NMDA-blocking pharmaceutical compositions

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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A61K 3135

Patent

active

052848671

ABSTRACT:
The use of a compound of the formula: ##STR1## having the (3S,4S) configuration, and which is essentially free of the (3R,4R) enantiomer, wherein A--B designates a 1(2) or a 6(1) double bond, R designates --CH.sub.3 or --CH.sub.2 OH, R.sup.1 designates a hydrogen atom or a lower acyl group, and R.sup.2 designates (A) a straight-chained or branched C.sub.6-12 alkyl radical; or (B) a group --O--R.sup.3, in which R.sup.3 is a straight-chained or branched C.sub.5-9 alkyl radical or a straight-chained or branched alkyl radical substituted at the terminal carbon atom by a phenyl group in the manufacture of a medicament for reducing or preventing glutamate neurotoxicity. Some of the above compounds are novel, and their preparation is described. Also described is a method of treating acute injuries to the central nervous system associated with excitatory amino acid neurotoxicity, a method of treating chronic degenerative disease associated with gradual selective neuronal loss and a method of treating poisonings affecting the central nervous system by administering a pharmaceutical composition containing the above compound.

REFERENCES:
patent: 4133819 (1979-01-01), Johnson
patent: 4179517 (1979-12-01), Mechoulam et al.
patent: 4209520 (1980-06-01), Johnson
patent: 4876276 (1989-10-01), Mechoulam et al.
Mechoulam et al., Tetrahedron Asymmetry 1: 315-319 (1990).
Choi, Neuron 1: 623-624 (1988).
Kloog et al., Biochemistry 27: 843-848 (1988).
Mechoulam et al., Experientia 44: 762-764 (1988).
Feigenbaum et al., Pharmacol. Biochem. Behav. 16: 235-240 (1982).

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