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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/2022/012622
Kind Code:
A1
Abstract:
Disclosed herein 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)
WANG ZHIWEI (CN)
Application Number:
PCT/CN2021/106482
Publication Date:
January 20, 2022
Filing Date:
July 15, 2021
Export Citation:
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Assignee:
BEIGENE LTD (GB)
LEI BAILIN (CN)
International Classes:
C07D401/12; A61K31/4015; A61K31/403; A61K31/495; A61K31/496; A61K31/4965; A61K31/497; A61K31/506; A61K31/675; A61P35/00; C07D401/02; C07D401/14; C07D471/00; C07D487/00; C07F9/02; C07F9/50; C07F9/53; C07F11/00
Domestic Patent References:
WO2021036922A12021-03-04
WO2020200291A12020-10-08
WO2019113071A12019-06-13
WO2017204445A22017-11-30
WO2019040274A12019-02-28
WO2020113233A12020-06-04
WO2019015655A12019-01-24
Foreign References:
CN112079866A2020-12-15
CN109912655A2019-06-21
CN110684015A2020-01-14
CN109422733A2019-03-05
Other References:
SUN NING; REN CHAOWEI; KONG YING; ZHONG HUI; CHEN JINJU; LI YAN; ZHANG JIANSHUI; ZHOU YUEDONG; QIU XING; LIN HAIFAN; SONG XIAOLING: "Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, ELSEVIER, AMSTERDAM, NL, vol. 193, 29 February 2020 (2020-02-29), AMSTERDAM, NL , XP086118072, ISSN: 0223-5234, DOI: 10.1016/j.ejmech.2020.112190
CHUNG HYO KANG, DONG HO LEE, CHONG OCK LEE, JAE DU HA, CHI HOON PARK, JONG YEON HWANG: "Induced protein degradation of anaplastic lymphoma kinase (ALK) by proteolysis targeting chimera (PROTAC)", BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, ELSEVIER, AMSTERDAM NL, vol. 505, no. 2, 28 September 2018 (2018-09-28), Amsterdam NL , pages 542 - 547, XP055765181, ISSN: 0006-291X, DOI: 10.1016/j.bbrc.2018.09.169
Attorney, Agent or Firm:
WU, FENG & ZHANG (CN)
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