Title:
SOS1 DEGRADATION AGENT AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/223034
Kind Code:
A1
Abstract:
An SOS1 degradation agent and a preparation method therefor and an application thereof. Specifically, disclosed is a compound of formula I: S-L-E(I), wherein L is a linking chain, which links S and E by means of covalent bonds; E is a small molecule ligand of an E3 ubiquitin ligase complex; and S is the structure shown in S7. The compound of formula I is capable of degrading and/or inhibiting SOS1 protein in cells, and can be used for treating and/or preventing related diseases or conditions mediated by SOS1 or caused by interaction of SOS1 and Ras, or SOS1 and Rac.
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Inventors:
YE ZHENGQING (CN)
FENG YAN (CN)
LI SHIQIANG (CN)
DING CHENLI (CN)
WANG QIAO (CN)
WEI HONG (CN)
XIE SHUCHEN (CN)
FENG YAN (CN)
LI SHIQIANG (CN)
DING CHENLI (CN)
WANG QIAO (CN)
WEI HONG (CN)
XIE SHUCHEN (CN)
Application Number:
PCT/CN2022/088561
Publication Date:
October 27, 2022
Filing Date:
April 22, 2022
Export Citation:
Assignee:
SHANGHAI LEADINGTAC PHARMACEUTICAL CO LTD (CN)
International Classes:
C07D239/94; A61K31/517; A61P35/00; C07D409/14
Domestic Patent References:
WO2022061348A1 | 2022-03-24 | |||
WO2018172250A1 | 2018-09-27 | |||
WO2019140380A1 | 2019-07-18 | |||
WO2018115380A1 | 2018-06-28 |
Foreign References:
CN112218859A | 2021-01-12 |
Other References:
ZHOU, CHUAN ET AL.: "Discovery of the First-in-Class Agonist-Based SOS1 PROTACs Effective in Human Cancer Cells Harboring Various KRAS Mutations.", J. MED. CHEM., vol. 65, 1 March 2022 (2022-03-01), pages 3923 - 3942, XP055978386, DOI: 10.1021/acs.jmedchem.1c01774
HILLIG, R. C. ET AL.: "Discovery of Potent SOS1 Inhibitors that Block RAS Activation Via Disruption of the RAS–SOS1 Interaction.", PNAS, vol. 116, no. 7, 12 February 2019 (2019-02-12), pages 2551 - 2560, XP055841142, DOI: 10.1073/pnas.1812963116
HILLIG, R. C. ET AL.: "Discovery of Potent SOS1 Inhibitors that Block RAS Activation Via Disruption of the RAS–SOS1 Interaction.", PNAS, vol. 116, no. 7, 12 February 2019 (2019-02-12), pages 2551 - 2560, XP055841142, DOI: 10.1073/pnas.1812963116
Attorney, Agent or Firm:
SHANGHAI BESHINING LAW OFFICE (CN)
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