Cyclic amino acid derivatives

Details Cyclic amino acid derivatives Cyclic amino acid derivatives

1994-06-22

1996-04-09

Ivy, C. Warren

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546326, 549 77, 549 76, 562426, 562427, 562503, 562504, 562505, 562506, 562507, 514438, 514562, A61K 3144, A61K 31195, C07C23582, C07D21382

Patent

active

055062440

ABSTRACT:
Disclosed are the compounds of formula I ##STR1## wherein R represents hydrogen, lower alkyl, carbocyclic or heterocyclic aryl-lower alkyl or cycloalkyl-lower alkyl; R.sub.1 represents hydrogen, lower alkyl, cycloalkyl, carbocyclic aryl or heterocyclic aryl, or biaryl; R.sub.3 represents hydrogen or acyl; R.sub.4 represents hydrogen, lower alkyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, biaryl or biaryl-lower alkyl; R.sub.5 represents hydrogen or lower alkyl; or R.sub.4 and R.sub.5 together with the carbon atom to which they are attached represent cycloalkylidene or benzo-fused cycloalkylidene; A together with the carbon atom to which it is attached represents 3 to 10 membered cycloalkylidene or 5 to 10 membered cycloalkenylidene radical which may be substituted by lower alkyl or aryl-lower alkyl or may be fused to a saturated or unsaturated carbocyclic 5-7-membered ring; or A together with the carbon to which it is attached represents 5 or 6 membered oxacycloalkylidene, thiacycloalkylidene or azacycloalkylidene optionally substituted by lower alkyl or aryl-lower alkyl; or A together with the carbon atom to which it is attached represents 2,2-norbornylidene; m is 0, 1, 2 or 3; and COOR.sub.2 represents carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester, disulfide derivatives derived from said compounds wherein R.sub.3 is hydrogen; and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for preparation of said compounds; intermediates; and methods of treating disorders in mammals which are responsive to ACE and NEP inhibition by administration of said compounds to mammals in need of such treatment.

REFERENCES:
patent: 4093739 (1978-06-01), Martin
patent: 4132803 (1979-01-01), Martin
patent: 5208236 (1993-05-01), Neustadt
J. Med. Chem. 1985, 28, 910-914 Martin et al.

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