PRMT5 inhibitors

CN119731162APending Publication Date: 2025-03-28BEIJING EARTHWISE TECH CO LTD
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Patent Information

Application Number
CN202380060543.X
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2023-08-09
Filing Date
2023-08-18
Publication Date
2025-03-28

AI Technical Summary

Technical Problem

Existing PRMT5 inhibitors have dose-limiting toxic and side effects, especially a greater impact on normal cells, and it is difficult to target MTAP-deficient tumor cells without affecting MTAP normal cells.

Method used

Develop an MTA synergistic inhibitor targeting the PRMT5/MTA complex, which can selectively inhibit PRMT5 activity, reduce the impact on the PRMT5/SAM complex, and improve the safety and effectiveness of the drug through excellent ADMET properties.

Benefits of technology

Effectively inhibits the activity of PRMT5 in tumor cells, reduces the toxic side effects on normal cells, improves the treatment window, improves the therapeutic effect on MTAP-deficient tumor cells, and reduces the impact on MTAP normal cells.

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Abstract

The invention provides a PRMT5 inhibitor as shown in a formula (I), or pharmaceutically acceptable salts, isotope variants, tautomers, stereoisomers, prodrugs, polymorphs, hydrates or solvates of the PRMT5 inhibitor, or pharmaceutically acceptable salts, isotope variants, tautomers, stereoisomers, prodrugs, polymorphs, hydrates or solvates of the PRMT5 inhibitor. The invention also provides a preparation method of the compound, a pharmaceutical composition containing the compound, and an effect of the compound in prevention and treatment of cancers. # imgabs0 #
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