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    PROCOAGULANT COMPOUNDS
    1.
    发明公开
    PROCOAGULANT COMPOUNDS 有权
    促凝剂化合物

    公开(公告)号：EP2858659A1

    公开(公告)日：2015-04-15

    申请号：EP13799785.4

    申请日：2013-06-07

    申请人： Biogen Idec MA Inc.

    发明人： HONG, Vu Phong ,  MEZO, Adam R. ,  SALAS, Joe ,  PETERS, Robert

    IPC分类号： A61K38/02 ,  A61K38/36 ,  A61P7/02

    摘要： The present disclosure provides protease-activatable procoagulant compounds comprising a procoagulant polypeptide, e.g., a procoagulant peptide and/or clotting factor, and a linker comprising a protease-cleavable substrate (e.g., a synthetic thrombin substrate) and a self-immolative spacer (e.g., p-amino benzyl carbamate). Upon cleavage of the protease-cleavable substrate by a protease (e.g., thrombin), the self-immolative spacer cleaves itself from the procoagulant polypeptide such that the polypeptide is in an underivatized and active form. Also provided are pharmaceutical compositions, methods for treating bleeding disefficacy orders using the disclosed compounds, methods of enhancing in vivo of procoagulant polypeptides, methods of increasing the efficacy of proteolytic cleavage of compounds comprising procoagulant polypeptides, methods of activating procoagulant polypeptides, and methods of releasing a procoagulant polypeptide from a heterologous moiety such as PEG.

    摘要翻译： 本公开内容提供蛋白酶活化促凝血化合物，其包含促凝血多肽（例如促凝血肽和/或凝血因子）和包含蛋白酶可切割底物（例如，合成凝血酶底物）和自我免疫间隔物（例如， ，氨基甲酸对氨基苄基酯）。 在蛋白酶可切割的底物被蛋白酶（例如凝血酶）切割后，自我牺牲间隔物从促凝血多肽切割自身，使得多肽处于未衍生化和活性形式。 还提供了药物组合物，使用所公开的化合物治疗出血病症的方法，增强促凝血多肽的体内功效的方法，提高包含促凝血多肽的化合物的蛋白水解切割的功效的方法，活化促凝血多肽的方法以及释放方法 来自异源部分如PEG的促凝血多肽。