公开(公告)号：US20180263998A1

公开(公告)日：2018-09-20

申请号：US15516567

申请日：2015-10-08

Applicant: Eisai R&D Management Co., Ltd.

Inventor： Yasuhiro Zaima ,  Kazuo Kazama ,  Shuntaro Arase ,  Kentaro Nagane ,  Kanta Horie ,  Yosuke Ueki

IPC: A61K31/542

CPC classification number: A61K31/542 ,  A61K9/2018 ,  A61K9/2054 ,  A61P25/28

Abstract: The present invention provides a pharmaceutical composition comprising a compound represented by formula (1): or N-[3-((4aS,5R,7aS)-2-amino-5-methyl-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl]-5-difluoromethylpyrazine-2-carboxamide, or a pharmaceutically acceptable salt of the foregoing, and a salt of a compound having a C12-22 saturated aliphatic hydrocarbon group.

公开(公告)号：US11026944B2

公开(公告)日：2021-06-08

申请号：US16819341

申请日：2020-03-16

Applicant: Eisai R&D Management Co., Ltd.

Inventor： Margaret Moline ,  Gina Pastino ,  Yurie Akimoto ,  Yasuhiro Zaima ,  Nobuya Suzuki ,  Nobuo Yoshida

IPC: A61K31/506 ,  A61K9/48 ,  A61K9/00 ,  A61K9/20

Abstract: In the present invention, compound such as (1R,2S)-2-(((2,4-dimethylpyrimidin-5-yl)oxy)methyl)-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl) cyclopropanecarboxamide have been found to be potent orexin receptor antagonists, and may be useful in the treatment of sleep disorders such as insomnia, as well as for other therapeutic uses.

公开(公告)号：US10702529B2

公开(公告)日：2020-07-07

申请号：US16255116

申请日：2019-01-23

Applicant: Eisai R&D Management Co., Ltd.

Inventor： Margaret Moline ,  Gina Pastino ,  Yurie Akimoto ,  Yasuhiro Zaima ,  Nobuya Suzuki ,  Nobuo Yoshida

IPC: A61K31/506 ,  A61K9/48 ,  A61K9/00 ,  A61K9/20

Abstract: In the present invention, compound such as (1R,2S)-2-(((2,4-dimethylpyrimidin-5-yl)oxy)methyl)-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl) cyclopropanecarboxamide have been found to be potent orexin receptor antagonists, and may be useful in the treatment of sleep disorders such as insomnia, as well as for other therapeutic uses.

公开(公告)号：US10188652B2

公开(公告)日：2019-01-29

申请号：US15519676

申请日：2015-10-21

Applicant: Eisai R&D Management Co., Ltd.

Inventor： Margaret Moline ,  Gina Pastino ,  Yurie Akimoto ,  Yasuhiro Zaima ,  Nobuya Suzuki ,  Nobuo Yoshida

IPC: A61K31/506 ,  A61K9/00 ,  A61K9/20 ,  A61K9/48

Abstract: In the present invention, compound such as (1R,2S)-2-(((2,4-dimethylpyrimidin-5-yl)oxy)methyl)-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl) cyclopropanecarboxamide have been found to be potent orexin receptor antagonists, and may be useful in the treatment of sleep disorders such as insomnia, as well as for other therapeutic uses.

公开(公告)号：US20230103250A1

公开(公告)日：2023-03-30

申请号：US17787752

申请日：2021-01-14

Applicant: Eisai R&D Management Co., Ltd.

Inventor： Taichi ABE ,  Yusuke AYATA ,  Nobuya SUZUKI ,  Yurie AKIMOTO ,  Futoshi SHIKATA ,  Yasuhiro Zaima ,  Nobuo YOSHIDA

IPC: A61K31/506 ,  A61K9/20 ,  A61K9/16

Abstract: There is provided a pharmaceutical composition comprising lemborexant exhibiting a favorable dissolution profile by using a granular material having a 90% cumulative diameter (D90) of 64 μm or less as a lemborexant active pharmaceutical ingredient.

公开(公告)号：US10117876B2

公开(公告)日：2018-11-06

申请号：US15516567

申请日：2015-10-08

Applicant: Eisai R&D Management Co., Ltd.

Inventor： Yasuhiro Zaima ,  Kazuo Kazama ,  Shuntaro Arase ,  Kentaro Nagane ,  Kanta Horie ,  Yosuke Ueki

IPC: A61K31/542 ,  C07D513/04 ,  A61K9/20

CPC classification number: A61K31/542 ,  A61K9/2018 ,  A61K9/2054 ,  A61P25/28

Abstract: The present invention provides a pharmaceutical composition comprising a compound represented by formula (1): or N-[3-((4aS,5R,7aS)-2-amino-5-methyl-4a,5,7,7a-tetrahydro-4H-furo[3,4-d] [1,3]thiazin-7a-yl)-4-fluorophenyl]-5-difluoromethylpyrazine-2-carboxamide, or a pharmaceutically acceptable salt of the foregoing, and a salt of a compound having a C12-22 saturated aliphatic hydrocarbon group.

公开(公告)号：US10076524B1

公开(公告)日：2018-09-18

申请号：US15516567

申请日：2015-10-08

Applicant: Eisai R&D Management Co., Ltd.

Inventor： Yasuhiro Zaima ,  Kazuo Kazama ,  Shuntaro Arase ,  Kentaro Nagane ,  Kanta Horie ,  Yosuke Ueki

IPC: A61K31/542 ,  C07D513/04 ,  A61K9/20

CPC classification number: A61K31/542 ,  A61K9/2018 ,  A61K9/2054 ,  A61P25/28

Abstract: The present invention provides a pharmaceutical composition comprising a compound represented by formula (1): or N-[3-((4aS,5R,7aS)-2-amino-5-methyl-4a,5,7,7a-tetrahydro-4H-furo[3,4-d] [1,3]thiazin-7a-yl)-4-fluorophenyl]-5-difluoromethylpyrazine-2-carboxamide, or a pharmaceutically acceptable salt of the foregoing, and a salt of a compound having a C12-22 saturated aliphatic hydrocarbon group.