The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
Triarylmethane Fluorophores Resistant to Oxidative Photobluing
作者:Alexey N. Butkevich、Mariano L. Bossi、Gražvydas Lukinavičius、Stefan W. Hell
DOI:10.1021/jacs.8b11036
日期:2019.1.16
Spectral stability of small-molecule fluorescent probes is required for correct interpretation and reproducibility of multicolor fluorescence imaging data, in particular under high (de)excitation light intensities of super-resolutionimaging or in single-molecule applications. We propose a synthetic approach to a series of spectrally stable rhodamine fluorophores based on sequential Ru- and Cu-catalyzed
多色荧光成像数据的正确解释和再现需要小分子荧光探针的光谱稳定性,特别是在超分辨率成像的高(去)激发光强度下或在单分子应用中。我们提出了一种基于连续 Ru 和 Cu 催化转化的一系列光谱稳定罗丹明荧光团的合成方法,使用化学计量分析在其他荧光团的背景下评估它们对光漂白和光转换的稳定性,并证明了荧光团光产物的化学反应性。已经确定了提供抗光转换三芳基甲烷荧光团的取代模式,并证明了非蓝色标记在活细胞 STED 纳米显微镜中的适用性。
Compounds of formula (I) as described hereinprocesses for their production and their use as anti-cancer agents.
本文描述的式(I)化合物,其生产方法及其作为抗癌药物的用途。
[EN] TRIOXACARCIN-ANTIBODY CONJUGATES AND USES THEREOF<br/>[FR] CONJUGUÉS TRIOXACARCINE-ANTICORPS ET UTILISATIONS ASSOCIÉES
申请人:HARVARD COLLEGE
公开号:WO2019032961A1
公开(公告)日:2019-02-14
Provided herein are trioxacarcin-antibody drug conjugates of Formula (I): and pharmaceutically acceptable salts thereof, wherein R7 is -L-B, wherein L is a linking group, and B is an antibody or antibody fragment. Also provided are methods of preparing the antibody-drug conjugates, pharmaceutically acceptable compositions thereof, and methods of their use and treatment. Further provided are precursors to the trioxacarcin- antibody drug conjugates (e.g., compounds of Formula (II), novel trioxacarcins without an antibody conjugated thereto), pharmaceutical compositions thereof, and methods of their use and treatment.
[EN] ACYCLIC CYANOETHYLPYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS<br/>[FR] CYANOÉTHYLPYRAZOLO PYRIDONES ACYCLIQUES EN TANT QU'INHIBITEURS DE JANUS KINASE
申请人:MERCK SHARP & DOHME
公开号:WO2014146493A1
公开(公告)日:2014-09-25
The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.