Diacid-containing benzimidazole compounds for treatment of neuro

Details Diacid-containing benzimidazole compounds for treatment of neuro Diacid-containing benzimidazole compounds for treatment of neuro

1992-01-02

1993-06-01

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514394, 514400, 548113, 548252, 548253, 548254, 5483061, 5483094, 5483097, 5483101, A61K 31415, C07D23364, C07D40304

Patent

active

052160033

ABSTRACT:
A class of diacid-containing benzimidazole compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest 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 X is one or more groups attachable at one or more of the 4-, 5-, 6- and 7-ring positions not occupied by the phosphonoalkyl moiety; wherein each X 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 each of R.sup.10, R.sup.13 and R.sup.14 is independently selected from hydrido, alkyl, benzyl and phenyl; and wherein V is selected from hydrido and acyl; or a pharmaceutically-acceptable salt thereof.

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