Pyrrolopyrimidine FGFR2/3 Inhibitor Selectivity for Antitumor Therapy

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Solution Overview

Problem

Current FGFR inhibitors exhibit limited therapeutic effects, high drug resistance, and significant side effects, necessitating the development of highly active and selective FGFR2 and/or FGFR3 inhibitors for cancer treatment.

Innovation Solution

A pyrrolopyrimidine derivative is developed as an FGFR2 and/or FGFR3 inhibitor, represented by specific structural formulas, which can be used in pharmaceutical compositions to prepare anti-tumor drugs.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If pan-FGFR inhibitors are used to target multiple FGFR isoforms, then broad coverage is achieved, but therapeutic effectiveness decreases and drug resistance increases

Engineering Contradiction:

Improvecoverage of FGFR isoformsVSAvoidtherapeutic effectiveness

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The patent applies local quality by designing the pyrrolopyrimidine derivative with specific structural features (substituents at positions 5, 6, or 7 of the pyrrolopyrimidine ring) that enable selective binding to FGFR2 and/or FGFR3 isoforms while excluding FGFR1 and FGFR4. This localized molecular design achieves isoform-specific inhibition, resolving the contradiction between broad coverage and therapeutic effectiveness.

Inventive Principle:

Principle #3Local quality

2Adaptability or versatility

If pan-FGFR inhibitors are used, then multiple FGFR targets are addressed, but toxic side effects increase

Engineering Contradiction:

Improvetargeting capabilityVSAvoidtoxic side effects

Core Design Contradiction:

Adaptability or versatilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs local quality by engineering the pyrrolopyrimidine core structure with specific substituents that confer selectivity for FGFR2 and/or FGFR3 over other FGFR isoforms. This selective targeting reduces off-target effects and toxic side effects associated with pan-FGFR inhibition, while maintaining the ability to address multiple cancer types through FGFR2/3 involvement.

Inventive Principle:

Principle #3Local quality

3Reliability

If FGFR1/4 inhibition is enhanced to increase therapeutic effect, then tumor growth suppression improves, but hyperphosphatemia and diarrhea increase

Engineering Contradiction:

Improvetumor growth suppressionVSAvoidhyperphosphatemia and diarrhea

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies the extraction principle by removing FGFR1 and FGFR4 from the inhibition profile through selective molecular design. The pyrrolopyrimidine derivative is structurally optimized to specifically inhibit FGFR2 and/or FGFR3 while sparing FGFR1 and FGFR4, thereby extracting the harmful effects (hyperphosphatemia and diarrhea) associated with FGFR1/4 inhibition while preserving anti-tumor efficacy through FGFR2/3 targeting.

Inventive Principle:

Principle #2Taking out (Extraction)

Data Source

PatentEP4722216A1Pyrrolopyrimidine derivative and use thereof in medicine

Publication Date: 2026.04.08 KANGBAIDA (SICHUAN) BIOTECHNOLOGY CO LTD

Figure 1~2

AI summary

The present invention relates to a pyrrolopyrimidine derivative represented by general formula (I) or a pharmaceutically acceptable salt, stereoisomer or deuterated compound thereof, a composition thereof, and a use thereof in medicine.