7-Hydroxy-CBD-C4 Anticonvulsant Activity in Epilepsy

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Solution Overview

Problem

Current anti-epileptic drugs (AEDs) fail to provide seizure freedom for approximately 30% of epilepsy patients, known as treatment-resistant epilepsy, necessitating the development of new compounds with anticonvulsant properties.

Innovation Solution

The development of novel compounds 7-hydroxy-cannabidol-C4 (7-OH-CBD-C4) and 7-carboxy-cannabidiol-C4 (7-COOH-CBD-C4), which are biologically active and can be administered via various routes, including oral, transdermal, and nasal, for the treatment of epilepsy, either alone or in combination with existing AEDs.

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

Engineering Contradiction:
Improveseizure freedom rateVSAvoidtreatment resistance
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent modifies the chemical structure of existing CBD derivatives by changing parameters such as hydroxylation at position 7 and chain length (C4 variant), creating new compounds with potentially improved anticonvulsant activity to overcome treatment resistance

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention combines multiple structural features (cannabidiol backbone, C4 chain, 7-hydroxy or 7-carboxy substitution) to create composite molecular structures that may synergistically enhance anticonvulsant properties while reducing treatment resistance

Inventive Principle:
Principle #40Composite materials

2Reliability

If new compounds are developed for treatment-resistant epilepsy, then potential therapeutic benefits increase, but development complexity and time increase

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidcompound development complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent focuses on specific structural modifications (7-hydroxy and 7-carboxy groups on C4-cannabidiol) rather than exploring all possible CBD derivatives, segmenting the search space to identify promising candidates more efficiently

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent builds upon preliminary data showing anticonvulsant activity of related CBD derivatives, using this prior knowledge to guide the development of more potent compounds and reduce unnecessary exploration

Inventive Principle:
Principle #10Preliminary action

Data Source

PatentUS20240254072A1Derivatives of cannabidiol-c4 for the treatment of epilepsy
Publication Date: 2024.08.01 JAZZ PHARM RES UK LTD
  • US20240254072A1 patent drawing
  • US20240254072A1 patent drawing
  • US20240254072A1 patent drawing

AI summary

The present invention relates to compounds that are pharmaceutically active and methods of preparation thereof. The compounds of the invention are 7-hydroxy-cannabidol-C4 (7-OH-CBD-C4) and 7-carboxy-cannabidiol-C4 (7-COOH-CBD-C4). The compounds of the invention are 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 compounds of the invention.