公开(公告)号：US10072005B2

公开(公告)日：2018-09-11

申请号：US15875069

申请日：2018-01-19

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

Inventor： Andrew Payne ,  Jose Luis Castro Pineiro ,  Louise Michelle Birch ,  Afzal Khan ,  Alan James Braunton ,  James Edward Kitulagoda ,  Motohiro Soejima

IPC: C07D471/04 ,  A61K31/437 ,  C07D401/04

CPC classification number: C07D471/04 ,  C07D401/04

Abstract: 4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as Alzheimer-type dementia (AD) or dementia with Lewy bodies (DLB), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient.

公开(公告)号：US20180208593A1

公开(公告)日：2018-07-26

申请号：US15875069

申请日：2018-01-19

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

Inventor： Andrew Payne ,  Jose Luis Castro Pineiro ,  Louise Michelle Birch ,  Afzal Khan ,  Alan James Braunton ,  James Edward Kitulagoda ,  Motohiro Soejima

IPC: C07D471/04 ,  C07D401/04

CPC classification number: C07D471/04 ,  C07D401/04

Abstract: 4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as Alzheimer-type dementia (AD) or dementia with Lewy bodies (DLB), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient.

公开(公告)号：US20160244445A1

公开(公告)日：2016-08-25

申请号：US15025996

申请日：2014-09-30

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

Inventor： Andrew Payne ,  Jose Luis Castro Pineiro ,  Louise Michelle Birch ,  Afzal Khan ,  Alan James Braunton ,  James Edward Kitulagoda ,  Motohiro Soejima

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07D401/04

Abstract: 4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as Alzheimer-type dementia (AD) or dementia with Lewy bodies (DLB), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient.

公开(公告)号：US09926312B2

公开(公告)日：2018-03-27

申请号：US15025996

申请日：2014-09-30

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

Inventor： Andrew Payne ,  Jose Luis Castro Pineiro ,  Louise Michelle Birch ,  Afzal Khan ,  Alan James Braunton ,  James Edward Kitulagoda ,  Motohiro Soejima

IPC: C07D471/04 ,  A61K31/437 ,  C07D401/04

CPC classification number: C07D471/04 ,  C07D401/04

Abstract: 4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as Alzheimer-type dementia (AD) or dementia with Lewy bodies (DLB), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient.

公开(公告)号：US20150094328A1

公开(公告)日：2015-04-02

申请号：US14501355

申请日：2014-09-30

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

Inventor： Andrew Payne ,  Jose Luis Castro Pineiro ,  Louise Michelle Birch ,  Afzal Khan ,  Alan James Braunton ,  James Edward Kitulagoda ,  Motohiro Soejima

IPC: C07D401/04

CPC classification number: C07D471/04 ,  C07D401/04

Abstract: 4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as Alzheimer-type dementia (AD) or dementia with Lewy bodies (DLB), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient.

Abstract translation: 作为毒蕈碱乙酰胆碱受体（mAChR）M1的调节剂的4-氮杂吲哚衍生物，其可用于预防或疾病改善或对症治疗与神经系统疾病如阿尔茨海默氏型痴呆（AD）或路易体痴呆相关的认知缺陷 （DLB）和包含4-氮杂吲哚衍生物作为活性成分的药物组合物。

公开(公告)号：US08940734B2

公开(公告)日：2015-01-27

申请号：US14057403

申请日：2013-10-18

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

Inventor： Adrian Hall ,  Christopher Neil Farthing ,  Jose Luis Castro Pineiro

IPC: C07D513/04 ,  A61K31/542

CPC classification number: C07D513/04

Abstract: The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or —C≡N; and pharmaceutically acceptable salts thereof; which compound 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.

Abstract translation: 本发明涉及式（I）的稠合氨基二氢噻嗪衍生物：其中X是氢或氟; A是CH或N; Y是甲基，乙基，一氟甲基，二氟甲基，三氟甲基，二氟乙基，甲氧基，乙氧基，甲氧基甲基或-C≡N; 及其药学上可接受的盐; 该化合物具有A＆bgr; 产生抑制作用或BACE1抑制作用，可用作由A＆Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。

公开(公告)号：US20140142091A1

公开(公告)日：2014-05-22

申请号：US14057403

申请日：2013-10-18

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

Inventor： Adrian Hall ,  Christopher Neil Farthing ,  Jose Luis Castro Pineiro

IPC: C07D513/04

CPC classification number: C07D513/04

Abstract: The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or —C≡N; and pharmaceutically acceptable salts thereof; which compound 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.

Abstract translation: 本发明涉及式（I）的稠合氨基二氢噻嗪衍生物：其中X是氢或氟; A是CH或N; Y是甲基，乙基，一氟甲基，二氟甲基，三氟甲基，二氟乙基，甲氧基，乙氧基，甲氧基甲基或-C≡N; 及其药学上可接受的盐; 该化合物具有A＆bgr; 产生抑制作用或BACE1抑制作用，可用作由A＆Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。