Amide aldehyde dehydrogenase agonists, methods of synthesis and uses thereof

By developing amide-based aldehyde dehydrogenase agonists to enhance ALDH2 activity, the pharmacokinetic problems of existing small molecule agonists have been solved, enabling effective treatment of acute alcohol poisoning and various health conditions.

CN117105868BActive Publication Date: 2026-06-26THE NAVAL MEDICAL UNIV OF PLA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2023-05-19
Publication Date
2026-06-26

AI Technical Summary

Technical Problem

Existing ALDH2 small molecule agonists suffer from pharmacokinetic problems such as poor water solubility, low activity, and short half-life, which hinder their clinical application. Furthermore, carriers of low-activity ALDH2 variants face a high risk of oxidative stress-related diseases, including cardiovascular and cerebrovascular diseases, diabetes, and neurodegenerative diseases.

Method used

A class of amide-based aldehyde dehydrogenase agonists has been developed, specifically consisting of a compound of formula I and its stereoisomers, pharmaceutically acceptable salts, hydrates, or solvates, to enhance the expression or activity of ALDH2, administered via intramuscular, intravenous, subcutaneous, or oral routes, for the treatment of diseases or symptoms associated with aldehyde dehydrogenase 2 activity.

Benefits of technology

It enhances the activity of ALDH2, reduces the accumulation of acetaldehyde in the body, and prevents damage to the human body caused by acetaldehyde. It has potential clinical application value and can fundamentally treat acute alcohol poisoning and prevent various health diseases.

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Abstract

The application belongs to the technical field of pharmaceutical chemistry, and particularly relates to an amide aldehyde dehydrogenase agonist, a synthesis method and purposes thereof. The amide compound provided by the application shows higher agonistic activity to ALDH2, so the compound has the potential to prepare a therapeutic drug for a disease related to ALDH2 activity; (2) the amide compound of the application has obviously improved activity and water solubility compared with a positive control, and has better drug property. Therefore, the compound of the application has a good development prospect.
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Citation Information

Patent Citations

  • Modulators of aldehyde dehydrogenase activity and methods of use thereof

    CN102209541A