LANTHANIDE METAL CHELATE SECURITY FEATURE
    3.
    发明申请

    公开(公告)号:WO2021211706A1

    公开(公告)日:2021-10-21

    申请号:PCT/US2021/027283

    申请日:2021-04-14

    摘要: A chelate and associated security feature including a lanthanide metal and a ligand of formula (1), formula (2), or formula (3), where each of R1-R7 in formula (1) is independently selected from the group consisting of H, OH, NH2, Cl, F, OMe, OAr, OCF3, CF3, alkyl, aryl, phenyl, OPh, and heteroaromatic, where each of R1-R5 in formula (2) is independently selected from the group consisting of H, OH, NH2, Cl, F, OMe, OAr, OCF3, CF3, NMe2, ON, alkyl, aryl, phenyl, OPh, and heteroaromatic, and where Re in formula (2) is selected from the group consisting of H, ΝH2, Cl, F, OMe, OAr, OCF3, CF3, NMe2, CN, alkyl, aryl, phenyl, OPh, and heteroaromatic, and where each of R1-R5 in formula (3) is independently selected from the group consisting of H, OH, NH2, Cl, F, OMe, OAr, OCF3, CF3, alkyl, aryl, phenyl, OPh, and heteroaromatic.

    NOVEL SUBSTITUTED SULFONYLUREA DERIVATIVES
    6.
    发明申请

    公开(公告)号:WO2019043610A1

    公开(公告)日:2019-03-07

    申请号:PCT/IB2018/056619

    申请日:2018-08-30

    摘要: The present invention relates to novel heterocyclic compounds of the general formula (I) their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers and polymorphs. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds and their use as the compounds of the invention belong to the family of NOD-like receptor family (NLR) protein NLRP3 modulators. The present invention thus relates to novel NLRP3 modulators as well as to the use of the novel inhibitor compounds in the treatment of diseases or conditions as well as treatment of disease states mediated by NLRP3 as well as treatment of diseases or conditions in which interleukin 1β activity and interleukin-18 (IL-18) is implicated.

    IN SITU VISUALIZATION OF KINASE ACTIVITY
    9.
    发明申请
    IN SITU VISUALIZATION OF KINASE ACTIVITY 审中-公开
    激酶活性的现场可视化

    公开(公告)号:WO2018035296A1

    公开(公告)日:2018-02-22

    申请号:PCT/US2017/047297

    申请日:2017-08-17

    摘要: Kinases can be engineered to utilize an ATP analog that is not readily utilized by wild-type kinases by introducing a mutation in the ATP-binding pocket. However, application of this method has been limited by the membrane impermeability of the ATP analog. Provided herein are methods for in situ visualization of substrates of an analog-sensitive kinase, the method comprising a mild fixation step. Also provided herein are kits comprising a fixative, an ATP analog, and an agent for detecting the substrates modified by the ATP analog.

    摘要翻译: 通过在ATP结合口袋中引入突变,可以将激酶设计成利用野生型激酶不易利用的ATP类似物。 然而,该方法的应用受到ATP类似物膜不可渗透性的限制。 本文提供了用于原位显现模拟敏感激酶底物的方法,所述方法包括温和固定步骤。 本文还提供了包含固定剂,ATP类似物和用于检测由ATP类似物修饰的底物的试剂的试剂盒。

    NOVEL BENZOTHIAZOLE DERIVATIVES WITH ENHANCED BIOLOGICAL ACTIVITY
    10.
    发明申请
    NOVEL BENZOTHIAZOLE DERIVATIVES WITH ENHANCED BIOLOGICAL ACTIVITY 审中-公开
    具有增强生物活性的新型苯并噻唑衍生物

    公开(公告)号:WO2017025980A3

    公开(公告)日:2017-04-06

    申请号:PCT/IN2016000207

    申请日:2016-08-12

    IPC分类号: C07D277/62

    摘要: The present invention discloses novel conjugates of benzothiazole derivatives with cystine and glucosamine and their method of synthesis. Their method of synthesis is easy and eco-friendly, avoiding the use of hazardous materials or reactions, The compounds offer technical advantages of increased solubility, potency, selectivity and biological activity. The novel compounds show antibacterial, antifungal and anticancer activities. Formula, physico-chemical data and biological activity of the novel derivatives are as given in Tables 1 to 9.

    摘要翻译: 本发明公开了苯并噻唑衍生物与胱氨酸和葡糖胺的新型结合物及其合成方法。 它们的合成方法简单且环保,避免使用有害物质或反应。这些化合物具有提高溶解度,效力,选择性和生物活性的技术优势。 这些新化合物显示出抗菌,抗真菌和抗癌活性。 新型衍生物的分子式,物理化学数据和生物活性如表1至9所示。