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, and ankylosing spondylitis, 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 include pharmaceutically acceptable salts, designed to inhibit or modulate RORγ activity, offering potential therapeutic benefits for 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 for existing conditions, but the treatments are inadequate due to limited availability of effective RORγ modulators
Solution Approach 1:
The patent segments the broad category of autoimmune and inflammatory diseases into specific indications (multiple sclerosis, rheumatoid arthritis, psoriasis, ankylosing spondylitis) and develops targeted RORγ modulators for each, allowing tailored treatment approaches for different conditions while sharing a common mechanistic basis
Solution Approach 2:
The patent employs systematic variation of chemical parameters in the RORγ modulator compounds (Formula I structures with varying substituents R1-R7) to optimize binding affinity, selectivity, and pharmacological properties, thereby improving treatment effectiveness across different disease states
2Adaptability or versatility
If novel RORγ modulators (Formula I compounds) are developed, then targeted modulation of RORγ activity is achieved, but this requires overcoming the limited availability of effective modulators
Solution Approach 1:
The patent systematically varies chemical parameters in Formula I compounds (substituents at positions R1-R7, core structures) to generate a library of RORγ modulators with optimized properties for reliable and effective treatment of autoimmune and inflammatory diseases
Solution Approach 2:
The RORγ modulators act as intermediary compounds that bind to and modulate the RORγ nuclear receptor, thereby mediating the therapeutic effect between the administered drug and the pathological Th17 cell differentiation process
Data Source
AI summary
The preseent invention relates to novel retinoid-related orphan receptor gamma(RORγ)modulators and their use in the treatment ofdiseases mediated by RORγ.