公开(公告)号：US10723703B2

公开(公告)日：2020-07-28

申请号：US16193232

申请日：2018-11-16

申请人： Sumitomo Dainippon Pharma Co., Ltd.

发明人： Izumi Sasaki ,  Tomohiro Toyoda ,  Hidefumi Yoshinaga ,  Itaru Natsutani ,  Yoko Takahashi

IPC分类号： C07D231/20 ,  C07D231/44 ,  C07D493/08 ,  C07D231/22 ,  C07D231/38 ,  C07D231/18 ,  C07D405/06

摘要： 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.

公开(公告)号：US10183913B2

公开(公告)日：2019-01-22

申请号：US15990026

申请日：2018-05-25

申请人： Sumitomo Dainippon Pharma Co., Ltd.

发明人： Izumi Sasaki ,  Tomohiro Toyoda ,  Hidefumi Yoshinaga ,  Itaru Natsutani ,  Yoko Takahashi

IPC分类号： C07D231/20 ,  C07D231/18 ,  C07D231/38 ,  C07D405/06 ,  C07D493/08

摘要： 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.

公开(公告)号：US11312688B2

公开(公告)日：2022-04-26

申请号：US16903646

申请日：2020-06-17

申请人： Sumitomo Dainippon Pharma Co., Ltd.

发明人： Izumi Sasaki ,  Tomohiro Toyoda ,  Hidefumi Yoshinaga ,  Itaru Natsutani ,  Yoko Takahashi

IPC分类号： C07D231/20 ,  C07D231/18 ,  C07D231/38 ,  C07D405/06 ,  C07D493/08 ,  C07D231/22 ,  C07D231/44

摘要： 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.

公开(公告)号：US10087146B2

公开(公告)日：2018-10-02

申请号：US15491130

申请日：2017-04-19

申请人： Sumitomo Dainippon Pharma Co., Ltd.

发明人： Izumi Sasaki ,  Tomohiro Toyoda ,  Hidefumi Yoshinaga ,  Itaru Natsutani ,  Yoko Takahashi

IPC分类号： C07D231/20 ,  C07D231/38 ,  C07D405/06 ,  C07D493/08 ,  C07D231/18

摘要： 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.