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    Fused heterocycle derivative, medicinal composition containing the same, and medicinal use thereof
    33.
    发明授权
    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：US08058245B2

    公开(公告)日：2011-11-15

    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： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61K31/7052

    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 如糖尿病，餐后高血糖症，葡萄糖耐量减低，糖尿病并发症或肥胖症，式R1至R4表示H，OH，氨基等; R5和R6表示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（E1表示H，F或OH; E表示H，F，甲基等），以及包含 相同的药物用途。

    Nitrogen-containing heterocyclic derivatives, medicinal compositions containing the same and medicinal use thereof
    34.
    发明授权
    Nitrogen-containing heterocyclic derivatives, medicinal compositions containing the same and medicinal use thereof 失效
    含氮杂环衍生物，含有该杂环衍生物的医药组合物及其医药用途

    公开(公告)号：US07655633B2

    公开(公告)日：2010-02-02

    申请号：US10540519

    申请日：2003-12-19

    申请人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masayuki Isaji

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

    CPC分类号： C07H17/02 ,  A61K31/706

    摘要： The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein X1 represents N or CR1; X2 represents N or 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.

    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X1表示N或CR1; X2表示N或CR2; X3表示N或CR3; X4表示N或CR4; 并且条件是X1至X4中的一个或两个表示N; R代表任选取代的C 3-8环烷基，任选取代的C 6-10芳基等; R1至R4表示H，卤素原子等）或其药学上可接受的盐或其前药，其在人SGLT2中具有优异的抑制活性，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，糖尿病并发症，肥胖症等，包含其的药物组合物及其药用用途。

    Glucopyranosyloxybenzylbenzene derivatives and medicinal use thereof
    35.
    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。

    Glucopyranosyloxypyrazole derivatives and use thereof in medicines
    36.
    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：US07429568B2

    公开(公告)日：2008-09-30

    申请号：US11247332

    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： A01N43/04 ,  A61K31/70 ,  C07H17/00

    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; 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 derivatives, medicinal compositions containing the same, medicinal uses thereof, and intermediates therefor
    37.
    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。

    Glucopyranosyloxypyrazole derivative medicinal composition containing the same medicinal use thereof and intermediate therefor
    38.
    发明授权
    Glucopyranosyloxypyrazole derivative medicinal composition containing the same medicinal use thereof and intermediate therefor 失效
    含有相同药用的吡喃葡萄糖氧吡唑衍生物药物组合物及其中间体

    公开(公告)号：US07217697B2

    公开(公告)日：2007-05-15

    申请号：US10479083

    申请日：2002-05-27

    申请人： Hiroaki Shiohara ,  Hideki Fujikura ,  Nobuhiko Fushimi ,  Fumiaki Ito ,  Masayuki Isaji

    发明人： Hiroaki Shiohara ,  Hideki Fujikura ,  Nobuhiko Fushimi ,  Fumiaki Ito ,  Masayuki Isaji

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

    CPC分类号： C07D231/20 ,  C07H15/26 ,  C07H17/02

    摘要： 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, diabetic complications or obesity, pharmaceutical compositions comprising the same, pharmaceutical uses thereof and production intermediates 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 1是氢原子或羟烷基; Q和T之一是由通式表示的基团; 另一个是任选取代的烷基或环烷基; R 2是卤素原子，羟基，任意取代的烷基，任意取代的烷氧基，烷硫基，通式为-AR 3的基团， 其中A是单键，氧原子，亚甲基，亚乙基，-OCH 2 - 或-CH 2 O-; 和R 3是环烷基，杂环烷基，任选取代的芳基，任选取代的噻唑基或任选取代的吡啶基，其药学上可接受的盐或其前药，其具有优异的抑制性 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症相关的疾病的药物，其药物组合物，药物组合物及其生产中间体。

    Glucopyranosyloxypyrazole derivatives and medicinal use thereof
    39.
    发明授权
    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：US07189702B2

    公开(公告)日：2007-03-13

    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： A01N43/04 ,  A61K31/70 ,  C07H17/00

    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。

    Glucopyranosyloxypyrazole derivatives and use thereof in medicines
    40.
    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：US07084123B2

    公开(公告)日：2006-08-01

    申请号：US10451926

    申请日：2001-12-25

    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 ,  C07H17/00

    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; 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。