Patent ID: 6627754
Filing Date: 2003-09-30
Classification: A61K,A61P,C07D

Abstract:
A compound of the formula or the pharmaceutically acceptable salt thereof; whereinR1 is a group of the formula wherein y is 0, 1 or 2;R4 is selected from the group consisting of hydrogen, (C1-C6)alkyl, (C1-C6)alkylsulfonyl, (C2-C6)alkenyl, (C2-C6)alkynyl wherein the alkyl, alkenyl and alkynyl groups are optionally substituted by deuterium, hydroxy, amino, trifluoromethyl, (C1-C4)alkoxy, (C1-C6)acyloxy, (C1-C6)alkylamino, ((C1-C6)alkyl)2amino, cyano, nitro, (C2-C6)alkenyl, (C2-C6)alkynyl or (C1-C6)acylamino; or R4 is (C3-C10)cycloalkyl wherein the cycloalkyl group is optionally substituted by deuterium, hydroxy, amino, trifluoromethyl, (C1-C6)acyloxy, (C1-C6)acylamino, (C1-C6)alkylamino, ((C1-C6)alkyl)2amino, cyano, cyano(C1-C6)alkyl trifluoromethyl(C1-C6)alkyl, nitro, nitro(C1-C6)alkyl or (C1-C6) acylamino; R5 is a piperidinyl substituted by one to five carboxy, cyano, amino, deuterium, hydroxy, (C1-C6)alkyl, (C1-C6)alkoxy, halo, (C1-C6)acyl, (C1-C6)alkylamino, amino((C1-C6)alkyl, (C1-C6)alkoxy-COâ€”NH, (C1-C6)alkylamino-COâ€”, (C2-C6)alkenyl, (C2-C6) alkynyl, (C1-C6)alkylamino, amino(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy((C1-C6)alkyl, (C1-C6)acyloxy((C1-C6)alkyl, nitro, cyano(C1-C6)alkyl, halo(C1-C6)alkyl, nitro((C1-C6)alkyl, trifluoromethyl, trifluoromethyl(C1-C6)alkyl, (C1-C6)acylamino, (C1-C6)acylamino((C1-C6)alkyl, (C1-C6)alkoxy(C1-C6)acylamino, amino(C1-C6)acyl, amino((C1-C6)acyl((C1-C6)alkyl, (C1-C6)alkylamino(C1-C6)acyl, ((C1-C6)alkyl)2amino(C1-C6)acyl, R15R16Nâ€”COâ€”Oâ€”, R15R16Nâ€”COâ€”(C1-C6)alkyl, (C1-C6)alkyl-S(O)m, R15R16NS(O)m, R15R16NS(O)m (C1-C6)alkyl, R15S(O)m R16N, R15S(O)mR16N(C1-C6)alkyl wherein m is 0, 1 or 2 and R15 and R16 are each independently selected from hydrogen or (C1-C6)alkyl; or a group of the formula wherein a is 0, 1, 2, 3 or 4;b, c, e, f and g are each independently 0 or 1;d is 0, 1, 2, or 3;X is S(O)n wherein n is 0, 1 or 2; oxygen, carbonyl or â€”C(&boxH;N-cyano)-;Y is S(O)n wherein n is 0, 1 or 2; or carbonyl; andZ is carbonyl, C(O)Oâ€”, C(O)NRâ€” or S(O)n wherein n is 0, 1 or 2;R6, R7, R8, R9, R10 and R11 are each independently selected from the group consisting of hydrogen or (C1-C6)alkyl optionally substituted by deuterium, hydroxy, amino, trifluoromethyl, (C1-C6)acyloxy, (C1-C6)acylamino, (C1-C6)alkylamino, ((C1-C6)alkyl)2amino, cyano, cyano(C1-C6)alkyl, trifluoromethyl(C1-C6)alkyl, nitro, nitro(C1-C6)alkyl or (C1-C6)acylamino; R12 is carboxy, cyano, amino, oxo, deuterium, hydroxy, trifluoromethyl, (C1-C6)alkyl, trifluoromethyl(C1-C6)alkyl, (C1-C6)alkoxy, halo, (C1-C6)acyl, (C1-C6)alkylamino, ((C1-C6)alkyl)2 amino, amino(C1-C6)alkyl, (C1-C6)alkoxy-COâ€”NH, (C1-C6)alkylamino-COâ€”, (C2-C6)alkenyl, (C2-C6) alkynyl, (C1-C6)alkylamino, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy(C1-C6)alkyl, (C1-C6)acyloxy((C1-C6)alkyl, nitro, cyano(C1-C6)alkyl, halo(C1-C6)alkyl, nitro((C1-C6)alkyl, trifluoromethyl, trifluoromethyl(C1-C6)alkyl, (C1-C6)acylamino, (C1-C6)acylamino(C1-C6)alkyl, (C1-C6)alkoxy(C1-C6)acylamino, amino((C1-C6)acyl, amino((C1-C6)acyl((C1-C6)alkyl, (C1-C6)alkylamino(C1-C6)acyl, ((C1-C6)alkyl)2amino(C1-C6)acyl, R15R16Nâ€”COâ€”Oâ€”, R15R16Nâ€”COâ€”(C1-C6)alkyl, R15C(O)NH, R15OC(O)NH, R15NHC(O)NH, (C1-C6)alkyl-S(O)m, (C1-C6)alkyl-S(O)mâ€”(C1-C6)alkyl, R15R16NS(O)m, R15R16NS(O)m (C1-C6)alkyl, R15S(O)mR16N, R15S(O)mR16N(C1-C6)alkyl wherein m is 0, 1 or 2 and R15 and R16 are each independently selected from hydrogen or (C1-C6)alkyl; R2 and R3 are each hydrogen.