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    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof
    1.
    发明授权
    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof 失效
    吡喃葡萄糖氧基苄基苯衍生物，含有它们的药物组合物及其制备中间体

    公开(公告)号：US07053060B2

    公开(公告)日：2006-05-30

    申请号：US10432905

    申请日：2001-11-20

    申请人： Hideki Fujikura ,  Toshihiro Nishimura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Norihiko Kikuchi ,  Kenji Katsuno ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Toshihiro Nishimura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Norihiko Kikuchi ,  Kenji Katsuno ,  Masayuki Isaji

    IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H15/00 ,  C07H17/00

    CPC分类号： C07H15/203

    摘要： 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.

    摘要翻译： 本发明涉及由以下通式表示的吡喃葡萄糖氧基苄基苯衍生物：其中R 1表示氢原子，羟基，取代或未取代的氨基，氨基甲酰基，取代或未取代的（低级烷基 ）基团，取代或未取代的（低级烷氧基）基团等; R 2表示氢原子或低级烷基; 和R 3表示取代或未取代的（低级烷基）基团，取代或未取代的（低级烷氧基）基团，取代或未取代的（低级烷硫基）等，或其药学上可接受的盐，其中 在人SGLT2中具有抑制活性，并且可用作预防或治疗与高血糖相关的疾病如糖尿病，糖尿病并发症或肥胖症的药剂，包含其的药物组合物及其中间体。

    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof
    2.
    发明申请
    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof 失效
    吡喃葡萄糖氧基苄基苯衍生物，含有它们的药物组合物及其制备中间体

    公开(公告)号：US20050059614A1

    公开(公告)日：2005-03-17

    申请号：US10978413

    申请日：2004-11-02

    申请人： Hideki Fujikura ,  Toshihiro Nishimura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Norihiko Kikuchi ,  Kenji Katsuno ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Toshihiro Nishimura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Norihiko Kikuchi ,  Kenji Katsuno ,  Masayuki Isaji

    IPC分类号： A61P3/04 ,  A61P3/10 ,  A61P43/00 ,  C07H15/203 ,  A61K31/70 ,  C07H5/04 ,  C07H5/06

    CPC分类号： C07H15/203

    摘要： 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.

    摘要翻译： 本发明涉及由以下通式表示的吡喃葡萄糖基 - 氧苄基苯衍生物：其中R 1表示氢原子，羟基，取代或未取代的氨基，氨基甲酰基，取代或未取代的（低级烷基） 取代或未取代的（低级烷氧基）等。 R 2表示氢原子或低级烷基; 和R 3表示具有抑制活性的取代或未取代的（低级烷基）基团，取代或未取代的（低级烷氧基）基团，取代或未取代的（低级烷硫基）等，或其药学上可接受的盐 人SGLT2，并且可用作预防或治疗与高血糖相关的疾病（如糖尿病，糖尿病并发症或肥胖症）的药剂，包含其的药物组合物及其中间体。

    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates for the preparation of the derivatives
    3.
    发明授权
    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates for the preparation of the derivatives 有权
    吡喃葡萄糖氧基苄基苯衍生物，含有该衍生物的药物组合物和用于制备衍生物的中间体

    公开(公告)号：US07045665B2

    公开(公告)日：2006-05-16

    申请号：US10959505

    申请日：2004-10-07

    申请人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Kazuya Tatani ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Yoshiki Tokutake ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Kazuya Tatani ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Yoshiki Tokutake ,  Masayuki Isaji

    IPC分类号： C07C39/12 ,  C07C27/10 ,  C07C33/18

    CPC分类号： C07H15/203

    摘要： 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.

    摘要翻译： 本发明涉及由以下通式表示的苄基酚衍生物：其中R 11表示氢原子或被保护的羟基（低级烷基）基团; R 12表示低级烷基，低级烷氧基，低级烷硫基，被保护的羟基（低级烷基），被保护的羟基（低级烷氧基），被保护的羟基（低级烷硫基 ）基团，低级烷氧基取代的（低级烷基）基团，低级烷氧基取代的（低级烷氧基基团）或低级烷氧基取代的（低级烷硫基）基团; 条件是当R 11是氢原子时，R 12不是甲基，乙基，异丙基，叔丁基或甲氧基 或其盐，其用作制备在人SGLT2中具有抑制活性的吡喃葡萄糖氧基苄基苯化合物的中间体，并且可用于治疗与高血糖相关的疾病如糖尿病。

    Nitrogenous heterocyclic derivative, medicinal composition containing the same, medical use thereof, and intermediate therefor
    6.
    发明申请
    Nitrogenous heterocyclic derivative, medicinal composition containing the same, medical use thereof, and intermediate therefor 失效
    含氮杂环衍生物，含有它们的药物组合物，其医疗用途及其中间体

    公开(公告)号：US20050049203A1

    公开(公告)日：2005-03-03

    申请号：US10481013

    申请日：2002-06-17

    申请人： Toshihiro Nishimura ,  Hideki Fujikura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Kenji Katsuno ,  Masayuki Isaji

    发明人： Toshihiro Nishimura ,  Hideki Fujikura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Kenji Katsuno ,  Masayuki Isaji

    IPC分类号： A61P3/04 ,  A61P3/10 ,  A61P43/00 ,  C07H17/02 ,  A61K31/7052

    CPC分类号： C07H17/02 ,  Y02P20/55 ,  Y10S514/866 ,  Y10S514/909

    摘要： 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 atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, or prodrugs thereof which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses and production intermediates thereof.

    摘要翻译： 本发明提供由以下通式表示的含氮杂环衍生物：其中X 1和X 3独立地表示N或CH; X 2表示N或CR 2; X 4表示N或CR 3; 并且条件是X 1，X 2，X 3和X 4中的一个或两个表示N; R 1表示氢原子，卤素原子，低级烷基，低级烷氧基，低级烷硫基，低级烷氧基取代的（低级烷基），低级烷氧基取代的（低级烷氧基） 低级烷氧基（低级烷氧基） - 取代（低级烷基）基团，环状低级烷基，卤代（低级烷基）基团或由通式HO-A表示的基团：其中A表示低级亚烷基， 低级亚烷基氧基或低级亚烷基硫基; R 2表示氢原子，卤素原子，低级烷基，环状低级烷基，低级烷氧基，氨基，（低级酰基）氨基，单（低级烷基）氨基或 二（低级烷基）氨基; R 3表示可用作预防或治疗与糖尿病，糖尿病并发症或肥胖症等高血糖症相关疾病的药剂的氢原子或低级烷基或其药学上可接受的盐或其前体药物，药物 含有它们的组合物，及其制药用途和生产中间体。

    Glucopyranosyloxy benzylbenzene derivatives, medicinal compositions containing the same and intermediates for the preparation of the derivatives
    7.
    发明授权
    Glucopyranosyloxy benzylbenzene derivatives, medicinal compositions containing the same and intermediates for the preparation of the derivatives 有权
    吡喃葡萄糖氧基苄基苯衍生物，含有该衍生物的药物组合物和用于制备衍生物的中间体

    公开(公告)号：US07465712B2

    公开(公告)日：2008-12-16

    申请号：US10221843

    申请日：2001-03-15

    申请人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Kazuya Tatani

    发明人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Kazuya Tatani

    IPC分类号： A01N43/04 ,  A61K31/70

    CPC分类号： C07H15/203

    摘要： The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a hydroxy(lower alkyl) group; and R2 represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a hydroxy(lower alkyl) group, a hydroxy(lower alkoxy) group, a hydroxy(lower alkylthio) group etc., and salts thereof, which have an excellent inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, obesity etc., and intermediates thereof.

    摘要翻译： 本发明涉及由以下通式表示的吡喃葡萄糖氧基苄基苯衍生物：其中R1表示氢原子或羟基（低级烷基）; 和R2表示低级烷基，低级烷氧基，低级烷硫基，羟基（低级烷基），羟基（低级烷氧基），羟基（低级烷硫基） 在人SGLT2中具有优异的抑制活性，可用作预防或治疗糖尿病，肥胖症等及其中间体。

    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof
    8.
    发明申请
    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof 审中-公开
    吡喃葡萄糖氧基苄基苯衍生物，含有它们的药物组合物及其制备中间体

    公开(公告)号：US20050113315A1

    公开(公告)日：2005-05-26

    申请号：US10978331

    申请日：2004-11-02

    申请人： Hideki Fujikura ,  Toshihiro Nishimura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Norihiko Kikuchi ,  Kenji Katsuno ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Toshihiro Nishimura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Norihiko Kikuchi ,  Kenji Katsuno ,  Masayuki Isaji

    IPC分类号： A61P3/04 ,  A61P3/10 ,  A61P43/00 ,  C07H15/203 ,  A61K31/704 ,  C07H5/04

    CPC分类号： C07H15/203

    摘要： 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.

    摘要翻译： 本发明涉及由以下通式表示的吡喃葡萄糖氧基苄基苯衍生物：其中R 1表示氢原子，羟基，取代或未取代的氨基，氨基甲酰基，取代或未取代的（低级烷基 ）基团，取代或未取代的（低级烷氧基）基团等; R 2表示氢原子或低级烷基; 和R 3表示取代或未取代的（低级烷基）基团，取代或未取代的（低级烷氧基）基团，取代或未取代的（低级烷硫基）等，或其药学上可接受的盐，其中 在人SGLT2中具有抑制活性，并且可用作预防或治疗与高血糖相关的疾病如糖尿病，糖尿病并发症或肥胖症的药剂，包含其的药物组合物及其中间体。

    Glucopyranosyloxybenzylbenzene derivatives and medicinal use thereof
    9.
    发明授权
    Glucopyranosyloxybenzylbenzene derivatives and medicinal use thereof 有权
    吡喃葡萄糖氧基苄基苯衍生物及其医药用途

    公开(公告)号：US07541341B2

    公开(公告)日：2009-06-02

    申请号：US10467823

    申请日：2002-02-13

    申请人： Nobuhiko Fushimi ,  Kazuya Tatani ,  Hideki Fujikura ,  Toshihiro Nishimura ,  Minoru Fujioka ,  Takeshi Nakabayashi ,  Masayuki Isaji

    发明人： Nobuhiko Fushimi ,  Kazuya Tatani ,  Hideki Fujikura ,  Toshihiro Nishimura ,  Minoru Fujioka ,  Takeshi Nakabayashi ,  Masayuki Isaji

    IPC分类号： A61K31/70 ,  C07H15/00 ,  C07H17/00

    CPC分类号： C07H15/203

    摘要： 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.

    摘要翻译： 本发明提供由以下通式表示的吡喃葡萄糖氧基苄基苯衍生物：其中P表示氢原子或形成前药的基团; R1表示氢原子，任选取代的氨基，氨基甲酰基，任选取代的低级烷基，任选取代的低级烷氧基等; R2表示氢原子或低级烷基; R3代表任意取代的低级烷基，任意取代的低级烷氧基，任意取代的低级烷硫基等，它们具有改善的口服吸收，并且在人SGLT2中具有抑制活性，因此可用作 预防或治疗与糖尿病，糖尿病并发症或肥胖症等高血糖相关的疾病或其药学上可接受的盐及其药学用途。

    Nitrogenous heterocyclic derivatives, medicinal compositions containing the same, medicinal uses thereof, and intermediates therefor
    10.
    发明授权
    Nitrogenous heterocyclic derivatives, medicinal compositions containing the same, medicinal uses thereof, and intermediates therefor 失效
    含氮杂环衍生物，含有它们的药物组合物，其医药用途及其中间体

    公开(公告)号：US07271153B2

    公开(公告)日：2007-09-18

    申请号：US10481013

    申请日：2002-06-17

    申请人： Toshihiro Nishimura ,  Hideki Fujikura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Kenji Katsuno ,  Masayuki Isaji

    发明人： Toshihiro Nishimura ,  Hideki Fujikura ,  Nobuhiko Fushimi ,  Kazuya Tatani ,  Kenji Katsuno ,  Masayuki Isaji

    IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H15/24

    CPC分类号： C07H17/02 ,  Y02P20/55 ,  Y10S514/866 ,  Y10S514/909

    摘要： 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 atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, or prodrugs thereof which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses and production intermediates thereof.

    摘要翻译： 本发明提供由以下通式表示的含氮杂环衍生物：其中X 1和X 3独立地表示N或CH; X 2表示N或CR 2; X 4表示N或CR 3; 并且条件是X 1，X 2，X 3和X 4中的一个或者两个表示N ; R 1表示氢原子，卤素原子，低级烷基，低级烷氧基，低级烷硫基，低级烷氧基取代的（低级烷基），低级烷氧基取代的（低级烷基） 低级烷氧基）基团，低级烷氧基（低级烷氧基） - 取代（低级烷基）基团，环状低级烷基基团，卤代（低级烷基）基团或由通式HO-A-表示的基团，其中A表示 低级亚烷基，低级亚烷基氧基或低级亚烷基硫基; R 2表示氢原子，卤素原子，低级烷基，环状低级烷基，低级烷氧基，氨基，（低级酰基）氨基，单（低级） 烷基）氨基或二（低级烷基）氨基; R 3表示氢原子或低级烷基，或其药学上可接受的盐或其前药，其可用作预防或治疗与高血糖相关的疾病如糖尿病，糖尿病 并发症或肥胖症，包含其的药物组合物及其药物用途和生产中间体。