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    Cyclic compounds useful as inhibitors of platelet glycoprotein IIB/IIIA
    9.
    发明授权
    Cyclic compounds useful as inhibitors of platelet glycoprotein IIB/IIIA 失效
    可用作血小板糖蛋白IIB / IIIA抑制剂的循环化合物

    公开(公告)号：US5635477A

    公开(公告)日：1997-06-03

    申请号：US461611

    申请日：1995-06-05

    申请人： William F. Degrado ,  Sharon A. Jackson ,  Shaker A. Mousa ,  Anju Parthasarathy ,  Michael Sworin ,  Maria Rafalski

    发明人： William F. Degrado ,  Sharon A. Jackson ,  Shaker A. Mousa ,  Anju Parthasarathy ,  Michael Sworin ,  Maria Rafalski

    IPC分类号： A61K38/00 ,  C07K7/56 ,  C07K14/75 ,  A61K38/12

    CPC分类号： C07K14/75 ,  C07K7/56 ,  A61K38/00

    摘要： This invention relates to novel cyclic compounds containing carbocyclic ring systems useful as antagonists of the platelet glycoprotein IIb/IIIa complex, to pharmaceutical compositions containing such cyclic compounds, with or without other therapeutic agents, and to methods of using these compounds, with or without other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of other thromboembolic disorders. This invention also relates to methods of using the cyclic compounds of the invention in combination with anti-coagulants such as warfarin or heparin, or additional anti-platelet agents such as aspirin, piroxicam or ticlopidine, or thrombin inhibitors such as boropeptides, hirudin or argatroban, or thrombolytic agents such as tissue plasminogen activator, anistreplase, urokinase or streptokinase, or combinations thereof, for the treatment of thromboembolic disorders. A representative compound of the invention is cyclo(D-Val-(.sup..alpha. N-methyl Arg)-Gly-Asp-(3-aminomethylbenzoic acid).

    摘要翻译： 本发明涉及含有可用作血小板糖蛋白IIb / IIIa复合物的拮抗剂的碳环系的新型环状化合物，含有或不含其它治疗剂的含有环状化合物的药物组合物，以及使用或不使用其它治疗剂的方法 治疗剂，用于抑制血小板聚集，作为血栓溶解剂，和/或用于治疗其他血栓栓塞障碍。 本发明还涉及使用本发明的环状化合物与抗凝血剂如华法林或肝素或另外的抗血小板药如阿司匹林，吡罗昔康或噻氯匹定或凝血酶抑制剂如硼多肽，水蛭素或阿加曲班联合使用的方法 ，或血栓溶解剂如组织纤溶酶原激活剂，anistreplase，尿激酶或链激酶或其组合，用于治疗血栓栓塞性疾病。 本发明的代表性化合物是环（D-Val-（αN-甲基Arg）-Gly-Asp-（3-氨基甲基苯甲酸）。