6-Hydroxy-CBD-C4 Anticonvulsant Activity in Treatment-Resistant Epilepsy

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Solution Overview

Problem

Current anti-epileptic drugs (AEDs) are ineffective for 30% of epilepsy patients, leading to treatment-resistant epilepsy, particularly in children and young adults, who often suffer from neurological damage due to frequent seizures, necessitating the development of new therapeutic options.

Innovation Solution

The novel compound 6-hydroxy-cannabidol-C4 (6-OH-CBD-C4) is synthesized and used in pharmaceutical compositions for administration via various routes, including oral, transdermal, and nasal, to treat epilepsy, either alone or in combination with existing AEDs, through a process involving acylation, oxidation, and reduction steps.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing anti-epileptic drugs are used, then most patients can control their symptoms, but 30% of patients cannot achieve seizure freedom and develop treatment-resistant epilepsy

Engineering Contradiction:
Improveseizure control effectivenessVSAvoidtreatment resistance
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent introduces a novel chemical compound with a modified molecular structure (6-hydroxy-cannabidol-C4) that differs from existing AEDs. This structural parameter change enables the compound to interact with different neuronal targets and pathways, potentially overcoming treatment resistance in patients who do not respond to conventional AEDs

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention combines the cannabidol-C4 core structure with a hydroxyl group at the 6-position to create a composite molecular structure. This composite approach integrates the known anti-convulsant properties of cannabidol-C4 with the additional functional group, aiming to enhance or modify the pharmacological profile to treat resistant epilepsy

Inventive Principle:
Principle #40Composite materials

2Reliability

If children undergo frequent seizures, then epilepsy symptoms manifest, but neurological damage occurs causing cognitive, behavioral and motor delays

Engineering Contradiction:
Improveseizure controlVSAvoidneurological damage
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent aims to prevent neurological damage by administering the novel compound before seizures cause cumulative harm. The compound is designed to proactively stabilize neuronal excitability and prevent seizure onset, thereby protecting the developing brain from the harmful effects of repeated seizures in pediatric patients

Inventive Principle:
Principle #9Preliminary anti-action

3Measurement precision

If diagnosis investigations are undertaken for childhood epilepsy, then the cause can be identified, but diagnosis may take some time

Engineering Contradiction:
Improvediagnosis accuracyVSAvoiddiagnosis time
Core Design Contradiction:
Measurement precisionVSLoss of time

Solution Approach 1:

The patent provides a therapeutic solution that can be implemented while diagnostic investigations are ongoing or completed. The novel compound offers immediate treatment potential without requiring extended diagnostic periods, allowing parallel pursuit of both accurate diagnosis and effective symptom management

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

Data Source

PatentUS20240360060A16-hydroxy-cannabidiol-c4
Publication Date: 2024.10.31 JAZZ PHARM RES UK LTD
  • US20240360060A1 patent drawing
  • US20240360060A1 patent drawing
  • US20240360060A1 patent drawing

AI summary

The present invention relates to a compound that is pharmaceutically active and methods of preparation thereof. The compound of the invention is 6-hydroxy-cannabidol-C4 (6-OH-CBD-C4). The compound of the invention is related to cannabidiol (CBD). CBD is a non-psychoactive cannabinoid which has been used to treat various diseases and disorders. While such treatments hold promise, there remains a need in the art for more effective treatments and this has been brought about by way of the compound of the invention.