PCSK9 inhibitor, preparation method therefor, and use thereof

By developing PCSK9 small molecule inhibitor compounds represented by general formula (I), the problems of existing large molecule inhibitors requiring injection and high cost have been solved, achieving safe and effective oral lipid-lowering effects, reducing LDL-C and Lp(a) levels, and meeting the treatment needs of cardiovascular diseases.

WO2026158284A1PCT designated stage Publication Date: 2026-07-30ZHUHAI UNITED LAB
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Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
ZHUHAI UNITED LAB
Filing Date
2026-01-20
Publication Date
2026-07-30

AI Technical Summary

Technical Problem

Most existing PCSK9 inhibitors are large molecule drugs that require injection and are expensive. There is a lack of oral PCSK9 small molecule inhibitors, which cannot meet the needs of effective treatment for cardiovascular diseases.

Method used

To develop a small molecule inhibitor compound of general formula (I) and its isomers or pharmaceutically acceptable salts that reduce LDL-C levels by binding to the PCSK9 protein for the treatment of cardiovascular disease and hyperlipidemia (a).

Benefits of technology

This study provides a safe and metabolically beneficial oral PCSK9 small molecule inhibitor that can effectively reduce LDL-C and Lp(a), offering a new approach for the prevention and treatment of cardiovascular diseases.

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Abstract

The present invention belongs to the field of pharmaceutical chemistry, and disclosed are a PCSK9 inhibitor, a preparation method therefor, and use thereof. Specifically, the present invention relates to a compound represented by formula (I), an isomer thereof, or a pharmaceutically acceptable salt thereof, and use thereof as an inhibitor in the treatment of hypercholesterolemia and cardiovascular diseases for lipid lowering.
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