Patent · US Expired

Diacid-containing benzimidazole compounds for treatment of neurotoxic injury

US5216003A · kind A · utility

33Cited by
3References
38Claims
0Family size

Assignee

Inventor

Key dates

Filing dateJan 2, 1992
Grant dateJun 1, 1993
Priority date
Expiry dateJan 2, 2012

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07F9/65583
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

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.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.