Preparation and use of novel MAO-b inhibitor containing tetralin-1-amine structure

By synthesizing compounds containing tetrahydronaphth-1-amine structures, the selectivity and safety issues of existing MAO-B inhibitors were resolved, achieving highly selective inhibition of MAO-B, improving Parkinson's disease symptoms and reducing the generation of oxygen free radicals.

WO2026077192A1 Publication Date: 2026-04-16CHONGQING MEDICAL UNIVERSITY
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Patent Information

Application Number
PCT/CN2025/121628
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-10-08
Filing Date
2025-09-16
Publication Date
2026-04-16

AI Technical Summary

Technical Problem

Existing MAO-B inhibitors are non-selective and irreversible, leading to serious adverse reactions such as orthostatic hypotension, hypertensive crisis, caseous reaction, and liver toxicity, and cannot effectively relieve Parkinson's disease symptoms.

Method used

To develop a compound containing a tetrahydronaphth-1-amine structure, and to synthesize a highly selective MAO-B inhibitor via coupling, reduction and amino substitution reactions, and to prepare it in pharmaceutically acceptable forms such as hydrochloride.

Benefits of technology

It achieves highly selective inhibition of MAO-B, reduces the generation of peroxides in dopamine oxidation metabolism, reduces the production of oxygen free radicals, prevents dopamine degradation, improves Parkinson's disease symptoms, and delays the death of substantia nigra cells.

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Abstract

Provided in the present invention are preparation and use of a novel MAO-B inhibitor containing a tetralin-1-amine structure, which belong to the field of medicines. The derivative is a compound represented by formula I, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof. The compound of the present invention can be used for inhibiting monoamine oxidase (MAO), especially selectively inhibiting MAO-B. The compound can be used for treating diseases such as Parkinson's disease, Alzheimer's disease, and emotional disorders, and exhibits good application prospects.
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