Nova Patents
AT433447T

Pyrimidine compounds

Abstract

A compound of formula (I) ** see formula wherein R 1 is selected from the group consisting of H, halo, alkyl, alkenyl, alkynyl; R 2 is selected from the group consisting of halo, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, - (R 7) g- C (O) R 6, - (R 7) g-CO2R 6, - (R 7) gC (O) N (R 6) 2, - (R 7) g-OR 6, -O (R7) g-Ay, - (R 7) gS (O) eR 6, - (R 7) gN ( R 6) 2, - (R 7) g N (R 6) C (O) R 6, - (R 7) g-CN, - (R 7) g-SCN, -NO 2, -N 3 Ay and 5- to 9-membered containing 1 or 2 heteroatoms selected from N, O and S; each R 3 is same or different and is independently H or alkyl; Y is selected from the group consisting -C (O) R 8, -C (S) R 8, -S (O) eR 9, -N (R 9) 2, -N (R 9) -S (O) eR 9, and -N (R 9) -C (O) R9, or Y, together with C-2 and C-3 form a fused ring system of formula a: wherein R 8 is selected from the group consisting alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, Ay, Het, 6-O- (R7) g-Ay, -O- (R 7) g-Het, -N (R 6) 2, - N (R 6) - (R 7) g-Ay, -N (R 6) - (R 7) g-Het, -N (R 6) - (R 7) g-OR 6, -N (R 6 ) - (R 7) gc (O) R 6 -N (R 6) - (R 7) g-CO 2 R 6, -N (R 6) - (R 7) g-SO2R 6 and -N (R 6) - (R 7) g N (R 6) 2; each R 9 is same or different and is independently selected from the group consisting of H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, Ay and Het; c is 0 or 1; Z 1, Z 2, Z 3 and Z 4 each independently he selected from the group consisting of C, O, S and N, wherein when c is 0, at least one of Z 1, Z 2 and Z 3 is C and wherein when c is 1, at least two of Z 1, Z 2, Z 3 and Z 4 are C; each dotted line represents an optional double bond; d is 0, 1 or 2; each R 10 is the same or different and is independently selected from the group consisting of halo, alkyl, oxo, hydroxy, mercapto and amino; a is 0, 1, 2 or 3; each R 4 is the same or different and are independently selected from the group consisting of halo, alkyl, - (R 7) gcicloalquilo, - (R 7) gC (O) R 6, - (R 7) g -CO 2 R 6, - (R 7) gc (O) N (R 6) 2, - (R 7) g-OR 6, - (R 7) gS (O) eR 6, - (R 7) g N (R 6) 2, - (R 7) gN (R 6) C (O) R6, each e is the same or different and is independently 0, 1 or 2; b is 0, 1, 2, 3, 4 or 5; each R 5 is the same or different and is a group of formula (R 7) gR 11, each R 6 is the same or different and are independently selected from the group consisting of H selected, alkyl, alkenyl, alkynyl, cycloalkyl and cycloalkenyl; g is 0 or 1; R 7 is alkylene or alkenylene; Ay is aryl; Het is a heterocycle or heteroaryl of 5 or 6 members containing 1, 2 or 3 heteroatoms selected from the group consisting of N, O and S; R 11 is selected from the group consisting of halo, alkyl, alkenyl, alkynyl, Ay, Het, -C (O) Het, -CO 2 R 6, -CO2Ay, -CO2Het, -C (O) N (R 6) 2, - C (O) N (R 6) Ay, -C (O) N (R 6) Het, -C (O) N (R 6) - (R 7) g N (R 6) 2, -C (O) N (R 6) - (R 7) g-CO2 R 6 -C (O) N (R 6) - (R 7) gS (O) eR 6 -OR 6, -O- (R 7) g Ay, -O- (R7) g-Het, -OR 7 6, -OR 7 -N (R 6) 2, -S (O) eR 6, -S (O) e- (R7 ) g- Het, -S (O) e (R 7) g N (R 6) 2, -S (O) e (R 7) g N (R 6) Het, -S (O) (R6 ) - (R 7) gc (O) Het, -N (R 6) 2, -N (R 6) - (R 7) g-Ay, -N (R 6) - (R 7) g-Het, -N (R 6) - (R 7) gC (O) R 6, -N (R 6) -C (O) - (R7) g-Het, -N (R 6) -C (O) - (R 7) g N (R 6) 2, -N (R 6) -C (O) - (R 7) g N (R 6) Het, -N (R 6) -C (O) - (R 7) gn (R 6) - (R 7 O) hN (R 6) -CO 2 R 6, -N (R 6) - (R 7) gS (O) eR 6 -N (R 6) - (R 7) gS (O) eHet, -N (R 6) -R 7 -N (R 6) 2, -N (R 6) -R 7 -OR 6, -CN, and -N 3; h is 1-20; wherein when R1 is -CH3, R2 is Br or NO2, both R3 are H, a is 0 and b is 0 or 1 wherein R 5 is -CO whether 2H, then Y is not -CO 2 H, "alkyl" (and "alkylene") is an alkyl (and alkylene) linear or branched C1-8 (optionally substituted one or more times with halogen or cyano), "alkenyl it" C 2-8 alkenyl is a linear or branched (optionally substituted one or more times by halogen or cyano), "alkynyl" is an alkynyl C 2-8 linear or branched (optionally substituted one or more times with halogen or cyano), "cycloalkyl" is a C3-8 cycloalkyl (optionally substituted on any available carbon with one or more substituents selected from the group consisting of halo, alkyl, alkenyl, alkynyl, hydroxyl, oxo, carboxyl, alkylcarboxyl, alkylether, mercapto, sulfonyl, sulfinyl, alkylsulfonyl, sulfonamido, amino, alkylamino, dialkylamino, acetylamino, amino sulfonamide and cyano), "cycloalkenyl" is a C 3-8 cycloalkenyl (optionally substituted on any available carbon with one or more substituents selected from the group consisting of halo, alkyl (including haloalkyl, e.g., perfluoroalkyl), alkenyl, alkynyl, hydroxyl, oxo , carboxyl, alkylcarboxyl, alkylether, mercapto, sulfonyl, sulfinyl, alkylsulfonyl, sulfonamido, amino, alkylamino, dialkylamino, acetylamino, amino and cyano), Ay is aryl which is monocyclic carbocyclic groups and bicyclic carbocyclic groups fused having 6 to 13 carbon atoms carbon and at least one aromatic ring (optionally substituted on any available carbon with one or more substituents selected from the group consisting of halo, alkyl, alkenyl, alkynyl, hydroxyl, carboxyl, alkylcarboxyl, alkylether, mercapto, sulfonyl, sulfinyl, alkylsulfonyl, sulfonamido, amino, alkylamino, dialkylamino, acetylamino, aminosulfonamido and cyano), "heterocycle" and "heterocyclic" are saturated or unsaturated nonaromatic monocyclic and bicyclic groups fused nonaromatic saturated or unsaturated, having the specified number of members and containing 1, 2, 3 or 4 heteroatoms selected from N, O and S (optionally substituted on any carbon or heteroatom with one or more substituents selected from the group consisting of halo, alkyl, alkenyl, alkynyl, oxo, hydroxyl, carboxyl, alkylcarboxyl, alkylether, mercapto, sulfonyl, sulfinyl, alkylsulfonyl, sulfonamido, amino, alkylamino, dialkylamino, acetylamino, amino and cyano), "heteroaryl" are aromatic monocyclic and bicyclic groups fused in which at least one ring is aromatic, having the number specified members and containing 1, 2, 3, or 4 heteroatoms selected from N, O and S (unless a different number of heteroatoms is specified) (optionally substituted on any available carbon or heteroatom with one or more substituents selected from group consisting of 51 null ES 2325440 T3 halo, alkyl, alkenyl, alkynyl, oxo, hydroxyl, carboxyl, alkylcarboxyl, alkylether, mercapto, sulfonyl, sulfinyl, alkylsulfonyl, sulfonamido, amino, alkylamino, dialkylamino, acetylamino, amino and cyano) . or a salt thereof or pharmaceutically acceptable solvates.

Term

No projected expiry on record.

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12 members in 7 offices

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DocumentOfficeKindDate
44879503United States of AmericaP
2004004197United States of AmericaW

Members12

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DocumentOfficeKind
WO2004074244A2World Intellectual Property Organization (WIPO)A2
WO2004074244A3World Intellectual Property Organization (WIPO)A3
EP1597251A2European Patent Office (EPO)A2
JP2006518386AJapanA
US2007010668A1United States of AmericaA1
US7514446B2United States of AmericaB2
EP1597251B1European Patent Office (EPO)B1
AT433447TThis recordAustriaT
ATE433447T1AustriaT1
DE602004021472D1GermanyD1
ES2325440T3SpainT3
JP4634367B2JapanB2