Substituted caprylolactam derivatives as antihypertensives, process for preparing and pharmaceutical composition comprising them

Abstract

Abstract The invention relates to caprylolactam derivatives of the formula: wherein R and R 3 are hydroxy, lower alkoxy, lower alkenoxy, aryloxy, arloweralkoxy; hydrogen, alkyl of from 1 to 12 carbon atoms which include branched and cyclic and unsaturated alkyl groups, substituted loweralkyl wherein the substituent(s) can be halo, lower alkoxy, hydroxy, aryloxy, amino, loweralkylamino, aminoloweralkylthio, aminoloweralkoxy, diloweralkylamino, acylamino, arylamino, guanidino, phthalimido, mercapto, loweralkylthio, arylthio, carboxy, carboxamido or carboloweralkoxy, arloweralkyl, arloweralkenyl, heteroarlower alkyl or heteroarlower alkenyl, substituted arloweralkyl, or substituted heteroarlower alkyl, or substituted heteroarlower alkenyl, wherein the aryl or heteroaryl substituents are halo, dihalo, lower alkyl, hydroxy, lower alkoxy, amino, aminomethyl, phenyloxy, acylamino, diloweralkylamino, loweralkylamino, carboxyl, haloloweralkyl, acyl or aroyl; arloweralkyl or heteroarloweralkyl substituted on the alkyl portion by amino, hydroxyl or acylamino; R 2 and R are hydrogen or lower alkyl; and the pharmaceutically acceptable salts thereof and a process for preparing them. Those compounds are useful as angiotensin converting enzyme inhibitors and as antihypertensives.

Inventors

• 👤 Elbert E. Harris
• 👤 Arthur A. Patchett
• 👤 Eugene D. Thorsett

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