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    Aminoguanidinyl- and Alkoxyguanidinyl-substituted phenyl acetamides as protease inhibitors
    4.
    发明授权
    Aminoguanidinyl- and Alkoxyguanidinyl-substituted phenyl acetamides as protease inhibitors 有权
    氨基胍基和烷氧基胍基取代的苯基乙酰胺作为蛋白酶抑制剂

    公开(公告)号：US06521663B2

    公开(公告)日：2003-02-18

    申请号：US09971000

    申请日：2001-10-05

    申请人： Wenxi Pan ,  Tianbao Lu ,  Thomas P. Markotan ,  Bruce E. Tomczuk

    发明人： Wenxi Pan ,  Tianbao Lu ,  Thomas P. Markotan ,  Bruce E. Tomczuk

    IPC分类号： C07C30930

    CPC分类号： C07D213/73 ,  A61K31/155 ,  A61K31/44 ,  C07C279/00 ,  C07C309/73 ,  C07C311/13 ,  C07C311/21 ,  C07D213/75 ,  A61K2300/00

    摘要： Phenyl acetamide compounds are described, including compounds of Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R3-R6, R11, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as thrombin and factor Xa. 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： 描述了苯基乙酰胺化合物，包括式I化合物或其溶剂合物，水合物或其药学上可接受的盐; 其中R3-R6，R11，B，Y和W在说明书中列出。 本发明的化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样的丝氨酸蛋白酶，如凝血酶和因子Xa。 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连接于制造用于血液收集，血液循环和血液储存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。

    Heteroaryl protease inhibitors and diagnostic imaging agents
    6.
    发明授权
    Heteroaryl protease inhibitors and diagnostic imaging agents 有权
    杂芳基蛋白酶抑制剂和诊断显像剂

    公开(公告)号：US06420397B1

    公开(公告)日：2002-07-16

    申请号：US09612591

    申请日：2000-07-07

    申请人： Wenxi Pan ,  Tianbao Lu ,  Richard M. Soll ,  Bruce E. Tomczuk

    发明人： Wenxi Pan ,  Tianbao Lu ,  Richard M. Soll ,  Bruce E. Tomczuk

    IPC分类号： A61K314412

    CPC分类号： C07D213/76 ,  C07D417/12

    摘要： Ketothiazole alkoxyguanidine and aminoguanidine analogs are described, including compounds of the Formula I: wherein X is O or NR9 and Het, A, R1, R7, R8, R12, R13, Ra, Rb, Rc, Z, m and n 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： 描述了酮噻唑烷氧基胍和氨基胍类似物，包括式I化合物：其中X是O或NR 9，并且阐述Het，A，R 1，R 7，R 8，R 12，R 13，R a，R b，R c，Z，m和n 在说明书中，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。