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：US20130296352A1

公开(公告)日：2013-11-07

申请号：US13914898

申请日：2013-06-11

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

Inventor： Yoshihiko Norimine ,  Kunitoshi Takeda ,  Koji Hagiwara ,  Yuichi Suzuki ,  Yuki Ishihara ,  Nobuaki Sato

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: A compound and/or pharmacologically acceptable salt thereof represented by the formula (I) has PDE9 inhibitory action, so that the intracerebral cGMP concentration is anticipated to be elevated. The PDE9 inhibitory action and the increase in cGMP lead to the improvement of learning and memory behaviors, and the compound (I) has applicability as a therapeutic agent for cognitive dysfunctions in Alzheimer's disease. wherein R1 is a hydrogen atom; R2 is an aromatic ring group, etc.; R3 is a hydrogen atom, etc; R4 is a hydrogen atom; R5 is an oxepanyl group, etc.; R6 is a hydrogen atom.

公开(公告)号：US08563565B2

公开(公告)日：2013-10-22

申请号：US13644745

申请日：2012-10-04

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

Inventor： Yoshihiko Norimine ,  Kunitoshi Takeda ,  Koji Hagiwara ,  Yuichi Suzuki ,  Yuki Ishihara ,  Nobuaki Sato

IPC: A01N43/54 ,  A01N43/58 ,  A01N43/60 ,  A61K31/505 ,  A61K31/535 ,  C07D413/00 ,  C07D487/00 ,  C07D471/00 ,  C07D403/00

CPC classification number: C07D471/04

Abstract: A compound and/or pharmacologically acceptable salt thereof represented by the formula (I) has PDE9 inhibitory action, so that the intracerebral cGMP concentration is anticipated to be elevated. The PDE9 inhibitory action and the increase in cGMP lead to the improvement of learning and memory behaviors, and the compound (I) has a potential use of a therapeutic agent for cognitive dysfunctions in Alzheimer's disease. wherein R1 is a hydrogen atom; R2 is an aromatic ring group, etc.; R3 is a hydrogen atom, etc; R4 is a hydrogen atom; R5 is an oxepanyl group, etc.; R6 is a hydrogen atom.

Abstract translation: 由式（I）表示的化合物和/或其药理学上可接受的盐具有PDE9抑制作用，从而预期脑内cGMP浓度升高。 PDE9抑制作用和cGMP的增加导致学习和记忆行为的改善，并且化合物（I）在阿尔茨海默病中具有治疗剂对认知功能障碍的潜在用途。 其中R1是氢原子; R2是芳环等; R3是氢原子等; R4是氢原子; R5是氧环丙烷基等。 R6是氢原子。

公开(公告)号：US20130143907A1

公开(公告)日：2013-06-06

申请号：US13644745

申请日：2012-10-04

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

Inventor： Yoshihiko Norimine ,  Kunitoshi Takeda ,  Koji Hagiwara ,  Yuichi Suzuki ,  Yuki Ishihara ,  Nobuaki Sato

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: A compound and/or pharmacologically acceptable salt thereof represented by the formula (I) has PDE9 inhibitory action, so that the intracerebral cGMP concentration is anticipated to be elevated. The PDE9 inhibitory action and the increase in cGMP lead to the improvement of learning and memory behaviors, and the compound (I) has applicability as a therapeutic agent for cognitive dysfunctions in Alzheimer's disease. wherein R1 is a hydrogen atom; R2 is an aromatic ring group, etc.; R3 is a hydrogen atom, etc; R4 is a hydrogen atom; R5 is an oxepanyl group, etc.; R6 is a hydrogen atom.

Abstract translation: 由式（I）表示的化合物和/或其药理学上可接受的盐具有PDE9抑制作用，从而预期脑内cGMP浓度升高。 PDE9抑制作用和cGMP增加导致学习和记忆行为的改善，化合物（I）具有作为阿尔茨海默病认知功能障碍治疗剂的适用性。 其中R1是氢原子; R2是芳环等; R3是氢原子等; R4是氢原子; R5是氧环丙烷基等。 R6是氢原子。