Substituted triazolo-pyridazine derivatives as ligands for...

Details Substituted triazolo-pyridazine derivatives as ligands for... Substituted triazolo-pyridazine derivatives as ligands for...

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/50 (2006.01) A61K 31/505 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) A61K 47/48 (2006.01) C07D 471/14 (2006.01) C07D 487/08 (2006.01) G01N 33/566 (2006.01)

Patent

CA 2260774

A class of substituted or 7,8-ring fused 1,2,4triazolo[4,3-b]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and a substituted alkoxy moiety at the 6-position, are selective ligands for GABA A receptors, in particular having high affinity for the a2 and/or 0 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 catégorie de dérivés de 1,2,4-triazolo[4,3-b]pyridazine substitués ou fusionnés à 7,8 anneaux, possédant à la position (3) un substituant cycloalkyle, phényle ou hétéroaryle éventuellement substitué et, à la position (6), une fraction d'alkoxy substitué, ces dérivés étant des ligands sélectifs pour récepteurs de GABAA présentant en particulier une grande affinité pour les sous-unités alpha 2 et/ou alpha 3 de ceux-ci, ce qui les rend utiles pour le traitement et/ou la prévention des troubles du système nerveux central, notamment l'anxiété et les convulsions.

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