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    • 105. 发明公开
    • BENZYL PIPERIDINE COMPOUND
    • BENZYL PIPERIDINE化合物
    • EP2463286A1
    • 2012-06-13
    • EP10806467.6
    • 2010-08-04
    • Dainippon Sumitomo Pharma Co., Ltd.
    • TOYODA, TomohiroNISHIDA, TomoakiYOSHINAGA Hidefumi
    • C07D405/06A61K31/453A61P25/22A61P25/24A61P43/00
    • C07D405/06
    • Provided is a new serotonin-reuptake inhibitor that exhibits affinity for serotonin-1A receptors. Said serotonin-reuptake inhibitor is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. In the formula, R 1 represents a hydrogen atom, a 2-hydroxyethyl group, or a 2-methoxyethyl group. R 2 represents one of the following bonded to a methylene group which is bonded to a piperidine ring: a chlorine atom bonded in a p-position; a bromine atom bonded in a p-position; a methyl group bonded in a p-position; a chlorine atom bonded in an m-position; or a bromine atom bonded in an m-position. Either Y 1 represents a hydrogen atom and Y 2 represents a hydrogen atom or a hydroxyl group, or Y 1 and Y 2 together represent an oxo group. Z represents a group represented by one of the following formulas: formula (3-1-1), formula (3-1-2), formula (3-2-1), formula (3-2-2), formula (3-3-1), formula (3-3-2), formula (3-4-1), or formula (3-4-2). However, if R 1 represents a 2-hydroxyethyl group or a 2-methoxyethyl group and Y 1 and Y 2 both simultaneously represent hydrogen atoms, then Z represents a group represented by one of the following formulas: formula (3-1-2), formula (3-2-1), formula (3-2-2), formula (3-3-1), formula (3-3-2), formula (3-4-1), or formula (3-4-2).
    • 提供了对血清素-1A受体表现出亲和力的新的5-羟色胺再摄取抑制剂。 所述血清素再摄取抑制剂是由式(1)表示的化合物或其药理学上可接受的盐。 式中,R 1表示氢原子,2-羟乙基或2-甲氧基乙基。 R2表示键合至与哌啶环键合的亚甲基的以下之一:键合于对位的氯原子; 键合在对位上的溴原子; 在对位键合的甲基; 键合在m位的氯原子; 或键合在间位的溴原子。 Y1表示氢原子,Y2表示氢原子或羟基,或者Y1和Y2一起表示氧代基。 Z表示由下式之一表示的基团:式(3-1-1),式(3-1-2),式(3-2-1),式(3-2-2),式 3-3-1),式(3-3-2),式(3-4-1)或式(3-4-2)。 但是,如果R1表示2-羟乙基或2-甲氧基乙基,并且Y1和Y2两者同时表示氢原子,则Z表示由下式之一表示的基团:式(3-1-2),式 (3-2-1),式(3-2-2),式(3-3-1),式(3-3-2),式(3-4-1)或式(3-4- 2)。