Substituted Tetrahydropyrans for Selective CCR2 Modulation
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current treatments for inflammatory disorders associated with CCR2 signaling, such as rheumatoid arthritis and obesity, have limitations in effectively modulating chemokine receptor activity, leading to incomplete disease management and potential side effects.
Innovation Solution
Development of compounds that modulate CCR2 activity by interacting with the CCR2 receptor, inhibiting ligand binding and reducing inflammatory responses, thereby treating CCR2-mediated conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments for inflammatory disorders are used, then disease management is achieved, but modulating chemokine receptor activity is incomplete leading to side effects
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of CCR2 modulator compounds through systematic variation of substituents at specific positions (R1-R6) on the core molecular framework. This structural parameter optimization enables fine-tuning of receptor binding affinity and selectivity, achieving more effective and selective CCR2 modulation while reducing off-target effects and side effects associated with less selective treatments
2Object-affected harmful factors
If CCR2 modulator compounds are developed, then inflammatory responses are reduced, but treatment specificity must be maintained to avoid affecting other chemokine receptors
Solution Approach 1:
The patent applies local quality by introducing specific substituent patterns at localized positions on the molecular structure. Different R groups (R1-R6) are strategically placed at specific ring positions to create localized interaction zones that selectively engage CCR2 receptor binding pockets. This localized structural differentiation enables high specificity for CCR2 while minimizing cross-reactivity with other chemokine receptors, allowing effective inflammatory response reduction with maintained treatment specificity
Data Source
AI summary
Compounds are provided that are modulators of the CCR2 receptor. The compounds have the general formula (Ia1′):and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of CCR2 receptors.