Nova Patents
IS7647A

Azaindole kinase inhibitors

Abstract

The present invention provides compounds of formula (I), and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula (I) compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.

Term

Term ended

Projected expiry passed 12 January 2025, 1.7 years ago.

  1. Priority
  2. Filed
  3. Projected expiry
  4. Today

26 claims: 14 independent, 12 dependent

  1. 1
    Einkaleyfisumsókn nr. 7647/2005 (PCT/US2003/022826) Patent Application No. 7647/2005 (PCT / US2003 / 022826) Application date:12.01.2005 Pre-emptive right from: 19.07.2002;02/13/2003 Umsóknardagur: 12.01.2005 Forgangsréttur frá: 19.07.2002;13.02.2003 Applicant: Bristol-Myers Squibb Company, US Umsækjandi: Bristol-Myers Squibb Company, Bandarikjunum Inventors: BHIDE, Rajeev;Uppfinningarmenn: BHIDE, Rajeev;CAI, Zhen-Wei;QIAN, Ligang;CAI, Zhen-Wei;QIAN, Ligang;BARBOSA, Stephanie;Bandarikjunum;Umboðsmaður: Kjartan Ragnars, hrl. BARBOSA, Stephanie;US;Agent: Kjartan Ragnars, Supreme Court Attorney. Icelandic translation of patent no. 1-26, p. 1-10 Islensk þýðing einkaleyfiskrafna nr. 1-26, bls. 1-10 New Chinese languages Nýir kínasatálmar CLAIMS Einkaleyfiskröfur: 1. Efnasamband með formulu (I): A compound of formula (I): where þar sem Z er valinn úr hópnum, sem samanstendur af O, S, N, OH, og Cl, með þeim fyrirvörum, að þegar Z er O eða S, er R41 ekki fyrir hendi, og ί 3 APR 2005 þegar Z er OH eða Cl, eru báðir R41 og R42 ekki fyrir hendi, og þegar Z er N, erR41 H;Z is selected from the group consisting of O, S, N, OH, and Cl, with the proviso that when Z is O or S, R41 not available, and ί 3 APR 2005 when Z is OH or Cl, both are R41 and r42 not available, and when Z is N, R is41 H;X and Y are independently selected from the group consisting of O, OCO, S, SO, SO2, CO, CO2, NR10, NRUCO, NO12CONR13, NR14CO2, NR15SO2, NR16SO2NR17, SO2NR18, CONR19, halogen, nitro and cyano, or X or Y are absent;X og Y eru sjálfstætt valdir úr hópnum, sem samanstendur af 0, OCO, S, SO, SO2, CO, CO2, NR10, NRUCO, NR12CONR13, NR14CO2, NR15SO2, NR16SO2NR17, SO2NR18, CONR19, halogen, nítró og cýanó, eða X eða Y eru ekki fyrir hendi;R1 er vetni, CH3, OH, OCH3, SH, SCH3, OCOR21, SOR22, SO2R23, SO2NR24R25, CO2R26, CONR27R28, NH2, NR29SO2NR30R31, NR32SO2R33, NR34COR3S, NR36CO2R37, NR38CONR39R40, halogen, nítró, eða cýanó;R1 is hydrogen, CH 3, OH, OCH 3, SH, SCH 3, OCOR21, SOR22, SO2R23, SO2NR24R25, CO2R26, CONR27R28, NH2, NR29SO2NR30R31, NR32SO2R33, NR34COR3S, NR36CO2R37, NR38CONR39R40, halogen, nitro, or cyano;R2 and r3 are independently hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, heterocyclo, substituted heterocyclo, aralkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, heterocycloalkyl or substituted heterocycloalkyl;with the proviso that when X is halo, nitro or cyano, R is absent and, when Y is halo, nitro or cyano, R is absent;R2 og R3 eru sjálfstætt vetni, alkýl, skiptitengdur alkýl, alkenýl, skiptitengdur alkenýl, alkýnýl, skiptitengdur alkýnýl, arýl, skiptitengdur arýl, heterósýkló, skiptitengdur heterósýkló, aralkýl, skiptitengdur aralkýl, heteróarýl, skiptitengdur heteróarýl, heterósýklóalkýl eða skiptitengdur heterósýklóalkýl;með þeim fyrirvara, að þegar X er haló, nítró eða cýanó, er R ekki fyrir hendi, og, þegar Y er haló, nítró eða cýanó, er R ekki fyrir hendi;R6 er H, alkýl, skiptitengdur alkýl, arýl, skiptitengdur arýl, heterósýkló, skiptitengdur heterósýkló, NR7R8, OR9 eða halogen;R6 is H, alkyl, substituted alkyl, aryl, substituted aryl, heterocyclo, substituted heterocyclo, NR7R8, OR9 or halogen;T 7 p9 p10 t ≥11 p1 p1 p1 η14 η · 5 p1 p1 p1 p9 p21 p24 κ, κ, κ, κ, κ, κ, κ, κ, κ, kκ, kκ, K, K, K, r25 R26, r27, r28_ r29, r30, r31, r32 r34, r35, r36, r38 r39 ðg r40 em independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclo, or substituted heterocyclo;T?7 p9 plO t> 11 pl2 pl3 η14 η·5 pl6 pl7 pl8 pl9 p21 p24 κ,κ,κ,κ ,κ ,κ ,κ ,κ ,κ ,κ ,κ ,κ ,κ , K , K , r25 R26, r27, r28_ r29, r30, r31, r32, r34, r35, r36, r38 r39 ðg R40 em sjálfstætt valdir úr hópnum, sem samanstendur af vetni, alkýl, skiptitengdum alkýl, arýl, skiptitengdum arýl, heteróarýl, skiptitengdum heteróarýl, heterósýkló, eða skiptitengdum heterósýkló;R22, R23, R33 and r37 are independently selected from the group consisting of alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclo, or substituted heterocyclo;R22, R23, R33 og R37 eru sjálfstætt valdir úr hópnum, sem samanstendur af alkýl, skiptitengdum alkýl, arýl, skiptitengdum arýl, heteróarýl, skiptitengdum heteróarýl, heterósýkló, eða skiptitengdum heterósýkló;R42 er i 3 APR 200b (R43)n, þar sem n jafngildir 0,1 eða 2 og hver R43 er sjálfstætt valinn úr hópnum, sem samanstendur af vetni, flúoró, klór og metýl;og R42 is in 3 APR 200b (R43)n, where n is equal to 0.1 or 2 and each R43 is independently selected from the group consisting of hydrogen, fluoro, chloro and methyl;and R44 er metýl, eða vetni, með þeim frekari fyrirvörum, að: R44 is methyl, or hydrogen, with further precautions that: a. R2 can not be hydrogen, if X is SO, SO2, NR13CO2, or NR142;and a. R2 getur ekki verið vetni, ef X er SO, SO2, NR13CO2, eða NR14SO2;og b. R3 can not be hydrogen, if Y is SO, SO2, NR13CO2, etc.14SO2;b. R3 getur ekki verið vetni, ef Y er SO, SO2, NR13CO2, eda NR14SO2;eda handhverfa, fjölhverfa, eða lyfjafræðilega tækt salt, forlyf, eða lausnarsamband þess, enantiomer, diastereomer, or pharmaceutically acceptable salt, prodrug, or solvate thereof,
  2. 5
    Efnasamband valid úr hópnum, sem samanstendur af:4-(4-Flúoró-2-metýl-7//-indól-5-ýloxý)-5-metýlpýrróló[2,lf][l,2,4]tríazín-6-ól, A compound valid from the group consisting of: 4- (4-Fluoro-2-methyl-7H-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin- 6-ol, 3 APR 200R 3 APR 200R 1- [4- (4-Fluoro-2-methyl-777-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy] -4- ( aminosulfonyl) amino butan-2-ol, 1- [4-(4-Flúoró-2-metýl-777-indól-5-ýloxý)-5-metý-pýrróló[2,l-f][l,2,4]tríazín-6-ýloxý]-4-(amínósúlfónýl)amínóbútan-2-ól, N- {3- [4- (4-Fluoro-2-methyl-7H-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazine -6-yloxy] -2-hydroxy-propyl} -methanesulfonamide, (2S) -3- [4- (4-Fluoro-2-methyl-77-indol-5-yloxy) -5-methylpyrrolo 2,1-f] [1,2,4] triazin-6-yloxy] -propan-1,2-diol, (27β) -3- [4- (4-Fluoro-2-methyl-7 -indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy ] -propan-1,2-diol, (27?) - 1- [4- (4-Fluoro-2-methyl-77-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy] -propan-2-ol, (25) 1- [4- (4-Fluoro-2-methyl-777-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy] -propan-2 (27?) 1- [4- (4-Fluoro-2-methyl-77] -indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin- 6-yloxy] -3-methoxy-propan-2-ol, (25) -1- [4- (4-Fluoro-2-methyl-77-indol-5-yloxy) -5-methylpyrrolo [ f] [1,2,4] triazin-6-yloxy] -3-methoxy-propan-2-ol, Ν- {3 - [4-(4-Flúoró-2-metýl- 7 7/- i ndó 1 - 5 -ýloxý)-5 -metý-pýrróló[2,1 -f] [ 1,2,4]tríazín-6-ýloxý]-2-hýdroxý-própýl} -metansúlfónamíð, (2.S)-3-[4-(4-Flúoró-2-metýl-77/-indól-5-ýloxý)-5-metý-pýrróló 2,1 -f] [ 1,2,4]tríazín-6-ýloxý]-própan-1,2-díól, (27?)-3-[4-(4-Flúoró-2-metýl-7//-indól-5-ýloxý)-5-metýlpýrróló 2,1 -f] [ 1,2,4]tríazín-6-ýloxý]-própan-1,2-díól, (27?)-l-[4-(4-Flúoró-2-metýl-/77-indól-5-ýloxý)-5-metýlpýrróló 2,1 -fj [ 1,2,4]tríazín-6-ýloxý]-própan-2-ól, (25)-l-[4-(4-Flúoró-2-metýl-777-indól-5-ýloxý)-5-metýlpýrróló 2,1 -f] [ 1,2,4]tríazín-6-ýloxý]-própan-2-ól, (27?)l-[4-(4-Flúoró-2-metýl-77/-indól-5-ýloxý)-5-metýlpýrróló [2,1 -f] [ 1,2,4]tríazm-6-ýloxý]-3-metoxý-própan-2-ól, (25)-l-[4-(4-Flúoró-2-metýl-77/-indól-5-ýloxý)-5-metýlpýrróló 2,1 -f] [ 1,2,4]tríazín-6-ýloxý]-3-metoxý-própan-2-ól, 2- [4- (4-Fluoro-2-methyl-77-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy] 2- [4-(4-Flúoró-2-metýl-77/-indól-5-ýloxý)-5-metýlpýrróló[2,1 -f] [ 1,2,4]tríazín-6-ýloxý]-etanól, N- {2- [4- (4-Fluoro-2-methyl-7H-indol-5-yloxy) -5-methyl-pyrrolo [2,1-f] [1,2,4] triazine-6- yloxy] -ethyl} methanesulfonamide, (27α) -1- [4- (4-Fluoro-2-methyl-777-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1 , 2,4] triazin-6-yloxy] -4-methanesulfonyl-butan-2-ol, (2S) -1- [4- (4-Fluoro-2-methyl-77-indol-5-yloxy) 5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy] -4-methanesulfonyl-butan-2-ol, N-{2-[4-(4-Flúoró-2-metýl-7//-indól-5-ýloxý)-5-metýl-pýrróló 2,1 -f][ 1,2,4]tríazín-6-ýloxý]-etýl}-metansúlfónamíð, (27?)-1 -[4-(4-Flúoró-2-metýl-777-indól-5-ýloxý)-5-metý-pýrróló [2,1 -f][ 1,2,4]tríazín-6-ýloxý]-4-metansúlfónýl-bútan-2-ól, (2S)~ 1 -[4-(4-Flúoró-2-metýl-77/-indól-5-ýloxý)-5-metý-pýrróló [2,1 -f] [ 1,2,4]tríazín-6-ýloxý]-4-metansúlfónýl-bútan-2-ól, 5-Methyl-4- (2-methyl-777-indol-5-yloxy) -6- (3-piperidinylpropoxy) -pyrrolo [2,1-f] [1,2,4] triazine, 5-Metýl-4-(2-metýl-777-indól-5-ýloxý)-6-(3-píperidín-lýlprópoxý)-pýrróló[2,1 -f] [ 1,2,4] tríazín, 4- (4-Fluoro-2-methyl-7H-indol-5-yloxy) -5-methyl-6- (2-piperidin-4-yl-ethoxy) -pyrrolo [2,1-f] [1,2,4 ] triazine, 7 7647 4-(4-Flúoró-2-metýl-7Æ-indól-5-ýloxý)-5-metýl-6-(2-píperidín-4ýl-etoxý)-pýrróló[2,1 -f] [ 1,2,4]tríazín, 7 7647 A / C 2005 A/K 2005 4- (4-Fluoro-2-methyl-777-indol-5-yloxy) -5-methyl-6- (3-pyridin-4-ylpropoxy) -pyrrolo [2,1-f] [1,2,4 ] triazine, {1- [4- (4-Fluoro-2-methyl-7H-indol-5-yloxy) -5-methyl-pyrrolo [2,1f] [1,2,4] triazin- 6-yloxymethyl] -3-methanesulfonyl-propyl} -dimethyl-amine, 71 4-(4-Flúoró-2-metýl-777-indól-5-ýloxý)-5-metýl-6-(3-pýridín-4-ýlprópoxý)-pýrróló[2,1 -f] [ 1,2,4]tríazín, {1 - [4-(4-F lúoró-2-metýl-7//-indól-5 -ýloxý)-5 -metýl-pýrróló[2,1 f] [ 1,2,4]tríazín-6"ýloxýmetýl] -3 -metansúlfónýl-própýl} -dímetýl-amín, 71 2- [4- (4-Fluoro-2-methyl-7-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy] -1- methylethylamine, {2- [4- (4-Fluoro-2-methyl-777-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy] 1-methylethyl} -methylamine, 2-[4-(4-Flúoró-2-metýl-7#-indól-5-ýloxý)-5-metýlpýrróló[2,1 -f][ 1,2,4]tríazín-6-ýloxý]-1 -metýletýlamín, {2-[4-(4-Flúoró-2-metýl-777-indól-5-ýloxý)-5-metýlpýrróló[2,1 -f] [ 1,2,4]tríazín-6-ýloxý] -1 -metýletýl} -metýlamín, 4- (4-Fluoro-2-methyl-777-indol-5-yloxy) -5-methyl-6- (morpholin-2-ylmethoxy) -pyrrolo [2,1-f] [1,2,4] tri azine, [(17?), 2 Y] -2-dimethylaminopropionic acid [2- [4- (4-Fluoro-2-methyl-777-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy] -1-methylethyl ester, [(1A), 25] -2-Amino-4-methylpentanoic acid [2- [4- (4-Fluoro-2-methyl -777-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy] -1-methylethyl ester, [(17?), 2S] -2- Aminopropionic acid 2- [4- (4-Fluoro-2-methyl-7,7-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy] -1 -methylethyl ester, 4-(4-Flúoró-2-metýl-777-indól-5-ýloxý)-5-metýl-6-(morfólín-2-ýlmetoxý)-pýrróló[2,1 -f] [ 1,2,4] trí azín, [(17?),2Y]-2-Dímetýlamínóprópíonsýru-[2-[4-(4-flúoró-2-metýl-777-indól-5-ýloxý)-5-metýlpýrróló[2,1 -f]-[ 1,2,4]tríazín-6-ýloxý]]-1 -metýletýl estri, [(1 A),25]-2-Amínó-4-metýlpentansýru [2-[4-(4-flúoró-2-metýl-777-indól-5-ýloxý)-5-metýlpýrróló[2,1 -fj[ 1,2,4]tríazín-6-ýloxý]]-1 -metýletýl estri, [(17?),2S]-2- Amínóprópíonsýru 2-[4-(4-flúoró-2-metýi-7/7-indól-5-ýloxý)-5-metýlpýrróló[2,l-fj[l,2,4]tríazín-6-ýloxý]-l-metýletýl estri, 4- (4-Fluoro-2-methyl-777-indol-5-yloxy) -6- (3-methanesulfonyl-propoxy) -5-methyl-pyrrolo [2,1-f] [1,2,4] triazine , and 4-(4-Flúoró-2-metýl-777-indól-5-ýloxý)-6-(3-metansúlfónýl-própoxý)-5-metýl-pýrróló[2,1 -f] [ 1,2,4]tríazín, og N- {3- [4- (4-Fluoro-2-methyl-7H-indol-5-yloxy) -5-methyl-pyrrolo [2,1-f] [1,2,4] triazin-6 -yloxy] -propyl} -methanesulfonamide. N-{3-[4-(4-Flúoró-2-metýl-7//-indól-5-ýloxý)-5-metýl-pýrróló[2,1 -f] [ 1,2,4]tríazín-6-ýloxý]-própýl }-metansúlfónamíð.
  3. 6
    Efnasamband valid úr hópnum, sem samanstendur af:A compound valid from the group consisting of: 4- (4-Fluoro-2-methyl-777-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-ol, (2S) -3- [4- (4-Fluoro-2-methyl-777-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy] -propan-1,2-diol, (27?) - 3- [4- (4-Fluoro-2-methyl-7,77-indol-5-yloxy) -5,747 4-(4-Flúoró-2-metýl-777-indól-5-ýloxý)-5-metýlpýrróló[2,lf] [ 1,2,4]tríazín-6-ól, (2S)-3-[4-(4-Flúoró-2-metýl-777-indól-5-ýloxý)-5-metýpýrróló [2,1 -f] [ 1,2,4]tríazín-6-ýloxý]-própan-1,2-díól, (27?)-3 - [4-(4-FIúoró-2-metýl- 7 77-indól-5 -ýloxý)-5 7647 3 APR 2005 metýlpýrróló 2,1 -f] [ 1,2,4]tríazín-6-ýloxý] -própan-1,2-díól, (27?)-l-[4-(4-Flúoró-2-metýl-7H-indól-5-ýloxý)-5-metýlpýrróló [2,1 -f] [ 1,2,4]tríazín-6-ýloxý]-própan-2-ól, (2S)~ 1 - [4-(4-Flúoró-2-metýl- 7/Z-indól - 5 -ý 1 oxý)-5 -metýlpýrróló [2,1 -f] [ 1,2,4]tríazm-6-ýloxý]-própan-2-ól, (27?)l-[4-(4-Flúoró-2-metýl-7/7- indól-5-ýloxý)-5-metýlpýrróló [2,1 -f][ 1,2,4]tríazín-6-ýloxý]-3-metoxý-própan-2-ól, (25)-1 - [4-(4-Flúoró-2-metýl- 1H- indól-5 -ýloxý)-5 -metýlpýrróló [2,1 -f][ 1,2,4]tríazín-6-ýloxý]-3-metoxý-própan-2-ól, 3 April 2005 methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy] -propan-1,2-diol, (27α) -1- [4- (4-Fluoro-2-methyl -7H-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy] -propan-2-ol, (2S) -1- [4- 4-Fluoro-2-methyl-7H-indol-5-yl-oxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazol-6-yloxy] -propan-2-ol , (27?) 1- [4- (4-Fluoro-2-methyl-7,7-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6 -Yloxy] -3-methoxy-propan-2-ol, (25) -1- [4- (4-Fluoro-2-methyl-1H-indol-5-yloxy) -5-methylpyrrolo [2,1-f ] [1,2,4] triazin-6-yloxy] -3-methoxy-propan-2-ol, 5-Methyl-4- (2-methyl-777-indol-5-yloxy) -6- (3-piperidin-1-ylpropoxy) -pyrrolo [2,1-f] [1,2,4] triazine, 5-Metýl-4-(2-metýl-777-indól-5-ýloxý)-6-(3-píperidín-l-ýlprópoxý)-pýrróló[2, l-f][ 1,2,4]tríazín, 4- (4-Fluoro-2-methyl-777-indol-5-yloxy) -5-methyl-6- (2-piperidin-4-yl-ethoxy) -pyrrolo [2,1-f] [1,2 , 4] triazine, 4-(4-Flúoró-2-metýl-777-indól-5-ýloxý)-5-metýl-6-(2-píperidín-4-ýl-etoxý)-pýrróló [2,1 -f] [ 1,2,4] tríazín, 2- [4- (4-Fluoro-2-methyl-1H-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy] -1- methylethylamine, [(17?), 2S] -2-Dimethylammopropionic acid [2- [4- (4-Fluoro-2-methyl-777-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy]] -1-methylethyl ester, [(17α), 25] -2-Ammo-4-methylpentanoic acid [2- [4- (4-Fluoro-2-methyl -77F-indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy] -1-methylethyl ester, [(17?), 25] -2 -Aminopropionic acid 2- [4- (4-Fluoro-2-methyl-77] -indol-5-yloxy) -5-methylpyrrolo [2,1-f] [1,2,4] triazin-6-yloxy] -1- methylethyl ester, 2- [4-(4-Flúoró-2-metýl- 1H - indól-5-ýloxý)- 5 -metýlpýrróló[2,1 -f] [ 1,2,4] trí azín-6-ýloxý] -1 -metýletýlamín, [(17?),2S]-2-Dímetýlammóprópíonsýru-[2-[4-(4-flúoró-2-metýl-777-indól-5-ýloxý)-5-metýlpýrróló[2,1 -f]-[ 1,2,4]tríazín-6-ýloxý]]-1 -metýletýl estri, [(17?),25]-2-Ammó-4-mefylpentansýru [2-[4-(4-flúoró-2-metýl-77F-indól-5-ýloxý)-5-metýlpýrróló[2,1 -f] [ 1,2,4]tríazín-6-ýloxý]]-1 -metýletýl estri, [(17?),25]-2-Amínóprópíonsýru 2-[4-(4-flúoró-2-metýl-77/-indól-5-ýloxý)-5-metýlpýrróló[2,l-f][l,2,4]tríazín-6-ýloxý]-l-metýletýl estri, 4- (4-Fluoro-2-methyl-777-indol-5-yloxy) -6- (3-methanesulfonyl-propoxy) -5-methyl-pyrrolo [2,1-f] [1,2,4] triazine , and 4-(4-Flúoró-2-metýl-777-indól-5-ýloxý)-6-(3-metansúlfónýl-própoxý)-5-metýl-pýrróló[2,1 -f][ 1,2,4]tríazín, og N- {3- [4- (4-Fluoro-2-methyl-777-indol-5-yloxy) -5-methyl-pyrrolo [2,1-f] [1,2,4] triazin-6-yloxy ] -propyl} -methanesulfonamide. N-{3-[4-(4-Flúoró-2-metýl-777-indól-5-ýloxý)-5-metýl-pýrróló [2,1 -f] [ 1,2,4]tríazín-6-ýloxý]-própýl} -metansúlfónamíð. p APR 2005 p Λ APR 2005
  4. 7
    Lyfjasamsetning, sem hefur að geyma að minnsta kosti eitt A pharmaceutical composition, which contains at least one Efnasambandanna samkvæmt einkaleyfiskrdfu nr. 1 og lyfjafrsdilega tskt burdarefni fyrir hana. The compounds of patent no. 1 and a pharmacologically toxic towel for her.
  5. 8
    Lyfjasamsetning, sem hefur ad geyma ad minnsta kosti eitt 8. Pharmaceutical composition, which contains at least one Efnasambandanna samkvæmt einkaleyfiskrdfu nr. 5 og lyfjaifsdilega tskt burdarefni fyrir hana. The compounds of patent no. 5 and a drug-resistant towel for her.
  6. 9
    Lyfjasamsetning, sem hefur ad geyma ad minnsta kosti eitt 9. Pharmaceutical composition, which contains at least one Efnasambandanna samkvsmt einkaleyfiskrdfu nr. 6 og lyfjafrsdilega tskt burdarefni fyrir hana. The compounds according to patent no. 6 and a pharmacologically toxic towel for her.
  7. 10
    A pharmaceutical composition comprising at least one or more of the compounds according to patent no. A composition with a pharmacologically acceptable carrier and at least one effective antidote for cancer as a cytotoxic active substance. 10. Lyfjasamsetning, sem hefur ad geyma ad minnsta kosti eitt eda fleiri Efnasambandanna samkvsmt einkaleyfiskrdfu nr. 1 ί samsetningu med lyfjafrsdilega tsku burdarefni og ad minnsta kosti einu virku vidbótarefni gegn krabbameini eda frumudrepandi virku efhi.
  8. 11
    A pharmaceutical composition comprising at least one or more of the compounds according to patent no. A pharmaceutical composition with a pharmaceutically acceptable carrier and at least one effective antidote for cancer as a cytotoxic active substance. 11. Lyfjasamsetning, sem hefur ad geyma ad minnsta kosti eitt eda fleiri Efnasambandanna samkvsmt einkaleyfiskrdfu nr. 5 ί samsetningu med lyfjafrsdilega tsku burdarefni og ad minnsta kosti einu virku vidbótarefni gegn krabbameini eda frumudrepandi virku efhi.
  9. 12
    A pharmaceutical composition comprising at least one or more of the compounds according to patent no. A combination with a pharmacologically acceptable carrier and at least one effective antidote for cancer as a cytotoxic active substance. 12. Lyfjasamsetning, sem hefur ad geyma ad minnsta kosti eitt eda fleiri Efnasambandanna samkvsmt einkaleyfiskrdfu nr. 6 ί samsetningu med lyfjafrsdilega tsku burdarefni og ad minnsta kosti einu virku vidbótarefni gegn krabbameini eda frumudrepandi virku efhi.
  10. 13
    Lyfjasamsetningin samkvsmt einkaleyfiskrdfu nr. 8, þar sem virka efnid gegn krabbameini eda frumudrepandi efnid er valid úr hdpnum, 13. The pharmaceutical composition according to patent no. 8, wherein active antidote to cancer or cytotoxic agent is valid from the hp, 5 APS >006 sem samanstendur af:línómíð, tálmar integrín-avp3-verkunar, angíóstatín, razoxan, tamoxifen, tóremífen, raloxífen, dróloxífen, joðoxífen, megestról acetat, anastrózól, letrózól, bórazól, exemestan, flútamíð, nílútamíð, bícalútamíð, cýpróteron acetat, góserelín acetat, leuprólíð, fínasteríð, herceptín, metallóprótínasa tálmar, tálmar úrókínasa plasmínógenvirkis viðtakaverkunar, vaxtarþáttarmótefni, vaxtarþáttar-viðtakamótefhi, bevacízúmab, cetuxímab, týrósínkínasatálmar, serín-/þreónín kínasa tálmar, metótrexat, 5-flúoróúracíl, púrín, adenósín hliðstæður, cýtósín arabínósíð, doxórúbicín, daunómýcín, epírúbicín, ídarúbicín, mítómýcín-C, dactínómýcín, mítramýcín, cisplatín, karbóplatín, nitursinnep, melfalan, klórambúcíl, búsúlfan, sýklófosfamíð, ífosfamíð, nítrósóúrea, þíótepa, víncristín, paclitaxel, dócetaxel, epóþílón hliðstæður, discódermólíð hliðstæður, eleúteróbín hliðstæður, etópósíð, tenípósíð, amsacrín, tópótecan, irínótecan, flavópýridól, próteasóm tálmar, þ. á m. bortezómíb og líffræðilegir svaraumbreytar. 5 APS> 006 comprising: linomomide, inhibitors of integrin-avp3-effect, angiotostatin, razoxan, tamoxifen, trememberphen, raloxifene, drooxoxifen, iodoxifene, megestrol acetate, anastrozole, letrozole, bosrazole, exemestane, flutamide, nilutamide, bicutamid, cyprotonate acetate , gosereline acetate, leuprolide, finasteride, herceptin, metalloproteinase inhibitors, inhibitors of urokinase plasminogen activator receptor function, growth factor antibodies, growth factor receptor, bevacizumab, cetuximab, tyrosine kinase inhibitors, serín- / threonine kinase inhibitors, methotrexate, 5-fluorouracil, purine, adenosine analogues, cytosine arabinoside , doxorubicin, daunomycin, epirubicin, idarubicin, mitomycin-C, dactinomycin, mitramycin, cisplatin, carboplatin, nitrosin, melphalan, chloromercil, busulfan, cyclophosphamide, phosphosphamide, nitroso urea, thiotep, vincristine, paclitaxel, docetaxel, epothelon analog Dur, disoddermide analogues, eleuterobine analogues, etoposide, teniposide, amsacrine, topotecan, irinotecan, flavopyridol, protease inhibitors, th. on m. bortezomib and biological responses.
  11. 14
    A method of inducing an effect on venous thromboembolism, comprising administering to a mammalian species an effective inducing amount of vasodilatation at least one of the compounds of patent specification no. 1. 14. Aðferð til að framkalla áhrif gegn æðanýmyndun og sem felur í sér að gefa spendýrategund, sem þess þarfnast, virkt framkallandi magn gegn æðanýmyndun að minnsta eins Efnasambandanna samkvæmt einkaleyfiskrofii nr. 1.
  12. 15
    A method of inducing reduced venous thrombosis, which comprises administering to a mammalian target species an effective vasodilator, a decreasing amount of at least one of the compounds according to patent specification no. 1. 15. Aðferð til að framkalla skerta æðagegndreypni og sem felur í sér að gefa spendýrategund, sem þess þarfhast, virkt æðagegndreypandi, skerðandi magn að minnsta kosti eins Efnasambandanna samkvaemt einkaleyfiskrofii nr. 1.
  13. 16
    Aðferð til að tálma prótínkínasavirkni vaxtarþáttaviðtaka og sem felur í sér að gefa spendýrategund, sem þess þarfnast, virkt prótínkínasa764 7 A method for inhibiting protein kinase activity of growth factor receptors and comprising administering to a mammalian species in need of active protein kinase 764 7 3 APP M(!$ tálmandi magn að minnsta kosti eins Efnasambandanna samkvæmt einkaleyfiskröfu nr. 1. 3 μM (%) inhibitory amount of at least one of the compounds of claim 1.
  14. 21
    A method of treating autoimmune diseases comprising administering to a mammalian species, in need thereof, the therapeutically effective amount of the composition according to claim no. 7. 21. Aðferð til að meðhöndla sjálfsnæmissjúkdóma og sem felur í sér að gefa spendýrategund, sem þess þarfnast, meðferðarlega virkt magn samsetningarinnar samkvæmt einkaleyfiskröfii nr. 7.
Independent claims14