Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1990-03-30
1991-11-12
Evans, J. E.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
562 11, A61K 3166, A61K 3113, A61K 31045, C07F 930
Patent
active
050648195
ABSTRACT:
Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.2 denotes hydrogen or alkyl, denotes an alkali metal or ammonium ion R.sup.6, or Z represents a protected or latent amino group Z.sup.0 and R.sup.4 denotes hydrogen or a hydroxy-protective group R.sup.5, any group R.sup.5 or R.sup.6 is replaced by hydrogen, and/or any group Z.sup.0 is converted into --NH.sub.2.
REFERENCES:
patent: 4322375 (1982-03-01), Maier et al.
patent: 4536355 (1985-08-01), Lee et al.
patent: 4618358 (1986-10-01), Maier
patent: 4656298 (1987-04-01), Dingwall et al.
Brit. J. Pharmacology, vol. 101, pp. 949-957 (1990).
Phosphorus and Sulfur, vol. 18, pp. 353-356 (1983).
Chem. Abstracts, 97:72585v (1982).
Baylis Eric K.
Bittiger Helmut
Frostl Wolfgang
Hall Roger G.
Maier Ludwig
Ciba-Geigy Corporation
Evans J. E.
Villamizar JoAnn
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