FGFR inhibitors and methods of use thereof

The novel compounds represented by Formula (I) serve as selective FGFR3 inhibitors, addressing the limitations of current FGFR inhibitors by enhancing selectivity and reducing toxicity, thereby offering an effective treatment for FGFR3-mediated diseases.

WO2025061029A1 Publication Date: 2025-03-273H PHARM CO LTD
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Patent Information

Application Number
PCT/CN2024/119392
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-02-02
Filing Date
2024-09-18
Publication Date
2025-03-27

AI Technical Summary

Technical Problem

Current FGFR inhibitors, such as pan-FGFR1/2/3 inhibitors, face challenges including on-target toxicity, particularly hyperphosphatemia, and lack of selectivity, which can lead to off-target toxicities. Additionally, existing treatments for FGFR3-mediated disorders like achondroplasia are limited in therapeutic efficacy and convenience.

Method used

Development of novel compounds represented by Formula (I) that act as selective FGFR3 inhibitors, offering a potential therapeutic solution for FGFR3-mediated diseases with improved selectivity and reduced off-target toxicities.

Benefits of technology

The selective FGFR3 inhibitors demonstrated in Formula (I) have the potential to effectively treat FGFR3-mediated diseases while minimizing adverse effects, providing a more targeted and efficacious approach compared to existing treatments.

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Abstract

Disclosed herein are novel compounds of Formula (I) and pharmaceutical composition, pharmaceutically acceptable salt, prodrug, solvate, hydrate, tautomer, and isomer thereof, useful as FGFR inhibitors to modulate or inhibit the activity of FGFR enzymes. Methods for treating disorders associated with FGFR signaling with the said compounds and compositions are also disclosed.
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