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    NOVEL UROKINASE INHIBITORS
    4.
    发明公开
    NOVEL UROKINASE INHIBITORS 有权
    新尿激酶抑制剂

    公开(公告)号：EP1940856A1

    公开(公告)日：2008-07-09

    申请号：EP06806436.9

    申请日：2006-10-20

    申请人： Universiteit Antwerpen

    发明人： AUGUSTYNS, Koen ,  JOOSSENS, Jurgen ,  VAN DER VEKEN, Pieter ,  LAMBEIR, Anne-Marie Virginie Renée ,  SCHARPÉ, Simon ,  HAEMERS, Achiel

    IPC分类号： C07F9/40

    CPC分类号： C07F9/4006 ,  C07F9/4084

    摘要： The present invention relates to novel compounds with inhibitory activity towards urokinase plasminogen activator (uPA); to methods for preparation of said uPA inhibitor compounds; to pharmaceutical compositions comprising said uPA inhibitor compounds; to the use of said uPA inhibitor compounds as a medicament and the use of said uPA inhibitor compounds for the preparation of a medicament for the treatment of conditions chosen from the group comprising cancer, tumour growth, tumour invasion, tumour metastasis, diabetic retinopathy, hemorrhagic atherosclerosis and inflammatory conditions, such as rheumatoid arthritis and psoriasis.

    NOVEL KLK4 INHIBITORS
    7.
    发明公开
    NOVEL KLK4 INHIBITORS 审中-公开
    NEUARTIGE KLK4-INHIBITOREN

    公开(公告)号：EP3122758A1

    公开(公告)日：2017-02-01

    申请号：EP15722454.4

    申请日：2015-03-30

    申请人： Universiteit Antwerpen

    发明人： JOOSSENS, Jurgen ,  AUGUSTYNS, Koen ,  LAMBEIR, Anne-Marie ,  VAN DER VEKEN, Pieter ,  VAN SOOM, Jeroen ,  MAGDOLEN, Viktor

    IPC分类号： C07F9/6539 ,  C07F9/6561

    CPC分类号： C07F9/6561 ,  A61K49/0052 ,  C07F9/4087 ,  C07F9/588 ,  C07F9/650964 ,  C07F9/650988 ,  C07F9/65182 ,  C07F9/6539 ,  C07F9/65515 ,  C07F9/655345 ,  C07F9/65583 ,  C07F9/65586 ,  C12Q1/37 ,  G01N2333/96433

    摘要： The present invention relates to novel compounds and probes which have a common chemical structure necessary to obtain potent inhibitory activity against KLK4 and/or may be used for the detection of KLK4 peptides and their activity. It further relates to the use of these compounds and methods for inhibiting and/or detecting KLK4 activity in vitro and in vivo by making use of said probes or inhibitors. The compounds of the invention differ from prior art compounds at least in the presence of phenyl guanidine (instead of e.g. benzyl guanidine) and/or the presence of a heteroatom in the tail group, their combined presence unexpectedly leading to potent and selective KLK4 inhibitory activity.

    摘要翻译： 本发明涉及具有获得对KLK4的有效抑制活性所必需的共同化学结构和/或可用于检测KLK4肽及其活性的新型化合物和探针。 它还涉及这些化合物和方法在体外和体内通过利用所述探针或抑制剂来抑制和/或检测KLK4活性的用途。 本发明的化合物至少在苯胍（而不是例如苄基胍）和/或尾组中存在杂原子的情况下与现有技术化合物不同，它们的组合存在意外地导致有效和选择性的KLK4抑制活性 。