Indole Compounds Modulating AhR for Cancer Therapy

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Solution Overview

Problem

Current treatments for cancer and immune system modulation lack effective compounds that specifically target the aryl hydrocarbon receptor (AhR) for therapeutic benefit.

Innovation Solution

Development of novel indole compounds that modulate AhR activity, including specific structures and their pharmaceutical compositions, for use in treating cancer and immune system stimulation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments are used for cancer and immune system modulation, then existing therapeutic options are available, but they lack effective compounds that specifically target the aryl hydrocarbon receptor (AhR)

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidtarget specificity
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by systematically varying the chemical structure of indole compounds (changing molecular parameters such as substituents at positions 3, 5, 6, and 7 of the indole ring) to optimize AhR binding affinity and selectivity. This allows the development of compounds with enhanced therapeutic effectiveness specifically targeted at AhR, resolving the contradiction between general therapeutic availability and specific receptor targeting.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If novel indole compounds are developed to specifically target AhR, then therapeutic effectiveness for cancer and immune modulation is improved, but the complexity of compound development and characterization increases

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidcompound development complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the complex task of AhR-targeted drug development into manageable sections: (1) designing core indole structures with specific substituent patterns, (2) synthesizing individual compound variants, (3) characterizing AhR binding properties, and (4) evaluating therapeutic effects. This segmented approach reduces the overall complexity while maintaining therapeutic effectiveness.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent systematically varies chemical parameters (substituents at different positions on the indole ring) to create a library of compounds with graded AhR binding affinities. This parameter-based approach allows for methodical optimization without requiring complete redesign of the entire development process, thereby managing complexity while improving therapeutic effectiveness.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS11891386B2Indole compounds and their use
Publication Date: 2024.02.06 ARIAGEN INC
  • US11891386B2 patent drawing
  • US11891386B2 patent drawing
  • US11891386B2 patent drawing

AI summary

The present disclosure relates to indole compounds and pharmaceutical compositions thereof, and their use in stimulating the immune system of patients in need thereof and in treating cancer.