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公开(公告)号：EP2241567A1
公开(公告)日：2010-10-20
申请号：EP09710649.6
申请日：2009-02-09
发明人： OZAKI, Fumihiro , SOEJIMA, Motohiro , ISHIDA, Tasuku , NORIMINE, Yoshihiko , KURUSU, Nobuyuki , DOI, Eriko , KANEKO, Toshihiko , HASEGAWA, Daiju , KOBAYASHI, Kiyoaki , YAMAMOTO, Noboru
IPC分类号： C07D451/06 , A61K31/439 , A61K31/46 , A61K31/4985 , A61K31/53 , A61K31/5377 , A61K31/5383 , A61K31/55 , A61P3/12 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/20 , A61P29/02 , A61P43/00 , C07D451/14 , C07D519/00
CPC分类号： C07D451/06 , C07D451/02 , C07D451/04 , C07D519/00
摘要： Compounds represented by formula (I) and pharmaceutically acceptable salts thereof have excellent sodium channel inhibitory action and are useful as therapeutic agents and analgesics for various kinds of neuralgia, neuropathy, epilepsy, insomnia, premature ejaculation and the like.
wherein Q represents ethylene, etc., R 1 , R 2 and R 3 represent hydrogen, etc., X 1 represents C 1-6 alkylene, etc., X 2 represents C 1-6 alkylene, etc., A 1 represents a 5- to 6-membered heterocyclic group, etc., and A 2 represents C 6-14 aryl, etc.摘要翻译： 由式（I）表示的化合物及其药学上可接受的盐具有优异的钠通道抑制作用，可用作各种神经痛，神经病，癫痫，失眠，早泄等的治疗剂和止痛剂。 其中Q表示乙烯等，R 1，R 2和R 3表示氢等，X 1表示C 1-6亚烷基等，X 2表示C 1-6亚烷基等，A 1表示 5-至6-元杂环基等，A 2表示C 6-14芳基等
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公开(公告)号：EP2233474B1
公开(公告)日：2015-08-05
申请号：EP09701914.5
申请日：2009-01-16
发明人： SUZUKI, Yuichi , MOTOKI, Takafumi , KANEKO, Toshihiko , TAKAISHI, Mamoru , ISHIDA, Tasuku , TAKEDA, Kunitoshi , KITA, Yoichi , YAMAMOTO, Noboru , KHAN, Afzal , DIMOPOULOS, Paschalis
IPC分类号： C07D279/08 , A61K31/4439 , A61K31/5415 , A61K31/542 , A61P25/28 , A61P43/00 , C07D417/10 , C07D417/12 , C07D513/04 , C07D417/14
CPC分类号： A61K31/542 , C07D279/08 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04
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公开(公告)号：EP2665731A1
公开(公告)日：2013-11-27
申请号：EP12703573.1
申请日：2012-01-19
发明人： TAKAISHI, Mamoru , ISHIDA, Tasuku
IPC分类号： C07D513/04 , A61P25/28
CPC分类号： C07D513/04 , A61K31/542 , A61K45/06
摘要： The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; R is monofluoromethyl or difluoromethyl; and pharmaceutically acceptable salts thereof; which compound has an Αβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Αβ and typified by Alzheimer-type dementia.
摘要翻译： 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; R是单氟甲基或二氟甲基; 和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，并且可用作由Aβ引起并以阿尔茨海默型痴呆为代表的神经退行性疾病的预防或治疗剂。
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公开(公告)号：EP2233474A1
公开(公告)日：2010-09-29
申请号：EP09701914.5
申请日：2009-01-16
发明人： SUZUKI, Yuichi , MOTOKI, Takafumi , KANEKO, Toshihiko , TAKAISHI, Mamoru , ISHIDA, Tasuku , TAKEDA, Kunitoshi , KITA, Yoichi , YAMAMOTO, Noboru , KHAN, Afzal , DIMOPOULOS, Paschalis
IPC分类号： C07D279/08 , A61K31/4439 , A61K31/5415 , A61K31/542 , A61P25/28 , A61P43/00 , C07D417/10 , C07D417/12 , C07D513/04
CPC分类号： A61K31/542 , C07D279/08 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04
摘要： A compound represented by the general formula:
or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C 6-14 aryl group or the like, L is -NR e CO- or the like (wherein R e is a hydrogen atom or the like), Ring B is a C 6-14 aryl group or the like, X is a C 1-3 alkylene group or the like, Y is a single bond or the like, Z is a C 1-3 alkylene group or the like, R 1 and R 2 are each independently a hydrogen atom or the like, and R 3 , R 4 , R 5 and R 6 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.摘要翻译： 由通式表示的化合物或其药学上可接受的盐或其溶剂合物，其中环A为C 6-14芳基等，L为-NR e CO-等（其中R e为 氢原子等），环B为C 6-14芳基等，X为C 1-3亚烷基等，Y为单键等，Z为C 1-3 亚烷基等，R 1和R 2各自独立地为氢原子等，R 3，R 4，R 5和R 6独立地为氢原子，卤素原子等，具有A 2生成 抑制作用或BACE1抑制作用，可用作由A 2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。
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