Cannabinoid Receptor Modulators for Alcohol Abuse Treatment

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Solution Overview

Problem

Current treatments for alcohol abuse and dependence are inadequate due to non-compliance and potential hepatotoxicity, and there is a need for safer and more effective therapeutic options for conditions modulated by cannabinoid receptors, such as pain and obesity.

Innovation Solution

Development of cannabinoid receptor modulators, specifically compounds of the formula and their analogs, which can act as CB1 or CB2 receptor agonists or antagonists to treat alcohol abuse and other disorders without the hepatotoxicity associated with existing treatments.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for alcohol abuse are used, then therapeutic effect is achieved, but hepatotoxicity occurs

Engineering Contradiction:
Improvetherapeutic effectVSAvoidhepatotoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by developing novel chemical compounds with modified molecular structures (formula I with specific substituents R1-R6) that alter the pharmacological parameters of cannabinoid receptor interaction. These structural modifications enable the compounds to achieve therapeutic effects while reducing hepatotoxicity by changing how the substance interacts with biological systems, specifically targeting CB1 and CB2 receptors with improved safety profiles.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If anandamide is used to activate CB1 receptors, then presynaptic inhibition is achieved, but rapid enzymatic hydrolysis occurs

Engineering Contradiction:
Improvereceptor activationVSAvoidstability in gastrointestinal tract
Core Design Contradiction:
ReliabilityVSDuration of action of stationary object

Solution Approach 1:

The patent applies this principle by designing synthetic cannabinoid compounds that, while structurally complex, are designed for single-use therapeutic administration. These compounds provide sufficient duration of action for therapeutic effect without requiring long-term stability in the gastrointestinal tract, as they are administered systemically rather than orally in a way that requires GI persistence. The compounds achieve their purpose in a single therapeutic dose.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The patent applies composite materials by creating complex molecular structures that combine multiple functional groups (amino, carbonyl, hydroxyl, and various substituted phenyl groups) within a single cannabinoid compound. This composite molecular architecture provides both the necessary receptor binding affinity for CB1/CB2 activation and improved metabolic stability compared to natural anandamide, resolving the contradiction between activity and stability.

Inventive Principle:
Principle #40Composite materials

Data Source

PatentEP1902034B1Novel cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation
Publication Date: 2011.03.30 ICHNOS SCIENCES SA
  • EP1902034B1 patent drawingFigure 1
  • EP1902034B1 patent drawingFigure 2
  • EP1902034B1 patent drawingFigure 3

AI summary

The present invention relates to novel cannabinoid receptor modulators, in particular cannabinoid 1 (CBl) or cannabinoid 2 (CB2) receptor modulators, and uses thereof for treating diseases, conditions and/or disorders modulated by a cannabinoid receptor (such as pain, neurodegenative disorders, eating disorders, weight loss or control, and obesity).