RORγ Modulators for Autoimmune Disease Treatment
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Solution Overview
Problem
Current treatments for autoimmune and inflammatory diseases mediated by RORγ, such as multiple sclerosis, rheumatoid arthritis, psoriasis, Crohn's disease, and asthma, are inadequate due to the limited availability of effective modulators that target RORγ activity.
Innovation Solution
Development of novel RORγ modulators, specifically compounds of Formula I, which can inhibit or modulate RORγ activity, providing a pharmaceutical solution for treating autoimmune and inflammatory diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments are used for autoimmune and inflammatory diseases, then treatment is provided, but the treatments are inadequate due to limited availability of effective modulators targeting RORγ activity
Solution Approach 1:
The patent segments the broad category of immune modulators into specific RORγ-targeted compounds with distinct chemical structures (Formula I and Formula II). This segmentation allows for targeted modulation of RORγ activity while avoiding off-target effects of broader immunosuppressants, thereby improving treatment reliability for RORγ-mediated diseases.
Solution Approach 2:
The patent employs parameter changes by modifying chemical structures (varying R1-R7 substituents, k and p values) to optimize RORγ binding affinity and selectivity. This systematic variation of molecular parameters enables the development of multiple modulators with different potency profiles, addressing the limited availability issue while maintaining effective treatment.
2Reliability
If novel RORγ modulators are developed, then effective treatment for autoimmune diseases is achieved, but this requires pharmaceutical research and development resources
Solution Approach 1:
The patent creates a universal platform (Formula I and Formula II structures) that can generate multiple RORγ modulators through systematic substitution variations. This multi-functional framework allows a single core structure to address multiple disease indications (psoriasis, asthma, rheumatoid arthritis, etc.), reducing overall development complexity while maintaining high effectiveness across different autoimmune conditions.
Data Source
AI summary
The present invention relates to novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ.