Phenyl Urea Derivatives Selective FPR1 Modulation

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Solution Overview

Problem

Current treatments for inflammatory diseases lack selective modulation of FPR1 and FPR2 receptors, which are critical for regulating inflammatory responses and healing processes, leading to inadequate management of inflammatory conditions.

Innovation Solution

Development of phenyl urea derivatives that selectively modulate FPR1 relative to FPR2, acting as receptor agonists, antagonists, or partial agonists to treat disorders associated with FPR modulation, including inflammatory diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for inflammatory diseases are used, then inflammatory conditions can be managed, but selective modulation of FPR1 and FPR2 receptors is lacking, leading to inadequate management

Engineering Contradiction:
Improveeffectiveness of inflammatory disease treatmentVSAvoidselective modulation capability of FPR1 and FPR2
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent segments the FPR receptor family into two distinct targets: FPR1 and FPR2. By designing compounds that can selectively modulate each receptor type independently, the invention enables differentiated therapeutic approaches for inflammatory diseases, allowing clinicians to target specific pathological mechanisms through FPR1 or FPR2 modulation as needed

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs parameter changes by developing compounds with varying selectivity profiles for FPR1 and FPR2. By adjusting molecular structure parameters of the phenyl urea derivatives, the invention creates a series of compounds with different degrees of selectivity, enabling optimization of therapeutic efficacy while minimizing off-target effects

Inventive Principle:
Principle #35Parameter changes

2Adaptability or versatility

If FPR1 and FPR2 are modulated without selectivity, then broad anti-inflammatory effects may be achieved, but inadequate management of specific inflammatory conditions results

Engineering Contradiction:
Improvebroad anti-inflammatory coverageVSAvoidmanagement efficacy of specific inflammatory conditions
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent introduces dynamic selectivity by designing compounds that can preferentially bind to either FPR1 or FPR2 based on specific inflammatory conditions. The phenyl urea derivatives exhibit adaptable binding characteristics that can be optimized for different disease states, allowing the same compound class to address diverse inflammatory pathologies with appropriate selectivity

Inventive Principle:
Principle #15Dynamics

Data Source

PatentUS11286234B2Phenyl urea derivatives as N-formyl peptide receptor modulators
Publication Date: 2022.03.29 ALLERGAN INC
  • US11286234B2 patent drawing
  • US11286234B2 patent drawing
  • US11286234B2 patent drawing

AI summary

The present invention relates to phenyl urea derivatives useful for the treatment of inflammatory diseases, pharmaceutical compositions containing them and their use as tools or as pharmaceuticals as modulators of the N-formyl peptide receptor (FPR), including FPR1 and FPR2, or as selective agonists of the FPR1 receptor.