RORγ Inverse Agonist Compounds for Autoimmune Inflammation
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Solution Overview
Problem
Current treatments for immune, inflammatory, metabolic, fibrotic, and cholestatic diseases associated with RORγt activity are limited, and there is a need for novel compounds that can effectively modulate RORγt to address these conditions.
Innovation Solution
Development of novel RORγ modulators, specifically inverse agonists, which can be administered to modulate RORγ activity and treat related diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments for immune and inflammatory diseases are used, then existing therapeutic options are available, but treatment effectiveness is limited and novel compounds are needed
Solution Approach 1:
The patent segments the broad category of immune and inflammatory diseases into specific disease indications (psoriasis, rheumatoid arthritis, multiple sclerosis, etc.) and develops targeted RORγt modulator compounds for each, allowing differentiated treatment approaches while maintaining overall therapeutic effectiveness
Solution Approach 2:
The patent employs parameter changes by developing novel chemical compounds with specific molecular structures (formula I and II) that modulate RORγt activity through controlled chemical parameters, thereby improving treatment effectiveness beyond existing therapies
2Reliability
If RORγt activity is modulated to treat inflammatory diseases, then therapeutic efficacy is improved, but understanding of molecular mechanisms is required
Solution Approach 1:
The patent uses RORγt as an intermediary molecular target that mediates the effect between the administered compounds and the inflammatory disease pathology. By targeting this specific nuclear receptor, the patent simplifies the complex molecular mechanisms into a detectable and measurable pathway for therapeutic evaluation
Data Source
Figure 1AA~1AC
Figure 1AD~1AF
Figure 1AG~1AI
AI summary
The present invention provides novel compounds of formula (la) that are modulators of RORgamma. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the modulation of RORgamma has therapeutic effects, for instance in autoimmune diseases, autoimmune-related diseases, inflammatory diseases, metabolic diseases, fibrotic diseases, or cholestatic diseases.