Patent ID: 6534506
Filing Date: 2003-03-18
Classification: A61P,C07D

Abstract:
A compound of the formula A: wherein:R1a and R1c are independently selected from: a) hydrogen, b) aryl, heterocycle, C3-C10 cycloalkyl, R10Oâ€”, R11S(O)mâ€”, R10C(O)NR10â€”, (R10)2Nâ€”C(O)â€”, CN, NO2, (R10)2Nâ€”C(NR10)â€”, R10C(O)â€”, R10OC(O)â€”, â€”N(R10)2, or R11OC(O)NR10â€”, c) unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C2-C6 alkenyl or unsubstituted or substituted C2-C6 alkynyl, wherein the substituent on the substituted C1-C6 alkyl, substituted C2-C6 alkenyl or substituted C2-C6 alkynyl is selected from unsubstituted or substituted aryl, heterocyclic, C3-C10 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, R10Oâ€”, R11S(O)mâ€”, R10C(O)NR10â€”, (R10)2Nâ€”C(O)â€”, CN, (R10)2Nâ€”C(NR10)â€”, R10C(O)â€”, R10OC(O)â€”, â€”N(R10)2, and R11OC(O)â€”NR10â€”, or two R1as or two R1cs on the same carbon atom may be combined to form â€”(CH2)tâ€”; R1b is selected from: a) hydrogen, b) aryl, heterocycle, C3-C10 cycloalkyl, (R10)2Nâ€”C(O)â€”, (R10)2Nâ€”C(NR10)â€”, R10C(O)â€”or R10OC(O)â€”, and c) unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C2-C6 alkenyl or unsubstituted or substituted C2-C6 alkynyl, wherein the substituent on the substituted C1-C6 alkyl, substituted C2-C6 alkenyl or substituted C2-C6 alkynyl is selected from unsubstituted or substituted aryl, heterocyclic, C3-C10 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, one or more fluorines, R10Oâ€”, R11S(O)mâ€”, R10C(O)NR10â€”, (R10)2Nâ€”C(O)â€”, CN, (R10)2Nâ€”C(NR10)â€”, R10C(O)â€”, R10OC(O)â€”, â€”N(R10)2, and R11OC(O)â€”NR10â€”; R2 and R3 are independently selected from H; unsubstituted or substituted C1-8 alkyl, unsubstituted or substituted C2-8 alkenyl, unsubstituted or substituted C2-8 alkynyl, unsubstituted or substituted aryl, unsubstituted or substituted heterocycle, â€ƒwherein the substituted group is substituted with one or more of: 1) aryl or heterocycle, unsubstituted or substituted with: a) C1-4 alkyl, b) (CH2)pOR6, C) (CH2)pNR6R7, d) halogen, e) CN, 2) C3-6 cycloalkyl, 3) OR6, 4) SR4, S(O)R4, SO2R4, R2 and R3 are attached to the same carbon atom and are combined to form â€”(CH2)uâ€” wherein one of the carbon atoms is optionally replaced by a moiety selected from O, S(O)m, â€”NC(O)â€”, and â€”N(COR10)â€”; and R4 is selected from C1-4 alkyl, C3-6 cycloalkyl, heterocycle, aryl, unsubstituted or substituted with: a) C1-4 alkoxy, b) aryl or heterocycle, c) halogen, d) HO, g) N(R10)2, or h) one or more fluorines; R5, R6 and R7 are independently selected from: 1) hydrogen, 2) R10C(O)â€”, or R10OC(O)â€”, and 3) C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, heterocycle, aryl, aroyl, heteroaroyl, arylsulfonyl, heteroarylsulfonyl, unsubstituted or substituted with one or more substituents selected from: a) R10Oâ€”, b) aryl or heterocycle, c) halogen, d) R10C(O)NR10â€”, g) N(R10)2, h) C3-6 cycloalkyl, i) C1-C6 perfluoroalkyl, j) (R 10)2Nâ€”C(NR10)â€”, k) R10OC(O)â€”, l) R11OC(O)NR10â€”, m) CN, and n) NO2; or R6 and R7 may be joined in a ring; and independently, R5 and R7 may be joined in a ring; R8 is independently selected from: a) hydrogen, b) unsubstituted or substituted aryl, unsubstituted or substituted heterocycle, C3-C10 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 perfluoroalkyl, F, Cl, Br, R12Oâ€”, R11S(O)mâ€”, R10C(O)NR10â€”, (R10)2NC(O)â€”, R102Nâ€”C(NR10)â€”, CN, NO2, R10C(O)â€”, R10OC(O)â€”, â€”N(R10)2, or R11OC(O)NR10â€”, and c) C1-C6 alkyl unsubstituted or substituted by unsubstituted or substituted aryl, unsubstituted or substituted heterocycle, C3-C10 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 perfluoroalkyl, F, Cl, Br, R10Oâ€”, R11S(O)mâ€”, R10C(O)NHâ€”, (R10)2NC(O)â€”, R102Nâ€”C(NR10)â€”, CN, R10C(O)â€”, R10OC(O)â€”, â€”N(R10)2, or R10OC(O)NHâ€”; R9 is selected from: a) hydrogen, b) C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 perfluoroalkyl, F, Cl, Br, R10Oâ€”, R11S(O)mâ€”, R10C(O)NR 10â€”, (R10)2NC(O)â€”, R102Nâ€”C(NR10)â€”, CN, NO2, R10C(O)â€”, R10OC(O)â€”, â€”N(R10)2, or R11OC(O)NR10â€”, and c) C1-C6 alkyl unsubstituted or substituted by C1-C6 perfluoroalkyl, F, Cl, Br, R10Oâ€”, R11S(O)mâ€”, R10C(O)NR10â€”, (R10)2NC(O)â€”, R102Nâ€”C(NR10)â€”, CN, R10C(O)â€”, R10OC(O)â€”, â€”N(R10)2, or R11OC(O)NR10â€”; R10 is independently selected from hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with one or more fluorines, benzyl, unsubstituted or substituted aryl and unsubstituted or substituted heterocycle; R11 is independently selected from C1-C6 alkyl, C1-C6 alkyl substituted with one or more fluorines, unsubstituted or substituted aryl and unsubstituted or substituted heterocycle; R12 is independently selected from hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with one or more fluorines, unsubstituted or substituted benzyl, unsubstituted or substituted aryl, unsubstituted or substituted heterocycle, and C1-C6 alkyl substituted with unsubstituted or substituted aryl or unsubstituted or substituted heterocycle; A1 is selected from a bond, â€”C(O)â€”, â€”C(O)NR10â€”, â€”NR10C(O)â€”, O, â€”N(R10)â€”, â€”S(O)2N(R10)â€”, â€”N(R10)S(O)2â€”, â€”NR10C(O)NR10â€” and S(O)m; A2 is selected from a bond, â€”C(O)â€”, â€”C(O)NR10â€”, â€”NR10C(O)â€”, O, â€”N(R10)â€”, â€”S(O)2N(R10)â€”, â€”N(R10)S(O)2â€”, â€”NR10C(O)NR10â€”, S(O)m and â€”C(R1c)2â€”; G1, G2 and G3 are independently selected from (R2,R3) and O; V is selected from: a) heterocycle, and b) aryl; W is S(O)m, O or CH2; X is selected from: a bond, â€”C(O)â€”, â€”NR10C(O)â€”, â€”N(R10)S(O)2â€” and S(O)2; Y is selected from a bond, â€”C(O)â€”, â€”C(O)NR10â€”, â€”C(O)Oâ€” and â€”S(O)m; Z1 is selected from unsubstituted or substituted aryl and unsubstituted or substituted heterocycle, wherein the substituted aryl or substituted heterocycle is substituted with one or more of: 1) C1-8 alkyl, C2-8 alkenyl or C2-8 alkynyl, unsubstituted or substituted with: a) C1-4 alkoxy, b) NR6R7, c) C3-6 cycloalkyl, d) aryl or heterocycle, e) HO, f) â€”S(O)mR4, g) â€”C(O)NR6R7, or h) one or more fluorines; 2) substituted or unsubstituted aryl or substituted or unsubstituted heterocycle, 3) halogen, 4) OR6, 5) NR6R7, 6) CN, 7) NO2, 8) CF3; 9) â€”S(O)mR4, 10) â€”OS(O)2R4, 11) â€”C(O)NR6R7, 12) â€”C(O)OR6, or 13) C3-C6 cycloalkyl; Z2 is selected from a bond, unsubstituted or substituted aryl and unsubstituted or substituted heterocycle, wherein the substituted aryl or substituted heterocycle is substituted with one or more of: 1) C1-8 alkyl, C2-8 alkenyl or C2-8 alkynyl, unsubstituted or substituted with: a) C1-4 alkoxy, b) NR6R7, c) C3-6 cycloalkyl, d) aryl or heterocycle, e) HO, f) â€”S(O)mR4, g) â€”C(O)NR6R7, or h) one or more fluorines; 2) substituted or unsubstituted aryl or substituted or unsubstituted heterocycle, 3) halogen, 4) OR6, 5) NR6R7, 6) CN, 7) NO2, 8) CF3; 9) â€”S(O)mR4, 10) â€”OS(O)2R4, 11) â€”C(O)NR6R7, 12) â€”C(O)OR6, or 13) C3-C6 cycloalkyl; m is independently 0, 1 or 2; n is 1 or 2; p is independently 0, 1, 2, 3 or 4; q is 1 or 2; r is 0 to 5; s is independently 0, 1, 2, 3 or 4; t is 2, 3, 4, 5 or 6; and u is 2, 3, 4 or 5; or a pharmaceutically acceptable salt or stereoisomer thereof.