Tricyclic pyrazolo-pyridazinone analogues as gaba-a receptor...

Details Tricyclic pyrazolo-pyridazinone analogues as gaba-a receptor... Tricyclic pyrazolo-pyridazinone analogues as gaba-a receptor...

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/50 (2006.01)

Patent

CA 2291689

A class of pyrazolo[4,3-c]pyridazin-3-one analogues of formula (I), substituted at the 2-position by an optionally substituted aryl or heteroaryl moiety, and wherein the pyridazine ring of the pyrazolo-pyridazinone ring system is fused to an alkylene chain, are selective ligands for GABAA receptors, in particular having 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.

On décrit un type d'analogues de pyrazolo[4,3-c]pyridazine-3 de la formule (I), substitué à la position 2 par une fraction aryle ou hétéroaryle éventuellement substitué, et dans lequel le noyau pyridazine du système cyclique pyrazolo-pyridazinone est lié à une chaîne alkylène. Lesdits analogues sont des ligands du récepteur GABA-A, qui ont en particulier une forte affinité pour le sous-groupe .alpha.2 et/ou .alpha.3 dudit récepteur, et conviennent donc pour le traitement et/ou la prévention de troubles du système nerveux central, notamment l'anxiété et les convulsions.

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