公开(公告)号：US20170137436A1

公开(公告)日：2017-05-18

申请号：US15346912

申请日：2016-11-09

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

Inventor： Toshiki Kurokawa ,  Yu Yoshida ,  Kogyoku Shin ,  Yoshihisa Kobayashi ,  Hironori Fukumoto ,  Kunitoshi Takeda ,  Yoshiaki Ohashi ,  Makoto Kotake ,  Tomoyuki Shibuguchi ,  Toru Watanabe ,  Yoichi Kita ,  Shinsuke Hirota ,  Takashi Fukuyama ,  Yasuaki Kamada

IPC: C07D491/147 ,  C07D491/052

CPC classification number: C07D491/147 ,  C07D491/052

Abstract: Compounds represented by formulae (I) to (XXII) or pharmaceutically acceptable salts thereof:

公开(公告)号：US08946211B2

公开(公告)日：2015-02-03

申请号：US13804691

申请日：2013-03-14

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

Inventor： Yuichi Suzuki ,  Takafumi Motoki ,  Toshihiko Kaneko ,  Mamoru Takaishi ,  Tasuku Ishida ,  Yoichi Kita ,  Kunitoshi Takeda ,  Noboru Yamamoto ,  Afzal Khan ,  Paschalis Dimopoulos

IPC: C07D513/02 ,  A61K31/542

CPC classification number: A61K31/542 ,  C07D279/08 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.

公开(公告)号：US11479552B2

公开(公告)日：2022-10-25

申请号：US17376452

申请日：2021-07-15

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

Inventor： Yu Yoshida ,  Yoichi Kita ,  Makoto Kotake ,  Keiichi Sorimachi ,  Toshiyuki Ohfusa ,  Takafumi Motoki ,  Taro Asaba

IPC: C07D401/14 ,  C07D471/08

Abstract: Provided are compounds represented by the following formulas (I), (II), (III) and (IV) having orexin type 2 receptor-activating activity, or their pharmaceutically acceptable salts.

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。

公开(公告)号：US20130203741A1

公开(公告)日：2013-08-08

申请号：US13804691

申请日：2013-03-14

Applicant: EISAI R&D MANAGEMENT CO., LTD.

Inventor： Yuichi Suzuki ,  Takafumi Motoki ,  Toshihiko Kaneko ,  Mamoru Takaishi ,  Tasuku Ishida ,  Yoichi Kita ,  Kunitoshi Takeda ,  Noboru Yamamoto ,  Afzal Khan ,  Paschalis Dimopoulos

IPC: A61K31/542

CPC classification number: A61K31/542 ,  C07D279/08 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.

公开(公告)号：US09738656B2

公开(公告)日：2017-08-22

申请号：US15346912

申请日：2016-11-09

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

Inventor： Toshiki Kurokawa ,  Yu Yoshida ,  Kogyoku Shin ,  Yoshihisa Kobayashi ,  Hironori Fukumoto ,  Kunitoshi Takeda ,  Yoshiaki Ohashi ,  Makoto Kotake ,  Tomoyuki Shibuguchi ,  Toru Watanabe ,  Yoichi Kita ,  Shinsuke Hirota ,  Takashi Fukuyama ,  Yasuaki Kamada

IPC: C07D491/147 ,  C07D491/052

CPC classification number: C07D491/147 ,  C07D491/052

Abstract: Compounds represented by formulae (I) to (XXII) or pharmaceutically acceptable salts thereof:

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。