Delta Opioid Receptor Modulators for Seizure-Free Pain Treatment

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Current delta opioid receptor agonists have shown potential for treating various CNS disorders but are hindered by seizure risks, necessitating the development of safe and effective delta opioid receptor modulators for conditions like neuropathic pain, migraines, depression, and anxiety.

Innovation Solution

Development of specific compounds such as B1049, B0704, B0707, B0720, B0876, B1079, B1145, B1205, B1211, B1365, and B1401, or their pharmaceutically acceptable salts, which can modulate delta opioid receptor activity to treat pain, migraines, headaches, depression, anxiety, and overactive bladder without causing seizures.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If delta opioid receptor agonists are used to treat CNS disorders, then therapeutic efficacy is improved, but seizure risk increases

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidseizure risk

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of delta opioid receptor ligands through systematic variations in molecular parameters (R1-R6 substituents, ring structures, stereochemistry) to transition from full agonists with seizure risk to modulators with improved safety profiles while maintaining therapeutic efficacy

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention inverts the traditional agonist approach by developing delta opioid receptor modulators that can function as agonists, antagonists, or partial agonists depending on conditions, thereby avoiding the seizure-inducing properties of full agonists while preserving therapeutic benefits

Inventive Principle:

Principle #13The other way round (Inversion)

2Adaptability or versatility

If selective delta opioid receptor agonists are developed, then treatment specificity is improved, but safety profile deteriorates due to seizure induction

Engineering Contradiction:

Improvetreatment specificityVSAvoidsafety profile

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The patent implements dynamics by creating compounds with dynamic functional properties that can adapt their activity (agonist/antagonist/partial agonist) based on receptor state and tissue context, allowing selective delta opioid receptor modulation without fixed seizure-inducing effects

Inventive Principle:

Principle #15Dynamics

Solution Approach 2:

The invention uses composite molecular structures combining multiple structural elements (heterocyclic rings, aromatic systems, linker moieties with specific R-group configurations) to achieve both selective delta opioid receptor binding and improved safety profile

Inventive Principle:

Principle #40Composite materials

Data Source

PatentUS20230203002A16-membered aza-heterocyclic containing delta-opioid receptor modulating compounds, methods of using and making the same

Publication Date: 2023.06.29 TREVENA INC

AI summary

The present embodiments are directed, in part, to compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof for modulating the activity of delta opioid receptor, biased and/or unbiased, and/or methods for treating pain, migraines, headaches, depression, Parkinsons Disease, anxiety, and/or overactive bladder, and other disorders and conditions described herein or any combination thereof.