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57 条记录 (耗时 0.031 秒)

    Fused heterocycle derivative, medicinal composition containing the same, and medicinal use thereof
    12.
    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：US07732596B2

    公开(公告)日：2010-06-08

    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： C07H7/06 ,  C07H7/04 ,  A61K31/7042

    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中的糖尿病，餐后高血糖，葡萄糖耐量降低，糖尿病并发症或肥胖症等高血糖代表由以下通式（S）表示的基团（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），另外表示H，OH，氨基等; R2和R3表示H，OH，氨基，卤素原子和任选取代的烷基等; A1代表O，S等; A2表示CH或N; 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; E2表示H，F，甲基等），以及包含 相同的药物用途。

    Glucopyranosyloxy benzylbenzene derivatives, medicinal compositions containing the same and intermediates for the preparation of the derivatives
    13.
    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。

    Glucopyranosyloxyprazole derivatives and use thereof in medicines
    15.
    发明申请
    Glucopyranosyloxyprazole derivatives and use thereof in medicines 有权
    吡喃葡萄糖基吡唑衍生物及其在药物中的应用

    公开(公告)号：US20060035847A1

    公开(公告)日：2006-02-16

    申请号：US11247356

    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： A61K31/7056 ,  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。

    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof
    18.
    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。

    FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES
    20.
    发明申请
    FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES 审中-公开
    熔融杂环衍生物及其用于医疗用途的方法

    公开(公告)号：US20110201815A1

    公开(公告)日：2011-08-18

    申请号：US13124336

    申请日：2009-10-14

    申请人： Kazuo Shimizu ,  Masato Iizuka ,  Hideki Fujikura ,  Yasushi Takigawa ,  Masahiro Hiratochi

    发明人： Kazuo Shimizu ,  Masato Iizuka ,  Hideki Fujikura ,  Yasushi Takigawa ,  Masahiro Hiratochi

    IPC分类号： C07D401/10 ,  C07D417/10

    CPC分类号： C07D401/04 ,  A61K31/427 ,  A61K31/443 ,  A61K31/4439 ,  C07D405/04 ,  C07D417/04

    摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused heterocyclic derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), T represents trifluoromethyl, nitro or cyano; ring Q represents heteroaryl; X1 and X2 independently represent CH or N; ring U represents aryl or heteroaryl; m represents integral number from 0 to 2; n represents integral number from 0 to 3; R1 represents a hydroxy group, amino or C1-6 alkyl; R2 represents C1-6 alkyl, C1-6 alkoxy C1-6 alkyl or the like.

    摘要翻译： 本发明提供了可用作预防或治疗与异常血浆尿酸水平等相关的疾病的药剂的化合物。 本发明涉及具有黄嘌呤氧化酶抑制活性的由下式（I）表示的稠合杂环衍生物，可用作预防或治疗与血浆尿酸水平异常有关的疾病，其前体药物，其盐或类似物 。 在式（I）中，T代表三氟甲基，硝基或氰基; 环Q表示杂芳基; X1和X2独立地表示CH或N; 环U表示芳基或杂芳基; m表示0〜2的整数; n表示0〜3的整数; R1表示羟基，氨基或C1-6烷基; R 2表示C 1-6烷基，C 1-6烷氧基C 1-6烷基等。