NR2B Receptor Modulators via Formula I Substituted Imidazopyridinones

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Solution Overview

Problem

Current treatments for neurological and psychiatric disorders associated with NR2B receptor activity lack effective modulators, limiting therapeutic options for conditions such as depression, Alzheimer's disease, Parkinson's disease, and pain management.

Innovation Solution

Development of compounds of Formula (I), which include specific chemical structures that modulate NR2B receptor activity, allowing for the creation of pharmaceutical compositions and methods for treating diseases mediated by NR2B receptor activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for neurological and psychiatric disorders are used, then existing therapeutic options are maintained, but effective modulators for NR2B receptor activity are lacking

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidtherapeutic options

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by systematically varying chemical structures (Formula I compounds with different R1, R2, R3, R4 substituents) to optimize NR2B receptor binding affinity and modulatory efficacy, thereby improving therapeutic effectiveness while expanding treatment options for disorders mediated by NR2B receptor activity

Inventive Principle:

Principle #35Parameter changes

2Adaptability or versatility

If compounds of Formula (I) are developed to modulate NR2B receptor activity, then new therapeutic avenues are opened, but the complexity of identifying effective modulators increases

Engineering Contradiction:

Improvetreatment avenuesVSAvoidcompound identification process

Core Design Contradiction:

Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent segments the complex molecule identification process into systematic chemical series (Formula I with defined substituent patterns), allowing for organized screening and development of NR2B modulators through structured chemical space exploration rather than random compound discovery

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent develops compounds of Formula (I) that serve as universal NR2B receptor modulators applicable across multiple neurological and psychiatric disorders (depression, Alzheimer's, Parkinson's, pain management), enabling a single compound class to address diverse conditions mediated by NR2B receptor activity

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentUS11759455B2Substituted 1H-imidazo[4,5-b]pyridin-2(3H)-ones and their use as GLUN2B receptor modulators

Publication Date: 2023.09.19 JANSSEN PHARMA NV

AI summary

Substituted 1H-imidazo[4,5-b]pyridin-2(3H)-ones as NR2B receptor ligands. Such compounds may be used in NR2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by NR2B receptor activity.