Patents by Inventor Hidetsugu Tsubouchi
Hidetsugu Tsubouchi 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: 9051333Abstract: The present invention provides a novel 6,7-dihydroimidazo[2,1-b][1,3]oxazine compound that has excellent bactericidal action against tubercle bacilli, multidrug-resistant tubercle bacilli, and atypical acid-fast bacilli. Specifically, the present invention provides a compound represented by Formula (1): or a salt thereof, wherein R1 represents tetrahydroisoquinolyl, tetrahydroquinolyl, tetrahydrobenzoazepinyl, benzoxazolyl, benzothiazolyl, indolyl, isoindolinyl, naphthyl, quinolyl, phenyl, biphenylyl, or pyridyl, these groups being optionally substituted, the phenyl, biphenylyl, and pyridyl represented by R1 each being substituted directly or via a linker with at least one group selected from the group consisting of tetrahydropyridyl, diazepanyl, diazabicycloheptanyl, tetrahydrotriazolopyrazinyl, tetrahydroimidazopyrazinyl, azabicyclooctanyl, oxazolyl, piperazinyl, piperidyl, thiazolyl, and the like, each of these groups being optionally substituted; and R2 represents hydrogen or lower alkyl.Type: GrantFiled: April 13, 2012Date of Patent: June 9, 2015Assignee: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Yoshikazu Kawano, Yoshikazu Haraguchi, Hirofumi Sasaki, Yukitaka Uematsu, Hidetsugu Tsubouchi, Hiromi Yata, Hiroshi Shimizu, Kazuho Kohashi, Motohiro Itotani, Kuninori Tai, Isao Takemura, Mikayo Hayashi, Hiroyuki Hashizume, Miki Matsuba, Izuru Nakamura, Xiuhao Chen, Makoto Matsumoto
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Publication number: 20140031342Abstract: The present invention provides a novel 6,7-dihydroimidazo[2,1-b][1,3]oxazine compound that has excellent bactericidal action against tubercle bacilli, multidrug-resistant tubercle bacilli, and atypical acid-fast bacilli. Specifically, the present invention provides a compound represented by Formula (1): or a salt thereof, wherein R1 represents tetrahydroisoquinolyl, tetrahydroquinolyl, tetrahydrobenzoazepinyl, benzoxazolyl, benzothiazolyl, indolyl, isoindolinyl, naphthyl, quinolyl, phenyl, biphenylyl, or pyridyl, these groups being optionally substituted, the phenyl, biphenylyl, and pyridyl represented by R1 each being substituted directly or via a linker with at least one group selected from the group consisting of tetrahydropyridyl, diazepanyl, diazabicycloheptanyl, tetrahydrotriazolopyrazinyl, tetrahydroimidazopyrazinyl, azabicyclooctanyl, oxazolyl, piperazinyl, piperidyl, thiazolyl, and the like, each of these groups being optionally substituted; and R2 represents hydrogen or lower alkyl.Type: ApplicationFiled: April 13, 2012Publication date: January 30, 2014Applicant: Otsuka Pharmaceutical Co., Ltd.Inventors: Yoshikazu Kawano, Yoshikazu Haraguchi, Hirofumi Sasaki, Yukitaka Uematsu, Hidetsugu Tsubouchi, Hiromi Yata, Hiroshi Shimizu, Kazuho Kohashi, Motohiro Itotani, Kuninori Tai, Isao Takemura, Mikayo Hayashi, Hiroyuki Hashizume, Miki Matsuba, Izuru Nakamura, Xiuhao Chen, Makoto Matsumoto
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Patent number: 8552188Abstract: The present invention provides a novel intermediate for manufacturing a 2,3-dihydroimidazo[2,1-b]oxazole compound with a high yield and a high purity, and a manufacturing method of the intermediate. The present invention provides an epoxy compound represented by the general formula (2): wherein, R1 represents a hydrogen or a lower alkyl group; and R2 represents a piperidyl group represented by the general formula (A1): (wherein, R3 represents a phenoxy group having a halogen-substituted lower alkoxy group substituted on a phenyl group, and the like) and the like; and n represents an integer of 1 to 6, a manufacturing method of the epoxy compound, and a manufacturing method of an oxazole compound using the epoxy method.Type: GrantFiled: November 15, 2012Date of Patent: October 8, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hidetsugu Tsubouchi, Yoshikazu Haraguchi, Satoshi Hayakawa, Naoto Utsumi, Shinichi Taira, Yoshihisa Tanada, Nobuhisa Fujita, Koichi Shinhama, Kimiyoshi Annaka, Takuya Furuta
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Patent number: 8344148Abstract: The present invention provides a novel intermediate for manufacturing a 2,3-dihydroimidazo[2,1-b]oxazole compound with a high yield and a high purity, and a manufacturing method of the intermediate. The present invention provides an epoxy compound represented by the general formula (2): wherein, R1 represents hydrogen or a lower alkyl group; and R2 represents a piperidyl group represented by the general formula (A1): (wherein, R3 represents a phenoxy group having a halogen-substituted lower alkoxy group substituted on a phenyl group, and the like) and the like; and n represents an integer of 1 to 6, a manufacturing method of the epoxy compound, and a manufacturing method of an oxazole compound using the epoxy compound.Type: GrantFiled: May 7, 2008Date of Patent: January 1, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hidetsugu Tsubouchi, Yoshikazu Haraguchi, Satoshi Hayakawa, Naoto Utsumi, Shinichi Taira, Yoshihisa Tanada, Nobuhisa Fujita, Koichi Shinhama, Kimiyoshi Annaka, Takuya Furuta
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Patent number: 8334248Abstract: The present invention provides a disinfectant that contains olanexidine in a concentration sufficient to exhibit an effective bactericidal effect, and that has hardly any side effects such as skin irritation. Specifically, the present invention provides a disinfectant containing an aqueous solution that contains olanexidine and at least an equimolar amount of gluconic acid, and substantially contains neither an acid other than gluconic acid nor a salt of the acid other than gluconic acid.Type: GrantFiled: September 10, 2010Date of Patent: December 18, 2012Assignees: Otsuka Pharmaceutical Co., Ltd., Otsuka Pharmaceutical Factory, Inc.Inventors: Kazuyoshi Miyata, Yasuhide Inoue, Akifumi Hagi, Motoya Kikuchi, Hitoshi Ohno, Kinji Hashimoto, Kinue Ohguro, Tetsuya Sato, Hidetsugu Tsubouchi, Hiroshi Ishikawa, Takashi Okamura, Koushi Iwata
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Publication number: 20120130082Abstract: The present invention relates to a 1-substituted-4-nitroimidazole compound represented by the general formula (1) or a salt thereof, (wherein R is a hydrogen atom, a lower alkoxy group-substituted lower alkyl group, a phenyl-lower alkoxy group-substituted lower alkyl group, a cyano-substituted lower alkyl group, a phenyl-lower alkyl group which may have lower alkoxy groups as the substituents in the phenyl ring or a group of the formula —CH2RA; X is a halogen atom or a group of the formula —S(O)n-R1) and method for preparing the same. The compound of the formula (1) is a useful compound as an intermediate for synthesis of various pharmaceutical and agricultural chemicals, particularly, as intermediates for antitubercular agents.Type: ApplicationFiled: January 31, 2012Publication date: May 24, 2012Inventors: Fumitaka GOTO, Noriaki Takemura, Tadaaki Otani, Takeshi Hasegawa, Hidetsugu Tsubouchi, Naoto Utsumi, Shigekazu Fujita, Hideaki Kuroda, Takuya Shitsuta, Hirofumi Sasaki
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Patent number: 8163753Abstract: The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (1) in the above formula (1), R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R1 and —(CH2)nR2 may form a spiro ring represented by the formula (30) below, together with the adjacent carbon atom (in the formula below, RRR represents a piperidyl group which may have substituents on the piperidine ring), (30) and R2 represents a benzothiazolyloxy group, quinolyloxy group, pyridyloxy group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.Type: GrantFiled: October 29, 2004Date of Patent: April 24, 2012Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hidetsugu Tsubouchi, Hirofumi Sasaki, Motohiro Itotani, Yoshikazu Haraguchi, Shin Miyamura, Makoto Matsumoto, Hiroyuki Hashizume, Tatsuo Tomishige, Masanori Kawasaki, Kinue Ohguro, Takumi Sumida, Takeshi Hasegawa, Kazuho Tanaka, Isao Takemura
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Patent number: 8129544Abstract: The present invention relates to a 1-substituted-4-nitroimidazole compound represented by the general formula (1) or a salt thereof, (wherein R is a hydrogen atom, a lower alkoxy group-substituted lower alkyl group, a phenyl-lower alkoxy group-substituted lower alkyl group, a cyano-substituted lower alkyl group, a phenyl-lower alkyl group which may have lower alkoxy groups as the substituents in the phenyl ring or a group of the formula —CH2RA; X is a halogen atom or a group of the formula —S(O)n-R1) and method for preparing the same. The compound of the formula (1) is a useful compound as an intermediate for synthesis of various pharmaceutical and agricultural chemicals, particularly, as intermediates for antitubercular agents.Type: GrantFiled: October 1, 2007Date of Patent: March 6, 2012Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Fumitaka Goto, Noriaki Takemura, Tadaaki Otani, Takeshi Hasegawa, Hidetsugu Tsubouchi, Naoto Utsumi, Shigekazu Fujita, Hideaki Kuroda, Takuya Shitsuta, Hirofumi Sasaki
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Publication number: 20100331423Abstract: The present invention provides a disinfectant that contains olanexidine in a concentration sufficient to exhibit an effective bactericidal effect, and that has hardly any side effects such as skin irritation. Specifically, the present invention provides a disinfectant containing an aqueous solution that contains olanexidine and at least an equimolar amount of gluconic acid, and substantially contains neither an acid other than gluconic acid nor a salt of the acid other than gluconic acid.Type: ApplicationFiled: September 10, 2010Publication date: December 30, 2010Applicants: Otsuka Pharmaceutical Co., Ltd., Otsuka Pharmaceutical Factory, Inc.Inventors: Kazuyoshi Miyata, Yasuhide Inoue, Akifumi Hagi, Motoya Kikuchi, Hitoshi Ohno, Kinji Hashimoto, Kinue Ohguro, Tetsuya Sato, Hidetsugu Tsubouchi, Hiroshi Ishikawa, Takashi Okamura, Koushi Iwata
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Patent number: 7829518Abstract: The present invention provides a disinfectant that contains olanexidine in a concentration sufficient to exhibit an effective bactericidal effect, and that has hardly any side effects such as skin irritation. Specifically, the present invention provides a disinfectant containing an aqueous solution that contains olanexidine and at least an equimolar amount of gluconic acid, and substantially contains neither an acid other than gluconic acid nor a salt of the acid other than gluconic acid.Type: GrantFiled: May 25, 2004Date of Patent: November 9, 2010Assignees: Otsuka Pharmaceutical Co., Ltd., Otsuka Pharmaceutical Factory, Inc,Inventors: Kazuyoshi Miyata, Yasuhide Inoue, Akifumi Hagi, Motoya Kikuchi, Hitoshi Ohno, Kinji Hashimoto, Kinue Ohguro, Tetsuya Sato, Hidetsugu Tsubouchi, Hiroshi Ishikawa, Takashi Okamura, Koushi Iwata
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Patent number: 7825080Abstract: The present invention provides a disinfectant that contains olanexidine in a concentration sufficient to exhibit an effective bactericidal effect, and that has hardly any side effects such as skin irritation. Specifically, the present invention provides a disinfectant containing an aqueous solution that contains olanexidine and at least an equimolar amount of gluconic acid, and substantially contains neither an acid other than gluconic acid nor a salt of the acid other than gluconic acid.Type: GrantFiled: October 27, 2006Date of Patent: November 2, 2010Assignees: Otsuka Pharmaceutical Co., Ltd., Otsuka Pharmaceutical Factory, Inc.Inventors: Kazuyoshi Miyata, Yasuhide Inoue, Akifumi Hagi, Motoya Kikuchi, Hitoshi Ohno, Kinji Hashimoto, Kinue Ohguro, Tetsuya Sato, Hidetsugu Tsubouchi, Hiroshi Ishikawa, Takashi Okamura, Koushi Iwata
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Patent number: 7807843Abstract: The present invention relates to a 1-substituted-4-nitroimidazole compound represented by the general formula (1) or a salt thereof, (wherein R is a hydrogen atom, a lower alkoxy group-substituted lower alkyl group, a phenyl-lower alkoxy group-substituted lower alkyl group, a cyano-substituted lower alkyl group, a phenyl-lower alkyl group which may have lower alkoxy groups as the substituents in the phenyl ring or a group of the formula —CH2RA; X is a halogen atom or a group of the formula —S(O)n-R1) and method for preparing the same. The compound of the formula (1) is a useful compound as an intermediate for synthesis of various pharmaceutical and agricultural chemicals, particularly, as intermediates for antitubercular agents.Type: GrantFiled: January 15, 2008Date of Patent: October 5, 2010Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Fumitaka Goto, Noriaki Takemura, Tadaaki Otani, Takeshi Hasegawa, Hidetsugu Tsubouchi, Naoto Utsumi, Shigekazu Fujita, Hideaki Kuroda, Takuya Shitsuta, Hirofumi Sasaki
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Publication number: 20100217005Abstract: The present invention provides a novel intermediate for manufacturing a 2,3-dihydroimidazo[2,1-b]oxazole compound with a high yield and a high purity, and a manufacturing method of the intermediate. The present invention provides an epoxy compound represented by the general formula (2): wherein, R1 represents hydrogen or a lower alkyl group; and R2 represents a piperidyl group represented by the general formula (A1): (wherein, R3 represents a phenoxy group having a halogen-substituted lower alkoxy group substituted on a phenyl group, and the like) and the like; and n represents an integer of 1 to 6, a manufacturing method of the epoxy compound, and a manufacturing method of an oxazole compound using the epoxy compound.Type: ApplicationFiled: May 7, 2008Publication date: August 26, 2010Inventors: Hidetsugu Tsubouchi, Yoshikazu Haraguchi, Satoshi Hayakawa, Naoto Utsumi, Shinichi Taira, Yoshihisa Tanada, Nobuhisa Fujita, Koichi Shinhama, Kimiyoshi Annaka, Takuya Furuta
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Publication number: 20080200689Abstract: The present invention relates to a 1-substituted-4-nitroimidazole compound represented by the general formula (1) or a salt thereof, (wherein R is a hydrogen atom, a lower alkoxy group-substituted lower alkyl group, a phenyl-lower alkoxy group-substituted lower alkyl group, a cyano-substituted lower alkyl group, a phenyl-lower alkyl group which may have lower alkoxy groups as the substituents in the phenyl ring or a group of the formula —CH2RA; X is a halogen atom or a group of the formula —S(O)n-R1) and method for preparing the same. The compound of the formula (1) is a useful compound as an intermediate for synthesis of various pharmaceutical and agricultural chemicals, particularly, as intermediates for antitubercular agents.Type: ApplicationFiled: January 15, 2008Publication date: August 21, 2008Inventors: Fumitaka Goto, Noriaki Takemura, Tadaaki Otani, Takeshi Hasegawa, Hidetsugu Tsubouchi, Naoto Utsumi, Shigekazu Fujita, Hideaki Kuroda, Takuya Shitsuta, Hirofumi Sasaki
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Publication number: 20080119478Abstract: The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (1) in the above formula (1), R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R1 and —(CH2)nR2 may form a spiro ring represented by the formula (30) below, together with the adjacent carbon atom (in the formula below, RRR represents a piperidyl group which may have substituents on the piperidine ring), (30) and R2 represents a benzothiazolyloxy group, quinolyloxy group, pyridyloxy group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.Type: ApplicationFiled: October 29, 2004Publication date: May 22, 2008Inventors: Hidetsugu Tsubouchi, Hirofumi Sasaki, Motohiro Itotani, Yoshikazu Haraguchi, Shin Miyamura, Makoto Matsumoto, Hiroyuki Hashizume, Tatsuo Tomishige, Masanori Kawasaki, Kinue Ohguro, Takumi Sumida, Takeshi Hasegawa, Kazuho Tanaka, Isao Takemura
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Patent number: 7368579Abstract: The present invention relates to a 1-substituted-4-nitroimidazole compound represented by the general formula (1) or a salt thereof, (wherein R is a hydrogen atom, a lower alkoxy group-substituted lower alkyl group, a phenyl-lower alkoxy group-substituted lower alkyl group, a cyano-substituted lower alkyl group, a phenyl-lower alkyl group which may have lower alkoxy groups as the substituents in the phenyl ring or a group of the formula —CH2RA; X is a halogen atom or a group of the formula —S(O)n—R1) and method for preparing the same. The compound of the formula (1) is a useful compound as an intermediate for synthesis of various pharmaceutical and agricultural chemicals, particularly, as intermediates for antitubercular agents.Type: GrantFiled: October 14, 2003Date of Patent: May 6, 2008Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Fumitaka Goto, Noriaki Takemura, Tadaaki Otani, Takeshi Hasegawa, Hidetsugu Tsubouchi, Naoto Utsumi, Shigekazu Fujita, Hideaki Kuroda, Takuya Shitsuta, Hirofumi Sasaki
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Publication number: 20080097107Abstract: The present invention relates to a 1-substituted-4-nitroimidazole compound represented by the general formula (1) or a salt thereof, (wherein R is a hydrogen atom, a lower alkoxy group-substituted lower alkyl group, a phenyl-lower alkoxy group-substituted lower alkyl group, a cyano-substituted lower alkyl group, a phenyl-lower alkyl group which may have lower alkoxy groups as the substituents in the phenyl ring or a group of the formula —CH2RA; X is a halogen atom or a group of the formula —S(O)n-R1) and method for preparing the same. The compound of the formula (1) is a useful compound as an intermediate for synthesis of various pharmaceutical and agricultural chemicals, particularly, as intermediates for antitubercular agents.Type: ApplicationFiled: October 1, 2007Publication date: April 24, 2008Inventors: Fumitaka Goto, Noriaki Takemura, Tadaaki Otani, Takeshi Hasegawa, Hidetsugu Tsubouchi, Naoto Utsumi, Shigekazu Fujita, Hideaki Kuroda, Takuya Shitsuta, Hirofumi Sasaki
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Patent number: 7262212Abstract: The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: wherein R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R2 represents a group —OR3 or the like, and R3 represents a hydrogen atom, C1-C6 alkyl group or the like, or R1 and —(CH2)nR2 may bind to each other together with carbon atoms adjacent thereto through nitrogen atoms so as to form a spiro ring represented by the general formula (H): wherein R41 is hydrogen, C1-C6 alkyl group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.Type: GrantFiled: October 10, 2003Date of Patent: August 28, 2007Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hidetsugu Tsubouchi, Hirofumi Sasaki, Hideaki Kuroda, Motohiro Itotani, Takeshi Hasegawa, Yoshikazu Haraguchi, Takeshi Kuroda, Takayuki Matsuzaki, Kuninori Tai, Makoto Komatsu, Makoto Matsumoto, Hiroyuki Hashizume, Tatsuo Tomishige, Yuji Seike, Masanori Kawasaki, Takumi Sumida, Shin Miyamura
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Publication number: 20070041866Abstract: The present invention provides a disinfectant that contains olanexidine in a concentration sufficient to exhibit an effective bactericidal effect, and that has hardly any side effects such as skin irritation. Specifically, the present invention provides a disinfectant containing an aqueous solution that contains olanexidine and at least an equimolar amount of gluconic acid, and substantially contains neither an acid other than gluconic acid nor a salt of the acid other than gluconic acid.Type: ApplicationFiled: October 27, 2006Publication date: February 22, 2007Inventors: Kazuyoshi Miyata, Yasuhide Inoue, Akifumi Hagi, Motoya Kikuchi, Hitoshi Ohno, Kinji Hashimoto, Kinue Ohguro, Tetsuya Sato, Hidetsugu Tsubouchi, Hiroshi Ishikawa, Takashi Okamura, Koushi Iwata
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Publication number: 20060189500Abstract: The present invention provides a disinfectant that contains olanexidine in a concentration sufficient to exhibit an effective bactericidal effect, and that has hardly any side effects such as skin irritation. Specifically, the present invention provides a disinfectant containing an aqueous solution that contains olanexidine and at least an equimolar amount of gluconic acid, and substantially contains neither an acid other than gluconic acid nor a salt of the acid other than gluconic acid.Type: ApplicationFiled: May 25, 2004Publication date: August 24, 2006Inventors: Kazuyoshi Miyata, Yasuhide Inoue, Akifumi Hagi, Motoya Kikuchi, Hitoshi Ohno, Kinji Hashimoto, Kinue Ohguro, Tetsuya Sato, Hidetsugu Tsubouchi, Hiroshi Ishikawa, Takashi Okamura, Koushi Iwata