Organic compounds -- part of the class 532-570 series – Organic compounds – Phosphorus acids or salts thereof
Patent
1989-07-12
1991-05-07
Evans, J. E.
Organic compounds -- part of the class 532-570 series
Organic compounds
Phosphorus acids or salts thereof
C07F 930, A61K 3166, A61K 3113, A61K 31045
Patent
active
050138634
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, 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 deontes 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: 4536355 (1985-08-01), Lee et al.
patent: 4618358 (1986-10-01), Maier
patent: 4656298 (1987-04-01), Dingwall et al.
Dingwall, Phosphorus and Sulfur, vol. 18, pp. 353-356, (1983).
Chem. Abstr. 97: 72585v (1982).
Lloyd et al., J. of Pharmacology and Experimental Therapeutics, vol. 235, No. 1 (1985).
Baylis Eric K.
Bittiger Helmut
Froostl Wolfgang
Hall Roger G.
Maier Ludwig
Ciba-Geigy Corporation
Evans J. E.
Villamizar JoAnn
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