BENZAZEPINE DERIVATIVES AS VASOPRESSIN ANTAGONISTS

摘要

The present invention is directed to novel benzoheterocyclic compounds of the formula: (see formula I) wherein R1 is H, halogen, OH, etc.; R2 is H, alkyl, halogen or alkoxy; R3 is phenyl-alkanoylamino, or (see formula II); R4 is H, -NR6R7, alkenyloxy, HO-alkyl, -O-CO-A-NR8R9, etc .; R5 is H, OH, etc., or a salt thereof. The compounds of the present invention have excellent vasopressin antagonistic activities and are useful as vasodilators; hypotensive agents, water diuretics, platelet agglutination inhibitors. The invention is also directed to a vasopressin antagonistic composition containing the novel benzoheterocyclic compounds as the active ingredient.