Patents by Inventor Masayuki Isaji
Masayuki Isaji 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: 7547680Abstract: The present invention provides benzimidazole derivatives represented by the following formula (I) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an inhibitory activity on sodium-dependent nucleoside transporter 2 and are useful for a disease associated with an abnormality of plasma uric acid level. The compounds of the present invention are useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; R1 and R2 are H, a halogen atom, cyano group, optionally substituted alkyl group, optionally substituted aryl group or the like; R3 is H, a halogen atom, optionally substituted alkyl group or the like; R4 and R5 are H, a halogen atom, OH or the like; and R6 and RX are H or OH: RY is F or OH.Type: GrantFiled: June 23, 2006Date of Patent: June 16, 2009Assignee: Kissei Pharmaceuticals, Co., Ltd.Inventors: Norihiko Kikuchi, Yoshinori Nonaka, Kazuya Tatani, Masahiro Hiratochi, Yu Kuramochi, Masayuki Isaji, Kazuo Shimizu, Takashi Miyagi
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Patent number: 7541341Abstract: The present invention provides glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein P represents a hydrogen atom or a group forming a prodrug; R1 represents a hydrogen atom, an optionally substituted amino group, a carbamoyl group, an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, etc.; R2 represents a hydrogen atom or a lower alkyl group; and R3 represents an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, an optionally substituted lower alkylthio group, etc., which have an improved oral absorption, and exert an inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, or pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.Type: GrantFiled: February 13, 2002Date of Patent: June 2, 2009Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Nobuhiko Fushimi, Kazuya Tatani, Hideki Fujikura, Toshihiro Nishimura, Minoru Fujioka, Takeshi Nakabayashi, Masayuki Isaji
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Publication number: 20090093419Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug; one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereofType: ApplicationFiled: July 9, 2008Publication date: April 9, 2009Applicant: Kissei Pharmaceutical Co. Ltd.Inventors: Hideki Fujikura, Nobuhiko Fushimi, Toshihiro Nishimura, Takeshi Nakabayashi, Masayuki Isaji
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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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Patent number: 7465713Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug; one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereType: GrantFiled: October 12, 2005Date of Patent: December 16, 2008Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hideki Fujikura, Nobuhiko Fushimi, Toshihiro Nishimura, Takeshi Nakabayashi, Masayuki Isaji
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Patent number: 7429568Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug; one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereoType: GrantFiled: October 12, 2005Date of Patent: September 30, 2008Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hideki Fujikura, Nobuhiko Fushimi, Toshihiro Nishimura, Takeshi Nakabayashi, 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: 7393838Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug; one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereType: GrantFiled: October 12, 2005Date of Patent: July 1, 2008Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hideki Fujikura, Nobuhiko Fushimi, Toshihiro Nishimura, Takeshi Nakabayashi, 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: 20080045466Abstract: The present invention provides pharmaceutical compositions useful as agents for the inhibition of progression of diseases associated with abnormal accumulation of liver lipids. In particular, the pharmaceutical compositions of the present invention which comprise as an active ingredient a sodium/glucose co-transporter 2 inhibitor are highly suitable as an agent for the inhibition of progression of not only common fatty liver but also non-alcholic fatty liver disease (NAFL), non-alcholic steatohepatitis (NASH), hypernutritive fatty liver, diabetic fatty liver, alcholic fatty liver disease toxic fatty liver or the like.Type: ApplicationFiled: July 19, 2005Publication date: February 21, 2008Inventors: Kenji Katsuno, Yoshikazu Fujimori, Masayuki Isaji
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Publication number: 20080038242Abstract: The present invention provides benzimidazole derivatives represented by the following formula (I) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an inhibitory activity on sodium-dependent nucleoside transporter 2 and are useful for a disease associated with an abnormality of plasma uric acid level. The compounds of the present invention are useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; R1 and R2 are H, a halogen atom, cyano group, optionally substituted alkyl group, optionally substituted aryl group or the like; R3 is H, a halogen atom, optionally substituted alkyl group or the like; R4 and R5 are H, a halogen atom, OH or the like; and R6 and RX are H or OH: RY is F or OH.Type: ApplicationFiled: June 23, 2006Publication date: February 14, 2008Inventors: Norhiko Kikuchi, Yoshinori Nonaka, Kazuya Tatani, Masahiro Hiratochi, Yu Kuramochi, Masayuki Isaji, Kazuo Shimizu, Takashi Miyagi
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Patent number: 7294618Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1, R2 and R3 represent a hydrogen atom or a halogen atom; R4 represents a lower alkyl group or a halo(lower alkyl) group; and R5 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, etc., a pharmaceutically acceptable salt thereof or a prodrug thereof., which exert an excellent inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutically acceptable salts thereof or prodrugs thereof, production intermediates thereof and pharmaceutical uses thereof.Type: GrantFiled: February 26, 2002Date of Patent: November 13, 2007Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Nobuhiko Fushimi, Hideki Fujikura, Toshihiro Nishimura, Kenji Katsuno, Masayuki Isaji
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Patent number: 7271153Abstract: The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein X1 and X3 independently represent N or CH; X2 represents N or CR2; X4 represents N or CR3; and with the proviso that one or two of X1, X2, X3 and X4 represent N; R1 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkoxy-substituted (lower alkyl) group, a lower alkoxy-substituted (lower alkoxy) group, a lower alkoxy(lower alkoxy)-substituted (lower alkyl) group, a cyclic lower alkyl group, a halo(lower alkyl) group or a group represented by the general formula: HO-A- wherein A represents a lower alkylene group, a lower alkyleneoxy group or a lower alkylenethio group; R2 represents a hydrogen atom, a halogen atom, a lower alkyl group, a cyclic lower alkyl group, a lower alkoxy group, an amino group, a (lower acyl)amino group, a mono(lower alkyl)amino group or a di(lower alkyl)amino group; and R3 represents a hydrogen aType: GrantFiled: June 17, 2002Date of Patent: September 18, 2007Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Toshihiro Nishimura, Hideki Fujikura, Nobuhiko Fushimi, Kazuya Tatani, Kenji Katsuno, Masayuki Isaji
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Publication number: 20070197449Abstract: The present invention provides nitrogen-containing fused cyclic 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 one of R1 and R4 represents a group represented by the following general formula (S) (in which R5 and R6 represent H, OH, a halogen atom, etc.; Q represents an alkylene group etc.; and ring A represents an aryl group etc.), and the other represents H, OH, an amino group, etc.; R2 and R3 represent H, OH, an amino group, a halogen atom, and an optionally substituted alkyl group, etc.; A1 represents O, S, etc.Type: ApplicationFiled: March 3, 2005Publication date: August 23, 2007Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Nobuhiko Fushimi, Hideki Fujikura, Masayuki Isaji
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Publication number: 20070197450Abstract: The present invention provides fused heterocyclic derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an 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 to R4 represent H, OH, an amino group, etc.; R5 and R6 represent H, OH, a halogen atom, an option ally substituted alkyl group, etc.; Q represents alkylene, alkenylene, etc.; ring A represents an aryl group or a heteroaryl group; the following ring (R1) represents a group represented by the following ring (R2); G represents a group represented by the following general formula (G-1) or (G-2) (E1 represents H, F or OH; and E represents H, F, a methyl group, etc.), and pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.Type: ApplicationFiled: March 3, 2005Publication date: August 23, 2007Inventors: Nobuhiko Fushimi, Masayuki Isaji, Hideki Fujikura
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Publication number: 20070191289Abstract: 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: ApplicationFiled: March 3, 2005Publication date: August 16, 2007Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Nobuhiko Fushimi, Hirotaka Teranishi, Kazuo Shimizu, Shigeru Yoneku, Fumiaki Ito, Masayuki Isaji
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Publication number: 20070185197Abstract: The present invention provides phenol derivatives represented by the following general formula or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an 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, obesity or the like, and pharmaceutical compositions comprising the same, and pharmaceutical uses thereof. In the chemical structure, R1 and R2 represent H, OH, NH2, etc.; R3and R4represent H, OH, a halogen atom, an optionally substituted alkyl group, etc.; ring A represents an aryl group or a heteroaryl group; G represents a group represented by the following general formula (G); E1 represents H or F; and E2 represents H, F, or a methyl group, etc.Type: ApplicationFiled: March 30, 2005Publication date: August 9, 2007Inventors: Hideki Fujikura, Nobuhiko Fushimi, Masayuki Isaji
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Patent number: 7217697Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 is a hydrogen atom or a hydroxyalkyl group; one of Q and T is a group represented by the general formula; the other is an optionally substituted alkyl group or a cycloalkyl group; and R2 is a halogen atom, a hydroxy group, an optionally substituted alkyl group, an optionally substituted alkoxy group, an alkylthio group, a group of the general formula: -A-R3 wherein A is a single bond, an oxygen atom, a methylene group, an ethylene group, —OCH2— or —CH2O—; and R3 is a cycloalkyl group, a heterocycloalkyl group, an optionally substituted aryl group, an optionally substituted tiazolyl group or an optionally substituted pyridyl group, pharmaceutically acceptable salts thereof or prodrugs thereof, which exert an excellent inhibitory activity in human SGLT1, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabeticType: GrantFiled: May 27, 2002Date of Patent: May 15, 2007Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hiroaki Shiohara, Hideki Fujikura, Nobuhiko Fushimi, Fumiaki Ito, Masayuki Isaji