Aryl Analog NRF2 Regulators for Oxidative Stress Management
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Solution Overview
Problem
Current treatments for various diseases such as COPD, asthma, and kidney diseases lack effective NRF2 regulators, leading to inadequate oxidative stress management and disease progression.
Innovation Solution
Development of aryl analogs and their pharmaceutical compositions that act as NRF2 regulators, capable of treating and preventing conditions associated with NRF2 imbalance by modulating the NRF2 pathway.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments are used for diseases like COPD and asthma, then disease management is maintained at conventional levels, but NRF2 regulation is insufficient leading to inadequate oxidative stress management and disease progression
Solution Approach 1:
The patent employs parameter changes by developing aryl analogs with modified chemical structures (varying substituents, core structures, and molecular weights) to optimize NRF2 regulation activity. This allows tuning of the compound's ability to regulate NRF2 while maintaining therapeutic efficacy for oxidative stress-related diseases
Solution Approach 2:
The patent utilizes composite materials by creating pharmaceutical compositions that combine aryl analog compounds with pharmaceutically acceptable excipients. This composite approach enables the active compound to function effectively in a biological system while maintaining stability and bioavailability
2Reliability
If NRF2 activity is increased to enhance cytoprotection and structural repair, then disease progression is slowed, but the complexity of regulating NRF2 balance increases
Solution Approach 1:
The patent uses intermediary compounds (aryl analogs) that act as mediators between the therapeutic goal and the NRF2 pathway. These compounds indirectly regulate NRF2 activity by modulating KEAP1-NRF2 interaction, avoiding the need for direct manipulation of the complex NRF2 regulatory system while achieving desired cytoprotection effects
Solution Approach 2:
The patent enables self-service by designing compounds that automatically regulate NRF2 activity in response to oxidative stress conditions. The aryl analogs function as NRF2 regulators that adaptively control the pathway based on cellular needs, eliminating the requirement for external monitoring and adjustment of the complex regulatory system
Data Source
AI summary
The present invention relates to aryl analogs, pharmaceutical compositions containing them and their use as NRF2 regulators.