Mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and ACE
AssigneeMerrell Dow Pharmaceuticals Inc.
InventorsGary A. Flynn, Philippe Bey, Alan M. Warshawsky, Douglas W. Beight, Shujaath Mehdi, Eugene L. Giroux, Timothy P. Burkholder, Edward D. Daugs, John F. French
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Abstract
The present invention relates to certain novel mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and of ACE.
Claims2
A composition comprising an assayable amount of a compound of the formula ##STR12## wherein A.sub.1 and A.sub.2 are each independently hydrogen or --COOR.sub.4 wherein R.sub.4 is hydrogen;
- --CH.sub.2 O--C(O)C(CH.sub.3).sub.3 ;
- a C.sub.1 -C.sub.4 alkyl;
- an Ar--Y-- group wherein Ar is phenyl or naphtyl group unsubstituted or substituted with from one to three substituents selected from the group consisting of methylenedioxy, hydroxy, C.sub.1 -C.sub.4 alkoxy, fluoro and chloro and Y is a C.sub.0 -C.sub.4 alkyl;
- or diphenylmethyl;
- with the proviso that where A.sub.1 is hydrogen, A.sub.2 is --COOR.sub.4, and where A.sub.1 is --COOR.sub.4, A.sub.2 is hydrogen;
- B.sub.1 and B.sub.2 are each independently hydrogen;
- hydroxy;
- --OR.sub.5 wherein R.sub.5 is a C.sub.1 -C.sub.4 alkyl or an Ar--Y-- group;
- or, where B.sub.1 and B.sub.2 are attached to adjacent carbon atoms, B.sub.1 and B.sub.2 can be taken together with said adjacent carbons to form a benzene ring or methylenedioxy;
- R.sub.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, --CH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 or an Ar--Y-- group;
- R.sub.3 is hydrogen, acetyl, --CH.sub.2 O--C(O)C(CH.sub.3).sub.3 or benzoyl;
- and
- n is an integer 0 or 1;
- in admixture or otherwise in association with an inert carrier.
A pharmaceutical composition comprising an effective immunosuppressive amount of a compound of the formula ##STR13## wherein B.sub.1 and B.sub.2 are each independently hydrogen;
- hydroxy;
- --OR.sub.5 wherein R.sub.5 is a C.sub.1 -C.sub.4 alkyl or an Ar--Y-- group wherein Ar is phenyl or naphtyl group unsubstituted or substituted with from one to three substituents selected from the group consisting of methylenedioxy, hydroxy, C.sub.1 -C.sub.4 alkoxy, fluoro and chloro and Y is a C.sub.0 -C.sub.4 alkyl;
- or, where B.sub.1 and B.sub.2 are attached to adjacent carbon atoms, B.sub.1 and B.sub.2 can be taken together with said adjacent carbons to form a benzene ring or methylenedioxy;
- R.sub.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, CH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 or an Ar--Y-- group;
- R.sub.3 is hydrogen, acetyl, --CH.sub.2 O--C(O)C(CH.sub.3).sub.3 or benzoyl;
- R.sub.4 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar--Y-- group, --CH.sub.2 O--C(O)C(CH.sub.3).sub.3 or diphenylmethyl;
- and ##STR14## wherein R.sub.6 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar--Y-- group and R.sub.7 is --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar--Y-- group.
- in admixture or otherwise in association with an inert carrier.
Dependencies are inferred from the claim text.