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Home Vasodialators Substituted-aminoalkylphosphinic-acids

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 Substituted aminoalkylphosphinic acids

Details
Inventors: Hall, Roger G.; Maier, Ludwig; Frostl, Wolfgang;
Assignee: Ciba-Geigy Corporation (Ardsley, NY)
Primary Examiner: Dees; Jose G.
Assistant Examiner: Frazier; Barbara S.
Attorney, Agent or Firm: Fishman; Irving M., Kaiser; Karen G.

P-substituted aminoalkylphosphinic acids of the formula ##STR1## wherein R denotes an optionally fluorinated methyl group, R.sub.1 denotes hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen or a fluorinated methyl group and R.sub.2 and R.sub.3 denote hydrogen or R.sub.2 denotes hydroxy, lower alkoxy or halogen and R.sub.3 is hydrogen or R.sub.2 and R.sub.3 together represent an oxo group, and their pharmaceutically acceptable salts are active as GABA.sub.b -agonists and can be used in the treatment of spinal spasticity, multiple sclerosis and cerebral palsy, trigeminus neuralgia, drug withdrawal syndromes and/or conditions of pain. They can be manufactured by methods known per se and suitable such methods are described.

DETAILED DESCRIPTION We claim: 1.
A method of treatment of spinal spasticity, multiple sclerosis, cerebral palsy, trigeminus neuralgia, drug withdrawal syndromes and/or conditions of pain, wherein a GABA.
sub.
B agonistic effective amount of a P-substituted aminoalkylphosphinic acid of the formula ##STR27## wherein R denotes an optionally fluorinated methyl group, R.
sub.
1 denotes hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen or a fluorinated methyl group and R.
sub.
2 and R.
sub.
3 denote hydrogen or R.
sub.
2 denotes hydroxy, lower alkoxy or halogen and R.
sub.
3 is hydrogen or R.
sub.
2 and R.
sub.
3 together represent an oxo group, or a pharmaceutically acceptable salt thereof, is administered to a warm-blooded organism in need of such treatment.
2.
A method of treatment of spinal spasticity, multiple sclerosis and/or cerebral palsy, wherein a muscle relaxant effective amount of a P-substituted aminoalkylphosphinic acid of the formula ##STR28## wherein R denotes an optionally fluorinated methyl group, R.
sub.
1 denotes hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen or a fluorinated methyl group and R.
sub.
2 and R.
sub.
3 denote hydrogen or R.
sub.
2 denoted hydroxy, lower alkoxy or halogen and R.
sub.
3 is hydrogen or R.
sub.
2 and R.
sub.
3 together represent an oxo group, or a pharmaceutically acceptable salt thereof, is administered to a warm-blooded organism in need of such muscle-relaxant treatment.
3.
A method of treatment of trigeminus neuralgia drug withdrawal syndromes and/or conditions of pain, wherein an analgesic effective amount of a P-substituted aminoalkylphosphinic acid of the formula ##STR29## wherein R denotes an optionally fluorinated methyl group, R.
sub.
1 denotes hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen or a fluorinated methyl group and R.
sub.
2 and R.
sub.
3 denote hydrogen or R.
sub.
2 denotes hydroxy, lower alkoxy or halogen and R.
sub.
3 is hydrogen or R.
sub.
2 and R.
sub.
3 together represent an oxo group, or a pharmaceutically acceptable salt thereof, is administered to a warm-blooded organism in need of such analgesic treatment



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