Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1991-06-20
1993-07-20
Rotman, Alan L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
558166, 562 11, 546 89, 514 89, A61K 3166, C07F 938, C07F 930, C07F 958
Patent
active
052293793
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: 2535175 (1949-05-01), Tawney
patent: 3184496 (1965-05-01), Baranavckas
patent: 3374288 (1968-03-01), Lange
patent: 3385822 (1968-03-01), Brown
patent: 3493639 (1970-02-01), Tavs
patent: 3637763 (1972-01-01), Firestone
patent: 3784590 (1974-01-01), Firestone
patent: 3812221 (1974-05-01), Braden
patent: 3970586 (1976-07-01), Schliebs
patent: 4064163 (1977-12-01), Drach
patent: 4322375 (1982-03-01), Maier
patent: 4390690 (1983-06-01), DiGiacamo
patent: 4399287 (1983-08-01), Baillie
patent: 4466913 (1984-08-01), Tsuruoka
patent: 4536355 (1985-08-01), Lee
patent: 4618358 (1986-10-01), Maier
patent: 4656298 (1987-04-01), Dingwall
patent: 4657899 (1987-04-01), Rzeszotarski
patent: 4740322 (1988-04-01), Thottathil
patent: 4772738 (1988-09-01), Dingwall
patent: 4908465 (1990-03-01), Dingwall
patent: 5004826 (1991-04-01), Dingwall
patent: 5013863 (1991-05-01), Baylis
patent: 5051524 (1991-09-01), Baylis
Neurology 41 (Supp. 1) 151, Abs. 1315 (1991).
Aust. J. Chem. 33, 292 (1980).
Br. J. Pharm. 101, 949.
Chem. Abs. 57, 5946 (1962).
Chem. Abs. 97, 92585v (1982).
J. Med. Chem. 27, 654 (1984).
J. Pharma and Experimental Ther. 235(1) (1985).
Bernasconi Raymond
Frostl Wolfgang
Marescaux Christian
Mickel Stuart J.
Schmutz Markus
Ciba-Geigy Corporation
Fishman Irving M.
Ikeler Barbara J.
Kaiser Karen G.
Rotman Alan L.
LandOfFree
Certain N-substituted-amino-alkane phosphinic acid derivatives h does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Certain N-substituted-amino-alkane phosphinic acid derivatives h, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Certain N-substituted-amino-alkane phosphinic acid derivatives h will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1760629