Nitrogen-Containing Heterocyclic Derivatives for GPR55 Treatment Coverage

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Solution Overview

Problem

There is a need for effective treatments targeting disorders associated with GPR55 activity, including Parkinson's Disease, Epilepsy, Anxiety, Pain/Analgesia, Depression, Alzheimer's Disease, and Neuroprotection, as current therapies do not fully address these conditions.

Innovation Solution

Development of nitrogen-containing heterocyclic derivatives that act as modulators of the GPR55 receptor, potentially providing therapeutic benefits in neurological and neurodegenerative disorders.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current therapies are used for treating neurological disorders, then treatment is provided, but they do not fully address the conditions associated with GPR55 activity

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidcoverage of GPR55-related disorders

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent develops novel nitrogen-containing heterocyclic compounds with specific molecular structures designed to modulate GPR55 receptor activity. By changing the chemical parameters of the compounds (nitrogen heterocyclic groups, specific substituents R1-R6), the invention creates substances that can effectively target GPR55-related disorders where current therapies fail, thereby improving treatment effectiveness and coverage

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent divides the treatment approach into specific compound classes (formula I compounds with defined structural components A1-A6 and substituents R1-R6). This segmentation allows for targeted development of GPR55 modulators with specific properties, enabling more precise and effective treatment of neurological disorders associated with GPR55 activity

Inventive Principle:

Principle #1Segmentation

2Reliability

If new GPR55 modulator compounds are developed, then therapeutic utility in neurological disorders is improved, but compound structure complexity increases

Engineering Contradiction:

Improvetherapeutic utilityVSAvoidcompound structure

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent systematically varies parameters within the compound structure (different nitrogen heterocyclic groups for A1-A6, various substituents for R1-R6 including halo, alkyl, alkenyl, alkynyl, cycloalkyl, and their derivatives) to optimize therapeutic utility while maintaining a manageable structural framework based on the core formula I

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates a universal compound platform (formula I) that can address multiple GPR55-related neurological disorders (Parkinson's Disease, Epilepsy, Anxiety, Pain, Depression, Alzheimer's Disease, and Neuroprotection). This multi-functional approach allows a single compound class to treat various conditions, reducing the need for entirely separate complex structures for each disorder

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentUS20250282728A1Nitrogen comprising heterocyclic derivatives for the treatment of disorders associated with GPR55 receptor

Publication Date: 2025.09.11 CEREVANCE INC

AI summary

The present invention provides compounds of formula (I) and pharmaceutically acceptable salts, solvates and prodrugs thereof: Formula (I) wherein n, R1, R2, R3, R4, R5, A1, A2, A3, A4 and A5 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly for use in treating disorders associated with GPR55 activity.