Substituted enantholactam derivatives as antihypertensives, a process for preparing and a pharmaceutical composition containing them, and intermediates.

摘要

The invention relates to enantholactam derivatives of the formula <CHEM> wherein R and R<4> are hydroxy, lower alkoxy, lower alkenoxy, aryloxy, diloweralkylamino lower alkoxy, hydroxy, dihydroxy, and acylamino substituted lower alkoxy, acyloxy lower alkoxy, arloweralkoxy, amino, hydroxyamino; R<1> is hydrogen, alkyl of from 1 to 12 carbon atoms which include branched and cyclic and unsaturated alkyl groups, substituted loweralkyl, arloweralkyl, arloweralkenyl, heteroarlower alkyl or heteroarlower alkenyl, substituted arloweralkyl, or substituted heteroarlower alkyl, or substituted heteroarlower alkenyl, wherein the aryl or heteroaryl portion is substituted, substituted arloweralkyl or substituted heteroarloweralkyl wherein the alkyl portion can be substituted, R<3> is hydrogen, lower alkyl, phenyl, substituted lower alkyl; and R<2> is hydrogen, lower alkyl, cycloalkyl, aminoalkyl, hydroxyalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, or heterocycloalkyl, or substituted aryl. The compounds are useful as angiotensin converting enzyme inhibitors and antihypertensives. The invention relates also to a process for preparing these compounds.