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：US20140051691A1

公开(公告)日：2014-02-20

申请号：US14113327

申请日：2012-04-25

申请人： Moriyasu Masui ,  Yasunori Mitsuoka ,  Syuhei Yoshida ,  Ken-ichi Kusakabe ,  Naohiro Onodera ,  Noriyuki Kurose

发明人： Moriyasu Masui ,  Yasunori Mitsuoka ,  Syuhei Yoshida ,  Ken-ichi Kusakabe ,  Naohiro Onodera ,  Noriyuki Kurose

IPC分类号： C07D413/14 ,  C07D413/12

CPC分类号： C07D413/14 ,  C07D413/12

摘要： The present invention provides a compound of formula (I): wherein —X═ is —CR7═ or —N═, ring B is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, R1 is substituted or unsubstituted alkyl or the like, R2 a and R2 b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R3 and R4 are each independently hydrogen, halogen, substituted or unsubstituted alkyl or the like, R5 is hydrogen, substituted or unsubstituted alkyl or the like, each R6 is independently halogen, hydroxy, substituted or unsubstituted alkyl or the like, R7 is hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like, p is an integer of 0 to 3, or a pharmaceutically acceptable salt thereof which has an effect of inhibiting amyloid β production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid β proteins.

摘要翻译： 本发明提供式（I）化合物：其中-X =是-CR 7 =或-N =，环B是取代或未取代的碳环或取代或未取代的杂环，R 1是取代或未取代的烷基等， R2a和R2b各自独立地为氢，取代或未取代的烷基等，R3和R4各自独立地为氢，卤素，取代或未取代的烷基等，R5为氢，取代或未取代的烷基等，各R6 独立地为卤素，羟基，取代或未取代的烷基等，R 7为氢，卤素，羟基，取代或未取代的烷基等，p为0〜3的整数，或其药学上可接受的盐， 抑制淀粉样蛋白β生成，特别是抑制BACE1的作用，并且其可用作由淀粉样蛋白β蛋白的产生，分泌和/或沉积诱导的疾病的治疗或预防剂。

公开(公告)号：US08883779B2

公开(公告)日：2014-11-11

申请号：US14113327

申请日：2012-04-25

申请人： Moriyasu Masui ,  Yasunori Mitsuoka ,  Syuhei Yoshida ,  Ken-ichi Kusakabe ,  Naohiro Onodera ,  Noriyuki Kurose

发明人： Moriyasu Masui ,  Yasunori Mitsuoka ,  Syuhei Yoshida ,  Ken-ichi Kusakabe ,  Naohiro Onodera ,  Noriyuki Kurose

IPC分类号： C07D265/04 ,  A61K31/5355 ,  C07D413/12 ,  C07D413/14

CPC分类号： C07D413/14 ,  C07D413/12

摘要： The present invention provides a compound of formula (I): wherein —X═ is —CR7═ or —N═, ring B is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, R1 is substituted or unsubstituted alkyl or the like, R2 a and R2 b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R3 and R4 are each independently hydrogen, halogen, substituted or unsubstituted alkyl or the like, R5 is hydrogen, substituted or unsubstituted alkyl or the like, each R6 is independently halogen, hydroxy, substituted or unsubstituted alkyl or the like, R7 is hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like, p is an integer of 0 to 3, or a pharmaceutically acceptable salt thereof which has an effect of inhibiting amyloid β production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid β proteins.

摘要翻译： 本发明提供式（I）化合物：其中-X =是-CR 7 =或-N =，环B是取代或未取代的碳环或取代或未取代的杂环，R 1是取代或未取代的烷基等， R2a和R2b各自独立地为氢，取代或未取代的烷基等，R3和R4各自独立地为氢，卤素，取代或未取代的烷基等，R5为氢，取代或未取代的烷基等，各R6 独立地为卤素，羟基，取代或未取代的烷基等，R 7为氢，卤素，羟基，取代或未取代的烷基等，p为0〜3的整数，或其药学上可接受的盐， 抑制淀粉样蛋白 特别是抑制BACE1的作用，其可用作由淀粉样蛋白的生产，分泌和/或沉积引起的疾病的治疗或预防剂。 蛋白质。