Patents by Inventor Mitsuo Nagai
Mitsuo Nagai 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: 20160215007Abstract: A method of producing 4-(((6S,9S)-1-(benzylcarbamoyl)-2,9-dimethyl-4,7-dioxo-8-(quinolin-8-ylmethyl)octahydro -1H-pyrazino[2,1-c][1,2,4]triazin-6-yl)methyl)phenyl dihydrogen phosphate, including a step of adding a reaction mixture 1 containing (6S,9S)-N-benzyl-6-(4-hydroxybenzyl)-2,9-dimethyl-4,7-dioxo-8-(quinolin-8-ylmethyl)octahydro -1H-pyrazino[2,1-c][1,2,4]triazine-1-carboxamide, triethylamine and a solvent to a reaction mixture 2 containing a phosphorylating agent and a solvent.Type: ApplicationFiled: September 9, 2014Publication date: July 28, 2016Applicant: PRISM Pharma Co., Ltd.Inventors: Minetaka ISOMURA, Yuki KOSAKA, Mitsuo NAGAI, Takenao ODAGAMI, Hiroyuki KOUJI
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Patent number: 9227942Abstract: 5-(Difluoromethyl)pyrazine-2-carboxylic acid, which is a raw material for the construction of 5-(difluoromethyl)pyrazine-2-carboxamide, which is a common partial structural motif of the compound having an A? production inhibitory action or a BACE1 inhibitory action, can be industrially advantageously produced by decarboxylating 5-[carboxy(difluoro)methyl]pyrazine-2-carboxylic acid, which is obtainable from 5-chloropyrazine-2-carboxylate.Type: GrantFiled: April 25, 2013Date of Patent: January 5, 2016Assignee: Eisai R&D Management Co., Ltd.Inventors: Kazuhiro Yoshizawa, Masayuki Omori, Yuzo Watanabe, Mitsuo Nagai, Masabumi Takahashi, Francis G. Fang
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Publication number: 20150087836Abstract: 5-(Difluoromethyl)pyrazine-2-carboxilic acid, which is a raw material for the construction of 5-(difluoromethyl)pyrazine-2-carboxamide, which is a common partial structural motif of the compound having an A production inhibitory action or a BACE1 inhibitory action, can be industrially advantageously produced by decarboxylating 5-[carboxy(difluoro)methyl]pyrazine-2-carboxylic acid, which is obtainable from 5-chloropyrazine-2-carboxylate.Type: ApplicationFiled: April 25, 2013Publication date: March 26, 2015Inventors: Kazuhiro Yoshizawa, Masayuki Omori, Yuzo Watanabe, Mitsuo Nagai, Masabumi Takahashi, Francis G. Fang
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Patent number: 7893068Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.Type: GrantFiled: October 29, 2007Date of Patent: February 22, 2011Assignees: Mercian Corporation, Eisai R&D Management Co., Ltd.Inventors: Yoshihiko Kotake, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
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Publication number: 20100311972Abstract: A method for producing a compound represented by the formula (I) the method comprising reacting in the presence of a condensation agent a compound represented by the formula (II) or a salt thereof with a compound represented by the formula (III) wherein R1 represents a 4-(4-methylpiperadin-1-yl) group or 3-hydroxyazetidin-1-yl group, R2, R3, R4 and R5 may be the same or different and each represents a hydrogen atom or a fluorine atom and R6 represents a hydrogen atom or a fluorine atom.Type: ApplicationFiled: February 13, 2009Publication date: December 9, 2010Inventor: Mitsuo Nagai
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Publication number: 20100280243Abstract: 4-(Substituted phenyl)hexahydropyrido[2,1-c][1,4]oxazin-6-one represented by formula (I) or a salt thereof is useful as an intermediate for the production of a bicyclic cinnamide compound which is an A? production inhibitor. 4-(Substituted phenyl)hexahydropyrido[2,1-c][1,4]oxazin-6-one or the salt thereof can be produced in an industrially advantageous manner by subjecting a compound represented by formula (II) or a salt thereof to an intramolecular condensation reaction.Type: ApplicationFiled: December 25, 2008Publication date: November 4, 2010Inventors: Akio Kayano, Mitsuo Nagai, Yorihisa Hoshino, Kazunori Wakasugi, Masaaki Matsuda, Atsushi Kamada, Minetaka Isomura, Yoshihiro Nishikawa, Seiji Yoshikawa, Daisuke Shimmyo
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Patent number: 7790885Abstract: A process for preparing a compound represented by the formula (I): comprising reacting a compound represented by the formula (II) or salt thereof: with a compound represented by the formula (III): in the presence of a condensation reagent, wherein R1 represents 1) optionally substituted azetidin-1-yl, 2) optionally substituted pyrrolidin-1-yl, 3) optionally substituted piperidin-1-yl, etc.; R2, R3, R4 and R5 may be the same or different and each represents hydrogen or fluorine; and R6 represents hydrogen or fluorine.Type: GrantFiled: August 27, 2007Date of Patent: September 7, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Mitsuo Nagai, Tomohiro Matsushima, Atsushi Kamada, Kazunori Wakasugi, Shuji Shirotori, Shinya Abe, Kazumasa Nara, Takahisa Sakaguchi
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Patent number: 7667052Abstract: The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution of Streptomyces sp. Mer. 11107 or a variant thereof, a pharmacologically acceptable salt thereof or a hydrate of them, and a process for producing it.Type: GrantFiled: August 30, 2005Date of Patent: February 23, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Yoshiharu Mizui, Takashi Sakai, Satoshi Yamamoto, Keisuke Komeda, Masanori Fujita, Akifumi Okuda, Kumiko Kishi, Jun Niijima, Mitsuo Nagai, Kiyoshi Okamoto, Masao Iwata, Yoshihiko Kotake, Toshimitsu Uenaka, Naoki Asai, Motoko Matsufuji, Tomohiro Sameshima, Naoto Kawamura, Kazuyuki Dobashi, Takashi Nakashima, Masashi Yoshida, Toshio Tsuchida, Susumu Takeda, Tomonari Yamada, Koji Norihisa, Takao Yamori
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Patent number: 7619100Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.Type: GrantFiled: October 29, 2007Date of Patent: November 17, 2009Assignees: Mercian Corporation, Eisai R&D Management Co., Ltd.Inventors: Yoshihiko Kotake, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
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Patent number: 7576204Abstract: A compound represented by the following general formula (I): (I) wherein R7 and R21 are the same or different and each represents optionally substituted C2-22 alkoxy, etc.; a pharmaceutically acceptable salt thereof or hydrates of the same. The compound (1) inhibits angiogenesis and inhibits the production of VEGF particularly under hypoxic conditions, which makes it useful as a remedy for solid cancer.Type: GrantFiled: July 31, 2003Date of Patent: August 18, 2009Assignees: Mercian Corporation, Eisai R&D Management Co., Ltd.Inventors: Mitsuo Nagai, Masashi Yoshida, Toshio Tsuchida
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Publication number: 20090163715Abstract: A compound represented by the general formula below or a salt thereof is a useful intermediate in the production of a [2-(3,3,5,5-tetramethylcyclohexyl)phenyl]piperazine compound that has excellent cell adhesion inhibitory effect and cell invasion inhibitory effect and therefore is useful as a therapeutic or prophylactic agent for various inflammatory diseases and autoimmune diseases induced by the adhesion and invasion of leukocytes, such as inflammatory bowel diseases (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. wherein R1 and R2 independently represent hydrogen or a protecting group for an amino group, or R1 and R2 bond together to form an optionally substituted pyrrole ring.Type: ApplicationFiled: May 25, 2006Publication date: June 25, 2009Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Mitsuo Nagai, Kazumasa Nara, Kazunori Wakasugi, Toshihiko Naito
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Patent number: 7550503Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.Type: GrantFiled: June 23, 2006Date of Patent: June 23, 2009Assignees: Eisai R& D Management Co., Ltd., Merican CorporationInventors: Yoshihiko Kotake, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
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Publication number: 20080275059Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.Type: ApplicationFiled: October 29, 2007Publication date: November 6, 2008Inventors: Yoshihiko KOTAKE, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
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Publication number: 20080255146Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.Type: ApplicationFiled: October 29, 2007Publication date: October 16, 2008Inventors: Yoshihiko KOTAKE, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
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Publication number: 20080214815Abstract: A process for preparing a compound represented by the formula (I): comprising reacting a compound represented by the formula (II) or salt thereof: with a compound represented by the formula (III): in the presence of a condensation reagent, wherein R1 represents 1) optionally substituted azetidin-1-yl, 2) optionally substituted pyrrolidin-1-yl, 3) optionally substituted piperidin-1-yl, etc.; R2, R3, R4 and R5 may be the same or different and each represents hydrogen or fluorine; and R6 represents hydrogen or fluorine.Type: ApplicationFiled: August 27, 2007Publication date: September 4, 2008Applicant: Eisai R&D Management Co., Ltd.Inventors: Mitsuo Nagai, Tomohiro Matsushima, Atsushi Kamada, Kazunori Wakasugi, Shuji Shirotori, Shinya Abe, Kazumasa Nara, Takahisa Sakaguchi
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Patent number: 7256178Abstract: Compounds represented by the following general formula (I), pharmacologically acceptable salts thereof or hydrates of the same: (I) wherein W represents and R3, R7, R16, R17, R20, R21 and R21? are the same or different and each represents hydrogen, etc. Because of inhibiting angiogenesis and inhibiting the production of VEGF particularly in hypoxia, the compounds (I) are useful as remedies for solid cancer.Type: GrantFiled: July 31, 2003Date of Patent: August 14, 2007Assignees: Eisai Co., Ltd., Mercian CorporationInventors: Yoshihiko Kotake, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Susumu Takeda, Takashi Nakashima, Masashi Yoshida, Toshio Tsuchida, Tomohiro Sameshima
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Publication number: 20060241171Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.Type: ApplicationFiled: June 23, 2006Publication date: October 26, 2006Inventors: Yoshihiko Kotake, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
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Publication number: 20060235002Abstract: A compound represented by the following general formula (I): (I) wherein R7 and R21 are the same or different and each represents optionally substituted C2-22 alkoxy, etc.; a pharmaceutically acceptable salt thereof or hydrates of the same. The compound (1) inhibits angiogenesis and inhibits the production of VEGF particularly under hypoxic conditions, which makes it useful as a remedy for solid cancer.Type: ApplicationFiled: July 31, 2003Publication date: October 19, 2006Inventors: Mitsuo Nagai, Masashi Yoshida, Toshio Tsuchida
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Patent number: 7093534Abstract: The invention comprises the steps of storing immersed or smothered raw material of soy beans including hulls in a storage chamber provided at the front part of a cylinder barrel, subsequently passing the stored raw material of soybeans through screens furnished at the front end of the cylinder barrel by driving a piston, and urging to press it out, thereby to manufacture a milk of the soy beans of the raw material being extremely refined. At this time, the screens are 60 to 500 meshes, and the pressure is 8.0 to 55.0 MPa.Type: GrantFiled: April 24, 2003Date of Patent: August 22, 2006Assignee: The Japan Steel Works, Ltd.Inventors: Mitsuo Nagai, Osamu Moriyama
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Publication number: 20060079572Abstract: The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution of Streptomyces sp. Mer. 11107 or a variant thereof, a pharmacologically acceptable salt thereof or a hydrate of them, and a process for producing it.Type: ApplicationFiled: August 30, 2005Publication date: April 13, 2006Inventors: Yoshiharu Mizui, Takashi Sakai, Satoshi Yamamoto, Keisuke Komeda, Masanori Fujita, Akifumi Okuda, Kumiko Kishi, Jun Niijima, Mitsuo Nagai, Kiyoshi Okamoto, Masao Iwata, Yoshihiko Kotake, Toshimitsu Uenaka, Naoki Asai, Motoko Matsufuji, Tomohiro Sameshima, Naoto Kawamura, Kazuyuki Dobashi, Takashi Nakashima, Masashi Yoshida, Toshio Tsuchida, Susumu Takeda, Tomonari Yamada, Koji Norihisa, Takao Yamori