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
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- ASTELLAS PHARMA INC
- 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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Smart Images
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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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