Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1983-05-17
1985-05-14
Berch, Mark L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
548263, 548264, 260239E, 548265, 548266, 2603303, 548267, 548268, 2603309, 548269, 548323, 544153, 548324, 548374, 544155, 548336, 514241, 544156, 514252, 514256, 544157, 514266, 514314, 544174, 514340, 514359, 544175, 514365, 514406, 544176, 514444, 514459, 544182, 544234, 544235, 544238, 544251, 544255, 546 48, 546 65, 546 90, 546115, 546116, 546183, 548153, 548183, 548184, 548185, 548187, 548189, 548209, 548210, 548213, 548214, 514461, 514469, C07D20322, C07D40112, C07D40312, A61K 31395
Patent
active
045171831
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, an aliphatic hydrocarbon radical which is saturated or can contain one or more unsaturations and can be substituted one or more times by halogen, alkoxy, hydroxyl, dialkylamino, dialkylaminoxy, cycloalkylamino, acylamino, acyl, nitro, alkylthio, alkylsulphinyl, alkylsulphonyl, cyano, carboxyl, alkoxycarbonyl or carbamoyl or by cycloalkyl or cycloalkenyl 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 cycloalkenyl 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, alkylsulphonyl, sulphamoyl, phenyl, trifluoromethyl, aryloxy, acyloxy or methylenedioxy radicals 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.
REFERENCES:
Bosies, Chem. Abs. 94, 15542t, (1980).
Kostyanovskii 85, 192460, (1976).
Kostyanovskii 81, 25474, (1974).
Kostyanovskii 87, 101491, (1977).
Bicker Uwe
Boerner Dietmar
Bosies Elmar
Kampe Wolfgang
Thiel Max
Berch Mark L.
Boehringer Mannheim GmbH
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