发明授权
US5252563A 5,6,7,8-tetrahydro-imidazo[1,2-a]pyrimidine compounds for treatment of neurotoxic injury 失效
5,6,7,8-四氢 - 咪唑并[1,2-a]嘧啶化合物,用于治疗神经毒性损伤

5,6,7,8-tetrahydro-imidazo[1,2-a]pyrimidine compounds for treatment of
neurotoxic injury
摘要:
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.
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