Azepine derivatives and their anti-thrombotic compositions and methods

摘要

Compounds of the formula <IMAGE> wherein n and m are each 1, 2 or 3, and the sum of n+m is 4; R1 is alkyl; alkenyl; unsubstituted, mono- or di-substituted aralkyl; unsubstituted, mono- or di-substituted benzoyl; alkoxycarbonyl; aralkoxycarbonyl; or, when m and n are each 2 and/or R2 and R3 are other than both hydrogen at the same time, also hydrogen; one of R2 and R3 is hydrogen or amino, and the other is carboxyl or alkoxycarbonyl; or, when R3 is hydrogen, R2 is hydrogen; amino; alkoxycarbonyl-amino; (unsubstituted or mono-substituted phenyl)-aminocarbonyl-; (unsubstituted or mono-substituted phenyl)ethylaminocarbonyl; azidocarbonyl; or hydrazinocarbonyl; X is oxygen, sulfur or <IMAGE> where R4 is hydrogen; alkyl; phenyl-alkyl; or phenyl; non-toxic, pharmacologically acceptable acid addition salts thereof; and, when R2 or R3 is carboxyl, non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as antithrombotics.