Tricyclic pyridone analogues as gaba-a receptor ligands

Details Tricyclic pyridone analogues as gaba-a receptor ligands Tricyclic pyridone analogues as gaba-a receptor ligands

C - Chemistry, Metallurgy

07

D

C07D 471/14 (2006.01) A61K 31/435 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2287929

A class of tricyclic pyridin-2-one analogues, substituted at the 3-position of the pyridone ring by an ester or thiazole 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 d'analogues de pyridin-2-one tricyclique, substitués en position 3 du noyau pyridone par un ester ou une fraction thiazole. Ces analogues sont des ligands sélectifs de récepteurs GABA¿A?. Ils présentent en particulier une grande affinité pour la sous-unité .alpha.2 et/ou à la sous-unité .alpha.3 de ces récepteurs et sont par conséquent utiles dans le traitement et/ou la prévention de troubles du système nerveux central, notamment l'anxiété et les convulsions.

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