公开(公告)号：US09458176B2

公开(公告)日：2016-10-04

申请号：US14190356

申请日：2014-02-26

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

Inventor： Mamoru Takaishi ,  Nobuhiro Sato ,  Tomoyuki Shibuguchi ,  Takafumi Motoki ,  Yoshinori Takahashi ,  Takeo Sasaki ,  Alan Braunton

IPC: A61K31/553 ,  C07D498/04

CPC classification number: C07D498/04

Abstract: A compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof works as an mGluR2 antagonist, and is applicable as a therapeutic agent for neurological disorders related to glutamate dysfunction and diseases involving the mGluR2, such as Alzheimer's disease: wherein R is a hydrogen atom, a C1-6 alkyl group or the like, R1 is a C1-6 alkyl group, a C1-6 alkoxy group or the like, R2 is a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or the like, R3 is a hydrogen atom, a C1-6 alkyl group or the like, and R4 is a C1-6 alkyl group or the like.

公开(公告)号：US12253526B2

公开(公告)日：2025-03-18

申请号：US17163993

申请日：2021-02-01

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

Inventor： Daiki Hara ,  Takafumi Motoki ,  Yuji Kazuta ,  Yoshihiko Norimine ,  Hiroyuki Amino ,  Masatoshi Suganuma ,  Shingo Fujiyama ,  Kazuto Yamashita ,  Masaya Okada ,  Yoichi Nishikawa ,  Shigeki Iwanaga

IPC: C09B57/00 ,  G01N21/64 ,  G01N33/58

Abstract: Disclosed is: a fluorescent dye comprising a compound, a tautomer of the compound, or a salt of the compound or the tautomer; a labeled composite substance comprising the fluorescent dye and a composite substance which are bonded to each other; a composition containing the fluorescent dye or the labeled composite substance; and a method for acquiring information about a substance of interest by a super-resolution microscopy.

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：US20160052937A1

公开(公告)日：2016-02-25

申请号：US14830970

申请日：2015-08-20

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

Inventor： Mamoru Takaishi ,  Nobuhiro Sato ,  Takafumi Motoki ,  Tomoyuki Shibuguchi

IPC: C07D498/04

CPC classification number: C07D498/04

Abstract: A compound represented by formula (I): wherein R is a methyl group or the like, R1 is a fluorine atom or the like, R2 is a hydrogen atom or a fluorine atom, R3 is a hydrogen atom, R4 is an ethyl group or the like, or a pharmaceutically acceptable salt thereof.

Abstract translation: 由式（I）表示的化合物：其中R是甲基等，R 1是氟原子等，R 2是氢原子或氟原子，R 3是氢原子，R 4是乙基或 或其药学上可接受的盐。

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：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：US20140243316A1

公开(公告)日：2014-08-28

申请号：US14190356

申请日：2014-02-26

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

Inventor： Mamoru Takaishi ,  Nobuhiro Sato ,  Tomoyuki Shibuguchi ,  Takafumi Motoki ,  Yoshinori Takahashi ,  Takeo Sasaki ,  Alan Braunton

IPC: C07D498/04

CPC classification number: C07D498/04

Abstract: A compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof works as an mGluR2 antagonist, and is applicable as a therapeutic agent for neurological disorders related to glutamate dysfunction and diseases involving the mGluR2, such as Alzheimer's disease: wherein R is a hydrogen atom, a C1-6 alkyl group or the like, R1 is a C1-6 alkyl group, a C1-6 alkoxy group or the like, R2 is a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or the like, R3 is a hydrogen atom, a C1-6 alkyl group or the like, and R4 is a C1-6 alkyl group or the like.

Abstract translation: 由下式（I）表示的化合物或其药学上可接受的盐作为mGluR2拮抗剂起作用，可用作与谷氨酸功能障碍相关的神经障碍和涉及mGluR2的疾病如阿尔茨海默氏病的治疗剂：其中R为 氢原子，C 1-6烷基等，R 1为C 1-6烷基，C 1-6烷氧基等，R 2为卤素原子，C 1-6烷基，C 1-6 烷氧基等，R3是氢原子，C1-6烷基等，R4是C1-6烷基等。

公开(公告)号：US20210255191A1

公开(公告)日：2021-08-19

申请号：US17163993

申请日：2021-02-01

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

Inventor： Daiki HARA ,  Takafumi Motoki ,  Yuji Kazuta ,  Yoshihiko Norimine ,  Hiroyuki Amino ,  Masatoshi Suganuma ,  Shingo Fujiyama ,  Kazuto Yamashita ,  Masaya Okada ,  Yoichi Nishikawa ,  Shigeki Iwanaga

IPC: G01N33/58 ,  C09B57/00 ,  G01N21/64

Abstract: Disclosed is: a fluorescent dye comprising a compound, a tautomer of the compound, or a salt of the compound or the tautomer; a labeled composite substance comprising the fluorescent dye and a composite substance which are bonded to each other; a composition containing the fluorescent dye or the labeled composite substance; and a method for acquiring information about a substance of interest by a super-resolution microscopy.