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Thrombocyte inhibition via vivo-morpholino knockdown of alpha IIb

机译:通过体内吗啉代击倒的αIIb抑制血小板。

摘要

Novel compounds comprising a guanidine-rich head covalently coupled to one or more oligonucleotide antisense sequences which are useful to modulate blood coagulation by affecting the expression of integrin αIIb or β3 are described herein. This invention also includes pharmaceutical compositions containing these compounds, with or without other therapeutic agents, and to methods of using these compounds as inhibitor of platelet aggregation, as thrombolytics, and/or for the treatment of other thromboembolic disorders. Vivo-MOs, which include eight guanidine groups dendrimerically arranged in the guanidine-rich head and two synthetic antisense morpholino oligonucleotides, are representative compounds of the present invention.
机译:本文描述了包含与一个或多个寡核苷酸反义序列共价偶联的富含胍的头部的新型化合物,其可用于通过影响整联蛋白αIIb或β3的表达来调节凝血。本发明还包括含有这些化合物,有或没有其他治疗剂的药物组合物,以及使用这些化合物作为血小板凝集抑制剂,溶栓剂和/或用于治疗其他血栓栓塞性疾病的方法。体内-MOs是本发明的代表性化合物,其包括在富胍基团的头部中以树枝状排列的八个胍基和两个合成的反义吗啉代寡核苷酸。

著录项

  • 公开/公告号US9801886B2

    专利类型

  • 公开/公告日2017-10-31

    原文格式PDF

  • 申请/专利权人 PUDUR JAGADEESWARAN;

    申请/专利号US201113015905

  • 发明设计人 PUDUR JAGADEESWARAN;

    申请日2011-01-28

  • 分类号C07D295;C40B30/06;C12N5;C12N15/113;A61K31/5377;C07D413/14;

  • 国家 US

  • 入库时间 2022-08-21 13:45:32

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