知搜-全球专利检索

  1. 登录
  2. 注册

搜索结果

68 条记录 (耗时 0.029 秒)

    Cyclic oxyguanidine pyrazinones as protease inhibitors
    5.
    发明授权
    Cyclic oxyguanidine pyrazinones as protease inhibitors 有权
    环氧乙酰吡嗪酮作为蛋白酶抑制剂

    公开(公告)号：US06476016B2

    公开(公告)日：2002-11-05

    申请号：US09905883

    申请日：2001-07-17

    申请人： Aihua Wang ,  Bruce Edward Tomczuk ,  Tianbao Lu ,  Richard M. Soll ,  John Curtis Spurlino ,  Roger Francis Bone

    发明人： Aihua Wang ,  Bruce Edward Tomczuk ,  Tianbao Lu ,  Richard M. Soll ,  John Curtis Spurlino ,  Roger Francis Bone

    IPC分类号： C07D41312

    CPC分类号： C07D413/12 ,  C07D413/14

    摘要： Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.

    摘要翻译： 描述了环状氧基胍吡嗪酮化合物，包括式I的化合物：其中R 3，R 4，R 5，W和A如说明书中所述，以及其水合物，溶剂合物或其药学上可接受的盐。 本发明的化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，如胰凝乳蛋白酶，胰蛋白酶，凝血酶，纤溶酶和因子Xa。 某些化合物通过直接，选择性抑制凝血酶表现出抗血栓形成活性。 描述了抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制栓塞形成的组合物。 本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂， 血线和支架。 另外，化合物可以被可检测地标记并用于血栓的体内成像。

    Heterocyclic protease inhibitors
    6.
    发明授权
    Heterocyclic protease inhibitors 有权
    杂环蛋白酶抑制剂

    公开(公告)号：US06326492B1

    公开(公告)日：2001-12-04

    申请号：US09578487

    申请日：2000-05-26

    申请人： Aihua Wang ,  Tianbao Lu ,  Bruce E. Tomczuk ,  Richard M. Soll ,  John Spurlino ,  Roger Bone

    发明人： Aihua Wang ,  Tianbao Lu ,  Bruce E. Tomczuk ,  Richard M. Soll ,  John Spurlino ,  Roger Bone

    IPC分类号： C07D26502

    CPC分类号： C07D413/12 ,  C07D413/14

    摘要： Described are compounds of the Formula VII: wherein Het, R1, R7 and A are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.

    摘要翻译： 描述了式VII的化合物：其中Het，R 1，R 7和A在本说明书中列出，以及其抑制蛋白水解酶如凝血酶的水合物，溶剂合物或其药学上可接受的盐。 还描述了制备这些化合物的方法。 本发明的化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，如胰凝乳蛋白酶，胰蛋白酶，凝血酶，纤溶酶和因子Xa。 某些化合物通过直接，选择性抑制凝血酶表现出抗血栓形成活性。 本发明包括用于抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制哺乳动物栓塞形成的组合物，其包含本发明化合物在药学上可接受的载体中。 本发明化合物的其它用途是作为凝血剂或者物理连接于制造用于血液收集，血液循环和血液储存中的装置的材料的抗凝剂，例如导管，血液透析机，采血注射器和管， 血线和支架。 另外，化合物可以被可检测地标记并用于血栓的体内成像。