C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/385, 260/337
C07D 203/22 (2006.01) C07D 403/12 (2006.01)
Patent
CA 1148962
ABSTRACT The present invention provides pharmaceutical compositions containing N-substituted aziridine-2- carboxylic acid derivatives of the general formula:- Image (I') wherein X is a carboxyl, a nitrile, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, an aliphatic hydrocarbon radical which is saturated or can contain one or more unsatur- ations and can be substituted one or more times by halogen, alkoxy, hydroxyl, dialkylamino, dialkylaminoxy, cycloalkylamino, acylamino, acyl, nitro, alkylthio, alkylsulphinyl, alkylsulphonyl, nitrilo, carboxyl, alkoxycarbonyl or carbamoyl or by cycloalkyl or cyclo- alkenyl radicals optionally carrying alkyl, alkoxy or alkoxycarbonyl radicals, optionally interrupted by hetero atoms and optionally bridged, or by an aryl, hetaryl, aryloxy, arylthio, acyloxy, alkoxycarbonylamino, or isothioureido radical, or R is a cycloalkyl or cyclo- alkenyl radical optionally substituted by alkyl, alkoxy or oxo groups, optionally interrupted by hetero atoms and optionally bridged, or is an aryl or hetaryl radical which can be substituted one or more times by halogen, alkoxy, alkyl, hydroxyl, alkoxycarbonyl, carbamoyl, dialkylamino, cycloalkylamino, acylamino, nitro, cyano, acyl, alkylthio, alkylsulphinyl, alkyl- sulphonyl, sulphamoyl, phenyl, trifluoromethyl, aryloxy, acyloxy or methylenedioxy radicals and R1 is a hydrogen atom or an alkyl or phenyl radical; and the pharma- cologically 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 R1 is a hydrogen atom, R is not a methyl, ethyl, iso- propyl 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.
345886
Bicker Uwe
Boerner Dietmar
Bosies Elmar
Kampe Wolfgang
Thiel Max
Boehringer Mannheim G.m.b.h.
Sherman
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