Pyrido-pyridazine derivatives as ligands for gaba receptors

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

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) A61K 31/5025 (2006.01) A61P 25/00 (2006.01) C07D 221/00 (2006.01) C07D 237/00 (2006.01)

Patent

CA 2384051

A class of pyrido[2,3-d]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 8-position, a substituted alkoxy moiety at the 2-position, and a range of substituents at the 3-position, are selective ligands for GABAA receptors, in particular having high affinity for the .alpha.2 and/or .alpha.3 and/or .alpha.5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

La présente invention concerne une classe de dérivés de pyrido[2,3-d]pyridazine possédant un substituant hétéroaryle, phényle ou cycloalkyle éventuellement substitué, en position 8, un groupe fonctionnel alkoxy substitué, en position 2, ainsi qu'une gamme de substituants en position 3. Ces dérivés représentent des ligands de sélection pour les récepteurs GABA¿A? et présentent notamment une grande affinité pour les sous-unités .alpha.2 et/ou .alpha.3 et/ou .alpha.5 de ces récepteurs. Ces dérivés sont, selon cette invention, bénéfique dans le traitement et/ou la prévention d'états défavorables du système nerveux central, y compris l'anxiété, les convulsions et les troubles cognitifs.

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