Patent ID: 6492358
Filing Date: 2002-12-10
Classification: A61P,C07D

Abstract:
A compound of the formula (I): whereinR1 is independently selected from the group consisting of halogen, nitro, hydroxy, C1-C8alkyl, C1-C8alkoxy, â€”NH2, â€”NHRA, â€”N(RA)2, â€”Oâ€”RA, â€”C(O)NH2, â€”C(O)NHRA, â€”C(O)N(RA)2, â€”NC(O)â€”RA, â€”SO2NHRA, â€”SO2N(RA)2, phenyl (optionally substituted with 1 to 3 RB) and heteroaryl (optionally substituted with 1 to 3 RB); where each RA is independently is independently selected from the group consisting of C1-C8alkyl, aryl (optionally substituted with 1 to 3 RB), C1-C8aralkyl (optionally substituted with 1 to 3 RB) and heteroaryl (optionally substituted with 1 to 3 RB); where each RB is independently selected from the group consisting of halogen, hydroxy, nitro, cyano, C1-C8alkyl, C1-C8alkoxy, C1-C8alkoxycarbonyl, carboxy C1-C8alkyl, C1-C8alkylsulfonyl, trifluoromethyl, trifluoromethoxy, amino, acetylamino, di(C1-C8alkyl)amino, di(C1-C8alkyl)amino C1-C8alkoxy, di(C1-C8alkyl) aminoacetyl C1-C8alkyl, di(C1-C8alkyl)aminoacetylamino, carboxyC1-C8alkylcarbonylamino, hydroxyC1-C8alkylamino, NHRA, N(RA)2 and heterocycloalkylC1-C8alkoxy; n is an integer from 0 to 4; X is NRD; where RD is selected from the group consisting of hydrogen, hydroxy, â€”ORA, C1-C8alkyl (wherein the alkyl is optionally substituted with one to three substituent independently selected from halogen, carboxy, amino, C1-C8alkylamino, di(C1-C8alkyl)amino, C1-C8alkoxycarbonyl, heteroaryl or heterocycloalkyl), heteroaryl and heteroarylcarbonyl (wherein the heteroaryl may be optionally substituted with phenyl or substituted phenyl, where the phenyl substituents are one to three RB); R2 is selected from the group consisting of C5-C10alkyl (optionally substituted with 1 to 3 RC), aryl (optionally substituted with 1 to 3 RB), heteroaryl (optionally substituted with 1 to 3 RB) and heterocycloalkyl (optionally substituted with 1 to 3 RB); where each RC is independently selected from the group consisting of halogen, hydroxy, nitro, NH2, NHRA and N(RA)2; Z is selected from the group consisting of CH2, CHOH and C(O); provided that when Z is CHOH or C(O), then X is NH; R4 is selected from the group consisting of hydrogen, hydroxy, carboxy, C1-C6alkylcarbonyl, C1-C6alkoxylcarbonyl, di(C1-C8alkyl)aminoalkoxycarbonyl, di(C1-C8alkyl)amino C1-C8alkylaminocarbonyl, and â€”CORF; where RF is selected from the group consisting of C1-C8alkyl, NH2, NHRA, NRA2, â€”C1-C8alkylâ€”NH2, â€”C1-C8alkylâ€”NHRA, â€”C1-C8alkylâ€”NRA2 and â€”NHâ€”C1-C8alkylâ€”NRA2; a is an integer from 0 to 1; Y is selected from the group consisting of CH2, C(O), C(O)O, C(O)â€”NH and SO2; is selected from the group consisting of naphthyl and heteroaryl; m is an integer from 0 to 2; R3 is independently selected from the group consisting of halogen, nitro, C1-C8alkyl, C1-C8alkoxy, trifluoromethyl, trifluoromethoxy, phenyl (optionally substituted with 1 to 3 RB), phenylsulfonyl, naphthyl, C1-C8aralkyl, heteroaryl (optionally substituted with 1 to 3 RB), NH2, NHRA and N(RA)2; provided that when is 2-furyl or 2-thienyl, then m is an integer from 1 to 2; and pharmaceutically acceptable salts thereof.