Title:
DEGRADATION OF ANDROGEN RECEPTOR (AR) BY CONJUGATION OF AR ANTAGONISTS WITH E3 LIGASE LIGAND AND METHODS OF USE
Document Type and Number:
WIPO Patent Application WO/2021/058017
Kind Code:
A1
Abstract:
Provided herein are novel bifunctional compounds formed by conjugating AR antagonist moieties with E3 ligase Ligand moieties, which function to recruit targeted proteins to E3 Ubiquitin ligase for degradation, and methods of preparation and uses thereof.
Inventors:
WANG HEXIANG (CN)
HUO CHANGXIN (CN)
QIU MING (CN)
WANG ZHIWEI (CN)
HUO CHANGXIN (CN)
QIU MING (CN)
WANG ZHIWEI (CN)
Application Number:
PCT/CN2020/118664
Publication Date:
April 01, 2021
Filing Date:
September 29, 2020
Export Citation:
Assignee:
BEIGENE LTD (KY)
WANG HEXIANG (CN)
WANG HEXIANG (CN)
International Classes:
C07D471/04; A61P35/00; C07D487/04
Domestic Patent References:
| WO2018098288A1 | 2018-05-31 | |||
| WO2017197056A1 | 2017-11-16 |
Foreign References:
| US20160244444A1 | 2016-08-25 | |||
| US20180312505A1 | 2018-11-01 | |||
| CN106727588A | 2017-05-31 |
Other References:
CHIARA MANIACI, SCOTT J. HUGHES, ANDREA TESTA, WENZHANG CHEN, DOUGLAS J. LAMONT, SONIA ROCHA, DARIO R. ALESSI, ROBERTO ROMEO, ALES: "Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation", NATURE COMMUNICATIONS, NATURE PUBLISHING GROUP, GB, vol. 8, no. 1, 10 December 2017 (2017-12-10), GB, XP055476041, ISSN: 2041-1723, DOI: 10.1038/s41467-017-00954-1
Attorney, Agent or Firm:
WU, FENG & ZHANG (CN)
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