Pyrazine Carbamate Modulators for GluN2B Receptor Activity

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Solution Overview

Problem

Current treatments for neurological and psychiatric disorders lack effective modulators for GluN2B-containing NMDA receptors, which are crucial for various brain functions and disorders, including depression, Alzheimer's disease, and pain management.

Innovation Solution

Development of compounds of Formula (I) and their pharmaceutically acceptable salts, solvates, isotopic variants, and N-oxides, which modulate GluN2B receptor activity, offering potential therapeutic agents for treating a range of neurological and psychiatric conditions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for neurological and psychiatric disorders are used, then existing therapeutic options are available, but effective modulators for GluN2B-containing NMDA receptors are lacking

Engineering Contradiction:

Improveeffectiveness of treatmentVSAvoidavailability of GluN2B receptor modulators

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by systematically varying chemical structures of pyrazine carbamate compounds (Formula I) to optimize GluN2B receptor modulation. Different substituents (R1-R6) and molecular parameters are adjusted to achieve desired pharmacological effects, addressing the lack of effective GluN2B modulators while maintaining treatment reliability

Inventive Principle:

Principle #35Parameter changes

2Adaptability or versatility

If compounds of Formula (I) are developed to modulate GluN2B receptor activity, then novel therapeutic approaches are provided, but the complexity of compound structure and synthesis increases

Engineering Contradiction:

Improvetherapeutic potential for neurological disordersVSAvoidcompound structure complexity

Core Design Contradiction:

Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the GluN2B modulator development into distinct compound series (Formula I, Ia, Ib, Ic, Id) with systematic substituent variations. This modular approach allows independent optimization of different molecular regions (R1-R6 substituents) to achieve therapeutic effects while managing structural complexity

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent applies universality by designing pyrazine carbamate compounds with multiple potential therapeutic applications across different neurological and psychiatric disorders (depression, Alzheimer's disease, pain management). The core pyrazine carbamate structure serves as a universal scaffold that can be adapted for various GluN2B-mediated conditions

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentUS11459336B2Pyrazine carbamates and their use as GluN2B receptor modulators

Publication Date: 2022.10.04 JANSSEN PHARMA NV

AI summary

Pyridine carbamates, pharmaceutical compositions containing pyridine carbamates, and uses of the pyridine carbamates and pharmaceutical compositions for modulating GluN2B receptors and for treating diseases, disorders, and medical conditions mediated by GluN2B receptor activity.