Purified (+)-cis-THC Enantiomer for Epilepsy Treatment

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Solution Overview

Problem

The therapeutic potential of (+)-cis-tetrahydrocannabinol (THC) has not been established, and existing methods do not effectively utilize this enantiomer for medicinal purposes due to its low natural occurrence and lack of understanding of its pharmacological activity compared to its (−)-trans isomer.

Innovation Solution

The development of highly purified (+)-cis-THC, either from plant extracts or synthetic production, for use as a medicament, with specific dosing ranges and combination with pharmaceutically acceptable excipients, demonstrating its efficacy in animal models of disease, particularly in epilepsy and seizure treatment.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Manufacturing precision

If highly purified (+)-cis-THC is produced through synthetic means or extraction, then the purity and therapeutic efficacy are improved, but the manufacturing complexity and cost increase

Engineering Contradiction:
Improvepurity of (+)-cis-THCVSAvoidmanufacturing process complexity
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The patent extracts (+)-cis-THC from cannabis plant material through purification processes, separating the desired enantiomer from other cannabinoids and plant compounds. This extraction approach obtains highly purified (+)-cis-THC while managing manufacturing complexity through established extraction and purification techniques.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent employs synthetic methods that control stereochemical parameters to produce enantiomerically pure (+)-cis-THC. By manipulating synthesis conditions and catalysts, the manufacturing process achieves high purity of the specific enantiomer while managing process complexity through controlled chemical transformations.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If (+)-cis-THC is used as a medicament, then therapeutic efficacy is improved, but the lack of established pharmacological data creates uncertainty

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidpharmacological data
Core Design Contradiction:
ReliabilityVSLoss of information

Solution Approach 1:

The patent conducts preliminary pharmacological studies and animal model testing to establish the safety and efficacy profile of (+)-cis-THC before clinical use. This preliminary action generates essential pharmacological data, reducing uncertainty and informing dosing recommendations for future therapeutic applications.

Inventive Principle:
Principle #10Preliminary action

3Quantity of substance

If natural cannabis plant strains are used to obtain (+)-cis-THC, then the compound is obtained naturally, but the concentration is too low for practical use

Engineering Contradiction:
Improveconcentration of (+)-cis-THCVSAvoidextraction efficiency
Core Design Contradiction:
Quantity of substanceVSEase of manufacture

Solution Approach 1:

The patent uses extraction and purification processes to concentrate (+)-cis-THC from low-concentration plant material. By selectively extracting and purifying the target compound, the method overcomes the low natural concentration issue while maintaining a practical starting material source.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent transitions from relying on natural plant concentrations to using synthetic production methods that can achieve high concentrations of (+)-cis-THC. This parameter change in the production approach directly addresses the low concentration limitation of natural sources.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS20220387377A1(+)-CIS tetrahydrocannabinol ((+)-CIS-THC) for use as a medicament
Publication Date: 2022.12.08 JAZZ PHARM RES UK LTD
  • US20220387377A1 patent drawing
  • US20220387377A1 patent drawing
  • US20220387377A1 patent drawing

AI summary

The present invention relates to a tetrahydrocannabinol (THC) type cannabinoid compound for use as a medicament. The THC-type cannabinoid is an enantiomer of the (−)-trans- tetrahydrocannabinol which is a naturally occurring cannabinoid that can be found in cannabis plant strains which have been bred to yield THC as the dominant cannabinoid. The particular enantiomer (+)-cis tetrahydrocannabinol has been found to have properties which are different from the naturally occurring (−)-trans-THC. The cannabinoid (+)-cis-THC has been found to occur in low concentrations in particular cannabis plant strains which have been bred to produce cannabidiol (CBD) as the dominant cannabinoid. Furthermore, the cannabinoid can be produced by synthetic means.