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    • 10. 发明申请
    • AZOARYLS AS REVERSIBLY MODULATABLE TUBULIN INHIBITORS
    • AZOARYLS作为可逆调节的TUBULIN抑制剂
    • WO2015166295A1
    • 2015-11-05
    • PCT/IB2014/001246
    • 2014-04-29
    • ECOLE NORMALE SUPERIEURE DE LYONUNIVERSITE CLAUDE BERNARD LYON ICENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUELUDWIG-MAXIMILIANS-UNIVERSITÄT MUNCHEN
    • THORN-SESHOLD, OliverBOROWIAK, MalgorzataTRAUNER, DirkHASSERODT, Jens
    • C09B29/01A61K41/00C09B29/08
    • C09B29/12A61K41/0042C09B29/0003C09B29/0014C09B29/0048C09B29/081C09B29/26G01N33/582
    • The invention concerns a new class of tubulin polymerisation inhibitors and their applications in research and medicine, notably in chemotherapy. The invention proposes new azoaryl derivatives of formula (I): as defined in Claim 1, which may be fully reversibly interconverted between non-tubulin-binding trans and tubulin-binding cis 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.
    • 本发明涉及一类新型的微管蛋白聚合抑制剂及其在研究和医学中的应用,特别是化疗。 本发明提出了式(I)的新的偶氮芳基衍生物:如权利要求1所定义,其可以通过照射或自发地完全可逆地相互转化在非微管蛋白结合反式和微管蛋白结合的顺式异构体形式之间。 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基结构的化合物,或者治疗其中微管蛋白聚合抑制活性具有有益效果的疾病,其中该化合物被施用于细胞, 关于微管蛋白聚合抑制作用,并且其中在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,在纤维素中或体内将其转化成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。