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    Fused heterocycle derivative, medicinal composition containing the same, and medicinal use thereof
    11.
    发明申请
    Fused heterocycle derivative, medicinal composition containing the same, and medicinal use thereof 有权
    稠合的杂环衍生物，含有它们的药物组合物及其医药用途

    公开(公告)号：US20070197450A1

    公开(公告)日：2007-08-23

    申请号：US10591421

    申请日：2005-03-03

    申请人： Nobuhiko Fushimi ,  Masayuki Isaji ,  Hideki Fujikura

    发明人： Nobuhiko Fushimi ,  Masayuki Isaji ,  Hideki Fujikura

    IPC分类号： A61K31/7052 ,  C07H17/02

    CPC分类号： C07D405/04 ,  A61K31/351 ,  A61K31/381 ,  A61K31/404 ,  A61K45/06 ,  C07D409/04 ,  A61K2300/00

    摘要： 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.

    摘要翻译： 本发明提供由以下通式（I）表示的稠合杂环衍生物或其药学上可接受的盐或其前药，其在人SGLT中表现出抑制活性，并且可用作预防或治疗与高血糖相关的疾病的药剂 例如糖尿病，餐后高血糖症，葡萄糖耐量降低，糖尿病并发症或肥胖症，式R 1至R 4代表H，OH，氨基等; R 5和R 6代表H，OH，卤素原子，选择性烯取代的烷基等; Q表示亚烷基，亚烯基等; 环A表示芳基或杂芳基; 下述环（R1）表示由下述环（R2）表示的基团。 G表示由以下通式（G-1）或（G-2）表示的基团（E 1）表示H，F或OH; E表示H，F，甲基等 ），以及包含其的药物组合物及其药物用途。

    Fused heterocycle derivative, medicinal composition containing the same, and medicinal use thereof
    12.
    发明申请
    Fused heterocycle derivative, medicinal composition containing the same, and medicinal use thereof 有权
    稠合的杂环衍生物，含有它们的药物组合物及其医药用途

    公开(公告)号：US20070197449A1

    公开(公告)日：2007-08-23

    申请号：US10591403

    申请日：2005-03-03

    申请人： Nobuhiko Fushimi ,  Hideki Fujikura ,  Masayuki Isaji

    发明人： Nobuhiko Fushimi ,  Hideki Fujikura ,  Masayuki Isaji

    IPC分类号： A61K31/7052 ,  C07H17/02 ,  A61K38/28 ,  A61K38/22

    CPC分类号： C07H17/00

    摘要： 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.; A2 represents CH or N; G represents a group represented by the following general formula (G-1) or (G-2) (E1 represents H, F or OH; and E2 represents H, F, a methyl group, etc.), and pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.

    摘要翻译： 本发明提供由以下通式表示的含氮稠合环状衍生物或其药学上可接受的盐或其前药，其在人SGLT中表现出优异的抑制活性，并且可用作预防或治疗与 R 1和R 4的式1中的高血糖症如糖尿病，餐后高血糖症，葡萄糖耐量降低，糖尿病并发症或肥胖症代表由以下通式表示的基团 （S）（其中R 5和R 6表示H，OH，卤素原子等; Q表示亚烷基等;环A表示 芳基等），另一个表示H，OH，氨基等; R 2和R 3代表H，OH，氨基，卤素原子和任选取代的烷基等; A 表示O，S等; A 2表示CH或N; G表示由以下通式（G-1）或（G-2）表示的基团（E 1）表示H，F或OH;且E 2表示H ，F，甲基等）及其药物组合物及其药物用途。

    Glucopyranosyloxypyrazole derivatives and medicinal use thereof
    14.
    发明申请
    Glucopyranosyloxypyrazole derivatives and medicinal use thereof 有权
    吡喃葡萄糖氧吡唑衍生物及其医药用途

    公开(公告)号：US20060142209A1

    公开(公告)日：2006-06-29

    申请号：US11358400

    申请日：2006-02-22

    申请人： Toshihiro Nishimura ,  Nobuhiko Fushimi ,  Hideki Fujikura ,  Kenji Katsuno ,  Yoshimitsu Komatsu ,  Masayuki Isaji

    发明人： Toshihiro Nishimura ,  Nobuhiko Fushimi ,  Hideki Fujikura ,  Kenji Katsuno ,  Yoshimitsu Komatsu ,  Masayuki Isaji

    IPC分类号： A61K31/7052

    CPC分类号： C07H15/203 ,  C07H17/02

    摘要： 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.

    摘要翻译： 本发明提供由以下通式表示的吡喃葡萄糖氧吡唑衍生物：其中Q和T之一表示由通式表示的基团，而另一个代表低级烷基或卤代（低级烷基）基团; R 1表示氢原子，任选取代的低级烷基，低级烯基，环状低级烷基等; R 2表示氢原子，任选取代的低级烷基，低级烷氧基，低级烯基，环状低级烷基，环状低级烷氧基等，其具有优异的 因此可用作预防或治疗与糖尿病，糖尿病并发症或肥胖症，糖尿病并发症或肥胖症，糖尿病并发症或肥胖症，其药学上可接受的盐或其前药，与其生产中间体及其药物用途有关的疾病的药物。

    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates for the preparation of the derivatives
    15.
    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。

    Glucopyranosyloxypyrazole derivatives and use thereof in medicines
    16.
    发明申请
    Glucopyranosyloxypyrazole derivatives and use thereof in medicines 有权
    吡喃葡萄糖氧吡唑衍生物及其在药物中的应用

    公开(公告)号：US20060025352A1

    公开(公告)日：2006-02-02

    申请号：US11247216

    申请日：2005-10-12

    申请人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Takeshi Nakabayashi ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Takeshi Nakabayashi ,  Masayuki Isaji

    IPC分类号： A61K31/7052 ,  C07H17/02

    CPC分类号： A61K45/06 ,  A61K31/7056 ,  C07H17/02 ,  A61K2300/00

    摘要： 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 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吡唑衍生物：其中R表示氢原子，低级烷基或形成前药的基团; Q和T表示由以下通式表示的基团：（其中P表示 氢原子或形成前药的基团），而另一个表示低级烷基或卤代（低级烷基）基团; R 2表示氢原子，低级烷基，低级烷氧基，低级烷硫基，卤代（低级烷基）或卤素原子; 并且条件是当R表示氢原子或低级烷基时，P不表示氢原子，或其药学上可接受的盐，其在人SGLT2中具有抑制活性并具有改善的口服吸收，因此可用作 用于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及其药学上可接受的盐及其药学用途。

    Nitrogenous heterocyclic derivative, medicinal composition containing the same, medical use thereof, and intermediate therefor
    19.
    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。

    Glucopyranosyloxypyrazole derivatives and use thereof in medicines
    20.
    发明授权
    Glucopyranosyloxypyrazole derivatives and use thereof in medicines 有权
    吡喃葡萄糖氧吡唑衍生物及其在药物中的应用

    公开(公告)号：US07989424B2

    公开(公告)日：2011-08-02

    申请号：US12169882

    申请日：2008-07-09

    申请人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Takeshi Nakabayashi ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Takeshi Nakabayashi ,  Masayuki Isaji

    IPC分类号： A01N43/04 ,  A61K31/70

    CPC分类号： A61K45/06 ,  A61K31/7056 ,  C07H17/02 ,  A61K2300/00

    摘要： 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 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吡唑衍生物：其中R表示氢原子，低级烷基或形成前药的基团; Q和T之一表示由通式表示的基团：（其中P表示氢原子或形成前药的基团），而另一个表示低级烷基或卤代（低级烷基）基团; R2表示氢原子，低级烷基，低级烷氧基，低级烷硫基，卤代（低级烷基）或卤素原子; 并且条件是当R表示氢原子或低级烷基时，P不表示氢原子，或其药学上可接受的盐，其在人SGLT2中具有抑制活性并具有改善的口服吸收，因此可用作 用于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及其药学上可接受的盐及其药学用途。