Carboxyalkyl derivatives useful as inhibitors of enkephalinase a

Details Carboxyalkyl derivatives useful as inhibitors of enkephalinase a Carboxyalkyl derivatives useful as inhibitors of enkephalinase a

1994-12-01

1995-12-05

Henley, III, Raymond

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

A61K 3155

Patent

active

054729599

ABSTRACT:
The invention relates to compounds of the formula ##STR1## wherein B.sub.1 and B.sub.2 are each independently hydrogen; hydroxy; --OR.sub.2 wherein R.sub.2 is a C.sub.1 -C.sub.4 alkyl or an Ar--Y group wherein Ar is aryl and Y is a hydrogen or C.sub.1 -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;
A is a bond, methylene or oxygen, sulfur, NR.sub.4 or NCOR.sub.5 wherein R.sub.4 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar--Y-- group and R.sub.5 is --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar--Y-- group; R.sub.3 is hydrogen or --CH.sub.2 OC(O)C(CH.sub.3).sub.3 ; R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or --CH.sub.2 OC(O)--C(CH.sub.3).sub.3 ; and n is an integer 1 to 3,
that are useful as inhibitors of enkephalinase and ACE.

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