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).

  • Publication number: 20070060531
    Abstract: The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl, etc.; one of Q and T represents a group selected from the following: , and the other represents -Z-Ar wherein Z represents —O—, —S—, etc.; Ar represents an optionally substituted C6-10 aryl, etc.; R represents an optionally substituted C3-8 cycloalkyl, an optionally substituted C6-10 aryl, etc., pharmaceutically acceptable salts thereof, and prodrugs thereof, which exhibit an excellent inhibitory activity in human sodium/glucose cotransporter (SGLT) and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates selected from glucose, fructose and mannose (diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, etc.
    Type: Application
    Filed: June 15, 2004
    Publication date: March 15, 2007
    Inventors: Norihiko Kikuchi, Hideki Fujikura, Shigeki Tazawa, Tokuhisa Yamato, Masayuki Isaji
  • Patent number: 7189702
    Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein one of Q and T represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; R1 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkenyl group, a cyclic lower alkyl group, etc.; R2 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkoxy group, a lower alkenyl group, a cyclic lower alkyl group, a cyclic lower alkoxy group, etc., 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: Grant
    Filed: February 22, 2006
    Date of Patent: March 13, 2007
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Toshihiro Nishimura, Nobuhiko Fushimi, Hideki Fujikura, Kenji Katsuno, Yoshimitsu Komatsu, Masayuki Isaji
  • Publication number: 20060247179
    Abstract: 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: Application
    Filed: March 24, 2004
    Publication date: November 2, 2006
    Inventors: Nobuhiko Fushimi, Shigeru Yonekubo, Hideyuki Muranaka, Hiroaki Shiohara, Hirotaka Teranishi, Kazuo Shimizu, Fumiaki Ito, Masayuki Isaji
  • Patent number: 7129381
    Abstract: The present invention relates to glucopyranosyl-oxybenzylbenzene derivatives represented by the general formula: wherein R1 represents a hydrogen atom, a hydroxy group, a substituted or unsubstituted amino group, a carbamoyl group, a substituted or unsubstituted(lower alkyl) group, a substituted or unsubstituted(lower alkoxy) group etc.; R2 represents a hydrogen atom or a lower alkyl group; and R3 represents a substituted or unsubstituted(lower alkyl) group, a substituted or unsubstituted(lower alkoxy) group, a substituted or unsubstituted(lower alkylthio) group etc., or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complication or obesity, pharmaceutical compositions comprising the same and intermediates thereof.
    Type: Grant
    Filed: November 2, 2004
    Date of Patent: October 31, 2006
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Hideki Fujikura, Toshihiro Nishimura, Nobuhiko Fushimi, Kazuya Tatani, Norihiko Kikuchi, Kenji Katsuno, Masayuki Isaji
  • Patent number: 7115575
    Abstract: The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and 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, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.
    Type: Grant
    Filed: July 28, 2005
    Date of Patent: October 3, 2006
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Hideki Fujikura, Toshihiro Nishimura, Kenji Katsuno, Masahiro Hiratochi, Akira Iyobe, Minoru Fujioka, Masayuki Isaji
  • Patent number: 7087579
    Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein one of Q and T represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; R1 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkenyl group, a cyclic lower alkyl group, etc.; R2 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkoxy group, a lower alkenyl group, a cyclic lower alkyl group, a cyclic lower alkoxy group, etc., 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: Grant
    Filed: February 26, 2002
    Date of Patent: August 8, 2006
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Toshihiro Nishimura, Nobuhiko Fushimi, Hideki Fujikura, Kenji Katsuno, Yoshimitsu Komatsu, Masayuki Isaji
  • Patent number: 7084123
    Abstract: 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 thereo
    Type: Grant
    Filed: December 25, 2001
    Date of Patent: August 1, 2006
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Hideki Fujikura, Nobuhiko Fushimi, Toshihiro Nishimura, Takeshi Nakabayashi, Masayuki Isaji
  • Publication number: 20060166899
    Abstract: 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: Application
    Filed: August 7, 2003
    Publication date: July 27, 2006
    Applicant: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Hirotaka Teranishi, Nobuhiko Fushimi, Shigeru Yonekubo, Kazuo Shimizu, Toshihide Shibazaki, Masayuki Isaji
  • Publication number: 20060142209
    Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein one of Q and T represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; R1 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkenyl group, a cyclic lower alkyl group, etc.; R2 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkoxy group, a lower alkenyl group, a cyclic lower alkyl group, a cyclic lower alkoxy group, etc., 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: Application
    Filed: February 22, 2006
    Publication date: June 29, 2006
    Inventors: Toshihiro Nishimura, Nobuhiko Fushimi, Hideki Fujikura, Kenji Katsuno, Yoshimitsu Komatsu, Masayuki Isaji
  • Publication number: 20060128635
    Abstract: 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 selected from the following groups: and the other represents —(CH2)n—Ar wherein Ar represents an optionally substituted C6-10 aryl group or an optionally substituted C1-9 heteroaryl group; and n represents an integral number from 0 to 2, an optionally substituted C1-6 alkoxyl group, an optionally substituted amino group, an optionally substituted C2-9 heterocycloalkyl group or an optionally substituted heterocycle-fused phenyl group; R represents an optionally substituted C3-8 cycloalkyl group, an optionally substituted C6-10 aryl group etc.
    Type: Application
    Filed: September 30, 2003
    Publication date: June 15, 2006
    Inventors: Hideki Fujikura, Norihiko Kikuchi, Shigeki Tazawa, Tokuhisa Yamato, Masayuki Isaji
  • Patent number: 7056892
    Abstract: The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and 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, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.
    Type: Grant
    Filed: July 27, 2005
    Date of Patent: June 6, 2006
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Hideki Fujikura, Toshihiro Nishimura, Kenji Katsuno, Masahiro Hiratochi, Akira Iyobe, Minoru Fujioka, Masayuki Isaji
  • Patent number: 7053060
    Abstract: The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein R1 represents a hydrogen atom, a hydroxy group, a substituted or unsubstituted amino group, a carbamoyl group, a substituted or unsubstituted (lower alkyl) group, a substituted or unsubstituted (lower alkoxy) group etc.; R2 represents a hydrogen atom or a lower alkyl group; and R3 represents a substituted or unsubstituted (lower alkyl) group, a substituted or unsubstituted (lower alkoxy) group, a substituted or unsubstituted (lower alkylthio) group etc., or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complication or obesity, pharmaceutical compositions comprising the same and intermediates thereof.
    Type: Grant
    Filed: November 20, 2001
    Date of Patent: May 30, 2006
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Hideki Fujikura, Toshihiro Nishimura, Nobuhiko Fushimi, Kazuya Tatani, Norihiko Kikuchi, Kenji Katsuno, Masayuki Isaji
  • Patent number: 7045665
    Abstract: The present invention relates to benzylphenol derivatives represented by the general formula: wherein R11 represents a hydrogen atom or a protected hydroxy(lower alkyl) group; and R12 represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a protected hydroxy(lower alkyl) group, a protected hydroxy(lower alkoxy) group, a protected hydroxy(lower alkylthio) group, a lower alkoxy-substituted (lower alkyl) group, a lower alkoxy-substituted (lower alkoxy) group or a lower alkoxy-substituted (lower alkylthio) group; with the proviso that R12 is not a methyl group, an ethyl group, an isopropyl group, a tert-butyl group or a methoxy group when R11 is a hydrogen atom, or a salt thereof, which are used as intermediates for making glucopyranosyloxybenzylbenzene compounds having inhibitory activity in human SGLT2 and are useful in treating diseases associated with hyperglycemia, such as diabetes.
    Type: Grant
    Filed: October 7, 2004
    Date of Patent: May 16, 2006
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Hideki Fujikura, Nobuhiko Fushimi, Toshihiro Nishimura, Kazuya Tatani, Kenji Katsuno, Masahiro Hiratochi, Yoshiki Tokutake, Masayuki Isaji
  • Publication number: 20060094667
    Abstract: 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;.
    Type: Application
    Filed: October 12, 2005
    Publication date: May 4, 2006
    Inventors: Hideki Fujikura, Nobuhiko Fushimi, Toshihiro Nishimura, Takeshi Nakabayashi, Masayuki Isaji
  • Publication number: 20060035840
    Abstract: The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein X1 represents Nor CR1; X2 represents Nor CR2; X3 represents N or CR3; X4 represents N or CR4; and with the proviso that one or two of X1 to X4 represent N; R represents optionally substituted C3-8 cycloalkyl, optionally substituted C6-10 aryl, etc.; R1 to R4 represent H, a halogen atom, etc.) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an excellent inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like, pharmaceutical compositions comprising the same, and medicinal uses thereof.
    Type: Application
    Filed: December 19, 2003
    Publication date: February 16, 2006
    Inventors: Hideki Fujikura, Toshihiro Nishimura, Kenji Katsuno, Masayuki Isaji
  • Publication number: 20060035847
    Abstract: 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 there
    Type: Application
    Filed: October 12, 2005
    Publication date: February 16, 2006
    Inventors: Hideki Fujikura, Nobuhiko Fushimi, Toshihiro Nishimura, Takeshi Nakabayashi, Masayuki Isaji
  • Publication number: 20060025352
    Abstract: 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;.
    Type: Application
    Filed: October 12, 2005
    Publication date: February 2, 2006
    Inventors: Hideki Fujikura, Nobuhiko Fushimi, Toshihiro Nishimura, Takeshi Nakabayashi, Masayuki Isaji
  • Publication number: 20050272669
    Abstract: 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: Application
    Filed: August 21, 2003
    Publication date: December 8, 2005
    Inventors: Nobuhiko Fushimi, Kazuo Shimizu, Shigeru Yonekubo, Hirotaka Teranishi, Masaki Tomae, Masayuki Isaji
  • Patent number: 6972283
    Abstract: The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and 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, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.
    Type: Grant
    Filed: January 20, 2004
    Date of Patent: December 6, 2005
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Hideki Fujikura, Toshihiro Nishimura, Kenji Katsuno, Masahiro Hiratochi, Akira Iyobe, Minoru Fujioka, Masayuki Isaji
  • Publication number: 20050261206
    Abstract: The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and 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, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.
    Type: Application
    Filed: July 28, 2005
    Publication date: November 24, 2005
    Inventors: Hideki Fujikura, Toshihiro Nishimura, Kenji Katsuno, Masahiro Hiratochi, Akira Iyobe, Minoru Fujioka, Masayuki Isaji