申请人:Conn Jeffrey P.
公开号:US20070208028A1
公开(公告)日:2007-09-06
Provided is a method of treating conditions and disorders for which full mGluR5 antagonists are potentially effective, such as, e.g., anxiety, epilepsy, schizophrenia and other psychotic disorders, Parkinson's disease, addictive disorders, and the like in a subject in need of such treatment, comprising administration to such subject of a therapeutically effective amount of a partial, non-competitive mGluR5 antagonist compound of the invention. Specific examples of partial MgluR5 antagonists provided include those compounds having the formula:
wherein: Z is, independently N or —CH—, provided that one, and only one Z is N; R is halogen (e.g., Br, F and the like), alkyl (e.g., methyl), alkenyl (e.g., CH═CH2, aryl (e.g., phenyl), heterocyclic (e.g., thiophenyl).
提供了一种治疗全mGluR5拮抗剂可能有效的疾病和疾病的方法,例如焦虑、癫痫、精神分裂症和其他精神障碍、帕金森病、成瘾性疾病等,适用于需要此类治疗的患者,包括向该患者施用本发明的部分、非竞争性mGluR5拮抗剂化合物的治疗有效量。所提供的部分MgluR5拮抗剂的具体例子包括具有以下式子的化合物:其中:Z独立地为N或—CH—,但仅有一个Z为N;R为卤素(例如Br、F等)、烷基(例如甲基)、烯基(例如CH═CH2)、芳基(例如苯基)、杂环(例如噻吩基)。