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。

公开(公告)号：US08592408B2

公开(公告)日：2013-11-26

申请号：US13685109

申请日：2012-11-26

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

Inventor： Adrian Hall ,  Christopher Neil Farthing

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，单氟甲基，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Aβ产生抑制作用或BACE1抑制作用，可用作由Abeta引起的以阿尔茨海默氏型痴呆为代表的神经变性疾病的预防或治疗剂。

公开(公告)号：US20130203740A1

公开(公告)日：2013-08-08

申请号：US13685109

申请日：2012-11-26

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

Inventor： Adrian Hall ,  Christopher Neil Farthing

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，单氟甲基，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Aβ产生抑制作用或BACE1抑制作用，可用作由Abeta引起的以阿尔茨海默氏型痴呆为代表的神经变性疾病的预防或治疗剂。