公开(公告)号：US20090247587A1

公开(公告)日：2009-10-01

申请号：US12413894

申请日：2009-03-30

申请人： Ayumu OKUDA ,  Takayuki MATSUDA ,  Toru MIURA ,  Koichi YAMAZAKI ,  Yuki YAMAGUCHI ,  Minoru KOURA ,  Sayaka KUROBUCHI ,  Yuuichiro WATANABE ,  Kimiyuki SHIBUYA

发明人： Ayumu OKUDA ,  Takayuki MATSUDA ,  Toru MIURA ,  Koichi YAMAZAKI ,  Yuki YAMAGUCHI ,  Minoru KOURA ,  Sayaka KUROBUCHI ,  Yuuichiro WATANABE ,  Kimiyuki SHIBUYA

IPC分类号： A61K31/4178 ,  C07D405/12 ,  C07D405/14 ,  C07D417/14 ,  A61K31/4439 ,  A61K31/427 ,  A61P3/00 ,  A61P17/00 ,  A61P29/00 ,  A61P25/28

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

摘要： The object 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. The solving means is a 1,3-dihydroisobenzofuran derivative represented by the following general formula (1) or salt thereof, or their solvate.

摘要翻译： 目的是提供可用作动脉粥样硬化的预防和/或治疗剂的新型LXRβ激动剂; 动脉硬化，如糖尿病引起的; 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。 解决方法是由以下通式（1）表示的1,3-二氢异苯并呋喃衍生物或其盐或其溶剂合物。

公开(公告)号：US20090286780A1

公开(公告)日：2009-11-19

申请号：US12394548

申请日：2009-02-27

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

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

IPC分类号： A61K31/4178 ,  C07D407/12 ,  C07D413/14 ,  A61K31/5377 ,  A61P3/00 ,  A61P25/00 ,  A61P17/00

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

摘要： 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.[Solving Means] A 2-oxochromene derivative represented by the following general formula (1) 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LXRβ激动剂; 动脉硬化，如糖尿病引起的; 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。 [解决方案]由以下通式（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：US20100249148A1

公开(公告)日：2010-09-30

申请号：US12815905

申请日：2010-06-15

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

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

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

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

摘要： A compound represented by the following general formula (I), wherein R1, R2, R3, R4 and R5 represent hydrogen atom, a halogen atom, a lower alkyl group and the like, R6 represents an alkyl group, a cycloalkyl group and the like, R7 and R8 represent hydrogen atom, a lower alkyl group, a (lower cycloalkyl)(lower alkyl) group and the like, R9 represents hydrogen atom, a halogen atom, a lower alkoxy group and the like, R10 and R11 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： 由下列通式（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，卤原子，低级烷基等，R 6表示烷基，环烷基等 ，R7和R8表示氢原子，低级烷基，（低级环烷基）（低级烷基）等，R9表示氢原子，卤素原子，低级烷氧基等，R10和R11表示氢原子 ，低级烷基，低级烷氧基，卤代（低级烷基）等，A表示6〜10个原子构成的杂环，对胆固醇酯转移蛋白（CETP）具有有效的抑制活性。

公开(公告)号：US20090082352A1

公开(公告)日：2009-03-26

申请号：US12100831

申请日：2008-04-10

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

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

IPC分类号： A61K31/5377 ,  C07D239/42 ,  A61K31/505

CPC分类号： C07D239/42 ,  C07D239/47 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

摘要： A compound represented by the following general formula (I), wherein R1, R2, R3, R4 and R5 represent hydrogen atom, a halo(lower alkyl) group, cyano group and the like, R6 represents an alkyl group, a cycloalkyl group and the like, R7, R8, R9 and R10 represent hydrogen atom, a halogen atom, a lower alkyl group, a halo(lower alkyl) group and the like, R11 and R12 represent hydrogen atom, a lower alkyl group, a (lower cycloalkyl) (lower alkyl) group and the like, and R13 represents hydrogen atom, a halogen atom, a lower alkoxy group and the like, 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，卤代（低级烷基）基，氰基等，R 6表示烷基，环烷基和 R 7，R 8，R 9和R 10表示氢原子，卤素原子，低级烷基，卤代（低级烷基）等，R 11和R 12表示氢原子，低级烷基，（低级环烷基 ）（低级烷基）等，R 13表示对胆固醇酯转移蛋白（CETP）具有强抑制活性的氢原子，卤素原子，低级烷氧基等。

公开(公告)号：US20090062306A1

公开(公告)日：2009-03-05

申请号：US12045982

申请日：2008-03-11

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

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

IPC分类号： A61K31/506 ,  C07D401/12 ,  C07D403/12

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

摘要： A compound represented by the following general formula (I), wherein R1, R2, R3, R4 and R5 represent hydrogen atom, a halogen atom, a lower alkyl group and the like, R6 represents an alkyl group, a cycloalkyl group and the like, R7 and R8 represent hydrogen atom, a lower alkyl group, a (lower cycloalkyl)(lower alkyl) group and the like, R9 represents hydrogen atom, a halogen atom, a lower alkoxy group and the like, R10 and R11 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： 由下列通式（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，卤原子，低级烷基等，R 6表示烷基，环烷基等 ，R7和R8表示氢原子，低级烷基，（低级环烷基）（低级烷基）等，R9表示氢原子，卤素原子，低级烷氧基等，R10和R11表示氢原子 ，低级烷基，低级烷氧基，卤代（低级烷基）等，A表示6〜10个原子构成的杂环，对胆固醇酯转移蛋白（CETP）具有有效的抑制活性。

公开(公告)号：US20090054474A1

公开(公告)日：2009-02-26

申请号：US11835127

申请日：2007-08-07

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

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

IPC分类号： A61K31/506 ,  C07D401/12 ,  A61P3/04

CPC分类号： C07D401/12

摘要： A compound represented by the following general formula (I) or a salt thereof, or a solvate thereof: (wherein R1, R2, R3, R4 and R5 are the same or different, and represent hydrogen atom, a halogen atom, a lower alkyl group etc., R6, R7 and R8 are the same or different, and represent hydrogen atom, a halogen atom, a lower alkyl group etc., R9 and R10 are the same or different, and represent hydrogen atom, a lower alkyl group, a (lower cycloalkyl)(lower alkyl) group etc., and R11 represents hydrogen atom, a halogen atom, a lower alkoxy group, a (lower alkyl)thio(lower alkoxy) group, a (lower alkyl)sulfinyl(lower alkoxy) group, a (lower alkyl)sulfonyl(lower alkoxy) group etc.), which has potent inhibitory activity on CETP.

摘要翻译： 由下列通式（I）表示的化合物或其盐或其溶剂化物：（其中R1，R2，R3，R4和R5相同或不同，表示氢原子，卤素原子，低级烷基 基团等，R6，R7和R8相同或不同，表示氢原子，卤素原子，低级烷基等，R9和R10相同或不同，表示氢原子，低级烷基， （低级环烷基）（低级烷基）等，R11表示氢原子，卤素原子，低级烷氧基，（低级烷基）硫代（低级烷氧基），（低级烷基）亚磺酰基（低级烷氧基） 基团，（低级烷基）磺酰基（低级烷氧基）等），其对CETP具有有效的抑制活性。