Fused ring compound and use thereof in KRAS inhibitor

By developing a new fused ring compound to optimize its structure and pharmacokinetic properties, the problems of low bioavailability and insufficient exposure of existing pan-KRAS inhibitors were solved, and effective inhibition and good pharmacokinetic performance of various KRAS mutants were achieved.

WO2025077770A1 Publication Date: 2025-04-17CHENGDU HYPERWAY PHARM CO LTD +1
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Patent Information

Application Number
PCT/CN2024/123898
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-07-15
Filing Date
2024-10-10
Publication Date
2025-04-17

AI Technical Summary

Technical Problem

The existing pan-KRAS inhibitors have problems with low bioavailability and insufficient exposure, and it is difficult to effectively inhibit various KRAS mutants.

Method used

Develop a new fused ring compound that can effectively inhibit various KRAS mutants by optimizing its structural and pharmacokinetic properties and improving its exposure and bioavailability in the body.

Benefits of technology

This compound can effectively block KRAS activity, has good oral exposure and pharmacokinetic properties, and is suitable for the preparation of drugs used to treat KRAS mutation-related cancers.

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Abstract

A fused ring compound, a pharmaceutical composition comprising same, and the use thereof. The compound has a structure as represented by formula (I), or is a tautomer, a mesomer, a racemate, an enantiomer, a diastereomer or a mixture form thereof, a metabolite, a metabolic precursor, an isotope-substituted form, a pharmaceutically acceptable salt, a hydrate, a solvate, a polymorph or a co-crystal thereof. The compound can be used for treating one or more cancers caused by KRAS mutation.
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