Pyrazino-pyridazine derivatives as ligands for gaba receptors

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

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/5025 (2006.01) A61P 25/00 (2006.01) C07D 237/00 (2006.01) C07D 241/00 (2006.01)

Patent

CA 2396199

A class of pyrazino[2,3-d]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 5-position, a substituted alkoxy moiety at the 3-position, and a range of substituents at the 2-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.

L'invention concerne une classe de dérivés de pyrazino[2,3-d]pyridazine, possédant un cycloalkyle, un phényle éventuellement substitué ou un substituant hétéroaryle en position 5, une fraction alcoxy substituée en position 3, et une série de substituants en position 2, constituée de ligands sélectifs destinés à des récepteurs GABA¿A?, présentant en particulier une affinité élevée pour les sous-unités .alpha.2 et/ou .alpha.3 et/ou .alpha.5 de ceux-ci, et utilisés de manière avantageuse dans le traitement et/ou la prévention de troubles indésirables du système nerveux central, notamment l'anxiété, les convulsions, et les troubles cognitifs.

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