Mercaptoacetylamide derivatives useful as inhibitors of...

Details Mercaptoacetylamide derivatives useful as inhibitors of... Mercaptoacetylamide derivatives useful as inhibitors of...

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) A61K 31/55 (2006.01) C07D 487/04 (2006.01) C07D 491/147 (2006.01) C07D 498/04 (2006.01) C07D 498/14 (2006.01) C07D 513/04 (2006.01) C07D 513/14 (2006.01) C07K 5/078 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2053340

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.

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