Salts and solid forms of cdk inhibitors
By developing polymorphic and salt forms of compound (I), the stability and solubility issues of existing CDK inhibitors have been resolved, enabling their effective application in the treatment of cancer and other diseases.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- GENENTECH INC
- Filing Date
- 2024-11-28
- Publication Date
- 2026-06-19
AI Technical Summary
Existing CDK inhibitors suffer from poor stability, low solubility, and high hygroscopicity during preparation and application, which affects their efficacy in treating cell proliferative diseases such as cancer.
Multiple crystalline and pharmaceutically acceptable salt forms of compound (I), including anhydrous and hydrate forms, were developed. Multiple polymorphic forms were identified by X-ray powder diffraction (XRPD) and thermogravimetric analysis (TGA). Form I and HCl salt form II, which have high stability and high solubility, were selected to improve its solid-state properties.
It improves the physical and chemical stability of compound (I), enhances its solubility in simulated gastrointestinal fluids, prolongs storage stability, and improves bioavailability, making it suitable for formulation manufacturing and administration.
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