公开(公告)号：EP2789347A1

公开(公告)日：2014-10-15

申请号：EP12854422.8

申请日：2012-11-28

申请人： Kowa Company, Ltd.

发明人： MURAKAMI, Takeshi ,  MURAKAMI, Kentaro ,  OHGIYA, Tadaaki ,  SHIBUYA, Kimiyuki

IPC分类号： A61K45/00 ,  A61K31/421 ,  A61K31/505 ,  A61P3/04 ,  A61P43/00 ,  C07D239/47 ,  C07D263/24 ,  C12N15/09

CPC分类号： A61K31/505 ,  A61K31/421 ,  C07D239/47 ,  C07D263/24

摘要： Provided is an agent for treating and/or preventing obesity. An agent for suppressing expression of NPC1L1 (Niemann-Pick disease, type C1, gene-like 1) and/or LIPG (Lipase, endothelial) mRNA, and an agent for preventing and/or treating obesity, each comprising, as an active ingredient, a compound having CETP inhibitory activity, or a salt thereof, or a solvate thereof.

摘要翻译： 提供了用于治疗和/或预防肥胖的药剂。 用于抑制NPC1L1（尼曼 - 皮克病，C1型，基因样1）和/或LIPG（脂肪酶，内皮）mRNA的表达的药剂，和用于预防和/或治疗肥胖症，每一个都包括作为活性成分的试剂 具有CETP抑制活性，或它们的盐，或其溶剂化物的化合物。

公开(公告)号：EP2383253A1

公开(公告)日：2011-11-02

申请号：EP09828871.5

申请日：2009-11-27

申请人： Kowa Company, Ltd.

发明人： KUSAKABE, Taichi ,  YAMAZAKI, Koichi ,  OHGIYA, Tadaaki ,  SHIBUYA, Kimiyuki

IPC分类号： C07C227/18 ,  C07C227/30 ,  C07C229/28 ,  C07C231/12 ,  C07C233/48 ,  C07B61/00

CPC分类号： C07C227/16 ,  C07C231/02 ,  C07C231/12 ,  C07C233/48 ,  C07C2601/14 ,  C07C229/28 ,  C07C233/31

摘要： A method for preparing a trans-{4-[(alkylamino)methyl]cyclohexyl}acetic acid, which is useful as a raw material compound for manufacture of medicaments and the like, comprising the step of reducing amide group of a compound represented by the following general formula (6) (R 1 represents hydrogen atom or a C 1-6 alkyl group, and R 2 represents a C 1-6 alkyl group, a C 3-6 cycloalkyl group, a (C 3-6 cycloalkyl)(C 1-6 alkyl) group, a C 6-10 aryl group, or a C 7-12 aralkyl group).

公开(公告)号：EP2098515B1

公开(公告)日：2012-02-08

申请号：EP07828095.5

申请日：2007-11-29

申请人： Kowa Company, Ltd.

发明人： MATSUDA, Takayuki ,  OKUDA, Ayumu ,  KOURA, Minoru ,  YAMAGUCHI, Yuki ,  KUROBUCHI, Sayaka ,  WATANABE, Yuichiro ,  SHIBUYA, Kimiyuki

IPC分类号： C07D233/72 ,  A61K31/4166 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/498 ,  A61P1/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00

CPC分类号： C07D233/72 ,  C07D233/76 ,  C07D233/78 ,  C07D235/02 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04

摘要： Disclosed is a novel LXRβ agonist which is useful as a prophylactic and/or therapeutic agent for arteriosclerosis including atherosclerosis and arteriosclerosis induced by diabetes, hyperlipemia, hypercholesterolemia, a fat-related disease, an inflammatory disease which is a disease induced by an inflammatory cytokine, a skin disease such as allergic skin disease, diabetes or Alzheimer's disease. Specifically disclosed is a carbinol derivative represented by the general formula (1), a salt thereof, or a solvate of the derivative or the salt.

公开(公告)号：EP1908747B1

公开(公告)日：2012-01-04

申请号：EP06781793.2

申请日：2006-07-27

申请人： Kowa Company, Ltd.

发明人： KOURA, Minoru ,  YAMAZAKI, Yukiyoshi ,  SHIBUYA, Kimiyuki

IPC分类号： C07C67/343 ,  C07C69/675 ,  C07B53/00 ,  C07B61/00

CPC分类号： C07B53/00 ,  C07B2200/07 ,  C07C67/343 ,  C07C69/675

摘要： A process by which an optically active 2-hydroxybutyric ester having a high optical purity is obtained in a high yield. The process, which is for producing an optically active 2-hydroxybutyric ester (1), is characterized by reacting an optically active 2,3-epoxypropionic ester (2) with a methyl Grignard reagent represented by CH3MgX (wherein X represents halogeno) in the presence of a copper catalyst used in an amount of 0.05-0.5 mol per mol of the ester (2). [In the formulae, R represents C1-6 alkyl or C7-8 aralkyl; X represents halogeno; and * indicates absolute S- or R-configuration.]

公开(公告)号：EP2281817A1

公开(公告)日：2011-02-09

申请号：EP09754469.6

申请日：2009-05-29

申请人： Kowa Company, Ltd.

发明人： YAMAGUCHI, Yuki ,  KOURA, Minoru ,  KUROBUCHI, Sayaka ,  MATSUDA, Takayuki ,  OKUDA, Ayumu ,  SUMIDA, Hisashi ,  WATANABE, Yuichiro ,  ENOMOTO, Takashi ,  SHIBUYA, Kimiyuki

IPC分类号： C07D233/72 ,  A61K31/4166 ,  A61K31/4178 ,  A61K31/4355 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P17/00 ,  A61P25/28 ,  A61P29/00 ,  A61P43/00 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04

CPC分类号： C07D233/72 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D491/048

摘要： It is to provide a novel LXRβ agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease.
It is a carbinol compound represented by the following general formula (I) or salt thereof, or their solvate.

摘要翻译： 提供可用作动脉粥样硬化的预防和/或治疗剂的新型LXR 2激动剂; 动脉硬化，如糖尿病; 血脂异常; 高胆固醇血症; 脂质相关疾病; 由炎性细胞因子引起的炎性疾病; 皮肤病如过敏性皮肤病; 糖尿病; 或阿尔茨海默病。 它是由以下通式（I）表示的甲醇化合物或其盐或其溶剂合物。

公开(公告)号：EP2248811A1

公开(公告)日：2010-11-10

申请号：EP09715052.8

申请日：2009-02-27

申请人： Kowa Company, Ltd.

发明人： OKUDA, Ayumu ,  MATSUDA, Takayuki ,  MIURA, Toru ,  OZAWA, Hidefumi ,  TOSAKA, Ayako ,  YAMAZAKI, Koichi ,  YAMAGUCHI, Yuki ,  KUROBUCHI, Sayaka ,  WATANABE, Yuuichirou ,  SHIBUYA, Kimiyuki

IPC分类号： C07D405/12 ,  A61K31/4178 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P25/28 ,  A61P29/00 ,  A61P37/00 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

CPC分类号： C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

摘要： [Object]
It is to provide a novel LXRβ agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes;dyslipidemia; hypercholesterolemia; lipid-reflated diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. A 2-oxochromene derivative represented by the following general formula (1) or salt thereof, or their solvate.

摘要翻译： [目的]提供一种可用作动脉粥样硬化的预防和/或治疗剂的新型LXR 2激动剂; 动脉硬化，如糖尿病;血脂异常; 高胆固醇血症; 脂质反流疾病; 由炎性细胞因子引起的炎性疾病; 皮肤病如过敏性皮肤病; 糖尿病; 或阿尔茨海默病。 由下列通式（1）表示的2-氧代色烯衍生物或其盐或其溶剂合物。

公开(公告)号：EP2138489A1

公开(公告)日：2009-12-30

申请号：EP08721875.6

申请日：2008-03-12

申请人： Kowa Company. Ltd.

发明人： OHGIYA, Tadaaki ,  MIURA, Toru ,  OKUDA, Ayumu ,  ARAI, Toshiharu ,  YAMAZAKI, Koichi ,  AOKI, Taro ,  MIYOSAWA, Katsutoshi ,  SHIBATA, Haruki ,  SHIBUYA, Kimiyuki

IPC分类号： C07D401/12 ,  A61K31/506 ,  A61P3/06 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D403/12 ,  C07D471/04

CPC分类号： C07D401/12 ,  C07D403/12 ,  C07D471/04

摘要： 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 halogen atom, a lower alkyl group and the like, R 6 represents an alkyl group, a cycloalkyl group and the like, R 7 and R 8 represent hydrogen atom, a lower alkyl group, a (lower cycloalkyl)(lower alkyl) group and the like, R 9 represents hydrogen atom, a halogen atom, a lower alkoxy group and the like, R 10 and R 11 represent hydrogen atom, a lower alkyl group, a lower alkoxy group, a halo(lower alkyl) group and the like, and A represents a heterocyclic ring constituted by 6 to 10 atoms, which has potent inhibitory activity on cholesterol ester transfer protein (CETP).

摘要翻译： 由以下通式（I）表示的化合物，其中R 1，R 2，R 3，R 4和R 5表示氢原子，卤素原子，低级烷基等，R 6表示烷基， 环烷基等，R 7和R 8表示氢原子，低级烷基，（低级环烷基）（低级烷基）等，R 9表示氢原子，卤素原子，低级烷氧基和 R 10和R 11表示氢原子，低级烷基，低级烷氧基，卤代（低级烷基）等，A表示由6〜10个原子构成的杂环，其具有强的抑制性 胆固醇酯转运蛋白（CETP）活性。

公开(公告)号：EP1908747A1

公开(公告)日：2008-04-09

申请号：EP06781793.2

申请日：2006-07-27

申请人： Kowa Company, Ltd.

发明人： KOURA, Minoru ,  YAMAZAKI, Yukiyoshi ,  SHIBUYA, Kimiyuki

IPC分类号： C07C67/343 ,  C07C69/675 ,  C07B53/00 ,  C07B61/00

CPC分类号： C07B53/00 ,  C07B2200/07 ,  C07C67/343 ,  C07C69/675

摘要： To provide a process for producing an optically active 2-hydroxybutyric ester at high yield and high optical purity.
The process for producing an optically active 2-hydroxybutyric ester (1), characterized in that the process includes reacting an optically active 2,3-epoxypropionic ester (2) with a methyl Grignard reagent CH 3 MgX (wherein X represents a halogen atom) in the presence of a copper catalyst in an amount of 0.05 to 0.5 mol with respect to 1 mol of (2) through the following scheme:

(wherein R represents a C1 to C6 alkyl group or a C7 or C8 aralkyl group; X represents a halogen atom; and * represents S- or R-absolute configuration).

摘要翻译： 提供以高产率和高光学纯度制备光学活性2-羟基丁酸酯的方法。 制备光学活性2-羟基丁酸酯（1）的方法，其特征在于该方法包括使光学活性2,3-环氧丙酸酯（2）与格氏试剂CH 3 MgX（其中X表示卤素原子） 在相对于1摩尔（2）的0.05摩尔的铜催化剂的存在下，通过以下方案：（其中R表示C1至C6烷基或C7或C8芳烷基; X表示 卤原子;和*表示S-或R-绝对构型）。

公开(公告)号：EP2573081B1

公开(公告)日：2017-07-12

申请号：EP11783277.4

申请日：2011-05-18

申请人： Kowa Company Ltd.

发明人： SHIBATA, Haruki ,  YOSHINAKA, Yasunobu ,  SHIBUYA, Kimiyuki

IPC分类号： A61K31/496 ,  A61P1/16 ,  A61P43/00

CPC分类号： C07D401/12 ,  A61K31/496

公开(公告)号：EP2383253B1

公开(公告)日：2014-03-19

申请号：EP09828871.5

申请日：2009-11-27

申请人： Kowa Company, Ltd.

发明人： KUSAKABE, Taichi ,  YAMAZAKI, Koichi ,  OHGIYA, Tadaaki ,  SHIBUYA, Kimiyuki

IPC分类号： C07C227/16 ,  C07C229/28 ,  C07C231/12 ,  C07C233/48 ,  C07B61/00 ,  C07C231/02

CPC分类号： C07C227/16 ,  C07C231/02 ,  C07C231/12 ,  C07C233/48 ,  C07C2601/14 ,  C07C229/28 ,  C07C233/31