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    • 44. 发明授权
    • Photographic products and processes employing novel nondiffusible
pyridylazo(dialkylamino) phenol magenta dye-releasing compounds and
precursors thereof
    • 使用新型非扩散性吡啶基偶氮(二烷基氨基)苯酚洋红色染料释放化合物及其前体的摄影产品和方法
    • US4357410A
    • 1982-11-02
    • US282611
    • 1981-07-13
    • Richard B. AndersonNorman W. Kalenda
    • Richard B. AndersonNorman W. Kalenda
    • C09B29/09C09B29/00C09B29/26G03C8/10G03C1/40G03C1/10G03C5/54G03C7/00
    • C09B29/0048C09B29/26G03C8/10
    • Photographic elements, diffusion transfer assemblages and processes are described which employ a novel nondiffusible compound having a releasable, pyridylazo(dialkylamino)phenol magenta dye moiety or precursor thereof, having the formula: ##STR1## wherein: (a) R represents hydrogen, a hydrolyzable moiety, or may be taken together with the NHSO.sub.2 group to which it is attached to form CAR;(b) R.sup.1 represents hydrogen, a hydrolyzable moiety or CAR;(c) R.sup.2 and R.sup.3 each independently represents hydrogen, CAR, an alkyl group of 1 to about 6 carbon atoms, or they can be taken together with the nitrogen to which they are attached to form a 5- or 6-membered heterocyclic ring, or one of R.sup.2 and R.sup.3 can be an aryl group having from 6 to about 10 carbon atoms; and(d) CAR represents a ballasted carrier moiety capable of releasing the diffusible magenta dye moiety or precursor thereof under alkaline conditions;with the proviso that at least one of R, R.sup.1, R.sup.2 and R.sup.3 is CAR.
    • 描述了摄影元件,扩散转移组合和方法,其采用具有下列通式的可释放的吡啶基偶氮(二烷基氨基)苯酚洋红染料部分或其前体的新型不扩散化合物:其中:(a)R表示氢,可水解 或者可以与其连接的NHSO 2基团一起形成CAR; (b)R1表示氢,可水解部分或CAR; (c)R 2和R 3各自独立地表示氢,CAR,1至约6个碳原子的烷基,或者它们可以与它们所连接的氮一起形成5-或6-元杂环, 或者R 2和R 3中的一个可以是具有6至约10个碳原子的芳基; 和(d)CAR表示在碱性条件下能够释放可扩散品红染料部分或其前体的压载载体部分; 条件是R,R 1,R 2和R 3中的至少一个为CAR。
    • 50. 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。