Title:
DEGRADATION OF (EGFR) BY CONJUGATION OF EGFR INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE
Document Type and Number:
WIPO Patent Application WO/2023/138607
Kind Code:
A1
Abstract:
Provided are novel bifunctional compounds formed by conjugating EGFR inhibitor 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:
LEI BAILIN (CN)
LIU HUAQING (CN)
HAN SONGZHE (CN)
ZHAO YIZHOU (CN)
WANG ZHIWEI (CN)
LIU HUAQING (CN)
HAN SONGZHE (CN)
ZHAO YIZHOU (CN)
WANG ZHIWEI (CN)
Application Number:
PCT/CN2023/072825
Publication Date:
July 27, 2023
Filing Date:
January 18, 2023
Export Citation:
Assignee:
BEIGENE LTD (GB)
LEI BAILIN (CN)
LEI BAILIN (CN)
International Classes:
C07D401/14; A61K31/496; A61K31/506; A61K31/675; A61P35/00; C07D401/12
Domestic Patent References:
| WO2022012623A1 | 2022-01-20 | |||
| WO2022012622A1 | 2022-01-20 | |||
| WO2022063106A1 | 2022-03-31 | |||
| WO2022068849A1 | 2022-04-07 | |||
| WO2022171123A1 | 2022-08-18 | |||
| WO2022228556A1 | 2022-11-03 | |||
| WO2019114770A1 | 2019-06-20 | |||
| WO2019015655A1 | 2019-01-24 | |||
| WO2016105518A1 | 2016-06-30 | |||
| WO2019196812A1 | 2019-10-17 | |||
| WO2020216371A1 | 2020-10-29 |
Other References:
SUN, N. ET AL.: "Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 193, 29 February 2020 (2020-02-29), XP086118072, DOI: 10.1016/j.ejmech.2020.112190
Attorney, Agent or Firm:
WU, FENG & ZHANG (CN)
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