公开(公告)号：US20170122958A1

公开(公告)日：2017-05-04

申请号：US15039350

申请日：2014-11-28

申请人： University of Dundee ,  Cambridge Enterprise Limited

发明人： Enrique Lin Shiao ,  Matthias Gerard Jacky Baud ,  Alessio Ciulli ,  Kwok-Ho Chan ,  Michael Zengerle

IPC分类号： G01N33/68 ,  C07D487/04 ,  C12N15/10

CPC分类号： G01N33/6803 ,  A61K31/5517 ,  C07D487/04 ,  C12N15/102 ,  G01N2500/04

摘要： A method of selectively inhibiting a bromodomain in the presence of other bromodomains comprising introducing a functionally silent mutation into the bromodomain in the presence of other wild type bromodomains and selectively inhibiting the mutated bromodomain.

公开(公告)号：US11179373B2

公开(公告)日：2021-11-23

申请号：US15557525

申请日：2016-03-14

申请人： University of Dundee

发明人： Alessio Ciulli ,  Michael Zengerle ,  Kwok-Ho Chan

IPC分类号： A61K31/426 ,  A61K31/4025 ,  A61K31/4196 ,  A61K31/381 ,  A61K31/551 ,  A61K31/16 ,  C07D417/14 ,  C07D417/12 ,  C07D487/04 ,  C07D495/14

摘要： There is provided novel small molecule E3 ubiquitin ligase protein binding ligand compounds, having utility in PROteolysis Targeted Chimeras (PROTACs), as well as processes for the preparation thereof, and use in medicine. There is particularly provided PROTACs which bind to a protein within the bromo- and Extra-terminal (BET) family of proteins, and especially to PROTACs including novel small molecule E3 ubiquitin ligase protein binding ligand compounds which selectively induce degradation of the BRD4 protein within the bromodomain of the BET family of proteins.