Non-heterocyclic .beta.-phenyl-.alpha.-aminopropionic acid n-phe

Details Non-heterocyclic .beta.-phenyl-.alpha.-aminopropionic acid n-phe Non-heterocyclic .beta.-phenyl-.alpha.-aminopropionic acid n-phe

1998-10-13

2000-09-05

McKane, Joseph

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

560 27, 560 37, 564157, 564182, 514563, 514616, 514620, 558414, A61K 31275, A61K 31165, C07C22936, C07C23304

Patent

active

061143812

ABSTRACT:
Compounds, compositions and methods of treatment are described to control brain damage associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a .beta.-phenyl-.alpha.-aminopropionic acid N phenyl amide compound as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.5 is independently selected from hydrido, fluoro, chloro, bromo, methyl and ethyl; wherein R.sup.3 is selected from hydroxy, methoxy, ethoxy, methoxycarbonyloxy, ethoxycarbonyloxy, (2-methylpropoxy)carbonyloxy and (2-propenyloxy) carbonyloxy; wherein each of R.sup.6, R.sup.7 and R.sup.8 is hydrido; wherein each of R.sup.9 and R.sup.10 is independently selected from hydrido, methyl and ethyl; wherein R.sup.11 is one or more groups independently selected from hydrido, fluoro, chloro, hydroxy, methoxy, methyl and ethyl; or a tautomer or enantiomer therefor, or a pharmaceutically-acceptable salt or ester thereof.

REFERENCES:
patent: 4695580 (1987-09-01), Ohashi et al.

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