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12 条记录 (耗时 0.015 秒)

    GLYCOPYRANOSYLOXYPYRAZOLE DERIVATIVES AND MEDICINAL USE THEREOF
    3.
    发明公开
    GLYCOPYRANOSYLOXYPYRAZOLE DERIVATIVES AND MEDICINAL USE THEREOF 有权
    糖皮质激素代谢物吡唑衍生物及其药物用途

    公开(公告)号：EP1364958A1

    公开(公告)日：2003-11-26

    申请号：EP02703898.3

    申请日：2002-02-26

    申请人： Kissei Pharmaceutical Co., Ltd.

    发明人： FUSHIMI, Nobuhiko ,  FUJIKURA, Hideki ,  NISHIMURA, Toshihiro ,  KATSUNO, Kenji ,  ISAJI, Masayuki

    IPC分类号： C07H17/02 ,  C07D233/70 ,  A61K31/7056 ,  A61P43/00 ,  A61P3/10 ,  A61P3/04 ,  A61P3/06 ,  A61P9/10 ,  A61P9/12 ,  A61P9/04 ,  A61P7/10 ,  A61P19/06

    CPC分类号： C07H17/02 ,  Y10S514/866

    摘要： The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula:
    wherein R 1 , R 2 and R 3 represent a hydrogen atom or a halogen atom; R 4 represents a lower alkyl group or a halo(lower alkyl) group; and R 5 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, etc., a pharmaceutically acceptable salt thereof or a prodrug thereof., 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R1，R2和R3代表氢原子或卤素原子; R4代表低级烷基或卤代（低级烷基）基团; R5表示氢原子，低级烷基，低级烷氧基，低级烷硫基等，其药学上可接受的盐或其前体药物，其在人类SGLT2中发挥优异的抑制活性，因此是有用的 作为预防或治疗糖尿病，糖尿病并发症或肥胖症等高血糖相关疾病，其药学上可接受的盐或其前药，其制备中间体及其药物用途的药物。

    GLYCOPYRANOSYLOXYPYRAZOLE DERIVATIVES AND MEDICINAL USE THEREOF
    6.
    发明公开
    GLYCOPYRANOSYLOXYPYRAZOLE DERIVATIVES AND MEDICINAL USE THEREOF 有权
    糖皮质激素代谢物吡唑衍生物及其药物用途

    公开(公告)号：EP1364957A1

    公开(公告)日：2003-11-26

    申请号：EP02703897.5

    申请日：2002-02-26

    申请人： Kissei Pharmaceutical Co., Ltd.

    发明人： NISHIMURA, Toshihiro ,  FUSHIMI, Nobuhiko ,  FUJIKURA, Hideki ,  KATSUNO, Kenji ,  KOMATSU, Yoshimitsu ,  ISAJI, Masayuki

    IPC分类号： C07H17/02 ,  C07D233/70 ,  C07D417/10 ,  C07D401/10 ,  A61K31/7056 ,  A61K31/706 ,  A61P43/00 ,  A61P3/10 ,  A61P3/04 ,  A61P3/06 ,  A61P9/10 ,  A61P9/12 ,  A61P9/04 ,  A61P7/10 ,  A61P19/06

    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; R 1 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkenyl group, a cyclic lower alkyl group, etc.; R 2 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糖基氧吡唑衍生物：其中Q和T之一表示由通式表示的基团，而另一个表示低级烷基或卤代（低级烷基）基团; R 1表示氢原子，可以具有取代基的低级烷基，低级烯基，环状低级烷基等。 R2表示在人SGLT2中发挥优异的抑制活性的氢原子，可以具有取代基的低级烷基，低级烷氧基，低级链烯基，环状低级烷基，环状低级烷氧基等， 作为用于预防或治疗糖尿病，糖尿病并发症或肥胖等高血糖症相关疾病，其药学上可接受的盐或其前药，其制备中间体及其药物用途的药物是有用的。

    GLYCOPYRANOSYLOXYPYRAZOLE DERIVATIVES AND MEDICINAL USE THEREOF
    9.
    发明授权
    GLYCOPYRANOSYLOXYPYRAZOLE DERIVATIVES AND MEDICINAL USE THEREOF 有权
    糖皮质激素代谢物吡唑衍生物及其药物用途

    公开(公告)号：EP1364957B1

    公开(公告)日：2008-12-31

    申请号：EP02703897.5

    申请日：2002-02-26

    申请人： Kissei Pharmaceutical Co., Ltd.

    发明人： NISHIMURA, Toshihiro ,  FUSHIMI, Nobuhiko ,  FUJIKURA, Hideki ,  KATSUNO, Kenji ,  KOMATSU, Yoshimitsu ,  ISAJI, Masayuki

    IPC分类号： C07H17/02 ,  C07D231/20 ,  A61K31/70 ,  A61P3/10

    CPC分类号： C07H15/203 ,  C07H17/02

    摘要： Glucopyranosyloxypyrazole derivatives represented by the following general formula (I) expressing an excellent human SGLT2 activity inhibitory effect and thus being useful as preventives or remedies for diseases caused by hyperglycemia such as diabetes, diabetic complications and obesity, pharmacologically acceptable salts thereof, prodrugs thereof, production intermediates thereof and medicinal use of the same: (I) wherein one of Q and T represents a group represented by the following general formula: while the other represents lower alkyl or lower haloalkyl; R represents hydrogen, optionally substituted lower alkyl, lower alkenyl, cyclic lower alkyl, etc.; and R represents hydrogen, optionally substituted lower alkyl, lower alkoxy, lower alkenyl, cyclic lower alkyl, cyclic lower alkoxy, etc.

    摘要翻译： 由下述通式（I）表示的吡喃葡萄糖氧基吡唑衍生物表现优异的人SGLT2活性抑制作用，因此可用作由高血糖引起的疾病例如糖尿病，糖尿病并发症和肥胖症的预防剂或治疗剂，其药理学上可接受的盐，其前药，生产 其中间体及其药物用途：（I）其中Q和T之一表示由下列通式表示的基团：而另一个表示低级烷基或低级卤代烷基; R 1代表氢，任选取代的低级烷基，低级烯基，环状低级烷基等; 并且R 2表示氢，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

    NITROGENOUS HETEROCYCLIC DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF AND INTERMEDIATE THEREFOR
    10.
    发明公开
    NITROGENOUS HETEROCYCLIC DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF AND INTERMEDIATE THEREFOR 审中-公开
    NITRO GENES杂环衍生物CONTAINING医疗用组合物，及其医药用途和中间体THEREFOR

    公开(公告)号：EP1405859A1

    公开(公告)日：2004-04-07

    申请号：EP02738729.9

    申请日：2002-06-17

    申请人： Kissei Pharmaceutical Co., Ltd.

    发明人： NISHIMURA, Toshihiro ,  FUJIKURA, Hideki ,  FUSHIMI, Nobuhiko ,  TATANI, Kazuya ,  KATSUNO, Kenji ,  ISAJI, Masayuki

    IPC分类号： C07H17/02 ,  A61K31/706 ,  A61P3/04 ,  A61P3/10 ,  A61P43/00

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

    摘要： The present invention is to provide a nitrogen-containing heterocyclic derivative represented by the general formula (I) or a pharmaceutically acceptable salt thereof, or a prodrug thereof, which exerts an excellent inhibitory activity in human SGLT2 and is useful as an agent for the prevention or treatment of a disease associated with hyperglycemia such as diabetes etc., or a pharmaceutical composition comprising the same and a pharmaceutical use thereof and a production intermediate thereof. In the general formula (I), X 1 and X 3 are N or CH; X 2 is N or CR 2 ; X 4 is N or CR 3 ; and with the proviso that one or two of X 1 , X 2 , X 3 and X 4 are N; and R 1 , R 2 and R 3 are a hydrogen atom etc.

    摘要翻译： Glucopyranosylheterocycle衍生物（I）是新的。 式（I）的Glucopyranosylheterocycle衍生物和它们的盐和前体药物是新的。 [图像] X 1>，X 3> N或CH; X 2> N或CR 2>; X 4为> N或CR 3>; 的R 1> H，卤素，A，OA，SA，AOA，OAOA，AOAOA，环烷基，低级卤代烷基或A 1 OH; 甲1lower亚烷基，低级alkenyleneoxy或低级亚烷硫基; R 2> H，卤素，A，环烷基，OA，NH 2，低级酰基氨基，NHA或NAA; ，R 3> H或A，并且A：低级烷基，条件没有一个或两个X 1> X 4> = N.因此独立权利要求中包含对式中间体化合物（II） - （IV）。 [图像] P“：H或前药基团; R 11>基团R 1>与A 1 OH由器10p A“取代; ，R 0>基团R 1 OH通过1W A A器10p 1和P 1个为H或羟基保护基团替代。 活动：降糖; 厌食; 降血脂; Antianteriosclerotic; 低血压; Cardiant; 抗炎; Uropathic。 作用机制：拮抗剂钠; 胆固醇拮抗剂。 在使用COS-7细胞，3-（4-乙基苄基）-2-（测试版-D-吡喃葡糖氧基）测定-4,6-二甲基吡啶有一个IC，用于50value甲基基-α-D-吡喃葡糖苷在41人SGLT2受体的结合 纳摩。