Imidazopyridine Derivatives Inhibit FGF Receptor Binding

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Solution Overview

Problem

Current therapies lack effective inhibitors for Fibroblast Growth Factors (FGFs), which are involved in various pathological conditions, including embryonic development and adult tissue processes.

Innovation Solution

Development of novel imidazopyridine derivatives that act as antagonists to the binding of FGFs to their receptors, specifically designed to inhibit their activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current therapies are used, then existing treatment options are available, but effective inhibition of FGF receptor binding is not achieved

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidavailability of effective inhibitors

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent segments the FGF receptor binding interface into specific molecular targets, designing imidazopyridine derivatives that selectively bind to particular regions of the FGF receptor complex. This segmentation allows for precise inhibition of pathological FGF signaling while preserving essential developmental functions.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The imidazopyridine derivatives act as intermediary molecules that bridge the gap between existing therapeutic approaches and the desired FGF inhibition. These compounds serve as mediators by binding to FGF receptors and modulating their activity, providing effective inhibition where current therapies fail.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Adaptability or versatility

If FGF activity is inhibited, then therapeutic potential for FGF-associated conditions is achieved, but binding to FGF receptors is blocked

Engineering Contradiction:

Improvetherapeutic potentialVSAvoidFGF receptor binding

Core Design Contradiction:

Adaptability or versatilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs parameter changes by modifying the chemical structure of imidazopyridine derivatives to optimize their binding affinity and selectivity. By adjusting molecular parameters such as substituent groups and stereochemistry, the compounds achieve high therapeutic potential while maintaining controlled inhibition of FGF receptor binding.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention applies local quality by designing compounds with specific functional groups positioned to interact with particular regions of the FGF receptor binding site. This localized interaction enables selective inhibition of pathological FGF signaling pathways while minimizing off-target effects.

Inventive Principle:

Principle #3Local quality

Data Source

PatentUS9452164B2Imidazopyridine derivatives, process for preparation thereof and therapeutic use thereof

Publication Date: 2016.09.27 SANOFI SA(FR)

AI summary

The invention relates to compounds corresponding to formula (I):in whichR2 and R3 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below:in which the wavy lines represent the phenyl nucleus to which R2 and R3 are attached.Preparation process and therapeutic use.