CYCLOHEXYLAMINE DERIVATIVE CONTAINING PHENYL GROUP, AND THERAPEUTIC AGENT FOR DISEASES ACCOMPANIED BY CENTRAL NERVOUS SYSTEM DISORDERS
申请人:Mita Shiro
公开号:US20110257225A1
公开(公告)日:2011-10-20
Disclosed is a novel cyclohexylamine derivative containing a phenyl group, which is useful as a novel sigma receptor ligand. Also disclosed is a therapeutic agent for diseases accompanied by a central nervous system disorder, which comprises the compound as an active ingredient. The therapeutic agent comprises a compound represented by general formula [1] or a pharmacologically acceptable salt thereof as an active ingredient:
wherein X and Y independently represent a hydrogen atom, a halogen atom, a trihalomethyl group, a dihalomethyl group, a monohalomethyl group, a methoxy group, a hydroxyl group, or an alkyl group having 1 to 3 carbon atoms; R1, R2, R3 and R4 independently represent a hydrogen atom, a hydroxyl group, an alkoxyl group having 1 to 3 carbon atoms, or an alkyl group having 1 to 3 carbon atoms; R5 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, or an alkylene group which has 2 to 4 carbon atoms and can bind to a carbon atom other than carbon atoms that bind to a nitrogen atom on the cyclohexyl ring to form a ring; n represents an integer of 1 to 5; and Z represents a sulfur atom, a carbon atom, or an oxygen atom.
本发明公开了一种含有苯基的新型环己胺衍生物,其作为新型σ受体配体具有用途。同时公开了一种治疗中枢神经系统疾病的治疗剂,其包含上述化合物作为活性成分。该治疗剂包含下式[1]所表示的化合物或其药理学上可接受的盐作为活性成分:其中,X和Y独立地表示氢原子、卤素原子、三卤甲基基团、二卤甲基基团、单卤甲基基团、甲氧基、羟基或1至3个碳原子的烷基基团;R1、R2、R3和R4独立地表示氢原子、羟基、1至3个碳原子的烷氧基或1至3个碳原子的烷基基团;R5表示氢原子、1至5个碳原子的烷基基团或具有2至4个碳原子的烷基烯基,可以与环己基环上除了与氮原子结合的碳原子以外的碳原子结合形成环;n表示1至5的整数;Z表示硫原子、碳原子或氧原子。