Patents by Inventor Koki Matsubara
Koki Matsubara 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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Publication number: 20230149382Abstract: The present invention relates to tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the P2X7 receptor.Type: ApplicationFiled: July 22, 2022Publication date: May 18, 2023Inventors: Hirohide NOGUCHI, Yoshimasa ARANO, Kazuo ANDO, Kazuki TOYOSHIMA, Toshihiko SONE, Koki MATSUBARA
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Patent number: 11439633Abstract: The present invention relates to tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the P2X7 receptor.Type: GrantFiled: December 4, 2020Date of Patent: September 13, 2022Assignees: RaQualia Pharma Inc., Asahi Kasei Pharma CorporationInventors: Yoshimasa Arano, Kazuki Toyoshima, Toshihiko Sone, Koki Matsubara
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Publication number: 20210085667Abstract: The present invention relates to tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the P2X7 receptor.Type: ApplicationFiled: December 4, 2020Publication date: March 25, 2021Applicants: RaQualia Pharma Inc., Asahi Kasei Pharma CorporationInventors: Hirohide NOGUCHI, Yoshimasa ARANO, Kazuo ANDO, Kazuki TOYOSHIMA, Toshihiko SONE, Koki MATSUBARA
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Publication number: 20200405706Abstract: The present invention relates to tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the P2X7 receptor.Type: ApplicationFiled: March 13, 2018Publication date: December 31, 2020Applicants: RaQualia Pharma Inc., Asahi Kasei Pharma CorporationInventors: Hirohide NOGUCHI, Yoshimasa ARANO, Kazuo ANDO, Kazuki TOYOSHIMA, Toshihiko SONE, Koki MATSUBARA
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Patent number: 8664243Abstract: (S)-1-(4-Chloro-5-isoquinolinesulfonyl)-3-(methylamino)pyrrolidine monohydrochloride and a crystal thereof, and a crystal of the aforementioned monohydrochloride having a major peak or peaks at one or more positions selected from the group consisting of positions where 2?s are about 13.9°, 21.5°, 21.7°, 22.4°, 22.8°, 24.5° and 35.0° in a powder X-ray diffraction spectrum, which have excellent properties as active ingredient of a medicament for prophylactic and/or therapeutic treatment of glaucoma and the like.Type: GrantFiled: June 27, 2012Date of Patent: March 4, 2014Assignee: Asahi Kasei Pharma CorporationInventors: Hitoshi Kida, Koki Matsubara, Shunsuke Kaneko
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Publication number: 20120270898Abstract: (S)-1-(4-Chloro-5-isoquinolinesulfonyl)-3-(methylamino)pyrrolidine monohydrochloride and a crystal thereof, and a crystal of the aforementioned monohydrochloride having a major peak or peaks at one or more positions selected from the group consisting of positions where 2?s are about 13.9°, 21.5°, 21.7°, 22.4°, 22.8°, 24.5° and 35.0° in a powder X-ray diffraction spectrum, which have excellent properties as active ingredient of a medicament for prophylactic and/or therapeutic treatment of glaucoma and the like.Type: ApplicationFiled: June 27, 2012Publication date: October 25, 2012Inventors: Hitoshi KIDA, Koki Matsubara, Shunsuke Kaneko
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Patent number: 8232292Abstract: (S)-1-(4-Chloro-5-isoquinolinesulfonyl)-3-(methylamino)pyrrolidine monohydrochloride and a crystal thereof, and a crystal of the aforementioned monohydrochloride having a major peak or peaks at one or more positions selected from the group consisting of positions where 2?s are about 13.9°, 21.5°, 21.7°, 22.4°, 22.8°, 24.5° and 35.0° in a powder X-ray diffraction spectrum, which have excellent properties as active ingredient of a medicament for prophylactic and/or therapeutic treatment of glaucoma and the like.Type: GrantFiled: July 1, 2008Date of Patent: July 31, 2012Assignee: Asahi Kasei Pharma CorporationInventors: Hitoshi Kida, Koki Matsubara, Shunsuke Kaneko, Yoshihito Kanzawa
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Patent number: 7964613Abstract: A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; G1 represents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; G2 represents a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; G3 represents hydrogen atom, a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkoxycarbonyl group, an acyl group, an acyloxy group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; Y represents a single bond, or —C(R3)(R4)— (R3 and R4 represent hydrogen atom, or an alkyl group, or alkylene groups which combine together to form a saturated hydrocarbon ring group); G4 represents hydroType: GrantFiled: February 27, 2008Date of Patent: June 21, 2011Assignee: Asahi Kasei Pharma CorporationInventors: Koki Matsubara, Atsushi Iesato, Akifumi Oomura, Koh Kawasaki, Rintaro Yamada, Minoru Seto
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Publication number: 20090156823Abstract: (S)-1-(4-Chloro-5-isoquinolinesulfonyl)-3-(methylamino)pyrrolidine monohydrochloride and a crystal thereof, and a crystal of the aforementioned monohydrochloride having a major peak or peaks at one or more positions selected from the group consisting of positions where 2?s are about 13.9°, 21.5°, 21.7°, 22.4°, 22.8°, 24.5° and 35.0° in a powder X-ray diffraction spectrum, which have excellent properties as active ingredient of a medicament for prophylactic and/or therapeutic treatment of glaucoma and the like.Type: ApplicationFiled: July 1, 2008Publication date: June 18, 2009Applicant: Asahi Kasei Pharma CorporationInventors: Hitoshi Kida, Koki Matsubara, Shunsuke Kaneko, Yoshihito Kanzawa
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Publication number: 20090048223Abstract: A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; G1 represents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; G2 represents a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; G3 represents hydrogen atom, a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkoxycarbonyl group, an acyl group, an acyloxy group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; Y represents a single bond, or —C(R3)(R4)— (R3 and R4 represent hydrogen atom, or an alkyl group, or alkylene groups which combine together to form a saturated hydrocarbon ring group); G4 represents hydroType: ApplicationFiled: February 27, 2008Publication date: February 19, 2009Applicant: Asahi Kasei Pharma CorporationInventors: Koki Matsubara, Atsushi Iesato, Akifumi Oomura, Koh Kawasaki, Rintaro Yamada, Minoru Seto
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Patent number: 6696573Abstract: A process for the preparation of tricyclic amino alcohol derivatives including 2-[N-[2-(9H-carbazol-2-yloxy)ethyl]]amino-1-[(3-methylsulfonylamino)phenyl]ethanol useful in the treatment of diabetes, obesity, hyperlipidemia and so on; and intermediates as represented by formula (5) or (6) or the like useful in the preparation, wherein R11 is hydrogen or the like; and *1 represents an asymmetric carbon atom. 2-Halo-1-(3-nitrophenyl)ethanone derivatives and 1-(3-nitrophenyl)oxirane derivatives, which are intermediates for the preparation of tricyclic amino alcohol derivatives, are easy of purification, and particularly optically active 1-(3-nitrophenyl)oxirane derivatives are effective in enhancing the optical purities of the final products.Type: GrantFiled: March 4, 2002Date of Patent: February 24, 2004Assignee: Asahi Kasei Kabushiki KaishaInventors: Koki Matsubara, Naoyuki Ishii, Masami Ogawa
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Publication number: 20030225289Abstract: A process for the preparation of tricyclic amino alcohol derivatives including 2-[N-[2-(9H-carbazol-2-yloxy)ethyl]]amino-1-[(3-methylsulfonylamino)phenyl]ethanol useful in the treatment of diabetes, obesity, hyperlipidemia and so on; and intermediates as represented by formula (5) or (6) or the like useful in the preparation, wherein R11 is hydrogen or the like; and *1 represents an asymmetric carbon atom. 2-Halo-1-(3-nitrophenyl)ethanone derivatives and 1-(3-nitrophenyl)oxirane derivatives, which are intermediates for the preparation of tricyclic amino alcohol derivatives, are easy of purification, and particularly optically active 1-(3-nitrophenyl)oxirane derivatives are effective in enhancing the optical purities of the final products.Type: ApplicationFiled: June 11, 2003Publication date: December 4, 2003Applicant: ASAHI KASEI KABUSHIKI KAISHAInventors: Koki Matsubara, Naoyuki Ishii, Masami Ogawa
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Patent number: 6495701Abstract: The present invention is directed to processes for the preparation of a compound useful for treating diabetes, obesity, hyperlipidemia and the like, which compound is represented by the formula (1): wherein R1 represents a lower alkyl group or a benzyl group; *1 represents an asymmetric carbon atom; R2 hydrogen atom, a halogen atom or a hydroxyl group; and A represents one of the following groups: wherein X represents NH, O or S; R6 represents a hydrogen atom, a hydroxyl group, an amino group or an acetylamino group; and *2 represents an asymmetric carbon atom when R6 is not a hydrogen atom, and to intermediates useful for the said processes. The processes of the present invention are convenient, practical preparing processes with low cost which comprise a small number of steps with good industrial work efficiency.Type: GrantFiled: September 26, 2001Date of Patent: December 17, 2002Assignee: Asahi Kasei Kabushiki KaishaInventors: Koki Matsubara, Hitoshi Kida