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

1993-10-21

1996-01-09

Kumar, Shailendra

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514 80, A61K 31675, A61K 31505

Patent

active

054829330

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.

REFERENCES:
patent: 4532243 (1985-07-01), Tully
patent: 4636502 (1987-01-01), Spitzer
patent: 4657899 (1987-04-01), Rzeszotarski et al.
patent: 4918064 (1990-04-01), Cordi et al.
S. M. Rothman et al, Annals of Neurology, 19 (2), (1986).
M. N. Perkins et al, Neuroscience Lett., 23, 333 (1981).
J. Davies et al, Neuroscience Lett., 21, 77 (1981).
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).

Affiliated with

Also associated with

Rating

Phosphonomethyl-imidazo[1,2-a]pyrimidine-2-carboxylic acid compo does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Phosphonomethyl-imidazo[1,2-a]pyrimidine-2-carboxylic acid compo, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Phosphonomethyl-imidazo[1,2-a]pyrimidine-2-carboxylic acid compo will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-1303225