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    Bivalent thrombin inhibitors
    1.
    发明授权
    Bivalent thrombin inhibitors 失效
    二价凝血酶抑制剂

    公开(公告)号：US6127337A

    公开(公告)日：2000-10-03

    申请号：US636698

    申请日：1996-06-28

    申请人： Yasuo Konishi ,  Zbigniew Szewczuk ,  Yuko Tsuda

    发明人： Yasuo Konishi ,  Zbigniew Szewczuk ,  Yuko Tsuda

    IPC分类号： A61K38/00 ,  C07K14/815 ,  A61K38/03 ,  C07K7/00

    CPC分类号： C07K14/815 ,  A61K38/00

    摘要： Hirudin is the most potent and specific thrombin inhibitor and is derived from the medicinal leech. It is reported to inhibit thrombin with an equilibrium dissociation constant (K.sub.i) value of 2.2.times.10.sup.-14 M. synthetic thrombin inhibitors have been designed based on the hirudin sequence but with a dramatically reduced size. The bulky active site inhibitor segment, hirudin.sup.1-48, has been substituted by small non-substrate type active site inhibitors of thrombin, e.g., dansyl-Arg-(D-pipecolic acid). The linker segment has also been modified using a combination of .omega.-amino acids to reduce the molecular weight but retaining sufficient length to span the two principal binding domains. Among the inhibitors designed, dansyl-Arg-(D-pipecolic acid)-(12-aminododecanoic acid)-4-aminobutyric acid)-Asp-Tyr-Glu-Pro-Ile-Pro-Glu-Glu-Ala-(L-.beta.-cyclohexylalamine)-(D-Glu)-OH (SEQ ID NO:45) showed the highest affinity and displays a competitive-type inhibition. The incorporation of the non-substrate type active site inhibitor segment and the linker of .omega.-amino acids into the bivalent thrombin inhibitors not only improved in vitro thrombin inhibitory activity to the pM level, overcame proteolytic susceptibility at the level of the "normal" scissile bond and confered high in vivo activity.

    摘要翻译： PCT No.PCT / CA94 / 00585 Sec。 371日期：1996年6月28日 102（e）日期1996年6月28日PCT 1994年10月25日PCT PCT。 第WO95 / 11921号公报 日期1995年5月4日水蛭素是最有效和特异性的凝血酶抑制剂，来源于药用水蛭。 据报道，以平均解离常数（Ki）值为2.2×10-14 M抑制凝血酶。已经基于水蛭素序列设计合成的凝血酶抑制剂，但其显着减小的大小。 大体积的活性位点抑制物片段，水蛭素1-48已经被小的非底物型的凝血酶活性位点抑制剂例如丹磺酰-Arg-（D-哌啶酸）所取代。 接头片段也已经使用ω-氨基酸的组合进行了修饰，以降低分子量，但保留足够的长度来跨越两个主要的结合结构域。 在设计的抑制剂中，丹磺酰-Arg-（D-哌啶酸） - （12-氨基十二烷酸）-4-氨基丁酸）-Asp-Tyr-Glu-Pro-Ile-Pro-Glu-Glu-Ala-（L- β-环己胺） - （D-Glu）-OH（SEQ ID NO：45）显示出最高的亲和力并显示出竞争性抑制。 将非底物型活性位点抑制物区段和ω-氨基酸接头加入到二价凝血酶抑制剂中不仅提高了对pM水平的体外凝血酶抑制活性，克服了在“正常”剪切水平下的蛋白水解敏感性 结合并提出高体内活性。

    Optical Analyzing Unit and Optical Analyzing Device
    4.
    发明申请
    Optical Analyzing Unit and Optical Analyzing Device 失效
    光学分析单元和光学分析设备

    公开(公告)号：US20070211254A1

    公开(公告)日：2007-09-13

    申请号：US10582188

    申请日：2004-12-08

    申请人： Tomohiko Matsushita ,  Takeo Nishikawa ,  Yuko Tsuda ,  Shigemi Norioka ,  Tetsuichi Wazawa ,  Shigeru Aoyama

    发明人： Tomohiko Matsushita ,  Takeo Nishikawa ,  Yuko Tsuda ,  Shigemi Norioka ,  Tetsuichi Wazawa ,  Shigeru Aoyama

    IPC分类号： G01N21/55

    CPC分类号： G01N21/7703 ,  G01N21/553

    摘要： At both ends of a waveguide 43 having a plurality of cores 51, light emitting elements 47 and light receiving elements 49 are disposed so as to face end faces of the cores 51. A switch 44 is overlapped over the waveguide 43. In the switch 44, switching windows 52 each can be switched between a state where light propagating through the core 51 is passed and a state where the light is reflected are arranged in the vertical and horizontal directions, and the switching windows 52 are arranged along the top faces of the cores 51. A test board 45 having a plurality of channels 60 in each of which a metallic thin film 61 is formed is disposed over the switch 44, and receptors 62 are fixed on the metallic thin film 61 in the channels 60. A specimen containing a specific ligand is passed in each of the channels 60.

    摘要翻译： 在具有多个芯51的波导43的两端，发光元件47和光接收元件49设置成面对芯51的端面。 开关44重叠在波导43上。 在开关44中，切换窗52各自可以在通过芯51传播的光通过的状态和反射光的状态沿垂直和水平方向布置，并且切换窗口52沿着 芯51的顶面。 具有多个通道60的测试板45中的每一个形成有金属薄膜61设置在开关44上方，并且通道60中的金属薄膜61上固定有受体62。 含有特定配体的样品通过每个通道60。

    Optical analyzing unit and optical analyzing device
    6.
    发明授权
    Optical analyzing unit and optical analyzing device 失效
    光学分析装置和光学分析装置

    公开(公告)号：US07342663B2

    公开(公告)日：2008-03-11

    申请号：US10582188

    申请日：2004-12-08

    申请人： Tomohiko Matsushita ,  Takeo Nishikawa ,  Yuko Tsuda ,  Shigemi Norioka ,  Tetsuichi Wazawa ,  Shigeru Aoyama

    发明人： Tomohiko Matsushita ,  Takeo Nishikawa ,  Yuko Tsuda ,  Shigemi Norioka ,  Tetsuichi Wazawa ,  Shigeru Aoyama

    IPC分类号： G01N21/55

    CPC分类号： G01N21/7703 ,  G01N21/553

    摘要： At both ends of a waveguide 43 having a plurality of cores 51, light emitting elements 47 and light receiving elements 49 are disposed so as to face end faces of the cores 51. A switch 44 is overlapped over the waveguide 43. In the switch 44, switching windows 52 each can be switched between a state where light propagating through the core 51 is passed and a state where the light is reflected are arranged in the vertical and horizontal directions, and the switching windows 52 are arranged along the top faces of the cores 51. A test board 45 having a plurality of channels 60 in each of which a metallic thin film 61 is formed is disposed over the switch 44, and receptors 62 are fixed on the metallic thin film 61 in the channels 60. A specimen containing a specific ligand is passed in each of the channels 60.

    摘要翻译： 在具有多个芯51的波导43的两端，发光元件47和光接收元件49设置成面对芯51的端面。 开关44重叠在波导43上。 在开关44中，切换窗52各自可以在通过芯51传播的光通过的状态和反射光的状态沿垂直和水平方向布置，并且切换窗口52沿着 芯51的顶面。 具有多个通道60的测试板45中的每一个形成有金属薄膜61设置在开关44上方，并且通道60中的金属薄膜61上固定有受体62。 含有特定配体的样品通过每个通道60。