AhR Modulator Compounds for Selective Inflammatory Disease Control
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Solution Overview
Problem
There is a need for potent and selective compounds that modulate Aryl hydrocarbon receptor (AhR) activity to treat various inflammatory conditions, as existing treatments are inadequate in effectively managing diseases such as inflammatory bowel disease, cartilage inflammation, and autoimmune disorders.
Innovation Solution
Development of 1-aryl-1,2,3,4-tetrahydro-β-carboline derivatives and their pharmaceutically acceptable salts, which act as potent and selective AhR-binding compounds, administered to subjects to treat inflammatory diseases and conditions by modulating AhR activity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing treatments are used for inflammatory conditions, then treatment coverage is provided, but effectiveness is inadequate
Solution Approach 1:
The patent modifies chemical parameters of AhR modulators by varying substituents at different positions (R1-R6, Ar groups) to optimize both effectiveness and broad applicability across different inflammatory conditions
2Reliability
If AhR activity is modulated to treat inflammatory diseases, then therapeutic benefits are achieved, but selective compound development is needed
Solution Approach 1:
The patent introduces specific substituent patterns at different positions of the core structure (e.g., R4 and R5 preferences, Ar group selections) to achieve selective AhR modulation with desired therapeutic outcomes
Solution Approach 2:
The patent optimizes molecular parameters including substituent types, positions, and combinations to enhance both selectivity for AhR and therapeutic effectiveness across various inflammatory conditions
Data Source
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AI summary
The present invention is generally directed towards compounds capable of binding the aryl hydrocarbon receptor and modulating its activity, methods of treating inflammatory conditions such as Crohn's disease using such compounds, and pharmaceutical compositions comprising such compounds. Also provided are methods of increasing levels of IL-22 in a subject and/or decreasing levels of IFN-γ in a subject.