Macrocyclic compound and application thereof in medicine

By developing a macrocyclic compound as a 3Cl protease inhibitor, the problem of insufficient inhibitory activity of existing anti-3Clpro inhibitors on coronavirus was solved, effective inhibition of SARS-CoV-2 was achieved, and good pharmacokinetic properties and safety were achieved.

CN119638737APending Publication Date: 2025-03-18SUNSHINE LAKE PHARMA CO LTD
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Patent Information

Application Number
CN202410098126.0
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-01-24
Publication Date
2025-03-18

AI Technical Summary

Technical Problem

The existing anti-3Clpro inhibitors have weak inhibitory activity on coronaviruses, especially SARS-CoV-2, and have problems such as single structure, weak enzyme inhibitory activity, and poor drug properties. It is difficult to effectively treat and prevent diseases or symptoms caused by coronavirus.

Method used

A macrocyclic compound was developed as an inhibitor of 3Cl protease, which has good inhibitory activity against coronaviruses, especially SARS-CoV-2, and has good pharmacokinetic properties, good solubility, good stability of liver microsomes, basically no inducible effect on liver drug enzymes and little toxicity.

Benefits of technology

This macrocyclic compound has good application prospects in the treatment and/or prevention of diseases or symptoms caused by coronaviruses, especially SARS-CoV-2, and can effectively inhibit the virus, and has good safety and drug properties.

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Abstract

The invention belongs to the technical field of medicines, and relates to a macrocyclic compound and application thereof in medicines. Specifically, the invention relates to a compound shown in a general formula (I) or a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and a pharmaceutical composition containing the compound, the invention relates to a compound and a pharmaceutical composition thereof, and application of the compound and the pharmaceutical composition in preparation of a medicine for preventing and / or treating diseases or symptoms caused by coronavirus, especially diseases or symptoms caused by novel coronavirus (SARS-CoV-2), and the variables in the formula (I) are defined in the specification. # imgabs0 #
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