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    AZOARYLS AS REVERSIBLY MODULATABLE TUBULIN INHIBITORS
    8.
    发明公开
    AZOARYLS AS REVERSIBLY MODULATABLE TUBULIN INHIBITORS 审中-公开
    AZOARYLE ALS REVERSIBEL MODULIERBARE TUBULININHIBITOREN

    公开(公告)号：EP3137554A1

    公开(公告)日：2017-03-08

    申请号：EP14747127.0

    申请日：2014-04-29

    申请人： Ecole Normale Supérieure de Lyon ,  Université Claude Bernard Lyon 1 ,  Centre National de la Recherche Scientifique ,  Ludwig-Maximilians-Universität München

    发明人： THORN-SESHOLD, Oliver ,  BOROWIAK, Malgorzata ,  TRAUNER, Dirk ,  HASSERODT, Jens

    IPC分类号： C09B29/01 ,  A61K41/00 ,  C09B29/08

    CPC分类号： C09B29/12 ,  A61K41/0042 ,  C09B29/0003 ,  C09B29/0014 ,  C09B29/0048 ,  C09B29/081 ,  C09B29/26 ,  G01N33/582

    摘要： as defined in Claim 1, which may be fully reversibly interconverted between non-tubulin-binding trans and tubulin-binding as isomeric forms, either by irradiation or spontaneously. The invention also concerns compounds with a azoaryl structure for use in studying the cytoskeleton and/or its associated processes, or in the treatment of a disease for which a tubulin polymerisation inhibition activity has a beneficial effect, wherein the compound is administered to the cell, organism or patient in need of such treatment in the trans form of the diazenyl bond, and where this trans form is inactive as regards a tubulin polymerisation inhibition effect, and where after photoisomerisation in vitro, in cellulo or in vivo to an azoaryl compound in its cis isomeric form of the diazenyl bond by the application of light, optionally with modification in vitro, in cellulo or in vivo of one or more substituents, the resultant cis form is active as regards a tubulin polymerisation inhibition effect.

    摘要翻译： 如权利要求1所定义，其可以通过照射或自发地在非微管蛋白结合反式和微管蛋白结合之间完全可逆地相互转化为异构形式。 本发明还涉及具有用于研究细胞骨架和/或其相关过程的偶氮芳族结构的化合物或治疗其中微管蛋白聚合抑制活性具有有益作用的疾病，其中将化合物施用于细胞， 生物体或患者需要以二氮烯基键的反式形式进行这种治疗，并且其中该反式形式在微管蛋白聚合抑制作用方面是无活性的，并且其中在体外光解异构化后，在纤维素中或在其体内对其中的偶氮芳基化合物 通过在纤维素或体内一个或多个取代基的应用光，任选地在体外进行修饰，所述顺式形式对于微管蛋白聚合抑制作用是有活性的，所述顺式异构体形式为二氮烯基键。