公开(公告)号：US08927721B2

公开(公告)日：2015-01-06

申请号：US13881250

申请日：2011-10-27

申请人： Yasunori Mitsuoka ,  Yuuji Kooriyama

发明人： Yasunori Mitsuoka ,  Yuuji Kooriyama

IPC分类号： C07D471/04 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/497

CPC分类号： C07D471/04

摘要： The present invention provides, for example, the following compound: wherein ring Z is pyridine or a carbocycle, each of which is substituted or unsubstituted, ring A is a carbocycle or a heterocycle, each of which is substituted or unsubstituted, R1 is substituted or unsubstituted alkyl or the like, R2a, R2b, R4a and R4b are each independently hydrogen or substituted or unsubstituted alkyl or the like, its pharmaceutically acceptable salt or a solvate thereof having an effect of inhibiting amyloid β production, especially a BACE1 inhibitory activity, and useful as a medicament for treating diseases induced by production, secretion or deposition of amyloid β proteins.

摘要翻译： 本发明例如提供以下化合物：其中环Z为吡啶或碳环，其各自为取代或未取代的环，A为碳环或杂环，各自为取代或未取代的，R 1为取代或未取代的 未取代的烷基等，R2a，R2b，R4a和R4b各自独立地为氢或取代或未取代的烷基等，其药学上可接受的盐或其溶剂化物具有抑制淀粉样蛋白和bgr的作用; 生产，特别是BACE1抑制活性，并且可用作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。

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：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：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：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：US20130217705A1

公开(公告)日：2013-08-22

申请号：US13881250

申请日：2011-10-27

申请人： Yasunori Mitsuoka ,  Yuuji Kooriyama

发明人： Yasunori Mitsuoka ,  Yuuji Kooriyama

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： The present invention provides, for example, the following compound: wherein ring Z is pyridine or a carbocycle, each of which is substituted or unsubstituted, ring A is a carbocycle or a heterocycle, each of which is substituted or unsubstituted, R1 is substituted or unsubstituted alkyl or the like, R2a, R2b, R4a and R4b are each independently hydrogen or substituted or unsubstituted alkyl or the like, its pharmaceutically acceptable salt or a solvate thereof having an effect of inhibiting amyloid β production, especially a BACE1 inhibitory activity, and useful as a medicament for treating diseases induced by production, secretion or deposition of amyloid β proteins.

摘要翻译： 本发明例如提供以下化合物：其中环Z为吡啶或碳环，其各自为取代或未取代的环，A为碳环或杂环，各自为取代或未取代的，R 1为取代或未取代的 未取代的烷基等，R2a，R2b，R4a和R4b各自独立地为氢或取代或未取代的烷基等，其药学上可接受的盐或其溶剂化物具有抑制淀粉样蛋白β生成，特别是BACE1抑制活性的作用，以及 可用作治疗由淀粉样β蛋白的产生，分泌或沉积诱导的疾病的药物。

公开(公告)号：US20120245155A1

公开(公告)日：2012-09-27

申请号：US13514907

申请日：2010-12-09

申请人： Syuhei Yoshida ,  Issei Kato ,  Kouki Fuchino ,  Yuuji Kooriyama ,  Yoshiyasu Baba ,  Norihiko Tanimoto

发明人： Syuhei Yoshida ,  Issei Kato ,  Kouki Fuchino ,  Yuuji Kooriyama ,  Yoshiyasu Baba ,  Norihiko Tanimoto

IPC分类号： A61K31/542 ,  C07D417/12 ,  C07D498/04 ,  A61P25/28 ,  C07D279/08 ,  C07D265/18 ,  A61K31/5365 ,  C07D513/04 ,  C07D413/12

CPC分类号： C07D265/18 ,  A61K9/0019 ,  A61K9/1623 ,  A61K9/2018 ,  C07D279/08 ,  C07D417/12 ,  C07D498/04 ,  C07D513/04

摘要： The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-βproteins.A compound of the formula (I): wherein R1, R2a, R2b, R3, R4, R5a, R5b, R6a, R6b, X, Y, Z, ring A and the dashed lines are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.

摘要翻译： 本发明例如提供下述化合物作为治疗或预防淀粉样蛋白质的生产，分泌或沉积诱导的疾病的药物。 式（I）的化合物：其中R1，R2a，R2b，R3，R4，R5a，R5b，R6a，R6b，Xb，R6a，R6b，X，Y，Z，环A和虚线在说明书中定义，其药学上可接受的盐 或其溶剂合物。

公开(公告)号：US20110237576A1

公开(公告)日：2011-09-29

申请号：US13123761

申请日：2009-10-22

申请人： Shuji Yonezawa ,  Yuusuke Tamura ,  Yuuji Kooriyama ,  Gaku Sakaguchi

发明人： Shuji Yonezawa ,  Yuusuke Tamura ,  Yuuji Kooriyama ,  Gaku Sakaguchi

IPC分类号： A61K31/538 ,  C07D401/12 ,  A61K31/513 ,  C07D405/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D409/14 ,  C07D413/12 ,  C07D239/22 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D487/04 ,  A61K31/519 ,  C07D401/14 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/4439 ,  C07D213/74 ,  A61K31/44 ,  A61P25/28

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04

摘要： The present invention provides a compound which has an effect of inhibiting amyloid-β production and is useful as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-β proteins. The present invention relates to a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein A is optionally substituted carbocyclic diyl or optionally substituted heterocyclic diyl; B is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is a group such as optionally substituted lower alkyl; R2 is a group such as hydrogen; and R3a and R3b are each independently a group such as hydrogen, provided that the following compound is excluded.

摘要翻译： 本发明提供了具有抑制淀粉样蛋白的作用的化合物。 并且可用作由淀粉样蛋白的生产，分泌和/或沉积诱导的疾病的治疗剂。 蛋白质。 本发明涉及由式（I）表示的化合物或其药学上可接受的盐或溶剂合物：其中A是任选取代的碳环二基或任选取代的杂环二基; B是任选取代的碳环基团或任选取代的杂环基团; R1是任选取代的低级烷基的基团; R2是氢， 并且R3a和R3b各自独立地为诸如氢的基团，条件是排除以下化合物。

公开(公告)号：US20110190279A1

公开(公告)日：2011-08-04

申请号：US12997802

申请日：2009-06-11

申请人： Akihiro Hori ,  Shuji Yonezawa ,  Chiaki Fujikoshi ,  Sae Matsumoto ,  Yuuji Kooriyama ,  Tatsuhiko Ueno ,  Terukazu Kato

发明人： Akihiro Hori ,  Shuji Yonezawa ,  Chiaki Fujikoshi ,  Sae Matsumoto ,  Yuuji Kooriyama ,  Tatsuhiko Ueno ,  Terukazu Kato

IPC分类号： A61K31/541 ,  C07D403/12 ,  A61K31/497 ,  C07D401/12 ,  A61K31/4439 ,  C07D417/12 ,  C07D417/14 ,  A61P25/28

CPC分类号： C07D417/12 ,  A61K9/0019 ,  A61K9/1623 ,  A61K9/2018 ,  C07D279/06 ,  C07D417/10 ,  C07D417/14 ,  C07D487/04

摘要： The following compound is provided as an agent for treating a disease induced by production, secretion and/or deposition of amyloid β protein, for example, a compound represented by the formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group, R1 is optionally substituted lower alkyl or the like, R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or the like, R3a and R3c are each independently hydrogen, halogen, hydroxy, optionally substituted lower alkyl or the like, or a pharmaceutically acceptable salt thereof, or a solvate thereof.

摘要翻译： 提供以下化合物作为治疗由淀粉样蛋白的生产，分泌和/或沉积引起的疾病的药剂; 蛋白质，例如由式（I）表示的化合物：其中环A是任选取代的碳环基或任选取代的杂环基，R 1是任选取代的低级烷基等，R 2a和R 2b各自独立地为氢，任选地 取代的低级烷基等，R3a和R3c各自独立地为氢，卤素，羟基，任选取代的低级烷基等，或其药学上可接受的盐或其溶剂合物。

公开(公告)号：US08703785B2

公开(公告)日：2014-04-22

申请号：US13123761

申请日：2009-10-22

申请人： Shuji Yonezawa ,  Yuuji Kooriyama ,  Gaku Sakaguchi

发明人： Shuji Yonezawa ,  Yuuji Kooriyama ,  Gaku Sakaguchi

IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D239/02

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04

摘要： The present invention provides a compound which has an effect of inhibiting amyloid-β production and is useful as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-β proteins. The present invention relates to a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein A is optionally substituted carbocyclic diyl or optionally substituted heterocyclic diyl; B is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is a group such as optionally substituted lower alkyl; R2 is a group such as hydrogen; and R3a and R3b are each independently a group such as hydrogen, provided that the following compound is excluded.

摘要翻译： 本发明提供了具有抑制淀粉样蛋白的作用的化合物。 并且可用作由淀粉样蛋白的生产，分泌和/或沉积诱导的疾病的治疗剂。 蛋白质。 本发明涉及由式（I）表示的化合物或其药学上可接受的盐或溶剂合物：其中A是任选取代的碳环二基或任选取代的杂环二基; B是任选取代的碳环基团或任选取代的杂环基团; R1是任选取代的低级烷基的基团; R2是氢， 并且R3a和R3b各自独立地为诸如氢的基团，条件是排除以下化合物。