Phenylbenzimidazole derivatives as ligands for gaba receptors

Details Phenylbenzimidazole derivatives as ligands for gaba receptors Phenylbenzimidazole derivatives as ligands for gaba receptors

C - Chemistry, Metallurgy

07

D

C07D 235/06 (2006.01) A61K 31/415 (2006.01) A61K 31/445 (2006.01) C07D 401/10 (2006.01) C07D 401/12 (2006.01) C07D 403/10 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2279929

A class of 1-phenylbenzimidazole derivatives, substituted at the meta position of the phenyl ring by a methylene-, carbonyl- or thiocarbonyl-linked amine moiety, are selective ligands for GABAA receptors, in particular having high affinity for the .alpha.2 and/or .alpha.3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.

L'invention concerne une classe de dérivés de 1-phénylbenzimidazole, substitués à la position meta de la chaîne de phényle par une fraction d'amine liée à du méthylène, du carbonyle ou du thiocarbonyle. Ces dérivés sont des ligands sélectifs pour les récepteurs de GABA¿A?, présentant, en particulier, une forte affinité pour la sous-unité .alpha.2 et/ou .alpha.3 de ces derniers. Par conséquent, ils sont très avantageux dans le traitement et/ou la prévention des troubles du système nerveux central, y compris de l'anxiété et des convulsions.

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