[EN] MODULATORS OF BTK PROTEOLYSIS AND METHODS OF USE<br/>[FR] MODULATEURS DE PROTÉOLYSE DE BTK ET PROCÉDÉS D'UTILISATION
申请人:UNIV YALE
公开号:WO2019177902A1
公开(公告)日:2019-09-19
The present disclosure relates to bifunctional compounds, which find utility as modulators of Burton's Tyrosine Kinase (BTK). In particular, the present disclosure is directed to bifunctional compounds. One end of a bifunctional compound includes a Von Hippel-Lindau, Cereblon, Inhibitors of Apotosis Proteins, or Mouse Double-Minute Homolog 2 ligand that binds to the respective E3 ubiquitin ligase. The other end of a bifunctional compound includes a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. Diseases or disorders that result from aggregation, accumulation, and/or overactivation of the target protein can be treated or prevented with compounds and compositions of the present disclosure.
Metal-Free Three-Component Oxyalkynylation of Alkenes
作者:Yangshan Li、Ran Lu、Shutao Sun、Lei Liu
DOI:10.1021/acs.orglett.8b02954
日期:2018.11.2
An unprecedented (NH4)2S2O8 mediated metal-free three-componentalkene oxyalkynylation using H2O or alcohol as oxygenation agent is described. Mechanistic studies suggested that the reversed regioselectivity should be dictated by an alkene radical cation intermediate.
描述了前所未有的(NH 4)2 S 2 O 8介导的使用H 2 O或醇作为氧化剂的无金属三组分链烯氧基炔基化反应。机理研究表明,逆向的区域选择性应由烯烃自由基阳离子中间体决定。