N-Substituted aziridine-2-carboxylic acid immunostimulant derivatives

US4397848A · kind A · utility

Assignee

• Boehringer Mannheim GmbH · DE

Inventors

• Elmar Bosies · Weinheim, DE
• Wolfgang Kampe
• Max Thiel
• Uwe Bicker · Mannheim, DE
• Dietmar Boerner · Worms, DE

Key dates

• Filing date: Feb 20, 1981
• Grant date: Aug 9, 1983
• Expiry date: Feb 20, 2001

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P37/06
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, or an optionally substituted aliphatic hydrocarbon radical or cycloalkyl or cycloalkenyl radical, and R.sub.1 is a hydrogen atom or an alkyl or phenyl radical; and the pharmacologically acceptable salts thereof, in admixture with a pharmaceutical diluent or carrier. The present invention also provides, as new compounds, N-substituted aziridine-2-carboxylic acid derivatives of general formula (I') but with the proviso that when X is a carbamoyl or alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, R is not a methyl, ethyl, isopropyl or benzyl radical; and the pharmacologically acceptable salts thereof, and also provides processes for the preparation of these new compounds. Furthermore, the present invention is concerned with the use of the compounds of general formula (I') and of the pharmacologically acceptable salts thereof for combating diseases associated with a weakening of the immune system.