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 2317484

A class of substituted 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position, a substituted alkoxy moiety at the 6-position, an optionally substituted N-linked nitrogen-containing aliphatic ring at the 7-position, and chloro at the 8-position, 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 porte sur une classe de dérivés 1,2,4-triazolo[4,3-b]pyridazine substitués possédant un substituant cycloalkyle, phényle ou hétéroaryle, éventuellement substitué, à la position 3, une fraction alcoxy substituée à la position 6, un noyau aliphatique éventuellement substitué renfermant un azote à liaison N, éventuellement substitué, à la position 7, et chloro à la position 8, ces dérivés étant des ligands sélectifs des récepteurs GABA¿A?, et ayant notamment une haute affinité pour la sous-unité .alpha.2 et/ou .alpha.3 de ces récepteurs. En conséquence, ils présentent un avantage dans le traitement et/ou la prévention des troubles du système nerveux central tels que l'anxiété et les convulsions.

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