Preparation method for salt of cyclic carbonate nucleoside compound and crystal form thereof

Stable cyclic carbonate nucleoside compounds were prepared by forming salts with acids, especially hydrobromide, which solved the problems of poor stability and water solubility of cyclic carbonate nucleoside compounds at room temperature, and enabled effective treatment of viruses such as the novel coronavirus.

WO2026031273A1 Publication Date: 2026-02-12GUANGDONG CHENKANG BIOTECHNOLOGY CO LTD
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Patent Information

Application Number
PCT/CN2024/113198
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-08-06
Filing Date
2024-08-19
Publication Date
2026-02-12

AI Technical Summary

Technical Problem

Existing cyclic carbonate nucleoside compounds are viscous gels at room temperature, poorly soluble in water, have poor chemical stability and poor drug-like properties, and are difficult to effectively treat diseases caused by novel coronavirus, feline infectious peritonitis virus, respiratory syncytial virus, and porcine epidemic diarrhea virus.

Method used

By forming salts with various acids, especially hydrobromide, cyclic carbonate nucleoside compound salts with crystal form A or crystal form B are prepared, thereby improving their physical and chemical stability, water solubility and solid properties, reducing hygroscopicity, and enhancing oral bioavailability.

Benefits of technology

The prepared cyclic carbonate nucleoside compound salts exhibit good physical and chemical stability, significantly improved water solubility, reduced hygroscopicity, and enhanced oral bioavailability, making them suitable for treating diseases caused by novel coronavirus, feline infectious peritonitis virus, respiratory syncytial virus, and porcine epidemic diarrhea virus.

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Abstract

The present invention relates to the technical field of medicine and relates to a salt of a cyclic carbonate nucleoside compound and a crystal thereof, and a preparation method therefor and a use thereof. The salt of the cyclic carbonate nucleoside compound has a structure represented by formula I. When Y is hydrobromic acid and n=1, the salt of the nucleoside compound exists in crystal form A or crystal form B. Crystal form A has the advantages of good physical and chemical stability, good solid-state properties, good water solubility, low hygroscopicity, high oral bioavailability, etc., and can be used in the preparation of a drug for treating and / or alleviating related diseases caused by viruses (especially novel coronavirus, feline infectious peritonitis virus, respiratory syncytial virus, porcine epidemic diarrhea virus, feline calicivirus, etc.).
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