申请人:Sumitomo Dainippon Pharma Co., Ltd.
公开号:US10087146B2
公开(公告)日:2018-10-02
The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1):
or a pharmaceutically acceptable salt thereof
wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl;
A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.;
and X is hydrogen or halogen etc.
本发明涉及一种新型血清素再摄取抑制剂,它还具有 5-HT2C 拮抗作用(抗抑郁和抗焦虑作用),特别是 5-HT2C 反激动作用,由化合物(1)组成:
或其药学上可接受的盐
其中R1、R2、R3和R4独立地为氢或C1-6烷基等;R5为C4-7烷基或-(CR8R9)r-E;R6、R7、R8和R9独立地为氢、氟或C1-6烷基;
A 是 C6-10 芳基或杂芳基等;r 是 1、2、3 或 4;E 是 C3-8 环烷基或 C6-10 芳基等;L 是氧、硫或-NR10-;n 是 1、2 或 3;R10 是氢或 C1-6 烷基等;
X 是氢或卤素等。