Glutamate (NMDA) receptor antagonists
AssigneeWarner-Lambert Company
InventorsChristopher F. Bigge, James J. Li
Life of this patent
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Abstract
Novel naphthyl-substituted .alpha.-amino acid derivatives, pharmaceutical compositions containing the same and a method of using the same, for the blockade of aspartate and glutamate receptors, are described. Novel intermediates of the napthyl-substituted .alpha.-amino acid derivatives are disclosed.
Claims2
A compound represented by the formula:
- ##STR28## wherein (a) m and n are independently an integer of 0 to 3;
- (b) Q is selected from the group consisting of:
- Br and PO.sub.3 Et.sub.2 ;
- (c) L is selected from the group consisting of Br and by the formulae ##STR29## and (d) X, Y and Z are independently hydrogen, halogen, amino, hydroxy, hydroxyalkyl having i to 6 carbon atoms, haloalkyl having 1 to 6 carbon atoms, cycloalkyl, aryl, aralkyl, aminoalkyl having 1 to 6 carbon atoms or alkoxy having 1 to 6 carbon atoms.
A compound selected from group consisting of 1-[3-(bromomethyl)-5-methylphenyl]naphthalene, 2-[3-(Bromomethyl)-5-methylphenyl]naphthalene, diethyl[3-methyl-5-(1-naphthalenyl)phenyl]methylphosphonate, diethyl[3-methyl-5-(2-naphthalenyl)phenyl]methylphosphonate, diethyl[3-(bromomethyl)-5-(1-naphthalenyl)phenyl]methylphosphonate, diethyl[3-bromomethyl)-5-(2-naphthalenyl)phenyl]methylphosphonate, diethyl(acetylamino)[[3-[(diethoxyphosphinyl)methyl]-5-(1-naphthalenyl)-ph enyl]methyl]propanedioate, diethyl(acetylamino)[[3-[(diethoxyphosphinyl)methyl]-5-(2-naphthalenyl)phe nyl]methyl]propanedioate, 1,1-dimethylethyl (2S-trans)-5-[[3(diethoxyphosphinyl)methyl]-5-(1-naphthalenyl) phenyl]methyl]-2-(1,1-dimethylethyl)-3-methyl-4-oxo-1-imidazolidinecarboxy late and 1,1-dimethylethyl (2S-trans)-5-[[3-(diethoxyphosphinyl)methyl]-5-(2naphthalenyl) phenyl]methyl]-2-(1,1-dimethylethyl)-3- methyl-4-oxo-1-imidazolidinecarboxylate.
Dependencies are inferred from the claim text.