Patents by Inventor Kimiyuki Shibuya
Kimiyuki Shibuya has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 8168666Abstract: There is provided a novel LXR? 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.Type: GrantFiled: November 29, 2007Date of Patent: May 1, 2012Assignee: Kowa Company, Ltd.Inventors: Takayuki Matsuda, Ayumu Okuda, Minoru Koura, Yuki Yamaguchi, Sayaka Kurobuchi, Yuuichirou Watanabe, Kimiyuki Shibuya
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Patent number: 8153634Abstract: [Object] To provide a novel LXR? 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.Type: GrantFiled: May 29, 2009Date of Patent: April 10, 2012Assignee: Kowa Company, Ltd.Inventors: Yuki Yamaguchi, Minoru Koura, Sayaka Kurobuchi, Takayuki Matsuda, Ayumu Okuda, Hisashi Sumida, Yuichiro Watanabe, Takashi Enomoto, Kimiyuki Shibuya
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Publication number: 20110288328Abstract: 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) (R1 represents hydrogen atom or a C1-6 alkyl group, and R2 represents a C1-6 alkyl group, a C3-6 cycloalkyl group, a (C3-6 cycloalkyl)(C1-6 alkyl) group, a C6-10 aryl group, or a C7-12 aralkyl group).Type: ApplicationFiled: November 27, 2009Publication date: November 24, 2011Applicant: KOWA COMPANY, LTD.Inventors: Taichi Kusakabe, Koichi Yamazaki, Tadaaki Ohgiya, Kimiyuki Shibuya
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Patent number: 8012989Abstract: 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).Type: GrantFiled: June 15, 2010Date of Patent: September 6, 2011Assignee: Kowa Company, Ltd.Inventors: Tadaaki Ohgiya, Toru Miura, Ayumu Okuda, Toshiharu Arai, Koichi Yamazaki, Taro Aoki, Katsutoshi Miyosawa, Haruki Shibata, Kimiyuki Shibuya
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Patent number: 8008306Abstract: To provide a novel LXR? 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.Type: GrantFiled: April 27, 2009Date of Patent: August 30, 2011Assignee: Kowa Company, Ltd.Inventors: Minoru Koura, Ayumu Okuda, Takayuki Matsuda, Yuki Yamaguchi, Hisashi Sumida, Sayaka Kurobuchi, Yuichiro Watanabe, Takashi Enomoto, Kimiyuki Shibuya
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Publication number: 20110207742Abstract: There is to provide is an agent for reduction of a lipid rich plaque, stabilization of a lipid rich plaque and/or prevention of rupture of a lipid rich plaque in an atherosclerotic lesion comprising an effective amount of 2-[4-[2-(benzimidazole-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-p yridyl]acetamide (hereinafter, referred to as compound 1), its pharmaceutically acceptable salt or a hydrate thereof and Pitavastatin, and a pharmaceutically acceptable carrier, wherein the agent is intended to be simultaneously administered, or separately administered with interval of time to a patient in need thereof There is also to provide a method for reduction of a lipid rich plaque, stabilization of a lipid rich plaque and/or prevention of rupture of a lipid rich plaque in an atherosclerotic lesion, comprising simultaneously administering, or separately administering with interval of time an effective amount of the compound 1, its pharmaceutically acceptable salt or a hydrate thereof and an effecType: ApplicationFiled: April 28, 2011Publication date: August 25, 2011Applicant: KOWA CO., LTD.Inventors: Hideyuki Kobayashi, Yasunobu Yoshinaka, Kimiyuki Shibuya
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Publication number: 20110166351Abstract: A novel method for preparing 5-[2-(methylthio)ethoxy]pyrimidin-2-amine useful as a regent or raw material for manufacture of medicaments, agricultural chemicals, and industrial products, which comprises alkanoylating the amino group of a 2-amino-4-alkoxypyrimidine, then converting the resultant into a 4-hydroxypyrimidine compound by a treatment with anhydrous aluminum chloride, further etherifying the 4-hydroxypyrimidine compound by a reaction with a 2-haloethyl methyl sulfide in the presence of a base, and removing the alkanoyl group to obtain 5-[2-(methylthio)ethoxy]pyrimidin-2-amine.Type: ApplicationFiled: September 11, 2009Publication date: July 7, 2011Applicant: KOWA COMPANY, LTD.Inventors: Koichi Yamazaki, Taichi Kusakabe, Tadaaki Ohgiya, Kimiyuki Shibuya
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Patent number: 7951822Abstract: The object is to provide a novel LXR? 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.Type: GrantFiled: March 30, 2009Date of Patent: May 31, 2011Assignee: Kowa Company, Ltd.Inventors: Ayumu Okuda, Takayuki Matsuda, Toru Miura, Koichi Yamazaki, Yuki Yamaguchi, Minoru Koura, Sayaka Kurobuchi, Yuichiro Watanabe, Kimiyuki Shibuya
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Patent number: 7919509Abstract: To provide a novel LXR? 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.Type: GrantFiled: February 27, 2009Date of Patent: April 5, 2011Assignee: Kowa Company, Ltd.Inventors: Ayumu Okuda, Takayuki Matsuda, Toru Miura, Hidefumi Ozawa, Ayako Tosaka, Koichi Yamazaki, Yuki Yamaguchi, Sayaka Kurobuchi, Yuichiro Watanabe, Kimiyuki Shibuya
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Patent number: 7884106Abstract: A method of stabilizing lipid-rich plaques and method of preventing the rupture thereof, characterized in that an effective amount of 2-[4-[2-(benzimidazol-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide, its acid adduct salt or a hydrate thereof is administered to patients with lipid-rich plaques. Prevention of plaque rupture and stabilization of plaques can be attained by reducing the occupancy of macrophages in lipid-rich plaques being unstable and tending to rupture among plaques being a lesion from a seat of atherosclerosis and simultaneously increasing the occupancy of collagen therein.Type: GrantFiled: August 19, 2004Date of Patent: February 8, 2011Assignee: Kowa Company, Ltd.Inventors: Kimiyuki Shibuya, Hideyuki Kobayashi, Yasunobu Yoshinaka
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Publication number: 20110015206Abstract: A method of stabilizing lipid-rich plaques and method of preventing the rupture thereof, characterized in that an effective amount of 2-[4-[2-(benzimidazol-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide, its acid adduct salt or a hydrate thereof is administered to patients with lipid-rich plaques. Prevention of plaque rupture and stabilization of plaques can be attained by reducing the occupancy of macrophages in lipid-rich plaques being unstable and tending to rupture among plaques being a lesion from a seat of atherosclerosis and simultaneously increasing the occupancy of collagen therein.Type: ApplicationFiled: August 17, 2010Publication date: January 20, 2011Applicant: KOWA CO., LTD.Inventors: Kimiyuki Shibuya, Hideyuki Kobayashi, Yasunobu Yoshinaka
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Publication number: 20100280013Abstract: [Object] It is to provide a novel LXR? 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.Type: ApplicationFiled: April 28, 2010Publication date: November 4, 2010Applicant: KOWA COMPANY, LTD.Inventors: Minoru Koura, Hisashi Sumida, Sayaka Kurobuchi, Takayuki Matsuda, Yuichiro Watanabe, Takashi Enomoto, Kimiyuki Shibuya, Sumiko Kurobuchi
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Publication number: 20100249148Abstract: 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).Type: ApplicationFiled: June 15, 2010Publication date: September 30, 2010Applicant: KOWA COMPANY, LTD.Inventors: Tadaaki OHGIYA, Toru MIURA, Ayumu OKUDA, Toshiharu ARAI, Koichi YAMAZAKI, Taro AOKI, Katsutoshi MIYOSAWA, Haruki SHIBATA, Kimiyuki SHIBUYA
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Publication number: 20100234599Abstract: This invention relates to a method for preparing an acid addition salt of a polyacidic basic compound, or a water adduct having basic site(s) stronger than pyridine. The method comprises reacting the polyacidic basic compound with an acid salt of pyridine. By the present invention, the number of moles of an added acid in the acid addition salt of the polyacidic basic compound can be readily changed to a number suited for the polyacidic basic compound as needed.Type: ApplicationFiled: April 16, 2010Publication date: September 16, 2010Applicant: Kowa Co., Ltd.Inventors: Kimiyuki Shibuya, Tadaaki Ohgiya, Takayuki Matsuda
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Patent number: 7790737Abstract: 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).Type: GrantFiled: March 11, 2008Date of Patent: September 7, 2010Assignee: Kowa Company, Ltd.Inventors: Tadaaki Ohgiya, Toru Miura, Ayumu Okuda, Toshiharu Arai, Koichi Yamazaki, Taro Aoki, Katsutoshi Miyosawa, Haruki Shibata, Kimiyuki Shibuya
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Patent number: 7790903Abstract: A process for obtaining a compound (1) and an intermediate thereof in high yield and high optical yield is provided. A process for producing a compound (4), the process including reacting a compound (2) with a compound (3) in the presence of a base; and a process for producing a compound (1), the process including reacting a compound (2) with a compound (3) in the presence of a base to yield a compound (4) and then deesterifying the compound (4). wherein R represents an alkyl group having 1 to 6 carbon atoms or an aralkyl group having 7 to 8 carbon atoms.Type: GrantFiled: February 23, 2006Date of Patent: September 7, 2010Assignee: Kowa Co., Ltd.Inventors: Yukiyoshi Yamazaki, Takaaki Araki, Minoru Koura, Kimiyuki Shibuya
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Patent number: 7767845Abstract: A process for producing an optically active 2-hydroxybutyric ester represented by formula (1): by reacting an optically active 2,3-epoxypropionic ester represented by formula (2): with a methyl Grignard reagent CH3MgX in the presence of a copper catalyst in an amount of 0.05 to 0.5 mol with respect to 1 mol of the 2,3-epoxypropionic ester.Type: GrantFiled: July 27, 2006Date of Patent: August 3, 2010Assignee: Kowa Co., Ltd.Inventors: Minoru Koura, Yukiyoshi Yamazaki, Kimiyuki Shibuya
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Patent number: 7750150Abstract: This invention relates to a method for preparing an acid addition salt of a polyacidic basic compound, or a water adduct having basic site(s) stronger than pyridine. The method comprises reacting the polyacidic basic compound with an acid salt of pyridine. By the present invention, the number of moles of an added acid in the acid addition salt of the polyacidic basic compound can be readily changed to a number suited for the polyacidic basic compound as needed.Type: GrantFiled: February 27, 2004Date of Patent: July 6, 2010Assignee: Kowa Co., Ltd.Inventors: Kimiyuki Shibuya, Tadaaki Ohgiya, Takayuki Matsuda
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Patent number: 7750019Abstract: 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.Type: GrantFiled: August 7, 2007Date of Patent: July 6, 2010Assignee: Kowa Company, Ltd.Inventors: Tadaaki Ohgiya, Toru Miura, Ayumu Okuda, Toshiharu Arai, Koichi Yamazaki, Taro Aoki, Katsutoshi Miyosawa, Haruki Shibata, Kimiyuki Shibuya
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Patent number: 7714141Abstract: The invention provides a process for producing an optically active butyric acid compound and a production intermediate therefore at high yield and high purity. The present invention provides a process for producing Compound (6), including reacting Compound (1) with optically active 2-trifluoromethanesulfonyloxybutyrolactone (2a) in the presence of a base or reacting optically active 2-hydroxybutyrolactone (2b) under Mitsunobu reaction conditions, to thereby form Compound (3); reacting Compound (3) with an alcohol and a halogenating agent, to thereby form Compound (4); dehalogenating Compound (4), to thereby form Compound (5); and de-esterifying Compound (5).Type: GrantFiled: May 30, 2006Date of Patent: May 11, 2010Assignee: Kowa Co., Ltd.Inventors: Yukiyoshi Yamazaki, Takaaki Araki, Minoru Koura, Kimiyuki Shibuya