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 31/5025 (2006.01) A61P 25/22 (2006.01)

Patent

CA 2359008

A class of substituted 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a difluoro- or trifluoro-substituted phenyl ring at the 3-position, a triazolyl-methoxy moiety at the 6-position, and a tert-butyl group at the 7-position, are selective ligands for GABA A receptors, in particular having high affinity for .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 de dérivés substitués de 1,2,4-triazolo[4,3-b]pyridazine, comportant une chaîne phényle difluoro- ou trifluoro-substituée en position 3, une fraction triazolyl-méthoxy en position 6, et un groupe tert-butyle en position 7, tenant lieu de ligands sélectifs pour récepteurs GABAA, et ayant en particulier une affinité élevée pour l'unité secondaire alpha 2 et/ou alpha 3 de ces récepteurs. Ce type de produit est donc utile dans le traitement et/ou la prévention des troubles du système nerveux central, y compris l'anxiété et les convulsions.

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