Mercaptoacetylamide tricyclic derivatives useful as inhibitors of enkephalinase

Claim 1

A compound of the Formula ##STR7## wherein B 1 and B 2 are each independently hydrogen; hydroxy; --OR 3 wherein R 3 is a C 1 -C 4 alkyl or an Ar-Y- group wherein Ar is phenyl or naphthyl group unsubstituted or substituted with from one to three substituents selected from the group consisting of methylenedioxy, hydroxy, C 1 -C 4 alkoxy, amino, nitro, fluoro and chloro and Y is a C 0 -C 4 alkyl; or, where B 1 and B 2 are attached to adjacent carbon atoms, B 1 and B 2 can be taken together with said adjacent carbons to form a benzene ring or methylenedioxy; R 1 is hydrogen, C 1 -C 8 alkyl, --CH 2 OCH 2 CH 2 OCH 3 or an Ar-Y- group; R 2 is hydrogen, acetyl, --CH 2 O--C(O)C(CH 3 ) 3 or benzoyl; and Z is --O--, --S--, ##STR8## or a bond wherein R 4 is hydrogen, a C 1 -C 4 alkyl or an Ar-Y- group and R 5 is --CF 3 , C 1 -C 10 alkyl or an Ar-Y- group; and the pharmaceutically acceptable salts and individual optical isomers thereof.

Claim 14

A method of inhibiting enkephalinase in a patient in need thereof comprising administering to said patient an effective enkephalinase inhibitory amount of a compound of the formula ##STR11## wherein B 1 and B 2 are each independently hydrogen; hydroxy; --OR 3 wherein R 3 is a C 1 -C 4 alkyl or an Ar-Y- group wherein Ar is phenyl or naphthyl group unsubstituted or substituted with from one to three substituents selected from the group consisting of methylenedioxy, hydroxy, C 1 -C 4 alkoxy, amino, nitro, fluoro and chloro and Y is a C 0 -C 4 alkyl; or, where B 1 and B 2 are attached to adjacent carbon atoms, B 1 and B 2 can be taken together with said adjacent carbons to form a benzene ring or methylenedioxy; R 1 is hydrogen, C 1 -C 8 alkyl, --CH 2 OCH 2 CH 2 OCH 3 or an Ar-Y- group; R 2 is hydrogen, acetyl, --CH 2 O--C(O)C(CH 3 ) 3 or benzoyl; and Z is --O--, --S--, ##STR12## or a bond wherein R 4 is hydrogen, a C 1 -C 4 alkyl or an Ar-Y- group and R 5 is --CH 3 , C 1 -C 10 alkyl or an Ar-Y- group; and the pharmaceutically acceptable salts and individual optical isomers thereof.

Claim 15

A method of inhibiting enkephalinase in a patient in need thereof comprising administering to said patient an effective enkephalinase inhibitory amount of a compound of the formula ##STR11## wherein B 1 and B 2 are each independently hydrogen; hydroxy; --OR 3 wherein R 3 is a C 1 -C 4 alkyl or an Ar-Y- group wherein Ar is phenyl or naphthyl group unsubstituted or substituted with from one to three substituents selected from the group consisting of methylenedioxy, hydroxy, C 1 -C 4 alkoxy, amino, nitro, fluoro and chloro and Y is a C 0 -C 4 alkyl; or, where B 1 and B 2 are attached to adjacent carbon atoms, B 1 and B 2 can be taken together with said adjacent carbons to form a benzene ring or methylenedioxy; R 1 is hydrogen, C 1 -C 8 alkyl, --CH 2 OCH 2 CH 2 OCH 3 or an Ar-Y- group; R 2 is hydrogen, acetyl, --CH 2 O--C(O)C(CH 3 ) 3 or benzoyl; and Z is --O--, --S--, ##STR12## or a bond wherein R 4 is hydrogen, a C 1 -C 4 alkyl or an Ar-Y- group and R 5 is --CH 3 , C 1 -C 10 alkyl or an Ar-Y- group; and the pharmaceutically acceptable salts and individual optical isomers thereof.