木脂素衍生物、其制备方法及用途

By structurally modifying arctigenin, lignan derivatives were developed, solving the problem of poor oral efficacy of existing inhibitors. This resulted in effective inhibition of mitochondrial respiratory chain complex I and improved oral pharmacokinetic properties, making it suitable for the treatment of tumors and age-related diseases.

CN117440947BActive Publication Date: 2026-07-17SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES +1

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES
Filing Date
2022-03-25
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Existing mitochondrial respiratory chain complex I inhibitors, such as arctigenin, are easily metabolized after oral administration, have poor pharmacokinetic properties, and low bioavailability, which limits their application as oral drugs. At the same time, tumors and senescent cells rely on the OXPHOS process for energy, and there is a lack of effective means of inhibition.

Method used

By structurally modifying arctigenin, a lignan derivative was developed, which improved the inhibitory activity against mitochondrial respiratory chain complex I and enhanced its oral pharmacokinetic properties.

Benefits of technology

It achieves effective inhibition of mitochondrial respiratory chain complex I, improves oral efficacy, has better drug-like properties, and is suitable for the prevention or treatment of diseases related to OXPHOS and age-related diseases.

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Abstract

本发明公开了一种木脂素衍生物、其制备方法及用途,所述木脂素衍生物结构如式I所示,式中,各取代基的定义如说明书和权利要求书中所述。本发明的木脂素衍生物,能够作为线粒体呼吸链复合物I抑制剂,抑制线粒体的氧化磷酸化作用及ATP的生成,用于预防和 / 或治疗与线粒体呼吸链复合物I活性或表达升高、或者线粒体氧化磷酸化作用增强相关的疾病。
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