Azepine derivatives and their anti-thrombotic compositions and methods

US4414225A · kind A · utility

Assignee

• Dr. Karl Thomae GmbH · DE

Inventors

• Robert Sauter · Biberach, DE
• Gerhart Griss · Zell am Harmersbach, DE
• Wolfgang Grell · Biberach, DE
• Rudolf Hurnaus · Großenhain, DE
• Bernhard Eisele · Biberach, DE
• Walter Haarmann
• Eckhard Rupprecht · Dinkelsbühl, DE

Key dates

• Filing date: Feb 12, 1982
• Grant date: Nov 8, 1983
• Expiry date: Feb 12, 2002

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D495/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Compounds of the formula ##STR1## wherein n and m are each 1, 2 or 3, and the sum of n+m is 4; PA0 R.sub.1 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 R.sub.2 and R.sub.3 are other than both hydrogen at the same time, also hydrogen; PA0 one of R.sub.2 and R.sub.3 is hydrogen or amino, and the other is carboxyl or alkoxycarbonyl; or, when R.sub.3 is hydrogen, PA0 R.sub.2 is hydrogen; amino; alkoxycarbonyl-amino; (unsubstituted or mono-substituted phenyl)-aminocarbonyl-; (unsubstituted or mono-substituted phenyl)ethylaminocarbonyl; azidocarbonyl; or hydrazinocarbonyl; PA0 X is oxygen, sulfur or ##STR2## where R.sub.4 is hydrogen; alkyl; phenyl-alkyl; or phenyl; non-toxic, pharmacologically acceptable acid addition salts thereof; and, when R.sub.2 or R.sub.3 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.