CA2053340C — Mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and ace

USPTO Abstract

The present invention relates to certain novel mercaptoace-tylamide derivatives of the formula: (see formulas) wherein A1 and A2 are each independently hydrogen or -COOR4 wherein R4 is hydrogen, -CH2O-C(O)C(CH3)3, a C1-C4 alkyl, an Ar-Y- group wherein Ar is aryl and Y is a C0-C4 alkyl, or diphenylmethyl, with the proviso that where A1 is hydrogen, A2 is -COOR4, and where A1 is -COOR4, A2 is hydrogen; B1 and B2 are each independently hydrogen, hydroxy, -OS5 wherein R5 is a C1-C4 alkyl or an Ar-Y- group, or where B1 and B2 are attached to adjacent carbon atoms, B1 and B2 can be taken together with said adjacent carbons to form a benzene ring or methylenedioxy; R2 is hydrogen, C1-C8 alkyl, -CH2OCH2CH2OCH3 or an Ar-Y-group; R3 is hydrogen, acetyl, -CH2O-C(O)C(CH3)3 or benzoyl; n is an integer 0 or 1; R4 is hydrogen, a C1-C4 alkyl or an Ar-Y- group, -CH2O-C(O)C(CH3)3 or diphenylmethyl; and Z is -O-, -S-, (See formulas) wherein R6 is hydrogen, a C1-C4 alkyl or an Ar-Y- group and R7 is -CF3, a C1-C10 alkyl or an Ar-Y- group;, which are useful as inhibitors of enkephalinase and ACE.