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

Details Certain N-substituted-amino-alkane phosphinic acid derivatives h Certain N-substituted-amino-alkane phosphinic acid derivatives h

1993-05-03

1995-04-18

Rotman, Alan L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Phosphorus containing other than solely as part of an...

546 22, 558166, 562 11, 549 6, 549218, 514 95, 514 99, 514114, C07F 958, C07F 9655, A61K 31675

Patent

active

054079225

ABSTRACT:
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.

REFERENCES:
patent: 5064819 (1991-11-01), Baylis et al.
Hosford et al. Evidence that GABA.sub.B Receptors Contribute to Seizures in the "Lethargic" Moose Model of Epilepsy. Epilepsia, 32 (Suppl. 3), p. 66 (1991).
Shead et al. .gamma.-Hydroxybutyrate Model of Absence: Involvement of GABA.sub.B and G-Protein-Mediate Mechanisms. Epilepsia, 32 (Suppl. 3), pp. 66-67 (1991).

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