Stereoisomers and deuterated derivatives of pyrazoloquinazoline compounds and uses thereof
By stereocyclizing and deuterating onvansertib, pyrazoloquinoline compounds were developed, which solved the problem of poor oral absorption and bioavailability of PLK1 inhibitors in clinical applications, achieving therapeutic effects with lower toxicity and better efficacy.
CN122404375APending Publication Date: 2026-07-17PHIL RIVERS TECH LTD
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Patent Information
- Application Number
- CN202610672711.6
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2023-04-20
- Filing Date
- 2024-01-17
- Publication Date
- 2026-07-17
AI Technical Summary
Technical Problem
Existing PLK1 inhibitors, such as onvansertib, suffer from poor oral absorption and bioavailability in clinical applications, resulting in significant differences in their efficacy and safety as a cancer treatment.
Method used
Stereoisomers and deuterated derivatives of pyrazoloquinoline compounds were developed by stereocyclization and deuteration of onvansertib, which optimized its oral absorption and bioavailability, reduced toxicity, and improved efficacy.
Benefits of technology
The improved compound showed lower toxicity and better efficacy in multiple animal studies, providing a wider range of effective molecules for different types of diseases and improving the treatment of diseases related to PLK1 dysregulation.
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Abstract
本公开提供了式 (I) 化合物的立体异构体、氘代衍生物或立体异构氘代衍生物，或其药学上可接受的盐、溶剂化物，其中R1和R2如本文所述，其可用作PLK1抑制剂，还提供了包含其的药物组合物，以及在治疗PLK1活性失调导致的疾病和病状和 / 或与PLK1相关的疾病和病状例如癌症中的用途。(I)
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