公开(公告)号：JP2008127393A

公开(公告)日：2008-06-05

申请号：JP2007301163

申请日：2007-11-21

Applicant: Kowa Co ,  興和株式会社

Inventor： OGIYA TADAAKI ,  MIURA TORU ,  OKUDA AYUMI ,  ARAI TOSHIHARU ,  YAMAZAKI KOICHI ,  AOKI TARO ,  MIYOSAWA KATSUTOSHI ,  SHIBATA HARUKI ,  SHIBUYA MASAYUKI

IPC: C07D239/47 ,  A61K31/505 ,  A61K31/506 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  C07D401/12

Abstract: PROBLEM TO BE SOLVED: To provide a compound that shows strong inhibitory action against cholesterol ester transferring protein (CETP), has good oral absorptivity and gives high concentration in blood. SOLUTION: The compound is represented by general formula (I) (wherein X 1 is carbonyl or sulfonyl, X 2 is N atom or C-R 12 , and R 1 , R 2 , R 3 , R 4 and R 5 are each an H atom, a halogen atom, a lower alkyl or the like, R 6 , R 7 , R 8 , and R 12 are each an H atom, a halogen atom, a lower alkyl, or the like, R 9 and R 10 are each an H atom, a lower alkyl, a lower cycloalkyl lower alkyl or the like, and R 11 is an H atom, a halogen atom, a lower alkoxy or the like). COPYRIGHT: (C)2008,JPO&INPIT

Abstract translation: 待解决的问题：为了提供对胆固醇酯转移蛋白（CETP）具有强抑制作用的化合物，具有良好的口服吸收性并且在血液中具有高浓度。 解决方案：该化合物由通式（I）表示（其中X 1是羰基或磺酰基，X 2 是N原子或CR 12 < / SP>和R 1 ，R 2 ，R 3 ，R 4 和R 5 R 2是H原子，卤素原子，低级烷基等，R 6，R 7， R 12和R 14各自为H原子，卤素原子，低级烷基等，各自独立地为 H原子，低级烷基，低级环烷基低级烷基等，R 11是H原子，卤素原子，低级烷氧基等）。 版权所有（C）2008，JPO＆INPIT

公开(公告)号：JP2013136572A

公开(公告)日：2013-07-11

申请号：JP2012263933

申请日：2012-12-03

Applicant: Kowa Co ,  興和株式会社

Inventor： OGIYA TADAAKI ,  MURAKAMI TAKESHI ,  MIYOSAWA KATSUTOSHI ,  SHIBUYA MASAYUKI ,  YAMAZAKI KOICHI ,  KUSAKABE TAICHI

IPC: C07D239/14 ,  A61K31/505 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  C12N15/09 ,  C12Q1/68

Abstract: PROBLEM TO BE SOLVED: To provide a low-molecular compound which has such an action as to decrease the amount of PCSK9 protein and increase the amount of LDL receptor, and to provide a medicine including the low-molecular compound as an active ingredient.SOLUTION: The medicine includes (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetate which is substantially optically-pure or a salt thereof, or solvates of them as an active ingredient.

Abstract translation: 要解决的问题：提供具有降低PCSK9蛋白质量和增加LDL受体量的作用的低分子化合物，并提供包含低分子化合物作为活性成分的药物。 ：该药物包括（S） - 反 - {4 - [（{2 - [（{1- [3,5-双（三氟甲基）苯基]乙基} {5- [2-（甲基磺酰基）乙氧基] - 基}氨基）甲基] -4-（三氟甲基）苯基}（乙基）氨基）甲基]环己基}乙酸乙酯，其基本上为光学纯的或其盐，或它们的溶剂合物作为活性成分。

公开(公告)号：JP2013129678A

公开(公告)日：2013-07-04

申请号：JP2013077362

申请日：2013-04-03

Applicant: Kowa Co ,  興和株式会社

Inventor： OGIYA TADAAKI ,  MIURA TORU ,  OKUDA AYUMI ,  ARAI TOSHIHARU ,  YAMAZAKI KOICHI ,  AOKI TARO ,  MIYOSAWA KATSUTOSHI ,  SHIBATA HARUKI ,  SHIBUYA MASAYUKI

IPC: C07D239/47 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  C07D401/12 ,  C07D413/12

CPC classification number: C07D239/42 ,  C07D239/47 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

Abstract: PROBLEM TO BE SOLVED: To provide a compound that is useful for producing a medicament for prophylactic or therapeutic treatment of diseases such as dyslipidemia.SOLUTION: There is provided the use of formula (I) for the production of a medicament for prophylactic or therapeutic treatment of dyslipidemia, arteriosclerosis, atherosclerosis, peripheral vascular disease, hyper-LDL-emia, hypo-HDL-emia, hypercholesterolemia, hypertriglyceridemia, familial hypercholesterolemia, cardiovascular disturbance, angina pectoris, ischemia, cardiac ischemia, thrombosis, myocardial infarction, reperfusion disturbance, angioplasty restenosis, or hypertension.

Abstract translation: 要解决的问题：提供可用于制备用于预防或治疗疾病如血脂异常的药物的化合物。解决方案：提供式（I）用于生产用于预防或治疗性治疗的药物的用途 血脂异常，动脉硬化，动脉粥样硬化，外周血管疾病，高LDL-emia，低HDL-emia，高胆固醇血症，高甘油三酯血症，家族性高胆固醇血症，心血管障碍，心绞痛，局部缺血，心肌缺血，血栓形成，心肌梗塞，再灌注障碍，血管成形术 再狭窄或高血压。

公开(公告)号：JP2010077116A

公开(公告)日：2010-04-08

申请号：JP2009192755

申请日：2009-08-24

Applicant: Kowa Co ,  興和株式会社

Inventor： OGIYA TADAAKI ,  MIURA TORU ,  OKUDA AYUMI ,  ARAI TOSHIHARU ,  YAMAZAKI KOICHI ,  AOKI TARO ,  MIYOSAWA KATSUTOSHI ,  SHIBATA HARUKI ,  SHIBUYA MASAYUKI ,  KUSAKABE TAICHI

IPC: C07D239/47 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61P3/06 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D403/12 ,  C07D413/12

Abstract: PROBLEM TO BE SOLVED: To provide a substance exhibiting strong inhibiting activity against a cholesterol ester transfer protein (CETP). SOLUTION: The compound is expressed by general formula (I) (R 1 , R 2 , R 3 , R 4 and R 5 are each a hydrogen atom, a halo-lower alkyl, a cyano group or the like; R 6 is an alkyl group, cycloalkyl group or the like; R 7 , R 8 , R 9 and R 10 are each hydrogen atom, a halogen atom, a lower alkyl group, a halo-lower alkyl group or the like; R 11 and R 12 are each a hydrogen atom, a lower alkyl group, a lower cycloalkyl-lower alkyl group or the like; and R 13 is a hydrogen atom, a halogen atom or the like). COPYRIGHT: (C)2010,JPO&INPIT

Abstract translation: 待解决的问题：提供对胆固醇酯转移蛋白（CETP）具有强抑制活性的物质。 解决方案：化合物由通式（I）表示（R 1 SP 1，R 2 SP 2，R SP 3，R SP 3， 4 和R 5 各自为氢原子，卤代低级烷基，氰基等; R 6为烷基，环烷基 或者类似物; R 6，R SP 3，R SP 9，和R 10 SP 10各自为氢原子，卤素 原子，低级烷基，卤代低级烷基等; R 11和R 12分别为氢原子，低级烷基，低级环烷基 - 低级烷基等; R 13是氢原子，卤素原子等）。 版权所有（C）2010，JPO＆INPIT

公开(公告)号：BRPI0810880A2

公开(公告)日：2016-07-19

申请号：BRPI0810880

申请日：2008-04-10

Applicant: KOWA CO

Inventor： OKUDA AYUMU ,  SHIBATA HARUKI ,  MIYOSAWA KATSUTOSHI ,  SHIBUYA KIMIYUKI ,  YAMAZAKI KOICHI ,  MIURA TORU ,  OHGIYA TADAAKI ,  AOKI TARO ,  ARAI TOSHIHARU

IPC: A61K31/505 ,  A61P3/06 ,  A61P7/02 ,  A61P9/00 ,  A61P43/00 ,  C07D239/42 ,  C07D403/12

公开(公告)号：CA2683534A1

公开(公告)日：2008-10-30

申请号：CA2683534

申请日：2008-04-10

Applicant: KOWA CO

Inventor： OHGIYA TADAAKI ,  MIURA TORU ,  AOKI TARO ,  MIYOSAWA KATSUTOSHI ,  YAMAZAKI KOICHI ,  OKUDA AYUMU ,  ARAI TOSHIHARU ,  SHIBUYA KIMIYUKI ,  SHIBATA HARUKI

IPC: C07D239/42 ,  A61K31/505 ,  A61P3/06 ,  A61P7/02 ,  A61P9/00 ,  A61P43/00 ,  C07D403/12

Abstract: This invention provides a compound represented by general formula (I) hav ing a high level of inhibitory activity against a cholesterol ester transfer protein (CETP) wherein R1, R2, R3, R4, and R5 represent a hydrogen atom, a halo-lower alkyl group, a cyano group or the like; R6 represents an alkyl gr oup, a cycloalkyl group or the like; R7, R8, R9, and R10 represent a hydroge n atom, a halogen atom, a lower alkyl group, a halo-lower alkyl group or the like; R11 and R12 represent a hydrogen atom, a lower alkyl group, a lower c ycloalkyl lower alkyl group or the like; and R13 represents a hydrogen atom, a halogen atom, a lower alkoxy group or the like.

公开(公告)号：AU2008241904A1

公开(公告)日：2008-10-30

申请号：AU2008241904

申请日：2008-04-10

Applicant: KOWA CO

Inventor： MIURA TORU ,  AOKI TARO ,  SHIBATA HARUKI ,  ARAI TOSHIHARU ,  OKUDA AYUMU ,  YAMAZAKI KOICHI ,  SHIBUYA KIMIYUKI ,  OHGIYA TADAAKI ,  MIYOSAWA KATSUTOSHI

IPC: C07D239/42 ,  A61K31/505 ,  A61P3/06 ,  A61P7/02 ,  A61P9/00 ,  A61P43/00 ,  C07D403/12

Abstract: A compound represented by the following general formula (I), wherein R 1 , R 2 , R 3 , R 4 and R 5 represent hydrogen atom, a halo(lower alkyl) group, cyano group and the like, R 6 represents an alkyl group, a cycloalkyl group and the like, R 7 , R 8 , R 9 and R 10 represent hydrogen atom, a halogen atom, a lower alkyl group, a halo(lower alkyl) group and the like, R 11 and R 12 represent hydrogen atom, a lower alkyl group, a (lower cycloalkyl)(lower alkyl) group and the like, and R 13 represents hydrogen atom, a halogen atom, a lower alkoxy group and the like, which has potent inhibitory activity on cholesterol ester transfer protein (CETP).

公开(公告)号：CY1116179T1

公开(公告)日：2017-02-08

申请号：CY151100285

申请日：2015-03-23

Applicant: KOWA CO

Inventor： OHGIYA TADAAKI ,  MIURA TORU ,  OKUDA AYUMU ,  ARAI TOSHIHARU ,  YAMAZAKI KOICHI ,  AOKI TARO ,  MIYOSAWA KATSUTOSHI ,  SHIBATA HARUKI ,  SHIBUYA KIMIYUKI

IPC: C07D239/42 ,  A61K31/505 ,  A61P3/06 ,  A61P7/02 ,  A61P9/00 ,  A61P43/00 ,  C07D403/12

Abstract: Μιαένωσηη οποίαπαριστάνεταιαπότονακόλουθογενικότύπο (I), όπουτα R1, R2, R3, R4 και R5 παριστάνουνάτομουδρογόνου, ομάδααλογονο (κατώτερουαλκυλίου), ομάδακυανόκαιπαρόμοιες, το R6 παριστάνειομάδααλκυλίου, ομάδακυκλοαλκυλίουκαιπαρόμοιες, τα R7, R8, R9 και R10 παριστάνουνάτομουδρογόνου, άτομοαλογόνου, ομάδακατώτερουαλκυλίου, ομάδααλογονο(κατώτερουαλκυλίου) καιπαρόμοιες, τα R11 και R12 παριστάνουνάτομουδρογόνου, ομάδακατώτερουαλκυλίου, ομάδα (κατώτερουκυκλοαλκυλ) (κατώτερουαλκυλίου) καιπαρόμοιες, καιτο R13 παριστάνειάτομουδρογόνου, άτομοαλογόνου, ομάδακατώτερουαλκοξυκαιπαρόμοιες, ηοποίαέχειισχυρήανασταλτικήδράσηεπίτηςπρωτεΐνηςμεταφοράςτουεστέραχοληστερόλης (CETP).

公开(公告)号：MX338024B

公开(公告)日：2016-03-31

申请号：MX2012014149

申请日：2011-06-03

Applicant: KOWA CO

Inventor： OHGIYA TADAAKI ,  YAMAZAKI KOICHI ,  MIYOSAWA KATSUTOSHI ,  MURAKAMI TAKESHI ,  SHIBUYA KIMIYUKI ,  KUSAKABE TAICHI

IPC: C07D239/47 ,  A61K31/505 ,  A61P3/06 ,  A61P9/10 ,  A61P13/08 ,  A61P13/12 ,  A61P17/06 ,  A61P19/10 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  A61P43/00

Abstract: El ácido (S)-trans-{4-[({2-[({1-[3,5-bis (trifluorometil) fenil] etil}{5-[2-(metilsulfonil)etoxi]pirimidin-2-il}amino)metil]-4-(tr ifluorometil)fenil} (etil)amino)metil]ciclohexil}acético sustancialmente ópticamente puro, o una sal de él o un solvato de él, que tiene acciones de reducción de la cantidad de proteína PCSK9 y aumento de la cantidad del receptor de LDL.

公开(公告)号：DK2149563T3

公开(公告)日：2015-02-02

申请号：DK08740159

申请日：2008-04-10

Applicant: KOWA CO

Inventor： OHGIYA TADAAKI ,  OKUDA AYUMU ,  ARAI TOSHIHARU ,  MIYOSAWA KATSUTOSHI ,  SHIBATA HARUKI ,  SHIBUYA KIMIYUKI ,  MIURA TORU ,  YAMAZAKI KOICHI ,  AOKI TARO

IPC: C07D239/42 ,  A61K31/505 ,  A61P3/06 ,  A61P7/02 ,  A61P9/00 ,  A61P43/00 ,  C07D403/12