[EN] IMIDAZO-PYRIDINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS<br/>[FR] DERIVES D'IMIDAZO-PYRIDINE UTILISES EN TANT QUE LIGANDS POUR LES RECEPTEURS GABA
申请人:MERCK SHARP & DOHME
公开号:WO2003099816A1
公开(公告)日:2003-12-04
A class of 8-fluoro-3-phenylimidazo[1,2-a]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group, or by a pyrrolidinonyl group, which is directly attached or bridged by an oxygen atom or by a -NH- or -OCH2- linkage, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 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.
一类8-氟-3-苯基咪唑并[1,2-a]吡啶衍生物,通过苯环的间位被一个可选择取代的芳基或杂环芳基团,或者通过一个吡咯烷基团取代,该吡咯烷基团直接连接或通过氧原子或-NH-或-OCH2-键连接,作为GABAA受体的选择性配体,特别是对其α2和/或α3和/或α5亚基具有高亲和力,因此在治疗和/或预防中枢神经系统的不良状况,包括焦虑、惊厥和认知障碍方面具有益处。