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公开(公告)号:US08815851B2
公开(公告)日:2014-08-26
申请号:US13768557
申请日:2013-02-15
申请人: Shionogi & Co., Ltd.
发明人: Naotake Kobayashi , Kazuo Ueda , Naohiro Itoh , Shinji Suzuki , Gaku Sakaguchi , Akira Kato , Akira Yukimasa , Akihiro Hori , Yuji Koriyama , Hidekazu Haraguchi , Ken Yasui , Yasuhiko Kanda
IPC分类号: C07D265/08 , C07D405/10 , A61K31/535
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 NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b 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; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.
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公开(公告)号:US10183949B2
公开(公告)日:2019-01-22
申请号:US15441385
申请日:2017-02-24
发明人: Tetsuo Nagano , Takayoshi Okabe , Hirotatsu Kojima , Mitsuyasu Kawaguchi , Osamu Nureki , Ryuichiro Ishitani , Hiroshi Nishimasu , Junken Aoki , Nobuyuki Tanaka , Yasuhiko Kanda , Yoshiyuki Kioi , Yusuke Tateno , Shiro Kida , Junji Yamane
IPC分类号: C07D491/107 , C07D239/47 , C07D239/36 , C07D405/12 , C07D401/12 , C07D403/06 , C07D413/06 , C07D471/08 , C07D409/12 , C07D417/12 , C07D413/12 , C07D403/12 , C07D401/04 , C07D403/04 , C07D471/10
摘要: A compound according to any one of formula (Ia) to (Ic), or its pharmaceutically acceptable salt: wherein R1, R2, R3, R4a, R4c, R5 are as defined in the description.
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公开(公告)号:US20140058097A1
公开(公告)日:2014-02-27
申请号:US14070202
申请日:2013-11-01
申请人: Shionogi & Co., Ltd.
发明人: Naotake Kobayashi , Kazuo Ueda , Naohiro Itoh , Shinji Suzuki , Gaku Sakaguchi , Akira Kato , Akira Yukimasa , Akihiro Hori , Yuuji Kooriyama , Hidekazu Haraguchi , Ken Yasui , Yasuhiko Kanda
IPC分类号: C07D471/04 , C07D295/192 , C07D279/06 , C07D285/36 , C07D277/18 , C07D405/04 , C07D295/155 , C07D265/08 , C07D417/12 , C07D417/04
CPC分类号: C07D471/04 , A61K9/0019 , A61K9/1623 , A61K9/2018 , A61K31/426 , A61K31/506 , A61K31/535 , A61K31/54 , A61K31/541 , A61K31/554 , C07D239/14 , C07D265/08 , C07D277/18 , C07D279/06 , C07D281/02 , C07D285/36 , C07D295/155 , C07D295/192 , C07D405/04 , C07D417/04 , C07D417/10 , C07D417/12 , A61K2300/00
摘要: A pharmaceutical composition for treating Alzheimer's disease 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, etc.; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2, R2b, R3a, R3b, R4a and R4b are each independently a hydrogen atom, halogen, hydroxy, etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 1 to 3; and R5 is a hydrogen atom, optionally substituted lower alkyl, etc.; its pharmaceutically acceptable salt, or a solvate thereof as an active ingredient.
摘要翻译: 一种用于治疗含有由通式(I)表示的化合物的阿尔茨海默病的药物组合物:其中环A是任选取代的碳环基团或任选取代的杂环基团; E为低级亚烷基等; X是S,O或NR1; R1是氢原子或低级烷基; R2,R2b,R3a,R3b,R4a和R4b各自独立地为氢原子,卤素,羟基等; n和m各自独立地为0〜3的整数, n + m为1〜3的整数, R5为氢原子,任意取代的低级烷基等; 其药学上可接受的盐或其溶剂合物作为活性成分。
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公开(公告)号:US09572813B2
公开(公告)日:2017-02-21
申请号:US14603979
申请日:2015-01-23
申请人: SHIONOGI & CO., LTD.
发明人: Ryuichi Kiyama , Yasuhiko Kanda , Yukio Tada , Toshio Fujishita , Takashi Kawasuji , Shozo Takechi , Masahiro Fuji
IPC分类号: A61K31/4015 , A61K31/4412 , A61K31/351 , A61K31/37 , A61K31/341 , A61K31/5377 , A61K31/4025 , A61K31/4155 , A61K31/4178 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/4427 , A61K31/4433 , A61K31/4439 , A61K31/4709 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , C07D207/38 , C07D307/46 , C07D401/04 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/06 , C07D407/06 , C07D409/06 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , A61K31/4196 , A61K31/513
CPC分类号: C07D417/06 , A61K31/351 , A61K31/4025 , A61K31/4155 , A61K31/4178 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/4427 , A61K31/4433 , A61K31/4439 , A61K31/4709 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/513 , A61K31/53 , A61K31/5377 , C07D207/38 , C07D307/46 , C07D311/24 , C07D401/04 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/06 , C07D407/06 , C07D409/06 , C07D409/14 , C07D413/04 , C07D413/06 , C07D417/04
摘要: The present invention provides an integrase inhibitor. The inventors have found the following compound of formula (I) possessing an integrase inhibitory activity. (wherein, RC and RD taken together with the neighboring carbon atoms form a ring which may be a condensed ring, Y is hydroxyl, mercapto or amino; Z is O, S or NH; RA is a group shown by (wherein, C ring is N-containing aromatic heterocycle) or the like).
摘要翻译: 本发明提供了一种整合酶抑制剂。 本发明人已经发现下列具有整合酶抑制活性的式(I)化合物。 (其中R C和R D与相邻的碳原子一起形成可以是稠环的环,Y是羟基,巯基或氨基; Z是O,S或NH; A>是由
表示的基团(其中,C环是含N芳香族杂环)等) -
公开(公告)号:US08895548B2
公开(公告)日:2014-11-25
申请号:US14070202
申请日:2013-11-01
申请人: Shionogi & Co., Ltd.
发明人: Naotake Kobayashi , Kazuo Ueda , Naohiro Itoh , Shinji Suzuki , Gaku Sakaguchi , Akira Kato , Akira Yukimasa , Akihiro Hori , Yuuji Kooriyama , Hidekazu Haraguchi , Ken Yasui , Yasuhiko Kanda
IPC分类号: A61K31/535 , A61K31/541 , C07D471/04 , C07D239/14 , C07D265/08 , C07D277/18 , C07D279/06 , C07D281/02 , C07D405/04 , C07D417/04 , C07D417/10 , C07D417/12 , C07D285/36 , C07D295/155 , C07D295/192
CPC分类号: C07D471/04 , A61K9/0019 , A61K9/1623 , A61K9/2018 , A61K31/426 , A61K31/506 , A61K31/535 , A61K31/54 , A61K31/541 , A61K31/554 , C07D239/14 , C07D265/08 , C07D277/18 , C07D279/06 , C07D281/02 , C07D285/36 , C07D295/155 , C07D295/192 , C07D405/04 , C07D417/04 , C07D417/10 , C07D417/12 , A61K2300/00
摘要: A pharmaceutical composition for treating Alzheimer's disease 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, etc.; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2, R2b, R3a, R3b, R4a and R4b are each independently a hydrogen atom, halogen, hydroxy, etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 1 to 3; and R5 is a hydrogen atom, optionally substituted lower alkyl, etc.; its pharmaceutically acceptable salt, or a solvate thereof as an active ingredient.
摘要翻译: 一种用于治疗含有由通式(I)表示的化合物的阿尔茨海默病的药物组合物:其中环A是任选取代的碳环基团或任选取代的杂环基团; E为低级亚烷基等; X是S,O或NR1; R1是氢原子或低级烷基; R2,R2b,R3a,R3b,R4a和R4b各自独立地为氢原子,卤素,羟基等; n和m各自独立地为0〜3的整数, n + m为1〜3的整数, R5为氢原子,任意取代的低级烷基等; 其药学上可接受的盐或其溶剂合物作为活性成分。
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公开(公告)号:US09029358B2
公开(公告)日:2015-05-12
申请号:US13941082
申请日:2013-07-12
申请人: Shionogi & Co., Ltd.
发明人: Naotake Kobayashi , Kazuo Ueda , Naohiro Itoh , Shinji Suzuki , Gaku Sakaguchi , Akira Kato , Akira Yukimasa , Akihiro Hori , Yuji Koriyama , Hidekazu Haraguchi , Ken Yasui , Yasuhiko Kanda
IPC分类号: C07D405/04 , C07D405/10 , A61K31/553 , C07D281/02 , C07D239/42 , A61K31/426 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/54 , A61K31/541 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/554 , C07D239/14 , C07D239/24 , C07D265/08 , C07D277/18 , C07D279/08 , 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
摘要: A composition having BACE 1 inhibitory activity containing a compound represented by the 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 NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a, and R4b, is each independently a hydrogen atom, halogen, or hydroxyl etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt or a solvate thereof.
摘要翻译: 一种具有BACE 1抑制活性的组合物,其含有式(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NR1; R1是氢原子或低级烷基; R2a,R2b,R3a,R3b,R4a和R4b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, R5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化物。
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