公开(公告)号：US20110105457A1

公开(公告)日：2011-05-05

申请号：US12988129

申请日：2009-04-16

申请人： Daisuke Taniyama ,  Kazuya Kano ,  Kazuya Okamoto ,  Masahiko Fujioka ,  Yasunori Mitsuoka

发明人： Daisuke Taniyama ,  Kazuya Kano ,  Kazuya Okamoto ,  Masahiko Fujioka ,  Yasunori Mitsuoka

IPC分类号： A61K31/5025 ,  C07D487/04 ,  A61K31/5377 ,  A61K31/55 ,  A61P29/00 ,  A61P35/00

CPC分类号： C07D487/04

摘要： The purpose of the present invention is to provide a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prevention/treatment of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. This was achieved by providing a substituted 2-amino-5,6-nitrogenated fused ring compound shown in the present specification, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明的目的是提供抑制PI3K活性以调节包括细胞的生长，分化，存活，增殖，迁移，代谢等的许多生物学过程的化合物或其药学上可接受的盐，因此 可用于预防/治疗包括炎性疾病，动脉硬化，血管/循环系统疾病，癌症/肿瘤，免疫系统疾病，细胞增殖性疾病，感染性疾病等疾病的疾病。 这是通过提供本说明书中所示的取代的2-氨基-5,6-氮化稠环化合物或其药学上可接受的盐来实现的。

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：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：US20110230472A1

公开(公告)日：2011-09-22

申请号：US13061328

申请日：2009-08-25

申请人： Yasunori Mitsuoka ,  Manami Masuda ,  Daisuke Taniyama

发明人： Yasunori Mitsuoka ,  Manami Masuda ,  Daisuke Taniyama

IPC分类号： A61K31/551 ,  A61K31/5377 ,  A61K31/53 ,  A61K31/501 ,  A61K31/4965 ,  A61K31/506 ,  A61K31/437 ,  A61K31/4725 ,  A61P29/00 ,  C07D513/04 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07D513/04 ,  C07D519/00

摘要： It is an object of the present invention to provide a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a ring-fused azole compound shown in the present specification, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明的目的是提供抑制PI3K活性以调节包括细胞的生长，分化，存活，增殖，迁移，代谢等许多生物学过程的活性的化合物或其药学上可接受的盐，并且是 因此可用于预防/治疗包括炎性疾病，动脉硬化，血管/循环系统疾病，癌症/肿瘤，免疫系统疾病，细胞增殖性疾病，感染性疾病等疾病。 通过提供本说明书中所示的环稠唑唑化合物或其药学上可接受的盐来解决上述问题。

公开(公告)号：US20120071475A1

公开(公告)日：2012-03-22

申请号：US13266200

申请日：2010-04-26

申请人： Daisuke Taniyama ,  Yasunori Mitsuoka ,  Kayoko Hata

发明人： Daisuke Taniyama ,  Yasunori Mitsuoka ,  Kayoko Hata

IPC分类号： A61K31/5377 ,  A61K31/506 ,  C07D487/04 ,  A61K31/5025 ,  A61K31/4725 ,  A61K31/444 ,  C07D277/82 ,  A61K31/428 ,  C07D471/04 ,  A61K31/437 ,  C07D231/40 ,  A61K31/415 ,  A61K31/4439 ,  A61P29/00 ,  C07D513/04

CPC分类号： C07D513/04 ,  C07D231/40 ,  C07D277/48 ,  C07D277/82 ,  C07D401/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： Provided is a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a urea derivative shown in the present specification, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明提供抑制PI3K活性调节细胞生长，分化，存活，增殖，迁移，代谢等许多生物学过程的化合物或其药学上可接受的盐，因此可用于预防/治疗 疾病包括炎性疾病，动脉硬化，血管/循环系统疾病，癌症/肿瘤，免疫系统疾病，细胞增殖性疾病，传染病等。 通过提供本说明书中所示的尿素衍生物或其药学上可接受的盐来解决上述问题。

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：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：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。