Triazolo-pyridazine derivatives as ligands for gaba receptors

Details Triazolo-pyridazine derivatives as ligands for gaba receptors Triazolo-pyridazine derivatives as ligands for gaba receptors

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/50 (2006.01) C07D 237/00 (2006.01) C07D 249/00 (2006.01)

Patent

CA 2315763

A class of substituted 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a fluoro-substituted phenyl ring at the 3-position and a heteroaryl-methoxy moiety at the 6-position, are selective ligands for GABA A 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 porte sur une classe de dérivés substitués de la 1,2,4-triazolo[4,3-b] pyridazine présentant un cycle phényle à substitution fluoro en position 3-, et un fragment hétéroaryle-méthoxy en position 6-. Ces dérivés, ligands sélectifs des récepteurs du GABAA, ont une forte affinité pour ses sous-unités alpha 2 et/ou alpha 3, et exercent de ce fait une action bénéfique dans le traitement ou la prévention de troubles du SNC, dont l'anxiété et les convulsions.

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