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1.发明公开Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors 有权氨基噻唑烷 - 和氨基四氢噻嗪衍生物BACE 1-抑制素
公开(公告)号：EP2612854A1
公开(公告)日：2013-07-10
申请号：EP13150548.9
申请日：2006-10-23
申请人： Shionogi & Co., Ltd.
发明人： Kobayashi, Naotake , Ueda, Kazuo , Itoh, Naohiro , Suzuki, Shinji , Sakaguchi, Gaku , Kato, Akira , Yukimasa, Akira , Hori, Akihiro , Koriyama, Yuji , Haraguchi, Hidekazu , Yasui, Ken , Kanda, Yasuhiko
IPC分类号： C07D239/14 , A61K31/426 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/54 , A61K31/541 , A61K31/545
CPC分类号： C07D417/14 , A61K9/0019 , A61K9/1623 , A61K9/2018 , A61K31/426 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/54 , A61K31/541 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/554 , C07D239/14 , C07D239/24 , C07D239/42 , C07D265/08 , C07D277/18 , C07D279/06 , C07D279/08 , C07D279/12 , C07D281/02 , C07D405/04 , C07D405/10 , C07D417/04 , C07D417/10 , C07D417/12 , C07D471/04
摘要： A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I):
wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group;
E is lower alkylene;
X is S, O, or NR 1 ;
R 1 is a hydrogen atom or lower alkyl;
R 2a , R 2b , R 3a , R 3b , R 4a and R 4b is each independently a hydrogen atom, halogen, or hydroxy etc.;
n and m are each independently an integer of 0 to 3;
n+m is an integer of 0 to 3;
R 5 is a hydrogen atom or substituted lower alkyl;
its pharmaceutically acceptable salt, or a solvate thereof.摘要翻译： 具有BACE 1抑制活性的组合物，其含有通式（I）表示的化合物：其中环A为任选取代的碳环基或任选取代的杂环基; E为低级亚烷基; X是S，O或NR 1; R 1是氢原子或低级烷基; R 2a，R 2b，R 3a，R 3b，R 4a和R 4b各自独立地为氢原子，卤素或羟基等; n和m各自独立地为0〜3的整数; n + m为0〜3的整数， R 5是氢原子或取代的低级烷基; 其药学上可接受的盐或其溶剂合物。
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2.发明授权
公开(公告)号：EP2597087B1
公开(公告)日：2016-03-30
申请号：EP13150550.5
申请日：2006-10-23
申请人： Shionogi & Co., Ltd.
发明人： Kobayashi, Naotake , Ueda, Kazuo , Itoh, Naohiro , Suzuki, Shinji , Sakaguchi, Gaku , Kato, Akira , Yukimasa, Akira , Hori, Akihiro , Koriyama, Yuji , Haraguchi, Hidekazu , Yasui, Ken , Kanda, Yasuhiko
IPC分类号： C07D239/14 , A61K31/505 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/554 , A61P25/28 , A61P43/00 , C07D239/24 , C07D265/08 , C07D277/18 , C07D279/06 , C07D279/08 , C07D281/02 , C07D405/04 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04
CPC分类号： C07D417/14 , A61K9/0019 , A61K9/1623 , A61K9/2018 , A61K31/426 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/54 , A61K31/541 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/554 , C07D239/14 , C07D239/24 , C07D239/42 , C07D265/08 , C07D277/18 , C07D279/06 , C07D279/08 , C07D279/12 , C07D281/02 , C07D405/04 , C07D405/10 , C07D417/04 , C07D417/10 , C07D417/12 , C07D471/04
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3.发明授权Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors 有权氨基噻唑烷和氨基四氢硫代吖庚因衍生物作为BACE1抑制剂
公开(公告)号：EP2612854B1
公开(公告)日：2015-04-29
申请号：EP13150548.9
申请日：2006-10-23
申请人： Shionogi & Co., Ltd.
发明人： Kobayashi, Naotake , Ueda, Kazuo , Itoh, Naohiro , Suzuki, Shinji , Sakaguchi, Gaku , Kato, Akira , Yukimasa, Akira , Hori, Akihiro , Koriyama, Yuji , Haraguchi, Hidekazu , Yasui, Ken , Kanda, Yasuhiko
IPC分类号： C07D239/14 , A61K31/426 , A61K31/505 , A61K31/535 , A61K31/54 , A61K31/55 , A61K31/551 , C07D239/24 , C07D265/08 , C07D277/18 , C07D279/06 , C07D281/02 , C07D405/04 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04
CPC分类号： C07D417/14 , A61K9/0019 , A61K9/1623 , A61K9/2018 , A61K31/426 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/54 , A61K31/541 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/554 , C07D239/14 , C07D239/24 , C07D239/42 , C07D265/08 , C07D277/18 , C07D279/06 , C07D279/08 , C07D279/12 , C07D281/02 , C07D405/04 , C07D405/10 , C07D417/04 , C07D417/10 , C07D417/12 , C07D471/04
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4.发明公开
公开(公告)号：EP2597087A1
公开(公告)日：2013-05-29
申请号：EP13150550.5
申请日：2006-10-23
申请人： Shionogi & Co., Ltd.
发明人： Kobayashi, Naotake , Ueda, Kazuo , Itoh, Naohiro , Suzuki, Shinji , Sakaguchi, Gaku , Kato, Akira , Yukimasa, Akira , Hori, Akihiro , Koriyama, Yuji , Haraguchi, Hidekazu , Yasui, Ken , Kanda, Yasuhiko
IPC分类号： C07D239/14 , A61K31/426 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/54 , A61K31/541
CPC分类号： C07D417/14 , A61K9/0019 , A61K9/1623 , A61K9/2018 , A61K31/426 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/54 , A61K31/541 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/554 , C07D239/14 , C07D239/24 , C07D239/42 , C07D265/08 , C07D277/18 , C07D279/06 , C07D279/08 , C07D279/12 , C07D281/02 , C07D405/04 , C07D405/10 , C07D417/04 , C07D417/10 , C07D417/12 , C07D471/04
摘要： A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I):
wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group;
E is lower alkylene;
X is S, O, or NR 1 ;
R 1 is a hydrogen atom or lower alkyl;
R 2a , R 2b , R 3a , R 3b , R 4a and R 4b is each independently a hydrogen atom, halogen, or hydroxy etc.;
n and m are each independently an integer of 0 to 3;
n+m is an integer of 0 to 3;
R 5 is a hydrogen atom or substituted lower alkyl;
its pharmaceutically acceptable salt, or a solvate thereof.摘要翻译： 具有BACE 1抑制活性的组合物，其含有通式（I）表示的化合物：其中环A为任选取代的碳环基或任选取代的杂环基; E为低级亚烷基; X是S，O或NR 1; R 1是氢原子或低级烷基; R 2a，R 2b，R 3a，R 3b，R 4a和R 4b各自独立地为氢原子，卤素或羟基等; n和m各自独立地为0〜3的整数; n + m为0〜3的整数， R 5是氢原子或取代的低级烷基; 其药学上可接受的盐或其溶剂合物。
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