Crystalline forms of nucleoside compounds

A novel crystalline form of ATV014 addresses solubility and stability issues, enhancing its therapeutic efficacy and storage stability, making it suitable for pharmaceutical applications.

JP7762931B2Active Publication Date: 2025-10-31SHENZHEN ANTIV PHARMA CO LTD
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Patent Information

Application Number
JP2024536512
Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Priority Date
2021-12-23
Filing Date
2022-05-17
Publication Date
2025-10-31
Estimated Expiration
2042-05-17

AI Technical Summary

Technical Problem

Existing forms of the nucleoside compound ATV014 lack optimal physicochemical properties such as solubility, stability, and bioavailability, which affect its therapeutic efficacy and storage stability.

Method used

Development of a novel crystalline form (Form I) of ATV014 with improved solubility, thermal stability, and low hygroscopicity, characterized by specific X-ray powder diffraction, differential scanning calorimetry, and thermogravimetric analysis patterns.

Benefits of technology

The novel crystalline form I exhibits enhanced stability under hygroscopic conditions, maintaining chemical purity and solubility, ensuring effective bioavailability and suitability for pharmaceutical formulations, particularly for treating viral infections like SARS-CoV-2.

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Abstract

The present invention provides a crystalline form of a nucleoside compound, which is crystalline form I of ATV014, which has good solubility and thermal stability, and has a better bioavailability and dissolution curve in certain formulations. Its good permeability and thermal stability make it suitable for use in certain pharmaceutical formulations.
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