Imidazo-triazine derivatives as ligands for gaba receptors

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01) A61K 31/4188 (2006.01) A61P 25/22 (2006.01) A61P 25/28 (2006.01)

Patent

CA 2484162

A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a - NH- linkage, and substituted on the phenyl ring by one or two further substituents as defined herein, being selective ligands for GABAA receptors, in particular having good affinity for the .alpha.2 and/or .alpha.3 and/or .alpha.5 subunit thereof, 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 porte sur une classe de dérivés de 7-phenylimidazo[1,2-b][1,2,4]triazine, substitués au niveau de la position meta du noyau phényl par un groupe aryle ou hétéroaryl à substitution facultative qui est directement lié ou ponté par un atome d'oxygène ou une liaison -NH-, et substitué sur le noyau phényl par au moins un substituants tels que définis ci-contre, lesquels sont des ligands sélectifs des récepteurs de GABA<SB>A</SB>, présentant notamment une bonne affinité avec la sous-unité .alpha.2 et/ou .alpha.3 et/ou .alpha.5, et sont par conséquent bénéfiques dans le traitement et/ou la prévention de conditions défavorables du système nerveux central, y compris l'anxiété, les convulsions et les troubles de la connaissance.

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