Phenylthiazolamine-based PI4KIIIβ inhibitor, preparation method therefor, pharmaceutical composition thereof and use thereof
By designing phenylthiazolid PI4KIIIβ inhibitors, the existing PI4KIIIβ inhibitors are solved, and the effective inhibition and anti-tumor activity of PI4KIIIβ enzymes is achieved, reducing costs and side effects.
WO2025148459A1 Publication Date: 2025-07-17NANJING HONGSHUN PHARMACEUTICAL TECHNOLOGY CO LTD +1
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Patent Information
- Application Number
- PCT/CN2024/125722
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2024-01-09
- Filing Date
- 2024-10-18
- Publication Date
- 2025-07-17
AI Technical Summary
Technical Problem
Existing PI4KIIIβ inhibitors are rarely studied in cancer treatment, and there is a lack of efficient PI4KIIIβ inhibitors for inhibiting PI3K/Akt/mTOR signaling pathways, and traditional treatments such as surgery, chemotherapy and radiation therapy have side effects and insufficient selectivity.
Method used
The development of phenylthiazolid PI4KIIIβ inhibitors has improved the inhibitory activity of PI4KIIIβ by optimizing substituent group design and combined with pharmaceutically acceptable salt and isomer forms to reduce costs and side effects.
Benefits of technology
It achieves efficient inhibition of PI4KIII β enzyme, significant anti-tumor activity, reduces the use dose and production costs, and reduces side effects.
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Abstract
Disclosed in the present invention is a phenylthiazolamine-based PI4KIIIβ inhibitor. The inhibitor is a substituted phenylthiazoleamine-based compound represented by general formula V, or a stereoisomer, hydrate, or pharmaceutically acceptable salt thereof. The inhibitor has the characteristic of effectively inhibiting a PI3K / Akt / mTOR signaling pathway of PI4KIII β, and has efficient and excellent PI4KIII β enzyme inhibitory activity, low costs, high efficacy, low toxicity, and a high yield of an intermediate product during synthesis, reducing resource waste, thus facilitating cost reduction; and the inhibitor has a small dosage requirement and significant activity when applied to anti-tumor drugs.
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