Sulfur and Selenium Cannabinoid Compounds for Receptor Selectivity
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Solution Overview
Problem
There is a scarcity of compounds that are potent, efficacious, and selective agonists or antagonists of CB1, CB2, GPR55, GPR18, GPR119, and other novel or putative cannabinoid receptors, while also being effective in treating various diseases and conditions.
Innovation Solution
Development of sulfur- and selenium-containing compounds that act as agonists and/or antagonists of cannabinoid receptors, along with methods of making these compounds and pharmaceutical compositions for treating metabolic disorders, psychiatric disorders, neurological disorders, pain disorders, gastrointestinal disorders, cancers, inflammation-related disorders, and substance overuse associated pathologies.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If natural cannabinoids are used, then therapeutic effects are achieved, but solubility and stability are insufficient
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of natural cannabinoids through systematic variations in substituents (R1-R6, R8-R11) at positions on the core cannabinoid molecule. These structural parameter changes improve solubility and stability while maintaining or enhancing therapeutic efficacy at cannabinoid receptors.
Solution Approach 2:
The patent creates composite chemical structures by combining the core cannabinoid scaffold with various functional groups and substituents. These composite molecular structures integrate the therapeutic properties of natural cannabinoids with improved pharmacokinetic properties including solubility and stability.
2Reliability
If Δ9-THC and CBD are used, then treatment effects are achieved, but psychotropic effects and limited receptor selectivity occur
Solution Approach 1:
The patent applies local quality by introducing specific substituents at particular positions (R1-R6, R8-R11) on the cannabinoid molecule to modulate receptor selectivity. Certain local structural modifications preferentially enhance affinity for CB2 receptors while reducing affinity for CB1 receptors, thereby reducing psychotropic effects while maintaining therapeutic benefits.
Solution Approach 2:
The patent inverts the typical cannabinoid profile by designing compounds that prioritize CB2 receptor selectivity over CB1 receptor activity. This inverted approach reverses the conventional pattern where CB1 activity dominates, thereby reducing psychotropic side effects while preserving anti-inflammatory and therapeutic effects through CB2 activation.
3Adaptability or versatility
If cannabinoid compounds are developed for broad disease treatment, then versatility is improved, but compound selectivity and potency are reduced
Solution Approach 1:
The patent applies universality by designing a core cannabinoid structure with multiple substitutable positions (R1-R6, R8-R11) that can be configured to target different cannabinoid receptors (CB1, CB2, GPR55, GPR18, GPR119). This universal scaffold enables a single compound design to potentially treat multiple disease conditions including metabolic disorders, inflammatory conditions, neurological disorders, and pain disorders.
Solution Approach 2:
The patent applies segmentation by dividing the cannabinoid molecule into a core scaffold and multiple independent substituent positions. Each position (R1-R6, R8-R11) can be independently optimized to enhance selectivity for specific receptors while maintaining the overall therapeutic profile, allowing precise tuning of potency and selectivity for different disease indications.
Data Source
AI summary
In accordance with the purpose(s) of the present disclosure, as embodied and broadly described herein, the disclosure, in one aspect, relates to sulfur- and selenium-containing compounds that act as agonists and/or antagonists of cannabinoid receptors, methods of making same, pharmaceutical compositions comprising the same, and methods of treating metabolic disorders, psychiatric disorders, neurological disorders, pain disorders, gastrointestinal disorders, cancers, inflammation-related disorders, substance abuse associated pathologies, and other conditions using the same.