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.

公开(公告)号：US20210163469A1

公开(公告)日：2021-06-03

申请号：US16604737

申请日：2018-04-13

申请人： University of Dundee

发明人： Alessio Ciulli ,  Chiara Maniaci ,  Scott J. Hughes ,  Andrea Testa

IPC分类号： C07D417/14

摘要： Compounds having the general structure A-L-B are presented wherein A and B are independently an E3 ubiquitin ligase protein binding ligand compound of formula 1A or 1B. Pharmaceutical compositions comprising these compounds and methods of use are also presented.

公开(公告)号：US20220127257A1

公开(公告)日：2022-04-28

申请号：US17567280

申请日：2022-01-03

申请人： University of Dundee

发明人： Alessio Ciulli ,  Chiara Maniaci ,  Scott J. Hughes ,  Andrea Testa

IPC分类号： C07D417/14

摘要： Compounds having the general structure A-L-B are presented wherein A and B are independently an E3 ubiquitin ligase protein binding ligand compound of formula 1A or 1B. Pharmaceutical compositions comprising these compounds and methods of use are also presented.

公开(公告)号：US11234988B2

公开(公告)日：2022-02-01

申请号：US16333454

申请日：2017-09-14

申请人： UNIVERSITY OF DUNDEE

发明人： Alessio Ciulli ,  Andrea Testa

IPC分类号： C07D207/00 ,  A61K31/551 ,  A61K47/54 ,  A61K47/55 ,  A61K31/4709 ,  A61K45/06 ,  C07D207/46 ,  C07D417/12 ,  C07D417/14 ,  C07D495/14 ,  C07D207/16 ,  C07K5/062 ,  C07K5/087 ,  A61K31/427

摘要： There is provided novel small molecule E3 ubiquitin ligase protein binding ligand compounds, and to their utility in PROteolysis Targeted Chimeras (PROTACs), as well as processes for their preparation thereof, and use in medicine. There is particularly provided novel small molecule E3 ubiquitin ligase protein binding inhibitor compounds based on a fluorohydroxyproline scaffold, to their utility as ligands in synthesizing novel PROTACs, and to synthetic methods therefor.

公开(公告)号：US20240252654A1

公开(公告)日：2024-08-01

申请号：US18252083

申请日：2021-10-19

申请人： University of Dundee ,  Promega Corporation

发明人： Alessio Ciulli ,  Andrea Testa ,  Chiara Maniaci ,  Nikolai Makukhin ,  Satomi Imaide ,  Danette Daniels ,  Kristin Riching

IPC分类号： A61K47/55 ,  A61K47/60

CPC分类号： A61K47/55 ,  A61K47/60

摘要： This invention particularly relates to trifunctional PROTACs of formula I as described herein which bind to a protein within the Bromo- and Extra-Terminal (BET) family of proteins, and especially to PROTACs including small molecule E3 ubiquitin ligase protein binding ligand compounds which induce preferential degradation of the BRD2 protein within the bromodomain of the BET family of proteins.

公开(公告)号：US11261179B2

公开(公告)日：2022-03-01

申请号：US16604737

申请日：2018-04-13

申请人： University of Dundee

发明人： Alessio Ciulli ,  Chiara Maniaci ,  Scott J. Hughes ,  Andrea Testa

IPC分类号： C07D417/14

摘要： Compounds having the general structure A-L-B are presented wherein A and B are independently an E3 ubiquitin ligase protein binding ligand compound of formula 1A or 1B. Pharmaceutical compositions comprising these compounds and methods of use are also presented.

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.