ΟΗ Η Η νη2 V-13-2 'Pr H H CH3 Et Η Η F ΟΗ Η Η νη2 V-13-3 'Pr H H ΟΗ(ΟΗ3)2 Et Η Η F ΟΗ Η Η νη2 V-13-4 'Pr H H CH2CH(CH3)2 Et Η Η F ΟΗ Η Η ΝΗ2 V-13-5 'Pr Η Η CH2Ph Et Η Η F ΟΗ Η Η νη2 V-13-6 /pr H H CH2-indol-3-yl Et Η Η F ΟΗ Η Η νη2 V-13-7 'Pr H H ch2ch2sch3 Et Η Η F ΟΗ Η Η νη2 V-13-8 j 'Pr l n3b * Η * Et Η Η F ΟΗ Η Η νη2 *R2 and R3b joined together by (CH^"to form five-membered ring. 2983472-1 -172- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Table V-14.

Xs Rl R2 R 3a "r35 ΊΓ R5 X Y RJ it R^ V-14-1 'Bu H H H Et H H F OH H H nh2 V-14-2 'Bu H H ch3 Et H H F OH H H nh2 V-14-3 'Bu H H CH(CH3)2 Et H H F OH H H nh2 V-14-4 'Bu H H CH2CH(CH3)2 Et H H F OH H H nh2 V-14-5 'Bu H H CH2Ph Et H H F OH H H nh2 V-14-6 'Bu H H CH2-indol-3-yl Et H H F OH H H nh2 V-14-7 'Bu H H CH2CH2SCH3 Et H H F OH H H nh2 V-14-8 'Bu * H 4 Et H H F OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table V-15.

Xs Έ” R2 'r33- "r35 R4 Rs Rb X Y ir r“ r5” V-15-1 Ph H H H Et H H F OH H H nh2 V-15-2 Ph Η H CH3 Et H H F OH H H nh2 V-15-3 Ph H H CHCCH,), Et H H F OH H H nh2 V-15-4 Ph H H CH2CH(CH3)2 Et H H F OH H H nh2 V-15-5 Ph Η H CH2Ph Et H H F OH H H nh2 V-15-6 Ph H H CH2-indol-3-yl Et H H F OH H H nh2 V-15-7 Ph Η H CH2CH2SCH3 Et H H F OH H H nh2 V-15-8 Ph * H ♦ Et H H F OH H H nh2 *R4 and Rejoined together by (0¾^ to form five-membered ring. 5 Table V-16. I » RL ...... 1 " a

Xs R1 R4 R3" Rjb R4 R5 Rb X Υ R7 R“ R9 V-16- 1 p-Me- Ph Η Η Η Et H Η F ΟΗ Η Η νη2 V-16- 2 p-Me- Ph Η Η ch3 Et Η Η F ΟΗ Η Η νη2 V-16- 3 p-Me- Ph Η Η CHiCHj), Et Η Η F ΟΗ Η Η νη2 V-16- 4 p-Me- Ph Η Η CH2CH(CH3)2 Et Η Η F ΟΗ Η Η νη2 V-16- p-Me- Η Η CH2Ph Et Η Η F ΟΗ Η Η νη2 5 Ph 2983472-1 -173-

WO 60137.0034WOUI PCT/US2008/058183

Ns T- “r5- R3a R4 Rs R4 X Y R'j R* Rs V-16- 6 p-Me- Ph H H CH2-indol-3- yi Et H H F OH H H nh2 V-16- 7 p-Me- Ph H H ch2ch2sch3 Et H H F OH H H nh2 V-16- p-Me- * H * Et H H F OH H H nh2

Ph *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table V-17.

Ns R1 R2 r3“ Rjb R4 r! R* X Y R7 Rtt Ry V-17-1 p-F-Ph H H H Et H H F OH H H NH2 V-17-2 p-F-Ph H H CH3 Et H H F OH H H nh2 V-17-3 p-F-Ph H H CH(CH3)2 Et H H F OH H H nh2 V-17-4 p-F-Ph H H CH2CH(CH3)2 Et H H F OH H H nh2 V-17-5 p-F-Ph H H CH2Ph Et H H F OH H H nh2 V-17-6 p-F-Ph H H CHrindol-3-yl Et H H F OH H H nh2 V-17-7 p-F-Ph H H CH2CH2SCH3 Et H H F OH H H nh2 V-17-8 p-F-Ph * H ♦ Et H H F OH H H nh2 *RZ and RJb joined together by (CHjjTto form five-membered ring.

Table V-18.

Ns R1 R2 R35” R3® R4 r3- R4 X Y r’ Rtt R* V-18-1 p-Cl-Ph H H H Et H H F OH H H nh2 V-18-2 p-Cl-Ph H H CH3 Et H H F OH H H nh2 V-18-3 p-CI-Ph H H ΟΗ(ΟΗ3)ϊ Et H H F OH H H nh2 V-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H H F OH H H nh2 V-18-5 p-Cl-Ph H H CH2Ph Et H H F OH H H nh2 V-18-6 p-Cl-Ph H H CH2-indol-3-yl Et H H F OH H H nh2 V-18-7 p-Cl-Ph H H CH2CH2SCH3 Et H H F OH H H nh2 V-18-8 p-Cl-Ph * H * Et H H F OH H H nh2 5 *R2 and R5b joined together by (ΌΗ^ to form five-membered ring.

Table V-19.

Ns R1 R2 R3’ R3b R4 Rs R6 X Υ R' R" R^ V-19-1 p-Br-Ph Η Η H Et Η Η F ΟΗ Η Η νη2 V-19-2 p-Br-Ph H H CH3 Et Η Η F ΟΗ Η Η νη2 V-19-3 p-Br-Ph H H CHtCHah Et Η Η F ΟΗ Η Η νη2 2983472-1 -174- PCT/US2008/058183 WO 2008/121634

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Xa R1 Ί?’ R3b R1 R4 X Y R7 r“ Ry V-19-4 p-Br-Ph H H CH2CH(CH3)2 Et H H F OH H H nh2 V-19-5 p-Br-Ph H H CH2Ph Et H H F OH H H nh2 V-19-6 p-Br-Ph H H CH2-indol-3-yl Et H H F OH H H nh2 V-19-7 p-Br-Ph H H ch2ch2sch3 Et H H F OH H H nh2 V-19-8 p-Br-Ph ♦ H * Et H H F OH H H nh2 *RJ and R3b joined together by (CH2)3 to form five-membered ring.

Table V-20.

Xa R2 RjB R3b R4 R5 R6 X Y R7 R“ R9 V-20-1 p-I-Ph Η H H Et H H F OH H H nh2 V-20-2 p-I-Ph H H ch3 Et H H F OH H H nh2 V-20-3 p-I-Ph H H CHCCHah Et H H F OH H H nh2 V-20-4 p-I-Ph H H CH2CH(CH3)2 Et H H F OH H H nh2 V-20-5 p-I-Ph H H CH2Ph Et H H F OH H H nh2 V-20-6 p-I-Ph H H CH2-indol-3-yl Et H H F OH H H nh2 V-20-7 p-I-Ph H H ch2ch2sch3 Et H H F OH H H nh2 V-20-8 p-I-Ph * H ♦ Et H H F OH H H nh2 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table V-21.

Xa R1 R7 Rjb R4 Rs R6 X Y R7 R8" R9 V-21-1 ch3 H Η Η "W H H F OH H H nh2 V-21-2 ch3 H Η ch3 'Pr H H F OH H H nh2 V-21-3 ch3 Η Η CH(CH3)2 'Pr H H F OH H H nh2 V-21-4 ch3 H Η CH2CH(CH3)2 'Pr H H F OH H H nh2 V-21-5 ch3 H Η CH2Ph 'Pr H H F OH H H nh2 V-21-6 ch3 Η Η CH2-indol-3-yl 'Pr H H F OH H H nh2 V-21-7 ch3 Η Η ch2ch2sch3 'Pr H H F OH H H nh2 V-21-8 ch3 * Η * 'Pr. H H F OH H H nh2 5 *R2 and Rejoined together by (0¾¼ to form five-membered ring.

Table V-22.

Xa R R2 R3« R3b R4 RJ R6 X Y r" R8 R9 V-22-1 Et Η H H "ΨΓ Η H F OH H H NH2 V-22-2 Et H H CH3 'Pr H H F OH H H nh2 V-22-3 Et H H o-kchOj 'Pr Η H F OH H H nh2 V-22-4 Et H H CH2CH(CH3)2 'Pr H H F OH H H nh2 2983472-1 -175- WO 2008/121634

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Ns R1 R2 r3^ R35 R4 ΊΓ R6 X Y r’ r“ ic V-22-5 Et H H CH2Ph H H F OH H H nh2 V-22-6 Et H H CH2-indol-3-yl 'Pr H H F OH H H nh2 V-22-7 Et H H CH2CH2SCH3 'Pr H H F OH H H nh2 V-22-8 Et * H * 'Pr H H F OH H H nh2 *R2 and Rejoined together by (CFhb to form five-membered ring.

Table V-23.

Ns R R3 R3a R3b R' Rs R6 X Y R7 R“ Rs V-23-1 "W H H H -IpP H H F OH H H nh2 V-23-2 'Pr H H ch3 'Pr H H F OH H H nh2 V-23-3 'Pr H H CH(CH3)2 'Pr H H F OH H H nh2 V-23-4 'Pr H H CH2CH(CH3)2 'Pr H H F OH H H nh2 V-23-5 'Pr H H CH2Ph 'Pr H H F OH H H nh2 V-23-6 'Pr H H CH2-indol-3-yl 'Pr H H F OH H H nh2 V-23-7 'Pr H H CH2CH2SCH3 'Pr H H F OH H H nh2 V-23-8 'Pr * H * 'Pr H H F OH H H nh2 *R2 and RJb joined together by (CH2)3 to form Five-membered ring.

Table V-24.

Ns IV R3" R7" R35 R4 R5 R6 X Y r“ ""R9- V-24-1 'Bu H H H "W H H F OH H H nh2 . V-24-2 'Bu H H ch3 'Pr H H F OH H H nh2 V-24-3 'Bu H H CHfCHjh ^r H H F OH H H nh2 V-24-4 'Bu H H CH2CH(CH3)2 'Pr H H F OH H H nh2 V-24-5 'Bu H H CH2Ph . 'Pr H H F OH H H nh2 V-24-6 'Bu H H CH2-indol-3-yl 'Pr H H F OH H H nh2 V-24-7 'Bu H H CH2CH2SCH3 'Pr H H F OH H H nh2 V-24-8 -j 'Bu * H ♦ 'Pr H H F OH H H nh2 —IJ 111 ....................... ................. ..... *R and R joined together by (CH2)3 to form five-membered ring.

Table V-25.

Ns R1 R3 R35" r36- ΊΤ V R‘ X Y r’ R8 r^“ V-25-1 Ph H H H H H F OH H H nh2 V-25-2 Ph H H CH3 'Pr H H F OH H H nh2 V-25-3 Ph H H CH(CH3)2 'Pr H H F OH H H nh2 V-25-4 Ph H H CH2CH(CH3)2 'Pr H H F OH H H nh2 V-25-5 Ph H H CH2Ph 'Pr H H F OH H. H nh2 2983472-1 -176- WO 2008/121634 PCT/US2008/058183

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Ns R1 R3 "R37" Ru R4 Rs R6 X Y R7 Rb R9 V-25-6 Ph H H CH2-indoI-3-yl "W H H F OH H H NH2 V-25-7 Ph H H CH2CH2SCH3 'Pr H H F OH H H nh2 V-25-8 Ph * H + 'Pr H H F OH H H NH2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table V-26. Na R1 RJ Rja R3b R4 R5 R6 X Y R Rs V-26- 1 p-Me- Ph H H H ipr H H F OH H H nh2 V-26- 2 p-Me- Ph H H ch3 'Pr H H F OH H H nh2 V-26- 3 p-Me- Ph H H CH(CH3)2 'Pr H H F OH H H nh2 V-26- 4 p-Me- Ph H H CH2CH(CH3)2 'Pr H H F OH H H nh2 V-26- 5 p-Me- Ph H H CH2Ph 'Pr H H F OH H H nh2 V-26- 6 p-Me- Ph H H CH2-indol-3- yi 'Pr H H F OH H H nh2 V-26- 7 p-Me- Ph H H CH2CH2SCH3 'Pr H H F OH H H nh2 V-26- 8 p-Me- Ph * H * 'Pr H H F OH H H nh2 *R2 and RJb joined together by (CHih to fonn five-membered ring.

Table V-27.

Na R‘ IF r3T IT RJ R4 X Υ ΊΓ R8 R’ V-27-1 p-F-Ph H H H JPr Η Η F ΟΗ Η Η ΝΗ2 V-27-2 p-F-Ph H H CH3 'Pr Η Η F ΟΗ Η Η νη2 V-27-3 p-F-Ph H H CH(CH3)j 'Pr Η Η F ΟΗ Η Η νη2 V-27-4 p-F-Ph H H CH2CH(CH3>2 'Pr Η Η F ΟΗ Η Η νη2 V-27-5 p-F-Ph H H CH2Ph 'Pr Η Η F ΟΗ Η Η νη2 V-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr Η Η F ΟΗ Η Η νη2 V-27-7 p-F-Ph H H CH2CH2SCH3 'Pr Η Η F ΟΗ Η Η νη2 V-27-8 “ϊϊπ—: p-F-Ph r»3b ;' I1" * H * 'Pr Η Η F ΟΗ Η Η νη2 W H r ' I I Mil. Mil I I I I I III llll *R and R joined together by (CH2)3 to form five-membered ring. 2983472-1 -177- PCT/US2008/058183 WO 2008/121634

Docket No. 6013 7.0034WOU1

Table V-28.

Ns R1 R2 R3a R3b RJ "rS" X Y Rz RK fT V-28-1 p-Cl-Ph H H H "W H H F OH H H nh2 V-28-2 p-Cl-Ph H H ch3 ipr H H F OH H H nh2 V-28-3 p-Cl-Ph H H CH(CH3)2 /pr H H F OH H H nh2 V-28-4 p-Cl-Ph H H CH2CH(CH3)2 jpr H H F OH H H nh2 V-28-5 p-Cl-Ph H H CH2Ph 'Pr H H F OH H H nh2 V-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr H H F OH H H nh2 V-28-7 p-Cl-Ph H H CH2CH2SCH3 'Pr H H F OH H H nh2 V-28-8 p-Cl-Ph * H * 'Pr H H F OH H H nh2 *R2 and R3b joined together by ((¾¼ to form five-membered ring.

Table V-29.

Ns R1 Ra R3. R3b R4 R3 R6 X Y R7 R“ R^ V-29-1 p-Br-Ph H H H “¥r“ H H F OH H H nh2 V-29-2 p-Br-Ph H H ch3 'Pr H H F OH H H nh2 V-29-3 p-Br-Ph H H CHCCHsh 'Pr H H F OH H H nh2 V-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr H H F OH H H nh2 V-29-5 p-Br-Ph H H CH2Ph 'Pr H H F OH H H nh2 V-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr H H F OH H H nh2 V-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr H H F OH H H nh2 V-29-8 p-Br-Ph * H * 'Pr H H F OH H H nh2 *R2 and RJ 6 joined together by (CH2)3 to form five-membered ring. 5 Table V-30.

1 ,p" ' I R R “.‘ML " ""'-J - g ‘ ' 'W

Ns r‘ R2 r3« R3b R4 R5 R6 X Y R7 R* R5 V-30-1 p-I-Ph Η H H JPr H H F OH H H nh2 V-30-2 p-I-Ph H H ch3 'Pr H H F OH H H nh2 V-30-3 p-I-Ph Η H CHCCHah Tr H H F OH H H nh2 V-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr H H F OH H H nh2 V-30-5 p-I-Ph H H CH2Ph 'Pr H H F OH H H nh2 V-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr H H F OH H H NH2 V-30-7 p-I-Ph H H CH2CH2SCH3 'Pr H H F OH H H NH2 V-30-8 —: p-I-Ph 1 * H * 'Pr H H F OH H H nh2 *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -178- WO 2008/121634 PCT/US2008/058183

DocketNo. 60137.0034WOU1

Table V-31.

Xa R1 R2 "r33" Ί?* ΊΓ"' R5 X Y R7 IT R5 V-3I-1 ch3 H H H "Bu H H F OH H H NH2 V-31-2 ch3 H H ch3 "Bu H H F OH H H nh2 V-31-3 ch3 H H CH(CH3)2 "Bu H H F OH H H nh2 V-31-4 ch3 H H CH2CH(CH3)2 "Bu H H F OH H H nh2 V-31-5 ch3 H H CH2Ph "Bu H H F OH H H nh2 V-31-6 ch3 H H CH2-indol-3-yl "Bu H H F OH H H nh2 V-31-7 ch3 H H CH2CH2SCH3 "Bu H H F OH H H nh2 V-31-8 ch3 * H * "Bu H H F OH H H nh2 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table V-32.

Xa R ΊΓ RJ‘ R35 R4 IT R6 X Y R' R“ R9 V-32-1 Et Η Η Η "Bu H H F OH H H nh2 V-32-2 Et Η Η ch3 "Bu H H F OH H H nh2 V-32-3 Et Η Η CH(CH3)2 "Bu H H F OH H H nh2 V-32-4 Et Η Η CH2CH(CH3)2 "Bu H H F OH H H nh2 V-32-5 Et Η Η CH2Ph "Bu H H F OH H H nh2 V-32-6 Et Η Η CH2-indol-3-yl "Bu H H F OH H H nh2 V-32-7 Et Η Η CH2CH2SCH3 "Bu H H F OH H H nh2 V-32-8 Et * Η ♦ "Bu H H F OH H H nh2 ♦R^ and^36 joined together by (CH2)3 to form five-membered ring. 5 Table V-33. ...... . .-. .. ....,1....-,.1.. J f g W B Λ

Xa R1 R2 R3« R3b R4 ΊΓ R6 X Y R7 R“ R9 V-33-1 Η H H "Bu H H F OH H H nh2 V-33-2 ’Pr H H CH3 "Bu H H F OH H H nh2 V-33-3 'Pr H H CH(CH3)2 "Bu H H F OH H H nh2 V-33-4 'Pr H H CH2CH(CH3)2 "Bu H . H F OH H H nh2 V-33-5 'Pr H H CH2Ph "Bu H H F OH H H nh2 V-33-6 'Pr H H CH2-indol-3-yl "Bu H H F OH H H nh2 V-33-7 'Pr Η H CH2CH2SCH3 "Bu H H F OH H H nh2 V-33-8 'Pr. * H * "Bu H H F OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-t -179- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table V-34.

Ns R2 R3“ R3b - R4 Rs R6 X Y r’ r“ "R^ V-34-1 'Bu H H H "Bu H H F OH H H nh2 V-34-2 'Bu H H ch3 "Bu H H F OH H H nh2 V-34-3 'Bu H H CH(CH3)2 "Bu H H F OH H H nh2 V-34-4 'Bu H H CH2CH(CH3)2 "Bu H H F OH H H nh2 V-34-5 'Bu H H CH2Ph "Bu H H F OH H H nh2 V-34-6 'Bu H H CH2-indol-3-yl "Bu H H F OH H H nh2 V-34-7 'Bu H H CH2CH2SCH3 "Bu H H F OH H H nh2 V-34-8 'Bu * H * "Bu H H F OH H H nh2 *R2 and R3” joined together by (CH2)3 to form five-membered·ring.

Table V-35. X2 R1 R1* r3. R3b R4 R5 R* X Y R7 RB Rs V-35-1 Ph Η Η Η "Bu H H F OH H H nh2 V-35-2 Ph Η Η ch3 "Bu H H F OH H H nh2 V-35-3 Ph Η Η CH(CH3)2 "Bu H H F OH H H nh2 V-35-4 Ph Η Η CH2CH(CH3)2 "Bu H H F OH H H nh2 V-35-5 Ph Η Η CH2Ph "Bu H H F OH H H nh2 V-35-6 Ph Η Η CH2-indo1-3-yl "Bu H H F OH H H nh2 V-35-7 Ph Η Η CH2CH2SCH3 "Bu H H F OH H H nh2 V-35-8 Ph * Η * "Bu H H F OH H H nh2 *RZ and R3" joined together by (Cthb to form five-membered ring. 5 Table V-36. I - - 1 > J..... B ' "’‘n1111· X2 R' RJ R3a R3b R4 R5 R6 X Y R7 R“ R9 V-36- 1 p-Me- Ph H H H "Bu H H F OH H H nh2 V-36- 2 p-Me- Ph H H CH3 "Bu H H F OH H H nh2 V-36- 3 p-Me- Ph H H CH(CH3)2 "Bu H H F OH H H nh2 V-36- 4 p-Me- Ph H H CH2CH(CH3)2 "Bu H H F OH H H nh2 V-36- 5 p-Me- Ph H H CH2Ph "Bu H H F OH H H nh2 V-36- p-Me- H H CH2-indol-3- "Bu H H F OH H H nh2

Ph 2983472-1 -180- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Ns R1 R2 R3· R3b R4 R5 R6 X Y R5- 6 yi V-36- 7 p-Me- Ph H H ch2ch2sch3 "Bu H H F OH H H nh2 V-36- 8 p-Me- Ph ♦ H * "Bu H H F OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five membered ring.

Table V-37.

Ns R1 R3 RJ. r’!) ΊΤ" R5 R6 X Y r'2 Λ5- V-37- p-F- Η H H "Bu H H F OH H H nh2 1 Ph V-37- p-F- H H CH3 "Bu H H F OH H H nh2 2 Ph V-37- p-F- H H ΟΗ(ΟΗ3)2 "Bu H H F OH H H nh2 3 Ph V-37- p-F- H H CH2CH(CH3)2 "Bu H H F OH H H nh2 4 Ph V-37- p-F- H H CH2Ph "Bu H H F OH H H nh2 5 Ph V-37- p-F- H H CH2-indoI-3- "Bu H H F OH H H nh2 6 Ph yi V-37- p-F- H H CH2CH2SCH3 "Bu H H F OH H H nh2 7 Ph V-37- p-F- * H * "Bu H H F OH H H nh2 8 Ph *R2 and Rejoined together by (CHab to form five-membered ring.

Table V-38. Ns R1 R3 RJa R3b R4 iv R6 X Y R7 R* R9 V-38- 1 p-Cl- Ph H Η Η "Bu H H F OH H H nh2 V-38- 2 p-Cl- Ph Η Η CH3 "Bu H H F OH H H nh2 V-38- 3 p-Cl- Ph Η Η CH(CH3)2 "Bu H H F OH H H nh2 VJ8- p-Cl- Η Η CH2CH(CH3)2 "Bu H H F OH H H nh2

Ph 2983472-1 -181- PCT/US2008/058183 WO 2008/121634 t ΛΛΟ

Docket No. 60137.0034WOU1 M “r1- “R3" r3. R3b -£3— Rs R6 X Y "r7" IF r^ 4 V-38- p-Cl- H H CH2Ph "Bu H H F OH H H nh2 5 Ph V-38- p-Cl- H H CH2-indol-3- "Bu H H F OH H H nh2 6 Ph yi V-38- p-Cl- H H ch2ch2sch3 "Bu H H F OH H H nh2 7 Ph V-38- p-Cl- * H * "Bu H H F OH H H nh2

Ph *R2 and RJ0 joined together by (ΟΗ2)3 to form five-membered ring.

Table V-39. K2 R' R2 -jpr- Έ15 R4 Rs R* X Y F? R* R^ V-39- 1 p-Br- Ph Η Η Η "Bu H H F OH H H nh2 V-39- 2 p-Br- Ph Η Η ch3 "Bu H H F OH H H nh2 V-39- 3 p-Br- Ph Η Η CH(CH3)2 "Bu H H F OH H H nh2 V-39- 4 p-Br- Ph Η Η CH2CH(CH3)2 "Bu H H F OH H H nh2 V-39- 5 p-Br- Ph Η Η CH2Ph "Bu H H F OH H H nh2 V-39- 6 p-Br- Ph Η Η CH2-indo)-3- yi "Bu H H F OH H H nh2 V-39- 7 p-Br- Ph Η Η CH2CH2SCH3 "Bu H H F OH H H nh2 V-39- 8 p-Br- Ph * Η * "Bu H H F OH H H nh2 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table V-40. Ka R* R2 R3* R3b R4 R3 R6 X Y ΊΓ R8 R^ V-40-1 p-I-Ph H H H "Bu H H F OH H H nh2 V-40-2 p-I-Ph H H CH3 "Bu H H F OH H H nh2 V-40-3 p-I-Ph H H CH(CH3)2 "Bu H H F OH H H nh2 2983472-1 -182- WO 2008/121634 ηηα.ΛνΓΜΐ1 uoctcet No. 60137.0034WOU1

Jia R1 R1 R3a R3b R4 R3 R6 X Y ΊΓ r“ V-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu H H F OH H H nh2 V-40-5 p-l-Ph H H CH2Ph "Bu H H F OH H H nh2 V-40-6 p-I-Ph H H CHa-indol-3-yl "Bu H H F OH H H nh2 V-40-7 p-I-Ph H H CH2CH2SCH3 "Bu H H F OH H H nh2 V-40-8 p-I-Ph * H * "Bu H H F OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table V-41.

Ns R RJ RJa R3b R4 R5 R6 X Y R7 R8 ΪΓ V-41-1 ch3 Η Η Η Bz H H F OH H H nh2 V-41-2 ch3 Η Η ch3 Bz H H F OH H H nh2 V-41-3 ch3 Η Η CH(CH3)j Bz H H F OH H H nh2 V-41-4 ch3 Η Η CH2CH(CH3)2 Bz H H F OH H H nh2 V-41-5 ch3 Η Η CH2Ph Bz H H F OH H H nh2 V-41-6 ch3 Η Η CH2-indol-3-yl Bz H H F OH H H nh2 V-41-7 ch3 Η Η CH2CH2SCH3 Bz H H F OH H H nh2 V-41-8 ch3 4 Η * Bz H H F OH H H nh2 *R2 and Rejoined together by (CH^a to form five-membered ring.

Table V-42.

Ns R R2 R3a R3b R4 R5 R4 X Y R7 R8 R* V-42-1 Et H H H Bz H H F OH H H NH2 V-42-2 Et H H ch3 Bz H H F OH H H nh2 V-42-3 Et H H CH(CH3)2 Bz H H F OH H H nh2 V-42-4 Et H H CH2CH(CH3)2 Bz H H F OH H H NH2 V-42-5 Et H H CH2Ph Bz H H F OH H H NH2 V-42-6 Et H H CH2-indol-3-yl Bz H H F OH H H nh2 V-42-7 Et H H CH2CH2SCH3 Bz H H F OH H H nh2 V-42-8 Et ♦ H Bz H H F OH H H nh2 5 *R2 and Rejoined together by (CFhb to form five-membered ring.

Table V-43.

Ns R ΊΓ RJa R3b R4 R3 R6 X Y ΊΓ R“ R^~ V-43-1 "W H H H Bz H H F OH H H nh2 V-43-2 'Pr Η H ch3 Bz H H F OH H H nh2 V-43-3 'Pr H H CH(CH3)2 Bz H H F OH H H nh2 V-43-3 'Pr Η HCHjEHtCH^ Bz Η H F OH Η H NH2 2983472-1 -183- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 V-43-6 'Pr H H CH2-indol-3-yl Bz H H F OH H H nh2 V-43-7 'Pr H H CH2CH2SCH3 Bz H H F OH H H nh2 V-43-8 'Pr * H ♦ Bz H H F OH H H nh2 *R2 and R30 joined together by (CH2)3 to form five-membered ring, Table V-44. Ns R2 "r^ “r35 R4 Rs R6 X Y r’ r“ R? V-44-1 'Bu H H H Bz H H F OH H H nh2 V-44-2 'Bu H H ch3 Bz H H F OH H H nh2 V-44-3 'Bu H H CH(CH3)2 Bz H H F OH H H nh2 V-44-4 'Bu H H CH2CH(CH3)2 Bz H H F OH H H nh2 V-44-5 'Bu H H CH2Ph Bz H H F OH H H nh2 V-44-6 'Bu H H CH2-indol-3-yl Bz H H F OH H H nh2 V-44-7 'Bu H H CH2CH2SCH3 Bz H H F OH H H nh2 V-44-8 'Bu * H * Bz H H F OH H H nh2 *R and R joined together by (0¼^ to form five-membered ring.

Table V-45.

Ns R1 r7- R35 R4 RJ R6 X Y R7" r“ V-45-1 Ph Η H H Bz H H F OH H H NH2 V-45-2 Ph H H CH3 Bz H H F OH H H nh2 V-45-3 Ph H H CHtCHah Bz H H F OH H H nh2 V-45-4 Ph H H CH2CH(CH3)2 Bz H H F OH H H nh2 V-45-5 Ph H H CH2Ph Bz H H F OH H H nh2 V-45-6 Ph H H CHa-indol-3-yl Bz H H F OH H H nh2 V-45-7 Ph H H CH2CH2SCH3 Bz H H F OH H H nh2 V-45-8 Ph * H * Bz H H F OH H H nh2 ♦R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table V-46.

Ns R‘ R4 RJe R^ R4 R5 R6 X Y r" R1 RB V-46- 1 p-Me- Ph H H H Bz H H F OH H H nh2 V-46- 2 p-Me- Ph H H ch3 Bz H H F OH H H nh2 V-46- 3 p-Me- Ph H H CH(CH3)2 Bz H H F OH H H nh2 V-46- p-Me- H H CH2CH(CH3)2 Bz H H F OH H H nh2 2983472-1 -184- PCT/US2008/058183 WO 2008/121634 ' _ Λη, „, τ,

Uocket No. 60137.0034WOU1

Xs T- R2 -r3T- r4” R5 R6 X Y R7 r“ "R5” 6 yi V-48- p-Cl- H H ch2ch2sch3 Bz H H F OH H H nh2 7 Ph V-48- p-Cl- * H * Bz H H F OH H H nh2

Ph *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table V-49. X2 R1 R2 R3" ΊΡ6 R5 R6 X Y R' "R5” Ίυ V-49- 1 p-Br- Ph H H H Bz H H F OH H H nh2 V-49- 2 p-Br- Ph H H CH3 Bz H H F OH H H nh2 V-49- 3 p-Br- Ph H H CH(CH3)2 Bz H H F OH H H nh2 V-49- 4 p-Br- Ph H H CH2CH(CH3)2 Bz H H F OH H H nh2 V-49- 5 p-Br- Ph H H CH2Ph Bz H H F OH H H nh2 V-49- 6 p-Br- Ph H H CH2-indol-3- yi Bz H H F OH H H nh2 V-49- 7 p-Br- Ph H H CH2CH2SCH3 Bz H H F OH H H nh2 V-49- p-Br- * H * Bz H H F OH H H nh2

Ph *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table V-50.

Xs R1 R2 r3. R3b R* R3 R6 X Y R7 RK Ίν V-50-1 p-I-Ph H H H Bz H H F OH H H nh2 V-50-2 p-I-Ph H H CH3 Bz H H F OH H H nh2 V-50-3 p-I-Ph H H CH(CH3)2 Bz H H F OH H H nh2 V-50-4 p-I-Ph H H CH2CH(CH3)2 Bz H H F OH H H nh2 V-50-5 p-I-Ph H H CH2Ph Bz H H F OH H H nh2 V-50-6 p-I-Ph H H CH2-indol-3-yl Bz H H F OH H H nh2 V-50-7 p-I-Ph H H CH2CH2SCH3 Bz H H F OH H H nh2 2983472-1 -186 - PCT/US2008/058183 WO 2008/121634.. ηΛα>Ιλνητη

uocKei No. 60137.0034WOU I

Xa R‘ R2 R?4 R3b Rs R6 X Y R7 R' R9 4 Ph V-46- p-Me- H H CH2Ph Bz H H F OH H H nh2 5 Ph V-46- p-Me- H H CH2-indol-3- Bz H H F OH H H nh2 6 Ph yi V-46- p-Me- H H ch2ch2sch3 Bz H H F OH H H nh2 7 Ph V-46- p-Me- * H 4 Bz H H F OH H H nh2

Ph *R2 and Rejoined together by (CHa)3 to form five-membered ring.

Table V-47.

Xs R‘ -r33T R4 Rs R4 X Y r’ r“ R9 V-47-1 p-F-Ph H H H Bz H H F OH H H NH2 V-47-2 p-F-Ph H H CH3 Bz H H F OH H H nh2 V-47-3 p-F-Ph H H CHCCH^ Bz H H F OH H H nh2 V-47-4 p-F-Ph H H CH2CH(CH3)2 Bz H H F OH H H nh2 V-47-5 p-F-Ph H H CH2Ph Bz H H F OH H H nh2 V-47-6 p-F-Ph H H CH2-indol-3-yl Bz H H F OH H H nh2 V-47-7 p-F-Ph H H CH2CH2SCH3 Bz H H F OH H H nh2 V-47-8 p-F-Ph 4 H 4 Bz H H F OH H H nh2 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table V-48.

Xs R1 R2 R3a R3t> R4 Rs R4 X Y R7 R8 R5 V-48- 1 p-Cl- Ph Η Η Η Bz H H F OH H . H NH2 V-48- 2 p-Cl- Ph Η Η ch3 Bz H H F OH H H nh2 V-48- 3 p-Cl- Ph Η Η CH(CH3)2 Bz H H F OH H H nh2 V-48- 4 p-Cl- Ph Η Η CH2CH(CH3)2 Bz H H F OH H H nh2 V-48- 5 p-Cl- Ph Η Η CH2Ph Bz H H F OH H H nh2 V-48- p-Cl- Η Η CH2-indol-3- Bz H H F OH H H nh2

Ph 2983472-1 -185- PCT/US2008/058183 WO 2008/121634 ΛΛΠ „„,ΛΤΤ,

Docket No. 60 J 37.0034WOU1 R1 R2 R3a R3b R4 R5 R6 X Y r’ Rs "1?~ V-50-8 p-I-Ph 1 Jb · · * h * Bz H H F OH H H nh2 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

VI

Table VI-1.

N° “R*“ RJ "IF" R3b ”r4" Rs R6 X Y r’ “IF VI-1-1 ch3 H H H ch3 H F H OH H H VI-1-2 ch3 H H ch3 ch3 H F H OH H H VI-1-3 ch3 H H CH(CH3)2 ch3 H F H OH H H VI-1-4 ch3 H H CH2CH(CH3)2 ch3 H F H OH H H VI-1-5 ch3 H H CH2Ph ch3 H F H OH H H VI-1-6 ch3 H H CHrindol-3-yl ch3 H F H OH H H VI-1-7 ch3 H H CH2CH2SCH3 ch3 H F H OH H H VI-1-8 ch3 * H * ch3 H F H OH H H 5 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table VI-2.

Ki R1 RJ r3. R3b R4 R5 R® X Υ R' R8 VI-2-1 Et H H H ch3 Η F Η ΟΗ Η Η VI-2-2 Et H H ch3 ch3 Η F Η ΟΗ Η Η VI-2-3 Et H H CH(CH3)2 ch3 Η F Η ΟΗ Η Η VI-2-4 Et H H CH2CH(CH3)2 ch3 Η F Η ΟΗ Η Η VI-2-5 Et H H CH2Ph ch3 Η F Η ΟΗ Η Η VI-2-6 Et H H CH2-indol-3-yl ch3 Η F Η ΟΗ Η Η VI-2-7 Et H H CH2CH2SCH3 ch3 Η F Η ΟΗ Η Η 2983472-1 -187- PCT/US2008/058183 WO 20»^gJ“l4Na ¢0137.0034WOU1

Ka ΤΓ ’Tr Rie Έ5 RJ R6 X Y R7 R8 VI-2-8 Et ♦ H * ch3 H F H OH H H *R2 and R3b joim ed together by (CH2)3 t to form fi ve-membered ring. Table VI-3. Ko r* R2 Τ’ R1 R4 X Y r' Ra VI-3-1 'Pr H H H ch3 H F H OH H H VI-3-2 'Pr H H ch3 ch3 H F H OH H H VI-3-3 'Pr H H CH(CH3)2 ch3 H F H OH H H VI-3-4 'Pr H H CH2CH(CH3)2 ch3 H F H OH H H VI-3-5 'Pr H H CHjPh ch3 H F H OH H H VI-3-6 'Pr H H CH2-indol-3-yl ch3 H F H OH H H VI-3-7 'Pr H H CH2CH2SCH3 ch3 H F H OH H H VI-3-8 'Pr * H * ch3 H F H OH H H *R2 and Rejoined together by (Cltb to form five-membered ring.

Table VI-4.

K2 R R2 RjB R3b R4 R5 R4 X Y R' R“ VI-4-ϊ 'Bu H H H ch3 Η F H OH H H VI-4-2 'Bu H H CH3 ch3 H F H OH H H VI-4-3 'Bu H H ΟΗ(ΟΗ3)2 ch3 Η F H OH H H VI-4-4 'Bu H H CH2CH(CH3)2 ch3 H F H OH H H VI-4-5 'Bu H H CH2Ph ch3 H F H OH H H VI-4-6 'Bu H H CHrindol-3-yl ch3 H F H OH H H VI-4-7 'Bu H H CH2CH2SCH3 ch3 H F H OH H H VI-4-8 'Bu * H * ch3 H F H OH H H 5 *R? and Rejoined together by (CHab to form five-membered ring. 2983472-1 -188- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Table VI-5.

X2 R1 R?e R3b R4 RJ R6 X Y r’ R“ VI-5-1 Ph H H H ch3 H F H OH H H VI-5-2 Ph H H ch3 ch3 H F H OH H H VI-5-3 Ph H H CH(CH3)2 ch3 H F H OH H H VI-5-4 Ph H H CH2CH(CH3)2 ch3 H F H OH H H VI-5-5 Ph H H CH2Ph ch3 H F H OH H H VI-5-6 Ph H H CH2-indol-3-yl ch3 H F H OH H H VI-5-7 Ph H H CH2CH2SCH3 ch3 H F H OH H H VI-5-8 Ph ♦ H * ch3 H F H OH H H *R2 and R36 joined together by (CH2)3 to form five-membered ring.

Table VI-6.

X2 R1 T" R3a TF R4 RJ Rfc X Y R7 R“ VI-6-1 p-Me-Ph H H H ch3 Η F H OH H H VR6-2 p-Me-Ph H H CH3 ch3 H F H OH H H VI-6-3 p-Me-Ph H H CH(CH3)2 ch3 H F H OH H H VI-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 H F H OH H H VI-6-5 p-Me-Ph H H CH2Ph ch3 H F H OH H H VI-6-6 p-Me-Ph H H CH2-indol-3-yl ch3 H F H OH H H VI-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 H F H OH H H VI-6-8 p-Me-Ph ♦ H * ch3 H F H OH H H *R^ and RJ0 joined together by (CH2)3 to form five-membered ring. 5 Table VI-7. 1 I M RL'~ ' J . ......- ..."U"

X2 R1 R3 RJa R3b R4 R5 R6 X Y R7 R“ VI-7-1 p-F-Ph H H H ch3 H F H OH H H VI-7-2 p-F-Ph H H ch3 CH3 H F H OH H H VI-7-3 p-F-Ph H H CH(CH3)2 ch3 H F H OH H H VI-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 H F H OH H H VI-7-6 p-F-Ph H H CH2Ph ch3 H F H OH H H VI-7-7 p-F-Ph H H CH2-indol-3-yl ch3 H F H OH H H VI-7-8 p-F-Ph H H CH2CH2SCH3 ch3 Ή F H OH H H VI-7-20 p-F-Ph * H * ch3 H F H OH H H *R2 and Rejoined together by (CFhb to form five-membered ring. 2983472-1 -189- PCT/US2008/058183 YVO 2008/121634 ΛΛ..„ΓΛ111

Docket No. 60137.0034WOU1

Table VI-8.

Ks R1 R1 -ψϊ- R36 R^“ Rs R6 X Y Ra VI-8-1 p-Cl-Ph H H H ch3 H F H OH H H VI-8-2 p-Cl-Ph H H ch3 ch3 H F H OH H H VI-8-3 p-CI-Ph H H CH(CH3)2 ch3 H F H OH H H VI-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 H F H OH H H VI-8-5 p-Cl-Ph H H CH2Ph ch3 H F H OH H H VI-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 H F H OH H H VI-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 H F H OH H H VI-8-8 p-CI-Ph ♦ H * ch3 H F H OH H H *R2 and RJb joined together by (CHhb to form five-membered ring. Table VI-9. RJ “"R3* R3* R4 Rs R6 X Y R7 Ru VI-9-1 p-Br-Ph H H H ch3 H F H OH H H VI-9-2 p-Br-Ph H H ch3 ch3 H F H OH H H VI-9-3 p-Br-Ph H H CH(CH3)2 ch3 H F H OH H H VI-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 H F H OH H H VI-9-6 p-Br-Ph H H CH2Ph ch3 H F H OH H H VI-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 H F H OH H H VI-9-8 p-Br-Ph H H CH2CH2SCH3 ch3 H F H OH H H VI-9-20 p-Br-Ph * H * ch3 H F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. Table VI-10. Ka R' R2 R31” R3b R4 R5 R6 X Y R7 r“ VI-10-1 p-I-Ph H H H ch3 H F H OH H H VI-10-2 p-I-Ph H H ch3 ch3 H F H OH H H VI-10-3 p-I-Ph H H CH(CH3)2 ch3 H F H OH H H VI-10-4 p-I-Ph H H CH2CH(CH3)i ch3 H F H OH H H VI-10-5 p-I-Ph H H CH2Ph ch3 H F H OH H H VI-10-6 p-I-Ph H H CH2-indol-3-yl ch3 H F H OH H H VI-10-7 p-I-Ph H H ch2ch2sch3 ch3 H F H OH H H VI-10-8 p-I-Ph * H * ch3 H F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -190- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Table Vl-ll.

Na Rl R3 RJfl T5 : R4 R> R6 X Y r Ra VI-11-1 ch3 H H H Et H F H OH H H VI-11-2 ch3 H H ch3 Et H F H OH H H VI-11-3 ch3 H H CH(CH3)2 Et H F H OH H H VI-11-4 ch3 H H CH2CH(CH3)2 Et H F H OH H H VI-11-5 ch3 H H CH2Ph Et H F H OH H H VI-11-6 ch3 H H CH2-indol-3-yl Et H F H OH H H VI-11-7 ch3 H H CH2CH2SCH3 Et H F H OH H H VI-11-8 “Χ7Γ2-T ch3 T^b- * H * Et H F H OH H H *R2 and Rejoined together by (CFkb to form five-membered ring.

Table VI-12.

N° R1 R2 R3" "R* R4 R3 R6 X Y ΊΓ R8 VI-12-1 Et H H H Et H F H OH H H VI-12-2 Et H H CH3 Et H F H OH H H VI-12-3 Et H H CHCCH,^ Et H F H OH H H VI-12-4 Et H H CH2CH(CH3)2 Et H F H OH H H VI-12-5 Et H H CH2Ph Et H F H OH H H VI-12-6 Et H H CH2-indoI-3-yl Et H F H OH H H VI-12-7 Et H H CH2CH2SCH3 Et H F H OH H H VI-12-8 Et * H ♦ Et H F H OH H H *R2 and RJb joined together by (CHa)3 to form five-membered ring. 5 Table VM 3. - ** HL '"

Ns R R3 R3" R3b R4 R5 R4 X Y R' R8 VI-13-1 "W H H H Et H F H OH H H VI-13-2 /pr H H ch3 Et H F H OH H H VI-13-3 'Pr H H CHtCHjh Et H F H OH H H VI-13-4 'Pr H H ΟΗ2ΟΗ(ΟΗ3)2 Et H F H OH H H VI-13-5 /Pr H H CH2Ph Et H F H OH H H VI-13-6 'Pr H H CH2-indol-3-yl Et H F H OH H H VI-13-7 'Pr H H CH2CH2SCH3 Et H F H OH H H VI-13-8 *Pr ή 3b”; * H * Et H F H OH H H ♦R2 and Rejoined together by (Cthht0 form five-membered ring.

2983472-J -191- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table VI-14.

Ns Rl R3b R4 r5" R6 X Y R7 R“ VI-14-1 'Bu H H H Et H F H OH H H VI-14-2 'Bu H H ch3 Et H F H OH H H VI-14-3 'Bu H H CH(CH3)2 Et H F H OH H H VI-14-4 'Bu H H CH2CH(CH3)2 Et H F H OH H H VI-14-5 'Bu H H CH2Ph Et H F H OH H H VI-14-6 'Bu H H CH2-indoI-3-yl Et H F H OH H H VI-14-7 'Bu H H ch2ch2sch3 Et H F H OH H H VI-14-8 "5^2-77.387: 'Bu * H * Et H F H OH H H *R7 and Rejoined together by (CHib to form five-membered ring.

Table VI-15.

Ns R1 R2 R3a r4" RJ R6 X Y R7 R# VI-15-1 Ph H H H Et H F H OH H H VI-15-2 Ph H H CH3 Et H F H OH H H VI-15-3 Ph H H CHiCH^ Et H p H OH H H VI-15-4 Ph H H CH2CH(CH3)2 Et H F H OH H H VI-15-5 Ph H H CH2Ph Et H F H OH H H VI-15-6 Ph H H CH2-indol-3-yl Et H F H OH H H VI-15-7 Ph H H CH2CH2SCH3 Et H F H OH H H VI-15-8 “Ϊ7Γ2-T Ph * H * Et H F H OH H H *R2 and R3*’joined together by (CH2)3 to form five-membered ring. 5 Table VI-16. —........................ w .» > e..... .........

Ns Rl R2 r3· R3b R4 RJ R6 X Y R7 R8 VI-16-1 p-Me-Ph H H H Et H F H OH H H VI-16-2 p-Me-Ph H H CH3 . Et H F H OH H H VI-16-3 p-Me-Ph H H CH(CH3)2 Et H F H OH H H VI-16-4 p-Me-Ph H H CH2CH(CH3)2 Et H F H OH H H VI-16-5 p-Me-Ph H H CH2Ph Et H F H OH H H VI-16-6 p-Me-Ph H H CH2-indol-3-yl Et H F H OH H H VI-16-7 p-Me-Ph H H CH2CH2SCH3 Et H F H OH H H VI-16-8 p-Me-Ph * H ♦ Et H F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. Table VI-17. Ns R’ R2 R3"- R35 R4 R5 R6 X Y R7 R“ 2983472-1 -192- PCT/US2008/058183 WO 2008/121634 . ,Λ1 __ ηΛ_ .,

Docket No. 60137.0034WOU1

Ns R1 R2 -jpr R3b R4 r! R6 X Y r’ fc VI-17-1 p-F-Ph H H H Et H F H OH H H VI-17-2 p-F-Ph H H ch3 Et H F H OH H H VI-17-3 p-F-Ph H H CHCCH^ Et H F H OH H H VI-17-4 p-F-Ph H H CH2CH(CH3)2 Et H F H OH H H VI-17-5 p-F-Ph H H CH2Ph Et H F H OH H H VI-17-6 p-F-Ph H H CH2-indol-3-yl Et H F H OH H H VI-17-7 p-F-Ph H H CH2CH2SCH3 Et H F H OH H H VI-17-8 p-F-Ph * H * Et H F H OH H H *R2 and Rejoined together by (0¾^ to form Five-membered ring

Table VI-18.

Ns R1 R2 R3b R4 R3 R6 X Y R7 R8 VI-18-1 p-Cl-Ph H H H Et H F H OH H H VI-18-2 p-Cl-Ph H H CH3 Et H F H OH H H VI-18-3 p-Cl-Ph H H CH(CH3)2 Et H F H OH H H VI-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H F H OH H H VI-18-5 p-Cl-Ph H H CH2Ph Et H F H OH H H VI-18-6 p-Cl-Ph H H CH2-indol-3-yl Et H F H OH H H VI-18-7 p-CI-Ph H H CH2CH2SCH3 Et H F H OH H H VI-18-8 p-Cl-Ph * H * Et H F H OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table VI-19.

Ns R1 R2 “R35- R3b R4 RJ R6 X Y R7 r“ VI-19-1 p-Br-Ph H H H Et H F H OH H H VI-19-2 p-Br-Ph H H ch3 Et H F H OH H H VI-19-3 p-Br-Ph H H CH(CH3)2 Et H F H OH H H VI-19-4 p-Br-Ph H H CH2CH(CH3)2 Et H F H OH H H VI-19-5 p-Br-Ph H H CH2Ph Et H F H OH H H VI-19-6 p-Br-Ph H H CH2-indol-3-yl Et H F H OH H H VI-19-7 p-Br-Ph H H CH2CH2SCH3 Et H F H OH H H VI-19-8 p-Br-Ph * H * Et H F H OH H H 5 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table VI-20.

Ns R’ R2 R3. R3b IT Rs R6 X Y R7 R8 VI-20-1 p-I-Ph H H H Et H F H OH H H 2983472-1 -193- PCT/US2008/058183 WO 2008/121634.. .nt„„ rvrMu/nin uocKet No. 60137.0034 wOU 1

Ns R1 r! “r37 “R* - R5 R* X Y R7 R8 VI-20-2 p-I-Ph H H ch3 Et H F H OH H H VI-20-3 p-I-Ph H H CH(CH3)2 Et H F H OH H H VI-20-4 p-I-Ph H H CH2CH(CH3)2 Et H F H OH H H VI-20-5 p-I-Ph H H CH2Ph Et H F H OH H H VI-20-6 p-I-Ph H H CH2-indol-3-yl Et H F H OH H H VI-20-7 p-I-Ph H H CH2CH2SCH3 Et H F H OH H H VI-20-8 p-I-Ph T^Jb· · . * H * Et H F H OH H H *R2 and RJb joined together by (0¾¼ to form five-membered ring.

Table VI-21.

Xa R1 R5 "r37 FC ΊΓ “R7- X Y IT R5^ Vl-21-1 CH3 H H H JPr H F H OH H H VI-21-2 ch3 H H ch3 'Pr H F H OH H H VI-21-3 ch3 H H CHiCHah 'Pr H F H OH H H VI-21-4 ch3 H H CH2CH(CH3)2 'Pr H F H OH H H VI-21-5 ch3 H H CH2Ph 'Pr H F H OH H H VI-21-6 ch3 H H CH2-indol-3-yl 'Pr H F H OH H H VI-21-7 ch3 H H CH2CH2SCH3 'Pr H F H OH H H VI-21-8 . ch3 * H * 'Pr H F H OH H H *R2 and RJb joined together by (CEhb to form five-membered ring.

Table VI-22.

X2 Rr “r37 “r35 r7" RJ R6 X Y R7 Ru VI-22-1 Et H H H "W H F H OH H H VI-22-2 Et H H CH3 'Pr H F H OH H H VI-22-3 Et H H CH(CH3)2 'Pr H F H OH H H VI-22-4 Et H H CH2CH(CH3)2 'Pr H F H OH H H VI-22-5 Et H H CH2Ph 'Pr H F H OH H H VI-22-6 Et H H CH2-indot-3-yl 'Pr H F H OH H H VI-22-7 Et H H CH2CH2SCH3 'Pr H F H OH H H VI-22-8 Et * H * 'Pr H F H OH H H 5 *R2 and R30 joined together by (CH^ to form five-membered ring.

Table VI-23.

Xa R R2 R3a R3t> R4 RJ R6 X Y R7 R8 VI-23-1 'Pr H H H 'Pr H F H OH H H VI-23-2 'Pr H H CH3 'Pr H F H OH H H 2983472-) -194- PCT/US2008/058183 WO 2008/121634 ΛΛΟ ,„7rvT1

Docket No. 60137.0034WOU 1

X° R1 ΊΓ R3a "R56 R4 RJ R6 X Y r’ R8 VI-23-3 'Pr H H CH(CH3)2 “'pT H F H OH H H VI-23-4 'Pr H H CH2CH(CH3)2 'Pr H F H OH H H VI-23-5 Tr H H CH2Ph 'Pr H F H OH H H VI-23-6 'Pr H H CH2-indol-3-yl 'Pr H F H OH H H VI-23-7 'Pr H H CH2CH2SCH3 'Pr H F H OH H H VI-23-8 :. /pr ΪΠΒΤ * H * 'Pr H F H OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table VI-24.

X2 R1 R2 "R35 nr R3 R6 X Y ΊΓ R8 VI-24-1 *Bu H H H 'Pr H F H OH H H VI-24-2 *Bu H H CH3 'Pr H F H OH H H VI-24-3 *Bu H H CHfCH^ 'Pr H F H OH H H VI-24-4 'Bu H H CH2CH(CH3)2 'Pr H F H OH H H VI-24-5 'Bu H H CH2Ph 'Pr H F H OH H H VI-24-6 H H CH2-indol-3-yl 'Pr H F H OH H H VI-24-7 'Bu H H CH2CH2SCH3 'Pr H F H OH H H VI-24-8 'Bu * H * 'Pr H F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table VI-25.

Xs R R2 R3’ R3b R4 Rs R6 X Y r R8 VI-25-1 Ph H H H "W H F H OH H H VI-25-2 Ph H H ch3 'Pr H F H OH H H VI-25-3 Ph H H CH(CH3)2 'Pr H F H OH H H VI-25-4 Ph H H CH2CH(CH3)2 'Pr H F H OH H H VI-25-5 Ph H H CH2Ph 'Pr H F H OH H H VI-25-6 Ph H H CH2-indol-3-yl 'Pr H F H OH H H . VI-25-7 Ph H H CH2CH2SCH3 'Pr H F H OH H H VI-25-8 Ph * H * 'Pr H F H OH H H 5 *R2 and Rejoined together by (CH^ to form five-membered ring.

Table VI-26.

X° R1 R' R3" R’ R4^ R3 R6 X Y R2 R8 VI-26-1 p-Me-Ph H H H 'Pr H F H OH H H VI-26-2 p-Me-Ph H H ch3 'Pr H F H OH H H VI-26-3 p-Me-Ph H H CHCCHa), 'Pr H F H OH H H 2983472-1 -195- WO 2008/121634 . nnQ,WOII1 uocKei No. 60137.0034WOU1

Xa R1 R2 Rib R4 R5 Ίτ X Y R7 R8 VI-26-4 p-Me-Ph H H CH2CH(CH3)2 /Pr H F H OH H H VI-26-5 p-Me-Ph H H CHaPh 'Pr H F H OH H H VI-26-6 p-Me-Ph H H CH2-indol-3-yI 'Pr H F H OH H H VI-26-7 p-Me-Ph H H CH2CH2SCH3 'Pr H F H OH H H VI-26-8 p-Me-Ph * H ♦ 'Pr H F H OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table VI-27.

Xa Rl R2 R3b R5 R6 X Y R R8 VI-27-1 p-F-Ph H H H 'Pr H F H OH H H VI-27-2 p-F-Ph H H ch3 'Pr H F H OH H H VI-27-3 p-F-Ph H H CH(CH3)2 'Pr H F H OH H H VI-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr H F H OH H H VI-27-5 p-F-Ph H H CH2Ph 'Pr H F H OH H H VI-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr H F H OH H H VI-27-7 p-F-Ph H H CH2CH2SCH3 'Pr H F H OH H H VI-27-8 p-F-Ph * H * 'Pr H F H OH H H *R2 and Rejoined together by (CHjja to form five-membered ring.

Table VI-28.

Xa R1 ΊΓ R3’ R3b R4 R5 R6 X Y IV R8 VI-28-1 p-Cl-Ph H H H “W H F H OH H H VI-28-2 p-Cl-Ph H H ch3 'Pr H F H OH H H VI-28-3 p-Cl-Ph H H CH(CH3)2 'Pr H F H OH H H VI-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr H F H OH H H VI-28-5 p-Cl-Ph H H CH2Ph Tr H F H OH H H VI-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr H F H OH H H VI-28-7 p-Cl-Ph H H CH2CH2SCH3 'Pr H F H OH H H VI-28-8 p-Cl-Ph * H ♦ 'Pr H F H OH H H 5 *R2 and RJb joined together by (CH^ to form five-membered ring.

Table VI-29.

Xs R1 TF -jps- R3b R4 Rs R6 X Y R7 R8 VI-29-1 p-Br-Ph H H H 'Pr H F H OH H H VI-29-2 p-Br-Ph H H ch3 'Pr H F H OH H H VI-29-3 p-Br-Ph H H CHCCHah 'Pr H F H OH H H VI-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr H F H OH H H 2983472-1 -196- PCT/US2008/058183 WO 2008/121634. τ zni„ π uocKet No. 60137.0034WOU1

Ns R1 ir R3a "R* R4 kr R6 X Y R R8 VI-29-5 p-Br-Ph H H CH2Ph 'Pr H F H OH H H VI-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr H F H OH H H VI-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr H F H OH H H VI-29-8 “ΣΪ72—T p-Br-Ph · i * H * 'Pr H F H OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table VI-30.

Na Rl R2 R17 “r35 R5 R6 X Y Ίν IT VI-30-1 p-I-Ph H H H "W H F H OH H H VI-30-2 p-I-Ph H H ch3 'Pr H F H OH H H VI-30-3 p-I-Ph H H CHICHah 'Pr H F H OH H H VI-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr H F H OH H H VI-30-5 p-I-Ph H H CH2Ph 'Pr H F H OH H H VI-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr H F H OH H H VI-30-7 p-I-Ph H H CH2CH2SCH3 'Pr H F H OH H H VI-30-8 p-I-Ph * H * 'Pr H F H OH H H ♦R2 and Rejoined together by (Cl-hb to form five-membered ring.

Table VI-31.

Ns R1 R2 R3a R3®- R4 R^ R6 X Y r" R8 VI-31-1 ch3 Η H H ”Bu H F H OH H H VI-31-2 ch3 H H CH3 "Bu H F H OH H H VI-31-3 ch3 H H CH(CH3)2 "Bu H F H OH H H VI-31-4 ch3 H H CH2CH(CH3)2 "Bu H F H OH H H VI-31-5 ch3 H H CH2Ph "Bu H F H OH H H VI-31-6 ch3 H H CH2-indol-3-yl "Bu H F H OH H H VI-31-7 ch3 H H CH2CH2SCH3 "Bu H F H OH H H VI-31-8 ch3 * H « "Bu H F H OH H H 5 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table VI-32.

Ns R RJ R3“ R3” R4 R5 R* X Y R7 R8 VI-32-1 Et H H H "Bu H F H OH H H VI-32-2 Et H H ch3 "Bu H F H OH H H VI-32-3 Et H H CH(CH3), "Bu H F H OH H H VI-32-4 Et H H CH2CH(CH3)2 "Bu H F H OH H H VI-32-5 Et H H CH2Ph "Bu H F H OH H H 2983472-1 -197- PCT/US2008/058183 WO 2008/121634 M ,niQ_ nnQ/1U7nT11 uocKet No. 60137.0034WOU1

Xs R1 R2 R3a R4 r! R0 X Y ΊΓ ΊΓ VI-32-6 Et H H CH2-indol-3-yl "Bu H F H OH H H VI-32-7 Et H H CH2CH2SCH3 "Bu H F H OH H H VI-32-8 Et ♦ H * "Bu H F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table VI-33.

Xa R R2 RJa R3b R4 RJ R6 X Y R? IC VI-33-1 *Pr H H H "Bu H F H OH H H VI-33-2 'Pr H H ch3 "Bu H F H OH H H VI-33-3 'Pr H H CH(CH3)2 "Bu H F H OH H H VI-33-4 'Pr H H CH2CH(CH3)2 "Bu H F H OH H H VI-33-5 'Pr H H CH2Ph "Bu H F H OH H H VI-33-6 'Pr H H CH2-indol-3-yl "Bu H F H OH H H VI-33-7 fpr H H ch2ch2sch3 "Bu H F H OH H H VI-33-8 'Pr ♦ H * "Bu H F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table VI-34.

Xs R R2 RSa IP5- R4 Rs R6 X Y R7 Ra VI-34-1 'Bu H H H "Bu H F H OH H H VI-34-2 'Bu H H ch3 "Bu H F H OH H H VI-34-3 'Bu H H CH(CH3)2 "Bu H F H OH H H VI-34-4 'Bu H H CH2CH(CH3)2 "Bu H F H OH H H VI-34-5 “Bu H H CH2Ph "Bu H F H OH H H VI-34-6 'Bu H H CH2-indol-3-yl "Bu H F H OH H H VI-34-7 'Bu H H CH2CH2SCH3 "Bu H F H OH H H VI-34-8 'Bu * H * "Bu H F H OH H H

Hl I II· II MW'I·! ......... I II ,1,1111 5 *R and R joined together by (CH2)3 to form five-membered ring.

Table VI-35.

R1 R2 r3. ΊΡ5 R4 r! Re X Y ΊΓ ΊΓ VI-35-1 Ph H H H "Bu H F H OH H H VI-35-2 Ph H H ch3 "Bu H F H OH H H VI-35-3 Ph H H CH(CH3h "Bu H F H OH H H VI-35-4 Ph H H CH2CH(CH3)2 "Bu H F H OH H H VI-35-5 Ph H H CH2Ph "Bu H F H OH H H VI-35-6 Ph H H CH2-indol-3-yl "Bu H F H OH H H 2983472-1 198- WO 2008(121634 Να 6Q137.0034WOU1 PCT/US2008/058183

Ns R1 RJ R" R4 Rs I? X Y R7 r“ VI-35-7 Ph H H ch2ch2sch3 "Bu H F H OH H H VI-35-8 - J Ph ίΠΒΤ ♦ H * "Bu H F H OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring

Table VI-36.

Xfi R‘ R3 r3“ R3b RJ V" X Y R7 R8 VI-36-1 p-Me-Ph H H H "Bu H F H OH H H VI-36-2 p-Me-Ph H H ch3 "Bu H F H OH H H VI-36-3 p-Me-Ph H H CH(CH3)2 "Bu H F H OH H H VI-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu H F H OH H H VI-36-5 p-Me-Ph H H CH2Ph "Bu H F H OH H H VI-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu H F H OH H H VI-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu H F H OH H H VI-36-8 p-Me-Ph * H * "Bu H F H OH H H *R2 and R3” joined together by "(CHjh to form five-membered ring.

Table VI-37.

Ks R‘ R3 "r35" "R35 R4 RJ R6 X Y R7 VI-37-1 p-F-Ph H H H "Bu H F H OH H H VI-37-2 p-F-Ph H H CH3 "Bu H F H OH H H VI-37-3 p-F-Ph H H CHCCH,), "Bu H F H OH H H VI-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu H F H OH H H VI-37-5 p-F-Ph H H CH2Ph "Bu H F H OH H H VI-37-6 p-F-Ph H H CH2-indol-3-yl "Bu H F H OH H H VI-37-7 p-F-Ph H H CH2CH2SCH3 "Bu H F H OH H H VI-37-8 “Ϊ7Γ2-r p-F-Ph ™Jb· ·- * H * "Bu H F H OH H H *R2 and RJD joined together by (Ct^ to form five-membered ring. 2983472-1 -199- PCT/US2008/058183

WO 2008/121634M uocKet No. 60137.0034WOU1

Table VI-38.

Ns R1 R2 R3a ’r35 R4 ΊΓ R6 X Y R7 ’R’H VI-38-1 p-Cl-Ph H H H "Bu H F H OH H H . VI-38-2 p-Cl-Ph H H ch3 "Bu H F H OH H H VI-38-3 p-Cl-Ph H H CH(CH3)2 "Bu H F H OH H H VI-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H F H OH H H VI-38-5 p-Cl-Ph H H CH2Ph "Bu H F H OH H H VI-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu H F H OH H H VI-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu H F H OH H H VI-38-8 p-Cl-Ph * H * "Bu H F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table VI-39.

Ns R1 R2 RJa R3b R4 RJ R6 X Y Tr Rb VI-39-1 p-Br-Ph H H H "Bu H F H OH H H VI-39-2 p-Br-Ph H H ch3 "Bu H F H OH H H VI-39-3 p-Br-Ph H H CH(CH3)2 "Bu H F H OH H H VI-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu H F H OH H H VI-39-5 p-Br-Ph H H CH2Ph "Bu H F H OH H H VI-39-6 p-Br-Ph H H CH2-indo]-3-yl "Bu H F H OH H H VI-39-7 p-Br-Ph H H CH2CH2SCH3 "Bu H F H OH H H VI-39-8 p-Br-Ph ♦ H * "Bu H F H OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table VI-40. ' i n Ik — ..--.1... .——j

Ns R1 R2 R3. R3b R4 ΊΓ R6 X Y ΊΓ R8 VI-40-1 p-I-Ph H H H "Bu H F H OH H H VI-40-2 p-I-Ph H H CH3 "Bu Η F H OH H H VI-40-3 p-I-Ph H H ΟΗ(ΟΗ3)2 "Bu H F H OH H H VI-40-4 p-I-Ph H H CHjCHCCH^ "Bu H F H OH H H VI-40-5 p-I-Ph H H CH2Ph "Bu H F H OH H H VI-40-6 p-I-Ph H H CHrindol-3-y1 "Bu H F H OH H H VI-40-7 p-I-Ph H H ch2ch2sch3 "Bu H F H OH H H Vl-40-8 _ □ p-I-Ph nJb · · . « H * "Bu H F H OH H H M 1 RL i ·ι > i i i i ........ *R and R joined together by (CH2)3 to form five-membered ring. 2983472-1 -200- PCT/US2008/058183 WO 2008/121634. T ΛΛ1 „ nn„.U/„T,, nocKet No. 60137.0034WOU1

Table VI-41.

n° R1 R2 R35 R R5 R6 X Y R' IT VI-41-1 ch3 H H H Bz H F H OH H H VI-41-2 ch3 H H ch3 Bz H F H OH H H VI-41-3 ch3 H H CH(CH3)2 Bz H F H OH H H VI-41-4 ch3 H H CH2CH(CH3)2 Bz H F H OH H H VI-41-5 ch3 H H CH2Ph Bz H F H OH H H VI-41-6 ch3 H H CH2-indol-3-yl Bz H F H OH H H VI-41-7 ch3 H H CH2CH2SCH3 Bz H F H OH H H VI-41-8 ch3 * H ♦ Bz H F H OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table VI-42.

Ns R1 R2 R3 R3b Ic Rs R6 X Y r’ R1* VI-42-1 Et H H H Bz H F H OH H H VI-42-2 Et H H CH3 Bz H F H OH H H VI-42-3 Et H H CH(CH3)2 Bz H F H OH H H VI-42-4 Et H H CH2CH(CH3)2 Bz H F H OH H H Vl-42-5 Et H H CH2Ph Bz H F H OH H H VI-42-6 Et H H CH2-indol-3-yl Bz H F H OH H H VI-42-7 Et H H CH2CH2SCH3 Bz H F H OH H H VI-42-8 Et * H * Bz H F H OH H H *R7 and Rejoined together by (ΟΗ2)3 to form five-membered ring. 5 Table VI-43. .- ---i „, -M., , -L. .....................,,., . ' , ,- ., I I 1

Ns R R7 R3. R3b R4 Rs R6 X Y R’ R# VI-43-1 "W H H H Bz H F H OH H H VI-43-2 'Pr H H CH3 Bz H F H OH H H VI-43-3 'Pr H H CH(CH3)j Bz H F H OH H H VI-43-4 'Pr H H CH2CH(CH3)2 Bz H F H OH H H VI-43-5 'Pr H H CH2Ph Bz H F H OH H H VI-43-6 ‘Pr H H CH2-indol-3-yI Bz H F H OH H H VI-43-7 'Pr H H CH2CH2SCH3 Bz H F H OH H Ifl VI-43-8 'Pr ♦ H * Bz H F H OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -201- WO 2008/121634 ΖΛ1„ Λ/ν,„„,Λ1τ1

Docket No. 60137.003 4WOU1 PCT/US2008/058183

Table VI-44.

Ns R RJ R3" R^ Iv Rs R6 X Y r" r8 VI-44-1 'Bu H H H Bz H F H OH H H VI-44-2 'Bu H H ch3 Bz H F H OH H H VI-44-3 'Bu H H CH(CH3)2 Bz H F H OH H H VI-44-4 'Bu H H CH2CH(CH3)2 Bz H F H OH H H VI-44-5 'Bu H H CH2Ph Bz H F H OH H H VI-44-6 'Bu H H CHrindol-3-yl Bz H F H OH H H VI-44-7 'Bu H H CH2CH2SCH3 Bz H F H OH H H VI-44-8 'Bu ♦ H * Bz H F H OH H H *R2 and RJb joined together by (CTfeb to form five-membered ring

Table VI-45.

Na R R2 r3. R3b R4 R5 R6 X Y R’ R" VI-45-1 Ph H H H Bz H F H OH H H VI-45-2 Ph H H ch3 Bz H F H OH H H VI-45-3 Ph H H CH(CH3)2 Bz H F H OH H H VI-45-4 Ph H H CH2CH(CH3)2 Bz H F H OH H H VI-45-5 Ph H H CH2Ph Bz H F H OH H H VI-45-6 Ph H H CH2-indol-3-yl Bz H F H OH H H VI-45-7 Ph H H ch2ch2sch3 Bz H F H OH H H VI-45-8 *«2 . .. Ph J b · * H * Bz H F H OH H H *R2 and R30 joined together by (CH2)3 to form five-membered ring. 5 Table VI-46. ' ---AL. " J II ! .I,·· I— ,111 ..<

Ns R1 “r37" R6 X Y R8 VI-46-1 p-Me-Ph H H H Bz H F H OH H H VI-46-2 p-Me-Ph H H ch3 Bz H F H OH H H VI-46-3 p-Me-Ph H H CHtCHah Bz H F H OH H H VI-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz H F H OH H H VI-46-5 p-Me-Ph H H CH2Ph Bz H F H OH H H VI-46-6 p-Me-Ph H H CH2-indol-3-yl Bz H F H OH H H VI-46-7 p-Me-Ph H H CH2CH2SCH3 Bz H F H OH H H VI-46-8 -τ p-Me-Ph ϊπβτί—r: * H « Bz H F H OH H H *R2 and Rejoined together by (0¾^ to form five-membered ring. 2983472-1 -202- WO 2008/121634., _n_ .. uocKet No. 60137.0034WOU1

Table VI-47.

Xs R' ΊΡ" R3a R3b “ST Rs R6 X Y R R* VI-47-1 p-F-Ph H H H Bz H F H OH H H VI-47-2 p-F-Ph H H ch3 Bz H F H OH H H VI-47-3 p-F-Ph H H CH(CH3)2 Bz H F H OH H H VI-47-4 p-F-Ph H H CH2CH(CH3)2 Bz H F H OH H H VI-47-5 p-F-Ph H H CH2Ph Bz H F H OH H H VI-47-6 p-F-Ph H H CH2-indot-3-yl Bz H F H OH H H VI-47-7 p-F-Ph H H CH2CH2SCH3 Bz H F H OH H H VI-47-8 p-F-Ph * H * Bz H F H OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table VI-48.

Ns R1 R1 r3. R,b R4 RJ R6 X Y R7 Rb VI-48-1 p-Cl-Ph H H H Bz H F H OH H H VI-48-2 p-Cl-Ph H H CH3 Bz H F H OH H H VI-48-3 p-CI-Ph H H CHCCHj), Bz H F H OH H H VI-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H F H OH H H VI-48-5 p-Cl-Ph H H CH2Ph Bz H F H OH H H VI-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz H F H OH H H VI-48-7 p-Cl-Ph H H ch2ch2sch3 Bz H F H OH H H VI-48-8 p-Cl-Ph ♦ H * Bz H F H OH H H *Ra and RJt} joined together by (CH2)3 to form five-membered ring. 5 Table VI-49. . -...... 1 w a

Ns R ΊΓ R3“ R3b R4 R5 R6 X Y R7 R“ VI-49-1 p-Br-Ph H H H Bz H F H OH H H VI-49-2 p-Br-Ph H H CH3 Bz H F H OH H H VI-49-3 p-Br-Ph H H CH(CH3)2 Bz H F H OH H H VI-49-4 p-Br-Ph H H CHjCHCCHjh Bz H F H OH H H VI-49-5 p-Br-Ph H H CH2Ph Bz H F H OH H H VI-49-6 p-Br-Ph H H CH2-indol-3-yl Bz H F H OH H H VI-49-7 p-Br-Ph H H CH2CH2SCH3 Bz H F H OH H H VI-49-8 . I p-Br-Ph * H * Bz H F H OH H H *R2 and RJt) joined together by (CH2)3 to form five-membered ring. 2983472-1 -203- WO 2008/121634 . ' Λ|__ ηηπ ,„,ΛΪΤΙ

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table VI-50.

Na R1 R2 "R^ R4 R5 X Y R R8 VI-50-1 p-I-Ph H H H Bz H F H OH H H VI-50-2 p-I-Ph H H ch3 Bz H F H OH H H VI-50-3 p-I-Ph H H CH(CH3)2 Bz H F H OH H H VI-50-4 p-I-Ph H H CH2CH(CH3)2 Bz H F H OH H H VI-50-5 p-I-Ph H H CH2Ph Bz H F H OH H H VI-50-6 p-I-Ph H H CH2-indol-3-yl Bz H F H OH H H VI-50-7 p-I-Ph H H CH2CH2SCH3 Bz H F H OH H H VI-50-8 p-I-Ph * H ♦ Bz H F H OH H H ♦R^ and R3b joined together by (CH2)3 to form five-membered ring.

Table VII-1.

Ns Rl R11 R3‘ R3* R4 R5 R6 X Υ R8 Ry VII-1-1 ch3 H H H ch3 H F Η ΟΗ Η Η νη2 VH-1-2 ch3 H H CH3 ch3 H F Η ΟΗ Η Η νη2 VII-1-3 ch3 H H CH(CH3)2 ch3 H F Η ΟΗ Η Η νη2 VII-1-4 ch3 H H CH2CH(CH3)2 ch3 Η F Η ΟΗ Η Η νη2 VII-1-5 ch3 H H CH2Ph ch3 Η F Η ΟΗ Η Η νη2 VII-1-6 ch3 H H CH2-indol-3-yl ch3 Η F Η ΟΗ Η Η νη2 VII-1-7 ch3 H H ch2ch2sch3 ch3 Η F Η ΟΗ Η Η νη2 VII-1-8 . ch3 ♦ H ♦ ch3 Η F Η ΟΗ Η Η νη2 *R7 and RJb joined together by (CH2)3 to form five-membered ring 2983472-1 -204- PCT/US2008/058183 WO 2008/121634ντ , ΛΛ„ .„,ΛΓ,,

Docket No. 60137.0034WOU1

Table VII-2.

Ns Rl RJ R3“ R^ R4 Rs R6 X Y R7 R8 R? VII-2-1 Et H H H ch3 H F H OH H H NH2 VII-2-2 Et H H ch3 ch3 H F H OH H H nh2 VII-2-3 Et H H CH(CH3)2 ch3 H F H OH H H nh2 VII-2-4 Et H H CH2CH(CH3)2 ch3 H F H OH H H nh2 VII-2-5 Et H H CH2Ph ch3 H F H OH H H nh2 VII-2-6 Et H H CH2-indol-3-yl ch3 H F H OH H H nh2 VII-2-7 Et H H CH2CH2SCH3 ch3 H F H OH H H nh2 VII-2-8 Et * H * ch3 H F H OH H H nh2 *RZ and Rejoined together by (CH2)3 to form five-membered ring.

Table VII-3.

Xa R1 R2 RJa Rib R4 Rs R6 X Υ R' R’ R9 VII-3-1 'Pr Η Η Η ch3 Η F Η ΟΗ Η Η νη2 VII-3-2 'Pr Η Η ch3 ch3 Η F Η ΟΗ Η Η νη2 VII-3-3 'Pr Η Η CH(CH3)2 ch3 Η F Η ΟΗ Η Η νη2 VII-3-4 'Pr Η Η CH2CH(CH3)2 ch3 Η F Η ΟΗ Η Η νη2 VII-3-5 'Pr Η Η CH2Ph ch3 Η F Η ΟΗ Η Η νη2 VII-3-6 'Pr Η Η CH2-indoI-3-yl ch3 Η F Η ΟΗ Η Η νη2 VII-3-7 'Pr Η Η CH2CH2SCH3 ch3 Η F Η ΟΗ Η Η νη2 VII-3-8 'Pr ♦ Η * ch3 Η F Η ΟΗ Η Η νη2 *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table VII-4. ‘............— — I --— 1 ......— · -I > I I 1 M -

Xa R R2 R3. Rib R4 Rs R6 X Y R7 R8 Rtf VI1-4-1 ΊΒΰ" H H H CH3 H F H OH H H nh2 VH-4-2 'Bu H H ch3 ch3 H F H OH H H nh2 VII-4-3 'Bu H H CHCCH,), ch3 H F H OH H H nh2 VII-4-4 'Bu H H CH2CH(CH3)2 ch3 H F H OH H H nh2 VII-4-5 'Bu H H CH2Ph ch3 H F H OH H H nh2 VII-4-6 'Bu H H CH2-indol-3-y1 ch3 H F H OH H H nh2 VII-4-7 'Bu H H CH2CH2SCH3 ch3 H F H OH H H nh2 VII-4-8 'Bu * H * ch3 H F H OH H H nh2 *R and R joined together by (CH2)3 to form five-membered ring. 2983472-1 -205 - PCT/US2008/058183 WO 2008/121634 ,.. _ ηΛ- ,uzrkT „

Docket No. 60137,0034WOU1

Table VII-5.

Xs R1 ΊΓ R3a R3b R^ R* R6 X Y F R# F VII-5-1 Ph H H H ch3 H F H OH H H nh2 VII-5-2 Ph H H ch3 ch3 H F H OH H H nh2 VH-5-3 Ph H H CH(CH3)2 ch3 H F H OH H H nh2 VII-5-4 Ph H H CH2CH(CH3)2 ch3 H F H OH H H nh2 VII-5-5 Ph H H CH2Ph ch3 H F H OH H H nh2 VII-5-6 Ph H H CH2-indol-3-yl ch3 H F H OH H H nh2 VII-5-7 Ph H H CH2CH2SCH3 ch3 H F H OH H H nh2 VII-5-8 Ph * H * ch3 H F H OH H H nh2 *R2 and RJb joined together by (CHah to form five-membered ring.

Table VII-6. ϋ R1 "ipr- "R35 F R5” F" X Y R7 R# F VII-6- p-Me-1 Ph H H H ch3 H F H OH H H NH2 VII-6- p-Me-2 Ph H H ch3 ch3 H F H OH H H nh2 VII-6- p-Me-3 Ph H H CHfCH^ ch3 H F H OH H H nh2 VII-6- p-Me-4 Ph H H CH2CH(CH3)2 ch3 H F H OH H H nh2 VII-6- p-Me-5 Ph H H CH2Ph ch3 H F H OH H H nh2 VII-6- p-Me-6 Ph H H CH2-indol-3- yi ch3 H F H OH H H nh2 VII-6- p-Me-7 Ph H H ch2ch2sch3 ch3 H F H OH H H nh2 VII-6- p-Me-8 Ph * H * ch3 H F H OH H H nh2 *R2 and RJb joined together by (0¾^ to form five-membered ring.

Table VII-7. R1 R2 R3‘ R3b R* R5 R6 X Y R7 R“ R^ VII-7-1 p-F- Ph H H Η ch3 H F H OH H H nh2 VII-7-2 p-F- Ph H H ch3 ch3 Η F H OH H H nh2 VII-7-3 p-F- H H CH(CH3)2 ch3 H F Η OH H H nh2 2983472-1 -206- PCT/US2008/058183 WO 2008/121634M rni„ vocicet No. 60137.0034WOU1

Xs R' R2 R3" R3b VII-7-4 Ph p-F- H H CH2CH(CH3)2 VI1-7-6 Ph p-F- H H CH2Ph VII-7-7 Ph p-F- H H CHrindol-3- VII-7-8 Ph p-F- H H yi ch2ch2sch3 VII-7- Ph p-F- ♦ H * 20 Ph ΊΓ R6 X Y r’ R8 R9 ch3 H F H OH H H NH2 ch3 H F H OH H H nh2 ch3 H F H OH H H nh2 ch3 H F H OH H H nh2 ch3 H F H OH H H nh2 *R2 and R·36 joined together by (CH2)3 to form five-membered ring.

Table VII-8. X2 Rl R2 R3a R* R4 ΊΓ R6 X Y R7 R8 R9 VII-8- 1 p-Cl- Ph Η H H ch3 Η F H OH H H NH2 VII-8- 2 p-Cl- Ph H H CH3 ch3 H F H OH H H nh2 VII-8- 3 p-Cl- Ph H H CH(CH3)2 ch3 H F H OH H H nh2 Vn-8- 4 p-Cl- Ph H H CH2CH(CH3)2 ch3 H F H OH H H nh2 VII-8- 5 p-Cl- Ph H H CH2Ph ch3 H F H OH H H nh2 VII-8- 6 p-Cl- Ph H H CH2-indol-3- yl ch3 H F H OH H H nh2 VII-8- 7 p-Cl- Ph H H CH2CH2SCH3 ch3 H F H OH H H nh2 VII-8- 8 p-Cl- Ph * H * ch3 H F H OH H H nh2 R RL· hm^—Mil· II ,, ιι·ι···ιι· *R and R joined together by (CH2)3 to form five-membered ring.

Table VII-9. Xs R R2 RJa R3t> R4 R5 R6 X Y R7 R“ R9 VI1-9- 1 p-Br- Ph H H H ch3 Η F Η OH H H nh2 VII-9- p-Br- Ph H H CH3 ch3 H F H OH H H nh2 2983472-1 -207- PCT/US2008/058183 WO 2008/121634.. ..... Λ__ ..vr.T n

Docket No. 60137.0034WOU1

Ks R1 R2 R3a r36 R4 R5 R6 X Y i? κ R5^ 2 VII-9- p-Br- H H CH(CH3)2 ch3 H F H OH H H NH2 3 Ph VII-9- p-Br- H H CH2CH(CH3)2 ch3 H F H OH H H nh2 4 Ph VII-9- p-Br- H H CH2Ph ch3 H F H OH H H nh2 6 Ph VII-9- p-Br- H H CH2-indol-3- ch3 H F H OH H H nh2 7 Ph yi VII-9- p-Br- H H ch2ch2sch3 ch3 H F H OH H H nh2 8 Ph VII-9- p-Br- * H * ch3 H F H OH H H nh2 *R2 and R30 joined together by (CH2)3 to form five-membered ring.

Table VII-10. R1 “IF R3a R3“ R4 R5 R6 X Y R7 R® R9 VII-10- 1 p-I- Ph H H H ch3 H F H OH H H nh2 vn-io- 2 p-I- Ph H H ch3 ch3 H F H OH H H nh2 VI1-10- 3 p-I- Ph H H CH(CH3)2 ch3 H F H OH H H nh2 VII-10- 4 p-I- Ph H H CH2CH(CH3)2 ch3 H F H OH H H nh2 VII-10- 5 p-I- Ph H H CH2Ph ch3 H F H OH H H nh2 VII-10- 6 p-I- Ph H H CH2-indol-3- yi ch3 H F H OH H H nh2 VII-I0- 7 p-I- Ph H H CH2CH2SCH3 ch3 H F H OH H H nh2 VII-10- 8 p-I- Ph * H * ch3 H F H OH H H nh2

...... I Rl· II I *R and R joined together by (CH^ to form five-membered ring. 2983472-1 -208- PCT/US2008/058183 WO 2008/121634.. ,... .,

uocKet No. 60137.0034WOUI

Table VII-11.

Xs R1 R2 R3a "R35 R4 Iv R6 X Y R7 R8 R^ VII-11-1 ch3 H H H Et H F H OH H H NH2 VII-11-2 ch3 H H ch3 Et H F H OH H H nh2 VII-11-3 ch3 H H CH(CH3)2 Et H F H OH H H nh2 VII-11-4 ch3 H H CH2CH(CH3)2 Et H F H OH H H nh2 VII-11-5 ch3 H H CH2Ph Et H F H OH H H nh2 VII-11-6 ch3 H H CH2-indol-3-yl Et H F H OH H H nh2 VII-11-7 ch3 H H CH2CH2SCH3 Et H F H OH H H nh2 VII-11-8 ch3 J* H * Et H F H OH H H nh2 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table VII-12.

Xs R I? R3’ R3” R4 R5 R6 X Y R7 R8 R^ V1I-12-1 Et H H H Et H F H OH H H NH2 VII-12-2 Et H H CH3 Et H F H OH H H nh2 VII-12-3 Et H H CH(CH3)2 Et H F H OH H H nh2 VII-12-4 Et H H CH2CH(CH3)2 Et H F H OH H H nh2 VII-12-5 Et H H CH2Ph Et H F H OH H H nh2 VH-12-6 Et H H CH2-indol-3-yl Et H F H OH H H nh2 VII-12-7 Et H H CH2CH2SCH3 Et H F H OH H H nh2 VII-12-8 Et + H ♦ Et H F H OH H H nh2 *R2 and R36 joined together by (CH2)3 to form five-membered ring. 5 Table VII-13. ' I Rl ί SI11 J naw

Xs R R3 R3* R3t> R4 RJ R6 X Y R7 R“ R5^ VII-13-1 ipr Η Η Η Et H F H OH H H nh2 Vn-13-2 /pr Η Η ch3 Et H F H OH H H nh2 VII-13-3 'Pr Η Η CH(CH3)2 Et H F H OH H H nh2 VII-13-4 'pr Η Η CH2CH(CH3)2 Et H F H OH H H nh2 VII-13-5 /pr Η Η CH2Ph Et H F H OH H H nh2 VII-13-6 'Pr Η Η CH2-indol-3-yl Et H F H OH H H nh2 V1I-13-7 'Pr Η Η CH2CH2SCH3 Et H F H OH H H nh2 VII-13-8 -77 'Pr * Η * Et H F H OH H H nh2 *R2 and R3b joined together by (CHib to form five-membered ring. 2983472-1 -209- PCT/US2008/058183 WO 2008/121634 M inm αλί au/ητ τ ι uocKei No. 60137.0034WOU1

Table VII-14. -Jfe RJ R 3b R36 R’ R5 R6 X Y R' R1 I? VII- 'Bu H H H Et H F H OH H H nh2 14-1 VII- 'Bu H H ch3 Et H F H OH H H nh2 14-2 VII- Έιι H H CH(CH3)2 Et H F H OH H H nh2 14-3 VII- 'Bu H H CH2CH(CH3)2 Et H F H OH H H nh2 14-4 VII- 'Bu H H CH2Ph Et H F H OH H H nh2 14-5 VII- 'Bu H H CHa-indol-3-yl Et H F H OH H H nh2 14-6 VII- 'Bu H H CH2CH2SCH3 Et H F H OH H H nh2 14-7 VII- 'Bu * H * Et H F H OH H H nh2 14-8 *R2 and RJ0 joined together by (CH2)3 to form five-membered ring. Table VII-15. "jfe R1" R* R3« 1 R3b R4 RJ R6 X Y R7 R5- R9' VII-15-1 Ph H H H Et H F H OH H H nh2 VH-15-2 Ph H H ch3 Et H F H OH H H nh2 VII-15-3 Ph H H CHiCH^ Et H F H OH H H nh2 VII-15-4 Ph H H CH2CH(CH3)2 Et H F H OH H H nh2 VII-15-5 Ph H H CH2Ph Et H F H OH H H nh2 VII-15-6 Ph H H CH2-indol-3-yl Et H F H OH H H nh2 VII-15-7 Ph H H ch2ch2sch3 Et H F H OH H H nh2 VII-15-8 Ph * H ♦ Et H F H OH H H nh2 *RZ and R3b joined together by (CPhb to form five-membered ring. Table VII-16. ip- RJ R3‘ R3b R4 R! R6 X Y R7 R# R9 VII-16- p-Me- H Η H Et H F H OH H Η NH2 2983472-1 -210- WO 2008/121634 K1 zn. „ uocKet No. 60137.0034WOU1

Ns r‘ ~ΊΡ~ “r35" R35 ΊΓ Ic R6 X Y tr r“ Ί7 1 C\ 1 p-Me- Ph H H ch3 Et H F H OH H H nh2 VII-16- 3 p-Me- Ph H H CH(CH3)2 Et H F H OH H H nh2 VII-16- 4 p-Me- Ph H H CH2CH(CH3)2 Et H F H OH H H nh2 VII-16- 5 p-Me- Ph H H CH2Ph Et H F H OH H H nh2 VII-16- 6 p-Me- Ph H H CH2-indol-3- yi Et H F H OH H H nh2 VH-16- 7 p-Me- Ph H H ch2ch2sch3 Et H F H OH H H nh2 VII-16- p-Me- ♦ H * Et H F H OH H H nh2

Ph *R^ and RJbjoined together by (0Η2)3 to form five-membered ring.

Table VII-17.

Ns R1 R2 R3a R3b R4 R3 R6 X Y R8 R9 VIJ-17- 1 p-F- Ph H H H Et H F H OH H H NH2 VII-17- 2 p-F- Ph H H ch3 Et H F H OH H H nh2 VII-17- 3 p-F- Ph H H CH(CH3)2 Et H F H OH H H nh2 VII-17- 4 p-F- Ph H H CH2CH(CH3)2 Et H F H OH H H nh2 VII-17- 5 p-F- Ph H H CH2Ph Et H F H OH H H nh2 VII-17- 6 p-F- Ph H H CH2-indol-3- yi Et H F H OH H H nh2 VII-17- 7 p-F- Ph H H CH2CH2SCH3 Et H F H OH H H nh2 VII-17- 8 p-F- Ph * H * Et H F H OH H H nh2 *R2 and Rat]oined together by (CH2)3 to form five-membered ring. 2983472-1 -211- PCT/US2008/058183 WO 2008/121634.. ,ηι _ nnOjKwrkT T1 uocKei No. 60137.0034WOU1

Table VII-18.

Xa R1 R2 R3b IF R* R6 X Y R7 Rs VII-18- 1 p-Cl- Ph H H H Et H F H OH H H nh2 VII-18- 2 p-Cl- Ph H H ch3 Et H F H OH H H nh2 VII-18- 3 p-Cl- Ph H H CH(CH3)2 Et H F H OH H H nh2 VII-18- 4 p-Cl- Ph H H CH2CH(CH3)2 Et H F H OH H H nh2 VII-18- 5 p-Cl- Ph H H CH2Ph Et H F H OH H H nh2 VII-18- 6 p-Cl- Ph H H CH2-indol-3- yi Et H F H OH H H nh2 VII-18- 7 p-Cl- Ph H H ch2ch2sch3 Et H F H OH H H nh2 VII-18- p-Cl- * H ♦ Et H F H OH H H nh2

Ph *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table VII-19.

Xa Rl R2 Rj. R3b R4 R5 R6 X Y R7 R» Rs VII-19- 1 p-Br- Ph Η H H Et H F H OH H H nh2 VII-19- 2 p-Br- Ph H H ch3 Et H F H OH H H nh2 VII-19- 3 p-Br- Ph H H CH(CH3)2 Et H F H OH H H nh2 VII-19- 4 p-Br- Ph H H CH2CH(CH3)2 Et H F H OH H H nh2 VII-19- 5 p-Br- Ph H H CH2Ph Et H F H OH H H nh2 VII-19- 6 p-Br- Ph H H CHrindol-3- yi Et H F H OH H H nh2 VII-19- 7 p-Br- Ph H H CH2CH2SCH3 Et H F H OH H H nh2 VII-19- p-Br- * H * Et H F H OH H H nh2 2983472-1 -212- WO 2008/121634.. .ΛΙ „ ηΛ0 ,u/ru „ uocKet No. 60137.0034WOU1 PCT/US2008/058183

Xs Rl R2 r3« “R36 R4 Rs R6 X Y R7 Rs if 8 Ph *R2 and R3b joined tog ether by (Cl-hb to form fi ve-memt tered ring. Table VI [-20. Xs R1 R2 'r35 R4 Rs R4 X Y R' Rg R9 VII-20-1 p-I-Ph H H H Et H F H OH H H nh2 VII-20-2 p-I-Ph H H ch3 Et H F H OH H H nh2 VII-20-3 p-I-Ph H H CH(CH3)2 Et H F H OH H H nh2 VII-20-4 p-I-Ph H H CH2CH(CH3)2 Et H F H OH H H nh2 VII-20-5 p-I-Ph H H CH2Ph Et H F H OH H H nh2 VII-20-6 p-I-Ph H H CH2-indol-3-yl Et H F H OH H H nh2 VII-20-7 p-I-Ph H H CH2CH2SCH3 Et H F H OH H H nh2 VII-20-8 p-I-Ph ♦ H * Et H F H OH H H nh2 ♦if and Rejoined together by (CH2)3 to form five-membered ring.

Table VII-21.

Xs R1^ R2 R3‘ R3b R4 RJ if X Y R7 R8 R9 VII-21-1 CH3 H H H 'Pr H F H OH H H nh2 VII-21-2 ch3 H H ch3 'Pr H F H OH H H nh2 VU-21-3 ch3 H H CH(CH3)2 'Pr H F H OH H H nh2 VII-21-4 ch3 H H CH2CH(CH3)2 'Pr H F H OH H H NH2 VII-21-5 ch3 H H CH2Ph 'Pr H F H OH H H nh2 VII-21-6 ch3 H H CH2-indol-3-yl 'Pr H F H OH H H nh2 VII-21-7 ch3 H H CH2CH2SCH3 'Pr H F H OH H H nh2 VII-21-8 ch3 * H * 'Pr H F H OH H H nh2 5 *R2 and R30 joined together by (0¾^ to form five-membered ring.

Table VII-22.

Xs ir R2 R3· R3b R4 R5 R6 X Y If R1 R9 VII-22-1 Et H H H H F H OH H H NH2 VII-22-2 Et H H ch3 'Pr H F H OH H H nh2 VII-22-3 Et H H CH(CH3)2 'Pr H F H OH H H nh2 VII-22-4 Et H H CHjCHiCHj), 'Pr H F H OH H H nh2 VII-22-5 Et H H CH2Ph 'Pr H F H OH H H nh2 VH-22-6 Et H H CH2-indol-3-yl 'Pr H F H OH H H nh2 VII-22-7 Et H H CH2CH2SCH3 'Pr H F H OH H H nh2 VH-22-8 Et * H * 'Pr H F H OH H H nh2 2983472-1 -213- PCT/US2008/058183 WO 2008/121634., Ληθ/1,νΛΤΤ1 uocKei No. 6013 7.0034WOU1 *R2 and R3t> joined together by (Cl·^ to form five-membered ring.

Table VII-23.

Ko R1 R2 “"Η35 R4 Iv R6 X Y R’ Ic R^ VII-23-1 'Pr H H H "W H F H OH H H NH2 VII-23-2 'Pr H H ch3 'Pr H F H OH H H nh2 VII-23-3 'Pr H H CH(CH3)2 'Pr H F H OH H H nh2 VII-23-4 'Pr H H CH2CH(CH3)2 'Pr H F H OH H H nh2 VU-23-5 'Pr H H CH2Ph 'Pr H F H OH H H nh2 VII-23-6 'Pr H H CH2-indol-3-yl 'Pr H F H OH H H nh2 VII-23-7 'Pr H H CH2CH2SCH3 'Pr H F H OH H H nh2 VII-23-8 'Pr * H * 'Pr H F H OH H H nh2 *R2 and R36 joined together by (CH2)3 to form five-membered ring.

Table VII-24.

Ko R R2 R3b R4 R5 R6 X Y R Rm R^ VII-24-1 'Bu H H H JPr H F H OH H H NH2 VII-24-2 'Bu H H CH3 'Pr H F H OH H H nh2 VII-24-3 'Bu H H CH(CH3)2 'Pr H F H OH H H nh2 VII-24-4 'Bu H H CH2CH(CH3)2 'Pr H F H OH H H nh2 VII-24-5 'Bu H H CH2Ph 'Pr H F H OH H H nh2 VII-24-6 'Bu H H CH2-indol-3-yi 'Pr H F H OH H H nh2 VU-24-7 'Bu H H CH2CH2SCH3 'Pr H F H OH H H nh2 VII-24-8 'Bu * H * 'Pr H F H OH H H nh2 5 *R2 and R3b joined together by (CH2)3 to fbrm^ve-membered ring.

Table VU-25.

Ks R R2 R3" R3b R4 R5 R6 X Y R’ R8 R^ VII-25-1 Ph H H H “ΨΓ H F H OH H H nh2 VII-25-2 Ph H H ch3 'Pr H F H OH H H nh2 VII-25-3 Ph H H CHCCHj), 'Pr H F H OH H H nh2 VU-25-4 Ph H H CH2CH(CH3)2 'Pr H F H OH H H nh2 VII-25-5 Ph H H CH2Ph 'Pr H F H OH H H nh2 VII-25-6 Ph H H CH2-indol-3-yl 'Pr H F H OH H H nh2 VH-25-7 Ph H H CH2CH2SCH3 'Pr H F H OH H H nh2 VII-25-8 j r Ph * H * 'Pr H F H OH H H nh2 *R2 and R3b joined together by ((¾¼ to form five-membered ring. 2983472-1 -214- PCT/US2008/058183 WO 2008/121634.. „ tnn_ . .. uocKet No. 60137.0034WOU1

Table VII-26.

Xe R' R2 “ipr -pB R4 RJ R0 X Y R7 r“ VII-26- 1 p-Me- Ph H H H 'Pr H F H OH H H NH2 VII-26- 2 p-Me- Ph H H ch3 'Pr H F H OH H II nh2 VII-26- 3 p-Me- Ph H H CH(CH3)2 'Pr H F H OH H H nh2 VII-26- 4 p-Me- Ph H H CH2CH(CH3)2 'Pr H F H OH H H nh2 VII-26- 5 p-Me- Ph H H CH2Ph 'Pr H F H OH H H nh2 VII-26- 6 p-Me- Ph H H CH2-indol-3- yi 'Pr H F H OH H H nh2 Vn-26- 7 p-Me- Ph H H ch2ch2sch3 'Pr H F H OH H H nh2 VII-26- 8 p-Me- Ph * H * 'Pr H F H OH H H nh2 *R2 and RJt> joined together by (CHih to form five-membered ring.

Table VII-27.

Xs R‘ R2 R3t R26 R4 RJ R6 X Y R7 R“ [<5 VII-27- 1 p-F- Ph H H H 'Pr H F H OH H H nh2 VII-27- 2 p-F- Ph H H ch3 'Pr H F H OH H H nh2 VII-27- 3 p-F- Ph H H CHiCH,), ipr H F H OH H H nh2 VII-27- 4 p-F- Ph H H CHjCHCCHih Tr H F H OH H H nh2 VII-27- 5 p-F- Ph H H CH2Ph 'Pr H F H OH H H nh2 VII-27- 6 p-F- Ph H H CH2-indol-3- yi 'Pr H F H OH H H nh2 VLI-27- 7 p-F- Ph H H CH2CH2SCH3 'Pr H F H OH H H nh2 VII-27- p-F- * H * 'Pr H F H OH H H nh2 2983472-1 -215- PCT/US2008/058183 WO 2008/121634 - ηΛο,ην™ π uocKet No. 60137.0034WOU 1

Nb R1 R2 R3“ ’ R3b R4 R5 R6 X Y R7 R? R9 8 Ph *R2 and R3b joined together by (CFkb to form five-membered ring.

Table VII-28.

Xs Rl R2 R36 IC R R6 X Y R; R8 Ί7 VII-28- 1 p-Cl- Ph H H H "¥7" H F H OH H H nh2 VII-28- 2 p-CI- Ph H H ch3 'Pr H F H OH H H nh2 VII-28- 3 p-Cl- Ph H H CH(CH3)2 'Pr H F H OH H H nh2 VII-28- 4 p-Cl- Ph H H CHjCHCCHsh 'Pr H F H OH H H nh2 VU-28- 5 p-Cl- Ph H H CH2Ph 'Pr H F H OH H H nh2 VII-28- 6 p-Cl- Ph H H CH2-indol-3- yi 'Pr H F H OH H H nh2 VII-28- 7 p-Cl- Ph H H CH2CH2SCH3 'Pr H F H OH H H nh2 VII-28- p-Cl- ♦ . H ♦ 'Pr H F H OH H H nh2

Ph *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table VII-29.

Xs R1 R1 r3« R* R4 R5 R6 X Υ R7 R“ R5 VII-29- 1 p-Br- Ph Η Η Η 'Pr Η F Η ΟΗ Η Η ΝΗ2 VII-29- 2 p-Br- Ph Η Η ch3 'Pr Η F Η ΟΗ Η Η νη2 VII-29- 3 p-Br- Ph Η Η CHCCHj^ 'Pr Η F Η ΟΗ Η Η νη2 VII-29- 4 p-Br- Ph Η Η CH2CH(CH3)2 *Ργ Η F Η ΟΗ Η Η νη2 VII-29- 5 p-Br- Ph Η Η CH2Ph 'Pr Η F Η ΟΗ Η Η νη2 VII-29- p-Br- Η Η CH2-indoI-3- 'Pr Η F Η ΟΗ Η Η νη2

Ph 2983472-1 -216- WO 2008ΛΠ634Νθ 6Q137.0034WOU1 PCT/US2008/058183

Na r1 R2 "r37 "R35 R4 RJ R6 X Y R7 r“ R5 6 yi VII-29- p-Br- H H ch2ch2sch3 'Pr H F H OH H H NH2 7 Ph VII-29- p-Br- * H * 'Pr H F H OH H H nh2

Ph *R2 and Rejoined together by (CH2)3 to form five-memberedring.

Table VII-30.

Na R‘ R2 RJa R3b R4 R' R6 X Y R' R“ R9 VI1-30- 1 VI1-30- 2 p-I-Ph H H H JPr H F H OH H H NH2 p-I-Ph H H CH3 'Pr H F H OH H H nh2 VII-30- 3 p-I-Ph H H CH(CH3)2 'Pr H F H OH H H nh2 VII-30- 4 p-I-Ph H H CH2CH(CH3)2 'Pr H F H OH H H nh2 VII-30- 5 p-I-Ph H H CH2Ph 'Pr H F H OH H H nh2 VII-30- 6 p-I-Ph H H CH2-indol-3-yl 'Pr H F H OH H H nh2 VII-30- 7 p-I-Ph H H CH2CH2SCH3 'Pr H F H OH H H nh2 VII-30- 8 ' 'j p-I-Ph * H ♦ 'Pr H F H OH H H nh2 *R2 and R3b joined together by (CH^ to form five-membered ring. 2983472-1 -217- WO 2008/121634.. <n|„ nfn/1wrvn uocKet No. 60137.0034 WOU1 PCT/US2008/058183

Table VII-31.

Ns Rl r’j ηρτ "R^ -R4'· RJ R0 X Y R7 RB R* VI1-314 ch3 H H H "Bu H F H OH H H nh2 VII-31-2 ch3 H H ch3 "Bu H F H OH H H nh2 VII-31-3 ch3 H H CH(CH3)2 "Bu H F H OH H H nh2 VII-31-4 ch3 H H CH2CH(CH3)2 "Bu H F H OH H H nh2 VII-31-5 ch3 H H CH2Ph "Bu H F H OH H H nh2 VII-31-6 ch3 H H CH2-indol-3-yl "Bu H F H OH H H nh2 VII-31-7 ch3 H H CH2CH2SCH3 "Bu H F H OH H H nh2 VII-31-8 ch3 * H * "Bu H F H OH H H nh2 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table VII-32.

Ns 1?" R2 -jpr R3b R4 if R6 X Υ Ra R9 VII-32-1 Et H H H "Bu Η F Η ΟΗ Η Η ΝΗ2 VII-32-2 Et H H ch3 "Bu Η F Η ΟΗ Η Η νη2 VII-32-3 Et H H CH(CH3)2 "Bu Η F Η ΟΗ Η Η νή2 VII-32-4 Et H H CH2CH(CH3)2 "Bu Η F Η ΟΗ Η Η νη2 V1I-32-5 Et H H CH2Ph "Bu Η F Η ΟΗ Η Η νη2 VII-32-6 Et H H CH2-indol-3-yl "Bu Η F Η ΟΗ Η Η νη2 VII-32-7 Et H H ch2ch2sch3 "Bu Η F Η ΟΗ Η Η νη2 VII-32-8 Et * H * "Bu Η F Η ΟΗ Η Η νη2 *R2 and Rjb joined together by (CH2)3 to form five-membered ring.

Ns R1 R2 R3’ R4 EC R6 X Y if R# R9 VII-33-1 ipr Η Η Η "Bu H F H OH H H NH2 VII-33-2 'Pr Η Η ch3 "Bu H F H OH H H nh2 VII-33-3 'Ργ Η Η CH(CH·,), "Bu H F H OH H H nh2 VII-33-4 /ρΓ Η Η CH2CH(CH3)2 "Bu H F H OH H H nh2 VII-33-5 'Pr Η Η CH2Ph "Bu H F H OH H H nh2 VII-33-6 /Ργ Η Η CH2-indol-3-yl "Bu H F H OH H H nh2 VII-33-7 /pr Η Η CH2CH2SCH3 "Bu H F H OH H H nh2 VII-33-8 'Pr * Η * "Bu H F H OH H H nh2 *R* and R30 joined together by (CH2)3 to form five-membered ring. 2983472-1 -218- PCT/US2008/058183 WO 2008/121634 ΛΛ„„„,Λ, „

Docket No. 60137.0034WOU1

Table V1I-34. Ττλ n1 R1 R2 R3" R3b ΊΤ~ R5 R6 X Y ΊΓ R8 Rs VII-34-1 'Bu H H H "Bu H F H OH H H NH2 VII-34-2 'Bu H H ch3 "Bu H F H OH H H nh2 VII-34-3 'Bu H H CHCCH^ "Bu H F H OH H H nh2 VII-34-4 'Bu H H CH2CH(CH3)2 "Bu H F H OH H H nh2 VII-34-5 'Bu H H CH2Ph "Bu H F H OH H H nh2· VII-34-6 'Bu H H CH2-indol-3-yl "Bu H F H OH H H nh2 VII-34-7 'Bu H H CH2CH2SCH3 "Bu H F H OH H H nh2 VII-34-8 'Bu * H * "Bu H F H OH H H nh2 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table VII-3S.

Tfk d' R1 R3 R3‘ R3b R4 r! R4 X Y R8" "R7- VII-35-1 Ph H H H "Bu H F H OH H H nh2 VII-35-2 Ph H H CH3 "Bu H F H OH H H nh2 VII-35-3 Ph H H CH(CH3)2 "Bu H F H OH H H nh2 VII-35-4 Ph H H CH2CH(CH3)2 "Bu H F H OH H H nh2 VI1-35-5 Ph H H CH2Ph "Bu H F H OH H H nh2 VII-35-6 Ph H H CH2-indo!-3-yl "Bu H F H OH H H nh2 VII-35-7 Ph H H CH2CH2SCH3 "Bu H F H OH H H nh2 VII-35-8 . r Ph Γ3ΒΤ- * H * "Bu H F H OH H H nh2 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Ns R1 R2 -jpr- "r35 R4 ΊΓ R4 X Y R7 R8 Ry VII- 36-1 p-Me- Ph H H H "Bu H F H OH H H nh2 VII- 36-2 p-Me- Ph H H ch3 "Bu H F H OH H H nh2 VII- 36-3 p-Me- Ph H H CH(CHj)j "Bu H F H OH H H nh2 VII- 36-4 p-Me- Ph H H CHjCHiCH^ "Bu H F H OH H H nh2 VII- 36-5 p-Me- Ph H H CH2Ph "Bu H F H OH H H nh2 VII- p-Me- Ph H H CH2-indol-3- "Bu H F H OH H H nh2 2983472-1 -219- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Ns "R1- "R3" R3a -R4” Ίν R6 X Y r’ Rtt R^ 36-6 yi VII- p-Me- H H ch2ch2sch3 "Bu H F H OH H H NH2 36-7 Ph VII- p-Me- * H * "Bu H F H OH H H nh2 36-8 Ph *R^ and Rejoined together by (CH2)3 to form five-membered ring"

Table VII-37.

Ns r1 R2 R3a -ps R4 Rs R6 X Υ ί? Ιν R5^ VII-37- 1 p-F- Ph H H H "Bu Η F Η ΟΗ Η Η ΝΗ2 VII-37- 2 p-F- Ph H H ch3 "Bu Η F Η ΟΗ Η Η νη2 VII-37- 3 p-F- Ph H H CHiCH^ "Bu Η F Η ΟΗ Η Η νη2 VII-37- 4 p-F- Ph H H CH2CH(CH3)2 "Bu Η F Η ΟΗ Η Η νη2 Vn-37- 5 p-F- Ph H H CH2Ph "Bu Η F Η ΟΗ Η Η νη2 VII-37- 6 p-F- Ph H H CH2-indol-3- yi "Bu Η F Η ΟΗ Η Η νη2 VII-37- 7 p-F- Ph H H ch2ch2sch3 "Bu Η F Η ΟΗ Η Η νη2 VII-37- 8 p-F- Ph * H * "Bu Η F Η ΟΗ Η Η νη2 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table VII-38. Ns R R^ RJa R3b R4 R5 R6 X Y R7 R" κ VII- 38-1 p-Cl- Ph H H H ”Bu H F H OH H H nh2 VII- 38-2 p-Cl- Ph H H ch3 "Bu H F H OH H H nh2 VII- 38-3 p-Cl- Ph H H CH(CH3)2 "Bu H F H OH H H nh2 VII- p-CI- H H CH2CH(CH3)2 "Bu H F H OH H H nh2

Ph 2983472-1 -220- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Ns R1 R2 R5” IC ΊΓ rs' X Y R R8 R9 38-4 VII- p-Cl- H H CH2Ph ”Bu H F H OH H H nh2 38-5 Ph VII- p-Cl- H H CH2-indoI-3- "Bu H F H OH H H nh2 38-6 Ph yi VII- p-Cl- H H CH2CH2SCH3 ”Bu H F H OH H H nh2 38-7 Ph VII- p-Cl- * H * ”Bu H F H OH H H nh2 38-8 "ΪΤΓ2 Ph , τ-xJb · · *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table VII-39.

Ns R1 R2 R3" -jps ΊΤ~ R5 ir X Y R7 ΊΓ "r7 VII- p-Br- Η H H "Bu H F H OH H H nh2 39-1 Ph VII- p-Br- H H ch3 MBu H F H OH H H nh2 39-2 Ph VII- p-Br- H H CH(CH3)2 rtBu H F H OH H H nh2 39-3 Ph VII- p-Br- H H CH2CH(CH3)2 MBu H F H OH H H nh2 39-4 Ph VII- p-Br- H H CH2Ph rtBu H F H OH H H nh2 39-5 Ph VII- p-Br- H H CH2-indol-3- ”Bu H F H OH H H nh2 39-6 Ph yi vn- p-Br- H H CH2CH2SCH3 rtBu H F H OH H H nh2 39-7 Ph VII- p-Br- ♦ H * ”Bu H F H OH H H nh2 39-8 Ph *R2i and RJb join ed to gethe :r by (CH2)3 to form fi ve-membered ring. Tab! e VII-40. Ns R‘ R2 RJl “r3® R4 RJ R® X Y R7 R“ Ry VII-40- p-I- H Η Η ”Bu H F H OH H H NH2 1 Ph VII-40- p-I- Ph Η Η ch3 ”Bu H F H OH H H nh2 2983472-1 -221- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ns R' R* R30 R3” R4 RJ R6 X Y r“ 2 VII-40- p-I- H H CH(CH3h "Bu H F H OH H H nh2 3 Ph VII-40- p-I- H H CH2CH(CH3)2 "Bu H F H OH H H nh2 4 Ph VII-40- p-I- H H CH2Ph "Bu H F H OH H H nh2 5 Ph VII-40- p-I- H H CH2-indol-3- "Bu H F H OH H H nh2 6 Ph y] VII-40- p-I- H H CH2CH2SCH3 "Bu H F H OH H H nh2 7 Ph VII-40- p-I- * H ♦ "Bu H F H OH H H NH2

Ph *R2 and R3” joined together by (CH2)3 to form five-membered ring.

Table VII-41.

Ka R1 r2 R3· R3b R4 Rs R6 X Y R’ R1 R9 VII-41-1 CH3 H H H Bz H F H OH H H nh2 VII-41-2 ch3 H H CH3 Bz H F H OH H H nh2 VII-41-3 ch3 H H CH(CH3>2 Bz H F H OH H H nh2 VII-41-4 ch3 H H CHjCHCCH^ Bz H F H OH H H nh2 VII-41-5 ch3 H H CH2Ph Bz H F H OH H H nh2 VI1-41-6 ch3 H H CHrindol-3-yl Bz H F H OH H H nh2 VII-41-7 ch3 H H CH2CH2SCH3 Bz H F H OH H H nh2 VII-41-8 ch3 ♦ H ♦ Bz H F H OH H H nh2 *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -222- PCT/US2008/058183 WO 2008/121634 . ,Α1„ηη-4Η,ΛΙΙ1 uocKet No. 60137.0034WOU1

Table VlI-42. N° R1 R2 RJa “R36 TT" RJ R6 X Y R7 Ra Ry VII-42-1 Et H H H Bz H F H OH H H NH2 VII-42-2 Et H H ch3 Bz H F H OH H H nh2 V1I-42-3 Et H H CH(CH3)2 Bz H F H OH H H nh2 VII-42-4 Et H H CH2CH(CH3)2 Bz H F H OH H H nh2 VII-42-5 Et H H CHzPh Bz H F H OH H H nh2 VII-42-6 Et H H CHrindol-3-yl Bz H F H OH H H nh2 VII-42-7 Et H H ch2ch2sch3 Bz H F H OH H H nh2 VII-42-8 ^τλ’2 , r Et iJb * H * Bz H F H OH H H nh2 *R2 and RJb joined together by (CFhb to form five-membered ring.

Table VII-43. J<2 R2 R3a R3b R4 r! R6 X Υ R7 ΊΤ Ίΐ5 VH-43-1 'Pr Η H H Bz H F H ΟΗ Η Η ΝΗ2 VII-43-2 'Pr H Η ch3 Bz H F Η ΟΗ Η Η νη2 VII-43-3 'Pr H H CH(CH3)2 Bz H F Η ΟΗ Η Η νη2 VII-43-4 'Pr H H CH2CH(CH3)2 Bz H F Η ΟΗ Η Η νη2 VII-43-5 'Pr H H CH2Ph Bz H F Η ΟΗ Η Η νη2 VII-43-6 'Pr H H CH2-indol-3-yl Bz H F Η ΟΗ Η Η νη2 VII-43-7 'Pr H H ch2ch2sch3 Bz H F Η ΟΗ Η Η νη2 VII-43-8 'Pr ♦ H * Bz H F Η ΟΗ Η Η νη2 *R2 and RJb joined together by (CHz)3 to form five-membered ring. 5 Table VII-44.

..........f ·ι » . ι B Ν2 R R2 R3“ R3b R4 R3 R6 X Y R7 R“ R5 VII-44-1 *Bu H H H Bz H F H OH H H NH2 VII-44-2 'Bu H H ch3 Bz H F H OH H H nh2 VII-44-3 'Bu H H CH(CH3)2 Bz H F H OH H H nh2 νΠ-44-4 'Bu H H CH2CH(CH3)2 Bz H F H OH H H NHj VII-44-5 'Bu H H CH2Ph Bz H F H OH H H nh2 VII-44-6 'Bu H H CH2-indol-3-yl Bz H F H OH H H nh2 VII-44-7 'Bu H H ch2ch2sch3 Bz H F H OH H H nh2 VII-44-8 'Bu * H ♦ Bz H F H OH H H nh2 *R2 and RJb joined together by (Cifcb to form five-membered ring. 2985472-1 -223- PCT/US2008/058183 WO 2008/121634., ,Λ1„„ Ληα4λνηιη uocKei No, 60137.0034WOU1

Table VII-45.

Ns R* R2 ~£3T R3b R4 Rs R6 X Y R7 R" VII-45-1 Ph H H H Bz H F H OH H H NH2 VII-45-2 Ph H H ch3 Bz H F H OH H H nh2 VII-45-3 Ph H H CH(CH3)2 Bz H F H OH H H nh2 VII-45-4 Ph H H CH2CH(CH3)2 Bz H F H OH H H nh2 VII-45-5 Ph H H CH2Ph Bz H F H OH H H nh2 VII-45-6 Ph H H CH2-indol-3-yl Bz H F H OH H H nh2 VII-45-7 Ph H H CH2CH2SCH3 Bz H F H OH H H nh2 VII-45-8 Ph * H * Bz H F H OH H H nh2 *R2 and joined together by (CH2)3 to form five-membered ring.

Table VII-46.

Ns R1 R2 r3. R,: R4 R5 R6 X Y R' R* VII- 46-1 p-Me- Ph Η Η Η Bz H F H OH H H nh2 VII- 46-2 p-Me- Ph Η Η ch3 Bz H F H OH H H nh2 VII- 46-3 p-Me- Ph Η Η CHCCHa^ Bz H F H OH H H nh2 VII- 46-4 p-Me- Ph Η Η CH2CH(CH3)2 Bz H F H OH H H nh2 VII- 46-5 p-Me- Ph Η Η CH2Ph Bz H F H OH H H nh2 VII- 46-6 p-Me- Ph Η Η CH2-indol-3- yi Bz H F H OH H H nh2 VII- 46-7 p-Me- Ph Η Η CH2CH2SCH3 Bz H F H OH H H nh2 VII- 46-8 p-Me- Ph ♦ Η * Bz H F H OH H H nh2 *R2 and R3b joined together by (CHibt0 ^orm five-membered ring.

Table VII-47. Ns R1 R2 R3’ R3b R4 R3 R6 X Y R7 R8 R’ VII-47- 1 p-F- Ph Η Η Η Bz Η F Η OH Η Η νη2 VII-47- p-F- Ph Η Η ch3 Bz Η F Η OH Η Η νη2 2983472-1 -224- PCT/US2008/058183 WO 2008/121634χ. <Λ1„_ „ uocxet No. 60137.0034WOU1

Ns R' R36 R ΊΓ R6 X Y r“ R5 2 VII-47- p-F- H H CH(CH3)2 BZ H F H OH H H nh2 3 Ph VII-47- p-F- H H CH2CH(CH3)2 Bz H F H OH H H nh2 4 Ph VII-47- p-F- H H CH2Ph Bz H F H OH H H nh2 5 Ph VII-47- p-F- H H CH2-tndol-3- Bz H F H OH H H nh2 6 Ph yi VII-47- p-F- H H ch2ch2sch3 Bz H F H OH H H nh2 7 Ph VII-47- p-F- 4 H ♦ Bz H F H OH H H nh2 8 Ph *R2 and Rejoined together by (CH2)3 to form five-membered ring

Table VII-48.

Ns R1 RJ R3a R3b Ic Rs R6 X Y R' R' Ry Vn-48- 1 p-CI- Ph Η H H Bz H F H OH H H NH2 VII-48- 2 p-Cl- Ph H H CH3 Bz H F H OH H H nh2 Vn-48- 3 p-Cl- Ph Η H CH(CH3)2 Bz Η F H OH H H nh2 VII-48- 4 p-Cl- Ph H H CH2CH(CH3)2 Bz H F H OH H H nh2 VD-48- 5 p-Cl- Ph H H CH2Ph Bz H F H OH H H nh2 VII-48- 6 p-Cl- Ph H H CH2-indol-3- yi Bz Η F H OH H H nh2 VII-48- 7 p-Cl- Ph H H ch2ch2sch3 Bz H F H OH H H nh2 VH-48- 8 -T p-CI- Ph n3b- . 4 H 4 Bz H F H OH H H nh2

W Ml· " !"*·.ι.ι··ι·ι·*·*^·ι I I . I *R and R joined together by (CFfeb to form five-membered ring. 2983472-1 -225- PCT/US2008/058183 WO 2008/121634

Docket No. 60137,0034WOU1

Table VU-49. R' R3 R^ "R36 R4 Rs R6 X Y ir r“ κ VII-49- 1 p-Br- Ph H H H Bz H F H OH H H nh2 VII-49- 2 p-Br- Ph H H ch3 Bz H F H OH H H nh2 VII-49- 3 p-Br- Ph H H CH(CH3)2 Bz H F H OH H H nh2 VII-49- 4 p-Br- Ph H H CH2CH(CH3)2 Bz H F H OH H H nh2 VII-49- 5 p-Br- Ph H H CH2Ph Bz H F H OH H H nh2 VI1-49- 6 p-Br- Ph H H CH2-indol-3- yi Bz H F H OH H H nh2 VII-49- 7 p-Br- Ph H H ch2ch2sch3 Bz H F H OH H H nh2 VII-49- p-Br- ♦ H * Bz H F H OH H H nh2

Ph *R2 and R3b joined together by (CEfe)? to form five-membered ring.

Table VII-50.

No R* R3 rJh Rab R4 RJ Iv X Y R’ R* R9 VII-50- p-I- H H H Bz H F H OH H H NH2 1 Ph VII-50- p-I- H H ch3 Bz H F H OH H H nh2 2 Ph VII-50- p-I- H H CH(CH3)2 Bz H F H OH H H nh2 3 Ph VII-50- p-I- H H CH2CH(CH3)2 Bz H F H OH H H nh2 4 Ph VII-50- p-I- H H CH2Ph Bz H F H OH H H nh2 5 Ph VII-50- p-I- H H CH2-indol-3- Bz H F H OH H H nh2 6 Ph yi VII-50- p-I- H H ch2ch2sch3 Bz H F H OH H H nh2 7 Ph VII-50- p-I- * H * Bz H F H OH H H nh2 2983472-1 -226- PCT/US2008/058183 WO 2008/121634 , „

Docket No. 60137.0034WOU 1

Ife R1 R2 R3a R3b R4 R5 R6 X Y R7 R8 R9 8 Ph ♦R12 and Rejoined together by (ΟΗ2)3 to form five-membered ring.

Table VIII-1.

Ns R1 R3a Rib R^ R5 R6 X Y r' r“ Vin-1-1 CH3 H H H ch3 H ch3 OH OH H H VID-1-2 ch3 H H ch3 ch3 H ch3 OH OH H H VHI-1-3 ch3 H H CH(CH3)2 ch3 H ch3 OH OH H H VIII-1-4 ch3 H H CH2CH(CH3)2 ch3 H ch3 OH OH H H VIII-1-5 ch3 H H CH2Ph ch3 H ch3 OH OH H H VIII-1-6 ch3 H H CH2-indol-3-yl ch3 H ch3 OH OH H H Vni-1-7 ch3 H H CH2CH2SCH3 ch3 H ch3 OH OH H H VIU-1-8 ch3 « H * ch3 H ch3 OH OH H H 1 ' ’Ik 5 *R and R joined together by (CH2)3 to form five-membered ring. 2983472-1 -227- PCT/US2008/058183 WO 2008/121634 „ Λη0/ηνΛΙ „ uocxet No. 60137.0034WOU1

Table VIII-2.

Xs R1 "R3" "R^ T* R4 Rs R6 X Y R8 VIII-2-1 Et H H H ch3 H ch3 OH OH H H VIH-2-2 Et H H ch3 ch3 H ch3 OH OH H H VlII-2-3 Et H H CHtCHak ch3 H ch3 OH OH H H VIII-2-4 Et H H CH2CH(CH3)2 ch3 H ch3 OH OH H H VIII-2-5 Et H H CH2Ph ch3 H ch3 OH OH H H VHI-2-6 Et H H CH2-indol-3-yl ch3 H ch3 OH OH H H VHI-2-7 Et H H CH2CH2SCH3 ch3 H ch3 OH OH H H VHI-2-8 Et * H * ch3 H ch3 OH OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table VIII-3.

Xa R R2 r3> R3b R4 Rs R6 X Y R7 R8 VHI-3-1 'Pr H H H CH3 H ch3 OH OH H H VIII-3-2 ipr H H CH3 ch3 Η ch3 OH OH H H VHI-3-3 ίρΓ H H CHiCH^ ch3 Η ch3 OH OH H H VIII-3-4 'Pr H H CH2CH(CH3)2 ch3 Η ch3 OH OH H H VII1-3-5 'Pr H H CH2Ph CH3 Η ch3 OH OH H H VIII-3-6 ,pr H H CH2-indol-3-yl ch3 Η ch3 OH OH H H VIII-3-7 *Pr H H CH2CH2SCH3 ch3 Η ch3 OH OH H H Vin-3-8 fpr ♦ H ♦ ch3 Η ch3 OH OH H H *R2 and RJb joined together by (CH^ to form five-membered ring. 5 Table VIII-4. .1 i— Ml .—ι II···-.·. , ..................

X° R* R2 RJl RJb R4 R5 R4 X Y R7 R8 VIII-4-1 *Bu H H H ch3 H ch3 OH OH H H VHI-4-2 feu H H CH3 ch3 Η ch3 OH OH H H VIII-4-3 'Bu H H CHCCHj), ch3 H ch3 OH OH H H VIII-4-4 'Bu H H CH2CH(CH3)2 ch3 H ch3 OH OH H H VIII-4-5 'Bu H H CH2Ph ch3 H ch3 OH OH H H VHI-4-6 Έιι H H CH2-indol-3-yl ch3 Η ch3 OH OH H H VIH-4-7 H H CH2CH2SCH3 ch3 H ch3 OH OH H H VIH-4-8 feu -.3b · * H * ch3 H ch3 OH OH H H *R2 and Rdt> joined together by (CH2)3 to form five-membered ring. 2983472»! -228- WO 2008/121634κτ zn, „„ nn„„,νΛΜ.. PCT/US2008/058183 vocKei No. 60137.0034WOU1

Table VHI-5.

Xa R2 R3" ΪΤ R4 RJ R6 X Y V Ra VI11-5-1 Ph H H H ch3 H ch3 OH OH H H VIII-5-2 Ph H H ch3 ch3 H ch3 OH OH H H VIII-5-3 Ph H H CH(CH3)2 ch3 H ch3 OH OH H H V1II-5-4 Ph H H CH2CH(CH3)2 ch3 H ch3 OH OH H H VIII-5-5 Ph H H CH2Ph ch3 H ch3 OH OH H H Vin-5-6 Ph H H CHj-indol-3-yI ch3 H ch3 OH OH H H VIH-5-7 Ph H H ch2ch2sch3 ch3 H ch3 OH OH H H VIII-5-8 J τ Ph ♦ H * ch3 H ch3 OH OH H H *R4 and Rejoined together by ((¾^ to form five-membered ring.

Table VIII-6.

Xa R1 R3a R3b R4 R5 Re X Y R’ R8 VIII-6- 1 p-Me- Ph H H H ch3 H ch3 OH OH H H vm-6- 2 p-Me- Ph H H CH3 ch3 H ch3 OH OH H H VIH-6- 3 p-Me- Ph H H CH(CH3)2 ch3 H ch3 OH OH H H viu-6- 4 p-Me- Ph H H CH2CH(CH3)2 ch3 H ch3 OH OH H H VIII-6- 5 p-Me- Ph H H CH2Ph ch3 H ch3 OH OH H H VIII-6- 6 p-Me- Ph H H CH2-indol-3- yi ch3 H ch3 OH OH H H VHI-6- 7 p-Me- Ph H H CH2CH2SCH3 ch3 H ch3 OH OH H H VIII-6- 8 p-Me- Ph * H * ch3 H ch3 OH OH H H *R2 and Rejoined together by (CHab to form five-membered ring.

Table VIII-7. Xs R R2 RJa R3b R4 R3 R6 X Y ΊΓ r“ VIH-7-1 p-F-Ph H H H ch3 H ch3 OH OH Η Η VIH-7-2 p-F-Ph H H CH3 ch3 H ch3 OH OH Η Η VIII-7-3 p-F-Ph H H CH(CH3)2 ch3 H ch3 OH OH Η Η 2983472-1 -229- PCT/US2008/058183 WO 2008/121634 χ. , A. 0 „ AA„ ...,-.,. uocKet No. 60137.0034WOU1

Xs R1 p- "R^ R3b TT R6 X Y R7" -RT VIH-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 H ch3 OH OH H H VIII-7-6 p-F-Ph H H CH2Ph ch3 H ch3 OH OH H H Vin-7-7 p-F-Ph H H CH2-indol-3-yl ch3 H ch3 OH OH H H VIII-7-8 p-F-Ph H H CH2CH2SCH3 ch3 H ch3 OH OH H H VIII-7-20 p-F-Ph * H * ch3 H ch3 OH OH H H *RZ and Rejoined together by (CH2)3 to form five-membered ring.

Table VIII-8.

Xs R1 R2 R3‘ RJb R4 R5 Rb X Y R' R VIH-8-1 p-Cl-Ph H H H ch3 H ch3 OH OH H H VIH-8-2 p-Cl-Ph H H CH3 ch3 Η ch3 oh OH H H VIII-8-3 p-Cl-Ph H H CH(CH3)2 ch3 H ch3 OH OH H H VIII-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 H ch3 oh OH H H VHI-8-5 p-Cl-Ph H H CH2Ph ch3 H ch3 OH OH H H VIII-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 Η ch3 OH OH H H VIII-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 H ch3 OH OH H H V1U-8-8 p-Cl-Ph * H * ch3 Η ch3 OH OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table VIII-9.

Xs R1 R2 R3* “r35 R4 rs R6 X Y R7 Ru VIU-9-1 p-Br- H H H ch3 H ch3 OH OH H H Ph VIII-9-2 p-Br- H H ch3 ch3 H ch3 OH OH H H Ph VIII-9-3 p-Br- H H CH(CH3)2 ch3 H ch3 OH OH H H Ph VIII-9-4 p-Br- H H CH2CH(CH3)2 ch3 H ch3 OH OH H H Ph VIH-9-6 p-Br- H H CH2Ph ch3 H ch3 OH OH H H Ph VIII-9-7 p-Br- H H CH2-indol-3- ch3 H ch3 OH OH H H Ph yi VIII-9-8 p-Br- H H CH2CH2SCH3 ch3 Η ch3 OH OH H H Ph VIU-9- p-Br- * H * ch3 H ch3 OH OH H H 20 Ph *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -230- PCT/US2008/058J83 WO 2008/121634.. ,Λ1 „„ nn„ .Π/Λ1 π uocKei No. 60137.0034WOU1

Table VIII-10.

Na Rl R? ”r*- -R3* ΊΓ~ RJ R* X Y R7 r" V1H-10-1 p-I-Ph H H H ch3 H ch3 OH OH H H VIH-10-2 p-I-Ph H H ch3 ch3 H ch3 OH OH H H VI1I-10-3 p-I-Ph H H CHCCl·^ ch3 H ch3 OH OH H H VHI-10-4 p-I-Ph H H CH2CH(CH3)2 ch3 H ch3 OH OH H H VIH-10-5 p-I-Ph H H CH2Ph ch3 H ch3 OH OH H H Vni-10-6 p-I-Ph H H CHrindol-3-yl ch3 H ch3 OH OH H H VIII-10-7 p-I-Ph H H CH2CH2SCH3 ch3 H ch3 OH OH H H VHI-10-8 p-I-Ph * H * ch3 H ch3 OH OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table VIII-11.

R R2 r3« R3b IC Rs R6 X Y ΊΓ R“ VIII-11-1 ch3 H H H Et H CH3 OH OH H H VIII-11-2 ch3 H H CH3 Et H ch3 OH OH H H VIII-11-3 ch3 H H CH(CH3)2 Et H ch3 OH OH H H VHI-11-4 ch3 H H CH2CH(CH3)2 Et H ch3 OH OH H H VIII-11-5 ch3 H H CH2Ph Et H ch3 OH OH H H VHI-11-6 ch3 H H CH2-indol-3-yl Et H ch3 OH OH H H VIU-11-7 ch3 H H CH2CH2SCH3 Et H ch3 OH OH H H VHI-11-8 ch3 * H * Et H ch3 OH OH H H ♦R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table VIII-12. ........ | η i . n . a

Na R R2 R35 R4 R5 R6 X Y R7 R8 VIII-12-1 Et H H H Et H CH3 OH OH H H Vin-12-2 Et H H ch3 Et H ch3 OH OH H H VIII-12-3 Et H H CHiCH,), Et H ch3 OH OH H H VIII-12-4 Et H H CH2CH(CH3)2 Et H ch3 OH OH H H VIII-12-5 Et H H CH2Ph Et H ch3 OH OH H H VIH-12-6 Et H H CH2-indol-3-yl Et H ch3 OH OH H H VIH-12-7 Et H H CH2CH2SCH3 Et H ch3 OH OH H H VIII-12-8 it. Et 35ΤΊ ♦ H * Et H ch3 OH OH H H ♦R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -231- PCT/US2008/058183 WO 2008/121634.. vocicet No. 60137.0034 WOUl

Table VIII-13.

K2 ΊΓ" R2 R3b R4 RJ R6 X Y R7 Rs VIII-13-1 'Pr H H H Et H ch3 OH OH H H VIII-13-2 'Pr H H ch3 Et H ch3 OH OH H H VIII-13-3 'Pr H H CH(CH3)2 Et H ci-i3 OH OH H H VIH-13-4 'Pr H H CH2CH(CH3)2 Et H ch3 OH OH H H VIII-13-5 'Pr H H CH2Ph Et H ch3 OH OH H H VIII-13-6 'Pr H H CH2-indot-3-yl Et H ch3 OH OH H H VIII-13-7 'Pr H H CH2CH2SCH3 Et H ch3 OH OH H H VIII-13-8 ipr * H >k Et H ch3 OH OH H H *R2 and R36 joined together by (CH2)3 to form five-membered ring.

Table VI1I-14.

Ns R R2 RJ‘ R3b R4 R5 R6 X Y I? Rs VIII-14-1 fBu H H H Et H ch3 OH OH H H VIII-14-2 'Bu H H ch3 Et H ch3 OH OH Η Η VIII-14-3 'Bu H H CHCCH,), Et H ch3 OH OH H Η VIII-14-4 'Bu H H CH2CH(CH3)2 Et H ch3 OH OH H Η VIII-14-5 'Bu H H CH2Ph Et H ch3 OH OH H Η VIII-14-6 'Bu H H CHrindol-3-yl Et H ch3 OH OH H Η VIII-14-7 'Bu H H CH2CH2SCH3 Et H ch3 OH OH H Η ΥΙΠ-14-8 'Bu * H * Et H ch3 OH OH H Η *R4 and RJb ioin&amp; dtoge ther b y (CH2)3 to form five-membered rii ig. 5 Table VIII-15.

' . .R.- —| I, ---------- ------ - - ί " ' U

Ns R R2 R3’ R3b ir R5 R4 X Y R’ r“ Vin-15-l Ph H Η Η Et H CH3 OH OH H H VHI-15-2 Ph H Η ch3 Et H ch3 OH OH H H VIII-15-3 Ph H Η CH(CH3)2 Et H ch3 OH OH H H VHI-15-4 Ph H Η CH2CH(CH3)2 Et H ch3 OH OH H H VIII-15-5 Ph Η Η CH2Ph Et H ch3 OH OH H H VIII-15-6 Ph Η Η CH2-indol-3-yl Et H ch3 OH OH H H VHI-15-7 Ph Η Η ch2ch2sch3 Et H ch3 OH OH H H VII1-15-8 _ jk, Ph * Η * Et H ch3 OH OH H H *Ra and Rejoined together by (Clkb to form five-membered ring. 2983472-1 -232- PCT/US2008/058183 WO 2008/121634.. nnQ/nvnT1] uocxei No. 60137.0034WOU1

Table VI1I-16.

Ns R1 “R5" R3" r3„ r R5 R6 X Y ir ic VIII-16- 1 p-Me- Ph H H H Et H ch3 OH OH H H VIII-16- 2 p-Me- Ph H H CH3 Et H ch3 OH OH H H VIII-16- 3 p-Me- Ph H H CH(CH3)2 Et H ch3 OH OH H H VIII-16- 4 p-Me- Ph H H CH2CH(CH3)2 Et H ch3 OH OH H H VIII-16- 5 p-Me- Ph H H CH2Ph Et H ch3 OH OH H H VIII-16- 6 p-Me- Ph H H CH2-indol-3- yi Et H ch3 OH OH H H VIlI-16- 7 p-Me- Ph H H ch2ch2sch3 Et H ch3 OH OH H H VIII-16- 8 p-Me- Ph * H ♦ Et H ch3 OH OH H H *R2 and R30 joined together by (CH2)3 to form five-membered ring.

Table V1II-17.

Ns R1 r1- r3. r” R4 Rs R6 X Y R7 Ra VIII-17-1 p-F-Ph H H H Et H ch3 OH OH H H VIII-17-2 p-F-Ph H H CH3 Et H ch3 OH OH H H VIII-17-3 p-F-Ph H H CH(CH3)2 Et H ch3 OH OH H H VIII-17-4 p-F-Ph H H CH2CH(CH3)2 Et H ch3 OH OH H H VIII-17-5 p-F-Ph H H CH2Ph Et H ch3 OH OH H H VIII-17-6 p-F-Ph H H CH2-indol-3-yl Et H ch3 OH OH H H VIII-17-7 p-F-Ph H H CH2CH2SCH3 Et H ch3 OH OH H H VHI-17-8 p-F-Ph * H * Et H ch3 OH OH H H *R2 and R3” joined together by (CH2)3 to form five-membered ring. 5 TabIeVIII-18. 1 ' ' t -n . '

Ns R1 R3 R3· R3b iF R3 R6 X Y R7 RK VIH-18-1 p-Cl-Ph H H H Et H CH3 OH OH H H VIII-18-2 p-Cl-Ph H H CH3 Et H ch3 OH OH H H VIII-18-3 p-CI-Ph H H CHCCHah Et H ch3 OH OH H H 2983472-1 -233- PCT/US2008/058183 WO 2008/121634κτ „. „ ΛΛΟ ..,

Docket No. 60137.0034WOU1

N2 R1 R5 R3a IF T" Rs R6 X Y iT R8 VIII-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H ch3 OH OH H H VHI-18-5 p-Cl-Ph H H CH2Ph Et H ch3 OH OH H H VHI-18-6 p-Cl-Ph H H CH2-indol-3-yl Et H ch3 OH OH H H VIII-18-7 p-Cl-Ph H H CH2CH2SCH3 Et H ch3 OH OH H H VIII-18-8 p-Cl-Ph ♦ H * Et H ch3 OH OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table VIII-19.

Ns R1. RJ RJa R3b ir R5 R6 X Y r' R* VIII-19-1 p-Br-Ph H H H Et H CH3 OH OH H H VIII-19-2 p-Br-Ph H H CH3 Et H ch3 OH OH H H VIII-19-3 p-Br-Ph H H CH(CH3)2 Et H ch3 OH OH H H VHI-I9-4 p-Br-Ph H H CH2CH(CH3)2 Et H ch3 OH OH H H VIII-19-5 p-Br-Ph H H CH2Ph Et H ch3 OH OH H H VUI-19-6 p-Br-Ph H H CH2-indol-3-yl Et H ch3 OH OH H H Vin-19-7 p-Br-Ph H H CH2CH2SCH3 Et H ch3 OH OH H H VIII-19-8 p-Br-Ph * H * Et H ch3 OH OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table VIII-20.

Ns r1- R2 r3. “r35 R4 R5 R6 X Y iu R“ VIII-20-1 p-I-Ph H H H Et H CH3 OH OH H H VIH-20-2 p-I-Ph H H CH3 Et H ch3 OH OH H H VUI-20-3 p-I-Ph H H CH(CH3)2 Et H ch3 OH OH H H VIII-20-4 p-I-Ph H H CH2CH(CH3)2 Et H ch3 OH OH H H VIII-20-5 p-I-Ph H H CH2Ph Et H ch3 OH OH H H VHI-20-6 p-I-Ph H H CH2-indol-3-yt Et H ch3 OH OH H H VIII-20-7 p-I-Ph H H CH2CH2SCH3 Et, H ch3 OH OH H H VIII-20-8 p-I-Ph * H * Et H ch3 OH OH H H 5 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table VIII-21.

Ns R1 R2 R3' -p; R4 RJ R6 X Y r’ R8 VIII-21-1 CH3 H H H ipr H CH3 OH OH H H VIII-21-2 ch3 H H ch3 'Pr H ch3 OH OH H H VHI-21-3 ch3 H H CH(CH3)2 'Pr H ch3 OH OH H H VIII-21-4 ch3 H H CH2CH(CH3)2 'Pr H ch3 OH OH H H 2983472-1 -234- PCT/US2008/058183 WO 2008/121634. ΛΛα,πνηττι uocKei No. 60137,0034WCHJ1

Ns R1 R2 R38 R4 R5 R' X Y I?’ R" VIH-21-5 ch3 H H CH2Ph "W H ch3 OH OH H H VIII-21-6 CH3 H H CH2-indol-3-yl 'Pr H ch3 OH OH H H VIII-21-7 ch3 H H CH2CH2SCH3 'Pr H ch3 OH OH H H VIII-21-8 ch3 + H * 'Pr H ch3 OH OH H H *RZ and R3b joined together by (CH2)3 to form five-membered ring.

Table VJII-22.

Jfe R R2 Rs“ R3b R4 R' R6 X Y R7 R“ VHI-22-1 Et H H H "W H ch3 OH OH H H VIII-22-2 Et H H ch3 'Pr H ch3 OH OH H H VII1-22-3 Et H H CH(CH3)2 'Pr H ch3 OH OH H H VIII-22-4 Et H H CH2CH(CH3)2 'Pr H ch3 OH OH H H VIII-22-5 Et H H CH2Ph 'Pr H ch3 OH OH H H VIII-22-6 Et H H CH2-indol-3-yl 'Pr H ch3 OH OH H H VIII-22-7 Et H H CH2CH2SCH3 'Pr H ch3 OH OH H H VHI-22-8 Et * H * 'Pr H ch3 OH OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table VIII-23.

Ns RJ R3 -jpr R35 RJ R^ X Y R* I? VHI-23-1 "Ψτ~ H H H 'Pr H ch3 OH OH H H VIII-23-2 'Pr H H ch3 'Pr H ch3 OH OH H H VIII-23-3 'pr H H CH(CH3)2 'Pr H ch3 OH OH H H VHI-23-4 'Pr H H CH2CH(CH3)2 'Pr H ch3 OH OH H H VHI-23-5 'Pr H H CH2Ph 'Pr H ch3 OH OH H H VIII-23-6 'Pr H H CH2-indol-3-yI 'Pr H ch3 OH OH H H VIII-23-7 'Pr H H CH2CH2SCH3 'Pr H ch3 OH OH H H VIII-23-8 'Pr * H * 'Pr H ch3 OH OH H H 5 *R2 and Rejoined together by (Cifeb to form five-membered ring.

Table VIII-24.

R Ic “ipr "r^ R'“ R6 X Y V R1 VIII-24-1 'Bu H H H TF H ch3 OH OH H H VHI-24-2 'Bu H H CH3 'Pr H ch3 OH OH H H VIII-24-3 *Bu H H CH(CH3)2 'Pr H ch3 OH OH H H VHI-24-4 'Bu H H CH2CH(CH3)2 'Pr H ch3 OH OH H H VIII-24-5 'Bu H H CH2Ph 'Pr H ch3 OH OH H H 2983472-1 -235- WO 2008/121634Νθ. 60137ioo34WoU1 PCT/US2008/058183

Xs T? RJ R3a R3b Ί?~ R5 X Y r’ R8 VIII-24-6 'Bu H H CH2-indol-3-yl /pr H ch3 OH OH H H VHI-24-7 'Bu H H CH2CH2SCH3 'Pr H ch3 OH OH H H VIII-24-8 'Bu + H ♦ 'Pr H ch3 OH OH H H *R2 and Rejoined together by (CFhk to form five-membered ring.

Table V1II-25.

Xs Rl Ί?” -£ΪΓ ~^E R5 R^ X Y R7 R8 VIII-25-1 Ph H H H "W H ch3 OH OH H H VHI-25-2 Ph H H ch3 'Pr H ch3 OH OH H H VIII-25-3 Ph H H CH(CH3)2 'Pr H ch3 OH OH H H VIII-25-4 Ph H H CH2CH(CH3)2 'Pr H ch3 OH OH H H VIII-25-5 Ph H H CH2Ph 'Pr H ch3 OH OH H H VW-25-6 Ph H H CH2-indol-3-yl 'Pr H ch3 OH OH H H VIII-25-7 Ph H H CH2CH2SCH3 Tr H ch3 OH OH H H VIU-25-8 Ph * H * 'Pr H ch3 OH OH H H *R2 and Rejoined together by (ΟΗ2)3 to form Five-membered ring.

Table VUI-26.

Xs R1 R2 r3« R^ Rs R6 X Y R7 Ra VII1-26- 1 p-Me- Ph H H H ”7p^ Η CH3 OH OH H H Vin-26- 2 p-Me- Ph H H CH3 'Pr Η ch3 OH OH H H VUI-26- 3 p-Me- Ph H H ΟΗ(ΟΗ3)2 'Pr Η ch3 OH OH H H VIII-26- 4 p-Me- Ph H H CH2CH(CH3)2 'Pr Η ch3 OH OH H H Vin-26- 5 p-Me- Ph H H CH2Ph 'Pr Η ch3 OH OH H H VIII-26- 6 p-Me- Ph H H CH2-indol-3- yi 'Pr Η ch3 OH OH H H VIU-26- 7 p-Me- Ph H H ch2ch2sch3 'Pr Η ch3 OH OH H H VUI-26- p-Me- « H * 'Pr Η ch3 OH OH H H

Ph 5 *R'i and RJb joined together by to form five-membered ring. 2983472-1 -236- WO 2008/121634., mwi/atii uocKet No. 60137.OO34WOU1

Table VIII-27. D1

Ns R1 ~F “F “F R5 R6 X Y r’ r“ VIII-27-1 p-F-Ph H H H Jpr H ch3 OH OH H H VIII-27-2 p-F-Ph H H CH3 'Pr H ch3 OH OH H H VIII-27-3 p-F-Ph H H CH(CH3)2 ipr H ch3 OH OH H H VIII-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr H ch3 OH OH H H VIII-27-5 p-F-Ph H H CH2Ph 'Pr H ch3 OH OH H H VHI-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr H ch3 OH OH H H VHI-27-7 p-F-Ph H H CH2CH2SCH3 'Pr H ch3 OH OH H H VIII-27-8 p-F-Ph * H ♦ 'Pr H ch3 OH OH H H *R2 and RJb joined together by (ΟΗ2)3 to form five-membered ring.

Table VIII-28.

Ns R1 R2 R3‘ R* Rs R6 X Y R7 R8 VIH-28-1 p-Cl-Ph H H H "W H CH3 OH OH H H VIH-28-2 p-Cl-Ph H H CH3 'Pr H ch3 OH OH H H VIII-28-3 p-Cl-Ph H H CH(CH3)2 'Pr H ch3 oh OH H H Vm-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr H ch3 OH OH H H VIII-28-5 p-Cl-Ph H H CH2Ph 'Pr H ch3 OH OH H H VIH-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr H ch3 OH OH H H VIII-28-7 p-Cl-Ph H H CH2CH2SCH3 'Pr H ch3 OH OH H H VIII-28-8 p-Cl-Ph ♦ H ♦ 'Pr H ch3 OH OH H H *R2 and RJt> joined together by (CH2)3 to form five-membered ring 5 Table VIII-29.

'T.............«...Μ.,.»—..·· I n__ J .....I H

Ns R1 R2 R3a R3b iF R5 R6 X Y IV R8 Vin-29-1 p-Br-Ph H H H FT" H ch3 OH OH H H VIH-29-2 p-Br-Ph H H CH3 'Pr H ch3 OH OH H H VIII-29-3 p-Br-Ph H H CHCCHah 'Pr H ch3 OH OH H H VIH-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr H ch3 OH OH H H VIII-29-5 p-Br-Ph H H CH2Ph 'Pr H ch3 OH OH H H VIII-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr H ch3 OH OH H H VIII-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr H ch3 OH OH H H VHI-29-8 1 ΓΊ p-Br-Ph 3b'·' '·'" j - * H * 'Pr H ch3 OH OH H H *R2 and R30 joined together by (CH2)3 to form five-membered ring. 2983472-1 -237- WO 2008/121634 . ..... PCT/US2008/058183 uocicet No. 60137.0034W0U1

Table V1II-30.

Ns R1 “r37 “Ν’5 R4 r!“ R4 X Y r’ Ra VIH-30-1 p-I-Ph H H H "W H ch3 OH OH H H VIII-30-2 p-I-Ph H H ch3 'Pr H ch3 OH OH H H VHI-30-3 p-I-Ph H H CH(CH3)2 'Pr H ch3 OH OH H H VIIl-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr H ch3 OH OH H H VHI-30-5 p-I-Ph H H CH2Ph /pr H ch3 OH OH H H VIII-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr H ch3 OH OH H H VIII-30-7 p-I-Ph H H CH2CH2SCH3 'Pr H ch3 OH OH H H VIH-30-8 p-I-Ph * H * 'Pr H ch3 OH OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table VIII-31.

Ns R RJ R3a R3b R4 R5 R6 X Y R' R“ VIH-31-1 CH3 Η Η Η "Bu H ch3 OH OH H H VHI-3I-2 ch3 Η Η ch3 "Bu H ch3 oh OH H H VIII-31-3 ch3 Η Η ΟΗ(ΟΗ3)2 "Bu H ch3 OH OH H H VIII-31-4 ch3 Η Η CH2CH(CH3)2 "Bu H ch3 OH OH H H VIlI-31-5 ch3 Η Η CH2Ph "Bu H ch3 OH OH H H VIII-31-6 ch3 Η Η CH2-indol-3-yl "Bu H ch3 OH OH H H VIU-31-7 ch3 Η Η CH2CH2SCH3 "Bu H ch3 OH OH H H VIH-31-8 ch3 * Η ♦ "Bu H ch3 OH OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table VIII-32. 1 — ‘1 R IL ' 1 ' J —y— I, »- ., ...

Ns r R2 RJ< R3b R4 RJ R4 X Y R7 R" VHI-32-1 Et H H H "Bu H ch3 OH OH H H VIII-32-2 Et H H ch3 "Bu Η ch3 OH OH Η H VIII-32-3 Et H H ch(ch3)2 "Bu H ch3 OH OH H H VIII-32-4 Et H H CH2CH(CH3)2 “Bu H ch3 OH OH Η H VUI-32-5 Et H H CH2Ph "Bu H ch3 OH OH H H VHI-32-6 Et H H CH2-indol-3-yl "Bu Η ch3 OH OH Η Η VIU-32-7 Et H H ch2ch2sch3 "Bu Η ch3 OH OH H Η VIII-32-8 Et * H * "Bu Η ch3 OH OH Η Η *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -238- WO 2008/121634 Κΐ ,ηι Q_ ηη1,»,ΛΙ11 uoctcei No. 60137.0034 WOUl

Table VIII-33.

Ns R1 R2 “R* "η*” R* R6 X Y R7 r“ VIII-33-1 'Pr H H H "Bu H ch3 OH OH H H VI1I-33-2 fPr H H ch3 "Bu H ch3 OH OH H H VIII-33-3 'Pr H H CH(CH3)2 "Bu H ch3 OH OH H H VIII-33-4 'Pr H H CH2CH(CH3)2 "Bu H ch3 OH OH H H VIII-33-5 'Pr H H CH2Ph "Bu H ch3 OH OH H H VIII-33-6 'Pr H H CH2-indol-3-yl "Bu H ch3 OH OH H H VIII-33-7 'Pr H H CH2CH2SCH3 "Bu H ch3 OH OH H H VIII-33-8 'Pr + H ♦ "Bu H ch3 OH OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table VIII-34.

Ns ir R1 Rji R3b R4 Rs R6 X Y R7 Ra VIII-34-1 'Bu H H H "Bu H ch3 OH OH H H VIII-34-2 'Bu H H CH3 "Bu H ch3 OH OH H H VUI-34-3 'Bu H H CH(CH3)2 "Bu H ch3 OH OH H H VUI-34-4 'Bu H H CH2CH(CH3)2 "Bu H ch3 OH OH H H Vin-34-5 'Bu H H CH2Ph "Bu H ch3 OH OH H H VIII-34-6 'Bu H H CH2-indol-3-yl "Bu H ch3 OH OH H H VIII-34-7 'Bu H H CH2CH2SCH3 "Bu H ch3 OH OH H H VUI-34-8 'Bu * H * "Bu H ch3 OH OH H H *R2 and R3” joined together by (CH2)a to form five-membered ring. 5 Table VIII-35.

II···· r . - - - .......... ......._ ί -z..... >1 B

Ns R R3« RJb R4 fV R6 X Y ΊΓ R1 Vm-35-1 Ph H H H "Bu H ch3 OH OH H H VIII-35-2 Ph H H CH3 "Bu H ch3 OH OH H H VIII-35-3 Ph H H CH(CH3)2 "Bu H ch3 OH OH H H VIH-35-4 Ph H H CH2CH(CH3)2 "Bu H ch3 OH OH H H VUI-35-5 Ph H H CH2Ph "Bu H ch3 OH OH H H VIII-35-6 Ph H H CH2-indol-3-yl "Bu H ch3 OH OH H H VIII-35-7 Ph H H CH2CH2SCH3 "Bu H ch3 OH OH H H VIII-35-8 Ph * H * "Bu H ch3 OH OH H H *Rii and R3b joined together by (ΟΗ2)3 to form five-membered ring. 2983472-1 -239- WO 2008/121634M ηη7/1\νηττι uocKet No. 60137.0034WOU1 PCT/US2008/058183

Table VIII-36. — r2" R30 r35 R4 R5 R6 X Y R7 iv VIII-36- p-Me-1 Ph H H H "Bu H ch3 OH OH H H VIII-36- p-Me-2 Ph H H ch3 "Bu H ch3 OH OH H H VIII-36- p-Me-3 Ph H H CH(CH3)2 "Bu H ch3 OH OH H H VIII-36- p-Me-4 Ph H H CH2CH(CH3)2 "Bu H ch3 OH OH H H VIII-36- p-Me-5 Ph H H CH2Ph "Bu H ch3 OH OH H H VIII-36- p-Me- H H CH2-indol-3- "Bu H ch3 OH OH H H 6 Ph yi VIII-36- p-Me-7 Ph H H ch2ch2sch3 "Bu H ch3 OH OH H H VIII-36- p-Me-8 Ph * H * "Bu H ch3 OH OH H H *R2 and RJt> joined together by (CH2)3 to form five-membered ring. Table VIII-37. Ns R1 R2 R3“ "r35 R4 R5 R6 X Y R7 R“ VIII-37-1 p-F-Ph H H H "Bu H ch3 OH OH H H VIII-37-2 p-F-Ph H H CH3 "Bu H ch3 OH OH H H VIII-37-3 p-F-Ph H H CHfCH^ "Bu H ch3 OH OH H H VIII-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu H ch3 OH OH H H VIII-37-5 p-F-Ph H H CH2Ph "Bu H ch3 OH OH H H VIII-37-6 p-F-Ph H H CH2-indol-37yI "Bu H ch3 OH OH H H VIII-37-7 p-F-Ph H H ch2ch2sch3 "Bu H ch3 OH OH H H VIH-37-8 p-F-Ph * H * "Bu H ch3 OH OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring. Table VIII-38. R1 R1 “r35 R4 R3 Rfi X Y R’ R8 VIII-38- I p-CI- Ph H H H "Bu H ch3 oh OH H H VIII-38- p-Cl- Ph H H CH3 "Bu H ch3 OH OH Η Η 2983472-] -240- W0 2θ08ϋ£ί8? No. 60137.0034WOU1 PCT/US2008/058183

Xa Rl R2 -pr R3b R4 R3 R6 X Y R7 R* 2 VIII-38- 3 p-Cl- Ph H H CH(CH3)2 "Bu H ch3 OH OH H H VIII-38- 4 p-Cl- Ph H H CH2CH(CH3)2 "Bu H ch3 OH OH H H Vin-38- 5 p-Cl- Ph H H CH2Ph "Bu H ch3 OH OH H H VIH-38- 6 p-Cl- Ph H H CH2-indol-3- yi "Bu H ch3 OH OH H H VIII-38- 7 p-Cl- Ph H H ch2ch2sch3 "Bu H ch3 OH OH H H VIII-38- p-Cl- * H * "Bu H ch3 OH OH H H

Ph *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table VIII-39.

Xs Rl R2 RJa R3b R4 R5 R6 X Y R' • Ra VUI-39- 1 p-Br- Ph H H H "Bu H ch3 OH OH H H VUI-39- 2 p-Br- Ph H H ch3 "Bu H ch3 OH OH H Η Vm-39- 3 p-Br- Ph H H CH(CH3)2 "Bu H ch3 OH OH H H VIII-39- 4 p-Br- Ph H H CH2CH(CH3)2 "Bu H ch3 OH OH H H VUI-39- 5 p-Br- Ph H H CH2Ph "Bu H ch3 OH OH H Η V11I-39- 6 p-Br- Ph H H CH2-indol-3- yi "Bu H ch3 OH OH H H VIII-39- 7 p-Br- Ph H H CH2CH2SCH3 "Bu H ch3 OH OH H H VIII-39- 8 _ .1 T p-Br- Ph ♦ H * "Bu H ch3 OH OH H Η ♦R^ and R36 joined together by (CH2)3 to form five-membered ring. 2983472-1 -241- WO 2008/121634No. 60i37.0034WOUl PCT/US2008/058183

Table VIII-40.

Ns R1 R2 Rja I?'- R4 RJ R6 X Y ΊΓ VIII-4G-1 p-I-Ph H H H "Bu H ch3 OH OH H H VIII-40-2 p-I-Ph H H ch3 "Bu H ch3 OH OH H H VIII-40-3 p-I-Ph H H CH(CH3)2 "Bu H ch3 OH OH H H VIII-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu H ch3 OH OH H H VHI-40-5 p-I-Ph H H CH2Ph "Bu H ch3 OH OH H H VIII-40-6 p-I-Ph H H CH2-indol-3-yl "Bu H ch3 OH OH H H VIII-40-7 p-I-Ph H H CH2CH2SCH3 "Bu H ch3 OH OH H H VIII-40-8 p-I-Ph 4 H * "Bu H ch3 OH OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table ΥΠΙ-41.

Xs R1 R4 RJ“ R3t> R4 Rs R6 X Y R' R* VIII-41-1 CH3 H H H Bz H ch3 OH OH H H VIII-41-2 CH3 H H CH3 Bz H CH3 OH OH H H VUI-41-3 ch3 H H CHCCHah Bz H CH3 OH OH H H VIII-41-4 ch3 H H CH2CH(CH3)2 Bz H ch3 OH OH H H VIII-41-5 ch3 H H CH2Ph Bz H ch3 OH OH H H VIII-41-6 ch3 H H CH2-indol-3-yl Bz H ch3 OH OH H H VHI-41-7 ch3 H H CH2CH2SCH3 Bz H ch3 OH OH H H VIII-41-8 ch3 ♦ H * Bz H ch3 OH OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table VIII-42. 11 " I ' , .......... II I I j J .......... ,1, —*..... '

Xs R R1 R3“ R3b R4 Rs R6 X Y R7 R8 Vni-42-1 Et H H H Bz H CH3 OH OH H H Vni-42-2 Et H H CH3 Bz H ch3 OH OH H H VHI-42-3 Et H H CH(CH3)2 Bz H ch3 OH OH H H VIII-42-4 Et H H CH2CH(CH3)2 Bz H ch3 OH OH H H VIII-42-5 Et H H CH2Ph Bz H ch3 OH OH H H VIII-42-6 Et H H CH2-indol-3-yI Bz H ch3 OH OH H H VIII-42-7 Et H H CH2CH2SCH3 Bz H ch3 OH OH H H VIII-42-8 ' . n Et * H * Bz H ch3 OH OH H H IR 11 IIL 11 ...... 11 *R and R joined together by (CKhk to form five-membered ring. 2983472-1 -242- WO 2008/121634Νθ 6Q137,0034WOU1 PCT/US2008/058183

Table VIII-43.

Ns "R1” R2 R3’ ΊΓ“ Rs R6 X Y r“ VIH-43-1 'Pr H H H Bz H ch3 OH OH H H VIII-43-2 'Pr H H ch3 Bz H ch3 OH OH H H VIII-43-3 'Pr H H CH(CH3)2 Bz H ch3 OH OH H H VIII-43-4 ‘Pr H H CH2CH(CH3)2 Bz H ch3 OH OH H H VIII-43-5 'Pr H H CH2Ph Bz H ch3 OH OH H H VIII-43-6 'Pr H H CH2-indol-3-yl Bz H ch3 OH OH H H VIII-43-7 'Pr H H CH2CH2SCH3 Bz H ch3 OH OH H H VIII-43-8 'Pr ♦ H ♦ Bz H ch3 OH OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table VIII-44.

Ns RT" !? R7* R3b R^ ΊΓ R6 X Y R' Ra V1H-44-1 'Bu H H H Bz H ch3 OH OH H H VHI-44-2 'Bu H H CH3 Bz H ch3 OH OH H H VUI-44-3 'Bu H H CHCCH^ Bz H ch3 OH OH H H VIU-44-4 'Bu H H CH2CH(CH3)2 Bz H ch3 OH OH H H VHI-44-5 'Bu H H CH2Ph Bz H ch3 OH OH H H VIII-44-6 'Bu H H CHrindol-3-yl Bz H ch3 OH OH H H VIII-44-7 'Bu H H CH2CH2SCH3 Bz H ch3 OH OH H H VHI-44-8 'Bu * H ♦ Bz H ch3 OH OH H H *R2 and R36 joined together by (CH2)3 to form five-membered ring. 5 Table VIII-45. 1 1 X 1- XL " ' ' ' J 1 “ ' 1 f.'L·'· "* <1 fl

Ns R R* r3. R3b IT R5 R* X Y R7 R8 VIH-45-1 Ph H H H Bz H ch3 OH OH H H VIU-45-2 Ph H H CH3 Bz H ch3 OH OH H H VIII-45-3 Ph H H ΟΗ(ΟΗ3)ί Bz H ch3 OH OH H H VIII-45-4 Ph H H CH2CH(CH3)2 Bz H ch3 OH OH H H VIII-45-5 Ph H H CH2Ph Bz H ch3 OH OH H H VIII-45-6 Ph H H CH2-indol-3-yl Bz H ch3 OH OH H H VIII-45-7 Ph H H CH2CH2SCH3 Bz H ch3 OH OH H H VHI-45-8 Ph * H * Bz H ch3 OH OH H H *R2 and R30 joined together by (Ctbb to form five-membered ring. 2983472-1 -243- WO 2008/121634 No_ 60i 37,0034WOU1 PCT/US2008/058183

Table VIII-46.

Xa Rl R2 R3’ ΊΓ" R6 X Y R7 R“ VIII-46- 1 p-Me- Ph H H H Bz H ch3 OH OH H H VIII-46- 2 p-Me- Ph H H ch3 Bz H ch3 OH OH H H VIII-46- 3 p-Me- Ph H H CH(CH3)2 Bz H ch3 OH OH H H VIII-46- 4 p-Me- Ph H H CH2CH(CH3)2 Bz H ch3 OH OH H H VIII-46- S p-Me- Ph H H CH2Ph Bz H ch3 OH OH H H VIII-46- 6 p-Me- Ph H H CH2-tndol-3- yi Bz H ch3 OH OH H H VIII-46- 7 p-Me- Ph H H ch2ch2sch3 Bz H ch3 OH OH H H VIII-46- p-Me- * H * Bz H ch3 OH OH H H

Ph *R2 and R31’joined together by (CH2)3 to form five-membered ring.

Table Vffl-47.

Xa Rl r'·1 Rj. r35 r3·” Rs R^ X Y R7 ΊΓ VIII-47-1 p-F-Ph H H H Bz H CH3 OH OH H H VIII-47-2 p-F-Ph H H ch3 Bz H ch3 OH OH H H VIII-47-3 p-F-Ph H H CH(CH3)2 Bz H ch3 OH OH H H VIII-47-4 p-F-Ph H H CH2CH(CH3)2 Bz H ch3 OH OH H H VIII-47-5 p-F-Ph H- H CHaPh Bz H ch3 OH OH H H VIII-47-6 p-F-Ph H H CH2-indol-3-yl Bz H ch3 OH OH H H VIH-47-7 p-F-Ph H H CH2CH2SCH3 Bz H ch3 OH OH H H VIII-47-8 p-F-Ph * H * Bz H ch3 OH OH H H *R2 and RJt) joined together by (0¾^ to form five-membered ring. 5 Table VIII-48. " I "'W' "y··'··' Wl J -

Xs R1 RJ r3. R3b R4 Ic R6 X Y R7 R8 VIII-48-1 p-Cl-Ph H H H Bz H ch3 OH OH H H VIH-48-2 p-Cl-Ph H H ch3 Bz H ch3 OH OH H Η VIII-48-3 p-Cl-Ph H H CH(CH3)2 Bz Η ch3 OH OH H Η 2983472-1 -244- WO 2θθ8β21634 No 60137.0034WOU1 PCT/US2008/058.183

R' R2 R3a "P R4 Rs X Y r" Rm VIH-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H CHj OH OH H H VIII-48-5 p-Cl-Ph H H CH2Ph Bz H ch3 OH OH H H VIII-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz H ch3 OH OH H H VIII-48-7 p-Cl-Ph H H CH2CH2SCH3 Bz H CHj OH OH H H VIII-48-8 p-Cl-Ph * H * Bz H CHj OH OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table VIII-49.

Ns R1 R2 r3o Rab IT Rs R6 X Y R R“ VIII-49-1 p-Br-Ph H H H Bz H CHj OH OH H H Vin-49-2 p-Br-Ph H H CH3 Bz H CHj OH OH H H VIII-49-3 p-Br-Ph H H CHiCHj^ Bz H CH3 OH OH H H VHI-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz H CH3 OH OH H H νΐΙΙτ49-5 p-Br-Ph H H CH2Ph Bz H CHj OH OH H H VIII-49-6 p-Br-Ph H H CH2-indol-3-yl Bz H CHj OH OH H H VIII-49-7 p-Br-Ph H H CH2CH2SCH3 Bz H CHj OH OH H H VIII-49-8 p-Br-Ph * H ♦ Bz H CHj OH OH H H *R2 and R3b joined together by (CHib to form five-membered ring.

Table VIII-50.

N2 Rl IF R3* RJb r4- R5 Rfi X Y ΊΓ R8 VIH-50-1 p-I-Ph H H H Bz H CHj OH OH H H VHI-5G-2 p-I-Ph H H CHj Bz H CHj OH OH H H VIII-50-3 p-I-Ph H H CH(CHj)2 Bz H CHj OH OH H H VIII-50-4 p-I-Ph H H CH2CH(CH3)2 Bz H CHj OH OH H H VIII-50-5 p-I-Ph H H CH2Ph Bz H CHj OH OH H H VHI-50-6 p-I-Ph H H CH2-indol-3-yl Bz H CHj OH OH H H VHI-50-7 p-I-Ph H H CH2CH2SCH3 Bz H CHj OH OH H H VIII-50-8 p-I-Ph Jb τ Γ "7 * H ♦ Bz H CHj OH OH H H *R2 and RJt> joined together by (ΟΗ2)3 to form five-membered ring. 2983472-1 -245- PCT/US2008/058183 60137.0034WOU1 WO 2008/121634

Docket No,

IX

Table IX-1.

X2 R1 r'2 R3· “r36 R4 RJ X Y V r“ IX-1-1 ch3 H H H ch3 H ch3 F OH H H IX-1-2 ch3 H H ch3 ch3 H ch3 F OH H H IX-1-3 ch3 H H CH(CH3)2 ch3 H ch3 F OH H H IX-1-4 ch3 H H CH2CH(CH3)2 ch3 H ch3 F OH H H IX-1-5 ch3 H H CH3Ph ch3 H ch3 F OH H H IX-1-6 ch3 H H CH2-indol-3-yl ch3 H ch3 F OH H H IX-1-7 ch3 H H CH2CH2SCH3 ch3 H ch3 F OH H H IX-1-8 ch3 * H ♦ ch3 H ch3 F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Xfi R ΊΓ Rj. R3b R4 ΊΓ R6 X Y R7 R" IX-2-1 Et H H H CH3 H ch3 F OH Η Η ΪΧ-2-2 Et H H CH3 ch3 H ch3 F OH Η Η IX-2-3 Et H H CH(CH3)2 ch3 H ch3 F OH Η Η IX-2-4 Et H H CH2CH(CH3)2 ch3 H ch3 F OH Η Η IX-2-5 Et H H CH2Ph ch3 H ch3 F OH Η Η IX-2-6 Et H H CH2-indol-3-yl ch3 H ch3 F OH Η Η IX-2-7 Et H H CH2CH2SCH3 ch3 H ch3 F OH Η Η IX-2-8 Et * H ♦ ch3 H ch3 F OH Η Η *R2 and R30 joined together by (Cthb to form five-membered ring. 2983472-1 -246- PCT/US2008/058183 WO 2008/121634 ΛΛ0..νΛιγι

Docket No. 60137.0034WOU1

Table DC-3.

Ns R1 ΊΓ R3" T* ir Rs R6 X Y R7 IX-3-1 'Pr H H H ch3 H ch3 F OH H H IX-3-2 'Pr H H ch3 ch3 H ch3 F OH H H IX-3-3 'Pr H H CH(CH3)2 ch3 H ch3 F OH H H IX-3-4 'Pr H H CH2CH(CH3)2 ch3 H ch3 F OH H H IX-3-5 Tr H H CH2Ph ch3 H ch3 F OH H H IX-3-6 'Pr H H CH2-indol-3-yI ch3 H ch3 F OH H H IX-3-7 'Pr H H CH2CH2SCH3 ch3 H ch3 F OH H H IX-3-8 'Pr * H * ch3 H ch3 F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table DC-4.

Ns R R3 r3- R3b R4 R5 R6 X Y R7 R“ IX-4-1 'Bu H H H ch3 H CH3 F OH H H IX-4-2 'Bu H H ch3 ch3 H ch3 F OH H H IX-4-3 'Bu H H CH(CH3)2 ch3 H ch3 F OH H H IX-4-4 'Bu H H CH2CH(CH3)2 ch3 H ch3 F OH H H ΪΧ-4-5 'Bu H H CH2Ph ch3 H ch3 F OH H H IX-4-6 'Bu H H CH2-indol-3-yl ch3 H ch3 F OH H H IX-4-7 'Bu H H CH2CH2SCH3 ch3 H ch3 F OH H H IX-4-8 'Bu * H * ch3 H ch3 F OH H H ♦R2"andR3b joined together by (CHj^ to form five-membered ring. 5 Table IX-5. I R 11 ’RL — I III·· »

Ns R R3 R3. R3b R4 Rs R6 X Y R7 R8 IX-5-1 Ph H H H ch3 H CH3 F OH H H IX-5-2 Ph H H ch3 ch3 H ch3 F OH H H IX-5-3 Ph H H CH(CH3)i ch3 H ch3 F OH H H IX-5-4 Ph H H CH2CH(CH3)2 ch3 H ch3 F OH H H IX-5-5 Ph H H CH2Ph ch3 H ch3 F OH H H IX-5-6 Ph H H CH2-indol-3-yI ch3 H ch3 F OH H H IX-5-7 Ph H H ch2ch2sch3 ch3 H ch3 F OH H H IX-5-8 Ph. * H * ch3 H ch3 F OH H H *R2 and R3b joined together by (CHih to form five-membered ring. 2983472-1 - 247 - PCT/US2008/058183 WO 2008/121634 __ ΛΛ. „

UocKet No. 60137.0034WOU1

Table IX-6.

Ns Rl R2 "r35 “S’” iV X Y R7 Rs 1X-6-1 p-Me-Ph H H H ch3 H ch3 F OH H H 1X-6-2 p-Me-Ph H H ch3 ch3 H ch3 F OH H H IX-6-3 p-Me-Ph H H CH(CH3)2 ch3 H ch3 F OH H H 1X-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 H ch3 F OH H H IX-6-5 p-Me-Ph H H CHaPh ch3 H ch3 F OH H H IX-6-6 p-Me-Ph H H CH2-indol-3-yl ch3 H ch3 F OH H H ΪΧ-6-7 p-Me-Ph H H ch2ch2sch3 ch3 H ch3 F OH H H IX-6-8 p-Me-Ph * H ♦ ch3 H ch3 F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table IX-7.

Na R1 ΊΓ RJa R30 R4 R5 R6 X Y R7 R“ IX-7-1 p-F-Ph H H H CH3 H ch3 F OH H H IX-7-2 p-F-Ph H H ch3 ch3 H ch3 F OH H H IX-7-3 p-F-Ph H H CH(CH3)2 ch3 H ch3 F OH H H IX-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 H ch3 F OH H H IX-7-6 p-F-Ph H H CH2Ph ch3 H ch3 F OH H H IX-7-7 p-F-Ph H H CH2-indol-3-yl ch3 H ch3 F OH H H IX-7-8 p-F-Ph H H CH2CH2SCH3 ch3 H ch3 F OH H H IX-7-20 p-F-Ph 4 H ♦ ch3 H ch3 F OH H H *R^ and R3b joined together by (CH2)3 to form five-membered ring. 5 Table IX-8.

........ ..... ! 1 ' I .--.-11..1..-.- . B

No R R2 r3« RJb R4 RJ R6 X Y R7 R" IX-8-1 p-Cl-Ph H H H 0¾ H ch3 F OH H H IX-8-2 p-Cl-Ph H H ch3 CH3 H ch3 F OH H H IX-8-3 p-Cl-Ph H H CH(CH3)2 ch3 H ch3 F OH H H IX-8-4 p-CI-Ph H H CH2CH(CH3)3 ch3 H ch3 F OH H H IX-8-5 p-Cl-Ph H H CH3Ph ch3 H ch3 F OH H H IX-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 H ch3 F OH H H IX-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 H ch3 F OH H H IX-8-8 "1^2 "" p-Cl-Ph * H * ch3 H ch3 F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -248- PCT/US2008/058183 WO 2008/121634 ΛΛ,,,,,ητιι

Docket No. 60137.0034WOU1

Table IX-9.

Xs R' R2 RJa "F” Rs X Y R Ra IX-9-1 p-Br-Ph H H H ch3 H ch3 F OH H H IX-9-2 p-Br-Ph H H ch3 ch3 H ch3 F OH H H IX-9-3 p-Br-Ph H H CH(CH3)2 ch3 H ch3 F OH H H IX-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 H ch3 F OH H H IX-9-6 p-Br-Ph H H CH2Ph ch3 H ch3 F OH H H IX-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 H ch3 F OH H H IX-9-8 p-Br-Ph H H CH2CH2SCH3 ch3 H ch3 F OH H H IX-9-20 p-Br-Ph * H * ch3 H ch3 F OH H H *R* and Rejoined together by (CH2)3 to form five-membered ring.

Table IX-10.

Xs Rl R2 R3’ R3b R4 RJ Ιν X Y R7 R“ IX-10-1 p-I-Ph H H H CH3 H ch3 F OH H H IX-10-2 p-I-Ph H H ch3 ch3 Η ch3 F OH H H IX-10-3 p-I-Ph H H CHiCHj), ch3 Η ch3 F OH H H IX-10-4 p-I-Ph H H CH2CH(CH3)2 ch3 Η ch3 F OH H H IX-10-5 p-I-Ph H H CH2Ph ch3 Η ch3 F OH H H IX-10-6 p-I-Ph H H CH2-indol-3-yl ch3 Η ch3 F OH H H IX-10-7 p-I-Ph H H CH2CH2SCH3 ch3 Η ch3 F OH H H IX-10-8 p-I-Ph ♦ H * ch3 Η ch3 F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table IX-11. , .,., ' Kl ii i l J . m fl

Xs R2 R3* R3b R4 R3 Rfc X Y R' R“ IX-11-1 ch3 H H H Et H ch3 F OH H H IX-11-2 ch3 H H CH3 Et H ch3 F OH H H IX-11-3 ch3 H H CH(CH3)2 Et H ch3 F OH H H 1X-11-4 ch3 H H CH2CH(CH3)2 Et H ch3 F OH H H IX-11-5 ch3 H H CH2Ph Et H ch3 F OH H H IX-11-6 ch3 H H CH2-indol-3-yl Et H ch3 F OH H H IX-11-7 ch3 H H CH2CH2SCH3 Et H ch3 F OH H H IX-11-8 .1 ch3 773b · * H * Et H ch3 F OH H H *R2 and Rejoined together by (CH^'to farm five-membered ring. 2983472-1 -249- WO ^8//^1634^ 60137>0034WOU1 PCT/US2008/058183

Table IX-12.

X® Rl R7 R3‘ “r35 R4 Rs R6 X Y R7 Ra IX-12-1 Et H H H Et H ch3 F OH H H IX-12-2 Et H H ch3 Et H ch3 F OH H H IX-12-3 Et H H CH(CH3)2 Et H ch3 F OH H H IX-12-4 Et H H CH2CH(CH3)2 Et H ch3 F OH H H IX-12-5 Et H H CH2Ph Et H ch3 F OH H H IX-12-6 Et H H CH2-indol-3-yl Et H ch3 F OH H H ‘ IX-12-7 Et H H CH2CH2SCH3 Et H ch3 F OH H H IX-12-8 Et * H ♦ Et H ch3 F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table IX-13.

X° R1 RJ R3a r35 R4 Rr R6 X Y R7 ΊΓ IX-13-1 'Pr H H H Et H CH3 F OH H H IX-13-2 'Pr H H ch3 Et H ch3 F OH H H IX-13-3 'Pr H H CH(CH3)2 Et H ch3 F OH Η H IX-13-4 'Pr H H CH2CH(CH3)2 Et H ch3 F OH H H IX-13-5 'Pr H H CH2Ph Et H ch3 F OH H H IX-13-6 'Pr H H CH2-indol-3-yl Et H ch3 F OH H H IX-13-7 'Pr H H CH2CH2SCH3 Et H ch3 F OH H H IX-13-8 'Pr T»3b · * H * Et H ch3 F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table IX-14.

I A 4.' ·™·Μ J ' g .....- ' MB

Xa Rl R2 r3‘ R3b R4 R5 R6 X Y Iv R8 IX-14-1 ΙϋΓ" H H H Et H ch3 F OH H H IX-14-2 'Bu Η H CH3 Et H ch3 F OH H H 1X-14-3 'Bu H Η CH(CH3)2 Et H ch3 F OH H H IX-14-4 'Bu H H CH2CH(CH3)2 Et H ch3 F OH H H IX-14-5 'Bu H H CH2Ph Et H ch3 F OH Η Η IX-14-6 'Bu H H CH2-indol-3-yl Et H ch3 F OH H H IX-14-7 'Bu H H CH2CH2SCH3 Et H ch3 F OH Η H IX-14-8 □i 'Bu rdb· ·— 4 H * Et H ch3 F OH H H *R2 and RJb joined together by (CHJ^to form five-membered ring. 2983472-1 -250- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table IX-15.

Ns R1 R2 r3“ R3b R4 R5 Rfc X Y r" R8 IX-15-1 Ph H H H Et H ch3 F OH H H IX-15-2 Ph H H CHj Et H ch3 F OH H H IX-15-3 Ph H H CH(CH3)2 Et H ch3 F OH H H IX-15-4 Ph H H CH2CH(CH3)2 Et H ch3 F OH H H IX-15-5 Ph H H CH2Ph Et H ch3 F OH H H IX-15-6 Ph H H CH2-indol-3-yl Et H ch3 F OH H H IX-15-7 Ph H H CH2CH2SCH3 Et H ch3 F OH H H IX-15-8 Ph * H * Et H ch3 F OH H H *R2 and R3b joined together by (CHj)3 to form five-membered ring.

Table IX-16.

Ns R1 R2 R3‘ R35 R4 r3- R6 X Y R7 r“ IX-16-1 p-Me-Ph H H H Et H CH3 F OH H H IX-16-2 p-Me-Ph H H ch3 Et H ch3 F OH H H IX-16-3 p-Me-Ph H H CH(CH3)2 Et H ch3 F OH H H IX-16-4 p-Me-Ph H H CH2CH(CH3)2 Et H ch3 F OH H H IX-16-5 p-Me-Ph H H CH2Ph Et H ch3 F OH H H IX-16-6 p-Me-Ph H H CH2-indol-3-yl Et H ch3 F OH H H IX-16-7 p-Me-Ph H H CH2CH2SCH3 Et H ch3 F OH H H IX-16-8 .1 p-Me-Ph * H * Et H ch3 F OH H H *R2 and RJt) joined together by (CH2)3 to form five-membered ring.

Ns R‘ ΊΓ R3a R3b R4 Rs R6 X Y R7 R8 IX-17-1 p-F-Ph H H H Et H ch3 F OH H Η IX-17-2 p-F-Ph H H CH3 Et H ch3 F OH H H IX-17-3 p-F-Ph H H CHCCHah Et H ch3 F OH H H IX-17-4 p-F-Ph H H CH2CH(CH3)2 Et H ch3 F OH H H IX-17-5 p-F-Ph H H CH2Ph Et H ch3 F OH H Η IX-17-6 p-F-Ph H H CH2-indol-3-yl Et H ch3 F OH H H IX-17-7 p-F-Ph H H ch2ch2sch3 Et H ch3 F OH H H IX-17-8 *n2 ...1 p-F-Ph T-Jtj ! ! * H * Et H ch3 F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -251- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU I

Table IX-18.

Xa R1 r3" "r35" R3b T" R5 R6 X Y if R“ 1X-18-1 p-Cl-Ph H H H Et H ch3 F OH H H IX-18-2 p-Cl-Ph H H ch3 Et H ch3 F OH H H IX-18-3 p-Cl-Ph H H CHCCHab Et H ch3 F OH H H IX-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H ch3 F OH H H IX-18-5 p-Cl-Ph H H CH2Ph Et H ch3 F OH H H IX-18-6 p-Cl-Ph H H CH2-indol-3-yl Et H ch3 F OH H H IX-18-7 p-Cl-Ph H H ch2ch2sch3 Et H ch3 F OH H H IX-18-8 '7' p-Cl-Ph * H * Et H ch3 F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table IX-19.

Xs Rl "R3- R3a "r35 R4 r! R* X Y R7 r“ IX-19-1 p-Br-Ph H H H Et H ch3 F OH H H IX-19-2 p-Br-Ph H H ch3 Et H ch3 F OH H H IX-19-3 p-Br-Ph H H CHiCHab Et H ch3 F OH H H IX-19-4 p-Br-Ph H H CH2CH(CH3)2 Et H ch3 F OH H H IX-19-5 p-Br-Ph H H CH2Ph Et H ch3 F OH H H IX-19-6 p-Br-Ph H H CH2-indol-3-yl Et H ch3 F OH H H IX-19-7 p-Br-Ph H H CH2CH2SCH3 Et H ch3 F OH H H IX-19-8 p-Br-Ph * H ♦ Et H ch3 F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table IX-20. ' * ...........-···· ^ 1- IL I 1 . I .2 - -- ' - 'Ji 1 U 1

Xs R1 R2 R3" RJb R4 R3 R6 X Y R R“ IX-20-1 p-I-Ph H H H Et H CH3 F OH H H IX-20-2 p-I-Ph H H CH3 Et H ch3 F OH H H IX-20-3 p-I-Ph H H CH(CH3)2 Et H ch3 F OH H H IX-20-4 p-I-Ph H H CH2CH(CH3)i Et H ch3 F OH H H IX-20-5 p-I-Ph H H CH2Ph Et H ch3 F OH H H IX-20-6 p-I-Ph H H CH2-indol-3-yl Et H ch3 F OH H H IX-20-7 p-I-Ph H H CH2CH2SCH3 Et H ch3 F OH H H IX-20-8 “ΪΪ72-T p-I-Ph r*3b; . . * H * Et H ch3 F OH H H *R and R joined together by (CH2)3 to form five-membered ring. 2983472-1 -252- PCT/US2008/058183 WO 2008/121634

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Table IX-21.

Ns R R1 r3. R36 R4 RJ R* X Y R* IX-21-1 ch3 H H H "ΤΓ H ch3 F OH H H IX-21-2 ch3 H H ch3 'Pr H ch3 F OH H H IX-21-3 ch3 H H CH(CH3)2 'Pr H ch3 F OH H H IX-21-4 ch3 H H CH2CH(CH3)2 'Pr H ch3 F OH H H IX-21-5 ch3 H H CH2Ph 'Pr H ch3 F OH H H IX-21-6 ch3 H H CHa-indol-3-yl 'Pr H ch3 F OH H H IX-21-7 ch3 H H CH2CH2SCH3 'Pr H ch3 F OH H H IX-21-8 ch3 * H * 'Pr H ch3 F OH H H *R2 and R3b joined together by (CFhb to form five-membered ring.

Table IX-22.

Ns R R4 rJ5 R3b R4 R5 R* X Y R7 R# IX-22-1 Et H H H 'Pr H ch3 F OH H H IX-22-2 Et H H ch3 'Pr H ch3 F OH H H IX-22-3 Et H H CH(CH3)2 'Pr H ch3 F OH H H 1X-22-4 Et H H CH2CH(CH3)a 'Pr H ch3 F OH H H IX-22-5 Et H H CH2Ph 'Pr H ch3 F OH H H IX-22-6 Et H H CH2-indol-3-yl 'Pr H ch3 F OH H H IX-22-7 Et H H CH2CH2SCH3 'Pr H ch3 F OH H H IX-22-8 Et * H * 'Pr H ch3 F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table IX-23. ~ " i □ 1- TU '......-.....- J -------···! Τ.“'.Ί· ·“·· " n·"»·»-

Ns R R2 R3" R3b R4 Rs X Y ΪΓ Ru IX-23-1 'Pr H H H 'Pr H CH3 F OH H H IX-23-2 'Pr H H CH3 'Pr H ch3 F OH H H IX-23-3 'Pr H H CHCCH^ 'Pr H ch3 F OH H H IX-23-4 'Pr H H CH2CH(CH3)2 'Pr H ch3 F OH H H IX-23-5 'Pr H H CH2Ph 'Pr H ch3 F OH H H IX-23-6 'Pr H H CH2-indol-3-yl 'Pr H ch3 F OH H H IX-23-7 'Pr H H CH2CH2SCH3 'Pr H ch3 F OH H H IX-23-8 *n2 i 'Pr * H * 'Pr H ch3 F OH H H *R2 and R3b joined together by (ΟΗ2)3 to form five-membered ring. 2983472-1 -253- WO 2008/121634 PCT/US2008/058183

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Table IX-24.

Ns -R1- R2 r3s R3b R4 ΊΓ R6 X Y r7 r“ IX-24-1 'Bu H H H “’Pr" H ch3 F OH H H IX-24-2 'Bu H H ch3 'Pr H ch3 F OH H H IX-24-3 'Bu H H CH(CH3)2 'Pr H ch3 F OH H H IX-24-4 Έυ H H CH2CH(CH3)2 'Pr H ch3 F OH H H IX-24-5 'Bu H H CHjPh 'Pr H ch3 F OH H H IX-24-6 'Bu H H CH2-indol-3-yl 'Pr H ch3 F OH H H IX-24-7 'Bu H H CH2CH2SCH3 'Pr H CHa F OH H H IX-24-8 'Bu * H * 'Pr H ch3 F OH H H *R and R joined together by (ΟΗ2)3 to form five-membered ring.

Table IX-25.

Ns R* R2 Rj. R3b R4 R3 R6 X Y R7 R* IX-25-1 Ph H H H “'pT H CH3 F OH H H IX-25-2 Ph H H CH3 'Pr H ch3 F OH H H IX-25-3 Ph H H CH(CH3)2 'Pr H ch3 F OH H H IX-25-4 Ph H H CH2CH(CH3)2 'Pr H ch3 F OH H H 1X-25-5 Ph H H CH2Ph 'Pr H ch3 F OH H H IX-25-6 Ph H H CH2-indol-3-yl 'Pr H ch3 F OH H H IX-25-7 Ph H H CH2CH2SCH3 'Pr H ch3 F OH H H IX-25-8 “*772-T Ph T->3b - * H * 'Pr H ch3 F OH H H *R^ and Rejoined together by (0¾)^ to form five-membered ring.

Ns R1 iF RJ“ -r36 R4 ΊΓ Rs X Y "IF R8 IX-26-1 p-Me-Ph H H . H H CH3 F OH H Η IX-26-2 p-Me-Ph H H ch3 'Pr H ch3 F OH Η Η IX-26-3 p-Me-Ph H H CHCCH^ 'Pr H ch3 F OH Η Η IX-26-4 p-Me-Ph H H ΟΗ2ΟΗ(ΟΗ3)2 'Pr H ch3 F OH Η Η IX-26-5 p-Me-Ph H H CH2Ph 'Pr H ch3 F OH Η Η IX-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr H ch3 F OH Η Η IX-26-7 p-Me-Ph H H ch2ch2sch3 'Pr H ch3 F OH Η Η IX-26-8 p-Me-Ph sab'.· · 7; « H * 'Pr H ch3 F OH Η Η *R4 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -254- WO 2008/121634

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Table IX-27.

Jf2 R1 R1 R3 RJb R4 R5 R6 X Y r’ R8 IX-27-1 p-F-Ph H H H H ch3 F OH H H IX-27-2 p-F-Ph H H ch3 'Pr H ch3 F OH H H IX-27-3 p-F-Ph H H CH(CH3)2 'Pr H ch3 F OH H H IX-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr H ch3 F OH H H IX-27-5 p-F-Ph H H CH2Ph 'Pr H ch3 F OH H H IX-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr H ch3 F OH H H IX-27-7 p-F-Ph H H CH2CH2SCH3 'Pr H ch3 F OH H H IX-27-8 p-F-Ph ♦ H * 'Pr H ch3 F OH H H *R2and RJb joined together by (CH2)3 to form five-membered ring.

Table IX-28.

Na R’ R2 R3" R3b R4 Rs R6 X Y R7 R8 IX-28-1 p-Cl-Ph H H H -7p7“ H CH3 F OH H H IX-28-2 p-Cl-Ph H H ch3 'Pr H ch3 F OH H H IX-28-3 p-Cl-Ph H H CH(CH3)2 'Pr H ch3 F OH H H IX-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr H ch3 F OH H H IX-28-5 p-Cl-Ph H H CH2Ph 'Pr H ch3 F OH H H IX-28-6 p-Cl-Ph H H CH2-indoI-3-yl 'Pr H ch3 F OH H H IX-28-7 p-Cl-Ph H H CH2CH2SCH3 'Pr H ch3 F OH H H IX-28-8 p-Cl-Ph * H * 'Pr H ch3 F OH H H

>J 111 ll ............ I ♦R and R joined together by (0¾^ to form five-membered ring. 5 Table IX-29. 1 R- 11 "ί!|· 1 J .......... W »

Na R1 R2 RJa R3b R4 R3 R* X Y ΊΓ R8 IX-29-1 p-Br-Ph H H H 'Pr H CH3 F OH H H IX-29-2 p-Br-Ph H H ch3 'Pr H ch3 F OH H H IX-29-3 p-Br-Ph H H CH(CH3)2 'Pr H ch3 F OH H H IX-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr H ch3 F OH H H IX-29-5 p-Br-Ph H H CH2Ph 'Pr H ch3 F OH H H IX-29-6 p-Br-Ph H H CH2-indol-3-yI 'Pr H ch3 F OH H H IX-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr H ch3 F OH H H IX-29-8 - J p-Br-Ph · · . * H * 'Pr H ch3 F OH H H *Rzand R3b joined together by (CH2)j to form five-membered ring. 2983472-1. -255- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table IX-30.

R1 R2 R3a - - R4 RJ IV x Y R8 IX-30-1 p-I-Ph H H H "W H ch3 F OH H H IX-30-2 p-I-Ph H H ch3 'Pr H ch3 F OH H H IX-30-3 p-I-Ph H H CH(CH3)2 'Pr H ch3 F OH H H IX-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr H ch3 F OH H H IX-30-5 p-I-Ph H H CH2Ph 'Pr H ch3 F OH H H IX-30-6 p-I-Ph H H CHrindol-3-y] 'Pr H ch3 F OH H H IX-30-7 p-I-Ph H H ch2ch2sch3 'Pr H ch3 F OH H H IX-30-8 p-I-Ph * H * 'Pr H ch3 F OH H H *R^ and RJb joined together by (CH2)3 to form five-membered ring.

Table IX-3I.

Na R R2 Rj0 R3" R4 Iv R6 x Y ΊΓ R8 IX-31-1 CH3 H Η Η "Bu H ch3 F OH H H IX-31-2 ch3 Η Η ch3 "Bu H ch3 F OH H H IX-31-3 ch3 Η Η CH(CH3)2 "Bu H ch3 F OH H H IX-31-4 ch3 Η Η CH2CH(CH3)2 "Bu H ch3 F OH H H IX-31-5 ch3 Η Η CH2Ph "Bu H ch3 F OH H H ΪΧ-31-6 ch3 Η Η CH2-indoI-3-yl "Bu H ch3 F OH H H IX-31-7 ch3 Η Η CH2CH2SCH3 "Bu H ch3 F OH H H IX-31-8 ch3 * Η * "Bu H ch3 F OH H H *R2 and R30 joined together by (CH^b to form five-membered ring. 5 Table IX-32. -- —......... . I *1 ............... J 1 a

J& R‘ R2 R3. R3b R4 Rs R6 x Y R’ R8 IX-32-1 Et H H H "Bu H CH3 F OH H H IX-32-2 Et H H CH3 "Bu H ch3 F OH H H IX-32-3 Et H H CHiCH^ "Bu H ch3 F OH H H IX-32-4 Et H H CH2CH(CH3>2 "Bu H ch3 F OH H H IX-32-5 Et H H CH2Ph "Bu H ch3 F OH H H IX-32-6 Et H H CH2-indol-3-yl "Bu H ch3 F OH H H IX-32-7 Et H H CH2CH2SCH3 "Bu H ch3 F OH H H IX-32-8 “Ϊ772-r Et * H * "Bu H ch3 F OH H H *R2 and RJD joined together by (CH2)3 to form five-membered ring. 2983472-1 -256- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table IX-33.

Na R1 R35 Rs R4 X Y R7 R8 ΪΧ-33-1 'Pr H H H "Bu H ch3 F OH H H IX-33-2 'Pr H H ch3 "Bu H ch3 F OH H H IX-33-3 'Pr H H CH(CH3)2 "Bu H ch3 F OH H H IX-33-4 'Pr H H CH2CH(CH3)2 "Bu H ch3 F OH H H IX-33-5 'Pr H H CH2Ph "Bu H ch3 F OH H H IX-33-6 'Pr H H CH2-indol-3-yl "Bu H ch3 F OH H H IX-33-7 'Pr H H CH2CH2SCH3 "Bu H ch3 F OH H H IX-33-8 'Pr * H * "Bu H ch3 F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table IX-34.

Xa R R2 Rja R3b R4 R5 R6 X Y R7 r“ IX-34-1 'Bu H H H "Bu H CH3 F OH H H IX-34-2 'Bu H H ch3 "Bu H ch3 F OH H H ΪΧ-34-3 'Bu H H CH(CH3)2 "Bu H ch3 F OH H H IX-34-4 'Bu H H CH2CH(CH3)2 "Bu H ch3 F OH H H IX-34-5 'Bu H H CH2Ph "Bu H ch3 F OH H H IX-34-6 'Bu H H CH2-indol-3-yl "Bu H CH3 F OH H H ΪΧ-34-7 'Bu H H ch2ch2sch3 "Bu H ch3 F OH H H ΪΧ-34-8 'Bu ♦ H ♦ "Bu H ch3 F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table IX-35. - - _ I'·11 J J J ...... W —

Xa R R2 R3" R3B R^ Rs Rft X Y R7 R8 IX-35-1 Ph H H H "Bu H ch3 F OH H H IX-35-2 Ph H H CH3 "Bu H ch3 F OH H H IX-35-3 Ph H H CH(CH3)2 "Bu H ch3 F OH H H IX-35-4 Ph H H CH2CH(CH3)2 "Bu H ch3 F OH H H IX-35-5 Ph H H CH2Ph "Bu H ch3 F OH H H IX-35-6 Ph H H CH2-indol-3-yl "Bu H ch3 F OH H H IX-35-7 Ph H H CH2CH2SCH3 "Bu H ch3 F OH H H IX-35-8 *«2- . Ph * H * "Bu H ch3 F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -257- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table IX-36.

Ns R1 R2 RJa RJb R4 R5 R6 X Y R i? IX-36-1 p-Me-Ph H H H "Bu H ch3 F OH H H IX-36-2 p-Me-Ph H H ch3 "Bu H ch3 F OH H H IX-36-3 p-Me-Ph H H CH(CH3)2 "Bu H ch3 F OH H H IX-36-4 p-Me-Ph H H CH2CH(CH3>2 "Bu H ch3 F OH H H IX-36-5 p-Me-Ph H H CH2Ph "Bu H ch3 F OH H H IX-36-6 p-Me-Ph H H CH2-indoi-3-yl "Bu H ch3 F OH H H IX-36-7 p-Me-Ph H H ch2ch2sch3 "Bu H ch3 F OH H H IX-36-8 p-Me-Ph * H * "Bu H ch3 F OH H H *R2 and R'”’joined together by (CH2)3 to form five-membered ring?

Table IX-37.

R1 R2 R3· R3b R4 R’ R0 X Y R7 R" IX-37-1 p-F-Ph Η Η H "Bu H CH3 F OH Η H IX-37-2 p-F-Ph Η H CH3 "Bu H CH3 F OH Η H IX-37-3 p-F-Ph Η H CH(CH3)2 "Bu H CH3 F OH Η H IX-37-4 p-F-Ph Η H CH2CH(CH3)2 "Bu H CH3 F OH Η H IX-37-5 p-F-Ph Η H CH2Ph "Bu H CH3 F OH Η H IX-37-6 p-F-Ph Η H CH2-indol-3-yl "Bu H CH3 F OH Η H IX-37-7 p-F-Ph Η H CH2CH2SCH3 "Bu H CH3 F OH Η H IX-37-8 p-F-Ph * H ♦ "Bu H CH3 F OH Η H *R4 and Rejoined together by (CH2)3 to form five-membered ring. Table IX-38. Ns R1 R2 R3a R3b R4 R5 R6 X Y R7 R“ IX-38-1 p-Cl-Ph Η Η H "Bu H CH3 F OH Η H 1X-38-2 p-Cl-Ph Η H CH3 "Bu H CH3 F OH Η H IX-38-3 p-Cl-Ph Η Η ΟΗ(ΟΗ3)2 "Bu Π U1I3 F OH Η H IX-38-4 p-Cl-Ph Η H CH2CH(CH3)2 "Bu H CH3 F OH Η H IX-38-5 p-Cl-Ph Η H CH2Ph "Bu H CH3 F OH Η H IX-38-6 p-Cl-Ph Η H CH2-indol-3-yl "Bu H CH3 F OH Η H IX-38-7 p-Cl-Ph Η H CH2CH2SCH3 "Bu H CH3 F OH Η H IX-38-8 p-Cl-Ph -.«3b: : ♦ H * "Bu H CH3 F OH Η H M WL· ll ιι·ι I i ·ιι ll I·· ll *R and R joined together by (CH^ to form five-membered ring. 2983472-1 -258- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table IX-39.

Ns R1 "R2" "r35" "R35 R4 RJ R6 X Y R ΊΓ IX-39-1 p-Br-Ph H H H "Bu H ch3 F OH H H IX-39-2 p-Br-Ph H H ch3 "Bu H ch3 F OH H H IX-39-3 p-Br-Ph H H CH(CH3)2 "Bu H ch3 F OH H H IX-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu H ch3 F OH H H IX-39-5 p-Br-Ph H H CH2Ph "Bu H ch3 F OH H H IX-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu H ch3 F OH H H 1X-39-7 p-Br-Ph H H CH2CH2SCH3 "Bu H ch3 F OH H H IX-39-8 p-Br-Ph * H * "Bu H ch3 F OH H H *R2 and R3b joined together by (¢^2)3 to form five-membered ring.

Table IX-40.

Ns R1 R3 R3a R3b R4 R R4 X Y R7 R8 IX-40-1 p-I-Ph H H H "Bu H ch3 F OH H H IX-40-2 p-I-Ph H H ch3 "Bu H ch3 F OH H H IX-40-3 p-I-Ph H H CH(CH3)2 "Bu H CH3 F OH H Η IX-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu H ch3 F OH H H IX-40-5 p-I-Ph H H CH2Ph "Bu H ch3 F OH H Η IX-40-6 p-I-Ph H H CH2-indoI-3-yl "Bu H ch3 F OH H H IX-40-7 p-I-Ph H H CH2CH2SCH3 "Bu H ch3 F OH H H IX-40-8 p-I-Ph ♦ H * "Bu H ch3 F OH H H ♦R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table IX-41. 1 1 1 -v - ' "J I 1 11 1 . > B—

Ns R RJ Rj. R3b R4 R5 R4 X Y R7 R8 IX-41-1 CHa H H H Bz H CH3 F OH H H IX-41-2 ch3 H H ch3 Bz H ch3 F OH H Η IX-41-3 ch3 H H CH(CH3)2 Bz H ch3 F OH H H IX-41-4 ch3 H H CH2CH(CH3)2 Bz H ch3 F OH H H IX-41-5 ch3 H H CH2Ph Bz H ch3 F OH H H IX-41-6 ch3 H H CH2-indol-3-yl Bz Η ch3 F OH H H IX-41-7 ch3 H H CH2CH2SCH3 Bz H ch3 F OH H H IX-41-8 *r,2 j ch3 * H * Bz H ch3 F OH H H ♦R2 and R3t> joined together by (CH2)3 to form five-membered ring. 2983472-1 -259- WO 2008/121634

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Table IX-42.

Xs R1 R2 R3a R3' T< R5 R6 X Y R7 IC IX-42-1 Et H H H Bz H ch3 F OH H H IX-42-2 Et H H ch3 Bz H ch3 F OH H H IX-42-3 Et H H CH(CH3)2 Bz H ch3 F OH H H IX-42-4 Et H H CH2CH(CH3)2 Bz H ch3 F OH H H IX-42-5 Et H H CHaPh Bz H ch3 F OH H H IX-42-6 Et H H CHj-indol-3-yl Bz H ch3 F OH H H IX-42-7 Et H H CH2CH2SCH3 Bz H ch3 F OH H H IX-42-8 Et * H * Bz H ch3 F OH H H *R and R joined together by (CH2)3 to form five-membered ring.

Table IX-43.

Xs R R2 R3‘ R3b R4 R5 R6 X Y R7 R8 IX-43-1 'Pr H H H Bz H ch3 F OH H H IX-43-2 'Pr H H ch3 Bz H ch3 F OH H A IX-43-3 /pr H H CH(CH3)a Bz H ch3 F OH H H IX-43-4 /pr H H CH2CH(CH3)2 Bz H ch3 F OH H H IX-43-5 fPr H H CH2Ph Bz H ch3 F OH H H IX-43-6 'Pr H H CH2-indol-3-yl Bz H ch3 F OH H H IX-43-7 'Pr H H CH2CH2SCH3 Bz H ch3 F OH H H IX-43-8 'Pr * H * Bz H ch3 F OH H H 10 *R2 and R3b joined together by to form five-membered ring.

Table IX-44.

Xs R IT R3· R3b R4 ΊΓ R6 X Y "R7" R8 ΪΧ-44-1 H H H Bz H CH3 F OH H H IX-44-2 'Bu H H ch3 Bz H ch3 F OH H H IX-44-3 'Bu H H CH(CH3)2 Bz H ch3 F OH H H IX-44-4 'Bu H H CH2CH(CH3)2 Bz H ch3 F OH H H IX-44-5 'Bu H H CH2Ph Bz H ch3 F OH H H IX-44-6 'Bu H H CH2-indoI-3-yI Bz H ch3 F OH H H IX-44-7 'Bu H H CH2CH2SCH3 Bz H ch3 F OH H H IX-44-8 Έυ T%3bV * H * Bz H ch3 F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -260- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU 1

Table IX-45.

Xs R1 r3" R3a -R115 R4 R5 R6 X Y IV Iv IX-45-1 Ph H H H Bz H ch3 F OH H H IX-45-2 Ph H H ch3 Bz H ch3 F OH H H IX-45-3 Ph H H CH(CH3)2 Bz H ch3 F OH H H IX-45-4 Ph H H CH2CH(CH3)2 Bz H ch3 F OH H H IX-45-5 Ph H H CH2Ph Bz H ch3 F OH H H IX-45-6 Ph H H CH2-indoI-3-yl Bz H ch3 F OH H H IX-45-7 Ph H H CH2CH2SCH3 Bz H ch3 F OH H H IX-45-8 Ph * H * Bz H ch3 F OH H H *R4 and RJb joined together by ((¾)} to form five-membered ring

Table IX-46.

Xa R1 R2 R3’ R3b R4 R3 R6 X Y R7 r“ IX-46-1 p-Me-Ph H H H Bz H CH3 F OH H H IX-46-2 p-Me-Ph H H CH3 Bz H ch3 F OH H H IX-46-3 p-Me-Ph H H CHCCH^ Bz H ch3 F OH H H IX-46-4 p-Me-Ph H H CHjCHfCH^ Bz H ch3 F OH H H IX-46-5 p-Me-Ph H H CH2Ph Bz H ch3 F OH H H IX-46-6 p-Me-Ph H H CH2-indol-3-yl Bz H ch3 F OH H H IX-46-7 p-Me-Ph H H CH2CH2SCH3 Bz H ch3 F OH H H IX-46-8 p-Me-Ph * H * Bz H ch3 F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table IX-47. 1 I K H_ HL J 1 · > ' ..... H '

Xs R' R2 R3· R3b R4 RJ R6 X Y R' R8 IX-47-1 p-F-Ph H H H Bz H CH3 F OH H Η IX-47-2 p-F-Ph H H CH3 Bz H ch3 F OH H H IX-47-3 p-F-Ph H H CH(CH3)2 Bz H ch3 F OH H H IX-47-4 p-F-Ph H H CH2CH(CH3)2 Bz H ch3 F OH H H IX-47-5 p-F-Ph H H CH2Ph Bz H ch3 F OH Η H IX-47-6 p-F-Ph H H CH2-indol-3-yl Bz H ch3 F OH H H IX-47-7 p-F-Ph H H CH2CH2SCH3 Bz H ch3 F OH H H IX-47-8 “ΪΚ2—r p-F-Ph n3b: · * H * Bz H ch3 F OH H H *R2 and Rejoined together by (CH^ to form five-membered ring 2983472-1 -261- WO 2008/121634 PCT/US2008/058183

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Table IX-48.

Ns R1 FT r3. R35 I? R6 X Y r' r“ IX-48-1 p-Cl-Ph H H H Bz H ch3 F OH H H IX-48-2 p-Cl-Ph H H ch3 Bz H ch3 F OH H H IX-48-3 p-Cl-Ph H H CH(CH3)2 Bz H ch3 F OH H H IX-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H ch3 F OH H H IX-48-5 p-Cl-Ph H H CH2Ph Bz H ch3 F OH H H IX-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz H ch3 F OH H H IX-48-7 p-Cl-Ph H H ch2ch2sch3 Bz H ch3 F OH H H IX-48-8 p-Cl-Ph * H * Bz H ch3 F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table IX-49.

Jfe R1 R2 r3. R3tl R4 Rs R6 X Y R7 R“ IX-49-1 p-Br-Ph H H H Bz H CH3 F OH H H IX-49-2 p-Br-Ph H H CH3 Bz H ch3 F OH H H IX-49-3 p-Br-Ph H H CH(CH3)2 Bz H ch3 F OH H H IX-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz H ch3 F OH H H 1X-49-5 p-Br-Ph H H CH2Ph Bz H ch3 F OH H H IX-49-6 p-Br-Ph H H CH2-indot-3-yl Bz H ch3 F OH H H IX-49-7 p-Br-Ph H H CH2CH2SCH3 Bz H ch3 F OH H H IX-49-8 p-Br-Ph 4 H * Bz H ch3 F OH H H ♦R*4 and R3b joined together by (CH^3 to form five-membered ring. 5 Table IX-50.

1' - R ' 1. 2·· J··' 1 t ' W

Ns R1 ir R3. R3b R4 R3 R6 X Y R7 R8 IX-SO-1 p-I-Ph H H H Bz H CH3 F OH H H IX-50-2 p-I-Ph H H ch3 Bz H ch3 F OH H H IX-50-3 p-I-Ph H H CHCCH^ Bz H ch3 F OH H H IX-50-4 p-I-Ph H H CH2CH(CH3)2 Bz H ch3 F OH H H IX-50-5 p-I-Ph H H CH2Ph Bz H ch3 F OH H H IX-50-6 p-I-Ph H H CHrindol-3-yl Bz H ch3 F OH H H ΪΧ-50-7 p-I-Ph H H CH2CH2SCH3 Bz H ch3 F OH H H IX-50-8 _ . p-I-Ph r»3b· · . * H ♦ Bz H ch3 F OH H H 1 1 UL· ......... ........... ' 1 Him·'·.......... ........... . *R and R joined together by (CH2)3 to form five-membered ring. 2983472-1 -262- WO 2008/121634 PCT/US2008/058183

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Table X-l.

Jfe R1 R2 "r57 "Έ5 R4 R3 R6 X Y r" R8 X-l-1 ch3 H H H ch3 H F F OH H H X-l-2 ch3 H H ch3 ch3 H F F OH H H X-l-3 ch3 H H CH(CH3)2 ch3 H F F OH H H X-l-4 ch3 H H CH3CH(CH3)2 ch3 H F F OH H H X-l-5 ch3 H H CH2Ph ch3 H F F OH H H X-l-6 ch3 H H CH2-indol-3-yl ch3 H F F OH H H X-l-7 ch3 H H CH2CH2SCH3 ch3 H F F OH H H X-l-8 ___ ch3 * H * ch3 H F F OH H H *RX and Rejoined together by (CH2)3 to form five-membered ring.

Xs R1 R2 ηρτ T5- R4 R6 X Y r’ R8 X-2-1 Et H H H ch3 H F F OH H H X-2-2 Et H H ch3 ch3 H F F OH H H X-2-3 Et H H CH(CH3)2 ch3 H F F OH H H X-2-4 Et H H CH2CH(CH3)2 ch3 H F F OH H H X-2-5 Et H H CH2Ph ch3 H F F OH H H X-2-6 Et H H CH2-indol-3-yl ch3 H F F OH H H X-2-7 Et H H ch2ch2sch3 ch3 H F F OH H H X-2-8 Et « Jb · < H ♦ ch3 H F F OH H H ♦R2 and Rejoined together by (0¾¼ to form five-membered ring. 2983472-1 -263- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table X-3.

Ns ΊΓ~ R2 r3‘ R4 R* R6 X Y R7 R8 X-3-1 ipr H H H ch3 H F F OH H H X-3-2 'Pr H H ch3 ch3 H F F OH H H X-3-3 'Pr H H CH(CH3)2 ch3 H F F OH H H X-3-4 'Pr H H CH2CH(CH3)2 ch3 H F F OH H H X-3-5 'Pr H H CH2Ph ch3 H F F OH H H X-3-6 'Pr H H CH2-indol-3-yl ch3 H F F OH H H X-3-7 'Pr H H CH2CH2SCH3 ch3 H F F OH H H X-3-8 'Pr * H * ch3 H F F OH H H *R2 and RJb joined together by (CIhb to form five-membered ring.

Table X-4.

Xs R R2 R3« R3b R4 r! R6 X Υ R7 R8 X-4-1 'Bu H H H ch3 Η F F ΟΗ Η Η X-4-2 'Bu H H ch3 ch3 H F F ΟΗ Η Η X-4-3 'Bu H H CH(CH3)2 ch3 Η F F ΟΗ Η Η X-4-4 'Bu H H CH2CH(CH3)2 ch3 Η F F ΟΗ Η Η X-4-5 'Bu H H' CH2Ph ch3 Η F F ΟΗ Η Η X-4-6 'Bu H H CH2-tndol-3-yl ch3 Η F F ΟΗ Η Η X-4-7 'Bu H H ch2ch2sch3 ch3 Η F F ΟΗ Η Η X-4-8 'Bu * H ♦ ch3 Η F F ΟΗ Η Η *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table X-5. l R R- TL 'J 'g' - '"W".........

Χ2 R R2 r3. R36 R4^ Rs R6 X Y R’ R8 Χ-5-1 Ph H H H ch3 H F F OH H H Χ-5-2 Ph H H ch3 ch3 H F F OH H H Χ-5-3 Ph H H CH(CH3)2 ch3 H F F OH H H Χ-5-4 Ph H H CH2CH(CH3)2 ch3 H F F OH H H Χ-5-5 Ph H H CH2Ph ch3 H F F OH H H Χ-5-6 Ph H H CH2-indol-3-yl ch3 H F F OH H H Χ-5-7 Ph H H ch2ch2sch3 ch3 H F F OH H H Χ-5-8 ... Ph j T-.J0 * H * ch3 H F F OH H H *R2 and R36 joined together by (Clhb to form five-membered ring. 2983472-1 -264- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOUl

Table X-6.

Jfe Rl Ra R3’ R3® R4 RJ R6 X Y R7 ΊΓ X-6-1 p-Me-Ph H H H ch3 H F F OH H H X-6-2 p-Me-Ph H H ch3 ch3 H F F OH H H X-6-3 p-Me-Ph H H CH(CH3)2 ch3 H F F OH H H X-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 H F F OH H H X-6-5 p-Me-Ph H H CH2Ph ch3 H F F OH H H X-6-6 p-Me-Ph H H CH2-indol-3-yl ch3 H F F OH H H X-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 H F F OH H H X-6-8 p-Me-Ph * H * ch3 H F F OH H H *R^ and R3b joined together by (CFhb to form five-membered ring.

Table X-7.

Ns R‘ ΊΓ RJl R3® R^ R5 R6 X Y ΊΓ R8 X-7-1 p-F-Ph H H H CH3 H F F OH H H X-7-2 p-F-Ph H H ch3 ch3 H F F OH H H X-7-3 p-F-Ph H H CH(CH3)2 ch3 H F F OH H H X-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 H F F OH H H X-7-6 p-F-Ph H H CH2Ph ch3 H F F OH H H X-7-7 p-F-Ph H H CH2-indol-3-yl ch3 H F F OH H H X-7-8 p-F-Ph H H CH2CH2SCH3 ch3 H F F OH H H X-7-20 p-F-Ph * H t ch3 H F F OH H H JJ Ml .....— — *R and R joined together by (CHjb to form five-membered ring. 5 Table X-8.

Na R1 R3 Rj- R3b R4 Rs R6 X Y r" r“ X-8-1 p-Cl-Ph H H H CH3 H F F OH H H X-8-2 p-Cl-Ph H H CH3 ch3 H F F OH H H X-8-3 p-Cl-Ph H H ΟΗ(ΟΗ3)2 ch3 H F F OH H H X-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 H F F OH H H X-8-5 p-Cl-Ph H H CH2Ph ch3 H F F OH H H X-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 H F F OH H H X-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 H F F OH H H X-8-8 *r»2 p-Cl-Ph j π30 · .· . ♦ H * ch3 H F F OH H H *R2 and Re joined together by (CHsb to form five-membered ring. 2983472-1 -265- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU I

Table X-9.

Xs R' “R2" r^ Rjb R4 R5 r5- X Y R7 r“ X-9-1 p-Br-Ph H H H ch3 H F F OH H H X-9-2 p-Br-Ph H H ch3 ch3 H F F OH H H X-9-3 p-Br-Ph H H CH(CH3)2 ch3 H F F OH H H X-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 H F F OH H H X-9-6 p-Br-Ph H H CH2Ph ch3 H F F OH H H X-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 H F F OH H H X-9-8 p-Br-Ph H H CH2CH2SCH3 ch3 H F F OH H H X-9-20 p-Br-Ph * H ♦ ch3 H F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table X-10.

R1 R2 R3a R3b R4 R5 R* X Y R8 X-10-1 p-I-Ph Η Η H ch3 H F F OH H H X-10-2 p-I-Ph Η H CH3 ch3 H F F OH H H X-10-3 p-I-Ph Η H CH(CH3)2 ch3 H F F OH H H X-10-4 p-I-Ph Η H CH2CH(CH3)2 ch3 H F F OH H H X-10-5 p-I-Ph Η H CH2Ph ch3 H F F OH H H X-10-6 p-I-Ph Η H CH2-indol-3-yl CH3 H F F OH H H X-10-7 p-I-Ph Η H CH2CH2SCH3 ch3 H F F OH H H X-10-8 p-I-Ph * H * ch3 H F F OH H H *R2 and R3” joined together by (CH2)3 to form five-membered ring. Table X-ll. “jfe R1 R2 R3B R3k R4 R5 R6 X *Y R7" Ra X-ll-1 CH3 Η Η H Et H F F OH H H X-ll-2 CH3 Η H CH3 Et H F F OH H H X-ll-3 CH3 Η Η CH(CH3>2 Et H F F OH H H X-ll-4 CH3 H H CH2CH(CH3)2 Et H F F OH H H X-ll-5 CH3 Η H CH2Ph Et H F F OH H H X-ll-6 CH3 Η H CH2-indol-3-yl Et H F F OH H H X-ll-7 ch3 h h ch2ch2sch3 Et H F F OH H H X-ll-8 CH3 * H * . J n3b : ; 77 \ . Et H F F OH H H ♦R^ and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -266- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU 1

Table X-12.

Ns Rl IF R3a "F R4 RJ R6 X Y R7 r X-12-1 Et H H H Et H F F OH H H X-12-2 Et H H ch3 Et H F F OH H H X-12-3 Et H H CH(CH3)2 Et H F F OH H H X-12-4 Et H H CH2CH(CH3)2 Et H F F OH H H X-12-5 Et H H CH2Ph Et H F F OH H H X-12-6 Et H H CH2-indol-3-yl Et H F F OH H H X-12-7 Et H H CH2CH2SCH3 Et H F F OH H H X-12-8 Et + H ♦ Et H F F OH H H *R2 and R30 joined together by (0¾¼ to form five-membered ring.

Table X-13.

Ns R Ra RJe R3b R4 Rs R6 X Y R7 R8 X-13-1 'Pr H H H Et H F F OH H H X-13-2 'Pr H H CH3 Et H F F OH H H X-13-3 'Pr H H CH(CH3)2 Et H F F OH H H X-13-4 'Pr H H CH2CH(CH3)2 Et H F F OH H H X-13-5 'Pr H H CH2Ph Et H F F OH H H X-13-6 'Pr H H CH2-indol-3-yl Et H F F OH H H X-13-7 'Pr H H CH2CH2SCH3 Et H F F OH H H X-13-8 'Pr * H * Et H F F OH H H *R2 and R3b joined together by (0¾¼ to form five-membered ring. 5 Table X-14. ' ........ 111 ""'"“j»....."J . .. . n ' a

Ns R R2 R 3a R3b R4 R5 R6 X Y R7 R“ X-14-1 'Bu H H H Et H F F OH H H X-14-2 'Bu H H ch3 Et H F F OH H H X-14-3 'Bu H H CH(CH3)2 Et H F F OH H H X-14-4 'Bu H H ΟΗ2ΟΗ(ΟΗ3)2 Et H F F OH H H X-14-5 'Bu H H CH2Ph Et H F F OH H H X-14-6 'Bu H H CH2-indoi-3-yl Et H F F OH H H X-14-7 'Bu H H CH2CH2SCH3 Et H F F OH H H X-14-8 -j * H * Et H F F OH H H W I I·· Mil..... II I I I I II II II I nn nm.i·» *R and R joined together by (0¾¼ to form five-membered ring. 2983472-1 -267- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table X-15.

X2 R1 R,J R3s R3b !? ΊΓ R6 X Y r' Ry X-15-1 Ph H H H Et H F F OH H H X-15-2 Ph H H ch3 Et H F F OH H H X-15-3 Ph H H CH(CH3)j Et H F F OH H H X-15-4 Ph H H CH2CH(CH3)2 Et H F F OH H H X-15-5 Ph H H CH2Ph Et H F F OH H H X-15-6 Ph H H CH2-indol-3-yl Et H F F OH H H X-15-7 Ph H H CH2CH2SCH3 Et H F F OH H H X-15-8 Ph ♦ H * Et H F F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table X-16. R1 R2 R3a R3b R4 R5 R6 X Y R7 R“ X-16-1 p-Me-Ph H Η H Et H F F OH H H X-16-2 p-Me-Ph H H CH3 Et H F F OH H H X-16-3 p-Me-Ph H H CH(CH3)2 Et H F F OH H H X-16-4 p-Me-Ph H H CH2CH(CH3)2 Et H F F OH H H X-16-5 p-Me-Ph H H CH2Ph Et H F F OH H H X-16-6 p-Me-Ph H H CH2-indol-3-yl Et H F F OH H H X-16-7 p-Me-Ph H H CH2CH2SCH3 Et H F F OH H H X-16-8 p-Me-Ph * H * Et H F F OH H H *R2 and RJt> joined together by (CH2)3 to form five-membered ring. Table X-17. Na R1 R2 r3. R3b R4 R5 R6 X Y R7 R# X-17-1 p-F-Ph H Η H Et H F F OH H H X-17-2 p-F-Ph H H CH3 Et H F F OH H H X-17-3 p-F-Ph H H CH(CH3)2 Et H F F OH H H X-17-4 p-F-Ph H Η ΟΗ2ΟΗ(ΟΗ3)2 Et H F F OH H H X-17-5 p-F-Ph H H CH2Ph Et H F F OH H H X-17-6 p-F-Ph H H CH2-indol-3-yl Et H F F OH H H X-17-7 p-F-Ph H H CH2CH2SCH3 Et H F F OH H H X-17-8 p-F-Ph * H ♦ Et H F F OH H H *R2 and Rejoined tot ’ether by ((¾½ to form five-membered ring. 2983472-1 -268- WO 2008/121634 , Λ „ τ,

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table X-I8.

Na R ΊΓ R3" i<4 R5 R6 X Y R7 Ra X-18-1 p-Cl-Ph H H H Et H F F OH H H X-18-2 p-Cl-Ph H H ch3 Et H F F OH H H X-18-3 p-Cl-Ph H H CH(CH3)2 Et H F F OH H H X-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H F F OH H H X-18-5 p-Ci-Ph H H CH2Ph Et H F F OH H H X-18-6 p-Cl-Ph H H CH2-indol-3-yl Et H F F OH H H X-18-7 p-Cl-Ph H H CH2CH2SCH3 Et H F F OH H H X-18-8 p-Cl-Ph * H * Et H F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table X-19.

Ns R1 R2 r3« RJb R4 R· R6 X Y R7 R8 X-19-1 p-Br-Ph H H H Et H F F OH H H X-19-2 p-Br-Ph H H ch3 Et H F F OH H H X-19-3 p-Br-Ph H H CH(CH3)2 Et H F F OH H H X-19-4 p-Br-Ph H H CH2CH(CH3)2 Et H F F OH H H X-19-5 p-Br-Ph H H CH2Ph Et H F F OH H H X-19-6 p-Br-Ph H H CH2-indol-3-yl Et H F F OH H H X-19-7 p-Br-Ph H H ch2ch2sch3 Et H F F OH H H X-19-8 “T77Z-j p-Br-Ph , T,3b: ·- * H * Et H F F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table X-20. I . R RL . --

Ns R1 "R2" -rJT -r3B R4 R5 R4 X Y R7 X-20-1 p-I-Ph H H H Et H F F OH H X-20-2 p-I-Ph H H ch3 Et H F F OH H X-20-3 p-I-Ph H H CH(CH3)2 Et H F F OH H X-20-4 p-I-Ph H H CH2CH(CH3)2 Et H F F OH H X-20-5 p-I-Ph H H CH2Ph Et H F F OH H X-20-6 p-I-Ph H H CH2-indol-3-yl Et H F F OH H X-20-7 p-I-Ph H H ch2ch2sch3 Et H F F OH H X-20-8 i p-I-Ph 1 «Jb. · * H * Et H F F OH H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -269- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table X-21.

Ns R1 R2 R^ Rib R4 R5 R6 X Y RH X-21-1 ch3 H H H ipr H F F OH H H X-21-2 ch3 H H ch3 'Pr H F F OH H H X-21-3 ch3 H H CH(CH3)2 'Pr H F F OH H H X-21-4 ch3 H H CH2CH(CH3)2 'Pr H F F OH H H X-21-5 ch3 H H CH2Ph 'Pr H F F OH H H X-21-6 ch3 H H CH2-indol-3-yl 'Pr H F F OH H H X-21-7 ch3 H H CH2CH2SCH3 'Pr H F F OH H H X-21-8 ch3 * H * 'Pr H F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table X-22.

Ns R R2 R3. R3b R4 ΊΓ R6 X Y R’ R“ X-22-1 Et H H H ’W H F F OH H H X-22-2 Et H H CH3 'Pr H F F OH H H X-22-3 Et H H CH(CH3)2 'Pr H F F OH H H X-22-4 Et H H CH2CH(CH3)2 'Pr H F F OH H H X-22-5 Et H H CH2Ph 'Pr H F F OH H H X-22-6 Et H H CH2-indol-3-yl 'Pr H F F OH H H X-22-7 Et H H CH2CH2SCH3 'Pr H F F OH H H X-22-8 Et * H * 'Pr H F F OH H H ♦R2 and Rejoined together by (0¾¼ to form five-membered ring. 5 Table X-23. - . --— -—w- _ b '‘..Ί1"·'”"!" J-— -. H-n—

Ns R R2 R3. R3b R4 r5 R$ X Y ΊΓ R" X-23-1 'Pr H H H "W H F F OH H H X-23-2 'Pr H H CH3 'Pr H F F OH H H X-23-3 'Pr H H ΟΗ(ΟΗ3)ϊ 'Pr H F F OH H H X-23-4 'Pr H H CH2CH(CH3)2 'Pr H F F OH H H X-23-5 'Pr H H CH2Ph 'Pr H F F OH H H X-23-6 'Pr H H CH2-indoI-3-yl 'Pr H F F OH H H X-23-7 'Pr H H CH2CH2SCH3 'Pr H F F OH H H X-23-8 -j 'Pr i n3b * H * 'Pr H F F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-t -270- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table X-24.

Ns r1- R2 R38 R35 R4 R’ R6 X Y tf Ra X-24-1 'Bu H H H -TpT" H F F OH H H X-24-2 'Bu H H ch3 'Pr H F F OH H H X-24-3 'Bu H H CH(CH3)2 'Pr H F F OH H H X-24-4 'Bu H H CH2CH(CH3)2 'Pr H F F OH H H X-24-5 'Bu H H CH2Ph 'Pr H F F OH H H X-24-6 ^U H H CH2-indol-3-yl 'Pr H F F OH H H X-24-7 'Bu H H CH2CH2SCH3 'Pr H F F OH H H X-24-8 'Bu * H * 'Pr H F F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table X-25.

Xs R R2 R3a R3b R4 R5 R6 X Y R7 R* X-25-1 Ph H H H '"’Pr’ H F F OH H H X-25-2 Ph H H ch3 . 'Pr H F F OH H H X-25-3 Ph H H CH(CH3)2 'Pr H F F OH H H X-25-4 Ph H H CH2CH(CH3)2 'Pr H F F OH H H X-25-5 Ph H H CH2Ph 'Pr H F F OH H H X-25-6 Ph H H CH2-indol-3-yl 'Pr H F F OH H H X-25-7 Ph H H CH2CH2SCH3 'Pr H F F OH H H X-25-8 Ph ΓΓΠΕ" * H ♦ 'Pr H F F OH H H *R2 and RJt> joined together by (CH2)3 to form five-membered ring.

Xa RJ R R3” R3b R4 RJ R6 X Y "p· X-26-1 p-Me-Ph H H H "V H F F OH H H X-26-2 p-Me-Ph H H ch3 'Pr H F F OH H H X-26-3 p-Me-Ph H H CHiCHj), ipr H F F OH H H X-26-4 p-Me-Ph H H CH2CH(CH3)2 'Pr H F F OH H H X-26-5 p-Me-Ph H H CH2Ph 'Pr H F F OH H H X-26-6 p-Me-Ph H H CH2-indol-3-yI 'Pr H F F OH H H X-26-7 p-Me-Ph H H CH2CH2SCH3 'Pr H F F OH H H X-26-8 . p-Me-Ph 1 <-J * H * 'Pr H F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -271- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table X-27.

Ns R1 IC R3s R R4 R3 X Y R’ r“ X-27-1 p-F-Ph H H H "W H F F OH H H X-27-2 p-F-Ph H H ch3 'Pr H F F OH H H X-27-3 p-F-Ph H H 'Pr H F F OH H H X-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr H F F OH H H X-27-5 p-F-Ph H H CH2Ph 'Pr H F F OH H H X-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr H F F OH H H X-27-7 p-F-Ph H H ch2ch2sch3 'Pr H F F OH H H X-27-8 p-F-Ph * H * 'Pr H F F OH H H ♦R1 and Rejoined together by (CH2)3 to form five-membered ring.

Table X-28.

Na Rl R2 RJa R3b R4 R3 R6 X Y r' R8 X-28-1 p-Cl-Ph H H H Pr H F F OH H H X-28-2 p-Cl-Ph H H ch3 'Pr H F F OH H H X-28-3 p-Cl-Ph H H CH(CH3)2 'Pr H F F OH H H X-28-4 p-Cl-Ph H H CH2CH(CH3)2 Pr H F F OH H H X-28-5 p-Cl-Ph H H CH2Ph 'Pr H F F OH H H X-28-6 p-Cl-Ph H H CH2-indol-3-yl Pr H F F OH H H X-28-7 p-Cl-Ph H H CH2CH2SCH3 'Pr H F F OH H H X-28-8 p-Cl-Ph ♦ H ♦ 'Pr H F F OH H H *R4 and Rdb joined together by (CH2)3 to form five-membered ring. 5 Table X-29, j i -g— " n b "

Ns R* R2 R3’ R3b R4 R3 R6 X Y -R7- R8 X-29-1 p-Br-Ph H H H Pr H F F OH H H X-29-2 p-Br-Ph H H ch3 'Pr H F F OH H H X-29-3 p-Br-Ph H H CH(CH3)2 'Pr H F F OH H H X-29-4 p-Br-Ph H H CHjCHCCHjfe 'Pr H F F OH H H X-29-5 p-Br-Ph H H CH2Ph Pr H F F OH H H X-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr H F F OH H H X-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr H F F OH H H X-29-8 ' j p-Br-Ph * H * 'Pr H F F OH H H *R* and Rejoined together by (0¾¼ to form five-membered ring. 2983472-1 -272- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table X-30.

Xs R1 R2 r3« R3b [<4 R* R6 X Y r’ Ru X-30-1 p-l-Ph H H H "ΎΓ H F F OH H H X-30-2 p-I-Ph H H ch3 ;Pr H F F OH H H X-30-3 p-I-Ph H H CH(CH3)2 /pr H F F OH H H X-30-4 p-l-Ph H H CH2CH(CH3)2 ipr H F F OH H H X-30-5 p-I-Ph H H CHjPh ,pr H F F OH H H X-30-6 p-I-Ph H H CH2-indol-3-yl fPr H F F OH H H X-30-7 p-I-Ph H H CH2CH2SCH3 ,pr H F F OH H H X-30-8 p-I-Ph * H * 4Pr H F F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table X-31.

X° R R3 R3a R3b R4 R5 R* X Y R; R# X-31-1 ch3 H H H "Bu H F F OH H H X-31-2 ch3 H H ch3 "Bu H F F OH H H X-31-3 ch3 H H CH(CH3)2 "Bu H F F OH H H X-31-4 ch3 H H CH2CH(CH3)2 "Bu H F F OH H H X-31-5 ch3 H H CH2Ph "Bu H F F OH H H X-31-6 ch3 H H CH2-indo]-3-yl "Bu H F F OH H H X-31-7 ch3 H H CH2CH2SCH3 "Bu H F F OH H H X-31-8 ch3 * H * "Bu H F F OH H H ♦R2 and RJt> joined together by (CH2)3 to form five-membered ring. 5 Table X-32. '1 ...........— _ .— —» " a

Xs R R2 R3" R3b R4 ΊΓ R6 X Y R7 Ru X-32-1 Et H H H "Bu H F F OH H H X-32-2 Et H H ch3 "Bu H F F OH H H X-32-3 Et H H ΟΗ(ΟΗ3)2 "Bu H F F OH H H X-32-4 Et H H CH2CH(CH3)2 "Bu H F F OH H H X-32-5 Et H H CH2Ph "Bu H F F OH H H X-32-6 Et H H CH2-indol-3-yl "Bu H F F OH H H X-32-7 Et H H CH2CH2SCH3 "Bu H F F OH H H X-32-8 -Π72-j Et Γ7Γ35" * H * "Bu H F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -273 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table X-33.

Ns R1 IF r3> “r5* r4 R5 R6 X Y R7 R8 X-33-1 ~W H H H "Bu H F F OH H H X-33-2 fpr H H ch3 "Bu H F F OH H H X-33-3 ’Pr H H CH(CH3)2 "Bu H F F OH H H X-33-4 'Pr H H CH2CH(CH3)2 "Bu H F F OH H H X-33-5 'Pr H H CH2Ph "Bu H F F OH H H X-33-6 'Pr H H CH2-indol-3-yl "Bu H F F OH H H X-33-7 'Pr H H CH2CH2SCH3 "Bu H F F OH H H X-33-8 'Pr * H * "Bu H F F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table X-34.

Ns R R2 RJ‘ R" R4 Rs R6 X Y R7 R1 X-34-1 'Bu H H H "Bu H F F OH H H X-34-2 'Bu H H CH3 "Bu H F F OH H H X-34-3 'Bu H H CH(CH3)2 "Bu H F F OH H H X-34-4 'Bu H H CH2CH(CH3)2 "Bu H F F OH H H X-34-5 'Bu H H CHaPh "Bu H F F OH H H X-34-6 'Bu H H CH2-indol-3-yl "Bu H F F OH H H X-34-7 'Bu H H CH2CH2SCH3 "Bu H F F OH H H X-34-8 'Bu * H * "Bu H F F OH H H *R2 and R3b joined together by (C%)3 to form five-membered ring. 5 Table X-35. I M n. ·ι .......... 1 J J J 1

Ns R R2 R3a R3b R4 RJ R6 X Y R7 R8 X-35-1 Ph H H H "Bu H F F OH H H X-35-2 Ph H H ch3 "Bu H F F OH H H X-35-3 Ph H H CH(CH3)a "Bu H F F OH H H X-35-4 Ph H H CH2CH(CH3)2 "Bu H F F OH H H X-35-5 Ph H H CH2Ph "Bu H F F OH H H X-35-6 Ph H H CH2-indol-3-yl "Bu H F F OH H H X-35-7 Ph H H CH2CH2SCH3 "Bu H F F OH H H X-35-8 _ j Ph ΓτΓΠΓ * H * "Bu H F F OH H H *R'2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -274- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table X-36.

Jte R1 R2 -r3T "r- R* R6 X Y R7 Ra X-36-1 p-Me-Ph H H H "Bu H F F OH H H X-36-2 p-Me-Ph H H ch3 "Bu H F F OH H H X-36-3 p-Me-Ph H H CH(CH3)2 "Bu H F F OH H H X-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu H F F OH H H X-36-5 p-Me-Ph H H CH2Ph "Bu H F F OH H H X-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu H F F OH H H X-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu H F F OH H H X-36-8 p-Me-Ph * H * "Bu H F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table X-37.

Xa R1 R3 RJ“ R3b R4 R5 R6 X Y R7 R“ X-37-1 p-F-Ph H H H "Bu H F F OH H H X-37-2 p-F-Ph H H CH3 "Bu H F F OH H H X-37-3 p-F-Ph H H CHCCHa), "Bu H F F OH H H X-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu H F F OH H H X-37-5 p-F-Ph H H CH2Ph "Bu H F F OH H H X-37-6 p-F-Ph H H CH2-indol-3-yl "Bu H F F OH H H X-37-7 p-F-Ph H H CH2CH2SCH3 "Bu H F F OH H H X-37-8 p-F-Ph * H * "Bu H F F OH H H *R2 and RJb joined together by to form five-membered ring. 5 Table X-38.

1 1 M ..............j — ... * .......... » B

Xa R1 R3 r3. R3b R4 Rs Rb X Y R# X-38-1 p-Cl-Ph H H H "Bu H F F OH H H X-38-2 p-Cl-Ph H H ch3 "Bu H F F OH H H X-38-3 p-Cl-Ph H H CH(CH3)2 "Bu H F F OH H H X-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H F F OH H H X-38-5 p-Cl-Ph H H CH2Ph "Bu H F F OH H H X-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu H F F OH H H X-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu H F F OH H H X-38-8 *t»2 ... - p-Ci-Ph * H * "Bu H F F OH H H *R2 and R3b joined together by (CHj)^ to form five-membered ring. 2983472-1 - 275 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU 1

Table X-39.

Ns R1 R2 R3a T* Rs R6 X Y I? Rh X-39-1 p-Br-Ph H H I-I "Bu H F F OH H H X-39-2 p-Br-Ph H H ch3 "Bu H F F OH H H X-39-3 p-Br-Ph H H CH(CH3)2 "Bu H F F OH H H X-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu H F F OH H H X-39-5 p-Br-Ph H H CH2Ph "Bu H F F OH H H X-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu H F F OH H H X-39-7 p-Br-Ph H H CH2CH2SCH3 "Bu H F F OH H H X-39-8 p-Br-Ph * H * "Bu H F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table X-40.

Ns Rl R2 Rj. R3b R^ Rs R6 X Y R7 R“ X-40-1 p-I-Ph H H H "Bu H F F OH H H X-40-2 p-I-Ph H H ch3 "Bu H F F OH H H X-40-3 p-I-Ph H H CH(CH3)2 "Bu H F F OH H H X-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu H F F OH H H X-40-5 p-I-Ph H H CH2Ph "Bu H F F OH H H X-40-6 p-I-Ph H H CH2-indol-3-yl "Bu H F F OH H H X-40-7 p-I-Ph H H CH2CH2SCH3 "Bu H F F OH H H X-40-8 p-I-Ph * H * "Bu H F F OH H H *R2 and RJb joined together by (Cthh to form five-membered ring. 5 Table X-41. i λ i w a

Ns R R2 R3. R3b R4 RJ R6 X Y R R8 X-41-1 CH3 H Η Η Bz H F F OH H H X-41-2 ch3 H Η ch3 Bz H F F OH H H X-41-3 ch3 H Η CH(CH3)2 Bz H F F OH H H X-41-4 ch3 Η Η CH2CH(CH3)2 Bz H F F OH H H X-41-5 ch3 Η Η CH2Ph Bz H F F OH H H X-41-6 ch3 Η Η CHrindol-3-yl Bz H F F OH H H X-41-7 ch3 Η Η CH2CH2SCH3 Bz H F F OH H H X-41-8 ch3 * Η * Bz H F F OH H H ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -276- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Table X-42.

Νξ R1 R2 R3® T5 R* Rs R4 X Y R7 Rb X-42-1 Et H H H Bz H F F OH H H X-42-2 Et H H ch3 Bz H F F OH H H X-42-3 Et H H CH(CH3)2 Bz H F F OH H H X-42-4 Et H H CH2CH(CH3)2 Bz H F F OH H H X-42-5 Et H H CH2Ph Bz H F F OH H H X-42-6 Et H H CH2-indol-3-yl Bz H F F OH H H X-42-7 Et H H CH2CH2SCH3 Bz H F F OH H H X-42-8 Et * H * Bz H F F OH H H *R2 and RJb joined together by ((¾^ to form five-membered ring.

Table X-43.

Ns R R2 R3® R3b R4 Rs R6 X Y R7 RB X-43-1 H H H Bz H F F OH H H X-43-2 'Pr H H ch3 Bz H F F OH H ή X-43-3 'Pr H H CH(CH3)2 Bz H F F OH H H X-43-4 'Pr H H CH2CH(CH3)2 Bz H F F OH H H X-43-5 'Pr H H CH2Ph Bz H F F OH H H X-43-6 'Pr H H CH2-indol-3-yl Bz H F F OH H H X-43-7 'Pr H H ch2ch2sch3 Bz H F F OH H H X-43-8 /pr * H * Bz H F F OH H H 10 *R2 and R3b joined together by (Cihb to form five-membered ring.

Table X-44.

Ns R* R7 R3® ""I?5 R4 R5 R4 X Y R7 Ra X-44-1 'Bu H H H Bz H F F OH H H X-44-2. *Bu H H ch3 Bz H F F OH H H X-44-3 'Bu H H CH(CH3)a Bz H F F OH H H X-44-4 'Bu H H CH2CH(CH3)2 Bz H F F OH H H X-44-5 'Bu H H CH2Ph Bz H F F OH H H X-44-6 'Bu H H CH2-indol-3-yI Bz H F F OH H H X-44-7 'Bu H H CH2CH2SCH3 Bz H F F OH H H X-44-8 *n2 . J 'Bu * H * Bz H F F OH H H *R2 and R36 joined together by (CFhb to form five-membered ring. 2983472-1 -277- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Table X-45.

Xs Rl R2 R3a r36- Ic R6 X Y R7 R11 X-45-1 Ph H H H Bz H F F OH H H X-45-2 Ph H H ch3 Bz H F F OH H H X-45-3 Ph H H CH(CH3)2 Bz H F F OH H H X-45-4 Ph H H CH2CH(CH3)2 Bz H F F OH H H X-45-5 Ph H H CH2Ph Bz H F F OH H H X-45-6 Ph H H CHrindol-3-yl Bz H F F OH H H X-45-7 Ph H H ch2ch2sch3 Bz H F F OH H H X-45-8 *n2 , Ph 1 nJb * H * Bz H F F OH H H *R2 and R3b joined together by (C%)3 to form five-membered ring.

Table X-46.

Xs R1 R2 r3« R3b R4 Rs R6 X Y ΊΓ R8 X-46-1 p-Me-Ph H H H Bz H F F OH H H X-46-2 p-Me-Ph H H ch3 Bz H F F OH H H X-46-3 p-Me-Ph H H CH(CH3)2 Bz H F F OH H H X-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz H F F OH H H X-46-S p-Me-Ph H H CH2Ph Bz H F F OH H H X-46-6 p-Me-Ph H H CH2-indol-3-yl Bz H F F OH H H X-46-7 p-Me-Ph H H CH2CH2SCH3 Bz H F F OH H H X-46-8 p-Me-Ph , nJb . i-3 * H ♦ Bz H F F OH H H

W RL. ............... I I *R and R joined together by (CH2)3 to form five-membered ring. 5 Table X-47. — l « ....... J .............. . . -"»

Xs R1 R2 R3a R3b R4 r! R* X Υ R7 R“ X-47-1 p-F-Ph H H H Bz H F F ΟΗ Η Η X-47-2 p-F-Ph H H ch3 Bz H F F ΟΗ Η Η X-47-3 p-F-Ph H H chcch-Oj Bz Η F F ΟΗ Η Η X-47-4 p-F-Ph H H CH2CH(CH3)2 Bz Η F F ΟΗ Η Η X-47-5 p-F-Ph H H CH2Ph Bz Η F F ΟΗ Η Η X-47-6 p-F-Ph H H CH2-indol-3-yl Bz Η F F ΟΗ Η Η X-47-7 p-F-Ph H H ch2ch2sch3 Bz Η F F ΟΗ Η Η X-47-8 p-F-Ph * H * Bz Η F F ΟΗ Η Η *R2 and RJt> joined together by (CH2)3 to form five-membered ring * Table X-48. Xs R R2 “ipr R4 Rs R6 X Υ R7 R* 29834724 -278- WO 2008/121634

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Ms Ra R3a" “F Ί? R3 R6 X Y R’ R1 X-48-1 p-Cl-Ph H H H Bz H F F OH H H X-48-2 p-Cl-Ph H H ch3 Bz H F F OH H H X-48-3 p-CI-Ph H H CH(CH3)2 Bz H F F OH H H X-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H F F OH H H X-48-5 p-Cl-Ph H H CH2Ph Bz H F F OH H H X-48-6 p-Cl-Ph H H CH2-indol-3-yI Bz H F F OH H H X-48-7 p-Cl-Ph H H ch2ch2sch3 Bz H F F OH H H X-48-8 p-Cl-Ph ♦ H * Bz H F F OH H H *R2 and RJt> joined together by (CHj)j to form five-membered ring.

Table X-49.

Ms R1 R2 K'1 R3b R4 R3 R6 X Y R7 R“ X-49-1 p-Br-Ph H H H Bz H F F OH H H X-49-2 p-Br-Ph H H CH3 Bz H F F OH H H X-49-3 p-Br-Ph H H CH(CH3)2 Bz H F F OH H H X-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz H F F OH H H X-49-5 p-Br-Ph H H CH2Ph Bz H F F OH H H X-49-6 p-Br-Ph H H CH2-indol-3-yl Bz H F F OH H H X-49-7 p-Br-Ph H H CHaCH2SCH3 Bz H F F OH H H X-49-8 p-Br-Ph * H * Bz H F F OH H H *R2 and RJt> joined together by (CH2)3 to form five-membered ring.

Table X-50.

Ma R1 IF r3b ~F R4 R3 R6 X Y R7 R8 X-50-1 p-I-Ph H H H Bz H F F OH H H X-50-2 p-I-Ph H H ch3 Bz H F F OH H H X-50-3 p-I-Ph H H CHCCH^ Bz H F F OH H H X-50-4 p-I-Ph H H ΟΗ2ΟΗ(ΟΗ3)2 Bz H F F OH H H X-50-5 p-I-Ph H H CH2Ph Bz H F F OH H H X-50-6 p-I-Ph H H CHrindol-3-yl Bz H F F OH H H X-50-7 p-I-Ph H H CH2CH2SCH3 Bz H F F OH H H X-50-8 p-I-Ph i «36 · Ϊ * H * Bz H F F OH H H *R2 and R36 joined together by (CH2)3 to form five-membered ring. 2983472-1 -279- WO 2008/121634 PCT/US2008/058183

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XI

Table XI-1.

Xs T<T R2 R3' "r3® R4 R5 R0 X Y R7 R8 XI-1-1 ch3 H H H ch3 H H F OH H H XI-1-2 ch3 H H ch3 ch3 H H F OH H H XI-1-3 ch3 H H CH(CH3)2 ch3 H H F OH H H XI-1-4 ch3 H H CH2CH(CH3)2 ch3 H H F OH H H XI-1-5 ch3 H H CH2Ph ch3 H H F OH H H XI-I-6 ch3 H H CHrindoI-3-yl ch3 H H F OH H H XM-7 CHj H H CH2CH2SCH3 ch3 H H F OH H H XI-1-8 ch3 . r»3b · ♦ H * ch3 H H F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

X» ΊΓ" R2 -jpr “R35 R4 r3" R6 X Y ΊΓ R8 XI-2-1 Et H H H ch3 Η H F OH H H XI-2-2 Et H H CH3 ch3 H H F OH H H XI-2-3 Et H H ΟΗ(ΟΗ3)2 ch3 H H F OH H H Xl-2-4 Et H H CH2CH(CH3)2 ch3 H H F OH H H XI-2-5 Et H H CH2Pb ch3 H H F OH H H XI-2-6 Et H H CH2-indol-3-yl ch3 H H F OH H H XI-2-7 Et H H CH2CH2SCH3 ch3 H H F OH H H XI-2-8 ' ' Et 1 * H * ch3 H H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -280- WO 2008/121634 PCT/US2008/058183

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Table XI-3.

Xs R1 R2 R3a R3b R4 v Ί?’" X Y R7 R8 XI-3-1 'Pr H H H ch3 H H F OH H H XI-3-2 fPr H H ch3 ch3 H H F OH H H XI-3-3 'Pr H H CH(CH3)2 ch3 H H F OH H H XI-3-4 fPr H H CH2CH(CH3)2 ch3 H H F OH H H XI-3-5 'Pr H H CHjPh ch3 H H F OH H H XI-3-6 'Pr H H CH2-indol-3-yl ch3 H H F OH H H XI-3-7 'Pr H H CH2CH2SCH3 ch3 H H F OH H H XI-3-8 'Pr * H ♦ ch3 H H F OH H H *R2 and R3t) joined together by (0¾¼ to form five-membered ring.

Table XI-4.

Xs “R1” Tr R3’ R3b R4 RJ R&amp; X Y R7 r“ XU-1 'Bu H H H CH3 H H F OH H H XI-4-2 'Bu H H ch3 ch3 H H F OH H H ΧΪ-4-3 'Bu H H CHiCHah ch3 H H F OH H H XI-4-4 'Bu H H CH2CH(CH3)2 ch3 H H F OH H H X1-4-S 'Bu H H CH2Ph ch3 H H F OH H H XI-4-6 'Bu H H CH2-indol-3-yl ch3 H H F OH H H XI-4-7 'Bu H H CH2CH2SCH3 ch3 H H F OH H H XI-4-8 'Bu * H * ch3 H H F OH H H ♦R2 and R315 joined together by (CH2)3 to form five-membered ring. 5 Table XI-5. 1 i 1 it - hl· ' j w

Xs R1 R1 r3. R3b . R4 rs R6 X Y r" R“ XI-5-1 Ph H H H ch3 H H F OH H H XI-5-2 Ph H H ch3 ch3 H H F OH H H Xl-5-3 Ph H H CHCCH^ ch3 H H F OH H H XI-5-4 Ph H H CHjCHCCHa), ch3 H H F OH H H XI-5-5 Ph H H CH2Ph ch3 H H F OH H H XI-5-6 Ph H H CH2-indol-3-yl ch3 H H F OH H H XI-5-7 Ph H H CH2CH2SCH3 ch3 H H F OH H H XI-5-8 Ph * H * ch3 H H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -281- WO 2008/121634 PCT/US2008/058183

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Table Xl-6.

X2 R1 R2 r3“ R5 R6 X Y R7 Ra XI-6-1 p-Me-Ph H H H ch3 H H F OH H H XI-6-2 p-Me-Ph H H ch3 ch3 H H F OH H H XI-6-3 p-Me-Ph H H CH(CH3)2 ch3 H H F OH H H XI-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 H H F OH H H XI-6-5 p-Me-Ph H H CH2Ph ch3 H H F OH H H XI-6-6 p-Me-Ph H H CH2-indol-3-yl ch3 H H F OH H H XI-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 H H F OH H H XI-6-8 p-Me-Ph * H * ch3 H H F OH H H *R2 and R3b joined together by (CHfek to form five-membered ring.

Table XI-7.

X2 R1 Ra r3. R3b R4 r! R6 X Y R7 R8 XI-7-1 p-F-Ph H H H CH3 H H F OH H H XI-7-2 p-F-Ph H H ch3 ch3 H H F OH H H XI-7-3 p-F-Ph H H CH(CH3)2 ch3 H H F OH H H XI-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 H H F OH H H XI-7-6 p-F-Ph H H CH2Ph ch3 H H F OH H H XI-7-7 p-F-Ph H H CH2-indol-3-yl ch3 Η H F OH H H XI-7-8 p-F-Ph H H CH2CH2SCH3 ch3 H H F OH H H XI-7-20 p-F-Ph * H * ch3 H H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XI-8. I I. - - — ! 1 ....... J \ 1 *.» J' * ' IT ’

Xs R R2 RJl R3b R4 R5 R6 X Y R7 Ra Xl-8-1 p-Cl-Ph H H H ch3 H H F OH H H XI-8-2 p-Cl-Ph H H ch3 ch3 H H F OH H H XI-8-3 p-CI-Ph H H CHCCHah ch3 H H F OH H H XI-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 H H F. OH H H XI-8-5 p-Cl-Ph H H CH2Ph ch3 H H F OH H H XI-8-6 p-Cl-Ph H H CH2-indol-3-y) ch3 H H F OH H H XI-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 H H F OH H H XI-8-8 —: p-Cl-Ph i : .· . * H • ch3 H H F OH H H *R2 and R36 joined together by (CH2)3 to form five-membered ring. 2983472-1 -282- WO 2008/121634 PCT/US2008/058183

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Table XI-9.

Jfe R1 "R3" r3b R3b rF- R* R6 X Y R’ r“ XI-9-1 p-Br-Ph H H H ch3 H H F OH H H XI-9-2 p-Br-Ph H H ch3 ch3 H H F OH H H XI-9-3 p-Br-Ph H H CH(CH3)2 ch3 H H F OH H H XI-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 H H F OH H H XI-9-6 p-Br-Ph H H CH2Ph ch3 H H F OH H H XI-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 H H F OH H H XI-9-8 p-Br-Ph H H CH2CH2SCH3 ch3 H H F OH H H XI-9-20 . j p-Br-Ph T-.J&amp; I ! J * H * ch3 H H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table ΧΜ0. — R3 Rie R3b R4 R* R* X Υ R’ ΊΓ XI-10-1 p-I-Ph H H H CH3 Η Η F ΟΗ Η Η XI-10-2 p-I-Ph H H ch3 ch3 Η Η F ΟΗ Η Η XI-10-3 p-I-Ph H H CH(CH3)2 ch3 Η Η F ΟΗ Η Η XI-10-4 p-I-Ph H H CH2CH(CH3)2 ch3 Η Η F ΟΗ Η Η XI-10-5 p-I-Ph H H CH2Ph ch3 Η Η F ΟΗ Η Η XI-10-6 p-I-Ph H H CH2-indol-3-yl ch3 Η Η F ΟΗ Η Η XI-10-7 p-I-Ph H H ch2ch2sch3 ch3 Η Η F ΟΗ Η Η XI-10-8 p-I-Ph * H * ch3 Η Η F ΟΗ Η Η *R2 and RJb joined together by (CH2)3 to form five-membered ring. Table XI-11. R1 R3 rjp. R35 R4 R* -£δ- X Υ R’ R8 XI-11-1 ch3 h H H Et H Η F ΟΗ Η Η XI-11-2 CH3 H H ch3 Et Η Η F ΟΗ Η Η XI-11-3 CH3 H H CHfCH^ Et Η Η F ΟΗ Η Η XI-11-4 CH3 H H CH2CH(CH3)2 Et Η Η F ΟΗ Η Η XI-11-5 CH3 H H CH2Ph Et Η Η F ΟΗ Η Η XI-11-6 CH3 H H CH2-indol-3-yl Et Η Η F ΟΗ Η Η XI-11-7 CH3 H H CH2CH2SCH3 Et Η Η F ΟΗ Η Η XI-11-8 CH3 * ..irJb· . H * Et Η Η F ΟΗ Η Η *R2 and Rejoined together by (CH2)j to form five-memberedring 2983472-1 -283 - WO 2008/121634 PCT/US2008/058183

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Table XI-12.

Na R1 R2 -pr· R3b R4 R5 R6 X Y r’ R8 XI-I2-1 Et H H H Et H H F OH H H XI-12-2 Et H H ch3 Et H H F OH H H XI-12-3 Et H H CH(CH3)2 Et H H F OH H H XI-12-4 Et H H CH2CH(CH3)2 Et H H F OH H H XI-12-5 Et H H CH2Ph Et H H F OH H H XI-12-6 Et H H CH2-indol-3-yl Et H H F OH H H XI-12-7 Et H H CH2CH2SCH3 Et H H F OH H H XI-12-8 Et * H * Et H H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XI-13.

R R3 Rj. R3b R4 R5 R6 X Y R7 R8 XI-13-1 'Pr H H H Et H H F OH H H XI-13-2 /pr H H CH3 Et H H F OH H H XI-13-3 'Pr H H CHCCHa), Et H H F OH H H XI-13-4 'Pr H H CH2CH(CH3)2 Et H H F OH H H XI-13-5 'Pr H H CH2Ph Et H H F OH H H XI-13-6 'Pr H H CH2-indol-3-yl Et H H F OH H H XI-13-7 'Pr H H CH2CH2SCH3 Et H H F OH H H XI-13-8 *n2 j 'Pr ♦ H * Et H H F OH H H *R2 and Rejoined together by (CH2)3to ^omi five-membered ring. 5 Table XI-14.

I ........ HL.........—' .'.""J' 1 ' - * J ' " R ' H

Xa R‘ R3 ~pr- "P5 R* R3 R4 X Y R’ R8 XI-14-1 'Bu H H H Et H H F OH H H XI-14-2 'Bu H H ch3 Et H H F OH H H XI-14-3 'Bu H H CHCCH^ Et H H F OH H H XI-14-4 'Bu H H CH2CH(CH3)3 Et H H F OH H H XI-14-5 *Bu H H CH2Ph Et H H F OH H H XI-14-6 'Bu H H CH2-indol-3-yl Et H H F OH H H XI-14-7 'Bu H H CH2CH2SCH3 Et H H F OH H H XI-14-8 'Bu > · · J * H * Et H H F OH H H ♦R2 and RJb joined together by (CH2)3t0 ^orm five-membered ring. 298M72-1 -284- WO 2008/121634 PCT/US2008/058183

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Table XI-15.

R1 R2 R3b "r35 R4 R4 R6 X Y R7 R" XI-15-1 Ph H H H Et H H F OH H H XI-15-2 Ph H H ch3 Et H H F OH H H XI-15-3 Ph H H CH(CH3)2 Et H H F OH H H XI-15-4 Ph H H CH2CH(CH3)2 Et H H F OH H H XI-15-5 Ph H H CH2Ph Et H H F OH H H XI-15-6 Ph H H CH2-indol-3-yl Et H H F OH H H XI-15-7 Ph H H CH2CH2SCH3 Et H H F OH H H XI-15-8 *n'2 j Ph * H * Et H H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XI-16.

R1 R2 R3' 1 R3b R4 R3 R6 X Y R7 R8 XI-16-1 p-Me-Ph Η H H Et H H F OH H H XI-16-2 p-Me-Ph Η H ch3 Et H H F OH H H XI-16-3 p-Me-Ph Η H CH(CH3)2 Et H H F OH H H XI-16-4 p-Me-Ph Η H CH2CH(CH3)2 Et H H F OH H H XI-16-5 p-Me-Ph Η H CH2Ph Et H H F OH H H XI-16-6 p-Me-Ph Η H CHrindol-3-yl Et H H F OH H H Xl-16-7 p-Me-Ph Η H CH2CH2SCH3 Et H H F OH H H XI-16-8 p-Me-Ph * H * Et H H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. TableXI-17. r2 r3b R35 R4 R5 R4 X Ϋ R7" R“ XI-17-1 p-F-Ph Η H H Et H H F OH H H XI-17-2 p-F-Ph Η H CH3 Et H H F OH H H XI-17-3 p-F-Ph Η H chccHjX Et H H F OH H H XI-17-4 p-F-Ph Η H CH2CH(CH3)2 Et H H F OH H H XI-17-5 p-F-Ph Η H CH2Ph Et H H F OH H H XI-17-6 p-F-Ph Η H CH2-indol-3-yl Et H H F OH H H XI-17-7 p-F-Ph Η H ch2ch2sch3 Et H H F OH H H XI-17-8 p-F-Ph * H * Et H H F OH H H ♦R* and Rejoined together by (Cthb to form five-membered ring. 2983472-) -285- WO 2008/121634 PCT/US2008/OS8183

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Table XI-18.

Xa R1 R2 -gsr T* V" R* R6 X Y r’ XI-18-1 p-CI-Ph H H H Et H H F OH H H XI-18-2 p-Cl-Ph H H ch3 Et H H F OH H H XI-18-3 p-Cl-Ph H H CH(CH3)2 Et H H F OH H H XI-18-4 p-CI-Ph H H CH2CH(CH3)2 Et H H F OH H H XI-18-5 p-Cl-Ph H H CH2Ph Et H H F OH H H XI-18-6 p-Cl-Pb H H CH2-indol-3-yl Et H H F OH H H XI-18-7 p-Cl-Ph H H CH2CH2SCH3 Et H H F OH H H XI-18-8 “ΐτπ—T p-CI-Ph * H * L·.. //IT! \ Et H H F OH i H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XI-19.

Xa R1 R2 “R31 R4 Rs R6 X Y R“ XI-19-1 p-Br-Ph H H H Et H H F OH H H XI-19-2 p-Br-Ph H H ch3 Et H H F OH H H XI-19-3 p-Br-Ph H H CH(CH3)2 Et H H F OH H H XI-19-4 p-Br-Ph H H CH2CH(CH3)2 Et H H F OH H H XI-19-5 p-Br-Ph H H CH2Ph Et H H F OH H H XI-19-6 p-Br-Ph H H CH2-indol-3-yl Et H H F OH H H XI-19-7 p-Br-Ph H H CH2CH2SCH3 Et H H F OH H H XI-19-8 p-Br-Ph * H Mi Et H H F OH H H *R2 and Rejoined together by (CH2>3 to form five-membered ring. Table XI-20. Xa R‘ R2 R3· R3b R4 RJ R6 X Y r’ R# XI-20-1 p-I-Ph H H H Et H H F OH H H XI-20-2 p-I-Ph H H ch3 Et H H F OH H H XI-20-3 p-I-Ph H H CH(CH3)2 Et H H F OH H H XI-20-4 p-I-Ph H H CH2CH(CH3)2 Et H H F OH H H XI-20-5 p-I-Ph H H CH2Ph Et H H F OH H H XI-20-6 p-I-Ph H H CH2-indol-3-yl Et H H F OH H H XI-20-7 p-I-Ph H H CH2CH2SCH3 Et H H F OH H H XI-20-8 p-I-Ph *n2 j - · * H ♦ Et H H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -286- WO 2008/121634 PCT/US2008/058183

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Table XI-21.

Ns Rl IF R3b R3b T” R5 R6 X Y R; if XI-21-1 ch3 H H H 'Pr H H F OH H H XI-21-2 ch3 H H ch3 'Pr H H F OH H H XI-21-3 ch3 H H CH(CH3)2 'Pr H H F OH H H XI-21-4 ch3 H H CH2CH(CH3)2 'Pr H H F OH H H XI-21-5 ch3 H H CH2Ph 'Pr H H F OH H H XI-21-6 ch3 H H CH2-indol-3-yl 'Pr H H F OH H H XI-21-7 ch3 H H CH2CH2SCH3 'Pr H H F OH H H XI-21-8 ch3 ♦ H ♦ 'Pr H H F OH H H *R2 and R3b joined together by (0¾¼ to form five-membered ring.

Table XI-22.

Na Rl "R2" “R37 “r* R4 “r5" R6 X Y R7 ΊΤ XI-22-1 Et H H H Jpr H H F OH H H XI-22-2 Et H H CH3 'Pr H H F OH H H XI-22-3 Et H H CH(CH3)2 'Pr H H F OH H H XI-22-4 Et H H CH2CH(CH3)2 'Pr H H F OH H H XI-22-5 Et H H CH2Ph 'Pr H H F OH H H XI-22-6 Et H H CH2-indol-3-yl 'Pr H H F OH H H XI-22-7 Et H H CH2CH2SCH3 'Pr H H F OH H H XI-22-8 “Ϊ7Γ2-T Et + H ♦ 'Pr H H F OH H H *R2 and R3b joined together by (CThbt0 fQrrn five-membered ring.

Na R1 R2 -rS" R3b R4 RJ R6 X Y R7 ic XI-23-1 "W H H H H H F OH H H XI-23-2 'Pr H H CH3 'Pr H H F OH H H XI-23-3 'Pr H H CH(CH3)2 'Pr H H F OH H H XI-23-4 'Pr H H CH2CH(CH3)2 'Pr H H F OH H H XI-23-5 'Pr H H CH2Ph 'Pr H H F OH H H XI-23-6 'Pr H H CH2-indol-3-yl 'Pr H H F OH H H XI-23-7 'Pr H H CH2CH2SCH3 Tr H H F OH H H XI-23-8 'Pr 4 H « 'Pr H H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -287- WO 2008/121634 PCT/US2008/058183

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Table XI-24.

“Jfe R1- R2 R3’ “R35 TT R6 X Y R’ R“ XI-24-1 'Bu H H H JPr H H F OH H H XI-24-2 'Bu H H ch3 'Pr H H F OH H H XI-24-3 'Bu H H CH(CH3)2 'Pr H H F OH H H XI-24-4 'Bu H H CH2CH(CH3)2 'Pr H H F OH H H XI-24-5 'Bu H H CHjPh 'Pr H H F OH H H XI-24-6 'Bu H H CH2-indol-3-yl 'Pr H H F OH H H XI-24-7 'Bu H H ch2ch2sch3 'Pr H H F OH H H XI-24-8 'Bu * H * 'Pr H H F OH H H ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. Table XI-25. “jfe R1” R2 R3* R3b R4 Rs R6 X Y R7 R8 XI-25-1 Ph H H H “W H H F OH H H XI-25-2 Ph H H ch3 'Pr H H F OH H H XI-2S-3 Ph H H CH(CH3)2 'Pr H H F OH H H XI-25-4 Ph H H CH2CH(CH3)2 'Pr H H F OH H H XI-25-5 Ph H H CH2Ph 'Pr H H F OH H H XI-25-6 Ph H H CH2-indol-3-yl 'Pr H H F OH H H XI-25-7 Ph H H CH2CH2SCH3 'Pr H H F OH H H XI-25-8 Ph “iT.'2 ♦ H * 'Pr H H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XI-26. .............— ...... ·ι .....ML· f JT fl

X® R1 R2 R3. "r3® R4 Rj R6 X Y R7 R“ XI-26-1 p-Me-Ph H H H 'Pr H H F OH H H XI-26-2 p-Me-Ph H H CH3 'Pr H H F OH H H XI-26-3 p-Me-Ph H H CHCCH,), Tr H H F OH H H XI-26-4 p-Me-Ph H H CH2CH(CH3)2 ^r H H F OH H H XI-26-5 p-Me-Ph H H CH2Ph 'Pr H H F OH H H XI-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr H H F OH H H . XI-26-7 p-Me-Ph H H CH2CH2SCH3 'Pr H H F OH H H XI-26-8 . .. J p-Me-Ph r.3b* f J. * H * /pr H H F OH H H *R2 and R36 joined together by (CH2)3 to form five-membered ring. 2983472-1 -288- WO 2008/121634

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Table XI-27.

M R1 v r3‘ “r36 ΊΤ R6 X Y R Ra XI-27-1 p-F-Ph H H H zPr H H F OH H H XI-27-2 p-F-Ph H H ch3 'Pr H H F OH H H XI-27-3 p-F-Ph H H CH(CH3)2 'Pr H H F OH H H XI-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr H H F OH H H XI-27-5 p-F-Ph H H CH2Ph 'Pr H H F OH H H XI-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr H H F OH H H XI-27-7 p-F-Ph H H CH2CH2SCH3 'Pr H H F OH H H XI-27-8 -T p-F-Ph * H * 'Pr H H F OH H H *R2 and R^6 joined together by (CIT^ to form five-membered ring.

Table XI-28.

Ka R1. R2 "1? R4 Rs R6 X Y R7 R“ XI-28-1 p-Cl-Ph H H H 7Pr H H F OH H H XI-28-2 p-CI-Ph H H CH3 'Pr H H F OH H H XI-28-3 p-Cl-Ph H H CH(CH3)2 'Pr H H F OH H H XI-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr H H F OH H H XI-28-5 p-Cl-Ph H H CH2Ph 'Pr H H F OH H H XI-28-6 p-Cl-Ph H H CHrindol-3-yl 'Pr H H F OH H H XI-28-7 p-Cl-Ph H H CH2CH2SCH3 'Pr H H F OH H H XI-28-8 p-Cl-Ph * H * 'Pr H H F OH H H *R2 and R3t> joined together by (CH2)3 to form five-membered ring. 5 Table XI-29. 1 I «I- - .1 ii n -

Xa R1 R2 R5· R3b R4 R5 R6 X Y R7 R“ XI-29-1 p-Br-Ph H H H “W H H F OH H H XI-29-2 p-Br-Ph H H CH3 'Pr H H F OH H H XI-29-3 p-Br-Ph H H CH(CH3)2 'Pr H H F OH H H XI-29-4 p-Br-Ph H H ΟΗ2ΟΗ(ΟΗ3)2 'Pr H H F OH H H XI-29-5 p-Br-Ph H H CH2Ph 'Pr H H F OH H H XI-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr H H F OH H H XI-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr H H F OH H H XI-29-8 "VT72-T p-Br-Ph ♦ H ♦ 'Pr H H F OH H H *R2 and RJb joined together by (CHsh to form five-membered ring. 2983472-1 -289- WO 2008/121634

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Table XI-30.

Ns “R1- "r35" R3b ίτ Rs R6 X Y R7 Ra ΧΪ-30-1 p-I-Ph H H H Jpr H H F OH H H XI-30-2 p-I-Ph H H ch3 'Pr H H F OH H H XI-30-3 p-I-Ph H H CH(CH3)2 'Pr H H F OH H H XI-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr H H F OH H H XI-30-5 p-I-Ph H H CH2Ph 'Pr H H F OH H H Xl-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr H H F OH H H XI-30-7 p-I-Ph H H CH2CH2SCH3 'Pr H H F OH H H XI-30-8 p-I-Ph * H * 'Pr H H F OH H H *R2 and RJb joined together by (CHzb to form five-membered ring.

Table XI-31.

Ns R R2 r3. R3b R4 R5 R6 X Y P7 R" XI-31-1 ch3 H H H "Bu H H F OH H H XI-31-2 ch3 H H CH3 "Bu H H F OH H H XI-31-3 ch3 H H CH(CH3)2 "Bu H H F OH H H XI-31-4 ch3 H H CH2CH(CH3)2 "Bu H H F OH H H XI-31-5 ch3 H H CH2Ph "Bu H H F OH H H XI-31-6 ch3 H H CH2-indol-3-yl "Bu H H F OH H H XI-31-7 ch3 H H CH2CH2SCH3 "Bu H H F OH H H XI-31-8 ch3 ♦ H * "Bu H H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Ns R1 "r35" "r35 R4 R3 R* X Y r’ R8 XI-32-1 Et H H H "Bu H H F OH H H XI-32-2 Et H H CH3 "Bu H H F OH H H XI-32-3 Et H H CH(CH3)2 "Bu H H F OH H H XI-32-4 Et H H CH2CH(CH3)2 "Bu H H F OH H H XI-32-5 Et H H CH2Ph "Bu H H F OH H H XI-32-6 Et H H CHa-indol-3-yl "Bu H H F OH H H XI-32-7 Et H H CH2CH2SCH3 "Bu H H F OH H H XI-32-8 ~*τλ2 Et * H ♦ "Bu H H F OH H H *R2 and Rib joined together by (CH2)3 to form five-membered ring. 2983472-1 -290- WO 2008/121634 PCT/US2008/058183

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Table XI-33.

Xs Rl "F R3“ R3t> R* Rs R6 X Y 1? I? XI-33-1 ‘Pr H H H "Bu H H F OH H H XI-33-2 'Pr H H ch3 "Bu H H F OH H H XI-33-3 ‘Pr H H CH(CH3)2 "Bu H H F OH H H XI-33-4 /pr H H CH2CH(CH3)2 "Bu H H F OH H H XI-33-5 'Pr H H CH2Ph "Bu H H F OH H H XI-33-6 fpr H H CH2-indol-3-yl "Bu H H F OH H H XI-33-7 fpr H H CH2CH2SCH3 "Bu H H F OH H H XI-33-8 'Pr 4 H * "Bu H H F OH H H *R2 and Rejoined together by (CFhb to form five-membered ring.

Table XI-34.

Xs R R2 RJ* RJb κ Rs R6 X Y R' R“ XI-34-1 'Bu H H H "Bu H H F OH H H XI-34-2 'Bu H H CH3 "Bu H H F OH H H ΧΪ-34-3 'Bu H H CH(CH3)2 "Bu H H F OH H H XI-34-4 'Bu H H CH2CH(CH3)2 "Bu H H F OH H H XI-34-5 'Bu H H CH2Ph "Bu H H F OH H H XI-34-6 'Bu H H CH2-indol-3-yl "Bu H H F OH H H XI-34-7 'Bu H H CH2CH2SCH3 "Bu H H F OH H H XI-34-8 'Bu * H 4 "Bu H H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XI-35. -- a 4 * " RL J ' “L 2 W ' U "

Xa R R2 RJa R3b R^ ΊΓ R6 X Y R7 R“ XI-35-1 Ph H H H "Bu H H F OH H H XI-35-2 Ph H H CH3 "Bu H H F OH H H XI-35-3 Ph H H CH(CH3)2 "Bu H H F OH H H XI-35-4 Ph H H CH2CH(CH3)2 "Bu H H F OH H H XI-35-5 Ph H H CH2Ph "Bu H H F OH H H XI-35-6 Ph H H CH2-indol-3-yl "Bu H H F OH H H XI-35-7 Ph H H CH2CH2SCH3 "Bu H H F OH H H XI-35-8 *n'2 . Ph n3b * H * "Bu H H F OH H H ♦R2 and joined together by (CH2)3 to form five-membered ring. 2983472-1 -291- WO 2008/121634 PCT/US2008/058183

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Table XI-36.

x° R1 "R2” Ra“ - R4 R6 X Y R7 r“ XI-36-1 p-Me-Ph H H H "Bu H H F OH H H XI-36-2 p-Me-Ph H H ch3 "Bu H H F OH H H XI-36-3 p-Me-Ph H H CH(CH3)2 "Bu H H F OH H H XI-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu H H F OH H H XI-36-5 p-Me-Ph H H CH2Ph "Bu H H F OH H H XI-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu H H F OH H H XI-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu H H F OH H H XI-36-8 p-Me-Ph * H ♦ "Bu H H F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XI-37.

R1 F R3. R3b R4^ Rs R6 X Y R' R8 XI-37-1 p-F-Ph H H H "Bu H H F OH H H ΧΪ-37-2 p-F-Ph H H ch3 "Bu H H F OH H H XI-37-3 p-F-Ph H H ΟΗ(ΟΗ3)2 "Bu H H F OH H H XI-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu H H F OH H H XI-37-5 p-F-Ph H H CH2Ph "Bu H H F OH H H XI-37-6 p-F-Ph H H CH2-indol-3-yl "Bu H H F OH H H XI-37-7 p-F-Ph H H ch2ch2sch3 "Bu H H F OH H H XI-37-8 p-F-Ph * H * "Bu H H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XI-38.

- .......I "W H- ' J B R _ II

Xs R‘ R7 R3a R3b R4 R5 R$ X Y R7 R8 XI-38-1 p-Cl-Ph H H H "Bu H H F OH H H XI-38-2 p-Cl-Ph H H CH3 "Bu H H F OH H H XI-38-3 p-Cl-Ph H H CH(CH3)2 "Bu H H F OH H H XI-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H H F OH H H XI-38-5 p-Cl-Ph H H CH2Ph "Bu H H F OH H H XI-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu H H F OH H H XI-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu H H F OH H H XI-38-8 p-CI-Ph i l J * H * "Bu H H F OH H H ♦R2 and R3b joined together by (CHabt0 form five-membered ring. 2983472-1 -292- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XI-39.

Ns R1 R2 r3. "R35 R5 R0 X Y Ί?" XI-39-1 p-Br-Ph H Η’ H "Bu H H F OH H H XI-39-2 p-Br-Ph H H ch3 "Bu H H F OH H H XI-39-3 p-Br-Ph H H CH(CH3)2 "Bu H H F OH H H XI-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu H H F OH H H XI-39-5 p-Br-Ph H H CH2Ph "Bu H H F OH H H XI-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu H H F OH H H XI-39-7 p-Br-Ph H H CH2CH2SCH3 "Bu H H F OH H H XI-39-8 p-Br-Ph * H * "Bu H H F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring

Table Xl-40.

Ns Rr" R2 R3” R3b R4 R’ R* X Y R7 R“ XI-40-1 p-I-Ph H H H "Bu H H F OH H H Xl-40-2 p-I-Ph H H ch3 "Bu H H F OH H H XI-40-3 p-I-Ph H H CH(CH3)2 "Bu H H F OH H H XI-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu H H F OH H H XI-40-5 p-I-Ph H H CH2Ph "Bu H H F OH H H XI-40-6 p-I-Ph H H CH2-indol-3-yl "Bu H H F OH H H XI-40-7 p-I-Ph H H ch2ch2sch3 "Bu H H F OH H H XI-40-8 p-I-Ph 4 H ♦ "Bu H H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XI-41.

—- ·ι — " J g— J '".7··“·" . 'W _ B

Ns R R2 r3« r30 R4 R3 R6 X Υ R7 R8 XI-41-1 ch3 Η Η Η Bz Η Η F ΟΗ Η Η XI-41-2 ch3 Η Η ch3 Bz Η Η F ΟΗ Η Η XI-41-3 ch3 Η Η CHCCH,), Bz Η Η F ΟΗ Η Η XI-41-4 ch3 Η Η CH2CH(CH3)2 Bz Η Η F ΟΗ Η Η XI-41-5 ch3 Η Η CH2Ph Bz Η Η F ΟΗ Η Η XI-41-6 ch3 Η Η CH2-indol-3-yl Bz Η Η F ΟΗ Η Η XI-41-7 ch3 Η Η ch2ch2sch3 Bz Η Η F ΟΗ Η Η XI-41-8 ch3 nib ! * Η * Bz Η Η F ΟΗ Η Η *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -293- WO 2008/121634

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Table XI-42.

N° R1 R2 R3" R3b F RJ R6 X Y R7 r" XI-42-1 Et H H H Bz H H F OH H H XI-42-2 Et H H ch3 Bz H H F OH H H XI-42-3 Et H H CH(CH3)2 Bz H H F OH H H XI-42-4 Et H H CH2CH(CH3)2 Bz H H F OH H H XI-42-5 Et H H CH2Ph Bz H H F OH H H XI-42-6 Et H H CH2-indol-3-yl Bz H H F OH H H XI-42-7 Et H H CH2CH2SCH3 Bz H H F OH H H XI-42-8 ... j Et * H ♦ Bz H H F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XI-43.

Ns R1 R5 R3a ~R* R4 Rs R6 X Y ΊΓ Ic XI-43-1 'Pr H H H Bz H H F OH H H XI-43-2 'Pr H H CH3 Bz H H F OH H ή XI-43-3 'Pr H H CH(CH3)2 Bz H H F OH H H XI-43-4 'Pr H H CH2CH(CH3)2 Bz H H F OH H H XI-43-5 'Pr H H CH2Ph Bz H H F OH H H XI-43-6 ipr H H CH2-indol-3-yl Bz H H F OH H H XI-43-7 /Pr H H CH2CH2SCH3 Bz H H F OH H H XI-43-8 'Pr * H * Bz H H F OH H H 10 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XI-44.

X° r’ Ra R3* F- Iv RJ IF X Y r7" r“ XI-44-1 'Bu H H H Bz H H F OH H H XI-44-2 'Bu H H CH3 Bz H H F OH H H XI-44-3 "Bu H H CHiCHs), Bz H H F OH H H XI-44-4 'Bu H H CH2CH(CH3)2 Bz H H F OH H H XI-44-5 'Bu H H CH2Ph Bz H H F OH H H XI-44-6 'Bu H H CHrindol-3-yl Bz H H F OH H H XI-44-7 ^U H H CH2CH2SCH3 Bz H H F OH H H XI-44-8 *n2 . Έυ A3b · * H * Bz H H F OH H H *R2 and R3t) joined together by (CH2)3 to form five-membered ring. 2983472-1 -294- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XI-45.

Xs R1 R2 R3fl r35 R4 R6 X Y R7 XI-45-1 Ph H H H Bz H H F OH H H XI-45-2 Ph H H ch3 Bz H H F OH H H XI-45-3 Ph H H CH(CH3)2 Bz H H F OH H H XI-45-4 Ph H H CH2CH(CH3)2 Bz H H F OH H H XI-45-5 Ph H H CH2Ph Bz H H F OH H H XI-45-6 Ph H H CH2-indol-3-yl Bz H H F OH H H XI-45-7 Ph H H CH2CH2SCH3 Bz H H F OH H H XI-45-8 ... . Ph r.3b · * H * Bz H H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XI-46.

Xs R1 "R2" r3. -jpB R4 Rs R&amp; X Y R7 R’ XI-46-1 p-Me-Ph H H H Bz H H F OH H H XI-46-2 p-Me-Ph H H CH3 Bz H H F OH H H XI-46-3 p-Me-Ph H H CH(CH3)2 Bz H H F OH H H XI-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz H H F OH H H XI-46-5 p-Me-Ph H H CH2Ph Bz H H F OH H H XI-46-6 p-Me-Ph H H CH2-indol-3-yl Bz H H F OH H H XI-46-7 p-Me-Ph H H CH2CH2SCH3 Bz H H F OH H H XI-46-8 p-Me-Ph * H * Bz H H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XI-47. I W H- ""HL 1 *'"· - J I i W '"d-’

Xs R* R2 R“ R3b R^ RJ R6 X Y R7 R" XI-47-1 p-F-Ph H H H Bz H H F OH H H XI-47-2 p-F-Ph H H CH3 Bz H H F OH H H XI-47-3 p-F-Ph H H CHCCH^ Bz H H F OH H H XI-47-4 p-F-Ph H H CH2CH(CH3>2 Bz H H F OH H H XI-47-5 p-F-Ph H H CH2Ph Bz H H F OH H H XI-47-6 p-F-Ph H H CH2-indol-3-yl Bz H H F OH H H XI-47-7 p-F-Ph H H CH2CH2SCH3 Bz H H F OH H H XI-47-8 p-F-Ph * H * Bz H H F OH H H *R2 and RJb joined together by (0¾)^ to form five-membered ring. 2983472-1 -295- WO 2008/121634 PCT/US2008/058183

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Table XI-48.

Xs r1 ΊΡ" “R35 Rs R0 X Y R XI-48-1 p-Cl-Ph H H H Bz H H F OH H H XI-48-2 p-Cl-Ph H H ch3 Bz H H F OH H H XI-48-3 p-Cl-Ph H H CH(CH3)2 Bz H H F OH H H XI-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H H F OH H H XI-48-5 p-Cl-Ph H H CH2Ph Bz H H F OH H H XI-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz H H F OH H H XI-48-7 p-Cl-Ph H H CH2CH2SCH3 Bz H H F OH H H XI-48-8 p-Cl-Ph ♦ H * Bz H H F OH H H *R^ and Rejoined together by (CEbb to form five-membered ring.

Table XI-49.

X° R1 R2 r3B R3b R* R3 R6 X Y R7 R8 XI-49-1 p-Br-Ph H H H Bz H H F OH H H XI-49-2 p-Br-Ph H H ch3 Bz H H F OH H H XI-49-3 p-Br-Ph H H ORCHjX Bz H H F OH H H XI-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz H H F OH H H XI-49-5 p-Br-Ph H H CH2Ph Bz H H F OH H H XI-49-6 p-Br-Ph H H CH2-indol-3-yl Bz H H F OH H H XI-49-7 p-Br-Ph H H CH2CH2SCH3 Bz H H F OH H H XI-49-8 p-Br-Ph ♦ H * Bz H H F OH H H ♦R* and R30 joined together by (CH2)3 to form five-membered ring. 5 Table XI-50. 1 —1 * .. ·ι·ί' I — ..... , -

Xa R1 R2 R3a R3b R^ R5 R6 X Y R7 R8 XI-50-1 p-I-Ph H H H Bz H H F OH H H XI-50-2 p-I-Ph H H ch3 Bz H H F OH H H XI-50-3 p-I-Ph H H CHiCH^ Bz H H F OH H H XI-50-4 p-I-Ph H H CH2CH(CH3)2 Bz H H F OH H H XI-50-5 p-I-Ph H H CH2Ph Bz H H F OH H H XI-50-6 p-I-Ph H H CH2-indol-3-yl Bz H H F OH H H XI-50-7 p-I-Ph H H CH2CH2SCH3 Bz H H F OH H H XI-50-8 l p-I-Ph ; - ♦ H * Bz H H F OH H H *R2 and RJt) joined together by (CH2)3 to form five-membered ring. 2983472-1 -296- WO 2008/121634 PCT/US2008/058183

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ΧΠ

Table XII-1.

Xs Rl R2 TP5" R3b R4 R5 R4 X Y r Rs XH-1-1 ch3 H H H ch3 n3 F F OH H H ΧΠ-1-2 ch3 H H ch3 ch3 n3 F F OH H H XII-1-3 ch3 H H CH(CH3)2 ch3 n3 F F OH H H XII-1-4 ch3 H H CH2CH(CH3)z ch3 n3 F F OH H H XII-1-5 ch3 H H CH2Ph ch3 n3 F F OH H H XI I-1-6 ch3 H H CHrindol-3-yl ch3 n3 F F OH H H ΧΠ-1-7 ch3 H H ch2ch2sch3 ch3 n3 F F OH H H XI1-1-8 ch3 ♦ H * ch3 n3 F F OH H H *R2 and RJb joined together by (ΟΗί)3 to form five-membered ring.

Xs "R1" R2 R3· ΊΡ5 R4 R5 R4 X Y r" r“ ΧΠ-2-1 Et H H H CH3 n3 F F OH H H XII-2-2 Et H H CH3 ch3 n3 F F OH H H XII-2-3 Et H H CH(CH3)2 ch3 n3 F F OH H H XII-2-4 Et H H CH2CH(CH3)2 ch3 n3 F F OH H H XII-2-5 Et H H CH2Ph ch3 n3 F F OH H H XII-2-6 Et H H CH2-indol-3-yl ch3 n3 F F OH H H XII-2-7 Et H H CH2CH2SCH3 ch3 n3 F F OH H H XII-2-8 Et T.Jb * H ♦ ch3 n3 F F OH H H ♦R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -297- WO 2008/121634 PCT/US2008/058183

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Table ΧΠ-3.

N° R1 r2 Ί<3β R4 -R5" R6 X Y R7 r8” XH-3-1 'Pr H H H ch3 n3 F F OH H H ΧΙΪ-3-2 'Pr H H ch3 ch3 n3 F F OH H H XII-3-3 'Pr H H CH(CH3)2 ch3 n3 F F OH H H XII-3-4 'Pr H H CHzCH(CH3)2 ch3 n3 F F OH H H XII-3-5 'Pr H H CH2Ph ch3 n3 F F OH H H ΧΠ-3-6 ‘Pr H H CH2-indol-3-yl ch3 n3 F F OH H H XII-3-7 'Pr H H CH2CH2SCH3 ch3 n3 F F OH H H ΧΠ-3-8 'Pr ♦ H * ch3 n3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XII-4.

Ns R1 R3 R3a r38 R4 rs R6 X Y R’ r“ ΧΠ-4-1 'Bu H H H ch3 n3 F F OH H H XH-4-2 'Bu H H ch3 ch3 n3 F F OH H H XIM-3 'Bu H H CH(CH3)2 ch3 n3 F F OH H H XI1-4-4 'Bu H H CH2CH(CH3)2 ch3 n3 F F OH H H XII-4-5 'Bu H H CHaPh ch3 n3 F F OH H H XH-4-6 'Bu H H CH2-indol-3-yl ch3 n3 F F OH H H XII-4-7 'Bu H H ch2ch2sch3 ch3 n3 F F OH H H XII-4-8 '*^2 '7 'Bu r,3b·. ♦ H * ch3 n3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Ns R1 R1 R3a "r36 R4 r! Rfi X Y r’ R8 XH-5-1 Ph H H H CH3 n3 F F OH H H ΧΠ-5-2 Ph H H ch3 ch3 n3 F F OH H H ΧΠ-5-3 Ph H H CH(CH3)2 ch3 n3 F F OH H H XII-5-4 Ph H H CH2CH(CH3)2 ch3 n3 F F OH H H XII-5-5 Ph H H CH2Ph ch3 n3 F F OH H Η ΧΠ-5-6 Ph H H CHrindol-3-yl ch3 n3 F F OH H H XII-5-7 Ph H H CH2CH2SCH3 ch3 n3 F F OH H Η XII-5-8 Ph ♦ H ♦ ch3 n3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -298- WO 2008/121634 PCT/US2008/058183

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Table XI1-6.

Ns -R1 IF F” R3b R4 R5 "F X Y R7 R8 XII-6-1 p-Me-Ph H H H ch3 n3 F F OH H H XII-6-2 p-Me-Ph H H ch3 ch3 n3 F F OH H H XI1-6-3 p-Me-Ph H H CH(CH3)2 ch3 n3 F F OH H H XU-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 n3 F F OH H H ΧΠ-6-5 p-Me-Ph H H CH2Ph ch3 n3 F F OH H H XH-6-6 p-Me-Ph H H CH2-indoi-3-yl ch3 n3 F F OH H H XII-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 n3 F F OH H H XII-6-8 p-Me-Ph * H * ch3 n3 F F OH H H *R2 and RJb joined together by (CHib to form five-membered ring.

Table X1I-7.

Xa Rl R^ “r31" R4 Ίν R6 X Y R7 Ic XII-7-1 p-F-Ph H H H CH3 n3 F F OH H H XU-7-2 p-F-Ph H H CH3 ch3 n3 F F OH H H XII-7-3 p-F-Ph H H CHiCHa), ch3 n3 F F OH H H ΧΪΙ-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 n3 F F OH H H XII-7-6 p-F-Ph H H CH2Ph ch3 n3 F F OH H H XII-7-7 p-F-Ph H H CH2-indol-3-yl ch3 n3 F F OH H H XII-7-8 p-F-Ph H H CH2CH2SCH3 ch3 n3 F F OH H H XII-7-20 p-F-Ph * H * ch3 n3 F F OH H H *R2 and Rejoined together by (CHak to form five-membered ring. 5 Table XII-8. i1-· 1 n 'j' _ i g - _ _ - R 'ra*"

Xa R1 R1 R3e R3b R4 RJ R6 X Y R7 R8 XII-8-1 p-Cl-Ph H H H ch3 n3 F F OH H H XII-8-2 p-Cl-Ph H H ch3 ch3 n3 F F OH H H XII-8-3 p-CI-Ph H H CH(CH3)2 ch3 n3 F F OH H H XII-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 n3 F F OH H H XII-8-5 p-Cl-Ph H H CH2Ph ch3 n3 F F OH H H XII-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 n3 F F OH H H XU-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 n3 F F OH H H XU-8-8 p-Cl-Ph r,3b’“ · J * H * ch3 n3 F F OH H H *R2 and RJb joined together by (CHah to form five-membered ring. 2983472-1 -299- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XII-9.

Ns R1 R2 Rjr "R35 R5 IT X Y R7 Rtt XII-9-1 p-Br-Ph H H H ch3 n3 F F OH H H XII-9-2 p-Br-Ph H H ch3 ch3 n3 F F OH H H XI1-9-3 p-Br-Ph H H CH(CH3)2 ch3 n3 F F OH H H X1I-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 n3 F F OH H H XII-9-6 p-Br-Ph H H CH2Ph ch3 n3 F F OH H H ΧΠ-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 n3 F F OH H H XII-9-8 p-Br-Ph H H CH2CH2SCH3 ch3 n3 F F OH H H XII-9-20 -77 p-Br-Ph —r; ♦ H * ch3 n3 F F OH II H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XII-10.

Ns R1 R1 R3‘ R3b R1- R5 R6 X Y R7" R11 XH-10-1 p-I-Ph Η Η Η CH3 n3 F F OH H H XH-10-2 p-I-Ph Η Η ch3 ch3 n3 f F OH H H XII-10-3 p-I-Ph Η Η CH(CH3)2 ch3 n3 f F OH H H XII-10-4 p-I-Ph Η Η CH2CH(CH3)2 ch3 n3 f F OH H H XU-10-5 p-I-Ph Η Η CH2Ph ch3 n3 f F OH H H XII-10-6 p-I-Ph Η Η CH2-indol-3-yl ch3 n3 f F OH H H XII-10-7 p-I-Ph Η Η CH2CH2SCH3 ch3 n3 f F OH H H XU-10-8 p-I-Ph ♦ Η * ch3 n3 f F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. Table XII-11. Ns R’ R3 ' R3a R35 R* Rs R6 X Y R7 R8 ΧΙΙ-Π-1 ch3 h Η H Et n3 F f OH H H ΧΠ-11-2 ch3 h Η ch3 Et n3 F F OH H H ΧΠ-11-3 ch3 h Η ΟΗ(ΟΗ3)2 Et n3 F F OH H H XII-11-4 ch3 h Η CH2CH(CH3)2 Et n3 F F OH H H XII-11-5 ch3 h Η CH2Ph Et n3 F F OH H H XII-11-6 ch3 h Η CH2-indol-3-yl Et n3 F F OH H H ΧΠ-11-7 ch3 h Η CH2CH2SCH3 Et n3 F F OH H H XII-11-8 “T77Z-77 ch3 * —3 Η * Et n3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -300- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Table XII-12. X° Rl R3 "r37 R3b R5 R6 X Y r’ R* XII-12-1 Et H H H Et n3 F F OH H H XH-12-2 Et H H ch3 Et n3 F F OH H H XII-12-3 Et H H CHfCHj), Et n3 F F OH H H XII-12-4 Et H H CH2CH(CH3)2 Et n3 F F OH H H XII-12-5 Et H H CH2Ph Et n3 F F OH H H XII-12-6 Et H H CH2-indol-3-yl Et n3 F F OH H H ΧΠ-12-7 Et H H CH2CH2SCH3 Et n3 F F OH H H ΧΠ-12-8 Et * H 4 Et n3 F F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XI1-13.

Jfe R1 R2 R3' 1 RJb R4 R5 R6 X Y R R“ XII-13-1 'Pr H H H Et n3 F F OH H H XII-13-2 'Pr H H CH3 Et n3 F F OH H H XII-13-3 'Pr H H CH(CH3)2 Et n3 F F OH H H ΧΠ-13-4 'Pr H H CH2CH(CH3)2 Et n3 F F OH H H XII-13-5 'Pr H H CH2Ph Et n3 F F OH H H XII-13-6 'Pr H H CH2-indol-3-yl Et n3 F F OH H H XH-13-7 'Pr H H CH2CH2SCH3 Et n3 F F OH H H ΧΠ-13-8 'Pr ♦ H 4 Et n3 F F OH H H *R3 and RJb joined together by (CH2)3 to form five-membered ring. Table XII-14. Xs R1 R3 R 3a "r35 R4 r! R6 X Y R^ R8 XII- *Bu H H H Et N F F OH Η H 14-1 3 XII- 'Bu H H CH3 Et N F F OH Η H 14-2 3 XII- *Bu H H CH(CH3)2 Et N F F OH Η H 14-3 3 XII- *Bu H H CH2CH(CH3)2 Et N F F OH Η H 14-4 3 XH- 'Bu H H CH2Ph Et N F F OH Η H 14-5 3 2983472-) -301 - PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Na R1 R5 R 3a “r3* Rs R6 X Y R7 r“ XH- “1Bu“ H H CH2-indol-3-yl Et N F F OH H H 14-6 3 XII- 'Bu H H ch2ch2sch3 Et N F F OH H H 14-7 3 XII- 'Bu * H * Et N F F OH H H 14-8 .. j nJb ; 3 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XII-15.

Na R1 r1" RJ R6 X Y R r“ XII-15-1 Ph H H H Et n3 F F OH H H XI I-15-2 Ph H H ch3 Et n3 F F OH H H XII-15-3 Ph H H CH(CH3)3 Et n3 F F OH H H XII-15-4 Ph H H CH2CH(CH3)2 Et n3 F F OH H H XII-15-5 Ph H H CH2Ph Et n3 F F OH H H XII-15-6 Ph H H CH2-indol-3-yl Et n3 F F OH H H XII-15-7 Ph H H CH2CH2SCH3 Et n3 F F OH H H XII-15-8 *n2 it Ph 731ΓΓ" ♦ H * Et N3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XII-16.

Ns R1 "r3- "r33” R3b R4 RJ R* X Y R7 r“ XII-16-1 p-Me-Ph H H H Et n3 F F OH H H XII-16-2 p-Me-Ph H H ch3 Et n3 F F OH H H XII-16-3 p-Me-Ph H H CHCCHah Et n3 F F OH H H XII-16-4 p-Me-Ph H H CH2CH(CH3)2 Et n3 F F OH H H XII-16-5 p-Me-Ph H H CH2Ph Et n3 F F OH H H XII-16-6 p-Me-Ph H H CH2-indol-3-yt Et n3 F F OH H H XII-I6-7 p-Me-Ph H H CH2CH2SCH3 Et n3 F F OH H H ΧΠ-16-8 p-Me-Ph * H * Et n3 F F OH H H 5 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

TableXII-17.

Ns R R2 R3· R3b R4 Rs Rb X Y R7 R8 XII-17-1 p-F-Ph H H H Et n3 F F OH H H XII-17-2 p-F-Ph H H ch3 Et n3 F F OH H H 2983472-1 -302- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/O58183

He “r1 "R7" "r'7' R3b ΊΓ R6 X Y R7 R8 ΧΠ-17-3 p-F-Ph H H CH(CH3)2 Et n3 F F OH H H XII-17-4 p-F-Ph H H CH2CH(CH3)2 Et n3 F F OH H H ΧΠ-17-5 p-F-Ph H H CHjPh Et n3 F F OH H H XH-17-6 p-F-Ph H H CH2-indol-3-yl Et n3 F F OH H H XII-17-7 p-F-Ph H H CH2CH2SCH3 Et n3 F F OH H H XH-17-8 j r p-F-Ph Jb· : j * H * Et n3 F F OH H H *R2 and Rejoined together by (0¾¼ to form five-membered ring?

Table XII-18.

Ns R‘ R2 r3« “R35 R4 Rs R6 X Y R7 R11 XII-18-1 p-Cl-Ph H H H Et n3 F F OH H H ΧΠ-18-2 p-Cl-Ph H H CH3 Et n3 F F OH H H XII-18-3 p-Cl-Ph H H CH(CH^ Et n3 F F OH H H XII-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et n3 F F OH H H ΧΙΪ-18-5 p-CI-Ph H H CH2Ph Et n3 F F OH H H XII-18-6 p-Cl-Ph H H CH2-indol-3-yl Et n3 F F OH H H ΧΠ-18-7 p-Cl-Ph H. H CH2CH2SCH3 Et n3 F F OH H H ΧΠ-18-8 ~ p-CI-Ph ,3b : ·—T. * H * Et n3 F F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table ΧΠ-19.

Ns R1 R2 Rja "R35 R4 R3 R6 X Y "r7" Jr ΧΠ-19-1 p-Br-Ph H H H Et n3 F F OH H H XH-19-2 p-Br-Ph H H CH3 Et n3 F F OH H H XII-19-3 p-Br-Ph H H CHCCHjh Et n3 F F OH H H XII-19-4 p-Br-Ph H H CH2CH(CH3)2 Et n3 F F OH H H X1I-19-5 p-Br-Ph H H CH2Ph Et n3 F F OH H H XII-19-6 p-Br-Ph H H CH2-indol-3-yl Et n3 F F OH H H XII-19-7 p-Br-Ph H H CH2CH2SCH3 Et n3, F F OH H H XII-19-8 _ j t p-Br-Ph ,3b: : -J , * H * Et n3 F F OH H H ♦R2 and Rejoined together by (0¾¼ to form five-membered ring?

Table XII-20.

Ns “R1- r2 “r31- - r4 Rs r6 X Y R’ XH-20-1 p-I-Ph H H H Et n3 F F OH H XII-20-2 p-I-Ph H H ch3 Et n3 F F OH H ΧΠ-20-3 p-I-Ph H H CH(CH3)2 Et n3 F F OH H 2983472-1 -303- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Xa 1· R2 R3a R3b ΊΓ ΊΓ R4 X Y R7 Χ1Ϊ-20-4 p-I-Ph H H CH2CH(CH3)2 Et n3 F F OH H ΧΠ-20-5 p-I-Ph H H CH2Ph Et n3 F F OH H ΧΠ-20-6 p-I-Ph H H CH2-indol-3-yl Et n3 F F OH H XII-20-7 p-I-Ph H H CH2CH2SCH3 Et n3 F F OH H ΧΠ-20-8 p-I-Ph Π5Τ7—' * H * Et __Λ n3 F F OH H *R2 and RJb joined together by (0¾^ to form five-membered ring.

Table XII-21.

X° R1 R2 R4 Rs R4 X Y r’ r“ XH-21-1 CH3 H H H 'T’r" n3 F F OH H H XII-21-2 ch3 H H ch3 'Pr n3 F F OH H H XH-21-3 ch3 H H CH(CH3)2 Tr n3 F F OH H H XII-21-4 ch3 H H CH2CH(CH3)2 'Pr n3 F F OH H H ΧΠ-21-5 ch3 H H CH2Ph 'Pr n3 F F OH H H XII-21-6 ch3 H H CH2-indol-3-yl 'Pr n3 F F OH H H XII-21-7 ch3 H H CH2CH2SCH3 'Pr n3 F F OH H H XII-21-8 ch3 ♦ H * 'Pr n3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XII-22.

Xa “F" R2 r3. R3b R4 RJ R4 X Y R7 R“ XII-22-1 Et H H H 'Pr n3 F F OH H H XII-22-2 Et H H CH3 'Pr n3 F F OH H H XII-22-3 Et H H CH(CH3)2 'Pr n3 F F OH H H XII-22-4 Et H H CH2CH(CH3)2 'Pr n3 F F OH H H XII-22-5 Et H H CH2Ph 'Pr n3 F F OH H H ΧΠ-22-6 Et H H CH2-indol-3-yl 'Pr n3 F F OH H H XH-22-7 Et H H CH2CH2SCH3 'Pr n3 F F OH H H ΧΠ-22-8 -77 Et * H * 'Pr n3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XU-23.

Xs “F" R2 R35 R4 R* R4 X Y R7 R" XII-23-1 'Pr H H H "Ψϊ7 n3 F F OH H H XII-23-2 'Pr H H ch3 ^r n3 F F OH H H ΧΠ-23-3 'Pr H H CH(CH3)j 'Pr n3 F F OH H H XII-23-4 'Pr H H CH2CH(CH3)2 'Pr n3 F F OH H H 2983472-1 -304- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Ns R1 r3b ΊΡ5 fT R6 X Y ΊΓ R’ XII-23-5 'Pr H H CH2Ph "W n3 F F OH H H ΧΠ-23-6 'Pr H H CH2-indol-3-yl 'Pr n3 F F OH H H ΧΠ-23-7 'Pr H H CH2CH2SCH3 'Pr n3 F F ΌΗ H H ΧΠ-23-8 ''Τ'; 'Pr * H * 'Pr n3 F F OH H H *R2 and joined together by (CH2)3 to form five-membered ring.

Table ΧΠ-24.

Ns R1 R3 R3a r*- R4 r7- r6 X Y R’ R8 XII-24-1 'Bu H H H 'Pr n3 F F OH H H XII-24-2 'Bu H H CH3 'Pr n3 F F OH H H ΧΠ-24-3 'Bu H H CH(CH3)2 'Pr n3 F F OH H H ΧΠ-24-4 'Bu H H CH2CH(CH3)2 'Pr n3 F F OH H H XII-24-5 'Bu H H CH2Ph 'Pr n3 F F OH H H XII-24-6 H H CH2-indol-3-yl 'Pr n3 F F OH H H XI1-24-7 'Bu H H CH2CH2SCH3 'Pr n3 F F OH H H XII-24-8 'Bu * H * 'Pr n3 F F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table ΧΠ-25.

Ns R R4 R3. RJb R4 Rs R6 X Y R' R8 XII-25-1 Ph H H H 'Pr n3 F F OH H H XII-25-2 Ph H H ch3 'Pr n3 F F OH H H XII-25-3 Ph H H CH(CH3)2 *Pr n3 F F OH H H XII-25-4 Ph H H CH2CH(CH3)2 'Pr n3 F F OH H H ΧΠ-25-5 Ph H H CH2Ph 'Pr n3 F F OH H H ΧΠ-25-6 Ph H H CH2-indol-3-yl 'Pr n3 F F OH H H ΧΠ-25-7 Ph H H CH2CH2SCH3 'Pr n3 F F OH H H XU-25-8 Ph * H * 'Pr n3 F F OH H H 5 *R2 and RJb joined together by (CFhb to form five-membered ring.

Table X1I-26.

Ns Rl R2 r3« R3b R4 R5 R6 X Y r’ ΊΓ XII-26-1 p-Me-Ph H H H Τϋ" n3 F F OH H H XU-26-2 p-Me-Ph H H CH3 'Pr n3 F F OH H H XII-26-3 p-Me-Ph H H CH(CH3)2 'Pr n3 F F OH H H XU-26-4 p-Me-Ph H H CH2CH(CH3)2 'Pr n3 F F OH H H ΧΠ-26-5 p-Me-Ph H H CH2Ph 'Pr n3 F F OH H H 2983472-1 -305- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034 WOUI lib R1 R2 R3a R3b R4 RJ R6 X Y R? 1?

XII-26-6 p-Me-Ph Η H CHrindol-3-yl JPr N3 F F OH Η H

XII-26-7 p-Me-Ph Η H CH2CH2SCH3 'Pr N3 F F OH Η H

XII-26-8 p-Me-Ph * H * N3 F F OH Η H *R2 and RJb joined together by (CI-I2)3 to form five-membered ring.

Table XII-27.

Ns Rl R1 R3· "r36 R4 Rs R6 X Y IT IF XII-27-1 p-F-Ph H H H "ΨΓ n3 F F OH H H XII-27-2 p-F-Ph H H CH3 'Pr n3 F F OH H H ΧΠ-27-3 p-F-Ph H H CH(CH,)2 Tr n3 F F OH H H XII-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr n3 F F OH H H ΧΠ-27-5 p-F-Ph H H CH2Ph 'Pr n3 F F OH H H ΧΠ-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr n3 F F OH H H ΧΠ-27-7 p-F-Ph H H CH2CH2SCH3 'Pr n3 F F OH H H XII-27-8 p-F-Ph * H * 'Pr n3 F F OH H H *R2 and RJt> joined together by (CH2)3 to form five-membered ring.

Table XII-28.

Ns R1 ΊΓ R3a Rs r5" X Y IT Ra XH-28-1 p-Cl-Ph H H H 'Pr n3 F F OH H H XII-28-2 p-CI-Ph H H ch3 'Pr n3 F F OH H H ΧΠ-28-3 p-Cl-Ph H H CH(CH3)2 'Pr n3 F F OH H H ΧΠ-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr n3 F F OH H H XH-28-5 p-Cl-Ph H H CH2Ph 'Pr n3 F F OH H H XII-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr n3 F F OH H H XII-28-7 p-Cl-Ph H H CH2CH2SCH3 Tr n3 F F OH H H XII-28-8 p-Cl-Ph * H * 'Pr n3 F F OH H H 5 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XII-29.

Ns R1 ΪΓ -£3. R3b R4 r5" R6 X Y ΊΓ Ru XH-29-1 p-Br-Ph H H H "W n3 F F OH H H XH-29-2 p-Br-Ph H H ch3 'Pr n3 F F OH H H ΧΠ-29-3 p-Br-Ph H H CH(CH3)2 'Pr n3 F F OH H H XU-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr n3 F F OH H H XU-29-5 p-Br-Ph H H CH2Ph 'Pr n3 F F OH H H XH-29-6 p-Br-Ph H H CH2-indol-3-y] 'Pr n3 F F OH H H 2983472-1 -306- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOUi

Xa R1 r! R3a R3b R4 R* R6 X Y R7 R8 XII-29-7 p-Br-Ph H H ch2ch2sch3 'Pr n3 F F OH H H ΧΠ-29-8 p-Br-Ph i3b· : . * H ♦ 'Pr „ λ. ,, n3 F F OH H H *R^ and Rejoined together by (CH2)3 to form five-membered ring.

Table XII-30.

Xa Rl -gjr- T?* R4 RJ X Y R7 R8 Xll-30-1 p-I-Ph H H H "¥T n3 F F OH H H ΧΠ-30-2 p-I-Ph H H CH3 'Pr n3 F F OH H H ΧΠ-30-3 p-I-Ph H H CH(CHj)2 'Pr n3 F F OH H H XII-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr n3 F F OH H H ΧΠ-30-5 p-I-Ph H H CH2Ph 'Pr n3 F F OH H H ΧΠ-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr n3 F F OH H H XII-30-7 p-I-Ph H H CH2CH2SCH3 'Pr n3 F F OH H H XII-30-8 ο,τλ '2 J T p-I-Ph Jb· - * H * 'Pr n3 F F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XII-31.

Xa R* RJ "r35" R3b R4 R5 R6 X Y R8 XU-31-1 ch3 H H H "Bu n3 F F OH H H XII-31-2 CH3 H H ch3 "Bu n3 F F OH H H XII-31-3 ch3 H H CHCCH,), "Bu n3 F F OH H H XII-31-4 ch3 H H CH2CH(CH3)2 "Bu n3 F F OH H H XII-31-5 ch3 H H CH2Ph "Bu n3 F F OH H H XII-31-6 ch3 H H CH2-mdol-3-yl "Bu n3 F F OH H H XII-31-7 ch3 H H CH2CH2SCH3 "Bu n3 F F OH H H XU-31-8 *ηϊ j t ch3 »3b * H ♦ "Bu n3 F F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XII-32.

Xa R1 Ra Rja T8 r4 R! ΊΓ X Y R7 TT ΧΙΪ-32-1 Et H H H "Bu n3 F F OH H H XU-32-2 Et H H ch3 "Bu n3 F F OH H H XII-32-3 Et H H CHCCHj), "Bu n3 F F OH H H XII-32-4 Et H H CHzO-KCHah "Bu n3 F F OH H H XII-32-5 Et H H CH2Ph "Bu n3 F F OH H H XII-32-6 Et H H CH2-indol-3-yl "Bu n3 F F OH H H XII-32-7 Et H H CH2CH2SCH3 "Bu n3 F F OH H H 2983472-1 -307- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Xs R1 R2” R3a R3b R4 R4 R4 X Y R r“ XII-32-8 Et * H * "Bu n3 F F OH H H *RZ and R 3bjo ined toge ther by (CH2)3 to form five -membe red ring. Table ΧΠ -33. Xs R1 R2 R3a ΊΓε R4 R4 R4 X Y R; r“ XH-33-1 'Pr H H H "Bu n3 F F OH H H XII-33-2 'Pr H H ch3 "Bu n3 F F OH H H XII-33-3 'Pr H H CH(CH3)2 "Bu n3 F F OH H H XII-33-4 'Pr H H CH2CH(CH3)2 "Bu n3 F F OH H H ΧΠ-33-5 'Pr H H CH2Ph "Bu n3 F F OH H H ΧΠ-33-6 'Pr H H CH2-indol-3-yl "Bu n3 F F OH H H XII-33-7 'Pr H H ch2ch2sch3 "Bu n3 F F OH H H XII-33-8 *'n2 j"™ 'Pr * H * "Bu n3 F F OH H H *R2 and Rejoined together by (CHjfc to form five-membered ring.

Table ΧΠ-34.

Xa R1 TF r3. -p; R4 R4 R4 X Y ir R“ XII-34-1 'Bu H H H "Bu n3 F F OH H H ΧΠ-34-2 'Bu H H CH3 "Bu n3 F F OH H H XII-34-3 'Bu H H CH(CH3)2 "Bu n3 F F OH H H XH-34-4 'Bu H H CH2CH(CH3)2 "Bu n3 F F OH H H XH-34-5 'Bu H H CH2Ph "Bu n3 F F OH H H ΧΠ-34-6 'Bu H H CH2-indol-3-yl "Bu n3 F F OH H H ΧΠ-34-7 'Bu H H CH2CH2SCH3 "Bu n3 F F OH H H ΧΠ-34-8 'Bu ΓΠΓΓΤ· * H * "Bu n3 F F OH H H •R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XII-35.

Xa R1 R2 R4 FT R4 X Y R’ R“ XH-35-1 Ph H H H "Bu n3 F F OH H H ΧΠ-35-2 Ph H H ch3 "Bu n3 F F OH H H ΧΠ-35-3 Ph H H CHCCH^ "Bu n3 F F OH Η H XH-35-4 Ph H H CH2CH(CH3)2 "Bu n3 F F OH H H XII-35-5 Ph H H CH2Ph "Bu n3 F F OH H H ΧΠ-35-6 Ph H H CH2-indol-3-yl "Bu n3 F F OH H H ΧΠ-35-7 Ph H H CH2CH2SCH3 "Bu n3 F F OH H H XII-35-8 Ph ♦ H * "Bu n3 F F OH H H 2983472-1 -308- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XII-36.

Xs r! "R^ ηρΒ ΊΓ~ Rs R6 X Y R7 r“ XII-36-1 p-Me-Ph H H H "Bu n3 F F OH H H XII-36-2 p-Me-Ph H H ch3 "Bu n3 F F OH H H XII-36-3 p-Me-Ph H H CH(CH3)2 "Bu n3 F F OH H H ΧΠ-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu n3 F F OH H H XII-36-5 p-Me-Ph H H CH2Ph "Bu n3 F F OH H H XII-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu n3 F F OH H H XII-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu n3 F F OH H H XII-36-8 p-Me-Ph * H * "Bu n3 F F OH H H ♦Rz and R36 joined together by (CHj)3 to form five-membered ring.

Table ΧΠ-37.

Xs R1 R2 R~b R4 R5 R6 X Y R7 R8 XII-37-1 p-F-Ph H H H "Bu n3 F F OH H H ΧΠ-37-2 p-F-Ph H H CH3 "Bu n3 F F OH H H XII-37-3 p-F-Ph H H CHCCHah "Bu n3 F F OH H H XII-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu n3 F F OH H H ΧΠ-37-5 p-F-Ph H H CH2Ph "Bu n3 F F OH H H XII-37-6 p-F-Ph H H CH2-indol-3-yl "Bu n3 F F OH H H XH-37-7 p-F-Ph H H CH2CH2SCH3 "Bu n3 F F OH H H ΧΠ-37-8 p-F-Ph * H * "Bu n3 F F OH H H 5 *RZ and R3b joined together by (CH2)3 to form five-membered ring.

Table XII-38.

Xs R1 R2 R3. R3b R4 R6 X Y R7 r“ ΧΠ-38-1 p-Cl-Ph H H H "Bu n3 F F OH H H XII-38-2 p-Cl-Ph H H CH3 "Bu n3 F F OH H H XII-38-3 p-Cl-Ph H H CH(CH3)2 "Bu n3 F F OH H H ΧΠ-38-4 p-CI-Ph H H CHzCHCCHah "Bu n3 F F OH H H ΧΠ-38-5 p-Cl-Ph H H CH2Ph "Bu n3 F F OH H H XII-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu n3 F F OH H H XII-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu n3 F F OH H H XII-38-8 -.it p-Cl-Ph Π5ΤΊ-T. * H * "Bu n3 F F OH H H *RZ and R30 joined together by (CHjja to form five-membered ring. 2983472-1 -309- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XII-39.

Xa R1 R* R3* IF6 R4 R3 R4 X Y r’ r“ XII-39-1 p-Br-Ph H H H "Bu n3 F F OH H H XII-39-2 p-Br-Ph H H ch3 "Bu n3 F F OH H H XI1-39-3 p-Br-Ph H H CH(CH3)2 "Bu n3 F F OH H H XII-39-4 p-Br-Ph H H CHjCHiCH^ "Bu n3 F F OH H H XII-39-5 p-Br-Ph H H CHjPh "Bu n3 F F OH H H XII-39-6 p-Br-Ph H H CHj-indol-3-yl "Bu n3 F F OH H H XII-39-7 p-Br-Ph H H CHaCH2SCH3 "Bu n3 F F OH H H XII-39-8 ~-ΤΓ p-Br-Ph ,3b ί —T, * H * "Bu n3 F F OH H H *R2 and R3b joined together by (CFhb to form five-membered ring.

Table XII-40.

Xa R1 Ra R3' “R35 R4 r5- r4 X Y R7 R8 XH-40-1 p-I-Ph H H H "Bu n3 F F OH H H XII-40-2 p-I-Ph H H CH3 "Bu n3 F F OH H H ΧΠ-40-3 p-I-Ph H H CH(CH3)2 "Bu n3 F F OH H H ΧΠ-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu n3 F F OH H H XII-40-5 p-I-Ph H H CH2Ph "Bu n3 F F OH H H XH-40-6 p-I-Ph H H CH2-indol-3-yl "Bu n3 F F OH H H XII-40-7 p-I-Ph H H CH3CH2SCH3 "Bu n3 F F OH H H ΧΠ-40-8 p-I-Ph * H * "Bu n3 F F OH H H ♦R2 and RJt> joined together by (CH2)3 to form five-membered ring. 5 Table XII-41. ......... R WL1 J 1 '""IT" ':? ^"""1"

Xa R1 r2 R3' R3b R4 R5 R4 X Y R7 R8 ΧΠ-41-1 ch3 H H H Bz n3 F F OH H H XII-41-2 ch3 H H CH3 Bz n3 F F OH H H ΧΠ-41-3 ch3 H H CHCCH^ Bz n3 F F OH H H XII-41-4 ch3 H H CHaCHtCH,), Bz n3 F F OH H H XII-41-5 ch3 H H CH2Ph Bz n3 F F OH H H XII-41-6 ch3 H H CHj-indol-3-yl Bz n3 F F OH H H XII-41-7 ch3 H H CH2CH2SCH3 Bz n3 F F OH H H XH-41-8 ch3 * H ♦ Bz n3 F F OH H H *R2 and Rejoined together by (CHi)3 to form five-membered ring. 2983472-1 -310- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table ΧΠ-42.

Xs R1 R2 R3’ R3b R4 R5 R6 X Y ΊΤ Rs XII-42-1 Et H H H Bz n3 F F OH H H XII-42-2 Et H H CH3 Bz n3 F F OH H H ΧΠ-42-3 Et H H CH(CH3)2 Bz n3 F F OH H H ΧΠ-42-4 Et H H CH2CH(CH3)2 Bz n3 F F OH H H XII-42-5 Et H H CH2Ph Bz n3 F F OH H H ΧΠ-42-6 Et H H CH2-indol-3-yl Bz n3 F F OH H H ΧΠ-42-7 Et H H ch2ch2sch3 Bz n3 F F OH H H XI M2-8 Et * H * Bz n3 F F OH H H ♦R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XI1-43.

Xs R* R2 R3" R4 RJ R* X Y r’ Rg XU-43-1 'Pr H H H Bz n3 F F OH H H XII-43-2 'Pr H H ch3 Bz n3 F F OH H A XII-43-3 'Pr H H CH(CH,)i Bz n3 F F OH H H XIM3^4 'Pr H H CH2CH(CH3)2 Bz n3 F F OH H H XII-43-5 'Pr H H CH2Ph Bz n3 F F OH H H XII-43-6 'Pr H H CH2-indoI-3-yl Bz n3 F F OH H H ΧΠ-43-7 'Pr H H CH2CH2SCH3 Bz n3 F F OH H H XII-43-8 'Pr ♦ H ♦ Bz n3 F F OH H H 10 *R2 and R3b joined together by (Cl·^ to form five-membered ring.

Table XII-44.

Xs R1 "R7~" IF" “R^ IF R6 X Y R7 Ic XII-44-1 'Bu H H H Bz n3 F F OH H H ΧΠ-44-2 'Bu H H CH3 Bz n3 F F OH H H ΧΠ-44-3 'Bu H H CH(CH3)j Bz n3 F F OH H H XII-44-4 'Bu H H CH2CH(CH3)2 Bz n3 F F OH H H XH-44-5 'Bu H H CH2Ph Bz n3 F F OH H H XII-44-6 'Bu H H CH2-indol-3-yl Bz n3 F F OH H H XII-44-7 'Bu H H CHiCHiSCHs Bz n3 F F OH H H XII-44-8 "Tt 'Bu · · * H * Bz n3 F F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -311 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XII-45.

Ns R1 R2 r3‘ Ί?*-- ir R5 R6 X Y r’ ΧΠ-45-1 Ph H H H Bz n3 F F OH H H XH-45-2 Ph H H ch3 Bz n3 F F OH H H ΧΠ-45-3 Ph H H CH(CH3)2 Bz n3 F F OH H H XII-45-4 Ph H H CH2CH(CH3)2 Bz n3 F F OH H H XH-45-5 Ph H H CH2Ph Bz n3 F F OH H H XII-45-6 Ph H H CH2-indol-3-yl Bz n3 F F OH H H ΧΠ-45-7 Ph H H ch2ch2sch3 Bz n3 F F OH H H XII-45-8 Ph * H * Bz n3 F F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XII-46.

Ns R1 R2 R3’ R3b IT R5 R6 X Y R R“ XU-46-1 p-Me-Ph H H H Bz n3 F F OH H H ΧΠ-46-2 p-Me-Ph H H ch3 Bz n3 F F OH H H XII-46-3 p-Me-Ph H H CH(CH3)2 Bz n3 F F OH H H XII-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz n3 F F OH H H XII-46-5 p-Me-Ph H H CH2Ph Bz n3 F F OH H H ΧΠ-46-6 p-Me-Ph H H CH2-indol-3-yl Bz n3 F F OH H H XII-46-7 p-Me-Ph H H CH2CH2SCH3 Bz n3 F F OH H H XII-46-8 p-Me-Ph * H * Bz n3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XI1-47. 1 1 ' I II·-· Ml HI?" ....... '»-

Ns R R2 R3’ R3b R4 Rs R6 X Y R7 R" XU-47-1 p-F-Ph H H H Bz n3 F F OH H H ΧΠ-47-2 p-F-Ph H H CH3 Bz n3 F F OH H H XII-47-3 p-F-Ph H H CH(CH3)2 Bz n3 F F OH H H XH-47-4 p-F-Ph H H CH2CH(CH3)2 Bz n3 F F OH H H XII-47-5 p-F-Ph H H CH2Ph Bz n3 F F OH H H ΧΠ-47-6 p-F-Ph H H CH2-indol-3-yl Bz n3 F F OH H H XII-47-7 p-F-Ph H H CH2CH2SCH3 Bz n3 F F OH H H XII-47-8 —77 p-F-Ph ; -J * H * Bz n3 F F OH H H *R2 and RJb joined together by (CHfeb to form five-membered ring. 2983472-1 -312- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XII-48.

Xs R1 R^ Rj. R4 Rs R6 X Y R7 R8" XII-48-1 p-Cl-Ph H H H Bz n3 F F OH H H XII-48-2 p-Cl-Ph H H ch3 Bz n3 F F OH H H ΧΠ-48-3 p-Cl-Ph H H CH(CH3)2 Bz n3 F F OH H H ΧΠ-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz n3 F F OH H H Xll-48-5 p-Cl-Ph H H CH2Ph Bz n3 F F OH H H ΧΠ-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz n3 F F OH H H ΧΠ-48-7 p-Cl-Ph H H CH2CH2SCH3 Bz n3 F F OH H H ΧΠ-48-8 . r p-CI-Ph •,3b .· j * H * Bz n3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XII-49.

Ns R' RJ -pr -r” Ί?“ RJ R6 X Y R7 R8 XH-49-1 p-Br-Ph H H H Bz n3 F F OH H H XH-49-2 p-Br-Ph H H CH3 Bz n3 F F OH H H XII-49-3 p-Br-Ph H H CH(CH3)2 Bz n3 F F OH H H XTI-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz n3 F F OH H H XII-49-5 p-Br-Ph H H CH2Ph Bz n3 F F OH H H XII-49-6 p-Br-Ph H H CH2-indol-3-yl Bz n3 F F OH H H ΧΠ-49-7 p-Br-Ph H H CH2CH2SCH3 Bz n3 F F OH H H XH-49-8 p-Br-Ph ♦ H * Bz n3 F F OH H H ♦R2 and RJ0 joined together by (CH2)3 to form five-membered ring. 5 Table ΧΠ-50. I n— 1 Rl·. λ '. λ JC -----~ b —

X° R1 IF rJb R3b R4 R3 R6 X Y R7 R8 XII-50-1 p-I-Ph H H H Bz n3 F F OH H H XII-50-2 p-I-Ph H H CH3 Bz n3 F F OH H H XII-50-3 p-I-Ph H H CH(CH3)2 Bz n3 F F OH H H XII-50-4 p-I-Ph H H CH2CH(CH3)2 Bz n3 F F OH H H ΧΠ-50-5 p-I-Ph H H CH2Ph Bz n3 F F OH H H XII-50-6 p-I-Ph H H CH2-indol-3-yl Bz n3 F F OH H H XII-50-7 p-I-Ph H H CH2CH2SCH3 Bz n3 F F OH H H XII-50-8 p-I-Ph * H ♦ Bz n3 F F OH H H *R2and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 - 313 - WO 2008/121634 PCT/US2008/058183

Docket No. 60I37.0034WOU1

Table XIII-1.

Xs Rl ir r3. κ R4 ic Rfc X Y r’ Ra XIII-1-1 ch3 H H H ch3 n3 H F OH H H ΧΙΠ-1-2 ch3 H H ch3 ch3 n3 H F OH H H XIH-1-3 ch3 H H CH(CH3)2 ch3 n3 H F OH H H ΧΙΠ-1-4 ch3 H H CH2CH(CH3)2 ch3 n3 H F OH H H XIII-1-5 ch3 H H CH2Ph ch3 n3 H F OH H H XHI-1-6 ch3 H H CH2-indol-3-yl ch3 n3 H F OH H H ΧΙΠ-1-7 ch3 H H CH2CH2SCH3 ch3 n3 H F OH H H XIII-1-8 ch3 ♦ H * ch3 n3 H F OH H H *R^ and Rejoined together by (CHbk to form five-membered ring. 5 Table ΧΙΠ-2.

......H

Xa R R2 R3. R3b R5 R6 X Y r" R8 XIII-2-1 Et H H H CH3 n3 H F OH H H XIII-2-2 Et H H CH3 ch3 n3 H F OH H H XIII-2-3 Et H H CH(CH3)2 ch3 n3 H F OH H H XIII-2-4 Et H H CH2CH(CH3)2 ch3 n3 H F OH H H XIII-2-5 Et H H CH2Ph ch3 n3 H F OH H H XIII-2-6 Et H H CH2-indol-3-yl ch3 n3 H F OH H H ΧΠΙ-2-7 Et H H CH2CH2SCH3 ch3 n3 H F OH H H XIII-2-8 “ϊπι—τζ Et * H * ch3 n3 H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -314- WO 2008/121634

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Table ΧΪΙΙ-3.

Ns R1 R2 R3e “r35 R4 R6 X Y r" r“ XIII-3-1 'Pr H H H ch3 n3 H F OH H H XIII-3-2 'Pr H H ch3 ch3 n3 H F OH H H ΧΙΠ-3-3 'pr H H CH(CH3)2 ch3 n3 H F OH H H ΧΙΠ-3-4 'Pr H H CH2CH(CH3)2 ch3 n3 H F OH H H ΧΠΙ-3-5 'Pr H H CH2Ph ch3 n3 H F OH H H XIII-3-6 'Pr H H CHrindol-3-yI ch3 n3 H F OH H H ΧΙΠ-3-7 'Pr H H CH2CH2SCH3 ch3 n3 H F OH H H XIH-3-8 'Pr * H ♦ ch3 n3 H F OH H H *R2 and R36 joined together by (Cthb to form five-membered ring.

Table ΧΙΠ-4.

Ns R1 R2 R3t "R35 R4 Rs r5- X Y R? IF XHI-4-1 'Bu H H H ch3 n3 H F OH H H ΧΙΠ-4-2 'Bu H H ch3 ch3 n3 H F OH H H XIU-4-3 'Bu H H CHiCHj), ch3 n3 H F OH H H XIH-4-4 'Bu H H CH2CH(CH3)2 ch3 n3 H F OH H H XIII-4-5 'Bu H H CH2Ph ch3 n3 H F OH H H XIII-4-6 'Bu H H CH2-indol-3-yl ch3 n3 H F OH H H ΧΠΝ4-7 'Bu H H CH2CH2SCH3 ch3 n3 H F OH H H XHI-4-8 'Bu * H * ch3 n3 H F OH H H *R2 and RJb joined together by (CH2)j to form five-membered ring. 5 Table XIII-5.

— - I II···. I III· ' 1 J ....... - II

Na R R2 R3" R3b R4 Ic R6 X Y R' R8 XIH-5-1 Ph H H H ch3 n3 H F OH H H XIII-5-2 Ph H H CH3 ch3 n3 H F OH H H XIH-5-3 Ph H H CHCCH^ ch3 n3 H F OH H H XIH-5-4 Ph H H CH2CH(CH3)2 ch3 n3 H F OH H H ΧΙΠ-5-5 Ph H H CH2Ph ch3 n3 H F OH H H XIH-5-6 Ph H H CH2-indol-3-yl ch3 n3 H F OH H H XIH-5-7 Ph H H CH2CH2SCH3 ch3 n3 H F OH H H XIII-5-8 Ph * H * ch3 n3 H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -315- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XIH-6.

Xa R1 r3" TF- -R38 r^ R5 ”F’ X Y R7” r“ XIH-6-1 p-Me-Ph H H H ch3 n3 H F OH H H XIII-6-2 p-Me-Ph H H ch3 ch3 n3 H F OH H H XIII-6-3 p-Me-Ph H H CH(CH3)2 ch3 n3 H F OH H H XIII-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 n3 H F OH H H XIII-6-5 p-Me-Ph H H CH2Ph ch3 n3 H F OH H H XIII-6-6 p-Me-Ph H H CH2-indol-3-yl ch3 n3 H F OH H H XIII-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 n3 H F OH H H XIH-6-8 p-Me-Ph * H ♦ ch3 n3 H F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XIII-7.

Xa R1 RJ Rj. R3b R4 R3 R6 X Y R' R“ ΧΠΙ-7-1 p-F-Ph H H H ch3 n3 Η F OH H H XIH-7-2 p-F-Ph H H CH3 ch3 n3 H F OH H H XIU-7-3 p-F-Ph H H CH(CH3)2 ch3 n3 H F OH H H XIII-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 n3 H F OH H H ΧΙΠ-7-6 p-F-Ph H H CH2Ph ch3 n3 H F OH H H XIII-7-7 p-F-Ph H H CH2-indol-3-yl ch3 n3 H F OH H H XIII-7-8 p-F-Ph H H ch2ch2sch3 ch3 n3 H F OH H H XIII-7-20 p-F-Ph * H * ch3 n3 H F OH H H *R2 and joined together by (CH2)3 to form five-membered ring. 5 Table XIII-8. 1 n 1 1 "J f J ' R 1

Xa Rl R3 r3. R3b R4 R3 R4 X Y r" Ra ΧΙΠ-8-1 p-Cl-Ph H H H CH3 n3 H F OH H H XHI-8-2 p-CI-Ph H H CH3 ch3 n3 H F OH H H XIII-8-3 p-Cl-Ph H H CH(CH3)2 ch3 n3 H F OH H H ΧΙΠ-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 n3 H F OH H H XIII-8-5 p-Cl-Ph H H CH2Ph ch3 n3 H F OH H H XHI-8-6 p-Cl-Ph H H CH2-indo1-3-yl ch3 n3 H F OH H H ΧΠΙ-8-7 p-CI-Ph H H CH2CH2SCH3 ch3 n3 H F OH H H ΧΠΙ-8-8 -T, p-Cl-Ph -Jb · - i * H * ch3 n3 H F OH H H *R2 and RJb joined together by (CH2)3t0 f°rm five-membered ring. 2983472-1 -316- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table ΧΠΙ-9

Xa R1 R2 R3fl -jpc R4 r! R6 X Y R7 Ra ΧΠΙ-9-1 p-Br-Ph H H H ch3 n3 H F OH H H XIII-9-2 p-Br-Ph H H ch3 ch3 n3 H F OH H H ΧΠΙ-9-3 p-Br-Ph H H CH(CH3)2 ch3 n3 H F OH H H ΧΙΠ-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 n3 H F OH H H ΧΠΙ-9-6 p-Br-Ph H H CH2Ph ch3 n3 H F OH H H ΧΙΠ-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 n3 H F OH H H XIII-9-8 p-Br-Ph H H CH2CH2SCH3 ch3 n3 H F OH H H XIH-9-20 p-Br-Ph * H * ch3 n3 H F OH H H *R? and Rejoined together by (CH2)3 to form five-membered ring.

Table ΧΙΠ-10.

Xa R1 R2 R3’ R3b R4 R5 R6 X Υ R7 R8 ΧΙΠ-10-1 p-I-Ph H H H CH3 n3 Η F ΟΗ Η Η ΧΙΠ-10-2 p-I-Ph H H ch3 ch3 n3 Η F ΟΗ Η Η XIII-10-3 p-I-Ph H H CH(CH3)2 ch3 n3 Η F ΟΗ Η Η XIII-10-4 p-I-Ph H H CH2CH(CH3)2 ch3 n3 Η F ΟΗ Η Η XIII-10-5 p-I-Ph H H CH2Ph ch3 n3 Η F ΟΗ Η Η XIII-10-6 p-I-Ph H H CH2-indol-3-yl ch3 n3 Η F ΟΗ Η Η ΧΙΠ-10-7 p-I-Ph H H CH2CH2SCH3 ch3 n3 Η F ΟΗ Η Η ΧΙΠ-10-8 p-I-Ph * H * ch3 n3 Η F ΟΗ Η Η *RZ and Rjb joined together by (CHfeb to form five-membered ring. 5 Table XUI-11. "" ' I __ H R ML ' _ J ' _ I .. £ .....« a—

Χϊ R ΊΓ R3b R4 Rs R6 X Y R7 R8 ΧΙΙΙ-11-1 ch3 H H H Et n3 H F OH H H ΧΠΙ-11-2 ch3 H H CH3 Et n3 H F OH H H ΧΙΙΙ-11-3 ch3 H H ΟΗ(ΟΗ3)2 Et n3 H F OH H H XIH-H-4 ch3 H H CH2CH(CH3)2 Et n3 H F OH H H ΧΙΙΙ-11-5 ch3 H H CH2Ph Et n3 H F OH H H ΧΙΠ-11-6 ch3 H H CHrindol-3-yl Et n3 H F OH H H ΧΙΙΙ-11-7 ch3 H H CH2CH2SCH3 Et n3 H F OH H H ΧΙΙΙ-11-8 ch3 * H * Et n3 H F OH H H *R2 and RJo joined together by (CH2)3 to form five-membered ring. 2983472-1 -317- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table ΧΙΠ-12.

Xs R1 R2 -jpr "r38 “iF R5 R6 X Y r’ r“ ΧΙΠ-12-1 Et. H H H Et n3 H F OH H H ΧΙΠ-12-2 Et H H ch3 Et n3 H F OH H H ΧΙΠ-12-3 Et H H CH(CH3)2 Et n3 H F OH H H XIII-12-4 Et H H CH2CH(CH3)2 Et n3 H F OH H H XIII-12-5 Et H H CH2Ph Et n3 H F OH H H ΧΠΙ-12-6 Et H H CH2-indoI-3-yl Et n3 H F OH H H ΧΠΙ-12-7 Et H H CH2CH2SCH3 Et n3 H F OH H H XIII-12-8 Et * H * Et n3 H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIII-13.

Xs R R7 R3b R/ R5 R6 X Y R' R8 XIII-I3-1 'Pr H H H Et n3 H F OH H H XIII-13-2 'Pr H H CH3 Et n3 H F OH H H ΧΠΙ-13-3 'Pr H H CH(CH3)2 Et n3 H F OH H H ΧΠΙ-13-4 /pr H H CH2CH(CH3)2 Et n3 H F OH H H XHI-13-5 'Pr H H CH2Ph Et n3 H F OH H H XIH-13-6 'Pr H H CHrlndol-3-yl Et n3 H F OH H H ΧΙΠ-13-7 'Pr H H CH2CH2SCH3 Et n3 H F OH H H ΧΠΙ-13-8 J 1-. 'Pr ,3b' * H * Et n3 H F OH H H *R2 and R3b joined together by (CT^h to form five-membered ring. 5 Table XIII-14. W .....«. '^L· .11 "» .2 . '"W 'll"*"

Xs R* R2 R3a “r35 R4 R6 X Y It R8 XIII-14-1 'Bu H H H Et n3 H F OH H H XIH-14-2 'Bu H H ch3 Et n3 H F OH H H ΧΠΙ-14-3 'Bu H H CH(CH3)2 Et n3 H F OH H H XIH-14-4 'Bu H H CH2CH(CH3)2 Et n3 H F OH H H XIII-14-5 'Bu H H CH2Ph Et n3 H F OH H H XHI-14-6 'Bu H H CH2-indol-3-yl Et n3 H F OH H H XUI-14-7 'Bu H H ch2ch2sch3 Et n3 H F OH H H XIH-14-8 'Bu 4 H * Et n3 H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -318- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XIII-15.

R1 R2 R3a r4 Rs R6 X Y ΊΓ R“ XHI-15-1 Ph H H H Et n3 H F OH H H XIH-15-2 Ph H H ch3 Et n3 H F OH H H ΧΠΙ-15-3 Ph H H CH(CH3)2 Et n3 H F OH H H XIII-15-4 Ph H H CH2CH(CH3)2 Et n3 H F OH H H XIH-15-5 Ph H H CH2Ph Et n3 H F OH H H XIH-15-6 ' Ph H H CH2-indol-3-yl Et n3 H F OH H H ΧΠΜ5-7 Ph H H CH2CH2SCH3 Et n3 H F OH H H XIU-15-8 . n Ph 3b · · * H * Et n3 H F OH H H *R2 and Rejoined together by (CHa)3 to form five-membered ring.

Table XIII-16.

Ife R1 R2 —^35 “R35 R4 R5 R6 X Y R7 R8 ΧΠΙ-16-1 p-Me-Ph H H H Et N3 H F OH H H XIII-16-2 p-Me-Ph H H ch3 Et N3 H F OH H H XIII-16-3 p-Me-Ph H H CHCCH^ Et N3 H F OH H H XHI-16-4 p-Me-Ph H H CH2CH(CH3)2 Et N3 H F OH H H ΧΙΠ-16-5 p-Me-Ph H H CH2Ph Et N3 H F OH H H ΧΙΠ-16-6 p-Me-Ph H H CHrindol-3-yI Et N3 H F OH H H ΧΙΠ-16-7 p-Me-Ph H H CH2CH2SCH3 Et N3 H F OH H H XIII-16-8 p-Me-Ph * H *' Et N3 H F OH H H *R2 and RJb joined together by (CHj)3 to form five-membered ring. Table XIII-17. ~Νϋ R1 R2^ R3®- R35 R4 R1 R6 X Y r’ R8 XIII-17-1 p-F-Ph H H H Et N3 H F OH H H ΧΠΙ-17-2 p-F-Ph H H ch3 Et N3 H F OH H H ΧΙΠ-17-3 p-F-Ph H H CH(CH3)2 Et N3 H F OH H H ΧΠΙ-17-4 p-F-Ph H H CH2CH(CH3)2 Et N3 H F OH H H ΧΙΠ-17-5 p-F-Ph H H CH2Ph Et N3 H F OH H H XII1-17-6 p-F-Ph H H CH2-indol-3-yl Et N3 H F OH H H XIH-17-7 p-F-Ph H H CH2CH2SCH3 Et N3 H F OH H H XIII-17-8 p-F-Ph * H * Et N3 H F OH H H *R2 and Rejoined together by (Ctihb to form five-membered ring. 2983472-1 -319- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XIH-18. "λϊ\ D1

Ns R1 R2 R3e -pu R4 Rs V X Y F R8 ΧΙΙΙ-Ϊ8-1 p-Cl-Ph H H H Et n3 H F OH H H XIII-18-2 p-Cl-Ph H H ch3 Et n3 H F OH H H XIH-18-3 p-CI-Ph H H CH(CH3)2 Et n3 H F OH H H XIII-18-4 p-Cl-Ph H H CH2CPI(CH3)2 Et n3 H F OH H H XIII-18-5 p-Cl-Ph H H CH2Ph Et n3 H F OH H H XHI-18-6 p-Cl-Ph H H CHj-indol-3-yl Et n3 H F OH H H XIII-18-7 p-Cl-Ph H H CH2CH2SCH3 Et n3 H F OH H H XIII-18-8 p-Cl-Ph * H ♦ Et n3 H F OH H H *R2 and Rejoined together by (CFhb to form five-membered ring.

Table XHI-19.

Ns R1 R2 R3a R4 R6 X Y R7 R" X1II-19-1 p-Br-Ph H H H Et n3 H F OH H H ΧΙΠ-19-2 p-Br-Ph H H CH3 Et n3 H F OH H H XIII-19-3 p-Br-Ph H H CH(CH3)2 Et n3 H F OH H H XII1-19-4 p-Br-Ph H H CH2CH(CH3)2 Et n3 H F OH H H ΧΙΠ-19-5 p-Br-Ph H H CH2Ph Et n3 H F OH H H XIII-19-6 p-Br-Ph H H CHrindol-3-yl Et n3 H F OH H H XIII-19-7 p-Br-Ph H H CH2CH2SCH3 Et n3 H F OH H H ΧΙΠ-19-8 p-Br-Ph * H * Et n3 H F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XII1-20.

. — ,-----—«, ·~- , , 2—z - 1 "'B

Ns R1 R2 R3" R3b R4 RJ R6 X Y R7 R8 ΧΙΠ-20-1 p-I-Ph H H H Et n3 H F OH H H XIH-20-2 p-I-Ph H H CH3 Et n3 H F OH H H XIII-20-3 p-I-Ph H H CH(CH3)2 Et n3 H F OH H H XH1-20-4 p-I-Ph H H CH2CH(CH3)2 Et n3 H F OH H H ΧΙΠ-20-5 p-I-Ph H H CH2Ph Et n3 H F OH H H XIII-20-6 p-I-Ph H H CH2-indol-3-yI Et n3 H F OH H H ΧΙΠ-20-7 p-I-Ph H H CH2CH2SCH3 Et n3 H F OH H H XIII-20-8 —tt; p-I-Ph Jb · . * H * Et n3 H F OH H H *R2 and RJb joined together by (CH^ to form five-membered ring. 2983472-1 -320- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XIII-21.

Xs R1 R2 RJ« "r^ R4 Rs R6 X Y R7 Ra ΧΠΙ-21-1 ch3 H H H "¥7 n3 H F OH H H ΧΙΠ-21-2 ch3 H H ch3 'Pr n3 H F OH H H ΧΠΙ-21-3 ch3 H H CH(CH3)2 'Pr n3 H F OH H H ΧΠΙ-21-4 ch3 H H CH2CH(CH3)2 'Pr n3 H F OH H H ΧΙΪΙ-21-5 ch3 H H CH2Ph 'Pr n3 H F OH H H XIII-21-6 ch3 H H CH2-indol-3-yl 'Pr n3 H F OH H H X1I1-21-7 ch3 H H CH2CH2SCH3 'Pr n3 H F OH H H XIH-21-8 ch3 * H * 'Pr n3 H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring?

Table ΧΠΙ-22.

Xs R IV R3‘ R36 R4 R3 R6 X Y R' R ΧΙΠ-22-1 Et H H H JPr n3 H F OH H H XHI-22-2 Et H H ch3 'Pr n3 H F OH H H XHI-22-3 Et H H CH(CH3)2 'Pr n3 H F OH H H XIII-22-4 Et H H CHjCHtCHjh 'Pr n3 H F OH H H XIIl-22-5 Et H H CH2Ph 'Pr n3 H F OH H H XIH-22-6 Et H H CH2-indol-3-yl 'Pr n3 H F OH H H XHI-22-7 Et H H CH2CH2SCH3 'Pr n3 H F OH H H XIH-22-8 "ITS Et 3b · * H * 'Pr n3 H F OH H H *R2 and R3*5 joined together by (CHa^to form five-membered ring. 5 Table XIII-23. ' J ' 11" 1 1........ '' ' ' U*

Xs R1 R1 IF" R3b R4 r! R6 X Y R’ R8 XIII-23-1 ’Pr H H H 'Pr n3 H F OH H H XIU-23-2 'Pr H H ch3 'Pr n3 H F OH H H XIH-23-3 'Pr H H CH(CH3)2 'Pr n3 H F OH H H XHI-23-4 'Pr H H CH2CH(CH3)2 'Pr n3 H F OH H H ΧΙΠ-23-5 'Pr H H CH2Ph 'Pr n3 H F OH H H XIH-23-6 'Pr H H CH2-indol-3-yl 'Pr n3 H F OH H H ΧΠΙ-23-7 'Pr H H CH2CH2SCH3 'Pr n3 H F OH H H X1II-23-8 ipr * H ♦ 'Pr n3 H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. Table XIII-24. Xs R" R2 R3a R4 Rs R6 X Y RJ R8 2983472-1 -321 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Kfi R1 Ra “rF "R36 R4 RJ R6 X Y r’ R11 ΧΠΙ-24-1 jBu H H H n3 H F OH H H ΧΠΙ-24-2 'Bu H H ch3 'Pr n3 H F OH H H XIII-24-3 'Bu H H CH(CH3)2 'Pr n3 H F OH H H ΧΙΠ-24-4 'Bu H H CH2CH(CH3)2 'Pr n3 H F OH H H ΧΙΠ-24-5 'Bu H H CHzPh 'Pr n3 H F OH H H XIII-24-6 'Bu H H CH2-indol-3-yl 'Pr n3 H F OH H H ΧΙΠ-24-7 H H ch2ch2sch3 'Pr n3 H F OH H H ΧΙΠ-24-8 'Bu ♦ H ♦ 'Pr n3 H F OH H H *RZ and R3b joined together by (CFhbto f°rm five-membered ring.

Table XIII-25.

N° R1 R3 R3® R3b R4 ΊΤ R6 X Y R’ R“ XIII-25-1 Ph H H H 'Pr n3 H F OH H H XIII-25-2 Ph H H ch3 'Pr n3 H F OH H H XIII-25-3 Ph H H CH(CH3)2 'Pr n3 H F OH H H XIII-25-4 Ph H H CH2CH(CH3)2 'Pr n3 H F OH H H XHI-25-5 Ph H H CH2Ph 'Pr n3 H F OH H H XIII-25-6 Ph H H CH2-indol-3-yl 'Pr n3 H F OH H H ΧΠΙ-25-7 Ph H H CH2CH2SCH3 'Pr n3 H F OH H H XIII-25-8 “ϊϊπ—tt Ph ,3b : ΐ * H * 'Pr n3 H F OH H H *R2 and RJb joined together by (C^h to form five-membered ring.

Table XIH-26.

Xa Έ R2 R3® R3b R4 Rs R6 X Y R7 R3 XIH-26-1 p-Me-Ph H H H *Pr n3 H F OH H H ΧΠΙ-26-2 p-Me-Ph H H ch3 'Pr n3 H F OH H H ΧΠΙ-26-3 p-Me-Ph H H CHCCHah 'Pr n3 H F OH H H XIII-26-4 p-Me-Ph H H CH2CH(CH3)2 'Pr n3 H F OH H H XIII-26-5 p-Me-Ph H H CH2Ph 'Pr n3 H F OH H H XHI-26-6 p-Me-Ph H H CH2-indol-3-yl /pr n3 H F OH H H XHI-26-7 p-Me-Ph H H CH2CH2SCH3 'Pr n3 H F OH H H XIII-26-8 -ΤΐΤ p-Me-Ph 3b ·. · 1 , + H * 'Pr n3 H F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -322- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XIII-27.

Xs R1 R2 R3’ R?b R5 Rb X Y R7 R8 XIII-27-1 p-F-Ph Η Η H JPr n3 H F OH Η H ΧΙΠ-27-2 p-F-Ph Η H CH3 'Pr n3 H F OH Η H XIII-27-3 p-F-Ph Η H CH(CH3)2 'Pr n3 H F OH Η H ΧΠΙ-27-4 p-F-Ph Η H CH2CH(CH3)2 'Pr n3 H F OH Η H XIII-27-5 p-F-Ph Η H CH2Ph 'Pr n3 H F OH Η H XIH-27-6 p-F-Ph Η H CH2-indol-3-yl 'Pr n3 H F OH Η H XIII-27-7 p-F-Ph Η H CH2CH2SCH3 'Pr n3 H F OH Η H XHI-27-8 p-F-Ph * H * 'Pr n3 H F OH Η H ♦R2 and R3b joined together by (CH2)3 to form five-membered ring. Table ΧΙΠ-28. ”χϋ R1 R2 R3· R3b R4 R4 R6 X Y R7 R8 ΧΙΠ-28-1 p<l-Ph Η Η H JPr N3 H F OH Η H XIII-28-2 p-Cl-Ph Η H CH3 'Pr Na H F OH Η H ΧΙΙΪ-28-3 p-Cl-Ph Η H CH(CH3)2 'Pr n3 H F OH Η H XIU-28-4 p-Cl-Ph Η H CH2CH(CH3)2 'Pr N3 H F OH Η H ΧΠΙ-28-5 p-Cl-Ph Η H CH2Ph 'Pr n3 H F OH Η H XIII-28-6 p-Cl-Ph Η H CH2-indol-3-yl 'Pr Na H F OH Η H ΧΙΠ-28-7 p-Cl-Ph Η H CH2CH2SCH3 'Pr Na H F OH Η H XIH-28-8 p-Cl-Ph * H * 'Pr Na H F OH Η H *R2 and R3b joined together by (CHibt0 f°rm five-membered ring. 5 Table XilI-29. -Γ' 1-11

X° R1 "R7 R3· R3b R4 "R5- R6 X Y R7 R8 ΧΙΠ-29-1 p-Br-Ph H H H JPr n3 H F OH H H XIII-29-2 p-Br-Ph H H CHa 'Pr n3 H F OH H H XUI-29-3 p-Br-Ph H H CHCCHaX 'Pr n3 H F OH H H ΧΠΙ-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr N3 H F OH H H XIII-29-5 p-Br-Ph H H CH2Ph 'Pr Na H F OH H H XIII-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr Na H F OH H H XIII-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr Na H F OH H H Χ1Π-29-8 p-Br-Ph * H * 'Pr Na H F OH H H *R2 and Rejoined together by (0¾¼ to form five-membered ring. Table XIII-30. Xs R1 Ra RJl R3b R4 R4 R6 X Y R7 RH 2983472-1 -323 - WO 2008/121634

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Xa R1 R2 -pr ’"iC' IT RJ R6 X Y R Ra XIII-30-1 p-I-Ph H H H ;Pr n3 H F OH H H XIII-30-2 p-I-Ph H H ch3 'Pr n3 H F OH H H ΧΠΙ-30-3 p-I-Ph H H CH(CH3)2 ipr n3 H F OH H H XHI-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr n3 H F OH H H ΧΙΠ-30-5 p-I-Ph H H CH2Ph 'Pr n3 H F OH H H XIH-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr n3 H F OH H H ΧΙΠ-30-7 p-I-Ph H H CH2CH2SCH3 'Pr n3 H F OH H H ΧΙΠ-30-8 p-I-Ph + H * 'Pr n3 H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIII-31.

Xs R1 RJ r3# R3b R5 r6 X Y R“ XIU-31-1 CH3 H H H "Bu n3 H F OH H H ΧΠΙ-31-2 ch3 H H ch3 "Bu n3 H F OH H H ΧΙΠ-31-3 ch3 H H CH(CH3)2 "Bu n3 H F OH H H ΧΠΙ-31-4 ch3 H H CH2CH(CH3)2 "Bu n3 H F OH H H ΧΗΪ-31-5 ch3 H H CH2Ph "Bu n3 H F OH H H XIII-31-6 ch3 H H CH2-indol-3-yl "Bu n3 H F OH H H ΧΙΠ-31-7 ch3 H H CH2CH2SCH3 "Bu n3 H F OH H H XIH-31-8 ch3 * H ♦ "Bu n3 H F OH H H ♦R2 and R3b joined together by (0¾)] to form five-membered ring.

Table XIII-32.

Xa R2 -r3E R4 R5- R6 X Y V ΧΠΙ-32-1 Et H H H "Bu n3 H F OH H H ΧΙΠ-32-2 Et H H ch3 "Bu n3 H F OH H H ΧΙΠ-32-3 Et H H CHCCHaX "Bu n3 H F OH H H XIII-32-4 Et H H CH2CH(CH3)2 "Bu n3 H F OH H H XIII-32-5 Et H H CH2Ph "Bu n3 H F OH H H XHI-32-6 Et H H CHrindoI-3-yl "Bu n3 H F OH H H XIH-32-7 Et H H CH2CH2SCH3 "Bu n3 H F OH H H XIII-32-8 Et * H * "Bu n3 H F OH H H 5 *R2 and Rejoined together by (CH^ to form five-membered ring.

Table XIII-33.

Xa IV R2 R3. R3b R4 R5 R6 X Y R7 R“ ΧΙΠ-33-1 'Pr H H H "Bu n3 H F OH H H 2983472-1 -324- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058I83

Ns R1 R2 ηρτ R3b R4 R5 Ί?" X Y R’ Rb X1H-33-2 'Pr H H ch3 "Bu n3 H F OH H H Χ1Π-33-3 'Pr H H CH(CH3)2 "Bu n3 H F OH H H XHI-33-4 'Pr H H CH2CH(CH3)2 "Bu n3 H F OH H H XIII-33-5 'Pr H H CH2Ph "Bu n3 H F OH H H XIII-33-6 'Pr H H CHi-indol-3-yl "Bu n3 H F OH H H ΧΠΙ-33-7 'Pr H H CH2CH2SCH3 "Bu n3 H F OH H H XIII-33-8 'Pr * H * "Bu n3 H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIII-34.

Ns R R2 R3‘ R3b R4 Rs R6 X Υ R7 R8 ΧΙΠ-34-1 'Bu H H H "Bu n3 Η F ΟΗ Η Η XIII-34-2 'Bu H H ch3 "Bu n3 Η F ΟΗ Η Η ΧΠΙ-34-3 'Bu H H CH(CH3)2 "Bu n3 Η F ΟΗ Η Η XIII-34-4 'Bu H H CH2CH(CH3)2 "Bu n3 Η F ΟΗ Η Η ΧΙΠ-34-5 'Bu H H CH2Ph "Bu n3 Η F ΟΗ Η Η XIII-34-6 'Bu H H CH2-indol-3-yl "Bu n3 Η F ΟΗ Η Η XHI-34-7 ^u H H ch2ch2sch3 "Bu n3 Η F ΟΗ Η Η XIII-34-8 ^u * H * "Bu n3 Η F ΟΗ Η Η *RJ and RJb joined together by (CH2)3 to form five-membered ring.

Table XIIl-35.

Ns R R2 RJa R3b R4 RJ R6 X Y R7 R“ ΧΗΙ-35-1 Ph H H H "Bu n3 H F OH H H ΧΗΪ-35-2 Ph H H ch3 "Bu n3 H F OH H H ΧΙΙΙ-35-3 Ph H H CH(CH3)2 "Bu n3 H F OH H H ΧΙΗ-35-4 Ph H H CH2CH(CH3)2 "Bu n3 H F OH H H ΧΙΙΙ-35-5 Ph H H CH2Ph "Bu n3 H F OH H H Χ1Π-35-6 Ph H H CH2-indol-3-yl "Bu n3 H F OH H H ΧΙΙΙ-35-7 Ph H H CH2CH2SCH3 "Bu n3 H F OH H H ΧΙΙΙ-35-8 Ph * H * "Bu n3 H F OH H H 5 *R2 and Rejoined together by ((%)3 to form five-membered ring.

Table XHI-36._________ R1 R2 R3‘ R3b R’ Rs Rb X Y R7 R8

XIH-36-1 p-Me-Ph Η Η H "Bu N3 H F OH Η H

XIII-36-2 p-Me-Ph Η H CH3 "Bu N3 H F OH Η H 2983472-1 -325- WO 2008/121634 PCT/US2008/058183

Docket No, 60137.0034WOU i

Xs R1 R3 R3’ "R^ Rs R6 X Y R7 Rb XHI-36-3 p-Me-Ph H H CH(CH3)2 "Bu n3 H F OH H H ΧΠΙ-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu n3 H F OH H H XI11-3 6-5 p-Me-Ph H H CH2Ph "Bu n3 H F OH H H XIII-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu n3 H F OH H H XIII-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu n3 H F OH H H ΧΙΠ-36-8 p-Me-Ph * H * "Bu n3 H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIH-37.

R R2 Rj. R3b R4 Rs R6 X Y R7 RB XIII-37-1 p-F-Ph H H H "Bu n3 H F OH H H XIII-37-2 p-F-Ph H H CH3 "Bu n3 H F OH H H XIII-37-3 p-F-Ph H H CH(CH3)2 "Bu n3 H F OH H H ΧΠΙ-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu n3 H F OH H H XHI-37-5 p-F-Ph H H CH2Ph "Bu n3 H F OH H H XIII-37-6 p-F-Ph H H CHi-indol-3-yl "Bu n3 H F OH H H XIII-37-7 p-F-Ph H H CH2CH2SCH3 "Bu n3 H F OH H H XIII-37-8 _ _ J n p-F-Ph · ! J * H * "Bu n3 H F OH H H *R2 and Rejoined together by (0¾¼ to form five-membered ring.

Table ΧΙΠ-38.

Ns R1 “R3" ηρτ- R3b ΊΓ” Rs R6 X Y R’ r“ XIII-38-1 p-Cl-Ph H H H "Bu n3 H F OH H H XIH-38-2 p-Cl-Ph H H ch3 "Bu n3 H F OH H H XIH-38-3 p-Cl-Ph H H CH(CH3)2 "Bu n3 H F OH H H XIII-38-4 p-Cl-Ph H H CH2CH(CH3>2 "Bu n3 H F OH H H XIH-38-5 p-Cl-Ph H H CH2Ph "Bu n3 H F OH H H ΧΠΙ-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu n3 H F OH H H ΧΠΙ-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu n3 H F OH H H XIH-38-8 p-Cl-Ph ♦ H * "Bu n3 H F OH H H 5 *R2 and R3b joined together by (CH^ to form five-membered ring.

Table XIII-39.

Xs R' R^ R3’ R3b R4 R5 R* X Y R7 R“ XIII-39-1 p-Br-Ph H H H "Bu n3 H F OH H H XIH-39-2 p-Br-Ph H H ch3 "Bu n3 H F OH H H XlH-39-3 p-Br-Ph H H CH(CH3)2 "Bu n3 H F OH H H 2983472-1 -326- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Xs R‘ R2 R3· Ί?"' Rs Ί?· X Y r’ Rtt ΧΠΙ-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu n3 H F OH H H XIH-39-5 p-Br-Ph H H CH2Ph "Bu n3 H F OH H H ΧΙΠ-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu n3 H F OH H H XIII-39-7 p-Br-Ph H H CH2CH2SCH3 "Bu n3 H F OH H H ΧΠΙ-39-8 p-Br-Ph ♦ H * "Bu n3 H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIII-40.

X» R* RJa R3’ R’ R R6 X Y R' R8 ΧΙΠ-40-1 p-I-Ph H H H MBu n3 H F OH H H ΧΙΠ-40-2 p-I-Ph H H CH3 "Bu n3 H F OH H H XH1-40-3 p-I-Ph H H CH(CH3)a "Bu n3 H F OH H H ΧΠΙ-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu n3 H F OH H H ΧΠΙ-40-5 p-I-Ph H H CH2Ph "Bu n3 H F OH H H ΧΙΠ-40-6 p-I-Ph H H CH2-indol-3-yl "Bu n3 H F OH H H ΧΙΪΙ-40-7 p-I-Ph H H CH2CH2SCH3 "Bu n3 H F OH H H XIII-40-8 p-I-Ph * H ♦ "Bu n3 H F OH H H ♦R2 and Rejoined together by (CH2b to form five-membered ring.

Table ΧΙΠ-41.

Xa R1 r2 R3’ R4 Rs ~k X Y r" Ra XIII-41-1 ch3 H H H Bz n3 H F OH H H XIH-41-2 ch3 H H ch3 Bz n3 H F OH H H XIU-41-3 ch3 H H CHCCHs^ Bz n3 H F OH H H ΧΠΙ-41-4 ch3 H H CH2CH(CH3)2 Bz n3 H F OH H H ΧΙΠ-41-5 ch3 H H CH2Ph Bz n3 H F OH H H ΧΙΠ-41-6 ch3 H H CH2-indol-3-yl Bz n3 H F OH H H ΧΙΠ-41-7 ch3 H H CH2CH2SCH3 Bz n3 H F OH H H XII1-41-8 ch3 * H * Bz n3 H F OH H H 5 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIII-42.

Xs R R2 R3« R3b R4 IV R X Y R7 R“ ΧΙΠ-42-1 Et H H H Bz n3 H F OH Η H XIH-42-2 Et H H ch3 Bz n3 H F OH H H ΧΠΙ-42-3 Et H H CH(CH3)2 Bz n3 H F OH H H XIH-42-4 Et H H ΟΗ2ΟΗ(ΟΗ3)2 Bz n3 H F OH H H 2983472-1 -327- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Ms R1 R2 ΊΡΓ “r* R4 Rs R6 X Y R7 Rs ΧΙΙΪ-42-5 Et H H CH2Ph Bz n3 H F OH H H ΧΙΠ-42-6 Et H H CH2-indoI-3-yl Bz n3 H F OH H H ΧΠΙ-42-7 Et H H CH2CH2SCH3 Bz n3 H F OH H H XIH-42-8 Et * H ♦ Bz n3 H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIH-43. 'vk D1

Ns R R2 r3“ R3b R4 R5 R5 X Y E R8 XIH-43-1 'Pr H H H Bz n3 H F OH H H XIII-43-2 'Pr H H CH3 Bz n3 H F OH H H XJI1-43-3 'Pr H H CH(CH3)2 Bz n3 H F OH H ΧΙΠ-43-4 fPr H H CH2CH(CH3)2 Bz n3 H F OH H H XIII-43-5 'Pr H H CH2Ph Bz n3 H F OH H H ΧΙΠ-43-6 'Pr H H CH2-indol-3-yl Bz n3 H F OH H H XIII-43-7 'Pr H H ch2ch2sch3 Bz n3 H F OH H H XIII-43-8 'Pr ♦ H ♦ Bz n3 H F OH H H ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. 10 Table ΧΙΠ-44. ............ — I M " » wr ' — ........ J g U“

Ns R1 R2 R3a Hr” R4 Rs R6 X Y r’ Rs Χ1Π-44-1 H H H Bz n3 H F OH H H ΧΠΙ-44-2 'Bu H H CH3 Bz n3 H F OH H H XIII-44-3 'Bu H H CH(CH3)2 Bz n3 H F OH H H ΧΙΠ-44-4 'Bu H H CH2CH(CH3)2 Bz n3 H F OH H H XHI-44-5 'Bu H H CH2Ph Bz n3 H F OH H H XHI-44-6 'Bu H H CH2-indol-3-yl Bz n3 H F OH H H XIII-44-7 'Bu H H CH2CH2SCH3 Bz n3 H F OH H H ΧΠΙ-44-8 'Bu ♦ H * Bz n3 H F OH H H *R2 and Rejoined together by (CHaJj to form five-membered ring.

Table ΧΠΙ-45.

Ns R R2 RJa Rib R4 R1 R6 X Y R7 Rb ΧΙΠ-45-1 Ph H H H Bz n3 H F OH H H ΧΙΠ-45-2 Ph H H ch3 Bz n3 H F OH H H XIH-45-3 Ph H H CH(CH3)2 Bz n3 Η F OH H H 2983472-1 -328- WO 2008/121634 PCT/US2008/058183

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X» R1 R5 R3a R4 Rs R6 X Y r’ XIII-45-4 Ph H H CH2CH(CH3)2 Bz n3 H F OH H H XHI-45-5 Ph H H CH2Ph Bz n3 H F OH H H XIII-45-6 Ph H H CH2-indol-3-yl Bz n3 H F OH H H X1II-45-7 Ph H H CH2CH2SCH3 Bz n3 H F OH H H XIII-45-8 ""j'n Ph 3b ; ; * H * Bz n3 H F OH H H *R2 and Rejoined together by (¢112)3 to form five-membered ring.

Table XIII-46.

Xs R‘ "R3 1 R34 R4 R' R4 X Y R R8 ΧΠΙ-46-1 p-Me-Ph H H H Bz n3 H F OH H H ΧΙΠ-46-2 p-Me-Ph H H ch3 Bz n3 H F OH H H ΧΙΠ-46-3 p-Me-Ph H H CH(CH3)2 Bz n3 H F OH H H ΧΙΪΙ-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz n3 H F OH H H XIII-46-5 p-Me-Ph H H CH2Ph Bz n3 H F OH H H XHI-46-6 p-Me-Ph H H CH2-indol-3-yi Bz n3 H F OH H H ΧΠ1-46-7 p-Me-Ph H H CH2CH2SCH3 Bz n3 H F OH H H XIII-46-8 p-Me-Ph * H * Bz n3 H F OH H H ♦R2 and R3b joined together by (CH2)3 to form five-membered ring. Table XIII-47. Xs R1 R2 -jpr- R3b R4 R5 R4 X Y R7 R8 ΧΪΠ-47-1 p-F-Ph H H H Bz n3 H F OH H H XIH-47-2 p-F-Ph H H ch3 Bz n3 H F OH H H XUI-47-3 p-F-Ph H H CH(CH3)2 Bz n3 H F OH H H XUI-47-4 p-F-Ph H H CH2CH(CH3)2 Bz n3 H F OH H H ΧΙΠ-47-5 p-F-Ph H H CH2Ph Bz n3 H F OH H H XIII-47-6 p-F-Ph H H CH2-indol-3-yl Bz n3 H F OH H H XIH-47-7 p-F-Ph H H CH2CH2SCH3 Bz n3 H F OH H H ΧΙΠ-47-8 p-F-Ph ♦ H * Bz n3 H F OH H H *R2 and RJt> joined together by (CH2)3 to form five-membered ring. Table XIII-48. "Si £1 RJ r3. “r35 R4 R5 R4 X Y R’ R8 XIH-48-1 p-Cl-Ph H H H Bz n3 H F OH H H XHI-48-2 p-Cl-Ph H H CH3 Bz n3 H F OH H H XHI-48-3 p-Cl-Ph H H CH(CH3)2 Bz n3 H F OH H H XIII-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz n3 H F OH H H 2983472-1 -329- WO 2008/121634

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Xs R1 R2 r3. “P5 R5 X Y R7” R8 XIH-48-5 p-Cl-Ph H H CH2Ph Bz n3 H F OH H H XHI-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz n3 H F OH H H ΧΠΙ-48-7 p-Cl-Ph H H CH2CH2SCH3 Bz n3 H F OH H H XIII-48-8 p-Cl-Ph * H * Bz n3 H F OH H H *R2 and Rejoined together by (Cl-bb to form five-membered ring.

Table ΧΠΙ-49.

Xs r’ R3 R3* R3b R4 Rs R&amp; X Y R7 R“ XIH-49-1 p-Br-Ph H H H Bz n3 H F OH H H XIII-49-2 p-Br-Ph H H CH3 Bz n3 H F OH H H XIH-49-3 p-Br-Ph H H CH(CH3)2 Bz n3 H F OH H H ΧΙΠ-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz n3 H F OH H H ΧΠΙ-49-5 p-Br-Ph H H CH2Ph Bz n3 H F OH H H ΧΠΙ-49-6 p-Br-Ph H H CH2-indol-3-yl Bz n3 H F OH H H ΧΙΠ-49-7 p-Br-Ph H H CH2CH2SCH3 Bz n3 H F OH H H XIH-49-8 p-Br-Ph ♦ H * Bz n3 H F OH H H *R2 and R3b joined together by (CHz)3 to form five-membered ring.

Table XIII-50. X> R1 R7 XHI-50-1 p-I-Ph H ΧΠΙ-50-2 p-I-Ph H ΧΙΠ-50-3 p-I-Ph H XHI-50-4 p-I-Ph H XIH-50-5 p-I-Ph H ΧΠΙ-50-6 p-I-Ph H XHI-50-7 p-I-Ph H ΧΠΙ-50-8 p-I-Ph * r3S" R3b ΊΓ H H Bz H ch3 Bz H CH(CH3)2 Bz H CH2CH(CH3)2 Bz H CH2Ph Bz H CH2-indol-3-yl Bz H CH2CH2SCH3 Bz

RJ R6 X Y R7 IV n3 H F OH H H n3 H F OH H H n3 H F OH H H n3 H F OH H H n3 H F OH H H n3 H F OH H H n3 H F OH H H n3 H F OH H H H * Bz *R2 and R30 joined together by (CH2)3 to form five-membered ring. 2983472-1 -330- WO 2008/121634 PCT/US2008/058183

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Table XIV-1.

Ns Rl R2 R3· R3b R4 "R1" R4 X Y R7 r“ XIV-1-1 ch3 H H H ch3 n3 F H OH H H XIV-1-2 ch3 H H ch3 ch3 n3 F H OH H H XIV-1-3 ch3 H H CH(CH3)2 ch3 n3 F H OH H H XIV-1-4 ch3 H H CH2CH(CH3)2 ch3 n3 F H OH H H XIV-1-5 ch3 H H CH2Ph ch3 n3 F H OH H H XIV-1-6 ch3 H H CH2-indol-3-yl ch3 n3 F H OH H H XIV-1-7 ch3 H H ch2ch2sch3 ch3 n3 F H OH H H XIV-1-8 . i ch3 TJE :-7 * H 1* ch3 n3 F H OH H H *R2 and Rejoined together by to form five-membered ring.

Xa R1 R2 -£nr “r35 TT" R5 R6 X Y R’ Ic XIV-2-1 Et H H H ch3 n3 F H OH H H XIV-2-2 Et H H CH3 ch3 n3 F Η OH H H X1V-2-3 Et H H CH(CH3)2 ch3 n3 F H OH H H XIV-2-4 Et H H CH2CH(CH3)2 ch3 n3 F Η OH H H XTV-2-5 Et H H CH2Ph ch3 n3 F H OH H H XIV-2-6 Et H H CH2-indol-3-yl ch3 n3 F H OH H H XTV-2-7 Et H H CH2CH2SCH3 ch3 n3 F Η OH H H XIV-2-8 J i Et rdb ; * H * ch3 n3 F Η OH H H *R2 and Rdt> joined together by (0¾¼ to form five-membered ring. 2983472-1 -331 - WO 2008/121634 PCT/US2008/058183

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Table XIV-3.

Ns R1 R2 R3a R3b R4 Rs R6 X Y R7 XIV-3-1 'Pr H H H ch3 n3 F H OH H H XIV-3-2 Tr H H ch3 ch3 n3 F H OH H H XIV-3-3 *Pr H H CH(CH3)2 ch3 n3 F H OH H H XIV-3-4 iPr H H CH2CH(CH3)2 ch3 n3 F H OH H H XIV-3-5 'Pr H H CH2Ph ch3 n3 F H OH H H XIV-3-6 'Pr H H CH2-indol-3-yl ch3 n3 F H OH H H XIV-3-7 'Pr H H ch2ch2sch3 ch3 n3 F H OH H H XIV-3-8 »pr * H * ch3 n3 F H OH H H *R2 and RJb joined together by (CHj)3 to form five-membered ring.

Table XIV-4.

Ns RT R2 r3. R3b R4 R3 R6 X Y R' R“ XIV-4-1 lBu H H H ch3 n3 F H OH H H XIV-4-2 'Bu H H CH3 ch3 n3 F H OH H H XIV-4-3 'Bu H H CH(CH3)2 ch3 n3 F H OH H H XIV-4-4 'Bu H H CH2CH(CH3)2 ch3 n3 F H OH H H XIV-4-5 'Bu H H CH2Ph ch3 n3 F H OH H H XIV-4-6 ‘Bu H H CH2-indoi-3-yI ch3 n3 F H OH H H XIV-4-7 'Bu H H CH2CH2SCH3 ch3 n3 F H OH H H XIV-4-8 'Bu * H * ch3 n3 F H OH H H *R2 and R3b joined together by (0¾¼ to form five-membered ring. 5 Table XIV-5. " '! "n 'TC 11 - J 1 ' '1 r ~ u

Na R R2 R3* R3b R4 R3 R6 X Y R7 R“ XIV-5-1 Ph H H H CH3 n3 F H OH H H XIV-5-2 Ph H H ch3 ch3 n3 F H OH H H XIV-5-3 Ph H H CH(CH3)2 ch3 n3 F H OH H H XIV-5-4 Ph H H CH2CH(CH3)2 ch3 n3 F H OH H H XIV-5-5 Ph H H CH2Ph ch3 n3 F H OH H H XIV-5-6 Ph H H CH2-indol-3-yl ch3 n3 F H OH H H XIV-5-7 Ph H H CH2CH2SCH3 ch3 n3 F H OH H H XIV-5-8 Ph * H * ch3 n3 F H OH H H *Ra and R3b joined together by (0¾¼ to form five-membered ring. 2983472-1 -332- WO 2008/121634 PCT/US2008/058183

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Table XIV-6.

Xs R' R2 R3’ r35 R4 R1 R0 X Y R Rtf XIV-6-1 p-Me-Ph H H H ch3 n3 F H OH H H XIV-6-2 p-Me-Ph H H ch3 ch3 n3 F H OH H H X1V-6-3 p-Me-Ph H H CH(CH3)2 ch3 n3 F IT OH H H XIV-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 n3 F H OH H H XTV-6-5 p-Me-Ph H H CH2Ph ch3 n3 F H OH H H XIV-6-6 p-Me-Ph H H CH2-indol-3-yl ch3 n3 F H OH H H XIV-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 n3 F H OH H H XIV-6-8 p-Me-Ph * H * ch3 n3 F H OH H H *RZ and Rejoined together by (CHab to form five-membered ring.

Table XIV-7.

Xa R’ R2 Rj« Rib R4 R1 R6 X Y R' R’ XIV-7-1 p-F-Ph H H H ch3 n3 F H OH H H XIV-7-2 p-F-Ph H H ch3 ch3 n3 F H OH H H X1V-7-3 p-F-Ph H H CH(CH3)2 ch3 n3 F H OH H H XIV-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 n3 F Η OH H H XIV-7-6 p-F-Ph H H CH2Ph ch3 n3 F H OH H H XTV-7-7 p-F-Ph H H CH2-indol-3-yl ch3 n3 F H OH H H XIV-7-8 p-F-Ph H H CH2CH2SCH3 ch3 n3 F Η OH H H XIV-7-20 p-F-Ph * H * ch3 n3 F H OH H H •R* and R3b joined together by (CH2)a to form five-membered ring. 5 Table XIV-8. — .....- "I -* - _ RL ' f . R tf

X? Rl R2 r3. Rib R4 R5^ R5 X Y R7 R“ XIV-8-1 p-Cl-Ph H H H ch3 n3 F H OH H H XIV-8-2 p-Cl-Ph H H ch3 ch3 n3 F H OH H H XIV-8-3 p-CI-Ph H H CH(CH3)2 ch3 n3 F H OH H H XIV-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 n3 F H OH H H xrv-8-5 p-Cl-Ph H H CH2Ph ch3 n3 F H OH H H XIV-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 n3 F H OH H H XIV-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 n3 F H OH H H XTV-8-8 ji p-Cl-Ph : -J- * H ♦ ch3 n3 F H OH H H *R2 and R3&amp; joined together by (CH2)3 to form five-membered ring. 2983472-1 -333 - WO 2008/121634

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Table XIV-9.

Ns R1 R1 ηρτ ""ip5 TP” R5 R6 X Y R7 R8 XTV-9-1 p-Br-Ph H H H ch3 n3 F H OH H H XIV-9-2 p-Br-Ph H H ch3 ch3 n3 F H OH H H XTV-9-3 p-Br-Ph H H CH(CH,)2 ch3 n3 F H OH H H X1V-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 n3 F H OH H H XIV-9-6 p-Br-Ph H H CH2Ph ch3 n3 F H OH H H XIV-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 n3 F H OH H H XIV-9-8 p-Br-Ph H H CH2CH2SCH3 ch3 n3 F H OH H H XlV-9-20 p-Br-Ph * H * ch3 n3 F H OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XIV-10.

Ns R' R3 R3. R3b R4 R5 R6 X Y r R8 XIV-10-1 p-I-Ph H H H CH3 n3 F Η OH H H XIV-10-2 p-I-Ph H H ch3 ch3 n3 F H OH H H XIV-10-3 p-I-Ph H H CH(CH3)2 ch3 n3 F H OH H H XTV-10-4 p-I-Ph H H CH2CH(CH3)2 ch3 n3 F H OH H H XTV-10-5 p-I-Ph H H CH2Ph ch3 n3 F H OH H H XIV-10-6 p-I-Ph H H CH2-indol-3-yl ch3 n3 F H OH H H XIV-10-7 p-I-Ph H H CH2CH2SCH3 ch3 n3 F H OH H H XIV-10-8 p-I-Ph * H * ch3 n3 F H OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XIV-11. — ' 1 I ' 'W ' Rl 11 " ~ ‘ A ' "· 1 J ' *" jf "

Ns R RJ R3‘ R3b R4 RJ R6 X Y R7 R8 XIV-11-1 CH3 H H H Et n3 F H OH H H XIV-11-2 ch3 H H ch3 Et n3 F H OH H H XIV-11-3 ch3 H H CH(CH3)a Et n3 F H OH H H XIV-11-4 ch3 H H CH2CH(CH3)2 Et n3 F H OH H H XTV-11-5 ch3 H H CH2Ph Et n3 F H OH H H XTV-11-6 ch3 H H CH2-indol-3-yl Et n3 F H OH H H XIV-11-7 ch3 H H CH2CH2SCH3 Et n3 F H OH H H XIV-11-8 i n ch3 31) t'-·- ♦ H * Et n3 F H OH H H *R2 and R·30 joined together by (CH2)3 to form five-membered ring. 2983472-1 -334- WO 2008/121634 PCT/US2008/058183

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Table XIV-12.

R1 IF -pr R3b R4 R5 R6 X V R7 Rh XTV-12-1 Et H H H Et n3 F H OH H H XiV-12-2 Et H H ch3 Et n3 F H OH H H XIV-12-3 Et H H CH(CH3)2 Et n3 F H OH H H XIV-12-4 Et H H CH2CH(CH3)2 Et n3 F H OH H H XIV-12-5 Et H H CH2Ph Et n3 F H OH H H XIV-12-6 Et H H CH2-indol-3-yl Et n3 F H OH H H XTV-12-7 Et H H CH2CH2SCH3 Et n3 F H OH H H XIV-12-8 Et * H * Et n3 F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIV-13.

Xs R1 RJ if’ r R4 Rs R6 X Y R' if XTV-13-1 'Pr H H H Et n3 F H OH H H XIV-13-2 jPr H H ch3 Et n3 F H OH H H XTV-13-3 ‘Pr H H CH(CH3)2 Et n3 F H OH H H XIV-13-4 'Pr H H CH2CH(CH3)2 Et n3 F H OH H H XIV-13-5 ‘Pr H H CH2Ph Et n3 F H OH H H XTV-13-6 ‘Pr H H CH2-indol-3-yl Et n3 F H OH H H XIV-13-7 ‘Pr H H CH2CH2SCH3 Et n3 F, H OH H H XIV-13-8 'Pr * H * Et n3 F H OH H H ♦R2 and RJb joined together by (0¾¼ to form five-membered ring. 5 Table XIV-14. I"·1 "7Γ — —— HL — - '"'"Τ' '' fl

X« R1 RJ R3a R3b R4 R5 R6 X Y if R“ XIV-14-1 lBu H H H Et n3 F H OH H H XIV-14-2 'Bu H H CH3 Et n3 F H OH H H XTV-14-3 'Bu H H CH(CH3)2 Et n3 F H OH H H XIV-14-4 lBu H H CH2CH(CH3)2 Et n3 F H OH H H XIV-14-5 'Bu H H CH2Ph Et n3 F H OH H H XIV-14-6 'Bu H H CH2-indol-3-yl Et n3 F H OH H H XIV-14-7 'Bu H H CH2CH2SCH3 Et n3 F H OH H H XIV-14-8 'Bu * H ♦ Et n3 F H OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -335- WO 2008/121634

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Table XIV-15.

M R1 IF "R35 R4 Rs R6 X Y R7” R8 XIV-15-1 Ph H H H Et n3 F H OH H H XIV-15-2 Ph H H ch3 Et n3 F H OH H H X1V-15-3 Ph H H CH(CH3)2 Et n3 F H OH H H XIV-15-4 Ph H H CH2CH(CH3)2 Et n3 F H OH H H XIV-15-5 Ph H H CH2Ph Et n3 F H OH H H XIV-t5-6 Ph H H CH2-indol-3-yl Et n3 F H OH H H XIV-15-7 Ph H H CH2CH2SCH3 Et n3 F H OH H H XIV-15-8 Ph * H ♦ Et n3 F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIV-16.

X2 R’ R2 R38 R3b ΊΓ ΊΤ R* X Y ίΓ R11 XIV-16-1 p-Me-Ph H H H Et n3 F H OH H H XIV-16-2 p-Me-Ph H H CH3 Et n3 F H OH H H XIV-16-3 p-Me-Ph H H CHCCHjh Et n3 F H OH H H XIV-16-4 p-Me-Ph H H CH2CH(CH3)2 Et n3 F H OH H H XIV-16-5 p-Me-Ph H H CH2Ph Et n3 F H OH H H XIV-16-6 p-Me-Ph H H CH2-indol-3-yl Et n3 F H OH H H XIV-16-7 p-Me-Ph H H CH2CH2SCH3 Et n3 F H OH H H XIV-16-8 p-Me-Ph * H * Et n3 F H OH H H *R2 and R3b joined together by (Cl-hb to form five-membered ring. 5 TableXlV-17.

1 ..... 1 - H "· «J · 'IL" 1 > £ " " ~1 R ' - B

Xs R1 R2 r3. R3b R4 Rs R6 X Y R’ XIV-17-1 p-F-Ph H H H Et n3 F H OH H H XIV-17-2 p-F-Ph H H CH3 Et n3 F H OH H H XIV-17-3 p-F-Ph H H CH(CH3)2 Et n3 F H OH H H XIV-17-4 p-F-Ph H H CH2CH(CH3)2 Et n3 F H OH H H XIV-17-5 p-F-Ph H H CH2Ph Et n3 F H OH H H XTV-17-6 p-F-Ph H H CH2-indol-3-yl Et n3 F H OH H H XTV-.17-7 p-F-Ph H H CH2CH2SCH3 Et n3 F H OH H H XIV-17-8 -Τϊ7 p-F-Ph 3b !" i J * H ♦ Et n3 F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -336- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XIV-18.

Ns R1 R2 R^ F TT R5 R4 X Y R7 R8 XIV-18-1 p-CI-Ph H H H Et n3 F H OH H H XIV-18-2 p-Cl-Ph H H CHj Et n3 F H OH H H XIV-18-3 p-Cl-Ph H H CH(CH3)2 Et n3 F H OH H H XIV-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et n3 F H OH H H XIV-18-5 p-Cl-Ph H H CH2Ph Et n3 F H OH H H X1V-18-6 p-Cl-Ph H H CH2-indol-3-yl Et n3 F H OH H H XIV-18-7 p-CI-Ph H H CH2CH2SCH3 Et n3 F H OH H H X1V-18-8 p-Cl-Ph * H * Et n3 F H OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XIV-19.

Ns r‘ R2 R3’ -pg R4 R3 R6 X Y fU R8 XIV-19-1 p-Br-Ph H H H Et n3 F H OH H H XIV-19-2 p-Br-Ph H H ch3 Et n3 F H OH H H XIV-19-3 p-Br-Ph H H CH(CH3)2 Et n3 F H OH H H XIV-19-4 p-Br-Ph H H CH2CH(CH3)2 Et n3 F H OH H H XIV-19-5 p-Br-Ph H H CH2Ph Et n3 F H OH H H XIV-19-6 p-Br-Ph H H CH2-indol-3-yl Et n3 F H OH H H XIV-19-7 p-Br-Ph H H CH2CH2SCH3 Et n3 F H OH H H XIV-19-8 p-Br-Ph * H ♦ Et n3 F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XIV-20.

1 R· ' »IL " J ’/g” !'"2~ '"Τ’"- 2 ' "R — P

Ns R1 R2 R3’ R3b R4 Rs R6 X Y R’ R" XIV-20-1 p-I-Ph H H H Et n3 F H OH H H XIV-20-2 p-I-Ph H H CH3 Et n3 F H OH H H XTV-20-3 p-I-Ph H H CHCCHjH Et n3 F H OH H H XIV-20-4 p-I-Ph H H CH2CH(CH3)2 Et n3 F H OH H H XTV-20-5 p-I-Ph H H CH2Ph Et n3 F H OH H H XTV-20-6 p-I-Ph H H CH2-indol-3-yl Et n3 F H OH H H XIV-20-7 p-I-Ph H H CH2CH2SCH3 Et n3 F H OH H H XTV-20-8 • p-I-Ph ♦ H ♦ Et n3 F H OH H H *R2 and RJt> joined together by (CH2)3 to form five-membered ring. 2983472-1 -337- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XIV-21.

Ns R1 R2 R31 “r36 ΊΤ “iF R6 X Y R7 R8 xrv-2i-i ch3 H H H 'Pr n3 F H OH H H XIV-21-2 ch3 H H ch3 iPr n3 F H OH FI H XIV-21-3 ch3 H H CH(CH3)2 ipr n3 F H OH H ' H XIV-21-4 ch3 H H CH2CH(CH3)2 'Pr n3 F H OH H H XIV-21-5 ch3 H H CH2Ph iPr n3 F H OH H H XTV-21-6 ch3 H H CH2-indol-3-yl ‘Pr n3 F H OH H H XFV-21-7 ch3 H H CH2CH2SCH3 ipr n3 F H OH H H XIV-21-8 ch3 ♦ H * 'Pr n3 F H OH H H *R2 and Rejoined together by (ΟΗ2)3 to form five-membered ring.

Table XIV-22.

Ns R2 R3" R3b R4- R3 R6 X Y R R8 XIV-22-1 Et H H H ‘Pr n3 f H OH H H XrV-22-2 Et H H CH3 'Pr n3 f H OH H H XIV-22-3 Et H H CH(CH3)2 Tr n3 f H OH H H XIV-22-4 Et H H CH2CH(CH3)2 ‘Pr n3 f H OH H H XIV-22-5 Et H H CH2Ph 'Pr n3 f H OH H H XIV-22-6 Et H H CH2-indol-3-yl 'Pr n3 f H OH H H XIV-22-7 Et H H CH2CH2SCH3 'Pr n3 f H OH H H XIV-22-8 Et + H * 'Pr n3 f H OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring. Table XIV-23. Ns R R2 R3r “δ35 pT~ RJ R6 X Y R7 R8 XIV-23-1 Pr H H H 'Pr n3 f H OH H H XIV-23-2 Pr H H CH3 'Pr n3 f H OH H H XIV-23-3 Pr H H CH(CH3)2 'Pr n3 f H OH H H XIV-23-4 Pr H H CH2CH(CH3)2 'Pr n3 f H OH H H XIV-23-5 Pr H H CH2Ph ‘Pr n3 f H OH H H XIV-23-6 Pr H H CH2-indol-3-yI 'Pr n3 f H OH H H XIV-23-7 Pr H H CH2CH2SCH3 'Pr n3 f H OH H H XIV-23-8 Pr * H ♦ 'Pr n3 f H OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -338 - WO 2008/121634 PCT/US20O8/OS8183

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Table XIV-24.

x° R1 R2 jF ΊΓ“ R4 R6 X Y R; R8 XIV-24-1 ‘Bu H H H 'Pr n3 F H OH H H X1V-24-2 ’Bu H H ch3 iPr n3 F H OH H H XIV-24-3 ’Bu H H CH(CH3)2 ’Pr n3 F H OH H H XIV-24-4 lBu H H CH2CH(CH3)2 'Pr n3 F H OH H H XIV-24-5 ’Bu H H CH2Ph ’Pr n3 F H OH H H XIV-24-6 ’Bu H H CH2-indol-3-yl ‘Pr n3 F H OH H H XTV-24-7 ’Bu H H CHaCH2SCH3 'Pr n3 F H OH H H XTV-24-8 'Bu * H * iPr n3 F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIV-25.

X° R ic R3a R3b R R5 R6 X Y R R8 XTV-25-1 Ph H H H ‘Pr n3 F H OH H H X1V-25-2 Ph H H ch3 ‘Pr n3 F H OH H H XIV-25-3 Ph H H CHiCH^ 'Pr n3 F H OH H H XTV-25-4 Ph H H CH2CH(CH3h ipr n3 F H OH H H XIV-25-5 Ph H H CH2Ph ipr n3 F H OH H H XIV-25-6 Ph H H CH2-indol-3-yl ipr n3 F H OH H H XIV-25-7 Ph H H CH2CH2SCH3 ipr n3 F H OH H H XIV-25-8 Ph "3FT-· ♦ H * ipr n3 F H OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XIV-26.

1 1 >^·· " H "1 ' ---— . R'B

Xa R1 R2 -^35- T* R4 Rs R6 X Y r’ R8 XIV-26-1 p-Me-Ph H H H 'Pr n3 F H OH H H XTV-26-2 p-Me-Ph H H CH3 'Pr n3 F H OH H H X1V-26-3 p-Me-Ph H H CH(CH3)i ’Pr n3 F H OH II H XIV-26-4 p-Me-Ph H H CH2CH(CH3)2 ipr n3 F H OH H H XIV-26-5 p-Me-Ph H H CH2Ph ipr n3 F H OH H H XIV-26-6 p-Me-Ph H H CH2-indol-3-yl ipr n3 F H OH H H XIV-26-7 p-Me-Ph H H CH2CH2SCH3 ’Pr n3 F H OH H H XIV-26-8 —Tv: p-Me-Ph 3bI jT: * H 4 ’Pr n3 F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -339- wo 2008/121634 PCT/US2008/058183

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Table X1V-27.

Xs R1 R3 R3fl R3b R4 Rs R* X Y R7 iv XrV-27-ί p-F-Ph H H H 'Pr n3 F H OH H H XIV-27-2 p-F-Ph H H ch3 ipr n3 F H OH H H XIV-27-3 p-F-Ph H H CH(CH3)2 ‘Pr n3 F H OH H H XIV-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr n3 F H OH H H XTV-27-5 p-F-Ph H H CH2Ph iPr N3 F H OH H H XIV-27-6 p-F-Ph H H CH2-indol-3-yl ipr n3 F H OH H H XIV-27-7 p-F-Ph H H CH2CH2SCH3 ipr n3 F H OH H H XIV-27-8 p-F-Ph * H * ipr n3 F H OH H H *RZ and RJb joined together by (CHhb to form five-membered ring.

Table XIV-28. X° R1 R3 RJa R3b R4 RJ r6 X Υ R' R* XIV-28-1 p-Cl-Ph H H H 'Pr n3 F Η ΟΗ Η Η XIV-28-2 p-Cl-Ph H H ch3 ipr n3 F Η ΟΗ Η Η XIV-28-3 p-CI-Ph H H CH(CH3)2 ipr n3 F Η ΟΗ Η Η XIV-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr n3 F Η ΟΗ Η Η XIV-28-5 p-Cl-Ph H H CH2Ph ipr n3 F Η ΟΗ Η Η XIV-28-6 p-Cl-Ph H H CH2-indol-3-yl ipr n3 F Η ΟΗ Η Η XIV-28-7 p-Cl-Ph H H ch2ch2sch3 ‘Pr n3 F Η ΟΗ Η Η XIV-28-8 p-Ci-Ph * H * ‘Pr n3 F Η ΟΗ Η Η ♦R'4 and RJb joined together by (Cflhb to form five-membered ring. 5 Table XIV-29. ' *ν ..J g --, --, a-- Χ° R* R2 R3a TP5 R4 Rs R6 X Υ R7 R* XIV-29-1 p-Br-Ph H H H 'Pr n3 F Η ΟΗ Η Η XIV-29-2 p-Br-Ph H H ch3 'Pr n3 F Η ΟΗ Η Η XIV-29-3 p-Br-Ph H H CH(CH3)i 'Pr n3 F Η ΟΗ Η Η XIV-29-4 p-Br-Ph H H CH2CH(CH3)2 ‘Pr n3 F Η ΟΗ Η Η XIV-29-5 p-Br-Ph H H CH2Ph 'Pr n3 F Η ΟΗ Η Η XTV-29-6 ' p-Br-Ph H H CH2-indol-3-yl 'Pr n3 F Η ΟΗ Η Η XIV-29-7 p-Br-Ph H H ch2ch2sch3 'Pr n3 F Η ΟΗ Η Η XIV-29-8 p-Br-Ph * H * 'Pr n3 F Η ΟΗ Η Η *RZ and RJb joined together by (CHib to form five-membered ring. 2983472-1 -340- WO 2008/121634

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Table XIV-30.

VkDI

Xs Rl TF -£3T “r3® R4 Rs R6 X Y R7 R“ XIV-30-1 p-I-Ph H H H ;Pr n3 F H OH H H XIV-30-2 p-I-Ph H H ch3 'Pr n3 F H OH H H XIV-30-3 p-I-Ph H H CH(CH3)2 'Pr n3 F H OH H H XJV-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr n3 F H OH H H XIV-30-5 p-I-Ph H H CH2Ph fPr n3 F H OH H H XIV-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr n3 F H OH H H XIV-30-7 p-I-Ph H H CH2CH2SCH3 'Pr n3 F H OH H H XIV-30-8 p-I-Ph Jb·-. * H * 'Pr n3 F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIV-31. X° Rl R2 ηρτ R3b R4 R5 R6 X Υ R7 R* XIV-31-1 CH3 Η H H "Bu n3 F H ΟΗ Η Η XIV-31-2 ch3 H H ch3 "Bu n3 F H ΟΗ Η Η XIV-31-3 ch3 Η H CH(CH3)2 "Bu n3 F H ΟΗ Η Η XIV-31-4 ch3 H H CH2CH(CH3)2 "Bu n3 F H ΟΗ Η Η XIV-31-5 ch3 H H CH2Ph "Bu n3 F Η ΟΗ Η Η XIV-31-6 ch3 H H CH2-indol-3-yl "Bu n3 F Η ΟΗ Η Η XIV-31-7 ch3 H H ch2ch2sch3 "Bu n3 F Η ΟΗ Η Η XIV-31-8 ch3 * H * "Bu n3 F Η ΟΗ Η Η *R2 and R31* joined together by (CHafc to form five-membered ring. 5 Table XIV-32. 11 - » "I " R R- SL”- ' . J - < JL" -- ' "

X® R RJ R3’ R3” R4 R6 X Y R' Ra XIV-32-1 Et H H H "Bu n3 F H OH H H XIV-32-2 Et H H CH3 "Bu n3 F H OH H H XIV-32-3 Et H H CH(CH3)2 "Bu n3 F H OH H H XIV-32-4 Et H H CH2CH(CH3)2 "Bu n3 F H OH H H XIV-32-S Et H H CH2Ph "Bu n3 F H OH H H XIV-32-6 Et H H CH2-indol-3-yl "Bu n3 F H OH H H XIV-32-7 Et H H CH2CH2SCH3 "Bu n3 F H OH H H XIV-32-8 Et * H * "Bu n3 F H OH H H *R2 and RJb joined together by (CHa}j to form five-membered ring. 2983472-1 341- WO 2008/121634 PCT/US2008/058183

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Table XIV-33.

Ko R1 RJ R3b R4 RJ X Y i? R8 XIV-33-1 ’Pr H H H "Bu n3 F H OH H H XIV-33-2 ‘Pr H H ch3 "Bu n3 F H OH H H XIV-33-3 ‘Pr H H CH(CH3)2 "Bu n3 F H OH H H XTV-33-4 ’Pr H H CH2CH(CH3)2 "Bu n3 F H OH H H XIV-33-5 ipr H H CH2Ph "Bu n3 F H OH H H XIV-33-6 ipr H H CHrindol-3-yI "Bu n3 F H OH H H XIV-33-7 ipr H H CH2CH2SCH3 "Bu n3 F H OH H H XIV-33-8 ipr * H * "Bu n3 F H OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XIV-34.

X° R R2 RJ. R3b R4 Rs R6 X Y R' R8 XIV-34-1 lBu H H H "Bu n3 F H OH H H XIV-34-2 ‘Bu H H ch3 "Bu n3 F H OH H H XTV-34-3 ‘Bu H H CH(CH3)2 "Bu n3 F H OH H H XIV-34-4 ‘Bu H H CH2CH(CH3)j "Bu n3 F H OH H H XIV-34-5 ‘Bu H H CH2Fh "Bu n3 F H OH H H XIV-34-6 ‘Bu H H CH2-indoI-3-yl "Bu n3 F H OH H H XIV-34-7 ‘Bu H H ch2ch2sch3 "Bu n3 F H OH H H XIV-34-8 ‘Bu + H * "Bu n3 F H OH H H *R2 and Rejoined together by (Clfcb to form five-membered ring. 5 Table XIV-35. ,. — , H— HH—, I I·— -- - I,— · Μ Ή

Xs R ΊΓ RJa R3b R4 R5 R6 X Y R7 R8 XIV-35-1 Ph H H H "Bu n3 F H OH H H XTV-35-2 Ph H H ch3 "Bu n3 F H OH H H XTV-35-3 Ph H H ΟΗ(ΟΗ3)3 "Bu n3 F H OH H H XTV-35-4 Ph H H ch2ch(ch3)3 "Bu n3 F H OH H H XIV-35-5 Ph H H CH2Ph "Bu n3 F H OH H H XIV-35-6 Ph H H CH2-indol-3-yl "Bu n3 F H OH H H X1V-35-7 Ph H H CH2CH2SCH3 "Bu n3 F H OH H H XIV-35-8 Ph * H * "Bu n3 F H OH H H *R7 and joined together by (CH2)3 to form five-membered ring. 2983472-1 -342- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU I

Table XIV-36.

Ns R1 R2 'r35 R3b R4 R6 X Y IV R“ XIV-36-1 p-Me-Ph H H H "Bu n3 F H OH H H XJV-36-2 p-Me-Ph H H ch3 "Bu n3 F H OH H H XIV-36-3 p-Me-Ph H H CH(CH3)2 "Bu n3 F H OH H H XiV-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu n3 F H OH H H XIV-36-5 p-Me-Ph H H CH2Ph "Bu n3 F H OH H H XIV-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu n3 F H OH H H XIV-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu n3 F H OH H H XTV-36-8 i τί p-Me-Ph * H * "Bu n3 F H OH H H *RZ and Rejoined together by (CH2)3 to form five-membered ring.

Table XIV-37. Τϊλ D'

Ns R’ R2 R3a R38 R5 R^ X Y R7- R8 XIV-37-1 p-F-Ph H H H "Bu n3 F H OH H H XIV-37-2 p-F-Ph H H ch3 "Bu n3 F H OH H H XJV-37-3 p-F-Ph H H CH(CH3)a "Bu n3 F H OH H H XIV-37-4 p-F-Ph H H CHjCHCCH^ "Bu n3 F H OH H H XIV-37-5 p-F-Ph H H CH2Ph "Bu n3 F H OH f H H XIV-37-6 p-F-Ph H H CH2-indol-3-yl "Bu n3 F H OH H H XIV-37-7 p-F-Ph H H CH2CH2SCH3 "Bu n3 F H OH H H XIV-37-8 p-F-Ph * H * "Bu n3 F H OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. Table XIV-38. ~Ni R1 R2 “R37 R3b R4 R5 R6 X Y r’ r“ XIV-38-1 p-Cl-Ph H H H "Bu n3 F H OH H H XIV-38-2 p-Cl-Ph H H CH3 "Bu n3 F H OH H H XIV-38-3 p-Cl-Ph H H CH(CH3)2 "Bu n3 F H OH H H XIV-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu n3 F H OH H H XIV-38-5 p-Cl-Ph H H CH2Ph "Bu n3 F H OH H H X1V-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu n3 F H OH H H XIV-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu n3 F H OH H H XIV-38-8 p-Cl-Ph * H * "Bu n3 F H OH H H ♦R2 and RJb joined together by (CH2)3 to form five-membered ring. Table X1V-39. R1 R2 R3' “R313 R4 R3 R* X Y R7 R8 2983472-1 -343 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Ns R1 RJ iVa R3b R4 R6 X Y R7 Rm XIV-39-1 p-Br-Ph H H H "Bu n3 F H OH H H XIV-39-2 p-Br-Ph H H ch3 "Bu n3 F H OH H H XTV-39-3 p-Br-Ph H H CH(CH3)2 "Bu n3 F H OH H H XIV-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu n3 F H OH H H XIV-39-5 p-Br-Ph H H CH2Ph "Bu n3 F H OH H H XIV-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu n3 F H OH H H XIV-39-7 p-Br-Ph H H CH2CH2SCH3 "Bu n3 F H OH H H XIV-39-8 p-Br-Ph + H * "Bu n3 F H OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XIV-40.

Ns R‘ R2 R3b RJ R6 X Y r’ R8 XIV-40-1 p-l-Ph H H H "Bu n3 F H OH H H XIV-40-2 p-I-Ph H H CH3 "Bu n3 F H OH H H XIV-40-3 p-I-Ph H H ΟΗ(ΟΗ3)2 "Bu n3 F H OH H H xrv-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu n3 F H OH H H XIV-40-5 p-I-Ph H H CH2Ph "Bu n3 F H OH H H XIV-40-6 p-I-Ph H H CH2-indol-3-yI "Bu n3 F H OH H H XIV-40-7 p-I-Ph H H CH2CH2SCH3 "Bu n3 F H OH H H XIV-40-8 “Ϊ7Π-TT p-I-Ph ♦ H ♦ "Bu n3 F H OH H H *R2 and R3b joined together by (Cl·^ to form five-membered ring.

Table XIV-41.

Ns R1 -rI- -r3T R3b R4 "R5" R6 X Y R7 R# XIV-41-1 ch3 Η H Η Bz n3 F H OH H H XIV-41-2 ch3 H H CH3 Bz n3 F H OH H H XTV-41-3 ch3 H Η CH(CH3)2 Bz n3 F H OH H H XIV-41-4 ch3 H H CH2CH(CH3)2 Bz n3 F H OH H H XTV-41-5 CH3 H Η CH2Ph Bz n3 F H OH H H XIV-41-6 ch3 Η Η CH2-indol-3-yl Bz n3 F H OH H H XIV-41-7 ch3 H Η ch2ch2sch3 Bz n3 F H OH H H XIV-41-8 ch3 * Η * Bz n3 F H OH H H 5 *R2 and Rejoined together by (CFhfe to form five-membered ring.

29S3472.J -344- WO 2008/121634

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Table XI V-42.

Xs r' R2 rJ. -rTB Rs R6 X Y R7" r“ XIV-42-1 Et H H H Bz n3 F H OH H H XIV-42-2 Et H H ch3 Bz n3 F H OH H H XIV-42-3 Et H H CH(CH3)2 Bz n3 F H OH H H XIV-42-4 Et H H CH2CH(CH3)2 Bz n3 F H OH H H XIV-42-5 Et H H CH2Ph Bz n3 F H OH H H XTV-42-6 Et H H CH2-indol-3-yl Bz n3 F H OH H H XIV-42-7 Et H H ch2ch2sch3 Bz n3 F H OH H H X1V-42-8 Et * H * Bz n3 F H OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XIV-43,

Tk n1

Xs R R2 R3" R3b R^ RJ R6 X Y R7 R“ XTV-43-1 ‘Pr H H H Bz n3 F H OH H H XIV-43-2 ‘Pr H H ch3 Bz n3 F H OH H ί XIV-43-3 'Pr H H CH(CH3)2 Bz n3 F H OH H H XIV-43-4 ipr H H CH2CH(CH3)2 Bz n3 F H OH H H XTV-43-5 Tr H H. CH2Ph Bz n3 F H OH H H XIV-43-6 'Pr H H CH2-indol-3-yl Bz n3 F H OH H H XTV-43-7 ‘Pr H H CH2CH2SCH3 Bz n3 F H OH H H XIV-43-8 ipr * H ♦ Bz n3 F H OH H H 10 *R2 and R3b joined together by (0¾¼ to form five-membered ring.

Table XIV-44.

Xs R1 RJ R3> -r3B R4 RJ R6 X Y R7 Ru XIV-44-1 ‘Bu H H H Bz n3 F H OH H H XTV-44-2 lBu H H CH3 Bz n3 F H OH H H XIV-44-3 ‘Bu H H CH(CH3b Bz n3 F H OH H H XIV-44-4 'Bu H H CH2CH(CH3)2 Bz n3 F H OH H H XIV-44-5 lBu H H CH2Ph Bz n3 F H OH H H XTV-44-6 lBu H H CH3-indol-3-yl Bz n3 F H OH H H XTV-44-7 lBu H H CH2CH2SCH3 Bz n3 F H OH H H xrv-44-8 *·η2 'Ί π 'Bu 3B * H * Bz n3 F H OH H H ♦R2 and RJb joined together by (CHa)3 to form five-membered ring. 2983472-1 -345 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XIV-45.

Ns R1 RJ R3a R3b R4 Rs X Y r7 X1V-45-1 Ph H H H Bz n3 F H OH H H XIV-45-2 Ph H H ch3 Bz n3 F H OH H H XIV-45-3 Ph H H CH(CH3)2 Bz n3 F H OH H H XIV-45-4 Ph H H CH2CH(CH3)2 Bz n3 F H OH H H XIV-45-5 Ph H H CH2Ph Bz n3 F H OH H H XTV-45-6 Ph H H CH2-indol-3-yl Bz n3 F H OH H H XIV-45-7 Ph H H CH2CH2SCH3 Bz n3 F H OH H H XIV-45-8 - . Ph Jb · ϊ * H * Bz n3 F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIV-46.

Ns R1 R3 “R3” 1 R3b r3 r6 X Y R7 RB XIV-46-1 p-Me-Ph H H H Bz n3 F H OH H H XIV-46-2 p-Me-Ph H H ch3 Bz n3 f H OH H H XIV-46-3 p-Me-Ph H H CH(CH3)2 Bz n3 f H OH H H XJV-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz n3 f H OH H H XIV-46-5 p-Me-Ph H H CH2Ph Bz n3 f H OH H H XIV-46-6 p-Me-Ph H H CH2-indol-3-yl Bz n3 f H OH H H XIV-46-7 p-Me-Ph H H ch2ch2sch3 Bz n3 f H OH H H XIV-46-8 p-Me-Ph * H * Bz n3 f H OH H H *R2 and R3” joined together by (CH2)3 to form five-membered ring. Table XIV-47. Ns R1 RJ R3· pE R4 r5 R6 X Y R7 R“ XIV-47-1 p-F-Ph H H H Bz n3 f H OH H H XTV-47-2 p-F-Ph H H ch3 Bz n3 f H OH H H XIV-47-3 p-F-Ph H H CH(CHj)2 Bz n3 f H OH H H XIV-47-4 p-F-Ph H H CH2CH(CH3)2 Bz n3 f H OH H H XIV-47-5 p-F-Ph H H CH2Ph Bz n3 f H OH H H XIV-47-6 p-F-Ph H H CH2-indol-3-yl Bz n3 f H OH H H XTV-47-7 p-F-Ph H H CH2CH2SCH3 Bz n3 f H OH H H XIV-47-8 p-F-Ph * H * Bz n3 f H OH H H *R2 and joined together by (CH2)3t0 form five-membered ring. 29834724 -346- WO 2008/121634

Docket No. 60137.0034WOU 1 PCT/US2008/058183

Table XIV-48.

R1 R3 R3a R4 Rs Rfc X Y R’ Rh XIV-48-1 p-Cl-Ph H H H Bz n3 F H OH H H XIV-48-2 p-Cl-Ph H H ch3 Bz n3 F H OH H H XIV-48-3 p-CI-Ph H H CHCCHjX Bz n3 F H OH H H XIV-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz n3 F H OH H H XIV-48-5 p-Cl-Ph H H CH2Ph Bz n3 F H OH H H XIV-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz n3 F H OH H H XIV-48-7 p-CI-Ph H H CH2CH2SCH3 Bz n3 F H OH H H XIV-48-8 - '"77 p-Cl-Ph ,3b: : ♦ H * Bz n3 F H OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XIV-49.

Ife R1 R2 “r31 Rib R4 "ΊΓ r6 X Y T RH XIV-49-1 p-Br-Ph H H H Bz n3 F H OH H H XIV-49-2 p-Br-Ph H H ch3 Bz n3 F H OH H H XIV-49-3 p-Br-Ph H H CH(CH3)2 Bz n3 F H OH H H X1V-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz n3 F H OH H H XIV-49-5 p-Br-Ph H H CH2Ph Bz n3 F H OH H H XIV-49-6 p-Br-Ph H H CH2-indol-3-yl Bz n3 F H OH H H XIV-49-7 p-Br-Ph H H CH2CH2SCH3 Bz n3 F H OH H H XIV-49-8 p-Br-Ph * H * Bz n3 F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. Table XIV-50. Xa Rl R2 R3* "r35 R4 r! R6 X Y R’ Ru XIV-50-1 p-I-Ph H H H Bz n3 F H OH H H XIV-50-2 p-I-Ph H H ch3 Bz n3 F H OH H H XIV-50-3 p-I-Ph H H CH(CH3)2 Bz n3 F H OH H H XTV-50-4 p-I-Ph H H CH2CH(CH3)2 Bz n3 F H OH H H XIV-50-5 p-I-Ph H H CH2Ph Bz n3 F H OH H H XIV-50-6 p-I-Ph H H CH2-indol-3-yl Bz n3 F H OH H H XIV-50-7 p-I-Ph H H CH2CH2SCH3 Bz n3 F H OH H H XIV-50-8 p-I-Ph T»3b ! ! j" « H * Bz n3 F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -347- WO 2008/121634 PCT/US2008/058183

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XV

Table XV-1.

Na r' ΊΓ ηρτ R3b V” IF R6 X Y R7 R# XV-1-1 ch3 H H H ch3 F F H OH H H XV-1-2 ch3 H H ch3 ch3 F F H OH H H XV-1-3 ch3 H H CH(CH3)2 ch3 F F H OH H H XV-1-4 ch3 H H CH2CH(CH3)2 ch3 F F H OH H H XV-1-5 ch3 H H CH2Ph ch3 F F H OH H H XV-1-6 ch3 H H CH2-indol-3-yl ch3 F F H OH H H XV-1-7 ch3 H H CH2CH2SCH3 ch3 F F H OH H H XV-1-8 J ch3 * H ♦ ch3 F F H OH H H *R7 and Rejoined together by (CFhb to form five-membered ring?

N° R’ R2 R3i -r3E R4 Rs Rfi X Y R7 Ra XV-2-1 Et H H H ch3 F F H OH H H XV-2-2 Et H H ch3 ch3 F F H OH H H XV-2-3 Et H H CH(CH3)2 ch3 F F H OH H H XV-2-4 Et H H CH2CH(CH3)2 ch3 F F H OH H H XV-2-5 Et H H CH2Ph ch3 F F H OH H H XV-2-6 Et H H CH2-indol-3-yl ch3 F F H OH H H XV-2-7 Et H H CH2CH2SCH3 ch3 F F H OH H H XV-2-8 Et * H * ch3 F F H OH H H ♦R7 and Rejoined together by (CH2)3 to form five-membered ring. 2943472-1 -348- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XV-3.

Xa R1 R3 -£ΠΓ Rjb R4 R3 R6 X Y R1 r“ XV-3-1 'Pr H H H ch3 F F H OH H H XV-3-2 'Pr H H ch3 ch3 F F H OH H H XV-3-3 'Pr H H CH(CH3)2 ch3 F F H OH H H XV-3-4 'Pr H H CH2CH(CH3)2 ch3 F F H OH H H XV-3-5 /Pr H H CH2Ph ch3 F F H OH H H XV-3-6 'Pr H H CH2-indol-3-yl ch3 F F H OH H H XV-3-7 'Pr H H CH2CH2SCH3 ch3 F F H OH H H XV-3-8 'pr * H ♦ ch3 F F H OH H H *R2 and RJb joined together by"(CH2b to form five-membered ring.

Table XV-4.

Xa R R1 R3" R3b R4 R3 R6 X Y R7 Rtt XV-4-1 'Bu H H H ch3 F F H OH H H XV-4-2 'Bu H H ch3 ch3 F F H OH H H XV-4-3 'Bu H H CH(CH3)2 ch3 F F H OH H H XV-4-4 'Bu H H CH2CH(CH3)2 ch3 F F H OH H H XV-4-5 'Bu H H CH2Ph ch3 F F H OH H H XV-4-6 'Bu H H CH2-indoJ-3-yl ch3 F F H OH H H XV-4-7 'Bu H H CH2CH2SCH3 ch3 F F H OH H H XV-4-8 'Bu ♦ H * ch3 F F H OH H H *RX and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XV-5.

Xa R R2 r3. R3b R^ R3 R6 X Y r" R" XV-5-1 Ph H H H CH3 F F Η OH H H XV-5-2 Ph H H ch3 ch3 F F H OH H H XV-5-3 Ph H H CH(CH3)2 ch3 F F H OH H H XV-5-4 Ph H H CH2CH(CH3)2 ch3 F F H OH H H XV-5-5 Ph H H CH2Ph ch3 F F H OH H H XV-5-6 Ph H H CHrindol-3-yl ch3 F F H OH H H XV-5-7 Ph H H CH2CH2SCH3 ch3 F F H OH H H XV-5-8 ” Ϊ Ph Tv3b · * H ♦ ch3 F F H OH H H *R2 and R3b joined together by (ΟΗ2)3 to form five-membered ring. 2983472-1 -349- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XV-6.

Ns r1 R3 R3a “S* r5" R6 X Y r’ R· XV-6-1 p-Me-Ph H H H ch3 F F H OH H H XV-6-2 p-Me-Ph H H ch3 ch3 F F H OH H H XV-6-3 p-Me-Ph H H CH(CH3)2 ch3 F F H OH H H XV-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 F F H OH H H XV-6-5 p-Me-Ph H H CH2Ph ch3 F F H OH H H XV-6-6 p-Me-Ph H H CH2-indol-3-yl ch3 F F H OH H H XV-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 F F H OH H H XV-6-8 p-Me-Ph r*3b · : -J * H ♦ ch3 F F H OH H H *R2 and RJb joined together by (CHzb to form five-membered ring.

Table XV-7.

Ns R1 R3 “R35 R4 Rs R6 X Υ R’ ΊΡ XV-7-1 p-F-Ph H H H ch3 F F H ΟΗ Η Η XV-7-2 p-F-Ph H H ch3 ch3 F F H ΟΗ Η Η XV-7-3 p-F-Ph H H CHCCH^ ch3 F F H ΟΗ Η Η XV-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 F F Η ΟΗ Η Η XV-7-6 p-F-Ph H H CH2Ph ch3 F F Η ΟΗ Η Η XV-7-7 p-F-Ph H H CH2-indol-3-yl ch3 F F Η ΟΗ Η Η XV-7-8 p-F-Ph H H CH2CH2SCH3 ch3 F F Η ΟΗ Η Η XV-7-20 -T p-F-Ph · · j ♦ H ♦ ch3 F F Η ΟΗ Η Η *R2 and RJb joined together by (Chfeb to form five-membered ring.

Table XV-8.

Ns R1 R3 R3b R4 Rs R6 X Y IF r“ XV-8-1 p-Cl-Ph H H H ch3 F F H OH H H XV-8-2 p-Cl-Ph H H ch3 ch3 F F Η OH H H XV-8-3 p-Cl-Ph H H CHCCHa^ ch3 F F H OH H H XV-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 F F Η OH H H XV-8-5 p-Cl-Ph H H . CH2Ph ch3 F F H OH H H XV-8-6 p-Cl-Ph H H CH2-indoI-3-yl ch3 F F Η OH H H XV-8-7 p-Ci-Ph H H ch2ch2sch3 ch3 F F H OH H H XV-8-8 “7772-7 p-Cl-Ph _ * H * ch3 F F H OH H H ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -350- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XV-9.

Ks R1 R7 R3" "R35 “ R4 R5 R6 X Y R7 R8 XV-9-1 p-Br-Ph H H H ch3 F F H OH H H XV-9-2 p-Br-Ph H H ch3 ch3 F F H OH H H XV-9-3 p-Br-Ph H H CH(CH3)2 ch3 F F H OH H H XV-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 F F H OH H H XV-9-6 p-Br-Ph H H CH2Ph ch3 F F H OH H H XV-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 F F H OH H H XV-9-8 p-Br-Ph H H ch2ch2sch3 ch3 F F H OH H H XV-9-20 —Τΐ p-Br-Ph * H * ch3 F F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XV-10.

Ns R1 R2 R3b R4 RJ R6 X Υ Tr R8 XV-10-1 p-I-Ph H H H ch3 F F H ΟΗ Η Η XV-10-2 p-I-Ph H H CH3 ch3 F F Η ΟΗ Η Η XV-10-3 p-I-Ph H H CH(CH3)2 ch3 F F H ΟΗ Η Η XV-10-4 p-I-Ph H H CH2CH(CH3)2 ch3 F F Η ΟΗ Η Η XV-10-5 p-I-Ph H H CH2Ph ch3 F F Η ΟΗ Η Η XV-10-6 p-I-Ph H H CH2-indol-3-yl ch3 F F Η ΟΗ Η Η XV-10-7 p-I-Ph H H CH2CH2SCH3 ch3 F F Η ΟΗ Η Η XV-10-8 p-I-Ph * H + ch3 F F Η ΟΗ Η Η ♦R2 and Rejoined together by (CH2)3 to form five-membered ring.

Κ2 R1 r3" R3b R4 Rs R* X Y r’ R8 XV-11-1 ch3 Η Η Η Et F F H OH H H XV-11-2 ch3 Η Η ch3 Et F F H OH H H XV-11-3 ch3 Η Η CH(CH3)2 Et F F H OH H H XV-11-4 ch3 Η Η CH2CH(CH3)2 Et F F H OH H Η XV-11-5 ch3 Η Η CH2Ph Et F F H OH H H XV-11-6 ch3 Η Η CH2-indol-3-yl Et F F H OH H H XV-11-7 ch3 Η Η CH2CH2SCH3 Et F F H OH H H XV-11-8 J τ ch3 ,3b·!. « Η * Et F F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -351 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XV-12.

No Rl R2 R3a "r35 R4 R1 R6 X Y r" Rb XV-12-1 Et H H H Et F F H OH H H XV-12-2 Et H H ch3 Et F F H OH H H XV-12-3 Et H H CH(CH3)2 Et F F H OH H H XV-12-4 Ef H H CH2CH(CH3)2 Et F F H OH H H XV-12-5 Et H H CH2Ph Et F F H OH H H XV-12-6 Et H H CHrindol-3-yl Et F F H OH H H XV-12-7 Et H H CH2CH2SCH3 Et F F H OH H H XV-12-8 Et ♦ H ♦ Et F F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XV-13.

Na Iv R4 Rj« R3b R4 R3 R6 X Y R' R’ XV-13-1 ’Pr H H H Et F F H OH H H XV-13-2 'Pr H H ch3 Et F F H OH H H XV-13-3 ipr H H CH(CH3)2 Et F F H OH H H XV-13-4 'Pr H H CH2CH(CH3)2 Et F F H OH H H XV-13-5 'Pr H H CH2Ph Et F F H OH H H XV-13-6 /pr H H CH2-indol-3-yl Et F F H OH H H XV-13-7 fPr H H CH2CH2SCH3 Et F F H OH H H XV-13-8 'Pr i3b · + H * Et F F H OH H H *RZ and RJ&amp; joined together by (CH^ to form five-membered ring. 5 Table XV-14.

......." > I .....R PH.™—1"HL— — I '""'R "U

Ns Rl “R3- -jps- “5* R4 Rs R6 X Y V R8 XV-14-1 'Bu H H H Et F F H OH H ' H XV-14-2 'Bu H H ch3 Et F F H OH H H XV-14-3 'Bu H H CH(CH3)2 Et F F H OH H H XV-14-4 'Bu H H CH2CH(CH3)2 Et F F H OH H H XV-14-5 'Bu H H CH2Ph Et F F H OH H H XV-14-6 feu H H CH2-indol-3-yI Et F F H OH H H XV-14-7 'Bu H H ch2ch2sch3 Et F F H OH H H XV-14-8 'Bu * H * Et F F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -352- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XV-15.

N« Rl Έ r3b R4 R5 R X Y r Ra XV-15-1 Ph H H H Et F F H OH H H XV-15-2 Ph H H ch3 Et F F H OH H H XV-15-3 Ph H H CH(CH3)2 Et F F H OH H H XV-15-4 Ph H H CH2CH(CH3)2 Et F F H OH H H XV-15-5 Ph H H CH2Ph Et F F H OH H H XV-15-6 Ph H H CHrindol-3-yl Et F F H OH H H XV-15-7 Ph H H ch2ch2sch3 Et F F H OH H H XV-15-8 J Ύ Ph * H * Et F F H OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XV-16.

Ns R’ Ί?’ R3’ Ί&amp;Γ R3 R6 X Y R Rtt XV-16-1 p-Me-Ph H H H Et F F H OH H H XV-16-2 p-Me-Ph H H CH3 Et F F H OH H H XV-16-3 p-Me-Ph H H CH(CH3)2 Et F F H OH H H XV-16-4 p-Me-Ph H H ΟΗ2ΟΗ(ΟΗ3)2 Et F F H OH H H XV-16-5 p-Me-Ph H H CH2Ph Et F F H OH H H XV-16-6 p-Me-Ph H H CH2-indol-3-yl Et F F H OH H H XV-16-7 p-Me-Ph H H CH2CH2SCH3 Et F F H OH H H XV-16-8 p-Me-Ph * H * Et F F H OH H H ♦R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XV-17. ......... ' ..... W. ML ' 1" J"" ' - I 2 1 1 ·' ' "W ' '"a 1

Ns R1 R2 Rj« R36 R R5 R6 X Y R7 R“ XV-17-1 p-F-Ph H H H Et F F H OH H H XV-17-2 p-F-Ph H H CH3 Et F F H OH H H XV-17-3 p-F-Ph H H CH(CH3)2 Et F F H OH H H XV-17-4 p-F-Ph H H CH2CH(CH3)2 Et F F H OH H H XV-17-5 p-F-Ph H H CH2Ph Et F F H OH H H XV-17-6 p-F-Ph H H CHrindol-3-yl Et F F H OH H H XV-17-7 p-F-Ph H H CH2CH2SCH3 Et F F H OH H H XV-17-8 p-F-Ph * H * Et F F H OH H H *R2 and RJb joined together by (0¾^t0 form five-membered ring. 2983472-1 -353- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XV-18.

Ns ΊΓ "r2" R3n “R* — — R4 R5 R6 X Y R7 R8 XV-18-1 p-Cl-Ph H H H Et F F H OH H H XV-18-2 p-Cl-Ph H H ch3 Et F F H OH H H XV-18-3 p-Cl-Ph H H CH(CH3)2 Et F F H OH H H XV-18-4 p-Cl-Ph H H CHjCHCCHj), Et F F H OH H H XV-18-5 p-Cl-Ph H H CH2Ph Et F F H OH H H XV-18-6 p-Cl-Ph H H CH2-indoi-3-yl Et F F H OH H H XV-18-7 p-Cl-Ph H H ch2ch2sch3 Et F F H OH H H XV-18-8 p-Cl-Ph * H * Et F F H OH H H *R2 and RJb joined together by (CH2)3 to form Five-membered ring.

Table XV-19.

Ns R1 RJ R3t R3b R4 Rs R6 X Y R7 R“ XV-19-1 p-Br-Ph H H H Et F F H OH H H XV-19-2 p-Br-Ph H H CH3 Et F F H OH H H XV-19-3 p-Br-Ph H H CH(CH3)2 Et F F H OH H H XV-19-4 p-Br-Ph H H CH2CH(CH3)2 Et F F H OH H H XV-19-5 p-Br-Ph H H CHjPh Et F F H OH H H XV-19-6 p-Br-Ph H H CH2-indol-3-yl Et F F H OH H H XV-19-7 p-Br-Ph H H CH2CH2SCH3 Et F F H OH H H XV-19-8 p-Br-Ph * H * Et F F H OH H H ♦R2 and Rejoined together by (CH^ to form five-membered ring. 5 Table XV-20. 1 I RL J.....Tf * -- ' B"

Ns R1 R3 R3. R3b R4 Ic R6 X Y R R8 XV-20-1 p-I-Ph H H H Et F F H OH H H XV-20-2 p-I-Ph H H CH3 Et F F H OH H H XV-20-3 p-I-Ph H H CH(CH3)2 Et F F H OH H H XV-20-4 p-I-Ph H H CH2CH(CH3)2 Et F F H OH H H XV-20-5 p-I-Ph H H CH2Ph Et F F H OH H H XV-20-6 p-I-Ph H H CH2-indol-3-yl Et F F H OH H H XV-20-7 p-I-Ph H H CH2CH2SCH3 Et F F H OH H H XV-20-8 _ JT p-I-Ph * H * Et F F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -354- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XV-21.

Ns IF R3a "R35 R4 R5 R6 X Y R r“ XV-21-1 ch3 H H H "W F F H OH H H XV-21-2 ch3 H H ch3 'Pr F F H OH H H XV-21-3 ch3 H H CH(CH3)2 'Pr F F H OH H H XV-21-4 ch3 H H CH2CH(CH3)2 'Pr F F FI OH H H XV-21-5 ch3 H H CH2Ph 'Pr F F H OH H H XV-21-6 ch3 H H CH2-indol-3-yl 'Pr F F H OH H H XV-21-7 ch3 H H CH2CH2SCH3 'Pr F F H OH H H XV-21-8 ch3 ♦ H ♦ 'Pr F F H OH H H *R2 and R3tJ joined together by (CH2)3 to form five-membered ring.

Table XV-22.

Xfk o1

Na R1 R2 R3® R35 R4 Rs R6 X Y R' R“ XV-22-1 Et H H H F F H OH H H XV-22-2 Et H H CH3 'Pr F F H OH H H XV-22-3 Et H H CHCCHa), 'Pr F F H OH H H XV-22-4 Et H H CH2CH(CH3)a 'Pr F F H OH H H XV-22-5 Et H H CH2Ph 'Pr F F H OH H H XV-22-6 Et H H CH2-indol-3-yl 'Pr F F H OH H H XV-22-7 Et H H CH2CH2SCH3 'Pr F F H OH H H XV-22-8 Et 4 H * 'Pr F F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XV-23. .....•I-. 'R— - R-- .......... J-—I-Z"TE---~ R—“Π-

Na R' R2 r3, R3b r4 R5 Rb X Y R7 Rb XV-23-1 'Pr H H H 'Pr F F H OH H H XV-23-2 'Pr H H CH3 'Pr F F H OH H H XV-23-3 'Pr H H CH(CH3)2 'Pr F F H OH H H XV-23-4 'Pr H H CH2CH(CH3)2 'Pr F F H OH H H XV-23-5 'Pr H H CH2Ph 'Pr F F H OH H H XV-23-6 'Pr H H CH2-indol-3-yl 'Pr F F H OH H H XV-23-7 'Pr H H CH2CH2SCH3 'Pr F F H OH H H XV-23-8 IT 'Pr T3BT" * H * 'Pr F F H OH H H *R2 and Rejoined together by (CHj)3 to form five-membered ring. 2983472-) -355 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XV-24.

Xs R1 R2 r3. "r3* R4 R5 R:T" X Y r’ R1* XV-24-1 'Bu H H H F F H OH H H XV-24-2 *Bu H H ch3 'Pr F F H OH H H XV-24-3 'Bu H H CH(CH3)2 fPr F F H OH H H XV-24-4 'Bu H H CH2CH(CH3)2 'Pr F F H OH H H XV-24-5 'Bu H H CH2Ph 'Pr F F H OH H H XV-24-6 ΊΒιι H H CH2-indol-3-yl 'Pr F F H OH H H XV-24-7 'Bu H H CH2CH2SCH3 'Pr F F H OH H H XV-24-8 'Bu * H * 'Pr F F H OH H H *R2 and R3t> joined together by (CH^i'to form five-membered ring.

Table XV-25.

J&amp; R R5 r3. R3® R4 R5 R6 X Y R7 R* XV-25-1 Ph H H H 'Pr F F H OH H H XV-25-2 Ph H H CH3 'Pr F F H OH H H XV-25-3 Ph H H CH(CH3)2 'Pr F F H OH H H XV-25-4 Ph H H CH2CH(CH3)2 'Pr F F H OH H H XV-25-5 Ph H H CH2Ph 'Pr F F H OH H H XV-25-6 Ph H H CH2-indol-3-yl 'Pr F F H OH H H XV-25-7 Ph H H CH2CH2SCH3 'Pr F F H OH H H XV-25-8 jτ Ph ♦ H * 'Pr F F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XV-26. .......... I R .......... J ’"~ί /

Xa R* RJ "R^ R35 R4 Rs R6 X Y R7 ic XV-26-1 p-Me-Ph H H H 'Pr F F H OH H H XV-26-2 p-Me-Ph H H ch3 'Pr F F H OH H H XV-26-3 p-Me-Ph H H CH(CH3)2 Tr F F H OH H H XV-26-4 p-Me-Ph H H CHiCHiCHaJa 'Pr F F Η OH H H XV-26-5 p-Me-Ph H H CH2Ph 'Pr F F H OH H H XV-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr F F H OH H H XV-26-7 p-Me-Ph H H ch2ch2sch3 fpr F F H OH H H XV-26-8 *τλ2 J T p-Me-Ph * H * 'Pr F F H OH H H *R2 and R3b joined together by (CH2)j to form five-membered ring. 2983472-1 -356- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XV-27.

Ns R1 R3 R3’ “r35 R2 Rs R6 X Y ΊΓ Ru XV-27-1 p-F-Ph H H H JPr F F H OH H H XV-27-2 p-F-Ph H H CH3 'Pr F F H OH H H XV-27-3 p-F-Ph H H CH(CH3)2 'Pr F F H OH H H XV-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr F F H OH H H XV-27-5 p-F-Ph H H CH2Ph 'Pr F F H OH H H XV-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr F F H OH H H XV-27-7 p-F-Ph H H CH2CH2SCH3 'Pr F F H OH H H XV-27-8 p-F-Ph * H * 'Pr F F H OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XV-28.

Ns R1 R3 R3" R3b R4 R5 R6 X Y R' R8 XV-28-1 p-Cl-Ph H H H 'Pr F F H OH H H XV-28-2 p-Cl-Ph H H ch3 'Pr F F Η OH H H XV-28-3 p-Cl-Ph H H CHCCH^ 'Pr F F H OH H H XV-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr F F Η OH H H XV-28-5 p-Cl-Ph H H CH2Ph 'Pr F F H OH H H XV-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr F F Η OH H H XV-28-7 p-Cl-Ph H H ch2ch2sch3 'Pr F F H OH H H XV-28-8 p-Cl-Ph * H * 'Pr F F H OH H H ♦R2 and Rejoined together by (0¾¼ to form five-membered ring. 5 Table XV-29. 1 I » — I — «I ....... -Γ-' _ __ R ·»··»η

Ns R‘ R2 R3‘ R30 R4 RJ R* X Y ΊΓ R8 XV-29-1 p-Br-Ph H H H ΎΓ F F H OH H H XV-29-2 p-Br-Ph H H ch3 'Pr F F H OH H H XV-29-3 p-Br-Ph H H CH(CH3)2 'Pr F F H OH H H XV-29-4 p-Br-Ph H H CH2CH(CH3)2 Tr F F H OH H H XV-29-5 p-Br-Ph H H CH2Ph Tr F F H OH H H XV-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr F F H OH H H XV-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr F F H OH H H XV-29-8 p-Br-Ph * H * 'Pr F F H OH H H *R2 and R joined together by (0¾¼ to form five-membered ring. 2983472-1 -357- WO 2008/121634 PCT/US2008/058183

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Table XV-30.

Ns R1 R2 R3a "r35 Ί?"· R5 R6 X Y R7 R8 XV-30-1 p-I-Ph H H H Jpr F F H OH H H XV-30-2 p-I-Ph H H ch3 'Pr F F H OH H H XV-30-3 p-I-Ph H H CH(CH3)z 'Pr F F H OH H H XV-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr F F H OH H H XV-30-5 p-I-Ph H H CH2Ph fPr F F H OH H H XV-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr F F H OH H H XV-30-7 p-I-Ph H H CH2CH2SCH3 fpr F F H OH H H XV-30-8 p-I-Ph * H * 'Pr F F H OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XV-31.

Ns R R2 R3‘ R3b R4 R5 R6 X Y R' R8 XV-31-1 ch3 H H H "Bu F F H OH H H XV-31-2 ch3 H H CH3 "Bu F F H OH H H XV-31-3 ch3 H H CH(CH3)2 "Bu F F H OH H H XV-31-4 ch3 H H CH2CH(CH3)2 "Bu F F H OH H H XV-31-5 ch3 H H CH2Ph "Bu F F H OH H H XV-31-6 ch3 H H CH2-indol-3-yl "Bu F F H OH H H XV-31-7 ch3 H H CH2CH2SCH3 "Bu F F H OH H H XV-31-8 ch3 * H * "Bu F F H OH H H *R2 and R36 joined together by (CH2)3 to form five-membered ring. 5 Table XV-32.

Ns IV R2 R3’ R3b R4 R5 R6 X Y R' R8 XV-32-1 Et H H H "Bu F F H OH H H XV-32-2 Et H H ch3 "Bu F F H OH H H XV-32-3 Et H H ΟΗ(ΟΗ3)2 "Bu F F H OH H H XV-32-4 Et H H CHaCHCCHah "Bu F F H OH H H XV-32-5 Et H H CH2Ph "Bu F F H OH H H XV-32-6 Et H H CH2-indol-3-yl "Bu F F H OH H H XV-32-7 Et H H CH2CH2SCH3 "Bu F F H OH H H XV-32-8 A r. 1 J τ Et ♦ H * "Bu F F H OH H H *R2 and RJb joined together by (CHjfc to form five-membered ring. 2983472-1 -358- WO 2008/121634 PCT/US2008/058183

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Table XV-33.

Ns R1 R2 r3. R4 R5 R4 X Y R7 r“ XV-33-1 'Pr H H H "Bu F F H OH H H XV-33-2 'Pr H H ch3 "Bu F F H OH H H XV-33-3 zPr H H CH(CH3)2 "Bu F F H OH H H XV-33-4 'Pr H H CH2CH(CH3)2 "Bu F F H OH H H XV-33-5 'Pr H H CHjPh "Bu F F H OH H H XV-33-6 ipr H H CH2-indol-3-yl "Bu F F H OH H H XV-33-7 'Pr H H CH2CH2SCH3 "Bu F F H OH H H XV-33-8 'Pr * H * "Bu F F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XV-34.

Ns R1 R2 R3" R3b R^ ΊΓ R4 X Y R7 R“ XV-34-1 feu H H H "Bu F F H OH H H XV-34-2 'Bu H H ch3 "Bu F F H OH H H XV-34-3 'Bu H H CH(CH3)2 "Bu F F H OH H H XV-34-4 *Bu H H CH2CH(CH3)2 "Bu F F H OH H H XV-34-5 'Bu H H CH2Ph "Bu F F H OH H H XV-34-6 'Bu H H CH2-indol-3-yl "Bu F F H OH H H XV-34-7 'Bu H H CH2CH2SCH3 "Bu F F H OH H H XV-34-8 'Bu * H ♦ "Bu F F H OH H H ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XV-35.

" I -1- "'"TIL - 'J-“I-ΠΕ--- W U

Ns IV R2 Rj. R3b R4 ΊΓ R4 X Y R7 R“ XV-35-1 Ph H H H "Bu F F H OH H H XV-35-2 Ph H H ch3 "Bu F F H OH H H XV-35-3 Ph H H CHCCH,), "Bu F F H OH H H XV-35-4 Ph H H CH2CH(CH3)2 "Bu F F H OH H H XV-35-5 Ph H H CH2Ph "Bu F F H OH H H XV-35-6 Ph H H CH2-indol-3-yl "Bu F F H OH H H XV-35-7 Ph H H CH2CH2SCH3 "Bu F F H OH H H XV-35-8 Ph * H * "Bu F F H OH H H *R2 and Rejoined together by (CHjfc to form five-membered ring. 2983472-1 -359- WO 2008/121634

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Table XV-36.

Xs R1 R2 R,a R3b R4 Rs R6 X Y R7" r“ XV-36-1 p-Me-Ph H H H "Bu F F H OH H H XV-36-2 p-Me-Ph H H ch3 "Bu F F H OH H H XV-36-3 p-Me-Ph H H CH(CH3)2 "Bu F F H OH H H XV-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu F F H OH H H XV-36-5 p-Me-Ph H H CH2Ph "Bu F F H OH H H XV-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu F F H OH H H XV-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu F F H OH H H XV-36-8 p-Me-Ph ♦ H ♦ "Bu F F H OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XV-37.

Xa R1 RJ R3" R3b R4 R5 Rb X Y R7 R8 XV-37-1 p-F-Ph H H H "Bu F F H OH H H XV-37-2 p-F-Ph H H ch3 "Bu F F H OH H H XV-37-3 p-F-Ph H H CH(CH3)2 "Bu F F H OH H H XV-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu F F H OH H H XV-37-5 p-F-Ph H H CH2Ph "Bu F F H OH H H XV-37-6 p-F-Ph H H CHrindol-3-yl "Bu F F H OH H H XV-37-7 p-F-Ph H H CH2CH2SCH3 "Bu F F H OH H H XV-37-8 p-F-Ph * H * "Bu F F H OH H H *RZ and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XV-38. 1 R 1- 1 *" I 1 u

Xa R‘ R2 R3* R3b R4 RJ R6 X Y R’ R8 XV-38-1 p-Cl-Ph H H H "Bu F F H OH H H XV-38-2 p-Cl-Ph H H CH3 "Bu F F H OH H H XV-38-3 p-Cl-Ph H H CH(CH3)2 "Bu F F H OH H H XV-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu F F H OH H H XV-38-5 p-CI-Ph H H CH2Ph "Bu F F H OH H H XV-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu F F H OH H H XV-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu F F H OH H H XV-38-8 \ p-Cl-Ph * H * "Bu F F H OH H H *R2 and R3t) joined together by (CFh^ to form five-membered ring. 2983472-1 -360- WO 2008/121634 PCT/US2008/058183

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Table XV-39. ΚΓ» D1

Ns R1 R3 -jpr “R3® 7 'Τ’·· T" R6 X Y F F XV-39-1 p-Br-Ph H H H "Bu F F H OH H H XV-39-2 p-Br-Ph H H ch3 "Bu F F H OH H H XV-39-3 p-Br-Ph H H CH(CH3)2 "Bu F F H OH H H XV-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu F F H OH H H XV-39-5 p-Br-Ph H H CH2Ph "Bu F F H OH H H XV-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu F F H OH H H XV-39-7 p-Br-Ph H H CH2CH2SCH3 "Bu F F H OH H H XV-39-8 p-Br-Ph * H * "Bu F F H OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XV-40.

Ns Rl RJ Rj. R3b R4 R5 R6 X Y R7 R8 XV-40-1 p-l-Ph H H H "Bu F F H OH H H XV-40-2 p-I-Ph H H ch3 "Bu F F H OH H H XV-40-3 p-I-Ph H H CHfCH^ "Bu F F H OH H H XV-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu F F H OH H H XV-40-5 p-I-Ph H H CH2Ph "Bu F F H OH H H XV-40-6 p-I-Ph H H CH2-indol-3-yl "Bu F F H OH H H XV-40-7 p-I-Ph H H CH2CH2SCH3 "Bu F F H OH H H XV-40-8 p-I-Ph * H * "Bu F F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XV-41.

———“ D

Ns R R3 R3b R5 R6 X Y R7 R“ XV-41-1 ch3 H H H Bz F F H OH H H XV-41-2 ch3 H H CH3 Bz F F H OH H H XV-41-3 ch3 H H CH(CH3)2 Bz F F H OH H H XV-41-4 ch3 H H CH2CH(CH3)2 Bz F F H OH H H XV-41-5 ch3 H H CH2Ph Bz F F H OH H H XV-41-6 ch3 H H CH2-indol-3-yl Bz F F H OH H H XV-41-7 ch3 H H ch2ch2sch3 Bz F F H OH H H XV-41-8 ch3 * H ♦ Bz F F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -361 - WO 2008/121634 PCT/US2008/058183

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Table XV-42.

Xs RJ "kr r®· Ί?5 R4 RJ R6 X Y R r XV-42-1 Et H H H Bz F F H OH H H XV-42-2 Et H H ch3 Bz F F H OH H H XV-42-3 Et H H CH(CH,)j Bz F F H OH H H XV-42-4 Et H H CH2CH(CH3)2 Bz F F H OH H H XV-42-5 Et H H CHiPh Bz F F H OH H H XV-42-6 Et H H CH2-indol-3-yl Bz F F H OH H H XV-42-7 Et H H CH2CH2SCH3 Bz F F H OH H H XV-42-8 Et ♦ H * Bz F F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XV-43.

Xa R R2 R3· R3b R4 R5 R6 X Y R' R* XV-43-1 *Pr H H H Bz F F H OH H H XV-43-2 'Pr H H ch3 Bz F F H OH H ή XV-43-3 'Pr H H CHCCH^ Bz F F H OH H H XV-43-4 'Pr H H CH2CH(CH3)2 Bz F F H OH H H XV-43-5 Tr H H CH2Ph Bz F F H OH H H XV-43-6 'Pr H H CH2-indol-3-yl Bz F F H OH H H XV-43-7 'Pr H H CH2CH2SCH3 Bz F F H OH H H XV-43-8 'Pr * H * Bz F F H OH H H 10 *R2 and R3b joined together by (CH2)3 to form live-membered ring.

Table XV-44.

Xa R1 R1 -pr "r36 R4 RJ R4 X Y R7" R8 XV-44-1 'Bu H H H Bz F F H OH H H XV-44-2 *Bu H H CH3 Bz F F H OH H H XV-44-3 'Bu H H CHfCH^ Bz F F H OH H H XV-44-4 'Bu H H CH2CH(CH3)2 Bz F F H OH H H XV-44-5 'Bu H H CH2Ph Bz F F H OH H H XV-44-6 'Bu H H CH2-indol-3-yl Bz F F H OH H H XV-44-7 "Bu H H CH2CH2SCH3 Bz F F H OH H H XV-44-8 +R2, .τ 'Bu >3b : '· * H * Bz F F H OH H H *R2 and R3b joined together by (0¾¼ to form five-membered ring. 2983472-1 -362- WO 2008/121634 PCT/US2008/058183

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Table XV-45. "kfk U1

n° R1 R2 R3’ R* Rs R6 X Y R7" R8 XV-45-1 Ph H H H Bz F F H OH H H XV-45-2 Ph H H ch3 Bz F F H OH H H XV-4S-3 Ph H H OTO Bz F F H OH H H XV-45-4 Ph H H CH2CH(CH3)2 Bz F F H OH H H XV-45-5 Ph H H CH2Ph Bz F F H OH H H XV-45-6 Ph H H CH2-indol-3-yl Bz F F H OH H H XV-45-7 Ph H H CH2CH2SCH3 Bz F F H OH H H XV-45-8 Ph ♦ H Bz F F H OH H H *RJ and R3b joined together by (CH2)3 to form five-membered ring

Table XV-46.

Rl R2 r3, ‘ R3b R4 R3 R6 X Y R7 R* XV-46-1 p-Me-Ph H H H Bz F F H OH H H XV-46-2 p-Me-Ph H H CHj Bz F F H OH H H XV-46-3 p-Me-Ph H H CH(CH3)2 Bz F F H OH H H XV-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz F F H OH H H XV-46-5 p-Me-Ph H H CH2Ph Bz F F H OH H H XV-46-6 p-Me-Ph H H CH2-indol-3ryl Bz F F H OH H H XV-46-7 p-Me-Ph H H CH2CH2SCH3 Bz F F H OH H H XV-46-8 p-Me-Ph * H * Bz F F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. . Table XV-47. Ns Rl R2 R3* R3b R4 R5 R6 X Y R' r“ XV-47-1 p-F-Ph H H H Bz F F H OH H H XV-47-2 p-F-Ph H H CH3 Bz F F H OH H H XV-4 7-3 p-F-Ph H H CH(CH3)2 Bz F F H OH H H XV-47-4 p-F-Ph H H CH2CH(CH3)2 Bz F F H OH H H XV-47-5 p-F-Ph H H CH2Ph Bz F F H OH H H XV-47-6 p-F-Ph H H CH2-indol-3-yl Bz F F H OH H H XV-47-7 p-F-Ph H H CH2CH2SCH3 Bz F F H OH H H XV-47-8 p-F-Ph * H * Bz F F H OH H H *R2 and R3b joined toge ther by (CH2)3 to form five-membered i ring. 2983472-1 - 363 - WO 2008/121634 PCT/US2008/058183

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Table XV-48.

Xs r‘ ΊΡ~ Rir ~R3H R4 Rs R6 X Y r’ Ic XV-48-1 p-Cl-Ph H H H Bz F F H OH H H XV-48-2 p-Cl-Ph H H ch3 Bz F F H OH H H XV-48-3 p-Cl-Ph H H CH(CH3)2 Bz F F H OH H H XV-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz F F H OH H H XV-48-5 p-Cl-Ph H H CH2Ph Bz F F H OH H H XV-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz F F H OH H H XV-48-7 p-Cl-Ph H H CH2CH2SCH3 Bz F F H OH H H XV-48-8 p-Cl-Ph * H * Bz F F H OH H H *R2 and RJb joined together by (CHi)^ to form five-membered ring.

Table XV-49. "kik D1

X° R1 R2 RJa R3b r R5 R6 X Y R7 R8 XV-49-1 p-Br-Ph H H H Bz F F H OH H H XV-49-2 p-Br-Ph H H ch3 Bz F F H OH H H XV-49-3 p-Br-Ph H H CHCCH^ Bz F F H OH H H XV-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz F F H OH H H XV-49-5 p-Br-Ph H H CH2Ph Bz F F H OH H H XV-49-6 p-Br-Ph H H CH2-indol-3-yl Bz F F H OH H H XV-49-7 p-Br-Ph H H CH2CH2SCH3 Bz F F H OH H H XV-49-8 p-Br-Ph * H * Bz F F H OH H H *R2 and RJb joined together by (ΟΗ2)3 to form five-membered ring. 5 Table XV-50. — I— " -Ml -J “If f Λ_- ' ’« u"

Ns R* R2 R3. R3b R4 R5 Rfc X Y R7 R8 XV-50-1 p-I-Ph H H H Bz F F H OH H H XV-50-2 p-I-Ph H H ch3 Bz F F H OH H H XV-50-3 p-I-Ph H H CH(CH3)2 Bz F F H OH H H XV-50-4 p-I-Ph H H CH2GH(CH3)2 Bz F F H OH H H XV-50-5 p-I-Ph H H CH2Ph Bz F F Η OH H H XV-50-6 p-I-Ph H H CH2-indol-3-yl Bz F F H OH H H XV-50-7 p-I-Ph H H CH2CH2SCH3 Bz F F H OH H H XV-50-8 p-I-Ph »3b ; i ♦ H * Bz F F H OH H H ♦R* and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -364- WO 2008/121634 PCT/US2008/058183

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XVI

Table XVI-1.

Xs R1 R3 R3" Ίκ35 Rs R6 X Y r" R8 XVI-1-1 ch3 H H H ch3 F F F OH H H XVI-1-2 ch3 H H ch3 ch3 F F F OH H H XVI-1-3 ch3 H H CH(CHj)j ch3 F F F OH H H XVI-1-4 ch3 H H CH2CH(CH3)2 ch3 F F F OH H H XVI-1-5 ch3 H H CH2Ph ch3 F F F OH H H XV1-1-6 ch3 H H CH2-indol-3-yI ch3 F F F OH H H XVI-1-7 ch3 H H CH2CH2SCH3 ch3 F F F OH H H XVI-1-8 ch3 * H + ch3 F F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XVI-2. - i n—:—n. "il- 1 .i—“O'"

Xa R R2 R3a R3b R4 R3 R6 X Y R7 R“ XVI-2-1 Et H H H CH3 F F F OH H H XVI-2-2 Et H H ch3 ch3 F F F OH H H XVI-2-3 Et H H CH(CH3)2 ch3 F F F OH H H XVI-2-4 Et H H CH2CH(CH3)2 ch3 F F F OH H H XVI-2-5 Et H H CH2Ph ch3 F F F OH H H XVI-2-6 Et H H CH2-indol-3-yl ch3 F F F OH H H XVI-2-7 Et H H CH2CH2SCH3 ch3 F F F OH H H XVI-2-8 Et * H * ch3 F F F OH H H *R2 andR3» joined together by (CH2bt0 ^0ΠΏ five-membered ring. 2983472-1 -365- WO 2008/121634 PCT/US2008/058183

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Table XV1-3. d '

Ns R1 R3 R3"” “ft»” R3 "r5" X Y R7” E? XV1-3-1 H H H ch3 F F F OH H H XVI-3-2 'Pr H H ch3 ch3 F F F OH H H XVI-3-3 'Pr H H CH(CH3)2 ch3 F F F OH H H XVI-3-4 'Pr H H CH2CH(CH3)2 ch3 F F F OH H H XVI-3-5 'Pr H H CH2Ph ch3 F F F OH H H XVI-3-6 'Pr H H CH2-indol-3-yl ch3 F F F OH H H XVI-3-7 'Pr H H CH2CH2SCH3 ch3 F F F OH H H XVI-3-8 'Pr * H * ch3 F F F OH H H *R2 and R3b joined together by (ΟΗ2)3 to form five-membered ring.

Table XVI-4.

Ns R1 R3 Rj« R3b R4 R3 Iv X Y R7 R“ XVI-4-1 7Bu H H H ch3 F F F OH H H XVI-4-2 'Bu H H CH3 ch3 F F F OH H H XVI-4-3 'Bu H H CH(CH3)2 ch3 F F F OH H H XVI-4-4 'Bu H H CH2CH(CH3)2 ch3 F F F OH H H XVI-4-5 'Bu H H CH2Ph ch3 F F F OH H H XVI-4-6 'Bu H H CH2-indol-3-yl CH3 F F F OH H H XVI-4-7 'Bu H H ch2ch2sch3 ch3 F F F OH H H XVI-4-8 'Bu ♦ H * ch3 F F F OH H H *RZ and Rejoined together by (CH^ to form five membered ring. 5 Table XVI-5. 1 '1' M - HL" 4Γ" ” 1 J "M" --¾ J. !2'r" B‘"

Ns R R3 R3‘ R3b R4 R3 IF X Y R7 R8 XVI-5-1 Ph H H H CH3 F F F OH H H XVI-5-2 Ph H H CH3 ch3 F F F OH H H XVI-S-3 Ph H H CH(CH3)2 ch3 F F F OH H H XV1-5-4 Ph H H CH2CH(CH3)2 ch3 F F F OH H H XVI-5-5 Ph H H CH2Ph ch3 F F F OH H H XVI-5-6 Ph H H CH2-indol-3-yl ch3 F F F OH H H XVI-5-7 Ph H H CH2CH2SCH3 ch3 F F F OH H H XVI-5-8 "3 , Ph r»3B j. * H ♦ ch3 F F F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -366- WO 2008/121634 PCT/US2008/058183

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Table XVI-6.

Ns R1 R2 “r37 R4 R1 R6 X Y iT Ra XVI-6-1 p-Me-Ph H H H CH3 F F F OH H H XVI-6-2 p-Me-Ph H H CHa CHa F F F OH H H XVI-6-3 p-Me-Ph H H CH(CH3)2 CH3 F F F OH H H XVI-6-4 p-Me-Ph H H CH2CH(CH3)2 CH3 F F F OH H H XVI-6-5 p-Me-Ph H H CH2Ph CHa F F F OH H H XVI-6-6 p-Me-Ph H H CH2-indol-3-yl CHj F F F OH H H XVI-6-7 p-Me-Ph H H CHjCH2SCH3 CHa F F F OH H H XVI-6-8 p-Me-Ph * H ♦ CHa F F F OH H H *R2 and R30 joined together by (CH2)3 to form five-membered ring.

Table XVI-7.

Ns R' R2 Rja R3b R4 R5 Rb X Y ΊΓ R8 XVI-7-1 p-F-Ph H H H CH3 F F F OH H H XVI-7-2 p-F-Ph H H CHa CHa F F F OH H H XVI-7-3 p-F-Ph H H CH(CH3)2 CH3 F F F OH H H XVI-7-4 p-F-Ph H H CHaCHCCHah ch3 F F F OH H H XVI-7-6 p-F-Ph H H CH2Ph ch3 F F F OH H H XVI-7-7 p-F-Ph H H CH2-indol-3-yl CHa F F F OH H H XVI-7-8 p-F-Ph H H CH2CH2SCH3 CH3 F F F OH H H XVI-7-20 p-F-Ph ♦ H * CH3 F F F OH H H ♦R2 and RJb joined together by (Clhb to form five-membered ring. 5 Table XVI-8. 1 H HL -— 1 "~J £ ’ L"~IT~

Ns R’ R2 R3. R36 R R5 R6 X Y R7 R8 XVI-8-1 p-Cl-Ph H H H CH3 F F F OH H H XVI-8-2 p-Cl-Ph H H ch3 CH3 F F F OH H H XVI-8-3 p-Cl-Ph H H CHCCHah CHa F F F OH H H XVI-8-4 p-Cl-Ph H H CH2CH(CH3)3 CHa F F F OH H H XVI-8-5 p-Cl-Ph H H CH2Ph CHa F F F OH H H XVI-8-6 p-Cl-Ph H H CHrindol-3-yl CHa F F F OH H H XVI-8-7 p-Cl-Ph H H CH2CH2SCH3 CHa F F F OH H H XVI-8-8 p-Cl-Ph * H * CHa F F F OH H H *R^ and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -367- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XVI-9.

Xa R’ R2 R3a r35 ΊΤ" R5 R4 X Y V Rb XVI-9-1 p-Bf-Ph H H H ch3 F F F OH H H XV1-9-2 p-Br-Ph H H ch3 ch3 F F F OH H H XVI-9-3 p-Br-Ph H H CH(CH3)2 ch3 F F F OH H H XVI-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 F F F OH H H XVI-9-6 p-Br-Ph H H CH2Ph ch3 F F F OH H H XVI-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 F F F OH H H XVI-9-8 p-Br-Ph H H CH2CH2SCH3 ch3 F F F OH H H XVI-9-20 p-Br-Ph * H * ch3 F F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVI-10.

Xa Rl RJ R3" r” R3 R4 X Y R7 r“ XVI-10-1 p-I-Ph H H H ch3 F F F OH H H XVI-10-2 p-I-Ph H H ch3 ch3 F F F OH H H XVI-10-3 p-I-Ph H H CH(CH3>2 ch3 F F F OH H H XVI-10-1 p-I-Ph H H CH2CH(CH3)2 ch3 F F F OH H H XVI-10-5 p-I-Ph H H CH2Ph ch3 F F F OH H H XVI-10-6 p-I-Ph H H CH2-indoI-3-yI ch3 F F F OH H H XVI-10-7 p-I-Ph H H CH2CH2SCH3 ch3 F F F OH H H XVI-10-8 p-I-Ph * H * ch3 F F F OH H H ♦R? and Rejoined together by (CH^b to form five-membered ring.

Xa R1 R2 r3. “R36 ir R5 R4 X Y R7 R“ XVI-11-1 ch3 H H H Et F F F OH H H XVI-11-2 ch3 H H CH3 Et F F F OH H H XVI-11-3 ch3 H H CH(CH3)2 Et F F F OH H H XVI-11-4 ch3 H H CH2CH(CH3)2 Et F F F OH H H XVI-11-5 ch3 H H CH2Ph Et F F F OH H H XVI-11-6 ch3 H H CH2-indol-3-yl Et F F F OH H H XVI-11-7 ch3 H H CH2CH2SCH3 Et F F F OH H H XVI-11-8 ch3 * H * Et F F F OH H H ♦R* and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -368- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XVI-12.

X2 R1 R2 "r37" R3b R4 R4 X Y R7 lv XVI-12-1 Et H H H Et F F F OH H H XVI-12-2 Et H H CH3 Et F F F OH H H XVI-12-3 Et H H CH(CH3)2 Et F F F OH H H XVI-12-4 Et H H CH2CH(CH3)2 Et F F F OH H H XVI-12-5 Et H H CH2Ph Et F F F OH H H XVI-12-6 Et H H CHrindol-3-yl Et F F F OH H H X VI-12-7 Et H H CH2CH2SCH3 Et F F F OH H H XVI-12-8 Et 3BV * H * Et F F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVI-13.

X» R1 R2 R3a R4 R3 R6 X Y r" Ru XVI-13-1 'Pr H H H Et F F F OH H H XVI-13-2 'Pr H H ch3 Et F F F OH H H XVl-13-3 'Pr H H CHCCHa): Et F F F OH H H XVI-13-4 /Pr H H CH2CH(CH3)2 Et F F F OH H H XVI-13-5 ‘Pr H H CH2Ph Et F F F OH H H XV1-13-6 'Pr H H CH2-indol-3-yl Et F F F OH H H XVI-13-7 zPr H H CH2CH2SCH3 Et F F F OH H H XVI-13-8 *Pr * H * Et F F F OH H H *R and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XVI-14. --- 11 ' —I R-TT- RL 1 -1- .,,- , — —II-

Xa “R1- r2- “r37- “r35 R4 R5 R6 X Y r’ R8 XVI-14-1 teii H H H Et F F F OH H H XVI-14-2 'Bu H H CH3 Et F F F OH H H XVI-14-3 'Bu H H CHCCHa), Et F F F OH H H XVI-14-4 *Bu H H CH2CH(CH3)2 Et F F F OH H H XVI-14-5 'Bu H H CH2Ph Et F F F OH H H XVI-14-6 'Bu H H CH2-indol-3-yl Et F F F OH H H XVI-14-7 'Bu H H CH2CH2SCH3 Et F F F OH H H XVI-14-8 'Bu * H * Et F F F OH H H ♦R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -369- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XVI-15.

Ns R1 R3 R3’ "r35 Rs X Y r7" R8 XVI-15-1 Ph H H H Et F F F OH H H XVI-15-2 Ph H H ch3 Et F F F OH H H XVI-15-3 Ph H H CHiCHah Et F F F OH H H XVI-15-4 Ph H H CH2CH(CH3)2 Et F F F OH H H XVI-15-5 Ph H H CH2Ph Et F F F OH H H XVI-15-6 Ph H H CH2-indol-3-yl Et F F F OH H H XVI-15-7 Ph H H CH2CH2SCH3 Et F F F OH H H XVI-15-8 Ph * H * Et F F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XV1-16.

Ns R1 R2 R3' ’ R3b R4 RJ IT X Y R' R8 XVI-16-1 p-Me-Ph H H H Et F F F OH H H XVI-16-2 p-Me-Ph H H CH3 Et F F F OH H H XV1-16-3 p-Me-Ph H H CHiCHa^ Et F F F OH H H XVI-16-4 p-Me-Ph H H CH2CH(CH3)2 Et F F F OH H H XVI-16-5 p-Me-Ph H H CH2Ph Et F F F OH H H XVI-16-6 p-Me-Ph H H CH2-indol-3-yl Et F F F OH H H XVI-16-7 p-Me-Ph H H CH2CH2SCH3 Et F F F OH H H XVI-16-8 p-Me-Ph * H * Et F F F OH H H *R2 and RJb joined together by (CHj^ to form five-membered ring. TableXVI-17. “jfe R1 R3- R35- R3b R4 RJ R* X Y R' R1 XVI-17-1 p-F-Ph H H H Et F F F OH H H XVI-17-2 p-F-Ph H H ch3 Et F F F OH H H XVI-17-3 p-F-Ph H H CH(CH3)2 Et F F F OH H H XVI-17-4 p-F-Ph H H CH2CH(CH3)2 Et F F F OH H H XVI-17-5 p-F-Ph H H CH2Ph Et F F F OH H H XVI-17-6 p-F-Ph H H CH2-indol-3-yl Et F F F OH H H XVI-17-7 p-F-Ph H H CH2CH2SCH3 Et F F F OH H H XVI-17-8 p-F-Ph * H ♦ Et F F F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -370- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XVI-18.

Xa Rl R2 "r37* R3b R4 Rs R6 X Y ΊΓ XVI-18-1 p-Cl-Ph H H H Et F F F OH H H XVI-18-2 p-Cl-Ph H H ch3 Et F F F OH H H XVI-18-3 p-Cl-Ph H H CH(CH3)2 Et F F F OH H H XVI-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et F F F OH H H XVI-18-5 p-Cl-Ph H H CH2Ph Et F F F OH H H XVI-18-6 p-Ct-Ph H H CH2-indol-3-yl Et F F F OH H H XVI-18-7 p-Cl-Ph H H CH2CH2SCH3 Et F F F OH H H XVI-18-8 p-Cl-Ph ♦ H * Et F F F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XVI-19.

Xa Rl R2 R3' R3b R4 Rs R* X Y R7 rB XVI-19-1 p-Br-Ph H H H Et F F F OH H H X VI-19-2 p-Br-Ph H H ch3 Et F F F OH H H XVI-19-3 p-Br-Ph H H CH(CH3)2 Et F F F OH H H XVI-19-4 p-Br-Ph H H CH2CH(CH3)2 Et F F F OH H H XVI-19-5 p-Br-Ph H H CH2Ph Et F F F OH H H XVI-19-6 p-Br-Ph H H CH2-indol-3-yl Et F F F OH H H XVI-19-7 p-Br-Ph H H CH2CH2SCH3 Et F F F OH H H XVI-19-8 -77; p-Br-Ph ; ; j * H ♦ Et F F F OH H H *R2 and RJb joined together by (062)3 to form five-membered ring.

Xa R1 R2 R3a ήρε R4 RJ R6 X Y XVI-20-1 p-I-Ph H H H Et F F F OH H XVI-20-2 p-I-Ph H H CH3 Et F F F OH H XVI-20-3 p-I-Ph H H CHfCH^ Et F F F OH H XVI-20-4 p-I-Ph H H CH2CH(CH3)2 Et F F F OH H XVI-20-5 p-I-Ph H H CH2Ph Et F F F OH H XVI-20-6 p-I-Ph H H CH2-indol-3-yl Et F F F OH H XVI-20-7 p-I-Ph H H CH2CH2SCH3 Et F F F OH H XVI-20-8 p-I-Ph 3b ; ; -J * H * Et F F F OH H *R2 and R30 joined together by (CH2)3 to form five-membered ring. 2983472-1 -371- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XVI-2L

X2 R1 R2 Ί?· R3b ΊΤ Rs R6 X Y R r“ XVI-21-1 ch3 H H H 'pr F F F OH H H XVI-21-2 ch3 H H ch3 'Pr F F F OH H H XVI-21-3 ch3 H H CH(CH3)2 'Pr F F F OH H H XVI-21-4 ch3 H H CH2CH(CH3)2 'Pr F F F OH H H XVI-21-5 ch3 H H CH2Ph 'Pr F F F OH H H XV1-21-6 ch3 H H CH2-indol-3-yl 'Pr F F F OH H H XVI-21-7 ch3 H H ch3ch2sch3 'Pr F F F OH H H XVI-21-8 ch3 * H * 'Pr F F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVI-22.

Xs R1 R5 ”ipr IF Ί?“ R5 R6 X Y r’ R8 XVI-22-1 Et H H H "'pT F F F OH H H XVI-22-2 Et H H CH3 'Pr F F F OH H H XVI-22-3 Et H H CH(CH3)2 'Pr F F F OH H H XVI-22-4 Et H H CH2CH(CH3)2 'Pr F F F OH H H XVI-22-5 Et H H CH2Ph 'Pr F F F OH H H XV1-22-6 Et H H CH2-indol-3-yl 'Pr F F F OH H H XVI-22-7 Et H H CH2CH2SCH3 'Pr F F F OH H. H XVI-22-8 „ j n Et Jb * * H * 'Pr F F F OH H H *R2 and Rejoined together by (CH-jb to form five-membered ring.

X2 R1 RJ r3« -r3E R* R6 X Y iF iF XVI-23-1 'Pr H H H “tT F F F OH H H XVI-23-2 'Pr H H ch3 'Pr F F F OH H H XVI-23-3 'Pr H H CH(CH3)2 'Pr F F F OH H H XVI-23-4 'Pr H H CH2CH(CH3)2 'Pr F F F OH H H XVI-23-5 'Pr H H CH2Ph 'Pr F F F OH H H XVI-23-6 'Pr H H CH2-indol-3-yl 'Pr F F F OH H H XVI-23-7 'Pr H H CH2CH2SCH3 'Pr F F F OH H H XVI-23-8 “7^2- 'Pr * H ♦ 'Pr F F F OH H H *R2 and R3b joined together by (CPhh to form five-membered ring. 2983472-1 -372- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XVI-24.

Ns Rl F -£3a- -p; R4 R5 R4 X Y F R8 XVI-24-1 'Bu H H H F F F OH H H XVI-24-2 'Bu H H ch3 'Pr F F F OH H H XVI-24-3 'Bu H H CH(CH3)2 'Pr F F F OH H H XVI-24-4 feu H H CH2CH(CH3)2 'Pr F F F OH H H XVI-24-5 'Bu H H CH2Ph 'Pr F F F OH H H XVI-24-6 'Bu H H CH2-indol-3-yl 'Pr F F F OH H H XVI-24-7 'Bu H H ch2ch2sch3 'Pr F F F OH H H XVI-24-8 *«2 in 'Bu 3b · · ♦ H * Pr F F F OH H H *R2 and R30 joined together by (CH2)3 to form five-membered ring.

Table XVI-25.

Ns R1 TF R3b “R3® R4 Rs R4 X Y R7 rH XVI-25-1 Ph H H H Pr F F F OH H H XVI-25-2 Ph H H ch3 'Pr F F F OH H H XVI-25-3 Ph H H CH(CHj)2 'Pr F F F OH H H XVI-25-4 Ph H H CH2CH(CH3)2 'Pr F F F OH H H XVI-25-5 Ph H H CH2Ph 'Pr F F F OH H H XVI-25-6 Ph H H CH2-indol-3-yl 'Pr F F F OH H H XVI-25-7 Ph H H ch2ch2sch3 'Pr F F F OH H H XVI-25-8 "7772-T7 Ph .3b · < * H ♦ 'Pr F F F OH H H *R2 and R30 joined together by (CH2)3 to form five-membered ring

Ns R‘ R3 "r3T "Έ5 R4 RJ R6 X Y R7 R8 XVI-26-1 p-Me-Ph H H H Pr F F F OH H H XVI-26-2 p-Me-Ph H H ch3 Pr F F F OH H H XVJ-26-3 p-Me-Ph H H CHCCH,), 'Pr F F F OH H H XVI-26-4 p-Me-Ph H H CH2CH(CH3)2 Pr F F F OH H H XVI-26-5 p-Me-Ph H H CH2Ph 'Pr F F F OH H H XVI-26-6 p-Me-Ph H H CH2-indoi-3-yl Pr F F F OH H H XVI-26-7 p-Me-Ph H H ch2ch2sch3 Pr F F F OH H H XVI-26-8 “"772-77; p-Me-Ph ,3b· : * H * 'Pr F F F OH H H ♦R' and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -373- W Ο 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XVI-27.

X° “R1 R2 ΊΡ7" R3b R4 R5 R6 X Y R7 R8 XVI-27-1 p-F-Ph H H H "W F F F OH H H XV1-27-2 p-F-Ph H H ch3 'Pr F F F OH H H XV1-27-3 p-F-Ph H H . CH(CH3)2 'Pr F F F OH H H XVI-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr F F F OH H H XVI-27-5 p-F-Ph H H CH2Ph 'Pr F F F OH H H XVI-27-6 p-F-Ph H H CH2-indol-3-yI 'Pr F F F OH H H XVI-27-7 p-F-Ph H H CH2CH2SCH3 'Pr F F F OH H H XVI-27-8 p-F-Ph * H ♦ 'Pr F F F OH H H *R2 and Rejoined together by (CHak to form five-membered ring.

Table XVI-28.

Xa R1 R2 RJ‘ R3b R4 RJ R6 X Y R7 R8 XV1-28-1 p-Cl-Ph H H H JPr F F F OH H H XVI-28-2 p-Cl-Ph H H CH3 'Pr F F F OH H H XVI-28-3 p-Cl-Ph H H CH(CH3)2 'Pr F F F OH H H XVI-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr F F F OH H H XV1-28-5 p-Cl-Ph H H CH2Ph 'Pr F F F OH H H XVI-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr F F F OH H H XVI-28-7 p-Cl-Ph H H CH2CH2SCH3 'Pr F F F OH H H XVI-28-8 p-Cl-Ph * H * fPr F F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XVI-29. ’ 1 ' 1 1 M H·""' *L ' 1 1 g 1 '"f u

Xa Rl R2 R3‘ R3b R4 R! R6 X Y R7 R8 XVI-29-1 p-Br-Ph H H H 'Pr F F F OH H H XVI-29-2 p-Br-Ph H H ch3 'Pr F F F OH H H XVI-29-3 p-Br-Ph H H CH(CH·,), 'Pr F F F OH H H XVI-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr F F F OH H H XVI-29-5 p-Br-Ph H H CH2Ph 'Pr F F F OH H H XVI-29-6 p-Br-Ph H H CH2-indol-3-yI 'Pr F F F OH H H XVI-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr F F F OH H H XVI-29-8 “Ϊ772- p-Br-Ph 35ΤΊ—77 * H * Tr F F F OH H H *R2 and R30 joined together by (CH^ to form five-membered ring. 2983472-1 -374 WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XVI-30.

Xa R1 R2 R3“ R3b R4 Rs R6 X Y r' r“ XV1-30-1 p-l-Ph H H H ’’Pr” F F F OH H H XVI-30-2 p-l-Ph H H CH3 'Pr F F F OH H H XVI-30-3 p-I-Ph H H CH(CH3)2 'Pr F F F OH H H XVI-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr F F F OH H H XVI-30-5 p-I-Ph H H CH2Ph 'Pr F F F OH H H XVI-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr F F F OH H H XVI-30-7 p-I-Ph H H CH2CH2SCH3 'Pr F F F OH H H XVI-30-8 —ττ: p-I-Ph —3 * H * 'Pr F F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVI-31. d·

Xa R‘ R2 ηρϊ- R3b R4 R6 X Y R Ra XVI-31-1 ch3 H H H "Bu F F F OH H H XVI-31-2 ch3 H H CH3 "Bu F F F OH H H XVI-31-3 ch3 H H CH(CH3)2 "Bu F F F OH H H XVI-31-4 ch3 H H CH2CH(CH3)2 "Bu F F F OH H H XVI-31-5 ch3 H H CH2Ph "Bu F F F OH H H XVI-31-6 ch3 H H CH2-indol-3-yl "Bu F F F OH H H XVI-31-7 ch3 H H CH2CH2SCH3 "Bu F F F OH H H XVI-31-8 ch3 * H * "Bu F F F OH H H ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XVI-32. W 1Γ" <iL·—~ 11 J " 2 IPT- R ”11"

Xa R R2 R3‘ R3b R4 R5 R6 X Y R7 R‘ XVI-32-1 Et H H H "Bu F F F OH H H XV1-32-2 Et H H ch3 "Bu F F F OH H H XVI-32-3 Et H H ΟΗ(ΟΗ3)2 "Bu F F F OH H H XVI-32-4 Et H H CH2CH(CH3)2 "Bu F F F OH H H XVI-32-5 Et H H CH2Ph "Bu F F F OH H H XVI-32-6 Et H H CH2-indol-3-yl "Bu F F F OH H H XVI-32-7 Et H H ch2ch2sch3 "Bu F F F OH H H XVI-32-8 ι τ, Et 3b · * Ή * "Bu F F F OH H H *R2 and Rejoined together by (CHabt0 form five-membered ring. 2983472-1 -375- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XVI-33.

x° R1 R3 R3e~ —35 R4 R5 R6 X Y r’ r“ XVI-33-1 'Pr H H H "Bu F F F OH H H XVI-33-2 'Pr H H ch3 "Bu F F F OH H H XVI-33-3 'Pr H H CH(CH3)2 "Bu F F F OH H H XVI-33-4 'Pr H H CH2CH(CH3)a "Bu F F F OH H H XVI-33-5 "Pr H H CH2Ph "Bu F F F OH H H XVI-33-6 'Pr H H CH2-indol-3-y1 "Bu F F F OH H H XVI-33-7 'Pr H H CH2CH2SCH3 "Bu F F F OH H H XVI-33-8 'Pr * H * "Bu F F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVI-34.

X° r R3 r3b R3b R4 R3 R6 X Y R7 R8 XVI-34-1 'Bu H H H "Bu F F F OH H H XVI-34-2 "Bu H H ch3 "Bu F F F OH H H XVI-34-3 'Bu H H CH(CH3)2 "Bu F F F OH H H XVI-34-4 'Bu H H CH2CH(CH3)2 "Bu F F F OH H H XVI-34-5 'Bu H H CH2Ph "Bu F F F OH H H XVI-34-6 'Bu H H CH2-indoI-3-yl "Bu F F F OH H H XVI-34-7 'Bu H H CH2CH2SCH3 "Bu F F F OH H H XVI-34-8 'Bu * H ♦ "Bu F F F OH H H *R2 and Rejoined together by (CFhh to form five-membered ring. 5 Table XVI-35.

Xs R R3 R3' R3b R4 RJ R6 X Y R7 R8 XVI-35-1 Ph H H H "Bu F F F OH H H XVI-35-2 Ph H H ch3 "Bu F F F OH H H XVI-35-3 Ph H H CHCCHjh "Bu F F F OH H H XVI-35-4 Ph H H CH2CH(CH3)2 "Bu F F F OH H H XVI-35-5 Ph H H CH2Ph "Bu F F F OH H H XVI-35-6 Ph H H CH2-indoI-3-yl "Bu F F F OH H H XVI-35-7 Ph H H CH2CH2SCH3 "Bu F F F OH H H XVI-35-8 - Τπ Ph ,3b · ; ♦ H * "Bu F F F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -376- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XVI-36.

Ns R1 RJ R2e R3b R4 R5 "R^ X Y R’ r“ XVI-36-1 p-Me-Ph H H H "Bu F F F OH H H XVI-36-2 p-Me-Ph H H ch3 "Bu F F F OH H H XVI-36-3 p-Me-Ph H H CH(CH3)2 "Bu F F F OH H H XVI-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu F F F OH H H XVI-36-5 p-Me-Ph H H CH2Ph "Bu F F F OH H H XVI-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu F F F OH H H XVI-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu F F F OH H H XVI-36-8 in p-Me-Ph ,3b - j ♦ H * "Bu F F F OH H H *R2 and Rejoined together by (CHab to form five-membered ring.

Table XVI-37.

“jfe r! R2 R3‘ R3b R4 R5 R6 X ; y r’ rb XVI-37-1 p-F-Ph Η Η H "Bu F F F OH Η H XVI-37-2 p-F-Ph Η H CH3 "Bu F F F OH Η H XVI-37-3 p-F-Ph Η H CH(CH3)2 "Bu F F F OH Η H XVI-37-4 p-F-Ph Η H CH2CH(CH3)2 "Bu F F F OH Η H XVI-37-5 p-F-Ph Η H CH2Ph "Bu F F F OH Η H XVI-37-6 p-F-Ph Η H CH2-indol-3-yl "Bu F F F OH Η H XVI-37-7 p-F-Ph Η H CH2CH2SCH3 "Bu F F F OH Η H XVI-37-8 p-F-Ph * H * "Bu F F F OH Η H *R2 and RJb joined together by (CH2)3 to form five-membered ring. Table XVI-38. R2 R3a R3b R4 r5 r6 : X Y R7 R8 XVI-38-1 p-Cl-Ph Η Η H "Bu F F ] F OH Η H XVI-38-2 p-Cl-Ph Η H CH3 "Bu F F : F OH Η H XVJ-38-3 p-Cl-Ph Η H CH(CH3)2 "Bu f f : F OH Η H XVI-38-4 p-Cl-Ph Η H CH2CH(CH3)2 "Bu F F F OH Η H XVI-38-5 p-Cl-Ph Η H CH2Ph "Bu F F F OH Η H XV1-38-6 p-Cl-Ph Η H CH2-indol-3-yl "Bu f f : F OH Η H XVI-38-7 p-CI-Ph Η H CH2CH2SCH3 "Bu F F F OH Η H XV1-38-8 p-Cl-Ph Tn2.-j'n3bT· .j; * H · "Bu F F F OH Η H ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -377- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XVI-39.

X2 Rl R2 R3a R3b R4 Rs “ΪΓ X Y R7 Ry XVI-39-1 p-Br-Ph H H H "Bu F F F OH H H XVI-39-2 p-Br-Ph H H ch3 "Bu F F F OH H H XVI-39-3 p-Br-Ph H H CH(CH3)2 "Bu F F F OH H H XVI-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu F F F OH H H XVI-39-5 p-Br-Ph H H CH2Ph "Bu F F F OH H H XVI-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu F F F OH H H XVI-39-7 p-Br-Ph H H CH2CH2SCH3 "Bu F F F OH H H XVI-39-8 p-Br-Ph 3B77T—77 * H * "Bu F F F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XVI-40.

Ife ΪΓ~ R3" R3b RJ R6 X Y k7 R8 XVI-40-1 p-l-Ph H H H "Bu F F F OH H H XVI-40-2 p-I-Ph H H CH3 "Bu F F F OH H H XVI-40-3 p-I-Ph H H CH(CH3)2 "Bu F F F OH H H XVI-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu F F F OH H H XVI-40-5 p-I-Ph H H CH2Ph ”Bu F F F OH H H XVI-40-6 p-I-Ph H H CH2-indoi-3-yl "Bu F F F OH H H XVI-40-7 p-I-Ph H H CH2CH2SCH3 "Bu F F F OH H H XVI-40-8 p-I-Ph * H * "Bu F F F OH H H *R2 and R30 joined together by (CH2)3 to form five-membered ring. Table XVI-41. 1 R3e R4 RJ R6 X Y R7 R8 XVI-41-1 CH3 H H H Bz F F F OH H H XVI-41-2 CH3 H H CH3 Bz F F F OH H H XVI-41-3 CH3 H H CH(CH3)2 Bz F F F OH H H XVI-41-4 CH3 H H CH2CH(CH3)2 Bz F F F OH H H XVI-41-5 CH3 H H CH2Ph Bz F F F OH H H XVI-41-6 CH3 H H CH2-indol-3-yl Bz F F F OH H H XVI-41-7 CH3 H H ch2ch2sch3 Bz F F F OH H H XVI-41-8 CH3 * H ♦ Bz F F F OH H H ♦R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -378- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XVI-42.

X® R1 R3 R3a R3b R4 R5 R6 X Y R' Rtt XVI-42-1 Et H H H Bz F F F OH H H XVI-42-2 Et H H ch3 Bz F F F OH H H XVI-42-3 Et H H CH(CH,)2 Bz F F F OH H H XVI-42-4 Et H H CH2CH(CH3)2 Bz F F F OH H H XVI-42-5 Et H H CH2Ph Bz F F F OH H H XVI-42-6 Et H H CH2-indol-3-yI Bz F F F OH H H XVI-42-7 Et H H CH2CH2SCH3 Bz F F F OH H H XVI-42-8 Et * H * Bz F F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table X VI-43.

Xa R1" R2 r3. R3b R4 R5 R6 X Y R' R8 XVI-43-1 H H H Bz F F F OH H H XVI-43-2 'Pr H H ch3 Bz F F F OH H A XVI-43-3 'Pr H H CH» Bz F F F OH H H XVI-43-4 'Pr H H CH2CH(CH3)2 Bz F F F OH H H XVI-43-5 'Pr H H CH2Ph Bz F F F OH H H XVI-43-6 'Pr H H CH2-indol-3-yl Bz F F F OH H H XVI-43-7 'Pr H H CH2CH2SCH3 Bz F F F OH H H XVI-43-8 ‘Pr ♦ H ♦ Bz F F F OH H H 10 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XVI-44.

Xs R1 R3 R3’ R3b R4 Rs R6 X Y R7 r“ XVI-44-1 'Bu H H H Bz F F F OH H H XVI-44-2 'Bu H H ch3 Bz F F F OH H H XVI-44-3 'Bu H H CH(CH3)2 Bz F F F OH H H XVI-44-4 'Bu H H CH2CH(CH3)2 Bz F F F OH H H XVI-44-5 'Bu H H CH2Ph Bz F F F OH H H XVI-44-6 'Bu H H CH2-indol-3-yl Bz F F F OH H H XVI-44-7 'Bu H H CH2CH2SCH3 Bz F F F OH H H XVI-44-8 _ J P 'Bu 7Jb· Γ. * H * Bz F F F OH H H *R2 and R3b joined together by (Cl^b to form five-membered ring. 2983472-1 -379- WO 2008/121634 PC17US2008/058183

Docket No. 6013 7.0034WOU1

Table X VI-45.

Xs R1 R3 R3r R3b R4 R* R6 X Y r’ ip- XVII-45-1 Ph H H H Bz F F F OH H H XVII-45-2 Ph H H ch3 Bz F F F OH H H XVII-45-3 Ph H H CH(CH3)j Bz F F F OH H H XVII-45-4 Ph H H CH2CH(CH3)2 Bz F F F OH H H XVII-45-5 Ph H H CH2Ph Bz F F F OH H H XVII-45-6 Ph H H CH2-indol-3-yl Bz F F F OH H H XVII-45-7 Ph H H ch2ch2sch3 Bz F F F OH H H XVII-45-8 _ . r> Ph 3b; ϊ * H * Bz F F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVI-46.

X2 R1 R3 “R3r “r36 R4 “F R6 X Y R’ Ra XVII-46-1 p-Me-Ph H H H Bz F F F OH H H XVII-46-2 p-Me-Ph H H ch3 Bz F F F OH H H XVII-46-3 p-Me-Ph H H CH(CH3)2 Bz F F F OH H H XVII-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz F F F OH H H XVII-46-5 p-Me-Ph H H CH2Ph Bz F F F OH H H XVII-46-6 p-Me-Ph H H CH2-indol-3-yl Bz F F F OH H H XVII-46-7 p-Me-Ph H H CH2CH2SCH3 Bz F F F OH H H XVIM6-8 p-Me-Ph * H ♦ Bz F F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table X VI-47.

> M ' ! I·——. U

X° R1 R2 R3« R3b R4 Rs R6 X Y R7 R“ XVU-47-1 p-F-Ph H H H Bz F F F OH H H XVII-47-2 p-F-Ph H H CH3 Bz F F F OH H H XVII-47-3 p-F-Ph H H ΟΗ(ΟΗ3)2 Bz F F F OH H H XVII-47-4 p-F-Ph H H CH2CH(CH3)2 Bz F F F OH H H XVII-47-5 p-F-Ph H H CH2Ph Bz F F F OH H H XVII-47-6 p-F-Ph H H CH2-indol-3-yl Bz F F F OH H H XVII-47-7 p-F-Ph H H CH2CH2SCH3 Bz F F F OH H H XVI1-47-8 p-F-Ph * H * Bz F F F OH H H *R2 and R36 joined together by (CTfeh to form five-membered ring. 2983472-1 -380- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/G58183

Table XVI-48.

Na R1 Έ -pr ηρΕ R4 R5 R6 X Y R7 XVII-48-1 p-Cl-Ph H H H Bz F F F OH H H XVII-48-2 p-Cl-Ph H H ch3 Bz F F F OH H H XVII-48-3 p-CI-Ph H H CH(CH3)2 Bz F F F OH H H XVII-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz F F F OH H H XVII-48-5 p-Cl-Ph H H CH2Ph Bz F F F OH H H XVII-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz F F F OH H H XVII-48-7 p-Cl-Ph H H CH2CH2SCH3 Bz F F F OH H H XVII-48-8 p-Cl-Ph ♦ H * Bz F F F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XVI-49.

N° R1 R2 Rj. R3b R4 R3 R6 X Y R' R8 XVII-49-1 p-Br-Ph H H H Bz F F F OH H H XVII-49-2 p-Br-Ph H H CH3 Bz F F F OH H H XVII-49-3 p-Br-Ph H H CHfCH^ Bz F F F OH H H XVII-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz F F F OH H H XVII-49-5 p-Br-Ph H H CH2Ph Bz F F F OH H H XVII-49-6 p-Br-Ph H H CH2-indol-3-yI Bz F F F OH H H XVI1-49-7 p-Br-Ph H H CH2CH2SCH3 Bz F F F OH H H XVII-49-8 p-Br-Ph * H * Bz F F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XVI-50. --- I-X-_ ML"— ' J-ΤΊ-_ Jt"’ __---- * •zru-

Na R' R2 RJa R3b R4 R5 R6 X Y R2 R“ XVII-50-1 p-I-Ph H H H Bz F F F OH H H XVII-50-2 p-I-Ph H H CH3 Bz F F F OH H H XV1I-50-3 p-I-Ph H H CH(CH3)2 Bz F F F OH H H XVII-50-4 p-I-Ph H H CHjCHCCHah Bz F F F OH H H XVII-50-5 p-I-Ph H H CH2Ph Bz F F F OH H H XVII-50-6 p-l-Ph H H CH2-indol-3-yl Bz F F F OH H H XVII-50-7 p-l-Ph H H CH2CH2SCH3 Bz F F F OH H H XVII-50-8 J nJ p-I-Ph b: ϊ - J * H * Bz F F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring 29S3472-1 -381- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

XVII

Table XVII-1.

Xs R1 R2 T7- R3b R4 Rs ~R*“ X Y Iv IF xvn-l-l ch3 H H H ch3 F H F OH H H XVII-1-2 ch3 H H ch3 ch3 F H F OH H H XVII-1-3 ch3 H H CH(CH3)2 ch3 F H F OH H H XVII-1-4 ch3 H H CHjCHCCHah ch3 F H F OH H H XVII-1-5 ch3 H H CH2Ph ch3 F H F OH H H XVII-1-6 ch3 H H CH2-indol-3-yl ch3 F H F OH H H XVII-1-7 ch3 H H CH2CH2SCH3 ch3 F H F OH H H XVII-1-8 ch3 ♦ H * ch3 F H F OH H H *R2 and Rejoined together by (CHj)j to form five-membered ring.

Table XVII-2.

Ns ΊΓ R2 rJ. R3b R4 R5 R8- X Y ΊΓ r” XVII-2-1 Et H H H CH3 F H F OH H H XVII-2-2 Et H H ch3 ch3 F H F OH H H XVII-2-3 Et H H CH(CH3)2 ch3 F H F OH H H XVII-2-4 Et H H CH2CH(CH3)2 ch3 F H F OH H H XVII-2-5 Et H H CH2Ph ch3 F H F OH H H XVII-2-6 Et H H CH2-indol-3-yl ch3 F H F OH H H XVH-2-7 Et H H CH2CH2SCH3 ch3 F H F OH H H XVII-2-8 *t~.2 j 1-. Et 3ΤΓ77 * H * ch3 F H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -382- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XVII-3.

Xs R1 ΊΓ R3a R3b “r*~ R5 X Y R7 r“ XVII-3-1 "W H H H ch3 F H F OH H H XVII-3-2 'Pr H H ch3 ch3 F H F OH H H XVII-3-3 'Pr H H CH(CH3)2 ch3 F H F OH H II XVII-3-4 'Pr H H CH2CH(CH3)2 ch3 F H F OH H H XVII-3-5 ipr H H CH2Ph ch3 F H F OH H H XVII-3-6 'Pr H H CH2-indol-3-yl ch3 F H F OH H H XVII-3-7 'Pr H H CH2CH2SCH3 ch3 F H F OH H H XVII-3-8 'Pr * H * ch3 F H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVII-4.

X° T" R1 “r37· R3b R4’ Rr R6 X Y R7 RB XVII-4-1 H H H ch3 F Η F OH H H XVII-4-2 'Bu H H CH3 ch3 F H F OH H H XVII-4-3 'Bu H H CH(CH3)2 ch3 f H F OH H H XVH-4-4 feu H H CH2CH(CH3)2 ch3 f H F OH H H XVII-4-5 'Bu H H CH2Ph ch3 f H F OH H H XVII-4-6 'Bu H H CH2-indol-3-yl ch3 f H F OH H H XVII-4-7 'Bu H H CH2CH2SCH3 ch3 f H F OH H H XVH-4-8 'Bu ♦ H ♦ ch3 f H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. Table XVII-5. X2 R RJ Rj. R3b R4 R5 R6 X Y R r“ XVII-5-1 Ph H H H ch3 f H F OH H H XVII-5-2 Ph H H CH3 ch3 f H F OH H H XVH-5-3 Ph H H CH(CH3)2 ch3 f H F OH H H XVII-5-4 Ph H H CH2CH(CH3)2 ch3 f H F OH H H XVH-5-5 Ph H H CH2Ph ch3 f H F OH H H XVII-5-6 Ph H H CH2-indoI-3-yl ch3 f H F OH H H XVII-5-7 Ph H H CH2CH2SCH3 ch3 f H F OH H H XVII-5-8 jt-, Ph 35777 * H ♦ ch3 f H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -383- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XVII-6.

Xs R1 R2 ΊΡ5- --- ΊΓ” R4 X Y IT Ra XVII-6-1 p-Me-Ph H H H ch3 F H F OH H H XVII-6-2 p-Me-Ph H H ch3 ch3 F H F OH H H XVII-6-3 p-Me-Ph H H CH(CH3)2 ch3 F H F OH H H XVII-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 F H F OH H H XVII-6-5 p-Me-Ph H H CH2Ph ch3 F H F OH H H XVII-6-6 p-Me-Ph H H CH2-indol-3-yl ch3 F H F OH H H XVII-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 F H F OH H H XVII-6-8 p-Me-Ph ♦ H ♦ ch3 F H F OH H H *R2 and R3b joined together by (CiHhb to form five-membered ring.

Table XVII-7.

Xs R' R2 R3· R4 R5 R4 X Y I? r“ XVII-7-1 p-F-Ph H H H CH3 F H F OH H H XVI1-7-2 p-F-Ph H H ch3 ch3 F H F OH H H XVII-7-3 p-F-Ph H H CH(CH3)2 ch3 F H F OH H H XVII-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 F H F OH H H XVII-7-6 p-F-Ph H H CH2Ph ch3 F H F OH H H XVI1-7-7 p-F-Ph H H CHrindol-3-yl ch3 F H F OH H H XVH-7-8 p-F-Ph H H CH2CH2SCH3 ch3 F H F OH H H XVII-7-20 p-F-Ph * H * ch3 F H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XVII-8. ' ' I ' '“n H RL ' . I . '

Xs R1 R2 r3. R3b I? Ic R4 X Υ R7 R8 XVII-8-1 p-Cl-Ph H H H ch3 F H F ΟΗ Η Η XVII-8-2 p-Cl-Ph H H ch3 ch3 F H F ΟΗ Η Η XVII-8-3 p-Cl-Ph H H CH(CH3)2 ch3 F H F ΟΗ Η Η XVII-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 F Η F ΟΗ Η Η XVII-8-5 p-Cl-Ph H H CH2Ph ch3 F Η F ΟΗ Η Η XVII-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 F Η F ΟΗ Η Η XVn-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 F Η F ΟΗ Η Η XVH-8-8 *772“ J r p-Cl-Ph —77 * H * ch3 F Η F ΟΗ Η Η *R2 and RJb joined together by (CH^ to form five-membered ring. 2983472-1 -384- WO 2008/121634

Docket No. 60137.0034WOU1 PCTZUS2008/058183

Table XVII-9.

Ns "R1 R3a IF ΊΓ“ R5 R6 X Y R7 r“ XVII-9-1 p-Br-Ph H H H ch3 F H F OH H H XVII-9-2 p-Br-Ph H H ch3 ch3 F H F OH H H XVII-9-3 p-Br-Ph H H CHiCHak ch3 F H F OH H H XVlI-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 F H F OH H H XVII-9-6 p-Br-Ph H H CH2Ph ch3 F H F OH H H XVII-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 F H F OH H H XVII-9-8 p-Br-Ph H H CH2CH2SCH3 ch3 F H F OH H H XVH-9-20 p-Br-Ph * H * ch3 F H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVII-10.

Ns R1 R2 R3. R3b R* R1 R6 X Υ R' R XVII-10-1 p-I-Ph H H H CH3 F Η F ΟΗ Η Η XVII-10-2 p-I-Ph H H ch3 ch3 F Η F ΟΗ Η Η XVII-10-3 p-I-Ph H H CH(CH3)2 ch3 F Η F ΟΗ Η Η XVII-10-4 p-I-Ph H H CH2CH(CH3)2 ch3 F Η F ΟΗ Η Η XVII-10-5 p-I-Ph H H CH2Ph ch3 F Η F ΟΗ Η Η XVII-10-6 p-I-Ph H H CH2-indol-3-yl ch3 F Η F ΟΗ Η Η XVII-10-7 p-I-Ph H H CH2CH2SCH3 ch3 F Η F ΟΗ Η Η XVII-10-8 p-I-Ph * H * ch3 F Η F ΟΗ Η Η *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XVII-11. " I ft IL·”· M U-!

Ns R R2 Rj« R3b R4 R5 R6 X Y RT R8 XVII-11-1 ch3 H H H Et F H F OH H H XVII-11-2 ch3 H H ch3 Et F H F OH H H XVII-11-3 ch3 H H CH(CH3)2 Et F H F OH H H XVII-11-4 ch3 H H CH2CH(CH3)2 Et F H F OH H H XVII-11-5 ch3 H H CH2Ph Et F H F OH H H XVII-11-6 ch3 H H CH2-indol-3-yl Et F H F OH H H ΧνΐΙ-11-7 ch3 H H CH2CH2SCH3 Et F H F OH H H XVII-11-8 . τ,' ch3 15"· ; '. * H ♦ Et F H F OH H H *R2 and Rejoined together by (CHib to form five-membered ring. 2983472-1 385 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XVJI-12.

Na R1 R2 R3a R4 R5 R6 X Y R7 R8 XVH-12-1 Et H H H Et F H F OH H H XVII-12-2 Et H H ch3 Et F H F OH H H XVH-12-3 Et H H CH(CH3)2 Et F H F OH H H XVII-12-4 Et H H CH2CH(CH3)2 Et F H F OH H H XVII-12-5 Et H H CH2Ph Et F H F OH H H XVH-12-6 Et H H CH2-indol-3-yl Et F H F OH H H XVII-12-7 Et H H CH2CH2SCH3 Et F H F OH H H XVII-12-8 Et * H ♦ Et F H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring

Table XVII-13.

Ns R1 R2 r3. R4 ΊΓ R6 X Y R7" R8 XVII-13-1 'Pr H H H Et F H F OH H H XVII-13-2 'Pr H H CH3 Et F H F OH H H XVII-13-3 'Pr H H CH(CH3)2 Et F H F OH H H XVII-13-4 'Pr H H CH2CH(CH3)2 Et F H F OH H H XVII-13-5 'Pr H H CH2Ph Et F H F OH H H XVII-13-6 'Pr H H CH2-indol-3-yl Et F H F OH H H XVn-13-7 'Pr H H CH2CH2SCH3 Et F H F OH H H XVII-13-8 'Pr * H * Et F H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. Table XVII-14.

Ns R1 -jpr- "R35 R4 Ί7" R6 X Y R7 R8 XVH-14-1 "^7“ H H H Et F H F OH H H XVII-14-2 'Bu H H CH3 Et F H F OH H H XVII-14-3 'Bu H H emeu), Et F H F OH H H XVII-14-4 'Bu H H CH2CH(CH3)2 Et F H F OH H H XVJI-14-5 'Bu H H CH2Ph Et F H F OH H H XVII-14-6 'Bu H H CH2-indol-3-yl Et F H F OH H H XVII-14-7 'Bu H H CH2CH2SCH3 Et F H F OH H H XVII-14-8 'Bu • H * Et F H F OH H H *R2 and Rejoined together by (0¾^ to form five-membered ring. 2983472-1 386- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XVII-15.

Xs R1 R2 Ria R3b R5 T" X Y iv R“ XVII-15-1 Ph H H H Et F H F OH H H XVII-15-2 Ph H H ch3 Et F H F OH H H XV1I-15-3 Ph H H CH(CH3)2 Et F H F OH H H XVII-15-4 Ph H H CH2CH(CH3)2 Et F H F OH H H XVII-15-5 Ph H H CH2Ph Et F H F OH H H XVII-15-6 Ph H H CH2-indol-3-yl Et F H F OH H H XVII-15-7 Ph H H CH2CH2SCH3 Et F H F OH H H XVII-15-8 Ph ) · : * H * Et F H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVII-16.

Xs R1 R2 R3’ "r35 R4 Rs R4 X Y R’ r“ XVH-16-1 p-Me-Ph H H H Et F H F OH H H XVI I-16-2 p-Me-Ph H H CH3 Et F H F OH H H XVII-16-3 p-Me-Ph H H CH(CH3)2 Et F H F OH H H XVII-16-4 p-Me-Ph H H CH2CH(CH3)3 Et F H F OH H H XVII-16-5 p-Me-Ph H H CH2Ph Et F H F OH H H XVII-16-6 p-Me-Ph H H CHrindol-3-yl Et F H F OH H H XVII-16-7 p-Me-Ph H H CH2CH2SCH3 Et F H F OH H H XVII-16-8 p-Me-Ph * H « Et F H F OH H H *lV and R3” joined together by (CH2)3 to form five-membered ring. 5 Table XVII-17. , I·—, I Ill- III J g Λ - . - Ο

X° Rl R2 R3’ R3b R4 Rs R4 X Y R7 Ra XVII-17-1 p-F-Ph H H H Et F H F OH H H XVII-17-2 p-F-Ph H H CH3 Et F H F OH H H XVII-17-3 p-F-Ph H H CH(CH3)2 Et F H F OH H H XVII-17-4 p-F-Ph H H CH2CH(CH3)2 Et F H F OH H H XVII-17-5 p-F-Ph H H CH2Ph Et F H F OH H H XVII-17-6 p-F-Ph H H CH2-indol-3-yl Et F H F OH H H XVII-17-7 p-F-Ph H H CH2CH2SCH3 Et F H F OH H H XVII-17-8 l·'" J nJ p-F-Ph bi! J x * H * Et F H F OH H H *R2 and Rejoined together by (0¾^ to form five-membered ring. 2983472-1 -387- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XVII-18.

Xs R1 R2 ηρτ “R315 R4 R6 X Y iT Rb XVH-18-1 p-Cl-Ph H H H Et F H F OH H H XVII-18-2 p-Cl-Ph H H ch3 Et F H F OH H H XVII-18-3 p-Cl-Ph H H CH(CH3)2 Et F H F OH H H XVII-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et F H F OH H H XVII-18-5 p-Cl-Ph H H CH2Ph Et F H F OH H H XVII-18-6 p-Cl-Ph H H CH2-indol-3-yl Et F H F OH H H XVII-18-7 p-Cl-Ph H H CH2CH2SCH3 Et F H F OH H H XVII-18-8 p-Cl-Ph * H 4 Et F H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVII-19.

Ns Rl R2 Rj0 R3b R4 R5 R6 X Y R' R8 XVII-19-1 p-Br-Ph H H H Et F H F OH H H XVII-19-2 p-Br-Ph H H CH3 Et F H F OH H H XVII-19-3 p-Br-Ph H H CH(CH3)2 Et F H F OH H H XVII-19-4 p-Br-Ph H H CH2CH(CH3)2 Et F H F OH H H XVII-19-5 p-Br-Ph H H CH2Ph Et F H F OH H H XVII-19-6 p-Br-Ph H H CH2-indol-3-yt Et F H F OH H H XVII-19-7 p-Br-Ph H H CH2CH2SCH3 Et F H F OH H H XVlI-19-8 p-Br-Ph * H * Et F H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XVII-20. " 1 ' I"· J. III. - » 1··^ . 11' ‘

Xs R1 R2 R3a R3b R4 R6 X Y R7 R1 XVII-20-1 p-I-Ph H H H Et F H F OH H H XVII-20-2 p-I-Ph H H CH3 Et F H F OH H H XVII-20-3 p-I-Ph H H ΟΗ(ΟΗ3)2 Et F H F OH H H XVII-20-4 p-I-Ph H H CH2CH(CH3)2 Et F H F OH H H XVII-20-5 p-I-Ph H H CH2Ph Et F H F OH H H XVII-20-6 p-I-Ph H H CH2-indot-3-yl Et F· H F OH H H XVII-20-7 p-I-Ph H H CH2CH2SCH3 Et F H F OH H H XVII-20-8 p-I-Ph * H * Et F H F OH H H ♦R2 and RJb joined together by (CH2)3 to form five-membered ring. »83472-1 -388- WO 2008/121634 PCT/US2008/058183

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Table XVII-2L

Xs "F ” ΊΓ R3a “R36 R4 R5 R0 X Y F F XVII-21-1 ch3 H H H "W F H F OH H H XVII-21-2 ch3 H H ch3 'Pr F H F OH H H XVII-21-3 ch3 H H CH(CH3)2 'Pr F H F OH H H XVII-21-4 ch3 H H CH2CH(CH3)2 'Pr F H F OH H H XVH-21-5 ch3 H H CH2Ph 'Pr F H F OH H H XVII-21-6 ch3 H H CH2-indol-3-yl 'Pr F H F OH H H XVII-21-7 ch3 H H CH2CH2SCH3 'Pr F H F OH H H XVII-21-8 ch3 * H * 'Pr F H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XVII-22.

Xs R1 R2 R3a "R^- R4 Rs R6 X Y ΊΓ R* XVII-22-1 Et H H H ~W F H F OH H H XVII-22-2 Et H H CH3 'Pr F H F OH H H XVII-22-3 Et H H CH(CH3)3 'Pr F H F OH H H XVII-22-4 Et H H CH2CH(CH3)2 'Pr F H F OH H H XVH-22-5 Et H H CH2Ph 'Pr F H F OH H H XVn-22-6 Et H H CHrindol-3-yl 'Pr F H F OH H H XVII-22-7 Et H H CH2CH2SCH3 'Pr F H F OH H H XVII-22-8 '"TrU Et b ; ·. * H * 'Pr F H F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Xs “r1” R2 R3“ "R35 R4 RJ R6 X Y r" Rb XVII-23-1 'Pr H H H F H F OH H H XV1I-23-2 fpr H H CH3 'Pr F H F OH H H XVn-23-3 'Pr H H CH(CH3)2 'Pr F H F OH H H XVII-23-4 'Pr H H CH2CH(CH3)2 'Pr F H F OH H H XVII-23-5 'Pr H H CH2Ph 'Pr F H F OH H H XVII-23-6 'Pr H H CH2-indol-3-yl 'Pr F H F OH H H XVII-23-7 'Pr H H CH2CH2SCH3 'Pr F H F OH H H XVII-23-8 'Pr * H * 'Pr F H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -389' WO 2008/121634 PCT/US2008/058183

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Table XVII-24.

Xa R1 R2 "R33” R- ΊΓ TT X Y F R8 XVII-24-1 'Bu H H H F H F OH H H XVII-24-2 'Bu H H ch3 'Pr F H F OH H H XVII-24-3 'Bu H H CH(CH3)2 'Pr F H F OH H H XVII-24-4 'Bu H H CH2CH(CH,)2 'Pr F H F OH H H XVII-24-5 'Bu H H CH2Ph 'Pr F H F OH H H XVII-24-6 'Bu H H CH2-Lndol-3-yl 'Pr F H F OH H H XVII-24-7 'Bu H H CH2CH2SCH3 <pr F H F OH H H XV1I-24-8 'Bu * H « 'Pr F H F OH H H *RZ and Rejoined together by (CH^ to form five-membered ring.

Table XVU-25. " ............... I M m

Xa Rl R2 R” R3b R4 R5 R6 X Y R7 R8 XVII-25-1 Ph H H H “W F H F OH H H XVII-25-2 Ph H H ch3 'Pr F H F OH H H XVII-25-3 Ph H H CH(CH3)2 'Pr F H F OH H H XVII-25-4 Ph H H CH2CH(CH3)2 'Pr F H F OH H H XVII-25-5 Ph H H CH2Ph 'Pr F H F OH H H XVII-25-6 Ph H H CH2-indol-3-yl 'Pr F H F OH H H XVII-25-7 Ph H H CH2CH2SCH3 'Pr F H F OH H H XVII-25-8 Ph * H * 'Pr F H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Xa r‘ R2 r3« "r35 RJ R6 X Y r’ R8 XVII-26-1 p-Me-Ph H H H F H F OH H H XVII-26-2 p-Me-Ph H H ch3 'Pr F H F OH H H XVII-26-3 p-Me-Ph H H CH(CH3)2 'Pr F H F OH H H XVII-26-4 p-Me-Ph H H CH2CH(CH3)2 'Pr F H F OH H H XVII-26-5 p-Me-Ph H H CH2Ph 'Pr F H F OH H H XVII-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr F H F OH H H XVU-26-7 p-Me-Ph H H CH2CH2SCH3 'Pr F H F OH H H XVH-26-8 p-Me-Ph ♦ H * 'Pr F H F OH H H *R2 and Rejoined together by (0¾¼ to form five-membered ring. 2983472-1 -390- WO 2008/121634 PCT/US2008/058183

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Table XV11-27. D1

Xs R’ R2 R3‘ R3b R4 R3 R6 X Y R7 R8 XVII-27-1 p-F-Ph Η Η H 'Pr F H F OH Η H XVII-27-2 p-F-Ph Η H CH3 'Pr F H F OH Η H XVn-27-3 p-F-Ph Η H CH(CH3)2 fPr F H F OH Η H XVII-27-4 p-F-Ph Η H CH2CH(CH3)2 'Pr F H F OH Η H XVH-27-5 p-F-Ph Η H CH2Ph 'Pr F H F OH Η H XVII-27-6 p-F-Ph Η H CH2-indol-3-yl 'Pr F H F OH Η H XVII-27-7 p-F-Ph Η H CH2CH2SCH3 'Pr F H F OH Η H XVII-27-8 p-F-Ph * H * 'Pr F H F OH Η H *R2 and RJb joined together by (CH2)3 to form five-membered ring. Table XVI1-28. Xs Rl R2 R3" R5b R4 R3 R6 X Y R7 R8 XVH-28-1 p-Cl-Ph Η Η H JPr F" H F OH Η H XVII-28-2 p-Cl-Ph Η H CH3 'Pr F H F OH Η H XVII-28-3 p-Cl-Ph Η H CH(CH3)2 'Pr F H F OH Η H XVII-28-4 p-Ci-Ph Η H CH2CH(CH3)2 'Pr F H F OH Η H XVII-28-5 p-Cl-Ph Η H CH2Ph 'Pr F H F OH Η H XVII-28-6 p-Cl-Ph Η H CH2-indoI-3-yl 'Pr F H F OH Η H XVH-28-7 p-Cl-Ph Η H CH2CH2SCH3 'Pr F H F OH Η H XVII-28-8 p-Cl-Ph ♦ H * 'Pr F H F OH Η H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Xs R‘ R2 rJ. R4 R4 X Y ΊΓ Ra XVII-29-1 p-Br-Ph H H H 'Pr F H F OH H H XVII-29-2 p-Br-Ph H H ch3 'Pr F H F OH H H XV11-29-3 p-Br-Ph H H CH(CH3)2 'Pr F H F OH H H XVII-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr F H F OH H H XVII-29-5 p-Br-Ph H H CH2Ph 'Pr F H F OH H H XVII-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr F H F OH H H XVII-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr F H F OH H H XVI1-29-8 p-Br-Ph * H ♦ 'Pr F H F OH H H *R2 and RJ0 joined together by (CHjb to form five-membered ring. 2983472-1 -391 - WO 2008/121634 PCT/US2008/058183

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Table XVIl-30.

Ns R' R2 R3a R4 R* R6 X Y R R3 XVII-30-1 p-l-Ph H H H JPr F H F OH H H XVII-3G-2 p-I-Ph H H ch3 'Pr F H F OH H H XVII-30-3 p-I-Ph H H CH(CH3)2 'Pr F H F OH H H XVII-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr F H F OH H H XVII-30-5 p-I-Ph H H CH2Ph 'Pr F H F OH H H XVII-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr F H F OH H H XV1I-3Q-7 p-I-Ph H H CH2CH2SCH3 'Pr F H F OH H H XVII-30-8 p-I-Ph * H ♦ 'Pr F H F OH H H *RJ and Rejoined together by (CH2)aTto form five-membered ring.

Table XVII-31.

Na R RJ Rj. R3b R^ Rs R6 X Y R' R" XVII-31-1 CH3 H H H "Bu F H F OH H H XVII-31-2 ch3 H H ch3 "Bu F H F OH H H XVII-31-3 ch3 H H CH(CH3)2 "Bu F H F OH H H XVII-31-4 ch3 H H CH2CH(CH3)2 "Bu F H F OH H H XVII-31-5 ch3 H H CH2Ph "Bu F H F OH H H XVII-31-6 ch3 H H CH2-indol-3-yl "Bu F H F OH H H XVII-31-7 ch3 H H CH2CH2SCH3 "Bu F H F OH H H XVII-31-8 ch3 * H * "Bu F H F OH H H *RJ and R3b joined together by (Cthb to form five-membered ring. 5 Table XVII-32.

— — I R Jl- ' 4L ........ - J g -*— U

Ns R R2 R3‘ R3b R4 Rs R6 X Y R7 R1 XVII-32-1 Et H H H "Bu F H F OH H H XVII-32-2 Et H H ch3 "Bu F H F OH H H XVII-32-3 Et H H CH(CH3)2 "Bu F H F OH H H XVII-32-4 Et H H CH2CH(CH3)2 "Bu F H F OH H H XVII-32-5 Et H H CH2Ph "Bu F H F OH H H XVII-32-6 Et H H CH2-indol-3-yl "Bu F H F OH H H XVII-32-7 Et H H CH2CH2SCH3 "Bu F H F OH H H XVII-32-8 Et * H * "Bu F H F OH H H *R2 and R30 joined together by (0¾^ to form five-membered ring. 2983472-1 -392- WO 2008/121634 PCT/US2008/058183

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Table XVII-33.

Ns Rl R11 r3. R3b R4 R5 IF X Y ΊΓ I? XVII-33-1 'Pr H H H "Bu F H F OH H H XV1I-33-2 'Pr H H ch3 "Bu F H F OH H H XVH-33-3 'Pr H H CH(CH3)2 "Bu F H F OH H H XVII-33-4 ipr H H CH2CH(CH3)2 "Bu F H F OH H H XVII-33-5 'Pr H H CH2Ph "Bu F H F OH H H XVH-33-6 'Pr H H CH2-indol-3-yl "Bu F H F OH H H XVII-33-7 'Pr H H CH2CH2SCH3 "Bu F H F OH H H XVII-33-8 'Pr * H * "Bu F H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVII-34.

Ns R1^ R2 R3’ R3b R4 R5 Rb X Y R7 R8 XVII-34-1 'Bu H H H "Bu F H F OH H H XVII-34-2 'Bu H H ch3 "Bu F H F OH H H XVU-34-3 'Bu H H CHCCHa), "Bu F H F OH H H XVII-34-4 'Bu H H CH2CH(CH3)2 "Bu F H F OH H H XVII-34-5 'Bu H H CH2Ph "Bu F H F OH H H XVH-34-6 'Bu H H CH2-indol-3-yl "Bu F H F OH H H XVII-34-7 'Bu H H CH2CH2SCH3 "Bu F H F OH H H XVII-34-8 'Bu * H * "Bu F H F OH H H *R2 and joined together by (CH^ to form five-membered ring. 5 Table XVII-35. 11 1 R — Ιί. 1 IL '" J 1 ' -- W IT"

Ns R RJ rJ« R3b R4 ΊΓ R6 X Y R7 R8 XVII-35-1 Ph H H H "Bu F H F OH H H XVII-35-2 Ph H H ch3 "Bu F H F OH H H XVI1-35-3 Ph H H CH(CH3)a "Bu F H F OH H H XVII-35-4 Ph H H CH2CH(CH3)2 "Bu F H F OH H H XVII-35-5 Ph H H CH2Ph "Bu F H F OH H H XVII-35-6 Ph H H CH2-indol-3-yl "Bu F H F OH H H XVII-35-7 Ph H H CH2CH2SCH3 "Bu F H F OH H H XVII-35-8 ~ΙτΓ2-ΤΤΓ Ph Jb : ' * H * "Bu F H F OH H H ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -393- WO 2008/121634 PCT/US2008/058183

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Table XVII-36.

Ns Rl Ί?’ R3ir R3b R4 RJ R6 X Y r’ IF XVII-36-1 p-Me-Ph H H H "Bu F H F OH H H XVII-36-2 p-Me-Ph H H ch3 "Bu F H F OH H H XVH-36-3 p-Me-Ph H H CHiCHOz "Bu F H F OH H H XVII-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu F H F OH H H XVH-36-5 p-Me-Ph H H CH2Ph "Bu F H F OH H H XVII-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu F H F OH H H XVII-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu F H F OH H H XVII-36-8 p-Me-Ph * H * "Bu F H F OH H H *R2 and R3” joined together by (CH2)3 to form five-membered ring.

Table XVII-37.

Ns Rl RJ R3‘ R3b R4 R5 R6 X Y R7 R“ XVII-37-1 p-F-Ph H H H "Bu F H F OH H H XVII-37-2 p-F-Ph H H ch3 "Bu F H F OH H H XVII-37-3 p-F-Ph H H CH(CH3)z "Bu F H F OH H H XVII-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu F H F OH H H XVII-37-5 p-F-Ph H H CH2Ph "Bu F H F OH H H XVH-37-6 p-F-Ph H H CH2-mdot-3-yl "Bu F H F OH H H XVU-37-7 p-F-Ph H H CH2CH2SCH3 "Bu F H F OH H H XVI1-37-8 p-F-Ph * H * "Bu F H F OH H H *R2 and RJb joined together by (CHib to form five-membered ring. 5 Table XVII-38,

» ' i ” 111" " -. "2 - B

Ns R1 Ra R3" R3b R4 R3 R6 X Y R7 Ra XVn-38-1 p-Cl-Ph H H H "Bu F H F OH H H XVII-38-2 p-Cl-Ph H H ch3 "Bu F H F OH H H XVII-38-3 p-Cl-Ph H H CHCCH^ "Bu F H F OH H H XVII-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu F H F OH H H XVH-38-5 p-Cl-Ph H H CH2Ph "Bu F H F OH H H XVII-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu F H F OH H H XVn-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu F H F OH H H XVII-38-8 p-Ci-Ph b~~; · LjT * H ♦ "Bu F H F OH H H *R2 and R^b joined together by (CH2)3 to form five-membered ring. 2983472-1 -394- WO 2008/121634 PCT/US2008/058183

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Table XVII-39.

X2 R1 R2 RJa T5 R4 R3 R6 X Y R r“ XVII-39-1 p-Br-Ph H H H "Bu F H F OH H H XVII-39-2 p-Br-Ph H H ch3 "Bu F H F OH H H XV1I-39-3 p-Br-Ph H H CH(CH3)2 "Bu F H F OH H H XVI1-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu F H F OH H H XVII-39-5 p-Br-Ph H H CH2Ph "Bu F H F OH H H XVII-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu F H F OH H H XVI1-39-7 p-Br-Ph H H ch2ch2sch3 "Bu F H F OH H H XVI1-39-8 p-Br-Ph * H * "Bu F H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVII-40.

Xe R1 R2 Rj. R3b R4 R3 R6 X Y R' R8 XVI1-40-1 p-I-Ph H H H "Bu F H F OH H H XVII-40-2 p-I-Ph H H CHj "Bu F H F OH H H XVII-40-3 p-I-Ph H H CHiCHa), "Bu F H F OH H H XVII-40-4 p-I-Ph H H CHjCHCCHa}, "Bu F H F OH H H XVII-40-5 p-I-Ph H H CH2Ph "Bu F H F OH H H XVII-40-6 p-I-Ph H H CH2-indol-3-yl "Bu F H F OH H H XVII-40-7 p-I-Ph H H CH2CH2SCH3 "Bu F H F OH H H XVII-40-8 p-I-Ph * H * "Bu F H F OH H H ♦R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XVII-41. - | —< Mil — » - ,1.-,,...- - ... "-It— X° R R2 Rj. R3b R4 R3 R6 X Υ R7 R# XVII-41-1 CH3 H H H Bz F H F ΟΗ Η Η XVII-41-2 ch3 H H ch3 Bz F H F ΟΗ Η Η XVH-41-3 ch3 H H CH(CH3)2 Bz F Η F ΟΗ Η Η XVII-41-4 ch3 H H CH2CH(CH3)2 Bz F Η F ΟΗ Η Η XVII-41-5 ch3 H H CH2Ph Bz F Η F ΟΗ Η Η XVII-41-6 ch3 H Η CH2-indol-3-yl Bz F Η F ΟΗ Η Η XVI1-41-7 ch3 Η H CH2CH2SCH3 Bz F Η F ΟΗ Η Η XVII-41-8 ch3 ♦ H * Bz F Η F ΟΗ Η Η *R2 and Rejoined together by ((¾^ to form five-membered ring. 2983472-1 -395- WO 2008/121634

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Table XVII-42.

Ns R1 R3 R3b RJ R6 X Y R7 R’ XVI1-42-1 Et H H H Bz F H F OH H H XVII-42-2 Et H H ch3 Bz F H F OH H H XVII-42-3 Et H H CH(CH3)2 Bz F H F OH H H XVH-42-4 Et H H CH2CH(CH3)2 Bz F H F OH H H XVI1-42-5 Et H H CH2Ph Bz F H F OH H H XVII-42-6 Et H H CH2-indoI-3-yl Bz F H F OH H H XVII-42-7 Et H H CH2CH2SCH3 Bz F H F OH H H XVII-42-8 Et * H * Bz F H F OH H H *R2 and RJt> joined together by (CH2)3 to form five-membered ring.

Table XVII-43.

Na R R3 r3> R3b R4 R* R6 X Y R R8 XVII-43-1 'Pr H H H Bz F H F OH H H XViI-43-2 'Pr H H ch3 Bz F H F OH H pi XVII-43-3 'Pr H H ΟΗ(ΟΗ3)2 Bz F H F OH H H XVII-43-4 ipr H H CH2CH(CH3)2 Bz F H F OH H H XVH-43-5 'Pr H H CH2Ph Bz F H F OH H H XVII-43-6 'Pr H H CH2-indol-3-y1 Bz F H F OH H H XVII-43-7 'Pr H H CH2CH2SCH3 Bz F H F OH H H XVI1-43-8 'Pr ♦ H * Bz F H F OH H H 10 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XVII-44.

Xa R R2 R3a R3t> R4 RJ R6 X Y R7 R8 XVII-44-1 'Bu H H H Bz F H F OH H H XVH-44-2 'Bu H H CH3 Bz F H F OH H H XVII-44-3 'Bu H H CHCCHs), Bz F H F OH H H XVII-44-4 'Bu H H CH2CH(CH3)2 Bz F H F OH H H XVII-44-5 'Bu H H CH2Ph Bz F H F OH H H XVII-44-6 *Bu H H CH2-indol-3-yl Bz F H F OH H H XVII-44-7 'Bu H H CH2CH2SCH3 Bz F H F OH H H XVII-44-8 'Bu * H * Bz F H F OH H H ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -396- WO 2008/121634 PCT/US2008/058183

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Table XVII-45.

Ns R2 R3’ R3b ir ΊΓ R6 X Y R7 Ra XVII-45-1 Ph H H H Bz F H F OH H H XVII-45-2 Ph H H ch3 Bz F H F OH H H XVII-45-3 Ph H H CH(CH3)2 Bz F H F OH H H XVII-45-4 Ph H H CH2CH(CH3)2 Bz F H F OH H H XVII-45-5 Ph H H CH2Ph Bz F H F OH H H XVII-45-6 Ph H H CH2-indol-3-yl Bz F H F OH H H XVII-45-7 Ph H H CH2CH2SCH3 Bz F H F OH H H XVH-45-8 Ph * H * Bz F H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XVII-46.

Ns Rl R2 RJl . R3b R4 R5 R6 X Υ R7 R“ XVII-46-1 p-Me-Ph H H H Bz F Η F ΟΗ Η Η XVII-46-2 p-Me-Ph H H CH3 Bz F Η F ΟΗ Η Η XVII-46-3 p-Me-Ph H H CH(CH3)2 Bz F Η F ΟΗ Η Η XVII-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz F Η F ΟΗ Η Η XVH-46-5 p-Me-Ph H H CH2Ph Bz F Η F ΟΗ Η Η XVII-46-6 p-Me-Ph H H CH2-indol-3-yl Bz F Η F ΟΗ Η Η XVII-46-7 p-Me-Ph H H ch2ch2sch3 Bz F Η F ΟΗ Η Η XVII-46-8 p-Me-Ph .♦ H * Bz F Η F ΟΗ Η Η ♦R2 and RJb joined together by (CH2)3 to form five-membered ring. Table XVII-47. “ife R1 R2 r3T- “r35 R4 R3 R4 X Υ R7 Ra XVII-47-1 p-F-Ph H H H Bz F Η F ΟΗ Η Η XVII-47-2 p-F-Ph H H ch3 Bz F Η F ΟΗ Η Η XVH-47-3 p-F-Ph H H CH(CH3)2 Bz F Η F ΟΗ Η Η XVII-47-4 p-F-Ph H H CH2CH(CH3)2 Bz F Η F ΟΗ Η Η XVII-47-5 p-F-Ph H H CH2Ph Bz F Η F ΟΗ Η Η XVII-47-6 p-F-Ph H H CHa-indol-3-yl Bz F Η F ΟΗ Η Η XVII-47-7 p-F-Ph H H ch2ch2sch3 Bz F Η F ΟΗ Η Η XVII-47-8 p-F-Ph * H * Bz F Η F ΟΗ Η Η *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -397- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOUl

Table XVII-48.

Xs "R1 R2 R3“ R4 R5 R6 X Y R7 r“ XVII-48-1 p-CI-Ph H H H Bz F H F OH H H XVII-48-2 p-Cl-Ph H H ch3 Bz F H F OH H H XVII-48-3 p-Cl-Ph H H CH(CH3)2 Bz F H F OH H H XVII-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz F H F OH H H XVII-48-5 p-Cl-Ph H H CH2Ph Bz F H F OH H H XVII-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz F H F OH H H XVII-48-7 p-Ct-Ph H H CH2CH2SCH3 Bz F H F OH H H XVII-48-8 p-Cl-Ph * H * Bz F H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVII-49.

X° R1 R2 R3. R3b R4 R5 R6 X Y R7 R8 XVII-49-1 p-Br-Ph H H H Bz F H F OH H H XVI1-49-2 p-Br-Ph H H CH3 Bz F H F OH H H XVII-49-3 p-Br-Ph H H CH(CH3): Bz F H F OH H H XVII-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz F H F OH H H XVII-49-5 p-Br-Ph H H CH2Ph Bz F H F OH H H XVII-49-6 p-Br-Ph H H CH2-indol-3-yl Bz F H F OH H H XVn-49-7 p-Br-Ph H H ch2ch2sch3 Bz F H F OH H H XVII-49-8 p-Br-Ph * H * Bz F H F OH H H *R2 and RJCl joined together by (CH2)3 to form five-membered ring. 5 Table XVII-50. « ..... I — M ' g- HL ~ - J I - 2 - 1 Jll

Xa R1 R2 r3« R3b R4^ R5 Iv X Y ΊΓ R8 XVH-50-1 p-I-Ph H H H Bz F H F OH H H XVII-50-2 p-I-Ph H H ch3 Bz F H F OH H H XVII-50-3 p-I-Ph H H CHCCHs), Bz F H F OH H H XVII-50-4 p-I-Ph H H CH2CH(CH3)2 Bz F H F OH H H XVII-50-5 p-I-Ph H H CH2Ph Bz F H F OH H H XV1I-50-6 p-I-Ph H H CH2-indol-3-yl Bz F H F OH H H XVII-50-7 p-I-Ph H H CH2CH2SCH3 Bz F H F OH H H XVII-50-8 p-I-Ph ♦ H * Bz F H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -398- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XVIII-1.

R1 R2 r3. R3b R4 R5 R6 X Y R8 XVIII-1-1 ch3 H H H ch3 OCH3 F H OH H H XVIII-1-2 ch3 H H ch3 ch3 OCH3 F H OH H H XVIH-1-3 ch3 H H CH(CH3)2 ch3 och3 F H OH H H XVIH-1-4 ch3 H H CH2CH(CH3)2 ch3 och3 F H OH H H XVHI-1-5 ch3 H H CPI2Ph ch3 och3 F H OH H H XVIII-1-6 ch3 H H CH2-indol-3-yl ch3 och3 F H OH H H XVni-1-7 ch3 H H CH2CH2SCH3 ch3 och3 F H OH H H XVIII-1-8 ch3 ♦ H ♦ ch3 och3 F H OH H H *R2 and Rejoined together by (CHsbt0 form five-membered ring. 5 Table XVIII-2. I---- .1- I . -- ''"Τ. ΠΙ. ' ..... - J---, I-----_ , — — ----— D—

Na R R2 R3* R3b R4 R5 Rb X Y R7 R8 XVI11-2-1 Et H H H CH3 och3 F H OH H H XVHI-2-2 Et H H ch3 ch3 och3 F H OH H H XVIII-2-3 Et H H CH^H^ ch3 och3 F H OH H H XVIII-2-4 Et H H CH2CH(CH3)2 ch3 och3 F H OH H H XVHI-2-5 Et H H CH2Ph ch3 och3 F H OH H H XVIH-2-6 Et H H CH2-indol-3-yl ch3 OCHj F H OH H H XVIII-2-7 Et H H CH2CH2SCH3 ch3 och3 F H OH H H XVIII-2-8 Et * H * ch3 och3 F H OH H H ♦R2 and R^ joined together by (CH^ to form five-membered ring. 2983472-1 -399- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XVIII-3.

R1 "F R31 R3” Rs R6 X Y Ra XVHI-3-1 'Pr H H H ch3 och3 F H OH H H XVIH-3-2 'Pr H H ch3 ch3 och3 F H OH H H XVIH-3-3 'Pr H H CH(CH3)2 ch3 och3 F H OH H H XVIII-3-4 'Pr H H CH2CH(CH3)2 ch3 och3 F H OH H H XVHI-3-5 'Pr H H CH2Ph ch3 och3 F H OH H H XVIII-3-6 'Pr H H CH2-indol-3-yl ch3 och3 F H OH H H XVHI-3-7 'Pr H H CH2CH2SCH3 ch3 och3 F H OH H H XVIII-3-8 'Pr * H ♦ ch3 och3 F H OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring

Table XVIII-4.

Ns R1 R2 R" R3b R4 R5 IF X Y R' R XVIU-4-1 'Bu H H H ch3 och3 F H OH H Η XVHI-4-2 'Bu H H ch3 ch3 och3 F Η OH H Η XVIIM-3 'Bu H H CH(CH3)2 ch3 och3 F H OH H Η XVIIM-4 'Bu H H CH2CH(CH3)2 ch3 och3 F H OH H Η XVHI-4-5 'Bu H H CH2Ph ch3 och3 F H OH Η Η XVIII-4-6 'Bu H H CH2-indol-3-yl ch3 och3 F H OH H Η XVIII-4-7 'Bu H H CH2CH2SCH3 ch3 och3 F H OH H Η XVIII-4-8 ib t * H * ch3 och3 F H OH H Η ♦R? and R3b joined together by (CH2)3 to form five-membered ring.

Table ΧΥΙΠ-5.

Ns R1 RJ -r3T r3S r4- R5 Rfc X Y R7 R8 XVIII-5-1 Ph H H H ch3 OCHa F H OH H H XVIII-5-2 Ph H Η ch3 ch3 och3 F H oh H H XVIH-5-3 Ph H H CH(CH3)2 ch3 och3 F H OH H H XVIII-5-4 Ph H H CH2CH(CH3)2 ch3 och3 F Η OH H H XVHI-5-5 Ph Η Η CH2Ph ch3 och3 F H OH H H XVIII-5-6 Ph H H CH2-indol-3~yl ch3 och3 F H OH H H XVIII-5-7 Ph Η H CH2CH2SCH3 ch3 och3 F H OH H H XVIII-5-8 J nJ Ph rrr * H * ch3 och3 F .H OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -400- WO 2008/121634

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Ns R1 R34 R3b R4 R3 R6 X Y ΊΓ Ra XVIII-6- 1 p-Me- Ph H H H ch3 och3 F H OH H H XVIH-6- 2 p-Me- Ph H H ch3 ch3 och3 F H OH H H XVHI-6- 3 p-Me- Ph H H CHiCH,), ch3 och3 F H OH H H XVHI-6- 4 p-Me- Ph H H CH2CH(CH3)2 ch3 och3 F H OH H H XVIII-6- 5 p-Me- Ph H H CH2Ph ch3 och3 F H OH H H XVIII-6- 6 p-Me- Ph H H CH2-indol-3- yi ch3 och3 F H OH H H XVIII-6- 7 p-Me- Ph H H ch2ch2sch3 ch3 och3 F H OH H H XVIII-6- p-Me- * H * ch3 och3 F H OH H H

Ph *R2 and Rejoined together by (Cl-hbt0 f°rm five-membered ring.

Table XVIII-7.

Ns R1 R7 RJ. R3b R‘ R3 R4 X Y R7 R8 XVin-7-1 p-F- Ph H H H CH3 OCH3 F H OH H H XVIII-7-2 p-F- Ph H H CH3 ch3 och3 F H OH H H XVIII-7-3 p-F- Ph H H CH(CH3)2 ch3 och3 F H OH H H XVIII-7-4 p-F- Ph H H CH2CH(CH3)2 ch3 och3 F H OH H H XVIII-7-6 p-F- Ph H H CH2Ph ch3 och3 F H OH H H XVIII-7-7 p-F- Ph H H CH2-indol-3- yi ch3 och3 F H OH H H XVHI-7-8 p-F- Ph H H CH2CH2SCH3 ch3 och3 F H OH H H XVHI-7- 20 p-F- Ph ·. j * H * ch3 och3 F H OH H H ♦R2 and RJb joined together by (0¾^to form five-membered ring. 2983472-1 -401 - WO 2008/121634

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Table XVIli-8.

Ns -R1- R2 “r37" "r* R4 R5 TT X Y ΊΓ Rtt XVIII-8- 1 p-CI- Ph H H H ch3 och3 F H OH H H XVIII-8- 2 p-Cl- Ph H H ch3 ch3 och3 F H OH H H XV1II-8- 3 p-Cl- Ph H H CH(CH3)2 ch3 och3 F H OH H H XVIII-8- 4 p-Cl- Ph H H CH2CH(CH3)2 ch3 och3 F H OH H H XVIII-8- 5 p-Cl- Ph H H CH2Ph ch3 och3 F H OH H H XVIII-8- 6 p-Cl- Ph H H CH2-indol-3- yi ch3 och3 F H OH H H XVIII-8- 7 p-Cl- Ph H H ch2ch2sch3 ch3 och3 F H OH H H XVIII-8- p-Cl- ♦ H ♦ ch3 och3 F H OH H H

Ph *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XVIII-9.

Ns R1 R2 RJ« R3b R4 R5 R6 X Y R' R8 XVHI-9- 1 p-Br- Ph H H H ch3 OCH3 F H OH H H XVIII-9- 2 p-Br- Ph H H CH3 ch3 och3 F H OH H H XVIIl-9- 3 p-Br- Ph H H CH(CH3)2 ch3 och3 F H OH H H XVHI-9- 4 p-Br- Ph H H CH2CH(CH3)2 ch3 och3 F H OH H H XVIII-9- 6 p-Br- Ph H H CH2Ph ch3 och3 F H OH H H XV1II-9- 7 p-Br- Ph H H CH2-indol-3- yi ch3 och3 F H OH H H XVni-9- 8 p-Br- Ph H H CH2CH2SCH3 ch3 och3 F H OH H H XVIII-9- p-Br- ♦ H ♦ ch3 OCHj F H OH H H 2983472-1 -402- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOUI Na R1 R2 r3- Rib R4 R5 R6 X Y R7 R 20 Ph *R2 and Rejoined together by (CH2)3 to form five-membered ring. Table X VIII-10. Na R1 R2 -pr -r3K R4 R5 R* X Y R7 r“ XVIII-10- p-I- H H H ch3 och3 F H OH H H 1 Ph XVIII-10- p-I- H H ch3 ch3 och3 F H OH H H 2 Ph XVIII-10- p-I- H H CH(CH3)2 ch3 och3 , F H OH H H 3 Ph XVUI-1G- p-I- H H CH2CH(CH3)2 ch3 och3 F H OH H H 4 Ph XVIII-10- p-I- H H CH2Ph ch3 och3 F H OH H H 5 Ph XVIII-10- p-I- H H CH2-indol-3- ch3 och3 F H OH H H 6 Ph yi . XVIII-10- p-1- H H ch2ch2sch3 ch3 och3 F H OH H H 7 Ph XVIII-10- p-I- * H * ch3 och3 F H OH H H

Ph *R2 and R3b joined together by (CHhbto form five-membered ring.

Table XVIII-11.

Na R R2 RJa Rib R4 RJ R6 X Y R7 R“ xvni-ll-l ch3 H H H Et OCH3 F Η OH H H XVIII-11-2 ch3 H H CH3 Et och3 F H OH H H XVIII-11-3 ch3 H H CHfCH,), Et och3 F H OH H H XVIU-11-4 ch3 H H CH2CH(CH3)2 Et och3 F H OH H H XVIII-11-5 ch3 H H CH2Ph Et och3 F H OH H H XV1H-11-6 ch3 H H CH2-indol-3-yl Et och3 F H OH H H XVHI-11-7 ch3 H H CH2CH2SCH3 Et och3 F H OH H H XVHI-11-8 ch3 * H * Et och3 F H OH H H •R2andRJi joined together by (CH2)3 to form five-membered ring. 2983472-1 -403 - WO 2008/121634

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Table XVIII-12.

Xs R1 R2 r3. R36 R4 R5 R6 X Y R8 XVIH-12-1 Et H H H Et och3 F H OH H H XVIII-12-2 Et H H ch3 Et och3 F H OH H H XVIII-12-3 Et H H CHCCHa^ Et och3 F H OH H H XVIII-12-4 Et H H CH2CH(CH3)2 Et och3 F H OH H H XVIH-12-5 Et H H CH2Ph Et och3 F H OH H H XVIII-12-6 Et H H CHrindol-3-yl Et och3 F H OH H H XVIII-12-7 Et H H CH2CH2SCH3 Et och3 F H OH H H XVIII-12-8 Et * H * Et och3 F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVIII-13.

Xs R R2 RJ. R3b R4 R3 R6 X Y R7 R8 XVHI-13-1 'Pr H H H Et OCH3 F H OH H H XVIII-13-2 /ρΓ H H CH3 Et och3 F H OH H H XVin-13-3 'Pr H H CH(CH3)2 Et och3 F H OH H H XVIII-13-4 'Pr H H CH2CH(CH3)2 Et och3 F H OH H H XV HI-13-5 'Pr H H CH2Ph Et och3 F H OH H H XV1II-13-6 'Pr H H CH2-indol-3-yl Et och3 F H OH H H XVIII-13-7 'Pr H H CH2CH2SCH3 Et och3 F H OH H H XVHI-13-8 'Pr * H * Et och3 F H OH H H ♦R2 and RJb joined together by (0¾^ to form five-membered ring.

Table XVIII-I4.

Xs R1 R 2 -rK- R4 R5 R4 X Y r’ r“ XVIII-14-1 “Bu H H H Et och3 F H OH H H XVIIl-14-2 'Bu H H ch3 Et och3 F H OH H H XVIII-14-3 'Bu H H CH(CH3)2 Et och3 F H OH H H XVIII-14-4 'Bu H H CH2CH(CH3)2 Et och3 p H OH H H XVIII-14-5 *Bu H H CH2Ph Et och3 F H OH H H XVIII-14-6 ^u H H CH2-indol-3-yl Et och3 F H OH H H XVIH-14-7 *Bu H H CH2CH2SCH3 Et och3 F H OH H H XVIII-14-8 *t»2 . ... 'Bu * H * Et och3 F H OH H H *R2 and Rejoined together by (Chhh to form five-membered ring. 2983472-1 -404- WO 2008/121634 PCT/US2008/058183

Docket No. 60I37.0034WOU1

Table XVIII-15. Ίΰλ D1

Xs R1 R2 R3· R3b R4 R5 R6 X Y R7 Ra xviii is-i Ph H H H Et och3 F H OH H H XVIII-15-2 Ph H H ch3 Et och3 F H OH H H XVI1I-15-3 Ph H H CH(CH,)2 Et OCH3 F H OH H H XVIII-15-4 Ph H H CH2CH(CH3)2 Et och3 F H OH H H XVIII-15-5 Ph H H CH2Ph Et och3 F H OH H H XVIH-15-6 Ph H H CH2-indol-3-yl Et och3 F H OH H H XVHI-15-7 Ph H H CH2CH2SCH3 Et och3 F H OH H H XVIII-15-8 Ph * H ♦ Et och3 F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVIII-16.

Xs R1 R2 R3a R4 R3 R6 X Y ΊΓ R8" XV1II-16- 1 p-Me- Ph H H H Et OCHa F H OH H H XVIII-16- 2 p-Me- Ph H H CHa Et OCH3 F H OH H H XVIII-16- 3 p-Me- Ph H H CH(CH3)a Et OCHa F . H OH H H XVin-16- 4 p-Me- Ph H H CH2CH(CH3)2 Et OCH3 F H OH H H XVIII-16- 5 p-Me- Ph H H CH2Ph Et OCH3 F H OH H H XVIII-16- 6 p-Me- Ph H H CH2-indol-3- yi Et och3 F H OH H H XVIII-16- 7 p'Me- Ph H H CH2CH2SCHa Et OCHa F H OH H H XVIII-16- 8 p-Me- Ph * H * Et OCHa F H OH H H *R2 and Rejoined together by (CAbbto ^οπη five-membered ring.

Table XV1II-17. Xs R1 R7 R3* R3t, R4 R3 R6 X Y R' R* XVIII-17-1 p-F-Ph H H H Et OCHa F H OH H H XVIII-17-2 p-F-Ph H H CHa Et OCHa F H OH H H XVHI-17-3 p-F-Ph H H CHiCHah Et OCHa F H OH H H 2983472-1 -405- WO 2008/121634

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N2 R1 V RJa "R35 R4 R5 R6 X Y R7 R8 XVIII-17-4 p-F-Ph H H CH2CH(CH3)2 Et och3 F H OH H H XVIII-17-5 p-F-Ph H H CH2Ph Et och3 F H OH H H XVIII-17-6 p-F-Ph H H CH2-indol-3-yl Et och3 F H OH H H XVIII-17-7 p-F-Ph H H CH2CH2SCH3 Et och3 F H OH H H XVIII-17-8 p-F-Ph * H * Et och3 F H OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XVIII-18.

Ns R1 R2 R38 R4 R5 R6 X Y r' R8 XVIII-18- 1 p-Cl- Ph H H H Et OCH3 F H OH H H XVIII-18- 2 p-Cl- Ph H H ch3 Et och3 F H OH H H XVIII-I8- 3 p-Cl- Ph H H CH(CH3)2 Et och3 F H OH H H XVIII-18- 4 p-Cl- Ph H H CH2CH(CH3)2 Et och3 F H OH H H XVIII-18- 5 p-Cl- Ph H H CH2Ph Et och3 F H OH H H XVIII-18- 6 p-Cl- Ph H H CH2-indol-3- yi Et och3 F H OH H H XV111-18- 7 p-CI- Ph H H ch2ch2sch3 Et och3 F H OH H H XVIII-18- p-Cl- * H * Et och3 F H OH H H

Ph *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVIII-19.

Ns R1 RJ Rj> R3b R4 R5 R6 X Y Iv R8 XVIII-19- 1 p-Br- Ph H H H Et OCH3 F H OH H H XVIII-19- 2 p-Br- Ph H H CH3 Et och3 F H OH H H XVIU-19- 3 p-Br- Ph H H CH(CH3)2 Et och3 F H OH H H XVIII-19- p-Br- H H CH2CH(CH3)2 Et och3 F H OH H H

Ph 2983472-1 -406- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ns R' FF r3s "iF TT R5 R4 X y ΊΓ R8" 4 XVHI-19- 5 p-Br- Ph H H CH2Ph Et och3 F H OH H H XVIII-19- 6 p-Br- Ph H H CH2-indoI-3- yi Et och3 F H OH H H XVIII-19- 7 p-Br- Ph H H ch2ch2sch3 Et och3 F H OH H H XVHI-19- p-Br- * H * Et och3 F H OH H H

Ph *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVIII-20.

Ns Rl R2 RJ« R3b R4 R5 R6 X Y R' R8 XVHI-20-ϊ p-I-Ph H H H Et och3 F H OH H H XVIH-20-2 p-I-Ph H H ch3 Et och3 F H OH Η H XVIlI-20-3 p-I-Ph H H CHCCH,), Et och3 F H OH H H XVHI-20-4 p-I-Ph H H CH2CH(CH3)2 Et och3 F H OH H H XVIII-20-5 p-I-Ph H H CH2Ph Et och3 F H OH H H XVIII-20-6 p-I-Ph H H CH2-indol-3-yl Et och3 F Η OH H H XVIII-20-7 p-I-Ph H H ch2ch2sch3 Et och3 F Η OH H H XVHI-20-8 p-I-Ph * H ♦ Et och3 F Η OH H Η *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XVIH-21.

Ns Rl R2 r3. R4 R5 R4 X Υ Ίν R8 XVIII-21-1 ch3 Η Η Η *Pr och3 F Η ΟΗ Η Η XVIII-21-2 ch3 H Η ch3 'Pr och3 F H ΟΗ Η Η XVIII-21-3 ch3 Η Η CH(CH3)2 'Pr och3 F Η ΟΗ Η Η XVIII-21-4 ch3 H Η CH2CH(CH3)2 'Pr och3 F Η ΟΗ Η Η XVin-21-5 ch3 Η Η CH2Ph 'Pr och3 F Η ΟΗ Η Η XVIU-21-6 ch3 H Η CH2-indol-3-yl 'Pr och3 F Η ΟΗ Η Η XVIII-21-7 ch3 H Η ch2ch2sch3 Ψγ och3 F Η ΟΗ Η Η XVin-21-8 ch3 4 Η 4 'Pr och3 F Η ΟΗ Η Η 5 *R2 and R30 joined together by (CHjih to forrn five-membered ring. 2983472-1 -407- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XVIII-22.

Ns R1 V R3a R3b R4 R5 X Y IT ΊΓ XVIIJ-22-1 Et H H H 'Pr och3 F H OH H H XVIII-22-2 Et H H ch3 'Pr och3 F H OH H H XVIII-22-3 Et H H CH(CH3)2 'Pr och3 F H OH H H XVI11-22-4 Et H H CH2CH(CH3)2 'Pr och3 F H OH H H XVIII-22-5 Et H H CH2Ph 'Pr och3 F H OH H H XVHI-22-6 Et H H CHrindoi-3-yl 'Pr och3 F H OH H H XVIII-22-7 Et H H ch2ch2sch3 'Pr och3 F H OH H H XVIII-22-8 Et * H * fpr och3 F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVII1-23.

Ns J? R2 R3a R3t> R4 R5 R6 X Y R' Rtt XVHI-23-1 *Pr H H H och3 F H OH H H XV1II-23-2 ipr H H CH3 /pr och3 F H OH H H XVIII-23-3 'Pr H H CH(CH3)2 'Pr och3 F H OH H H XVIII-23-4 'Pr H H CH2CH(CH3)2 'Pr och3 F H OH H H XVIII-23-5 'Pr H H CH2Ph 'Pr och3 F H OH H H XVIII-23-6 'Pr H H CH2-indol-3-yl 'Pr och3 F H OH H H XVHI-23-7 'Pr H H CH2CH2SCH3 'Pr och3 F H OH H H XVIII-23-8 'Pr * H « 'Pr och3 F H OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XVI1I-24. 1 " I M -«IL --- ' ..‘J ’"ί ' Z* o™

Ns R R2 RJ< R3b IC R5 R* X Y R7 R“ XVHI-24-1 *Bu H H H 'Pr OCH3 F H OH H H XVHI-24-2 'Bu H H ch3 'Pr och3 F H OH H H XVIH-24-3 'Bu H H CH(CH3)2 Pr och3 F H OH H H XVIH-24-4 'Bu H H CH2CH(CH3)2 'Pr och3 F H OH H H XVIII-24-5 'Bu H H CH2Ph 'Pr och3 F H OH H H XVI1I-24-6 *Bu H H CH2-indol-3-yl 'Pr och3 F H OH H H XVIII-24-7 'Bu H H CH2CH2SCH3 'Pr och3 F H OH H H XVHI-24-8 'Bu * H * 'Pr och3 F H OH H H ♦R* and R30 joined together by (CH2)3 to form five-membered ring? 2933472-1 -408- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XVIII-25.

X° R1 R2 R3a IF IF- Rs R6 X Y R7 R“ XVIH-25-1 Ph H H H ~τΓ och3 F H OH H H XVIII-25-2 Ph H H CH3 'Pr och3 F H OH H H XVIU-25-3 Ph H H CH(CH3)2 'Pr och3 F H OH H H XVIII-25-4 Ph H H CH2CH(CH3)2 'Pr och3 F H OH H H XVHI-25-5 Ph H H CH2Ph 'Pr och3 F H OH H H XVIII-25-6 Ph H H CH2-indol-3-yl 'Pr och3 F H OH H H XVIII-25-7 Ph H H CH2CH2SCH3 'Pr OCHa F H OH H H XVIH-25-8 Ph * H ♦ 'Pr och3 F H OH H H *R2 and Rejoined together by (CHbk to form five-membered ring.

Table XVIII-26.

Xs R1 R2 R3· IF R4 R3 R6 X Y r’ Ru XVIII-26- p-Me-1 Ph H H H JPr OCH3 F H OH H H XVIII-26- p-Me-2 ph H H CH3 'Pr och3 F H OH H H XVIII-26- p-Me-3 Ph H H CHfCHa), 'Pr och3 F H OH H H XVIII-26- p-Me-4 Ph H H CH2CH(CH3)2 'Pr och3 F H OH H H XVIII-26- p-Me-5 Ph H H CH2Ph /pr och3 F H OH H H XVIII-26- p-Me- H H CH2-indol-3- 'Pr och3 F H OH H H 6 Ph yi XVIII-26- p-Me-7 Ph H H CH2CH2SCH3 Tr och3 F H OH H H XVIII-26- p-Me-8 Ph * H ♦ Tr och3 F H OH H H *R2 and R3b joined together by (CHbb to form five-membered ring. Table XVIII-27. Xa Rl R2 -pr- R3b R4 R5 R6 X Y R7 Rs XVIII-27- p-F-1 Ph H H H 'Pr och3 F H OH H H XVIII-27- p-F- H H CH3 'Pr och3 F H OH H H

Ph 2983472-1 -409- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Xs R1 R2 R3’ ΊΡυ R4 R* X Y r’ r“ 2 XVIII-27- p-F- H H CH(CH3)2 'Pr och3 F H OH H H 3 Ph XVIII-27- p-F- H H CH2CH(CH3)2 'Pr och3 F H OH H H 4 Ph XVIII-27- p-F- H H CH2Ph 'Pr och3 F H OH H H 5 Ph XVIII-27- p-F- H H CH2-indol-3- 'Pr och3 F H OH H H 6 Ph yi XVIII-27- p-F- H H ch2ch2sch3 'Pr och3 F H OH H H 7 Ph XVIII-27- p-F- ♦ H * 'Pr och3 F H OH H H

Ph *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XVIII-28.

Xs R1 RJ r3« R3b R1 R3 R6 X Y R7 R8 XVIII-28- 1 p-Cl- Ph H H H 'Pr OCH3 F Η OH H H XVIII-28- 2 p-Cl- Ph H H ch3 Pr och3 F H OH H H XVIII-28- 3 p-Cl- Ph H H CH(CH3)2 'Pr och3 F H OH H H XVIU-28- 4 p-CI- Ph H H CH2CH(CH3)2 'Pr och3 F H OH H H XVIII-28- 5 p-Cl- Ph H H CH2Ph 'Pr och3 F H OH H H XVIII-28- 6 p-Cl- Ph H H CH2-indol-3- yi 'Pr och3 F H OH H H XVIII-28- 7 p-Cl- Ph H H CH2CH2SCH3 'Pr och3 F H OH H H XVIII-28- 8 p-Cl- Ph ft ! · ! . * H * 'Pr och3 F H OH H H *R2 and RJtl joined together by (CH2)3 to form five-membered ring. 2983472-1 -410- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XVIII-29.

Ns R1 R2 R3a "R35 ; R4 R3 r X Y R’ Iv XVIII-29- 1 p-Br- Ph H H H och3 F H OH H H XVIII-29- 2 p-Br- Ph H H ch3 'Pr och3 F H OH H H XVIU-29- 3 p-Br- Ph H H CH(CH3)2 'Pr och3 F H OH H H XVIII-29- 4 p-Br- Ph H H CH2CH(CH3)2 'Pr och3 F H OH H H XVHI-29- 5 p-Br- Ph H H CH2Ph /pr och3 F H OH H H XVIH-29- 6 p-Br- Ph H H CH2-indol-3- yi 'Pr och3 F H OH H H XVin-29- 7 p-Br- Ph H H ch2ch2sch3 'Pr och3 F H OH H H XVIII-29- p-Br- * H * 'Pr och3 F H OH H H

Ph *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XVIII-30.

Ns R‘ R2 "ru "r35 R4 r5 r6 X Y V r XVI11-30-1 p-I-Ph H H H 'Pr och3 F H OH H H XV1II-30-2 p-I-Ph H H ch3 'Pr och3 F H OH H Η XVI1I-30-3 p-I-Ph H H CHCCHa^ 'Pr och3 F H OH H H XVIII-30-4 p-l-Ph H H CH2CH(CH3)2 'Pr och3 F H OH H H XVIII-30-5 p-I-Ph H H CH2Ph 'Pr och3 F H OH H H XVIII-30-6 p-I-Ph H H CH2-indol-3-yI 'Pr och3 F H OH H H XVIII-30-7 p-I-Ph H H CH2CH2SCH3 'Pr och3 F H OH H H XVIII-30-8 p-I-Ph * H ♦ 'Pr och3 F H OH H H ♦R2 and Rejoined together by (CHfeb to form five-membered ring. 5 Table XVIII-31. - —I — -. mp· j "i i L" " a

X2 R r2 R3. Rjb R4 R3 R6 X Y R7 R* XVHI-31-1 ch3 H H H "Bu och3 F Η OH H H XVIII-31-2 ch3 H H ch3 "Bu och3 F H OH H H XVIII-31-3 ch3 H H ΟΗ(ΟΗ3)2 "Bu och3 F H OH H H 2983472-1 -411 - WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ns R1 R2 R3n "IP ΊΓ" Rs R4 X Y r’ Ra XVIII-31-4 ch3 H H CH2CH(CH3)2 "Bu och3 F H OH H H XVIII-31-5 ch3 H H CH2Ph "Bu och3 F H OH H H XV1II-31-6 ch3 H H CH2-indol-3-yl "Bu och3 F H OH H H XVIII-31-7 ch3 H H CH2CH2SCH3 "Bu och3 F H OH H H XVIII-31-8 ch3 * H * "Bu och3 F H OH H H *R2 and Rejoined together by (0¾)} to form five-membered ring.

Table XVII1-32.

Ns i? RJ r3« R3b R4 Rs R4 X Y R' R8 XVIH-32-1 Et H H H "Bu OCH3 F H OH Η Η XVIH-32-2 Et H H CH3 "Bu och3 F H OH Η Η XVIII-32-3 Et H H CH(CH3)2 "Bu och3 F Η OH Η Η XVIII-32-4 Et H H CH2CH(CH3)2 "Bu och3 F H OH Η Η XVIII-32-5 Et H H CH2Ph "Bu och3 F H OH Η Η XVIU-32-6 Et H H CH2-indol-3-yl "Bu och3 F H OH Η Η XVIII-32-7 Et H H ch2ch2sch3 "Bu och3 F H OH Η Η XVHI-32-8 Et ♦ H * "Bu och3 F H OH Η Η *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XV1II-33.

R1 R2 r3o -r35 R4 R3 R4 X Y R7 r“ XVHI-33-1 'Pr Η Η Η "Bu och3 F H OH H H XVIII-33-2 'Ργ Η Η ch3 "Bu och3 F H OH H H XV1II-33-3 'Ργ Η Η ΟΗ(ΟΗ3)2 "Bu och3 F H OH H H XVIII-33-4 'Ργ Η Η CH2CH(CH3)2 "Bu och3 F H OH H H XVni-33-5 'Ργ Η Η CH2Ph "Bu och3 F H OH H H XVIH-33-6 'Ργ Η Η CH2-indol-3-yl "Bu och3 F H OH H H XVIII-33-7 'Ργ Η Η CH2CH2SCH3 "Bu och3 F H OH H H XVHI-33-8 'Ργ * Η * "Bu och3 F H OH H H 5 *R2 and Rejoined together by (CH2)3 to form five-membered ring

Table XVIII-34.

Ns R R2 r3« Rib R4 R5 R4 X Y ΊΓ r“ XVHI-34-1 H H H "Bu OCH3 F Η OH H H XVIH-34-2 *Bu H H ch3 "Bu och3 F H OH H H XVIII-34-3 Έυ H H ΟΗ(ΟΗ3)ϊ "Bu och3 F H OH H H XVIII-34-4 'Bu H H CH2CH(CH3)2 "Bu och3 F H OH H H 2983472-1 -412- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Ns R1 R2 R3’ -jpu R4 R3 R6 X Y R7 r“ XVIII-34-5 'Bu H H CH2Ph "Bu OCHj F H OH H H XVIII-34-6 'Bu H H CH2-indol-3-yl "Bu och3 F H OH H H XVIH-34-7 'Bu H H CH2CH2SCH3 "Bu och3 F H OH H H XVIII-34-8 'Bu * H * "Bu och3 F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVIII-35.

Na R R2 RJl R3b R4 R3 R4 X Y R R8 XVIII-35-1 Ph H H H "Bu och3 F H OH H H XVHI-35-2 Ph H H ch3 "Bu och3 F H OH H H XVHI-35-3 Ph H H CHiCHa), "Bu och3 F H OH H H XVIII-35-4 Ph H H CH2CH(CH3)2 "Bu och3 F H OH H H XVIII-35-5 Ph H H CH2Ph "Bu och3 F H OH H H XVIII-35-6 Ph H H CH2-indol-3-yl "Bu och3 F H OH H H XVIII-35-7 Ph H H CH2CH2SCH3 "Bu och3 F H OH H H XVIII-35-8 Ph ♦ H * "Bu och3 F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVIII-36.

Rl R2 RJ* R3b R4 R3 R4 X Y R' R“ XVIII- 36-1 p-Me- Ph H H H "Bu OCH3 F H OH H H XVIII- 36-2 p-Me- Ph H H CH3 "Bu och3 F H OH H H XVIII- 36-3 p-Me- Ph H H CH(CH3)2 "Bu och3 F H OH H H XVIII- 36-4 p-Me- Ph H H CH2CH(CH3)2 "Bu och3 F H OH H H XVIII- 36-5 p-Me- Ph H H CH2Ph "Bu och3 F H OH H Η XVIII- 36-6 p-Me- Ph H H CH2-indoI-3- yi "Bu och3 F H OH H H XVIII- 36-7 p-Me- Ph H H CH2CH2SCH3 "Bu och3 F H OH H H XVIII- 36-8 p-Me- Ph * H * "Bu och3 F H OH H H 2983472-1 -413- WO 2008/121634 ΛΛ_ „

Docket No. 60137.0034WOU1 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVIII-37. PCT/US2008/058183

Xa Rl “R2” R3a "r35 r4 X Y R R8 XVIII-37- p-F- H H H "Bu och3 f H OH H H 1 Ph XVIII-37- p-F- H H ch3 "Bu och3 f H OH H H 2 Ph XVIII-37- p-F- H H CH(CH3)2 "Bu och3 f H OH H H 3 Ph XVIII-37- p-F- H H CH2CH(CH3)2 "Bu och3 f H OH H H 4 Ph XVIII-37- p-F- H H CH2Ph "Bu och3 f H OH H H 5 Ph XVIII-37- p-F- H H CH2-indol-3- "Bu och3 f H OH H H 6 Ph yi XVIII-37- p-F- H H CH2CH2SCH3 "Bu och3 f H OH H H 7 Ph XVIII-37- p-F- ♦ H * "Bu och3 f H OH H H 8 Ph *RZ and Rejoined together by (CH2)3 to form five-membered ring. Table XVI1I-38. Xa R1 R2 R3b R4 R5 R6 X Y RJ R8 XVIII-38- p-Cl- H H H "Bu och3 f H OH H H 1 Ph XVIII-38- p-Cl- H H CH3 "Bu och3 f H OH H H 2 Ph XVIII-38- p-Cl- H H CHCCHa), "Bu och3 f H OH H H 3 Ph XVIII-38- p-Cl- H H CH2CH(CH3)2 "Bu och3 f H OH H H 4 Ph XVIII-38- p-Cl- H H CH2Ph "Bu och3 f H OH H H 5 Ph XVIII-38- p-Cl- H H CHrindol-3- "Bu och3 f H OH H H 6 Ph yi XVIII-38- p-Cl- H H CH2CH2SCH3 "Bu och3 f H OH H H

Ph 2983472-1 -414- WO 2008/121634 PCT/US2008/0S8183

Docket No. 60137.0034WOU1

x° r1 R3 -pr- ηρυ - - R6 X Y r’ R8 7 XVIII-38- 8 p-Cl- Ph * H * "Bu och3 F H OH H H *R4 and Rejoined together by (CH2)3 to form five-membered ring. Table XVIII-39. Na R1 R3 R3·’ _ R4 R3 R6 X Y R7 R8 XVIII-39- 1 p-Br- Ph H H H "Bu och3 F H OH H H XVni-39- 2 p-Br- Ph H H ch3 "Bu och3 F H OH H H XVIII-39- 3 p-Br- Ph H H CH(CH3)2 "Bu och3 F H OH H H XVIII-39- 4 p-Br- Ph H H CH2CH(CH3)2 "Bu och3 F H OH H H XVIII-39- 5 p-Br- Ph H H CH2Ph "Bu och3 F H OH H H XVIII-39- 6 p-Br- Ph H H CH2-indol-3- yi "Bu och3 F H OH H H XVII1-39- 7 p-Br- Ph H H CH2CH2SCH3 "Bu och3 F H OH H H XVIII-39- p-Br- * H ♦ "Bu och3 F H OH H H

Ph *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XVIII-40.

Xs R1 R3 "r35 R4 R4 r6 X Y R’ XVIII-40- p-I- H H H "Bu OCH3 F Η OH H H 1 Ph XVIII-40- p-I- H H CH3 "Bu och3 F H OH H H 2 Ph XVIII-40- p-I- H H CH(CH3)2 "Bu och3 F H OH H H 3 Ph XVIH-40- p-I- H H CH2CH(CH3)2 "Bu och3 F H OH H H 4 Ph XVIII-40- p-I- H H CH2Ph "Bu och3 F H OH H H

Ph 2983472-1 -415- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Xs R1 R2 R30 "r35 1?" R6 X Y R7 Ic 5 XVIII-40- p-I- H H CH2-indol-3- ”Bu och3 F H OH H H 6 Ph yi XVIH-40- p-I- H H ch2ch2sch3 rtBu och3 F H OH H H 7 Ph XVIH-40- p-I- * H * ”Bu och3 F H OH H H

Ph ♦R1 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVI1I-41.

___ _ I

Xs R R2 r3. R3b R4 R3 R X Y R7 R XVIII-41-1 ch3 Η Η H Bz och3 F Η OH H H XVIII-41-2 ch3 H H ch3 Bz och3 F H OH H H XVIII-41-3 ch3 H H CH(CH3)2 Bz och3 F H OH H H XVIII-41-4 ch3 H H CH2CH(CH3)2 Bz och3 F H OH H H XVIII-41-5 ch3 Η H CH2Ph Bz OCHa F H OH H H XVI1I-41-6 ch3 H H CHrindol-3-yl Bz OCH3 F H OH H H XVIII-41-7 ch3 H H CH2CH2SCH3 Bz OCH3 F Η OH H H XVIII-41-8 ch3 * Η Bz och3 F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVIII-42.

X2 R1 -jpr "S* R4 "R1 R6 X Y Ί<7 R“ XVHI-42-1 Et H H H Bz OCH3 F H OH H H XVIU-42-2 Et H H CH3 Bz och3 F H OH H H XVIII-42-3 Et H H CHCCH^ Bz OCH3 F H OH H H XVHI-42-4 Et H H CH2CH(CH3)2 Bz och3 F H OH H H XVIH-42-5 Et H H CH2Ph Bz och3 F H OH H H XVIII-42-6 Et H H CH2-indol-3-yl Bz och3 F H OH H H XVIII-42-7 Et H H CH2CH2SCH3 Bz och3 F H OH H H XVIII-42-8 Et * H * Bz och3 F H OH H H 5 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XVffl-43.

Xs R R2 RJ“ R3b R R3 R6 X Y R' R" XVHI-43-1 'Pr H H H Bz OCH3 F H OH H H XVIII-43-2 'Pr H H ch3 Bz OCH3 F H OH H H 2983472-1 -416- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

XVIII-43-3 XVIII-43-4 XVIII-43-5 XVIII-43-6 XVII1-43-7 'Pr fPr 'Pr 'Pr 'Pr H H H H H H H H H H CH(CH3)2 CH2CH(CH3)2 CH2Ph CH2-indol-3-yl CH2CH2SCH3 Bz Bz Bz Bz Bz och3 och3 och3 och3 och3 F F F F F H H H H H OH OH OH OH OH H H H H H H H H H H XVIII-43-8 'Pr * H * Bz och3 F H OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring

Table XVIII-44.

Ns R R2 R3. R3b R4 Rs R6 X Y R7 R“ XVIII-44-1 'Bu H H H Bz OCH3 F H OH H H XVIII-44-2 'Bu H H CH3 Bz och3 F H OH H H XVHI-44-3 'Bu H H CHiCH^ Bz och3 F H OH H H XVIII-44-4 'Bu H H CH2CH(CH3)2 Bz och3 F H OH H H XVIII-44-5 'Bu H H CH2Ph Bz och3 F H OH H H XVIII-44-6 'Bu H H CH2-indoI-3-yl Bz och3 F H OH H H XVHI-44-7 'Bu H H CH2CH2SCH3 Bz och3 F H OH H H XVin-44-8 'Bu * H ♦ Bz och3 F H OH H H ♦R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XVII1-45.

Ns R R2 RJ“ R3b R4 R3 Rb X Υ R7 R8 XVIII-45-1 Ph H H H Bz OCH3 F H OH H H XVIII-45-2 Ph H H CH3 Bz och3 F Η OH H H XVIII-45-3 Ph H H CH(CH3)2 Bz och3 F H OH H H XVIH-45-4 Ph H H CH2CH(CH3)2 Bz OCHa F H OH H H XVIII-45-5 Ph H H CH2Ph Bz och3 F Η OH H H XVIH-45-6 Ph H H CH2-indol-3-yl Bz och3 F Η OH H H XVIII-45-7 Ph H H CH2CH2SCH3 Bz och3 F Η OH H H XVIH-45-8 Ph ♦ H * Bz och3 F Η OH H H *R2 and R3t ’joined together by (CH2)3 to form five-membered ring. Table XVIII-46. Ns R R2 R3a R3b R4 Rs R6 X Y R7 R8 XVIII-46- p-Me-j Ph H H H Bz OCH3 F H OH H H XVIII-46- p-Me- H H ch3 Bz och3 F H OH H H 2 Ph 2983472-1 -417- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

-R1 "r2- r5“ R3b R4 R5 If X Y R7 R« XVIII-46- p-Me-3 Ph H H CH(CH3)2 Bz och3 F H OH H H XVIII-46- p-Me-4 Ph H H CH2CH(CH3)2 Bz och3 F H OH H H XVIII-46- p-Me-5 Ph H H CH2Ph Bz och3 F H OH H H XVIII-46- p-Me- H H CH2-indol-3- Bz OCHj F H OH H H 6 Ph yi XVIII-46- p-Me-7 Ph H H ch2ch2sch3 Bz och3 F H OH H H XVIII-46- p-Me- * H * Bz och3 F H OH H H

Ph *R2 and Rejoined together by (CPhh to form five-membered ring.

Table XVIII-47.

Xa R1 RJ RJa R3b R* R5 R6 X Y R R8 XVin-47- 1 p-F- Ph H H H Bz OCH3 F H OH H H XV1II-47- 2 p-F- Ph H H ch3 Bz och3 F H OH H H XVIII-47- 3 p-F- Ph H H CH(CH3)2 Bz och3 F H OH H H XVIII-47- 4 p-F- Ph H H CH2CH(CH3)2 Bz och3 F H OH H H XVIII-47- 5 p-F- Ph H H CH2Ph Bz och3 F H OH H H XVIH-47- 6 p-F- Ph H H CH2-indol-3- yi Bz och3 F H OH H H XVIII-47- 7 p-F- Ph H H CH2CH2SCH3 Bz och3 F H OH H H XVIII-47- 8 p-F- Ph * H * Bz och3 F H OH H H •R2andR” joined together by (CH2)3 to form five-membered ring. . Table XVIII-48. Xa R' R5 -jpr R3b R4 R5 Rft X Y R7 R* 2983472-1 -418- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ha Rl “F Ίκ*’ R3b ΊΓ“ R5 R* X Y ΤΓ R*1 XVin-48- 1 p-Cl- Ph H H H Bz och3 F H OH H H XVTII-48- 2 p-CI- Ph H H ch3 Bz och3 F H OH H H XVIII-48- 3 p-Cl- Ph H H CH(CH3)2 Bz och3 F H OH H H XVIII-48- 4 p-CI- Ph H H CH2CH(CH3)2 Bz och3 F H OH H H XVIIl-48- 5 p-Cl- Ph H H CH2Ph Bz och3 F H OH H H XVIII-48- 6 p-Cl- Ph H H CH2-indol-3- yi Bz och3 F H OH H H XVIII-48- 7 p-Cl- Ph H H ch2ch2sch3 Bz och3 F H OH H H XV1II-48- p-CI- * H ♦ Bz och3 F H OH H H

Ph *R2 and R3” joined together by (CH2)3 to form five-membered ring.

Table XVIII-49.

Ha Rl RJ‘ R3b R4 R3 R6 X Y R7 R# XVIII-49- 1 p-Br- Ph H H H Bz och3 F H OH H H XVIII-49- 2 p-Br- Ph H H ch3 Bz och3 F H OH H H XVUI-49- 3 p-Br- Ph H H CH(CH3)i Bz och3 F H OH H H XVIII-49- 4 p-Br- Ph H H CH2CH(CH3)2 Bz OCH3 F H OH H H XVIH-49- 5 p-Br- Ph H H CH2Ph Bz OCH3 F H OH H H XVIH-49- 6 p-Br- Ph H H CH2-indol-3- yi Bz och3 F H OH H H XVIII-49- 7 p-Br- Ph H H ch2ch2sch3 Bz OCHa F H OH H H XVIH-49- 8 p-Br- Ph * H ♦ Bz OCH3 F H OH H H 2983472-1 -419- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XVIII-50.

Xa R* R2 IT3' ίΤ^ - - "F" "R5-” X Y ΊΓ R* XVIII-50-1 p-I-Ph H H H Bz och3 F H OH H H XVIII-50-2 p-I-Ph H H ch3 Bz och3 F H OH H H XVIII-50-3 p-I-Ph H H CH(CH3)2 Bz och3 F H OH H H XVIII-50-4 p-I-Ph H H CH2CH(CH3)2 Bz och3 F H OH H H XVIII-50-5 p-I-Ph H H CH2Ph Bz och3 F H OH H H XVIII-50-6 p-I-Ph H H CH2-indol-3-yl Bz och3 F H OH H H XVHI-50-7 p-I-Ph H H CH2CH2SCH3 Bz och3 F H OH H H XVIII-50-8 p-I-Ph * H * Bz och3 F H OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

XIX 5 Table XIX-1. " i *rc — 11 j'"· 1 f Il

Xa R1 R2 Ra‘ "R36- R4 Rs R6 X Y R; R“ XIX-1-1 ch3 H H H ch3 OCH3 F F OH Η H XIX-1-2 ch3 H H ch3 ch3 och3 F F OH H H XIX-1-3 ch3 H H CH(CH3)2 ch3 och3 F F OH Η Η XIX-1-4 ch3 H H CH2CH(CH3)2 ch3 och3 F F OH H Η XIX-1-5 ch3 H H CH2Ph ch3 och3 F F OH H Η XIX-1-6 ch3 H H CH2-indol-3-yl ch3 och3 F F OH H Η XIX-1-7 ch3 H H CH2CH2SCH3 ch3 och3 F F OH H Η XIX-1-8 ch3 * H « ch3 och3 F F OH H Η *R2 and R36 joined together by (CH2)3 to form five-membered ring.

Table XIX-2. 2983472-1 -420- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Xs R2 r3b R3b R4 R5 R6 X Y R Rb XIX-2-1 Et H H H ch3 och3 F F OH H H XIX-2-2 Et H H CH3 ch3 och3 F F OH H H XIX-2-3 Et H H CH(CH3)2 ch3 och3 F F OH H H XIX-2-4 Et H H CH2CH(CH3)2 ch3 och3 F F OH H H XIX-2-5 Et H H CH2Ph ch3 och3 F F OH H H XIX-2-6 Et H H CH2-indol-3-yl ch3 och3 F F OH H H XIX-2-7 Et H H CH2CH2SCH3 ch3 och3 F F OH H H XIX-2-8 Et * H * ch3 och3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIX-3.

Xa R1 R2 R3a "R35 R4 R5 R6 X Y R1 r“ XIX-3-1 'Pr H H H ch3 och3 F F OH H H XIX-3-2 'Pr H H ch3 ch3 och3 F F OH H H XJX-3-3 'Pr H H CH(CH3)2 ch3 och3 F F OH H H XIX-3-4 'Pr H H CH2CH(CH3)2 ch3 och3 F F OH H H XIX-3-5 'Pr H H CH2Ph ch3 och3 F F OH H H XIX-3-6 'Pr H H CH2-indoI-3-yI ch3 och3 F F OH H H XIX-3-7 'Pr H H CH2CH2SCH3 ch3 och3 F F OH H H XIX-3-8 'Pr * H * ch3 och3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIX-4.

Xa R2 R3‘ I? RJ R6 X Y f? Ra XIX-4-1 Έιι H H H ch3 och3 F F OH H H XIX-4-2 'Bu H H ch3 ch3 och3 F F OH H H XIX-4-3 'Bu H H CH(CH3)i ch3 och3 F F OH H H XIX-4-4 'Bu H H CH2CH(CH3)2 ch3 och3 F F OH H H XIX-4-5 'Bu H H CH2Ph ch3 och3 F F OH H H XIX-4-6 'Bu H H CH2-indol-3-yI ch3 och3 F F OH H H XIX-4-7 'Bu H H CH2CH2SCH3 ch3 och3 F F OH H H XIX-4-8 Τ7ΓΖ-Τΐ *Bu n.3b ! * H * ch3 och3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -421- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XIX-5.

N° R1 R?' R3’ R3b R4 r3 R6 X Y r’ R“ XIX-5-1 Ph H H H ch3 och3 F F OH H H XIX-5-2 Ph H H ch3 ch3 och3 F F OH H H XIX-5-3 Ph H H CH(CH3)2 ch3 och3 F F OH H H XIX-5-4 Ph H H CH2CH(CH3)2 ch3 och3 F F OH H H XIX-5-5 Ph H H CH2Ph ch3 och3 F F OH H H XIX-5-6 Ph H H CH2-indol-3-yl ch3 och3 F F OH H H XIX-5-7 Ph H H ch2ch2sch3 ch3 och3 F F OH H H XIX-5-8 Ph * H 4 ch3 och3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIX-6. R1 R2 R3’ Rib R3 R6 X Y R2 R8 XIX-6- 1 p-Me- Ph H H H ch3 OCH3 F F OH H Η XIX-6- 2 p-Me- Ph H H CH3 ch3 och3 F F OH H Η XIX-6- 3 p-Me- Ph H H CH(CH3)2 ch3 och3 F F OH H Η XIX-6- 4 p-Me- Ph H H CH2CH(CH3)2 ch3 och3 F F OH Η Η XIX-6- 5 p-Me- Ph H H CH2Ph ch3 och3 F F OH Η Η XIX-6- 6 p-Me- Ph H H CH2-indol-3- yi ch3 och3 F F OH Η Η XIX-6- 7 p-Me- Ph H H ch2ch2sch3 ch3 och3 F F OH Η Η XIX-6- 8 p-Me- Ph * H ♦ ch3 och3 F F OH Η Η ♦R^ and Rejoined together by (CPhb to form five-membered ring.

Table ΧΙΧ-7. Κ2 R1 R2 r3* R3b R* R? R6 X Y R’ Rb ΧΙΧ-7-1 p-F-Ph Η Η Η ch3 och3 F F OH Η H ΧΙΧ-7-2 p-F-Ph Η Η ch3 ch3 och3 F F OH H H ΧΙΧ-7-3 p-F-Ph Η Η CHCCH^ ch3 och3 F. F OH H Η 2983472-1 -422- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Xs R1 R2 R3’ R3„ R5 R6 X Y R Rh ΧΪΧ-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 och3 F F OH H H XIX-7-6 p-F-Ph H H CH2Ph ch3 och3 F F OH H H ΧΪΧ-7-7 p-F-Ph H H CH2-indol-3-yl ch3 och3 F F OH H H X1X-7-8 p-F-Ph H H CH2CH2SCH3 ch3 och3 F F OH H H ΧΪΧ-7-20 p-F-Ph * H ♦ ch3 och3 F F OH H H *R2 and R3b joined together by to form five-membered ring.

Table XIX-8.

Xs R1 R3b R3b R4 R5 R6 X Y I? R# XIX-8-1 p-Cl-Ph H H H ch3 och3 F F OH H H XIX-8-2 p-Ct-Ph H H ch3 ch3 och3 F F OH H H XIX-8-3 p-Cl-Ph H H chcch,). ch3 och3 F F OH H H XIX-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 och3 F F OH H H XIX-8-5 p-Cl-Ph H H CH2Ph ch3 och3 F F OH H H XIX-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 och3 F F OH H H XIX-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 och3 F F OH H H XIX-8-8 p-Cl-Ph * H * CH3 och3 F F OH H H *R2 and Rjb joined together by (CH2)3 to form five-membered ring.

Table XIX-9. Xs R1 R3 RJa R3b R4 R3 R6 X Y R7 R* XIX-9-1 p-Br- Ph H H H ch3 OCH3 F F OH H H XIX-9-2 p-Br- Ph H H ch3 ch3 och3 F F OH H H XIX-9-3 p-Br- Ph H H CH(CH3)2 ch3 och3 F F OH H H XIX-9-4 p-Br- Ph H H CH2CH(CH3)2 ch3 och3 F F OH H H XIX-9-6 p-Br- Ph H H CH2Ph ch3 och3 F F OH H H XIX-9-7 p-Br- Ph H H CH2-indol-3- yi ch3 och3 F F OH H H XIX-9-8 p-Br- Ph H H ch2ch2sch3 ch3 och3 F F OH H H XIX-9- 20 p-Br- Ph * H * ch3 och3 F F OH H H 5 *R2 and RJb joined together by (CH2)3to form five-membered ring. 2983472-1 -423- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XIX-10.

Xa R' “r2” r3b Tv* R4 R5 R6 X Y R7 R“ XIX-10-1 p-I-Ph H H H ch3 och3 F F OH H H XIX-10-2 p-I-Ph H H ch3 ch3 och3 F F OH H H XIX-10-3 p-I-Ph H H CH(CH3)2 ch3 och3 F F OH H H XIX-10-4 p-I-Ph H H CH2CH(CH3)2 ch3 OCHj F F OH H H XIX-10-5 p-I-Ph H H CH2Ph ch3 och3 F F OH H H XIX-10-6 p-I-Ph H H CHrindol-3-yl ch3 och3 F F OH H H XIX-10-7 p-I-Ph H H CH2CH2SCH3 ch3 och3 F F OH H H XIX-10-8 . n p-I-Ph .3b - · + H ♦ ch3 och3 F F OH H H *R2 and RJb joined together by (CFUb to form five-membered ring.

Table XIX-11.

Xs R1 R2 R3a R3b ΊΓ R5 R6 X Y R7 r" XIX-11-1 CH3 Η Η Η Et och3 F F OH H H XIX-11-2 ch3 Η Η ch3 Et och3 F F OH H H XIX-11-3 ch3 Η Η CH(CH3)2 Et och3 F F OH H H XIX-11-4 ch3 Η Η CH2CH(CH3)2 Et och3 F F OH H H XIX-11-5 ch3 Η Η CH2Ph Et och3 F F OH H H XIX-11-6 ch3 Η Η CH2-indol-3-yl Et och3 F F OH H H XIX-11-7 ch3 Η Η ch2ch2sch3 Et och3 F F OH H H XIX-11-8 7,72“ ; Ϊ, ch3 .'Jb'· * * Η * Et och3 F F OH H H *R2 and Rejoined together by (CJ-hb to form five-membered ring.

Xa R1 R2 “r35" "R36 R4 R5 R6 X Y R R« XIX-12-1 Et H H H Et OCH3 F F OH H H XIX-12-2 Et H H ch3 Et och3 F F OH H H XIX-12-3 Et H H CH(CH3)2 Et och3 F F OH H H XIX-12-4 Et H H CH2CH(CH3)2 Et och3 F F OH H H XIX-12-5 Et H H CH2Ph Et och3 F F OH H H XIX-12-6 Et H H CH2-indol-3-yl Et och3 F F OH H H XIX-12-7 Et H H CH2CH2SCH3 Et och3 F F OH H H XIX-12-8 J τι Et □ET- * H * Et och3 F F OH H H *R2 and RJb joined together by (CH^ to form five-membered ring. 2983472-1 -424- WO 2008/121634

Docket No. 6013 7.0034WOU1 PCT/US2008/058183

Table XIX-13.

X2 R1 R2 ' R35- "R36 R5 R4 X Y iT R* XIX-13-1 'Pr H H H Et och3 F F OH H H XIX-13-2 'Pr H H ch3 Et och3 F F OH H H X1X-13-3 'Pr H H CH(CH3)2 Et och3 F F OH H H XIX-13-4 'Pr H H CH2CH(CH3)2 Et och3 F F OH H H XIX-13-5 'Pr H H CH2Ph Et och3 F F OH H H XIX-13-6 'Pr H H CH2-indol-3-yl Et och3 F F OH H H XIX-13-7 'Pr H H CH2CH2SCH3 Et och3 F F OH H H XIX-13-8 'Pr ♦ H * Et och3 F F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XIX-14.

Xa R1 R2 R3· R4 R5 R6 X Y r’ r" XIX-14-1 'Bu H H H Et och3 F F OH H H XIX-14-2 'Bu H H ch3 Et och3 F F OH H H XIX-14-3 'Bu H H CHCCHjh Et och3 F F OH H H XIX-14-4 'Bu H H CH2CH(CH3)2 Et och3 F F OH H H XIX-14-5 'Bu H H CH2Ph Et och3 F F OH H H XIX-14-6 'Bu H H CH2-indol-3-yl Et och3 F F OH H H XIX-14-7 'Bu H H CH2CH2SCH3 Et och3 F F OH H H XIX-14-8 xn2 in 'Bu 3b . . + H ♦ Et och3 F F OH H H *RZ and Rejoined together by (CH2)3 to form five-membered ring.

X» R1 V R3· “I*35- R4 R5 R6 X Y R7 R“ XIX-15-1 Ph H H H Et och3 F F OH H H XIX-15-2 Ph H H ch3 Et och3 F F OH H H XIX-15-3 Ph H H CHCCH,), Et och3 F F OH H H XIX-15-4 Ph H H CH2CH(CH3)2 Et och3 F F OH H H XIX-15-5 Ph H H CH2Ph Et och3 F F OH H H XIX-15-6 Ph H H CH2-indol-3-yl Et och3 F F OH H H XIX-15-7 Ph H H CH2CH2SCH3 Et och3 F F OH H H XIX-15-8 Ph » H * Et och3 F F OH H H ♦Rz and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -425 - WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XIX-16.

Xa R1 "ΊΓ "r^ R4 R3 R6 X Y R7 R# XLX-16- 1 p-Me- Ph H H H Et och3 F F OH H H X1X-16- 2 p-Me- Ph H H ch3 Et och3 F F OH H H XIX-16- 3 p-Me- Ph H H CH(CH3)2 Et och3 F F OH H H XIX-16- 4 p-Me- Ph H H CH2CH(CH3)2 Et och3 F F OH H H XIX-16- 5 p-Me- Ph H H CH2Ph Et och3 F F OH H H XIX-16- 6 p-Me- Ph H H CH2-indol-3- yi Et och3 F F OH H H X1X-16- 7 p-Me- Ph H H ch2ch2sch3 Et och3 F F OH H H XIX-16- 8 i i p-Me- Ph <Jb- ·—3Ί * H * Et och3 F F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table ΧΪΧ-17.

Xa R1 R2 -rST T?6 R4 R3 1? X Y R7 R® XIX-17-1 p-F-Ph H H H Et OCH3 F F OH H H XIX-17-2 p-F-Ph H H ch3 Et och3 F F OH H H XIX-17-3 p-F-Ph H H CH(CH3)2 Et och3 F F OH H H XIX-17-4 p-F-Ph H H CH2CH(CH3)2 Et och3 F F OH H H XIX-17-5 p-F-Ph H H CH2Ph Et och3 F F OH H H XIX-17-6 p-F-Ph H H CH2-indol-3-yl Et OCHa F F OH H H XIX-17-7 p-F-Ph H H ch2ch2sch3 Et och3 F F OH H H XIX-17-8 p-F-Ph * H * Et och3 F F OH H H ♦R2 and R3b joined together by (CH2)j to form five-membered ring. 5 TableXIX-18. '^· ·ιr- r 'Ri· ' A * 1 f fl

Xs Rl R2 r3* R3b R4 R3 R6 X Y R7 R* XIX-18-1 p-CI-Ph H H H Et OCH3 F F OH H H XIX-18-2 p-Cl-Ph H H ch3 Et och3 F F OH H H XIX-18-3 p-Cl-Ph H H CHiCHah Et och3 F F OH H H 2983472-1 -426- WO 2008/121634

Docket No. 6013 7.0034 WOU1 PCT/US2008/058183

Ns R1 r! R3a R3„ R4 RJ R6 X Y R’ r“ XIX-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et OCHa F F OH H H XIX-18-5 p-Cl-Ph H H CH2Ph Et och3 F F OH H H XIX-18-6 p-Cl-Ph H H CH2-indoI-3-yl Et och3 F F OH H H XIX-18-7 p-Cl-Ph H H CH2CH2SCH3 Et och3 F F OH H H XIX-18-8 p-Cl-Ph ,3b: it J x * H * Et och3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIX-19.

Ns R1 r! “r35’ “R36 R4 R5 R6 X Y r’ R8 XIX-19-1 p-Br-Ph H H H Et och3 F F OH H H XIX-19-2 p-Br-Ph H H ch3 Et och3 F F OH H H XIX-19-3 p-Br-Ph H H CHCCH,), Et och3 F F OH H H XIX-19-4 p-Br-Ph H H CH2CH(CH3)2 Et och3 F F OH H H XIX-19-5 p-Br-Ph H H CH2Ph Et och3 F F OH H H XIX-19-6 p-Br-Ph H H CH2-indol-3-yl Et och3 F F OH H H XIX-19-7 p-Br-Ph H H CH2CH2SCH3 Et och3 F F OH H H XIX-19-8 p-Br-Ph ♦ H * Et och3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIX-20.

Ns R1 R3 r35" -p; R4 r3 “r5" X Y R7 XIX-20-1 p-l-Ph H H H Et OCHj F F OH H XIX-20-2 p-I-Ph H H ch3 Et OCH3 F F OH H X1X-20-3 p-I-Ph H H CH(CH3)2 Et och3 F F OH H XIX-20-4 p-I-Ph H H CH2CH(CH3>2 Et och3 F F OH H XIX-20-5 p-I-Ph H H CH2Ph Et och3 F F OH H XIX-20-6 p-I-Ph H H CH2-indol-3-yl Et och3 F F OH H XIX-20-7 p-I-Ph H H CH2CH2SCH3 Et och3 F F OH H XIX-20-8 p-I-Ph * H ♦ Et och3 F F OH H 5 *R2 and RJb joined together by (CHab to form five-membered ring.

Table XIX-21.

Ns r’ ΊΓ "r31" ΊΡ- TF R5 r6 X Y r’ R8 XIX-21-1 ch3 Η Η Η ipr och3 F F OH H H XIX-21-2 ch3 Η Η ch3 'Pr och3 F F OH H H XIX-21-3 ch3 Η Η CHiCHj), 'Pr och3 F F OH H H XIX-21-4 ch3 Η Η CH2CH(CH3)2 'Pr och3 F F OH H H 2983472-1 -427- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Xa R1 R2 R3" R3b IT R5 R6 X Y R7 Rh XIX-21-5 ch3 H H CH2Ph och3 F F OH H H XIX-21-6 ch3 H H CHrindol-3-y! 'Pr och3 F F OH H H X1X-21-7 ch3 H H CH2CH2SCH3 'Pr och3 F F OH H H XIX-21-8 , τι ch3 ,3b ·· ♦ H * 'Pr och3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIX-22.

Xa R1 R2 ΊΡ - - r4” RJ R6 X Y ΤΓ r“ XIX-22-1 Et H H H "W OCH3 F F OH H H XIX-22-2 Et H H ch3 'Pr och3 F F OH H H XIX-22-3 Et H H CHCCHah 'Pr och3 F F OH H H XIX-22-4 Et H H CH2CH(CH3)2 'Pr och3 F F OH H H XIX-22-5 Et H H CH2Ph fpr och3 F F OH H H XIX-22-6 Et H H CH2-indol-3-yl 'Pr och3 F F OH H H XIX-22-7 Et H H CH2CH2SCH3 'Pr och3 F F OH H H XIX-22-8 ,7-. Et 3FT" * H ♦ 'Pr och3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIX-23.

Xa R1 R3’ ~R3t> R4 Rs R6 X Y R7 R“ XIX-23-1 "W H H H ~7pT OCH3 F F OH H H XIX-23-2 'Pr H H CH3 'Pr och3 F F OH H H XIX-23-3 ‘Pr H H CHtCHah 'Pr och3 F F OH H H XIX-23-4 'Pr H H CH2CH(CH3)2 'Pr och3 F F OH H H XIX-23-5 'Pr H H CH2Ph 'Pr och3 F F OH H H XIX-23-6 'Pr H H CH2-indol-3-yl 'Pr och3 F F OH H H XIX-23-7 'Pr H H CH2CH2SCH3 'Pr och3 F F OH H H XIX-23-8 'Pr * H * 'Pr och3 F F OH H H 5 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table ΧΓΧ-24.

Xa R1 R2 R35" ΊΡ5 R4 R3 R6 X Y r’ r" XIX-24-1 feu H H H och3 F F OH H H XIX-24-2 'Bu H H CH3 ^r och3 F F OH H H XIX-24-3 'Bu H H CHtCH^ 'Pr och3 F F OH H H XIX-24-4 'Bu H H ΟΗ2ΟΗ(ΟΗ3)2 'Pr och3 F F OH H. H XIX-24-5 'Bu H H CH2Ph 'Pr och3 F F OH H H 2983472-1 -428- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Xs ΊΓ" R2 R5’ R3b R4 Rs R6 X Y ΊΓ Rs XIX-24-6 'Bu H H CH2-indol-3-yl ’W och3 F F OH H H XIX-24-7 'Bu H H CH2CH2SCH3 'Pr och3 F F OH H H XIX-24-8 'Bu jb'·:·" * H * 'Pr och3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIX-25.

X» R1 R2 “r31- R3b "R4" R5 R6 X Y R7 R8 XIX-25-1 Ph H H H 'Pr och3 F F OH H H XIX-25-2 Ph H H ch3 'Pr och3 F F OH H H XIX-25-3 Ph H H CH(CH3)2 'Pr och3 F F OH H H XIX-25-4 Ph H H CH2CH(CH3)2 'Pr och3 F F OH H H XIX-25-5 Ph H H CH2Ph 'Pr och3 F F OH H H XIX-25-6 Ph H H CH2-indol-3-yl 'Pr och3 F F OH H H XIX-25-7 Ph H H CH2CH2SCH3 Tr och3 F F OH H H XIX-25-8 Ph * H * 'Pr och3 F F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XIX-26.

Xa R1 R2 R3a r35 R4 R5 R6 X Y ΊΓ R8 XIX-26- 1 p-Me- Ph H H H /pr och3 F F OH H H XIX-26- 2 p-Me- Ph H H ch3 'Pr och3 F F OH H H XIX-26- 3 p-Me- Ph H H ΟΗ(ΟΗ3)2 'Pr och3 F F OH Η H XIX-26- 4 p-Me- Ph H H CH2CH(CH3)2 'Pr och3 F F OH H H XIX-26- 5 p-Me- Ph H H CH2Ph 'Pr och3 F F OH H H XIX-26- 6 p-Me- Ph H H CH2-indol-3- yi 'Pr och3 F F OH H H XIX-26- 7 p-Me- Ph H H ch2ch2sch3 'Pr och3 F F OH H H XIX-26- p-Me- * H * /pr och3 F F OH H H

Ph 5 *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -429- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XIX-27.

K9 R2 "R^ "r^ ΊΤ Rs R6 X Y R; R8 XIX-27-1 p-F-Ph H H H 'Pr och3 F F Oil H FI X1X-27-2 p-F-Ph H H ch3 'Pr och3 F F OH H H XIX-27-3 p-F-Ph H H CH(CH3)2 'Pr och3 F F OH H H XIX-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr och3 F F OH H H XIX-27-5 p-F-Ph H H CH2Ph 'Pr och3 F F OH H H XIX-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr och3 F F OH H H XIX-27-7 p-F-Ph H H CH2CH2SCH3 'Pr och3 F F OH H H XIX-27-8 "1^2' TV p-F-Ph ,3b- * H * 'Pr och3 F F OH H H *RzandR3b joined together by (CH2)3 to form five-membered ring.

Table XIX-28. X® R1 ΊΓ R5’ “r35 R4 R5 R6 X Y R' R8 XIX-28-1 p-Cl-Ph H H H “¥r" OCH3 F F OH H Η XIX-28-2 p-Cl-Ph H H ch3 'Pr och3 F F oh H Η XIX-28-3 p-Cl-Ph H H CH(CH3)2 'Pr och3 F F oh Η Η XIX-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr och3 F F oh Η Η XIX-28-5 p-Cl-Ph H H CH2Ph 'Pr och3 F F oh Η Η XIX-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr och3 F F oh Η Η XIX-28-7 p-CI-Ph H H CH2CH2SCH3 'Pr och3 F F oh Η Η XIX-28-8 p-CI-Ph ,3b · ♦ H * 'Pr 0CH3 F F OH Η Η ♦R2 and R30 joined together by (CPfeb to form five-membered ring. X® R1 R2 R3^ Rib R4 r5 R6 X Y I? R8 ΧΙΧ-29-1 p-Br-Ph H H H 'Pr och3 F F OH H Η ΧΙΧ-29-2 p-Br-Ph H H CH3 'Pr och3 F F OH Η Η ΧΙΧ-29-3 p-Br-Ph H H CH(CH3h Pr och3 F F OH H Η ΧΙΧ-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr och3 F F OH H Η XIX-29-S p-Br-Ph H H CH2Ph 'Pr och3 F F OH Η Η ΧΙΧ-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr och3 F F OH Η Η ΧΙΧ-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr och3 F F OH Η Η ΧΙΧ-29-8 - J η p-Br-Ph ,3b * H ♦ 'Pr och3 F F OH Η Η *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -430- WO 2008/121634

Docket No. 6013 7.0034WOU I PCT/US2008/058183

Table XIX-30.

Ns R1 r3b “R* R4 R5 R6 X Y R7 R11 XIX-30-1 p-I-Ph H H H 'Pr och3 F F OH H H XIX-30-2. p-I-Ph H H ch3 'Pr OCII3 F F OH H H XIX-30-3 p-I-Ph H H CH(CH3)2 'Pr och3 F F OH H H XIX-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr och3 F F OH H H XIX-30-S p-I-Ph H H CH2Ph 'Pr och3 F F OH H H XIX-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr och3 F F OH H H X1X-30-7 p-I-Ph H H CH2CH2SCH3 'Pr och3 F F OH H H XIX-30-8 p-I-Ph ♦ H ♦ 'Pr och3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIX-31.

Ns R1 r2" R3a R3b R4 RJ R6 X Y R7 r" XIX-31-1 CH3 H H H "Bu och3 F F OH H H XIX-31-2 ch3 H H ch3 "Bu och3 F F OH H H XIX-31-3 ch3 H H CH(CH3)2 "Bu och3 F F OH H H XIX-31-4 ch3 H H CH2CH(CH3)2 "Bu och3 F F OH H H XIX-31-5 ch3 H H CH2Ph "Bu och3 F F OH H H XIX-31-6 ch3 H H CH2-indol-3-yl "Bu och3 F F OH H H X1X-31-7 ch3 H H CH2CH2SCH3 "Bu och3 F F OH H H XIX-31-8 — ch3 .30 · · H "Bu och3 F F OH H H *R2 and R3” joined together by (Ctfeb to form five-membered ring.

Ns R1 R2 Rjb R4 R? R6 X Y R7" R# XIX-32-1 Et H H H "Bu OCH3 F F OH H H XIX-32-2 Et H H ch3 "Bu och3 F F OH H H XIX-32-3 Et H H CHCCHah "Bu och3 F F OH H H XIX-32-4 Et H H CH2CH(CH3)2 "Bu och3 F F OH H H XIX-32-5 Et H H CH2Ph "Bu och3 F F OH H H XIX-32-6 Et H H CH2-indol-3-yl "Bu OCH3 F F OH H H XIX-32-7 Et H H ch2ch2sch3 "Bu och3 F F OH H H XIX-32-8 _ i r. Et * H * "Bu och3 F F OH H H *RZ and Rejoined together by (CH2)3 to form five-membered ring 2983472-1 -431 - WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XIX-33.

Ns R1 R2 “r31" "R35 ΊΓ" Rs R6 X Y R’ R* XIX-33-1 'Pr H H H "Bu och3 F F OH H H XIX-33-2 'Pr H H ch3 "Bu och3 F F OH H H XIX-33-3 zPr H H CH(CH3)a "Bu och3 F F OH H H XIX-33-4 'Pr H H CH2CH(CH3)2 "Bu och3 F F OH H H XIX-33-5 'Pr H H CH2Ph "Bu och3 F F OH H H XIX-33-6 'Pr H H CH2-indol-3-yl "Bu och3 F F OH H H XIX-33-7 'Pr H H CH2CH2SCH3 "Bu och3 F F OH H H XIX-33-8 j ΤΊ 'Pr ♦ H * "Bu och3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIX-34.

Na Rl R2 R3“ "R3® ΊΤ" T?— Ra X Y R7 R8 XIX-34-1 'Bu H H H "Bu och3 F F OH H Η XIX-34-2 'Bu H H ch3 "Bu och3 F F OH H H XIX-34-3 'Bu H H CH(CH3)2 "Bu och3 F F oh Η H XIX-34-4 'Bu H H CH2CH(CH3)2 "Bu och3 F F oh H H XtX-34-5 'Bu H H CH2Ph "Bu och3 F F OH H Η XIX-34-6 'Bu H H CHj-indol-3-yl "Bu och3 F F OH Η H XIX-34-7 'Bu H H ch2ch2sch3 "Bu och3 F F OH H H XIX-34-8 Jt- 'Bu □b· · * H * "Bu och3 F F OH H H *R2 and RJb joined together by (CH^b to form five-membered ring.

Table XIX-35.

Ns R1 R2 "R35" R3b ΊΤ“ r5— R6 X Y r’ R8" XIX-35-1 Ph H H H "Bu och3 F F OH H H XIX-35-2 Ph H H ch3 "Bu och3 F F OH H H XIX-35-3 Ph H H CH(CH3)2 "Bu och3 F F OH H H XIX-35-4 Ph H Η CH2CH(CH3)a "Bu och3 F F OH H H XIX-35-5 Ph Η H CHaPh "Bu och3 F F OH, H H XIX-35-6 Ph H H CHa-indol-3-y] "Bu och3 F F OH H H XIX-35-7 Ph H H CH2CH2SCH3 "Bu och3 F F OH H H XIX-35-8 . n Ph 3ΒΎ7· * H • "Bu och3 F F OH H H *R2 and Rejoined together by (CHabt0 ^οπη five-membered ring. 2983472-1 -432- WO 2008/121634

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Table XIX-36.

Ns Rl “Τ’ ' Rs "r35 R5 R6 X Y r” R8 X1X-36- 1 p-Me- Ph H H H "Bu och3 F F OH H H XIX-36- 2 p-Me- Ph H H ch3 "Bu och3 F F OH H H XIX-36- 3 p-Me- Ph H H CH(CH3)2 "Bu och3 F F OH H H XIX-36- 4 p-Me- Ph H H CH2CH(CH3)2 "Bu och3 F F OH H H XIX-36- S p-Me- Ph H H CH2Ph "Bu och3 F F OH H H XIX-36- 6 p-Me- Ph H H CH2-indol-3- yi "Bu och3 F F OH H H XIX-36- 7 p-Me- Ph H H ch2ch2sch3 "Bu och3 F F OH H H XIX-36- 8 j i p-Me» Ph 6”·" ”-j * H * "Bu och3 F F OH H H *R2 and RJbjoined together by (CFbb to ^orm five-membered ring.

Table XIX-37.

Ns R1 R2 r55" R3b R4 Έ— R4 X Y R7 R8 XIX-37-1 p-F-Ph H H H "Bu och3 F F OH H H XIX-37-2 p-F-Ph H H ch3 "Bu och3 F F oh H H XIX-37-3 p-F-Ph H H CH(CH3)2 "Bu och3 F F OH H H XIX-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu och3 F F OH H H XIX-37-5 p-F-Ph H H CH2Ph "Bu och3 F F OH H H XIX-37-6 p-F-Ph H H CH2-indol-3-yl "Bu och3 F F OH H H XIX-37-7 p-F-Ph H H ch2ch2sch3 "Bu och3 F F OH H H XIX-37-8 p-F-Ph * H * "Bu och3 F F OH H H *R2 and R: Jb joined together by (CHjb to form five-membered ring. Table XIX-38. Ns R1 R2 r^ R4 R3 R4 X Y r’ r“

XIX-38- 1 p-CI- Ph H H H "Bu OCH3 F F OH H H XIX-38- p-Cl- Ph H H ch3 "Bu och3 F F OH H H 2983472-1 »433 - WO 2008/121634 PCT/US2008/058183

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Xs R1 R2 RJs - - R5 R6 X Y K 2 XIX-38- 3 p-CI- Ph H H CH(CH3)2 "Bu och3 F F OH H H XIX-38- 4 p-Cl- Ph H H CH2CH(CH3)2 "Bu och3 F F OH H H XIX-38- 5 p-Cl- Ph H H Cl-I2Ph "Bu och3 F F OH H H XIX-38- 6 p-Cl- Ph H H CH2-indol-3- yi "Bu och3 F F OH H H XIX-38- 7 p-CI- Ph H H ch2ch2sch3 "Bu och3 F F OH H H XIX-38- p-CI- * H ♦ "Bu och3 F F OH H H

Ph *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XIX-39.

Xs R1 R2 RJl R3b R4 R5 R6 X Y R' R“ X1X-39- 1 p-Br- Ph H H H "Bu OCH3 F F OH H H XIX-39- 2 p-Br- Ph H H ch3 "Bu och3 F F OH H H XIX-39- 3 p-Br- Ph H H CH(CH3>2 "Bu och3 F F OH H H XIX-39- 4 p-Br- Ph H H CH2CH(CH3)2 "Bu och3 F F OH H H XIX-39- 5 p-Br- Ph H H CH2Ph "Bu och3 F F OH H H XIX-39- 6 p-Br- Ph H H CH2-indol-3- yi "Bu och3 F F OH H H X1X-39- 7 p-Br- Ph H H ch2ch2sch3 "Bu och3 F F OH H H XIX-39- 8 p-Br- Ph * H 4 "Bu och3 F F OH H H *R2 and R30 joined together by to form five-membered ring. 2983472-1 -434- WO 2008/121634 PCT/US2008/058183

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Table XIX-40, D1

Ns R1 "F* -p; “F~ Rs R6 X Y Ίΐ Ru XIX-40-1 p-l-Ph H H H ”Bu och3 F F OH H H XIX-40-2 p-I-Ph H H ch3 ”Bu och3 F F OH H H XIX-40-3 p-I-Ph H H CH(CH3)j flBu och3 F F OH H H XIX-40-4 p-I-Ph H H CH2CH(CH3)2 ”Bu och3 F F OH H H XIX-40-5 p-l-Ph H H CH2Ph "Bu och3 F F OH FI H X1X-40-6 p-I-Ph H H CHrindol-3-yl "Bu OCH, F F OH H H XIX-40-7 p-I-Ph H H CH2CH2SCH3 ”Bu och3 F F OH H H XIX-40-8 p-I-Ph * H * ”Bu och3 F F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XIX-41.

Ns R R5 R3a R3b R4 R5 R6 X Y R7 R" XIX-41-1 ch3 Η H H Bz OCH3 F F OH H H XIX-41-2 ch3 H H CH3 Bz och3 F F OH H H XIX-41-3 ch3 Η H CH(CH3)2 Bz och3 F F OH H H XIX-41-4 ch3 H H CH2CH(CH3)2 Bz och3 F F OH H H XIX-41-5 ch3 Η H CH2Ph Bz och3 F F OH H H XIX-41-6 ch3 H H CH2-indol-3-yl Bz och3 F F OH H H XIX-41-7 ch3 H H CH2CH2SCH3 Bz och3 F F OH H H XIX-41-8 ch3 * H * Bz ocfi3 F F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XIX-42. I — J ... g 1 '»" I »

Ns R RJ Rj. R3b R4 R5 R5 X Y R7 R" XIX-42-1 Et H H H Bz och3 F F OH H H XIX-42-2 Et H H ch3 Bz och3 F F OH H H XIX-42-3 Et H H CHiCHa), Bz och3 F F OH H H XIX-42-4 Et H H CH2CH(CH3)2 Bz och3 F F OH H H XIX-42-5 Et H H CH2Ph Bz och3 F F OH H H XIX-42-6 Et H H CHrindol-3-yl Bz och3 F F OH H H XIX-42-7 Et H H CH2CH2SCH3 Bz och3 F F OH H H XIX-42-8 Et * H * Bz och3 F F OH H H *R2 and R3” joined together by (CH^ to form five-membered ring. 2983472-1 -435- WO 2008/121634

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Table XIX-43.

Ns R1 r2" "Έ35" R3b V RJ R6 X Y R7 R8 XIX-43-1 'Pr H H H Bz och3 F F OH H H XIX-43-2 'Pr H H ch3 Bz och3 F F OH H H XIX-43-3 'Pr H H CH(CH3)2 Bz och3 F F OH H H XIX-43-4 /Pr H H CH2CH(CH3)2 Bz och3 F F OH H H XIX-43-5 'Pr H H CH2Ph Bz och3 F F OH H H XIX-43-6 'Pr H H CH2-indol-3-yl Bz och3 F F OH H H XIX-43-7 'Pr H H CH2CH2SCH3 Bz och3 F F OH H H XIX-43-8 'Pr * H * Bz och3 F F OH H H *R2 and R3b joined together by (CFbb to form five-membered ring.

Table XIX-44.

Ns Ί<Γ r3. R36 R4 R* R6 X Y R7 R8 XIX-44-1 'Bu H H H Bz och3 F F OH H Η XIX-44-2 'Bu H H CH3 Bz och3 F F oh Η Η XIX-44-3 'Bu H H CH(CH3)2 Bz och3 F F oh Η Η XIX-44-4 'Bu H H CH2CH(CH3)2 Bz och3 F F oh Η Η XIX-44-5 'Bu H H CH2Ph Bz och3 F F oh Η Η XIX-44-6 'Bu H H CH2-indol-3-y1 Bz och3 F F oh Η Η XIX-44-7 'Bu H H CH2CH2SCH3 Bz och3 F F OH Η Η XIX-44-8 'Bu * H * Bz och3 F F OH Η Η *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XIX-45.

I rt— hl ' ' 4 1 .........2' -- B

Ns R ΊΓ RJ“ R3b R4 R5 R6 X Y R7 R8 ΧΙΧ-45-1 Ph H H H Bz OCH3 F F OH H H ΧΙΧ-45-2 Ph H H CH3 Bz och3 F F OH H H ΧΙΧ-45-3 Ph H H CH(CH3)2 Bz och3 F F OH H H ΧΙΧ-45-4 Ph H H CH2CH(CH3)2 Bz och3 F F OH H H ΧΙΧ-45-5 Ph H H CH2Ph Bz och3 F F OH H H ΧΙΧ-45-6 Ph H H CH2-indol-3-yt Bz och3 F F OH H H ΧΙΧ-45-7 Ph H H CH2CH2SCH3 Bz och3 F F OH H H ΧΙΧ-45-8 J ΤΛ Ph 3b > · * H * Bz och3 F F OH H H *R2 and R3b joined together by (CHab to form five-membered ring. 2983472-1 -436- WO 2008/121634

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Table XIX-46.

Ns Rl R2 R4 R3 R6 X Y R’ R^ XIX-46- 1 p-Me- Ph H H H Bz och3 F F OH H H XIX-46- 2 p-Mc- Ph H H ch3 Bz och3 F F OH H H XIX-46- 3 p-Me- Ph H H CH(CH3>2 Bz och3 F F OH H H XIX-46- 4 p-Me- Ph H H CH2CH(CH3)2 Bz och3 F F OH H H XIX-46- 5 p-Me- Ph H H CH2Ph Bz och3 F F OH H H XIX-46- 6 p-Me- Ph H H CH2-indol-3- yi Bz och3 F F OH H H XIX-46- 7 p-Me- Ph H H ch2ch2sch3 Bz och3 F F OH H H XIX-46- p-Me- * H * Bz och3 F F OH H H

Ph *R2 and RJb joined together by (Clhb to form five-membered ring.

Table XIX-47.

Ns R1 R2 “r35" R3b ΊΓ" Rs r6 X Y r' XIX-47-1 p-F-Ph H H H Bz OCH3 F F OH H H XIX-47-2 p-F-Ph H H ch3 Bz och3 F F OH H H XIX-47-3 p-F-Ph H H CH(CH3)2 Bz och3 F F OH H H XIX-47-4 p-F-Ph H H CHjCH(CH3)3 Bz och3 F F OH H H XIX-47-5 p-F-Ph H H CH2Ph Bz och3 F F OH H H XIX-47-6 p-F-Ph H H CH2-indoI-3-yl Bz och3 F F OH H H XIX-47-7 p-F-Ph H H CH2CH2SCH3 Bz och3 F F OH H H XIX-47-8 p-F-Ph * H * Bz och3 F F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XIX-48. ' 'T 1 H It- HL - J g· - J' 1 ‘TB-

Ns R1 R2 r3« R3b R4 R3 R4 X Y R7 R“ XIX-48-1 p-CI-Ph H H H Bz OCH3 F F OH H H XIX-48-2 p-Cl-Ph H H ch3 Bz och3 F F OH H H XIX-48-3 p-Cl-Ph H H CH(CH3)2 Bz och3 F F OH H H 2983472-1 -437- WO 2008/121634

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Xs T R2 ΊΡ7 R4 R6 X Y RT R’ XIX-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz OCHj F F OH H H ΧΪΧ-48-5 p-Cl-Ph H H CH2Ph Bz och3 F F OH H H XIX-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz och3 F F OH H H XIX-48-7 p-Cl-Ph H H CH2CH2SCH3 Bz och3 F F OH H H XIX-48-8 p-Cl-Ph * H * Bz och3 F F OH H H *R2 and Rejoined together by to form five-membered ring.

Table XIX-49.

Ns R1 R2 R3e R3” R4 R5 R6 X Y R' R8 XIX-49-1 p-Br-Ph H H H Bz OCH3 F F OH H H XIX-49-2 p-Br-Ph H H ch3 Bz och3 F F oh H H XIX-49-3 p-Br-Ph H H CH(CH3)2 Bz och3 F F oh H H XIX-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz och3 F F oh H H XIX-49-5 p-Br-Ph H H CH2Ph Bz och3 F F oh H H XIX-49-6 p-Br-Ph H H CH2-indol-3-yl Bz och3 F F OH H H XIX-49-7 p-Br-Ph H H CH2CH2SCH3 Bz och3 F F OH H H XIX-49-8 p-Br-Ph ♦ H * Bz och3 F F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XIX-50.

Ns R1 R2 R3" R4 R5 R* X Y R’ R8 XIX-50-1 p-I-Ph H H H Bz OCH3 p F OH H H XIX-50-2 p-I-Ph H H CH3 Bz OCH3 F F OH H H XIX-50-3 p-I-Ph H H CH(CH3)2 Bz och3 F F oh H H XIX-50-4 p-i-Ph H H CH2CH(CH3)2 Bz och3 F F oh H H XIX-50-5 p-I-Ph H H CH2Ph Bz och3 F F oh H H XIX-50-6 p-I-Ph H H CH2-indol-3-yl Bz och3 F F OH H H XIX-50-7 p-I-Ph H H CH2CH2SCH3 Bz och3 F F OH H H XIX-50-8 p-I-Ph .3b · 1 * H * Bz och3 F F OH H H *R2 and RJb joined together by (Cl·^ to form five-membered ring. 2983472-1 -438- WO 2008/121634 PCT/US2008/058183

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XX

Table XX-1.

Jia ΊΓ“ ΊΓ r3. R4 Rj R6 X Y ΊΓ Ϊ? XX-1-1 ch3 H H H ch3 och3 H F OH H H XX-1-2 CHj H H ch3 ch3 och3 H F OH H H XX-1-3 ch3 H H CH(CH3)2 ch3 och3 H F OH H H XX-1-4 ch3 H H CH2CH(CH3)2 ch3 och3 H F OH H H XX-1-5 ch3 H H CH2Ph ch3 och3 H F OH H H XX-1-6 ch3 H H CH2-indot-3-yl ch3 och3 H F OH H H XX-1-7 ch3 H H ch2ch2sch3 ch3 och3 H F OH H H XX-1-8 ch3 * H ★ ch3 och3 H F OH H H *R2 and R36 joined together by (CH^to form five-membered ring.

Table XX-2.

Jia Rl R1 -r3T- R3b R4 R5 R* X Y r’ r“ XX-2-1 Et H H H ch3 OCH3 Η F OH H H XX-2-2 Et H H CH3 ch3 och3 H F OH Η H XX-2-3 Et H H CH(CH,)j ch3 och3 H F OH H H XX-2-4 Et H H CH2CH(CH3)2 ch3 och3 H F OH Η H XX-2-5 Et H H CH2Ph ch3 och3 H F OH H H XX-2-6 Et H H CH2-indol-3-yl ch3 och3 H F OH H H XX-2-7 Et H H CH2CH2SCH3 ch3 och3 H F OH Η H XX-2-8 j' Et r»3b * H * ch3 och3 Η F OH H H *R2 and R30 joined together by (CH^ to form five-membered ring. 2983472-1 -439- WO 2008/121634

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Table XX-3.

Xa R1 R2 R3“ "F R4 R5 R6 X Y R Ra XX-3-1 'Pr H H H ch3 och3 H F OH H H XX-3-2 ipr H H ch3 ch3 och3 H F OH H H XX-3-3 'Pr H H CH(CH3)2 ch3 och3 H F OH H H XX-3-4 'Pr H H CH2CH(CH3)2 ch3 och3 H F OH H H XX-3-5 'Pr H H CH2Ph ch3 och3 H F OH H H XX-3-6 'Pr H H CH2-indol-3-yl ch3 och3 H F OH H H XX-3-7 'Pr H H CH2CH2SCH3 ch3 och3 H F OH H H XX-3-8 'Pr ♦ H * ch3 och3 H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XX-4.

Xs R1 R1 RjR R3b r^ R5 R6 X Y R' Rb XX-4-1 'Bu H H H ch3 och3 H F OH H H XX-4-2 'Bu H H ch3 ch3 och3 H F OH H H XX-4-3 'Bu H H CH(CH3)2 ch3 och3 H F OH H H XX-4-4 'Bu H H CH2CH(CH3)2 ch3 ocfi3 H F OH H H XX-4-5 'Bu H H CH2Ph ch3 och3 H F OH H H XX-4-6 'Bu H H CH2-indol-3-yl ch3 och3 H F OH H H XX-4-7 'Bu H H CH2CH2SCH3 ch3 och3 H F OH H H XX-4-8 'Bu "r73h ♦ H ♦ ch3 och3 H F OH H H *R2 and RJ0 joined together by (CH2)3 to form five-membered ring.

Xs ir R1 rSb "r*- R^’ R5 R6 X Y R1 Ru XX-5-1 Ph H H H CH3 och3 H F OH H H XX-5-2 Ph H H ch3 ch3 och3 H F OH H H XX-5-3 Ph H H ΟΗ(ΟΗ3)2 ch3 och3 H F OH H H XX-5-4 Ph H H CH2CH(CH3)2 ch3 och3 H F OH H H XX-5-5 Ph H H CH2Ph ch3 och3 H F OH H H XX-5-6 Ph H H CH2-indol-3-yI ch3 och3 H F OH H H XX-5-7 Ph H H CH2CH2SCH3 ch3 och3 H F OH H H XX-5-8 Ph * H * ch3 och3 H F OH H H *RZ and RJb joined together by (0¾¼ to form five-membered ring. 2983472-1 -440- WO 2008/12J 634 PCT/US2008/058183

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Table XX-6.

X2 T R3 R3’ "r35 R4 Rs Ίτ X Y r’ r“ XX-6-1 p-Me-Ph H H H ch3 och3 H F OH H H XX-6-2 p-Me-Ph H H ch3 ch3 OCH3 H F OH H H XX-6-3 p-Me-Ph H H CH(CH3)2 ch3 och3 H F OH H H XX-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 och3 H F OH H H XX-6-5 p-Me-Ph H H CH2Ph ch3 och3 H F OH H H XX-6-6 p-Me-Ph H H CH2-indol-3-yl ch3 och3 H F OH H H XX-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 och3 H F OH H H XX-6-8 ATt'2 J p-Me-Ph * H * ch3 och3 H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XX-7. X2 ~R>- R3 IF’ "r^ R? ΕΓ X Υ r R" XX-7-1 p-F-Ph H H H ch3 och3 Η F ΟΗ Η Η XX-7-2 p-F-Ph H H CH3 ch3 och3 Η F ΟΗ Η Η XX-7-3 p-F-Ph H H CH(CH3)2 ch3 och3 Η F ΟΗ Η Η XX-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 och3 Η F ΟΗ Η Η XX-7-6 p-F-Ph H H CH2Ph ch3 och3 Η F ΟΗ Η Η XX-7-7 p-F-Ph H H CH2-indol-3-yl ch3 och3 Η F ΟΗ Η Η XX-7-8 p-F-Ph H H CH2CH2SCH3 ch3 och3 Η F ΟΗ Η Η XX-7-20 *n2 J i p-F-Ph * H + ch3 och3 Η F ΟΗ Η Η ♦R2 and RJb joined together by (CH2)3 to form five-membered ring.

Κ2 R1 R3 IF "r35 R4 R5 R6 X Y r“ ΧΧ-8-1 p-Cl-Ph H H H ch3 och3 H F OH Η H ΧΧ-8-2 p-Cl-Ph H H ch3 ch3 och3 H F OH H H ΧΧ-8-3 p-Cl-Ph H H CH(CH3)2 ch3 och3 H F OH H H ΧΧ-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 OCH, H F OH H H ΧΧ-8-5 p-Cl-Ph H H CH2Ph ch3 och3 H F OH H H ΧΧ-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 och3 Η F OH H H ΧΧ-8-7 p-Cl-Ph H H ch2ch2sch3 ch3 och3 Η F OH H H ΧΧ-8-8 - J p-Cl-Ph «3b·-;-:—: * H * ch3 och3 Η F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -441 - WO 2008/121634

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Table XX-9.__

Tfe R1 R2 R3’ R3b r’ R5 R0 X Ύ R* Rb

XX-9-1 p-Br- Ph H H H ch3 och3 H F OH XX-9-2 p-Br- Ph H H ch3 ch3 och3 H F OH XX-9-3 p-Br- Ph H H CH(CH3)2 ch3 och3 H F OH XX-9-4 p-Br- Pb H H CH2CH(CH3)2 ch3 och3 H F OH XX-9-6 p-Br- Ph H H CH2Ph ch3 och3 H F OH XX-9-7 p-Br- Ph H H CH2-indo1-3-yl ch3 och3 H F OH XX-9-8 p-Br- Ph H H CH2CH2SCH3 ch3 och3 H F OH XX-9- 20 p-Br- Ph ♦ H * ch3 och3 H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XX-10.

r1- R2 R,ji R3b R4 R5 R6 X Y R7 R8 XX-10-1 p-I-Ph H H H CH3 OCH3 H F OH H H XX-10-2 p-I-Ph H H CH3 CH3 och3 H F OH H H XX-10-3 p-I-Ph H H CH(CH3)2 ch3 och3 H F OH H H XX-10-4 p-I-Ph H H CHjCHCCH,), ch3 och3 H F OH H H XX-10-5 p-I-Ph H H CH2Ph ch3 och3 H F OH H H XX-10-6 p-I-Ph H H CH2-indol-3-yl ch3 och3 H F OH H H XX-10-7 p-I-Ph H H CH2CH2SCH3 ch3 och3 H F OH H H XX-10-8 p-I-Ph * H * ch3 och3 H F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XX-11.

'^· ’ t·'^ H'· R"...... RL ,M 1 ' ‘1 I "* 2 T U

Xs R1 R2 R3. R3b R4 Rs R6 X Υ R7 R8 XX-11-1 ch3 Η H Η Et och3 H F ΟΗ Η Η XX-11-2 ch3 H Η ch3 Et och3 Η F ΟΗ Η Η XX-11-3 ch3 H Η CHCCH^ Et och3 Η F ΟΗ Η Η XX-11-4 ch3 H Η CH2CH(CH3)2 Et och3 Η F ΟΗ Η Η XX-11-5 ch3 Η Η CH2Ph Et och3 Η F ΟΗ Η Η XX-11-6 ch3 H Η CHrindol-3-yl Et och3 Η F ΟΗ Η Η XX-11-7 ch3 H Η CH2CH2SCH3 Et och3 Η F ΟΗ Η Η 2983472-1 -442- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Ns R1 R2 —£ϊϊ ”r* R4 R5 R6 X Y re r“ XX-11-8 ch3 * H * Et och3 H F OH H H *R2 and R,b joined together by (CH2)3 to form five-membered ring. Table XX-12. R R2 R3* R3b R4 Rs R6 X Y R R11 XX-12-1 Et H H H Et och3 H F OH H H XX-12-2 Et H H ch3 Et och3 H F OH H H XX-12-3 Et H H CH(CH3)2 Et och3 H F OH H H XX-12-4 Et H H CH2CH(CH3)2 Et och3 H F OH H H XX-12-5 Et H H CH2Ph Et och3 H F OH H H XX-12-6 Et H H CH2-indol-3-yl Et och3 H F OH H H XX-12-7 Et H H CH2CH2SCH3 Et och3 H F OH H H XX-12-8 Et * H * Et och3 H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XX-13. R1 R2 R3a R5® R4 R5 R6 X Y r’ R“ XX-13-1 'Pr H H H Et 0CH3 H F OH H H XX-13-2 'Pr H H CH3 Et och3 Η F OH H H XX-13-3 'Pr H H CH(CH3)2 Et och3 H F OH H H XX-13-4 'Pr H H CH2CH(CH3)2 Et och3 H F OH H H XX-13-5 fpr H H CH2Ph Et och3 H F OH H H XX-13-6 'Pr H H CHrindol-3-yl Et och3 H F OH H H XX-13-7 'Pr H H CH2CH2SCH3 Et och3 H F OH H H XX-13-8 'Pr ♦ H * Et och3 H F OH H H ♦R2 and R3b joined together by (0¾¼ to form five-membered ring. 2983472-1 -443- WO 2008/121634

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Table XX-14.

Xs R2 r3. -p; R4 R5 ΊΤ X Y r“ XX-14-1 'Bu H H H Et och3 H F OH H H XX-14-2 'Bu H H ch3 Et och3 H F OH H H XX-14-3 'Bu H H CH(CH3)2 Et och3 H F OH H H XX-14-4 'Bu H H CH2CH(CH3)2 Et och3 H F OH H H XX-14-5 'Bu H H CH2Ph Et och3 H F OH H H XX-14-6 'Bu H H CH2-indol-3-yl Et OCH3 H F OH H H XX-14-7 'Bu H H ch2ch2sch3 Et och3 H F OH H H XX-14-8 'Bu * H ♦ Et och3 H F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XX-15.

Xs R R2 R3i R35 R4 R5 R6 X Y R' Rs XX-15-1 Ph H H H Et och3 Η F OH H H XX-15-2 Ph H H CH3 Et och3 H F OH H H XX-15-3 Ph H H CH(CH3)2 Et och3 H F OH H H XX-15-4 Ph H H CH2CH(CH3)2 Et och3 H F OH H H XX-15-5 Ph H H CH2Ph Et och3 H F OH H H XX-15-6 Ph H H CH2-indol-3-yl Et och3 H F OH H H XX-15-7 Ph H H CH2CH2SCH3 Et och3 H F OH H H XX-15-8 Ph * H * Et och3 H F OH H H *R2 and RJt> joined together by (CH2)3 to form five-membered ring. 5 Table XX-16.

...... - .- ......... j - - J

Xs R1 R2 RJi R3b 1C R5 Rs X Y ΊΓ R* XX-16-1 p-Me-Ph H H H Et OCH3 H F OH H H XX-16-2 p-Me-Ph H H ch3 Et och3 H F OH H H XX-16-3 p-Me-Ph H H CH(CH3)2 Et och3 H F OH H H XX-16-4 p-Me-Ph H H CH2CH(CH3)2 Et och3 H F OH H H XX-16-5 p-Me-Ph H H CH2Ph Et 00¾ H F OH H H XX-16-6 p-Me-Ph H H CH2-indol-3-yl Et och3 H F OH H H XX-16-7 p-Me-Ph H H CH2CH2SCH3 Et 0CH3 H F OH H H XX-16-8 p-Me-Ph * H ♦ Et och3 H F OH H H *R2 and RJt> joined together by (0¾^ to form five-membered ring. 2983472-1 -444- WO 2008/121634

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Table XX-17.

Na R1 R2 -jpr- "r35 R5 R5" X Y R7 1c XX-17-I p-F-Ph H H H Et och3 H F OH H H XX-17-2 p-F-Ph H H ch3 Et och3 H F OH H H XX-17-3 p-F-Ph H H CH(CH3)2 Et och3 H F OH H H XX-17-4 p-F-Ph H H CH2CH(CH3)2 Et och3 H F OH H H XX-17-5 p-F-Ph H H CH2Ph Et och3 H F OH H H XX-17-6 p-F-Ph H H CH2-indol-3-yl Et och3 II F OH H H XX-17-7 p-F-Ph H H CH2CH2SCH3 Et och3 H F OH H H XX-17-8 p-F-Ph * H * Et och3 H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XX-18.

TFfe R1 R2 -pr- "R3® Rs R6 X Y R7 R8 XX-18-1 p-Cl-Ph H H H Et och3 H F OH H H XX-18-2 p-CI-Ph H H CH3 Et och3 H F OH H H XX-18-3 p-Cl-Ph H H ΟΗ(ΟΗ3)2 Et och3 H F OH H H XX-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et och3 H F OH H H XX-18-5 p-Cl-Ph H H CH2Ph Et och3 H F OH H H XX-18-6 p-Cl-Ph H H CH2-indoI-3-yl Et och3 H F OH H H XX-18-7 p-Cl-Ph H H CH2CH2SCH3 Et och3 H F OH H H XX-18-8 p-Cl-Ph * H * Et och3 H F OH H H ♦Rz and R3b joined together by (CH2)3 to form five-membered ring. Table XX-19. Ife R1 R2 R3a "r3® R4 R3 R6 X Y R; R8 XX-19-1 p-Br-Ph H H H Et och3 H F OH H H XX-19-2 p-Br-Ph H H ch3 Et och3 H F OH H H XX-19-3 p-Br-Ph H H CH(CH3)2 Et och3 H F OH H H XX-19-4 p-Br-Ph H H CH2CH(CH3)2 Et och3 H F OH H H XX-19-5 p-Br-Ph H H CHaPh Et och3 H F OH H H XX-19-6 p-Br-Ph H H CH2-indol-3-yl Et och3 H F OH H H XX-19-7 p-Br-Ph H H CH2CH2SCH3 Et och3 H F OH H H XX-19-8 p-Br-Ph j Tk3b » · J * H * Et och3 H F OH H H *R2 and R31* joined together by (CH2)3 to form five-membered ring, 2983472-1 -445 - WO 2008/121634

Docket No. 60137.0034WOUI PCT/US2008/058183

Table XX-20.

N° "R1 ir” R3' R3b R4 T R6 X Y r’ Rtt XX-20-1 p-I-Ph H H H Et och3 H F OH H H XX-20-2 p-I-Ph H H ch3 Et och3 H F OH H H XX-20-3 p-I-Ph H H CH(CH3)2 Et och3 H F OH H H XX-20-4 p-I-Ph H H CH2CH(CH3)2 Et och3 H F OH H H XX-20-5 p-I-Ph H H CH2Ph Et 0CH3 H F OH H H XX-20-6 p-I-Ph H H CH2-indol-3-yl Et och3 H F OH H H XX-20-7 p-I-Ph H H CH2CH2SCH3 Et och3 H F OH H H XX-20-8 p-I-Ph -.3 b ; )¼ H ♦ Et och3 H F OH H H *R7 and R3b joined together by (CH2)3 to form five-membered ring.

Table XX-21.

Ns R1 R5a ----- R4 R5 R6 X Y R’ R“ XX-21-1 ch3 H H H ipr OCH3 H F OH H H XX-21-2 ch3 H H CH3 'Pr och3 H F OH H H XX-21-3 ch3 H H CH(CH3)2 'Pr och3 H F OH H H XX-21-4 ch3 H H CH2CH(CH3)2 'Pr och3 H F OH H H XX-21-5 ch3 H H CH2Ph 'Pr och3 H F OH H H XX-21-6 ch3 H H CH2-indol-3-yl 'Pr och3 H F OH H H XX-21-7 ch3 H H CH2CH2SCH3 'Pr och3 H F OH H H XX-21-8 ch3 * H * 'Pr och3 H F OH H H *R2 and R3b joined together by (CH^ to form five-membered ring.

Na R1 “R3- r3« R3b -R4” Έ— Rfc X Y r" Rtf XX-22-1 Et H H H 'Pr OCH3 H F OH H H XX-22-2 Et H H CH3 'Pr OCH3 H F OH H H XX-22-3 Et H H CH(CH3)2 'Pr och3 H F OH H H XX-22-4 Et H H CH2CH(CH3)2 'Pr och3 H F OH H H XX-22-5 Et H H CH2Ph 'Pr och3 H F OH H H XX-22-6 Et H H CH2-indol-3-yl 'Pr och3 H F OH H H XX-22-7 Et H H CH2CH2SCH3 'Pr och3 H F OH H H XX-22-8 J, Et ♦ H * 'Pr och3 H F OH H H *R2 and RJb joined together by (CHa)3 to form five-membered ring. 2983472-1 -446- WO 2008/12 J 634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XX-23.

X2 RJ R2 R3" "R^ IT RJ R6 X Y ir R8 XX-23-1 'Pr H H H 'Pr och3 H F OH H H XX-23-2 'Pr H H ch3 'Pr 0CH3 H F OH H H XX-23-3 'Pr H H CH(CH3)2 'Pr och3 H F OH H H XX-23-4 'Pr H H CH2CH(CH3)2 'Pr och3 H F OH H H XX-23-5 'Pr H H CH2Ph 'Pr och3 H F OH H H XX-23-6 'Pr H H CH2-indot-3-yl 'Pr och3 H F OH H H XX-23-7 'Pr H H CH2CH2SCH3 'Pr och3 H F OH H H XX-23-8 __ j τ 'Pr * H * 'Pr och3 H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XX-24.

Xe Rl R2 R3· "r35 R4 R5 R* X Υ R7 R8 XX-24-1 'Bu H H H "W OCH3 H F ΟΗ Η Η XX-24-2 'Bu H H ch3 'Pr och3 Η F ΟΗ Η Η XX-24-3 'Bu H H CH(CH3)2 'Pr och3 Η F ΟΗ Η Η XX-24-4 'Bu H H CH2CH(CH3)2 'Pr och3 Η F ΟΗ Η Η XX-24-5 'Bu H H CH2Ph 'Pr och3 Η F ΟΗ Η Η XX-24-6 'Bu H H CH2-indot-3-yl Tr och3 Η F ΟΗ Η Η XX-24-7 'Bu H H CH2CH2SCH3 Tr och3 Η F ΟΗ Η Η XX-24-8 'Bu ♦ H * 'Pr och3 Η F ΟΗ Η Η ♦R2 and Rejoined together by (CH2)j to form five-membered ring. 5 Table XX-25. —I W 11 HL· - '"'Vi I ~ --.. >1' -. U '

Xi R IF R” R3b R4 R5 R6 X Y R7 R“ ΧΧ-25-1 Ph H H H 'Pr och3 H F OH H H ΧΧ-25-2 Ph H H ch3 Tr och3 H F OH H H ΧΧ-25-3 Ph H H CH(CH3)2 'Pr och3 Η F OH H H ΧΧ-25-4 Ph H H CH2CH(CH3)2 'Pr och3 H F OH H H ΧΧ-25-5 Ph H H CH2Ph 'Pr och3 H F OH H H ΧΧ-25-6 Ph H H CH2-indol-3-yl 'Pr och3 H F OH H H ΧΧ-25-7 Ph H H ch2ch2sch3 'Pr och3 H F OH H H ΧΧ-25-8 Ph * H * 'Pr och3 H F OH H H ♦R2 and Rejoined together by (0¾^ to form five-membered ring. 2983472-1 -447- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XX-26.

Xs R1 R2 RJa R3b R4 r5— TT X Y F RK XX-26-1 p-Me-Ph H H H 'Pr och3 H F OH H H XX-26-2 p-Me-Ph H H ch3 'Pr och3 H F OH H H XX-26-3 p-Me-Ph H H CH(CH3)2 'Pr och3 H F OH H H XX-26-4 p-Me-Ph H H CH2CH(CH3)2 'Pr och3 H F OH H H XX-26-5 p-Me-Ph H H CH2Ph 'Pr och3 H F OH H H XX-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr och3 H F OH H H XX-26-7 p-Me-Ph H H CH2CH2SCH3 'Pr och3 H F OH H H XX-26-8 ',"7 p-Me-Ph ♦ H * 'Pr och3 H F OH H H *R2 and R3b joined Together by ((¾¼ to form five-membered ring.

Table XX-27.

Xs R1 R3 R3’ R36 R4 Rs R6 X Y r" Rh XX-27-1 p-F-Ph H H H “ΨΓ OCH3 Η F OH H H XX-27-2 p-F-Ph H H ch3 'Pr och3 H F OH H H XX-27-3 p-F-Ph H H CH(CH3h 'Pr och3 H F OH H H XX-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr och3 H F OH H H XX-27-5 p-F-Ph H H CH2Ph 'Pr och3 H F OH H H XX-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr och3 H F OH H H XX-27-7 p-F-Ph H H CH2CH2SCH3 'Pr och3 H F OH H H XX-27-8 p-F-Ph * H * 'Pr och3 H F OH H H *RZ and R3tJ joined together by to form five-membered ring. 5 Table XX-28. " " 1----- 1 M "'I'V’· _ J ' _ 1 _ X"' _ - _ »1 B "

Xs R1 R2 R" R3b iv R3 R6 X Y R7 R“ XX-28-1 p-Cl-Ph H H H 'Pr OCR, Η F OH H H XX-28-2 p-Cl-Ph H H CH3 'Pr OCH3 H F OH H H XX-28-3 p-Cl-Ph H H CH(CH3)2 'Pr och3 Η F oh H H XX-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr och3 H F oh H H XX-28-5 p-Cl-Ph H H CH2Ph 'Pr och3 H F oh H H XX-28-6 p-Cl-Ph H H CH2-indol-3-yI 'Pr och3 Η F oh H H XX-28-7 p-Cl-Ph H H CH2CH2SCH3 'Pr och3 Η F OH H H XX-28-8 —— p-Cl-Ph »3b ·—r * H * 'Pr och3 Η F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -448- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XX-29.

Xs R‘ Rr' R” R3b R4 "R5 R6 X Y R7 I? XX-29-1 p-Br-Ph H H H "ΎΓ och3 H F OH H H XX-29-2 p-Br-Ph H H CH3 'Pr och3 H F OH H H XX-29-3 p-Br-Ph H H CH(CH3)2 'Pr och3 H F OH H H XX-29-4 p-Br-Ph H H CH2CH(CH3)2 fPr och3 H F OH H H XX-29-5 p-Br-Ph H H CH2Ph 'Pr och3 H F OH H H XX-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr och3 H F OH H H XX-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr och3 H F OH H H XX-29-8 -Τι p-Br-Ph ,3b: : j , * H * 'Pr och3 H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XX-30.

Xs r1- ΤΓ “F "Ρ R4 R5 R6 X Y "P Rb XX-30-J p-I-Ph Η Η Η -ψτ och3 H F OH H H XX-30-2 p-I-Ph Η Η CH3 'Pr och3 H F OH H H XX-30-3 p-I-Ph Η Η CH(CH3)2 'Pr och3 H F OH H H XX-30-4 p-I-Ph Η Η CH2CH(CH3)2 'Pr och3 H F OH H H XX-30-5 p-I-Ph Η Η CH2Ph 'Pr och3 H F OH H H XX-30-6 p-I-Ph Η Η CH2-indol-3-yl 'Pr och3 H F OH H H XX-30-7 p-I-Ph Η Η CH2CH2SCH3 'Pr och3 H F OH H H XX-30-8 —τί; p-I-Ph t— * Η * 'Pr och3 H F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XX-31.

Xs R1 RJ r3. R3b R4 R5 r6 X Υ R7 Ra XX-31-1 ch3 H H Η "Bu och3 H F ΟΗ Η Η XX-31-2 ch3 Η Η ch3 "Bu och3 Η F ΟΗ Η Η XX-31-3 ch3 H H CH(CH3)2 "Bu och3 Η F ΟΗ Η Η XX-31-4 ch3 H Η CH2CH(CH3)2 "Bu och3 Η F ΟΗ Η Η XX-31-S ch3 Η Η CH2Ph "Bu och3 Η F ΟΗ Η Η XX-31-6 ch3 H Η CH2-indol-3-yl "Bu och3 Η F ΟΗ Η Η XX-31-7 ch3 H Η ch2ch2sch3 "Bu och3 Η F ΟΗ Η Η XX-31-8 ch3 ,3b · T • Η ♦ "Bu och3 Η F ΟΗ Η Η *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -449- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XX-32.

Ns TT R3" “P R4 Rs R6 X Y r’ R8 XX-32-1 Et H H H "Bu och3 H F OH H H XX-32-2 Et H H ch3 "Bu och3 H F OH H H XX-32-3 Et H H CH(CH3)2 "Bu och3 H F OH H H XX-32-4 Et H H CH2CH(CH3)2 "Bu och3 H F OH H H XX-32-5 Et H H CH2Ph "Bu och3 H F OH H H XX-32-6 Et H H CH2-indol-3-yl "Bu och3 H F OH H H XX-32-7 Et H H CH2CH2SCH3 "Bu och3 H F OH H H XX-32-8 Et ♦ H * "Bu och3 H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XX-33.

Ns R1 R^ R31 RJb R4 R3 R6 X Y R’ R8 XX-33-1 'Pr H H H "Bu OCH3 H F OH H H XX-33-2 'Pr H H ch3 "Bu och3 H F OH H H XX-33-3 'Pr H H CH(CH3)2 "Bu och3 H F OH H H XX-33-4 Tr H H CH2CH(CH3)2 "Bu och3 H F OH H H XX-33-5 'Pr H H CH2Ph "Bu och3 H F OH H H XX-33-6 'Pr H H CH2-indol-3-yl "Bu och3 H F OH H H XX-33-7 'Pr H H CH2CH2SCH3 "Bu och3 H F OH H H XX-33-8 'Pr * H * "Bu och3 H F OH H H *R2 and R3b joined together by (Cf^fe to form five-membered ring. 5 Table XX-34.

rt" 1 'n™ "4Γ 1 " j i i -- J

Ns R R2 R3a R3b R4 R5 R6 X Y R R“ XX-34-1 Ίν? H H H "Bu OCH3 H F OH H H XX-34-2 'Bu H H CH3 "Bu och3 H F OH H H XX-34-3 'Bu H H CHtCH,), "Bu och3 H F OH H H XX-34-4 'Bu H H CH2CH(CH3)2 "Bu och3 H F OH H H XX-34-5 'Bu H H CH2Ph "Bu och3 H F OH H H XX-34-6 'Bu H H CH2-indol-3-yl "Bu och3 H F OH H H XX-34-7 'Bu H H CH2CH2SCH3 "Bu och3 H F OH H H XX-34-8 'Bu * H ♦ "Bu och3 H F OH H H *R2 and RJb joined together by (CH2)3 to form five-membered ring. Table XX-35. Ns R R2 R3“ R3b R4 R5 R&amp; X Y R7 R8 2983472-1 -450- PCT/US2008/058183 WO 2008/121634 uocKet No. 60137.0034WOU1

Ns R1 R2 -pr R3b R4 "R5 Rfi X Y ΊΓ "r5” XX-35-1 Ph H H H "Bu och3 H F OH H H XX-35-2 Ph H H CHj "Bu och3 H F OH H H XX-35-3 Ph H H CH(CH3)2 "Bu och3 H F OH H H XX-35-4 Ph H H CH2CH(CH3)2 "Bu och3 H F OH H H XX-35-5 Ph H H CH2Ph "Bu och3 H F OH H H XX-35-6 Ph H H CH2-indol-3-yl "Bu och3 H F OH H H XX-35-7 Ph H H CH2CH2SCH3 "Bu och3 H F OH H H XX-35-8 Ph ♦ H * "Bu och3 H F OH H H *R2 and R3b joined together by (CH2)3 to form five-tnembered ring.

Table XX-36.

Na “r1 R2 R35" R4 R5 R6 X Υ ΊΓ R8 XX-36- 1 p-Me- Ph H H H "Bu OCH3 Η F ΟΗ Η Η XX-36- 2 p-Me- Ph H H CH3 "Bu och3 Η F ΟΗ Η Η XX-36- 3 p-Me- Ph H H ΟΗ(ΟΗ3)ϊ "Bu och3 Η F ΟΗ Η Η XX-36- 4 p-Me- Ph H H CH2CH(CH3)2 "Bu och3 Η F ΟΗ Η Η XX-36- 5 p-Me- Ph H H CH2Ph "Bu och3 Η F ΟΗ Η Η XX-36- 6 p-Me- Ph H H CH2-indol-3- yi "Bu och3 Η F ΟΗ Η Η XX-36- 7 p-Me- Ph H H ch2ch2sch3 "Bu och3 Η F ΟΗ Η Η XX-36- 8 p-Me- Ph * H * "Bu och3 Η F ΟΗ Η Η *R2 and Rejoined together by (CH^i to form five-membered ring.

Table ΧΧ-37. Ns R' R2 r3. R3b R* R5 R6 X Y R“ ΧΧ-37-1 p-F-Ph H H H "Bu OCH3 H F OH H H ΧΧ-37-2 p-F-Ph H H CH3 "Bu och3 H F OH H H ΧΧ-37-3 p-F-Ph H H CH(CH3)2 "Bu och3 H F OH H H ΧΧ-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu och3 H F OH H H 2983472-1 -451- PCT/US2008/058183 WO 2008/121634 τ „Λ_ π uocKei No. 60137.0034WOU1

x° R1 r! R3a Rib R4 R5 R6 X Y r’ R8 XX-37-5 p-F-Ph H H CH2Ph "Bu och3 H F OH H H XX-37-6 p-F-Ph H H CH2-indol-3-yl "Bu och3 H F OH H H XX-37-7 p-F-Ph H H CH2CH2SCH3 "Bu och3 H F OH H H XX-37-8 p-F-Ph ♦ H * "Bu och3 H F OH H H *R2 and R311 joined together by (CH2)s to form five-membered ring.

Table XX-38.

X° R R2 rJb Rib R4 R5 R6 X Y R7 R8 XX-38-1 p-Cl-Ph H H H "Bu och3 Η F OH H H XX-38-2 p-Cl-Ph H H CH3 "Bu och3 H F OH H H XX-38-3 p-Cl-Ph H H CH(CH3)2 "Bu och3 H F OH H H XX-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu och3 H F OH H H XX-38-5 p-Cl-Ph H H CH2Ph "Bu och3 H F OH H H XX-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu och3 H F OH H H XX-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu och3 H F OH H H XX-38-8 p-Cl-Ph ♦ H * "Bu och3 H F OH H H *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XX-39.

Xs R R2 R3’ R3b R4 R5- R6 X Y IT ΊΤ XX-39-1 p-Br-Ph H H H "Bu OCH3 Η F OH H H XX-39-2 p-Br-Ph H H ch3 "Bu och3 H F OH H H XX-39-3 p-Br-Ph H H CH(CH3)2 "Bu och3 H F OH H H XX-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu och3 H F OH H H XX-39-5 p-Br-Ph H H CH2Ph "Bu och3 H F OH H H XX-39-6 p-Br-Ph H H CHrindol-3-yI "Bu och3 H F OH H H XX-39-7 p-Br-Ph H H CH2CH2SCH3 "Bu och3 H F OH H H XX-39-8 p-Br-Ph * H * "Bu och3 H F OH H H 5 *R2 and Rejoined together by (ΟΗ2)3 to form five-membered ring.

Table XX-40.

Xa R1 R2 Rj. Rib R4 R5 R* X Y IT Ru XX-40-1 p-I-Ph H H H "Bu OCH3 H F OH H H XX-40-2 p-I-Ph H H CH3 "Bu och3 H F OH H H XX-40-3 p-I-Ph H H CH(CH3)2 "Bu och3 H F OH H H XX-40-4 p-I-Ph H H CHjCHCCH^ "Bu och3 H F OH H H XX-40-5 p-I-Ph H H CH2Ph · "Bu och3 H F OH H H 2983472-1 -452- PCT/US2008/058183 WO 2008/121634 , nrny1u/nTT1 uocKet No. 60137.0034WOU1

Xa R3 Rje "R36 R4 R3 ΊΓ X Y r’ R* XX-40-6 p-I-Ph H H CH2-indol-3-yl "Bu och3 H F OH H H XX-40-7 p-I-Ph H H CH2CH2SCH3 "Bu och3 H F OH H H XX-40-8 -it p-I-Ph T5b ·.* ' * H * "Bu och3 H F OH H H ♦R·4 and Rejoined together by (CH2)3 to form five-membered ring.

Table XX-41.

Xs R1 R3 ~R3r Ί?5 R4 Rs R6 X Y R7 R8 XX-41-1 CH3 Η Η Η Bz och3 H F OH H H XX-41-2 ch3 Η Η ch3 Bz och3 H F OH H H XX-41-3 ch3 Η Η CH(CH3)2 Bz och3 H F OH H H XX-41-4 ch3 Η Η CH2CH(CH3)2 Bz och3 H F OH H H XX-41-5 ch3 Η Η CH2Ph Bz och3 H F OH H H XX-41-6 ch3 Η Η CH2-indol-3-yl Bz och3 H F OH H H XX-41-7 ch3 Η Η CH2CH2SCH3 Bz och3 H F OH H H XX-41-8 ch3 * Η * Bz och3 H F OH H H *R2 and R3b joined together by (0¾¼ to form five-membered ring.

Table XX-42.

Xs R RJ RJ* Rib IT R5 R6 X Υ R7 R8 XX-42-1 Et H H H Bz OCH3 H F ΟΗ Η Η XX-42-2 Et H H CH3 Bz och3 Η F ΟΗ Η Η XX-42-3 Et H H CH(CH3)2 Bz och3 Η F ΟΗ Η Η XX-42-4 Et H H CH2CH(CH3)2 Bz och3 Η F ΟΗ Η Η XX-42-5 Et H H CH2Ph Bz och3 Η F ΟΗ Η Η XX-42-6 Et H H CH2-indol-3-yl Bz och3 Η F ΟΗ Η Η XX-42-7 Et H H CH2CH2SCH3 Bz och3 Η F ΟΗ Η Η XX-42-8 Et * H * Bz och3 Η F ΟΗ Η Η 5 *R'i and R3b joined togetherby (0¾¼ to form five-membered ring.

Table XX-43.

Xs Ίυ ic R3. Rib R4 R3 R6 X Υ R7 R8 ΧΧ-43-1 Ψγ Η Η Η Bz och3 Η F ΟΗ Η Η ΧΧ-43-2 Τγ Η Η ch3 Bz och3 Η F ΟΗ Η Η ΧΧ-43-3 'Pr Η Η CH(CH^ Bz och3 Η F ΟΗ Η Η ΧΧ-43-4 'Pr Η Η CH2CH(CH3)2 Bz och3 Η F ΟΗ Η Η ΧΧ-43-5 'Pr Η Η CH2Ph Bz och3 Η F ΟΗ Η Η ’Ff Μ M GtiiGPfefckyl ig e&amp;h Η £ ΘΗ Η ft 2983472-1 -453 - PCT/US2008/058183 WO 2008/121634 τ ΛΛΟ ,„,ΛΤΤ1

UocKet No. 60137.0034WOUI

XX-43-8 'Pr * H * Bz OCH3 H F OH Η H *R2 and R3b joined together by (0¾^ to form five-membered ring.

Table XX-44.

Xs R1 R2 R3‘ IC R3 R* X Y R7 RH XX-44-1 'Bu H H H Bz och3 H F OH H H XX-44-2 'Bu H H ch3 Bz och3 H F OH H H XX-44-3 'Bu H H CH(CH3)2 Bz och3 H F OH H H XX-44-4 'Bu H H CH2CH(CH3)2 Bz och3 H F OH H H XX-44-5 'Bu H H CH2Ph Bz och3 H F OH H H XX-44-6 'Bu H H CH2-indol-3-yl Bz och3 H F OH H H XX-44-7 'Bu H H CH2CH2SCH3 Bz och3 H F OH H H XX-44-8 'Bu ♦ H * Bz och3 H F OH H H *R2 and R3 b j oined together by (CH2)3 to form five-membered ri ng

Table XX-45.

Xs R R2 r3« RJb R4 R5 R6 X Y R7 R* XX-45-1 Ph H H H Bz OCH3 H F OH H H XX-45-2 Ph H H CH3 Bz och3 H F OH H H XX-45-3 Ph H H CH(CH3)2 Bz och3 H F OH H H XX-45-4 Ph H H CH2CH(CH3)2 Bz och3 H F OH H H XX-45-5 Ph H H CH2Ph Bz och3 H F OH H H XX-45-6 Ph H H CH2-indol-3-yl Bz och3 H F OH H H XX-45-7 Ph H H CH2CH2SCH3 Bz och3 H F OH H H XX-45-8 jt Ph * H 4 Bz och3 H F OH H H

W ' ............ I - W *R and R joined together by (CH2)3 to form five-membered ring. 2983472-1 -454- WO 20θ8Π2}634Να 60137.0034WOU1 PCT/US2008/058183

Table XX-46.

"Tfk D

Ns R2 “ipr R4 Rs R6 X Y R’ Rtt XX-46-1 p-Me-Ph H H H Bz och3 H F OH H H XX-46-2 p-Me-Ph H H ch3 Bz och3 H F OH H H XX-46-3 p-Me-Ph H H CH(CH3)2 Bz och3 H F OH H H XX-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz och3 H F OH H H XX-46-5 p-Me-Ph H H CH2Ph Bz och3 H F OH H H XX-46-6 p-Me-Ph H H CH2-indol-3-yl Bz och3 H F OH H H XX-46-7 p-Me-Ph H H CH2CH2SCH3 Bz och3 H F OH H H XX-46-8 p-Me-Ph * H * Bz och3 H F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XX-47.

Ns R‘ f<7 R35” IF R4 R3 R6 X Υ R ΊΤ XX-47-1 p-F-Ph H H H Bz och3 H F ΟΗ Η Η XX-47-2 p-F-Ph H H ch3 Bz och3 H F ΟΗ Η Η XX-47-3 p-F-Ph H H CH(CH3)2 Bz och3 Η F ΟΗ Η Η XX-47-4 p-F-Ph H H CH2CH(CH3)2 Bz och3 Η F ΟΗ Η Η XX-47-5 p-F-Ph H H CH2Ph Bz och3 Η F ΟΗ Η Η XX-47-6 p-F-Ph H H CH2-indol-3-yl Bz och3 Η F ΟΗ Η Η XX-47-7 p-F-Ph H H CH2CH2SCH3 Bz och3 Η F ΟΗ Η Η XX-47-8 p-F-Ph * H * Bz och3 Η F ΟΗ Η Η *R2 and RJb joined together by (CH2>3 to form five-membered ring. 5 Table XX-48.

I H R AL 1 J J Λ 1 " AU

Ns R1 R2 R3‘ p R^ RJ R6 X Y r" R# ΧΧ-48-1 p-Cl-Ph H H H Bz och3 H F OH H H ΧΧ-48-2 p-Cl-Ph H H ch3 Bz och3 H F OH H H ΧΧ-48-3 p-Cl-Ph H H CH(CH3)2 Bz och3 H F OH H H ΧΧ-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz och3 H F OH H H ΧΧ-48-5 p-Cl-Ph H H CH2Ph Bz och3 H F OH H H ΧΧ-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz och3 H F OH H H ΧΧ-48-7 p-Cl-Ph H H ch2ch2sch3 Bz och3 H F OH H H ΧΧ-48-8 p-Cl-Ph * H * Bz och3 H F OH H H *R2 and Re joined together by (CHib to form five-membered ring. 2983472-1 -455- WO 2008/121634 Νθ. 6oi37,o034WOU1 PCT/US2008/058183

Table XX-49.

Jf2 R1 RJ R3’ R3b R4 R5-^ R6 X Y R7 Rb XX-49-1 p-Br-Ph H H H Bz och3 H F OH H H XX-49-2 p-Br-Ph H H ch3 Bz och3 H F OH H H XX-49-3 p-Br-Ph H H CH(CH3)2 Bz och3 H F OH H H XX-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz och3 H F OH H H XX-49-5 p-Br-Ph H H CH2Ph Bz och3 H F OH H H XX-49-6 p-Br-Ph H H CH2-indol-3-yl Bz och3 H F OH H H XX-49-7 p-Br-Ph H H CH2CH2SCH3 Bz och3 H F OH H H XX-49-8 p-Br-Ph * H * Bz och3 H F OH H H *R2 and R3D joined together by (CH2)3 to form five-membered ring. Table XX-50. Xs R‘ R7 R35” R35 R4 R5 R6 X Y R7 Rtt XX-50-1 p-I-Ph H H H Bz och3 H F OH H H XX-50-2 p-I-Ph H H ch3 Bz och3 H F OH H H XX-50-3 p-I-Ph H H CH(CH3)2 Bz och3 H F OH H H XX-50-4 p-I-Ph H H CH2CH(CH3)2 Bz och3 H F OH H H XX-50-5 p-I-Ph H H CH2Ph Bz och3 H F OH H H XX-50-6 p-I-Ph H H CH2-indol-3-yl Bz och3 H F OH H H XX-50-7 p-I-Ph H H CH2CH2SCH3 Bz och3 H F OH H H XX-50-8 ”ϊτ p-I-Ph ♦ H ♦ Bz och3 H F OH H H *R2 and RJtJ joined together by (ΟΗ2)3 to form five-membered ring.

XXI 2983472-1 -456- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Table XXI-1.

Xs R1 R2 -pr- -pu R4 (? R* X Y XXI-1-1 ch3 H H H ch3 H ch3 F OH XXI-1-2 ch3 H H ch3 ch3 H ch3 F OH XXI-1-3 ch3 H H CH(CH3)2 ch3 H ch3 F OH XXI-1-4 ch3 H H CH2CH(CH3)2 ch3 H ch3 F OH XXI-1-5 ch3 H H CH2Ph ch3 H ch3 F OH XXI-1-6 ch3 H H CH2-indol-3-yl ch3 H ch3 F OH XXI-1-7 ch3 H H CH2CH2SCH3 ch3 H ch3 F OH XXI-1-8 ch3 ♦ H ♦ ch3 H ch3 F OH *R2 and RJb joined together by (CH2):1 to form five-membered ring.

Table ΧΧΪ-2.

Xs R R2 R3· R3b R4 Rs R6 X Y XXI-2-1 Et H H H CH3 H ch3 F OH XXI-2-2 Et H H ch3 ch3 H ch3 F OH XXI-2-3 Et H H CH(CH3)2 ch3 H ch3 F OH XXI-2-4 Et H H CHaCHCCHa)! ch3 H ch3 F OH XXI-2-5 Et H H CH2Ph ch3 H ch3 F OH XXI-2-6 Et H H CH2-indol-3-yl ch3 H ch3 F OH XXI-2-7 Et H H CH2CH2SCH3 ch3 H ch3 F OH XXI-2-8 Et * H * ch3 H ch3 F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXI-3. I . « < ........ J - - , .................

Xs R R2 R3b R3U R4 Rs R6 X Y XXI-3-1 H H H CH3 H CH3 F OH XXI-3-2 Tr H H CH3 ch3 H ch3 F OH XXI-3-3 'Pr H. H CHCCH,), ch3 H ch3 F OH XXI-3-4 'Pr H H CH2CH(CH3)2 ch3 H ch3 F OH XXI-3-5 'Pr H H CH2Ph ch3 H ch3 F OH XXI-3-6 'Pr H H CH2-indol-3-yl ch3 H ch3 F OH XXI-3-7 'Pr H H CH2CH2SCH3 ch3 H ch3 F OH XXI-3-8 'Pr * H * ch3 H ch3 F OH *R2 and Rejoined together by (Clhb to form five-membered ring. 2983472-1 -457- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXI-4.

N° R1 R2 R3a "R35 Rs R6 X Y XXI-4-1 'Bu H H H ch3 H ch3 F OH XXI-4-2 'Bu H H ch3 ch3 H ch3 F OH XXI-4-3 'Bu H H CH(CH3)2 ch3 H ch3 F OH XXI-4-4 'Bu H H CH2CH(CH3)2 ch3 H ch3 F OH XXI-4-5 'Bu H H CH2Ph ch3 H ch3 F OH XXI-4-6 'Bu H H CH2-indol-3-yl ch3 H ch3 F OH XXI-4-7 'Bu H H CH2CH2SCH3 ch3 H ch3 F OH XXI-4-8 'Bu * H * ch3 H ch3 F OH ♦R* and R3b joined together by (0-12)3 to form five-membered ring.

Table XXI-5.

Ns R fC R3a R3b R4 Rs R6 X Y XXI-5-1 Ph H H H ch3 H ch3 F OH XXI-5-2 Ph H H CH3 ch3 H ch3 F OH XXI-5-3 Ph H H CH(CH3)2 ch3 Η ch3 F OH XXI-5-4 Ph H H CH2CH(CH3)2 ch3 H ch3 F OH ΧΧΪ-5-5 Ph H H CH2Ph gh3 H ch3 F OH XXI-5-6 Ph H H CH2-indol-3-yl ch3 H ch3 F OH XXI-5-7 Ph H H CH2CH2SCH3 ch3 H ch3 F OH XXI-5-8 Ph * H ♦ ch3 H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XXI-6.

I - — 11 MJ» ! """' -- J

Na R’ RJ R3e "r35 ΊΓ" R5 R6 X Y XXI-6-1 p-Me-Ph H H H ch3 H ch3 F OH XXI-6-2 p-Me-Ph H H ch3 ch3 H ch3 F OH XXI-6-3 p-Me-Ph H H CHCCH^ ch3 H ch3 F OH XXI-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 H ch3 F OH XXI-6-5 p-Me-Ph H H CH2Ph ch3 H ch3 F OH XXI-6-6 p-Me-Ph H H CHrindol-3-yI ch3 H ch3 F OH XXI-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 H ch3 F OH XXI-6-8 p-Me-Ph * H ♦ CH, H ch3 F OH *R2 and Rjb joined together by (CH2)3 to form five-membered ring. 2983472-1 -458- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Table XXI-7.

Xfi R1 r! "r37" "R36- R4 RJ IV' X Y XXI-7-1 p-F-Ph H H H ch3 H ch3 F OH XXI-7-2 p-F-Ph H H ch3 ch3 H ch3 F OH XX1-7-3 p-F-Ph H H ch(ch3)2 ch3 H ch3 F OH XXI-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 H ch3 F OH XXI-7-6 p-F-Ph H H CH2Ph ch3 H ch3 F OH XXI-7-7 p-F-Ph H H CH2-indol-3-yl ch3 H ch3 F OH XX1-7-8 p-F-Ph H H CH2CH2SCH3 ch3 H ch3 F OH XXI-7-20 *nr;Tr p-F-Ph .3b: · * H * ch3 H ch3 F OH *R2 and Rejoined together by (CH2)3t0 f°rrn five-membered ring.

Table XXI-8.

Xs R1 R3 R3‘ "r35 R4 rs R6 X Y XXI-8-1 p-Cl-Ph H H H ch3 H ch3 F OH XXI-8-2 p-Cl-Ph H H ch3 ch3 H ch3 F OH XXI-8-3 p-Cl-Ph H H CH(CH3)2 ch3 H ch3 F OH XXI-8-4 p-Cl-Ph H H CHiCHiCH^ ch3 H ch3 F OH XXI-8-5 p-Cl-Ph H H CH2Ph ch3 H ch3 F OH XXI-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 H ch3 F OH XXI-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 H ch3 F OH XXI-8-8 p-Ct-Ph * H ♦ ch3 H ch3 F OH *R2 and RJb joined together by (CHabt0 form five-membered ring. 5 Table XXI-9. ------ ,, , -—-.,-

Xs R1 R2 R3a R3b R4 R5 R6 X Y XXI-9-1 p-Br-Ph H H H ch3 H ch3 F OH XXI-9-2 p-Br-Ph H H CH3 ch3 H ch3 F OH XXI-9-3 p-Br-Ph H H CHCCH,), ch3 H ch3 F OH XXI-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 H ch3 F OH XXI-9-6 p-Br-Ph H H CH2Ph ch3 Η ch3 F OH XXI-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 H ch3 F OH XXI-9-8 p-Br-Ph H H CH2CH2SCH3 ch3 H ch3 F OH XXI-9-20 “7772-777 p-Br-Ph 3b * ; * H * ch3 Η ch3 F OH ♦R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -459- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXI-10.

Ns ΊΓ- R2 ΊΡ“ R3b R4 R5 R6 X Y XXI-10-1 p-I-Ph H H H ch3 H ch3 F OH XXI-10-2 p-l-Ph H H CHj ch3 H ch3 F OH XX1-10-3 p-I-Ph H H CH(CH3)2 ch3 H ch3 F OH ΧΧΙ-10-4 p-I-Ph H H CH2CH(CH3)2 ch3 H ch3 F OH XXI-10-5 p-I-Ph H H CH2Ph ch3 H ch3 F OH XXI-10-6 p-I-Ph H H CH2-indol-3-yl ch3 H ch3 F OH XXI-10-7 p-I-Ph H H CH2CH2SCH3 ch3 H ch3 F OH XXI-10-8 p-I-Ph * H * ch3 H ch3 F OH *R7 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXI-11.

X2 R1 R2 R3a R3b R4 R5 R6 X Y XXI-11-1 ch3 H H H Et H CH3 F OH XX I-11-2 ch3 H H CH3 Et H ch3 F OH XXI-11-3 ch3 H H CH(CH3)i Et H ch3 F OH XXI-11-4 ch3 H H CH2CH(CH3)2 Et H ch3 F OH ΧΧΙ-Π-5 ch3 H H CH2Ph Et H ch3 F OH XXI-11-6 ch3 H H CH2-indol-3-yl Et H ch3 F OH XXI-11-7 ch3 H H CH2CH2SCH3 Et H ch3 F OH XXI-11-8 ch3 ♦ H * Et H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XXI-12.

— < J· ! J Λ "I

Ns R ΊΓ R3. R3b R4 R3 R6 X Y XXI-12-1 Et H H H Et H ch3 F OH XXI-12-2 Et H H CH3 Et H ch3 F OH XXI-12-3 Et H H CH(CH3)2 Et H ch3 F OH XXI-12-4 Et H H CH2CH(CH3)2 Et H ch3 F OH XXI-12-5 Et H H CH2Ph Et H ch3 F OH XXI-12-6 Et H H CH2-indol-3-yl Et H ch3 F OH XXI-12-7 Et H H CH2CH2SCH3 Et H ch3 F OH XXI-12-8 Et * H * Et H ch3 F OH *R2 and Rejoined together by (CHbb to form five-membered ring. 2983472-1 -460- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXI-13.

Ns R1 R2 R3" R3b tr RJ R6 X Y XXI-13-1 'Pr H H H Et H ch3 F OH XXI-13-2 'Pr H H ch3 Et H ch3 F OH XXI-13-3 ‘Pr H H CH(CH3)2 Et H ch3 F OH XXI-13-4 ‘Pr H H CH2CH(CH3)2 Et H ch3 F OH XXI-13-5 'Pr H H CH2Ph Et H ch3 F OH XXI-13-6 'Pr H H CH2-indol-3-yI Et H ch3 F OH XXI-13-7 'Pr H H CH2CH2SCH3 Et H ch3 F OH XXI-13-8 'Pr * H * Et H ch3 F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XX1-14.

Xa R2 RJa R3b R4 Rs Rb X Y XXI-14-1 *Bu H H H Et H CH3 F OH XXI-14-2 'Bu H H CH3 Et H ch3 F OH XXI-14-3 'Bu H H CH(CH3)2 Et H ch3 F OH XXI-14-4 'Bu H H CH2CH(CH3)2 Et H ch3 F OH XXI-14-5 'Bu H H CH2Ph Et H ch3 F OH XXI-14-6 'Bu H H CH2-indol-3-yl Et H ch3 F OH XXI-14-7 'Bu H H CH2CH2SCH3 Et H ch3 F OH ΧΧΪ-14-8 *Bu * H * Et H ch3 F OH *R2 and RJD joine· d toge ither t iy (CHili to form five-membered rii ig. 5 TableXXI-15.__

Xa R’ R2 R3’ R3b R4 R5 R6 X Y XXI-15-1 Ph Η H H Et H CH3 F OH XX1-15-2 Ph H H ch3 Et H ch3 F OH XXI-15-3 Ph H H CHiCH^ Et H ch3 F OH XXI-15-4 Ph H H CH2CH(CH3)2 Et H ch3 F OH XXI-15-5 Ph H H CH2Ph Et Η ch3 F OH XXI-15-6 Ph H H CH2-indoI-3-yl Et H ch3 F OH XXI-15-7 Ph H H CH2CH2SCH3 Et H ch3 F OH XXI-15-8 Ph * H * Et H ch3 F OH ♦R2 and RJb joined together by (CHife to form five-membered ring. 2983472-1 -461- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

TableXXI-16.

X° R1 R2 RSa RJb R4 Rs R6 X Y XXI-16-1 p-Me-Ph H H H Et H ch3 F OH XXI-16-2 p-Me-Ph H H ch3 Et H ch3 F OH XXI-16-3 p-Me-Ph H H CH(CH3)2 Et H ch3 F OH XXI-16-4 p-Me-Ph H H CH2CH(CH3)2 Et H ch3 F OH XXI-16-5 p-Me-Ph H H CH2Ph Et H ch3 F OH XXI-16-6 p-Me-Ph H H CHrindol-3-yl Et H ch3 F OH XXI-16-7 p-Me-Ph H H CH2CH2SCH3 Et H ch3 F OH XXI-16-8 p-Me-Ph * H * Et H ch3 F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXI-17.

Xa R1 R2 R3“ R4 R5 R6 X Y XXI-17-1 p-F-Ph H H H Et H ch3 F OH XXI-17-2 p-F-Ph H H ch3 Et H ch3 F OH XXI-17-3 p-F-Ph H H CH(CH3)2 Et H ch3 F OH XXI-17-4 p-F-Ph H H CH2CH(CH3)2 Et H ch3 F OH XXI-17-5 p-F-Ph H H CH2Ph Et H ch3 F OH XXI-17-6 p-F-Ph H H CH2-indol-3-yl Et H ch3 F OH XXI-17-7 p-F-Ph H H CH2CH2SCH3 Et H ch3 F OH XXI-17-8 p-F-Ph * H * Et H ch3 F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 TableXXI-18. »- * 4. J|L J f f

Xa R' R2 R3· R3b R4 R^ R* X Y XXI-18-1 p-Cl-Ph H H H Et H CH3 F OH XXI-18-2 p-Cl-Ph H H CH3 Et H ch3 F OH XXI-18-3 p-Cl-Ph H H CHCCH^ Et H ch3 F OH XXI-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H ch3 F OH XXI-18-5 p-Cl-Ph H H CH2Ph Et H ch3 F OH XXI-18-6 p-Cl-Ph H H CH2-indol-3-yl Et H ch3 F OH XXI-18-7 p-Cl-Ph H H CH2CH2SCH3 Et H ch3 F OH XXI-18-8 p-CI-Ph * H ♦ Et H ch3 F OH *R and R joined together by (CH2)3 to form five-membered ring. 2983472-1 -462- WO 2008/121634

Docket No. 60137.0034WOUI PCT/US2008/058183

Table XXI-19.

x° T- R2 r’· "r56 R4 R4 X Y XXI-19-1 p-Br-Ph H H H Et H ch3 F OH XX1-19-2 p-Br-Ph H H ch3 Et H ch3 F OH XXI-19-3 p-Br-Ph H H CH(CH3)2 Et H ch3 F OH XXI-19-4 p-Br-Ph H H CH2CH(CH3)2 Et H ch3 F OH XXI-19-5 p-Br-Ph H H CH2Ph Et H ch3 F OH XXI-19-6 p-Br-Ph H H CH2-indol-3-yl Et H ch3 F OH XXI-19-7 p-Br-Ph H H CH2CH2SCH3 Et H ch3 F OH XXI-19-8 _ J p p-Br-Ph .3b i · □ * H * Et H ch3 F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXI-20.

Xs R1 R2 R3 R* ΊΓ Rs R4 X Y XXI-20-I p-I-Ph H H H Et H ch3 F OH XXI-20-2 p-I-Ph H H ch3 Et H ch3 F OH XXI-20-3 p-I-Ph H H CH(CH3)2 Et H ch3 F OH XXI-20-4 p-I-Ph H H CH2CH(CH3)2 Et H CHj F OH XXI-20-5 p-I-Ph H H CH2Ph Et H ch3 F OH XXI-20-6 p-I-Ph H H CH2-indol-3-yl Et H ch3 F OH XXI-20-7 p-I-Ph H H CH2CH2SCH3 Et H ch3 F OH XXI-20-8 .v; p-I-Ph 3b . j * H * Et H ch3 F OH *R2 and R3b joined together by (Cfcbb to form five-membered ring.

X2 R R2 r3. R3b R4 R5 R6 X Y XXI-21-1 CH3 Η H H Pr H ch3 F OH XX1-21-2 ch3 H H CH3 Pr H ch3 F OH XXI-21-3 ch3 Η H CH(CH3)2 Pr H ch3 F OH XXI-21-4 ch3 H H CH2CH(CH3)2 'Pr H ch3 F OH XXI-21-5 ch3 H H CH2Ph Pr H ch3 F OH XXI-21-6 ch3 H H CH2-indol-3-yl 'Pr H ch3 F OH XXI-21-7 ch3 H H CH2CH2SCH3 Pr H ch3 F OH XXI-21-8 _ J η ch3 3b · · * H * Pr H ch3 F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -463- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXI-22.

Ns R1 R2 “r37 -R35 R4 R3 R6 X Y XXI-22-1 Et H H H JPr H ch3 F OH XXI-22-2 Et H H ch3 'Pr H ch3 F OH XXI-22-3 Et H H CHCCHs^ 'Pr H ch3 F OH XXI-22-4 Et H H 'Pr H ch3 F OH XXI-22-5 Et H H CH2Ph 'Pr H ch3 F OH XXI-22-6 Et H H CH2-indol-3-yl 'Pr H ch3 F OH XXI-22-7 Et H H CH2CH2SCH3 'Pr H ch3 F OH XXI-22-8 Et * H * 'Pr H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXI-23.

Ns R1 R2 -jpr -p; R4 R3 R6 X Y XX1-23-1 Jpr H H H ;Pr H CH3 F OH XXI-2 3-2 'Pr H H CH3 'Pr H ch3 F OH XXI-23-3 'Pr H .H CH(CH3)j 'Pr H ch3 F OH XXI-23-4 'Pr H H CH2CH(CH3)2 'Pr H ch3 F OH XXI-23-5 'Pr H H CH2Ph 'Pr H ch3 F OH XXI-23-6 'Pr H H CH2-indol-3-yl 'Pr H ch3 F OH XXI-23-7 'Pr H H CH2CH2SCH3 'Pr H ch3 F OH XXI-23-8 fpr * H * 'Pr H ch3 F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXI-24. I IM - «. J — ,

Ns R R2 r3. RJb R4 R3 R6 X Y XXI-24-1 -’βϊΓ H H H ’W H CH3 F OH XXI-24-2 'Bu H H CH3 'Pr H ch3 F OH XXI-24-3 'Bu H H CH(CH3)2 'Pr H ch3 F OH XXI-24-4 'Bu H H CHiCHCCH^ 'Pr H ch3 F OH XXI-24-5 'Bu H H CH2Ph 'Pr H ch3 F OH XXI-24-6 'Bu H H CH2-indol-3-yl 'Pr H ch3 F OH XXI-24-7 'Bu H H CH2CH2SCH3 'Pr H ch3 F OH XXI-24-8 'Bu * H * 'Pr H ch3 F OH *R2 and RJ&amp; joined together by (Cflbfe to form five-membered ring. 2983472-1 -464- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXI-25.

Xs r1- Rjr - - “r R1 R6 X γ XXI-25-1 Ph H H H. 'Pr H ch3 F OH XXI-25-2 Ph H H ch3 'Pr H ch3 F OH XXI-25-3 Ph H H CH(CH3)2 'Pr H ch3 F OH XXI-25-4 Ph H H CH2CH(CH3)2 'Pr H ch3 F OH XXI-25-5 Ph H H CH2Ph 'Pr H ch3 F OH XXI-25-6 Ph H H CH2-indoI-3-yl 'Pr H ch3 F OH XXI-25-7 Ph H H CH2CH2SCH3 'Pr H ch3 F OH XXI-25-8 Ph * H * 'Pr H ch3 F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXI-26.

Xs Rl ΊΓ "r35" R3b R4 R6 X Y XXI-26-1 p-Me-Ph H H H 'Pr H ch3 F OH XXI-26-2 p-Me-Ph H H CH3 'Pr H ch3 F OH XXI-26-3 p-Me-Ph H H CH(CH,)2 'Pr H ch3 F OH XXI-26-4 p-Me-Ph H H CH2CH(CH3)2 'Pr H ch3 F OH XXI-26-5 p-Me-Ph H H CH2Ph 'Pr H ch3 F OH XXI-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr H ch3 F OH XXI-26-7 p-Me-Ph H H CH2CH2SCH3 'Pr H ch3 F OH XXI-26-8 p-Me-Ph , * H * 'Pr H ch3 F OH ♦R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXI-27. " i1 1 " r n- '1 i Ί 11

Xs R1 Ra r3. R3b R4 R5 R4 X Y XXI-27-1 p-F-Ph H H H TpT H CH3 F OH XXI-27-2 p-F-Ph H H CH3 'Pr H ch3 F OH XXI-27-3 p-F-Ph H H CH(CH3)2 'Pr H ch3 F OH XXI-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr H ch3 F OH XXI-27-5 p-F-Ph H H CH2Ph 'Pr H ch3 F OH XXI-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr H ch3 F OH XXI-27-7 p-F-Ph H H CH2CH2SCH3 'Pr H ch3 F OH XXI-27-8 p-F-Ph —T * H * 'Pr H ch3 F OH *R2 and RJb joined together by (CHjh to form five-membered ring. 2983472-1 -465- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXI-28.

Ns R1 R3 r35" "r3* R4 R1 IF- X Y XXI-28-1 p-CI-Ph H H H Tr H ch3 F OH XXI-28-2 p-Cl-Ph H H ch3 'Pr H ch3 F OH XXI-28-3 p-CI-Ph H H CH(CH3)2 'Pr H ch3 F OH XXI-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr H CHa F OH XXI-28-5 p-CI-Ph H H CH2Ph 'Pr H ch3 F OH XXI-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr H ch3 F OH XXI-28-7 p-Cl-Ph H H CH2CH2SCH3 'Pr H ch3 F OH XXI-28-8 p-Cl-Ph * H * 'Pr H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXI-29.

Xs R1 R3 R3“ R35 I? r! R6 X Y XXI-29-1 p-Br-Ph H H H '“'pi7 H ch3 F OH XXI-29-2 p-Br-Ph H H CH3 'Pr H CHa F OH XXI-29-3 p-Br-Ph H H CH(CH3)2 'Pr H ch3 F OH XXI-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr H ch3 F OH XX1-29-5 p-Br-Ph H H CH2Ph 'Pr H ch3 F OH XXI-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr H ch3 F OH XXI-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr H ch3 F OH XXI-29-8 p-Br-Ph * H * 'Pr H ch3 F OH *R2 and RJb joined together by (Cthb to form five-membered ring. 5 Table XXI-30.

IW... - J

Xs R1 R3 r3. R3b R4 ΊΓ R6 X Y XXI-30-1 p-I-Ph H H H Ψγ H ch3 F OH XXI-30-2 p-l-Ph H H ch3 fpr H ch3 F OH XXI-30-3 p-l-Ph H H CH(CH3)2 'Pr H ch3 F OH XXI-30-4 p-I-Ph H H CH2CH(CH3)2 /ρΓ H ch3 F OH XXI-30-5 p-I-Ph H H CH2Ph Tr H ch3 F OH XXI-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr H ch3 F OH XX1-30-7 p-I-Ph H H CH2CH2SCH3 'Pr H ch3 F OH XXI-30-8 2-------. p-I-Ph ;3b · · J * H * /pr H ch3 F OH *R2 and Rejoined together by (CH^ to form five-membered ring. 2983472-1 -466- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Table XX1-31.

Ns Έ” R3 R3* "'P R4 Rs R6 X Y XXI-31-1 ch3 H H H "Bu H ch3 F OH XXI-31-2 ch3 H H ch3 "Bu H ch3 F OH XXI-31-3 ch3 H H CH(CH3)2 "Bu H ch3 F OH XXI-31-4 ch3 H II CH2CH(CH3)2 "Bu H ch3 F OH XXI-31-5 ch3 H H CH2Ph "Bu H ch3 F OH XXI-31-6 ch3 H H CH2-indol-3-yl "Bu H ch3 F OH XXI-31-7 ch3 H H CH2CH2SCH3 "Bu H ch3 F OH XXI-31-8 ,Τϊ ch3 * H * "Bu H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXI-32.

Ns R1 R3 r3. R3b R4 RJ R6 X Y XXI-32-1 Et H H H "Bu H CH3 F OH XXI-32-2 Et H H ch3 "Bu H ch3 F OH XXI-32-3 Et H H 0Η(0Η3)ί "Bu H ch3 F OH XXI-32-4 Et H H CH2CH(CH3)2 "Bu H ch3 F OH XXI-32-5 Et H H CH2Ph "Bu H ch3 F OH XX1-32-6 Et H H CH2-indol-3-yl "Bu H ch3 F OH XXI-32-7 Et H H CH2CH2SCH3 "Bu H ch3 F OH XXI-32-8 Et * H * "Bu H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XXI-33. — I — 1 ' t R 4L ' J ' * '2 1 ' - _ _ 11 "

Ns R R3 R3‘ R3b R4 Rs R’ X Y XXI-33-1 'Pr H H H "Bu H ch3 F OH XXI-33-2 'Pr H H CH3 "Bu H ch3 F OH XXI-33-3 /Pr H H CHiCH,), "Bu H ch3 F OH XXI-33-4 'Pr H H CH2CH(CH3)2 "Bu H ch3 F OH XXI-33-5 'Pr H H CH2Ph "Bu H ch3 F OH XXI-33-6 'Pr H H CH2-indol-3-yi "Bu H ch3 F OH XXI-33-7 'Pr H H CH2CH2SCH3 "Bu H ch3 F OH XXI-33-8 'Pr * H * "Bu H ch3 F OH ♦R2 and R3b joined together by (0¾¼ to form five-membered ring. 2983472-1 -467- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXI-34.

Ns R1 R2 Ί?Γ R5" R6 X Y XXI-34-1 'Bu H H H "Bu H ch3 F OH XXI-34-2 'Bu H H ch3 "Bu H ch3 F OH XXI-34-3 'Bu H H CH(CH3)2 "Bu H ch3 F OH XXI-34-4 'Bu H H CH2CH(CH3)2 "Bu H ch3 F OH XXI-34-5 'Bu H H CH2Ph. "Bu H ch3 F OH XXI-34-6 *Bu H H CH2-indol-3-yl "Bu H ch3 F OH XXI-34-7 'Bu H H CH2CH2SCH3 "Bu H ch3 F OH XXI-34-8 'Bu * H ♦ "Bu H ch3 F OH *R2 and R3b joined together by (Cl-^bt0 fQrm five-membered ring.

Table XXI-35.

Ns R R2 RJl R3b R7 Rs R6 X Y XXI-35-1 Ph H H H "Bu H ch3 F OH XXI-35-2 Ph H H CH3 "Bu H ch3 F OH XXI-35-3 Ph H H CH(CH3)2 "Bu H ch3 F OH XXI-35-4 Ph H H CH2CH(CH3)2 "Bu H ch3 F OH XXI-35-5 Ph H H CH2Ph "Bu H ch3 F OH XXI-35-6 Ph H H CH2-indol-3-yl "Bu H ch3 F OH XXI-35-7 Ph H H CH2CH2SCH3 "Bu H ch3 F OH XXI-35-8 *«2 . Ph 3F777 * H * "Bu H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XXI-36. ....... i « hl j ""'.τι i ...../..-1

Ns R‘ R2 R3i R3b Ίτ IV R* X Y ΧΧΪ-36-1 p-Me-Ph H H H "Bu H ch3 F OH XXI-36-2 p-Me-Ph H H ch3 "Bu H ch3 F OH XXI-36-3 p-Me-Ph H H ΟΗ(ΟΗ3)5 "Bu H ch3 F OH XXI-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu Η ch3 F OH XXI-36-5 p-Me-Ph H H CH2Ph "Bu Η ch3 F OH XXI-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu Η ch3 F OH XXI-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu Η ch3 F OH XXI-36-8 *n'2 j τλ p-Me-Ph 3F771—777 * H * "Bu Η ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -468- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXI-37.

Ns R3 R^ R3b R4 R* X Y XXI-37-1 p-F-Ph H H H "Bu H ch3 F OH XXI-37-2 p-F-Ph H H ch3 "Bu H ch3 F OH XXI-37-3 p-F-Ph H H CH(CH3)2 "Bu H ch3 F OH XXI-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu H ch3 F OH XXI-37-5 p-F-Ph H H CHjPh "Bu H ch3 F OH XX1-37-6 p-F-Ph H H CH2-indol-3-yl "Bu H ch3 F OH XXI-37-7 p-F-Ph H H ch2ch2sch3 "Bu H ch3 F OH XXI-37-8 p-F-Ph ♦ H * "Bu H ch3 F OH *RZ and Rejoined together by (CH2)3 to form five-membered ring.

Table XXI-38. D1

Ns R1 tc RJ“ R3b R4 R5 R6 X Y XXI-38-1 p-CI-Ph H H H "Bu H CH3 F OH XXI-38-2 p-Cl-Ph H H ch3 "Bu H ch3 F OH XXI-38-3 p-Cl-Ph H H CH(CH3)2 "Bu H ch3 F OH XXI-38-4 p-Ci-Ph H H CH2CH(CH3)2 "Bu H ch3 F OH XXI-38-5 p-Cl-Ph H H CH2Ph "Bu H ch3 F OH XXI-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu H ch3 F OH XXI-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu H ch3 F OH XXI-38-8 p-Cl-Ph * H * "Bu H ch3 F OH *RZ and RJb joined together by (CH2)3 to form five-membered ring.

Ns R1 R3 R3" R3b R4 r! ΊΤ" X Y XXI-39-1 p-Br-Ph H Η Η "Bu H ch3 F OH XXI-39-2 p-Br-Ph H Η ch3 "Bu H ch3 F OH XXI-39-3 p-Br-Ph Η Η chcch^ "Bu Η ch3 F OH XXI-39-4 p-Br-Ph Η Η CH2CH(CH3)2 "Bu H ch3 F OH XXI-39-5 p-Br-Ph Η Η CH2Ph "Bu Η ch3 F OH XXI-39-6 p-Br-Ph Η Η CH2-indol-3-yl "Bu Η ch3 F OH XXI-39-7 p-Br-Ph Η Η ch2ch2sch3 "Bu Η ch3 F OH XXI-39-8 p-Br-Ph 3b ·„ j * ♦ Η * "Bu Η ch3 F OH *R2 and R30 joined together by (CH2)3 to form five-membered ring. 2983472-i -469- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXI-40.

Ha R‘ 'I?’ R3“ Ί?5 R4 Rs R6 X Y XXI-40-1 p-I-Ph H H H "Bu H ch3 F OH ΧΧΪ-40-2 p-I-Ph H H ch3 "Bu H ch3 F OH XXI-40-3 p-I-Ph H H CH(CH3)2 "Bu H ch3 F OH XXI-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu H ch3 F OH XXI-40-5 p-I-Ph H H CH2Ph "Bu H ch3 F OH XXI-40-6 p-I-Ph H H CH2-indol-3-yl "Bu H ch3 F OH XXI-40-7 p-I-Ph H H CH2CH2SCH3 "Bu H ch3 F OH XXI-40-8 p-I-Ph * H * "Bu H ch3 F OH *R2 and RJb joined together by (CKfek to form five-membered ring.

Table XXI-41.

Ha R1 r2 R3‘ R3b R4 R3 R6 X Y XXI-41-1 ch3 Η H H Bz H CH3 F OH XXI-41-2 ch3 H H ch3 Bz H ch3 F OH XXI-41-3 ch3 H H CH(CH3)2 Bz H ch3 F OH XXI-41-4 ch3 H H CH2CH(CH3)2 Bz H ch3 F OH XXI-41-5 ch3 H H CH2Ph Bz H ch3 F OH XXI-41-6 ch3 H H CH2-indol-3-y] Bz H ch3 F OH XXI-41-7 ch3 H H CH2CH2SCH3 Bz H ch3 F OH XXI-41-8 ch3 ♦ H * Bz H ch3 F OH *R2 and R3” joined together by (CH2)3 to form five-membered ring. 5 Table XXI-42. 1 | R ^L"· ‘"’Hl. J ..11

Ha R R2 R3* R3b R4 ΊΓ R* X Y XXI-42-1 Et Η Η Η Bz H CH3 F OH XXI-42-2 Et Η Η ch3 Bz H ch3 F OH XXI-42-3 Et Η Η CH(CHj)j Bz H ch3 F OH XXI-42-4 Et Η Η ΟΗ2ΟΗ(ΟΗ3)ϊ Bz H ch3 F OH XXI-42-5 Et Η Η CH2Ph Bz H ch3 F OH XXI-42-6 Et Η Η CH2-indol-3-yl Bz H ch3 F OH XXI-42-7 Et Η Η CH2CH2SCH3 Bz H ch3 F OH XXI-42-8 Et * Η * Bz H ch3 F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -470- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXI-43.

Xs T” R3 ηρτ- R» R4 R6 X Y XXI-43-1 'Pr H H H Bz H ch3 F OH XXI-43-2 'Pr H H ch3 Bz H ch3 F OH XXI-43-3 ipr H H CH(CH3)2 Bz H ch3 F OH XXI-43-4 'Pr H H CH2CH(CH,)j Bz H ch3 F OH XXI-43-5 'Pr H H CH2Ph Bz H ch3 F O$I XXI-43-6 'Pr H H CHj-indol-3-yl Bz H ch3 F OH XXI-43-7 'Pr H H CH2CH2SCH3 Bz H ch3 F OH XXI-43-8 'Pr ♦ H * Bz H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXI-44.

Xs R1 RJ‘ R31> R4 R5 R6 X Y XXI-44-1 'Bu H H H Bz H CH3 F OH XXI-44-2 'Bu H H CH3 Bz H ch3 F OH XXI-44-3 'Bu H H CH(CH3)2 Bz H ch3 F OH XXI-44-4 'Bu H H CH2CH(CH3)2 Bz H ch3 F OH XXI-44-5 H H CH2Pb Bz H ch3 F OH XXI-44-6 'Bu H H CH2-indol-3-yl Bz H ch3 F OH XXI-44-7 'Bu H H CH2CH2SCH3 Bz H ch3 F OH XXI-44-8 'Bu • H ♦ Bz H ch3 F OH 10 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXI-45.

Xs r R2 R3b R4^ R3 R6 X Y XXI-45-1 Ph Η H H Bz H ch3 F OH XXI-45-2 Ph H H CH3 Bz H ch3 F OH XXI-45-3 Ph H H ΟΗ(ΟΗ3)2 Bz H ch3 F OH XXI-45-4 Ph H H ΟΗ2ΟΗ(ΟΗ3)2 Bz H ch3 F OH XXI-45-5 Ph H H CH2Ph Bz H ch3 F OH XXI-45-6 Ph H H CH2-indol-3-yl Bz H ch3 F OH XXI-45-7 Ph H H CH2CH2SCH3 Bz H ch3 F OH XXI-45-8 "7712 7777 Ph 36777 * H * Bz H ch3 F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -471 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXI-46.

Ns R1 r'j R3a “r^ R4 IF “R^ X Y XXI-46-1 p-Me-Ph H H H Bz H ch3 F OH XXI-46-2 p-Me-Ph H H ch3 Bz H ch3 F OH XXI-46-3 p-Me-Ph H H a-KCHak Bz H CH3 F OH XXI-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz H ch3 F OH XXI-46-5 p-Me-Ph H H CH2Ph Bz H ch3 F OH XXI-46-6 p-Me-Ph H H CH2-indol-3-yl Bz H ch3 F OH XXI-46-7 p-Me-Ph H H CH2CH2SCH3 Bz H ch3 F OH XXI-46-8 p-Me-Ph * H ♦ Bz H ch3 F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table ΧΧΪ-47.

Ns Rl R2 RJe R3b R4 Rs R6 X Y XXI-47-1 p-F-Ph H H H Bz H CH3 F OH XXI-47-2 p-F-Ph H H ch3 Bz H ch3 F OH XXI-47-3 p-F-Ph H H CH(CH3)2 Bz H ch3 F OH XXI-47-4 p-F-Ph H H CH2CH(CH3)2 Bz H ch3 F OH XXI-47-5 p-F-Ph H H CH2Ph Bz H ch3 F OH XXI-47-6 p-F-Ph H H CH2-indol-3-yl Bz H CH3 F OH XXI-47-7 p-F-Ph H H CH2CH2SCH3 Bz H ch3 F OH XXI-47-8 p-F-Ph 3Β-ΓΊ-r * H * Bz H CH3 F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Ns R1 R2 jpr "R35 R4 ΊΓ R6 X Y XXI-48-1 p-Cl-Ph Η H H Bz H CH3 F OH XX1-48-2 p-CI-Ph H H CH3 Bz H CH3 F OH XXI-48-3 p-Cl-Ph H H CH(CH3)2 Bz H CH3 F OH XXI-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H CHa F OH XXI-48-5 p-Cl-Ph H H CH2Ph Bz H CH3 F OH XXI-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz H CHa F OH XXI-48-7 p-Cl-Ph H H CH2CH2SCH3 Bz H CH3 F OH XXI-48-8 p-Cl-Ph ΓΤ5Τ-·—77 * H * Bz H CH3 F OH *R4 and RJ0 joined together by (CH2)3 to form five-membered ring. 2983472-1 -472- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXI-49.

Ns R’ R2 r3. R3b R4 R5 R6 X Y XXI-49-1 p-Br-Ph H H H Bz H ch3 F OH XXI-49-2 p-Br-Ph H H ch3 Bz H ch3 F OH XXI-49-3 p-Br-Ph H H CH(CH3)2 Bz H ch3 F OH XXI-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz H ch3 F OH XXI-49-5 p-Br-Ph H H CH2Ph Bz H ch3 F OH XXI-49-6 p-Br-Ph H H CH2-indol-3-yl Bz H ch3 F OH XXI-49-7 p-Br-Ph H H ch2ch2sch3 Bz H ch3 F OH XXI-49-8 p-Br-Ph * H * Bz H ch3 F OH *R2 and R2b joined together by (CH2)3 to form five-membered ring.

Table XXI-50.

Ns R' R2 RJl R3b R4 Rs R6 X Y XXI-50-1 p-I-Ph H H H Bz H CH3 F OH XXI-50-2 p-I-Ph H H ch3 Bz H ch3 F OH XXI-50-3 p-l-Ph H H CH(CH3)2 Bz H ch3 F OH XXI-50-4 p-I-Ph H H CH2CH(CH3)2 Bz H ch3 F OH XX1-50-5 p-I-Ph H H CH2Ph Bz H ch3 F OH XXI-50-6 p-I-Ph H H CH2-indol-3-yl Bz H ch3 F OH XXI-50-7 p-I-Ph H H ch2ch2sch3 Bz H ch3 F OH XXI-50-8 Λ'τλ'2 -η p-I-Ph .JO ; ; j * H ♦ Bz H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

XXII 2983472-1 -473 - WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXII-1.

Xa R1 R2 R3t R4 R* Rfc X Y XXII-M ch3 H H H ch3 H F H OH XXII-1-2 ch3 H H ch3 ch3 H F H OH XXH-1-3 ch3 H H CH(CH3)2 ch3 H F H OH XXH-1-4 ch3 H H CH2CH(CH3)2 ch3 H F H OH XXII-1-5 ch3 H H CH2Ph ch3 H F H OH XXII-1-6 ch3 H H CH2-indol-3-yl ch3 H F H OH XXII-1-7 ch3 H H CH2CH2SCH3 ch3 H F H OH XX1I-1-8 ch3 .3b"; ! * H * ch3 H F H OH *R2 and R36 joined together by (0¾)} to form five-membered ring.

Table XXII-2.

Xa "R1" R2 R3‘ -R35 R4 Rs R6 X Y ΧΧΠ-2-1 Et H H H CH3 H F H OH XXII-2-2 Et H H CH3 ch3 H F H OH XXH-2-3 Et H H CH(CH3)2 ch3 H F H OH XXI1-2-4 Et H H CH2CH(CH3)2 ch3 H F H OH XXII-2-5 Et H H CH2Ph ch3 H F H OH XXII-2-6 Et H H CH2-indol-3-yl ch3 H F H OH ΧΧΠ-2-7 Et H H CH2CH2SCH3 ch3 H F H OH XXII-2-8 —-TV Et ΠΠΓ7" * H * ch3 H F H OH *R2 and RJb joined together by (ΟΗ2)3 to form five-membered ring. 5 Table XXII-3. 1 ' T I “ R»’—"IL· HL”*1 "J" 1 'ie

Xa R1 R2 R3a r3® R4 RJ R6 X Y ΧΧΠ-3-1 'Pr H H H ch3 H F H OH ΧΧΠ-3-2 'Pr H H ch3 ch3 H F H OH XXII-3-3 'Pr H H CHCCH,), ch3 H F H OH XXII-3-4 'Pr H H CH2CH(CH3)2 ch3 H F H OH XXII-3-5 /Pr H H CH2Ph ch3 H F H OH ΧΧΠ-3-6 'Pr H H CH2-indol-3-yl ch3 H F H OH XXII-3-7 /pr H H CH2CH2SCH3 ch3 H F H OH XXH-3-8 'Pr * H * ch3 H F H OH *Ra and R^ joined together by (CH2)3 to form five-membered ring. 2983472-1 -474- WO 2008/121634

Docket No. 60137.0034WOU I PCT/US2008/058183

Table XX1I-4.

Xs R1 R2 r3. R3b R4 R5 R6 X Y XXH-4-1 'Bu H H H ch3 H F H OH XXII-4-2 'Bu H H ch3 ch3 H F H OH ΧΧΠ-4-3 'Bu H H CH(CH3)2 ch3 H F H OH XXII-4-4 'Bu H H CH2CH(CH3)2 ch3 H F H OH XXII-4-5 'Bu H H CH2Ph ch3 H F H OH ΧΧΠ-4-6 'Bu H H CH2-indol-3-yl ch3 H F H OH ΧΧΠ-4-7 'Bu H H CH2CH2SCH3 ch3 H F H OH XXH-4-8 'Bu * H * ch3 H F H OH *R2 and Rjb joined together by (CH2)3t0 form five-membered ring.

Table XXII-5.

X» R R2 R3· R3b R4 RJ Rb X Y XXII-5-1 Ph H H H ch3 H F H OH XXII-5-2 Ph H H ch3 ch3 H F H OH XXH-5-3 Ph H H ch(ch3)2 ch3 H F H OH XXII-5-4 Ph H H CH2CH(CH3)2 ch3 H F H OH XXII-5-5 Ph H H CH2Ph ch3 H F H OH XXII-5-6 Ph H H CH2-indol-3-yl ch3 H F H OH ΧΧΠ-5-7 Ph H H CH2CH2SCH3 ch3 H F H OH ΧΧΠ-5-8 J T- Ph .3b" · * H * ch3 H F H OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXI1-6.

' 1 R 'IL J

Xs R1 R2 “rH" R4 ΊΓ R6 X Υ XXH-6-1 p-Me-Ph H H H ch3 H F Η ΟΗ ΧΧΠ-6-2 p-Me-Ph H H CH3 ch3 Η F Η ΟΗ XXII-6-3 p-Me-Ph H H CHiCHah ch3 Η F Η ΟΗ XXU-6-4 p-Me-Ph H H CHjCHCCHjh ch3 Η F Η ΟΗ XXII-6-5 p-Me-Ph H H CH2Ph ch3 Η. F Η ΟΗ XXH-6-6 p-Me-Ph H H CH2-indol-3-yl ch3 Η F Η ΟΗ XXII-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 Η F Η ΟΗ XXII-6-8 *n2 . r p-Me-Ph »3bTT-j·:: • H ♦ ch3 Η F Η ΟΗ *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -475- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXI1-7.

Χϋ R’ r5- r3„ Ί?~" Rs R6 X Y XXII-7-1 p-F-Ph H H H ch3 H F H OH XXII-7-2 p-F-Ph H H ch3 ch3 H F H OH XXII-7-3 p-F-Ph H H CH(CH3)2 ch3 H F H OH ΧΧΠ-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 H F H OH XXH-7-6 p-F-Ph H H CH2Ph ch3 H F H OH ΧΧΠ-7-7 p-F-Ph H H CH2-indol-3-yl ch3 H F H OH XXH-7-8 p-F-Ph H H CH2CH2SCH3 ch3 H F H OH ΧΧΠ-7-20 p-F-Ph b · · . * H * ch3 H F H OH *R2 and RJb joined together by (CFLbt0 form five-membered ring.

Table XXII-8.

Ks Rl R2 -r3H- R3b R4 R5 R6 X Y ΧΧΠ-8-1 p-Cl-Ph H H H CH3 Η F H OH XXII-8-2 p-Cl-Ph H H ch3 ch3 H F H OH ΧΧΠ-8-3 p-Cl-Ph H H CH(CH3)2 ch3 H F H OH XXI1-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 H F H OH XXU-8-5 p-Cl-Ph H H CH2Ph ch3 H F H OH XXII-8-6 p-Cl-Ph H H CH2-indol-3-yi ch3 H F H OH XXII-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 H F H OH XXH-8-8 p-Cl-Ph ♦ H ♦ ch3 H F H OH *R? and RJb joined together by(CH2)3 to form five-membered ring. 5 Table XXII-9. 1' I ' 11 . * R - 1 . 1 ill·. » 11,1 1 — J I ' 2 ' - 1

Xs R' R2 r3. R3b R4 Rs R6 X Y ΧΧΠ-9-1 p-Br-Ph H H H ch3 H F H OH XXII-9-2 p-Br-Ph H H ch3 ch3 H F H OH XXI1-9-3 p-Br-Ph H H CHCCHjh ch3 H F H OH ΧΧΠ-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 H F H OH XXI1-9-6 p-Br-Ph H H CH2Ph ch3 H F H OH ΧΧΠ-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 H F H OH ΧΧΠ-9-8 p-Br-Ph H H CH2CH2SCH3 ch3 H F H OH XXII-9-20 p-Br-Ph —777 * H * ch3 H F H OH *R4 and RJb joined together by (<%);» to form five-membered ring. 2983472-1 -476- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXII-10.

Xs R‘ R* R3’ “r35 R4 rs R* X Y ΧΧΠ-10-1 p-I-Ph H H H ch3 H F H OH XXII-10-2 p-I-Ph H H ch3 ch3 H F H OH XXII-10-3 p-I-Ph H H CH(CH3>2 ch3 H F H OH ΧΧΠ-10-4 p-I-Ph H H CH2CH(CH3)2 ch3 H F H OH XXII-10-5 p-I-Ph H H CH2Ph ch3 H F H OH XXII-10-6 p-I-Ph H H CH2-indol-3-yl ch3 H F H OH XXII-10-7 p-I-Ph H H CH2CH2SCH3 ch3 H F H OH ΧΧΠ-10-8 p-I-Ph * H * ch3 H F H OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXII-11.

X° R RJ r3. R3b R4 R5 R6 X Y XXII-11-1 ch3 H H H Et H F H OH XXII-11-2 ch3 H H ch3 Et H F H OH XXII-11-3 ch3 H H ΟΗζΟΗ^ Et H F H OH XXII-11-4 ch3 H H CH2CH(CH3)2 Et H F H OH XXII-11-5 ch3 H H CH2Ph Et H F H OH XXII-11-6 ch3 H H CH2-indol-3-yl Et H F H OH XXII-11-7 ch3 H H CH2CH2SCH3 Et H F H OH XXII-11-8 ch3 * H * Et H F H OH *RZ and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXII-12. ' I V HL 111 J J -

Xa R R2 r3- R3b R4 R5 R6 X Y XXII-12-1 Et H H H Et H F H OH XXII-12-2 Et H H CH3 Et H F H OH XXII-12-3 Et H H CHCCHah Et H F H OH XXH-12-4 Et H H CH2CH(CH3)2 Et H F H OH XXII-12-5 Et H H CH2Ph Et H F H OH ΧΧΠ-12-6 Et H H CH2-indoI-3-yl Et H F H OH XXII-12-7 Et H H CH2CH2SCH3 Et H F H OH XXH-12-8 *τι2 J nj Et 6T“T ♦ H ♦ Et H F H OH *RZ and R3b joined together by (CHj^ to form five-membered ring. 2983472-1 -477- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXII-13. d'

Xs R1 R2 "R33" R4 RJ R6 X Y ΧΧΠ-13-1 'Pr H H H Et H F H OH ΧΧΠ-13-2 'Pr H H ch3 Et H F H OH XXI I-13-3 'Pr H H CH(CH3)2 Et H F H OH XXII-13-4 'Pr H H CH2CH(CH3)2 Et H F H OH XXH-13-5 'Pr H H CH2Ph Et H F H OH ΧΧΠ-13-6 *Pr H H CH2-indol-3-yl Et H F H OH XXII-13-7 'Pr H H CH2CH2SCH3 Et H F H OH ΧΧΠ-13-8 'Pr * H * Et H F H OH *RZ and R3b joined together by (CH2)3 to form five-membered ring.

Table ΧΧΠ-14.

Xs R‘ R2 r3. R3b R* R5 R6 X Y XXH-14-1 rBu H H H Et H F H OH ΧΧΠ-14-2 'Bu H H CH3 Et H F H OH XXH-14-3 'Bu H H CH(CH3)2 Et H F H OH XXII-14-4 'Bu H H CH2CH(CH3)2 Et H F H OH XXII-14-5 'Bu H H CH2Ph Et H F H OH XXII-14-6 'Bu H H CH2-indoI-3-yl Et H F H OH ΧΧΠ-14-7 'Bu H H CH2CH2SCH3 Et H F H OH XXII-14-8 *Bu ♦ H * Et H F H OH *R2 and R^ joined together by (0¾^ to form five-membered ring. 5 Table XXI1-15. . ........ - i h slim j 111 ' i .. f

Xs R R2 R3a R3b R4 Rs R6 X Y ΧΧΠ-15-1 Ph H H H Et H F H OH XXII-15-2 Ph H H ch3 Et H F H OH XXU-15-3 Ph H H ΟΗ(ΟΗ3)ϊ Et H F H OH XXII-15-4 Ph H H CH2CH(CH3)2 Et H F H OH XXII-15-5 Ph H H CH2Ph Et H F H OH ΧΧΠ-15-6 Ph H H CH2-indol-3-yl Et H F H OH XXII-15-7 Ph H H CH2CH2SCH3 Et H F H OH ΧΧΠ-15-8 Ph * H * Et H F H OH ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -478- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXII-16.

Ns R' Ra r3. R30 R4 R5 R6 X Y ΧΧΠ-16-1 p-Me-Ph H H H Et H F H OH XXII-16-2 p-Me-Ph H H ch3 Et H F H OH XXII-16-3 p-Me-Ph H H CH(CH3)2 Et H F H OH ΧΧΠ-16-4 p-Me-Ph H H CH2CH(CH3)2 Et H F H OH XXII-16-5 p-Me-Ph H H CHjPh Et H F H OH XXII-16-6 p-Me-Ph H H CH2-indol-3-yl Et H F H OH XXH-16-7 p-Me-Ph H H CH2CH2SCH3 Et H F H OH ΧΧΠ-16-8 p-Me-Ph * H * Et H F H OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXII-17.

Ns R1 R2 rj. R3b R4 Rs R6 X Y XXII-17-1 p-F-Ph H H H Et H F H OH XXII-17-2 p-F-Ph H H ch3 Et H F H OH XXII-17-3 p-F-Ph H H ΟΗ(ΟΗ3)2 Et H F H OH XXH-17-4 p-F-Ph H H CH2CH(CH3)2 Et H F H OH ΧΧΠ-17-5 p-F-Ph H H CH2Ph Et H F H OH XXII-17-6 p-F-Ph H H CH2-indol-3-yl Et H F H OH XXII-17-7 p-F-Ph H H CH2CH2SCH3 Et H F H OH XXH-17-8 p-F-Ph ♦ H ♦ Et H F H OH ♦R2 and R30 joined together by (CThbt0 f°rm five-membered ring. 5 TableXXII-18. - 1 ' . H IL . 1

Xs R' R2 R3· R3b R4 Rs R6 X Y XXII-18-1 p-Cl-Ph H H H Et H F H OH ΧΧΠ-18-2 p-Cl-Ph H H ch3 Et H F H OH XXH-18-3 p-Cl-Ph H H CH(CH3)2 Et H F H OH XXII-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H F H OH XXII-18-5 p-Cl-Ph H H CH2Ph Et H F H OH XXII-18-6 p-Cl-Ph H H CH2-indol-3-yI Et H F H OH ΧΧΠ-18-7 p-Cl-Ph H H CH2CH2SCH3 Et H F H OH ΧΧΠ-18-8 p-Cl-Ph * H * Et H F H OH ♦R2 and RJb joined together by (Cl·^ to form five-membered ring. 2983472-1 -479- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXII-19.

Ns R' RSa “R36 R4 R5 R6 X Y XXII-19-1 p-Br-Ph H H H Et H F H OH XXII-19-2 p-Br-Ph H H ch3 Et H F H OH XXII-19-3 p-Br-Ph H H CH(CH3)2 Et H F H OH XXII-19-4 p-Br-Ph H H CH2CH(CH3)2 Et H F H OH XXII-19-5 p-Br-Ph H H CH2Ph Et H F H OH XXH-19-6 p-Br-Ph H H CH2-indol-3-yl Et H F H OH XXII-19-7 p-Br-Ph H H CH2CH2SCH3 Et H F H OH XXII-19-8 p-Br-Ph * H * Et H F H OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXII-20.

Ns R1 R2 Rj. R3b R^ R3 R6 X Y XXII-20-1 p-I-Ph H H H Et H F H OH XXH-20-2 p-I-Ph H H ch3 Et H F H OH XXI1-2 0-3 p-I-Ph H H CH(CH3)2 Et H F H OH XXII-20-4 p-I-Ph H H CH2CH(CH3)2 Et H F H OH XXII-20-S p-I-Ph H H CH2Ph Et H F H OH ΧΧΠ-20-6 p-I-Ph H H CH2-indol-3-yI Et H F H OH XXII-20-7 p-I-Ph H H CH2CH2SCH3 Et H F H OH ΧΧΠ-20-8 p-I-Ph * H ♦ Et H F H OH *RJ and Rib joined together by (CH2)3 to form five-membered ring. 5 Table XXII-21. — 1 1 W ' IL—-· 11 - J £

Ns R R3 Rj. R3b R4 R3 R6 X Y XXH-21-1 ch3 H H H Η F H OH ΧΧΠ-21-2 ch3 H H ch3 'Pr H F H OH XXH-21-3 ch3 H H ΟΗ(ΟΗ3)2 ipr H F H OH XXII-21-4 ch3 H H CH2CH(CH3)2 'Pr H F H OH XXII-21-5 ch3 H Η CH2Ph 'Pr H F H OH XXII-21-6 ch3 H H CH2-indol-3-yl 'Pr H F H OH XXII-21-7 ch3 H H ch2ch2sch3 'Pr H F H OH XXII-21-8 " nJ ch3 b · - '7 * H * fpr H F H OH *RZ and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -480- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXII-22.

Xs R1 R1 -jpr IF R4 R5 R6 X Y XXH-22-1 Et H H H 'Pr H F H OH XXII-22-2 Et H H ch3 'Pr H F H OH XXH-22-3 Et H H CH(CH3)2 'Pr H F H OH XXII-22-4 Et H H CH2CH(CH3)2 'Pr H F H OH XXH-22-5 Et H H CH2Ph 'Pr H F H OH XXII-22-6 Et H H CH2-indol-3-yl 'Pr H F H OH XXII-22-7 Et H H CH2CH2SCH3 'Pr H F H OH ΧΧΠ-22-8 Et * H * 'Pr H F H OH *R2 and Rejoined together by (Chbb to form five-membered ring.

Table XXII-23.

Xs R Ic R3b R4 R5 R6 X Y XXII-23-1 H H H 'Pr H F H OH XXI1-23-2 'Pr H H CH3 'Pr H F H OH XXII-23-3 'Pr H H CH(CH3)2 'Pr H F H OH XXII-23-4 'Pr H H CH2CH(CH3)2 'Pr H F H OH ΧΧΠ-23-5 'Pr H H CH2Ph 'Pr H F H OH XXH-23-6 'Pr H H CH2-indol-3-yl 'Pr H F H OH XXII-23-7 'Pr H H CH2CH2SCH3 'Pr H F H OH XXII-23-8 'Pr * H ♦ 'Pr H F H OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XXII-24. ...... 1 R Hi— 3L ' 1 — J- Ξ g

Xs R R3 RJ‘ R3b R4 ΊΓ R6 X Y XXII-24-1 Έιι H H H ;Pr H F H OH XXH-24-2 'Bu H H CH3 'Pr H F H OH XXII-24-3 'Bu H H CH(CH3)2 'Pr H F H OH XXII-24-4 'Bu H H CH2CH(CH3)2 ipr H F H OH XXH-24-5 'Bu H H CH2Ph 'Pr. H F H OH ΧΧΠ-24-6 'Bu H H CH2-indol-3-yl Tr H F H OH XXII-24-7 'Bu H H CH2CH2SCH3 'Pr H F H OH ΧΧΠ-24-8 nJ 'Bu b · Λ~~ * H * 'Pr H F H OH *R2 and Rejoined together by (CHjfe to form five-membered ring. 2983472-1 -481 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXII-25.

Xa R2 "r55" R3b R4 R5” R6 X Y ΧΧΠ-25-1 Ph H H H Jpr H F H OH XXII-25-2 Ph H H ch3 'Pr H F H OH XXH-25-3 Ph H H CH(CH3)2 'Pr H F H OH XXII-25-4 Ph H H CH2CH(CH3)2 'Pr H F H OH XXII-25-5 Ph H H CH2Ph 'Pr H F H OH ΧΧΠ-25-6 Ph H H CH2-indol-3-yl 'Pr H F H OH ΧΧΠ-25-7 Ph H H CH2CH2SCH3 'Pr H F H OH XXII-25-8 Ph * H ♦ 'Pr H F H OH *R2 and RJb joined together by (CHab to form five-membered ring.

Table XXI1-26.

Xa R1 R1 r3a R3b R4 RJ R4 X Y XXII-26-1 p-Me-Ph H H H 'Pr H F H OH ΧΧΠ-26-2 p-Me-Ph H H CH3 'Pr H F H OH XXII-26-3 p-Me-Ph H H CH(CH3)2 'Pr H F H OH XXII-26-4 p-Me-Ph H H CH2CH(CH3>2 'Pr H F H OH XXII-26-5 p-Me-Ph H H CH2Ph 'Pr H F H OH XXII-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr H F H OH XXH-26-7 p-Me-Ph H H CH2CH3SCH3 'Pr H F H OH ΧΧΠ-26-8 p-Me-Ph ♦ H * 'Pr H F H OH *R2 and R30 joined together by (CH2)3 to form five-membered ring. 5 Table XXII-27. — — — I ' .......""J . J ··

Xa Rl R4 R1* R3” R4 Rs R6 X Y XXII-27-1 p-F-Ph H H H *Pr H F H OH XXH-27-2 p-F-Ph H H ch3 'Pr H F H OH XXII-27-3 p-F-Ph H H CH(CH3)2 H F H OH ΧΧΠ-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr Η F H OH XXII-27-5 p-F-Ph H H CH2Ph 'Pr H F H OH XXII-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr H F H OH XXI1-27-7 p-F-Ph H H ch2ch2sch3 'Pr Η F H OH XXII-27-8 nJ p-F-Ph t>! ! J X * H * 'Pr H F H OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -482- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXII-28.

Xs R1 R2 pi- R3b Rs R6 X Y ΧΧΠ-28-1 p-Cl-Ph H H H “W" H F H OH XXH-28-2 p-Cl-Ph H H ch3 'Pr H F H OH XXII-28-3 p-Cl-Ph H H CH(CH3)2 'Pr H F H OH XXII-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr H F H OH ΧΧΠ-28-5 p-CI-Ph H H CH2Ph 'Pr H F H OH XXII-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr H F H OH XXII-28-7 p-Cl-Ph H H CH2CH2SCH3 'Pr H F H OH XXU-28-8 p-Cl-Ph * H * 'Pr H F H OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXII-29.

X° R1 R2 R3a R3b R4 RJ R6 X Y XXII-29-1 p-Br-Ph H H H 'Pr H F H OH ΧΧΠ-29-2 p-Br-Ph H H ch3 'Pr H F H OH XXII-29-3 p-Br-Ph H H CHiCHa), 'Pr H F H OH ΧΧΠ-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr H F H OH ΧΧΠ-29-5 p-Br-Ph H H CH2Ph 'Pr H F H OH XXII-29-6 p-Br-Ph H H CH2-indol-3-yl *Ργ H F H OH XXII-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr H F H OH XXII-29-8 “Ϊ7ΓΤ7777Π1 p-Br-Ph 577-—77" ♦ H * 'Pr H F H OH *R2 and Rejoined together by (CH^ to form five-membered ring.

Xs Rl R3 "r35" R3b R4 R6 X Y XXH-30-1 p-I-Ph H H H 'Pr H F H OH XXII-30-2 p-I-Ph H H ch3 'Pr H F H OH XXII-30-3 p-I-Ph H H CHCCHa^ 'Pr H F H OH XXII-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr H F H OH XXII-30-5 p-I-Ph H H CH2Ph 'Pr H F H OH XXI1-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr H F H OH ΧΧΠ-30-7 p-I-Ph H H CH2CH2SCH3 'Pr H F H OH XXII-30-8 p-I-Ph ♦ H ♦ 'Pr H F H OH ♦R2 and R^ joined together by (0¾¼ to form five-membered ring. 2983472-1 -483- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXII-31.

Xa R1 R1 r3« "r35 R4 Rs R6 X Y XXII-31-1 ch3 H H H "Bu H F H OH XXII-31-2 ch3 H H ch3 "Bu H F H OH ΧΧΠ-31-3 ch3 H H CH(CH3)2 "Bu H F H OH XXII-31-4 ch3 H H CH2CH(CH3)2 "Bu H F H OH ΧΧΠ-31-5 ch3 H H CH2Ph "Bu H F H OH XXII-31-6 ch3 H H CH2-indol-3-yl "Bu H F H OH ΧΧΠ-31-7 ch3 H H CH2CH2SCH3 "Bu H F H OH XXII-31-8 ch3 * H * "Bu H F H OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXII-32.

Xa R R2 R3‘ R3b R4 R5 R6 X Y XXII-32-1 Et H H H "Bu H F H OH XXH-32-2 Et H H CH3 "Bu H F H OH XXH-32-3 Et H H CH(CH3)2 "Bu H F H OH XXII-32-4 Et H H CH2CH(CH3)2 "Bu H F H OH XXH-32-5 Et H H CH2Ph "Bu H F H OH XXII-32-6 Et H H CH2-indol-3-yl "Bu H F H OH XXH-32-7 Et H H CH2CH2SCH3 "Bu H F H OH ΧΧΠ-32-8 Et * H * "Bu H F H OH ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table ΧΧΠ-33. — 1 1 — j ..i i m 1

Xe R R2 R3‘ R3b R4 R3 R6 X Y XXH-33-1 'Pr H H H "Bu H F H OH XXII-33-2 'Pr H H CH3 "Bu H F H OH XXII-33-3 /Pr H H CH(CH3)2 "Bu H F H OH XXII-33-4 *Pr H H CH2CH(CH3)2 "Bu H F H OH XXII-33-5 /Pr H H CH2Ph "Bu H F H OH ΧΧΠ-33-6 ‘Pr H H CH2-indol-3-yl "Bu H F H OH XXH-33-7 'Pr H H CH2CH2SCH3 "Bu H F H OH XXII-33-8 'Pr * H * "Bu H F H OH *R2 and R3b joined together by (Cl^b to form five-membered ring. 2983472-1 -484- WO 2008/121634 PCT/US2008/058183

Docket No. 6013 7.0034WOU 1

Table XXII-34.

Na R1 ' R3“” "r* R4 RJ Rfi X Y ΧΧΠ-34-1 'Bu H H H "Bu H F H OH XXH-34-2 'Bu H H ch3 "Bu H F H OH XXII-34-3 'Bu H H CHCCH,), "Bu H F H OH XXII-34-4 'Bu H H CH2CH(CH3)2 "Bu H F H OH XXII-34-5 'Bu H H CH2Ph "Bu H F H OH XXH-34-6 'Bu H H CH2-indol-3-yl "Bu H F H OH XXII-34-7 'Bu H H CH2CH2SCH3 "Bu H F H OH XXII-34-8 'Bu ♦ H * "Bu H F H OH *R2 and R3b joined together by (CH^ to form five-membered ring.

Table XXII-35.

Ns R R2 R3" R3b R4 R5 R6 X Y XXH-35-1 Ph H H H "Bu H F H OH ΧΧΠ-35-2 Ph H H CH3 "Bu H F H OH XXH-35-3 Ph H H CH(CH3)2 "Bu H F H OH XXH-35-4 Ph H H CH2CH(CH3)2 "Bu H F H OH ΧΧΙΪ-35-5 Ph H H CH2Ph "Bu H F H OH XXII-35-6 Ph H H CH2-indol-3-yl "Bu H F H OH XXII-35-7 Ph H H CH2CH2SCH3 "Bu H F H OH XXII-35-8 “Σ7Γ2- Ph ib; * H * "Bu H F H OH *RZ and R3b joined together by (CH^ to form five-membered ring. 5 Table XX1I-36. I R W HL 1 J ' " J1 " ---

Ns Rl R2 R3‘ R3" R4 ΊΓ R6 X Y XXII-36-1 p-Me-Ph H H H "Bu H F H OH XXII-36-2 p-Me-Ph H H CH3 "Bu H F H OH ΧΧΠ-36-3 p-Me-Ph H H CHCCHaX "Bu H F H OH XXII-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu H F H OH XXII-36-5 p-Me-Ph H H CH2Ph "Bu H F H OH XXH-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu H F H OH XXII-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu H F H OH ΧΧΠ-36-8 p-Me-Ph ib ; ; j a - * H * "Bu H F H OH *R2 and R36 joined together by (CH2)3 to form five-membered ring. 2983472-1 -485- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXIl-37.

X? R1 Ra R3' R4 R5” R6 X Y ΧΧΠ-37-1 p-F-Ph H H H "Bu H F H OH XXII-37-2 p-F-Ph H H ch3 "Bu H F H OH ΧΧΠ-37-3 p-F-Ph H H CH(CH3)2 "Bu H F H OH XXH-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu H F H OH XXH-37-5 p-F-Ph H H CH2Ph "Bu H F H OH ΧΧΙΪ-37-6 p-F-Ph H H CH2-indol-3-yl "Bu H F H OH XXII-37-7 p-F-Ph H H CH2CH2SCH3 "Bu H F H OH XXII-37-8 . tTJI p-F-Ph ) · · J Λ * H * "Bu H F H OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXII-38.

X° R1 R5 R3· "R3B R4 RJ R6 X Y XXII-38-1 p-Cl-Ph H H H "Bu H F H OH ΧΧΠ-38-2 p-Cl-Ph H H CH3 "Bu H F H OH XXII-38-3 p-Cl-Ph H H CH(CH3)2 "Bu H F H OH XXII-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H F H OH XXII-38-5 p-Cl-Ph H H CHaPh "Bu H F H OH XXII-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu H F H OH XXH-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu H F H OH XXII-38-8 p-Cl-Ph * H * "Bu H F H OH ♦R4 and RJb joined together by (CFhbt0 fQrm five-membered ring. 5 Table XXII-39. 11 . I1»'—·' 1' RL ' " — J I J —

Xs R‘ ΊΓ R3b R4 ΊΓ R6 X Y XXII-39-1 p-Br-Ph H H H "Bu H F H OH ΧΧΠ-39-2 p-Br-Ph H H CH3 "Bu H F H OH XXII-39-3 p-Br-Ph H H CH(CH3)2 "Bu H F H OH XXII-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu H F H OH XXH-39-5 p-Br-Ph H H CH2Ph "Bu H F H OH ΧΧΙΪ-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu H F H OH XXH-39-7 p-Br-Ph H H CH2CH2SCH3 "Bu H F H OH XXII-39-8 p-Br-Ph * H ♦ "Bu H F H OH *R2 and Rejoined together by (Ctfeb to form five-membered ring. 2983472-1 -486- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU 1

Table XXH-40.

Ns R‘ R3a -p; R4 R5 R4 X Y XXII-40-1 p-I-Ph H H H "Bu H F H OH ΧΧΠ-40-2 p-I-Ph H H ch3 "Bu H F H OH XXII-40-3 p-I-Ph H H CH(CH3)2 "Bu H F H OH XXII-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu H F H OH ΧΧΠ-40-5 p-I-Ph H H CH2Ph "Bu H F H OH XXII-40-6 p-I-Ph H H CH2-indol-3-yl "Bu H F H OH ΧΧΠ-40-7 p-I-Ph H H CH2CH2SCH3 "Bu H F H OH ΧΧΠ-40-8 p-I-Ph * H * "Bu H F H OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXII-41.

Ns R R2 R3' R3b R4 R5 R6 X Y ΧΧΠ-41-1 ch3 Η H H Bz H F H OH XXII-41-2 ch3 H H ch3 Bz H F H OH XXII-41-3 ch3 H H CH(CH3)2 Bz H F H OH XXII-41-4 ch3 H H CH2CH(CH3)2 Bz H F H OH XXII-41-5 ch3 H H CH2Ph Bz H F H OH XXII-41-6 ch3 H H CH2-indol-3-yl Bz H F H OH XXII-41-7 ch3 H H CH2CH2SCH3 Bz H F H OH ΧΧΠ-41-8 aηϊ -i n. ch3 16- - . ♦ H * Bz H F H OH *R2 and RJ0 joined together by (CH2)3 to form five-membered ring.

Ns r’ R5 “R35" -R3* R4 Rs R4 X Y XXII-42-1 Et H H H Bz H F H OH XXII-42-2 Et H H CH3 Bz H F H OH XXII-42-3 Et H H CH(CH3)2 Bz H F H OH XXH-42-4 Et H H CH2CH(CH3)2 Bz H F H OH ΧΧΠ-42-5 Et H H CH2Ph Bz H F H OH ΧΧΠ-42-6 Et H H CH2-indol-3-yl Bz H F H OH XXH-42-7 Et H H CH2CH2SCH3 Bz H F H OH XXH-42-8 “ΙΪ72— Et * H * Bz H F H OH ♦R^ and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -487- WO 2008/121634

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Table XXII-43.

Ns R1 R3 R3" "r^ R4 R5 R6 X Y XXII-43-1 'Pr H H H Bz H F H OH XXII-43-2 'Pr H H ch3 Bz H F H OH XXII-43-3 'Pr H H CH(CH3)2 Bz H F H OH XXH-43-4 'Pr H H CH2CH(CH3)2 Bz H F H OH ΧΧΠ-43-5 'Pr H H CH2Ph Bz H F H O£ ΧΧΠ-43-6 'Pr H H CH2-indol-3-yl Bz H F H OH ΧΧΙΪ-43-7 'Pr H H CH2CH2SCH3 Bz H F H OH XXII-43-8 'Pr * H * Bz H F H OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXII-44.

Ns Rl R3 “r35 R4 RJ R6 X Y XXU-44-1 'Bu H H H Bz H F H OH XXH-44-2 'Bu H H ch3 Bz H F H OH XXI1-4 4-3 'Bu H H CH(CH3)2 Bz H F H OH XXII-44-4 'Bu H H CH2CH(CH3)2 Bz H F H OH ΧΧΠ-44-5 'Bu H H CH2Ph Bz H F H OH XXII-44-6 *Bu H H CH2-indol-3-yl Bz H F H OH XXII-44-7 'Bu H H CH2CH2SCH3 Bz H F H OH XXII-44-8 'Bu * H * Bz H F H OH 10 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXII-45.

Ns R R2 R3" R3b R4 R3 R6 X Y XXH-45-1 Ph H H H Bz H F H OH ΧΧΠ-45-2 Ph H H ch3 Bz H F H OH ΧΧΠ-45-3 Ph H H CH(CH3)2 Bz H F H OH XXII-45-4 Ph H H CH2CH(CH3)2 Bz H F H OH ΧΧΠ-45-5 Ph H H CH2Ph Bz H F H OH XXII-45-6 Ph H H CH2-indol-3-yI Bz H F H OH ΧΧΠ-45-7 Ph H H CH2CH2SCH3 Bz H F H OH XXH-45-8 -τπτ—-773ΐ Ph > · ; * H * Bz H F H OH *R2 and RJb joined together by (CH^ to form five-membered ring. 2983472-1 -488- WO 2008/121634

Docket No. 60137.0034WOD 1 PCT/US2008/058183

Table ΧΧΠ-46.

Xa R1 IT R4 R5 R6 X Y XXII-46-1 p-Me-Ph H H H Bz H F H OH XXII-46-2 p-Me-Ph H H ch3 Bz H F H OH XXH-46-3 p-Me-Ph H H CH(CH3)j Bz H F H OH XXII-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz H F H OH XXII-46-5 p-Me-Ph H H CH2Ph Bz H F H OH ΧΧΠ-46-6 p-Me-Ph H H CH2-indol-3-yl Bz H F H OH XXII-46-7 p-Me-Ph H H CH2CH2SCH3 Bz H F H OH XXII-46-8 p-Me-Ph * H * Bz H F H OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXII-47.

Xa R1 R2 R3« R3b R4 Rs R6 X Y XXII-47-1 p-F-Ph H H H Bz H F H OH XXH-47-2 p-F-Ph H H ch3 Bz H F H OH ΧΧΠ-47-3 p-F-Ph H H CHCCHah Bz H F H OH ΧΧΠ-47-4 p-F-Ph H H CH2CH(CH3)2 Bz H F H OH XXII-47-5 p-F-Ph H H CH2Ph Bz H F H OH XXII-47-6 p-F-Ph H H CH2-indol-3-yl Bz H F H OH XXII-47-7 p-F-Ph H H CH2CH2SCH3 Bz H F H OH XXH-47-8 p-F-Ph * H * Bz H F H OH *R2 and R3b joined together by (CHfeb to form five-membered ring. 5 Table ΧΧΠ-48. 11 < " ‘M HL J" ML ...... i . i j

Xe R1 R2 R3. R3b R4 ΊΓ R6 X Y XXII-48-1 p-Cl-Ph H H H Bz H F H OH XXII-48-2 p-CI-Ph H H ch3 Bz H F H OH XXII-48-3 p-Cl-Ph H H CH(CH3)2 Bz H F H OH XXII-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H F H OH XXII-48-5 p-Cl-Ph H H CH2Ph Bz H F H OH ΧΧΠ-48-6 p-Cl-Ph H H CH2-indot-3-yl Bz H F H OH XXII-48-7 p-Cl-Ph H H CH2CH2SCH3 Bz H F H OH XXII-48-8 p-Cl-Ph b · · j . * H ♦ Bz H F H OH *R2 and R3D joined together by (CH2)3 to form five-membered ring. 2983472-1 -489- WO 2008/121634 PCT/US2008/058183

DocketNo. 60137.0034WOU1

Table XXII-49.

N° R‘ R2 R3fl "R^ Rs •c X Y ΧΧΠ-49-1 p-Br-Ph H H H Bz H F H OH XXH-49-2 p-Br-Ph H H ch3 Bz H F H OH XXII-49-3 p-Br-Ph H H CH(CH3)2 Bz H F H OH ΧΧΠ-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz H F H OH XXH-49-5 p-Br-Ph H H CH2Ph Bz H F H OH XXII-49-6 p-Br-Ph H H CH2-indol-3-yl Bz H F H OH XX1I-49-7 p-Br-Ph H H CH2CH2SCH3 Bz H F H OH XXII-49-8 JnJi p-Br-Ph > ! · _ J ♦ H + Bz H F H OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXII-50.

Xs R' R2 R3' "R* R4 Rs R6 X Y XXII-50-1 p-I-Ph H H H Bz H F H OH XXII-50-2 p-I-Ph H H ch3 Bz H F H OH ΧΧΠ-50-3 p-I-Ph H H CH(CH3)2 Bz H F H OH XXII-50-4 p-I-Ph H H CH2CH(CH3)2 Bz H F H OH XXII-50-5 p-I-Ph H H CH2Ph Bz H F H OH XXII-50-6 p-I-Ph H H CH2-indol-3-yl Bz H F H OH ΧΧΠ-50-7 p-I-Ph H H CH2CH2SCH3 Bz H F H OH XXH-50-8 ' n. p-I-Ph ϊκτί—t: * H * Bz H F H OH ♦R4 and R30 joined together by (CH2)3 to form five-membered ring.

XXIII

Table XXIII-1.__

Ife R1 R2 R3‘ RJb R4 R5 R6 X Y XXIII-1-1 ch3 h h h“ ch3 η f f oh 2983472-1 -490 - WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ns Rl r! R3b~ R3b R4 R6 X Y XXHI-1-2 ch3 H H ch3 ch3 H F F OH ΧΧΠΙ-1-3 ch3 H H CH(CH3)2 ch3 H F F OH ΧΧΙΠ-1-4 ch3 H H CH2CH(CH3)2 ch3 H F F OH ΧΧΠΙ-1-5 ch3 H H CH2Ph ch3 H F F OH XXIII-1-6 ch3 H H CH2-indol-3-yl ch3 H F F OH XXIII-1-7 ch3 H H CH2CH2SCH3 ch3 H F F OH ΧΧΠΙ-1-8 ch3 * H * ch3 H F F OH *R2 and Rejoined together by (CFbb to form five-membered ring.

Table XXIII-2.

Ns R R2 rJ« R3b R4 RJ R6 X Y XXIII-2-1 Et H H H CH3 H F F OH XXIH-2-2 Et H H CH3 ch3 H F F OH XXIII-2-3 Et H H ΟΗ(ΟΗ3)2 ch3 H F F OH ΧΧΙΪΙ-2-4 Et H H CH2CH(CH3)2 ch3 H F F OH ΧΧΙΠ-2-5 Et H H CH2Ph ch3 H F F OH XXIII-2-6 Et H H CH2-indol-3-yl ch3 H F F OH XXI11-2-7 Et H H CH2CH2SCH3 ch3 H F F OH ΧΧΙΠ-2-8 Et * H * ch3 H F F OH *R2 and R30 joined together by (CH2)3 to form five-membered ring.

Table XXIII-3.

Ns R1 R2 r3. "r35 R4 R5" R4 X Y ΧΧΙΠ-3-1 ipr H H H ch3 H F F OH XXIH-3-2 'Pr H H ch3 ch3 H F F OH XXIH-3-3 'Pr H H CH(CH3)2 ch3 H F F OH XXIH-3-4 'Pr H H CH2CH(CH3)2 ch3 H F F OH XXIII-3-5 'Pr H H CH2Ph ch3 H F F OH XXIII-3-6 'Pr H H CH2-indol-3-yl ch3 H F F OH XXIII-3-7 ipr H H CH2CH2SCH3 ch3 H F F OH ΧΧΠΙ-3-8 'Pr * H * ch3 H F F OH 5 ♦R* and RJb joined together by (CH2)3 to form five-membered ring.

Table XXIIM.

Ns R R1 RJi R3b R4 R5 R6 X Y XXIU-4-1 *Bu H H H ch3 H F F OH ΧΧΠΙ-4-2 'Bu H H ch3 ch3 H F F OH 2983472-1 -491- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ns "F” r^ R3a r35 TT“ -R5" R4 X Y ΧΧ1Π-4-3 'Bu H H CH(CH3)2 ch3 H F F OH ΧΧΙΠ-4-4 'Bu H H CH2CH(CH3)2 ch3 H F F OH XXI1I-4-5 "Bu H H CH2Ph ch3 H F F OH XXIII-4-6 'Bu H H CH2-indol-3-yl ch3 H F F OH ΧΧΠΙ-4-7 'Bu H H CH2CH2SCH3 ch3 H F F OH XXHI-4-8 'Bu ♦ H * ch3 H F F OH ♦R·2 and Rejoined together by (CHi)3 to form five-membered ring.

Table XXIII-5.

Na R1 R2 Rj. R3b R4 R3 tv X Y XXIII-5-1 Ph H H H ch3 H F F OH XXIII-5-2 Ph H H CH3 ch3 H F F OH XX HI-5-3 Ph H H CH(CH3)2 ch3 H F F OH ΧΧΠΙ-5-4 Ph H H CH2CH(CH3)2 ch3 H F F OH XXHI-5-5 Ph H H CH2Ph ch3 H F F OH XXIII-5-6 Ph H H CH2-indol-3-yl ch3 Η F F OH XXIH-5-7 Ph H H CH2CH2SCH3 ch3 Η F F OH XXIII-5-8 ......77» Ph 3b ·Τ * H * ch3 Η F F OH *R2 and RJt) joined together by (0-12)3 to form five-membered ring.

Table ΧΧΙΠ-6.

Ns R1 R2 -r3T- R36 R4 R4 R4 X Y XXI11-6-1 p-Me-Ph H H H CH3 H F F OH ΧΧΠΙ-6-2 p-Me-Ph H H ch3 ch3 H F F OH XXHI-6-3 p-Me-Ph H H CHCCHa), ch3 H F F OH XXIII-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 H F F OH ΧΧΠΙ-6-5 p-Me-Ph H H CH2Ph ch3 H F F OH XXIII-6-6 p-Me-Ph H H CH2-indol-3-yI ch3 H F F OH XXHI-6-7 p-Me-Ph H H ch2ch2sch3 ch3 Η F F OH XXIH-6-8 p-Me-Ph ♦ H * ch3 H F F OH 5 *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table ΧΧΙΠ-7.

Ns R1 R2 RJe R3b R4 Ic R4 X Y ΧΧΠΙ-7-1 p-F-Ph H H H CH3 H F F OH ΧΧΙΠ-7-2 p-F-Ph H H CH3 ch3 H F F OH XXIII-7-3 p-F-Ph H H CH(CH3)3 ch3 H F F OH 2983472-1 -492- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Ns Rl R3a "r35 R4 r X Y XXII1-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 H F F OH ΧΧΙΠ-7-6 p-F-Ph H H CH2Ph ch3 H F F OH XXHI-7-7 p-F-Ph H H CH2-indol-3-yl ch3 H F F OH XXIII-7-8 p-F-Ph H H CH2CH2SCH3 ch3 H F F OH XXII1-7-20 p-F-Ph * H * ch3 H F F OH *R2 and R3t> joined together by (CH2)3 to form five-membered ring.

Table XXIII-8.

N2 Rl R2 Rja R3^ R4 RJ R1 X Y XXHI-8-1 p-Cl-Ph H H H ch3 Η F F OH ΧΧΙΠ-8-2 p-Cl-Ph H H ch3 ch3 H F F OH XXIII-8-3 p-Cl-Ph H H CH(CH3)2 ch3 H F F OH XXIII-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 H F F OH ΧΧΠΙ-8-5 p-Cl-Ph H H CH2Ph CH3 H F F OH XXIII-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 H F F OH XXIII-8-7 p-Cl-Ph H H CH2CH2SCH3 CH3 H F F OH XXHI-8-8 . nJ p-Cl-Ph ,b · . ♦ H * ch3 H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXIII-9.

Ns R‘ R3a T5 R4 RJ R6 X Υ XXIII-9-1 p-Br-Ph H H H CH3 Η F F ΟΗ ΧΧΠΙ-9-2 p-Br-Ph H H CH3 ch3 H F F ΟΗ XXIII-9-3 p-Br-Ph H H CHCCHah ch3 Η F F ΟΗ XXIH-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 Η F F ΟΗ XXIII-9-6 p-Br-Ph H H CH2Ph ch3 Η F F ΟΗ XXIII-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 Η F F ΟΗ XXIII-9-8 p-Br-Ph H H CH2CH2SCH3 ch3 Η F F ΟΗ XXHI-9-20 p-Br-Ph * H * ch3 Η F F ΟΗ 5 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table ΧΧΙΠ-10.

Ns R1 R2 RJ“ Rjb R4 R5 R6 X Y ΧΧΙΙΙ-10-1 p-1-Ph Η Η Η ch3 H F F OH ΧΧΙΠ-10-2 p-1-Ph Η Η ch3 ch3 Η F F OH ΧΧΙΙΙ-10-3 p-1-Ph Η Η CHCCHah ch3 Η F F OH ΧΧΗΙ-10-4 p-1-Ph Η Η CH2CH(CH3)2 ch3 Η F F OH 2983472-1 -493- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Rl R3 R37 “r* ” R4 RJ R6 X Y XXIII-10-5 p-I-Ph H H CH2Ph ch3 H F F OH XXIII-10-6 p-I-Ph H H CH2-indol-3-yl ch3 H F F OH ΧΧΠΙ-10-7 p-I-Ph H H CH2CH2SCH3 ch3 H F F OH ΧΧΙΠ-10-8 p-I-Ph * H * ch3 H F F OH *R; and Rejoined together by (CH2)3 to form five-membered ring

Table XXIII-ll.

Ka R R5 RJ“ R3b R4 Rs R6 X Y ΧΧΙΠ-11-1 ch3 H Η Η Et H F F OH ΧΧΙΠ-11-2 ch3 Η Η ch3 Et H F F OH ΧΧΙΠ-11-3 ch3 Η Η CH(CH3)2 Et H F F OH XXIH-11-4 ch3 Η Η CH2CH(CH3)2 Et H F F OH XXHI-11-5 ch3 Η Η CH2Ph Et H F F OH XXIII-11-6 ch3 Η Η CH2-indol-3-yt Et H F F OH XX1II-11-7 ch3 Η Η CH2CH2SCH3 Et H F F OH XXIII-11-8 ch3 * Η * Et H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXIII-12.

Ka R1 RJ. R3b R4 Rs R6 X Y ΧΧΪΙΙ-12-1 Et H H H Et H F F OH XXHI-12-2 Et H H CH3 Et H F F OH XXIII-12-3 Et H H ch<ch3)2 Et H F F OH ΧΧΙΠ-12-4 Et H H CH2CH(CH3)2 Et H F F OH XXHI-12-5 Et H H CH2Ph Et H F F OH ΧΧΠΙ-12-6 Et H H CH2-indol-3-yl Et H F F OH XXHI-12-7 Et H H CH2CH2SCH3 Et H F F OH XXUI-12-8 Et * H * Et H F F OH 5 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table ΧΧΠΙ-13.

Jia R3 R3. R3b R4 r R6 X Y ΧΧΙΠ-13-1 'Pr H H H Et H F F OH XXIH-13-2 'Pr H H ch3 Et H F F OH ΧΧΙΠ-13-3 'Pr H H CH(CH3)2 Et H F F OH XXIII-13-4 'Pr H H CH2CH(CH3)2 Et H F F OH ΧΧΙΠ-13-5 'Pr H H CH2Ph Et H F F OH 2983472-1 494- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ns R1 R5 R30 ΊΡ; R4 RJ R4 X Y ΧΧΠΙ-13-6 'Pr H H CH2-indol-3-yl Et H F F OH ΧΧΙΠ-13-7 'Pr H H CH2CH2SCH3 Et H F F OH ΧΧΠΙ-13-8 'Pr ♦ H * Et H F F OH *R2 and Rejoined together by (CF^b to form five-membered ring.

Table XXIII-14.

Ns R1 R1 R3a T* i?” ΪΓ" R6 X Y ΧΧΠΙ-14-1 'Bu H H H Et H F F OH XXHI-14-2 ‘Bu H H ch3 Et H F F OH XXHI-14-3 'Bu H H CH(CH3)2 Et H F F OH XXHI-14-4 'Bu H H CH2CH(CH3)2 Et H F F OH XXHM4-5 tell H H CH2Ph Et H F F OH XXHI-14-6 'Bu H H CH2-indol-3-yl Et H F F OH XXIH-14-7 'Bu H H CH2CH2SCH3 Et H F F OH XXIII-14-8 j 'Bu * H * Et H F F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXIII-15.

Xs R1 R2 Ra* R3b R4 R3 R4 X Y XXIII-15-1 Ph H H H Et H F F OH ΧΧΠΙ-15-2 Ph H H CH3 Et H F F OH XXIH-15-3 Ph H H ΟΗ(ΟΗ3)2 Et H F F OH XXIH-15-4 Ph H H CH2CH(CH3)2 Et H F F OH ΧΧΠΙ-15-5 Ph H H CH2Ph Et H F F OH XXIII-15-6 Ph H H CH2-indol-3-yl Et H F F OH XXIII-15-7 Ph H H CH2CH2SCH3 Et H F F OH XXHI-15-8 Ph * H ♦ Et H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXIII-16.

Xs R1 ΊΓ Rja R3b R4 R5"" R4 X Y XXIII-16-1 p-Me-Ph H H H Et H F F OH XXIH-16-2 p-Me-Ph H H CH3 Et H F F OH XXHI-I6-3 p-Me-Ph H H CH(CH3)2 Et H F F OH XXIII-16-4 p-Me-Ph H H CH2CH(CH3)2 Et H F F OH XXHI-16-5 p-Me-Ph H H CH2Ph Et· H F F OH XXIH-16-6 p-Me-Ph H H CH2-indol-3-yl Et H F F OH 2983472-1 -495 WO 2008/121634

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Rl R3 R3a Rjb R4 i? R4 X Y ΧΧΠΙ-16-7 p-Me-Ph H H CH2CH2SCH3 Et H F F OH XXII1-16-8 p-Me-Ph ♦ H * Et H F F OH *R2 and RJb joined together by (0-12)3 to form five-membered ring. Table ΧΧΙΠ-17. K· R* R3* R R5 R6 X Y ΧΧΠΙ-17-1 p-F-Ph H H H Et H F F OH ΧΧΠΙ-Ι7-2 p-F-Ph H H ch3 Et H F F OH XXHI-17-3 p-F-Ph H H CH(CH3)2 Et H F F OH ΧΧΠΙ-17-4 p-F-Ph H H CH2CH(CH3)2 Et H F F OH XXIII-17-5 p-F-Ph H H CH2Ph Et H F F OH XXIH-17-6 p-F-Ph H H CH2-indol-3-yl Et H F F OH XXIH-17-7 p-F-Ph H H CH2CH2SCH3 Et H F F OH ΧΧΙΠ-17-8 p-F-Ph * H * Et H F F OH *R2 and R31’joined together by (CH2)3 to form five-membered ring.

Table ΧΧΙΠ-18.

R‘ R2 R3a ΊΡ5 R4 R5" R4 X Y XXIII-18-1 p-Cl-Ph H H H Et H F F OH ΧΧΠ1-18-2 p-Cl-Ph H H ch3 Et H F F OH XXHM8-3 p-Cl-Ph H H CH(CH3)2 Et H F F OH XXIU-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H F F OH XXIII-18-5 p-Cl-Ph H H CH2Ph Et H F F OH XXIII-18-6 p-Cl-Ph H H CH2-indol-3-yl Et H F F OH XXIII-18-7 p-Cl-Ph H H ch2ch2sch3 Et H F F OH XXII I-18-8 “ΪΪ72-7736" p-CI-Ph ♦ H ♦ Et H F F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -496- WO 2008/121634 PCT/US2008/058183

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Table ΧΧΠΙ-19.

Ns R1 - R3b R3b R4 RJ R6 X Y ΧΧΙΠ-19-1 p-Br-Ph H H H Et H F F OH XXHI-19-2 p-Br-Ph H H ch3 Et H F F OH XXIII-19-3 p-Br-Ph H H CH(CH3)2 Et H F F OH ΧΧΠΙ-19-4 p-Br-Ph H H CH2CH(CH3)2 Et H F F OH ΧΧΙΠ-19-5 p-Br-Ph H H CH2Ph Et H F F OH ΧΧΙΠ-19-6 p-Br-Ph H H CH2-indol-3-yl Et H F F OH ΧΧΙΠ-19-7 p-Br-Ph H H CH2CH2SCH3 Et H F F OH XXIII-19-8 '7-r>3b" p-Br-Ph * H ♦ Et H F F OH *R2 and Rejoined together by (Cl-fcb to form five-membered ring.

Table XXIU-20,

Xs R1 R2 “R5i" - - R4 R* X Y XXIH-20-1 p-I-Ph H H H Et H F F OH ΧΧΙΠ-20-2 p-I-Ph H H CH3 Et H F F OH XXIH-20-3 p-I-Ph H H CHCCH,), Et H F F OH XXI1I-20-4 p-I-Ph H H CH2CH(CH3)2 Et H F F OH XXHI-20-5 p-I-Ph H H CH2Ph Et H F F OH XXHI-20-6 p-I-Ph H H CH2-indol-3-y] Et H F F OH XXIH-20-7 p-l-Ph H H CH2CH2SCH3 Et H F F OH XXHI-20-8 p-I-Ph ♦ H * Et H F F OH ♦R2 and R30 joined together by (CH2)3 to form five-membered ring.

Ns Rl R2 R3‘ T6 R4 RJ X Y XXIII-21-1 ch3 H H H "ΦΓ H F F OH XXIII-21-2 ch3 H H ch3 'Pr H F F OH ΧΧΠΙ-21-3 ch3 H H CH(CH3)2 'Pr H F F OH ΧΧΙΠ-21-4 ch3 H H CH2CH(CH3)2 'Pr H F F OH XXI11-21-5 ch3 H H CH2Ph 'Pr H F F OH XXHI-21-6 ch3 H H CH2-indol-3-yl 'Pr H F F OH XXIH-21-7 ch3 H H CH2CH2SCH3 'Pr H F F OH ΧΧΠΙ-21-8 ch3 * H ♦ 'Pr H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -497- WO 2008/121634

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Table XXIII-22.

Xa R2 “r35" R3b R4 Rs R6 X Y XXIII-22-1 Et H H H 'pr H F F OH XXI11-22-2 Et H H ch3 'Pr H F F OH XXIII-22-3 Et H H CH(CH3)2 'Pr H F F OH ΧΧΠΙ-22-4 Et H H CH2CH(CH3)2 'Pr H F F OH ΧΧΙΠ-22-5 Et H H CH2Ph 'Pr H F F OH XXIH-22-6 Et H H CH2-indol-3-yl 'Pr H F F OH ΧΧΠΙ-22-7 Et H H CH2CH2SCH3 'Pr H F F OH XXHI-22-8 Et * H * 'Pr H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXIII-23.

Xs R1 R2 Rj. R3b R4 R! R6 X Y XXIII-23-1 'Pr H H H 'Pr H F F OH XXI11-23-2 'Pr H H ch3 'Pr H F F OH ΧΧΙΠ-23-3 'Pr H H CH(CH3)2 'Pr H F F OH XXII1-23-4 'Pr H H CH2CH(CH3)2 'Pr H F F OH XXIII-23-5 'Pr H H CH2Ph 'Pr H F F OH ΧΧΙΠ-23-6 'Pr H H CH2-indol-3-yl 'Pr H F F OH XXIII-23-7 'Pr H H CH2CH2SCH3 'Pr H F F OH XXI1I-23-8 'Pr * H * Tr H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XXUI-24. , -< I» — II ..I·.——

Xs R R2 R3" R3b Ic Rr R6 X Υ ΧΧΠΙ-24-Ι 'Bu H H H Η F F ΟΗ XXIII-24-2 'Bu H H ch3 'Pr Η F F ΟΗ XXHI-24-3 'Bu H H ΟΗ(ΟΗ3)2 'Pr Η F F ΟΗ XXIII-24-4 'Bu H H CH2CH(CH3)2 'Pr Η F F ΟΗ XXIH-24-5 'Bu H H CH2Ph Tr Η F F ΟΗ XXIII-24-6 'Bu H H CH2-indol-3-yl 'Pr Η F F ΟΗ ΧΧΙΠ-24-7 'Bu H H ch2ch2sch3 'Pr Η F F ΟΗ XXIU-24-8 'Bu * H 4 'Pr Η F F ΟΗ *R2 and R3b joined together by (CHbb to form five-membered ring.

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Table ΧΧΠΙ-25.

Ns R3 Rja "r35 R4 Rs ΊΓ· X Y ΧΧΙΠ-25-1 Ph H H H 'Pr H F F OH ΧΧΠΙ-25-2 Ph H H ch3 'Pr H F F OH XXIII-25-3 Ph H H CH(CH3)2 'Pr H F F OH XXIH-25-4 Ph H H CH2CH(CH3)2 'Pr H F F OH ΧΧΠΙ-25-5 Ph H H CH2Ph 'Pr H F F OH XXIII-25-6 Ph H H CH2-indol-3-yl 'Pr H F F OH XX1II-25-7 Ph H H CH2CH2SCH3 'Pr H F F OH XX111-25-8 Ph * H * 'Pr H F F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table ΧΧΠΙ-26.

Ns Έ- R2 r3. R3b R4 R* R6 X Y XXIH-26-1 p-Me-Ph H H H 'Pr H F F OH XXHI-26-2 p-Me-Ph H H CH3 'Pr H F F OH XXI11-26-3 p-Me-Ph H H CH(CH3)2 'Pr H F F OH XXIII-26-4 p-Me-Ph H H CH2CH(CH3)2 'Pr H F F OH XX1U-26-5 p-Me-Ph H H CH2Ph 'Pr H F F OH ΧΧΙΠ-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr H F F OH XXIH-26-7 p-Me-Ph H H CH2CH2SCH3 'Pr H F F OH XXIII-26-8 p-Me-Ph * H * 'Pr H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XXIH-27. — I " R R, 'IL ' ' "‘"-I" . ί

Ns R1 ΊΓ RJa R3b R4 Rs R6 X Y XXIH-27-1 p-F-Ph H H H 'Pr H F F OH XXIII-27-2 p-F-Ph H H CH3 'Pr H F F OH XXIH-27-3 p-F-Ph H H CHCCHaX Tr H F F OH XXHI-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr H F F OH XXHI-27-5 p-F-Ph H H CH2Ph /pr H F F OH XXIII-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr H F F OH XXIII-27-7 p-F-Ph H H CH2CH2SCH3 'Pr H F F OH XXIII-27-8 T77Z-Τ7Γ5Β p-F-Ph * H * Tr H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -499- WO 2008/121634 PCT/US2008/058183

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Table XXIII-2 8.

Na Rl R2 r3° R3b R4 RJ R6 X Y ΧΧΠΙ-28-1 p-Cl-Ph H H H 'pT H F F OH XXHI-28-2 p-Cl-Ph H H ch3 'Pr H F F OH XXHI-28-3 p-Cl-Ph H H CH(CH3)2 'Pr H F F OH XXIII-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr H F F OH XXHI-28-5 p-Cl-Ph H H CH2Ph 'Pr H F F OH XX1II-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr H F F OH ΧΧΠΙ-28-7 p-CI-Ph H H CH2CH2SCH3 'Pr H F F OH XXIII-28-8 p-Cl-Ph * H * 'Pr H F F OH *R2 and R3b joined together by (CThb to form five-membered ring.

Table ΧΧΙΠ-29.

Xa R1 R2 R3. R3b R4 RJ R6 X Y XXIH-29-1 p-Br-Ph H H H -TpT" H F F OH XXIU-29-2 p-Br-Ph H H CH3 'Pr H F F OH XXIH-29-3 p-Br-Ph H H CH(CH3)2 'Pr H F F OH XXIH-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr H F F OH ΧΧΠΙ-29-5 p-Br-Ph H H CH2Ph 'Pr H F F OH XXIII-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr H F F OH XXIII-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr H F F OH XXIII-29-8 p-Br-Ph * H * 'Pr H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table ΧΧΙΠ-30. 111 1 1 ». WL ....... "J*”- 1 J „ "

Xa Rl R2 R3. R3b R R3 R6 X Y XXIU-30-1 p-l-Ph H H H 'Pr H F F OH ΧΧΠΙ-30-2 p-I-Ph H H ch3 'Pr H F F OH XXIII-30-3 p-I-Ph H H CH(CH3)2 'Pr H F F OH XXIII-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr H F F OH XXIlI-30-5 p-I-Ph H H CH2Ph 'Pr H F F OH XXIII-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr H F F OH XXIII-30-7 p-I-Ph H H ch2ch2sch3 Tr H F F OH ΧΧΙΠ-30-8 p-I-Ph * H * 'Pr H F F OH ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -500- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table ΧΧΙΠ-31.

Ns R1 R2 Rja "F r4 RJ R6 X Y XXIH-31-1 ch3 H H H "Bu H F F OH ΧΧ1Π-31-2 ch3 H H ch3 "Bu H F F OH XX1H-31-3 ch3 H H CH(CH3)2 "Bu H F F OH XXIII-31-4 ch3 H H CH2CH(CH3)2 "Bu H F F OH ΧΧΙΠ-31-5 ch3 H H CHjPh "Bu H F F OH XXIII-31-6 ch3 H H CH2-indol-3-yl "Bu H F F OH ΧΧΠΙ-31-7 ch3 H H CH2CH2SCH3 "Bu H F F OH XXIII-31-8 ch3 * H * "Bu H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring?

Table ΧΧ1Π-32.

Ns R RJ R3a R3b R4 R5 R6 X Υ XX1II-32-1 Et H H H "Bu Η F F ΟΗ XXIII-32-2 Et H H ch3 "Bu Η F F ΟΗ ΧΧΙΠ-32-3 Et H H CH(CH3)2 "Bu Η F F ΟΗ XXIII-32-4 Et H H CH2CH(CH3)2 "Bu Η F F ΟΗ XXIII-32-5 Et H H CH2Ph "Bu Η F F ΟΗ XXIII-32-6 Et H H CH2-indol-3-yl "Bu Η F F ΟΗ XXIII-32-7 Et H H ch2ch2sch3 "Bu Η F F ΟΗ XXH1-32-8 Et ♦ H * "Bu Η F F ΟΗ ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XXI1I-33. - 1 — ~i->5 —n _ *l'· 1 _<l __ . _

Ns R R2 R3a Rib R4 R5 R6 X Y ΧΧΙΙΙ-33-1 'Pr H H H "Bu H F F OH ΧΧΙΠ-33-2 'Pr H H ch3 "Bu H F F OH ΧΧΠΙ-33-3 fpr H H CH(CH3)2 "Bu H F F OH ΧΧΙΙΙ-33-4 'Pr H H CH2CH(CH3)2 "Bu H F F OH ΧΧΙΗ-33-5 fPr H H CH2Ph "Bu H F F OH ΧΧΙΙΙ-33-6 'Pr H H CH2-indol-3-yl "Bu H F F OH ΧΧΗΙ-33-7 Ψγ H H CH2CH2SCH3 "Bu H F F OH ΧΧΙΙΙ-33-8 'Pr * H * "Bu H F F OH ♦R2 and R3b joined together by ((%¼ to form five-membered ring, 2983472-1 -501 - WO 2008/121634

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Table XXI1I-34.

n° ΊΓ~ R2 "r* R4 R* R6 X Y XXI1I-34-1 *Bu H H H "Bu H F F OH XXIH-34-2 'Bu H H ch3 "Bu H F F OH ΧΧΙΠ-34-3 'Bu H H CHCCHa), "Bu H F F OH ΧΧΠΙ-34-4 'Bu H H CH2CH(CH3)2 "Bu H F F OH XXIH-34-5 'Bu H H CH2Ph "Bu H F F OH ΧΧΙΠ-34-6 'Bu H H CH2-indol-3-yl "Bu H F F OH XXIII-34-7 'Bu H H CH2CH2SCH3 "Bu H F F OH ΧΧΠΙ-34-8 'Bu * H * "Bu H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table ΧΧΙΠ-35.

Ns R RJ r3. R3b R4 R3 Rb X Y XXIII-35-1 Ph H H H "Bu H F F OH XXIII-35-2 Ph H H ch3 "Bu H F F OH ΧΧΠΙ-35-3 Ph H H CH(CH3)2 "Bu H F F OH XXIII-35-4 Ph H H CH2CH(CH3)2 "Bu H F F OH XXIII-35-5 Ph H H CH2Ph ”Bu H F F OH ΧΧΠΙ-35-6 Ph H H CH2-indol-3-yl "Bu H F F OH XXIII-35-7 Ph H H CH2CH2SCH3 "Bu H F F OH ΧΧΙΠ-35-8 Ph * H * "Bu H F F OH

Table XXIII-36.

Ns Rl Rl R3” “r35 R4 R3 R6 X Y ΧΧΙΠ-36-1 p-Me-Ph H H H "Bu H F F OH XXIII-36-2 p-Me-Ph H H ch3 "Bu H F F OH XXIII-36-3 p-Me-Ph H H CHCCH^ "Bu H F F OH XXHI-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu H F F OH ΧΧΠΙ-36-5 p-Me-Ph H H CH2Ph "Bu H F F OH XXIII-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu H F F OH XXIII-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu H F F OH XXIII-36-8 p-Me-Ph * H * "Bu H F F OH *R2 and RJ0 joined together by (CH2)3 to form five-membered ring. 2983472-1 -502- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table ΧΧΠΙ-37.

X£ R1 R2 R3ir R3b ΊΓ“ RJ Rb X Y ΧΧΠΙ-37-1 p-F-Ph H H H "Bu H F F OH XX1H-37-2 p-F-Ph H H ch3 "Bu H F F OH XXIII-37-3 p-F-Ph H H CH(CHj)2 ”Bu H F F OH ΧΧΠΙ-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu H F F OH XXIH-37-5 p-F-Ph H H CH2Ph "Bu H F F OH XXIII-37-6 p-F-Ph H H CH2-indol-3-yl "Bu H F F OH XXIII-37-7 p-F-Ph H H CH2CH2SCH3 "Bu H F F OH ΧΧΙΠ-37-8 p-F-Ph ♦ H * "Bu H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXI1I-38.

Na R1 ΊΓ R3. R3b R* Rs Rb X Y ΧΧΠΙ-38-1 p-Cl-Ph H H H "Bu H F F OH XXIII-38-2 p-Cl-Ph H H ch3 "Bu H F F OH XXIII-38-3 p-Cl-Ph H H CH(CH3)2 "Bu H F F OH XXIII-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H F F OH XXIH-38-5 p-Cl-Ph H H CH2Ph "Bu H F F OH XXUI-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu H F F OH ΧΧΙΠ-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu H F F OH XXIII-38-8 p-Cl-Ph * H ♦ "Bu H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XXIII-39. I,.. I, - -

Ns R' R2 R3· R3b R2 R5 R6 X Y XXIH-39-1 p-Br-Ph H H H "Bu H F F OH ΧΧΙΠ-39-2 p-Br-Ph H H ch3 "Bu H F F OH ΧΧΙΠ-39-3 p-Br-Ph H H CH(CH3)2 "Bu H F F OH XXHI-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu H F F OH ΧΧΙΠ-39-5 p-Br-Ph H H CH2Ph "Bu H F F OH ΧΧΙΠ-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu H F F OH ΧΧΠΙ-39-7 p-Br-Ph H H ch2ch2sch3 "Bu H F F OH ΧΧΙΠ-39-8 .....< «3b p-Br-Ph * H * "Bu H F F OH ♦R2 and Rejoined together by (CRhb to form five-membered ring. 2983472-1 -503- WO 2008/121634

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Table XXIII-40.

Xs R1 R2 RJo "R35 R4 Rs R6 X Y XXIII-40-1 p-I-Ph H H H rtBu H F F OH XXIII-40-2 p-I-Ph H H ch3 ”Bu H F F OH ΧΧΠΙ-40-3 p-I-Ph H H CH(CH3)2 wBu H F F OH ΧΧΠΙ-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu H F F OH XXIII-40-5 p-I-Ph H H CH2Ph "Bu H F F OH ΧΧΠΙ-40-6 p-I-Ph H H CH2-indol-3-yl "Bu H F F OH XXIH-40-7 p-I-Ph H H CH2CH2SCH3 "Bn H F F OH ΧΧΙΠ-40-8 p-I-Ph * H * "Bu H F F OH ♦R* and Rejoined together by (CFfch to form five-membered ring.

Table XXIII-41.

Xs IT RJ r3- R3b R4 R6 X Y xxin-41-i CH3 H H H Bz H F F OH XXIII-41-2 ch3 H H ch3 Bz H F F OH XXIII-41-3 ch3 Η H CH(CH3)2 Bz H F F OH XXIII-41-4 ch3 H H CH2CH(CH3)2 Bz H F F OH ΧΧΠΙ-41-5 ch3 H H CH2Ph Bz H F F OH XXI11-41-6 ch3 H H CH2-indol-3-yl Bz H F F OH XXIII-41-7 ch3 H H CH2CH2SCH3 Bz H F F OH XXIII-41-8 ch3 * H * Bz H F F OH *RZ and RJ0 joined together by (Cl·^ to form five-membered ring. 5 Table XXIII-42. '"» 1 ·Ι·Μ^Λ 'Hi J 1 .....— ,

Xs R R2 r3« R3b R4 R5 R6 X Y XXIH-42-1 Et H H H Bz H F F OH XXIII-4 2-2 Et H H CH3 Bz H F F OH XXIII-42-3 Et H H CH(CH3)2 Bz H F F OH XXIH-42-4 Et H H CH2CH(CH3)2 Bz H F F OH ΧΧΙΠ-42-5 Et H H CH2Ph Bz H F F OH XXIU-42-6 Et H H CH2-indol-3-yl Bz H F F OH XXII1-42-7 Et H H CH2CH2SCH3 Bz H F F OH XXHI-42-8 Et * H * Bz H F F OH *RZ and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -504- WO 2008/121634

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Table ΧΧΠ1-43.

Xa R1 R3a “R35 R4 R5 R6 X Y XXIH-43-1 'pr H H H Bz H F F OH XXIU-43-2 'Pr H H ch3 Bz H F F OH ΧΧΙΠ-43-3 'Pr H H CH(CH3)2 Bz H F F OH XXIH-43-4 'Pr H H CH2CH(CH3)2 Bz H F F OH XXHI-43-5 'Pr H H CH2Ph Bz H F F XXIH-43-6 'Pr H H CH2-indol-3-yl Bz H F F OH XXHI-43-7 'Pr H H ch2ch2sch3 Bz H F F OH XXIH-43-8 'Pr * H * Bz H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXIII-44. d1

Xa R1 R2 R3‘ R3b R4 R5 R6 X Y ΧΧΙΠ-44-1 *Bu H H H Bz H F F OH XXIH-44-2 'Bu H H ch3 Bz H F F OH ΧΧΙΠ-44-3 'Bu H H CH(CH3)2 Bz H F F OH XXIII-44-4 'Bu H H CH2CH(CH3)2 Bz H F F OH ΧΧΠΙ-44-5 'Bu H H CH2Ph Bz H F F OH ΧΧΙΠ-44-6 'Bu H H CH2-indol-3-yl Bz H F F OH ΧΧΠΙ-44-7 'Bu H H CH2CH2SCH3 Bz H F F OH XXIH-44-8 'Bu * H * Bz H F F OH 10 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXIII-45.

Xa R R2 r3. R3b R4 R R“ X Y XXIII-45-1 Ph H H H Bz H F F OH XXIII-45-2 Ph H H CH3 Bz H F F OH XXIII-45-3 Ph H H CHCCHa), Bz H F F OH XXIH-45-4 Ph H H CH2CH(CH3)2 Bz H F F OH XXHI-45-5 Ph H H CH2Ph Bz H F F OH XXIII-45-6 Ph H H CH2-indol-3-yl Bz H F F OH XX1H-45-7 Ph H H CH2CH2SCH3 Bz H F F OH XXIH-45-8 Ph * H * Bz H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -505 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table ΧΧΙΠ-46.

Ns R1 RJ R3a ΊΡ5 R4 R3 R4 X Y ΧΧΠΙ-46-1 p-Me-Ph H H H Bz H F F OH XXIH-46-2 p-Me-Ph H H ch3 Bz H F F OH XXHI-46-3 p-Me-Ph H H CH(CH3)2 Bz H F F OH ΧΧΙΠ-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz H F F OH XXHI-46-5 p-Me-Ph H H CH2Ph Bz H F F OH XXIH-46-6 p-Me-Ph H H CH2-indol-3-yl Bz H F F OH XXIH-46-7 p-Me-Ph H H CH2CH2SCH3 Bz H F F OH XXIH-46-8 p-Me-Ph ♦ H * Bz H F F OH *R2 and Rejoined together by (Cbhb to f°rm five-membered ring.

Table ΧΧΙΠ-47.

Ns R1 RJ‘ R3b R4 R3 R6 X Y ΧΧΙΠ-47-1 p-F-Ph H H H Bz H F F OH ΧΧΠΙ-47-2 p-F-Ph H H CH3 Bz H F F OH ΧΧΙΠ-47-3 p-F-Ph H H CHCCH^ Bz H F F OH XXIII-47-4 p-F-Ph H H CH2CH(CH3)2 Bz H F F OH XXIII-47-5 p-F-Ph H H CH2Ph Bz H F F OH XXIII-47-6 p-F-Ph H H CH2-indol-3-yl Bz H F F OH XXIH-47-7 p-F-Ph H H CH2CH2SCH3 Bz H F F OH ΧΧΙΠ-47-8 p-F-Ph * H * Bz H F F OH *R2 and R36 joined together by (ΟΗ2)3 to form five-membered ring. 5 Table XXIII-48. I I - I — — - —, —HI— ' " — j " I "1

Ns R' R2 R3* R3b' R4 R3 R4 X Y ΧΧΙΠ-48-1 p-Cl-Ph H H H Bz H F F OH XXIII-48-2 p-Cl-Ph H H CH3 Bz H F F OH XXHI-48-3 p-Cl-Ph H H CH(CH3)2 Bz H F F OH XXHI-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H F F OH ΧΧΠΙ-48-5 p-Cl-Ph H H CH2Ph Bz H F F OH ΧΧΠΙ-48-6 p-Cl-Ph H H CH2-indoI-3-yl Bz H F F OH XXIH-48-7 p-Cl-Ph H H CH2CH2SCH3 Bz H F F OH XXIH-48-8 p-Cl-Ph * H ♦ Bz H F F OH *R4 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -506- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table ΧΧΠΙ-49.

Jfe R1 R3 R3b "R^ Rs R6 X Y XX1II-49-1 p-Br-Ph H H H Bz H F F OH ΧΧΙΠ-49-2 p-Br-Ph H H CH3 Bz H F F OH XXIII-49-3 p-Br-Ph H H CH(CH3)2 Bz H F F OH XXIII-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz H F F OH ΧΧΙΠ-49-5 p-Br-Ph H H CH2Ph Bz H F F OH XXIII-49-6 p-Br-Ph H H CH2-indol-3-yl Bz H F F OH XXIII-49-7 p-Br-Ph H H CH2CH2SCH3 Bz H F F OH ΧΧΠΙ-49-8 p-Br-Ph * H * Bz H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table ΧΧΠΙ-50.

R3 R3b R4 R3 R6 X Y XXIII-50-1 p-I-Ph H H H Bz Η F F OH ΧΧΙΠ-50-2 p-I-Ph H H ch3 Bz H F F OH XXIH-50-3 p-I-Ph H H CH(CH3)2 Bz Η F F OH ΧΧΙΠ-50-4 p-I-Ph H H CH2CH(CH3)2 Bz H F F OH ΧΧΙΠ-50-5 p-I-Ph H H CHaPh Bz H F F OH ΧΧΙΠ-50-6 p-I-Ph H H CH2-indol-3-yl Bz Η F F OH XXIH-50-7 p-I-Ph H H CH2CH2SCH3 Bz Η F F OH XXIII-50-8 p-I-Ph * H * Bz Η F F OH ♦R2 and Rejoined together by (CH2)3 to form five-membered ring.

XXIV

Table XXIV-1,_r—r^_

>6 R1 R2 R3‘ R3b R4 R3 R6 X Y XXIV-1-1 ch3 h h h ch3 h h f oh 2983472-1 -507- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034 WOU 1

x° r’ R2 R3b R4 Rs R6 X Y XXIV-1-2 ch3 H H ch3 ch3 H H F OH XXIV-1-3 ch3 H H CH(CH3)2 ch3 H H F OH XXIV-1-4 ch3 H H CH2CH(CH3)2 ch3 H H F OH XXIV-1-5 CHj H H CH2Ph ch3 H H F OH XXIV-1-6 ch3 H H CH2-indol-3-yl ch3 H H F OH XXIV-1-7 ch3 H H CH2CH2SCH3 ch3 H H F OH XXIV-1-8 —j τ,ΐ ch3 lb; ·. * H * ch3 H H F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXIV-2.

Xs R1 R2 R3a T* R4 R’ R6 X Υ XXIV-2-1 Et H H H ch3 Η Η F ΟΗ XXIV-2-2 Et H H ch3 ch3 H Η F ΟΗ XXIV-2-3 Et H H CHfiCHah ch3 Η Η F ΟΗ XXIV-2-4 Et H H CH2CH(CH3)2 ch3 Η Η F ΟΗ XXIV-2-5 Et H H CH2Ph ch3 Η Η F ΟΗ XXIV-2-6 Et H H CH2-indol-3-yl ch3 Η Η F ΟΗ XXIV-2-7 Et H H CH2CH2SCH3 ch3 Η Η F ΟΗ XXIV-2-8 Et * H * ch3 Η Η F ΟΗ *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXIV-3.

Xa R1 R2 Rs R35 R4- RJ R6 X Υ XXTV-3-1 'Pr Η Η Η CH3 H Η F ΟΗ XXIV-3-2 'Ργ Η Η ch3 ch3 Η Η F ΟΗ XX1V-3-3 'Pr Η Η CHCCH^ ch3 Η Η F ΟΗ XXIV-3-4 'Pr Η Η CH2CH(CH3)2 ch3 Η Η F ΟΗ XXIV-3-5 'Ργ Η Η CH2Ph ch3 Η Η F ΟΗ ΧΧΓΥ-3-6 'Pr Η Η CH2-indol-3-yl ch3 Η Η F ΟΗ XXIV-3-7 'Pr Η Η CH2CH2SCH3 ch3 Η Η F ΟΗ XXIV-3-8 fpr * Η * ch3 Η Η F ΟΗ 5 *R2 and Re joined together by (CH2)3 to form five-membered ring.

Table XXIV-4.

Xs R R2 r3« R3t, R4 RJ R6 X Y XXJV-4-1 'Bu Η Η Η ch3 H H F OH XXIV-4-2 'Bu Η Η ch3 ch3 H H F OH 2983472-1 -508 - WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ns R1 R2 R3’ R3b R4 Rs R6 X Y XXIV-4-3 *Bu H H CH(CH3)2 ch3 H H F OH XX1V-4-4 'Bu H H CH2CH(CH3)2 ch3 H H F OH XXIV-4-5 'Bu H H CH2Ph ch3 H H F OH XXIV-4-6 'Bu H H CHj-indol-3-yl ch3 H H F OH XXIV-4-7 'Bu H H CH2CH2SCH3 ch3 H H F OH XXIV-4-8 'Bu * H ♦ ch3 H H F OH *R4 and Rejoined together by (CH2)s to form five-membered ring.

Table XXIV-5.

Ns R1 Ra R,Jl R3b R4 r5" R6 X Y XXIV-5-1 Ph H H H ch3 H H F OH XX1V-5-2 Ph H H ch3 ch3 H H F OH XXIV-5-3 Ph H H CH(CH3)2 ch3 H H F OH XXIV-5-4 Ph H H CH2CH(CH3)2 ch3 H H F OH XXIV-5-5 Ph H H CH2Ph ch3 H H F OH XXIV-5-6 Ph H H CH2-indol-3-yl ch3 H H F OH XXIV-5-7 Ph H H CH2CH2SCH3 ch3 H H F OH XXIV-5-8 Ph * H * ch3 H H F OH ♦R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXIV-6.

Ns R1 R2 R3’ -r3B R4 R5 R6 X Y XXIV-6-1 p-Me-Ph H H H ch3 H H F OH XXIV-6-2 p-Me-Ph H H ch3 ch3 H H F OH XXIV-6-3 p-Me-Ph H H CH(CH3)2 ch3 H H F OH XXIV-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 H H F OH XXIV-6-5 p-Me-Ph H H CH2Ph ch3 H H F OH XXIV-6-6 p-Me-Ph H H CH2-indol-3-yl ch3 H H F OH XXIV-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 H H F OH XXIV-6-8 p-Me-Ph * H * ch3 H H F OH 5 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXIV-7.

Ns R* RJ R31 r36 R4 r R6 X Y XXIV-7-1 p-F-Ph H H H ch3 Η H F OH XXIV-7-2 p-F-Ph H H ch3 ch3 H H F OH XXIV-7-3 p-F-Ph H H CH(CH3)2 ch3 H H F OH 2983472-1 -509- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Nfi R’ R3 R3a” "r* —— R4 R3 "l?" X Y XXIV-7-4 p-F-Ph H H CH2CH(CH3>2 ch3 H H F OH XXIV-7-6 p-F-Ph H H CH2Ph ch3 H H F OH XXIV-7-7 p-F-Ph H H CH2-indol-3-yl ch3 H H F OH XXIV-7-8 p-F-Ph H H CH2CH2SCH3 ch3 H H F OH XXIV-7-20 p-F-Ph * H * ch3 H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXIV-8.

Ns R1 R3 Rja R3b R4 Rs Rb X Y XXIV-8-1 p-Cl-Ph H H H CH3 Η H F OH XXIV-8-2 p-Cl-Ph H H ch3 ch3 H H F OH XXIV-8-3 p-CI-Ph H H CH(CH3)j ch3 H H F OH XXIV-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 H H F OH XXIV-8-5 p-Cl-Ph H H CH2Ph ch3 H H F OH XX1V-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 H H F OH XXIV-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 H H F OH XXIV-8-8 J n p-Cl-Ph 3ΤΓΊ- * H * ch3 H H F OH *R2 and R3b joined together by (ΟΗ2)3 to form five-membered ring.

Table XXIV-9.

Ns R1 ir r3b R36 R4 R’ X Υ XXIV-9-1 p-Br-Ph H H H ch3 Η Η F ΟΗ XXIV-9-2 p-Br-Ph H H ch3 ch3 Η Η F ΟΗ XXIV-9-3 p-Br-Ph H H CH(CH3)2 ch3 Η Η F ΟΗ XXIV-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 Η Η F ΟΗ XXIV-9-6 p-Br-Ph H H CH2Ph ch3 Η Η F ΟΗ XXIV-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 Η Η F ΟΗ XXrV-9-8 p-Br-Ph H H ch2ch2sch3 ch3 Η Η F ΟΗ XX1V-9-20 p-Br-Ph * H * ch3 Η Η F ΟΗ 5 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXIV-10.

Ns R1 IV Rj. Rib R4 Rs R6 X Υ XXIV-HM p-1-Ph Η Η Η ch3 Η Η F ΟΗ XXIV-10-2 p-1-Ph Η Η ch3 ch3 Η Η F ΟΗ XXIV-10-3 p-1-Ph Η Η CH(CH3)j ch3 Η Η F ΟΗ XXIV-10-4 p-1-Ph Η Η CH2CH(CH3)2 ch3 Η Η F ΟΗ 2983472-1 -510- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ns R1 R3 Ria Rs R4 X Y XXIV-IO-5 p-I-Ph H H CH2Ph ch3 H H F OH XXIV-10-6 p-I-Ph H H CH2-indol-3-yl ch3 H H F OH XXTV-10-7 p-I-Ph H H CH2CH2SCH3 ch3 H H F OH XXIV-10-8 p-I-Ph * H ♦ ch3 H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXIV-11.

Ns R Ίν R3« R3b R4 R4 R4 X Y XXIV-11-1 ch3 H H H Et H H F OH XXIV-I1-2 ch3 H H ch3 Et H H F OH XXIV-11-3 ch3 H H CH(CH3)2 Et H H F OH XXIV-11-4 ch3 H H CH2CH(CH3)2 Et H H F OH XXIV-ll-5 ch3 H H CH2Ph Et H H F OH XXIV-11-6 ch3 H H CH2-lndol-3-yl Et H H F OH XXIV-11-7 ch3 H H CH2CH2SCH3 Et H H F OH XXIV-11-8 i ch3 1 · * * H * Et H H F OH *R2 and Rejoined together by (Cibb to form five-membered ring.

Table XXIV-12.

Ns R1 R3 R3a "r3E R4 R R4 X Y xxrv-12-i Et H H H Et H H F OH XXIV-12-2 Et H H CH3 Et H H F OH XXIV-12-3 Et H H CH(CH3)2 Et H H F OH XXIV-12-4 Et H H CH2CH(CH3)2 Et H H F OH XXIV-12-5 Et H H CH2Ph Et H H F OH XXIV-12-6 Et H H CH2-indot-3-yl Et H H F OH XXIV-12-7 Et H H. CH2CH2SCH3 Et H H F OH XXIV-12-8 Et * H * Et H H F OH 5 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXIV-13.

Ns R R3 R3· R3b R4 R5 R4 X Y XXIV-13-1 iPr H H H Et H H F OH XXIV-13-2 fpr H H ch3 Et Η H F OH XXIV-13-3 'Pr H H CHfCH^ Et H H F OH XXIV-13-4 'Pr H H CH^HfCH^ Et Η H F OH XXIV-13-5 'Pr H H CH2Ph Et H H F OH 2983472-1 -511- WO 2008/121634

Docket No. 60137.0034WOU 1 PCT/US2008/058183

Ha Rl R2 R3a TT “R5" R6 X Y XXIV-13-6 'Pr H H CH2-indol-3-yl Et H H F OH XXIV-13-7 'Pr H H CH2CH2SCH3 Et H H F OH XXrV-13-8 'Pr * H * Et H H F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXIV-14.

Ha R1 R2 r3. R3b R4 RJ R6 X Y XX1V-14-1 'Bu H H H Et H H F OH XXIV-14-2 'Bu H H CH3 Et H H F OH XXIV-14-3 'Bu H H CH(CH3)2 Et H H F OH XXIV-14-4 'Bu H H CH2CH(CH3)2 Et H H F OH XXIV-14-5 'Bu H H CH2Ph Et H H F OH XX1V-14-6 'Bu H H CH2-indol-3-yl Et H H F OH XXIV-14-7 feu H H CH2CH2SCH3 Et H H F OH XXIV-14-8 'Bu * H * Et H H F OH ♦R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXIV-15.

Ha R R2 RJa R3b Ir R5 X Y XXIV-15-1 Ph H H H Et H H F OH XXIV-15-2 Ph H H CH3 Et H H F OH XX1V-15-3 Ph H H CHCCHah Et H H F OH XXIV-15-4 Ph H H CH2CH(CH3)2 Et H H F OH XXIV-15-5 Ph H H CH2Ph Et H H F OH XXIV-15-6 Ph H H CH2-indol-3-yl Et H H F OH XXIV-15-7 Ph H H CH2CH2SCH3 Et H H F OH XXTV-15-8 Ph ♦ H ♦ Et H H F OH 5 *R2 and RJb joined together by (Cihfe to form five-membered ring.

Table XXIV-16.

Ha ' Rl R2 rj. R3b R4 R5 R6 X Y XXIV-16-1 p-Me-Ph H H H Et H H F OH XXIV-16-2 p-Me-Ph H H CH3 Et H H F OH XX1V-16-3 p-Me-Ph H H CH(CH3)2 Et H H F OH XXIV-16-4 p-Me-Ph H H CH2CH(CH3)2 Et H H F OH XXIV-16-5 p-Me-Ph H H CH2Ph Et H H F OH XXIV-16-6 p-Me-Ph H H CH2-indol-3-yl Et H H F OH 2983472-1 -512- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

X2 Rl R3 : r3« ' R36 “ ~r* Rs R5 X Y XXIV-16-7 p-Me-Ph H H CH2CH2SCH3 Et H H F OH XXIV-16-8 p-Me-Ph * H ♦ Et H H F OH *R2 and Rejoined together by (0¾¼ to form five-membered ring. Table XXIV-17. Rl R1 R3. R3b R4 R5 R6 X Y XXIV-17-1 p-F-Ph H H H Et H H F OH XXIV-17-2 p-F-Ph H H ch3 Et H H F OH XXIV-17-3 p-F-Ph H H CH(CH3)2 Et H H F OH XXIV-17-4 p-F-Ph H H CH2CH(CH3)2 Et H H F OH XXIV-17-5 p-F-Ph H H CH2Ph Et H H F OH XXIV-17-6 p-F-Ph H H CH2-indol-3-yl Et H H F OH XXIV-17-7 p-F-Ph H H CH2CH2SCH3 Et H H F OH XXIV-17-8 4^2 p-F-Ph * H * Et H H F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXIV-18.

Xs R1 R2 RSe “R35 R4 R’ R6 X Y XXIV-18-1 p-Cl-Ph H H H Et H H F OH XXIV-18-2 p-Cl-Ph H H CH3 Et H H F OH XXIV-18-3 p-Cl-Ph H H CH(CH3)i Et H H F OH XXIV-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H H F OH XXIV-18-5 p-Cl-Ph H H CH2Ph Et H H F OH XXIV-18-6 p-CI-Ph H H CH2-indol-3-yl Et H H F OH XXIV-18-7 p-Cl-Ph H H CH2CH2SCH3 Et H H F OH XXIV-18-8 p-Cl-Ph 1 · · J A * H * Et H H F OH *R2 and Rejoined together by (0¾¼ to form five-membered ring.

Table XXIV-19.

Xo R‘ ΊΓ R35" R4 RJ Rfc X Y XXIV-19-1 p-Br-Ph H H H Et H H F OH XXIV-19-2 p-Br-Ph H H ch3 Et H H F OH XXIV-19-3 p-Br-Ph H H CH(CH3)2 Et H H F OH XXIV-19-4 p-Br-Ph H H CH2CH(CH3)2 Et H H F OH XXIV-19-5 p-Br-Ph H H CH2Ph Et H H F OH XXIV-19-6 p-Br-Ph H H CH2-indol-3-yl Et H H F OH XXIV-19-7 p-Br-Ph H H CH2CH2SCH3 Et H H F OH 2983472-1 -513- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ns R‘ R3 R3a R3b R4 Rs R6 X Y XXIV-19-8 p-Br-Ph * H * Et H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. Table XXIV-20. Ns R1 RJ RJa R* R R5 R® X Y XXIV-20-1 p-I-Ph H H H Et H H F OH XXIV-20-2 p-I-Ph H H ch3 Et H H F OH XXIV-20-3 p-I-Ph H H CH(CH3)2 Et H H F OH XXIV-20-4 p-I-Ph H H CH2CH(CH3)2 Et H H F OH XXTV-20-5 p-I-Ph H H CH2Ph Et H H F OH XXIV-20-6 p-I-Ph H H CH2-indol-3-yl Et H H F OH XXIV-20-7 p-I-Ph H H CH2CH2SCH3 Et H H F OH XXIV-20-8 '7^2 '.”^ 3 b p-I-Ph * H * Et H H F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXIV-21.

Ns R1 R3 R3e R3b R4 R5" R6 X Y XXIV-21-1 ch3 H H H H H F OH XXIV-21-2 ch3 Η H CH3 'Pr H H F OH XXIV-21-3 ch3 H H CH(CH3)2 'Pr H H F OH XXIV-21-4 ch3 H H CH2CH(CH3)2 'Pr H H F OH XXIV-21-5 ch3 H H CH2Ph /pr H H F OH XXIV-21-6 ch3 H H CH2-indol-3-yl 'Pr H H F OH XXIV-21-7 ch3 H H CH2CH2SCH3 'Pr H H F OH XX1V-21-8 ch3 * H * fpr H H F OH 5 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXIV-22.

Ns R1 R2 “r35" R3b R4 R3 R6 X Y XXIV-22-1 Et H H H "W H H F OH xxrv-22-2 Et H H CH3 'Pr H H F OH XXIV-22-3 Et H H CH(CH3)2 'Pr H H F OH XXIV-22-4 Et H H CH2CH(CH3)2 'Pr H H F OH XXIV-22-5 Et H H CH2Ph 'Pr H H F OH XXIV-22-6 Et H H CH2-indol-3-yl Tr H H F OH XXIV-22-7 Et H H ch2ch2sch3 'Pr Η H F OH XXIV-22-8 Et * H ♦ 'Pr H H F OH 2983472-1 - 514 - WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 *R2 and R3b joined together by (C 112)3 to form five-membered ring.

Table XXIV-23.

Ns R1 TF“ R3‘ “R* R4 R5" R6 X Y XXIV-23-1 'Pr H H H 'Pr H H F OH XXIV-23-2 'Pr H H ch3 'Pr H H F OH XXIV-23-3 'Pr H H CH(CH3)2 'Pr H H F OH XXIV-23-4 'Pr H H CH2CH(CH3)2 'Pr H H F OH XX1V-23-5 'Pr H H CH2Ph 'Pr H H F OH XXIV-23-6 'Pr H H CH2-indol-3-yl 'Pr H H F OH XXIV-23-7 fpr H H ch2ch2sch3 'Pr H H F OH XXIV-23-8 .....'7772 "“"."WJb'' 'Pr * H * 'Pr H H F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXIV-24.

Ns R1 R2 r3‘ "R36 R4 RJ R6 X Y XXTV-24-1 TkT H H H ΎΓ H H F OH XXIV-24-2 'Bu H H ch3 'Pr H H F OH XXIV-24-3 'Bu H H CHiCHah 'Pr H H F OH XXIV-24-4 'Bu H H CH2CH(CH3)3 'Pr H H F OH XXIV-24-5 'Bu H H CH2Ph 'Pr H H F OH XXIV-24-6 'Bu H H CH2-indol-3-yl 'Pr H H F OH XXIV-24-7 'Bu H H CH2CH2SCH3 'Pr H H F OH XXIV-24-8 jTTJF 'Bu * H ♦ 'Pr H H F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXIV-25.

Ns Rl R2 R R3b R4 IF R6 X Y XXIV-25-1 Ph H H H JPr H H F OH XXIV-25-2 Ph H H ch3 'Pr H H F OH XXIV-25-3 Ph H H CHiCHa), 'Pr H H F OH XXIV-25-4 Ph H H CH2CH(CH3)2 'Pr H H F OH XXIV-25-5 Ph H H CH2Ph 'Pr H H F OH XXIV-25-6 Ph H H CH2-indol-3-yl 'Pr H H F OH XXIV-25-7 Ph H H CH2CH2SCH3 'Pr H H F OH XX1V-25-8 Ph * H * 'Pr H H F OH *R2 and Rjb joined together by (CH2)3 to form five-membered ring. 2983472-1 -515- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXIV-26.

Ns R1 R2 -jpr R3b “I?" RJ R6 X Y XXIV-26-1 p-Me-Ph H H H 'Pr H H F OH XXIV-26-2 p-Me-Ph H H ch3 'Pr H H F OH XXIV-26-3 p-Me-Ph H H CH(CH3)2 'Pr H H F OH XX1V-26-4 p-Me-Ph H H CH2CH(CH3)2 Tr H H F OH XXTV-26-5 p-Me-Ph H H CH2Ph 'Pr H H F OH XX1V-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr H H F OH XXIV-26-7 p-Me-Ph H H CH2CH2SCH3 'Pr H H F OH XXIV-26-8 p-Me-Ph 4 H ♦ 'Pr H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring

Table XXIV-27.

Ns R1 R37 “r35 R4 Rs R6 X Y XXIV-27-1 p-F-Ph H H H "W H H F OH XXIV-27-2 p-F-Ph H H ch3 'Pr H H F OH XXIV-27-3 p-F-Ph H H CH(CH3)2 'Pr H H F OH XXTV-27-4 p-F-Ph H H CH2CH(CH3)j Tr H H F OH XXTV-27-5 p-F-Ph H H CH2Ph 'Pr H H F OH XXIV-27-6 p-F-Ph H H CH2-indol-3-yl Tr H H F OH XXIV-27-7 p-F-Ph H H CH2CH2SCH3 'Pr H H F OH XXTV-27-8 p-F-Ph ♦ H ♦ 'Pr H H F OH ♦R* and R3b joined together by (CHafc to form five-membered ring. 5 Table XXIV-28. ' I H ' '3^ L-IL " J "Γ

Ns R‘ R2 R3* R3” R4 R6 X Y XXIV-28-1 p-Cl-Ph H H H JPr H H F OH XXIV-28-2 p-Cl-Ph H H CH3 'Pr H H F OH XXIV-28-3 p-Cl-Ph H H CH(CH3)2 'Pr H H F OH XXIV-28-4 p-Cl-Ph H H CH2CH(CH3)2 Tr H H F OH XXTV-28-5 p-Cl-Ph H H CH2Ph 'Pr H H F OH XXIV-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr H H F OH XXIV-28-7 p-CI-Ph H H CH2CH2SCH3 'Pr H H F OH XXIV-28-8 ~ϊπ2- p-CI-Ph * H * 'Pr H H F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -516- WO 2008/121634

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Table XXIV-29.

Ns R1 R3a R4 R5 X Y XXIV-29-1 p-Br-Ph H H H JPr H H F OH XXIV-29-2 p-Br-Ph H H ch3 'Pr H H F OH XXIV-29-3 p-Br-Ph H H CH(CH3)2 'Pr H H F OH XXIV-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr H H F OH XXIV-29-5 p-Br-Ph H H CH2Ph 'Pr H H F OH XXIV-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr H H F OH XXIV-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr H H F OH XXIV-29-8 p-Br-Ph * H * 'Pr H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXIV-30.

Ns R1 Rz RJa R3b R5 R6 X Y XXIV-30-1 p-I-Ph H H H 'Pr H H F OH XXIV-30-2 p-I-Ph H H ch3 'Pr H H F OH XXTV-30-3 p-I-Ph H H CH(CH3)2 'Pr H H F OH XXIV-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr H H F OH XXIV-30-5 p-I-Ph H H CH2Ph 'Pr H H F OH XXIV-30-6 p-I-Ph H H CH2-indol-3-yl Tr H H F OH XXIV-30-7 p-I-Ph H H CH2CH2SCH3 'Pr H H F OH XXIV-30-8 p-I-Ph ♦ H ♦ 'Pr H H F OH ♦R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XXIV-31. ....."i-n "1 :—- 1'' ’j- ,.. *

Ns R1 RJ Rj. R3b iC Rs R6 X Y XXIV-31-1 ch3 H H H "Bu H H F OH XXIV-31-2 ch3 H H CH3 "Bu H H F OH XXIV-31-3 ch3 H H CH(CH3)2 "Bu H H F OH XX1V-31-4 ch3 H H CH2CH(CH3)2 "Bu H H F· OH XXIV-31-5 ch3 H H CH2Ph "Bu H H F OH XXIV-31-6 ch3 H H CH2-indol-3-yl “Bu H H F OH XXIV-31-7 ch3 H H CH2CH2SCH3 "Bu H H F OH XXIV-31-8 ch3 * H * “Bu H H F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -517-. WO 2008/121634

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Table XXIV-32.

Ns R1 RJ T5" TT” R5 "F" X Y XXIV-32-1 Et H H H "Bu H H F OH XXIV-32-2 Et H H ch3 "Bu H H F OH XXIV-32-3 Et H H CH(CH3)2 "Bu H H F OH XXIV-32-4 Et H H CH2CH(CH3)2 "Bu H H F OH XXIV-32-5 Et H H CH2Ph "Bu H H F OH XXIV-32-6 Et H H CH2-indol-3-yl "Bu H H F OH XXIV-32-7 Et H H CH2CH2SCH3 "Bu H H F OH XXIV-32-8 Et * H * "Bu H H F OH *R2 and R2b joined together by (Cl-hb to form five-membered ring.

Table XXIV-33.

Ns R1 R3" -jpB R4 Rs R6 X Y XXTV-33-1 'Pr H H H "Bu H H F OH XXIV-33-2 'Pr H H CH3 "Bu H H F OH XXIV-33-3 'Pr H H CH(CH3)2 "Bu H H F OH XXIV-33-4 'Pr H H CH2CH(CH3)2 "Bu H H F OH XXIV-33-5 'Pr H H CH2Ph "Bu H H F OH XXIV-33-6 'Pr H H CH2-indol-3-yl "Bu H H F OH XXIV-33-7 'Pr H H CH2CH2SCH3 "Bu H H F OH XXIV-33-8 'Pr * H ♦ "Bu H H F OH *R2 and RJd joined together by (CH2)3 to form five-membered ring.

Table XXIV-34.

Ns R1 R3· "r35 R4 R5 R4 X Y XXIV-34-1 "W H H H "Bu H H F OH XXIV-34-2 *Bu H H ch3 "Bu H H F OH XXIV-34-3 'Bu H H CH(CH3)2 "Bu H H F OH XXIV-34-4 'Bu H H CH2CH(CH3)2 "Bu H H F OH XXIV-34-5 'Bu H H CH2Ph "Bu H H F OH XXIV-34-6 'Bu H H CH2-indol-3-yl "Bu H H F OH XXIV-34-7 'Bu H H CH2CH2SCH3 "Bu H H F OH XXTV-34-8 “^772- teii ί · ! * H * "Bu H H F OH ♦R2 and R3b joined together by (CHab to form five-membered ring. 2983472-1 -518- WO 2008/121634 . Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXIV-35.

X2 R1 R2 -pr R3b R4 R5 R6 X Y XXIV-35-1 Ph H H H "Bu H H F OH XXIV-35-2 Ph H H ch3 "Bu H H F OH XXIV-35-3 Ph H H CH(CH3)2 "Bu H H F OH XXIV-35-4 Ph H H CH2CH(CH3)2 "Bu H H F OH XXIV-35-5 Ph H H CH2Ph "Bu H H F OH XXIV-35-6 Ph H H CH2-indol-3-yl "Bu H H F OH XXIV-35-7 Ph H H CH2CH2SCH3 "Bu H H F OH XXIV-35-8 Ph * H ♦ "Bu H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XX1V-36.

Ns “r1 RJ R3’ “r35 R* R6 X Y XXIV-36-1 p-Me-Ph H H H "Bu H H F OH XXIV-36-2 p-Me-Ph H H ch3 "Bu H H F OH XXIV-36-3 p-Me-Ph H H CH(CH3)2 "Bu H H F OH XXIV-36-4 p-Me-Ph H H ΟΗ2ΟΗ(ΟΗ3)2 "Bu H H F OH XXIV-36-5 p-Me-Ph H H CH2Ph "Bu H H F OH XXIV-36-6 p-Me-Ph H H CH2-indol-3-y1 "Bu H H F OH XXIV-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu H H F OH XXIV-36-8 p-Me-Ph * H ♦ "Bu H H F OH *RZ and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XXIV-37. "..... - . ' "..J !2"l" 2

Xs R' R2 R3a R3b R4 R5 R6 X Y XXIV-37-1 p-F-Ph H H H "Bu H H F OH XXIV-37-2 p-F-Ph H H ch3 "Bu H H F OH XXIV-37-3 p-F-Ph H H CHCCH^ "Bu H H F OH XXIV-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu H H F OH XXIV-37-5 p-F-Ph H H CHzPh "Bu H H F OH XXIV-37-6 p-F-Ph H H CH2-indol-3-yl "Bu H H F OH XXIV-37-7 p-F-Ph H H CH2CH2SCH3 "Bu H H F OH XXIV-37-8 p-F-Ph * H * "Bu H H F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -519- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXIV-38.

Ns "R1- R2 R3’ "r35 R4 R5 R6 X Y XXIV-38-1 p-Cl-Ph H H H "Bii H H F OH XXIV-38-2 p-Cl-Ph H H ch3 "Bu H H F OH XXIV-38-3 p-Cl-Ph H H CH(CH3)2 "Bu H H F OH XXIV-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H H F OH XXIV-38-5 p-Cl-Ph H H CH2Ph "Bu H H F OH XXIV-38-6 p-Cl-Ph H H CH2-indol-3-yl MBu H H F OH XXIV-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu H H F OH XXIV-38-8 p-Ci-Ph * H * "Bu H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXIV-39.

Ns R1 R2 R3b R4 R3 R6 X Y XXTV-39-1 p-Br-Ph H H H "Bu H H F OH XX1V-39-2 p-Br-Ph H H ch3 "Bu H H F OH XXIV-39-3 p-Br-Ph H H CH(CH3)2 ”Bu H H F OH XX1V-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu H H F OH XXIV-39-5 p-Br-Ph H H CH2Ph "Bu H H F OH XXIV-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu H H F OH XXIV-39-7 p-Br-Ph H H CH2CH2SCH3 "Bu H H F OH XXTV-39-8 p-Br-Ph * H * "Bu H H F OH *R2 and Rejoined together by (Cihb to form five-membered ring. 5 Table XXIV-40. 1 ..... 1·——»^ -- J . , J .

Ns R1 R2 r3· R3b R4 Rs R6 X Y XXIV-40-1 p-l-Ph H H H "Bu H H F OH XXIV-40-2 p-I-Ph H H CH3 "Bu H H F OH XXIV-40-3 p-I-Ph H H CH(CH3)2 "Bu H H F OH XXIV-40-4 p-l-Ph H H CH2CH(CH3)2 "Bu H H F OH XXIV-40-5 p-I-Ph H H CH2Ph "Bu H H F OH XXIV-40-6 p-I-Ph H H CH2-indol-3-yl "Bu H H F OH XXIV-40-7 p-I-Ph H H CH2CH2SCH3 "Bu H H F OH XXIV-40-8 ΤΓ72 j n3b p-I-Ph * H * "Bu H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -520- WO 2008/121634

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Table XXIV-41.

Ns Rl r! R3a R4 R5 R6 X Y XXIV-41-1 ch3 H H H Bz H H F OH XXIV-41-2 ch3 H H ch3 Bz H H F OH XXTV-41-3 ch3 H H CH(CH3)2 Bz H H F OH XXIV-41-4 ch3 H H CH2CH(CH3)2 Bz H H F OH XX1V-41-5 ch3 H H CH2Ph Bz H H F OH XXIV-41-6 ch3 H H CH2-mdol-3-yl Bz H H F OH XXIV-41-7 ch3 H H CH2CH2SCH3 Bz H H F OH XXIV-41-8 ch3 * H * Bz H H F OH *R2 and Rejoined together by (CFfeb to form five-membered ring.

Table XX1V-42.

N° R1 R2 R3· R3b R4 Rs R6 X Y XX1V-42-1 Et H H H Bz H H F OH XXIV-42-2 Et H H CH3 Bz H H F OH XX TV-42-3 Et H H CH(CH3)2 Bz H H F OH XXIV-42-4 Et H H CH2CH(CH3)2 Bz H H F OH XXTV-42-5 Et H H CH2Ph Bz H H F OH XXIV-42-6 Et H H CH2-indol-3-yl Bz H H F OH XXTV-42-7 Et H H CH2CH2SCH3 Bz H H F OH XXIV-42-8 Et * H * Bz H H F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XXIV-43. I . HL 1 1 1 "T!'.

Xs R RJ< R3b R4 R3 R6 X Y XXIV-43-1 »pr H H H Bz H H F OH XXIV-43-2 'Pr H H CH3 Bz H H F OH XXIV-43-3 'Pr H H CH(CH3)2 Bz H H F OH XXIV-43-4 'Pr H H CH2CH(CH3)2 Bz H H F OH XXIV-43-5 /pr H H CH2Ph Bz H H F OH XXIV-43-6 'Pr H H CH2-indol-3-yl Bz H H F OH XXIV-43-7 'Pr H H CH2CH2SCH3 Bz H H F d#i XXIV-43-8 'Pr * H * Bz H H F OH ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-t - 521 - WO 2008/121634

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Table XXIV-44.

Xs R1 R2 R3" R3b R4 Rs R4 X Y XXIV-44-1 'Bu H H H Bz H H F OH XXIV-44-2 'Bu H H ch3 Bz H H F OH XXIV-44-3 'Bu H H CH(CH3)2 Bz H H F OH XXTV-44-4 'Bu H H CH2CH(CH3)2 Bz H H F OH XXIV-44-5 ^u H H CH2Ph Bz H H F OH XXIV-44-6 'Bu H H CH2-indol-3-yl Bz H H F OH XXTV-44-7 'Bu H H CH2CH2SCH3 Bz H H F OH XXIV-44-8 'Bu * H * Bz H H F OH *R2 and Rib joined together by (CH2)3 to form five-membered ring.

Table XXI V-45.

Xa R R2 r3. r30 R4 Rs R6 X Y XXIV-45-1 Ph H H H Bz H H F OH XXTV-45-2 Ph H H ch3 Bz H H F OH XXIV-45-3 Ph H H CH(CH3)2 Bz H H F OH XXIV-45-4 Ph H H ΟΗ2ΟΗ(ΟΗ3)2 Bz H H F OH XXTV-45-5 Ph H H CH2Ph Bz .H H F OH XXIV-4 5-6 Ph H H CHrindol-3-yl Bz H H F OH XXIV-45-7 Ph H H CH2CH2SCH3 Bz H H F OH XXIV-45-8 Ph ♦ H * Bz H H F OH ♦R2 and R30 joined together by (CH2)3 to form five-membered ring. 5 Table XXIV-46. ---- 1 ’ i - ‘—11^- -wr-' J 'a-. ’Z ' -—..........

Xa R' R2 RJ‘ Rib r4- Rs R4 X Y XXIV-46-1 p-Me-Ph H H H Bz H H F OH XXIV-46-2 p-Me-Ph H H ch3 Bz H H F OH XXIV-46-3 p-Me-Ph H H CHtCHjh Bz H H F OH XXIV-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz H H F OH XXIV-46-5 p-Me-Ph H H CH2Ph Bz H H F OH XXIV-46'6 p-Me-Ph H H CH2-indol-3-yl Bz H H F OH XXIV-46-7 p-Me-Ph H H CH2CH2SCH3 Bz H H F OH XXIV-46-8 p-Me-Ph * H * Bz H H F OH *R2 and Rejoined together by (CHjjb to form five-membered ring. 2983472-1 -522- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXIV-47.

R‘ R3 Rj" R3b R4 Rs R6 X Y XXTV-47-1 p-F-Ph H H H Bz H H F OH XXIV-47-2 p-F-Ph H H ch3 Bz H H F OH XXTV-47-3 p-F-Ph H H CH(CH3)2 Bz H H F OH XXIV-47-4 p-F-Ph H H CH2CH(CH3)2 Bz H H F OH XXIV-47-5 p-F-Ph H H CH2Ph Bz H H F OH XXIV-47-6 p-F-Ph H H CH2-indol-3-yl Bz H H F OH XXIV-47-7 p-F-Ph H H CH2CH2SCH3 Bz H H F OH XXIV-47-8 p-F-Ph 4 H * Bz H H F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXIV-48.

Xs R1 Ra R“ R3b R4 Rs R6 X Y XXIV-48-1 p-Cl-Ph H H H Bz H H F OH XXIV-48-2 p-Cl-Ph H H ch3 Bz H H F OH XXIV-48-3 p-Cl-Ph H H CHCCH,), Bz H H F OH XXIV-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H H F OH XXIV-48-5 p-Cl-Ph H H CH2Ph Bz H H F OH XXIV-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz H H F OH XXTV-48-7 p-Cl-Ph H H CH2CH2SCH3 Bz H H F OH XXIV-48-8 p-Cl-Ph * H * Bz H H F OH *R2 and R3b joined together by (0¾¼ to form five-membered ring. 5 Table XXIV-49. ' « - I II 2 1 2 *"""

X° R1 R1 Rj. R3b R4 R5 R6 X Y XXIV-49-1 p-Br-Ph H H H Bz H H F OH XXIV-49-2 p-Br-Ph H H CH3 Bz H H F OH XXIV-49-3 p-Br-Ph H H CHiCH,), Bz H H F OH xxrv-49-4 p-Br-Ph H H CHjCHCCHj), Bz H H F OH XXTV-49-5 p-Br-Ph H H CH2Ph Bz H H F OH XXTV-49-6 p-Br-Ph H H CH2-indol-3-yl Bz H H F OH XXIV-49-7 p-Br-Ph H H CH2CH2SCH3 Bz H H F OH XXIV-49-8 p-Br-Ph * H 4 Bz H H F OH *R2 and RJt> joined together by (CH^ to form five-membered ring. 2983472-) -523- WO 2008/121634

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Table XXIV-50.

X° R1 ΊΓ Rja R3b R4 R* R6 X Y XXIV-50-1 p-l-Ph H H H Bz H H F OH XXIV-50-2 p-I-Ph H H ch3 Bz H H F OH XXIV-50-3 p-I-Ph H H CH(CH3)2 Bz H H F OH XXIV-50-4 p-I-Ph H H CH2CH(CH3)2 Bz H H F OH XXIV-50-5 p-I-Ph H H CH2Ph Bz H H F OH XXIV-50-6 p-I-Ph H H CH2-indol-3-yt Bz H H F OH XXIV-50-7 p-I-Ph H H CH2CH2SCH3 Bz H H F OH XXIV-50-8 p-I-Ph * H * Bz H H F OH *R2 and Rejoined together by (CThbt0 form five-membered ring.

XXV

Table XXV-1.

Xs R1 R3 r3. R3b R4 r! R6 X Y XXV-l-I ch3 H H H ch3 H ch3 F OH XXV-1-2 ch3 H H ch3 ch3 H ch3 F OH XXV-1-3 ch3 H H CH(CH3)2 ch3 H ch3 F OH XXV-1-4 ch3 H H CH2CH(CH3)2 ch3 H ch3 F OH XXV-1-5 ch3 H H CH2Ph ch3 H ch3 F OH XXV-1-6 ch3 H H CH2-indol-3-yl ch3 H ch3 F OH XXV-1-7 ch3 H H CH2CH2SCH3 ch3 H ch3 F OH XXV-1-8 ch3 * H * ch3 H ch3 F OH *R2 and Rejoined together by (CHbfc to form five-membered ring. 2983472-1 -524- WO 2008/121634

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Table XXV-2.

Ns R1 R3’ -pg R4 Rs R6 X Y XXV-2-1 Et H H H ch3 H ch3 F OH XXV-2-2 Et H H ch3 ch3 H ch3 F OH XXV-2-3 Et H H CH(CH3)2 ch3 H ch3 F OH XXV-2-4 Et H H CH2CH(CH3)2 ch3 H ch3 F OH XXV-2-5 Et H H CH2Ph ch3 H ch3 F OH XXV-2-6 Et H H CH2-indol-3-yl ch3 H ch3 F OH XXV-2-7 Et H H CH2CH2SCH3 ch3 H ch3 F OH XXV-2-8 Et * H ♦ ch3 H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXV-3.

Ns R1 R2 r3i R3b R4 R5 R6 X Y XXV-3-1 'Pr H H H ch3 H CH3 F OH XXV-3-2 'Pr H H ch3 ch3 Η ch3 F OH XXV-3-3 Zpr H H CH(CH3)2 ch3 H ch3 F OH XXV-3-4 'Pr H H CH2CH(CH3)2 ch3 H ch3 F OH XXV-3-5 'Pr H H CH2Ph ch3 H ch3 F OH XXV-3-6 'Pr H H CH2-indol-3-yl ch3 H ch3 F OH XXV-3-7 'Pr H H CH2CH2SCH3 ch3 H ch3 F OH XXV-3-8 'Pr ♦ H ♦ ch3 H ch3 F OH *R2 and RJb joined together by (ΟΗ2)3 to form five-membered ring. 5 Table XXV-4. " «I n ΊΙΤ — I. - a “

Ns · R R3 R3" R3b R4 R3 Rfr X Y XXV-4-1 'Bu H H Η CH3 Η CH3 F OH XXV-4-2 'Bu H H CH3 ch3 H ch3 F OH XXV-4-3 'Bu H H CH(CH3)j ch3 H ch3 F OH XXV-4-4 'Bu H H CH2CH(CH3)2 ch3 H ch3 F OH XXV-4-5 'Bu H H CH2Ph ch3 H ch3 F OH XXV-4-6 'Bu H Η CH2-indol-3-yl ch3 H ch3 F OH XXV-4-7 'Bu H Η CH2CH2SCH3 ch3 H ch3 F OH XXV-4-8 'Bu * Η * ch3 H ch3 F OH ♦R2 and RJ6 joined together by (CH2)3 to form five-membered ring. 2983472-1 -525- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXV-5.

Ns R1 R2 R3s R3b R4 R5 R6 X Y XXV-5-1 Ph H H H ch3 H ch3 F OH XXV-5-2 Ph H H ch3 ch3 H ch3 F OH XXV-5-3 Ph H H CH(CH3), ch3 H ch3 F OH XXV-5-4 Ph H H CH2CH(CH3)2 ch3 H ch3 F OH XXV-5-5 Ph H H CH2Ph ch3 H ch3 F OH XXV-5-6 Ph H H CH2-indol-3-yl cfi3 H ch3 F OH XXV-5-7 Ph H H CH2CH2SCH3 ch3 H ch3 F OH XXV-5-8 Ph * H * ch3 H ch3 F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXV-6.

Ns R’ R5r R3b R4 RJ R6 X Y XXV-6-1 p-Me-Ph H H H ch3 H CH3 F OH XXV-6-2 p-Me-Ph H H ch3 ch3 Η ch3 F OH XXV-6-3 p-Me-Ph H H CH(CH3)2 ch3 H ch3 F OH XXV-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 H ch3 F OH XXV-6-5 p-Me-Ph H H CH2Ph ch3 H ch3 F OH XXV-6-6 p-Me-Ph H H CH2-indol-3-yl ch3 H ch3 F OH XXV-6-7 p-Me-Ph H H ch2ch2sch3 ch3 H ch3 F OH XXV-6-8 p-Me-Ph ♦ H * ch3 H ch3 F OH *R2 and R36 joined together by (Cl-hb to form five-membered ring. 5 Table XXV-7. I R. ' "*IL ' I ‘ "2'

Ns R’ R2 r3. R3b R4 R5 R6 X Y XXV-7-1 p-F-Ph H H H ch3 H CH3 F OH XXV-7-2 p-F-Ph H H ch3 ch3 H ch3 F OH XXV-7-3 p-F-Ph H H CH(CH3)2 ch3 H ch3 F OH XXV-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 H ch3 F OH XXV-7-6 p-F-Ph H H CH2Ph ch3 H ch3 F OH XXV-7-7 p-F-Ph H H CH2-indol-3-yl ch3 H ch3 F OH XXV-7-8 p-F-Ph H H ch2ch2sch3 CH3 H ch3 F OH XXV-7-20 “^772-TTt p-F-Ph 3b : * . j 4 * H * ch3 H ch3 F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -526- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXV-8.

Xs Rl R1 RJ. R3b R4 R6 X Y XXV-8-1 p-Cl-Ph H H H ch3 H ch3 F OH XXV-8-2 p-Cl-Ph H H ch3 ch3 H ch3 F OH XXV-8-3 p-CI-Ph H H CH(CH3)2 ch3 H ch3 F OH XXV-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 H ch3 F OH XXV-8-5 p-Cl-Ph H H CH2Ph ch3 H ch3 F OH XXV-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 H ch3 F OH XXV-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 H ch3 F OH XXV-8-8 p-Cl-Ph * H ♦ ch3 H ch3 F OH ♦R* and R3b joined together by (CH2)3 to form five-membered ring.

Table XXV-9.

Ns R1 R2 r3. R35 R4 R5 R6 X Y XXV-9-1 p-Br-Ph H H H ch3 H ch3 F OH XXV-9-2 p-Br-Ph H H ch3 ch3 H ch3 F OH XXV-9-3 p-Br-Ph H H CH(CH3)2 ch3 H ch3 F OH XXV-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 H ch3 F OH XXV-9-6 p-Br-Ph H H CH2Ph ch3 H ch3 F OH XXV-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 H ch3 F OH XXV-9-8 p-Br-Ph H H ch2ch2sch3 ch3 H ch3 F OH XXV-9-20 p-Br-Ph * H * ch3 H ch3 F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXV-10. '''r i « n " .it . g - ,.i

Xs R1 R3 R3. R3b R4 R5 R&amp; X Y XXV-10-1 p-I-Ph H H H CH3 H ch3 F OH XXV-10-2 p-I-Ph H H CH3 ch3 H ch3 F OH XXV-10-3 p-I-Ph H H CH(CH3)2 ch3 H ch3 F OH XXV-10-4 p-I-Ph H H CH2CH(CH3)2 ch3 H ch3 F OH XXV-10-5 p-I-Ph H H CH2Ph ch3 H ch3 F OH XXV-10-6 p-I-Ph H H CH2-indol-3-yl ch3 H ch3 F OH XXV-10-7 p-I-Ph H H CH2CH2SCH3 ch3 H ch3 F OH XXV-10-8 . J τι j p-I-Ph b= · "7Γ * H * ch3 H ch3 F OH *R4 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -527- WO 2008/121634

Docket No. 6O137.O034WOU1 PCT/US2008/058183

Table XXV-il.

Xs R* R2 RJa R3b R4 Rs R6 X Y XXV-11-1 ch3 H H H Et H ch3 F OH XXV-11-2 ch3 H H ch3 Et H ch3 F OH XXV-11-3 ch3 H H CH(CH3)2 Et H ch3 F OH XXV-11-4 ch3 H H CH2CH(CH3)2 Et H ch3 F OH XXV-11-5 ch3 H H CH2Ph Et H ch3 F OH XXV-11-6 ch3 H H CH2-indol-3-yl Et H ch3 F OH XXV-11-7 ch3 H H CH2CH2SCH3 Et H ch3 F OH XXV-11-8 ch3 * H * Et H ch3 F OH *R2 and Rejoined together by_(CH2)3 to form five-membered ring.

Table XXV-12.

Xs R' R2 R3‘ Rib RJ R4 X Y XXV-12-1 Et H H H Et H CH3 F OH XXV-12-2 Et H H ch3 Et H ch3 F OH XXV-I2-3 Et H H CH(CH3)2 Et H ch3 F OH XXV-12-4 Et H H CH2CH(CH3)2 Et H ch3 F OH XXV-12-5 Et H H CH2Ph Et H ch3 F OH XXV-12-6 Et H H CH2-indol-3-yl Et H ch3 F OH XXV-12-7 Et H H CH2CH2SCH3 Et H ch3 F OH XXV-12-8 :-/73 Et B777 * H * Et H ch3 F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Xs r’ R2 R3“ -r3F R4 R5 R4 X Y XXV-13-1 'Pr H H H Et H ch3 F OH XXV-13-2 ipr H H ch3 Et H ch3 F OH XXV-13-3 'Pr H H CH(CH3)i Et H ch3 F OH XXV-13-4 'Pr H H CH2CH(CH3)2 Et H ch3 F OH XXV-13-5 ipr H H CH2Ph Et H ch3 F OH XXV-13-6 'Pr H H CH2-indol-3-yl Et H ch3 F OH XXV-13-7 'Pr H H CH2CH2SCH3 Et H ch3 F OH XXV-13-8 -77? 'Pr JETT" * H * Et H ch3 F OH *RJ and RJb joined together by (CHj)3 to form five-membered ring. 2983472-1 -528- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXV-14.

Xa R1 R3 R3' R3b RJ R6 X Y XXV-14-1 'Bu H H H Et H ch3 F OH XXV-14-2 'Bu H H CHj Et H ch3 F OH XXV-14-3 'Bu H H CH(CH3)2 Et H ch3 F OH XXV-14-4 'Bu H H CH2CH(CH3)2 Et H ch3 F OH XXV-14-5 'Bu H H CH2Ph Et H ch3 F OH XXV-14-6 'Bu H H CH2-indol-3-yl Et H ch3 F OH XXV-14-7 'Bu H H ch2ch2sch3 Et H ch3 F OH XXV-14-8 'Bu * H * Et H ch3 F OH *R2 and R3b joined together by (ΟΗ2)3 to form five-membered ring.

Table XXV-15.

Xa R1 R2 R3a R3b 1?’ RJ R4 X Y XXV-15-1 Ph H H H Et H ch3 F OH XXV-15-2 Ph H H ch3 Et H ch3 F OH XXV-15-3 Ph H H CH(CH3)2 Et H ch3 F OH XXV-15-4 Ph H H CH2CH(CH3)2 Et H ch3 F OH XXV-15-5 Ph H H CH2Ph Et H ch3 F OH XXV-15-6 Ph H H CH2-indoI-3-yl Et H ch3 F OH XXV-15-7 Ph H H CH2CH2SCH3 Et H ch3 F OH XXV-15-8 atU „j n Ph 3b · * H ♦ Et H ch3 F OH ♦R2 and R30 joined together by (ΟΗ2)3 to form five-membered ring.

Table XXV-16.

Ns T- R3 r3“ "r^ R4 T" R4 X Y XXV-16-1 p-Me-Ph H H H Et H ch3 F OH XXV-16-2 p-Me-Ph H H ch3 Et H ch3 F OH XXV-16-3 p-Me-Ph H H CH(CH3)2 Et H ch3 F OH XXV-16-4 p-Me-Ph H H CH2CH(CH3)2 Et H ch3 F OH XXV-16-5 p-Me-Ph H H CH2Ph Et H ch3 F OH XXV-16-6 p-Me-Ph H H CH2-indol-3-yl Et H ch3 F OH XXV-16-7 p-Me-Ph H H CH2CH2SCH3 Et H ch3 F OH XXV-16-8 p-Me-Ph * H * Et H ch3 F OH *R2 and R3” joined together by (CH2)3 to form five-membered ring. 2983472-1 -529- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXV-17.

Tlik D 1

X2 R1 Ra R3a “F" Rs R6 X Y XXV-17-1 p-F-Ph H H H Et H ch3 F OH XXV-17-2 p-F-Ph H H ch3 Et H ch3 F OH XXV-17-3 p-F-Ph H H CH(CH3)2 Et H ch3 F OH XXV-17-4 p-F-Ph H H CH2CH(CH3)2 Et H ch3 F OH XXV-17-5 p-F-Ph H H CH2Ph Et H ch3 F OH XXV-17-6 p-F-Ph H H CH2-indol-3-yl Et H ch3 F OH XXV-17-7 p-F-Ph H H CH2CH2SCH3 Et H ch3 F OH XXV-17-8 p-F-Ph ♦ H * Et H ch3 F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXV-18.

Jfe Rl R2 R3a R3t> R4 R5 R’ X Y XXV-18-1 p-Cl-Ph H H H Et H ch3 F OH XXV-18-2 p-Cl-Ph H H ch3 Et H ch3 F OH XXV-18-3 p-Cl-Ph H H CH(CH3)2 Et H ch3 F OH XXV-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H ch3 F OH XXV-18-5 p-Cl-Ph H H CH2Ph Et H ch3 F OH XXV-18-6 p-Cl-Ph H H CH2-indol-3-yl Et H ch3 F OH XXV-18-7 p-Cl-Ph H H CH2CH2SCH3 Et H ch3 F OH XXV-18-8 p-Cl-Ph * H * Et H ch3 F OH *R2 and R31’joined together by (CH^ to form five-membered ring. 5 TabteXXV-19. — " ' >*I j 1

Xa R1 R2 R3a R3b R4 ΊΓ R6 X Y XXV-19-1 p-Br-Ph H H H Et H ch3 F OH XXV-19-2 p-Br-Ph H H ch3 Et H ch3 F OH XXV-19-3 p-Br-Ph H H CH(CH3)2 Et H ch3 F OH XXV-19-4 p-Br-Ph H H CH2CH(CH3)2 Et H ch3 F OH XXV-19-5 p-Br-Ph H H CH2Ph Et H ch3 F OH XXV-19-6 p-Br-Ph H H CH2-indol-3-yl Et H ch3 F OH XXV-19-7 p-Br-Ph H H ch2ch2sch3 Et H ch3 F OH XXV-19-8 p-Br-Ph * H * Et H ch3 F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -530- WO 2008/121634

Docket No. 60137.0034WOUI PCT/US2008/058183

Table XXV-20.

X® Rl r51" F - R4 ΊΓ R6 X Y XXV-20-1 p-I-Ph H H H Et H ch3 F OH XXV-20-2 p-I-Ph H H ch3 Et H ch3 F OH XXV-20-3 p-I-Ph H H CH(CH3)2 Et H ch3 F OH XXV-20-4 p-I-Ph H H CH2CH(CH3)2 Et H ch3 F OH XXV-20-5 p-I-Ph H H CH2Ph Et H ch3 F OH XXV-20-6 p-I-Ph H H CH2-indol-3-yl Et H cfi3 F OH XXV-20-7 p-I-Ph H H CH2CH2SCH3 Et H ch3 F OH XXV-20-8 p-I-Ph * H * Et H ch3 F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXV-21.

Xa R1 R2 R3a R3" I?' Rs R4 X Y XXV-21-1 ch3 Η Η Η JPr H CH3 F OH XXV-21-2 ch3 H Η ch3 'Pr H ch3 F OH XXV-21-3 ch3 H Η CH(CH3)2 'Pr H ch3 F OH XXV-21-4 ch3 Η Η CH2CH(CH3)2 'Pr H ch3 F OH XXV-21-5 ch3 Η Η CH2Ph 'Pr H ch3 F OH XXV-21-6 ch3 Η Η CH2-indol-3-yl 'Pr H ch3 F OH XXV-21-7 ch3 Η Η CH2CH2SCH3 'Pr H ch3 F OH XXV-21-8 ch3 * Η * 'Pr H ch3 F OH *R2 and Rejoined together by (CH2)3t0 f°rm five-membered ring. 5 Table XXV-22. I , II ^-»7 'HL ‘ """" 1..1 J---- . .......... "

Xa R1 R2 RJe R3b R4 R5 R6 X Υ XXV-22-1 Et H H H TV H ch3 F OH XXV-22-2 Et H H ch3 Tr H ch3 F OH XXV-22-3 Et H H CHiCHa), 'Pr H ch3 F OH XXV-22-4 Et H H ΟΗ2ΟΗ(ΟΗ3)ϊ 'Pr H ch3 F OH XXV-22-5 Et H H CH2Ph 'Pr H ch3 F OH XXV-22-6 Et H H CH2-indol-3-yl 'Pr H ch3 F OH XXV-22-7 Et H H CH2CH2SCH3 'Pr H ch3 F OH XXV-22-8 Et * H * 'Pr H ch3 F OH ♦R2 and Rejoined together by (OTafe to form five-membered ring. 2983472-1 -531 - WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXV-23.

Ns Rl R2 RJa R3b TT R5 R6 X Y XXV-23-1 'Pr H H H H ch3 F OH XXV-23-2 zPr H H ch3 'Pr H ch3 F OH XXV-23-3 ‘Pr H H CH(CH3)2 'Pr H ch3 F OH XXV-23-4 Tr H H CH2CH(CH3)2 'Pr H ch3 F OH XXV-23-5 ‘Pr H H CH2Ph 'Pr H ch3 F OH XXV-23-6 'Pr H H CHrindol-3-yl 'Pr H ch3 F OH XXV-23-7 'Pr H H CH2CH2SCH3 'Pr H ch3 F OH XXV-23-8 'Pr * H * 'Pr H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXV-24.

Ns Rl R2 IF" T5 “ IP" R3 R* X Y XXV-24-1 'Bu H H H 'Pr H ch3 F OH XXV-24-2 'Bu H H ch3 'Pr H ch3 F OH XXV-24-3 'Bu H H ΟΗ(ΟΗ3\ 'Pr H ch3 F OH XXV-24-4 'Bu H H CH2CH(CH3)2 'Pr H ch3 F OH XXV-24-5 'Bu H H CH2Ph 'Pr H ch3 F OH XXV-24-6 'Bu H H CH2-indol-3-yl 'Pr H ch3 F OH XXV-24-7 'Bu H H ch2ch2sch3 'Pr H ch3 F OH XXV-24-8 'Bu * H * 'Pr H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XXV-25.

’ I W— - — RL 1 J . I

Ns R R2 R3· R3b R4 R5 R6 X Y XXV-25-1 Ph H H H "W H ch3 F OH XXV-25-2 Ph H H ch3 'Pr H ch3 F OH XXV-25-3 Ph H H 0-1(0¾¼ Tr H ch3 F OH XXV-25-4 Ph H H ΟΗ2ΟΗ(ΟΗ3)2 'Pr H ch3 F OH XXV-25-5 Ph H H CH2Ph 'Pr H ch3 F OH XXV-25-6 Ph H H CH2-indol-3-yI Tr H ch3 F OH XXV-25-7 Ph H H CH2CH2SCH3 'Pr H ch3 F OH XXV-25-8 Ph * H * 'Pr H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -532- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXV-26.

Xa R1 r2" R30 "r" R4 R5 Rfc X Y XXV-26-1 p-Me-Ph H H H >Pr H ch3 F OH XXV-26-2 p-Me-Ph H H ch3 'Pr H ch3 F OH XXV-26-3 p-Me-Ph H H 0-1((¾ 'Pr H ch3 F OH XXV-26-4 p-Me-Ph H H CH2CH(CH3)2 'Pr H ch3 F OH XXV-26-5 p-Me-Ph H H CH2Ph 'Pr H ch3 F OH XXV-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr H ch3 F OH XXV-26-7 p-Me-Ph H H CH2CH2SCH3 'Pr H ch3 F OH XXV-26-8 p-Me-Ph * H * 'Pr H ch3 F OH *R2 and Rejoined together by (CH2)a to form five-membered ring.

Table XXV-27.

Xa R1 R2 RJa RJb R4 Rs R6 X Y XXV-27-1 p-F-Ph H H H 'Pr H ch3 F OH XXV-27-2 p-F-Ph H H CH3 'Pr H ch3 F OH XXV-27-3 p-F-Ph H H CH(CH3)2 'Pr H ch3 F OH XXV-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr H ch3 F OH XXV-27-5 p-F-Ph H H CH2Ph 'Pr H ch3 F OH XXV-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr H ch3 F OH XXV-27-7 p-F-Ph H H CH2CH2SCH3 'Pr H ch3 F OH XXV-27-8 -77Γ p-F-Ph —rz * H * 'Pr H ch3 F OH *R2 and Rejoined together by (CHak to form five-membered ring.

Xa R1 R2 ~r3T R3b R4 R! R® X Y XXV-28-1 p-Cl-Ph H H H 'Pr H ch3 F OH XXV-28-2 p-Cl-Ph Η H ch3 'Pr H ch3 F OH XXV-28-3 p-Cl-Ph H Η CH(CH3)2 'Pr Η ch3 F OH XXV-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr Η ch3 F OH XXV-28-5 p-Cl-Ph Η Η CH2Ph 'Pr Η ch3 F OH XXV-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr Η ch3 F OH XXV-28-7 p-Cl-Ph H H CH2CH2SCH3 'Pr Η ch3 F OH XXV-28-8 J n p-Cl-Ph 36"ΓΊ—ΤΤΣ * H * 'Pr Η ch3 F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -533- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOO 1

Table XXV-29.

Ns R1 R1 ηρτ "r35 R4 RJ R6 X Y XXV-29-1 p-Br-Ph H H H ;Pr H ch3 F OH XXV-29-2 p-Br-Ph H H ch3 'Pr H ch3 F OH XXV-29-3 p-Br-Ph H H CH(CH3)2 'Pr H ch3 F OH XXV-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr H ch3 F OH XXV-29-5 p-Br-Ph H H CH2Ph 'Pr H ch3 F OH XXV-29-6 p-Br-Ph H H CH2-indol-3-yi 'Pr H ch3 F OH XXV-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr H ch3 F OH XXV-29-8 p-Br-Ph * H * 'Pr H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXV-30.

Ns R1 R2 "r35 R4 R5 R6 X Y XXV-30-1 p-I-Ph H H H H CH3 F OH XXV-30-2 p-I-Ph H H CH3 'Pr H ch3 F OH XXV-30-3 p-I-Ph H H CHCCH,), 'Pr H ch3 F OH XXV-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr H ch3 F OH XXV-30-5 p-I-Ph H H CH2Ph 'Pr H ch3 F OH XXV-30-6 p-I-Ph H H CHrindol-3-yl 'Pr H ch3 F OH XXV-30-7 p-I-Ph H H CH2CH2SCH3 'Pr H ch3 F OH XXV-30-8 p-I-Ph * H * 'Pr H ch3 F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XXV-31. ... 'HL " J ' — » - —

Ns R R2 R38 R3b R‘ R5 R6 X Y XXV-31-1 CH3 H H H "Bu H ch3 F OH XXV-31-2 ch3 H H CH3 "Bu H ch3 F OH XXV-31-3 ch3 H H 011(0¾¼ "Bu H ch3 F OH XXV-31-4 ch3 H H CH2CH(CH3)2 "Bu H ch3 F OH XXV-31-5 ch3 H H CH2Ph "Bu H ch3 F OH XXV-31-6 ch3 H H CH2-indol-3-yl "Bu H ch3 F OH XXV-31-7 ch3 H H CH2CH2SCH3 "Bu H ch3 F OH XXV-31-8 -7τΓ3 ch3 * H * "Bu H ch3 F OH *Ri and Rejoined together by (0¾¼ to fonn five-membered ring. 2583472-1 -534- WO 2008/121634

Docket No. 60137.0034 WOU1 PCT/US2008/058183

Table XXV-32. D1

Ns R1 RJ R3a R3b R4 Rs R5 X Y XXV-32-1 Et H H H "Bu II ch3 F OH XXV-32-2 Et H H ch3 "Bu H ch3 F OH XXV-32-3 Et H H CH(CH3)2 "Bu H ch3 F OH XXV-32-4 Et H H CH2CH(CH3)2 "Bu H ch3 F OH XXV-32-5 Et H H CH2Ph "Bu H ch3 F OH XXV-32-6 Et H H CH2-indoi-3-yl "Bu H ch3 F OH XXV-32-7 Et H H CH2CH2SCH3 "Bu H ch3 F OH XXV-32-8 Et * H * "Bu H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXV-33.

Ns Rl "R7" R3a “r* R4 RJ R6 X Y XXV-33-1 'Pr H H H "Bu H CH3 F OH XXV-33-2 'Pr H H CH3 "Bu H ch3 F OH XXV-33-3 fpr H H CHCCHah "Bu H ch3 F OH XXV-33-4 'Pr H H CH2CH(CH3)2 "Bu H ch3 F OH XXV-33-5 'Pr H H CH2Ph "Bu H ch3 F OH XXV-33-6 'Pr H H CHrSndol-3-yl "Bu H ch3 F OH XXV-33-7 'Pr H H CH2CH2SCH3 "Bu H ch3 F OH XXV-33-8 'Pr ♦ H * "Bu H ch3 F OH *R2 and RJb joined together by (0¾¼ to form five-membered ring. 5 Table XXV-34. 11 - M ......... — ' . J > / , 1

Ns R R* R3t R3b R4 R5 R6 X Y XXV-34-1 ^Bu“ H H H "Bu H CH3 F OH XXV-34-2 *Bu H H ch3 "Bu H ch3 F OH XXV-34-3 'Bu H H ΟΗ(ΟΗ3)ϊ "Bu H ch3 F OH XXV-34-4 'Bu H H CH2CH(CH3)2 "Bu H ch3 F OH XXV-34-5 'Bu H H CH2Ph "Bu H ch3 F OH XXV-34-6 'Bu H H CH2-indol-3-yl "Bu H ch3 F OH XXV-34-7 'Bu H H CH2CH2SCH3 "Bu H ch3 F OH XXV-34-8 'Bu * H * "Bu H ch3 F OH *R2 and RJb joined together by to form five-membered ring? 2983472-1 -535- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXV-35.

Na Tc Rv "r* R4 R5 R6 X Y XXV-35-1 Ph H H H "Bu H ch3 F OH XXV-35-2 Ph H H ch3 "Bu H ch3 F OH XXV-35-3 Ph H H CH(CH3)2 "Bu H ch3 F OH XXV-35-4 Ph H H CH2CH(CH3)2 "Bu H ch3 F OH XXV-35-5 Ph H H CH2Ph "Bu H ch3 F OH XXV-35-6 Ph H H CH2-indol-3-yl "Bu H ch3 F OH XXV-35-7 Ph H H CH2CH2SCH3 "Bu H ch3 F OH XXV-35-8 -777 Ph 3b ; * H * "Bu H ch3 F OH *R2 and RJb joined together by (0¾¼ to form five-membered ring.

Table XXV-36,

Ns R1 Ί?“ R3« R3b R4 RJ IF” X Y XXV-36-1 p-Me-Ph H H H "Bu H CH3 F OH XXV-36-2 p-Me-Ph H H CH3 "Bu H ch3 F OH XXV-36-3 p-Me-Ph H H CH(CH3)2 "Bu H ch3 F OH XXV-36-4 p-Me-Ph H H CHjCHCCHjh "Bu H ch3 F OH XXV-36-5 p-Me-Ph H H CH2Ph "Bu H ch3 F OH XXV-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu H ch3 F OH XXV-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu H ch3 F OH XXV-36-8 p-Me-Ph * H * "Bu H ch3 F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XXV-37. 11 " M ' 1 ' H Ji- ~ RL ........ J '.’’I ' *

Na R' R3 R3. R3b rV R6 X Y XXV-37-1 p-F-Ph Η H H "Bu H ch3 F OH XXV-37-2 p-F-Ph H H ch3 "Bu Η ch3 F OH XXV-37-3 p-F-Ph H H CH(CH3)2 "Bu H ch3 F OH XXV-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu Η ch3 F OH XXV-37-5 p-F-Ph H H CH2Ph "Bu H ch3 F OH XXV-37-6 p-F-Ph H H CH2-indol-3-yl "Bu Η ch3 F OH XXV-37-7 p-F-Ph H H ch2ch2sch3 "Bu H ch3 F OH XXV-37-8 p-F-Ph * Η * "Bu H ch3 F OH *R2 and RJb joined together by (0¾^t0 form five-membered ring. 2983472-1 -536- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXV-38.

Xs Rl R3 R30 "R35 R4 ΊΓ R6 X Y XXV-38-1 p-CI-Ph H H H "Bu H ch3 F OH XXV-38-2 p-Cl-Ph H H ch3 "Bu H ch3 F OH XXV-38-3 p-Cl-Ph H H CH(CH3)2 "Bu H ch3 F OH XXV-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H ch3 F OH XXV-38-5 p-Cl-Ph H H CH2Ph "Bu H ch3 F OH XXV-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu H ch3 F OH XXV-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu H ch3 F OH XXV-38-8 p-CI-Ph * H * "Bu H ch3 F OH *R2 and R3b joined together by (CFfeb to form five-membered ring.

Table XXV-39.

X° R1 R3 R3’ R3b R4 Rs R6 X Y XXV-39-1 p-Br-Ph H H H "Bu H ch3 F OH XXV-39-2 p-Br-Ph H H ch3 "Bu H ch3 F OH XXV-39-3 p-Br-Ph H H CH(CH3)2 "Bu H ch3 F OH XXV-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu H ch3 F OH XXV-39-5 p-Br-Ph H H CH2Ph "Bu H ch3 F OH XXV-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu H ch3 F OH XXV-39-7 p-Br-Ph H H ch2ch2sch3 "Bu H ch3 F OH XXV-39-8 p-Br-Ph * H * "Bu H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XXV-40. „.R. .......... ......n· — J g *2 '

X° Rl R3 Rj. R3b R4 R3 R6 X Y XXV-40-1 p-I-Ph H H H "Bu H ch3 F OH XXV-40-2 p-I-Ph H H ch3 "Bu H ch3 F OH XXV-40-3 p-I-Ph H H CH(CH3)2 "Bu H ch3 F OH XXV-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu H ch3 F OH XXV-40-5 p-I-Ph H H CH2Ph "Bu H ch3 F OH XXV-40-6 p-I-Ph H H CH2-indol-3-yl "Bu H ch3 F OH XXV-40-7 p-I-Ph H H ch2ch2sch3 "Bu H ch3 F OH XXV-40-8 p-I-Ph * H * "Bu H ch3 F OH *RZ and RJb joined together by (CHjtJa to form five-membered ring. 2983472-1 -537 - WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXV-41.

Xa R1 R* -r33" R4 V R6 X Y XXV-41-1 ch3 H H H Bz H ch3 F OH XXV-41-2 ch3 H H ch3 Bz H ch3 F OH XXV-41-3 ch3 H H CH(CHj)j Bz H ch3 F OH XXV-41-4 ch3 H H CH2CH(CH3)2 Bz H ch3 F OH XXV-41-5 ch3 H H CH2Ph Bz H ch3 F OH XXV-41-6 ch3 H H CH2-indol-3-yl Bz H ch3 F OH XXV-41-7 ch3 H H CH2CH2SCH3 Bz H ch3 F OH XXV-41-8 ch3 * H * Bz H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXV-42.

Xs Ry R4 R3. R3b R4 RJ Rfc X Y XXV-42-1 Et H H H Bz H CH3 F OH XXV-42-2 Et H H ch3 Bz H ch3 F OH XXV-42-3 Et H H CH(CH3)2 Bz H ch3 F OH XXV-42-4 Et H H CH2CH(CH3)2 Bz H ch3 F OH XXV-42-5 Et H H CH2Ph Bz H ch3 F OH XXV-42-6 Et H H CH2-indol-3-yl Bz H ch3 F OH XXV-42-7 Et H H CH2CH2SCH3 Bz H ch3 F OH XXV-42-8 Et JSV7 * H ♦ Bz H ch3 F OH *R2 and RJ0 joined together by (CH2)3 to form five-membered ring.

Table XXV-43.

Xa TT Ra "r3T- R3b R4 RJ R4 X Y XXV-43-1 'Pr H H H Bz H ch3 F OH XXV-43-2 'Pr H H CH3 Bz H ch3 F OH XXV-43-3 'Pr H H CH(CH3)2 Bz H ch3 F OH XXV-43-4 'Pr H H CH2CH(CH3)2 Bz H ch3 F OH XXV-43-5 'Pr H H CH2Ph Bz H ch3 F OH XXV-43-6 /pr H H CH2-indol-3-yl Bz H ch3 F OH XXV-43-7 'Pr H H ch2ch2sch3 Bz H ch3 F ¢¢1 XXV-43-8 'Pr * H * Bz H ch3 F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -538 - WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXV-44.

Ns R1 R2 R3a R3b r R5 R6 X Y XXV-44-1 'Bu H H H Bz H ch3 F OH XXV-44-2 'Bu H H ch3 Bz H ch3 F OH XXV-44-3 'Bu H H CH(CH3)2 Bz H ch3 F OH XXV-44-4 'Bu H H CH2CH(CH3)2 Bz H ch3 F OH XXV-44-5 'Bu H H CH2Ph Bz H ch3 F OH XXV-44-6 'Bu H H CH2-indol-3?yl Bz H ch3 F OH XXV-44-7 'Bu H H CH2CH2SCH3 Bz H ch3 F OH XXV-44-8 'Bu * H 4 Bz H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXV-45.

Ns R R2 R3‘ R3b R4 R5 R6 X Y XXV-45-1 Ph H H H Bz H CH3 F OH XXV-45-2 Ph H H ch3 Bz H ch3 F OH XXV-45-3 Ph H H CH(CH,)2 Bz H ch3 F OH XXV-45-4 Ph H H CH2CH(CH3)2 Bz H ch3 F OH XXV-45-5 Ph H H CH2Ph Bz H ch3 F OH XXV-45-6 Ph H H CH2-indol-3-yl Bz H ch3 F OH XXV-45-7 Ph H H CH2CH2SCH3 Bz H ch3 F OH XXV-45-8 Ph ♦ H ♦ Bz H ch3 F OH ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XXV-46. 1 ,IP I *L — " J ' " 1 ,IWT"‘

Ns R' R2 ηρτ -R35 R4 RJ R4 X Y XXV-45-1 p-Me-Ph H H H Bz H ch3 F OH XXV-46-2 p-Me-Ph H H CH3 Bz H ch3 F OH XXV-46-3 p-Me-Ph H H CH(CH3)2 Bz H ch3 F OH XXV-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz H ch3 F OH XXV-46-5 p-Me-Ph H H CH2Ph Bz H ch3 F OH XXV-46-6 p-Me-Ph H H CH2-indol-3-yl Bz H ch3 F OH XXV-46-7 p-Me-Ph H H CH2CH2SCH3 Bz H ch3 F OH XXV-46-8 p-Me-Ph 4 H 4 Bz H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -539- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXV-47.

Xa r‘ RJ R3a R4 R5 R6 X Y XXV-47-1 p-F-Ph H H H Bz H ch3 F OH XXV-47-2 p-F-Ph H H ch3 Bz H ch3 F OH XXV-47-3 p-F-Ph H H CH(CH3)2 Bz H ch3 F OH XXV-47-4 p-F-Ph H H CH2CH(CH3)2 Bz H ch3 F OH XXV-47-5 p-F-Ph H H CH2Ph Bz H ch3 F OH XXV-47-6 p-F-Ph H H CH2-indol-3-yI Bz H ch3 F OH XXV-47-7 p-F-Ph H H CH2CH2SCH3 Bz H ch3 F OH XXV-47-8 p-F-Ph * H Bz H ch3 F OH *R2 and Rejoined together by (ΟΗ2)3 to form five-membered ring.

Table XXV-48.

Xs Rl Ί?” R35" T® R4 R3 R6 X Y XXV-48-1 p-Cl-Ph H H H Bz H ch3 F OH XXV-48-2 p-Cl-Ph H H CH3 Bz H ch3 F OH XXV-48-3 p-Cl-Ph H H CH(CH3)2 Bz H ch3 F OH XXV-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H ch3 F OH XXV-48-5 p-Cl-Ph H H CH2Ph Bz H ch3 F OH XXV-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz H ch3 F OH XXV-48-7 p-Cl-Ph H H CH2CH2SCH3 Bz H ch3 F OH XXV-48-8 p-Cl-Ph * H * Bz H ch3 F OH *R2 and RJb joined together by (CHib to form five-membered ring. 5 Table XXV-49. 1— η ""4: —TC----t 2 1 >

X2 Rl R4 RJ‘ R3b R4 Rs R6 X Y XXV-49-1 p-Br-Ph H H H Bz H ch3 F OH XXV-49-2 p-Br-Ph H H ch3 Bz H ch3 F OH XXV-49-3 p-Br-Ph H H CH(CH3)2 Bz H ch3 F OH XXV-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz H ch3 F OH XXV-49-5 p-Br-Ph H H CH2Ph Bz H ch3 F OH XXV-49-6 p-Br-Ph H H CHa-indol-3-yl Bz H ch3 F OH XXV-49-7 p-Br-Ph H H ch2ch2sch3 Bz H ch3 F OH XXV-49-8 p-Br-Ph 4 H 4 Bz H ch3 F OH ♦R2 and RJt> joined together by (CH2)3 to form five-membered ring. 2983472-1 -540- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXV-50.

Ns “R1 R2 r3« R3b R4 R5 1? X Y XXV-50-1 p-I-Ph H H H Bz H ch3 F OH XXV-50-2 p-I-Ph H H ch3 Bz H ch3 F OH XXV-50-3 p-I-Ph H H CHCCHsh Bz H ch3 F OH XXV-50-4 p-I-Ph H H CH2CH(CH3)2 Bz H ch3 F OH XXV-50-5 p-I-Ph H H CH2Ph Bz H ch3 F OH XXV-50-6 p-I-Ph H H CH2-indoI-3-yl Bz H ch3 F OH XXV-50-7 p-I-Ph H H CH2CH2SCH3 Bz H ch3 F OH XXV-50-8 *n2 “j p-I-Ph ♦ H * Bz H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

5 XXVI

Table XXVI-1.

Ns R1 R2 RSl "R35- R4 R5 "R5" X Y XX VI-1-1 ch3 H H H ch3 H F H OH XXVI-1-2 ch3 H H ch3 ch3 H F H OH XX VI-1-3 ch3 H H CH(CH3)2 CH3 H F H OH XX VI-1-4 ch3 H H CH2CH(CH3)j ch3 H F H OH XXVI-1-5 ch3 H H CH2Ph ch3 H F H OH XX VI-1-6 CH3 H H CH2-indol-3-yI ch3 H F H OH XXVI-1-7 ch3 H H CH2CH2SCH3 ch3 H F H OH XXVI-1-8 J ch3 lb . * H ch3 H F H OH *R2 and Rejoined together by to form five-membered ring. 2983472-1 -541- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXVI-2.

X2 R1 R2 R3a R4 R3 R6 X Y XX VI-2-1 Et H H H ch3 H F H OH XX VI-2-2 Et H H ch3 ch3 H F H OH XX VI-2-3 Et H H CH(CHj)2 ch3 H F H OH XX VI-2-4 Et H H CH2CH(CH3)2 ch3 H F H OH XX VI-2-5 Et H H CH2Ph ch3 H F H OH XXVI-2-6 Et H H CH2-indol-3-yl ch3 H F H OH XXVI-2-7 Et H H CH2CH2SCH3 ch3 H F H OH XXVI-2-8 Et * H ♦ ch3 H F H OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXVI-3.

R* T" R3· I?5 R4 Rj R® X Y XXVI-3-1 /pr H H H ch3 Η F H OH XXVI-3-2 'Pr H H ch3 ch3 H F H OH XXVI-3-3 'Pr H H CHCCH,), ch3 H F H OH XXVI-3-4 fpr H H CH2CH(CH3)2 ch3 Η F H OH XXVI-3-5 ipr H H CH2Ph ch3 H F H OH XXVI-3-6 /Pr H H CHrindol-3-yl ch3 Η F H OH XXVI-3-7 ipr H H CH2CH2SCH3 ch3 Η F H OH XXVI-3-8 /Pr ♦ H ♦ ch3 Η F H OH *R2 and RJt> joined together by (CH2)3 to form five-membered ring. 5 Table XX VI-4. 1 ' I ' H ' ’""RT . .'HL ...... J"" N° R R2 RJa Rib R4 R5 R6 X Υ XXVI-4-1 "7B? H H H ch3 H F Η ΟΗ XXVI-4-2 'Bu H H CH3 ch3 Η F Η ΟΗ XXVI-4-3 'Bu H H CH(CH3)2 ch3 Η F Η ΟΗ XXVI-4-4 'Bu H H CH^CHjh ch3 Η F Η ΟΗ XXV1-4-5 "Bu H H CH2Ph ch3 Η F Η ΟΗ XXVI-4-6 'Bu H H CH2-indol-3-yl ch3 Η F Η ΟΗ XXVI-4-7 'Bu H H ch2ch2sch3 ch3 Η F Η ΟΗ XXVI-4-8 'Bu * H * ch3 Η F Η ΟΗ ♦R2 and Rejoined together by ((¾¼ to form five-membered ring. 2983472*1 -542- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXVI-5.

Ns ir R2 R3a R3b R4 Rs R6 X Y XXVI-S-1 Ph H H H ch3 H F H OH XXVI-5-2 Ph H H ch3 ch3 H F H OH XXVI-5-3 Ph H H CH(CH3)2 ch3 H F H OH XXVI-5-4 Ph H H CH2CH(CH3)2 CH3 H F H OH XXVI-5-5 Ph H H CH2Ph ch3 H F H OH XXVI-5-6 Ph H H CH2-indol-3-yl ch3 H F H OH XX VI-5-7 Ph H H CH2CH2SCH3 ch3 H F H OH XXVI-5-8 Ph * H * ch3 H F H OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXVI-6,

Ns Rl R2 R3· r5 R6 X Y XX VI-6-1 p-Me-Ph H H H ch3 H F H OH XXVI-6-2 p-Me-Ph H H ch3 ch3 H F H OH XXVI-6-3 p-Me-Ph H H CH(CH3)2 ch3 H F H OH XXVI-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 H F H OH XXVI-6-5 p-Me-Ph H H CH2Ph ch3 H F H OH XXVI-6-6 p-Me-Ph H H CH2-indol-3-yl ch3 H F H OH XXVI-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 H F H OH XXVI-6-8 p-Me-Ph * H * ch3 H F H OH *R2 and Rjb joined together by (CH2)3 to form five-membered ring. 5 Table XXVI-7.

1 ' ....... 'I·· M RL 1 J

Ns R1 R2 R3a R3b R4 R3 R6 X Y XXVI-7-1 p-F-Ph H H H CH3 H F H OH XXVI-7-2 p-F-Ph H H ch3 ch3 H F H OH XXVI-7-3 p-F-Ph H H CH(CH3)2 ch3 H F H OH XX VI-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 H F H OH XXVI-7-6 p-F-Ph H H CH2Ph ch3 H F H OH XXVI-7-7 p-F-Ph H H CH2-indol-3-yl ch3 H F H OH XXVI-7-8 p-F-Ph H H CH2CH2SCH3 ch3 H F H OH XXVI-7-20 p-F-Ph * H * ch3 H F H OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -543- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXVI-8.

Xs R1 Rsir “R35 R4 Rs 1?' X Y XXVI-8-1 p-Cl-Ph H H H ch3 H F H OH XXVI-8-2 p-Cl-Ph H H CH3 ch3 H F H OH XXVI-8-3 p-Cl-Ph H H CH(CH3)2 ch3 H F H OH XXVI-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 H F H OH XXVI-8-5 p-Cl-Ph H H CH2Ph ch3 H F H OH XXVI-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 H F H OH XXVI-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 H F H OH XXVI-8-8 p-Cl-Ph 3b ί · -jx. * H * ch3 H F H OH *R2 and R3b joined together by (Clfcb to form five-membered ring.

Table XXVI-9.

Xa RJ R2 R3a R3b R4 R* R6 X Y XXVI-9-1 p-Br-Ph H H H CH3 H F H OH XXVI-9-2 p-Br-Ph H H ch3 ch3 H F H OH XXVI-9-3 p-Br-Ph H H CH(CH3)2 ch3 H F H OH XXVI-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 H F H OH XX VI-9-6 p-Br-Ph H H CH2Ph ch3 H F H OH XXVI-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 H F H OH XXVI-9-8 p-Br-Ph H H CH2CH2SCH3 ch3 H F H OH XXVI-9-20 Τ7Γ3Γ p-Br-Ph ♦ H * ch3 H F H OH *R2 and RJb joined together by (CHife to form five-membered ring.

Xa R1 R2 "r35" -r3B- R4 R1 R* X Y XX VI-10-1 p-I-Ph H H H ch3 H F H OH XXVI-10-2 p-I-Ph H H ch3 ch3 H F H OH XXVI-10-3 p-I-Ph H H CH(CH3)2 ch3 H F H OH XXVI-10-4 p-I-Ph H H CH2CH(CH3)2 ch3 Η F H OH XXVI-10-5 p-I-Ph H H CH2Ph ch3 H F H OH XXVI-10-6 p-I-Ph H H CH2-indol-3-yt ch3 H F H OH XXVI-10-7 p-I-Ph H H ch2ch2sch3 ch3 H F H OH XXVI-10-8 “j r»3b p-I-Ph * H * ch3 H F H OH *R2 and Re joined together by (Ctbb to form five-membered ring. 2983472-1 -544- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXV1-11.

n° R1 R2 -£sr -p; R4 Rs R6 X Y XXVI-ll-l ch3 H H H Et H F H OH XX VI-11-2 ch3 H H ch3 Et H F H OH XX VI-11-3 ch3 H H CH(CHj)2 Et H F H OH XXVI-11-4 ch3 H H CH2CH(CH3)2 Et H F H OH XXVI-11-5 ch3 H H CH2Ph Et H F H OH XXVI-11-6 ch3 H H CH2-indoI-3-yl Et H F H OH XX VI-11-7 ch3 H H CH2CH2SCH3 Et H F H OH XX VI-11-8 "in 2 "'VnJb" ch3 * H ♦ Et H F H OH *R2 and RJb joined together by (CHhh to form five-membered ring.

Table XXVI-12.

Na R1 R2 r3. "r35 R4 R5 R6 X Y XX VI-12-1 Et H H H Et H F H OH XXVI-12-2 Et H H CH3 Et H F H OH XX VI-12-3 Et H H CHCCHs), Et H F H OH XXVI-12-4 Et H H CH2CH(CH3)2 Et H F H OH XX VI-12-5 Et H H CH2Ph Et H F H OH XXVI-12-6 Et H H CH2-indol-3-yl Et H F H OH XXVI-12-7 Et H H CH2CH2SCH3 Et H F H OH XX VI-12-8 Et * H * Et H F H OH ♦R2 and RJb joined together by (CH2)3 to form five membered ring. 5 Table XXVI-13. 11 "" I n rj " ^L " ...... J Λ -Τ'

Ns R2 R3' "R36 R4 RJ R6 X Y XXVI-13-1 'Pr H H H Et H F H OH XX VI-13-2 'Pr H H CH3 Et H F H OH XXVI-13-3 'Pr H H CHCCH^ Et H F H OH XXVI-13-4 'Pr H H CH2CH(CH3)2 Et H F H OH XXVI-13-5 'Pr H H CH2Ph Et H F H OH XXVI-13-6 'Pr H H CH2-indol-3-yl Et H F H OH XXVI-13-7 'Pr H H CH2CH2SCH3 Et H F H OH XX VI-13-8 “7^2- 'Pr r · * * H * Et H F H OH *R2 and RJt> joined together by (CH2)3 to form five-membered ring. 2983472-1 • -545- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXVI-14.

K2 R1 R3 R3" R3b R4 Rs R0 X Y XX VI-14-1 'Bu H H H Et H F H OH XXVI-14-2 'Bu H H ch3 Et H F H OH XXVI-14-3 'Bu H H CH(CH3)2 Et H F H OH XXVI-14-4 'Bu H H CH2CH(CH3)2 Et H F H OH XX VI-14-5 'Bu H H CH2Ph Et H F H OH XXVI-14-6 'Bu H H CH2-indol-3-yl Et H F H OH XXVI-14-7 'Bu H H CH2CH2SCH3 Et H F H OH XXVI-14-8 'Bu * H * Et H F H OH ♦R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXVI-15.

Ns R1 R3 r3- R3b R4 R> Rb X Y XXVI-15-1 Ph H H H Et H F H OH XXVI-15-2 Ph H H ch3 Et H F H OH XXVI-15-3 Ph H H CH(CH3)2 Et H F H OH XXVI-15-4 Ph H H CH2CH(CH3)2 Et H F H OH XXVI-15-5 Ph H H CH2Ph Et H F H OH XXVI-15-6 Ph H H CH2-indol-3-yl Et H F H OH XXVI-15-7 Ph H H ch2ch2sch3 Et H F H OH XXV I-15-8 Ph * H * Et H F H OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XXVI-16. 1 ” ""I ' ."< HL1"' ......... - J g ‘ -1

Ns R1 R3 R3. R3b R4 R5 R6 X Y XX VI-16-1 p-Me-Ph H H H Et H F H OH XXVI-16-2 p-Me-Ph H H CH3 Et H F H OH XXVI-16-3 p-Me-Ph H H CH(CH3)i Et H F H OH XXVI-16-4 p-Me-Ph H H CH2CH(CH3)2 Et H F H OH XX VI-16-5 p-Me-Ph H H CH2Ph Et H F H OH XXVI-16-6 p-Me-Ph H H CH2-indol-3-yl Et H F H OH XXVI-16-7 p-Me-Ph H H CH2CH2SCH3 Et H F H OH XXVI-16-8 p-Me-Ph * H * Et H F H OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -546- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXVI-17.

Ns "F R2 R3i~ Rab T" R5 R6 X Y XXVI-17-1 p-F-Ph H H H Et H F H OH XXVI-17-2 p-F-Ph H H ch3 Et H F H OH XXVI-17-3 p-F-Ph H H CH(CH3)2 Et H F H OH XXVI-17-4 p-F-Ph H H CH2CH(CH3)2 Et H F H OH XXVI-17-5 p-F-Ph H H CH2Ph Et H F H OH XXVI-17-6 p-F-Ph H H CH2-indol-3-yl Et H F H OH XXVI-I7-7 p-F-Ph H H CH2CH2SCH3 Et H F H OH XX VI-17-8 p-F-Ph * H * Et H F H OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXVI-18.

Ns R* R2 R3’ Rab Ίυ R5 R6 X Y XXVI-18-1 p-Ci-Ph H H H Et H F H OH XXVI-18-2 p-Cl-Ph H H ch3 Et H F H OH XXVI-18-3 p-Cl-Ph H H CH(CH3)2 Et H F H OH XXVI-18-4 p-Ci-Ph H H CH2CH(CH3)2 Et H F H OH XXVI-18-5 p-Cl-Ph H H CH2Ph Et H F H OH XXVI-18-6 p-Cl-Ph H H CHa-indol-3-yl Et H F H OH XX VI-18-7 p-CI-Ph H H CH2CH2SCH3 Et H F H OH XXVI-18-8 . j p-Cl-Ph * H ♦ Et H F H OH ♦R2 and Rejoined together by (CKfeb to form five-membered ring.

Ns R‘ Ru ’F*“ R35 R4 ΊΓ R6 X Y XXVI-19-1 p-Br-Ph H H H Et H F H OH XXVI-19-2 p-Br-Ph H H ch3 Et H F H OH XX VI-19-3 p-Br-Ph H H CH(CH3)2 Et H F H OH XXVI-19-4 p-Br-Ph H H CH2CH(CH3)2 Et H F H OH XXVI-19-5 p-Br-Ph H H CHaPh Et H F H OH XXVI-19-6 p-Br-Ph H H CHa-indol-3-yl Et H F H OH XX VI-19-7 p-Br-Ph H H CH2CH2SCH3 Et H F H OH XX VI-19-8 p-Br-Ph * H * Et H F H OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -547- WO 2008/121634

Docket No. 60137.OO34WOU1 PCT/US2008/058183

Table XXVI-20.

Xa R1 R3 "r33" R5 I? X Y XXVI-20-1 p-I-Ph H H H Et H F H OH XX VI-20-2 p-I-Ph H H ch3 Et H F H OH XXVI-20-3 p-I-Ph H H CHCCHjfc Et H F H OH XX VI-20-4 p-I-Ph H H CH2CH(CH3)2 Et H F H OH XXVI-20-5 p-I-Ph H H CH2Ph Et H F H OH XXVI-20-6 p-I-Ph H H CH2-indol-3-yl Et H F H OH XX VI-20-7 p-I-Ph H H CH2CH2SCH3 Et H F H OH XXVI-20-8 p-I-Ph * H * Et H F H OH *R2 and Rejoined together by (0¾^ to form five-membered ring.

Table XXV1-21.

Xa R R3 RJa R3b R4 Rs R6 X Y XXVI-21-1 ch3 H Η Η "W H F H OH XX VI-21-2 ch3 Η Η ch3 'Pr H F H OH XXV1-21-3 ch3 Η Η CH(CHj)j 'Pr H F H OH XX VI-21-4 ch3 Η Η CH2CH(CH3)2 'Pr H F H OH XX VI-21-5 ch3 Η Η CHaPh 'Pr H F H OH XXVI-21-6 ch3 Η Η CH2-indol-3-yl 'Pr H F H OH XXVI-21-7 ch3 Η Η CH2CH2SCH3 'Pr H F H OH XX VI-21-8 ch3 ♦ Η * 'Pr H F H OH *R2 and R3b joined together by (CHib to form five-membered ring.

Table XXVI-22.

Xa R* R3 R3" R3b R4 R5 R® X Y XXVI-22-1 Et H H H Ψγ H F H OH XXVI-22-2 Et H H ch3 'Pr H F H OH XXVI-22-3 Et H H CH(CH3)2 'Pr H F H OH XXVI-22-4 Et H H CH2CH(CH3)2 'Pr H F H OH XX VI-22-5 Et H H CH2Ph 'Pr H F H OH XXVI-22-6 Et H H CH2-indol-3-yl 'Pr H F H OH XXVI-22-7 Et H H CH2CH2SCH3 'Pr H F H OH XX VI-22-8 j Et * H * 'Pr H F H OH 2983472-1 -548- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXVI-23.

Ns Rl R2 "r35" r35 R5 R6 X Y XXVI-23-1 'Pr H H H “ΨΓ H F H OH XXVI-23-2 'Pr H H ch3 'Pr H F H OH XXVI-23-3 ipr H H CH(CH3)2 'Pr H F H OH XX VI-23-4 ‘Pr H H CH2CH(CH3)2 'Pr H F H OH XX VI-23-5 ‘Pr H H CH2Ph 'Pr H F H OH XXVI-23-6 'Pr H H CH2-indol-3-yl 'Pr H F H OH XX VI-23-7 'Pr H H CH2CH2SCH3 'Pr H F H OH XXVI-23-8 fPr ♦ H ♦ 'Pr H F H OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXVI-24.

Ns R1 R2 "R31” "R35 — R4 R5 R6 X Y XXVI-24-1 'Bu H H H Jpr H F H OH XX VI-24-2 'Bu H H CH3 'Pr H F H OH XXVI-24-3 'Bu H H CH(CH3)2 'Pr H F H OH XX VI-24-4 'Bu H H CH2CH(CH3)2 'Pr H F H OH XXVI-24-5 'Bu H H CH2Ph 'Pr H F H OH XXVI-24-6 'Bu H H CH2-indol-3-yl 'Pr H F H OH XXVI-24-7 'Bu H H CH2CH2SCH3 'Pr H F H OH XXVI-24-8 'Bu * H * 'Pr H F H OH *R2 and^Jb joined together by (ΟΗ2)3 to form five-membered ring. 5 Table XXVI-25. .......... I I m .....-w,-> ,1·. . «

Ns R R2 R3· R3b IT Rs R6 X Y XXVI-25-1 Ph H H H H F H OH XX VI-25-2 Ph H H CH3 ^r H F H OH XX VI-25-3 Ph H H CH(CH3)2 'Pr H F H OH XX VI-25-4 Ph H H CH2CH(CH3)2 Ψγ H F H OH XXVI-25-5 Ph H H CH2Ph 'Pr H F H OH XXVI-25-6 Ph H H CH2-indol-3-yl 'Pr H F H OH XXVI-25-7 Ph H H CH2CH2SCH3 'Pr H F H OH XXVI-25-8 Ph l· · · * H « >pr H F H OH *R2 and Rejoined together by (Ctfcb to form five-membered ring. 2983472-1 -549- WO 2008/121634 PCT/US2008/058183

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Table XXVI-26.

X2 R1- R2 R3a -R3E- IT R5 R6 X Y XXVI-26-1 p-Me-Ph H H H ?Γ H F H OH. XXVI-26-2 p-Me-Ph H H ch3 ipr H F H OH XXVI-26-3 p-Me-Ph H H CH(CH3)2 ,pr H F H OH XXVI-26-4 p-Me-Ph H H CH2CH(CH3)2 'Pr H F H OH XX VI-26-5 p-Me-Ph H H CH2Ph 'Pr H F H OH XXVI-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr H F H OH XXVI-26-7 p-Me-Ph H H CH2CH2SCH3 'Pr H F H OH XXVI-26-8 3 b p-Me-Ph * H * 'Pr H F H OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXVI-27.

R1 R2 r35- Rib R2 fc R6 X Y XXVI-27-1 p-F-Ph H H H "W H F H OH XXVI-27-2 p-F-Ph H H ch3 'Pr H F H OH XXVI-27-3 p-F-Ph H H CHtCH,), 'Pr H F H OH XXVI-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr H F H OH XXVI-27-5 p-F-Ph H H CH2Ph 'Pr H F H OH XX VI-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr H F H OH XX VI-27-7 p-F-Ph H H CH2CH2SCH3 'Pr H F H OH XX VI-27-8 p-F-Ph ♦ H * 'Pr H F H OH *R2 and RJb joined together by (CH^ to form five-membered ring. 5 Table XXVI-28.

11 ' 1 1 H "M·11 ...-J

X2 R1 ΊΓ r3« Rib iv Rs R° X Y XXVI-28-1 p-Cl-Ph H H H "W H F H OH XX VI-28-2 p-Cl-Ph H H CH3 'Pr H F H OH XXVI-28-3 p-Cl-Ph H H CH(CH3)2 'Pr H F H OH XXVI-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr H F H OH XXVI-28-5 p-Cl-Ph H H CH2Ph 'Pr H F H OH XXVI-28-6 p-CI-Ph H H CHrindol-3-yl 'Pr H F H OH XX VI-28-7 p-CI-Ph H H CH2CH2SCH3 'Pr H F H OH XXVI-28-8 . jnJb p-Cl-Ph * H * 'Pr H F H OH *R2 and RJb joined together by to form five-membered ring. 2983472-1 -550- WO 2008/121634 PCT/US2008/058183

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Table XXVI-29.

Na R* R? ηρτ- “it* R4 r5" R6 X Y XXVI-29-1 p-Br-Ph H H H 'Pr H F H OH XXVI-29-2 p-Br-Ph H H ch3 'Pr H F H OH XXVI-29-3 p-Br-Ph H H CH(CH3)2 'Pr H F H OH XXVI-29-4 p-Br-Ph H H CH2CH(CH3)2 ipr H F H OH XXVI-29-5 p-Br-Ph H H CH2Ph 'Pr H F H OH XXVI-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr H F H OH XX VI-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr H F H OH XX VI-29-8 p-Br-Ph * H * 'Pr H F H OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXVI-30.

Ns R‘ R2 R3i R3b R4 Rs R6 X Y XX VI-30-1 p-I-Ph H H H Jpr H F H OH XXVI-30-2 p-I-Ph H H ch3 'Pr H F H OH XXVI-30-3 p-l-Ph H H CH(CH3)2 'Pr H F H OH XXVI-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr H F H OH XXV1-30-5 p-I-Ph H H CH2Ph Tr H F H OH XXVI-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr H F H OH XXVI-30-7 p-I-Ph H H CH2CH2SCH3 'Pr H F H OH XXVI-30-8 p-I-Ph * H * 'Pr H F H OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXVI-31. ' . 'ji“ bi: .- j-—-- ·*

Ns R R2 R3· Rib R4 R3 R6 X Y XXVI-31-1 ch3 H H H "Bu H F H OH XXVI-31-2 ch3 H H ch3 "Bu H F H OH XXVI-31-3 ch3 H H CH(CH3)2 "Bu H F H OH XXVI-31-4 ch3 H H CH2CH(CH3)2 ”Bu H F H OH XX VI-31-5 ch3 H H CH2Ph "Bu H F H OH XX VI-31-6 ch3 H H CH2-indol-3-yl "Bu H F H OH XX VI-31-7 ch3 H H CH2CH2SCH3 "Bu H F H OH XX VI-31-8 ch3 * H * "Bu H F H OH *R2 and R30 joined together by (CH2)3 to form five-membered ring. 2983472-1 -551 - WO 2008/121634 PCT/US2008/058183

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Table XXVI-32.

Ns R1 R2 R3" “r3® R4 RJ Ίν X Y XXVI-32-1 Et H H H MBu H F H OH XX VI-32-2 Et H H ch3 "Bu H F H OH XXVI-32-3 Et H H CH(CH3)2 "Bu H F H OH XXVI-32-4 Et H H CH2CH(CH3)2 "Bu H F H OH XXVI-32-5 Et H H CH2Ph "Bu H F H OH XXVI-32-6 Et H H ' CHrindol-3-yl "Bu H F H OH XX VI-32-7 Et H H ch2ch2sch3 "Bu H F H OH XXVI-32-8 Et * H * "Bu H F H OH *R2 and Rejoined together by (CH^ to form five-membered ring.

Table XXVI-33.

Ns “R1" ΊΓ R3a R3b R4 ΊΓ R6 X Y XXVI-33-1 “ΤΓ H H H "Bu H F H OH XXVI-33-2 ;Pr H H ch3 "Bu H F H OH XXVI-33-3 'Pr H H CHCCHa), "Bu H F H OH XXVI-33-4 ipr H H CH2CH(CH3)2 "Bu H F H OH XXVI-33-5 'pr H H CH2Ph "Bu H F H OH XXVI-33-6 'Pr H H CH2-indol-3-yl "Bu H F H OH XXVI-33-7 'Pr H H CH2CH2SCH3 "Bu H F H OH XXVI-33-8 'Pr ♦ H * "Bu H F H OH •R* and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXVI-34.

Ns R R2 R31 R3b R4 R5 Rfc X Y XX VI-34-1 2Bu H H H "Bu H F H OH XXVI-34-2 *Bu H H ch3 "Bu H F H OH XX VI-34-3 ’Bu H H CH(CH3)2 "Bu H F H OH XXVI-34-4 *Bu H H CH2CH(CH3)2 "Bu H F H OH XXVI-34-5 "Bu H H CH2Ph "Bu H F H OH XXVI-34-6 *Bu H H CHrindol-3-yl "Bu H F H OH XX VI-34-7 rBu H H CH2CH2SCH3 "Bu H F H OH XXVI-34-8 J T»3b ’flu * H * "Bu H F H OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 552-

W°2,To»o.60137.0034WOUI PCT/US2008/058183

Table XXVI-35.

Ns R1 R2 R3a r35 If” R* R6 X Y XXVI-35-1 Ph H H H "Bu H F H OH XX VI-35-2 Ph H H ch3 "Bu H F H OH XX VI-35-3 Ph H H CH(CH3)2 "Bu H F H OH XXVI-35-4 Ph H H CH2CH(CH3)2 "Bu H F H OH XX VI-35-5 Ph H H CH2Ph "Bu H F H OH XXVI-35-6 Ph H H CH2-indol-3-yl "Bu H F H OH XX VI-35-7 Ph H H ch2ch2sch3 "Bu H F H OH XXVI-35-8 Ph ♦ H "Bu H F H OH *R^ and RJb joined together by (CH2)3 to form five-membered ring.

Table XXVI-36.

Ns "R1 R2 "R3^ “R36-- - RJ R6 X Y XXVI-36-1 p-Me-Ph H H H "Bu H F H OH XXVI-36-2 p-Me-Ph H H ch3 "Bu H F H OH XXVI-36-3 p-Me-Ph H H ΟΗ(ΟΗ3)2 "Bu H F H OH XXVI-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu H F H OH XXVI-36-5 p-Me-Ph H H CH2Ph "Bu H F H OH XXV1-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu H F H OH XXVI-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu H F H OH XX VI-36-8 p-Me-Ph * H * "Bu H F H OH *R2 and R3l> joined together by (CH2)3 to form five-membered ring. 5 Table XXVI-37. 1 — A H 1 HL J---1 ' ..........

Ns R1 R2 RJa R3b R4 R5 R6 X Y XXVI-37-1 p-F-Ph H H H "Bu H F H OH XX VI-37-2 p-F-Ph H H ch3 "Bu H F H OH XX VI-37-3 p-F-Ph H H CH(CH3)2 "Bu H F H OH XX VI-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu H F H OH XXVI-37-5 p-F-Ph H H CH2Ph "Bu H F H OH XXVI-37-6 p-F-Ph H H CH2-mdoI-3-yl "Bu H F H OH XX VI-37-7 p-F-Ph H H CH2CH2SCH3 "Bu H F H OH XX VI-37-8 p-F-Ph ♦ H * "Bu H F H OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -553- WO 2008/121634 PCT/US2008/058183

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Table XXVI-38.

Xa R1 "R3" R3a "r35 Ίυ Rs R6 X Y XXVI-38-1 p-Cl-Ph H H H "Bu H F H OH XXVI-38-2 p-Cl-Ph H H ch3 "Bu H F H OH XXVI-38-3 p-Cl-Ph H H CH(CH3)2 "Bu H F H OH XXVI-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H F H OH XXVI-38-5 p-Cl-Ph H H CH2Ph "Bu H F H OH XXV1-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu H F H OH XXVI-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu H F H OH XX VI-38-8 p-Cl-Ph ♦ H "Bu H F H OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXVI-39.

Xa R' RJ “R35" "r35 R4 R "R5- X Y XXVI-39-1 p-Br-Ph H H H "Bu H F H OH XX VI-39-2 p-Br-Ph H H ch3 "Bu H F H OH XXVI-39-3 p-Br-Ph H H CH(CH3)2 "Bu H F H OH XXVI-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu H F H OH XXVI-39-5 p-Br-Ph H H CH2Ph "Bu H F H OH XXVI-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu H F H OH XXVI-39-7 p-Br-Ph H H CH2CH2SCH3 "Bu H F H OH XXVI-39-8 p-Br-Ph * H * "Bu H F H OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXVI-40.

Xa R1 R2 r3“ "R^ R4 RJ R6 X Y XX VI-40-1 p-I-Ph H H H "Bu H F H OH XX VI-40-2 p-I-Ph H H ch3 "Bu H F H OH XX VI-40-3 p-I-Ph H H CH(CH3)2 "Bu H F H OH XXVI-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu H F H OH XXVI-40-5 p-I-Ph H H CH2Ph "Bu H F H OH XXVI-40-6 p-I-Ph H H CH2-indol-3-yl "Bu H F H OH XXVI-40-7 p-I-Ph H H CH2CH2SCH3 "Bu H F H OH XXVI-40-8 “Ϊ7Τ2- p-I-Ph * H * "Bu H F H OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -554- WO 2008/121634 PCT/US2008/058183

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Table XXVI-4I.

X° R1 R2 R3a ~^3B R4 Rs R* X Y XX VI-41-1 ch3 H H H Bz H F H OH XXVI-41-2 ch3 H H ch3 Bz H F H OH XXVI-41-3 ch3 H H CH(CH3)2 Bz H F H OH XXVI-41-4 ch3 H H CH2CH(CH3)2 Bz H F H OH XXVI-41-5 ch3 H H CH2Ph Bz H F H OH XX VI-41-6 ch3 H H CH2-indol-3-yl Bz H F H OH XXVI-41-7 ch3 H H CH2CH2SCH3 Bz H F H OH XXVI-41-8 ch3 4 H * Bz H F H OH *R2 and Rejoined together by (CH?^ to form five-membered ring.

Table XXVI-42.

Xs R R2 R3‘ R36 R3 R6 X Y XX VI-42-1 Et H H H Bz H F H OH XXVI-42-2 Et H H CH3 Bz H F H OH XXVI-42-3 Et H H CH(CH3)2 Bz H F H OH XXVI-42-4 Et H H CH2CH(CH3)2 Bz H F H OH XXVI-42-5 Et H H CH2Ph Bz H F H OH XXVI-42-6 Et H H CH2-indoI-3-yl Bz H F H OH XX VI-42-7 Et H H CH2CH2SCH3 Bz H F H OH XXVI-42-8 Et * H * Bz H F H OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XX VI-43. ....... .......... 1 * H- HL I I >J I 1..,.11 i » u

X2 Rl R2 R3. R3b R4^ R3 R6 X Y XXVI-43-1 ‘Pr H H H Bz H F H OH XX VI-43-2 fpr H H CH3 Bz H F H OH XX VI-43-3 'Pr H H CHCCH^ Bz H F H OH XXVI-43-4 'Pr H H CH2CH(CH3)2 Bz H F H OH XXVI-43-5 'Pr H H CH2Ph Bz H F H OH XXVI-43-6 'Pr H H CH2-indol-3-yl Bz H F H OH XXVI-43-7 /pr H H CH2CH2SCH3 Bz H F H 0½ XXVI-43-8 'Pr * H * Bz H F H OH ♦R2 and R3b joined together by (CH^fe to form five-membered ring. 2983472-1 -555 - WO 2008/121634

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Table XXVI-44.

Ns R2 R3a -p; R4 Rs R^ X Y XX VI-44-1 zBu H H H Bz H F H OH XXVI-44-2 'Bu H H ch3 Bz H F H OH XXVI-44-3 'Bu H H CH(CH3)2 Bz H F H OH XX VI-44-4 'Bu H H CH2CH(CH3)2 Bz H F H OH XX VI-44-5 'Bu H H CH2Ph Bz H F H OH XX VI-44-6 'Bu H H CH2-indol-3-yl Bz H F H OH XX VI-44-7 'Bu H H CH2CH2SCH3 Bz H F H OH XXVI-44-8 'Bu ★ H * Bz H F H OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXVI-45.

Ns R R2 R3* R3b R4 Rs R6 X Y XXVI-45-1 Ph H H H Bz H F H OH XXVI-45-2 Ph H H CH3 Bz H F H OH XXVI-45-3 Ph H H CH(CH3)2 Bz H F H OH XX VI-45-4 Ph H H CH2CH(CH3)2 Bz H F H OH XX VI-45-5 Ph H H CH2Ph Bz H F H OH XX VI-4 5-6 Ph H H CHrindol-3-yl Bz H F H OH XXVI-45-7 Ph H H CH2CH2SCH3 Bz H F H OH XX VI-4 5-8 Ph * H * Bz H F H OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXYI-46. T ......< M 1 J 1 ' >'

Ns R1 Iv r3« Rjb R4 Rs R4 X Y XXVI-46-1 p-Me-Ph H H H Bz H F H OH XXVI-46-2 p-Me-Ph H H CH3 Bz H F H OH XXVI-46-3 p-Me-Ph H H CH(CH3)2 Bz H F H OH XXVI-4 6-4 p-Me-Ph H H CH2CH(CH3)2 Bz H F H OH XXVI-46-5 p-Me-Ph H H CH2Ph Bz H F H OH XXVI-46-6 p-Me-Ph H H CH2-indol-3-yl Bz H F H OH XXVI-46-7 p-Me-Ph H H CH2CH2SCH3 Bz H F H OH XXVI-46-8 *r>’2 J n3b~ p-Me-Ph * H * Bz H F H OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -556- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXVI-47.

Xa r1- R2 R*"- "R* R4 R3 R* X Y XX VI-47-1 p-F-Ph H H H Bz H F H OH XXVI-47-2 p-F-Ph H H ch3 Bz H F H OH XXVI-47-3 p-F-Ph H H CH(CH3)2 Bz H F H OH XXVI-47-4 p-F-Pb H H CH2CH(CH3)2 Bz H F H OH XX VI-47-5 p-F-Ph H H CH2Ph Bz H F H OH XXVI-47-6 p-F-Ph H H CH2-indol-3-yl Bz H F H OH XXVI-47-7 p-F-Ph H H ch2ch2sch3 Bz H F H OH XXVI-47-8 p-F-Ph * H * Bz H F H OH *R2 and RJt> joined together by (0¾)] to form five-membered ring.

Table XXVI-48.

Xa R1 R2 "R^ Ί?5 R3 R6 X Y XXVI-48-1 p-Cl-Ph H H H Bz H F H OH XXVI-48-2 p-Cl-Ph H H CH3 Bz H F H OH XXVI-48-3 p-Cl-Ph H H CH(CH3)2 Bz H F H OH XX VI-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H F H OH XXVI-48-5 p-Cl-Ph H H CH2Ph Bz H F H OH XXVI-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz H F H OH XXVI-48-7 p-Cl-Ph H H CH2CH2SCH3 Bz H F H OH XXVI-48-8 p-Cl-Ph * H * Bz H F H OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Xa Rl RJ R3“ "R* R4 R3 R6 X Y XX VI-49-1 p-Br-Ph H H H Bz H F H OH XXVI-49-2 p-Br-Ph H H ch3 Bz H F H OH XXVI-49-3 p-Br-Ph H H CHCCH,), Bz H F H OH XXVI-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz H F H OH XXVI-49-5 p-Br-Ph H H CH2Ph Bz H F H OH XX VI-49-6 p-Br-Ph H H CH2-indol-3-yl Bz H F H OH XXVI-49-7 p-Br-Ph H H CH2CH2SCH3 Bz H F H OH XXVI-49-8 j «3b p-Br-Ph * H * Bz H F H OH *R2 and RJt> joined together by (CH2)3 to form five-membered ring. 2983472-1 -557- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXVI-50.

R' R2 -pr R3b R4 Rr R6 X Y XX VI-S0-1 p-I-Ph H H H Bz H F H OH XX VI-50-2 p-I-Ph H H ch3 Bz H F H OH XXVI-50-3 p-I-Ph H H CH(CH3h Bz H F H OH XXVI-50-4 p-I-Ph H H CH2CH(CH3)2 Bz H F H OH XX VI-SO-5 p-I-Ph H H CH2Ph Bz H F H OH XXVI-50-6 p-I-Ph H H CHrindol-3-yl Bz H F H OH XX VI-50-7 p-I-Ph H H ch2ch2sch3 Bz H F H OH XXVI-50-8 i nJb p-I-Ph * H ♦ Bz H F H OH *R2 and R3b joined together by (CH^ to form five-membered ring.

5 XXVn

Table XXVII-1.

Ns r’ r2 pr ρ5- R4 r3" R4 X Y XXVH-1-1 ch3 H Η Η ch3 H F F OH XXVII-1-2 ch3 Η Η ch3 ch3 H F F OH XXVH-1-3 ch3 Η Η CH(CH3)2 ch3 H F F OH XXVII-1-4 ch3 Η Η CH2CH(CH3)2 ch3 H F F OH XXVII-1-5 ch3 Η Η CH2Ph ch3 H F F OH XXVH-1-6 ch3 Η Η CH2-indol-3-yl ch3 H F F OH XXVII-1-7 ch3 Η Η CH2CH2SCH3 ch3 Η F F OH XXVII-1-8 j'A'Jb' ch3 * Η * ch3 Η F F OH *R2 and RJb joined together by (012)3 to form five-membered ring. 2983472-1 -558- WO 2008/121634

Docket No. 60137.0034WOUI PCT/US2008/058183

Table XXVII-2.

Xfi R1 R1 “r3* r5 R6 X Y XXVII-2-1 Et H H H ch3 H F F OH XXVII-2-2 Et H H ch3 ch3 H F F OH XXVII-2-3 Et H H CH(CH3)2 ch3 H F F OH XXVII-2-4 Et H H CH2CH(CH3)2 ch3 H F F OH XXVII-2-5 Et H H CH2Ph ch3 H F F OH XXVII-2-6 Et H H CH2-indol-3-yl ch3 H F F OH XXVU-2-7 Et H H CH2CH2SCH3 ch3 H F F OH XXVH-2-8 Et * H * ch3 H F F OH *R^ and R3b joined together by (CHab to form five-membered ring.

Table XXVII-3. X9 R1 ΊΓ R3* R3b R4 rj R6 X Υ XXVII-3-I JPr H H H ch3 Η F F ΟΗ XXVII-3-2 'Pr H H ch3 ch3 Η F F ΟΗ XXVII-3-3 'Pr H H CH(CH3)2 ch3 Η F F ΟΗ XXVII-3-4 'Pr H H CH2CH(CH3)2 ch3 Η F F ΟΗ XXVH-3-5 'Pr H H CH2Ph ch3 Η F F ΟΗ XXVH-3-6 'Pr H H CH2-indol-3-yl ch3 Η F F ΟΗ XXVII-3-7 'Pr H H CH2CH2SCH3 ch3 Η F F ΟΗ XXVII-3-8 'Pr * H * ch3 Η F F ΟΗ *R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XXVI1-4. I 4 ‘Τ' HL ' J ’""I 1---- Χ2 R RJ R3. R3b R4 RJ R6 X Υ XXVII-4-1 'Βυ H H H CH3 Η F F ΟΗ XXVII-4-2 'Bu H H ch3 ch3 H F F ΟΗ XXVH-4-3 'Bu H H CH(CH3)2 ch3 Η F F ΟΗ XXVII-4-4 'Bu H H CHiCHCCH,), ch3 Η F F ΟΗ XXVH-4-5 'Bu H H CH2Ph ch3 Η F F ΟΗ XXVII-4-6 'Bu H H CH2-indol-3-yI ch3 Η F F ΟΗ XXVII-4-7 'Bu H H CH2CH2SCH3 ch3 Η F F ΟΗ XXVI1-4-8 ^u * H * ch3 Η F F ΟΗ *R2 and Rejoined together by (0¾^ to form five-membered ring. 2983472-1 -559- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXVII-5.

Ns R1 Ra R3‘~ -jpu- I? ΊΓ R6 X Y XXV1I-5-1 Ph H H H ch3 H F F OH XXVII-5-2 Ph H H ch3 ch3 H F F OH XXVII-5-3 Ph H H CH(CH3)2 ch3 H F F OH XXVII-5-4 Ph H H CH2CH(CH3)2 ch3 H F F OH XXVH-5-5 Ph H H CHjPh ch3 H F F OH XXVII-5-6 Ph H H CH2-indoI-3-yl ch3 H F F OH XXVII-5-7 Ph H H CH2CH2SCH3 ch3 H F F OH XXVII-5-8 Ph * H ♦ ch3 H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXVII-6.

Ns Rl R3 R3· R3b R3 R6 X Y XXVII-6-1 p-Me-Ph H H H ch3 H F F OH XXVII-6-2 p-Me-Ph H H ch3 ch3 H F F OH XXVII-6-3 p-Me-Ph H H ΟΗ(ΟΗ3)2 ch3 H F F OH XXVII-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 H F F OH XXVII-6-5 p-Me-Ph H H CH2Ph ch3 H F F OH XXVII-6-6 p-Me-Ph H H CH2-indol-3-yl ch3 H F F OH XXVII-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 H F F OH XXVII-6-8 p-Me-Ph * H * ch3 H F F OH *R2 and Rejoined together by (CHbb to form five-membered ring. 5 Table XXVII-7. ' I .. H HL.....- J - g 1

Ns R‘ ΊΓ RJa R3b R4 R5 R6 X Y XXVH-7-1 p-F-Ph H H H CH3 H F F OH XXVII-7-2 p-F-Ph H H ch3 ch3 H F F OH XXVII-7-3 p-F-Ph H H CH(CH3)2 ch3 H F F OH XXVII-7-4 p-F-Ph H H CHjCHCCHj)! ch3 H F F OH XXVII-7-6 p-F-Ph H H CH2Ph ch3 H F F OH XXVII-7-7 p-F-Ph H H CH2-indol-3-yl ch3 H F F OH XXVII-7-8 p-F-Ph H H CH2CH2SCH3 ch3 H F F OH XXVII-7-20 p-F-Ph * H * ch3 H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -560- WO 2008/121634

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Table XXVII-8.

Ns ΊΪ RJ r31" R3b R4 Rs ΊΓ X Y XXVH-8-1 p-Cl-Ph H H H ch3 H F F OH XXVI1-8-2 p-Cl-Ph H H ch3 ch3 H F F OH XXVII-8-3 p-Cl-Ph H H CH(CH3)2 ch3 H F F OH XXVII-8-4 p-CJ-Ph H H CH2CH(CH3)2 ch3 H F F OH XXVII-8-5 p-Cl-Ph H H CHjPh ch3 H F F OH XXVII-8-6 p-Cl-Pb H H CH2-indol-3-yl ch3 H F F OH XXVI1-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 H F F OH ; XXVII-8-8 p-Cl-Ph * H * ch3 H F F OH *R2 and R3b joined together by (CFhb to form five-membered ring.

Table XXVII-9.

Ns R’ RJ r3. R3b R4 R5 R6 X Y XXVII-9-1 p-Br-Ph H H H ch3 H F F OH XXVII-9-2 p-Br-Ph H H ch3 ch3 H F F OH XXVII-9-3 p-Br-Ph H H CH(CH3)2 ch3 H F F OH XXVII-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 H F F OH XXVII-9-6 p-Br-Ph H H CH2Ph ch3 H F F OH XXVII-9-7 p-Br-Ph H H CHa-indol-3-yl ch3 H. F F OH XXVII-9-8 p-Br-Ph H H CH2CH2SCH3 ch3 H F F OH XXV1I-9-20 p-Br-Ph * H * ch3 H F F OH ♦R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXVII-10. ........... I ......Μ — · Il "HL ' J -·« 1

Ns Rl Ra R3b R4 Rs R* X Y XXVII-10-1 p-I-Ph H H H ch3 H F F OH XXVI I-10-2 p-I-Ph H H ch3 ch3 H F F OH XXVIM0-3 p-I-Ph H H CHiCHah ch3 H F F OH XXVTI-10-4 p-I-Ph H H CH2CH(CH3)2 ch3 H F F OH XXVII-10-5 p-I-Ph H H CH2Ph ch3 H F F OH XXVH-10-6 p-I-Ph H H CH2-indol-3-yl ch3 H F F OH XXVII-10-7 p-I-Ph H H ch2ch2sch3 ch3 H F F OH XXVII-10-8 nJb . p-I-Ph * H * ch3 H F F OH *R2 and RJb joined together by (0¾¼ to form five-membered ring. 2983472-1 -561 - WO 2008/121634

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Table XXVII-11.

Xa R1 R2 r3. R3b R4 R5 ]<5 X Y XXVU-11-1 ch3 H H H Et H F F OH XX VI I-11-2 ch3 H H ch3 Et H F F OH XXVH-11-3 ch3 H H CH(CH3)2 Et H F F OH XXVn-ll-4 ch3 H H CH2CH(CH3)2 Et H F F OH XXVII-11-5 ch3 H H CH2Ph Et H F F OH XXVII-11-6 ch3 H H CH2-indol-3-yl Et H F F OH XX VI I-11-7 ch3 H H CH2CH2SCH3 Et H F F OH XXVH-11-8 ch3 ♦ H ♦ Et H F F OH *RJ and Rejoined together by (CFfeb to form five-membered ring.

Table XXVII-12.

Xs R R7 RJs R3® R4 R3 R6 X Y XXVH-12-1 Et H H H Et H F F OH XXVII-12-2 Et H H ch3 Et H F F OH XXVII-12-3 Et H H CH(CH3)2 Et H F F OH XXVII-12-4 Et H H CH2CH(CH3)2 Et H F F OH XXVH-12-5 Et H H CH2Ph Et H F F OH XXVII-12-6 Et H H CH2-indol-3-yl Et H F F OH XXVII-12-7 Et H H CH2CH2SCH3 Et H F F OH XXVII-12-8 Et * H * Et H F F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXVII-13. 1 R R- nv J—

Xa R R2 R3b IT R3 R6 X Y XXVII-13-1 ’Pr H H H Et H F F OH XXVII-13-2 /Pr H H ch3 Et H F F OH XXVII-13-3 'Pr H H CH(CH,)j Et H F F OH XXVU-13-4 'Pr H H CH2CH(CH3)2 Et H F F OH XXVII-13-5 'Pr H H CH2Ph Et H F F OH XXVII-13-6 'Pr H H CH2-indol-3-yl Et H F F OH XXVII-13-7 'Pr H H CH2CH2SCH3 Et H F F OH XXVH-13-8 2 . jV3b 'Pr * H * Et H F F OH *R^ and R3b joined together by (CH2)3 to form five-membered ring. 2983472-Ϊ -562- WO 2008/121634

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Table XXVII-14.

Ns R* "Ί?' R3" R3b R4 RJ R6 X Y XXVII-14-1 fBu H H H Et H F F OH XXVII-14-2 'Bu H H ch3 Et H F F OH XXVII-14-3 'Bu H H CH(CH3)2 Et H F F OH XXVII-14-4 'Bu H H CH2CH(CH3)2 Et H F F OH XXVII-14-5 'Bu H H CH2Ph Et H F F OH XXVH-14-6 'Bu H H ‘ CH2-indol-3-yl Et H F F OH XXVII-14-7 'Bu H H ch2ch2sch3 Et H F F OH XXVH-14-8 'Bu * H ♦ Et H F F OH *R2 and RJb joined together by (CHbfc to form five-membered ring.

Table XXVII-15.

Ns ir R1 "R^ ΊΓ r! R6 X Y XXVII-15-1 Ph H H H Et H F F OH XXVII-15-2 Ph H H ch3 Et H F F OH XXVII-15-3 Ph H H CHCCHa), Et H F F OH XXVII-15-4 Ph H H CH2CH(CH3)2 Et H F F OH XXVH-15-5 Ph H H CH2Ph Et H F F OH XXVII-15-6 Ph H H CH2-indol-3-yl Et H F F OH XXVII-15-7 Ph H H CH2CH2SCH3 Et H F F OH XXVII-15-8 Ph * H * Et H F F OH *R2 and joined together by (CH2)3 to form five-membered ring.

Table XXVII-16.

Ns R1 r2" R37* "R55 ΊΓ R5 Rfc X Y XXVU-16-1 p-Me-Ph H H H Et H F F OH XXVII-16-2 p-Me-Ph H H CH3 Et H F F OH XXVII-16-3 p-Me-Ph H H CH(CH3>2 Et H F F OH XXVII-16-4 p-Me-Ph H H CH2CH(CH3)2 Et H F F OH XXVII-16-5 p-Me-Ph H H CH2Ph Et H F F OH XXVII-16-6 p-Me-Ph H H CH2-indol-3-yl Et H F F OH XXVII-16-7 p-Me-Ph H H CH2CH2SCH3 Et H F F OH XXVII-16-8 “ίπτ—γτπκ- p-Me-Ph * H * Et H F F OH *R^ and RJb joined together by (CHija to form five-membered ring. 2983472-1 -563 - WO 2008/121634

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Table XXVII-17.

Ns r1 R2 ’"r3"” R3” R4 R5 R6 X Y XXV1I-17-1 p-F-Ph H H H Et H F F OH XXVII-17-2 p-F-Ph H H ch3 Et H F F OH XXVII-17-3 p-F-Ph H H CH(CH3)2 Et H F F OH XXVIU7-4 p-F-Ph H H CH2CH(CH3)2 Et H F F OH XXVII-17-5 p-F-Ph H H CH2Ph Et H F F OH XXVII-17-6 p-F-Ph H H CHrindol-3-yl Et H F F OH XXVII-17-7 p-F-Ph H H CH2CH2SCH3 Et H F F OH XXVII-17-8 p-F-Ph * H * Et H F F OH *R2 and Rejoined together by (CHj)3 to form five-membered ring.

Table XXVII-18.

Ns R1 R2 RJ‘ R3b R4 ΊΓ R6 X Y XXVII-18-1 p-Cl-Ph H H H Et H F F OH XXVII-18-2 p-Cl-Ph H H ch3 Et H F F OH XXVH-18-3 p-Cl-Ph H H CHfCH^ Et H F F OH XXVII-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H F F OH XXVII-18-5 p-Cl-Ph H H CH2Ph Et H F F OH XXVII-18-6 p-Cl-Ph H H CH2-indol-3-yl Et H F F OH XXVII-18-7 p-Cl-Ph H H ch2ch2sch3 Et H F F OH XXVH-18-8 p-CI-Ph * H ♦ Et H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XXVII-19. ....... " I ' R RL J g ' .

Ns R1 R2 RJa R3b R* R5 R6 X Y XXVII-19-1 p-Br-Ph H H H Et H F F OH XXVII-19-2 p-Br-Ph H H ch3 Et H F F OH XXVn-19-3 p-Br-Ph H H CHiCHah Et H F F OH XXVI1-19-4 p-Br-Ph H H CH2CH(CH3)2 Et H F F OH XXVII-19-5 p-Br-Ph H H CH2Ph Et H F F OH XXVII-19-6 p-Br-Ph H H CH2-indol-3-yl Et H F F OH XXVII-19-7 p-Br-Ph H H CH2CH2SCH3 Et H F F OH XXVII-19-8 '*«2. "77>3b p-Br-Ph ♦ H * Et H F F OH ♦R2 and RJb joined together by (0¾¼ to form five-membered ring. 2983472-1 -564- WO 2008/121634

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Table XXVII-20.

Xa R1 R2 R3a "r36 R5 R6 X Y XXVH-20-1 p-I-Ph H H H Et H F F OH XXVII-20-2 p-I-Ph H H ch3 Et H F F OH XXVII-20-3 p-l-Ph H H ORCHah Et H F’ F OH XXVII-20-4 p-l-Ph H H CH2CH(CH3)2 Et H F F OH XXVII-20-5 p-I-Ph H H CH2Ph Et H F F OH XXVII-20-6 p-I-Ph H H CH2-indol-3-yl Et H F F OH XXVII-20-7 p-I-Ph H H ch2ch2sch3 Et H F F OH XXVII-20-8 p-I-Ph * H * Et H F F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXVII-21.

Xa R RJ R3' R3b R4 R3 R6 X Y XXVII-21-1 ch3 Η Η Η H F F OH XXVII-21-2 ch3 H Η ch3 'Pr H F F OH XXVII-21-3 ch3 H Η CHCCH^ 'Pr H F F OH XXVII-21-4 ch3 Η Η CH2CH(CH3)2 'Pr H F F OH XXVII-21-5 ch3 Η Η CH2Ph 'Pr H F F OH XXVII-21-6 ch3 Η Η CH2-indol-3-yl 'Pr H F F OH XXVII-21-7 ch3 Η Η CH2CH2SCH3 /pr H F F OH XXVI1-21-8 ch3 * Η * 'Pr H F F OH *R2 and RJB joined together by (CH2)3 to form five-membered ring. 5 Table XXVII-22. I R R -..1--111 J -...... II II - . .

Xa R RJ r3. R3b R4 R5 R6 X Y XXVII-22-1 Et H H H 'Pr H F F OH XXVII-22-2 Et H H ch3 'Pr H F F OH XXVII-22-3 Et H H CH(CH3)2 /pr H F F OH XXVII-22-4 Et H H CH2CH(CH3)2 'Pr H F F OH XXVII-22-5 Et H H CH2Ph 'Pr H F F OH XXVII-22-6 Et H H CH2-indol-3-yl 'Pr H F F OH XXVII-22-7 Et H H CH2CH2SCH3 'Pr H F F OH XXVII-22-8 “*«’2 ... k3b Et * H * 'Pr H F F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -565- WO 2008/121634 PCT/US2008/0S8183

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Table XXVH-23.

Ns R1 R2 R3· R3b TF ΊΓ R6 X Y XXVII-23-1 'Pr H H H "Ύτ" H F F OH XXVH-23-2 'Pr H H ch3 'Pr H F F OH XXVH-23-3 'Pr H H CH(CHj)i 'Pr H F F OH XXVII-23-4 Ψγ H H CHjCHiCHa^ 'Pr H F F OH XXVII-23-5 ipr H H CH2Ph 'Pr H F F OH XXVII-23-6 'Pr H H CH2-indol-3-yl 'Pr H F F OH XXVH-23-7 'Pr H H CH2CH2SCH3 'Pr H F F OH XXVII-23-8 'Pr * H * 'Pr H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXVII-24.

Ns R RJ Rj8 R3b R4 ΊΓ R6 X Y XXVII-24-1 'Bu H H H 'Pr H F F OH XXVII-24-2 'Bu H H ch3 'Pr H F F OH XXV1I-24-3 'Bu H H CHiCHa), 'Pr H F F OH XXVII-24-4 'Bu H H CH2CH(CH3)2 'Pr H F F OH XXVII-24-5 'Bu H H CH2Ph 'Pr H F F OH XXVU-24-6 'Bu H H CH2-indol-3-yl 'Pr H F F OH XXVII-24-7 'Bu H H CH2CH2SCH3 'Pr H F F OH XXVII-24-8 'Bu * H * 'Pr H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XXVII-25. 1 1 " 1 I H-. HL1

Na R R2 R3b R4 R5 Rb X Y XXVn-25-1 Ph H H H 'Pr H F F OH XXVII-25-2 Ph H H CH3 *Pr H F F OH XXVH-25-3 Ph H H CHCCHah ^r H F F OH XXVII-25-4 Ph H H CH2CH(CH3)2 *Pr H F F OH XXVII-25-5 Ph H H CH2Ph 'Pr H F F OH XXVII-25-6 Ph H H CH2-indol-3-yl *Pr H F F OH XXVII-25-7 Ph H H CH2CH2SCH3 'Pr H F F OH XXVII-25-8 . . n’Jb" Ph * H * 'Pr H F F OH ♦R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472.1 -566- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXVII-26.

Kfi R1 R2 R3a R3b R4 Rs R6 X Y XXVII-26-1 p-Me-Ph H H H 'Pr H F F OH XXVII-26-2 p-Me-Ph H H ch3 'Pr H F F OH XXVH-26-3 p-Me-Ph H H CH(CH3)2 'Pr H F F OH XXVII-26-4 p-Me-Ph H H CH2CH(CH3)2 'Pr H F F OH XXVII-26-5 p-Me-Ph H H CH2Ph Tr H F F OH XXVII-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr H F F OH XXVII-26-7 p-Me-Ph H H CH2CH2SCH3 'Pr H F F OH XXVII-26-8 p-Me-Ph * H * 'Pr H F F OH *R2 and RJb joined together by ((¾¼ to form five-membered ring.

Table XXVII-27.

Ns R1 RJ "r36 R4 Rs R6 X Y XXVII-27-1 p-F-Ph H H H H F F OH XXVII-27-2 p-F-Ph H H CH3 'Pr H F F OH XXVII-27-3 p-F-Ph H H CH(CH3>2 'Pr H F F OH XXVII-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr H F F OH XXVII-27-5 p-F-Ph H H CH2Ph 'Pr H F F OH XXVII-27-6 p-F-Ph H H CH2-lndol-3-yl 'Pr H F F OH XXVH-27-7 p-F-Ph H H CH2CH2SCH3 'Pr H F F OH XXVU-27-8 p-F-Ph * H * Tr H F F OH *R2 and R3b joined together by (CHj)3 to form five-membered ring.

Table XXVII-28.

Xs R1 RJ "r3”" R35 R4 r! R6 X Y XXVn-28-1 p-CI-Ph H H H /pr H F F OH XXVII-28-2 p-Cl-Ph H H CH3 Tr H F F OH XXVII-28-3 p-Cl-Ph H H CH(CH3)2 'Pr H F F OH XXVII-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr H F F OH XXVII-28-5 p-Cl-Ph H H CH2Ph H F F OH XXVII-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr H F F OH XXVI1-2 8-7 p-Cl-Ph H H CH2CH2SCH3 'Pr H F F OH XXVII-28-8 ~Σ772 . rJb‘ p-Cl-Ph * H * 'Pr H F F OH ♦R2 and Rejoined together by (CHjjTto form five-membered ring. 2983472-1 -567- WO 2008/121634 PCTZUS2008/058183

Docket No. 60137.0034WOU1

Table XXVII-29.

Ns R1 "R3" R38 "r35 r4 Rs R4 X Y XXVII-29-1 p-Br-Ph H H H JPr H F F OH XXVII-29-2 p-Br-Ph H H ch3 'Pr H F F OH XXVII-29-3 p-Br-Ph H H CH(CH3)2 'Pr H F F OH XXVII-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr H F F OH XXVH-29-5 p-Br-Ph H H CH2Ph 'Pr H F F OH XXVII-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr H F F OH XXVII-29-7 p-Br-Ph H H ch2ch2sch3 'Pr H F F OH XXVII-29-8 p-Br-Ph * H * 'Pr H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXVII-30.

Xa R1 R2 RJa R3b R4 R5 X Y XXVIl-30-1 p-I-Ph H H H H F F OH XXVII-30-2 p-I-Ph H H ch3 'Pr H F F OH XXVII-30-3 p-I-Ph H H CHCCHj), 'Pr H F F OH XXVII-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr H F F OH XXVII-30-5 p-I-Ph H H CH2Ph ipr H F F OH XXVII-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr H F F OH XXVII-30-7 p-I-Ph H H CH2CH2SCH3 'Pr H F F OH XXVII-30-8 p-I-Ph * H * 'Pr H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXVII-31.

Xa ΊΓ“ R2 r’· "r35 R4 Rs R4 X Y XXVH-31-1 ch3 H H H ”Bu H F F OH XXVH-31-2 ch3 H Η ch3 ”Bu H F F OH XXVII-31-3 ch3 H H CHiCH^ ffBu H F F OH XXVII-31-4 ch3 H H CH2CH(CH3)2 "Bu H F F OH XXVII-31-5 ch3 H H CH2Ph ”Bu H F F OH XXVII-31-6 ch3 H H CH2-indol-3-yl "Bu H F F OH XXVII-31-7 ch3 H H ch2ch2sch3 "Bu H F F OH XXVH-31-8 ~-Γλ-Jb- ch3 * H * "Bu H F F OH *R^ and R3b joined together by (CH^ to form five-membered ring. 2983472-1 r 568 - WO 2008/121634

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Table XXVU-32.

X° R1 R2 "F “R36 ΊΤ” r! R6 X Y XXVH-32-1 Et H H H "Bu H F F OH XXVII-32-2 Et H H ch3 "Bu H F F OH XXVII-32-3 Et H H CH(CH3)2 "Bu H F F OH XXVII-32-4 Et H H CH2CH(CH3)2 "Bu H F F OH XXVII-32-5 Et H H CH2Ph "Bu H F F OH XXVII-32-6 Et H H CH2-indol-3-yl "Bu H F F OH XXVII-32-7 Et H H CH2CH2SCH3 "Bu H F F OH XXVIl-32-8 Et * H ♦ "Bu H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXVII-33.

Xa R r2 RJa R3b R4 R3 R6 X Y XXVII-33-1 'Pr H H H "Bu H F F OH XXVII-33-2 /pr H H CH3 "Bu H F F OH XXVII-33-3 'Pr H H CH(CH3)2 "Bu H F F OH XXVI1-33-4 'Pr H H CH2CH(CH3)2 "Bu H F F OH XXVII-33-5 'Pr H H CH2Ph "Bu H F F OH XXVII-33-6 'Pr H H CH2-indol-3-yl "Bu H F F OH XXVII-33-7 'Pr H H CH2CH2SCH3 "Bu H F F OH XXVII-33-8 'Pr ♦ H * "Bu H F F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXVII-34.

- — - < 11111. J

Xa R R1 R3’ RJb R4 R3 R6 X Y ΧΧνΠ-34-ϊ *Bu H H H "Bu H F F OH XXVII-34-2 *Bu H H ch3 "Bu H F F OH XXVII-34-3 'Bu H H CHCCHah "Bu H F F OH XXVII-34-4 'Bu H H CH2CH(CH3)2 "Bu H F F OH XXVII-34-5 'Bu H H CH2Ph "Bu H F F OH XXVII-34-6 'Bu H H CH2-indol-3-yl "Bu H F F OH XXVII-34-7 'Bu H H CH2CH2SCH3 "Bu H F F OH XXVII-34-8 'Bu * H * "Bu H F F OH *R2 and R3” joined together by (CH2)3 to form five-membered ring. 2983472-) -569- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXVII-35.

X° RJ R2 R3‘ '~(F r’- R5 (? X Y XXVII-35-1 Ph H H H "Bu H F F OH XXVII-35-2 Ph H H ch3 "Bu H F F OH XXV1I-35-3 Ph H H CH(CH3)2 "Bu H F F OH XXV1I-35-4 Ph H H CH2CH(CH3)2 "Bu H F F OH XXVII-35-5 Ph H H CH2Ph "Bu H F F OH XXVII-35-6 Ph H H CH2-indol-3-yl "Bu H F F OH XXVII-35-7 Ph H H ch2ch2sch3 "Bu H F F OH XXVII-35-8 Ph * H ♦ "Bu H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXVII-36.

Xa R’ R2 R3“ R3b R4 RJ R6 X Y XXVII-36-1 p-Me-Ph H H H "Bu H F F OH XXVH-36-2 p-Me-Ph H H ch3 "Bu H F F OH XXVII-36-3 p-Me-Ph H H CH(CH3)2 "Bu H F F OH XXVII-36-4 p-Me-Ph H H CHjCH(CH3)2 "Bu H F F OH XXVII-36-5 p-Me-Ph H H CH2Ph "Bu H F F OH XXVII-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu H F F OH XXVII-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu H F F OH XXVII-36-8 p-Me-Ph * H ♦ "Bu H F F OH ♦R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXVII-37.

| "W - I ,,-, J

Xa R1 R2 R3· R3b R4 R5 R6 X Y XXVII-37-1 p-F-Ph H H H "Bu H F F OH XXVII-37-2 p-F-Ph H H ch3 "Bu H F F OH XXVII-37-3 p-F-Ph H H CH(CH3)2 "Bu H F F OH XXVII-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu H F F OH XXVH-37-5 p-F-Ph H H CH2Ph "Bu H F F OH XXVII-37-6 p-F-Ph H H CH2-indol-3-yl "Bu H F F OH XXVI1-37-7 p-F-Ph H H CH2CH2SCH3 "Bu H F F OH XXVH-37-8 p-F-Ph * H * "Bu H F F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -570- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXVII-38.

Ms r1 R3"” ΊΤ" R5 κ X Y XXVII-38-1 p-Cl-Ph H H H "Bu H F F OH XXVII-38-2 p-Cl-Ph H H ch3 "Bu H F F OH XXVII-38-3 p-Cl-Ph H H CH(CH3)2 "Bu H F F OH XXVH-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H F F OH XXVII-38-5 p-Cl-Ph H H CH2Ph "Bu H F F OH XXVII-38-6 p-Cl-Ph H H CH2-indoI-3-yl "Bu H F F OH XXVII-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu H F F OH XXVII-38-8 p-Cl-Ph * H * "Bu H F F OH *R2 and RJb joined together by (CII2)3 to form five-membered ring.

Table XXVII-39. ·

Ms R1 R R3a R3b R4 RJ R6 X Y XXVH-39-1 p-Br-Ph H H H "Bu H F F OH XXVH-39-2 p-Br-Ph H H ch3 "Bu H F F OH XXVII-39-3 p-Br-Ph H H CH(CH3)2 "Bu H F F OH XXVII-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu H F F OH XXVII-39-5 p-Br-Ph H H CH2Ph "Bu H F F OH XXVII-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu H F F OH XXVII-39-7 p-Br-Ph H H CH2CH2SCH3 "Bu H F F OH XXVII-39-8 p-Br-Ph * H * "Bu H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XXVII-40. "" ...... ' I ' iR H- ' 'RIT—' 'J B / . -.

Ms Rl RJ R3. R3 R4 R5 R6 X Y XXVH-40-1 p-I-Ph H H H "Bu H F F OH XXVII-40-2 p-I-Ph H H ch3 "Bu H F F OH XXVII-40-3 p-l-Ph H H CH(CH3)2 "Bu H F F OH XXVII-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu H F F OH XXVII-40-5 p-I-Ph H H CH2Ph "Bu H F F OH XXVH-40-6 p-I-Ph H H CH2-indol-3-yl "Bu H F F OH XXVII-40-7 p-I-Ph H H CH2CH2SCH3 "Bu H F F OH XXVII-40-8 p-l-Ph * H ♦ "Bu H F F OH ♦R2 and R36 joined together by (Clfck to form five-membered ring. 2983472-1 -571 - WO 2008/121634

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Table XX VII-41.

Ha R3 RJa -r3B R4 R5 R6 X Y XXVII-41-1 ch3 H H H Bz H F F OH XXVII-41-2 ch3 H H ch3 Bz H F F OH XXVII-41-3 ch3 H H CH(CH3)2 Bz H F F OH XXVII-41-4 ch3 H H CH2CH(CH3)2 Bz H F F OH XXVI1-41-5 ch3 H H CH2Ph Bz H F F OH XXVII-41-6 ch3 H H CH2-indol-3-yl Bz H F F OH XXVII-41-7 ch3 H H CH2CH2SCH3 Bz H F F OH XXVII-41-8 ch3 * H ♦ Bz H F F OH *RZ and Rejoined together by (CHafc to form five-membered ring.

Table XXVII-42.

Ha R R3 RJ“ R3b R4 Rs R6 X Y XXVH-42-1 Et H H H Bz H F F OH XXVII-42-2 Et H H ch3 Bz H F F OH XXVII-42-3 Et H H CH(CH3)2 Bz H F F OH XXVII-42-4 Et H H CH2CH(CH3)2 Bz H F F OH XXVII-42-5 Et H H CH2Ph Bz H F F OH XXVII-42-6 Et H H CH2-indol-3-yl Bz H F F OH XXVII-42-7 Et H H CH2CH2SCH3 Bz H F F OH XXVII-42-8 Et * H * Bz H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XXVII-43. -- ' I ...... 'J g .JT " -

Ha R r* R3. R3b R4 Rs Rfc X Y XXVII-43-1 H H H Bz H F F OH XXVH-43-2 'Pr H H ch3 Bz H F F OH XXVII-43-3 *Pr H H CH(CH3)2 Bz H F F OH XXVII-43-4 'Pr H H CH2CH(CH3)2 Bz H F F OH XXVII-43-5 'Pr H H CH2Ph Bz H F F OH XXVII-43-6 'Pr H H CH2-indol-3-yl Bz H F F OH XXVII-43-7 'Pr H H CH2CH2SCH3 Bz H F F 4ft XXVII-43-8 'Pr * H * Bz H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -572- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXVJI-44.

Ns 1P“ R2 R3a "IF- R4 R4 R6 X Y XXVII-44-1 'Bu H H H Bz H F F OH XXVII-44-2 'Bu H H ch3 Bz H F F OH XXVII-44-3 'Bu H H CH(CH3)2 Bz H F F OH XXVII-44-4 'Bu H H CH2CH(CH3)2 Bz H F F OH XXVII-44-5 'Bu H H CH2Ph Bz H F F OH XXVII-44-6 'Bu H H CH2-indol-3-yl Bz H F F 0H ΧΧΥΠ-44-7 'Bu H H ch2ch2sch3 Bz H F F OH XXVII-44-8 'Bu * H * Bz H F F OH *R2 and Rejoined together by (CHa^ to form five-membered ring.

Table XXVII-45.

Ns F R3 R3b R4 Rs R^ X Y XXVIM 5-1 Ph H H H Bz H F F OH XXVII-45-2 Ph H H ch3 Bz H F F OH XXVII-45-3 Ph H H CH(CH3)2 Bz H F F OH XXVII-45-4 Ph H H CH2CH(CH3)2 Bz H F F OH XXVII-45-5 Ph H H CH2Ph Bz H F F OH XXVII-45-6 Ph H H CH2-indol-3-yl Bz H F F OH XXVII-45-7 Ph H H CH2CH2SCH3 Bz H F F OH XXVII-45-8 ini itaJL· Ph ♦ H * Bz H F F OH *RJ and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXVII-46.

1 ' f ...... . . W J . I

Ns R1 ΊΓ R3a R3b R4 R6 X Y XXVn-46-1 p-Me-Ph H H H Bz H F F OH XXVU-46-2 p-Me-Ph H H CH3 Bz H F F OH XXVII-46-3 p-Me-Ph H H CH(CH3)i Bz H F F OH XXVII-46-4 p-Me-Ph H H CH2CH(CH3>2 Bz H F F OH XXVII-46-5 p-Me-Ph H H CH2Ph Bz H F F OH XXVII-46-6 p-Me-Ph H H CHrindol-3-yl Bz H F F OH XXVII-46-7 p-Me-Ph H H CH2CH2SCH3 Bz H F F OH XXVII-46-8 / j nJb p-Me-Ph * H * Bz H F F OH *R^ and R36 joined together by (CH2)3 to form five-membered ring. 2983472-1 -573 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXVII-47.

Xs r1- R3 R3il R4 RJ R6 X Y XXVII-47-1 p-F-Ph H H H Bz H F F OH XXVII-47-2 p-F-Ph H H ch3 Bz H F F OH XXVII-47-3 p-F-Ph H H CH(CH3)2 Bz H F F OH XXVII-47-4 p-F-Ph H H CH2CH(CH3)2 Bz H F F OH XXVII-47-5 p-F-Ph H H CH2Ph Bz H F F OH XXVII-47-6 p-F-Ph H H CH2-indol-3-yl Bz H F F OH XXVII-47-7 p-F-Ph H H CH2CH2SCH3 Bz H F F OH XXV1I-47-8 p-F-Ph * H * Bz H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXVII-48. D1

Xs Rl R2 R3a R3b R4 R5 R6 X Y XXVII-48-1 p-Cl-Ph H H H Bz H F F OH XXVII-48-2 p-Ct-Ph H H ch3 Bz H F F OH XXVII-48-3 p-Cl-Ph H H CHfCHah Bz H F F OH XXVII-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H F F OH XXVII-48-5 p-Cl-Ph H H CH2Ph Bz H F F OH XXVII-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz H F F OH XXVII-48-7 p-Cl-Ph H H CH2CH2SCH3 Bz H F F OH XXVII-48-8 p-Cl-Ph * H * Bz H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XXVII-49. I H-'Ll. HL ...... "J" ' 2 -

Xs R’ RJ RJ. R3b R4 R3 R6 X Y XXVU-49-1 p-Br-Ph H H H Bz H F F OH XXVII-49-2 p-Br-Ph H H CH3 Bz H F F OH XXVII-49-3 p-Br-Ph H H CH(CH3)3 Bz H F F OH XXVII-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz H F F OH XXVII-49-5 p-Br-Ph H H CH2Ph Bz H F F OH XXVII-49-6 p-Br-Ph H H CH2-indol-3-yl Bz H F F OH XXVH-49-7 p-Br-Ph H H CH2CH2SCH3 Bz H F F OH XXVII-49-8 p-Br-Ph * H ♦ Bz H F F OH *R2 and R3” joined together by (CT^ to form five-membered ring. 2983472-1 -574- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXVH-50. D1

Xs R1 R2 “R35” R3b IT ΊΡ~ X Y XXVII-50-1 p-I-Ph H H H Bz H F F OH XXVII-50-2 p-I-Ph H H ch3 Bz H F F OH XXVII-50-3 p-I-Ph H H CH(CH3)2 Bz H F F OH XXVI1-50-4 p-I-Ph H H CH2CH(CH3)2 Bz H F F OH XXVII-50-5 p-I-Ph H H CHjPh Bz H F F OH XXVII-50-6 p-I-Ph H H CHa-indol-3-yl Bz H F F OH XXVI1-5 0-7 p-I-Ph H H CH2CH2SCH3 Bz H F F OH XXVU-50-8 p-I-Ph ♦ H ♦ Bz H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

5 xxvra

Table XXVni-l.

Xs R1 R2 R3a R3b R4 Rs R4 X Y XXVIII-1-1 ch3 H H H ch3 H H F OH XXVIII-1-2 ch3 H H ch3 ch3 H H F OH XXVIII-1-3 ch3 H H CH(CH3)2 ch3 H H F OH XXVIII-1-4 ch3 H H CH2CH(CH3)2 ch3 H H F OH XXVHI-1-5 ch3 H H CH2Ph ch3 H H F OH XXVIII-1-6 ch3 H H CH2-indol-3-yl ch3 H H F OH XXVIII-1-7 ch3 H H CH2CH2SCH3 ch3 H H F OH XXVHI-1-8 ch3 * H * ch3 H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -575- WO 2008/121634

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Table XXVIII-2.

Ns R1 R2 “r33” “r33 'I?-'·· r5 i? X Y XXVIII-2-1 Et H H H ch3 H H F OH XXVHI-2-2 Et H H ch3 ch3 H H F OH XXVIII-2-3 Et H H CHCCEhh ch3 H H F OH XXVHI-2-4 Et H H CH2CH(CH3)2 ch3 H H F OH XXVIII-2-5 Et H H CH2Ph ch3 H H F OH XXVHI-2-6 Et H H CH2-indol-3-yi ch3 H H F OH XXV1II-2-7 Et H H CH2CH2SCH3 ch3 H H F OH XXVIII-2-8 Et * H * ch3 H H F OH *R2 and RJt) joined together by (CH2)3 to form five-membered ring.

Table XXVIII-3.

Na R R2 RJa R3b R4 Rs R6 X Y XXVHI-3-1 'Pr H H H ch3 H H F OH XXVI11-3-2 'Pr H H CH3 ch3 H H F OH XXVIIl-3-3 'Pr H H CHCCH,), ch3 H H F OH XXVHI-3-4 'Pr H H CH2CH(CH3)2 ch3 H H F OH XXVIII-3-5 'Pr H H CH2Ph ch3 H H F OH XXVHI-3-6 'Pr H H CH2-indol-3-yl ch3 H H F OH XXVIII-3-7 'Pr H H CH2CH2SCH3 ch3 H H F OH XXVHI-3-8 'Pr ♦ H * ch3 H H F OH *R2 and RJb joined together by (CH^ to form five-membered ring. 5 Table XX VIII-4. ....... 1 * R- ".....J—

Ns R R2 R3. R3b R4 R3 R6 X Y XXVHI-4-I 'Bu H H H ch3 H H F OH XXVIII-4-2 *Bu H H CH3 ch3 Η H F OH XXVI11-4-3 'Bu H H CHCCH^ ch3 H H F OH XXVIII-4-4 'Bu H H ΟΗ2ΟΗ(ΟΗ3)2 ch3 H H F OH XXVUI-4-5 'Bu H H CH2Ph ch3 H H F OH XXVIII-4-6 'Bu H H CH2-indol-3-yl ch3 H H F OH XXVIII-4-7 *Bu H H CH2CH2SCH3 ch3 H H F OH XXVHI-4-8 'Bu « H * ch3 H H F OH *R2 and Rejoined together by (CH^ to form five-membered ring. 2983472-1 -576- WO 2008/121034 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXVIII-5.

N° R1 R2 R3· T* R4 R* R4 X Y XXVni-5-1 Ph H H H ch3 H H F OH XXVIII-5-2 Ph H H ch3 ch3 H H F OH XXVIII-5-3 Ph H H CH(CH3)2 ch3 H H F OH XXVIII-5-4 Ph H H CH2CH(CH3)2 ch3 H H F OH XXVIH-5-5 Ph H H CH2Ph ch3 H H F OH XXVIII-5-6 Ph H H CH2-indol-3-yl ch3 H H F OH XXVIII-5-7 Ph H H CH2CH2SCH3 ch3 H H F OH XXVIII-5-8 J Ph * H ♦ ch3 H H F OH *R2 and Rejoined together by (Clhkt0 f°rm five-membered ring.

Table XXVIII-6.

Ns "R1- R2 R3a T* R4 R5 R4 X Y XXVIII-6-1 p-Me-Ph H H H CH3 H H F OH XXV1II-6-2 p-Me-Ph H H CH3 ch3 H H F OH XXVI1I-6-3 p-Me-Ph H H CHCCHa), ch3 H H F OH XXVIII-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 H H F OH XXVIII-6-5 p-Me-Ph H H CH2Ph ch3 H H F OH XXVIII-6-6 p-Me-Ph H H CH2-indol-3-yl ch3 H H F OH XXVIII-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 H H F OH XXVHI-6-8 p-Me-Ph + H * ch3 H H F OH *R2 and Rejoined together by (CFhb to form five-membered ring. 5 Table XXVIII-7. —1 II - * ' q.““" J I - Jt -Ξ-

Ns R* R2 Rj« R3b R4 R5 R6 X Y XXVHI-7-1 p-F-Ph H H H ch3 H H F OH XXVIII-7-2 p-F-Ph H H ch3 ch3 H H F OH XXVni-7-3 p-F-Ph H H CH(CH3)2 ch3 H H F OH XXVIII-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 H H F OH XXVIII-7-6 p-F-Ph H H CH2Ph ch3 H H F OH XXVHI-7-7 p-F-Ph H H CHrindol-3-yl ch3 H H F OH XXVIII-7-8 p-F-Ph H H CH2CH2SCH3 ch3 H H F OH XXVHI-7-20 J .. . nJb · p-F-Ph * H * ch3 H H F OH ♦R1 and RJb joined together by (CH2)a to form five-membered ring. 2983472-1 -577- WO 2008/121634

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Table XXVIII-8.

Ns R1 R2- R3r" R3b 7Τ“ R* R* X Y XXVIII-8-1 p-CI-Ph H H H ch3 H H F OH XXVIII-8-2 p-Cl-Ph H H ch3 ch3 H H F OH XXVHI-8-3 p-Cl-Ph H H CH(CH3)2 ch3 H H F OH XXVIII-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 H H F OH XXVHI-8-5 p-Cl-Ph H H CH2Ph ch3 H H F OH XXVIII-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 H H F OH XXVIII-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 H H F OH XXVIH-8-8 p-Cl-Pb * H + ch3 H H F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. Table XXVII1-9. "Jfe R1 R3 r3« R3b R4 RJ R6 X Y XXVIII-9-1 p-Br-Ph H H H ch3 H H F OH XXVIII-9-2 p-Br-Ph H H ch3 ch3 H H F OH XXVIII-9-3 p-Br-Ph H H CH(CH3)2 ch3 H H F OH XXVI11-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 H H F OH XXVIII-9-6 p-Br-Ph H H CH2Ph ch3 H H F OH XXVIlI-9-7 p-Br-Ph H H CH2-indoi-3-yl ch3 H H F OH XXVIII-9-8 p-Br-Ph H H ch2ch2sch3 ch3 H H F OH XXVIII-9-20 p-Br-Ph * H * ch3 H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. Table XXVIII-10. "7^ R1 R3 rST- r3B R4 R5 R6 X Y XXVIH-10-1 p-I-Ph H H H ch3 H H F OH XXVIII-10-2 p-I-Ph H H ch3 ch3 H H F OH XXVIlI-10-3 p-I-Ph H H CH(CH3)2 ch3 H H F OH XXVHI-10-4 p-I-Ph H H CH2CH(CH3)2 ch3 H H F OH XXVIII-10-5 p-I-Ph H H CH2Ph ch3 H H F OH XXVIII-10-6 p-I-Ph H H CH2-indol-3-yl ch3 H H F OH XXVIII-10-7 p-I-Ph H H CH2CH2SCH3 ch3 H H F OH XXVHI-10-8 p-I-Ph * H ♦ ch3 H H F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -578- WO 2008/121634

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Table XXVIII-U.

Ns R1 R2 “ipr "IF R5 TF X Y xxvni-ll-l ch3 H H H Et H H F OH XXVIII-11-2 ch3 H H ch3 Et H H F OH XXVHI-11-3 ch3 H H CH(CH3)2 Et H H F OH XXVHI-11-4 ch3 H H CH2CH(CH3)2 Et H H F OH XXVHI-11-5 ch3 H H CH2Ph Et H H F OH XXVIH-11-6 ch3 H H CH2-indol-3-yl Et H H F OH XXVIII-11-7 ch3 H H CH2CH2SCH3 Et H H F OH XXVIII-11-8 ch3 + H * Et H H F OH *R2 and R3b joined together by (0¾¼ to form five-membered ring.

Table XXVin-12.

Ns R R3 R1. R3b R4 Rs R6 X Y XXVHI-12-1 Et H H H Et H H F OH XXVIII-12-2 Et H H CH3 Et H H F OH XXVI1I-12-3 Et H H CH(CH3)2 Et H H F OH XXVI11-12-4 Et H H CH2CH(CH3)2 Et H H F OH XXVIII-12-5 Et H H CH2Ph Et H H F OH XXVIII-12-6 Et H H CH2-indol-3-yl Et H H F OH XXVHI-12-7 Et H H CH2CH2SCH3 Et H H F OH XXVIII-12-8 Et ♦ H * Et H H F OH *R2 and R36 joined together by (CH2)3 to form five-membered ring. 5 TableXXVIIl-13. ...................... <1 J -

Ns R R2 RJa R3b R4 RJ R6 X Y XXVIII-13-1 Jpr H H H Et H H F OH XXVIII-13-2 'Pr H H CH3 Et H H F OH XXVHI-13-3 'Pr H H CH(CH3)2 Et H H F OH XXVHI-13-4 'Pr H H CH2CH(CH3)2 Et H H F OH XXVIH-13-5 'Pr H H CH2Ph Et H H F OH XXVIII-13-6 'Pr H H CH2-indol-3-yl Et H H F OH XXVHI-13-7 'Pr H H CH2CH2SCH3 Et H H F OH XXVHI-13-8 'Pr * H * Et H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -579- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table XXVIII-14.

Na R1 R2 R3a ~Ί?5 R4 Rs R6 X Y XXVIH-14-1 'Bu H H H Et H H F OH XXV1II-14-2 'Bu H H ch3 Et H H F OH XXVIII-14-3 'Bu H H CH(CH3)2 Et H H F OH XXVIIJ-14-4 'Bu H H CH2CH(CH3)2 Et H H F OH XXVIII-14-5 'Bu H H CH2Ph Et H H F OH XXVHI-14-6 'Bu H H CH2-indol-3-yl Et H H F OH XXVHI-14-7 'Bu H H CH2CH2SCH3 Et H H F OH XXVHI-14-8 'Bu * H * Et H H F OH *R2 and Rejoined together by (Cl-hb to form five-membered ring.

Table XXVIII-15.

Ns R R2 R3« R3b R4 RJ R6 X Y XXVIU-15-1 Ph H H H Et H H F OH XXVHI-15-2 Ph H H ch3 Et H H F OH XXVIII-15-3 Ph H H CH(CH3)2 Et H H F OH XXVIII-15-4 Ph H H CH2CH(CH3)2 Et H H F OH XXVIII-15-5 Ph H H CH2Ph Et H H F OH XXVIII-15-6 Ph H H CH2-indol-3-yl Et H H F OH XXVIII-15-7 Ph H H CH2CH2SCH3 Et H H F OH XXVIII-15-8 Ph * H * Et H H F OH *R* and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXVIII-16. ' .1--1-, - I-'.— g ' ' "

Ns Rl R* r3. R3t> R4 Rs R6 X Y XXVUI-16-1 p-Me-Ph H H H Et H H F OH XXVHM6-2 p-Me-Ph H H ch3 Et H H F OH XXVHI-16-3 p-Me-Ph H H CH(CH3)2 Et H H F OH XXVIII-16-4 p-Me-Ph H· H CH2CH(CH3)2 Et H H F OH XXVIII-16-5 p-Me-Ph H H CH2Ph Et H H F OH XXVHI-16-6 p-Me-Ph H H CH2-indol-3-yl Et H H F OH XXVIII-16-7 p-Me-Ph H H CH2CH2SCH3 Et H H F OH XXVIII-16-8 p-Me-Ph * H * Et H H F OH *R2 and R30 joined together by (CH2)3 to form five-membered ring. 2983472·! -580- WO 2008/121634 ,

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Table ΧΧΥΠΙ-17.

N? “r1 r3. R3b ΊΓ RJ R6 X Y XXVHI-17-1 p-F-Ph H H H Et H H F OH XXVI1I-17-2 p-F-Ph H H ch3 Et H H F OH XXVIII-17-3 p-F-Ph H H CHtCHjh Et H H F OH XXVIIM7-4 p-F-Ph H H CH2CH(CH3)2 Et H H F OH XXVIII-17-5 p-F-Ph H H CH2Ph Et H H F OH XXVIII-17-6 p-F-Ph H H CH2-indol-3-yl Et H H F OH XXVIII-17-7 p-F-Ph H H CH2CH2SCH3 Et H H F OH XXVHI-17-8 p-F-Ph * H * Et H H F OH *R2 and Rejoined together by ((¾¼ to form five-membered ring.

Table XXVIII-18.

Ns R1 R2 Rj« R3b R4 R5 Rb X Y XX VIII-18-1 p-Cl-Ph H H H Et H H F OH XXVHI-18-2 p-Cl-Ph H H CH3 Et H H F OH XXVIII-18-3 p-Cl-Ph H H CH(CH3)2 Et H H F OH XXVHI-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H H F OH XXVH1-18-5 p-Cl-Ph H H CH2Ph Et H H F OH XXVI1I-18-6 p-Cl-Ph H H CH2-indol-3-yl Et H H F OH XXVI1I-18-7 p-Cl-Ph H H CH2CH2SCH3 Et H H F OH ΧΧΥΠΙ-18-8 p-Ci-Ph * H * Et H H F OH ♦R2 and R^” joined together by (ΟΗ2)3 to form five-membered ring. 5 Table XXV1II-19. --- ' 1 '1·' H HL IL ‘ — I 1 ' __ .....

Ns R‘ R3 R3b R4 Rj R6 X Y XXVIII-19-1 p-Br-Ph H H H Et H H F OH XXVIH-19-2 p-Br-Ph H H ch3 Et H H F OH XXVIII-19-3 p-Br-Ph H H CHCCHah Et H H F OH XXVHI-19-4 p-Br-Ph H H CH2CH(CH3)j Et H H F OH XXVHI-19-5 p-Br-Ph H H CH2Ph Et H H F OH XXVIII-19-6 p-Br-Ph H H CH2-indol-3-yl Et H H F OH XXVHI-19-7 p-Br-Ph H H CH2CH2SCH3 Et H H F OH XXVIII-19-8 ~*772- p-Br-Ph * H * Et H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -581 - WO 2008/121634 , Λ,τ

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Table XXVIII-20.

Kfi Rl T" "R35- R4 Rs R6 X Y XXVHI-20-1 p-I-Ph H H H Et H H F OH XXVI1I-20-2 p-I-Ph H H ch3 Et H H F OH XXVHI-20-3 p-I-Ph H H CH(CH3)2 Et H H F OH XXVIII-20-4 p-I-Ph H H CH2CH(CH3)2 Et H H F OH XXVIII-20-5 p-I-Ph H H CH2Ph Et H H F OH XXVHI-20-6 p-I-Ph H H CH2-indol-3-yl Et H H F OH XXVHI-20-7 p-I-Ph H H CH2CH2SCH3 Et H H F OH XXVHI-20-8 p-I-Ph * H * Et H H F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXVIII-21.

Ms R RJ R" R3b R4 R5 R6 X Y XXVHI-21-1 CH3 H H H "W H H F OH XXVHI-21-2 ch3 H H ch3 ipr H H F OH XXV1II-21-3 ch3 H H CH(CH3)2 'Pr H H F OH XXVIII-21-4 ch3 H H CH2CH(CH3)2 'Pr H H F OH XXVHI-21-5 ch3 H H CH2Ph 'Pr H H F OH XXVIII-21-6 ch3 H H CH2-indol-3-yl 'Pr H H F OH XXVIII-21-7 ch3 H H CH2CH2SCH3 'Pr H H F OH XXVIII-21-8 ch3 * H * 'Pr H H F OH *R2 and RJb joined together by (CHj^ to form five-membered ring. 5 Table XXVIII-22. 1 I H R- HL 1 »— J f " Z ~ ~

Ns R Ra R3" R3b R4 Rs R6 X Y XXVIII-22-1 Et H H H 'Pr H H F OH XXVIII-22-2 Et H H ch3 'Pr H H F OH XXVHI-22-3 Et H H CHCCHah 'Pr H H F OH XXVHI-22-4 Et H H CH2CH(CH3)2 'Pr H H F OH XXVIII-22-5 Et H H CH2Ph 'Pr H H F OH XXVHI-22-6 Et H H CH2-indol-3-yl 'Pr H H F OH XXVIII-22-7 Et H H CH2CH2SCH3 'Pr H H F OH XXVIH-22-8 Et * H ♦ 'Pr H H F OH *R2 and R3b joined together by (CH^ to form five-membered ring. 2983472-1 -582- WO 2008/12 J 634

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Table XXVIII-23.

Xs Rl R2 RJa TT R1 ΊΓ X Y XXVIII-23-1 'Pr H H H 'Pr H H F OH XXVIH-23-2 'Pr H H ch3 'Pr H H F OH XXVIII-23-3 "Pr H H CH(CH3)2 'Pr H H F OH XXVHI-23-4 'Pr H H CH2CH(CH3)2 'Pr H H F OH XXVIII-23-5 Tr H H CH2Ph 'Pr H H F OH XXVHI-23-6 Tr H H CH2-indol-3-yl 'Pr H H F OH XXVHI-23-7 'Pr H H CH2CH2SCH3 'Pr H H F OH XXVHI-23-8 'Pr * H * 'Pr H H F OH *R2 and Rejoined together by (Chbk to form five-membered ring.

Table XXVIII-24.

Xs R1 r r3. R3b R4 R5 R6 X Y XXVHI-24-I 'Bu H H H Jpr H H F OH XXVIII-24-2 'Bu H H CHj 'Pr H H F OH XXVHI-24-3 'Bu H H CHCCH^ 'Pr H H F OH XXVIIΪ-2 4-4 'Bu H H CH2CH(CH3)2 'Pr H H F OH XXVIII-24-5 'Bu H H CH2Ph 'Pr H H F OH XXVIII-24-6 'Bu H H CH2-indol-3-yl Tr H H F OH XXVIH-24-7 'Bu H H CH2CH2SCH3 Tr H H F OH XXVHI-24-8 'Bu * H * 'Pr H H F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XX VIII-25. 1 " - . — .... - I— . . lg II. I,.,—· —

Xs R R2 Rjfl R3b R4 RJ R6 X Y XXVHI-25-1 Ph H H H ipr H H F OH XXVIII-25-2 Ph H H ch3 'Pr H H F OH XXVIII-25-3 Ph H H CHiCHj): 'Pr H H F OH XXVIII-25-4 Ph H H CH3CH(CH3)2 'Pr H H F OH XXVHI-25-5 Ph H H CH2Ph 'Pr H H F OH XXVIII-25-6 Ph H H CH2-indol-3-yI 'Pr H H F OH XXVIII-25-7 Ph H H CH2CH2SCH3 'Pr H H F OH XXVIII-25-8 Ph * H * 'Pr H H F OH *R2 and R3b joined together by (CHjb to form five-membered ring. 2983472-1 -583- WO 2008/121634 ,

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Table XXVIII-26.

Ns R1 ΊΓ Rja r35 R4 Rs R6 X Y XXVHI-26-1 p-Me-Ph H H H JPr H H F OH XXVjHI-26-2 p-Me-Ph H H ch3 'Pr H H F OH XXVIH-26-3 p-Me-Ph H H CH(CH3)2 'Pr H H F OH XXVIII-26-4 p-Me-Ph H H CH2CH(CH3)2 'Pr H H F OH XXVIII-26-5 p-Me-Ph H H CH2Ph 'Pr H H F OH XXVIII-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr H H F OH XXVIII-26-7 p-Me-Ph H H ch2ch2sch3 'Pr H H F OH XXVIII-26-8 p-Me-Ph ♦ H 4 'Pr H H F OH *RZ and R3b joined together by (Clhh to form five-membered ring.

Table XXVUI-27.

Ns R1 RJ R3’ R3b R4 Rs R6 X Y XXVIII-27-1 p-F-Ph H H H Jpr H H F OH XXVUI-27-2 p-F-Ph H H CH3 'Pr H H F OH XXVII1-27-3 p-F-Ph H H CH(CH3)2 'Pr H H F OH XXVIII-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr H H F OH XXVni-27-5 p-F-Ph H H CH2Ph 'Pr H H F OH XXVIII-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr H H F OH XXVIII-27-7 p-F-Ph H H CH2CH2SCH3 'Pr H H F OH XXVIII-27-8 p-F-Ph ♦ H * 'Pr H H F OH ♦R2 and RJ0 joined together by (CHib to form five-membered ring. 5 Table XXVIII-28. 1 .......... R »Ι-·”Τ"'*υ ' ' ”ΙΙΊ·Ι"Τ,Ι"· > . .."I111

Ns R‘ R2 Rj. R3b R4 RJ R6 X Y XXVm-28-1 p-Cl-Ph H H H Jpr H H F OH XXVIII-28-2 p-Cl-Ph H H ch3 'Pr H H F OH XXVIII-28-3 p-Cl-Ph H H CH(CH3)2 'Pr H H F OH XXVIII-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr H H F OH XXVHI-28-5 p-Cl-Ph H H CH2Ph 'Pr H H F OH XXVIII-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr H H F OH XXVIII-28-7 p-Cl-Ph H H CH2CH2SCH3 'Pr H H F OH XXVIII-28-8 p-Cl-Ph * H * 'Pr H H F OH ♦R2 and joined together by (CH^ to form five-membered ring. 2983472-1 -584- WO 2008/121634

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Table XXVIII-29.

Ns R‘ RJ "r3^ R3b R4 R5 R6 X Y XXVIII-29-1 p-Br-Ph H H H JPr H H F OH XXVI1I-29-2 p-Br-Ph H H ch3 'Pr H H F OH XXVIII-29-3 p-Br-Ph H H CHiCH^ 'Pr H H F OH XXVIII-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr H H F OH XXV1II-29-5 p-Br-Ph H H CH2Ph 'Pr H H F OH XXVIII-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr H H F OH XXVIII-29-7 p-Br-Ph H H ch2ch2sch3 'Pr H H F OH XXVIII-29-8 p-Br-Ph * H * 'Pr H H F OH *R2 and Rejoined together by to form five-membered ring.

Table XXV1II-30.

Ns R1 R2 R3. R3b R4 Rs R6 X Y XXVIH-30-1 p-I-Ph H H H 'Pr H H F OH XXVIII-30-2 p-I-Ph H H CH3 'Pr H H F OH XXVIII-30-3 p-I-Ph H H CH(CH3)2 'Pr H H F OH XXVIII-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr H H F OH XXVH1-30-5 p-I-Ph H H CH2Ph 'Pr H H F OH XXVHI-30-6 p-I-Ph H H CH2-lndol-3-yl 'Pr H H F OH XXVHI-30-7 p-I-Ph H H CH2CH2SCH3 'Pr H H F OH XXVIII-30-8 p-I-Ph * H + 'Pr H H F OH *R2 and Rejoined together by (0-12)3 to form five-membered ring. 5 Table XXVIII-31. — I I ' 1 ' I m ill· ' ' J 2 . '

Ns R R2 r3. Rib R^ R? R6 X Y XXVUI-31-1 ch3 H H H "Bu H H F OH XXVHI-31-2 ch3 H H CH-, "Bu H H F OH XXVHI-31-3 ch3 H H CH(CH3fe "Bu H H F OH XXVIII-31-4 ch3 H H CH2CH(CH3)2 ”Bu H H F OH XXVIII-31-5 ch3 H H CH2Ph "Bu H H F OH XXVIII-31-6 ch3 H H CH2-indol-3-yl "Bu H H F OH XXVIII-31-7 ch3 H H CH2CH2SCH3 "Bu H H F OH XXVHI-31-8 ch3 H * "Bu H H F OH *R2 and RJb joined together by to form five-membered ring. 2983472-1 -585- WO 2008/121634

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Table XXVIII-32.

Ns R1 R2 ηρτ- "R^ R4 RJ R6 X Y XXVIII-32-1 Et H H H "Bu H H F OH XXVHI-32-2 Et H H ch3 "Bu H H F OH XXVHI-32-3 Et H H CH(CH3)2 "Bu H H F OH XXVHI-32-4 Et H H CH2CH(CH3)2 "Bu H H F OH XXVIII-32-5 Et H H CH2Ph "Bu H H F OH XXVHI-32-6 Et H H CH2-indol-3-yl "Bu H H F OH XXVHI-32-7 Et H H CH2CH2SCH3 "Bu H H F OH XXVIII-32-8 Et ♦ H * "Bu H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXVIII-33.

Ns Rl R2 R3. R3b R4 R5 R6 X Y XXVHI-33-1 'Pr H H H "Bu H H F OH XXVHI-33-2 'Pr H H CH3 "Bu H H F OH XXVHI-33-3 'Pr H H CH(CH3)2 "Bu H H F OH XXVIII-33-4 'Pr H H CH2CH(CH3)2 "Bu H H F OH XXVII1-33-5 'Pr H H CH2Ph "Bu H H F OH XXVIII-33-6 'Pr H H CH2-indol-3-yl "Bu H H F OH XXVin-33-7 'Pr H H CH2CH2SCH3 "Bu H H F OH XXVIII-33-8 'Pr ♦ H * "Bu H H F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXVUI-34. I " W ' J g‘ 2. nil· —

Ns R R2 Rj. R3b ir R5 R6 X Y XXVIIl-34-1 *Bu H H H "Bu H H F OH XXVHI-34-2 'Bu H H ch3 "Bu H H F OH XXVin-34-3 'Bu H H CH(CH3)2 "Bu H H F OH XXVIII-34-4 'Bu H H CH2CH(CH3)2 "Bu H H F OH XXVIII-34-5 <Bu H H CH2Ph "Bu H H F OH XXVIH-34-6 'Bu H H CH2-indoI-3-yl "Bu H H F OH XXVIII-34-7 'Bu H H CH2CH2SCH3 "Bu H H F OH XXVIII-34-8 'Bu ♦ H * "Bu H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -586- WO 2008/121634

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Table XXVIII-35.

Ns R1 R2 XXVHI-35-1 Ph H XXVHI-35-2 Ph H XXVIII-35-3 Ph H XXVIH-35-4 Ph H XXVIII-35-5 Ph H XXVHI-35-6 Ph H XXVIII-35-7 Ph H XXVHI-35-8 Ph ♦ R38 R3b Η H H CH3 H CH(CH3)2 H CH2CH(CH3)2 H CH3Ph H CH2-indol-3-yl H CH2CH2SCH3 H *

R4 R5 R6 X Y "Bu H H F OH "Bu H H F OH "Bu H H F OH "Bu H H F OH "Bu H H F OH "Bu H H F OH "Bu H H F OH "Bu H H F OH *R2 and Rejoined together by (0¾^ to form five-membered ring. 5

Table XXVIII-36.

Ns Rl R2 “Έ* —r3E R4 R5 I? X Y XXVHI-36-1 p-Me-Ph H H H "Bu H H F OH XXVHI-36-2 p-Me-Ph H H ch3 "Bu H H F OH XXVHI-36-3 p-Me-Ph H H CH(CH3)2 "Bu H H F OH XXVIII-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu H H F OH XXVHI-36-5 p-Me-Ph H H CH2Ph "Bu H H F OH XXVHI-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu H H F OH XXVIII-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu H H F OH XXVIH-36-8 p-Me-Ph 4 H * "Bu H H F OH *R2 and RJb joined together by (CHj^ to form five-membered ring. Table XX VIII-37. Ns R1 R2 R38" R35 R4 Rs R4 X Ϋ XXVIH-37-1 p-F-Ph H H H "Bu H H F OH XXVIII-37-2 p-F-Ph H H ch3 "Bu H H F OH XXVHI-37-3 p-F-Ph H H 01(0¾¼ "Bu H H F OH XXVIII-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu H H F OH XXVIII-37-5 p-F-Ph H H CH2Ph "Bu H H F OH XXVHI-37-6 p-F-Ph H H CH2-indol-3-yl "Bu H H F OH XXVIII-37-7 p-F-Ph H H ch2ch2sch3 "Bu H H F OH XXVIII-37-8 p-F-Ph * H * "Bu H H F OH *R2 and R31* joined together by (0¾¼ to form five-membered ring. 2983472-] -587- WO 2008/121634 . nMj1WAlI1

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Table XXVIII-38.

R2 R3a "R35 Ί<ί R5 X Y XXV1H-38-1 p-Cl-Ph H H H "Bu H H F OH XXVHI-38-2 p-Cl-Ph H H ch3 "Bu H H F OH XXVIII-38-3 p-Cl-Ph H H CH(CH3)2 "Bu H H F OH XXVHI-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H H F OH XXVIH-38-5 p-Cl-Ph H H CH2Ph "Bu H H F OH XXVHI-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu H H F OH XXV1II-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu H H F OH XXVIII-38-8 p-Cl-Ph * H * "Bu H H F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXVIII-39.

Xfi R1 R5 Rj. R3b R4 Rs R6 X Y XXVIII-39-1 p-Br-Ph H H H "Bu H H F OH XXVHI-39-2 p-Br-Ph H H ch3 "Bu H H F OH XXVHI-39-3 p-Br-Ph H H CH(CH3)2 "Bu H H F OH XXVHI-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu H H F OH XXVIII-39-5 p-Br-Ph H H CH2Ph "Bu H H F OH XXVin-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu H H F OH XXVHI-39-7 p-Br-Ph H H CH2CH2SCH3 "Bu H H F OH XXVTII-39-8 p-Br-Ph * H ♦ "Bu H H F OH *RZ and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXVIII-40.

X2 R1 R; R3. R3b R4 R5 R6 X Y XXVIII-40-1 p-I-Ph H H H "Bu H H F OH XXVIII-40-2 p-I-Ph H H ch3 "Bu H H F OH XXVIII-40-3 p-I-Ph H H CH(CH3)2 "Bu H H F OH XXVIH-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu H H F OH XXVIH-40-5 p-I-Ph H H CH2Ph "Bu H H F OH XXVI1I-40-6 p-I-Ph H H CH2-indol-3-yl "Bu H H F OH XXVIII-40-7 p-I-Ph H H CH2CH2SCH3 "Bu H H F OH XXVIII-40-8 p-I-Ph * H * "Bu H H F OH *R2 and R3b joined together by to form five-membered ring. 2983472-1 -588- WO 2008/121634 t ΛΛ„

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Table XXVIII-41.

Ns 'ir“ R3’ “R35 "S’" R3 R6 X Y XXVIII-4M ch3 H H H Bz H H F OH XXV1II-41-2 ch3 H H ch3 Bz H H F OH XXVIII-41-3 ch3 H H CH(CH3)2 Bz H H F OH XXVI11-41-4 ch3 H H CH2CH(CH3)2 Bz H H F OH XXVI11-41-5 ch3 H H CHjPh Bz H H F OH XXVIII-41-6 ch3 H H CH2-indol-3-yl Bz H H F OH XXVIII-41-7 ch3 H H CH2CH2SCH3 Bz H H F OH XXVIII-41-8 ch3 ♦ H * Bz H H F OH *R2 and R3b joined together by (Cibb to form five-membered ring.

Table XXVIII-42.

Ns R R1 R3. R3b R4 R5 R6 X Y XXVHI-42-1 Et H H H Bz H H F OH XXVIII-42-2 Et H H ch3 Bz H H F OH XXVIII-42-3 Et H H CH(CH3)a Bz H H F OH XXVIII-42-4 Et H H CH2CH(CH3)2 Bz H H F OH XXVHI-42-5 Et H H CH2Ph Bz H H F OH XXVHI-42-6 Et H H CH2-indoI-3-yl Bz H H F OH XXVHI-42-7 Et H H CH2CH2SCH3 Bz H H F OH XXVIII-42-8 Et * H * Bz H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XXVJII-43. — J·! _ J _ '

Ns R R* R“ R3b R4 Rs R6 X Y XXVHI-43-1 /pr H H H Bz H H F OH XXVII1-43-2 'Pr H H ch3 Bz H H F OH XXVIII-43-3 'Pr H H CH(CH3)2 Bz H H F OH XXVHI-43-4 'Pr H H CH2CH(CH3)2 Bz H H F OH XXVIII-43-5 'Pr H H CH2Ph Bz H H F OH XXVIII-43-6 'Pr H H CH2-indol-3-yl Bz H H F OH XXVIII-43-7 'Pr H H CH2CH2SCH3 Bz H H F 0Φί XXVHI-43-8 'Pr * H * Bz H H F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -589- WO 2008/121634

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Table XXVIII-44.

Ns T” R2 R3* R3b r3- Rs R6 X Y XXVHI-44-1 'Bu H H H Bz H H F OH XXVIII-44-2 'Bu H H ch3 Bz H H F OH XXVIII-44-3 'Bu H H CH(CH3)2 Bz H H F OH XXVH1-44-4 'Bu H H CH2CH(CH3)2 Bz H H F OH XXVHI-44-5 'Bu H H CH2Ph Bz H H F OH XXVIII-44-6 'Bu H H CH2-indol-3-yl Bz H H F OH XXVIII-44-7 'Bu H H CH2CH2SCH3 Bz H H F OH XXVIII-44-8 'Bu * H * Bz H H F OH *R2 and Rejoined together by (CH2)j to form five-membered ring.

Table XXVIII-45.

Ns R iC Rj. R3b R4 R5 R6 X Y XXVIII-45-1 Ph H H H Bz H H F OH XXVIII-45-2 Ph H H ch3 Bz H H F OH XXVIII45-3 Ph H H CH(CH3)2 Bz H H F OH XXVIII-45-4 Ph H H CH2CH(CH3)2 Bz H H F OH XXVIII-45-5 Ph H H CH2Ph Bz H H F OH XXVIII-45-6 Ph H H CH2-indol-3-yl Bz H H F OH XXVIII-45-7 Ph H H CH2CH2SCH3 Bz H H F OH XXVI11-45-8 Ph * H ♦ Bz H H F OH *R2 and RJb joined together by (CFbhto form five-membered ring. 5 Table XXVITI-46. '1 ' 'R * 1 H- RL ' J 1 J '

Ns R1 Ru R3a R36 R4 Rs R6 X Y XXVIII-46-1 p-Me-Ph H H H Bz H H F OH XXVHI-46-2 p-Me-Ph H H ch3 Bz H H F OH XXVHI-46-3 p-Me-Ph H H CHiCHsh Bz H H F OH XXVHI-46-4 p-Me-Ph H H CH3CH(CH3)2 Bz H H F OH XXVHI-46-5 p-Me-Ph H H CH2Ph Bz H H F OH XXVIII-46-6 p-Me-Ph H H CH2-indol-3-yI Bz H H F OH XXVHI-46-7 p-Me-Ph H H CH2CH2SCH3 Bz H H F OH XXVIH-46-8 T77Z-77Π5Τ p-Me-Ph * H * Bz H H F OH *R2 and RJb joined together by (0¾¼to form five-membered ring. 2983472-1 -590- WO 2008/121634 τ

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Table XXV1H-47. ΊΖ η ι

Ns Rl R2 R3a -£r- R5 R6 X Y XXV11I-47-1 p-F-Ph H H H Bz H H F OH XXVHI-47-2 p-F-Ph H H ch3 Bz H H F OH XXVIH-47-3 p-F-Ph H H CH(CH3)2 Bz H H F OH XXVIH-47-4 p-F-Ph H H CH2CH(CH3)2 Bz H H F OH XXVHI-47-5 p-F-Ph H H CH2Ph Bz H H F OH XXVHI-47-6 p-F-Ph H H CH2-indol-3-yl Bz H H F OH XXVIII-47-7 p-F-Ph H H CH2CH2SCH3 Bz H H F OH XXVHI-47-8 p-F-Ph * H * Bz H H F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXVI1I-48.

Xs R’ R2 R3. R3b R4 R3 R6 X Υ XXVHI-48-1 p-Cl-Ph H H H Bz Η Η F ΟΗ XXVIII-48-2 p-Cl-Ph H H ch3 Bz Η Η F ΟΗ XXVIII-48-3 p-Cl-Ph H H CH(CH3)2 Bz Η Η F ΟΗ XXVHI-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz Η Η F ΟΗ XXVIII-48-5 p-Cl-Ph H H CH2Ph Bz Η Η F ΟΗ XXVIII-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz Η Η F ΟΗ XXVIII-48-7 p-Cl-Ph H H ch2ch2sch3 Bz Η Η F ΟΗ XXVUI-48-8 p-Cl-Ph * H * Bz Η Η F ΟΗ *R2 and RJt} joined together by (CH2)3 to form five-membered ring. 5 Table XXVIII-49. " 1 " . w ”1™ ml - ."i,r- ς.~α~ «. —::

X® R R2 Rj. R3b R4 Rs R6 X Y XXVHI-49-1 p-Br-Ph H H H Bz H H F OH XXVIII-49-2 p-Br-Ph H H CH3 Bz H H F OH XXVIH-49-3 p-Br-Ph H H CHCCH,), Bz H H F OH XXVHI-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz H H F OH XXVHI-49-5 p-Br-Ph H H CH2Ph Bz H H F OH XXVUI-49-6 p-Br-Ph H H CH2-indol-3-yl Bz H H F OH XXVHI-49-7 p-Br-Ph H H CH2CH2SCH3 Bz H H F OH XXVHI-49-8 p-Br-Ph * H * Bz H H F OH ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -591- WO 2008/121634

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Table XXVIII-50.

R1 R2 -r"- "R35 R4 R5 R* X Y XXVIH-50-1 p-I-Ph H H H Bz H H F OH XXVIII-50-2 p-I-Ph H H ch3 Bz H H F OH XXVIII-50-3 p-I-Ph H H CH(CH3)2 Bz H H F OH XXVIII-50-4 p-l-Ph H H CH2CH(CH3)2 Bz H H F OH XXVIII-50-5 p-I-Ph H H CH2Ph Bz H H F OH XXVII1-506 p-I-Ph H H CH2-indol-3-yl Bz H H F OH XXVIH-50-7 p-I-Ph H H ch2ch2sch3 Bz H H F OH XXVIII-50-8 p-I-Ph * H * Bz H H F OH *R2 and Rejoined together by (CHajb to form five-membered ring.

XXIX

Table XXIX-1.

Ns R1 R2 "R31" Rjb R4 Rs R6 X Y XXIX-1-1 ch3 H H H CH3 H CH3 F OH XXIX-1-2 ch3 H H ch3 ch3 H ch3 F OH XXIX-1-3 ch3 H H CHCCHah ch3 H ch3 F OH XXIX-1-4 ch3 H H CH2CH(CH3)2 ch3 H ch3 F OH XXIX-1-5 ch3 H H CH2Ph ch3 H ch3 F OH XXIX-1-6 ch3 H H CH2-indol-3-yi ch3 H ch3 F OH XXIX-1-7 ch3 H H CH2CH2SCH3 ch3 H ch3 F OH XXIX-1-8 ch3 lb t * H * ch3 H ch3 F OH *R2 and Rejoined together by (CH^ to form five-membered ring. 2983472-1 -592- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXIX-2.

Xs r R2 R3a R3b r3" R6 X Y XXIX-2-1 Et H H H ch3 H ch3 F OH XXIX-2-2 Et H H ch3 ch3 H ch3 F OH XXIX-2-3 Et H H CH(CH3)2 ch3 H ch3 F OH XXIX-2-4 Et H H CH2CH(CH3)2 ch3 H ch3 F OH XXIX-2-5 Et H H CH2Ph ch3 H ch3 F OH XXIX-2-6 Et H H CH2-indol-3-yl ch3 H ch3 F OH XXIX-2-7 Et H H CH2CH2SCH3 ch3 H ch3 F OH XXIX-2-8 Et * H * ch3 H ch3 F OH *R2 and Rejoined together by (0½¼ to form five-membered ring.

Table XXIX-3.

X° R Rj. R3b R4 R5 R6 X Y XXIX-3-1 H H H ch3 H ch3 F OH XXIX-3-2 'Pr H H CH3 ch3 H ch3 F OH XXIX-3-3 'Pr H H CH(CH3)2 ch3 H ch3 F OH XXIX-3-4 'Pr H H CH2CH(CH3)2 ch3 H ch3 F OH XXIX-3-5 'Pr H H CH2Ph ch3 H ch3 F OH XXIX-3-6 'Pr H H CH2-indol-3-yl ch3 H ch3 F OH XXIX-3-7 'Pr H H CH2CH2SCH3 ch3 H ch3 F OH XXIX-3-8 'Pr ♦ H * ch3 H ch3 F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXIX-4. I 1 H RL 11 "J « .: 1

Xs R1 R2 r3. R3b R4 Rs R6 X Y XXIX-4-1 H H H ch3 Η CH3 F OH XXIX-4-2 'Bu H H CH3 ch3 H ch3 F OH ΧΧΪΧ-4-3 'Bu H H CHCCH,), ch3 H ch3 F OH XXIX-4-4 'Bu H H CH2CH(CH3)2 ch3 H ch3 F OH XXIX-4-5 'Bu H H CH2Ph ch3 H ch3 F OH XXIX-4-6 'Bu H H CH2-indol-3-yI ch3 H ch3 F OH XXIX-4-7 'Bu H H ch2ch2sch3 ch3 H ch3 F OH XXIX-4-8 *T»2 frR 'Bu lb · . * H * ch3 H ch3 F OH *R2 and R3b joined together by (CHafc to form five-membered ring. 2983472-1 -593- WO 2008/121634

Docket No. 60137.OO34WOU1 PCT/US2008/058183

Table XXIX-5.

X° R1 R2 R3i“ “r” R4 R5" R6 X Y XX1X-5-1 Ph H H H ch3 H ch3 F OH XXIX-5-2 Ph H H ch3 ch3 H ch3 F OH XXIX-5-3 Ph H H CH(CH3)2 ch3 H ch3 F OH XXIX-5-4 Ph H H CH2CH(CH3)2 ch3 H ch3 F OH XXIX-5-5 Ph H H CH3Ph ch3 H ch3 F OH XXIX-5-6 Ph H H CH2-indol-3-yl ch3 H ch3 F OH XXIX-5-7 Ph H H CH2CH2SCH3 ch3 H ch3 F OH XXIX-5-8 ♦ in Ph 3ETT * H ♦ ch3 H ch3 F OH *R2 and Rejoined together by (Cl-hb to form five-membered ring.

Table XXIX-6.

Xs R1 R2 rTi “R36 R4 R° X Y XXIX-6-1 p-Me-Ph H H H CH3 H CH3 F OH XXIX-6-2 p-Me-Ph H H CH3 ch3 H ch3 F OH XXIX-6-3 p-Me-Ph H H CH(CH3)2 ch3 H ch3 F OH XXIX-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 H ch3 F OH XXIX-6-5 p-Me-Ph H H CH2Ph ch3 H ch3 F OH XXIX-6-6 p-Me-Ph H H CH2-indoI-3-yl ch3 H ch3 F OH XXIX-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 H ch3 F OH XXIX-6-8 p-Me-Ph * H * ch3 H ch3 F OH *R2 and R3b joined together by (CPhh to form five-membered ring. 5 Table XXIX-7.

--- t 1. IL - -''T

X2 R1 Ra R3a Rib R4 R5 R6 X Y XXIX-7-1 p-F-Ph H H H CH3 Η ch3 F OH XXIX-7-2 p-F-Ph H H CH3 ch3 H ch3 F OH XXIX-7-3 p-F-Ph H H CHiCHjh ch3 Η ch3 F OH XXIX-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 H ch3 F OH XXIX-7-6 p-F-Ph H H CH2Ph ch3 Η ch3 F OH XXIX-7-7 p-F-Ph H H CH2-indol-3-yl ch3 Η ch3 F OH XXIX-7-8 p-F-Ph H H CH2CH2SCH3 ch3 Η ch3 F OH XXIX-7-20 p-F-Ph * H * ch3 Η ch3 F OH ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -594- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXIX-8.

Ns Rl R2 “r35" Ί?6 TT” Rs Rb X Y XXIX-8-1 p-CI-Ph H H H ch3 H ch3 F OH XXIX-8-2 p-Cl-Ph H H ch3 ch3 H ch3 F OH XXIX-8-3 p-Cl-Ph H H CH(CH3)2 ch3 H ch3 F OH XXIX-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 H ch3 F OH XXIX-8-5 p-Ci-Ph H H CH2Ph ch3 H ch3 F OH XXIX-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 H ch3 F OH XXIX-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 H ch3 F OH XXIX-8-8 p-Cl-Ph + H * ch3 H ch3 F OH *R2 and Rejoined together by (CHbk to form five-membered ring.

Table XXIX-9.

Ns R1 R2 R“ R3b R4 R3 R6 X Y XXIX-9-1 p-Br-Ph H H H ch3 H CH3 F OH XXIX-9-2 p-Br-Ph H H ch3 ch3 H ch3 F OH XXIX-9-3 p-Br-Ph H H CH(CH3)2 ch3 H ch3 F OH XXIX-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 H ch3 F OH XXIX-9-6 p-Br-Ph H H CH2Ph ch3 H ch3 F OH XXIX-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 H ch3 F OH ΧΧΪΧ-9-8 p-Br-Ph H H CH2CH2SCH3 ch3 H ch3 F OH XXIX-9-20 p-Br-Ph * H ♦ ch3 H ch3 F OH *R2 and RJb joined together by (CHib to form five-membered ring. 5 Table XXIX-10. 1 i n Jin ill·........ rr > "

Ns R' R2 R3a R3b R4 Rs Rb X Y XXIX-10-1 p-I-Ph H H H CH3 H CH3 F OH XXIX-10-2 p-I-Ph H H ch3 ch3 Η ch3 F OH XXIX-10-3 p-I-Ph H H CH(CH3)2 ch3 Η ch3 F OH XXIX-10-4 p-I-Ph H H CH2CH(CH3)2 ch3 Η ch3 F OH XXIX-10-5 p-I-Ph H H CH2Ph ch3 Η ch3 F OH XXIX-10-6 p-I-Ph H H CH2-indol-3-yl ch3 Η ch3 F OH XXIX-10-7 p-I-Ph H H CH2CH2SCH3 ch3 Η ch3 F OH XXIX-10-8 jnJb p-I-Ph ♦ H * ch3 Η ch3 F OH ♦R2 and R5b joined together by (CH2)3 to form five-membered ring. 2983472-1 - 595 - WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXIX-11.

Ns R1 R2 R3" R4 R3 R4 X Y XXIX-11-1 ch3 H H H Et H ch3 F OH XXIX-11-2 ch3 H H ch3 Et H ch3 F OH XXIX-11-3 ch3 H H CH(CH3)2 Et H ch3 F OH XXIX-11-4 ch3 H H CH2CH(CH3)2 Et H ch3 F OH XXIX-11-5 ch3 H H CH2Ph Et H ch3 F OH XXIX-11-6 ch3 H H CH2-indol-3-yl Et H ch3 F OH XXIX-11-7 ch3 H H CH2CH2SCH3 Et H ch3 F OH XXIX-I1-8 ch3 * H * Et H ch3 F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXIX-12.

Ns R R4 r3B R3b R4 R3 R6 X Y XXIX-12-1 Et H H H Et H CH3 F OH XXIX-12-2 Et H H ch3 Et H ch3 F OH XXIX-12-3 Et H H CH(CH3)2 Et H ch3 F OH XXIX-12-4 Et H H CH2CH(CH3)2 Et H ch3 F OH XXIX-12-5 Et H H CH2Ph Et H ch3 F OH XXIX-12-6 Et H H CH2-indol-3-yl Et H ch3 F OH XXIX-12-7 Et H H CH2CH2SCH3 Et H ch3 F OH XXIX-12-8 Et ♦ H * Et H ch3 F OH *R2 and Rejoined together by (0-12)3 to form five-membered ring. 5 Table XXIX-13.

' I " *2 M ' RL—11 1 ' J 1 J

Ns R R2 Rj. R3b R4 R3 R6 X Y XXIX-13-1 'Pr H H H Et H ch3 F OH XXIX-13-2 'Pr H H ch3 Et H ch3 F OH XXIX-13-3 fPr H H CH(CH3)2 Et H ch3 F OH XXIX-13-4 'Pr H H CH2CH(CH3)2 Et H ch3 F OH XXIX-13-5 'Pr H H CH2Ph Et H ch3 F OH XXIX-13-6 fpr H H CH2-indol-3-yl Et H ch3 F OH XX1X-137 'Pr H H ch2ch2sch3 Et H ch3 F OH XXIX-13-8 /Pr * H * Et H ch3 F OH *R2 and RJt> joined together by (CH2)3 to form five-membered ring. 2983472-1 -596- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXIX-14.

Xs R‘ R2 Rjb R4 R3 R6 X Y XXIX-14-1 'Bu H H H Et H ch3 F OH XXIX-14-2 'Bu H H ch3 Et H ch3 F OH XXIX-14-3 'Bu H H CH(CH3)2 Et H ch3 F OH XXIX-14-4 'Bu H H CH2CH(CH3) Et H ch3 F OH XXIX-14-5 'Bu H H 2 CH2Ph Et H ch3 F OH XXIX-14-6 'Bu H H CHrindol-3- yi Et H ch3 F OH XXIX-14-7 'Bu H H ch2ch2sch Et H ch3 F OH XXIX-14-8 'Bu ♦ H 3 * Et H ch3 F OH *R2 and joined together by (CH2)3 to form five-membered ring.

Table XX1X-15.

Xs R R2 R3> Rjb R4 Rs R6 X Y XXIX-15-1 Ph H H H Et H ch3 F OH XX1X-15-2 Ph H H ch3 Et H ch3 F OH XXIX-15-3 Ph H H CH(CH3)2 Et H ch3 F OH XXIX-15-4 Ph H H CH2CH(CH3)2 Et H ch3 F OH XXIX-15-5 Ph H H CH2Ph Et H ch3 F OH XXIX-15-6 Ph H H CH2-indol-3-yl Et H ch3 F OH XXIX-15-7 Ph H H CH2CH2SCH3 Et H ch3 F OH XXIX-15-8 Ph * H * Et H ch3 F OH ' *R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XXIX-16. — I — . I Ml .11..11- I I.,,·.—— -

Xs R1 R* R3· R3b R4 R3 R$ X Y XXIX-16-1 p-Me-Ph H H H Et H CH3 F OH XXIX-16-2 p-Me-Ph H H ch3 Et H ch3 F OH XXIX-16-3 p-Me-Ph H H CHCCH^ Et H ch3 F OH XXIX-16-4 p-Me-Ph H H CH2CH(CH3)2 Et H ch3 F OH XXIX-16-5 p-Me-Ph H H CH2Ph Et H ch3 F OH XXIX-16-6 p-Me-Ph H H CH2-indol-3-yl Et H ch3 F OH XXIX-16-7 p-Me-Ph H H CH2CH2SCH3 Et H ch3 F OH XXIX-16-8 p-Me-Ph * H * Et H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 29S3472-1 -597- WO 2008/121634

Docket No. 60I37.0034WOU1 PCT/US2008/058183

Table XXIX-17.

Xfi R1 IF r3. R3b Tr” R5 R6 X Y XXIX-17-1 p-F-Ph H H H Et H ch3 F OH XXIX-17-2 p-F-Ph H H ch3 Et H ch3 F OH XXIX-17-3 p-F-Ph H H CH(CH3)2 Et H ch3 F OH XXIX-17-4 p-F-Ph H H CH2CH(CH3)2 Et H ch3 F OH XXIX-17-5 p-F-Ph H H CH2Ph Et H ch3 F OH XXIX-17-6 p-F-Ph H H CHrindol-3-yl Et H ch3 F OH XXIX-17-7 p-F-Ph H H CH2CH2SCH3 Et H ch3 F OH XXIX-17-8 p-F-Ph * H ♦ Et H ch3 F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXIX-18.

Rl RJ R5' R3b R4 Rs [c X Y XXIX-18-1 p-Cl-Ph H H H Et H CH3 F OH XXIX-18-2 p-Cl-Ph H H CH3 Et H ch3 F OH XXIX-18-3 p-Cl-Ph H H CH(CH3)2 Et H ch3 F OH XXIX-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H ch3 F OH XXIX-18-5 p-Cl-Ph H H CH2Ph Et H ch3 F OH XXIX-18-6 p-Cl-Ph H H CH2-indol-3-yl Et H ch3 F OH XXIX-18-7 p-Cl-Ph H H CH2CH2SCH3 Et H ch3 F OH XXIX-18-8 p-Cl-Ph * H ♦ Et H ch3 F OH *R2 and RJb joined together by (CH^ to form five-membered ring. 5 Table XXIX-19. , i n~ j j

Xs R1 R2 R3· R3b R4 Rs R* X Y XXIX-19-1 p-Br-Ph H H H Et Η CH3 F OH XXIX-19-2 p-Br-Ph H H CH3 Et H ch3 F OH XXIX-19-3 p-Br-Ph H H CHiCH^ Et H ch3 F OH XXIX-19-4 p-Br-Ph H H CH2CH(CH3)2 Et H ch3 F OH XXIX-19-5 p-Br-Ph H H CH2Ph Et H ch3 F OH XXIX-19-6 p-Br-Ph H H CH2-indol-3-yl Et H ch3 F OH XXIX-19-7 p-Br-Ph H H ch2ch2sch3 Et H ch3 F OH XXIX-19-8 p-Br-Ph * H * Et H ch3 F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -598- WO 2008/121634

Docket No. 6OI37.0034WOU1 PCT/US2008/058183

Table XXIX-20.

R‘ i?’ R3a "R35 R4 R6 X Y XXIX-20-1 p-I-Ph H H H Et H ch3 F OH XXIX-20-2 p-I-Ph H H ch3 Et H ch3 F OH XXIX-20-3 p-I-Ph H H CH(CH3)2 Et H ch3 F OH XXIX-20-4 p-I-Ph H H CH2CH(CH3)2 Et H ch3 F OH XXIX-20-5 p-I-Ph H H CH2Ph Et H ch3 F OH XXIX-20-6 p-I-Ph H H CH2-indol-3-yl Et H ch3 F OH XXIX-20-7 p-I-Ph H H CH2CH2SCH3 Et H ch3 F OH XXIX-20-8 p-I-Ph * H * Et H ch3 F OH *R2 and R36 joined together by (CH2)3 to form five-membered ring.

Table XXIX-21.

Ns R1 R2 "r"" "r® R4 r! R* X Y XXIX-21-1 ch3 H H H 'Pr H ch3 F OH XXIX-21-2 ch3 H H ch3 ipr H ch3 F OH XXIX-21-3 ch3 H H CH(CH3)2 ipr H ch3 F OH XXIX-21-4 ch3 H H CH2CH(CH3)2 'Pr H ch3 F OH XXIX-21-5 ch3 H H CH2Ph 'Pr H ch3 F OH XXIX-21-6 ch3 H H CH2-indol-3-yl 'Pr H ch3 F OH XXIX-21-7 ch3 H H CH2CH2SCH3 Tr H ch3 F OH XXIX-21-8 ch3 * H * 'Pr H ch3 F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXIX-22. .. - t H 5L " J'' 2···Γ J- -

N° R R2 R3a R3b R4 R5 R6 X Y XXIX-22-1 Et H H H ~w H ch3 F OH XXIX-22-2 Et H H CH3 'Pr H ch3 F OH XXIX-22-3 Et H H CHiC^h 'Pr Η ch3 F OH XXIX-22-4 Et H H ΟΗ2ΟΗ(ΟΗ3)2 'Pr H ch3 F OH XXIX-22-5 Et H H CH2Ph 'Pr H ch3 F OH XXIX-22-6 Et H H CHrindoI-3-yl 'Pr H ch3 F OH XXIX-22-7 Et H Η CH2CH2SCH3 'Pr H ch3 F OH XXIX-22-8 ' *«2 ''j'VCJb Et * H ♦ 'Pr H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -599- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXIX-23.

•Xs R1 R3 Ir’ "r36 R4 R6 X Y XXIX-23-1 'Pr H H H 'Pr H ch3 F OH XXIX-23-2 Tr H H ch3 'Pr H ci-i3 F OH XXIX-23-3 'Pr H H CH(CH3)2 'Pr H ch3 F OH XXIX-23-4 'Pr H H CH2CH(CH3)2 'Pr H ch3 F OH XXIX-23-5 'Pr H H CH2Ph 'Pr H ch3 F OH XXIX-23-6 'Pr H H CH2-indol-3-yl 'Pr H ch3 F OH ΧΧΪΧ-23-7 'Pr H H ch2ch2sch3 'Pr H ch3 F OH XXIX-23-8 'Pr ♦ H ♦ 'Pr H ch3 F OH *R2 and Rejoined together by (0¾^ to form five-membered ring.

Table XXIX-24.

Na R Kr R3a R3b R4 Rs R6 X Y XXIX-24-1 'Bu H H H 'Pr H CH3 F OH XXEX-24-2 'Bu H H ch3 'Pr H ch3 F OH XXIX-24-3 'Bu H H CH(CH3)2 'Pr H ch3 F OH XXIX-24-4 'Bu H H CH2CH(CH3)2 'Pr H ch3 F OH XXIX-24-5 'Bu H H CH2Ph 'Pr H ch3 F OH XXIX-24-6 'Bu H H CH2-indol-3-yl 'Pr H ch3 F OH XXIX-24-7 'Bu H H CH2CH2SCH3 'Pr H ch3 F OH XXIX-24-8 'Bu * H * 'Pr H ch3 F OH *R2 and R3° joined together by (CH2)3 to form five-membered ring. 5 Table XXIX-25.

X2 R1 R3 R3a R3b R4 RJ R6 X Y XXIX-25-1 Ph H H H 'Pr H ch3 F OH XXIX-25-2 Ph H H ch3 'Pr H ch3 F OH XXIX-25-3 Ph H H CH(CH3)2 'Pr H ch3 F OH XXIX-25-4 Ph H H ΟΗ2ΟΗ(ΟΗ3)2 'Pr H ch3 F OH XXIX-25-5 Ph H H CH2Ph 'Pr H ch3 F OH XXIX-25-6 Ph H H CHrindol-3-yl /pr H ch3 F OH XXIX-25-7 Ph H H CH2CH2SCH3 'Pr H ch3 F OH XXIX-25-8 Ph * H * 'Pr H ch3 F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -600- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXIX-26.

Ns Rl R2 r3b R3b “S’" r^ X Y XXIX-26-1 p-Me-Ph H H H 'Pr H ch3 F OH XXIX-26-2 p-Me-Ph H H ch3 'Pr H ch3 F OH XXIX-26-3 p-Me-Ph H H CH(CH3)2 'Pr H ch3 F OH XXIX-26-4 p-Me-Ph H H CH2CH(CH3)2 'Pr H ch3 F OH XXIX-26-5 p-Me-Ph H H CH2Ph 'Pr H ch3 F OH XXIX-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr H ch3 F OH XXIX-26-7 p-Me-Ph H H CH2CH2SCH3 'Pr H ch3 F OH XXIX-26-8 p-Me-Ph * H * 'Pr H ch3 F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXIX-27.

Na Rl R3 R3b R4 R3 R6 X Y XXIX-27-1 p-F-Ph H H H “Ψτ" H CH3 F OH XXIX-27-2 p-F-Ph H H CH3 'Pr H ch3 F OH XXIX-27-3 p-F-Ph H H CH(CH3)2 'Pr H ch3 F OH XXIX-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr H ch3 F OH XXIX-27-5 p-F-Ph H H CH2Ph 'Pr H ch3 F OH XXIX-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr H ch3 F OH XXIX-27-7 p-F-Ph H H CH2CH2SCH3 'Pr H ch3 F OH XXIX-27-8 p-F-Ph * H * Tr- H ch3 F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXIX-28. — I .........-W HL " - . J 1

Xa Rl Rj. R3b R4 R3 Rfc X Y XXIX-28-1 p-Cl-Ph H H H 'Pr H CH3 F OH XXIX-28-2 p-Cl-Ph H H CH3 'Pr H ch3 F OH XXIX-28-3 p-Cl-Ph H H CHCCH^ 'Pr H ch3 F OH XXIX-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr H ch3 F OH XXIX-28-5 p-Cl-Ph H H CH2Ph 'Pr H ch3 F OH XXIX-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr H ch3 F OH XXIX-28-7 p-Cl-Ph H H CH2CH2SCH3 'Pr H ch3 F OH XXIX-28-8 ~7773E p-Cl-Ph 1 · · J i * H * 'Pr H ch3 F OH *R* and R3b joined together by (CH2)3 to form five-membered ring. 2983472-] -601- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXIX-29.

te R1 R2 Rja r35 R4 R5" Ra X Y XXIX-29-1 p-Br-Ph H H H "W H ch3 F OH XXIX-29-2 p-Br-Ph H H ch3 'Pr H ch3 F OH XXIX-29-3 p-Br-Ph H H CH(CH3)2 'Pr H ch3 F OH XXIX-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr H ch3 F OH XXIX-29-5 p-Br-Ph H H CH2Ph 'Pr H ch3 F OH XXIX-29-6 p-Br-Ph H H CH2-indol-3-yl Tr H ch3 F OH XXIX-29-7 p-Br-Ph H H CH2CH2SCH3 *Pr H ch3 F OH XXIX-29-8 p-Br-Ph * H * 'Pr H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XX1X-30.

Xa R1 R2 R3. R3b R4 R3 X Y XXIX-30-1 p-I-Ph H H H 'Pr H ch3 F OH XXIX-30-2 p-I-Ph H H CH3 'Pr H ch3 F OH XXIX-30-3 p-I-Ph H H CHCCH,), 'Pr H ch3 F OH XXIX-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr H ch3 F OH XXIX-30-5 p-I-Ph H H CH2Ph fpr H ch3 F OH XXIX-30-6 p-I-Ph H H CH2-indol-3-yl *Pr H ch3 F OH XXIX-30-7 p-I-Ph H H CH2CH2SCH3 *Pr H ch3 F OH XXIX-30-8 p-I-Ph * H * Tr H ch3 F OH ♦R2 and RJ0 joined together by to form five-membered ring.

Table XXIX-31.

Xa R1 RJ r35" "R35 R4 ΊΓ R* X Y XXIX-31-1 CH3 Η Η Η "Bu H ch3 F OH XXIX-31-2 ch3 H Η ch3 "Bu H ch3 F OH XXIX-31-3 ch3 Η Η CHiCHah "Bu H ch3 F OH XXIX-31-4 ch3 Η Η CH2CH(CH3)2 "Bu H ch3 F OH XXIX-31-5 ch3 Η Η CH2Ph "Bu Η ch3 F OH XXIX-31-6 ch3 Η Η CH2-indol-3-yl "Bu H ch3 F OH XXIX-31-7 ch3 Η Η ch2ch2sch3 "Bu H ch3 F OH XXIX-31-8 ch3 l· · ♦ ♦ Η * "Bu H ch3 F OH *R2 and Rejoined together by (Clfeb to form five-membered ring. 2983472-1 -602- WO 2008/121634 •DocketNo. 60137.0034WOU1 PCT/US2008/058183

Table XXIX-32.

x° R1 Ra R'fl “r35 R4 R6 X Y XXIX-32-1 Et H H H "Bu H ch3 F OH XXIX-32-2 Et H H ch3 "Bu H ch3 F OH XXIX-32-3 Et H H cto "Bu H ch3 F OH XXIX-32-4 Et H H CH2CH(CH3)2 "Bu H ch3 F OH XXIX-32-5 Et H H CH2Ph "Bu H ch3 F OH XXJX-32-6 Et H H CH2-indol-3-yl "Bu H ch3 F OH XXIX-32-7 Et H H CH2CH2SCH3 "Bu H ch3 F OH XXIX-32-8 Et * H * "Bu H ch3 F OH *R2 and Rejoined together by (CH2b to form five-membered ring.

Table XXIX-33.

Xs "Κ RJ r3« R3b R3 R6 X Y XXIX-33-1 'Pr H H H "Bu H ch3 F OH XX1X-33-2 'Pr H H ch3 "Bu H ch3 F OH XXIX-33-3 'Pr H H CH(CH3)2 "Bu H ch3 F OH XXIX-33-4 'Pr H H CH2CH(CH3)2 "Bu H ch3 F OH XXIX-33-5 'Pr H H CHaPh "Bu H ch3 F OH XXIX-33-6 'Pr H H CH2-indol-3-yl "Bu H ch3 F OH XXIX-33-7 ipr H H ch2ch2sch3 "Bu H ch3 F OH XXIX-33-8 'Pr * H * "Bu H ch3 F OH ♦R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XXIX-34. .,-1 HL 4 l '"I"

X2 r' R2 r3. R3b R3 R6 X Y XXIX-34-1 'Bu H H H "Bu H ch3 F OH XXIX-34-2 'Bu H H CH3 "Bu H ch3 F OH XXIX-34-3 'Bu H H CH(CH3)2 "Bu H ch3 F OH XXIX-34-4 'Bu H H CH2CH(CH3)2 "Bu H ch3 F OH XXIX-34-5 *Bu H H CH2Ph "Bu H ch3 F OH XXIX-34-6 'Bu H H CH2-indol-3-yl "Bu H ch3 F OH XXIX-34-7 'Bu H H CH2CH2SCH3 "Bu H ch3 F OH XXIX-34-8 'Bu ♦ H ♦ "Bu H ch3 F OH ♦R2 and RJb joined together by (CHabt0 ^orrn five-membered ring. 2983472-1 -603- W° 2008O2J634No gQl 37.0034W0U1 PCT/US2008/058183

Table XXIX-35.

Xa Rl R3 R3a r36 R4 Rs r6 X Y XXIX-35-1 Ph H H H "Bu H ch3 F OH XXIX-35-2 Ph H H ch3 "Bu H ch3 F OH XXIX-35-3 Ph H H CH(CH3)2 "Bu H ch3 F OH XXIX-35-4 Ph H H CH2CH(CH3)2 "Bu H ch3 F OH XXIX-35-5 Ph H H CH2Ph "Bu H ch3 F OH XXIX-35-6 Ph H H CH2-indol-3-yl "Bu H ch3 F OH XXIX-35-7 Ph H H CH2CH2SCH3 "Bu H ch3 F OH XXIX-35-8 Ph ♦ H * "Bu H ch3 F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring”

Table XXIX-36.

Xa "r1 R3 R3a - - - R4 R^ X Y XXIX-36-1 p-Me-Ph H H H "Bu H CH3 F OH XXIX-36-2 p-Me-Ph H H CH3 "Bu H ch3 F OH XXIX-36-3 p-Me-Ph H H CH(CH3)2 "Bu H ch3 F OH XXIX-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu H ch3 F OH XXIX-36-5 p-Me-Ph H H CH2Ph "Bu H ch3 F OH XXIX-36-6 p-Me-Ph H H CH2-indol-3-yl ”Bu H ch3 F OH XXIX-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu H ch3 F OH XXIX-36-8 p-Me-Ph ♦ H + "Bu H ch3 F OH *R2 and RJ0 joined together by (CH2)3 to form five-membered ring. 5 Table XX1X-37.__

Xa R1 R3 R3" R3b R4 R5 R6 X Y XXIX-37-1 p-F-Ph H H H "Bu H CH3 F OH XXIX-37-2 p-F-Ph H H ch3 "Bu H ch3 F OH XXIX-37-3 p-F-Ph H H CH(CH3)2 "Bu H ch3 F OH XXIX-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu H ch3 F OH XXIX-37-5 p-F-Ph H H CH2Ph "Bu H ch3 F OH XXIX-37-6 p-F-Ph H H CH2-indol-3-yl "Bu H ch3 F OH XXJX-37-7 p-F-Ph H Η CH2CH2SCH3 "Bu H ch3 F OH XXIX-37-8 . «3b p-F-Ph 1 ♦ ’ J _i_ ♦ H * "Bu H ch3 F OH W Rl ' ......... *R and R joined together by (CH2)3 to form five-membered ring. 2983472-1 -604- WO 2008/121634Νθ> 60137.0034WOU1 PCT/US2008/058183

Table XXIX-38.

X2 R1 RJ r3b Rjb R5 R6 X Y XXIX-38-1 p-Cl-Ph H H H "Bu H ch3 F OH XXIX-38-2 p-Cl-Ph H H ch3 "Bu H ch3 F OH XXIX-38-3 p-Cl-Ph H H CH(CH3)2 "Bu H ch3 F OH XX1X-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H ch3 F OH XXIX-38-5 p-Cl-Ph H H CH2Ph "Bu H ch3 F OH XXIX-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu H ch3 F OH XXIX-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu H ch3 F OH XXIX-38-8 p-Cl-Ph * H * "Bu H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXIX-39.

Xa R1 R2 R3" Rib R4 R5 R6 X Y XXIX-39-1 p-Br-Ph H H H "Bu H ch3 F OH XXIX-39-2 p-Br-Ph H H ch3 "Bu H ch3 F OH XXIX-39-3 p-Br-Ph H H CH(CH3)2 "Bu H ch3 F OH XXIX-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu H ch3 F OH XXIX-39-5 p-Br-Ph H H CH2Ph "Bu H ch3 F OH XX1X-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu H ch3 F OH XXIX-39-7 p-Br-Ph H H CH2CH2SCH3 "Bu H ch3 F OH XXIX-39-8 p-Br-Ph * H * "Bu H ch3 F OH fj ' "“‘ίΗ "*b in .....n i I,, *R and R joined together by (CH2)3 to form five-membered ring. 5 Table XX1X-40. '1 ..... iL .,,,. .

X2 R‘ R2 R31 R3” R4 Rs R6 X Y XXIX-40-1 p-I-Ph H H H "Bu H ch3 F OH XXIX-40-2 p-I-Ph H H CH3 "Bu H ch3 F OH XXIX-40-3 p-I-Ph H H CH(CH3)2 "Bu H ch3 F OH XXIX-4 0-4 p-I-Ph H H CH2CH(CH3)2 "Bu H ch3 F OH XXIX-40-5 p-I-Ph H H CH2Ph "Bu H ch3 F OH XXIX-40-6 p-I-Ph H H CHrindol-3-yl "Bu H ch3 F OH XXIX-40-7 p-I-Ph H H CH2CH2SCH3 "Bu H ch3 F OH XXIX-40-8 p-I-Ph * H * "Bu H ch3 F OH *R2 and RiSjoined together by (CH2)3 to form five-membered ring. 2983472-1 -605- WO 2008J2J634NOt 60137.0034WOU1 PCT/US2008/058183

Table XXIX-41.

Xs R1 R2 R3" R3b R4 R* Ί? X Y XXIX-41-1 ch3 H H H Bz H ch3 F OH XXIX-41-2 ch3 H H ch3 Bz H ch3 F OH XXIX-41-3 ch3 H H CH(CH3)2 Bz H ch3 F OH XXIX-41-4 ch3 H H CH2CH(CH3)2 Bz H ch3 F OH XXIX-41-5 ch3 H H CH2Ph Bz H ch3 F OH XXIX-41-6 ch3 H H CH2-indol-3-yl Bz H ch3 F OH XXIX-41-7 ch3 H H CH2CH2SCH3 Bz H ch3 F OH XXIX-41-8 ch3 * H * Bz H ch3 F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXIX-42.

X2 R* R2 R3’ R3b Ic fv R6 X Y XXIX-42-1 Et H H H Bz H ch3 F OH XXIX-42-2 Et H H ch3 Bz H ch3 F OH XXIX-42-3 Et H H CH(CH3h Bz H ch3 F OH XXIX-42-4 Et H H CH2CH(CH3)2 Bz H ch3 F OH XXIX-42-5 Et H H CH2Ph Bz H ch3 F OH XXIX-42-6 Et H H CH2-indol-3-yl Bz H ch3 F OH XXIX-42-7 Et H H CH2CH2SCH3 Bz H ch3 F OH XXIX-42-8 Et * H * Bz H ch3 F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXIX-43. "" '1 mi-

Xs R R2 r3. R3b R4 R5 R6 X Y XXIX-43-1 jPr H H H Bz H ch3 F OH XXIX-43-2 'Pr H H CH3 Bz H ch3 F OH XXIX-43-3 /Pr H H CHiCHah Bz H ch3 F OH XXIX-43-4 'Pr H H CHjCHfCH^ Bz H ch3 F OH XXIX-43-5 'Pr H H CH2Ph Bz H ch3 F OH XXIX-43-6 'Pr H H CH2-indol-3-yl Bz H ch3 F OH XXIX-43-7 'Pr H H CH2CH2SCH3 Bz H ch3 F XXIX-43-8 'Pr * H * Bz H ch3 F OH *R2 and Rejoined together by (Cthb to form five-membered ring. 2983472-1 -606- WO 2008/Π1634Νθί 60137i0034WOU1 PCT/US2008/058183

Table XXIX-44.

X2 R1 R3 IT Rs R6 X Y XXIX-44-1 'Bu H H H Bz H ch3 F OH XXIX-44-2 'Bu H H ch3 Bz H ch3 F OH XXIX-44-3 'Bu H H CH(CH3)2 Bz H ch3 F OH XXIX-44-4 'Bu H H CH2CH(CH3)2 Bz H ch3 F OH XXIX-44-5 'Bu H H CH2Ph Bz H ch3 F OH XX1X-44-6 'Bu H H CH2-indol-3-yl Bz H ch3 F OH XXIX-44-7 'Bu H H CH2CH2SCH3 Bz H ch3 F OH XXIX-44-8 'Bu * H * Bz H ch3 F OH *R2 and R3b joined together by (012)3 to form five-membered ring.

Table XXIX-45.

Xi R R3 RJe R3b R4 Rs R6 X Y XXIX-45-1 Ph H H H Bz H CH3 F OH XXIX-45-2 Ph H H ch3 Bz H ch3 F OH XXIX-45-3 Ph H H CH(CH3)2 Bz H ch3 F OH XX1X-45-4 Ph H H CH2CH(CH3)2 Bz H ch3 F OH XXIX-45-5 Ph H H CH2Ph Bz H ch3 F OH XXIX-45-6 Ph H H CH2-indol-3-yl Bz H ch3 F OH XXIX-45-7 Ph H H CH2CH2SCH3 Bz H ch3 F OH XXIX-45-8 Ph * H * Bz H ch3 F OH *R2 and R^loined together by (CHih to form five-membered ring. 5 Table XXIX-46._________

X2 R1 R3 R3" R35 R4 R! R6 X Y XXIX-46-1 p-Me-Ph H H H Bz H CH3 F OH XXIX-46-2 p-Me-Ph H H CH3 Bz H ch3 F OH XXIX-46-3 p-Me-Ph H H CH(CH3)2 Bz H ch3 F OH XXIX-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz H ch3 F OH XXIX-46-5 p-Me-Ph H H CH2Ph Bz H ch3 F OH XXIX-46-6 p-Me-Ph H H CH2-indol-3-yl Bz H ch3 F OH XXIX-46-7 p-Me-Ph H H CH2CH2SCH3 Bz H ch3 F OH XXIX-46-8 p-Me-Ph * H ♦ Bz H ch3 F OH *R2 and Rejoined together by (CHjb to form five-membered ring. 2983472-1 -607- W0 20080Vckci4Mo. 60137.0034WOU1 PCT/US2008/058183

Table XXIX-47.

Ns Rl R2 RJa "r* Ί?“ RJ R6 X Y XXIX-47-1 p-F-Ph H H H Bz H ch3 F OH XXIX-47-2 p-F-Ph H H ch3 Bz H ch3 F OH XXIX-47-3 p-F-Ph H H CH(CH3)2 Bz H ch3 F OH XXIX-47-4 p-F-Ph H H CH2CH(CH3)2 Bz H ch3 F OH XXIX-47-5 p-F-Ph H H CH2Ph Bz H ch3 F OH XXIX-47-6 p-F-Ph H H CH2-indol-3-yl Bz H ch3 F OH XXIX-47-7 p-F-Ph H H CH2CH2SCH3 Bz H ch3 F OH XXIX-47-8 p-F-Ph ♦ H ♦ Bz H ch3 F OH *R2 and R3b joined together by (012)3 to form five-membered ring.

Table XXIX-48.

Ns R’ R3 r3. R3b R4 Rs R6 X Y XXIX-48-1 p-Cl-Ph H H H Bz H ch3 F OH XXIX-48-2 p-Cl-Ph H H ch3 Bz H ch3 F OH XXIX-48-3 p-Cl-Ph H H CH(CH3)2 Bz H ch3 F OH XXIX-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H ch3 F OH XXIX-48-5 p-Cl-Ph H H CH2Ph Bz H ch3 F OH XXIX-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz H ch3 F OH XXIX-48-7 p-Cl-Ph H H CH2CH2SCH3 Bz H ch3 F OH XXIX-48-8 p-Cl-Ph * H * Bz H ch3 F OH *R^ and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXIX-49. 1 H R. HL J " :-'r ' 1

Ns R‘ R2 r3‘ R3b R4 Rs X Y XXIX-49-l p-Br-Ph H H H Bz H CH3 . F OH XXIX-49-2 p-Br-Ph H H CH3 Bz H ch3 F OH XXIX-49-3 p-Br-Ph H H CH(CH3)2 Bz H ch3 F OH XXIX-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz H ch3 F OH XXIX-49-5 p-Br-Ph H H CH2Ph Bz H ch3 F OH XXIX-49-6 p-Br-Ph H H CH2-indol-3-yl Bz H ch3 F OH XXIX-49-7 p-Br-Ph H H CH2CH2SCH3 Bz H ch3 F OH XXIX-49-8 p-Br-Ph * H * Bz H ch3 F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -608- W0 2θ08ύο2ϋκετ4Νο. 60137.0034WOU1 PCT/US2008/058183

Table XXIX-50.

Ns R1 RJ R3‘ “r35 R5 X Y XXIX-50-1 p-I-Ph H H H Bz H ch3 F OH XXJLX-50-2 p-I-Ph H H ch3 Bz H ch3 F OH XXIX-50-3 p-I-Ph H H CH(CH3)2 Bz H ch3 F OH XXIX-50-4 p-I-Ph H H CH2CH(CH3)2 Bz H ch3 F OH XXIX-50-5 p-I-Ph H H CH2Ph Bz H ch3 F OH XXIX-50-6 p-I-Ph H H CH2-indol-3-yl Bz H ch3 F OH XXIX-50-7 p-I-Ph H H CH2CH2SCH3 Bz H ch3 F OH XXIX-50-8 . j T.3b p-I-Ph * H ♦ Bz H ch3 F OH ♦R* and Rejoined together by (CH2)3 to form five-membered ring

5 XXX

Table XXX-1.

Ns R1 R* R3‘ R36 R4 Rs R6 X Y XXX-1-1 ch3 H H H CH3 H F Η OH XXX-1-2 ch3 H H ch3 ch3 H F H OH XXX-1-3 ch3 H H CH(CH3)2 ch3 Η F H OH XXX-1-4 ch3 H H CH2CH(CH3)2 ch3 H F H OH XXX-1-5 ch3 H H CH2Ph ch3 Η F H OH XXX-1-6 ch3 H H CH2-indol-3-yl ch3 H F Η OH XXX-1-7 ch3 H H ch2ch2sch3 ch3 Η F H OH XXX-1-8 it, ch3 3b· · * H * ch3 H F H OH 1 ""*< III III I· Rl .ίΊ»·κι·ιΐ — ι n ι i iu.mi ι i i u——w—......... *R and R joined together by (CH2)3 to form five-membered ring. 2983472-1 -609- W° 2008/Π1634Νθί 60137.0034W0U1 PCT/US2008/058183

Table XXX-2.

Xa R1 R3 R3“” “r3® rs R6 X Y XXX-2-1 Et H H H ch3 H F H OH XXX-2-2 Et H H ch3 ch3 H F H OH XXX-2-3 Et H H CH(CH3)2 ch3 H F H OH XXX-2-4 Et H H CH2CH(CH3)2 ch3 H F H OH XXX-2-5 Et H H CH2Ph ch3 H F H OH XXX-2-6 Et H H CH2-indol-3-yl ch3 H F H OH XXX-2-7 Et H H CH2CH2SCH3 ch3 H F H OH XXX-2-8 —rr Et □FT * H * ch3 H F H OH ♦R^ and Rjb joined together by (CHib to form five-membered ring.

Table XXX-3.

Xa R1 R3 R3a r35 R4 RJ R4 X Υ XXX-3-1 H H H CH3 H F Η ΟΗ XXX-3-2 'Pr H H ch3 ch3 H F Η ΟΗ XXX-3-3 'Pr H H CH(CH3)2 ch3 Η F Η ΟΗ XXX-3-4 'Pr H H CH2CH(CH3)2 ch3 Η F Η ΟΗ XXX-3-5 'Pr H H CH2Ph ch3 Η F Η ΟΗ XXX-3-6 'Pr H H CH2-indol~3-yl ch3 Η F Η ΟΗ XXX-3-7 'Pr H H CH2CH2SCH3 ch3 Η F Η ΟΗ XXX-3-8 ~ir>2 "j”? 'Pr ♦ H * ch3 Η F Η ΟΗ *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Xa R^ R3 R3" R3t> r^ RJ R4 X Y ΧΧΧ-4-1 *Bu H H H ch3 H F H OH ΧΧΧ-4-2 'Bu H H CH3 ch3 H F H OH ΧΧΧ-4-3 H H CH(CH3)a ch3 H F H OH ΧΧΧ-4-4 'Bu H H CH2CH(CH3)2 ch3 H F H OH ΧΧΧ-4-5 'Bu H H CH2Ph ch3 H F H OH ΧΧΧ-4-6 'Bu H H CH2-indol-3-yl ch3 H F H OH ΧΧΧ-4-7 'Bu H H CH2CH2SCH3 ch3 H F H OH ΧΧΧ-4-8 “ίπτ—77 'Bu Ub ·.:. ♦ H * ch3 H F H OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -610- WO 2008/121634Νθί 60137.0034WOU1 PCT/US2008/058183

Table XXX-5.

x° R1 R2 "r35" T5 ΊΓ~ R5 R? X Y XXX-5-1 Ph H H H ch3 H F H OH XXX-5-2 Ph H H ch3 ch3 H F H OH XXX-5-3 Ph H H CH(CH3)2 ch3 H F H OH XXX-5-4 Ph H H CH2CH(CH3)2 ch3 H F H OH XXX-5-5 Ph H H CH2Ph ch3 H F H OH XXX-5-6 Ph H H CH2-indol-3-yl ch3 H F H OH XXX-5-7 Ph H H CH2CH2SCH3 ch3 H F H OH XXX-5-8 7η Ph ,3h ! * H * ch3 H F H OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXX-6.

Xa Rl r r3b R3b R4 rT R6 X Y XXX-6-1 p-Me-Ph H H H ch3 H F H OH XXX-6-2 p-Me-Ph H H ch3 ch3 H F H OH XXX-6-3 p-Me-Ph H H CH(CH3)2 ch3 H F H OH XXX-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 H F H OH XXX-6-5 p-Me-Ph H H CH2Ph ch3 H F H OH XXX-6-6 p-Me-Ph H H CH2-indol-3-yl ch3 H F H OH XXX-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 H F H OH XXX-6-8 J τι p-Me-Ph ,3b- ... ,.- « H * ch3 H F H OH *R2 and RJt> joined together by ((¾¼ to form five-membered ring. 5 Table XXX-7. —J.— -

Xa R' R2 R3. R3b R4 R6 X Y XXX-7-1 p-F-Ph H H H ch3 Η F H OH XXX-7-2 p-F-Ph H H ch3 ch3 H F H OH XXX-7-3 p-F-Ph H H CHiCHah ch3 H F H OH XXX-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 H F H OH XXX-7-6 p-F-Ph H H CH2Ph ch3 H F H OH XXX-7-7 p-F-Ph H H CH2-indol-3-yl ch3 H F H OH XXX-7-8 p-F-Ph H H CH2CH2SCH3 ch3 H F H OH XXX-7-20 p-F-Ph 3b- * H ♦ ch3 H F H OH *R2 and R3b joined together by (CH2)3 to form five-membered ring? 2983472-1 -611 - WO 2008/121634 . ,Λ1„„ Aniyluzniu

juocicet No. 60137.0034WOU I PCT/US2008/058183

Table XXX-8.

Xs T R2 "R^ "r35 R4 RJ R4 X Y XXX-8-1 p-Cl-Ph H H H ch3 H F H OH XXX-8-2 p-Cl-Ph H H ch3 ch3 H F H OH XXX-8-3 p-Cl-Ph H H CH(CH3)2 ch3 H F H OH XXX-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 H F H OH XXX-8-5 p-Cl-Ph H H CH2Ph ch3 H F H OH XXX-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 H F H OH XXX-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 H F H OH XXX-8-8 p-Cl-Ph ♦ H * ch3 H F H OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXX-9.

Xa R1 R2 R3. RJb R4 R5 R6 X Y XXX-9-1 p-Br-Ph H H H ch3 H F Η OH XXX-9-2 p-Br-Ph H H ch3 ch3 H F H OH XXX-9-3 p-Br-Ph H H CH(CH3)2 ch3 H F H OH XXX-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 Η F H OH XXX-9-6 p-Br-Ph H H CH2Ph ch3 H F H OH XXX-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 H F H OH XXX-9-8 p-Br-Ph H H CH2CH2SCH3 ch3 H F H OH XXX-9-20 p-Br-Ph ♦ H ♦ ch3 H F H OH *R^ and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XXX-10. . 1 ' ...... I ' ' * H. II- 1 J' ....... f Jf

Xa R1 R2 R3" R3b R4^ R5 R4 X Y XXX-10-1 p-I-Ph H H H ch3 H F H OH XXX-10-2 p-I-Ph H H CH3 ch3 H F H OH XXX-10-3 p-I-Ph H H CHCCH^ ch3 H F H OH XXX-10-4 p-I-Ph H H ΟΗ,ΟΗίΟΗ,Χ ch3 H F H OH XXX-10-5 p-I-Ph H H CH2Ph ch3 H F H OH XXX-10-6 p-I-Ph H H CH2-indol-3-yl ch3 H F H OH XXX-10-7 p-I-Ph H H CH2CH2SCH3 ch3 H F H OH XXX-10-8 *r»7 . j nJ p-I-Ph b ; ; -J . ♦ H * ch3 H F H OH *R7 and R3b joined together by (CH2)3 to form five-membered ring 2983472-1 τ 612 - WO 2008/121634 . ηηθ/11νΛγ11 PCT/US2008/058183 uocKet No. 60137.0034WOU1

Table XXX-11.

Ns R1 r1" r3» "R* 1C R5 R6 X Y XXX-ll-1 ch3 H H H Et H F H OH XXX-11-2 ch3 H H ch3 Et H F H OH XXX-I1-3 ch3 H H CH(CH3)2 Et H F H OH XXX-11-4 ch3 H H CH2CH(CH3)2 Et H F H OH XXX-11-5 ch3 H H CH2Ph Et H F H OH XXX-11-6 ch3 H H CH2-indol-3-yl Et H F H OH XXX-11-7 ch3 H H CH2CH2SCH3 Et H F H OH XXX-11-8 ch3 ♦ H * Et H F H OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXX-12.

Na R R2 R3a R3b R4 r! R° X Y XXX-12-1 Et H H H Et H F H OH XXX-12-2 Et H H CH3 Et H F H OH XXX-12-3 Et H H CH(CH3)2 Et H F H OH XXX-12-4 Et H H CH2CH(CH3)2 Et H F H OH XXX-12-5 Et H H CH2Ph Et H F H OH XXX-12-6 Et H H CH2-indol-3-yl Et H F H OH XXX-12-7 Et H H CH2CH2SCH3 Et H F H OH XXX-12-8 Et * H ♦ Et H F H OH *R2 and RJb joined together by (0^2)3 to form five-membered ring. 5 Table XXX-13. ..... 1 M 'Mi JIL 1.11... 1 11 m

Ns R* R2 R3" R3b R4 RJ R° X Y XXX-13-1 'Pr H H H Et H F H OH XXX-13-2 /Pr H H CH3 Et H F H OH XXX-13-3 /pr H H CH(CH3)2 Et H F H OH XXX-13-4 'Pr H H CH2CH(CH3)2 Et H F H OH XXX-13-5 /Pr H H CH2Ph Et H F H OH XXX-13-6 'Pr H H CH2-indol-3-yl Et H F H OH XXX-13-7 'Pr H H CH2CH2SCH3 Et H F H OH XXX-13-8 'Pr * H ♦ Et H F H OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -613- W° 2θθ8/7υ2|634Νθι 60137O034WOU1 PCT/US2008/058183

Table XXX-14.

Xs R1 R2 R3’ Ίϊ36 R5 X Y XXX-14-1 'Bu H H H Et H F H OH XXX-14-2 'Bu H H ch3 Et H F H OH XXX-14-3 'Bu H H CH(CH3)2 Et H F H OH XXX-14-4 'Bu H H CH2CH(CH3)2 Et H F H OH XXX-14-5 ‘Bu H H CH2Ph Et H F H OH XXX-14-6 'Bu H H CH2-indol-3-yl Et H F H OH XXX-14-7 'Bu H H CH2CH2SCH3 Et H F H OH XXX-14-8 -. „3b · 'Bu * H ♦ Et H F H OH *R2 and RJb joined together by (CFhb to form five-membered ring.

Table XXX-15.

Xs R1 R2 R3a “R35 R6 X Y XXX-15-1 Ph H H H Et H F H OH XXX-15-2 Ph H H ch3 Et H F H OH XXX-15-3 Ph H H CH(CH3)2 Et H F H OH XXX-15-4 Ph H H CH2CH(CH3)2 Et H F H OH XXX-15-5 Ph H H CH2Ph Et H F H OH XXX-15-6 Ph H H CH2-indoI-3-yl Et H F H OH XXX-15-7 Ph H H CH2CH2SCH3 Et H F H OH XXX-15-8 Ph 3b * H * Et H F H OH *R2 and R31* joined together by (CH2)3 to form five-membered ring. 5 Table XXX-16. -1 1.......

Xa R1 R2 r35" R3b f? R5 R6 X Y XXX-16-1 p-Me-Ph H H H Et H F H OH XXX-16-2 p-Me-Ph H H ch3 Et H F H OH XXX-16-3 p-Me-Ph H H CH(CH3)2 Et H F H OH XXX-16-4 p-Me-Ph H H CH2CH(CH3)2 Et H F H OH XXX-16-5 p-Me-Ph H H CH2Ph Et H F H OH XXX-16-6 p-Me-Ph H H CH2-tndol-3-yl Et H F H OH XXX-16-7 p-Me-Ph H H CH2CH2SCH3 Et H F H OH XXX-16-8 p-Me-Ph Jb· · jx - * H * Et H F H OH *R2 and Rejoined together by (Cl·^ to form five-membered ring. 2983472-1 -614- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXX-17.

Ns R1 R2 r31" R3b R4 R3 R6 X Y XXX-17-1 p-F-Ph H H H Et H F H OH XXX-17-2 p-F-Ph H H ch3 Et H F H OH XXX-17-3 p-F-Ph H H CH(CH3)2 Et H F H OH XXX-17-4 p-F-Ph H H CH2CH(CH3)2 Et H F H OH XXX-17-5 p-F-Ph H H CH2Ph Et H F H OH XXX-17-6 p-F-Ph H H CH2-indol-3-yl Et H F H OH XXX-17-7 p-F-Ph H H CH2CH2SCH3 Et H F H OH XXX-17-8 p-F-Ph * H * Et H F H OH *R2 and R3b joined together by (0¼¼ to form five-membered ring.

Table XXX-18.

Ns R1 ’r3~ R34 R3b R4 R3 R6 X Y XXX-18-1 p-Cl-Ph H H H Et H F H OH XXX-18-2 p-Cl-Ph H H CH3 Et H F H OH XXX-18-3 p-Cl-Ph H H CHiCH,), Et H F H OH XXX-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H F H OH XXX-18-5 p-Cl-Ph H H CH2Ph Et H F H OH XXX-18-6 p-Cl-Ph H H CH2-indol-3-yl Et H F H OH XXX-18-7 p-Cl-Ph H H CH2CH2SCH3 Et H F H OH XXX-18-8 p-Cl-Ph * H * Et H F H OH *R2 and Rejoined together by (CHak to form five-membered ring. 5 TableXXX-19.

' ..... IIP J

Ns R' R2 R3" R3b R4 ΊΓ R6 X Y XXX-19-1 p-Br-Ph H H H Et H F H OH XXX-19-2 p-Br-Ph H H CH3 Et H F H OH XXX-19-3 p-Br-Ph H H CH(CH3)2 Et H F H OH XXX-19-4 p-Br-Ph H H CH2CH(CH3)2 Et H F H OH XXX-19-5 p-Br-Ph H H CH2Ph Et H F H OH XXX-19-6 p-Br-Ph H H CH2-indol-3-yl Et H F H OH XXX-19-7 p-Br-Ph H H CH2CH2SCH3 Et H F H OH XXX-19-8 -7"r73 p-Br-Ph bi; j a * H ♦ Et H F H OH *R2 and RJb joined together by (CI·^ to form five-membered ring. 2983472-1 -615- PCT/US2008/058183 WO 2008/121634 . rtMXn/nni L/ocKet No. 60137.0034WOUl

Table XXX-20.

Na R‘ R3 -pr R3b Rs R4 X Y XXX-20-1 p-I-Ph H H H Et H F H OH XXX-20-2 p-I-Ph H H ch3 Et H F H OH XXX-20-3 p-I-Ph H H CH(CH3)2 Et H F H OH XXX-20-4 p-I-Ph H H CH2CH(CH3)2 Et H F H OH XXX-20-5 p-I-Ph H H CH2Ph Et H F H OH XXX-20-6 p-I-Ph H H CH2-indol-3-yl Et H F H OH XXX-20-7 p-I-Ph H H CH2CH2SCH3 Et H F H OH XXX-20-8 ΤΤΓ2- p-I-Ph 3b · ♦ H ♦ Et H F H OH *R2 and R3b joined together by (CHjfc to form five-membered ring.

Table XXX-21.

Xs r’ r1 R3. -p R4 R5" R4 X Υ XXX-21-1 ch3 Η H Η JPr H F Η ΟΗ XXX-21-2 ch3 H Η ch3 'Pr Η F Η ΟΗ XXX-21-3 ch3 H H CH(CH3)2 /Pr Η F Η ΟΗ XXX-21-4 ch3 H H CH2CH(CH3)2 'Pr Η F Η ΟΗ XXX-21-5 ch3 H H CH2Ph 'Pr Η F Η ΟΗ XXX-21-6 ch3 H H CH2-indol-3-yl 'Pr Η F Η ΟΗ XXX-21-7 ch3 H H ch2ch2sch3 'Pr Η F Η ΟΗ XXX-21-8 ch3 * H * 'Pr Η F Η ΟΗ *R2 and R3b joined together by (CHafc to form five-membered ring. 5 Table XXX-22. i '-h Jiir j '"'ί £

Χ2 R R3 R3. R3b R4 R3 R6 X Y ΧΧΧ-22-1 Et H H Η 'Pr H F H OH ΧΧΧ-22-2 Et H H ch3 'Pr H F H OH ΧΧΧ-22-3 Et H H ΟΗ(ΟΗ3)2 ipr H F H OH ΧΧΧ-22-4 Et H H CHjCHCCHa^ 'Pr H F Η OH ΧΧΧ-22-5 Et H H CH2Ph Tr H F H OH ΧΧΧ-22-6 Et Η Η CH2-indoI-3-yl 'Pr H F H OH ΧΧΧ-22-7 Et H H CH2CH2SCH3 ipr H F H OH ΧΧΧ-22-8 Et * H ♦ 'Pr H F H OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -616- WO 2008/121634 τ ,Λ1„„ ΛηΊ,π/ηΤτι uocKei No. 60137.0034WOU1 PCT/US2008/058183

Table XXX-23.

x° Rl R2 R3’ I?* R5 R6 X Y XXX-23-1 *Pr H H H ”W H F H OH XXX-23-2 'Pr H H ch3 'Pr H F H OH XXX-23-3 'Pr H H CH(CH3)2 'Pr H F H OH XXX-23-4 'Pr H H CH2CH(CH3)2 'Pr H F H OH XXX-23-5 'Pr H H CH2Ph 'Pr H F H OH XXX-23-6 'Pr H H CHj-indol-3-yl 'Pr H F H OH XXX-23-7 'Pr H H CHjCHjSCH3 'Pr H F H OH XXX-23-8 'Pr * H ♦ 'Pr H F H OH *R2 and Rejoined together by (Clbb to form five-membered ring.

Table XXX-24.

Ns R R2 RJ" R3b R4 R5 R6 X Y XXX-24-1 'Bu H H H 'Pr Η F Η OH XXX-24-2 'Bu H H ch3 'Pr H F H OH XXX-24-3 'Bu H H CH(CH3)2 'Pr H F Η OH XXX-24-4 'Bu H H CH2CH(CH3)2 'Pr H F H OH XXX-24-5 'Bu H H CH3Ph 'Pr Η F H OH XXX-24-6 'Bu H H CH2-indol-3-yl 'Pr Η F H OH XXX-24-7 *Bu H H CH2CH2SCH3 'Pr Η F H OH XXX-24-8 'Bu ♦ H * 'Pr Η F H OH *R2 and RJb joined together by to form five-membered ring. 5 Table XXX-25. I 'M H "gL" R·--

Xs R R2 r3b R3b R4 Rs R6 X Y XXX-254 Ph H H H H F H OH XXX-25-2 Ph H H CH3 'Pr H F H OH XXX-25-3 Ph H H CHCCHaX 'Pr H F H OH XXX-254 Ph H H CH2CH(CH3)2 'Pr H F H OH XXX-25-5 Ph H H CH2Ph 'Pr H F H OH XXX-25-6 Ph H H CH2-indol-3-yl 'Pr H F H OH XXX-25-7 Ph H H CH2CH2SCH3 'Pr H F H OH XXX-25-8 Ph * H * 'Pr H F H OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 2983472-1 -617- WO 2008/121634 . nna/1uznT11 uocKei No. 60137.0034WOUl PCT/US2008/058183

Table XXX-26.

Ns R1 R2 Rjfl R3b R4 R* R6 X Y XXX-26-1 p-Me-Ph H H H 'Pr H F H OH XXX-26-2 p-Me-Ph H H ch3 'Pr H F H OH XXX-26-3 p-Me-Ph H H CH(CH3)2 'Pr H F H OH XXX-26-4 p-Me-Ph H H CH2CH(CH3)a 'Pr H F H OH XXX-26-5 p-Me-Ph H H CH2Ph 'Pr H F H OH XXX-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr H F H OH XXX-26-7 p-Me-Ph H H CH2CH2SCH3 'Pr H F H OH XXX-26-8 p-Me-Ph 3b: : □ ♦ H ♦ 'Pr H F H OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXX-27.

N° R‘ R2 R3a R3b R4 Rs R6 X Y XXX-27-1 p-F-Ph H H H 'Pr H F H OH XXX-27-2 p-F-Ph H H ch3 'Pr H F H OH XXX-27-3 p-F-Ph H H CH(CH3)2 'Pr H F H OH XXX-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr H F H OH XXX-27-5 p-F-Ph H H CH2Ph 'Pr H F H OH XXX-27-6 p-F-Ph H H CH2-indot-3-yl 'Pr H F H OH XXX-27-7 p-F-Ph H H CH2CH2SCH3 'Pr H F H OH XXX-27-8 p-F-Ph 3b ·· j x * H * 'Pr H F H OH ♦R2 and RJb joined together by (CHab to form five-membered ring.

Ns R1 R2 R3a r35 R4 r R* X Y XXX-28-1 p-Cl-Ph H H H 'Pr H F H OH XXX-28-2 p-Cl-Ph H H ch3 'Pr H F H OH XXX-28-3 p-Cl-Ph H H CH(CH3)a /pr H F H OH XXX-28-4 p-Cl-Ph H H CH2CH(CH3)a Tr H F H OH XXX-28-5 p-Ci-Ph H H CH2Ph 'Pr H F H OH XXX-28-6 p-Cl-Ph H H CHa-indol-3-yl 'Pr H F H OH XXX-28-7 p-Cl-Ph H H CH2CH2SCH3 'Pr H F H OH XXX-28-8 ~ p-Cl-Ph 3b·· jx * H * 'Pr H F H OH ♦R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -618- PCT/US2008/058183 WO 2008/121634 M <Λ1nna,uznTT1 uocKet No. 60137.0034WOU1

Table XXX-29.

Xa R1 ΊΓ R3b “R3® R4 R· R5 X Y XXX-29-1 p-Br-Ph H H H ’W’ H F H OH XXX-29-2 p-Br-Ph H H ch3 'Pr H F H OH XXX-29-3 p-Br-Ph H H CH(CH3)2 ’Pr H F H OH XXX-29-4 p-Br-Ph H H CH2CH(CH3)2 Tr H F H OH XXX-29-5 p-Br-Ph H H CH2Ph 'Pr H F H OH XXX-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr H F H OH XXX-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr H F H OH XXX-29-8 ....... p-Br-Ph Jb~. · . L * H ♦ 'Pr H F H OH ♦R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXX-30.

Xe Rl R2 "r3® R4 Rs R6 X Y XXX-30-1 p-I-Ph H H H "W H F H OH XXX-30-2 p-I-Ph H H CH3 'Pr H F H OH XXX-30-3 p-I-Ph H H ΟΗ(ΟΗ3)2 'Pr H F H OH XXX-30-4 p-I-Ph H H CH2CH(CH3)a 'Pr H F H OH XXX-30-5 p-I-Ph H H CH2Ph 'Pr H F H OH XXX-30-6 p-I-Ph H H CH2-indol-3-yI 'Pr H F H OH XXX-30-7 p-I-Ph H H ch2ch2sch3 'Pr H F H OH XXX-30-8 p-I-Ph * H ♦ 'Pr H F H OH *R2 and RJt) joined together by (CH2)3 to form five-membered ring. 5 Table XXX-31. ......—Ml J ..... ........

Xa R1 R2 R3a R3b R5 R6 X Y XXX-31-1 ch3 H H H rtBu H F H OH XXX-31-2 ch3 H H ch3 "Bu H F H OH XXX-31-3 ch3 H H CH(CH3)2 "Bu H F H OH XXX-31-4 ch3 H H CH2CH(CH3)2 "Bu H F H OH XXX-31-5 ch3 H H CH2Ph "Bu H F H OH XXX-31-6 ch3 H H CH2-indol-3-yl "Bu H F H OH XXX-31-7 ch3 H H ch2ch2sch3 "Bu H F H OH XXX-31-8 "7772-77? ch3 ΪΒ-. ; . 4 H * "Bu H F H OH *R2 and Rejoined together by (CH^toTform five-membered ring. 2983472-1 -619- PCT/US2008/058183

WO 2008/121634 T

Docket No. 60137.0034WOU1

Table XXX-32.

X° R1 R2 R3a R3b R4 ΊΓ X Y - XXX-32-1 Et H H H "Bu H F H OH XXX-32-2 Et H H ch3 "Bu H F H OH XXX-32-3 Et H H CH(CH3)2 "Bu H F H OH XXX-32-4 Et H H CH2CH(CH3)2 "Bu H F H OH XXX-32-5 Et H H CH2Ph "Bu H F H OH XXX-32-6 Et H H CH2-indol-3-yl "Bu H F H OH XXX-32-7 Et H H CH2CH2SCH3 "Bu H F H OH XXX-32-8 Et * H * "Bu H F H OH *R2 and RJb joined together by (CHib to form five-membered ring.

Table XXX-33.

Jfs R R2 R" R3b R4 R5 R6 X Y XXX-33-1 H H H "Bu H F H OH XXX-33-2 'Pr H H CH3 "Bu H F H OH XXX-33-3 'Pr H H CH(CH3)2 "Bu H F H OH XXX-33-4 'Pr H H CH2CH(CH3)2 "Bu H F H OH XXX-33-5 'Pr H H CH2Ph "Bu H F H OH XXX-33-6 'Pr H H CH2-indoI-3-yl "Bu H F H OH XXX-33-7 fpr H H CH2CH2SCH3 "Bu H F H OH XXX-33-8 'Pr * H * "Bu H F H OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XXX-34. 11 1 W RL ΛΊ"1 ·ι — ι«ι» ,

Xs R1 R2 R3· R3b R4^ R; R6 X Y XXX-34-1 "’'Bu” H H H "Bu H F H OH XXX-34-2 'Bu H H ch3 "Bu H F H OH XXX-34-3 'Bu H H CHCCH^ "Bu H F H OH XXX-34-4 'Bu H H CH2CH(CH3)2 "Bu H F H OH XXX-34-5 'Bu H H CH2Ph "Bu H F H OH XXX-34-6 'Bu H H CH2-indoI-3-yl "Bu H F H OH XXX-34-7 'Bu H H CH2CH2SCH3 "Bu H F H OH XXX-34-8 *«2 j 'Bu JG~· ; * H * "Bu H F H OH *R2 and RJb joined together by ((%¼ to form five-membered ring. 2983472-1 -620- PCT/US2008/058183 WO 2008/121634 ,

Docket No. 60137.0034WOU1

TableXXX-35.

Xa R1 R1 r37- R3b "r4- R6 X Y XXX-35-1 Ph H H H "Bu H F H OH XXX-35-2 Ph H H ch3 "Bu H F H OH XXX-35-3 Ph H H CH(CH3)2 "Bu H F H OH XXX-35-4 Ph H H CH2CH(CH3)2 "Bu H F H OH XXX-35-5 Ph H H CH2Ph "Bu H F H OH XXX-35-6 Ph H H CH2-indol-3-yl "Bu H F H OH XXX-35-7 Ph H H CH2CH2SCH3 "Bu H F H OH XXX-35-8 Ph * H * "Bu H F H OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXX-36.

Xa r1 Ί?' R3· "r35 R4 R5 Rj X Y XXX-36-1 p-Me-Ph H H H "Bu H F H OH XXX-36-2 p-Me-Ph H H ch3 "Bu H F H OH XXX-36-3 p-Me-Ph H H CH(CH3)2 "Bu H F H OH XXX-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu H F H OH XXX-36-5 p-Me-Ph H H CH2Ph "Bu H F H OH XXX-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu H F H OH XXX-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu H F H OH XXX-36-8 p-Me-Ph * H * "Bu H F H OH ♦R2 and Rejoined together by (0¾¼ to form five-membered ring. 5 Table XXX-37. 1 1 I « HL.......".......1,1.1—I—— J I, ·ιι .....

Xa R1 R2 R3a R3b R4^ Rs R6 X Y XXX-37-1 p-F-Ph H H H "Bu H F H OH XXX-37-2 p-F-Ph H H CH3 "Bu H F H OH XXX-37-3 p-F-Ph H H CH(CH^ "Bu H F H OH XXX-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu H F H OH XXX-37-5 p-F-Ph H H CH2Ph "Bu H F H OH XXX-37-6 p-F-Ph H H CH2-indol-3-yl "Bu H F H OH XXX-37-7 p-F-Ph H H CH2CH2SCH3 "Bu H F H OH XXX-37-8 p-F-Ph * H * "Bu H F H OH *R2 and Rejoined together by (0¾¼ to form fivemembered ring. 2983472-1 -621- PCT/US2008/058183 WO 2008/121634 ,

Docket No. 60137.0034WOD1

TableXXX-38.

Ns R1 ΊΓ RJa R1E R R3 ΊΓ X Y XXX-38-1 p-Cl-Ph H H H "Bu H F H OH XXX-38-2 p-Cl-Ph H H ch3 "Bu H F H OH XXX-38-3 p-Cl-Ph H H CH(CH3)2 "Bu H F H OH XXX-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H F H OH XXX-38-5 p-Cl-Ph H H CH2Ph "Bu H F H OH XXX-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu H F H OH XXX-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu H F H OH XXX-38-8 p-CI-Ph ♦ H * "Bu H F H OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXX-39.

Ns R' R2 R3 R3b R4 R3 Rfc X Y XXX-39-1 p-Br-Ph H H H "Bu H F H OH XXX-39-2 p-Br-Ph H H CH3 "Bu H F H OH XXX-39-3 p-Br-Ph H H CH(CH3)2 "Bu H F H OH XXX-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu H F H OH XXX-39-5 p-Br-Ph H H CH2Ph "Bu H F H OH XXX-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu H F H OH XXX-39-7 p-Br-Ph H H CH2CH2SCH3 "Bu H F H OH XXX-39-8 p-Br-Ph ♦ H * "Bu H F H OH ♦R2 and R3b joined together by ((¾)) to form five-membered ring. 5 Table XXX-40. ........ . *"····*Ι. RC~ J * 1 111

Ns R1 R2 R3a R3” R4 R3 R6 X Y XXX-40-1 p-I-Ph H H H "Bu H F H OH XXX-40-2 p-I-Ph H H ch3 "Bu H F H OH XXX-40-3 p-I-Ph H H CH(CH3)2 "Bu H F H OH XXX-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu H F H OH XXX-40-5 p-I-Ph H H CH2Ph "Bu H F H OH XXX-40-6 p-I-Ph H H CH2-indol-3-yl "Bu H F H OH XXX-40-7 p-I-Ph H H CH2CH2SCH3 "Bu H F H OH XXX-40-8 p-I-Ph # H * "Bu H F H OH *R2 and R31’joined together by (CH2)3 to form five-membered ring. 2983472-1 -622- WO 2008/121634 , nnOj1u/rAT11 uocKet No. 60137.0034WOU1

Table XXX-41.

Ns TT" -r3B R4 r5" "r5" X Y XXX-41-1 ch3 H H H Bz H F H OH XXX-41-2 ch3 H H ch3 Bz H F H OH XXX-41-3 ch3 H H CH(CH3)2 Bz H F H OH XXX-41-4 ch3 H H CH2CH(CH3)2 Bz H F H OH XXX-41-5 ch3 H H CH2Ph Bz H F H OH XXX-41-6 ch3 H H CH2-indol-3-yl Bz H F H OH XXX-41-7 ch3 H H CH2CH2SCH3 Bz H F H OH XXX-41-8 ch3 * H * Bz H F H OH *R2 and R5b joined together by (CH2)3 to form five-membered ring.

Table XXX-42.

Ns R1 R2 r3« R3b R4 R5 R6 X Y XXX-42-1 Et H H H Bz H F H OH XXX-42-2 Et H H CH3 Bz H F H OH XXX-42-3 Et H H CH(CH3)2 Bz H F H OH XXX-42-4 Et H H CH2CH(CH3)2 Bz H F H OH XXX-42-5 Et H H CH2Ph Bz H F H OH XXX-42-6 Et H H CH2-indol-3-yl Bz H F H OH XXX-42-7 Et H H CH2CH2SCH3 Bz H F H OH XXX-42-8 Et ♦ H * Bz H F H OH *RZ and RJ0 joined together by ((¾¼ to form five-membered ring. 5 Table XXX-43. 1 H ' R- *— I j ,. 1 1 1

Ns R* R2 R3· R3b R4 R3 R& X Y XXX-43-1 'Pr H H H Bz H F H OH XXX-43-2 'Pr H H CH3 Bz H F H OH XXX-43-3 /pr H H CH(CH3>2 Bz H F H OH XXX-43-4 'Pr H H CH2CH(CH3)2 Bz H F H OH XXX-43-5 ipr H H CH2Ph Bz H F H OH XXX-43-6 'Pr H H CH2-indol-3-yl Bz H F H OH XXX-43-7 'Pr H H CH2CH2SCH3 Bz H F H <$i XXX-43-8 fpr * H * Bz H F H OH *R2 and Rejoined together by (CH2)a to form five-membered ring. 2933472-1 -623- PCT/US2008/058183 WO 2008/121634 ΛΑΟ

Docket No. 60137.0034WOU1

Table XXX-44.

Ns R1 ΊΡ’ R3’ "R16 R4 "R5" R6 X Y XXX-44-1 ?Bu H H H Bz H F H OH XXX-44-2 'Bu H H ch3 Bz H F H OH XXX-44-3 'Bu H H CH(CH3)2 Bz H F H OH XXX-44-4 'Bu H H CH2CH(CH3)2 Bz H F H OH XXX-44-5 'Bu H H CH2Ph Bz H F H OH XXX-44-6 'Bu H H CH2-indol-3-yl Bz H F H OH XXX-44-7 'Bu H H CH2CH2SCH3 Bz H F H OH XXX-44-8 'Bu * H * Bz H F H OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXX-45.

Ns R" R3 r3. R3b R4 R5 R6 X Y XXX-45-1 Ph H H H Bz H F H OH XXX-45-2 Ph H H CH3 Bz H F H OH XXX-45-3 Ph H H CH(CH3)2 Bz H F H OH XXX-45-4 Ph H H CH2CH(CH3)2 Bz H F H OH XXX-45-5 Ph H H CH2Ph Bz H F H OH XXX-45-6 Ph H H CH2-indol-3-yl Bz H F H OH XXX-45-7 Ph H H CH2CH2SCH3 Bz H F H OH XXX-45-8 Ph 3b; ·: ♦ H * Bz H F H OH ♦R2 and RJb joined together by (CHjh to form five-membered ring. 5 Table XXX-46._______

Ns R’ R3 R3a R3b R4 RJ R6 X Y XXX-46-1 p-Me-Ph H H H Bz H F H OH XXX-46-2 p-Me-Ph H H CH3 Bz H F H OH XXX-46-3 p-Me-Ph H H CH(CH3>i Bz H F H OH XXX-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz H F H OH XXX-46-5 p-Me-Ph H H CH2Ph Bz H F H OH XXX-46-6 p-Me-Ph H H CH2-indol-3-yl Bz H F H OH XXX-46-7 p-Me-Ph H H CH2CH2SCH3 Bz H F H OH XXX46-8 j nJ p-Me-Ph b; · j . . * H * Bz H F H OH *R2 and R3b joined together by (Gfob to form five-membered ring. 2983472-] -624- WO 2008/121634 , ηΛ~,„,™τ1

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXX-47.

Xa R1 R* R3a R3b R4 Rs R6 X Y XXX-47-1 p-F-Ph H H H Bz H F H OH XXX-47-2 p-F-Ph H H ch3 Bz H F H OH XXX-47-3 p-F-Ph H H CH(CH3)2 Bz H F H OH XXX-47-4 p-F-Ph H H CH2CH(CH3)2 Bz H F H OH XXX-47-5 p-F-Ph H H CH2Ph Bz H F H OH XXX-47-6 p-F-Ph H H CHi-indol-3-yl Bz H F H OH XXX-47-7 p-F-Ph H H ch2ch2sch3 Bz H F H OH XXX-47-8 p-F-Ph b ! ; J x * H * Bz H F H OH ♦R1 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXX-48.

Xa R1 r! R3 “r^ R4 R5 R* X Y XXX-48-1 p-CI-Ph H H H Bz H F H OH XXX-48-2 p-Cl-Ph H H CH3 Bz H F H OH XXX-48-3 p-CI-Ph H H CH(CH3)2 Bz H F H OH XXX-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H F H OH XXX-48-5 p-CI-Ph H H CH2Ph Bz H F H OH XXX-48-6 p-Cl-Ph H H CH2-indol-3-yt Bz H F H OH XXX-48-7 p-CI-Ph H H CH2CH2SCH3 Bz H F H OH XXX-48-8 p-Cl-Ph * H * Bz H F H OH *RZ and Rejoined together by (Cthb to form five-membered ring. 5 Table XXX-49. 1 — I .......π « II II ·ΙΙ

Xs R1 R4 RJa R3b R4 R3 Iv X Y XXX-49-1 p-Br-Ph H H H Bz Η F H OH XXX-49-2 p-Br-Ph H H ch3 Bz H F H OH XXX-49-3 p-Br-Ph H H CH(CH3)2 Bz H F H OH XXX-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz H F H OH XXX-49-5 p-Br-Ph H H CH2Ph Bz H F H OH XXX-49-6 p-Br-Ph H H CH2-indol-3-yl Bz H F H OH XXX-49-7 p-Br-Ph H H ch2ch2sch3 Bz H F H OH XXX-49-8 p-Br-Ph * H ♦ Bz H F H OH *R2 and R3” joined together by (CH2)3 to form five-membered ring. 2983472-1 -625- PCT/US2008/058183 WO 2008/121634

Docket No. 6013 7.0034WOU1

Table XXX-50.

Xa R1 TF r3‘ RJt> R4 Rs R6 X Y XXX-50-1 p-I-Ph H H H Bz H F H OH XXX-50-2 p-I-Ph H H ch3 Bz H F H OH XXX-50-3 p-I-Ph H H CH(CH3)2 Bz H F H OH XXX-50-4 p-I-Ph H H CH2CH(CH3)2 Bz H F H OH XXX-50-5 p-I-Ph H H CHaPh Bz H F H OH XXX-50-6 p-I-Ph H H CH2-indoI-3-yl Bz H F H OH XXX-50-7 p-I-Ph H H CH2CH2SCH3 Bz H F H OH XXX-50-8 p-I-Ph * H ♦ Bz H F H OH *R2 and RJb joined together by (CHa)3 to form five-membered ring.

5 XXXI

Table XXXI-1.

Xa Rl RJ R3’ R3b R4 R5 R6 X Υ XXXI-1-1 CH3 H H H ch3 Η F F ΟΗ XXXI-1-2 ch3 H H ch3 ch3 Η F F ΟΗ XXXI-1-3 ch3 H H CH(CH3)a ch3 Η F F ΟΗ XXXI-1-4 ch3 H H CH2CH(CH3)2 ch3 Η F F ΟΗ XXXI-1-5 ch3 H H CH2Ph ch3 Η F F ΟΗ XXXI-1-6 ch3 H H CHj-indol-3-yI ch3 Η F F ΟΗ XXXI-1-7 ch3 H H CH2CH2SCH3 ch3 Η F F ΟΗ XXXI-1-8 fcn2 j n ch3 3b· · * H * ch3 Η F F ΟΗ *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -626- PCT/US2008/058183 WO 2008/121634 , T,

Docket No. 60137.0034WOU1

Table XXX1-2.

X2 IF R2 R3a Ί?6 r7- R5 R4 X Y XXXI-2-1 Et H H H ch3 H F F OH XXXI-2-2 Et H H ch3 ch3 H F F OH XXXI-2-3 Et H H CH(CH3)2 ch3 H F F OH XXXI-2-4 Et H H CH2CH(CH3)2 ch3 H F F OH XXXI-2-5 Et H H CH2Ph ch3 H F F OH XXXI-2-6 Et H H CH2-indol-3-yl ch3 H F F OH XXXI-2-7 Et H H CH2CH2SCH3 ch3 H F F OH XXXI-2-8 Et * H ♦ ch3 H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXXI-3.

Na TF R2 R3‘ R3b R4 IF R4 X Y ΧΧΧΙ-3-Ϊ “Tr” H H H CH3 Η F F OH XXXI-3-2 'Pr H H ch3 ch3 H F F OH XXXI-3-3 'Pr H H CH(CH3)2 ch3 H F F OH XXXI-3-4 /Pr H H CH2CH(CH3)2 ch3 H F F OH XXXI-3-5 'Pr H H CH2Ph ch3 H F F OH XXXI-3-6 'Pr H H CH2-indol-3-yl ch3 H F F OH XXXI-3-7 'Pr H H CH2CH2SCH3 ch3 H F F OH XXXI-3-8 'Pr * H 1¼ ch3 H F F OH *R2 and R30 joined together by (CH2)3 to form five-membered ring. 5 Table XXXI-4. I Μ V "‘IIL J . " —

Xa R R2 Rj« Rjb R4 Rs R4 X Y XXXI-4-1 'Bu H H H CH3 Η F F OH XXXI-4-2 'Bu H H CH3 ch3 H F F OH XXXI-4-3 'Bu H H CHfCH^ ch3 H F F OH XXXI-4-4 teii H H CH2CH(CH3)2 ch3 H F F OH XXXI-4-5 'Bu H H CH2Ph ch3 H F F OH XXXI-4-6 'Bu H H CH2-indol-3-yl ch3 H F F OH XXXI-4-7 'Bu H H CH2CH2SCH3 ch3 H F F OH XXXI-4-8 'Bu * H * ch3 H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -627- WO 2008/121634 ^Λ1 nno ..

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXXI-5.

Xs v R2 "r3B ~ie Rs R4 X Y XXXI-5-1 Ph H H H ch3 H F F OH XXXI-5-2 Ph H H ch3 ch3 H F F OH XXXI-5-3 Ph H H CH(CH3)2 ch3 H F F OH XXXI-5-4 Ph H H CH2CH(CH3)2 ch3 H F F OH XXXI-5-5 Ph H H CH2Ph ch3 H F F OH XXXI-5-6 Ph H H CH2-indol-3-yl ch3 H F F OH XXXI-5-7 Ph H H CH2CH2SCH3 ch3 H F F OH XXXI-5-8 Ph * H * ch3 H F F OH *R2 and R3b joined together by (Cl-hh to form five-membered ring.

Table XXXI-6.

Xa R1 R3* -r3B R4 R5 R4 X Y XXXI-6-1 p-Me-Ph H H H ch3 H F F OH XXXI-6-2 p-Me-Ph H H ch3 ch3 H F F OH XXXI-6-3 p-Me-Ph H H CH(CH3)2 ch3 H F F OH XXXI-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 H F F OH XXXI-6-5 p-Me-Ph H H CH2Ph ch3 H F F OH XXXI-6-6 p-Me-Ph H H CH2-indol-3-yl CH3 H F F OH XXXI-6-7 p-Me-Ph H H ch2ch2sch3 ch3 H F F OH XXXI-6-8 p-Me-Ph * H * ch3 H F F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXXI-7.

......... I R >11 ...... , - I I

Xs R1 R2 R3* R3b R4 Ri R4 X Y XXXI-7-1 p-F-Ph H H H ch3 H F F OH XXXI-7-2 p-F-Ph H H CH3 ch3 H F F OH XXXI-7-3 p-F-Ph H H CH(CH3)2 ch3 H F F OH XXXI-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 H F F OH XXXI-7-6 p-F-Ph H H CH2Ph ch3 H F F OH XXXI-7-7 p-F-Ph H H CH2-indoI-3-yl ch3 H F F OH XXXI-7-8 p-F-Ph H H CH2CH2SCH3 ch3 H F F OH XXXI-7-20 r,3b p-F-Ph * H * ch3 H F F OH *R4 and Rejoined together by (CHhb to form five-membered ring. 2943472-1 -628-

WO 2008ΖΠ1634Νθ^ 60137>0034WOUI PCT/US2008/058183

Table XXXI-8.

Ns R1 Tr" R3a RJb "R^ RJ r5" X Y XXXI-8-1 p-Cl-Ph H H H CH3 H F F OH XXXI-8-2 p-Cl-Ph H H ch3 ch3 H F F OH XXXI-8-3 p-Cl-Ph H H CH(CH3)2 ch3 H F F OH XXXI-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 H F F OH XXXI-8-5 p-Cl-Ph H H CH2Ph ch3 H F F OH XXXI-8-6 p-Cl-Ph H H CH2-indol-3-yl ch3 H F F OH XXXI-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 H F F OH XXXI-8-8 p-Cl-Ph * H * ch3 H F F OH *R2 and R3b joined together by (CHskt0 form five-membered ring.

Table XXX1-9.

Na R' RJ RJa R3b R4 r5 R6 X Υ XXXI-9-1 p-Br-Ph H H H ch3 H F F ΟΗ XXXI-9-2 p-Br-Ph H H CH3 ch3 H F F ΟΗ XXXI-9-3 p-Br-Ph H H CHCCHsh ch3 Η F F ΟΗ XXXI-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 Η F F ΟΗ XXXI-9-6 p-Br-Ph H H CH2Ph ch3 Η F F ΟΗ XXXI-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 Η F F ΟΗ XXX1-9-8 p-Br-Ph H H CHaCH2SCH3 ch3 Η F F ΟΗ XXXI-9-20 p-Br-Ph * H ♦ ch3 Η F F ΟΗ *R2 and R36 joined together by (CEhht0 fonn five-membered ring. 5 Table XXXI-10. "........ ' 1' Μ ' "TT*1L ",· 1 - I 1. 1 Λ 11

Ns R1 R* RJ“ R3b R4 Rs R6 X Y ΧΧΧΙ-104 p-1-Ph Η Η Η ch3 H F F OH ΧΧΧΙ-10-2 p-1-Ph Η Η ΟΗ3 ch3 Η F F OH ΧΧΧΙ-10-3 p-1-Ph Η Η CH(CH3)i ch3 H F F OH XXXI40-4 p-1-Ph Η Η CH2CH(CH3)2 ch3 H F F OH ΧΧΧΙ-10-5 p-1-Ph Η Η CH2Ph ch3 H F F OH ΧΧΧΙ-10-6 p-1-Ph Η Η CH2-indol-3-yl ch3 H F F OH ΧΧΧΙ-10-7 p-1-Ph Η Η CH2CH2SCH3 ch3 H F F OH XXXI-10-8 p-1-Ph * Η * ch3 H F F OH *R2 and Rejoined together by (CH^h to form five-membered ring. 2983472-1 -629 WO 2008/121634

Docket No. 60137.0034WOU1 PCT/ US2008/058183

Table XXXI-11.

Ns Rl R2 ηρτ "R3® TT R4 Iv X Y XXXI-11-1 ch3 H H H Et H F F OH XXXI-11-2 ch3 H H ch3 Et H F F OH XXXI-11-3 ch3 H H CH(CH3)2 Et H F F OH XXXM1-4 ch3 H H CH2CH(CH3)2 Et H F F OH XXXI-11-5 ch3 H H CH2Ph Et H F F OH XXXI-11-6 ch3 H H CH2-indol-3-yl Et H F F OH XXXI-11-7 ch3 H H CH2CH2SCH3 Et H F F OH XXXI-11-8 ch3 * H * Et H F F OH *R2 and Rejoined together by (Cthb to form five-membered ring.

Table XXXI-12.

Xs R1 R2 lPa~ R3” R4 IV R4 X Y XXXI-12-1 Et H H H Et H F F OH XXXI-12-2 Et H H CH3 Et H F F OH XXXI-12-3 Et H H CH(CH3)2 Et H F F OH XXXI-12-4 Et H H CH2CH(CH3)2 Et H F F OH XXXI-12-5 Et H H CH2Ph Et H F F OH XXXI-12-6 Et H H CH2-indol-3-yl Et H F F OH XXXI-12-7 Et H H CH2CH2SCH3 Et H F F OH XXXI-12-8 *7,2 Et > * * H * Et H F F OH *R2 and R30 joined together by (CH2)3 to form five-membered ring.

Table XXXI-13.

Xs R1 R2 R3a R3b R4 R5" R4 X Y XXXI-13-1 'Pr H H H Et H F F OH XXXI-13-2 'Pr H H ch3 Et H F F OH XXXI-13-3 'Pr H H CH(CH3)2 Et H F F OH XXXI-13-4 'Pr H H CH2CH(CH3)2 Et H F F OH XXXI-13-5 ήΡΓ H H CH2Ph Et H F F OH XXXI-13-6 'Pr H H CH2-indol-3-yl Et H F F OH XXXI-13-7 'Pr H H CH2CH2SCH3 Et H F F OH XXXI-13-8 -*772-7Τ7ΪΈ 'Pr 1 · * _ * H ♦ Et H F F OH *R2 and RJb joined together by (CFhb to form five-membered ring. 2983472-1 -630- WO 2008/J21634No^ 60137O034WOU1 PCT/US2008/058183

Table XXXI-14.

N° r1- R2 -ps- “R35 R4 R5 R6 X Y XXXI-14-1 'Bu H H H Et H F F OH XXXM4-2 'Bu H H ch3 Et H F F OH XXXI-14-3 'Bu H H CH(CH3)2 Et H F F OH XXXI-14-4 'Bu H H CH2CH(CH3)2 Et H F F OH XXXI-14-5 'Bu H H CH2Ph Et H F F OH XXXI-14-6 'Bu H H CHrindol-3-yl Et H F F OH XXXI-14-7 'Bu H H CH2CH2SCH3 Et H F F OH XXXI-14-8 —. r,jb· 'Bu ♦ H ♦ .Et H F F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXXI-15.

Ns R1 R3 R3‘ R* R4 R5 R6 X Y xxxr-15-ι Ph H H H Et H F F OH XXXI-15-2 Ph H H CH3 Et H F F OH XXXI-15-3 Ph H H CH(CH3)2 Et H F F OH XXXI-15-4 Ph H H CH2CH(CH3)2 Et H F F OH XXXI-15-5 Ph H H CH2Ph Et H F F OH XXXI-15-6 Ph H H CHrindoi-3-yl Et H F F OH XXXI-15-7 Ph H H CH2CH2SCH3 Et H F F OH XXXI-15-8 ; . «3b Ph ♦ H * Et H F F OH *R2 and RJt> joined together by (<%)3 to form five-membered ring.

Table XXXI-16.

Ns r‘ R3 "r5" -p R4 Rs Rfi X Y XXXI-16-1 p-Me-Ph H H H Et H F F OH XXXI-16-2 p-Me-Ph H H ch3 Et H F F OH XXXI-16-3 p-Me-Ph H H CH(CH3)2 Et H F F OH XXXI-16-4 p-Me-Ph H H CH2CH(CH3)2 Et H F F OH XXXI-16-5 p-Me-Ph H H CH2Ph Et H F F OH XXXI-16-6 p-Me-Ph H H CH2-indol-3-yl Et H F F OH XXXI-16-7 p-Me-Ph H H CH2CH2SCH3 Et H F F OH XXXI-16-8 -Ϊ7%2 j n3b p-Me-Ph ♦ H ♦ Et H F F OH *R2 and R36 joined together by (CH^ to form five-membered ring. 2983472-1 -631 - WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXXI-17.

Na R‘ R2 R3’ fc RJ IF X Y XXX1-17-1 p-F-Ph H H H Et H F F OH XXXI-17-2 p-F-Ph H H ch3 Et H F F OH XXXI-17-3 p-F-Ph H H CH(CH3)2 Et H F F OH XXXI-17-4 p-F-Ph H H CH2CH(CH3)2 Et H F F OH XXXI-17-5 p-F-Ph H H CH2Ph Et H F F OH XXXI-17-6 p-F-Ph H H CH2-indol-3-yl Et H F F OH XXXI-17-7 p-F-Ph H H ch2ch2sch3 Et H F F OH XXXI-17-8 p-F-Ph * H * Et H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXXI-18.

Ns R1 R2 RJ‘ Rjb R4 R3 R6 X Y XXXI-18-1 p-Cl-Ph H H H Et H F F OH XXXI-18-2 p-Cl-Ph H H ch3 Et H F F OH XXXI-18-3 p-Cl-Ph H H CH(CHj), Et H F F OH XXXI-18-4 p-CI-Ph H H CH2CH(CH3)2 Et H F F OH XXXI-18-5 p-Cl-Ph H H CH2Ph Et H F F OH XXXI-18-6 p-Cl-Ph H H CHrindol-3-yl Et H F F OH XXXI-18-7 p-Cl-Ph H H CH2CH2SCH3 Et H F F OH XXXI-18-8 p-CI-Ph * H * Et H F F OH *R2 and RJb joined together by (CH2)7to form five-membered ring. 5 Table XXXI-19. 'I11'·....... jj «I J j

Na Rl R2 R3h R3b R4 R3 R6 X Y XXXI-19-1 p-Br-Ph H H H Et H F F OH XXXI-19-2 p-Br-Ph H H ch3 Et H F F OH XXXI-19-3 p-Br-Ph H H CH(CH3)2 Et H F F OH XXXI-19-4 p-Br-Ph H H CH2CH(CH3)2 Et H F F OH XXXI-19-5 p-Br-Ph H H CH2Ph Et H F F OH XXXI-19-6 p-Br-Ph H H CHa-indol-3-yl Et H F F OH XXXI-19-7 p-Br-Ph H H CH2CH2SCH3 Et H F F OH XXXI-19-8 _ . p-Br-Ph * H * Et H F F OH *R2 and RJb joined together by (CHj)3 to form five-membered ring. 2983472-1 -632- WO 2008/121634 . PCT/US2008/058183 uocKet No. 60137.0034WOU1

Table XXXI-20.

n° R1 R2 RJa "r*. R4 R’ R4 X Y XXXI-20-1 p-I-Ph H H H Et H F F OH XXX1-20-2 p-I-Ph H H ch3 Et H F F OH XXXI-20-3 p-I-Ph H H CH(CH3)2 Et H F F OH XXXI-20-4 p-I-Ph H H CH2CH(CH3)2 Et H F F OH XXXI-20-5 p-I-Ph H H CH2Ph Et H F F OH XXXI-20-6 p-I-Ph H H CH2-indol-3-yl Et H F F OH XXXI-20-7 p-I-Ph H H CH2CH2SCH3 Et H F F OH XXXI-20-8 p-I-Ph * H ♦ Et H F F OH *R2 and Rejoined together by (CFhh to form five-membered ring.

Table XXXI-21.

Ns R R2 RJ‘ R3b R4 RJ R6 X Y XXXI-21-1 ch3 H H H TpT H F F OH XXXI-21-2 ch3 H H ch3 'Pr H F F OH XXXI-21-3 ch3 H H CH(CH3)2 'Pr H F F OH XXXI-21-4 ch3 H H CH2CH(CH3)2 'Pr H F F OH XXXI-21-5 ch3 H H CH2Ph 'Pr H F F OH XXXI-21-6 ch3 H H CH2-indol-3-yl 'Pr H F F OH XXXI-21-7 ch3 H H CH2CH2SCH3 'Pr H F F OH XXXI-21-8 ch3 ♦ H * 'Pr H F F OH *R2 and RJb joined together by (CHa)3 to form five-membered ring. 5 Table XXXI-22. 1 I H 4. 412 II··.·- ~ J 1 "

Ns . R R2 R3" R3b R4 R3 R4 X Y XXXI-22-1 Et H H H Ψγ H F F OH XXXI-22-2 Et H H ch3 'Pr H F F OH XXXI-22-3 Et H H CHCCHjX 'Pr H F F OH XXXI-22-4 Et H H CH2CH(CH3)2 'Pr H F F OH XXXI-22-5 Et H H CH2Ph 'Pr H F F OH XXXI-22-6 Et H H CH2-indol-3-yl 'Pr H F F OH XXXI-22-7 Et H H CH2CH2SCH3 'Pr H F F OH XXXI-22-8 __.. Et * H ♦ 'Pr H F F OH *R2 and RJt> joined together by (CH2)3 to form five-membered ring. 2983472-1 -633 - WO 2008/121634 T ,,,,™,,

DocKet No. 60137.0034WOU1 PCT/US2008/058183

Table XXXI-23.

Ns R1 IF” R3a R3b TF” R’ IF X Y XXX1-23-1 'Pr H H H JPr H F F OH XXXI-23-2 zPr H H ch3 'Pr H F F OH XXX1-23-3 'Pr H H CH(CH3)2 'Pr H F F OH XXX1-23-4 'Pr H H CH2CH(CH3)2 'Pr H F F OH XXXI-23-5 'Pr H H CH2Ph 'Pr H F F OH XXXI-23-6 /Pr H H CH2-indol-3-yl 'Pr H F F OH XXXI-23-7 'Pr H H CH2CH2SCH3 'Pr H F F OH XXXI-23-8 'Pr * H * 'Pr H F F OH *R2 and RJb joined together by (CHzb to form five-membered ring.

Table XXXI-24.

Ns r’ IF r3° R3b R4 RJ R6 X Y XXXI-24-1 ΊϋΓ H H H "W H F F OH XXXI-24-2 'Bu H H ch3 'Pr H F F OH XXXI-24-3 'Bu H H CH(CH3)2 'Pr H F F OH XXXI-24-4 'Bu H H CH2CH(CH3)2 'Pr H F F OH XXXI-24-5 'Bu H H CH2Ph 'Pr H F F OH XXX1-24-6 'Bu H H CH2-indol-3-yl 'Pr H F F OH XXXI-24-7 'Bu H H CH2CH2SCH3 'Pr H F F OH XXXI-24-8 "Ζ7Γ2-77ΠΪ7 'Bu * H * 'Pr H F F OH *R2 and R3b joined together by (CHjb to form five-membered ring.

Table XXXI-25.

Ns R1 ΊΓ “R^ R4 R3 R6 X Y XXXI-25-1 Ph H H H /pr H F F OH XXXI-25-2 Ph H H CHj 'Pr H F F OH XXXI-25-3 Ph H H CHCCH^ 'Pr H F F. OH XXXI-25-4 Ph H H CH2CH(CH3)2 'Pr H F F OH XXXI-25-5 Ph H H CH2Ph 'Pr H F F OH XXXI-25-6 Ph H H CH2-mdol-3-yl ^r H F F OH XXXI-25-7 Ph H H CH2CH2SCH3 'Pr H F F OH XXX1-25-8 Ph * H * 'Pr H F F OH *R2 and R30 joined together by (CH2)3 to form five-membered ring. 2983472-1 -634- PCT/US2008/058183 WO 2008/121634 ___ ,wrwT1 uocKet No. 60137.0034WOU1

Table XXXI-26.

x° R1- R2 IF7' R3b R4 R5 R6 X Y XXXI-26-1 p-Me-Ph H H H JPr H F F OH XXXI-26-2 p-Me-Ph H H ch3 /pr H F F OH XXXI-26-3 p-Me-Ph H H CH(CH3)2 fpr H F F OH XXXI-26-4 p-Me-Ph H H CH2CH(CH3)2 'Pr H F F OH XXXI-26-5 p-Me-Ph H H CH2Ph 'Pr H F F OH XXXI-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr H F F OH XXXI-26-7 p-Me-Ph H H CH2CH2SCH3 'Pr H F F OH XXXI-26-8 1T-.2 - p-Me-Ph * H ♦ 'Pr H F F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXXI-27.

Xs R1 “r35" R4 R3 Rfc X Y XXXI-27-1 p-F-Ph H H H H F F OH XXXI-27-2 p-F-Ph H H ch3 'Pr H F F OH ΧΧΧΪ-27-3 p-F-Ph H H ΟΗ(ΟΗ3)2 'Pr H F F OH XXXI-27-4 p-F-Ph H H CHjCHCCHah 'Pr H F F OH XXXI-27-5 p-F-Ph H H CH2Ph 'Pr H F F OH XXXI-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr H F F OH XXXI-27-7 p-F-Ph H H CH2CH2SCH3 'Pr H F F OH XXXI-27-8 p-F-Ph * H ♦ 'Pr H F F OH *R2 and RJb joined together by (0¾¼ to form five-membered ring. 5 Table XXX1-28.__

. X9 R1 R2 R3" R3b R4 R5 R6 X Y XXXI-28-1 p-Ci-Ph H H H 'Pr H F F OH XXXI-28-2 p-Cl-Ph H H CH3 'Pr H F F OH XXXI-28-3 p-Cl-Ph H H CH(CH3)2 'Pr H F F OH XXXI-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr H F F OH XXXI-28-5 p-Cl-Ph H H CH2Ph 'Pr H F F OH XXXI-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr H F F OH XXXI-28-7 p-Cl-Ph H H CH2CH2SCH3 'Pr H F F OH XXXI-28-8 p-Cl-Ph * H * 'Pr H F F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -635- PCT/US2008/058183 WO 2008/121634., ΖΛ1 __ ηηα>ηι/ηϊ „ uocxet No. 60137.0034WOU1

Table XXXI-29.

Ns R’ Ra R3i” R4 Rs R6 X Y XXXI-29-1 p-Br-Ph H H H 'Pr H F F OH XXXI-29-2 p-Br-Ph H H ch3 fPr H F F OH XXX1-29-3 p-Br-Ph H H CH(CH3)2 'Pr H F F OH XXXI-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr H F F OH XXXI-29-5 p-Br-Ph H H CH2Ph 'Pr H F F OH XXXI-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr H F F OH XXXI-29-7 p-Br-Ph H H CH2CH2SCH3 'Pr H F F OH XXXI-29-8 . .7315 p-Br-Ph * H * 'Pr H F F OH *R2 and Rejoined together by (0¾¼ to form Five-membered ring.

Table XXXI-30.

Ns R1 -R3- R3· Rjb IC Rs R6 X Y XXXI-30-1 p-I-Ph H H H “W H F· F OH XXXI-30-2 p-I-Ph H H ch3 'Pr H F F OH XXXI-30-3 p-I-Ph H H CH(CH3)2 'Pr H F F OH XXXI-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr H F F OH XXXI-30-5 p-I-Ph H H CH2Ph 'Pr H F F OH XXXI-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr H F F OH XXXI-30-7 p-I-Ph H H CH2CH2SCH3 Tr H F F OH XXXI-30-8 u.T-,2 ".TTjb" p-I-Ph * H ♦ 'Pr H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Ns R1 R3 R" R3b R4 R* R4 X Y XXXI-3M CH3 Η Η Η "Bu H F F OH XXXI-31-2 ch3 Η Η ch3 "Bu H F F OH XXXI-31-3 ch3 Η Η CH(CH3X "Bu H F F OH XXXI-31-4 ch3 Η Η CH2CH(CH3>2 "Bu H F F OH XXXI-31-5 ch3 Η Η CH2Ph "Bu H F F OH XXXI-31-6 ch3 Η Η CH2-indol-3-yl "Bu H F F OH XXXI-31-7 ch3 Η Η CH2CH2SCH3 "Bu H F F OH XXXI-31-8 .. . ch3 * Η ♦ "Bu H F F OH *R2 and Rejoined together by (0¾¼t0 fQrm five-membered ring. 2983472-1 -636- PCT/US2008/058183 WO 2008/121634 . ,ni__ nnQ,uzru ,. uocKet No. 60137.0034WOU1

Table XXXI-32.

Xa R1 R2 r55" r35 R4 ΊΓ R6 X Y XXXJ-32-1 Et H H H "Bu H F F OH XXXI-32-2 Et H H ch3 "Bu H F F OH XXXI-32-3 Et H H CHCCHa^ "Bu H F F OH XXXI-32-4 Et H H CH2CH(CH3)2 "Bu H F F OH XXXI-32-5 Et H H CH2Ph "Bu H F F OH XXXI-32-6 Et H H CH2-indol-3-yl "Bu H F F OH. XXXI-32-7 Et H H CH2CH2SCH3 "Bu H F F OH XXXI-32-8 Et * H * "Bu H F F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXXI-33.

Xa R R2 RJ“ R3b R4 Rs R6 X Y XXXI-33-1 ‘Pr H H H "Bu H F F OH XXXI-33-2 /Pr H H ch3 "Bu H F F OH XXXI-33-3 'Pr H H CH(CH3)2 "Bu H F F OH XXXI-33-4 /pr H H CH2CH(CH3)2 "Bu H F F OH XXXI-33-5 'Pr H H CH2Ph "Bu H F F OH XXXI-33-6 ‘Pr H H CH2-indol-3-yl "Bu H F F OH XXXI-33-7 /pr H H CH2CH2SCH3 "Bu H F F OH XXXI-33-8 'Pr ♦ H * "Bu H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 5 Table XXXI-34.

I 1 M RJ ....... I I I II III II II

Xa R R2 RJ“ R3b R4 RJ R6 X Y XXXI-34-1 H H H "Bu H F F OH XXXI-34-2 *Bu H H ch3 "Bu H F F OH XXXI-34-3 'Bu H H CH(CH3)2 "Bu H F F OH XXXI-34-4 'Bu H H CH2CH(CH3)2 "Bu H F F OH XXXI-34-5 'Bu H H CH2Ph "Bu H F F OH XXXI-34-6 'Bu H H CH2-indol-3-yl "Bu H F F OH XXXI-34-7 'Bu H H ch2ch2sch3 "Bu H F F OH XXXI-34-8 _ i 'Bu * H * "Bu H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -637- PCT/US2008/058183 WO 2008/121634 ___ uocKet No. 60137.0034WOU1

Table XXXI-35.

R1 RJ R3a -jpu R4 R* R6 X Y XXXI-35-1 Ph H H H "Bu H F F OH XXXI-35-2 Ph H H ch3 "Bu H F F OH XXXI-35-3 Ph H H CH(CH3)2 "Bu H F F OH XXXI-35-4 Ph H H CH2CH(CH3)2 "Bu H F F OH XXXI-35-5 Ph H H CH2Ph "Bu H F F OH XXXI-35-6 Ph H H CH2-indol-3-yl "Bu H F F OH XXXI-35-7 Ph H H CH2CH2SCH3 "Bu H F F OH XXXI-35-8 —.. j Ph * H * "Bu H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXXI-36.

Ns R‘ R2 ηρτ T*- R4 R* X Y XXXI-36-1 p-Me-Ph H H H "Bu H F F OH ΧΧΧΪ-36-2 p-Me-Ph H H ch3 "Bu H F F OH XXXI-36-3 p-Me-Ph H H CHCCHa), "Bu H F F OH XXXI-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu H F F OH XXXI-36-5 p-Me-Ph H H CH2Ph "Bu H F F OH XXXI-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu H F F OH XXXI-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu H F F OH XXXI-36-8 p-Me-Ph * H ♦ "Bu H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XXX1-37. —........... I W V— HL ............ 1 -g

Ns R* R2 R3a R35 R4 ΊΓ R5 X Y XXXI-37-1 p-F-Ph H H H "Bu H F F OH XXXI-37-2 p-F-Ph H H ch3 "Bu H F F OH XXXI-37-3 p-F-Ph H H CH(CH3)2 "Bu H F F OH XXXI-37-4 p-F-Ph H H CHjCHCCHa), "Bu H F F OH XXXI-37-5 p-F-Ph H H CH2Ph "Bu H F F OH XXXI-37-6 p-F-Ph H H CH2-indol-3-yl "Bu H F F OH XXXI-37-7 p-F-Ph H H CH2CH2SCH3 "Bu H F F OH XXXI-37-8 j p-F-Ph ♦ H * "Bu H F F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -638- PCT/US2008/058183 WO 2008/121634 ΛΛ„ ,,

Uocket No. 60137.0034WOUI

Table XXXI-38.

N° R1 R3a "R35 “S’” R1 R6 X Y XXXI-38-1 p-Cl-Ph H H H "Bu H F F OH XXXI-38-2 p-Cl-Ph H H ch3 "Bu H F F OH XXXI-38-3 p-Cl-Ph H H CH(CH3)2 "Bu H F F OH XXXI-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H F F OH XXXI-38-S p-Cl-Ph H H CH2Ph "Bu H F F OH XXX1-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu H F F OH XXXI-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu H F F OH XXXI-38-8 p-Cl-Ph * H * "Bu H F F OH *R2 and RJb joined together by (GHhb to form five-membered ring

Table XXXI-39.

Ns R1 R2 R3a Rib R4 R5 R6 X Y XXXI-39-1 p-Br-Ph H H H "Bu H F F OH XXXI-39-2 p-Br-Ph H H CH3 ”Bu H F F OH XXXI-39-3 p-Br-Ph H H CH(CH3)2 "Bu H F F OH XXX1-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu H F F OH XXXI-39-5 p-Br-Ph H H CH2Ph "Bu H F F OH XXXI-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu H F F OH XXXI-39-7 p-Br-Ph H H CH2CH2SCH3 ”Bu H F F OH XXXI-39-8 p-Br-Ph * H * "Bu H F F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXXI-40.

.......... I· III· I 1 1 HL"'·1·' ' ' ·—»»» II

Ns R1 R2 R3a Rib R4 R5 R6 X Y XXXI-40-1 p-I-Ph H H H "Bu H F F OH XXXI-40-2 p-I-Ph H H CH3 "Bu H F F OH XXXI-40-3 p-I-Ph H H ΟΗ(ΟΗ3)2 "Bu H F F OH XXXI-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu H F F OH XXXI-40-5 p-I-Ph H H CH2Ph "Bu H F F OH XXXI-40-6 p-I-Ph H H CH2-indol-3-yl "Bu H F F OH XXXI-40-7 p-I-Ph H H CH2CH2SCH3 "Bu H F F OH XXXI-40-8 . jnJb p-I-Ph * H * "Bu H F F OH ♦R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -639- WO 2008/j1o2c1gt4NOi 60137.0034WOU1 PCT/US2008/058183

Table XXXI-41.

Xe R1 R2 “r^ R3b T" Rs R6 X Y XXXI-41-1 ch3 H H H Bz H F F OH XXXI-41-2 ch3 H H ch3 Bz H F F OH XXXI-41-3 ch3 H H CH(CH3)2 Bz H F F OH XXXI-41-4 ch3 H H CHjCHCCH^ Bz H F F OH XXXI-41-5 ch3 H H CH2Ph Bz H F F OH XXXI-41-6 ch3 H H CH2-indol-3-yl Bz H F F OH XXXI-41-7 ch3 H H CH2CH2SCH3 Bz H F F OH XXXI-41-8 ch3 * H ♦ Bz H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXXI-42.

Xs R R2 R3" R3b R^ R5 R6 X Y XXXI-42-1 Et H H H Bz H F F OH XXXI-42-2 Et H H ch3 Bz H F F OH XXXI-42-3 Et H H CH(CH3)2 Bz H F F OH XXXI-42-4 Et H H CH2CH(CH3)2 Bz H F F OH XXXI-42-5 Et H H CH2Ph Bz H F F OH XXXI-42-6 Et H H CH2-indol-3-yl Bz H F F OH XXXI-42-7 Et H H CH2CH2SCH3 Bz H F F OH XXXI-42-8 Et * H * Bz H F F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXXI-43. 1 ' I M J .1

Xs R R2 R3. R3b R4 Rs R6 X Y XXXI-43-1 'Pr H H H Bz H F F OH XXXI-43-2 /Pr H H ch3 Bz H F F OH XXXI-43-3 'Pr H H CH(CH3)2 Bz H F F OH XXXI-43-4 'Pr H H CH2CH(CH3)2 Bz H F F OH XXXI-43-5 'Pr H H CH2Ph Bz H F F OH XXXI-43-6 /Pr H H CH2-indol-3-yl Bz H F F OH XXXI-43-7 /pr H H CH2CH2SCH3 Bz H F F XXXI-43-8 'Pr * H * Bz H F F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -640- WO 2008/121634 ,

Docket No. 60137.0034WOUt PCT/US2008/058183

Table XXXI-44.

N° R1 R2 R3a "r35 R4 R5 R6 X Y XXX1-44-1 'Bu H H H Bz H F F OH XXXI-44-2 'Bu H H ch3 Bz H F F OH XXXI-44-3 'Bu H H CH(CH3)2 Bz H F F OH XXXI-44-4 'Bu H H CH2CH(CH3)2 Bz H F F OH XXXI-44-5 'Bu H H CH2Ph Bz H F F OH XXXI-44-6 'Bu H H CH2-indol-3-yl Bz H F F OH XXXI-44-7 'Bu H H ch2ch2sch3 Bz H F F OH XXXI-44-8 'Bu * H * Bz H F F OH *R2 and R3b joined together by to form five-membered ring.

Table XXXI-45.

Ns R1 R2 R38 -p; Rs R6 X Y XXXI-45-1 Ph H H H Bz H F F OH XXXI-45-2 Ph H H ch3 Bz H F F OH XXXI-45-3 Ph H H CH(CH3)2 Bz H F F OH XXXI-45-4 Ph H H CH2CH(CH3)2 Bz H F F OH XXXI-45-5 Ph H H CH2Ph Bz H F F OH XXXI-45-6 Ph H H CH2-indol-3-yl Bz H F F OH XXXI-45-7 Ph H H CH2CH2SCH3 Bz H F F OH XXX1-45-8 JnOb Ph * H * Bz H F F OH *R2 and Rejoined together by (CH^" to form five-membered ring. 5 Table XXXI-46.

Na R‘ R2 R38 "r35 R4 Rj R6 X Y XXXI-46-1 p-Me-Ph H H H Bz H F F OH XXXI-46-2 p-Me-Ph H H ch3 Bz H F F OH XXXI-46-3 p-Me-Ph H H CH(CH3)2 Bz H F F OH XXXI-46-4 p-Me-Ph H H CHjCHiCH^ Bz H F F OH XXXI-46-5 p-Me-Ph H H CH2Ph Bz H F F OH XXXI-46-6 p-Me-Ph H H CH2-indol-3-yl Bz H F F OH XXXI-46-7 p-Me-Ph H H CH2CH2SCH3 Bz H F F OH XXXI-46-8 *n2 I TiJb p-Me-Ph * H ♦ Bz H F F OH *R2 and R4b joined together by (CH2)3 to form five-membered ring. 2983472-1 -641- WO 2008/121634

Docket No. 60137,0034WOU1 PCT/US2008/058183

Table XXXI-47.

Na R‘ R2 R3a R3b r^ Rs R6 X Y ΧΧΧΪ-47-1 p-F-Ph H H H Bz H F F OH XXXI-47-2 p-F-Ph H H ch3 Bz H F F OH XXXI-47-3 p-F-Ph H H CH(CH3)2 Bz H F F OH XXXI-47-4 p-F-Ph H H CH2CH(CH3)2 Bz H F F OH XXXI-47-5 p-F-Ph H H CH2Ph Bz H F F OH XXXI-47-6 p-F-Ph H H CH2-indol-3-yl Bz H F F OH XXXI-47-7 p-F-Ph H H CH2CH2SCH3 Bz H F F OH XXXI-47-8 p-F-Ph * H * Bz H F F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXXI-48.

Ns R1 R2 R3a R3b R4 R5 R6 X Y XXXI-48-1 p-Cl-Ph H H H Bz H F F OH XXXI-48-2 p-CI-Ph H H CH3 Bz H F F OH XXXI-48-3 p-Cl-Ph H H CH(CH3)2 Bz H F F OH XXXI-48-4 p-CI-Ph H H CH2CH(CH3)2 Bz H F F OH XXXI-48-5 p-Cl-Ph H H CH2Ph Bz H F F OH XXXI-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz H F F OH XXXI-48-7 p-Cl-Ph H H CH2CH2SCH3 Bz H F F OH XXXI-48-8 p-Cl-Ph * H * Bz H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XXXI-49. — | - J,.,— ,.··,· -

Ns R1 R2 R3a R35 IC R! R6 X Y XXXI-49-1 p-Br-Ph H H H Bz H F F OH XXXI-49-2 p-Br-Ph H H CH3 Bz H F F OH XXXI-49-3 p-Br-Ph H H ΟΗ(ΟΗ3)2 Bz H F F OH XXXI-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz H F F OH XXXI-49-5 p-Br-Ph H H CH2Ph Bz H F F OH XXXI-49-6 p-Br-Ph H H CH2-indol-3-yl Bz H F F OH XXXI-49-7 p-Br-Ph H H CH2CH2SCH3 Bz H F F OH XXXI-49-8 “ΪΪ72-77Ϊ3Ε p-Br-Ph + H * Bz H F F OH ♦fr and R3b joined together by (CH2)3 to form five-membered ring. 2983472-1 -642- PCT/US2008/058183 WO 2008/121634 τ /Λ1„ΛΛ(Μ„,ΛΤΤ,

Docket No. 60137.0034WOU1

Table XXXI-50.

N2 R‘ R2 r3‘ r55 R4 Rs R6 X Y XXXI-50-1 p-I-Ph H H H Bz H F F OH XXXI-50-2 p-I-Ph H H ch3 Bz H F F OH XXXI-50-3 p-I-Ph H H CH(CH3)2 Bz H F F OH XXXI-50-4 p-I-Ph H H CH2CH(CH3)2 Bz H F F OH XXXI-50-5 p-I-Ph H H CH2Ph Bz H F F OH XXXI-50-6 p-I-Ph H H CHrindol-3-yl Bz H F F OH XXXI-50-7 p-I-Ph H H CH2CH2SCH3 Bz H F F OH XXXI-50-8 p-I-Ph * H * Bz H F F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

XXXII 5 Table XXXII-1. - J' |

Ns R1 r’2 R1* "R* R4 Rs R6 X Y ΧΧΧΠ-1-1 ch3 H H H ch3 Η H F OH XXXII-1-2 ch3 Η H ch3 ch3 H H F OH ΧΧΧΠ-1-3 ch3 H Η CH(CH3)2 ch3 Η H F OH XXXII-1-4 ch3 H H CH2CH(CH3)2 ch3 H H F OH XXXII-1-5 ch3 H H CH2Ph ch3 H H F OH XXXII-1-6 ch3 H H CH2-indol-3-yl ch3 H H F OH XXXII-1-7 ch3 H H CH2CH2SCH3 ch3 H H F OH XXXII-1-8 ch3 <*> H * ch3 H H F OH ♦R2 and R36 joined together by (CHj^ to form five-membered ring.

Table XXXII-2.

Ns R R2 RJa R3b R4 R5 R6 X Y XXXII-2-1 Et H H H ch3 H H F OH 2983472-1 -643- WO 60137.0034WOUl PCT/US2008/058183

Ns ΊΓ Rs r3s ""S’” Ίν R4 X Y XXXII-2-2 Et H H ch3 ch3 H H F OH ΧΧΧΠ-2-3 Et H H CH(CH3)2 ch3 H H F OH XXXII-2-4 Et H H CH2CH(CH3)2 ch3 H H F OH XXXII-2-5 Et H H CH2Ph ch3 H H F OH XXXII-2-6 Et H H CH2-indol-3-yl ch3 H H F OH XXXII-2-7 Et H H CH2CH2SCH3 ch3 H H F OH XXXII-2-8 Et + H * ch3 H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXXII-3.

Na r1" Rs R3’ "R35 R4 R5 R4 X Y XXXII-3-1 'Pr H H H ch3 H H F OH XXXII-3-2 'Pr H H CH3 ch3 H H F OH XXXII-3-3 'Pr H H CH(CHj)2 ch3 H H F OH XXXII-3-4 'Pr H H CH2CH(CH3)2 ch3 H H F OH XXXII-3-5 ipr H H CH2Ph ch3 H H F OH XXXII-3-6 'Pr H H CH2-indol-3-yl ch3 H H F OH XXX1I-3-7 'Pr H H CH2CH2SCH3 ch3 H H F OH ΧΧΧΠ-3-8 Jpr * H * ch3 H H F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXXII-4.

Ns R1 R2 R3. R3b R4 R5 R4 X Y ΧΧΧΠ-4-1 'Bu H H H ch3 H H F OH XXXII-4-2 'Bu H H ch3 ch3 H H F OH XXXII-4-3 >Bu H H CH(CH3)2 ch3 Η H F OH XXXIM-4 fBu H H CH2CH(CH3)2 ch3 H H F OH XXXII-4-5 *Bu H H CH2Ph ch3 H H F OH XXXII-4-6 feu H H CH2-indoI-3-yl ch3 H H F OH XXXII-4-7 'Bu H H CH2CH2SCH3 ch3 H H F OH XXXII-4-8 *Bu * H ♦ ch3 H H F OH 5 *R2 and RJD joined together by (CH2)3 to form five-membered ring.

Table XXXII-5.

Ns R1 R2 Rj. R3b R4 R5 R4 X Y XXXII-5-1 Ph H H H ch3 Η H F OH ΧΧΧΠ-5-2 Ph H H CH3 ch3 H H F OH 2983472-1 -644- PCT/US2008/058183 WO 2008/121634 τ T1

Docket No. 60137.0034WOU1

Xs p" R3 “r53" 'kV: RJ R6 X Y XXXII-5-3 Ph H H CH(CH3)2 ch3 H H F OH XXXH-5-4 Ph H H CH2CH(CH3)2 ch3 H H F OH XXXII-5-5 Ph H H CH2Ph ch3 H H F OH ΧΧΧΠ-5-6 Ph H H CH2-indol-3-yl ch3 H H F OH ΧΧΧΠ-5-7 Ph H H CH2CH2SCH3 ch3 H H F OH XXXH-5-8 Ph * H * ch3 H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXXII-6.

X° R1 R3 -pr- - ΊΓ“ r5" R6 X Y ΧΧΧΠ-6-1 p-Me-Ph H H H ch3 H H F OH ΧΧΧΠ-6-2 p-Me-Ph H H ch3 ch3 H H F OH XXXII-6-3 p-Me-Ph H H CH(CH3)2 ch3 H H F OH XXXII-6-4 p-Me-Ph H H CH2CH(CH3)2 ch3 H H F OH ΧΧΧΠ-6-5 p-Me-Ph H H CH2Ph ch3 H H F OH ΧΧΧΠ-6-6 p-Me-Ph H H CH2-indol-3-yl ch3 H H F OH XXXII-6-7 p-Me-Ph H H CH2CH2SCH3 ch3 H H F OH XXXH-6-8 p-Me-Ph * H * ch3 H H F OH *R2 and R3b joined together by (0-12)3 to form five-membered ring.

Table XXXII-7.

Xs R1 R3 R3" Rjb R4 Rs R6 X Y XXXII-7-1 p-F-Ph H H H CH3 H H F OH XXXII-7-2 p-F-Ph H H CH3 ch3 H H F OH XXXII-7-3 p-F-Ph H H CH(CH3)2 ch3 H H F OH XXXII-7-4 p-F-Ph H H CH2CH(CH3)2 ch3 H H F OH XXXII-7-6 p-F-Ph H H CH2Ph ch3 H H F OH ΧΧΧΠ-7-7 p-F-Ph H H CH2-indol-3-yl ch3 H H F OH ΧΧΧΠ-7-8 p-F-Ph H H CH2CH2SCH3 ch3 H H F OH XXXII-7-20 p-F-Ph ♦ H • ch3 H H F OH 5 *R2 and R3” joined together by (CH2)3 to form five-membered ring.

Table ΧΧΧΠ-8.

Xa R* R3 R3* R3b R* Rs fc X Y XXXH-8-1 p-Cl-Ph H H H ch3 H H F OH XXXII-8-2 p-Cl-Ph H H CH3 ch3 H H F OH XXXII-8-3 p-Cl-Ph H H ORCH^ ch3 H H F OH 2983472-1 -645- PCT/US2008/058183 WO 2008/121634 ζΛ1ΜΛΜ,„,Λιη

Docket No. 60137.0034WOU1

Ns R’ R1 -jpr R4 RJ R X Y XXX1I-8-4 p-Cl-Ph H H CH2CH(CH3)2 ch3 H H F OH XXXI1-8-5 p-Cl-Ph H H CH2Ph ch3 H H F OH XXXII-8-6 p-Ci-Ph H H CH2-indol-3-yl ch3 H H F OH XXXII-8-7 p-Cl-Ph H H CH2CH2SCH3 ch3 H H F OH XXXII-8-8 p-Cl-Ph * H ♦ ch3 H H F OH *R2 and Rejoined together by (CH^b to form five-membered ring.

Table ΧΧΧΠ-9.

Xs R1 "ir Iv* ΊΪ® R^ RJ R4 X Y XXXII-9-1 p-Br-Ph H H H CH3 H H F OH XXXII-9-2 p-Br-Ph H H ch3 ch3 H H F OH XXXII-9-3 p-Br-Ph H H CH(CH3)2 ch3 H H F OH XXXII-9-4 p-Br-Ph H H CH2CH(CH3)2 ch3 H H F OH ΧΧΧΠ-9-6 p-Br-Ph H H CH2Ph ch3 H H F OH XXXII-9-7 p-Br-Ph H H CH2-indol-3-yl ch3 H H F OH XXXII-9-8 p-Br-Ph H H CH2CH2SCH3 ch3 H H F OH XXXII-9-20 p-Br-Ph * H * ch3 H H F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table ΧΧΧΠ-10.

Xa R1 r3- "r35” ' e?I: R4 R R4 X Y XXXII-10-1 p-I-Ph H H H ch3 H H F OH XXXII-10-2 p-I-Ph H H CH3 ch3 H H F OH XXXII-10-3 p-I-Ph H H CH(CH3)2 ch3 H H F OH XXXII-10-4 p-I-Ph H H CH2CH(CH3)2 ch3 H H F OH ΧΧΧΠ-10-5 p-I-Ph H H CH2Ph ch3 H H F OH XXXII-10-6 p-I-Ph H H CH2-indol-3-yl ch3 H H F OH XXXI I-10-7 p-I-Ph H H CH2CH2SCH3 ch3 H H F OH XXXII-10-8 p-I-Ph * H * ch3 H H F OH 5 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXXII-11.

Xa R R2 r3. R3b R4 R5 R4 X Y ΧΧΧΠ-11-1 CH3 H H H Et H H F OH ΧΧΧΠ-11-2 ch3 H H CH3 Et H H F OH ΧΧΧΠ-11-3 ch3 H H CHCCH^ Et H H F OH ΧΧΧΙΙ-Π-4 ch3 H H CH2CH(CH3)2 Et H H F OH 2983472-1 -646- PCT/US2008/058183 WO 2008/121634 . - _, 0 _ nno . .,

Docket No. 60137.0034WOU1

R1 r2 -pi- "r36 R4 R3 R6 X Y XXXH-11-5 ch3 H H CH2Ph Et H H F OH XXXII-11-6 ch3 H H CH2-indol-3-yl Et H H F Oil XXXII-I1-7 ch3 H H CH2CH2SCH3 Et H H F OH XXXIl-11-8 ch3 * H * Et H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXXII-12.

Xa ΊΓ R2 R3" R3b R R3 R5 X Y XXXII-12-1 Et H H H Et H H F OH XXXII-12-2 Et H H ch3 Et H H F OH XXX1I-12-3 Et H H CH(CH3)2 Et H H F OH XXXII-12-4 Et H H CH2CH(CH3)2 Et H H F OH XXXII-12-5 Et H H CH2Ph Et H H F OH ΧΧΧΠ-12-6 Et H H CH2-indol-3-yl Et H H F OH XXXII-12-7 Et H H CH2CH2SCH3 Et H H F OH XXXIl-12-8 Et * H ♦ Et H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXXII-13.

Xa R1 "rH "r35- R3b R4 R3 R6 X Y XXXII-13-1 'Pr H H H Et H H F OH ΧΧΧΠ-13-2 'Pr H H CH3 Et H H F OH XXXH-13-3 'Pr H H CHCCHah Et H H F OH XXXH-13-4 /pr H H CH2CH(CH3)2 Et H H F OH XXXII-13-5 fpr H H CH2Ph Et H H F OH XXXI1-13-6 'Pr H H CH2-indol-3-yI Et H H F OH XXXII-13-7 'Pr H H CH2CH2SCH3 Et H H F OH XXXII-13-8 Ψγ * H * Et H H F OH 5 *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXXII-14.

Xa R1 R2 RJa R3b Iv R3 R6 X Y ΧΧΧΠ-14-1 'Bu H H H Et H H F OH ΧΧΧΠ-14-2 H H ch3 Et H H F OH ΧΧΧΠ-14-3 'Bu H H CH(CH3)i Et H H ' F OH XXXII-14-4 'Bu H H CH2CH(CH3)2 Et H H F OH XXXH-14-5 'Bu H H CH2Ph Et H H F OH 2983472*1 -647- WO 2008/121634 τ ΛΛΠ,„,ΛΤΜ

Docket No. 60137.0034WOU1 PCT/US2008/058183

X® R' R3 Rju R5 R4 X Y ΧΧΧΠ-14-6 'Bu H H CH2-indol-3-yl Et H H F OH XXXII-14-7 'Bu H H CH2CH2SCH3 Et H H F OH XXXH-14-8 'Bu ♦ H * Et H H F OH *R2 and RJb joined together by (0¾ to form five-membered ring.

Table XXXII-15.

Xa rr R2 RJa R3b κ Rs Rs X Y XXXII-15-1 Ph H H H Et H H F OH XXXII-15-2 Ph H H ch3 Et H H F OH XXXII-15-3 Ph H H CHCCHj), Et H H F OH XXXII-15-4 Ph H H CH2CH(CH3)2 Et H H F OH XXXII-15-5 Ph H H CH2Ph Et H H F OH XXXII-15-6 Ph H H CH2-indol-3-yl Et H H F OH XXXII-15-7 Ph H H CH2CH2SCH3 Et H H F OH XXXH-15-8 Ph * H ♦ Et H H F OH *R2 and RJ0 joined together by (CH2)3 to form five-membered ring.

Table XXXII-16.

Xa R1 R2 Rj. Rjb R4 R5 R6 X Y XXXII-16-1 p-Me-Ph H H H Et H H F OH XXXH-16-2 p-Me-Ph H H ch3 Et H H F OH XXXII-16-3 p-Me-Ph H H ch(ch3)2 Et H H F OH ΧΧΧΠ-16-4 p-Me-Ph H H CH2CH(CH3)2 Et H H F OH XXXH-16-5 p-Me-Ph H H CH2Ph Et H H F OH ΧΧΧΠ-16-6 p-Me-Ph H H CH2-indol-3-yl Et H H F OH XXXH-16-7 p-Me-Ph H H CH2CH2SCH3 Et H H F OH XXXII-16-8 p-Me-Ph * H * Et H H F OH 5 *R2 and R3” joined together by (CH2)3 to form five-membered ring.

Table XXXII-17. X® R1 R2 R3“ R3b R4 R5 R4 X Y XXXH-17-1 p-F-Ph H H H Et H H F OH XXXII-17-2 p-F-Ph H H CH3 Et H H F OH ΧΧΧΠ-17-3 p-F-Ph H H CHCCHa), Et H H F OH XXXH-17-4 p-F-Ph H H CH2CH(CH3)2 Et H H F OH ΧΧΧΠ-17-5 p-F-Ph H H CH2Ph Et H H F OH XXXII-17-6 p-F-Ph H H CH2-indol-3-yl Et H H F OH 2983472-1 -648- PCT/US2008/058183 WO 2008/121634 ΖΛ1nnOylu™n

Docket No. 60137.0034WOU1

Ns R1 R2 R3· R3* R4 Rs R6 X Y ΧΧΧΠ-17-7 p-F-Ph H H ch2ch2sch3 Et H H F OH XXXII-17-8 p-F-Ph * H 4 Et H H F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. Table XXXII-18. Ns R' R2 Rj. R3b R4 R R6 X Y XXXII-18-1 p-Cl-Ph H H H Et H H F OH XXXII-18-2 p-Cl-Ph H H ch3 Et H H F OH ΧΧΧΠ-18-3 p-Cl-Ph H H CH(CH3)2 Et H H F OH XXXII-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H H F OH ΧΧΧΠ-18-5 p-Cl-Ph H H CH2Ph Et H H F OH XXXII-18-6 p-Cl-Ph H H CH2-indol-3-yl Et H H F OH XXXII-18-7 p-Cl-Ph H H CH2CH2SCH3 Et H H F OH XXXII-18-8 p-CI-Ph 4 H 4 Et H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXXII-19.

Ns R3" R3b R4 R5 r X Y XXXH-19-1 p-Br-Ph H H H Et H H F OH ΧΧΧΠ-19-2 p-Br-Ph H H CH3 Et H H F OH XXXII-19-3 p-Br-Ph H H CH(CHj)2 Et H H F OH XXXII-19-4 p-Br-Ph H H ΟΗ2ΟΗ(ΟΗ3)2 Et H H F OH XXXII-19-5 p-Br-Ph H H CH2Ph Et H H F OH XXXII-19-6 p-Br-Ph H H CH2-indol-3-yl Et H H F OH XXXII-19-7 p-Br-Ph H H ch2ch2sch3 Et H H F OH XXXII-19-8 p-Br-Ph 4 H 4 Et H H F OH 5 *RZ and R·”’joined together by (CH2)3 to form five-membered ring.

Table ΧΧΧΠ-20.

Ns R1 Rz R3a R3b r4 R5 R6 X Y XXXII-20-1 p-I-Ph H H H Et H H F OH XXXII-20-2 p-I-Ph H H ch3 Et H H F OH XXXII-20-3 p-I-Ph H H CH(CH3)2 Et H H F OH XXXII-20-4 p-I-Ph H H CH2CH(CH3)2 Et H H F OH XXXH-20-5 p-I-Ph H H CH2Ph Et H H F OH XXXII-20-6 p-I-Ph H H CH2-indol-3-yl Et H H F OH XXXII-20-7 p-I-Ph H H ch2ch2sch3 Et H H F OH 2983472-1 -649- PCT/US2008/058183 WO 2008/121634 τ ΛΜ ,„ΪΛ1Τ1

Docket No. 6013 7.0034WOU1

R1 R2 R3a R31’ R4 RJ R6 X Y

XXXII-20-8 p-I-Ph * H ♦ Et Η H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table ΧΧΧΠ-21.

X° r' R2 R3a Ίΐ4" R3 R6 X Y XXXII-21-1 CH3 H H H 'Pr H H F OH ΧΧΧΠ-21-2 ch3 H H ch3 'Pr H H F OH XXXII-21-3 ch3 H H CH(CH3>2 'Pr H H F OH XXXII-21-4 ch3 H H CH2CH(CH3)2 'Pr H H F OH XXXII-21-5 CH3 H H CH2Ph 'Pr H H F OH XXXH-21-6 ch3 H H CH2-indol-3-yl 'Pr H H F OH ΧΧΧΠ-21-7 ch3 H H CH2CH2SCH3 'Pr H H F OH XXXII-21-8 ch3 * H * 'Pr H H F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXXII-22.

Xa R1 R5 "r35” R3b R5" R6 X Y XXXII-22-1 Et H H H H H F OH XXXII-22-2 Et H H ch3 'Pr H H F OH XXXII-22-3 Et H H CH(CH3)2 ‘Pr H H F OH ΧΧΧΠ-22-4 Et H H CH2CH(CH3)2 'Pr H H F OH XXXII-22-5 Et H H CH2Ph 'Pr H H F OH XXXII-22-6 Et H H CH2-indol-3-yl 'Pr H H F OH ΧΧΧΠ-22-7 Et H H CH2CH2SCH3 'Pr H H F OH ΧΧΧΠ-22-8 Et « H ♦ 'Pr H H F OH *R2 and R^6 joined together by (ΟΗ2)3 to form five-membered ring.

Table XXXII-23.

Xa “R1" Rz R3a R4 r5" ΊΓ X Y ΧΧΧΠ-23-1 H H H *Pr H H F OH ΧΧΧΠ-23-2 Ψγ H H CH3 'Pr H H F OH XXXH-23-3 'Pr H H CH(CH3)2 Tr H H F OH XXXII-23-4 'Pr H H CH2CH(CH3)2 'Pr H H F OH ΧΧΧΙΪ-23-5 'Pr H H CH2Ph 'Pr H H F OH ΧΧΧΠ-23-6 'Pr H H CH2-indol-3-yl 'Pr H H . F OH XXX1I-23-7 'Pr H H CH2CH2SCH3 Tr H H F OH ΧΧΧΠ-23-8 'Pr * H ♦ 'Pr H H F OH 2983472-1 -650- PCT/US2008/058183 WO 2008/121634 , „„,Λ,„

Docket No. 60137.0034WOU1 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXXII-24.

Ns R1 R2 “R^" RJb R4 R5 R6 X Y XXXII-24-1 'Bu H H H 'Pr H H F OH XXXII-24-2 'Bu H H ch3 'Pr H H F OH XXXII-24-3 'Bu H H CH(CH3)2 'Pr H H F OH XXXII-24-4 'Bu H H CH2CH(CH3)2 'Pr H H F OH XXXII-24-5 'Bu H H CHaPh 'Pr H H F OH XXXII-24-6 'Bu H H CHa-indol-3-yl 'Pr H H F OH XXXII-24-7 'Bu H H CH2CH2SCH3 'Pr H H F OH XXXII-24-8 'Bu * H * 'Pr H H F OH ♦R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXX1I-25.

X° R1 R2 R3‘ R3b R4 R* Rfc X Y XXXII-25-1 Ph H H H ~¥r~ H H F OH XXXII-25-2 Ph H H ch3 'Pr H H F OH XXXH-25-3 Ph H H CH(CH3)a 'Pr H H F OH XXXII-25-4 Ph H H CH2CH(CH3)2 'Pr H H F OH XXXH-25-5 Ph H H CH2Ph 'Pr H H F OH XXXII-25-6 Ph H H CH2-indol-3-yl 'Pr H H F OH ΧΧΧΠ-25-7 Ph H H ch2ch2sch3 'Pr H H F OH XXXII-25-8 j r»3t> : Ph ♦ H * 'Pr H H F OH *R2 and joined together by (CH2)3 to form five-membered ring.

Table XXXII-26.

Xs R1 R2 R3“ R5® ir R! R6 X Y ΧΧΧΠ-26-1 p-Me-Ph H H H /ρΓ H H F OH XXXII-26-2 p-Me-Ph H H ch3 'Pr H H F OH ΧΧΧΠ-26-3 p-Me-Ph H H CHiCHj), 'Pr H H F OH ΧΧΧΠ-26-4 p-Me-Ph H H CH2CH(CH3)2 'Pr H H F OH XXXH-26-5 p-Me-Ph H H CH2Ph 'Pr H H F OH XXXH-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr H H F OH XXXII-26-7 p-Me-Ph H H CH2CH2SCH3 'Pr H H F OH XXXII-26-8 p-Me-Ph * H ♦ 'Pr H H F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -651 - WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table ΧΧΧΠ-27.

R1 Rj. r* R4 RJ R6 X Y XXXII-27-1 p-F-Ph H H H H H F OH XXXII-27-2 p-F-Ph H H ch3 'Pr H H F OH XXXII-27-3 p-F-Ph H H CH(CH3)2 'Pr H H F OH XXXH-27-4 p-F-Ph H H CH2CH(CH3)2 'Pr H H F OH XXXII-27-5 p-F-Ph H H CH2Ph 'Pr H H F OH ΧΧΧΠ-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr H H F OH ΧΧΧΠ-27-7 p-F-Ph H H CH2CH2SCH3 'Pr H H F OH ΧΧΧΠ-27-8 p-F-Ph ♦ H ♦ 'Pr H H F OH *R2 and joined together by (CH2)3 to form five-membered ring.

Table XXXII-28.

R1 R1 R3’ "r35 R3” R3 R6 X Y XXXII-28-1 p-Cl-Ph H H H w H H F OH XXXII-28-2 p-Cl-Ph H H CH3 'Pr H H F OH XXXII-28-3 p-Cl-Ph H H CH(CH3)2 'Pr H H F OH XXXII-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr H H F OH XXXII-28-5 p-Cl-Ph H H CH2Ph 'Pr H H F OH XXXII-28-6 p-Cl-Ph H H CH2-indol-3-yl Tr H H F OH ΧΧΧΠ-28-7 p-Cl-Ph H H CH2CH2SCH3 'Pr H H F OH XXXI1-28-8 p-Cl-Ph * H * 'Pr H H F OH *R2 and R30 joined together by (CH2)3 to form five-membered ring Table ΧΧΧΠ-29. jp RJ R3e Ίκ35 R4 R1 R6 X Y XXXII-29-1 p-Br-Ph H H H 'Pr H H F OH ΧΧΧΠ-29-2 p-Br-Ph H H ch3 'Pr H H F OH XXXII-29-3 p-Br-Ph H H CH(CH3)2 Tr H H F OH XXXII-29-4 p-Br-Ph H H CH2CH(CH3)2 'Pr H H F OH XXXII-29-5 p-Br-Ph H H CH2Ph 'Pr H H F OH XXXH-29-6 p-Br-Ph H H CH2-indol-3-yl 'Pr H H F OH XXXII-29-7 p-Br-Ph H H CH2CH2SCH3 Tr H H F OH XXXH-29-8 p-Br-Ph * H * 'Pr H H F OH *RZ and RJb joined together by (CH2)3 to form five-membered ring. 2983472-1 -652- PCT/US2008/058183 WO 2008/121634 7 ΛΛΟ„ΜίΛΤΤ1

Docket No. 60137.0034WOU1

Table XXXII-30.

Ns ΊΓ R3a R4 r! Rfc X Y XXXII-30-1 p-I-Ph H H H "W H H F OH XXXII-30-2 p-I-Ph H H ch3 'Pr H H F OH XXXII-30-3 p-I-Ph H H CH(CH3)2 'Pr H H F OH ΧΧΧΠ-30-4 p-I-Ph H H CH2CH(CH3)2 'Pr H H F OH XXXII-30-5 p-I-Ph H H CHjPh 'Pr H H F OH XXXII-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr H H F OH XXXII-30-7 p-I-Ph H H CH2CH2SCH3 'Pr H H F OH XXXII-30-8 p-I-Ph * H * 'Pr H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXXII-31.

Ns R R3 r3. R3b R4 R6 X Y XXXII-31-1 ch3 H H H "Bu H H F OH XXXII-31-2 ch3 H Η ch3 "Bu H H F OH ΧΧΧΠ-31-3 ch3 H H CH(CH3)2 "Bu H H F OH XXXII-31-4 ch3 H H CH2CH(CH3)2 "Bu H H F OH XXXII-31-5 ch3 H H CH2Ph "Bu H H F OH XXXII-31-6 ch3 H H CH2-indol-3-yl "Bu H H F OH XXXH-31-7 ch3 H H CH2CH2SCH3 "Bu H H F OH XXXII-31-8 ch3 * H * "Bu H H F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring. 5 Table XXXII-32. — 1 1 'HL·1· J 1 ' "J "

Ns R RJ r3« R3b R4 RJ R6 X Υ XXXII-32-1 Et H H H "Bu H Η F ΟΗ XXXII-32-2 Et H H CH3 "Bu H Η F ΟΗ ΧΧΧΠ-32-3 Et H H CH(CH3)2 "Bu H Η F ΟΗ XXXII-32-4 Et H H CH2CH(CH3)i "Bu H Η F ΟΗ ΧΧΧΠ-32-5 Et H H CH2Ph "Bu Η Η F ΟΗ XXXII-32-6 Et H H CH2-indol-3-yl "Bu Η Η F ΟΗ XXXII-32-7 Et H H CH2CH2SCH3 "Bu Η Η F ΟΗ XXXII-32-8 Et * H * "Bu Η Η F ΟΗ *R2 and RJb joined together by (CH2)3 to form five-membered ring. Table XXXII-33. Ns R IF RJ. RJb R4 Rs R6 X Υ 2983472-1 -653- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

N° R1 R3· "R36 r^ Rs R6 X Y ΧΧΧΠ-33-1 'Pr H H H "Bu H H F OH XXXII-33-2 'Pr H H ch3 "Bu H H F OH XXXH-33-3 Tr H H CH(CH3)2 "Bu H H F OH ΧΧΧΠ-33-4 'Pr H H CH2CH(CH3)2 "Bu H H F OH ΧΧΧΠ-33-5 'Pr H H CH2Ph "Bu H H F OH XXXII-33-6 'Pr H H CH2-indoI-3-yl "Bu H H F OH XXXII-33-7 'Pr H H CH2CH2SCH3 "Bu H H F OH XXXH-33-8 'Pr * H ♦ "Bu H H F OH *R2 and Rejoined together by (CH2)a to form five-membered ring.

Table XXXII-34.

Xs R RJ r3b R3b R4 RJ R6 X Y XXXH-34-1 'Bu H H H "Bu H H F OH XXXII-34-2 'Bu H H CH3 "Bu H H F OH ΧΧΧΠ-34-3 'Bu H H CHCCH,), "Bu H H F OH ΧΧΧΠ-34-4 'Bu H H CH2CH(CH3)2 "Bu H H F OH XXXII-34-5 'Bu H H CH2Ph "Bu H H F OH ΧΧΧΠ-34-6 'Bu H H CH2-indol-3-yl "Bu H H F OH XXXII-34-7 'Bu H H CH2CH2SCH3 "Bu H H F OH XXXH-34-8 'Bu * H * "Bu H H F OH *R2 and R36 joined together by (CH2)3 to form five-membered ring.

Table XXXI1-35.

X2 R IT R3* R3b R4 R5 Rfc X Y XXXH-35-1 Ph H H H "Bu H H F OH ΧΧΧΠ-35-2 Ph H H ch3 "Bu H H F OH ΧΧΧΠ-35-3 Ph H H CHCCH^ "Bu H H F OH XXXII-35-4 Ph H H CH2CH(CH3)2 "Bu H H F OH ΧΧΧΠ-35-5 Ph H H CH2Ph "Bu H H F OH XXXII-35-6 Ph H H CH2-indol-3-yl "Bu H H F OH XXXII-35-7 Ph H H CH2CH2SCH3 "Bu H H F OH XXXH-35-8 Ph * H * ”Bu H H F OH 5 *R2 and Rejoined together by (CHzb to form five-membered ring. 2983472-1 -654- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Table XXXH-36.

Xs R2 “F” "R35 R4 Rs R6 X Y XXXII-36-1 p-Me-Ph H H H "Bu H H F OH ΧΧΧΠ-36-2 p-Me-Ph H H ch3 "Bu H H F OH XXXI1-36-3 p-Me-Ph H H CH(CH3)2 "Bu H H F OH XXXI1-36-4 p-Me-Ph H H CH2CH(CH3)2 "Bu H H F OH XXXII-36-5 p-Me-Ph H H CH2Ph "Bu H H F OH ΧΧΧΠ-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu H H F OH XXXII-36-7 p-Me-Ph H H CH2CH2SCH3 "Bu H H F OH XXXII-36-8 *«2 i nJb · p-Me-Ph * H * "Bu H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring.

Table XXXII-37.

Xs Rl R7 r3« IF" R5 R* X Y XXXII-37-1 p-F-Ph H H H "Bu H H F OH XXXH-37-2 p-F-Ph H H ch3 "Bu H H F OH XXXH-37-3 p-F-Ph H H ΟΗ(ΟΗ3)2 "Bu H H F OH XXXH-37-4 p-F-Ph H H CH2CH(CH3)2 "Bu H H F OH XXXII-37-5 p-F-Ph H H CH2Ph "Bu H H F OH XXXII-37-6 p-F-Ph H H CH2-indol-3-yl "Bu H H F OH XXXII-37-7 p-F-Ph H H CH2CH2SCH3 "Bu H H F OH XXXII-37-8 p-F-Ph * H * "Bu H H F OH *R2 and Rejoined together by (CH2)3 to form five-membered ring. 5 Table XXXII-38.

" T »— ...... J J 1 « «.— M

Xs R1 R2 r3« Rjb R4^ R5 R6 X Y XXXII-38-1 p-Cl-Ph H H H "Bu H H F OH XXXII-38-2 p-Cl-Ph H H CH3 "Bu H H F OH XXXII-38-3 p-Cl-Ph H H CH(CH3)2 "Bu H H F OH XXXH-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H H F OH XXXII-38-5 p-Cl-Ph H H CH2Ph "Bu H H F OH ΧΧΧΙΪ-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu H H F OH XXXII-38-7 p-Cl-Ph H H CH2CH2SCH3 "Bu H H F OH XXXII-38-8 p-Cl-Ph * H * "Bu H H F OH

Ij ML i i *R and R joined together by (CH2)3 to form five-membered ring. 2983472*1 -655- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Table XXXII-39.

X° "R1 R3 RJa F f? R6 X Y ΧΧΧΠ-39-1 p-Br-Ph H H H "Bu H H F OH XXXI1-39-2 p-Br-Ph H H ch3 "Bu H H F OH XXXII-39-3 p-Br-Ph H H CH(CH3)2 "Bu H H F OH XXXII-39-4 p-Br-Ph H H CH2CH(CH3)2 "Bu H H F OH XXX1I-39-5 p-Br-Ph H H CH2Ph "Bu H H F OH XXXII-39-6 p-Br-Ph H H CH2-indol-3-yl "Bu H H F OH ΧΧΧΠ-39-7 p-Br-Ph H H CH2CH2SCH3 "Bu H H F OH XXXII-39-8 p-Br-Ph * H ♦ "Bu H H F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXXII-40.

Xa R1 R2 R3a Rjb R4 R R6 X Y XXXII-40-1 p-l-Ph H H H "Bu H H F OH XXXII-40-2 p-I-Ph H H ch3 "Bu H H F OH XXXI1-40-3 p-I-Ph H H CH(CH3)2 "Bu H H F OH ΧΧΧΠ-40-4 p-I-Ph H H CH2CH(CH3)2 "Bu H H F OH XXXII-40-5 p-I-Ph H H CH2Ph "Bu H H F OH XXXH-40-6 p-I-Ph H H CH2-indol-3-yl "Bu H H F OH XXXII-40-7 p-I-Ph H H CH2CH2SCH3 "Bu H H F OH XXXII-40-8 p-I-Ph * H ♦ "Bu H H F OH *R2 and R3b joined together by (CHi)j to form five-membered ring. 5 Table XXXH-41.

... I , I -- -.-1-1.,,- . I , ..,1. . — I

Xa R R3 R3a R3b R4 R5 R6 X Y XXXII-41-1 ch3 H Η Η Bz H H F OH ΧΧΧΠ-41-2 ch3 H Η οη3 Bz H H F OH ΧΧΧΠ-41-3 ch3 H Η chcch^ Bz H H F OH XXXII-41-4 ch3 Η Η CH2CH(CH3)2 Bz H H F OH XXXH-41-5 ch3 Η Η CH2Ph Bz H H F OH XXXH-41-6 ch3 Η Η CH2-indol-3-yl Bz H H F OH XXXII-41-7 ch3 Η Η CH2CH2SCH3 Bz H H F OH XXXH-41-8 *n2 ' j «3b' ch3 * Η * Bz H H F OH *R and R joined together by (CH2)3t0 fQrm five-membered ring. 2983472-1 -656- WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Table ΧΧΧΠ-42.

Ns R1 R2 r3. R3b Ί? R6 X Y XXXH-42-1 Et H H H Bz H H F OH XXXII-42-2 Et H H ch3 Bz H H F OH XXXII-42-3 Et H H CH(CH3)2 Bz H H F OH XXXH-42-4 Et H H CH2CH(CH3)2 Bz H H F OH XXXII-42-5 Et H H CH2Ph Bz H H F OH XXXII-42-6 Et H H CH2-indol-3-yl Bz H H F OH XXXIl-42-7 Et H H CH2CH2SCH3 Bz H H F OH ΧΧΧΠ-42-8 Et * H * Bz H H F OH *R2 and Rejoined together by (CHi)^ to form five-membered ring.

Table ΧΧΧΠ-43.

Ns R1 R2 rJb Rjb R4 R5 R6 X Y ΧΧΧΠ-43-1 'Pr H H H Bz H H F OH ΧΧΧΠ-43-2 'Pr H H CH3 Bz H H F oil ΧΧΧΠ-43-3 'Pr H H CH(CH3)a Bz H H F OH ΧΧΧΠ-43-4 'Pr H H CH2CH(CH3)2 Bz H H F OH XXXII-43-5 'Pr H H CH2Ph Bz H H F OH XXXII-43-6 'Pr H H CH2-indol-3-yl Bz H H F OH XXXII-43-7 'Pr H H CH2CH2SCH3 Bz H H F OH XXXII-43-8 'Pr * H * Bz H H F OH 10 *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XXXII-44.

Ns R1 ΊΓ R3’ R3b R4 R5 R6 X Y XXXH-44-1 'Bu H H H Bz H H F OH XXXJI-44-2 'Bu H H CH3 Bz H H F OH XXXII-44-3 'Bu H H CH(CH3)2 Bz H H F OH XXXII-44-4 'Bu H H CH2CH(CH3)2 Bz H H F OH ΧΧΧΠ-44-5 *Bu H H CH2Ph Bz H H F OH ΧΧΧΠ-44-6 'Bu H H CH2-indol-3-yl Bz H H F OH XXXII-44-7 'Bu H H CH2CH2SCH3 Bz H H F OH XXXII-44-8 iBu * H ♦ Bz H H F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXXII-45. 2983472-1 -657 - WO 2008/121634 PCT/US2008/058183

Docket No. 60137.0034WOU1

Xa R1 RJ Ra" R3b R4 RJ R6 X Y XXXII-45-1 Ph H H H Bz H H F OH XXXII-45-2 Ph H H ch3 Bz H H F OH XXXII-45-3 Ph H H CH(CH3)2 Bz H H F OH XXXH-45-4 Ph H H CH2CH(CH3)2 Bz H H F OH XXXII-45-5 Ph H H CH2Ph Bz H H F OH XXXII-45-6 Ph H H CH2-indol-3-yl Bz H H F OH XXXII-45-7 Ph H H CH2CH2SCH3 Bz H H F OH XXXII-45-8 Ph * H * Bz H H F OH *RZ and joined together by (CH2)3 to form five-membered ring.

Table XXXII-46.

Xa R1 r1 r3. IF R4 RJ IF X Y XXXH-46-1 p-Me-Ph H H H Bz H H F OH XXXII-46-2 p-Me-Ph H H CH3 Bz H H F OH XXXII-46-3 p-Me-Ph H H CH(CH3)2 Bz H H F OH ΧΧΧΠ-46-4 p-Me-Ph H H CH2CH(CH3)2 Bz H H F OH ΧΧΧΠ-46-5 p-Me-Ph H H CH2Ph Bz H H F OH XXXII-46-6 p-Me-Ph H H CH2-indol-3-yt Bz H H F OH XXXH-46-7 p-Me-Ph H H CH2CH2SCH3 Bz H H F OH XXXII-46-8 p-Me-Ph * H * Bz H H F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXXII-47.

Xa R1 F r3“ R' R! X Y ΧΧΧΠ-47-1 p-F-Ph H H H Bz H H F OH XXXII-47-2 p-F-Ph H H ch3 Bz H H F OH XXXII-47-3 p-F-Ph H H CH(CH3)2 Bz H H F OH XXXH-47-4 p-F-Ph H H CH2CH(CH3)2 Bz H H F OH ΧΧΧΠ-47-5 p-F-Ph H H CH2Ph Bz H H F OH ΧΧΧΠ-47-6 p-F-Ph H H CH2-indoI-3-yl Bz H H F OH XXXH-47-7 p-F-Ph H H CH2CH2SCH3 Bz H H F OH XXXII-47-8 p-F-Ph * H * Bz H H F OH 5 *Ri and RJb joined together by (CH2)3 to form five-membered ring.

Table ΧΧΧΠ-48.

Xa R1 R3 R3‘ Rib- R4 rf R6 X Y XXXH-48-1 p-Cl-Ph H H H Bz H H F OH . 2983472-1 -658- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

N> Rl R2 R3a RjE IC Ic X Y XXXII-48-2 p-Cl-Ph H H ch3 Bz H H F OH XXXII-48-3 p-Cl-Ph H H CH(CH3)2 Bz H H F OH ΧΧΧΠ-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H H F OH XXXII-48-5 p-Cl-Ph H H CH2Ph Bz H H F OH XXX1I-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz H H F OH XXXII-48-7 p-Cl-Ph H H CH2CH2SCH3 Bz H H F OH XXXII-48-8 p-Cl-Ph ♦ H * Bz H H F OH *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table ΧΧΧΠ-49.

Ns R1 R2 R3‘ Rib Rs R' X Y XXXII-49-1 p-Br-Ph H H H Bz H H F OH XXXII-49-2 p-Br-Ph H H ch3 Bz H H F OH ΧΧΧΠ-49-3 p-Br-Ph H H CHtCH^ Bz H H F OH XXXII-49-4 p-Br-Ph H H CH2CH(CH3)2 Bz H H F OH XXXII-49-5 p-Br-Ph H H CH2Ph Bz H H F OH ΧΧΧΠ-49-6 p-Br-Ph H H CH2-indol-3-yl Bz H H F OH ΧΧΧΠ-49-7 p-Br-Ph H H CH2CH2SCH3 Bz H H F OH XXXII-49-8 p-Br-Ph * H ♦ Bz H H F OH *R2 and RJb joined together by (CH2)3 to form five-membered ring.

Table XXXII-50.

Ns R1 I? R3. -r38 R4 R5 R6 X Y XXXII-50-1 p-I-Ph H H H Bz H H F OH XXXII-50-2 p-I-Ph H H ch3 Bz H H F OH XXXII-50-3 p-I-Ph H H CH(CH3)2 Bz H H F OH XXXU-50-4 p-I-Ph H H CH2CH(CH3)2 Bz H H F OH XXXII-50-5 p-I-Ph H H CH2Ph Bz H H F OH XXXII-50-6 p-I-Ph H H CH2-indol-3-yl Bz H H F OH ΧΧΧΠ-50-7 p-I-Ph H H CH2CH2SCH3 Bz H H F OH XXXII-50-8 *r»2 i T»3b" p-l-Ph ♦ H * Bz H H F OH *R2 and RJb joined together by (CHjh to form five-membered ring. 2983472-1 -659- WO 2008/Π]634^θ 60137O034WOU1 PCT/US2008/058183

DOSAGE, ADMINISTRATION, AND USE A sixth embodiment of the present invention is directed to a composition for the treatment of any of the viral agents disclosed herein said composition comprising a pharmaceutically acceptable medium selected from among an 5 excipient, carrier, diluent, and equivalent medium and a compound, that is intended to include its salts (acid or basic addition salts), hydrates, solvates, and crystalline forms can be obtained, represented by formula I.

It is contemplated that the formulation of the sixth embodiment can contain any of the compounds contemplated in any of the aspects of the first, 10 second, third, fourth, and fifth embodiments or those specifically recited in the tables above or exemplified herein, either alone or in combination with another compound of the present invention.

The compounds of the present invention may be formulated in a wide variety of oral administration dosage forms and carriers. Oral administration can 15 be in the form of tablets, coated tablets, hard and soft gelatin capsules, solutions, emulsions, syrups, or suspensions. Compounds of the present invention are efficacious when administered by suppository administration, among other routes of administration. The most convenient manner of administration is generally oral using a convenient daily dosing regimen which can be adjusted 20 according to the severity of the disease and the patient's response to the antiviral medication. A compound or compounds of the present invention, as well as their pharmaceutically acceptable salts, together with one or more conventional excipients, carriers, or diluents, may be placed into the form of pharmaceutical 25 compositions and unit dosages. The pharmaceutical compositions and unit dosage forms may be comprised of conventional ingredients in conventional proportions, with or without additional active compounds and the unit dosage forms may contain any suitable effective amount of the active ingredient commensurate with the intended daily dosage range to be employed. The 30 pharmaceutical compositions may be employed as solids, such as tablets or filled capsules, semisolids, powders, sustained release formulations, or liquids such as 2983472-1 -660- PCT/US2008/058183 WO 2008/121634 τ ΛΛ„ ,„,ΛΤΤ1

UocKet No. 60137.0034WOU1 suspensions, emulsions, or Filled capsules for oral use; or in the form of suppositories for rectal or vaginal administration. A typical preparation will contain from about 5% to about 95% active compound or compounds (w/w).

The term "preparation" or "dosage form" is intended to include both solid and 5 liquid formulations of the active compound and one skilled in the art will appreciate that an active ingredient can exist in different preparations depending on the desired dose and pharmacokinetic parameters.

The term "excipient" as used herein refers to a compound that is used to prepare a pharmaceutical composition, and is generally safe, non-toxic and 10 neither biologically nor otherwise undesirable, and includes excipients that are acceptable for veterinary use as well as human pharmaceutical use. The compounds of this invention can be administered alone but will generally be administered in admixture with one or more suitable pharmaceutical excipients, diluents or carriers selected with regard to the intended route of administration 15 and standard pharmaceutical practice. A "pharmaceutically acceptable salt" form of an active ingredient may also initially confer a desirable pharmacokinetic property on the active ingredient which were absent in the non-salt form, and may even positively affect the pharmacodynamics of the active ingredient with respect to its 20 therapeutic activity in the body. The phrase "pharmaceutically acceptable salt" of a compound as used herein means a salt that is pharmaceutically acceptable and that possesses the desired pharmacological activity of the parent compound. Such salts include: (1) acid addition salts, formed with inorganic acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, 25 and the like; or formed with organic acids such as glycolic acid, pyruvic acid, lactic acid, malonic acid, malic acid, maleic acid, fumaric acid, tartaric acid, citric acid, 3-(4-hydroxybenzoyl)benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, 1,2-ethane-disulfonic acid, 2-hydroxyethanesulfonic acid, benzenesulfonic acid, 4-chlorobenzenesulfonic 30 acid, 2-naphthaIenesulfonic acid, 4-toluenesulfonic acid, camphorsulfonic acid, lauryl sulfuric acid, gluconic acid, glutamic acid, salicylic acid, muconic acid, and the like or (2) basic addition salts formed with the conjugate bases of any of 2983472-1 -661- PCT/US2008/058183 WO 2008/121634 τ „

Docket No. 60137.0034WOU1 the inorganic acids listed above, wherein the conjugate bases comprise a cationic component selected from among Na+, K+, Mg2*, Ca2+, and NHgR 4.g+, in which R" is a Ct.3 alkyl and g is a number selected from among 0, 1,2, 3, or 4. It should be understood that all references to pharmaceutically acceptable salts 5 include solvent addition forms (solvates) or crystal forms (polymorphs) as defined herein, of the same acid addition salt.

Solid form preparations include powders, tablets, pills, capsules, suppositories, and dispersible granules. A solid carrier may be one or more substances which may also act as diluents, flavoring agents, solubilizers, 10 lubricants, suspending agents, binders, preservatives, tablet disintegrating agents, or an encapsulating material. In powders, the carrier generally is a finely divided solid which is a mixture with the finely divided active component. In tablets, the active component generally is mixed with the carrier having the necessary binding capacity in suitable proportions and compacted in the shape and size 15 desired. Suitable carriers include but are not limited to magnesium carbonate, magnesium stearate, talc, sugar, lactose, pectin, dextrin, starch, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose, a low melting wax, cocoa butter, and the like. Solid form preparations may contain, in addition to the active component, colorants, flavors, stabilizers, buffers, artificial and natural 20 sweeteners, dispersants, thickeners, solubilizing agents, and the like.

Liquid formulations also are suitable for oral administration include liquid formulation including emulsions, syrups, elixirs and aqueous suspensions. These include solid form preparations which are intended to be converted to liquid form preparations shortly before use. Emulsions may be prepared in 25 solutions, for example, in aqueous propylene glycol solutions or may contain emulsifying agents such as lecithin, sorbitan monooleate, or acacia. Aqueous suspensions can be prepared by dispersing the finely divided active component in water with viscous material, such as natural or synthetic gums, resins, methylcellulose, sodium carboxymethylcellulose, and other well known 30 suspending agents.

The compounds of the present invention may be formulated for administration as suppositories. A low meltingwax, such as a mixture of fatty 2983472-1 -662- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/0S8183 acid glycerides or cocoa butter is first melted and the active component is dispersed homogeneously, for example, by stirring. The molten homogeneous mixture is then poured into convenient sized molds, allowed to cool, and to solidify. 5 The compounds of the present invention may be formulated for vaginal administration. Pessaries, tampons, creams, gels, pastes, foams or sprays containing in addition to the active ingredient such carriers as are known in the art to be appropriate.

Suitable formulations along with pharmaceutical carriers, diluents and 10 expcipients are described in Remington: The Science and Practice of Pharmacy 1995, edited by E. W. Martin, Mack Publishing Company, 19th edition, Easton, Pennsylvania, which is hereby incorporated by reference. The compounds of the present invention can also be encapsulated in liposomes, such as those disclosed in U.S. Patent Nos. 6,180,134, 5,192,549, 5,376,380,6,060,080, 6,132,763, each 15 of which is incorporated by reference. A skilled formulation scientist may modify the formulations within the teachings of the specification to provide numerous formulations for a particular route of administration without rendering the compositions of the present invention unstable or compromising their therapeutic activity. 20 The modification of the present compounds to render them more soluble in water or other vehicle, for example, may be easily accomplished by minor modifications (e.g., salt formulation), which are well within the ordinary skill in the art. It is also well within the ordinary skill of the art to modify the route of administration and dosage regimen of a particular compound in order to manage 25 the pharmacokinetics of the present compounds for maximum beneficial effect in patients. A seventh embodiment of the present invention is directed to a use of the compound represented by formula I in the manufacture of a medicament for the treatment of any condition the result of an infection by any one of the following 30 viral agents: hepatitis C virus, West Nile virus, yellow fever virus, dengue virus, 2983472-1 -663- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 rhinovirus, polio virus, hepatitis A virus, bovine viral diarrhea virus and Japanese encephalitis virus.

The term "medicament" means a substance used in a method of treatment and/or prophylaxis of a subject in need thereof, wherein the substance includes, 5 but is not limited to, a composition, a formulation, a dosage form, and the like, comprising the compound of formula I. It is contemplated that the compound of the use of the compound represented by formula I in the manufacture of a medicament for the treatment of any of the antiviral conditions disclosed herein of the seventh embodiment can be any of the compounds contemplated in any of 10 the aspects of the first, second, third, fourth, fifth embodiments or those specifically recited in the tables above or exemplified herein, either alone or in combination with another compound of the present invention. A medicament includes, but is not limited to, any one of the compositions contemplated by the sixth embodiment of the present invention. 15 A eighth embodiment of the present invention is directed to a method of treatment and/or prophylaxis in a subject in need thereof said method comprises administering a therapeutically effective amount of the compound represented by formula I to the subject. A first aspect of the eighth embodiment is directed to a method of 20 treatment and/or prophylaxis in a subject in need thereof said method comprises administering a therapeutically effective of at least two or more different compounds falling within the scope of the compound represented by formula I to the subject. A second aspect of the eighth embodiment is directed to a method of 25 treatment and/or prophylaxis in a subject in need thereof said method comprises alternatively or concurrently administering a therapeutically effective of at least two compounds falling within the scope of the compound represented by formula I to the subject.

It is intended that a subject in need thereof is one that has any condition 30 the result of an infection by any of the viral agents disclosed herein, which includes, but is not limited to, hepatitis C virus, West Nile virus, yellow fever 2983472-1 -664- PCT/US2008/058183 WO 2008/121634 x

Docket No. 60137.0034WOU1 virus, dengue virus, rhinovirus, polio virus, hepatitis A virus, bovine viral diarrhea virus or Japanese encephalitis virus, flaviviridae viruses or pestiviruses or hepaciviruses or a viral agent causing symptoms equivalent or comparable to any of the above-listed viruses. 5 The term "subject" means a mammal, which includes, but is not limited to, cattle, pigs, sheep, chicken, turkey, buffalo, llama, ostrich, dogs, cats, and humans, preferably the subject is a human. It is contemplated that in the method of treating a subject thereof of the sixth embodiment can be any of the compounds contemplated in any of the aspects of the first, second, and third 10 embodiments or those specifically recited in the tables above, either alone or in combination with another compound of the present invention.

The term "therapeutically effective amount" as used herein means an amount required to reduce symptoms of the disease in an individual. The dose will be adjusted to the individual requirements in each particular case. That 15 dosage can vary within wide limits depending upon numerous factors such as the severity of the disease to be treated, the age and general health condition of the patient, other medicaments with which the patient is being treated, the route and form of administration and the preferences and experience of the medical practitioner involved. For oral administration, a daily dosage of between about 20 0.1 and about 10 g, including all values in between, such as 0.25, 0.5,0.75,1, 1.5,2,2.5, 3, 3.5,4,4.5, 5, 5.5, 6, 6.5,7, 7.5, 8, 8.5,9, and 9.5, per day should be appropriate in monotherapy and/or in combination therapy. A preferred daily dosage is between about 0.5 and about 7.5 g per day, more preferred 1.5 and about 6.0 g per day. Generally, treatment is initiated with a large initial "loading 25 dose" to rapidly reduce or eliminate the virus following by a decreasing the dose to a level sufficient to prevent resurgence of the infection. One of ordinary skill in treating diseases described herein will be able, without undue experimentation and in reliance on personal knowledge, experience and the disclosures of this application, to ascertain a therapeutically effective amount of the compounds of 30 the present invention for a given disease and patient.

Therapeutic efficacy can be ascertained from tests of liver function including, but not limited to protein levels such as serum proteins (e.g., albumin, 2983472-1 -665- PCT/US2008/058183 WO 2008/121634 τ

JJocket No. 60137.003 4WOUI clotting factors, alkaline phosphatase, aminotransferases (e.g., alanine transaminase, aspartate transaminase), 5'-nucleosidase, γ-glutaminyltranspeptidase, etc.), synthesis of bilirubin, synthesis of cholesterol, and synthesis of bile acids; a liver metabolic function, including, but not limited 5 to, carbohydrate metabolism, amino acid and ammonia metabolism.

Alternatively the therapeutic effectiveness may be monitored by measuring HCV-RNA. The results of these tests will allow the dose to be optimized. A third aspect of the eighth embodiment, is directed to a method of treatment and/or prophylaxis in a subject in need thereof said method comprises 10 administering to the subject a therapeutically effective of a compound represented by formula I and a therapeutically effective amount of another antiviral agent; wherein the administration is concurrent or alternative. It is understood that the time between alternative administration can range between 1-24 hours, which includes any sub-range in between including, 2,3,4, 5,6, 7, 15 8, 9, 10, 11,12, 13, 14,15, 16,17,18,19,20,21,22, and 23 hours. Examples of

"another antiviral agents" include, but are not limited to: HCV NS3 protease inhibitors (see WO 2008010921, WO 2008010921, EP 1881001, WO 2007015824, WO 2007014925, WO 2007014926, WO 2007014921, WO 2007014920, WO 2007014922, US 2005267018, WO 2005095403, WO

20 2005037214, WO 2004094452, US 2003187018, WO 200364456, WO

2005028502, and WO 2003006490); HCV NS5B Inhibitors (see US 2007275947, US20072759300, W02007095269, WO 2007092000, WO 2007076034, WO 200702602, US 2005-98125, WO 2006093801, US 2006166964, WO 2006065590, WO 2006065335, US 2006040927, US

25 2006040890, WO 2006020082, WO 2006012078, WO 2005123087, US

2005154056, US 2004229840, WO 2004065367, WO 2004003138, WO 2004002977, WO 2004002944, WO 2004002940, WO 2004000858, WO 2003105770, WO 2003010141, WO 2002057425, WO 2002057287, WO 2005021568, WO 2004041201, US 20060293306, US 20060194749, US

30 20060241064, US 6784166, WO 2007088148, WO 2007039142, WO

2005103045, WO 2007039145, WO 2004096210, and WO 2003037895); HCV NS4 Inhibitors (see WO 2007070556 and WO 2005067900); HCV NS5a Inhibitors (see US 2006276511, WO 2006120252, WO 2006120251, WO 2983472-1 -666- PCT/US2008/058183 WO 2008/121634 τ Λ/ν>,„,ΛΤΤ1

Docket No. 60137.0034WOU1 2006100310, WO 2006035061); Toll-like receptor agonists (seeWO 2007093901); and other inhibitors (see WO 2004035571, WO 2004014852, WO 2004014313, WO 2004009020, WO 2003101993, WO 2000006529). A fourth aspect of the eighth embodiment, is directed to a method of 5 treatment in a subject in need thereof said method comprises alternatively or concurrently administering a therapeutically effective of a compound represented by formula I and another antiviral agent to the subject. It is understood that the time between alternative administration can range between 1-24 hours, which includes any sub-range in between including, 2,3,4, 5,6,7, 10 8,9,10, 11, 12, 13, 14, 15, 16, 17, 18, 19,20,21,22, and 23 hours. A fifth aspect of the eighth embodiment, is directed to a method of treatment and/or prophylaxis in a subject in need thereof said method comprises administering to the subject a therapeutically effective of at least one compound represented by formula I and a therapeutically effective amount of another 15 antiviral agent; wherein the administration is concurrent or alternative. It is understood that the time between alternative administration can range between . 1-24 hours, which includes any sub-range in between including, 2,3,4, 5, 6,7, 8, 9, 10, 11, 12, 13, 14, 15, 16,17, 18, 19,20, 21,22, and 23 hours. A sixth aspect of the eighth embodiment, is directed to a method of 20 treatment in a subject in need thereof said method comprises alternatively or concurrently administering a therapeutically effective of at least one compound represented by formula I and another antiviral agent to the subject. It is understood that the time between alternative administration can range between 1-24 hours, which includes any sub-range in between including, 2,3,4, 5,6,7, 25 8,9, 10, 11, 12,13, 14, 15, 16, 17, 18, 19,20,21,22, and 23 hours.

It is contemplated that the another antiviral agent includes, but is not limited to interferon -a, interferon-β, pegylated interferon-α, ribavirin, levovirin, viramidine, another nucleoside HCV polymerase inhibitor, a HCV non-nucleoside polymerase inhibitor, a HCV protease inhibitor, a HCV helicase 30 inhibitor or a HCV fusion inhibitor. When the active compound or its derivative or salt are administered in combination with another antiviral agent the activity 2983472-t -667- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183 may be increased over the parent compound. When the treatment is combination therapy, such administration may be concurrent or sequential with respect to that of the nucleoside derivatives. "Concurrent administration” as used herein thus includes administration of the agents at the same time or at different times. 5 Administration of two or more agents at the same time can be achieved by a single formulation containing two or more active ingredients or by substantially simultaneous administration of two or more dosage forms with a single active agent.

It will be understood that references herein to treatment extend to 10 prophylaxis as well as to the treatment of existing conditions. Furthermore, the term "treatment" of a HCV infection, as used herein, also includes treatment or prophylaxis of a disease or a condition associated with or mediated by HCV infection, or the clinical symptoms thereof.

PROCESS FOR PREPARATION 15 An ninth embodiment of the present invention is directed to a process for preparing the compound of formula I, which comprises reacting a suitably substituted phosphochloridate compound 4 with a nucleoside analog 5

4 6 wherein the substituents R1, R2, R3a, R3b, R4, R5, X, Y, R6, and base have 20 their meanings as disclosed in the Detailed Description of the Invention and X' is a leaving group, such as Cl, Br, I, tosylate, mesylate, trifluoroacetate, tri fluorosulfonate, pentafluorophenoxide, p-NO2-phenoxide, or other commonly used leaving groups as disclosed in Advanced Organic Chemistry by March, Fourth Edition. Leaving groups and methods that can be used to effect the 25 formation of a phosphoramidate nucleoside conjugate are found in US 20060142238 and WO 2007095269. Preferably, the leaving group is Cl.

This reaction is performed in an anhydrous aprotic solvent such tetrahydrofuran, dioxane, or both tetrahydrofuran and dioxane, or any functional 2983472-1 -668- PCT/US2008/058183 WO 2008/121634 τ ,„ΓΛΙ,,

Docket No. 60137.0034WOU1 equivalent thereof, with tetrahydrofuran being the preferred solvent. The reaction is typically initiated at a temperature range from -78°C to 40°C with the preferred reaction temperature being between 0°C and room temperature. The nucleoside is first stirred with a base (5 to 12 equivalents) such as N- 5 methylimidazole, collidine, pyridine, 2,6-lutidine, 2, 6-'Bu-pyridine, etc. a tertiary amine base, such as triethylamine, diisopropylethylamine, etc., or an alkyl Grignard reagent, such as tBuMgCI, tBuMgBr, MeMgCl, MeMgBr, etc. The phosphorochloridate (3-10 equivalents) is dissolved in the reaction solvent and added to the mixture of the nucleoside and base. The reaction is then 10 allowed to stir over a period of time at a temperature between room temperature and 40°C for a period of 30 min to 24 hr. with the preferred reaction temperature being room temperature and time being 24 hr. The solvent is removed from the reaction mixture and the product is purified by chromatography on silica gel. A tenth embodiment of the present invention is directed to a product 15 obtained by a process which comprises reacting a suitably substituted phosphochloridate compound 4 with a nucleoside analog 5

4 s wherein the substituents R1, R2, R3a, R3b, R4, R5, X, Y, R6, X', and base have their meanings as disclosed in the Detailed Description of the Invention. 20 This reaction can be performed in an anhydrous aprotic solvent or other suitable solvent, such as tetrahydrofuran, dioxane, or a mixture of tetrahydrofuran and dioxane, with tetrahydrofuran being the preferred solvent. The reaction is typically initiated at a temperature range from -78°C to 40°C with the preferred reaction temperature being between 0°C and room temperature. 25 The nucleoside is first stirred with a base (5 to 12 equivalents) such as N-methylimidazole, a tertiary amine base or tButyl Magnesium Chloride. A phosphorochloridate (3-10 equivalents (or suitable "phosphoro-(leaving group)-date")) is dissolved in the reaction solvent and added to the mixture of the nucleoside and base. The reaction is then allowed to stir over a period of time at 2983472-1 -669- WO 2008/121634 τ

Docket No. 60137.0034WOU1 PCT/US2008/058183 a temperature between room temperature and 40°C for a period of 30 min to 24 hr. with the preferred reaction temperature being room temperature and time being 24 hr. The solvent is removed from the reaction mixture and the product is purified by chromatography on silica gel. 5 Compounds and Preparation

Phosphoramidate compounds of the present invention can be prepared by condensation of a nucleoside analog 5 with a suitably substituted phosphochloridate compound 4 (Scheme 1). The nucleoside analog is made by conventional procedures disclosed in any one of U.S. Published Application 10 Nos. 2005/0009737, 2006/0199783,2006/0122146, and 2007/0197463, each of which is incorporated by reference in its entirety.

Disclosed 1H-NMR values were recorded on a Varian AS-400 instrument. Mass spectral data were obtain using either a Micromass-Quattromicro API or a Waters Acquity. 15 Thus, by way of example only, a suitably substituted phenol can be reacted with phosphorus oxychloride (1) to afford an aryloxy phosphorodichloridate 2 (see Example 1) which is subsequently treated with a acid addition salt of an α-amino acid ester in the presence of TEA to afford an aryloxy phosphorochloridate 4. This arylalkoxy-amino acid phosphoramidate is 20 reacted with the nucleoside analog to provide the product I (for procedure see, e.g., C. McGuigan et al. Antiviral Res. 1992 17:311-321; D. Curley et al. Antiviral Res. 1990 14:345-356; McGuigan etal. Antiviral Chem. Chemother 1990 1(2):107-113). 2983472-1 -670-

Docket No. 60137.0034WOU1 WO 2008/121634 PCT/US2008/058183

Scheme 1

,3b o.

A* = CI“or Ts' :3¾

ci 4

HO

‘Base

The preparation of nucleoside phosphoramidates requires reacting an 5 appropriately substituted phosphochloridate with a nucleoside containing a free 5'-hydroxyl moiety. In cases where only one hydroxyl group is present, preparation of the phosphoramidate usually proceeds smoothly when the phosphochloridate is reacted with the desired nucleoside. In cases where the nucleoside contains more than one free hydroxyl group, preparation of the 10 appropriately protected nucleoside might be required. Silyl, acetonide or other alcohol protecting groups known in the art might be warranted for protection of the sugar moiety. For protection of the nucleoside base, protecting a free amino group may require amidine protection strategy.

Condensation of the phosphochloridate can be carried out on the 15 unprotected nucleoside. Since the 5-OH group of a nucleoside is much less hindered than the 3'-OH group, selective phosphoramidation is possible under carefully controlled conditions. After condensation to form a protected phosphoramidate nucleoside, deprotection to obtain the free phosphoramidate nucleoside can be carried out using standard protocols for nucleic acid 20 chemistry. In many cases, the desired product is readily separated from the starting material using column chromatography on silica gel. The synthetic scheme is summarized in Scheme 1. 2983472-1 -671 - PCT/US2008/058183 WO 2008/121634 ,Λ „

Docket No. 60137.0034WOU1 A further understanding of the disclosed embodiments will be appreciated by consideration of the following examples, which are only meant to be illustrative, and not limit the disclosed invention. EXAMPLE 1 ct— 'Ci o 2 5 General Procedure for Preparation of phosphorodichloridates i

+ Ri_0H o 1 A solution of the appropriate phenol R^OH (1 eq) and triethylamine (1 eq.) in anhydrous ether was added dropwise to a stirred solution of phosphoryl trichloride 1 (leq) at 0 °C over a period of 3 hours under nitrogen. Then the 10 temperature was warmed to room temperature, and the reaction was stirred overnight. The triethylamine salt was quickly removed with suction filtration and the filtrate concentrated in vacuo to dryness to afford 2 as an oil which was used without further purification. EXAMPLE 2 15 General Procedure for Preparation of phosphorochloridates ?'R’ ci—^j-ci o

R2 A' = Ct or Ts* 3 xP-ci A solution of triethylamine (2eq) in anhydrous dichloromethane was added dropwise to a solution of aryloxy-phosphodichloridate 2 (1 eq) and the 2 2983472-1 -672- WO 2008/121634 τ

Docket No. 60137.0034WOU1 PCT/US2008/058183 appropriate amino ester 3 (1 eq) in anhydrous dichloromethane with vigorous stirring at -78 °C over a period of 30 to 120 minutes. Then the reaction temperature was allowed to warm to room temperature and stirred over night.

Solvent was removed. The residue was washed with ethyl ether and filtered, the 5 filtrate was dried over reduced pressure to give 4. EXAMPLE 3

General Procedures for nucleoside phosphoramidate derivatives

10 A solution of the appropriate phosphorochloridate 4 (6.5 equivalents) in anhydrous tetrahydrofuran (THF) was added to a mixture of nucleoside 5 (1 equivalent) and N-methylimidazole (8 equivalents) in anhydrous THF with vigorous stirring at room temperature and the reaction mixture was stirred overnight. The solvent was removed in vacuo and the crude was purified by 15 column chromatography and/or preparative thin layer chromatography to give I. 2983472-1 -673- PCT/US2008/058183 WO 2008/121634 __ Ληο,..,ΛΙn

LiocKet No. 60137.0034WOU1 EXAMPLE 4

Preparation of 2'-deoxy-2'-fluoro-2’-C-inethyl uridine

2'-Deoxy-2,-fluoro-2'-C-methylcytidine (l.Og, 1 eq ) (Clark, J., et at, J. 5 Med, Chem., 2005, 48, 5504-5508) was dissolved in 10 ml of anhydrous pyridine and concentrated to dryness in vacuo. The resulting syrup was dissolved in 20 ml of anhydrous pyridine under nitrogen and cooled to 0°C with stirring. The brown solution was treated with benzoyl chloride (1.63g, 3eq) dropwise over 10 min. The ice bath was removed and stirring continued for 1.5h whereby 10 thin-layer chromatography (TLC) showed no remaining starting material. The mixture was quenched by addition of water (0.5 ml) and concentrated to dryness. The residue was dissolved in 50 mL of dichloromethane (DCM) and washed with saturated NaHCCh aqueous solution and H2O. The organic phase was dried over NaSC>4 and filtered, concentrated to dryness to give N43,,5’-tribenzoyl-2- 15 Deoxy-2'-fluoro-2'-C-methylcytidine (2.0 g, Yield: 91%). N4,3\5'-tribenzoyl-2-Deoxy-2,-fluoro-2’-C-methylcytidine (2.0g, 1 eq ) was refluxed in 80% aqueous AcOH overnight. After cooling and standing at room temperature (15 °C), most of the product precipitated and then was filtered 2983472-1 -674- W0 2WSL)ocketNo. 60137.0034 W0U1 PCT/US2008/058183 through a sintered funnel. White precipitate was washed with water and coevaporated with toluene to give a white solid. The filtrate was concentrated and co-evaporated with toluene to give additional product which was washed with water to give a white solid. Combining the two batches of white solid gave 1.50g 5 of 3',5'-dibenzoyl-2’-Deoxy-2'-fiuorO“2’-C-methyluridine (Yield: 91%).

To a solution of S'jS'-dibenzoyl^'-Deoxy-^-fluoro^'-C-methyluridine (1.5 g, leq) in MeOH (10 mL) was added a solution of saturated ammonia in MeOH (20mL). The reaction mixture was stirred at 0 °C for 30 min, and then warmed to room temperature slowly. After the reaction mixture was stirred for 10 another 18 hours, the reaction mixture was evaporated under reduced pressure to give the residue, which was purified by column chromatography to afford pure compound 2'-deoxy-2'-fluoro-2'-C-methyluridine (500 mg, Yield: 60 %). EXAMPLE 5 15

Preparation of 2,-Deoxy-2'-fluoro-2’-C-methyluridine 5’-(phenyl methoxyalanyl phosphate)

Phenyl methoxyalaninyl phosphorochloridate (1 g, 6.5 eq) dissolved in 3 mL of THF was added to a mixture of 2’-Deoxy-2,-fluoro-2'-C-methyluridine 20 (0.15 g,l eq) and N-methyl imidazole (0.3 g, 8 eq) in 3 mLTHF with vigorous stirring at room temperature, then the reaction was stirred overnight. Solvent was removed by reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25x30X2 mm column using a water / acetonitrile gradient elution mobile phase. The acetonitrile and water were 2983472-1 -675- PCT/US2008/058183 WO 2008/121634 t

Docket No. 60137.0034WOU1 removed under reduced pressure to give the desired product (50.1 mg, 15.6%). ‘H NMRCDMSO-iifi) δ 1.20-1.27 (m, 6H), 3.58 (d, J= 16.0 Hz, 3H), 3.75-3.92 (m, 2H), 4.015-4.379 (m, 2H), 5.54 (t, J- 10.2 Hz, 1H), 5.83-5.91 (m, 1H), 6.00-6.16 (m, 1H), 7.18 (d, /= 8.0 Hz, 2H), 7.22 (s, 1H), 7.35 (t,./- 4.4 Hz, 5 2H), 7.55 (s, 1H), 11.52 (s, 1H); MS, m/e 502 (M+l)+. EXAMPLE 6

Preparation of 2'-Deoxy-2'-fluoro-2'-C-methyluridine 5*-(phenyl methoxyvalyl phosphate)

ΖΣ

Phenyl methoxy-valyl phosphorochloridate (0.6 g, 3.6 eq) dissolved in 3 mL of THF was added to a mixture of 2'-Deoxy-2'-fluoro-2'-C-methyluridine (0.15 g, 1 eq) and N-methylimidazole (0.44 g, 9 eq) in 3 mL THF with vigorous stirring at room temperature, then the reaction was stirred overnight. Solvent was 15 removed by reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25x30X2 mm column using a water / acetonitrile gradient elution mobile phase. The acetonitrile and water were removed under reduced pressure to give the desired product (60 mg, 20%). lH NMR (DMSO-iffi) 8 0.74-0.847 (m, 6H), 1.20-1.28 (m, 3H), 1.89-1.92 (m, 1H), 20 3.50-3.54 (m, 1H), 3.58 (d, J= 10.4Hz, 3H), 3.72-3.95 (m, 1H), 4.03-4.05 (m, 1H), 4.23-4.43 (m, 2H), 5.56 (t, /= 16.0 Hz, 1H), 5.85-5.92 (m, 1H), 6.01-6.07 (m, 1H), 7.16-7.21 (m, 3H), 7.37 (t,/= 8 Hz, 2H), 7.55-7.60 (m, 1H), 11.52 (s, 1H); MS, m/e 530 (M+l)+. 2983472-1 -676- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 EXAMPLE 7

Preparation of 2'-Dcoxy-2’-fluoro-2,-C-inethyluridine 5’-(4-bromophenyl methoxy-valyl phosphate)

4-Bromophenyl methoxy-valyl phosphorochloridate (1 g, 3.4 eq) dissolved in 3 mL of THF was added to a mixture of 2'-deoxy-2'-fluoro-2'-C-methyluridine (0.2 g, 1 eq) and N-methylimidazole (0.35 g, 6 eq) in 3 mL THF with vigorous stirring at room temperature, then the reaction was stirred 10 overnight. Solvent was removed by reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25x30X2 mm column using a water / acetonitrile gradient elution mobile phase. The acetonitrile and water were removed reduced pressure to give the desired product (120 mg, 26%). 'H NMR (DMSO-4) δ 0.72-0.82 (m, 6H), 1.19-1.26 (m, 3H), 15 1.86-1.92 (m, 1H), 3.48-3.50 (m, 1H), 3.56 (d, 7= 12.0 Hz, 3H), 3.72-3.89 (m, 1H), 3.96-4.03 (m, 1H), 4.22-4.37 (m, 2H), 5.54-5.60 (m, 1H), 5.85-5.91 (m, 1H), 5.98-6.13 (m, 1H), 7.15 (d, 7= 8.0 Hz, 2H), 7.49-7.56 (m, 3H), 11.53 (s, 1H); MS, m/e 608 (M+l)+. 2983472-1 -677- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 EXAMPLE 8

Preparation of I'-Deoxy-l'-fluoro-l'-C-methyluridine 5*-(4-bromophenyl methoxy-alanyl phosphate)

4-Bromophenyl methoxy-alanyl phosphorochloridate (0.6 g, 5 eq) dissolved in 3 mL of THF was added to a mixture of 2,-deoxy-2'-fluoro-2’-C-methyluridine (0.15 g,l eq)and N-methyl imidazole (0.3 g, 7.8 eq) in 3 mLTHF with vigorous stirring at room temperature, then the reaction was stirred 10 overnight. Solvent was removed by reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25x30X2 mm column using a water / acetonitrile gradient elution mobile phase. The acetonitrile and water were removed under reduced pressure to give the desired product (40 mg, 12 %); ’HNMRiDMSO-rfe) δ 1.20-1.26 (m, 6H), 3.57 (d, J= 15 2.8 Hz, 3H), 3.84 (s, 1H), 3.97-4.03 (m, 1H), 4.21-4.25 (m, 1H), 4.33-4.37 (m, 2H), 5.54-5.60 (m, 1H), 5.83-5.89 (m, 1H), 5.98-6.19 (m, 1H), 7.16 (t, J = 10.2 Hz, 2H), 7.52-7.57 (m, 3H), 11.52 (s, 1 H); MS, m/e 580(M+l)+. EXAMPLE 9

Preparation of Ν^/ν,ΛΜ i methyl form a midi ny 1)-2'-deoxy-2’-flu oro-2'-C~ 20 methylcytidine

2'-Deoxy-2,-fiuoro-2'-C-methylcytidine (500 mg, 1.9 mmol) was stirred with dimethylformamide dimethyl acetal in DMF (10 mL). The resulting mixture was stirred af room temperature overnight. After solvent removal the 2983472-1 -678- WO 2008/121634 ΛΛΟ^1/ΛΤΪ1

Docket No. 60137.0034WOU1 PCT/US2008/058183 crude product was used for next step without further purification. EXAMPLE 10

Preparation of l^Deoxy-l'-fluoro-l’-C-methylcytidine 5*-(phenyl methoxy-alanyl phosphate)

Phenyl methoxyalaninyl phosphorochloridate (0.6 g, 6 eq) dissolved in 3 mL of THF was added to a mixture of N4-(7V, ^dimethyl formam id inyl)-2'-deoxy-2'-fluoro-2'-C-methylcytidine (0.15 g, 1 eq) and N-methylimidazole (0.3 g, 10 7.8 eq) in 3 mL THF with vigorous stirring at room temperature, then the reaction was stirred overnight. Solvent was removed by reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25x30X2 mm column using a water / acetonitrile gradient elution mobile phase. The acetonitrile and water were removed under reduced pressure to give 15 the desired product (62 mg, 20.6%). ’H NMR (DMSO-Je) 5 1.16 (d, J~ 23.2 Hz, 3H), 1.22 (d, /= 7.2 Hz, 3H), 3.56 (S, 3H), 3.69-3.75 (d, / = 25.6 Hz, 1H), 3.82-3.86 (m, 1H), 3.96-3.98 (m, 1H), 4.21-4.34 (m, 2H), 5.68 (d,/= 7.2 Hz, 1H), 5.75-5.77 (m, 1H), 6.07-6.16 (m, 1H), 7.15-7.19 (m, 3H), 7.2 (d, /= 9.2 Hz, 2H), 7.39 (t, /= 7.8 Hz, 2H), 7.48 (d, /= 9.2 Hz, 1H); MS, m/e 501(M+l)\ 2983472-1 -679- WO 2008/121634 r

Docket No. 60137.0034WOU1 PCT/US2008/058183 EXAMPLE ll

Preparation of i'-Deoxy-l’-fluoro-i’-C-methylcytidine 5,-(4-bromophcnyl methoxy-valyl phosphate)

4-Bromophenyl methoxy-valyl phosphorochloridate (l.O g, 3.4 eq.) dissolved in 3 mL of THF was added to a mixture of Ν4-(ΛζΝ-dimethylformamidinyl)-2’-deoxy-2'-fluoro-2'-C-methylcytidine (0.2 g,l eq.) and 10 N-methylimidazole (0.35 g, 6 eq.) in 3 mL THF with vigorous stirring at room temperature, then the reaction was stirred overnight. Solvent was removed by reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25x30X2 mm column using a water / acetonitrile gradient elution mobile phase. The acetonitrile and water were 15 removed under reduced pressure to give the desired product as a white solid (59 mg, 13%); 'HNMR (DMSO-ί/δ) δ 0.74-0.83 (m, 6H), 1.12-1.20 (m, 3H), l .89-1.92 (m, lH), 3.49-3.51 (m, lH), 3.55 (s, 3H), 3.59-3.68 (m, lH), 3.72-.383 (m, lH), 4.21-4.39 (m, 2H), 5.70-5.72 (m, lH), 5.76-5.83 (m, lH), 6.04-6.16 (m, lH), 7.15 (d, 7 = 13.0 Hz, 2H), 7.26 (s, lH), 7.33 (s, lH), 7.46-7.55 (m, lH), 20 7.56 (d, J = 4.4 Hz, 2H); MS, mte 607 (M+l)\ 2983472-1 -680- PCT/US2008/058183 WO 2008/121634 , ΛΛ„

Docket No. 60137.0034WOU1 EXAMPLE 12

Preparation of 2'-deoxy-2'-fluoro-2'-C-methylcytidine 5’-(phenyl methoxy-valyl phosphate)

Phenyl methoxy-valyl phosphorochloridate (0.6 g, 6 eq) dissolved in 3 mL of THF was added to a mixture of N4-(jV, jV-dimethyl form amid inyl)-2'-deoxy-2'-f]uoro-2'-C-methylcytidine (0.15 g,l eq) and N-methylimidazole (0.3 g, 10 7.8 eq) in 3 mL THF with vigorous stirring at room temperature, then the reaction was stirred overnight. Solvent was removed by reduced pressure The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25x30X2 mm column using a water / acetonitrile gradient elution mobile phase. The acetonitrile and water were removed under reduced pressure to give 15 the desired product as a white solid (86 mg, 42.9 %). ]H NMR (DMSO-^) δ 0.72-0.80 (m, 6H), 1.09-1.18 (m, 3H), 1.87-1.92 (m, 1H), 3.47-3.51 (m, 1H), 3.58 (s, 3H), 3.71-3.75 (m, IH), 3.97 (t, J= 11.2 Ηζ,ΙΗ), 4.22-4.37 (m, 2H), 5.70 (d, J= 8.0 Ηζ,ΙΗ), 5.76-5.84 (m, 1H), 6.01-6.15 (m, 1H), 7.13-7.18 (m, 3H), 7.27 (s, 2H), 7.34 (d, J- 4.0 Hz, 2H), 7.46-7.50 (m, 1H); MS, m/e 529 20 (M+l)+. 29M472-1 -681- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

EXAMPLES

Example numbers 13-54 and 56-66 are prepared using simitar procedures described for examples 5-8. The example number, compound identification, and NMR/MS details are shown below:

Ex. Rl R1 R31 R4 NMIVMS 13 Ph H H Me Et 1H NMR (DMSO-tf#) δ 1.12-1.16 (m, 3H), 1.2O-I.28(m.6H), 3.70-3.90 (m, 2H), 4,00-4.08 (m, 3H), 4.18-4.45 (m, 2H), 5.52-5.58 (m. 1H), 5.85-5.98 (m, tH). 6.00-6.20 (m. 2H), 7.16-7.23 (m. 3H). 7.37-7.40 (m, 2H). 7.54-7.60 (m, IH), 11.54(s.lH); MS, m/e516.1 (M+l)+ 14 1-Napth H H Me Bn 1H NMR (DMSO-de) 61.18-1.30 (m, 6H), 3.78-4.10 (m, 3H), 4.38-4.49 (m,2H), 4.99-5.11 (m, 2H), 5.28-5.40 (m, 1H), 5.85-6.10 (m, 2H), 6.30-6.41 (m, 1H), 7.28-7.32 (m, 5H), 7.41-7.60 (m, 5 H), 7.73- 7.76(m, IH), 7.94-8.1 l(m, IH), 8.13-8.15(m, 1H), 11.50(s.lH); MS, m/e 628.4 (M+l)+ 15 Ph H H H Me 1H NMR (DMSO-<4) δ 1.22 (d, J“22.4 Hz, 3H), 3.59(s, 3H), 3.63-3.69 (m, 2H), 3.74-3.8(m, 1H), 4.02(4 J-l 1.2Hz, 1H), 4.23-4.28(m, IH), 4.40-4.43 (m, IH), 5.57-5.60 (m, IH), 5.89(d, J-6.8 Hz, IH), 6.00-6.06(m, 2H), 7.15-7.23 (m, 3H), 7.35-7.39 (m, 2H),7.52(d, J-8 Hz, IH), 11,52(3,1H); MS, m/e 487.97 (M+l)+ 16 2,4-Cl- Ph H H Me Me IH NMR (DMSO-cfe) 5 1.22-1.28 (m, 6H), 3.57-3.60 (m, 3H), 3.84-3.92 (m,2H),4.003.04 (m, IH),4.31-4.44 (m,2H),5.54-5.61 (m, IH), 5.85-6.10(m,2H), 6.32-6.43 (m, IH),7.44-7,54 (m,3H), 7.72-7.75 (m, 1H), 11.54 (s. 1H); MS, m/e 570.2 (M+l)+ 17 1-Napth H H Me Me IH NMR (DMSO-rft) δ 1.15-1.27 (m, 6H), 3.51-3.55 (d, 3H), 3.85-3.96(m, 2H), 4.003.10(m, IH), 4.303.46(m,2H), 5.31-5.39(m, IH), 5.89-6.05(m,2H). 6.22-6.34 (m, IH), 7.44-7.60(m,5H),7.73-7.77 (m, IH), 7.93-7.96 (m. IH), 8.12-8.14 (m, 1H), 11.50(3.1H); MS, m/e 552.1 (M+l)+ 18 Ph * H * Me 1H NMR (DMSO-tf») 5 1.19(d,J*32.8Hz,3H), 1.69-1.84 (m,3H), 1.99-2.04 (m, IH), 3.16-3.21 (m,2H), 3.58 (s,3H),3.68-3.8(m, IH), 4.00 (m, 1H), 4.01 -4.13 (m. IH), 432335 (m, 1 H), 45 (d, J » 11.2 Hz, IH) 5.54 (d, J - 8.0 Hz, IH), 5.86 (s, IH), 5.6 (d, J -19.6 Hz, IH), 7.15-7.2 (m, 3H), 7.34 (t, J = 8.0 Hz, 2H), 7.51 (d, J - 8,0 Hz, IH), 11,38 (s, IH); MS, m/e527.93(M+l)+ 19 Ph H H Me n-Bu IH NMR (DMSO-40 δ 0.80-0.90 (m, 3H), 1.20-1.35 (m, 8H), 1.48-155 (m, 2H). 3.78-3.88 (m, 2H), 3.953.08 (m, 3H), 4.223.45 (m, 2H), 555-557(t, IH), 5.85-6.18 (m, 3H), 7.14-7.23 (m.3H),7.35-7.40 (m, 2H), 7.51-7.60 (d, 1H), 11.50 (s. IH); MS, m/e 544.2 (M+l)+ 20 Ph H H Me Bn 1H NMR (DMSO-d6) δ 130-1.30 (m, 6H), 3.723.05 (m, 3H), 4.23- 437 (m, 1HX4.323.45 (m, IH),5,07-5.10{ζ 2H), 552-5.56(t, IH), 2983472-1 -682- PCT/US2008/058183 WO 2008/121634 ήΛ^„ΛΤΤ,

Docket No. 60137.0034WOUI

Ex. R* R1 R3a IF" R4 NMR/MS 5.86-6.10(m, 2H),6.l3-6.2l(m,lH), 7.15-7,21 (m, 3H), 7,29-7.40 (m, 7H), 7,51-7.56 (d, 1H), 11,50 (s.lH); MS, m/c 578.2 (M+l)+ 21 4-F-Ph H H Me Me IH NMR (DMSO-rfe) 5 1.28-1.34 (tn, 6H), 3.65(d, J= 4 Hz, 3H), 3.85-3.96 (m, 2H), 4.06-4.12 (m, 1H), 4.30-4.34 (m,l H), 4.40-4,47 (m, 1H), 5.62-5.67 (m, 1H), 5.94-6.01(m, IH), 6,09 (d, >18.8 Hz, 1H), 6.17- 6.26(m, IH).7.27-7.33(m,4H),7.62(d. J = 7.6Hz, !H), 11.61 (s, IH) ; MS, m/e 519.94(M+1)+ 22 4-Cl-Ph H H Me Me 1H NMR (DMSO-tW 8 1.22-1.28 (m, 6H), 3.58 (d. 2H), 3.70- 3.95(m,2H), 3.95-4,08 (m,l H), 4.23-4.45 (m. 2H), 5,55-5,61 (t , 1H), 5.85-6.10 (m, 2H), 6.15-6.23{m,1 H). 7.20-7.26 (tn, 2H), 7.43-7,46 (m, 2H), 7.54-7.57 (d, 1H), 11.50 (s. 1H); MS, m/c 536,1 (M+l)+ 23 3,4-Cl- Ph H H Me Me IH NMR (DMSO-tZs) δ 1.13 (m, 6H), 3.49 (s, 3H), 3.61-3.85 (m, 2H), 3.90-3.93 (m, 1H), 4.164.22 (m, IH), 4.27-4.31 (m, IH), 5.47-5.52 (m, IH), 5.82 (d, J= 11.6 Hz, IH), 5.93(d, J = 19.2 Hz, IH), 6.15-6.25 (m, 1H), 7,13 (t, J = 9.6 Hz, 1H), 7.43 (d, J = 12Hz, 2H), 7.57 (d, J ° 6.0Hz, IH), 11.43(3, IH); MS, tn/e 569.85 (M+l)+ 24 Ph H H Me 2-Bu 1H NMR (DMSO-t/ί) δ 0.83 (d, J « 6.8 Hz, 6H), 1.20-1.26 (m, 6H). 1.79-1.86 (m, 1H), 3.73-3.90 (m, 4H), 4.01 (t, J = 11.2 Hz, 1H), 4.21 -4.28 (m, 1H), 4.33-4.42 (m, 1H), 5,54 (t, J « 7.6 Hz, 1H), 5.85-5.92 (m, 1H), 5.99-6.13 (m, 2H), 7.19 (t, J - 8 Hz, 3H), 7.36 (t, J - 7.6 Hz, 2H), 7.53 (d, J ° 7 6 Hz, 1H), 11.52 (s, 1H); MS, m/e 544.00 (M+l )+ 25 Ph H H Me i-Pr IH NMR (DMSO-4)6 1.13-1.28 (m, I2H), 3.74-3.81 (m,2H),3.95-4.08 (m.lH),4.20-4,45(m,2H),4.B3-4.87 (m. IH), 5.52-5.58 (m, 1H), 5.84-6.15 (m, 3H), 7.17-7,23 (m, 3H), 7.35-7.39 (m,2H), 7.54-7.57 (m, IH), 11.50 (s.lH); MS, m/e 530.2 (M+l)+ 26 4-MeO- Ph H H Me n-Bu 1HNMR (400MHz, DMSO-rfs): δ «0.78-0.82 (m, 3H), 1.29-1.47 (m, 8H), 1.49-1.54 (m,2H), 3.66-3.87 (m, 5H), 3.96-4.02 (m, 3H),4.21-4.39 (m,2H), 5.57 (t, J- 12.0Hz, IH). 5.84-6.05 (m, 3H),6.90 (dd, J1 “8.0Hz, J2=4.0Hz, 2H), 7.09-7.14 (dd, J > 16.0Hz, J2=4.0Hz, 2H), 7.55 (d, J =8.0Hz, 1H), 11.48-11.62 (s, 1H) 27 4-F-Ph H H Me Et IH NMR (DMSO-t/j) δ 1.12-1.28 (m, 9H), 3.72-3.94(m,2H) ,3.98-4.10 (m,3H),4.21-4.42(m,2H), 5.55-5.61 (t, IH), 5,85-6.20 (m, 3H), 7.18- 7.25 (m,4H), 7.55-7.58 (d. IH). 11.50(s.lH);MS, m/e 533.90 (M+1)+ 28 4-F-Ph H H Me i-Pr IHNMR(DMSO-rfs)5 1.13-1.30 (m, 12H),3.74-3.85(m,2H),3.98- 4.06(m,lH),4.234.4l(m,2H), 4.834.87 (m, IH),5.55-5.61 (t, IH), 5.85-6.12 (m,3H),7.18-7.24 (m,4H),7.55-7.58(d, IH), 11.50(s.lH); MS,m/e 547.91 (M+l)+ 29 4-F-Ph H H Me Bn lHNMR(DMSt>/i)5 1.10-1.23 (m,6H), 3.65-3,89(m,3H) ,4.104.30 (m,2H), 4.96-5.OO(rn^H), 5.46-5.50 (t, 1H), 5.75-5.96 (m, 2H), 6.04-6,12(m,IH), 7.05-7.11 (m,4H), 7.20-7.24 (d, 5H), 7.42-7.45(d,l H), 11.50 (s. 1H); MS, m/e 595.94 (M+l)+ 30 4-MeO- Ph H H Me i-Pr I HNMR (400MHz, DMSCW δ°1.15-1.27 (m, 12H), 3.71-3.89 (m, 5H), 3.984.02(m, IH),4.224.25 (m, 1H),4.334.39(m, IH),4.84-4.87(m, IH), 5.57 (t,> 12.0Hz, IH),5.91-6.03(m,3H),6.90(d,> 8.0Hz, 2H), 7.09-7.14 (m, 2H), 7.55 (d, > 8.0Hz, 1H), 11.51 (s, 1H) 31 2-Cl-Ph H H Me Bn 1H NMR (DMSO-di) 6 1.23 (m, 6 H), 3.934.00 (m, 3 H), 4.274.40 (m. 2H), 5.0(1, J“ 7,2 Hz, 2 H), 5.53 (m ,1 H), 5.80-6.0(m, 2 H), 6 J0(m, 1H), 7.15 (d, J» 2.4 Hz, 1 H), 7.27 (m, 6 H), 7.51 (m, 3 H), 11,5 (s, 1 H); MS, m/e 579.87{M+1)+ /596.78 (M+18)+ 2983472-1 -683- WO 2008/121634 . ,Λ1__ ....-,.T1 uocket No. 60137.0034WOU1 PCT/US2008/058183

Ex. R1 "r5- R3* Rib R^ NMR/MS 32 2,4-Cl- Ph H H Me n-Bu 1H NMR (DMSO-de) 5=0.82 (in, 3 H), 1.23 (m, 8 H), 1.47 (m, 2 H), 3.86 (m, 2 H), 3.84 (m, 3 H),4.274,43 (m, 2H), 5.5 (m . 1 H), 6.02 (in ,2 H), 6.35(m, 1H), 7.44 (m, 3 H), 7.77 (m, 1 Η), 11.5 (s, 1 H); MS, m/e 611.87((4+1 )+ 33 4-Me- Ph H H Me i-Pr 1H NMR (DMSO-oy 5 1.14-1.27 (m, 1211), 2.17-236 (m,3H), 3.73-3.82 (m, IH), 3.994.02 (m, IH), 4334.26 (m, 1H), 4.37-4.40 (m, IH), 4.82-4.88 (m, 1H), 5.52-5.58 (m, IH), 5.85-6.07 (m, 3H), 7.01-7,20 (m, 4H), 7.55 (d, J - 16Hz, 1H), 11,51 (s, 1H); MS, m/e 543.98 (M+l>+; 1108.86 (2M+23)+ 34 4-F-Ph H H Me n-Bu IH NMR (DMSO-ds) 5 0.82-0.89 (m,3H), 1.20-1.31 (m, 8H). 1.48-1.53 (m,2H), 3.77-3.90 (m^H) ,3.95-4.10 (m,3H), 4,21-4.45(m,2H), 5.56-5.61 (t, 1H), 5.83-6.20 (m, 3H), 7.18-7.25 (m,4H), 7.55-7.58 (d, IH), 11.50 (s.lH); MS, m/e 584.1 (M+23)+ 35 3,4- diCl-Ph H H Me Et lHNMR(DMSO-rfe)51.12-1.31 (m, 9H), 3.77-3,92 (m3H), 3.95-4,08 (m,3H),4.214.45(m3H),5.56-5,62 (t, IH), 5.80-6,11 (m,2H),6.18-6.33(m,lH), 7.18-7.25 (m,IH), 7.49-7.56{d, 2H), 7,62-7.67{m,lH), 11.50 (s. 1H); MS, m/e 606.1 (M+23)+ 36 2-CI-Ph H H Me i-Pr 1HNMR (400MHz, DMSO-rf»): δ “ 1.12-1.16 (m, 6H), 1.21 -1.27 (m, 6H), 3.79-3.85 (m, 2H>, 4,004.07 (m, IH),4384,32 (m, 1H),4.38-4.43(m, IH),4.83-4.87(m, IH),5,56(dd, J1-16.0HZ, J2”8.011z, 111), 5.85-6.12 (m, 2H), 6.20-6.33 (m. 1H), 7.19-7.22 (m, 1H), 7.33 (t, J= 16.0Hz, IH), 7.48-7.55 (m, 3H), 11.55 (s, IH) 37 4-MeO- Ph H H Me Bn lHNMR(400MHz, DMSCM): 6-1.19-1.26 (m, 6H), 3.69-3.70 (s, 3H), 3,87 (m, 2H), 3.99 (m, 1H), 4.20-4.21 (m, 1H), 4.35 (m, 1H), 5.07-5.09 (m, 2H), 5.54 (ζ J - 16.0Hz, 111), 5.85-5.92 (m, IH), 6.04-6.10 (m, 2H), 6.86 (d, J- 8.0Hz, 2H), 7.09 (dd, J1-16.0HZ, J2=4.0Hz, 2H), 7.30-7.34 (m,5H), 7.53 (s, IH), 11.52 (s, IH) 38 Ph H H Me n-Pen JH NMR (DMSO-d») 6 0.79-0.81 (m, 3H), 1.17-1.23 (m, 10H), 3.74-3.81 (m, 2H), 3.94-3.96 (m, 3H), 4.19-4,36 (m, 2H), 5.49-5.54 (m, IH), 5.87-6.08 (m^H), 7.14-7.33 (m, 3H), 7.31-7.35 (m, 2H), 7.51 (d, J - 8Hz, 1H), 11.51 (s, 1H); MS, m/e 557.9 (M+l)+; 1136.88 (2M+23)+ 39 4-Cl-Ph H H Me i-Pr IH NMR (DMSO-rf*) δ 1.04-1.19 (m, 12H), 3.76-3.80 (m, 2H), 3.98-4.08 (m, IH), 4.42-4.42 (m,2H),4.824.85 (m, IH), 5.55-5.60(m, 1H), 5.80-6.20 (m,3H),730-7.2 5(m, 2H), 7.43 (d, J - 8.8Hz, 1H), 7.54 (d, J - 8Hz, IH), 11.51 (s, IH); MS, m/e 563.88 (M+l)+; 1148.73 (2M+23)+ 40 4-Cl-Ph H H Me n-Bu IH NMR (DMSO-A) 5 0,85 (t, J - 7.2 Hz, 3H), 1.22-133 (m, 8H),1.45-1.53 (m, 2H), 3.80-3.87 (m, 2H), 3.96-4.04 (m, 3H), 4.24-4.27 (m, IH),4.35-4.39 (m, IH), 5.56-5.61 {m, IH), 5.82-6.11 (m, 2H), 6.15-6.18 (m, 1H), 7.20-7.56 (m, 4H), 7.51-7.57 (m.lH), 11.54 (3, 1H); MS, m/e577.95(M+l)+ 41 4-Cl-Ph H H Me Et 1H NMR (DMSO-4) 6 1.14 (t, J = 7.0Hz, 3H), 1.20-1.28 (ro, 6H),3.77-3.88 (m, 2H), 3.994.07 (m, 3H), 4.244.28 (m, 1H), 4.34-4.43 (m, IH), 5.56-5.61 (m, IH), 5.86-6.13 <m, 2H), 6.15-6.24 (m, 1H), 730-736 (m, 2H), 7.44 (d, J = 7,6Hz, 2H), 7.55 (d, J ° 7.6Hz, IH), 11.55(8, IH); MS, m/e549.11(M+1)+ 42 4-Me- Ph H H Me n-Bu IH NMR (DMSO-4) 8 0.79-0.83 (m,3H), 1.17-1.28 (m, 8H), 1.45- 1.47 (m, 2H). 232 (d, J « 2.8Hz, 1H), 3.70-3.90 (m, 2H), 3.95-3.98 2983472-1 -684- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Ex. R* "R5" "r15- -pr- R4 NMR/MS (m, 3H), 4.10-4.40 (m, 2H), 5.51 (t, IH), 5,80-5.90 (m, IH), 5.95-6.05 (m,2H),7.02-7.06(m,2H),7.51 (t, J “4.2Hz, 4H), 7.51 (d, IH), 11.51 (s, 1H); MS, m/e 557.99(M+1 1136.84(2 M+23>+ 43 4-Me- Phe H H Me Bn 1H NMR (DMSO-rfs) 5 1.16-1.24 (m, 6H), 2.22 (s, 3H), 3.65-4.03 (m,3H), 4.11-4.38 (m, 2H), 5.04-5.05 (m, 2H), 5.48-5.50 (m, 1H), 5.77-5.87 (mJ H),5.90-6.11 (m, 2H), 6.98-7.10 (m, 4H), 7.28-7.32 (in, 5H), 7.50 (t ,1H), 11.48 (s. 1H); MS, m/e 592.00 (M+l )+. 44 Ph H H Et Me 1H NMR (DMSO-44) δ 0.70-0.80 (m, 3H), 1.11 -1.26 (m, 3H), 1.42-1.61 (m, 2H), 3.50-3.54 (m, 3H), 3.58-3.80 (m, 2H), 3.91-4.02 (m, IH),4.12-4.38 (m, 2H), 5.47-5.52 (m,IH),5,90-6.03 (m,2H), 7.08-7.16 (m, 3H), 7.26-7.35 (m,2H),7.48 (1,1H),l 1.45 (s, IH); MS, m/e 515.95 (M+l)+; 1052.82 (2M+23)+ 45 Ph H H Me 4-F-Bn 'HNMR (400MHz, DMSO-rfs): δ 1.20-1.26 (m, 6H), 3.80-3.93 (m, 2H), 3.98 (s, 1H), 4.25-4.26 (m, 1H), 4.364.37 (m, 1H), 5.07 (s, 2H), 5.52-5.55 (m, 1H), 5.86-5.87(m, IH), 5.98-6.04 (m, IH),6.14-6.17 (m, 1H), 7.15-7.20 (m, 5H), 7.36 (dd. J - 20.0,8.0 Hz, 4H), 7.54 (s, 1H), 11.55 (s, IH) 46 4-Cl-Ph H H Me n-Bu 'HNMR (400MHz, DMSCMs): δ 1.21-1.28 (m,6H), 3.71-3.88 (m, IH), 3.91-3.98 (m, IH),4.004.01 (m, 1H), 4.234.27 (m, IH),4.35- 4.38(m, IH),5.08(d, 7 = 4.0Hz,2H),5.57(dd,7= 12.0,8,0Hz, IH), 5.91 (d, J - 8.0 Hz, 1H), 6,01 (d, J - 8.0 Hz, 1H), 6.22-6.24 (m, 1H), 7.17-7.23 (m, 2H), 7.31-7.40 (m,7H), 7.53 (s, IH), 11.50(s, IH) 47 Ph H H Me 3-Me-l- Bu 'H NMR (DMSO-ΐ/ί) δ 0.80-0.82 (m, 6H), 1.18-1.40 (m, 8H), 1.50-1.58 (m, IH), 3.71-3.82 (m, 3H), 3.97-3.4.01 (m, 3H), 4.214.40 (m, 2H), 5.30(1,7“ 8.6 Hz, tH),5.8l-6.10(m,3H), 7.15-7.20(m,3H), 7.32-7.36 (m, 2H), 7.48 (d,7“ 8.4 Hz, IH), 11.38 (a, 1H); MS, m/e 557.98 (M+l)+; 1136.88 (2M+23)4 48 3,4- diCl-Ph H H Me Bn Ή NMR (DMSO-ί/ί) δ 1,05-1.37 (m, 6H), 3.71-3.82 (m, 1H),3.87-4.02(m, 2H), 4.284.29(m, IH),4.36-4.38 (m, 1H),5.O4 (d,7-5.2Hz, 2H), 5.55-5.64 (m, IH),5.85-5.94 (m, IH),6.00-6.05 (m, IH), 6.29-6.40(m, IH),7.17-7.24 (m, IH), 7.30-7.41 (m, 5H), 7.45-7.58 (m,2H), 7.61 (d, 7" 4.0Hz, 1H), 11.53 (s, 1H); MS, m/«545.80(M+l )*; 49 Ph H H Me c-Hex 'H NMR (DMSO-dt) δ 1.18-1.41 (m, 12H), 1.59-1.67 (m,4H), 3.74-13.80(m, IH),3.964.02(m, IH),4.194.26(m, IH),4.314.39(m, IH),4.60(a, IH), 5.52(t,7“7.8 Hz, tH), 5.80-6.09(m, 3H), 7.15-7.20 (m, 3H), 7.32-7.36 (m, 2H), 7.52 (d, 7= 8 Hz, 1H), 11.50 (a, 1H); MS, m/e 569.98 (M+l)*; 592.14 (M+23)* 50 Ph H Me H n-Bu 1H NMR (DMSO-d») δ 0.76 (t, J - 7.2Hz, 3H), 1.10-1.22 (m, 8H), 1.38-1.43 (m, 2H), 3.72-3.75 (m, 2H), 3.87-3.93 (m, 3H), 4.144.21 (m, IH), 4.234.33 (m, IH), 5.46-5.54 (m, IH), 5.84-6.11 (m, 3H), 7.09-7.14(m,2H),7.27-7.32 (m,2H), 7.34-7.51 (m, IH), 11.47(8, IH); MS, m/e543.98(M+l)+ 51 Ph H Me H i-Pr 1H NMR (DMSQ-d») δ 1.39 (d, J - 7,2Hz, 6H), 1.19-1.29 (m, 6H), 3.65-3,75 (m, 2H), 3.954.05 (m, IH),4.204.22(m, IH),4,314.33 (m, IH),4.794.82 (m, IH), 5.48-5.57 (m, IH),5.84-5.91 (m, IH), 5.96-6.07 (m,2H),7.12-7.35 (m, 5H), 7.44-7.54 (m.lH), 11.49(5, IH); MS, m/e529.96(M+l)+ 52 Ph H Me H Bn Ή NMR (DMSO-Λ) δ 1.18-1.28 (m, 6H), 3.70-3.83 (m, 1H), 3.87-3.94 (m, IH),3.994.01 (m, IH),4.234.26 (m, tH), 4.334.37(m, 2983472-1 -685 - PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1

Ex. Rl RJ R3i R3b R4 NMR/MS 53 2-Cl-Ph H H Me n-Bu IH), 5.03-5.12 (rn, 2H), 5.51-5.59 (m, 1H), 5.87-5.90 (m, 1H), 5.95- 6.07 (m, 1H), 6.10-6.27 (m. 1H), 7.15-7.23 (m, 3H), 7.31-7.38 (m, 7H), 7,47-7.56 (in, 1H), 11.50 (s, 1H); MS, m/e577.99 (M+l)+ 'HNMR (400MHz, DMSO-74): δ 0.81-0.86 (m, 3H), 1.21-1.31 (m, 54 4-Br-Ph H H Me i-Pr 8H), 1.46-1.52 (m, 2H), 3.84-3.90 (m, 2H), 3.97-4.04 (m, 3H), 4.27- 4.41 (m,2H), 5.53-5.58 (m, IH), 5,82-5.95 (m, 1 Η), 5.96-6.10 (m, IH), 6.27-6.31 (m, IH), 7.19-7.22 (m, IH), 7,34 (dd,7*>8.0,4.0Hz, 1H), 7.47-7.55 (m, 3H), 11.55 (s, 1H) 'HNMR(400MHz, DMSO-rft): δ 1.10-1.14(m,6H), 120-127(m. 55 4-F-Ph H H Me c-Hex 6H), 3.74-3.81 (m,2H), 3.99-4.01 (m, IH), 4.214.25 (m, 1H),4.37- 4.38(m, IH), 4.81-4.85 (m, IH), 5.58 (dd, 7 - 8.0,4,0 Hz, IH), 5.82-5.95 (m, 1H), 5.96-6.09 (m, IH), 6.10-6.13 (m, 1H), 7,18 (dd, J = 12.0,8,0 Hz, 2H), 7.53-7.57 (m, 3H), 11.52 (s, 1H) 'H NMR (DMSO-40 5 1.20-1.44 (m, 12H), 1.60-1.71 (m,4H),3.75- 56 4-Br-Ph H H Me c-Hex 4.02 (m, 2H), 3.94-4.02 (m, IH), 4.194.26 (m, 2H), 4.594.61 (m, IH). 5.57 (t, J“8.4 Hz, IH), 5.85-6.06 (m, 3H), 7.17-7.23 (m, 4H), 7.54 (d,7= 8.4 Hz, IH), 11,50(8, IH); MS, m/e 587,92 (M+l)+ 'HNMR (400MHz, DMSO-7»): δ-1.18-1.46 (m, 12H), 1.6l-I.69(m, 57 Ph H H Et i-Pr 4H), 3.75-3.82 (m, 2H), 3.954.08 (in, 1H), 4.254,28 (m, 1H), 4.38 (s, 1H), 4.604.62 (m, 1H), 5.56-5.60 (m, 1H), 5.82-5.95 (m, 1H). 6.02-6.20 (m, 2H), 7.09-7.20 (m, 2H), 7.53-7.57 (m, 3H), 11.52 (s, 1H) MS, m/e 650.0 (M+3f 'HNMR (400MHz, DMSO-rf4): δ -0.75-0.82 (m, 3H), 1.12-1.26 (m, 58 Ph H H Et c-Hex 9H). 1.52-1.59 (m, 2H), 3.55-3.68 (m, IH), 3,72-3.85 (m, IH), 3.95-4.08 (m, IH), 4.184.28 (m, IH), 4.324.41 (m, IH), 4.834.86 (m, IH), 5.55 (m, 7,6Hz, IH), 5.99-6.04 (m, 2H), 6.05-6.10 (m, IH), 7.14-7.21 (m, 3H), 7.33-7.37 (m, 2H), 7,52-7.54 (m, IH), 11.53 (s, IH); MS,m/?566.07(M+23f 'HNMR (400MHz, DMSO-7e): δ 0.75-0,88 (m, 3H), 1.26-1.46 (m, 59 4-F-Ph H H Et c-Hex 9H), 1.52-1.69 (m, 6H), 3.60-3.63 (m, IH), 3.72-3.90 (m, IH), 4.02-4.03 (m, IH), 4.244.27 (m, IH), 4.374.38 (m, IH), 4.634.65 (m, IH), 5.55 (dd,7=8.0¾ 4.4Hz, IH), 5.80-5.95 (tn, IH), 6.00-6.07 (m, 2H), 7.15-7.22 (m, 3H), 7.34-7.38 (m, 2H), 7.54 (d, 7 =8.0Hz, IH), 11.55 (s, IH); MS, m/e 584.01 (M+l)+ ,606.17 (M+23)+ 'H NMR (DMSO-A) δ 0.75-0.84 (m, 3H), 124 (d, 7=22.8Hz, 3H), 60 Ph H H Me F-CHr 1.29-1.47 (m, 6H), 1.51-1.70 (m, 6H\ 3.59-3.66 (m, 1H), 3.77-3.84 (m, IH), 3.984.04 (m, IH), 421427(m, IH),4.344.41 (m, IH), 4.604.65(m, 1H),5.56-5.60 (m, IH), 5.84-5.90 (m, IH),6.00-6.08 (m, 2H), 720-724 (m, 4H), 7.56{dt 7“ 8,0Hz, IH), 11.49 <s, IH); MS, ι»Λ602.00(Μ+1)* 'H NMR (DMSO-A) 61.18-1.25(m, 6H), 3.71-3.89 (m, 2H), 3.92-3.99 CHr (m, IH),4.19427 (m,4H),4.484.61 (m,2H), 3,94-3.98 (m,2H), 4.11423 (m,4H),5.47-5.52 (m, IH), 6.01-6.11 (m, 1H), 5.90-6.14 (m, 2H), 7.1 5-721 (m, 3H), 7.32-7.36 (m, 2H), 7.46-7.57 (m, 1H), 11,49 (j,lH); MS, m4r 533.86 (M+l)+ 2983472-1 -686- WO 2008/121634 τ

Docket No, 60137.0034WOU1 PCT/US2008/058183

Ex. R1 R2 R3’ R3b NMR/MS 61 Ph H H Me f2ch- CHr Ή NMR (DMSO-di) S 1.17-1.24 (in, 6H), 3.67-3.81 (m, 1H), 3.89- 3.98 (m, 211),4.21-4,36 (m, 4H), 3,48-5.53 (m, 1H) , 5,82-6,05 (m. 2H), 6.18-6.22 (m, 2H), 7.15-7.20 (m, 3H), 7.32-7.36 (m , 2H), 7,51 (s, 1 Η), 11 50 (s, 1H); MS, m/e 551.92 (M+l )*; 62 Ph H H Me (CF3)2- CH- Ή NMR (DMS0-4J 5 1.13-1.29 (m, 6H), 3,67-3.81 (m, IH), 3.94- 4.32 (m, 4H), 5.47 (t, J - 8 Hz IH). 5.82-6.01 (m, 2H), 6.33-6.36 (m, IH), 6.70-6.78 (m, 1H), 7.09-7.15 (m, 3H). 7.28-7.32 (m , 2H), 7.43-7.46 (m, 1H), 11.44 (s, IH); MS, m/e 637,90 (M+l)+ 63 Ph H H Me (CH2F)2 -CH- 'H NMR (DMSO^s) δ 1.20-1.29 (m, 6H), 3.70-3.90 (m, IH), 3.91-4.12 (m, 2H), 4.204.33 (m, IH), 4.35-4.48 (m, IH), 4.524,55 (m, 2H) , 4.634.67 (m, 2H), 5.20-5.35 (m, IH), 5.56(1, J - 8.4 Hz, IH), 5.80-5.95 (m, IH), 5.95-6.10 (m, IH), 6.18-6.21 (m, IH), 7.18-7.23 (m, 3H), 7.35-7.39 (m , 2H), 7.54 (s, IH),11.55 (s, IH) ; MS, m/e 565.98 (M+l/ 64 Ph H H Me c-Pr- ch2- Ή NMR (DMSO-4) δ 0.20-0.24(m, 2H). O.47-O.48(m, 2H), 0.76-0.84(m, 3H), 1,03-1,05(m, IH), 1.23(dd, > 22.4 6,8 Hz 3H), 1.55-1,60(m, 2H), 3.61 -3.68(m, 1H), 3. 81-3.89 (m, 3H), 3.984.03(m, 1H), 4.234.29(m, IH), 4.354.41<m, IH), 5.56-6.00(m, IH) , 5.88-5.91(m, IH), 6.04-6. IO(m, 2H), 7.20-7.24(m, 4H), 7.55 (d, 7- 2.6 Hi IH),11.53 (a, IH); MS, m/e573.17 (M+l)* 65 Ph . j T>3b . H H Et c-Pen 'H NMR (DMSO-40 δ 0.75-0.83 (m, 3H), 1,20-1.28 (m, 3H), 1.49-1.63 (m, 8H), 1.76-1.80 (m, 2H), 3.58-3.60 (m, IH), 3.70-3.82 (m, IH), 3.984.05 (m, IH), 4.244.26 (m, IH) , 4.374.42 (m, IH), 5.03 (s, IH), 5.54-5.57 (m, IH), 5.90-6,00 (m,)H), 6.02-6.07 (m,2H), 7.15- 7.22 (m, 3H), 7,35-7.39 (m, 2H) 7.55 (d, J « 8.0 Hz, IH), 11.55 (s, IH); MS, m/e 570.03 (M+l/ *R^ and R3b together are -(CH2)j- as derived from L-proline

The purification procedure by Prep-HPLC:

Crude products were dissolved in methanol. Injection volumes of these 5 solutions were 5 mL.

The preparative HPLC system including 2 sets of Gilson 306 pumps, a Gilson 156 UV/Vis detector, a Gilson 215 injector &amp; fraction collector, with Unipoint control software. A Ymc 25x30x2 mm column was used. The mobile phase was HPLC grade water (A), and HPLC grade acetonitrile (B). Fractions 10 were collected into 100* 15mm glass tubes. HPLC gradient is shown in Table 1. Once the gradient was selected, acetonitrile solution was injected into HPLC system, and then fractions collected 2983472-] -687- WO2#0%1o»o.60.37.0034WOU1 PCT/US2008/058183 according to UV peaks. After the separation, each glass tubes were run MS test to collect the desired compounds. The fractions with target MS were combined in a well-weighted flask. Most of acetonitrile was removed under reduce pressure and the remaining solution was freeze-dried to give desired compound.

Table 1:

Preparative HPLC gradient Time (min) Flow rate (mL/min) %A %B 0 15 90 10 30 15 60 40

Preparation of Example 66 10 Scheme N 7—Cl

BzO p DEAO.PPti, BzO' F THF, ft overnight

BzO" p

NHj/THF nQh-nh, ΘΟ °C, overnight

BzO N 7— NHj

-N^N

BzO f r.t, overnight HO p

Xc QHHaN

EljWDCM HO p

Preparation of compound (b) 2983472-1 -688 - WO 2008/121634 ,

Docket No. 60137.0034WOU1 PCT/US2008/058183

To a solution of compound a (1 g, 2.69 mmol) in anhydrous THF (30 mL) was added dropwise 1 M solution of LiAl(OBu-/)3H in THF (2.69 mL, 2.69 mmol) at -20 °C. The reaction mixture was stirred for 2-3 h at the same temperature. EtOAc (100 mL) was added followed by saturated NH4CI solution 5 (10 mL) and reaction mixture was slowly brought to room temperature. Reaction mixture was extracted with EtOAc and washed with IN HC1 and water. Combined organic phase was evaporated to give 0.8 g of crude compound b as transparent oil, which was used directly for next reaction.

Preparation of compound (d) 10 To a solution of compound b (0.8 g, 2.1 mmol), compound c (0.45 g, 2.5 mmol) and PI13P (0.56 g, 2.1 mmol) in anhydrous THF (20 mL) under nitrogen atmosphere was added DEAD (1.8 mL). The reaction mixture was stirred at room temperature overnight. The reaction solution was concentrated under reduce pressure. The residue was separated by preparative layer chromatography 15 (hexanes:EtOAc = 3:1) to give crude compound d (0.8 g). The crude compound d was used to the next step without further purification.

Preparation of compound (e)

Compound d (0.8 g, 1.57 mmol) was dissolved in THF (2 mL) and THF saturated with ammonia (5 mL) was then added to this solution. The reaction 20 mixture was heated to 90 °C overnight. After 18 hours, the solution was cooled to room temperature by ice water, then the solvent was removed under reduced pressure and the residue was purified by column to give compound e (0.75 g) for the next step.

Preparation of compound (f) 25 Compound e (0.5 g, 1.01 mmol) was dissolved in methanol (2 mL) and methanol was saturated with ammonia (5 mL) was then added to this solution. The reaction mixture was stirred at room temperature overnight. After 18 hours, the solvent was removed under reduced pressure and the residue was purified by column to give crude compound f (0.15 g) for the next step. 30 Preparation of compound (i) A solution of triethylamine (1.07 g, 10.6 mmol) in anhydrous di chloromethane (15 mL) was added dropwise to a solution of compound g (1.16 2983472-1 -689- PCT/US2008/058183 WO 2008/121634

Docket No. 60137.0034WOU1 g, 5.3 mmol) and compound h (1.31 g, 5.3 mmol) in dichloromethane (10 mL) with vigorous stirring at -78 °C over a period of 2 hours. After completion of addition, the reaction temperature was allowed to warm to room temperature gradually and stirred over night. Then the solvent was removed under vacuum 5 and anhydrous ether 20 mL was added and the precipitated salt was filtered and the precipitate was washed with ether. The combined organic phase was concentrated to give the colorless oil of compound i (1.0 g).

Preparation of Compound 66 10 To a solution of compound j (0.1 g, 0.35 mmol) dissolved in 10 mL of anhydrous THF, stirred and added 0.4g NMI till the solution became clear, added compound i (0.8 g, 2.89 mmol) in 10 mL THF dropwise, stirred at r.t. overnight. Compound purity and identification was confirmed by LCMS. The solvent was evaporated and purified by Prep-HPLC to afford 66. (25 mg, Yield: 15 13.6%). 'H NMR (DMSO-i&amp;) δ 1.08 (d, J= 22.8 Hz, 3H), 1.17-1.24 (m, 3H), 3.50-3.52 (m, 3H), 3.78-3.83 (m, 1H), 4.10-4.13 (m, 1H), 4.24-4.44 (m, 2H), 5.85-5.92 (m, 1H), 6.01-6.11 (m,lH), 6.2.-6.27 (m, 1H), 7.08-7.19 (m, 4H), 7.31-7.38 (m, 3H), 8.15 (s, 1H), 8.26 (s, 1H); MS, m/c 525 (M+l)+. 20 Example numbers 67-74, identified below, were prepared using similar procedures disclosed for Example 66, above.

Example R" - NMR/MS 67 OH nh2 kHNMR (DMSO-£/6) δ 1.06-1.13 (m, 3H), 1.20-1.24 (m, 3H), 3.27-3.33(m, 3H), 3.56 (s, 1H), 3.82-3.88 (m, 1H), 4.07-4.13 (m, 1H), 4.25-4.40 (m, 2H), 5.85-5.87 (m, 1H), 5.98-6.09 (m, 2H), 6.59 (s, 32H), 7.14-7.37 (m, 3H), 7.35-7.37 (m, 2H), 7.79 (d, >7.2 Hz, 1H), 10.69 (s, 1H); MS, m/e 541 (M+l)+; 68 nh2 nh2 ‘H NMR (DMSO-rfe) δ 1.07 (d, >22.8 Hz, 3H), 1.19 (d, 7=7.2 Hz, 3H), 3.51 (s, 3H), 3.62 (s, 1H), 2983472-1 -690- PCT/US2008/058183 WO 2008/121634 τ „

Docket No. 60137.0034WOU1

Example R11 NMR/MS 3.75-3.81 (m, 1H), 4.05-4.11 (m, 1H), 4.27-4.42 (m, 2H), 5.79-5.83 (m, 1H), 5.92 (», 2H), 6.00-6.09 (m, 2H), 6.75 (s, 2H), 7.08-7.17 (m, 3H), 7.31-7.35 (m, 2H), 7.78 (s, 1H); MS, m/e 540 (M+l)+; 69 nh2 c-Pentyl-NH- 'HNMR (D.MSO-/6) δ 1.05 (d, /=22.8 Hz, 3H), 1.09-1.19 (m,3H), 1.48 (s, 4H), 1.66 (s, 1H), 1.86 (s, 1H),3.54 (d,/=14 Hz, 3H), 3.65 (s, 1H), 4.25-4.43 (m, 4H), 5.71-5.82 (m, 1H), 5.94-6.04 (m, 4H), 7.11-7.24 (m, 3H), 7.26-7.34 (m, 2H), 7.77(d,/=3.6 Hz, 1H); MS, m/e 608(M+l)+ 70 nh2 Ή NMR (DMSO-4s) δ 1.07 (d, /=22.4 Hz, 3H), 2.35-2.38 (m, 2H), 3.54 (d, /=9.2 Hz, 3H), 3.59-3.62 (m, 2H), 3,65 (s, 1H), 3.75-3.82 (m, 1H), 4.01-4.13 (m, 2H), 4.22-4.40 (m, 6H), 5.75-5.85 (m, 1H), 6.00-6.07 (m, 4H), 7.15-7.21 (m, 3H), 7.32-7.35 (m, 2H), 7.79 (d,/=4.0 Hz, 1H); MS, m/e 580 (M+l)+ 71 nh2 Et2N- Ή NMR (DMSO-afe) δ 1.06-1.28 (m, 12H), 3.55 (d, /=4.8 Hz, 3H), 3.79-3.87 (m, 4H), 4.07-4.12 (m, 2H), 4.29-4.42 (m, 3H), 5.75-5.82 (m, 1H), 5.94 (s, 2H), 6.04-6.10 (m, 2H), 7.14-7.22 (m, 3H), 7.31-7.37 (m, 2H), 7.82 (d,/=4.4 Hz, 1H); MS, m/e 596 (M+l)+ 72 nh2 n-Propyl-NH- Ή NMR (DMSO-rfe) δ 0.84 (t, /=7.2 Hz, 3H), 1.01- 1.01 (m, 3H), 1.09-1.12 (m, 3H), 1.51-1.56 (m, 2H), 3.48 (d, /=15.2 Hz, 3H), 3.79-3.82 (m, 1H), 4.04- 4.05 (m, 1H), 4.27-4.38 (m, 3H), 5.72-5.79 (m, 1H), 5.98-6.04 (m, 4H), 7.13-7.20 (m, 3H), 726-7.32 (tn, 2H), 7.76 (d, /=5.2 Hz, 1H); MS, m/e 582 (M+l)+ . 73 nh2 c-Butyl-NH- ‘H NMR (DMSO-/6) δ 1.02-1.08 (m, 3H), 1.18 (d, /=4.8 Hz, 3H), 1.44-1.61 (m, 2H) , 2.02-2.17 (m, 4H), 3.51 (d, /=10.8 Hz, 3H), 3.78-3.83 (m, 1H), 4.03-4.06 (m, 1H), 4.27-4.38 (m, 2H), 4.53-4.62 (m, 1H), 5.68-5.79 (m, 1H)> 5.95-6.04 (m, 4H), 7.11- 7.18 (m, 3H), 7.29-7.35 (m, 2H), 7.51-7.58 (m, 1H), 7.78 (d, /=5.2 Hz, 1H); MS, m/e 594 (M+l)+ 2983472-1 -691- WO 2008/121634

Docket No. 60137.0034WOU1 PCT/US2008/058183

Example ΊΕ1 Rl(J ............ NMR/MS 74 nh2 O Μθ-Ι^_ ‘H NMR (DMSO-i/e) δ 0.97-1.20 (m, 6H), 2.18 (s, 3H), 2.19 (s, 4H), 3.43-3.47(m, 3H), 3.75 (s, 1H), 4,01-4.06 (m, 4 H), 4.22-4.35 (m, 3H), 5.69-5.75 (m, 1H), 5.98-6.05 (m, 3H), 7.09-7.15 (m, 3H), 7.25- 7,29 (m, 2H), 7.77 (d, >3.6 Hz, 1H); MS, m/e 623 (M+l)+

Example numbers 75-80 are prepared using similar procedures disclosed for Example 66, above.

Example Γ£Π R,u 75 H n-propyl-NH- 76 H c-Butyl-NH- 77 H c-Pentyl-NH- 78 H -Nd 79 H O 80 H -O EXAMPLE 81

Certain exemplified compounds were obtained as mixture of diastereomers because of the chirality at phosphorous. The diastereomers were 2983472-1 -692-

WO 2008/121634 T

Docket No. 60137,0034WOU1 PCT/US2008/058183 separated on a Chiralpak-AS-H (2 X 25 cm) column under Supercritical Fluid

Chromatography (SFC) conditions using 20% methanol in carbon dioxide as solvent. The absolute stereochemistry of the P-chiral center of the diastereromers were not determined. However, chromatographic resolution of 5 these two diastereomers provides for isomers that are characterized as fast eluting and slow eluting isomers. Some examples are shown below.

Compound EC90 (uM) Example 15 (Diastereomeric mixture) 0.86 Fast Moving isomer of Example 15 1.35 Slow Moving isomer of Example 15 0.26 Example 39 (Diastereomeric mixture) 0.47 Fast Moving isomer of Example 39 0.78 Slow Moving isomer of Example 39 0.02 Example 49 (Diastereomeric mixture) 0.126 Fast Moving isomer of Example 49 0.03 Slow Moving isomer of Example 49 5.78 EXAMPLE 82 HCV replicon assay. HCV replicon RNA-containing Huh7 cells 10 (clone A cells; Apath, LLC, St. Louis, Mo.) were kept at exponential growth in Dulbecco's modified Eagle's medium (high glucose) containing 10% fetal bovine serum, 4 mM L-glutamine and 1 mM sodium pyruvate, 1 x nonessential amino acids, and G418 (1,000 pg/ml). Antiviral assays were performed in the same medium without G418. Cells were seeded in a 96-well plate at 1,500 cells per 15 well, and test compounds were added immediately after seeding. Incubation time 4 days. At the end of the incubation step, total cellular RNA was isolated (RNeasy 96 kit; Qiagen). Replicon RNA and an internal control (TaqMan rRNA control reagents; Applied Biosystems) were amplified in a single-step multiplex 2983472-1 -693- WO 2008/121634 , ftM«uAn,

Docket No. 60137.0034WOU1 PCT/US2008/058183 RT-PCR protocol as recommended by the manufacturer. The HCV primers and probe were designed with Primer Express software (Applied Biosystems) and covered highly conserved 5'-untranslated region (UTR) sequences (sense, 5'- AGCCATGGCGTTAGTA(T)GAGTGT-3', and antisense, 5'- 5 TTCCGCAGACCACTATGG-3'; probe, 5'-FAM-CCTCCAGGACCCCCCCTCCC-TAMRA-3').

To express the antiviral effectiveness of a compound, the threshold RT-PCR cycle of the test compound was subtracted from the average threshold RT-PCR cycle of the no-drug control (ACtHcv)· A ACt of 3.3 equals a 1 -log 10 10 reduction (equal to the 90% effective concentration [EC90]) in replicon RNA levels. The cytotoxicity of the test compound could also be expressed by calculating the AC^rna values. The AACt specificity parameter could then be introduced (ACtncv “ AC^rna), in which the levels of HCV RNA are normalized for the rRNA levels and calibrated against the no-drug control.

Ex # Compound LogtO Reduction at 50μΜ EC90 (μΜ) 5 -1.21 3.0 6 JtxiA -0.45 ND 7 0.31 ND 8 -1.48 2.11 298J472-1 -694- WO 2008/121634 . rnt__ ηΛΟ/1.νΛΛΤΓ1

Docket No. 60137.0034WOU1 .PCT/US2008/058183

Ex # Compound LoglO Reduction at 50μΜ EC90 (μΜ) 10 IV 0k r -1.25 19.15 11 YV"" όχ -0.55 ND 12 Mil, 0.31 ND 15 ND 0.86 25 ά~ υλ-Ηγ° / HO F -2.22 0.39 27 -2.25 0.66 28 -2.16 0.75 2983472-1 -695- WO 2008/121634 , t1

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ex # Compound LoglO Reduction at 50μΜ EC90 (μΜ) 36 cX> 1 = T ex / HO F -1.64 21.9 39 ί ά /* HO* F -1.78 0.47 49 .9 1 oW ‘ -2.69 0.126 53 -1.33 <0.3 54 >w? -1.55 0.57 55 9 A. -2.38 <0.3 69 )fO 0$ yrf^irQ HO* F NFfc -2.25 <0.3 2983472-1 -696- WO 2008/121634 r ΛΛ„,„,ΛΤΤ,

Docket No. 60137.0034WOU1 PCT/US2008/058183

Ex # Compound LoglO Reduction at 50μΜ EC90 (μΜ) 70 , P r·^ -or Ro λ-r N^< HO F Nht -2.25 <0.3 \4-BrPh): 4-bromo-phenyl.

The entire contents of 60/909,315, filed March 30,2007; 60/982,309, filed October 24, 2007; and 12/053,015, filed March 21,2008 are hereby 5 incorporated by reference in the present application so far as needed to supplement the present disclosure and/or rectify any errors. Moreover, the patent and non-patent references disclosed herein are incorporated by reference. In the event that the incorporated patent and non-patent reference contains a term that conflicts with a term disclosed in either one of the two Provisional 10 Applications or the present application text, the meaning of the term contained in the present application text and the two Provisional Applications controls provided that the overall meaning of the incorporated subject matter is not lost. 2983472-1 -697- cra&amp;’an , crnxan rwzn ατα inia^n pnow pnszn irn πτ “|»oa ,ρνιη ηχΰπ naoana ma™ na^maa np’ioa .zruwan rwaa mpnan pmi1? oxnm οιηπη Pi?

.(moia nannn) cras^an mwa

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Document	Office	Kind	Date
90931507	United States of America	P	2007-03-30
90931507	United States of America	P	2007-03-30
98230907	United States of America	P	2007-10-24
98230907	United States of America	P	2007-10-24
5301508	United States of America	A	2008-03-21
5301508	United States of America	A	2008-03-21
2008058183	United States of America	W	2008-03-26
2008058183	United States of America	W	2008-03-26
12053015	–	–	–
60909315	–	–	–
60982309	–	–	–
PCTUS2008058183	–	–	–
US20070909315P	–	–	–
US20070982309P	–	–	–
US20080053015	–	–	–
WO2008US58183	–	–	–

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Abstract

Term

5 SUMMARY OF THE INVENTION

2983472-J -13- WO 2008/121634 PCT/US2008/058183

DETAILED DESCRIPTION OF THE INVENTION

29S3472-I -96- PCT/US2008/058183 WO 2008/121634

II

I 2983472-1 -155- WO 2008/121634 PCT/US2008/058183

V 2983472-1 -167- PCT/US2008/058183 WO 2008/121634

WO 60137.0034WOUI PCT/US2008/058183

VI

2983472-J -191- WO 2008/121634

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XI

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29S3472.J -344- WO 2008/121634

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XXI 2983472-1 -456- PCT/US2008/058183 WO 2008/121634

IW... - J

XXII 2983472-1 -473 - WO 2008/121634

' 1 R 'IL J

XXIII

2983472-J -498- WO 2008/121634 PCT/US2008/058183

XXIV

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5 XXVI

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5 XXX

' ..... IIP J

WO 2008/121634 T

5 XXXI

I 1 M RJ ....... I I I II III II II

... I , I -- -.-1-1.,,- . I , ..,1. . — I

20 2005037214, WO 2004094452, US 2003187018, WO 200364456, WO

25 2006040890, WO 2006020082, WO 2006012078, WO 2005123087, US

30 20060241064, US 6784166, WO 2007088148, WO 2007039142, WO

HO

EXAMPLES

WO 2008/121634 T

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