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。

公开(公告)号：US20120059162A1

公开(公告)日：2012-03-08

申请号：US13192369

申请日：2011-07-27

申请人： Ken-ichi Kusakabe ,  Hiroshi Yoshida ,  Kohei Nozu ,  Hiroshi Hashizume ,  Genta Tadano ,  Jun Sato ,  Yuusuke Tamura ,  Yasunori Mitsuoka

发明人： Ken-ichi Kusakabe ,  Hiroshi Yoshida ,  Kohei Nozu ,  Hiroshi Hashizume ,  Genta Tadano ,  Jun Sato ,  Yuusuke Tamura ,  Yasunori Mitsuoka

IPC分类号： C07D487/04 ,  C07D498/04

CPC分类号： C07D487/04 ,  C07D498/04

摘要： Provided are a compound represented by general formula (1) and having a TTK inhibitory action and a medicine containing the compound. In formula (1), (X, Y, V, W) is (—N═, ═CR1—, ═N—, —CR7═), (—CR2═, ═N—, ═N—, —CR7═), etc.; A is an (un)substituted aromatic hydrocarbon ring, etc.; L is a single bond, —C(═O)—NRA—, etc.; Z is a group represented by the formula —NR3R4 or a group represented by the formula —OR5; R1 to R3, R6, and R7 each is a hydrogen atom, etc.; R4 and R5 each is an (un)substituted alkyl, etc.; and R8 is an (un)substituted cycloalkyl, etc.

摘要翻译： 提供由通式（1）表示的具有TTK抑制作用的化合物和含有该化合物的药物。 在式（1）中，（X，Y，V，W）是（-N =，= CR1-，...， - CR7 =），（-CR2 =，= N-，= N-，-CR7 = ）等 A是（未）取代的芳族烃环等; L是单键，-C（= O）-NRA-等; Z是由式-NR 3 R 4表示的基团或由式-OR 5表示的基团; R1至R3，R6和R7各自为氢原子等; R4和R5各自为（未）取代的烷基等; R8是（未）取代的环烷基等

公开(公告)号：US20140235626A1

公开(公告)日：2014-08-21

申请号：US14112400

申请日：2012-04-25

申请人： Yukio Tada ,  Ken-ichi Kusakabe ,  Genta Taadano

发明人： Yukio Tada ,  Ken-ichi Kusakabe ,  Genta Taadano

IPC分类号： C07D417/04 ,  C07D491/048 ,  C07D491/056 ,  C07D417/14

CPC分类号： C07D417/04 ,  A61K9/1623 ,  A61K9/2018 ,  A61K9/4858 ,  C07D417/14 ,  C07D491/048 ,  C07D491/056

摘要： The present invention provides a compound of formula (I): wherein ring B is substituted or unsubstituted carbocycle or heterocycle, R1 is substituted or unsubstituted alkyl or the like, R2a and R2b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R3, R4a and R4b are each independently hydrogen, halogen, substituted or unsubstituted alkyl or the like, a dashed line represents a presence or absence of a bond, R5 is hydrogen, substituted or unsubstituted alkyl or the like, R6 is 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：其中环B是取代或未取代的碳环或杂环，R 1是取代或未取代的烷基等，R 2a和R 2b各自独立地为氢，取代或未取代的烷基等，R 3 ，R4a和R4b各自独立地为氢，卤素，取代或未取代的烷基等，虚线表示键的存在或不存在，R 5为氢，取代或未取代的烷基等，R 6为卤素，羟基，取代的 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，其具有抑制淀粉样蛋白和bgr的作用; 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。