Title:
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE
Document Type and Number:
WIPO Patent Application WO/2022/143856
Kind Code:
A1
Abstract:
Disclosed herein are novel bifunctional compounds formed by conjugating BTK 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:
HUO CHANGXIN (CN)
WANG HEXIANG (CN)
LV GANG (CN)
WANG ZHIWEI (CN)
LIU HUAQING (CN)
WANG HEXIANG (CN)
LV GANG (CN)
WANG ZHIWEI (CN)
LIU HUAQING (CN)
Application Number:
PCT/CN2021/142801
Publication Date:
July 07, 2022
Filing Date:
December 30, 2021
Export Citation:
Assignee:
BEIGENE LTD (GB)
HUO CHANGXIN (CN)
HUO CHANGXIN (CN)
International Classes:
A61K31/519; C07D487/04; A61P35/00; C07D519/00
Domestic Patent References:
| WO2021219070A1 | 2021-11-04 | |||
| WO2021180103A1 | 2021-09-16 | |||
| WO2021018018A1 | 2021-02-04 | |||
| WO2021053495A1 | 2021-03-25 | |||
| WO2020263935A1 | 2020-12-30 | |||
| WO2018098288A1 | 2018-05-31 | |||
| WO2020252397A1 | 2020-12-17 | |||
| WO2019148150A1 | 2019-08-01 | |||
| WO2007026720A1 | 2007-03-08 |
Foreign References:
| CN113387931A | 2021-09-14 | |||
| CN104884458A | 2015-09-02 | |||
| CN110845500A | 2020-02-28 |
Other References:
TAKAYAMA, T. ; UMEMIYA, H. ; AMADA, H. ; YABUUCHI, T. ; KOAMI, T. ; SHIOZAWA, F. ; OKA, Y. ; TAKAOKA, A. ; YAMAGUCHI, A. ; ENDO, M: "Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM NL, vol. 20, no. 1, 1 January 2010 (2010-01-01), Amsterdam NL , pages 112 - 116, XP026808784, ISSN: 0960-894X
Attorney, Agent or Firm:
WU, FENG & ZHANG (CN)
Download PDF: