公开(公告)号：US20120015961A1

公开(公告)日：2012-01-19

申请号：US13260103

申请日：2010-03-29

申请人： Yuusuke Tamura ,  Shinji Suzuki ,  Sae Matsumoto ,  Akihiro Hori ,  Yuuji Kooriyama

发明人： Yuusuke Tamura ,  Shinji Suzuki ,  Sae Matsumoto ,  Akihiro Hori ,  Yuuji Kooriyama

IPC分类号： A61K31/44 ,  C07D241/24 ,  A61K31/4965 ,  C07D401/12 ,  A61K31/497 ,  C07C335/32 ,  A61K31/21 ,  C07D239/42 ,  A61K31/505 ,  A61K31/444 ,  C07D405/12 ,  A61P25/28 ,  A61P25/00 ,  A61P27/02 ,  A61P25/16 ,  C07D213/85

CPC分类号： C07D213/81 ,  C07C275/70 ,  C07C335/32 ,  C07D213/85 ,  C07D239/42 ,  C07D241/24 ,  C07D241/28 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12

摘要： The present invention provides, for example, a compound of the following formula (I): wherein R1 is substituted amino and the like, R2 is halogen and the like, R3 is substituted or unsubstituted lower alkyl and the like, RA and RB are each independently hydrogen, substituted or unsubstituted lower alkyl and the like, RC and RD are each independently hydrogen, substituted or unsubstituted lower alkyl, or RC and RD together with the carbon atom to which they are attached may form a substituted or unsubstituted carbocycle, and ring A is a carbocycle or a heterocycle, its pharmaceutically acceptable salt, or a solvate thereof as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-βproteins.

摘要翻译： 本发明提供例如下式（I）的化合物：其中R1是取代氨基等，R2是卤素等，R3是取代或未取代的低级烷基等，RA和RB各自 独立地是氢，取代或未取代的低级烷基等，RC和RD各自独立地为氢，取代或未取代的低级烷基或RC和RD与它们所连接的碳原子一起形成取代或未取代的碳环，并且环 A是碳环或杂环，其药学上可接受的盐或其溶剂合物作为由淀粉样蛋白质的蛋白质的产生，分泌和/或沉积诱导的疾病的治疗剂。

公开(公告)号：US08168630B2

公开(公告)日：2012-05-01

申请号：US12596796

申请日：2008-04-23

申请人： Yuusuke Tamura ,  Shinji Suzuki ,  Yukio Tada ,  Shuji Yonezawa ,  Chiaki Fujikoshi ,  Sae Matsumoto ,  Yuuji Kooriyama ,  Tatsuhiko Ueno

发明人： Yuusuke Tamura ,  Shinji Suzuki ,  Yukio Tada ,  Shuji Yonezawa ,  Chiaki Fujikoshi ,  Sae Matsumoto ,  Yuuji Kooriyama ,  Tatsuhiko Ueno

IPC分类号： C07D417/12 ,  C07D417/14 ,  A61K31/497 ,  A61K31/54

CPC分类号： C07C215/20 ,  A61K9/0019 ,  A61K9/1623 ,  A61K9/2018 ,  C07D279/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04

摘要： This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid β protein.

摘要翻译： 本发明提供式（I）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; R1是任选取代的低级烷基，任选取代的低级烯基，任选取代的低级炔基; R2a和R2b各自独立地为氢，任选取代的低级烷基或任选取代的酰基; R3a，R3b，R3c和R3d各自独立地为氢，卤素，羟基或任选取代的低级烷基等; 其药学上可接受的盐或溶剂合物，其可用于治疗由淀粉样蛋白的生产，分泌和/或沉积诱导的疾病; 蛋白。

公开(公告)号：US20100075957A1

公开(公告)日：2010-03-25

申请号：US12596796

申请日：2008-04-23

申请人： Yuusuke Tamura ,  Shinji Suzuki ,  Yukio Tada ,  Shuji Yonezawa ,  Chiaki Fujikoshi ,  Sae Matsumoto ,  Yuuji Kooriyama ,  Tatsuhiko Ueno

发明人： Yuusuke Tamura ,  Shinji Suzuki ,  Yukio Tada ,  Shuji Yonezawa ,  Chiaki Fujikoshi ,  Sae Matsumoto ,  Yuuji Kooriyama ,  Tatsuhiko Ueno

IPC分类号： A61K31/541 ,  C07D417/12 ,  A61P25/28

CPC分类号： C07C215/20 ,  A61K9/0019 ,  A61K9/1623 ,  A61K9/2018 ,  C07D279/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04

摘要： This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3 a, R3 b, R3 c and R3 d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid β protein.

摘要翻译： 本发明提供式（I）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; R1是任选取代的低级烷基，任选取代的低级烯基，任选取代的低级炔基; R2a和R2b各自独立地为氢，任选取代的低级烷基或任选取代的酰基; R3a，R3b，R3c和R3d各自独立地为氢，卤素，羟基或任选取代的低级烷基等; 其药学上可接受的盐或溶剂合物，其可用于治疗由淀粉样蛋白的生产，分泌和/或沉积诱导的疾病; 蛋白。

公开(公告)号：US08541408B2

公开(公告)日：2013-09-24

申请号：US13417786

申请日：2012-03-12

申请人： Yuusuki Tamura ,  Shinji Suzuki ,  Yukio Tada ,  Chiaki Fujikoshi ,  Sae Matsumoto ,  Yuuji Kooriyama

发明人： Yuusuki Tamura ,  Shinji Suzuki ,  Yukio Tada ,  Chiaki Fujikoshi ,  Sae Matsumoto ,  Yuuji Kooriyama

IPC分类号： C07D417/12 ,  C07D417/14 ,  A61K31/497 ,  A61K31/54

CPC分类号： C07C215/20 ,  A61K9/0019 ,  A61K9/1623 ,  A61K9/2018 ,  C07D279/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04

摘要： This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid β protein.

摘要翻译： 本发明提供式（I）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; R1是任选取代的低级烷基，任选取代的低级烯基，任选取代的低级炔基; R2a和R2b各自独立地为氢，任选取代的低级烷基或任选取代的酰基; R3a，R3b，R3c和R3d各自独立地为氢，卤素，羟基或任选取代的低级烷基等; 其药学上可接受的盐或溶剂合物，其可用于治疗由淀粉样β蛋白的产生，分泌和/或沉积诱导的疾病。

公开(公告)号：US08507479B2

公开(公告)日：2013-08-13

申请号：US13417786

申请日：2012-03-12

申请人： Yuusuki Tamura ,  Shinji Suzuki ,  Yukio Tada ,  Chiaki Fujikoshi ,  Sae Matsumoto ,  Yuuji Kooriyama

发明人： Yuusuki Tamura ,  Shinji Suzuki ,  Yukio Tada ,  Chiaki Fujikoshi ,  Sae Matsumoto ,  Yuuji Kooriyama

IPC分类号： C07D417/12 ,  C07D417/14 ,  A61K31/497 ,  A61K31/54

摘要： This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid β protein.

公开(公告)号：US20100160290A1

公开(公告)日：2010-06-24

申请号：US12597470

申请日：2008-04-23

申请人： Naotake Kobayashi ,  Kazuo Ueda ,  Naohiro Itoh ,  Shinji Suzuki ,  Gaku Sakaguchi ,  Akira Kato ,  Akira Yukimasa ,  Akihiro Hori ,  Yuuji Kooriyama ,  Hidekazu Haraguchi ,  Ken Yasui ,  Yasuhiko Kanda

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： A61K31/554 ,  C07D417/02 ,  A61K31/541 ,  C07D279/06 ,  C07D277/18 ,  A61K31/426 ,  C07D239/02 ,  A61K31/506 ,  C07D281/02 ,  A61P25/28

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; R2a, 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; R2a，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。

公开(公告)号：US20120258961A1

公开(公告)日：2012-10-11

申请号：US13518285

申请日：2010-12-22

申请人： Shinji Suzuki ,  Yuuji Kooriyama

发明人： Shinji Suzuki ,  Yuuji Kooriyama

IPC分类号： A61K31/54 ,  C12N9/99 ,  A61K31/541 ,  A61P25/28 ,  A61K31/536 ,  C07D413/12 ,  A61K31/5415 ,  C07D279/06 ,  C07D417/12 ,  C07D265/20

CPC分类号： C07D265/20 ,  A61K31/536 ,  A61K31/54 ,  A61K31/541 ,  A61K31/5415 ,  C07D279/06 ,  C07D279/16 ,  C07D413/12 ,  C07D417/12

摘要： The present invention provide a medicament for treating the diseases induced by production, secretion or deposition of amyloid-β proteins, for example, a compound of the following formula (I) wherein R1, R2a, R2b, R3a, R3b, R4a, R4b, ring A, Y and the dotted line are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.

摘要翻译： 本发明提供了用于治疗由淀粉样蛋白的生产，分泌或沉积诱导的疾病的药物。 蛋白质，例如下列通式（I）的化合物，其中R1，R2a，R2b，R3a，R3b，R4a，R4b，环A，Y和虚线在本说明书中定义，其药学上可接受的盐或溶剂合物 其中。

公开(公告)号：US08546380B2

公开(公告)日：2013-10-01

申请号：US13243971

申请日：2011-09-23

申请人： Naotake Kobayashi ,  Kazuo Ueda ,  Naohiro Itoh ,  Shinji Suzuki ,  Gaku Sakaguchi ,  Akira Kato ,  Akira Yukimasa ,  Akihiro Hori ,  Yuji Koriyama ,  Hidekazu Haraguchi ,  Ken Yasui ,  Yasuhiko Kanda

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： C07D279/00 ,  C07D265/00 ,  A61K31/535 ,  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 formula (I): wherein ring A is an optionally substituted heterocyclic group; E is lower alkylene; X is S; 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; or its pharmaceutically acceptable salt thereof.

摘要翻译： 一种具有BACE1抑制活性的组合物，其含有式（I）表示的化合物：其中环A为任选取代的杂环基; E为低级亚烷基; X是S; 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; 或其药学上可接受的盐。

公开(公告)号：US08633188B2

公开(公告)日：2014-01-21

申请号：US13243874

申请日：2011-09-23

申请人： Naotake Kobayashi ,  Kazuo Ueda ,  Naohiro Itoh ,  Shinji Suzuki ,  Gaku Sakaguchi ,  Akira Kato ,  Akira Yukimasa ,  Akihiro Hori ,  Yuji Koriyama ,  Hidekazu Haraguchi ,  Ken Yasui ,  Yasuhiko Kanda

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： A61K31/535 ,  A61K31/541 ,  C07D279/00 ,  C07D265/00

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.

摘要翻译： 一种具有BACE1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合物。

公开(公告)号：US08173642B2

公开(公告)日：2012-05-08

申请号：US12089409

申请日：2006-10-23

申请人： Naotake Kobayashi ,  Kazuo Ueda ,  Naohiro Itoh ,  Shinji Suzuki ,  Gaku Sakaguchi ,  Akira Kato ,  Akira Yukimasa ,  Akihiro Hori ,  Yuji Koriyama ,  Hidekazu Haraguchi ,  Ken Yasui ,  Yasuhiko Kanda

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： C07D417/12 ,  C07D417/14 ,  A61K31/497 ,  A61K31/54

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.

摘要翻译： 一种具有BACE1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合物。