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    LOW-MOLECULAR SERINE PROTEASES INHIBITORS COMPRISING POLYHYDROXY-ALKYL AND POLYHYDROXY-CYCLOALKYL RADICALS
    6.
    发明申请
    LOW-MOLECULAR SERINE PROTEASES INHIBITORS COMPRISING POLYHYDROXY-ALKYL AND POLYHYDROXY-CYCLOALKYL RADICALS 审中-公开
    包含聚羟基 - 烷基和聚羟基 - 环烷基基团的低分子丝氨酸蛋白酶抑制剂

    公开(公告)号：US20110071285A1

    公开(公告)日：2011-03-24

    申请号：US12850545

    申请日：2010-08-04

    申请人： Dieter Herr ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger

    发明人： Dieter Herr ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger

    IPC分类号： C07H15/26 ,  C07D277/30 ,  C07D409/12

    CPC分类号： A61K31/155 ,  C07H7/00 ,  C07H15/00

    摘要： The invention relates to novel amidines and quanidines, the production and use thereof and the use thereof as trypsine-type serine protease competitive inhibitors, especially thrombine and compliment proteases CIs and C1r. The invention also relates to pharmaceutical compositions which contain said compounds as active ingredients, in addition to the use of the compounds as thrombine inhibitors, anticoagulants, compliment inhibitors and anti-inflammatory agents. The novel compositions are characterised by the linkage of a serine protease inhibitor having amidine or guanidine functions with an alkyl radical having two or more hydroxyl functions, whereby said alkyl radical is derived from sugar derivates. Several sugar structural components or components derived from sugar can therefore be linked to each other. Said principle of linking sugar derivates enables oral active compounds to be obtained.

    摘要翻译： 本发明涉及新型脒和喹啉，其生产及其用途及其作为胰蛋白酶型丝氨酸蛋白酶竞争性抑制剂的用途，特别是血栓素和补体蛋白酶CI和C1r。 除了使用化合物作为血栓抑制剂，抗凝剂，补体抑制剂和抗炎剂之外，本发明还涉及含有所述化合物作为活性成分的药物组合物。 该新型组合物的特征在于具有脒或胍功能的丝氨酸蛋白酶抑制剂与具有两个或多个羟基官能团的烷基基团的连接，其中所述烷基衍生自糖衍生物。 因此，几种糖结构成分或来自糖的组分可以彼此连接。 所述连接糖衍生物的原理使得能够获得口服活性化合物。