Phosphonomethyl-imidazo[1,2-A]pyrimidine-2-carboxylic acid compo

Details Phosphonomethyl-imidazo[1,2-A]pyrimidine-2-carboxylic acid compo Phosphonomethyl-imidazo[1,2-A]pyrimidine-2-carboxylic acid compo

1994-03-14

1996-01-02

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Phosphorus containing other than solely as part of an...

514258, 544244, 544252, A61K 31505, C07F 909

Patent

active

054808766

ABSTRACT:
A class of phosphonomethyl-imidazo[1,2-a]pyrimidine-2-carboxylic acid compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest, hypoglycemia or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective 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, R.sup.2 and R.sup.6 is independently selected from hydrido, alkyl, allyl, cycloalkyl, cycloalkylalkyl, phenyl and benzyl; wherein Y.sub.m is --CH.sub.2 -- or --CH.sub.2 --CH.sub.2 --; where m is one; wherein X is one or more groups attachable at one or more of the 5-, 6- and 7-ring positions of the imidazo[1,2-a]pyrimidine ring system; wherein each x and T is independently selected from hydrido, halo, alkyl, cycloalkyl, cycloalkylalkyl, haloalkyl, alkenyl, alkynyl, phenyl, benzyl, hydroxy, hydroxyalkyl, alkoxy, phenoxy, alkoxyalkyl, benzyloxy, cyano, alkanoyl, alkylthio, arylthio and amino; or a pharmaceutically-acceptable salt thereof.

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S. M. Rothman et al, Annals of Neurology, 19 (2), (1986).
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K. Matoba et al, "Structural Modification of Bioactive Compound II. Syntheses of Aminophosphonic Acids", Chem. Pharm. Bull., 32 (10), 3918-3925 (1984).
D. E. Murphy et al, J. Pharmacol. Exp. Ther., 240 (3), 778-784 (1987).

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