Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1991-12-19
1993-10-12
Berch, Mark L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
514258, 544244, 544263, C07D48704, C07F 96521, A61K 31675, A61K 31505
Patent
active
052525635
ABSTRACT:
A class of 5,6,7,8-tetrahydro-imidazo[1,2-a]pyrimidine 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 Y.sub.m is --CH.sub.2 -- or --CH.sub.2 --CH.sub.2 --; wherein m is one; wherein A is selected from phosphonic acid/ester moieties and phosphonamide moities and wherein the A moiety is attached at the 5- or 7-ring position of the terahydro-imidazo[1,2-a]pyrimidine ring system; wherein B is selected from carboxylic acid/ester moieties and carboxamide moieties; wherein X is one or more groups attachable at one or more of the 5-, 6- or 7-ring positions not occupied by the A moiety; 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; wherein V is selected from hydrido and alkyl; or a pharmaceutically-acceptable salt thereof.
REFERENCES:
patent: 3923808 (1975-12-01), Van Gelder et al.
patent: 4438118 (1984-03-01), Staahle et al.
patent: 4657899 (1987-04-01), Rzeszotarski et al.
patent: 4918064 (1990-04-01), Cordi et al.
Barnes, Science 239 p. 254 (1988).
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).
Cordi Alexis A.
Sun Eric T.
Berch Mark L.
G. D. Searle & Company
Keane J. Timothy
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