[EN] IMIDAZO-PYRIMIDINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS<br/>[FR] DERIVES D'IMIDAZO-PYRIMIDINE COMME LIGANDS POUR LES RECEPTEURS GABA
申请人:MERCK SHARP & DOHME
公开号:WO2002074773A1
公开(公告)日:2002-09-26
A class of 3-phenylimidazo[1,2-a]pyrimidine 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 further substituted on the phenyl ring by alkyl, trifluoromethyl, alkoxy or one or two halogen atoms, especially fluoro, are selective ligands for GABAA receptors, in particular having good affinity for the a2 and/or a3 and/or a5 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.
一类3-苯基咪唑并[1,2-a]嘧啶衍生物,苯环的间位被取代为可选择取代的芳基或杂环基,该基团直接连接或通过氧原子或-NH-键桥接,并且苯环上进一步取代为烷基,三氟甲基,烷氧基或一个或两个卤素原子,特别是氟原子。这些化合物是GABAA受体的选择性配体,特别是对其中的a2和/或a3和/或a5亚基具有良好的亲和力,因此有助于治疗和/或预防中枢神经系统的不良症状,包括焦虑,抽搐和认知障碍。