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).

  • Publication number: 20170313664
    Abstract: It is an object of the present invention to provide a novel form of (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}acetic acid, which is useful for preventing and/or treating diseases such as dyslipidemia. (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}acetic acid hydrochloride.
    Type: Application
    Filed: May 15, 2017
    Publication date: November 2, 2017
    Applicant: KOWA COMPANY, LTD.
    Inventors: Koichi YAMAZAKI, Kennosuke MATSUDA, Taichi KUSAKABE, Tadaaki OHGIYA, Kimiyuki SHIBUYA
  • Patent number: 9682942
    Abstract: It is an object of the present invention to provide a novel form of (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}acetic acid, which is useful for preventing and/or treating diseases such as dyslipidemia. (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}acetic acid hydrochloride.
    Type: Grant
    Filed: May 30, 2014
    Date of Patent: June 20, 2017
    Assignee: KOWA COMPANY, LTD.
    Inventors: Koichi Yamazaki, Kennosuke Matsuda, Taichi Kusakabe, Tadaaki Ohgiya, Kimiyuki Shibuya
  • Patent number: 9540344
    Abstract: The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base.
    Type: Grant
    Filed: December 5, 2014
    Date of Patent: January 10, 2017
    Assignee: KOWA CO., LTD.
    Inventors: Noriaki Gomi, Tadaaki Ohgiya, Kimiyuki Shibuya
  • Patent number: 9272966
    Abstract: A method for preparing optically active 1-bromo-1-[3,5-bis(trifluoromethyl)-phenyl]ethane having a high optical purity, which comprises the step of brominating optically active 1-[3,5-bis(trifluoromethyl)phenyl]ethanol by using, as a brominating agent, (a) a combination of a phosphorus halide and hydrogen bromide, (b) a combination of 1,2-dibromo-1,1,2,2-tetrachloroethane and an organic phosphorous compound represented by the general formula (I): P(R1)(R2)(R3) (in the formula, R1, R2, and R3 independently represent a C6-10 aryl group, a C6-10 aryloxy group, a C1-10 alkyl group, a C1-10 alkoxyl group, a C3-6 cycloalkyl group, or a C3-6 cycloalkoxy group), or (c) a combination of N-bromosuccinimide and a dialkyl sulfide.
    Type: Grant
    Filed: July 21, 2011
    Date of Patent: March 1, 2016
    Assignee: Kowa Company, Ltd.
    Inventors: Taichi Kusakabe, Kennosuke Matsuda, Koichi Yamazaki, Tadaaki Ohgiya, Kimiyuki Shibuya
  • Publication number: 20160031827
    Abstract: It is an object of the present invention to provide a novel form of (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}acetic acid, which is useful for preventing and/or treating diseases such as dyslipidemia. (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}acetic acid hydrochloride.
    Type: Application
    Filed: May 30, 2014
    Publication date: February 4, 2016
    Applicant: KOWA COMPANY, LTD.
    Inventors: Koichi YAMAZAKI, Kennosuke MATSUDA, Taichi KUSAKABE, Tadaaki OHGIYA, Kimiyuki SHIBUYA
  • Publication number: 20150320748
    Abstract: The present invention is intended to provide a pharmaceutical product for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the present invention is also intended to provide a preventive and/or therapeutic agent for various diseases based on inhibition of expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and the present invention relates to an agent for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and relates also to a preventive and/or therapeutic agent for various diseases based on the inhibition of the expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the agent comprising a compound represented by Formula (I), its salt, or a solva
    Type: Application
    Filed: July 9, 2015
    Publication date: November 12, 2015
    Applicant: KOWA CO., LTD.
    Inventors: Kimiyuki SHIBUYA, Tadaaki Ohgiya, Takeshi Murakami
  • Publication number: 20150306098
    Abstract: The present invention is intended to provide a pharmaceutical product for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the present invention is also intended to provide a preventive and/or therapeutic agent for various diseases based on inhibition of expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and the present invention relates to an agent for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and relates also to a preventive and/or therapeutic agent for various diseases based on the inhibition of the expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the agent comprising a compound represented by Formula (I), its salt, or a solva
    Type: Application
    Filed: July 9, 2015
    Publication date: October 29, 2015
    Applicant: Kowa Co., Ltd.
    Inventors: Kimiyuki SHIBUYA, Tadaaki Ohgiya, Takeshi Murakami
  • Patent number: 9045460
    Abstract: The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base.
    Type: Grant
    Filed: August 25, 2011
    Date of Patent: June 2, 2015
    Assignee: KOWA CO., LTD.
    Inventors: Noriaki Gomi, Tadaaki Ohgiya, Kimiyuki Shibuya
  • Publication number: 20150087824
    Abstract: The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base.
    Type: Application
    Filed: December 5, 2014
    Publication date: March 26, 2015
    Applicant: KOWA CO., LTD.
    Inventors: Noriaki GOMI, Tadaaki OHGIYA, Kimiyuki SHIBUYA
  • Patent number: 8906895
    Abstract: Substantially optically pure (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}acetic acid, or a salt thereof, or a solvate thereof, which has actions of reducing amount of PCSK9 protein and increasing amount of LDL receptor.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: December 9, 2014
    Assignee: Kowa Company, Ltd.
    Inventors: Tadaaki Ohgiya, Takeshi Murakami, Katsutoshi Miyosawa, Kimiyuki Shibuya, Koichi Yamazaki, Taichi Kusakabe
  • Publication number: 20140303198
    Abstract: 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.
    Type: Application
    Filed: November 28, 2012
    Publication date: October 9, 2014
    Applicant: KOWA COMPANY, LTD.
    Inventors: Takeshi Murakami, Kentaro Murakami, Tadaaki Ohgiya, Kimiyuki Shibuya
  • Patent number: 8841478
    Abstract: 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: Grant
    Filed: November 27, 2009
    Date of Patent: September 23, 2014
    Assignee: Kowa Company, Ltd.
    Inventors: Taichi Kusakabe, Koichi Yamazaki, Tadaaki Ohgiya, Kimiyuki Shibuya
  • Publication number: 20140221390
    Abstract: Provided is a compound useful in the prevention and treatment of non-alcoholic steatohepatitis. A prophylactic and/or therapeutic agent for non-alcoholic steatohepatitis which contains, as the active ingredient, 2-[4-[2-(benzimidazol-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide, an acid-addition salt thereof, or a solvate of the same.
    Type: Application
    Filed: January 23, 2014
    Publication date: August 7, 2014
    Applicant: KOWA COMPANY, LTD.
    Inventors: Haruki Shibata, Yasunobu Yoshinaka, Kimiyuki Shibuya
  • Patent number: 8551985
    Abstract: [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: Grant
    Filed: April 28, 2010
    Date of Patent: October 8, 2013
    Assignee: Kowa Company, Ltd.
    Inventors: Minoru Koura, Hisashi Sumida, Takayuki Matsuda, Yuichiro Watanabe, Takashi Enomoto, Kimiyuki Shibuya, Sumiko Kurobuchi
  • Publication number: 20130225618
    Abstract: The present invention is intended to provide a pharmaceutical product for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the present invention is also intended to provide a preventive and/or therapeutic agent for various diseases based on inhibition of expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and the present invention relates to an agent for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and relates also to a preventive and/or therapeutic agent for various diseases based on the inhibition of the expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the agent comprising a compound represented by Formula (I), its salt, or a solva
    Type: Application
    Filed: October 3, 2011
    Publication date: August 29, 2013
    Applicant: KOWA CO., LTD.
    Inventors: Kimiyuki Shibuya, Tadaaki Ohgiya, Takeshi Murakami
  • Publication number: 20130225814
    Abstract: Substantially optically pure (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}acetic acid, or a salt thereof, or a solvate thereof, which has actions of reducing amount of PCSK9 protein and increasing amount of LDL receptor.
    Type: Application
    Filed: June 3, 2011
    Publication date: August 29, 2013
    Applicant: KOWA COMPANY, LTD.
    Inventors: Tadaaki Ohgiya, Takeshi Murakami, Katsutoshi Miyosawa, Kimiyuki Shibuya, Koichi Yamazaki, Taichi Kusakabe
  • Patent number: 8518936
    Abstract: Monohydrochloride acid addition salts of a polyacidic basic compound, or a water adduct having basic site(s) stronger than pyridine. These monohydrochlorides can be produced by reacting a polyacidic basic compound with an acid salt of pyridine.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: August 27, 2013
    Assignee: Kowa Co., Ltd.
    Inventors: Kimiyuki Shibuya, Tadaaki Ohgiya, Takayuki Matsuda
  • Publication number: 20130190540
    Abstract: A method for preparing optically active 1-bromo-1-[3,5-bis(trifluoromethyl)-phenyl]ethane having a high optical purity, which comprises the step of brominating optically active 1-[3,5-bis(trifluoromethyl)phenyl]ethanol by using, as a brominating agent, (a) a combination of a phosphorus halide and hydrogen bromide, (b) a combination of 1,2-dibromo-1,1,2,2-tetrachloroethane and an organic phosphorous compound represented by the general formula (I): P(R1)(R2)(R3) (in the formula, R1, R2, and R3 independently represent a C6-10 aryl group, a C6-10 aryloxy group, a C1-10 alkyl group, a C1-10 alkoxyl group, a C3-6 cycloalkyl group, or a C3-6 cycloalkoxy group), or (c) a combination of N-bromosuccinimide and a dialkyl sulfide.
    Type: Application
    Filed: July 21, 2011
    Publication date: July 25, 2013
    Applicant: Kowa Company, Ltd.
    Inventors: Taichi Kusakabe, Kennosuke Matsuda, Koichi Yamazaki, Tadaaki Ohgiya, Kimiyuki Shibuya
  • Publication number: 20130144054
    Abstract: The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base.
    Type: Application
    Filed: August 25, 2011
    Publication date: June 6, 2013
    Inventors: Noriaki Gomi, Tadaaki Ohgiya, Kimiyuki Shibuya
  • Publication number: 20130066075
    Abstract: Provided is a compound useful in the prevention and treatment of non-alcoholic steatohepatitis. A prophylactic and/or therapeutic agent for non-alcoholic steatohepatitis which contains, as the active ingredient, 2-[4-[2-(benzimidazol-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide, an acid-addition salt thereof, or a solvate of the same.
    Type: Application
    Filed: May 18, 2011
    Publication date: March 14, 2013
    Applicant: KOWA COMPANY, LTD.
    Inventors: Haruki Shibata, Yasunobu Yoshinaka, Kimiyuki Shibuya