Bridged ring compound, pharmaceutical composition thereof and use thereof

By providing novel bridged ring compounds, the problem of poor compliance of existing TNF-α inhibitors with large molecules is solved, achieving high efficiency of TNF-α inhibitory activity and low cardiotoxicity of small molecule compounds, and improving the bioavailability and metabolic stability of the compounds.

WO2026145577A1PCT designated stage Publication Date: 2026-07-09ETERN THERAPEUTICS (WUXI) CO LTD

Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
ETERN THERAPEUTICS (WUXI) CO LTD
Filing Date
2025-12-30
Publication Date
2026-07-09

AI Technical Summary

Technical Problem

Existing TNF-α inhibitors are mainly macromolecules, which have problems such as poor patient compliance, high production costs, and inconvenient storage and transportation. There is a lack of application of small molecule compounds.

Method used

A novel bridged ring compound is provided, which exhibits good TNF-α inhibitory activity, high exposure, excellent absolute bioavailability and low cardiotoxicity. The specific structure consists of a compound of formula (III) and its pharmaceutically acceptable salt, isotope substitute, solvate or solvate of salt.

Benefits of technology

This study achieved TNF-α inhibitory activity of small molecule compounds, improved the bioavailability and hepatic microsomal metabolic stability of the compounds, and reduced cardiotoxicity.

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Abstract

Disclosed in the present invention are a bridged ring compound, a pharmaceutical composition thereof and the use thereof. Specifically, disclosed in the present invention is a compound as shown in formula (III), a pharmaceutically acceptable salt thereof, an isotopically substituted substance thereof, a solvate thereof, or a solvate of the pharmaceutically acceptable salt thereof. The compound of the present invention has good biological activities and / or pharmacokinetic properties.
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