Cannabinoid Derivatives for Receptor Modulation

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Solution Overview

Problem

There is a need for novel ligands of cannabinoid receptors that have the potential for therapeutic benefit, as existing methods for isolating and purifying cannabinoids are inefficient and often result in low bioavailability and adverse effects due to smoking or other delivery methods.

Innovation Solution

Development of compounds of formula (I) and their pharmaceutical compositions, which can act as ligands to cannabinoid receptors, including CB1, CB2, and other related receptors, for the treatment or prevention of various diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If smoking Cannabis is used for medicinal purposes, then therapeutic benefits are achieved, but carcinogens and toxins are introduced causing lung damage and emphysema

Engineering Contradiction:

Improvetherapeutic benefitVSAvoidlung damage

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent extracts and isolates specific cannabinoids (CBD, CBC, CBG) from Cannabis plant material through purification processes, separating the therapeutic compounds from harmful combustion byproducts and toxins present in smoked plant matter

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent uses purified cannabinoid compounds as intermediaries to deliver therapeutic effects without requiring combustion of plant material, thereby eliminating direct exposure to carcinogens and toxins while maintaining CB1 and CB2 receptor modulation

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If smoking Cannabis is used for medicinal purposes, then therapeutic effects are achieved, but control over proper dosing is difficult due to active ingredient fluctuations

Engineering Contradiction:

Improvetherapeutic effectVSAvoiddosing control

Core Design Contradiction:

ReliabilityVSManufacturing precision

Solution Approach 1:

The patent replaces the mechanical process of smoking and burning plant material with controlled delivery systems that administer precise amounts of purified cannabinoids, enabling accurate dosing independent of plant varietal variations or growing conditions

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

Solution Approach 2:

The patent establishes controlled parameters for cannabinoid concentration and purity through purification processes, transforming the variable composition of raw plant material into standardized pharmaceutical compositions with consistent active ingredient levels

Inventive Principle:

Principle #35Parameter changes

3Reliability

If smoking Cannabis is used for medicinal purposes, then therapeutic benefits are achieved, but bioavailability of target compounds is relatively low

Engineering Contradiction:

Improvetherapeutic benefitVSAvoidbioavailability

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

The patent extracts purified cannabinoid compounds from plant material, removing impurities and enhancing the concentration of active ingredients to improve bioavailability compared to smoking whole plant matter

Inventive Principle:

Principle #2Taking out (Extraction)

Data Source

PatentUS12325709B2Cannabinoid derivatives

Publication Date: 2025.06.10 CANOPY GROWTH CORP

AI summary

This disclosure relates to cannabinoid derivatives of Formula (I), wherein R4 or R7 is a carboxamide group, pharmaceutical compositions comprising these compounds and methods of using the cannabinoid derivatives. These compounds are potential cannabinoid receptor inhibitors, including CB1 and CB2 receptors.