C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/385, 260/337
C07D 203/06 (2006.01) C07D 403/00 (2006.01)
Patent
CA 1142530
ABSTRACT The present invention provides pharmaceutical compositions containing at least one aziridine-2- carboxylic acid derivative which is substituted on the ring nitrogen atom and which have the general formula:- Image (I). wherein X is a carboxyl or nitrile group or an alkoxy- carbonyl radical or an unsubstituted or substituted carbamoyl group; R is a straight-chained or branched, saturated or mono-or polyunsaturated aliphatic hydro- carbon radical which is optionally substituted one or more times by halogen, alkoxy, hydroxyl, dialkylamino, cycloalkylamino, acylamino, acyl, nitro, alkylthio, alkylsulphinyl, alkylsulphonyl, nitrile, carbalkoxy or carbamoyl radicals or by cycloalkyl radicals optionally substituted by alkyl, alkoxy or carbalkoxy, or by cyclo- alkenyl radicals, which can optionally be bridged, or by an aliphatic or aromatic heterocyclic radical, by aryl, aryloxy, arylthio, acyloxy, alkoxy- carbonylamino or ureido groups, or R is a cycloalkyl or cycloalkenyl radical containing 3 to 10 carbon atoms which is optionally substituted by alkyl, alkoxy, alkoxycarbonyl or oxo groups and is also optionally interrupted by hetero atoms and optionally bridged by 1 to 3 carbon atoms, or R is an aryl or hetaryl radical, the aryl and hetaryl radicals being optionally substituted by halogen, alkoxy, alkyl, hydroxyl, carbalkoxy, carbamoyl. dialkylamino, cycloalkylamino, acylamino, nitro, cyano, acyl, alkylthio, alkylsulphinyl, alkylsulphonyl, sulphamoyl, phenyl, trifluoromethyl, aryloxy, acyloxy or methylene- dioxy, and R1 is a hydrogen atom or a saturated, straight-chain or branched alkyl radical containing up to 4 carbon atoms or a phenyl radical; or a pharmaceutically acceptable, pharmacologically compatible salt thereof some of the derivatives are novel and some are known; the derivatives are immune-stimulating therapeutic compounds of increased effectiveness, low toxicity while displaying no noteworthy side effects and being more stable and more simply administered than previously employed aziridines.
332281
Berger Herbert
Bicker Uwe
Bosies Elmar
Grafe Alfred
Kampe Wolfgang
Boehringer Mannheim G.m.b.h.
Swabey Ogilvy Renault
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