3,4-dihydroisoquinoline compound and use thereof
Novel 3,4-dihydroisoquinoline compounds with specific structural modifications exhibit enhanced PRMT5 inhibition and in vivo antitumor activity, addressing the limitations of current PRMT5 inhibitors.
CA3174311CActive Publication Date: 2026-07-07CSPC ZHONGQI PHARMACEUTICAL TECHNOLOGY (SHIJIAZHUANG) CO LTD
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Patent Information
- Authority / Receiving Office
- CA · CA
- Patent Type
- Patents
- Current Assignee / Owner
- CSPC ZHONGQI PHARMACEUTICAL TECHNOLOGY (SHIJIAZHUANG) CO LTD
- Filing Date
- 2021-06-01
- Publication Date
- 2026-07-07
AI Technical Summary
Technical Problem
Current PRMT5 inhibitors lack effective inhibitory activities against PRMT5 and tumor cells, particularly in terms of in vivo antitumor activity and oral administration performance.
Method used
Development of structurally novel 3,4-dihydroisoquinoline compounds, represented by formula (I), which include specific substituents and functional groups, such as pyrimidine rings and various cycloalkyl and heterocyclyl moieties, to enhance inhibitory activities against PRMT5 and tumor cells.
Benefits of technology
The novel compounds demonstrate better inhibitory activities against PRMT5 and MV4-11 cells in vitro, significant anti-tumor activity in vivo, and improved oral administration performance compared to existing drugs like GSK3326595.
✦ Generated by Eureka AI based on patent content.
Abstract
Provided in the present invention are a compound as represented by formula (I), or a pharmaceutically acceptable salt, a tautomer, a geometrical isomer, an optical isomer, a solvate or an isotopic derivative thereof, and the use thereof. The compound of the present invention has a significant inhibitory activity on PRMT5, has a significant inhibitory effect on tumor cells and in vivo tumor models, also has a good administration performance, and has clinical application potential for preventing and / or treating diseases which are at least partially mediated by PRMT5.
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