IDO Inhibitor Compounds Modulating Enzymatic Activity
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Solution Overview
Problem
Current IDO inhibitors have limitations in efficacy for treating proliferative disorders, cancer, viral infections, and autoimmune diseases, necessitating the development of new IDO modulators and compositions.
Innovation Solution
Compounds of formulas I and II, which include specific structural elements such as various substituents and functional groups, are developed to modulate IDO activity, offering potential therapeutic benefits in treating cancer, viral infections, and autoimmune diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current IDO inhibitors are used to treat proliferative disorders and cancer, then immune suppression is reduced, but efficacy is limited
Solution Approach 1:
The patent modifies the chemical structure of IDO inhibitors by changing molecular parameters such as substituting different groups at specific positions (e.g., R1, R2, R3 positions on the indole ring), varying linker lengths and types, and adjusting heteroatom positions. These parameter changes create a series of analogs with potentially improved efficacy and broader applicability across different disease states while maintaining the core inhibitory mechanism against IDO enzyme.
2Reliability
If IDO activity is inhibited to enhance immune response, then tumor growth is suppressed, but tryptophan degradation is reduced
Solution Approach 1:
The patent extracts and isolates the specific enzymatic function of IDO that catalyzes tryptophan degradation. By designing inhibitors that selectively target this enzymatic activity without affecting other metabolic pathways, the invention achieves immune response enhancement through IDO inhibition while minimizing unwanted effects on overall tryptophan metabolism and maintaining physiological balance.
3Reliability
If new IDO modulators are developed to overcome efficacy limitations, then therapeutic benefits are improved, but compound complexity increases
Solution Approach 1:
The patent segments the IDO inhibitor molecule into distinct functional modules: a core indole structure, various substituent groups (R1, R2, R3), linker regions, and heteroatom components. This segmentation allows for systematic optimization of each module independently to enhance therapeutic benefits while maintaining reasonable structural complexity through modular design principles.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
These compounds effectively inhibit IDO activity, providing therapeutic benefits in treating a range of diseases by modulating immune responses and enhancing tryptophan levels, thereby addressing the limitations of existing IDO inhibitors.
Implementation Method 1
Inhibitors of indoleamine 2,3-dioxygenase and methods of their use... IDO is an oxidoreductase and one of two enzymes that catalyze the first and rate-limiting step in the conversion of tryptophan to N-formylkynurenine... These compounds effectively inhibit IDO activity
Data Source
AI summary
There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.