Pharmaceutical composition containing a quinazoline compound

Bifunctional compounds targeting the G12D mutant KRAS protein through E3 ligase linkage offer a novel approach to treat colorectal and lung cancers by degrading and inhibiting the KRAS protein, addressing the inadequacy of existing treatments for KRAS G12D mutations.

JP2026522180APending Publication Date: 2026-07-07ASTELLAS PHARMA INC
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Patent Information

Application Number
JP2025565562
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2023-06-22
Filing Date
2024-06-21
Publication Date
2026-07-07

AI Technical Summary

Technical Problem

Current treatments for colorectal and lung cancers, particularly those with KRAS G12D mutations, are inadequate due to the lack of effective therapeutic agents, as existing drugs do not demonstrate efficacy in cancers with these mutations.

Method used

Development of bifunctional compounds comprising a quinazoline or quinoline heterocycle with specific substituents linked to an E3 ligase via a linker, which can bind to the G12D mutant KRAS protein, inducing its degradation and inhibiting its activity.

Benefits of technology

These compounds effectively degrade and inhibit the G12D mutant KRAS protein, providing a potential treatment for colorectal and lung cancers, especially those positive for the G12D mutant KRAS.

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Abstract

Compounds of formulas (I), (XXI), (XXII), and (XXIII) as defined herein, and salts thereof, are provided herein for use in the treatment of colorectal and / or lung cancer.
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