Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1995-01-20
1996-08-13
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
514 95, 514 99, 514114, A61K 31675, A61K 3167, A61K 31665, A61K 3166
Patent
active
055456316
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 (1950-12-01), Tawney
patent: 3184496 (1965-05-01), Baranauckas
patent: 3374288 (1968-03-01), Lange
patent: 3385822 (1968-05-01), Brown et al.
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 et al.
patent: 4322375 (1982-03-01), Maier et al.
patent: 4339443 (1982-07-01), Baillie et al.
patent: 4390690 (1983-06-01), DiGiacomo et al.
patent: 4399287 (1983-08-01), Baillie et al.
patent: 4466913 (1984-08-01), Tsuruoka et al.
patent: 4536355 (1985-08-01), Lee et al.
patent: 4618358 (1986-10-01), Maier
patent: 4656298 (1987-04-01), Dingwall et al.
patent: 4657899 (1987-04-01), Rzeszotarski
patent: 4740332 (1988-04-01), Thottathil
patent: 4772738 (1988-09-01), Dingwall et al.
patent: 4908465 (1990-03-01), Dingwall
patent: 5004826 (1991-04-01), Dingwall et al.
patent: 5013863 (1991-05-01), Baylis et al.
patent: 5051524 (1991-09-01), Baylis et al.
patent: 5064819 (1991-11-01), Baylis et al.
patent: 5243062 (1993-09-01), Dingwall et al.
patent: 5300679 (1994-04-01), Baylis et al.
patent: 5332729 (1994-07-01), Mickel et al.
patent: 5376684 (1994-12-01), Mickel
S. Trippett "New synthesis of acetylenes II. Reaction of triphenylphosphine with a-halo carbonyl compounds" Chem Abs. 57, (5946) (1962).
Annual Meeting of the Society for Neuroscience, New Orleans Nov. 10-15 (1991).
Journal of the International League Against Epilepsy, vol. 32 Supp. 3 (1991) 2 Ref's.
Walter et al "Herbicidal methylphosphinic acid derivatives" Chem Abs 97 (72585) 1982.
Gallagher et al "Organophosphorus Intermediates, VI* The Acid-Catalysed Reaction of Trialkyl Orthoformates with Phosphinic Acid" Aus. J. Chem. vol. 33, (1980) 287-94.
Cates et al "Phosphorus Analogues of .gamma.-Aminobatyric Acid a new Class of Anticonvulsant's" J Med. Chem. vol. 27 (1984) 654-659.
Dingwall et al "New Carboxylphosphonic and phosphinic acid structures of technical and biological interest" Phosphorus & Sulfur vol. 18, (1983) pp. 353-356.
Lloyd et al "Upregulation of .gamma.-Aminobutyric Acid (GABA) .beta. Binding Sites in Rat Frontal Cortex: A Common Action of Repeated Administration of Different Classes of Antidepressants and Electroshock" The Journal of Pharmacology and Experimental Therapeutics vol. 235 (1) 1985 pp. 191-199.
Liu et al "GABA.sub.b -Mediated Mechanisms in Experimental Absence Seizures" Neurology 41(Suppl) p. 151. entry 1315 (1991).
Seabrook et al "Electrophysiological characterization of potent agonists and antagonists at pre- and postsynaptic GABA.sub.B receptors on neurones in rat brain slices". Br. J. Phar. (1990) 101, 949-957.
Bernasconi Raymond
Fr ostl Wolfgang
Marescaux Christian
Mickel Stuart J.
Schmutz Markus
Ciba-Geigy Corporation
Fishman Irving M.
Jordan Kimberly
Kaiser Karen G.
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