Patent number: 4714757
Abstract: Aminopeptidase inhibitory activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl, carboxyalkyl, halo-substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl or heteroaryl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl, (heteroaryl)alkyl, ##STR2## R.sub.4 and R.sub.5 are each independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl, or (heteroaryl)alkyl;A is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, valyl, aspartyl, prolyl, norleucyl, or norvalyl; andn is an integer of 1 to 6.
Type:
Grant
Filed:
September 18, 1985
Date of Patent:
December 22, 1987
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Eric M. Gordon, Jollie D. Godfrey, Jr., Norma G. Delaney
Patent number: 4689414
Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3 or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;R.sub.5 is hydrogen, alkyl, aryl, arylalkyl, cyano, nitro, ##STR2## Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl-(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl-(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR3## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR4## amino, or substituted amino; m is 0 or an integer of 1 to 6;n is an integer of 1 to 6; andp is an integer of 2 to 6.
Type:
Grant
Filed:
February 24, 1986
Date of Patent:
August 25, 1987
Assignee:
E. R. Squibb & Sons, Inc.
Inventor:
Karnail Atwal