Arylamide compounds based on benzene ring supramolecular interactions, self-assembled morphologies and uses

By designing a self-assembly structure of aryl amide compounds with π-π stacking interaction, the problem of existing local anesthetic drugs being difficult to achieve long-lasting effects and having high toxicity was solved, achieving a low-toxicity and long-lasting local anesthetic effect.

CN113396139BActive Publication Date: 2026-07-24易天奇 +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
易天奇
Filing Date
2020-01-13
Publication Date
2026-07-24

AI Technical Summary

Technical Problem

Existing local anesthetics are difficult to achieve long-lasting local anesthesia and have problems with neuropathological toxicity and systemic toxicity, which cannot meet clinical needs.

Method used

A class of aryl amide compounds with atypical asymmetric gemini surfactant structures were designed. By self-assembling in water to form a supramolecular structure with π-π stacking, sustained-release and long-acting local anesthetic effects are achieved through anion exchange mechanisms, while reducing toxicity.

Benefits of technology

It achieves long-lasting local anesthesia, significantly reduces local and systemic toxicity, and meets the clinical need for long-lasting local anesthesia.

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Abstract

Arylamide compounds based on benzene ring supramolecular effect, self-assembly morphology and use. The structure of the compounds is shown in formula (I) and (II), which can self-assemble into spherical micelles and Janus particles with strong intermolecular π-π stacking effect in aqueous solvent, and can exert long-term local anesthetic effect in vivo, the local anesthetic and / or analgesic effect time can be more than 48 hours, the local neuropathic toxicity and systemic toxicity are significantly lower than the published long-acting local anesthetic molecules. As a biomaterial that can self-assemble into micelles in water and has local anesthetic effect, it can also be used as a formulation aid for preparations used as a biomaterial and delivery system for wrapping active pharmaceutical ingredients and / or drug carriers for treating symptoms such as pain, itching, etc., all of which have good prospects.
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