IDO Inhibitor Compounds Modulating Tryptophan Metabolism

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Solution Overview

Problem

Current IDO inhibitors have limitations in efficacy for treating proliferative disorders such as cancer, viral infections, and autoimmune diseases, necessitating the development of new IDO modulators and compositions.

Innovation Solution

Development of compounds of formula (I) and their pharmaceutical compositions that can modulate or inhibit indoleamine 2,3-dioxygenase (IDO) activity, including pharmaceutically acceptable salts, stereoisomers, and solvates, for use in treating cancer and other IDO-related diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current IDO inhibitors are used to treat proliferative disorders, then some therapeutic effect is achieved, but efficacy is limited

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoid适用范围
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of IDO inhibitors through various substituents (R1-R6, A, Q, X) to optimize therapeutic efficacy. The systematic variation of molecular parameters (chemical groups, positions, configurations) enables improved inhibition potency and broader applicability across different proliferative disorders while maintaining selective IDO inhibition.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If new IDO modulators are developed to improve efficacy, then therapeutic benefits are enhanced, but compound complexity increases

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoid化合物结构复杂性
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the IDO inhibitor molecule into distinct functional segments (core structure with defined A, Q, X, R1-R6 positions). Each segment can be independently optimized and combined, allowing systematic development of effective inhibitors while managing molecular complexity through modular design principles.

Inventive Principle:
Principle #1Segmentation

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

The compounds effectively modulate IDO activity, providing therapeutic benefits in treating cancer, viral infections, and autoimmune diseases by altering tryptophan metabolism and immunosuppression, offering improved efficacy over existing inhibitors.

Implementation Method 1

The compounds effectively modulate IDO activity, providing therapeutic benefits in treating cancer, viral infections, and autoimmune diseases by altering tryptophan metabolism and immunosuppression

Methodology Applied
Scientific EffectEnzyme inhibition: Enzyme

Data Source

PatentUS12145927B2Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
Publication Date: 2024.11.19 BRISTOL MYERS SQUIBB CO
  • US12145927B2 patent drawing
  • US12145927B2 patent drawing
  • US12145927B2 patent drawing

AI summary

The present invention provides compounds of formula (I) wherein all of the variables are as defined herein. These compounds are inhibitors of indoleamine 2,3-dioxygenase (IDO), which may be used as medicaments for the treatment of proliferative disorders, such as cancer, viral infections and/or autoimmune diseases.