Ciba-Geigy Corporation

Markus Schmutz

Stuart J Mickel

Raymond Bernasconi

Christian Marescaux

Wolfgang Frostl

Cesare Mondadori

Wolfgang Fr Ostl

Compounds having GABA.sub.B -antagonistic properties, for example those of formula I ##STR1## wherein one of the radicals R.sub.1, R.sub.2 and R.sub.3 is hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another is hydrogen or, in the case of R.sub.1 or R.sub.2, hydroxy or, in the case of R.sub.1, halogen or, in the case of R.sub.2 together with R.sub.2 ', oxo, and the remaining radical is hydrogen, R.sub.1 ' is hydrogen or halogen, R.sub.2 ' is hydrogen, hydroxy or, together with R.sub.2, is oxo, R.sub.4 and R.sub.5 are hydrogen or R.sub.4 is an araliphatic or heteroarylaliphatic radical and R.sub.5 is hydrogen or an aliphatic radical, and R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical having at least 2 carbon atoms or, when R.sub.1 is hydrogen or hydroxy, R.sub.2 is an aromatic radical and R.sub.1 ', R.sub.2 ' and R.sub.3 are hydrogen. R is methyl, and their pharmaceutically acceptable salts, can be used as active ingredients in medicaments for the treatment of epilepsies of the 'petit mal' type. The invention relates also to novel compounds of formula I and processes for the preparation thereof.

N-substituted aminoalkanephosphinic acid derivatives, compositions

Compounds having GABA.sub.B -antagonistic properties, for example those of formula I ##STR1## wherein one of the radicals R.sub.1, R.sub.2 and R.sub.3 is hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another is hydrogen or, in the case of R.sub.1 or R.sub.2, hydroxy or, in the case of R.sub.1, halogen or, in the case of R.sub.2 together with R.sub.2 ', oxo, and the remaining radical is hydrogen, R.sub.1 ' is hydrogen or halogen, R.sub.2 ' is hydrogen, hydroxy or, together with R.sub.2, is oxo, R.sub.4 and R.sub.5 are hydrogen or R.sub.4 is an araliphatic or heteroarylaliphatic radical and R.sub.5 is hydrogen or an aliphatic radical, and R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical having at least 2 carbon atoms or, when R.sub.1 is hydrogen or hydroxy, R.sub.2 is an aromatic radical and R.sub.1 ', R.sub.2 ' and R.sub.3 are hydrogen, R is methyl, and their pharmaceutically acceptable salts, can be used as active ingredients in medicaments for the treatment of epilepsies of the 'petit mal' type. The invention relates also to novel compounds of formula I and processes for the preparation thereof.

Certain N-substituted-amino-alkane phosphinic acid derivatives having

The present invention relates to novel pharmaceutical compositions having antiepileptic and antineuraglic action and containing (a) at least one anticonvulsive compound of the general formula I ##STR1## wherein X.sub.1 is hydrogen, halogen having an atomic number up to 35, or is cyano, and X.sub.2 and Y together are an additional bond, or X.sub.1 and X.sub.2 together are the oxo radical, or X.sub.1 is hydroxy, X.sub.2 is hydrogen and Y is also hydrogen, and (b) at least one nootropic compound of the vincamine type which has the general formula II ##STR2## wherein Z.sub.1 is lower alkoxycarbonyl, Z.sub.2 is hydroxy and Z.sub.3 is hydrogen, or Z.sub.2 and Z.sub.3 together are an additional bond, or one of Z.sub.1 and Z.sub.2 is hydroxy and the other is hydrogen and Z.sub.3 is also hydrogen, in particular vincamine (DCI rec.), in which Z.sub.1 is methoxycarbonyl, Z.sub.2 is hydroxy and Z.sub.3 is hydrogen, and also e.g., vinpocetin (DCI rec.), in which Z.sub.1 is ethoxycarbonyl and Z.sub.2 and Z.sub.3 together form an additional bond, as well as vincanol (DCI prop.), in which one of Z.sub.1 and Z.sub.2 is hydroxy and the other is hydrogen and Z.sub.3 is hydrogen, and the acid addition salts thereof, or at least one nootropic derivative of 2-pyrrolidinone, e.g. 2-oxo-1-pyrrolidineaetamide (piracetam) or one of its nootropic derivatives. The compounds of the general formula II e.g. vincamine, as well as the nootropic derivatives of 2-pyrrolidinone, e.g. piracetam, have in themselves virtually no anticonvulsive activity but potentiate the action of the compounds of the general formula I, e.g. carbamazepine.

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Schonenbuch, Switzerland

Markus Schmutz