CCL2 Inhibitor Compounds Blocking CCR2 Signaling

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Solution Overview

Problem

Current treatments for autoimmune, inflammatory, degenerative, and metabolic diseases associated with Monocyte chemoattractant protein-1 (MCP-1, also known as CCL2) and its signaling pathways through the CCR2 receptor are inadequate in effectively inhibiting the biological activity and downstream pathogenic processes.

Innovation Solution

Development of specific compounds, such as those described in Formulas 1 and 2, which inhibit the biological activity of CCL2 and its signaling pathway by decreasing the expression of pro-inflammatory cytokines, angiogenic proteins, and proteins promoting cellular adhesion and migration, thereby reducing the pathogenic effects of CCL2 in mammalian cells.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments are used for CCL2-associated diseases, then treatment is provided, but the biological activity of CCL2 and downstream pathogenic processes are not effectively inhibited

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidpathogenic processes
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent develops novel chemical compounds with specific molecular structures (Formulas 1 and 2) that represent parameter changes in the therapeutic agent. These compounds are designed to optimize binding affinity to CCL2 and enhance inhibition of downstream signaling pathways, directly addressing the inadequacy of current treatments in effectively inhibiting CCL2 biological activity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates synthetic compound analogs that replicate and enhance the therapeutic effect of natural CCL2 inhibitors. By designing compounds with optimized structural features based on the CCL2 binding interface, the invention produces improved copies of inhibitory molecules that more effectively block the CCL2-CCR2 interaction and downstream pathogenic processes

Inventive Principle:
Principle #26Copying

2Object-generated harmful factors

If compounds are designed to inhibit CCL2 signaling, then expression of pro-inflammatory cytokines and angiogenic proteins is reduced, but drug development complexity increases

Engineering Contradiction:
Improvepro-inflammatory cytokine expressionVSAvoidcompound structure complexity
Core Design Contradiction:
Object-generated harmful factorsVSDevice complexity

Solution Approach 1:

The patent divides the complex task of inhibiting CCL2 signaling into targeted molecular components. The compounds are designed with specific functional groups and structural motifs that selectively interact with CCL2, breaking down the complex signaling pathway into manageable inhibition targets. This segmentation approach reduces the complexity of achieving broad anti-inflammatory effects by focusing on key molecular interactions

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent introduces small molecule compounds as intermediaries between the CCL2 ligand and CCR2 receptor. These compounds act as molecular mediators that block the direct interaction between CCL2 and CCR2, thereby reducing the expression of downstream pro-inflammatory cytokines and angiogenic proteins without requiring direct modification of the cytokine genes themselves

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS11858876B2CCL2 inhibitors
Publication Date: 2024.01.02 LAPKO INC DBA AFECTA PHARM
  • US11858876B2 patent drawing
  • US11858876B2 patent drawing
  • US11858876B2 patent drawing

AI summary

Compounds, pharmaceutically acceptable salts, and pharmaceutical compositions thereof are disclosed that are useful for inhibition of the biological activity of CCL2, as well as methods of treatment for diseases involving the biological activity of CCL2.