公开(公告)号：US11660275B2

公开(公告)日：2023-05-30

申请号：US16975865

申请日：2019-03-18

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

Inventor： Hiroyuki Higashiyama ,  Hisashi Wakita ,  Yoshimasa Ito ,  Yoshihide Osada

IPC: A61K31/18 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/506

CPC classification number: A61K31/18 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/506

Abstract: Provided is a combination agent that combines N-[(1S)-2,2,5,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide with an AMPA-type glutamate receptor antagonist such as 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one or 2-fluoro-6-(3-fluoro-8-oxo-7-(pyridin-3-yl)-7,8-dihydro-6H-pyrano[3,2-b:5,4-b′]dipyridin-9-yl)benzonitrile, and it has potential for use as a therapeutic agent for epilepsy.

公开(公告)号：US20210000771A1

公开(公告)日：2021-01-07

申请号：US16975865

申请日：2019-03-18

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

Inventor： Hiroyuki Higashiyama ,  Hisashi Wakita ,  Yoshimasa Ito ,  Yoshihide OSADA

IPC: A61K31/18 ,  A61K31/444 ,  A61K31/4375 ,  A61K31/506

Abstract: Provided is a combination agent that combines N-[(1S)-2,2,5,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide with an AMPA-type glutamate receptor antagonist such as 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one or 2-fluoro-6-(3-fluoro-8-oxo-7-(pyridin-3-yl)-7,8-dihydro-6H-pyrano[3,2-b:5,4-b′]dipyridin-9-yl)benzonitrile, and it has potential for use as a therapeutic agent for epilepsy.

公开(公告)号：US09610262B2

公开(公告)日：2017-04-04

申请号：US15102046

申请日：2014-12-17

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

Inventor： Hiroyuki Higashiyama ,  Yuji Kazuta ,  Keisuke Hashimoto

IPC: A61K31/165 ,  A61K31/18

CPC classification number: A61K31/165 ,  A61K31/18

Abstract: The present invention is directed to a method of treating pain comprising the administering the following 1-indansulfamide compounds: N-[(1S)-2,2,5,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide, (−)-N-(7-chloro-2,2,5-trifluoro-2,3-dihydro-1H-inden-1-yl)sulfamide, N-[(1S)-2,2-difluoro-7-methyl-2,3-dihydro-1H-inden-1-yl]sulfamide, and N-[(1S)-2,2,5-trifluoro-7-methyl-2,3-dihydro-1H-inden-1-yl]sulfamide.

公开(公告)号：US09018260B2

公开(公告)日：2015-04-28

申请号：US14370633

申请日：2013-06-17

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

Inventor： Yuji Kazuta ,  Toru Watanabe ,  Keiichi Sorimachi ,  Minako Saito ,  Yoichi Kita ,  Toshiaki Tanaka ,  Hiroyuki Higashiyama ,  Takahisa Hanada ,  Tetsuyuki Teramoto ,  Takashi Kosasa ,  Yukio Ishikawa

IPC: A61K31/18 ,  C07C311/00 ,  C07C307/08 ,  C07C309/00

CPC classification number: C07C307/08 ,  A61K31/18 ,  C07C309/00 ,  C07C2602/08

Abstract: Novel indansulfamide derivatives or a pharmaceutically acceptable salt thereof such as N-[(1S)-2,2,5,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide, N-[(1S)-2,2,4,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide, (+)-N-(2,2,4,6,7-pentafluoro-2,3-dihydro-1H-inden-1-yl)sulfamide, have an action of improving Seizure Severity Index (Score) in mice kindling model. Thus the compounds or the salt thereof are expected as a drug for treating epilepsy.

Abstract translation: 新型的茚满磺酰胺衍生物或其药学上可接受的盐，例如N - [（1S）-2,2,5,7-四氟-2,3-二氢-1H-茚-1-基]磺酰胺，N - [（1S） -2,2,4,7-四氟-2,3-二氢-1H-茚-1-基]磺酰胺，（+） - N-（2,2,4,6,7-五氟-2,3- 二氢-1H-茚-1-基）磺酰胺，具有改善小鼠诱发模型中的发作严重程度指数（Score）的作用。 因此，期望化合物或其盐作为治疗癫痫的药物。

公开(公告)号：US20160303058A1

公开(公告)日：2016-10-20

申请号：US15102046

申请日：2014-12-17

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

Inventor： Hiroyuki Higashiyama ,  Yuji Kazuta ,  Keisuke Hashimoto

IPC: A61K31/165

CPC classification number: A61K31/165 ,  A61K31/18

Abstract: A medicine comprising a 1-indansulfamides compound such as N-[(1S)-2,2,5,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide, or N-[(1S)-2,2-difluoro-7-methyl-2,3-dihydro-1H-indene-1-yl]sulfamide or a pharmaceutically acceptable salt thereof, has an analgesic effects in the mouse hot-plate test and rat constriction nerve injury model and thus holds promise as a therapeutic agent for acute and chronic pain.

Abstract translation: 包含诸如N - [（1S）-2,2,5,7-四氟-2,3-二氢-1H-茚-1-基]磺酰胺的1-二氢化茚磺酰胺化合物或N - [（1S） -2,2-二氟-7-甲基-2,3-二氢-1H-茚-1-基]磺酰胺或其药学上可接受的盐在小鼠热板试验和大鼠收缩神经损伤模型中具有镇痛作用 因此作为急性和慢性疼痛的治疗剂具有希望。

公开(公告)号：US20140371319A1

公开(公告)日：2014-12-18

申请号：US14370633

申请日：2013-06-17

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

Inventor： Yuji Kazuta ,  Toru Watanabe ,  Keiichi Sorimachi ,  Minako Saito ,  Yoichi Kita ,  Toshiaki Tanaka ,  Hiroyuki Higashiyama ,  Takahisa Hanada ,  Tetsuyuki Teramoto ,  Takashi Kosasa ,  Yukio Ishikawa

IPC: C07C307/08

CPC classification number: C07C307/08 ,  A61K31/18 ,  C07C309/00 ,  C07C2602/08

Abstract: Novel indansulfamide derivatives or a pharmaceutically acceptable salt thereof such as N-[(1S)-2,2,5,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide, N-[(1S)-2,2,4,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide, (+)-N-(2,2,4,6,7-pentafluoro-2,3-dihydro-1H-inden-1-yl)sulfamide, have an action of improving Seizure Severity Index (Score) in mice kindling model. Thus the compounds or the salt thereof are expected as a drug for treating epilepsy.

Abstract translation: 新型的茚满磺酰胺衍生物或其药学上可接受的盐，例如N - [（1S）-2,2,5,7-四氟-2,3-二氢-1H-茚-1-基]磺酰胺，N - [（1S） -2,2,4,7-四氟-2,3-二氢-1H-茚-1-基]磺酰胺，（+） - N-（2,2,4,6,7-五氟-2,3- 二氢-1H-茚-1-基）磺酰胺，具有改善小鼠诱发模型中的发作严重程度指数（Score）的作用。 因此，期望化合物或其盐作为治疗癫痫的药物。