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    • 3. 发明授权
    • Benzyl piperidine compound
    • 苄基哌啶化合物
    • US08778970B2
    • 2014-07-15
    • US13388623
    • 2010-08-04
    • Tomohiro ToyodaTomoaki NishidaHidefumi Yoshinaga
    • Tomohiro ToyodaTomoaki NishidaHidefumi Yoshinaga
    • A61K31/453C07D405/10
    • 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, R1 represents a hydrogen atom, a 2-hydroxyethyl group, or a 2-methoxyethyl group. R2 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 Y1 represents a hydrogen atom and Y2 represents a hydrogen atom or a hydroxyl group, or Y1 and Y2 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 R1 represents a 2-hydroxyethyl group or a 2-methoxyethyl group and Y1 and Y2 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受体具有亲和性的新的5-羟色胺再摄取抑制剂。 所述5-羟色胺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。 在该式中,R 1表示氢原子,2-羟乙基或2-甲氧基乙基。 R 2表示与键合到哌啶环的亚甲基键合的下列之一:键合在对位的氯原子; 键合在p位的溴原子; 在p位上键合的甲基; 键合在m位的氯原子; 或结合在m位的溴原子。 Y1表示氢原子,Y2表示氢原子或羟基,Y1或Y2表示氧代基。 Z表示由下式表示的基团: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)。 然而,如果R1表示2-羟乙基或2-甲氧基乙基,Y1和Y2同时表示氢原子,则Z表示由下式表示的基团: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)。
    • 4. 发明授权
    • Benzylpiperizine compound
    • 苄基哌嗪化合物
    • US08557998B2
    • 2013-10-15
    • US13527612
    • 2012-06-20
    • Tomohiro Toyoda
    • Tomohiro Toyoda
    • C07D211/22
    • C07C309/73C07D211/22C07D211/32C07D311/22C07D313/08C07D405/06
    • Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a methyl group; R2 is a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.)
    • 公开了由式(1)表示的苄基哌啶化合物或其药学上可接受的盐,其可用作药物如抗抑郁剂。 (式(1)中,R 1表示氢原子或甲基,R 2表示相对于亚甲基的p位或m位的基团,表示在p位结合的氯原子,溴 在p位上键合的原子,在p位上键合的甲基,与m位相连的m位或与溴原子结合的氯原子; X表示亚甲基或氧原子; n表示 表示1〜3的整数。)
    • 6. 发明申请
    • BENZYL PIPERIDINE COMPOUND
    • 苄基哌啶化合物
    • US20120130077A1
    • 2012-05-24
    • US13388623
    • 2010-08-04
    • Tomohiro ToyodaTomoaki NishidaHidefumi Yoshinaga
    • Tomohiro ToyodaTomoaki NishidaHidefumi Yoshinaga
    • C07D405/10
    • 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, R1 represents a hydrogen atom, a 2-hydroxyethyl group, or a 2-methoxyethyl group. R2 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 Y1 represents a hydrogen atom and Y2 represents a hydrogen atom or a hydroxyl group, or Y1 and Y2 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 R1 represents a 2-hydroxyethyl group or a 2-methoxyethyl group and Y1 and Y2 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受体具有亲和性的新的5-羟色胺再摄取抑制剂。 所述5-羟色胺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。 在该式中,R 1表示氢原子,2-羟乙基或2-甲氧基乙基。 R 2表示与键合到哌啶环的亚甲基键合的下列之一:键合在对位的氯原子; 键合在p位的溴原子; 在p位上键合的甲基; 键合在m位的氯原子; 或结合在m位的溴原子。 Y1表示氢原子,Y2表示氢原子或羟基,Y1或Y2表示氧代基。 Z表示由下式表示的基团: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)。 然而,如果R1表示2-羟乙基或2-甲氧基乙基,Y1和Y2同时表示氢原子,则Z表示由下式表示的基团: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)。