Patents by Inventor Shigeru Yonekubo
Shigeru Yonekubo 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: 8324176Abstract: The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents an optionally substituted C1-6 alkylene group etc.; Z represents —RB, —CORC etc. in which RB represents an optionally substituted C1-6 alkyl group etc.; and RC represents an optionally substituted C1-6 alkyl group etc.; R4 represents H, an optionally substituted C1-6 alkyl group etc.; and R3, R5 and R6 represent H, a halogen atom etc.Type: GrantFiled: April 9, 2009Date of Patent: December 4, 2012Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Nobuhiko Fushimi, Kazuo Shimizu, Shigeru Yonekubo, Hirotaka Teranishi, Masaki Tomae, Masayuki Isaji
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Patent number: 8217069Abstract: [Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, —OW1, —SW1, —COW2, —NW3W4, —SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, —CO—Y, —SO2—Y, —S-(alkylene)-Y, —O-(alkylene)-Y, —SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.Type: GrantFiled: April 16, 2008Date of Patent: July 10, 2012Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Shigeru Yonekubo, Takashi Miyagi, Kohsuke Ohno, Mikie Kambara, Nobuhiko Fushimi
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Patent number: 7998975Abstract: The present invention provides nitrogen-containing fused-ring derivatives represented by the following general formula, or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, in the formula R1 represent H, an optionally substituted alkyl group, an alkenyl group, etc.; R2 represent H, a halogen atom or an alkyl group; R3 and R4 represent H, OH, a halogen atom, an optionally substituted alkyl group, etc.; Y represents CH or N; Q represents alkylene, alkenylene, etc.; ring A represents an aryl group or a heteroaryl group; G represents a group represented by the following general formula (G-1) or (G-2) (in which E1 represents H, F or OH; and E2 represents H, F, a methyl group, etc.Type: GrantFiled: February 15, 2008Date of Patent: August 16, 2011Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Nobuhiko Fushimi, Hirotaka Teranishi, Kazuo Shimizu, Shigeru Yonekubo, Fumiaki Ito, Masayuki Isaji
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Patent number: 7750145Abstract: A compound having an SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity, etc. It is a 1-substituted-3-(?-D-glycopyranosyl) nitrogen-containing heterocyclic compound represented by the general formula (I), a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or a solvate thereof; an SGLT inhibitor containing the same; a pharmaceutical composition containing the same and a combination pharmacy of them. In the formula, A represents an alkylene group or alkenylene group; B represents a single bond, —O—, —S— or —NH—; C represents an optionally substituted aryl or heteroaryl group; Q independently represents a carbon atom which a hydrogen atom or a substituent binds to, or a nitrogen atom.Type: GrantFiled: November 17, 2005Date of Patent: July 6, 2010Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Shigeru Yonekubo, Nobuhiko Fushimi
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Patent number: 7749972Abstract: The present invention provides a compound having an SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity or the like. It is a 1-substituted-7-(?-D-glycopyranosyloxy)(aza)-indole compound represented by the general formula (I), a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof: wherein R1 represents a halogen atom or the like; n represents j an integer number from 0 to 3; R2 represents a hydrogen atom or the like; X represents a carbon atom which a hydrogen atom or the like binds to, or a nitrogen atom; Q represents an alkylene group or an alkenylene group each of which may have an oxygen atom or a sulfur atom in the chain; and A represents an aryl or heteroaryl group which may have a substituent.Type: GrantFiled: February 14, 2006Date of Patent: July 6, 2010Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Nobuhiko Fushimi, Shigeru Yonekubo, Kohsuke Ohno
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Publication number: 20100130514Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides fused heterocyclic derivatives represented by the following general formula (I), pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A is 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; RA is halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl, etc.; ring B is aryl or heteroaryl; RB is halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl, etc.; E1 and E2 are oxygen atom, etc.; U is single bond or alkylene; X is a group represented by Y, —O-(alkylene)-Y or —O—Z (in which Y is Z or amino substituted by Z, etc.; Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.Type: ApplicationFiled: April 16, 2008Publication date: May 27, 2010Applicant: Kissei Pharmaceutical Co., Ltd.Inventors: Takashi Miyagi, Shigeru Yonekubo, Kohsuke Ohno, Mikie Kambara, Nobuhiko Fushimi
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Publication number: 20100112090Abstract: [Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, —OW1, —SW1, —COW2, —NW3W4, —SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, —CO—Y, —SO2—Y, —S-(alkylene)-Y, —O-(alkylene)-Y, —SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.Type: ApplicationFiled: April 16, 2008Publication date: May 6, 2010Applicant: KISSEI PHARMACEUTICAL CO., LTDInventors: Shigeru Yonekubo, Takashi Miyagi, Kohsuke Ohno, Mikie Kambara, Nobuhiko Fushimi
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Patent number: 7655632Abstract: The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents a single bond, a C1-6 alkylene group etc.; Z represents CO or SO2; R4 and R5 represent H, an optionally substituted C1-6 alkyl group etc.; and R3, R6 and R7 represent H, a halogen atom etc.Type: GrantFiled: April 17, 2008Date of Patent: February 2, 2010Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hirotaka Teranishi, Nobuhiko Fushimi, Shigeru Yonekubo, Kazuo Shimizu, Toshihide Shibazaki, Masayuki Isaji
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Patent number: 7635684Abstract: The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents an optionally substituted C1-6 alkylene group etc.; Z represents —RB, —CORC etc. in which RB represents an optionally substituted C1-6 alkyl group etc.; and RC represents an optionally substituted C1-6 alkyl group etc.; R4 represents H, an optionally substituted C1-6 alkyl group etc.; and R3, R5 and R6 represent H, a halogen atom etc.Type: GrantFiled: August 21, 2003Date of Patent: December 22, 2009Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Nobuhiko Fushimi, Kazuo Shimizu, Shigeru Yonekubo, Hirotaka Teranishi, Masaki Tomae, Masayuki Isaji
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Publication number: 20090203633Abstract: The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents an optionally substituted C1-6 alkylene group etc.; Z represents —RB, —CORC etc. in which RB represents an optionally substituted C1-6 alkyl group etc.; and RC represents an optionally substituted C1-6 alkyl group etc.; R4 represents H, an optionally substituted C1-6 alkyl group etc.; and R3, R5 and R6 represent H, a halogen atom etc.Type: ApplicationFiled: April 9, 2009Publication date: August 13, 2009Applicant: KISSEI PHARMACEUTICAL CO., LTDInventors: Nobuhiko Fushimi, Kazuo Shimizu, Shigeru Yonekubo, Hirotaka Teranishi, Masaki Tomae
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Patent number: 7566699Abstract: The present invention provides fused heterocyclic derivatives represented by the general formula: wherein R1 represents H, halogen, OH, etc.; R2 represents H, halogen or an alkyl group; R3 and R4 represent H, OH, halogen, etc.; Q represents alkylene, etc.; ring A represents aryl or heteroaryl; and G represents or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.Type: GrantFiled: March 24, 2004Date of Patent: July 28, 2009Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Nobuhiko Fushimi, Shigeru Yonekubo, Hideyuki Muranaka, Hiroaki Shiohara, Hirotaka Teranishi, Kazuo Shimizu, Fumiaki Ito, Masayuki Isaji
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Publication number: 20090074738Abstract: A compound having an SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity, etc. It is a 1-substituted-3-(?-D-glycopyranosyl) nitrogen-containing heterocyclic compound represented by the general formula (I), a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or a solvate thereof; an SGLT inhibitor containing the same; a pharmaceutical composition containing the same and a combination pharmacy of them. In the formula, A represents an alkylene group or alkenylene group; B represents a single bond, —O—, —S— or —NH—; C represents an optionally substituted aryl or heteroaryl group; Q independently represents a carbon atom which a hydrogen atom or a substituent binds to, or a nitrogen atom.Type: ApplicationFiled: November 17, 2005Publication date: March 19, 2009Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Shigeru Yonekubo, Nobuhiko Fushimi
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Publication number: 20090054356Abstract: [Objective] The present invention provides a compound having an SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity or the like. [Means to Solve the Problem] It is a 1-substituted-7-(?-D-glycopyranosyloxy)(aza)-indole compound represented by the general formula (I), a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof: wherein R1 represents a halogen atom or the like; n represents j an integer number from 0 to 3; R2 represents a hydrogen atom or the like; X represents a carbon atom which a hydrogen atom or the like binds to, or a nitrogen atom; Q represents an alkylene group or an alkenylene group each of which may have an oxygen atom or a sulfur atom in the chain; and A represents an aryl or heteroaryl group which may have a substituent.Type: ApplicationFiled: February 14, 2006Publication date: February 26, 2009Applicant: Kissei Pharmaceutical Co., Ltd.Inventors: Nobuhiko Fushimi, Shigeru Yonekubo, Kohsuke Ohno
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Publication number: 20080312153Abstract: The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents a single bond, a C1-6 alkylene group etc.; Z represents CO or SO2; R4 and R5 represent H, an optionally substituted C1-6 alkyl group etc.; and R3, R6 and R7 represent H, a halogen atom etc.Type: ApplicationFiled: April 17, 2008Publication date: December 18, 2008Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Hirotaka Teranishi, Nobuhiko Fushimi, Shigeru Yonekubo, Kazuo Shimizu, Toshihide Shibazaki, Masayuki Isaji
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Publication number: 20080188426Abstract: The present invention provides nitrogen-containing fused-ring derivatives represented by the following general formula, or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, in the formula R1 represent H, an optionally substituted alkyl group, an alkenyl group, etc.; R2 represent H, a halogen atom or an alkyl group; R3 and R4 represent H, OH, a halogen atom, an optionally substituted alkyl group, etc.; Y represents CH or N; Q represents alkylene, alkenylene, etc.; ring A represents an aryl group or a heteroaryl group; G represents a group represented by the following general formula (G-1) or (G-2) (in which E1 represents H, F or OH; and E2 represents H, F, a methyl group, etc.Type: ApplicationFiled: February 15, 2008Publication date: August 7, 2008Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Nobuhiko FUSHIMI, Hirotaka Teranishi, Kazuo Shimizu, Shigeru Yonekubo, Fumiaki Ito, Masayuki ISAJI
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Patent number: 7375087Abstract: The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents a single bond, a C1-6 alkylene group etc.; Z represents CO or SO2; R4 and R5 represent H, an optionally substituted C1-6 alkyl group etc.; and R3, R6 and R7 represent H, a halogen atom etc.Type: GrantFiled: August 7, 2003Date of Patent: May 20, 2008Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hirotaka Teranishi, Nobuhiko Fushimi, Shigeru Yonekubo, Kazuo Shimizu, Toshihide Shibazaki, Masayuki Isaji
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Patent number: 7375113Abstract: The present invention provides nitrogen-containing fused-ring derivatives represented by the following general formula, or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, in the formula R1 represent H, an optionally substituted alkyl group, analkenyl group, etc.; R2 represent H, a halogen atom or an alkyl group; R3 and R4 represent H, OH, a halogen atom, an optionally substituted alkyl group, etc.; Y represents CH or N; Q represents alkylene, alkenylene, etc.; ring A represents an aryl group or a heteroaryl group; G represents a group represented by the following general formula (G-1) or (G-2) (in which E1 represents H, F or OH; and E2 represents H, F, a methyl group, etc.Type: GrantFiled: March 3, 2005Date of Patent: May 20, 2008Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Nobuhiko Fushimi, Hirotaka Teranishi, Kazuo Shimizu, Shigeru Yonekubo, Fumiaki Ito, Masayuki Isaji
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Patent number: 7371730Abstract: The present invention provides crystals of 2-(4-methoxybenzyl)phenyl 6-O-ethoxycarbonyl-?-D-glucopyranoside, pharmaceutical compositions containing the same and their uses, which exhibit excellent SGLT2 inhibitory activities, and are useful for treating or preventing diseases associated with hyperglycemia.Type: GrantFiled: March 4, 2003Date of Patent: May 13, 2008Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Akira Iyobe, Hirotaka Teranishi, Kazuya Tatani, Shigeru Yonekubo, Masayuki Isaji
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Publication number: 20060247179Abstract: The present invention provides fused heterocyclic derivatives represented by the general formula: wherein R1 represents H, halogen, OH, etc.; R2 represents H, halogen or an alkyl group; R3 and R4 represent H, OH, halogen, etc.; Q represents alkylene, etc.; ring A represents aryl or heteroaryl; and G represents , or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.Type: ApplicationFiled: March 24, 2004Publication date: November 2, 2006Inventors: Nobuhiko Fushimi, Shigeru Yonekubo, Hideyuki Muranaka, Hiroaki Shiohara, Hirotaka Teranishi, Kazuo Shimizu, Fumiaki Ito, Masayuki Isaji
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Publication number: 20060166899Abstract: The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents a single bond, a C1-6 alkylene group etc.; Z represents CO or SO2; R4 and R5 represent H, an optionally substituted C1-6 alkyl group etc.; and R3, R6 and R7 represent H, a halogen atom etc.Type: ApplicationFiled: August 7, 2003Publication date: July 27, 2006Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Hirotaka Teranishi, Nobuhiko Fushimi, Shigeru Yonekubo, Kazuo Shimizu, Toshihide Shibazaki, Masayuki Isaji