E. R. Squibb Sons, Inc.

Squibb & Sons, Inc.

Das, Jagabandhu

Floyd, David M.

Krapcho, John

John Krapcho

Chester F Turk

Joseph Schwartz

Peter C Wade

David M Floyd

Joel C Barrish

George C Rovnyak

Spencer David Kimball

Jagabandhu Das

Eric M Gordon

Miguel A Ondetti

Edward W Petrillo, Jr

Peter W Sprague

John T Hunt

Gary J Grover

James L Bergey

Edward W Petrillo

David Mack Floyd

A novel pharmaceutical composition and method is disclosed for the treatment of cardiovascular diseases, e.g. myocardial ischemia and/or arrhythmia. The method and composition include an effective amount of a compound of the formula ##STR1## wherein X, Y, R, R.sub.1, A, A', m, n, p, p' and B are as defined herein.

Pharmaceutical composition and method for treating cardiovascular

This process enables preparation of the preferred (+)-threo enantiomer by resolution of its racemic mixture of a compound of the formula ##STR1## wherein Y.sup.1 and Y.sup.2 are each independently lower alkyl and R.sup.1 is hydrogen or lower alkyl. The compound is treated with a chiral acid (tartaric aicd preferred) in an organic solvent (ethanol preferred) to yield the (+)-threo enantiomer, which is then recovered from the reaction mixture. This enantiomer may then be used to produce the preferred (+)-cis enantiomer of certain benzothiazepine cardiovascular agents.

Process for resolving chiral intermediates used in making calcium

Novel compounds of the formula ##STR1## exhibit calcium channel blocking activity and are useful as cardiovascular agents.

Benzazepine derivatives

Vasodilating activity is exhibited by compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein X is --CH.sub.2 -- or --S--;

Benzazepine and benzothiazepine derivatives

Vasodilating activity is exhibited by compounds having the formula ##STR1## wherein X can be --S--or --CH.sub.2 --; and

Vasodilating activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof.

Spiro compounds of the formula ##STR1## wherein X is oxygen or sulfur. These compounds possess antgiotensin converting enzyme inhibition activity and are thus useful as anti-hypertension agents.

Acylmercaptoalkanoyl and mercaptoalkanoyl spiro compounds

Vasodilating activity is exhibited by compounds having the formula ##STR1## n is 2 or 3; X is oxygen or sulfur;

Benzothiazepine derivatives

Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids are useful for the treatment of hypertension.

Imido, amido and amino derivatives of mercaptoacyl prolines and

Compounds of the formula ##STR1## are useful as intermediates in the preparation of various hypotensive agents.

Certain-4-hydroxy-proline derivatives

Hypotensive activity is exhibited by compounds having the formula ##STR1## and salts thereof wherein R.sub.1 is alkyl, aryl, arylalkyl, cycloalkyl, or cycloalkylalkyl;

Esters of phosphinylalkanoyl substituted prolines

Carboxyalkyl dipeptides of the formula ##STR1## wherein R.sub.4 is a 3-, 4-, 5-, or 4,4-substituted proline are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity.

Growing community of inventors

Somerset, NJ, United States of America

John Krapcho