1-aryl-5-pyrazolones, pharmaceutical compositions and uses thereof

By designing 1-aryl-5-pyrazolone compounds and combining COX-2 selective inhibition and free radical scavenging functions, the cardiovascular and gastrointestinal side effects caused by existing NSAIDs have been resolved, achieving effective treatment for chronic inflammatory diseases.

CN120058611BActive Publication Date: 2026-06-02CHINA PHARM UNIV
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Patent Information

Application Number
CN202311600384.6
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2023-11-28
Publication Date
2026-06-02
Estimated Expiration
2043-11-28

AI Technical Summary

Technical Problem

While existing selective COX-2 inhibitors reduce gastrointestinal side effects, they increase the risk of cardiovascular events and stroke, and NSAID-induced free radical production is an important mechanism leading to these side effects.

Method used

A 1-aryl-5-pyrazolone compound was designed and hybridized with edaravone to obtain a compound with dual functions of selective COX-2 inhibition and free radical scavenging, which can be used to prepare pharmaceutical compositions for the treatment of chronic inflammatory diseases.

Benefits of technology

This compound effectively inhibits COX-2 and scavenge free radicals at micromolar concentrations, reducing cardiovascular and gastrointestinal side effects caused by NSAIDs. It has significant antioxidant stress and anti-inflammatory analgesic effects, and has better therapeutic effects on chronic inflammatory diseases such as psoriatic arthritis, rheumatoid arthritis, and osteoarthritis.

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Abstract

The application discloses a 1-aryl-5-pyrazolone compound and a pharmaceutical composition and application thereof. The compound has a structure selected from any one of the following structures, and also comprises a tautomer, a pharmaceutically acceptable salt or a mixture thereof: the compound can effectively inhibit COX-2 and effectively scavenge free radicals at a micromolar concentration level, can reduce cardiovascular and digestive tract side effects caused by NSAID-induced free radical production, and can also play a better treatment effect on chronic inflammatory diseases with pain through the synergistic effect of antioxidation stress and anti-inflammatory analgesia.
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