ROR-gamma Modulator Compounds for Autoimmune Disease Treatment
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Solution Overview
Problem
Current treatments for autoimmune diseases and inflammatory conditions mediated by RORγ, such as rheumatoid arthritis and psoriasis, lack effective modulators that specifically target RORγ to regulate T H 17 cells and non-T H 17 IL-17 producing cells effectively.
Innovation Solution
Development of novel RORγ modulator compounds, specifically designed to modulate the activity of RORγ, which are pharmaceutical compositions comprising compounds according to Formula I or their pharmaceutically acceptable salts, to treat autoimmune and inflammatory diseases by inhibiting RORγ activity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments are used for autoimmune diseases, then existing therapeutic options are available, but they lack effective modulators that specifically target RORγ to regulate T H 17 cells and non-T H 17 IL-17 producing cells
Solution Approach 1:
The patent segments the broad class of ROR modulators into specific subclasses with defined structural features (Formula I compounds with specific A1-A12, R1-R14 substitutions) that selectively target RORγ. This segmentation allows differentiation between RORγ-specific modulators and general ROR modulators, resolving the contradiction by providing treatments that are both effective and specifically adapted to RORγ.
Solution Approach 2:
The patent applies local quality by specifying particular structural characteristics at different positions (A1-A12 rings, R1-R14 substituents) of the molecular scaffold that confer RORγ selectivity. Each position has defined substituent options that locally modify the compound's interaction with RORγ, enabling specific targeting while maintaining overall therapeutic effectiveness.
2Reliability
If novel RORγ modulator compounds are developed, then specific regulation of T H 17 cells and non-T H 17 IL-17 producing cells is achieved, but the complexity of the compound structure increases
Solution Approach 1:
The patent employs a universal scaffold (core structure with A1-A12 positions) that can accommodate multiple different substituent patterns (R1-R14 variations) while maintaining RORγ modulation activity. This multi-functionality allows a single molecular framework to achieve specific RORγ regulation through diverse substituent combinations, reducing the need for entirely new complex structures for each specific application.
Solution Approach 2:
The patent achieves RORγ specificity by systematically varying molecular parameters (substituent types at A1-A12 positions, R1-R14 groups, stereochemistry) around a core scaffold. This parameter optimization approach allows tuning of specificity and potency without fundamentally changing the molecular architecture, thereby managing complexity while achieving reliable specific modulation.
Data Source
AI summary
The present invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof. The compounds can be used as inhibitors of RORy and are useful for the treatment of RORy mediated diseases.