公开(公告)号：US07919509B2

公开(公告)日：2011-04-05

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 ,  Yuichiro Watanabe ,  Kimiyuki Shibuya

发明人： Ayumu Okuda ,  Takayuki Matsuda ,  Toru Miura ,  Hidefumi Ozawa ,  Ayako Tosaka ,  Koichi Yamazaki ,  Yuki Yamaguchi ,  Sayaka Kurobuchi ,  Yuichiro Watanabe ,  Kimiyuki Shibuya

IPC分类号： A61K31/4166 ,  A61K31/427 ,  A61K31/45 ,  A61K31/422 ,  A61K31/4525 ,  C07D405/12 ,  C07D417/12 ,  C07D413/12 ,  C07D407/12

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： 提供一种新颖的LXR＆bgr 可用作动脉粥样硬化的预防和/或治疗剂的激动剂; 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：US07951822B2

公开(公告)日：2011-05-31

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 ,  Yuichiro Watanabe ,  Kimiyuki Shibuya

发明人： Ayumu Okuda ,  Takayuki Matsuda ,  Toru Miura ,  Koichi Yamazaki ,  Yuki Yamaguchi ,  Minoru Koura ,  Sayaka Kurobuchi ,  Yuichiro Watanabe ,  Kimiyuki Shibuya

IPC分类号： A61K31/4166 ,  A61K31/427 ,  A61K31/422 ,  A61K31/45 ,  A61K31/4525 ,  C07D405/12 ,  C07D417/12 ,  C07D413/12 ,  C07D407/12

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： 目的是提供一种新颖的LXR＆bgr; 可用作动脉粥样硬化的预防和/或治疗剂的激动剂; 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：US08008306B2

公开(公告)日：2011-08-30

申请号：US12430397

申请日：2009-04-27

申请人： Minoru Koura ,  Ayumu Okuda ,  Takayuki Matsuda ,  Yuki Yamaguchi ,  Hisashi Sumida ,  Sayaka Kurobuchi ,  Yuichiro Watanabe ,  Takashi Enomoto ,  Kimiyuki Shibuya

发明人： Minoru Koura ,  Ayumu Okuda ,  Takayuki Matsuda ,  Yuki Yamaguchi ,  Hisashi Sumida ,  Sayaka Kurobuchi ,  Yuichiro Watanabe ,  Takashi Enomoto ,  Kimiyuki Shibuya

IPC分类号： C07D215/12 ,  C07D215/233 ,  C07D241/40 ,  A61K31/4709 ,  A61K31/498

CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D405/14

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.A quinoline compound represented by the following general formula (1) or salt thereof, or their solvate.

摘要翻译： 提供一种新颖的LXR＆bgr 可用作动脉粥样硬化的预防和/或治疗剂的激动剂; 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。 由以下通式（1）表示的喹啉化合物或其盐或其溶剂化物。

公开(公告)号：US08153634B2

公开(公告)日：2012-04-10

申请号：US12474799

申请日：2009-05-29

申请人： Yuki Yamaguchi ,  Minoru Koura ,  Sayaka Kurobuchi ,  Takayuki Matsuda ,  Ayumu Okuda ,  Hisashi Sumida ,  Yuichiro Watanabe ,  Takashi Enomoto ,  Kimiyuki Shibuya

发明人： Yuki Yamaguchi ,  Minoru Koura ,  Sayaka Kurobuchi ,  Takayuki Matsuda ,  Ayumu Okuda ,  Hisashi Sumida ,  Yuichiro Watanabe ,  Takashi Enomoto ,  Kimiyuki Shibuya

IPC分类号： A61K31/4166 ,  A61K31/4178 ,  A61K31/4355 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  C07D401/02 ,  C07D401/06 ,  C07D405/14 ,  C07D405/02 ,  C07D491/048 ,  C07D233/72 ,  C07D403/02 ,  C07D403/06

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

摘要： [Object] 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 carbinol compound represented by the following general formula (I) or salt thereof, or their solvate.

摘要翻译： [目的]提供一种新型的LXR＆bgr; 可用作动脉粥样硬化的预防和/或治疗剂的激动剂; 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（I）表示的甲醇化合物或其盐或其溶剂化物。

公开(公告)号：US20100063119A1

公开(公告)日：2010-03-11

申请号：US12516944

申请日：2007-11-29

申请人： Takayuki Matsuda ,  Ayumu Okuda ,  Minoru Koura ,  Yuki Yamaguchi ,  Sayaka Kurobuchi ,  Yuuichirou Watanabe ,  Kimiyuki Shibuya

发明人： Takayuki Matsuda ,  Ayumu Okuda ,  Minoru Koura ,  Yuki Yamaguchi ,  Sayaka Kurobuchi ,  Yuuichirou Watanabe ,  Kimiyuki Shibuya

IPC分类号： A61K31/4164 ,  C07D233/72 ,  C07D405/10 ,  C07D409/04 ,  A61K31/4178

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

摘要： There is provided a novel LXRβ agonist useful as a preventative and/or therapeutic agent for arteriosclerosis; arteriosclerosis such as those resulting from diabetes; hyperlipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases caused by inflammatory cytokines, skin diseases such as allergic skin diseases, diabetes or Alzheimer's disease. The agonist is a carbinol derivative represented by the following general formula (1) or salt thereof, or their solvate.

摘要翻译： 提供了一个新颖的LXR＆bgr; 可用作动脉硬化的预防和/或治疗剂的激动剂; 动脉硬化，如糖尿病引起的; 高脂血症 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，皮肤疾病如过敏性皮肤疾病，糖尿病或阿尔茨海默病。 激动剂是由以下通式（1）表示的甲醇衍生物或其盐或其溶剂合物。

公开(公告)号：US08168666B2

公开(公告)日：2012-05-01

申请号：US12516944

申请日：2007-11-29

申请人： Takayuki Matsuda ,  Ayumu Okuda ,  Minoru Koura ,  Yuki Yamaguchi ,  Sayaka Kurobuchi ,  Yuuichirou Watanabe ,  Kimiyuki Shibuya

发明人： Takayuki Matsuda ,  Ayumu Okuda ,  Minoru Koura ,  Yuki Yamaguchi ,  Sayaka Kurobuchi ,  Yuuichirou Watanabe ,  Kimiyuki Shibuya

IPC分类号： A61K31/4015 ,  C07D233/32

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

摘要： There is provided a novel LXRβ agonist useful as a preventative and/or therapeutic agent for arteriosclerosis; arteriosclerosis such as those resulting from diabetes; hyperlipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases caused by inflammatory cytokines, skin diseases such as allergic skin diseases, diabetes or Alzheimer's disease. The agonist is a carbinol derivative represented by the following general formula (1) or salt thereof, or their solvate.

摘要翻译： 提供了一个新颖的LXR＆bgr; 可用作动脉硬化的预防和/或治疗剂的激动剂; 动脉硬化，如糖尿病引起的; 高脂血症 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，皮肤疾病如过敏性皮肤疾病，糖尿病或阿尔茨海默病。 激动剂是由以下通式（1）表示的甲醇衍生物或其盐或其溶剂合物。

公开(公告)号：US20100048610A1

公开(公告)日：2010-02-25

申请号：US12474799

申请日：2009-05-29

申请人： Yuki Yamaguchi ,  Minoru Koura ,  Sayaka Kurobuchi ,  Takayuki Matsuda ,  Ayumu Okuda ,  Hisashi Sumida ,  Yuuichirou Watanabe ,  Takashi Enomoto ,  Kimiyuki Shibuya

发明人： Yuki Yamaguchi ,  Minoru Koura ,  Sayaka Kurobuchi ,  Takayuki Matsuda ,  Ayumu Okuda ,  Hisashi Sumida ,  Yuuichirou Watanabe ,  Takashi Enomoto ,  Kimiyuki Shibuya

IPC分类号： A61K31/436 ,  C07D401/06 ,  A61K31/4439 ,  C07D491/056

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

摘要： [Object] 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 carbinol compound represented by the following general formula (I) or salt thereof, or their solvate.

摘要翻译： [目的]提供一种新型的LXR＆bgr; 可用作动脉粥样硬化的预防和/或治疗剂的激动剂; 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（I）表示的甲醇化合物或其盐或其溶剂化物。

公开(公告)号：US20100280013A1

公开(公告)日：2010-11-04

申请号：US12769104

申请日：2010-04-28

申请人： Minoru Koura ,  Hisashi Sumida ,  Sayaka Kurobuchi ,  Takayuki Matsuda ,  Yuichiro Watanabe ,  Takashi Enomoto ,  Kimiyuki Shibuya ,  Sumiko Kurobuchi

发明人： Minoru Koura ,  Hisashi Sumida ,  Sayaka Kurobuchi ,  Takayuki Matsuda ,  Yuichiro Watanabe ,  Takashi Enomoto ,  Kimiyuki Shibuya ,  Sumiko Kurobuchi

IPC分类号： A61K31/551 ,  C07D401/14 ,  C07D403/06 ,  C07D407/14 ,  A61P3/10 ,  A61P25/28 ,  A61P3/06 ,  A61P29/00 ,  A61K31/496 ,  A61P7/00 ,  A61P9/10 ,  A61P17/00

CPC分类号： C07D233/78 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D405/04 ,  C07D405/14 ,  C07D491/04

摘要： [Object] It is to provide a novel LXRβ agonist 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 carbinol compound represented by the following general formula (I) or salt thereof, or their solvate: (wherein, each V and W independently show N or C—R7; each X and Y independently show CH2, C═O, SO2, etc; Z shows CH or N; each R1, R2 and R7 independently show a hydrogen atom, C1-8 alkyl group, etc.; R3 shows C1-8 alkyl group; R4 shows an optionally substituted C6-10 aryl group or an optionally substituted 5- to 11-membered heterocyclic group; R5 and R6 show a hydrogen atom, etc.; L shows a C1-8 alkyl chain optionally substituted with an oxo group, etc.; and n shows any integer of 0 to 2.)

摘要翻译： [对象]提供一个新颖的LXR＆bgr; 可用作动脉粥样硬化的预防和/或治疗剂的激动剂; 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（I）表示的甲醇化合物或其盐或其溶剂化物：（其中，V和W各自独立地表示N或C-R7; X和Y各自独立地表示CH 2，C = O ，SO2等; Z表示CH或N;每个R1，R2和R7独立地表示氢原子，C1-8烷基等; R3表示C1-8烷基; R4表示任选取代的C6-10芳基 或任选取代的5至11元杂环基; R 5和R 6表示氢原子等; L表示任选被氧代基等取代的C 1-8烷基链; n表示0〜 2.）

公开(公告)号：US07750019B2

公开(公告)日：2010-07-06

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： C07D239/42 ,  A61K31/505

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。

公开(公告)号：US08012989B2

公开(公告)日：2011-09-06

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： A61K31/505

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。