A crystalline form of (S)-2-((3-((benzo[d][1,3]dioxol-5-yl)methyl)benzyl)- amino)propanamide

By preparing multiple crystal forms of (S)-2-((3-((benzo[d][1,3]dioxopenta-5-oxo)methyl)benzyl)-amino)propionamide, the problems of water solubility, hygroscopicity and stability of the compound were solved, and its drugability as a drug was improved, especially for the treatment of neuropathic pain.

CN122127303APending Publication Date: 2026-06-02ACADEMY OF MILITARY MEDICAL SCIENCES
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Patent Information

Application Number
CN202610442170.8
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-04-03
Publication Date
2026-06-02

AI Technical Summary

Technical Problem

Existing (S)-2-((3-((benzo[d][1,3]dioxopentane-5-oxo)methyl)benzyl)-amino)propionamide compounds suffer from poor water solubility, high hygroscopicity, and poor stability, which affect their drug-like properties as drug molecules.

Method used

Multiple crystal forms A, B, C, D, E, F, and G were developed. Through reactions of different acids with free bases, compound crystal forms with high solubility, low hygroscopicity, excellent stability, and improved bioavailability were prepared.

Benefits of technology

This study achieves high solubility, low hygroscopicity, excellent stability, and improved bioavailability of the compound, making it suitable for drug preparation and applicable to the treatment of neuropathic pain.

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Abstract

The present application relates to S ) -2-((3-((benzo[ d [1,3]dioxolane-5-oxomethyl)benzyl)-amino)propanamide, to pharmaceutical compositions containing it, and to the use of this crystalline form for the preparation of a medicament for the prevention and / or treatment of pain (e.g. neuropathic pain, including chronic neuropathic pain or neuropathological pain).
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Citation Information

Patent Citations

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    CN104761531A