C - Chemistry – Metallurgy – 07 – D
Patent
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 2315219
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, and an optionally substituted bicycloalkyl ring system at the 7-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.
Cette catégorie de dérivés de 1,2,4-triazolo3,4-bpyridazines substituées pourvus d'un substituant cycloalkyle, phényle ou hétéroaryle le cas échéant substitué en position 3, d'une fraction alcoxyle substituée en position 6, et d'un système cyclique bicycloalkyle le cas échéant substitué en position 7, forme des ligands sélectifs des récepteurs GABA¿A?, avec une haute affinité, en particulier, pour la sous-unité .alpha.2 et/ou .alpha.3 de ceux-ci, et est par conséquent utile dans le traitement et/ou la prévention de troubles du système nerveux central, y compris l'angoisse et les convulsions.
Carling William Robert
Moore Kevin William
Street Leslie Joseph
Merck Sharp & Dohme Limited
Ogilvy Renault
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