Pharmaceutically acceptable salts of substituted tetrahydrofuran derivatives, crystalline forms thereof and uses thereof

By preparing various medicinal salts of compound 1, the problem of its unsatisfactory physicochemical properties was solved, and a more stable and effective analgesic effect was achieved, which is suitable for treating various types of pain such as chronic pain, acute pain, and inflammatory pain.

CN120040431BActive Publication Date: 2026-06-09SHANDONG SUNCADIA MEDICINE CO LTD

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANDONG SUNCADIA MEDICINE CO LTD
Filing Date
2025-02-21
Publication Date
2026-06-09

AI Technical Summary

Technical Problem

Existing Nav1.8 inhibitors have undesirable defects in terms of drug physicochemical and biological properties, which affects their application in clinical treatment.

Method used

Pharmaceutically usable salts of compounds of Formula 1 were developed, including hydrochloride, sulfate, phosphate, methanesulfonate, p-toluenesulfonate, maleate, fumarate and tartrate, etc., and polymorphs were prepared by different chemical ratios and solvent systems to optimize their physicochemical properties.

Benefits of technology

The stability and pharmaceutical properties of the compound were improved, making it more suitable for industrial production and biological activity. It has analgesic effects and is suitable for treating a variety of pain types.

✦ Generated by Eureka AI based on patent content.

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Abstract

The present disclosure relates to a pharmaceutically acceptable salt of a substituted tetrahydrofuran derivative, a crystalline form thereof and uses. Specifically, the present disclosure provides a pharmaceutically acceptable salt of (2R, 3S, 4S, 5R)-3-(3, 4-difluoro-2-methoxyphenyl)-N-(2-((Z)-(N'-hydroxymethylcarbamimidoyl)pyridin-4-yl)-4, 5-dimethyl-5-(trifluoromethyl)tetrahydrofuran-2-carboxamide, a crystalline form thereof and a preparation method thereof, and the corresponding salt has good stability and can be better used for clinical treatment.
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