Usv Pharmaceutical Corporation

Rorer Pharmaceutical Corporation

Other

Usv Pharmaceutical Co.

Jerry W Skiles

John T Suh

Bruce E Williams

Alfred Schwab

Howard Jones

Raymond D Youssefyeh

John R Regan

Jeffrey N Barton

Bernard Loev

Paul R Menard

Fu-chih Huang

Edward S Neiss

John J Piwinski

James J Mencel

Paul Menard

Compounds of the formula ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.6, and R.sub.7 are independently hydrogen or lower alkyl.

Cyclic amides

##STR1## and pharmaceutically acceptable salts thereof, wherein: Ar is phenyl, naphthyl, heteroaryl, indole, or fused arylcycloalkyl optionally substituted with hydroxy, halo, CF.sub.3, NO.sub.2, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or aryloxy;

Aryl and heteroaryl substituted cycloalkyl compounds

This invention relates to new chemical compounds having valuable pharmaceutical activity. It particularly relates to stereoisomeric compounds possessing hypotensive activity, i.e., angiotensin converting enzyme inhibitory (ACEI) activity and having the structure ##STR1## wherein R and R.sub.9 are independently hydroxy, lower alkoxy, lower alkenoxy, di(lower alkyl)amino-lower alkoxy, hydroxy-lower alkoxy, acylamino-lower alkoxy, acryloxy-lower alkoxy, aryloxy, aryloxyl-lower alkoxy, amino, lower alkylamino, di-lower alkylamino, hydroxyamino, or aryl-lower alkylamino;

N-substituted-amido-amino acids

Compounds of the formula ##STR1## wherein R and R.sub.9 are independently hydroxy or lower alkoxy,

Compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein: Ar is phenyl, naphthyl, heteroaryl, indole, or fused arylcycloalkyl optionally substituted with hydroxy, halo, CF.sub.3, NO.sub.2, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or aryloxy;

Bisarylamines

Antihypertensive compounds of the structure ##STR1## wherein: n is an integer from 0 to 2 inclusive,

Antihypertensive lactams

Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are defined herein, which exhibit antihypertensive activity.

Antihypertensive derivatives

Carboxyalkyl dipeptide compounds

Compounds of the formula ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are as defined herein, having antihypertensive activity.

Angiotensin-converting enzyme inhibitors

This invention relates to new compounds of the formula ##STR1## wherein A is a hydroxy, lower alkoxy, lower alkenoxy, diloweralkylamino lower alkoxy, acylamino lower alkoxy, acyloxy, lower alkoxy, aryloxy, arloweralkyloxy, amino, loweralkylamino, diloweralkylamino, aryloweralkylamino, hydroxyamino, or substituted aryloxy, or substituted arloweralkoxy wherein the substituent is methyl, halo or methoxy; R.sub.1, R.sub.2, and R.sub.3 are each hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl, fused aryl-cycloalkyl, aralkyl, cycloalkyl, heterocyclic, substituted alkyl, alkenyl, or alkynyl groups in which the substituents are hydroxy, alkoxy, halo, amino, aminoalkyl, alkylamino, mercapto, or alkylmercapto, substituted cycloalkyl groups in which the substituents are alkyl, halo, haloalkyl, hydroxy, alkylamino, nitro or trifluoromethyl, and substituted aryl and heterocyclic groups in which the substituents are alkyl, hydroxy, alkoxy, hydroxyalkyl, halo, mercapto, alkylmercapto, mercaptoalkyl, haloalkyl, amino, alkylamino, aminoalkyl, nitro, methylenedioxy, or trifluoromethyl; X is hydrogen, alkyl, alkenyl or alkynyl of up to about 20 carbon atoms, aryl or aryl lower alkyl containing from about 7 to about 12 carbon atoms, heterocyclic or heterocyclic lower alkyl cycloalkyl or cycloalkylalkyl containing up to about 20 carbon atoms, or of the formula: ##STR2## wherein n=2, 3 or 4;

N-carboxy anhydride intermediates

Compounds of the structure: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl,

Blood pressure lowering n-pyridyl-, n-quinolyl-, and n-piperdyl-n-acyl

Antihypertensive N-benzimidazolyl- and N-imidazolyl-amino acid

Compounds of the formula ##STR1## wherein R and R.sub.9 are independently hydroxy and lower alkoxy,

N-Substituted-amindo-amino acids

Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substitutents are defined herein, which exhibit antihypertensive activity.

Growing community of inventors

Tuckahoe, NY, United States of America

Jerry W Skiles