(1R,5S)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane Opioid Adjunct

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Solution Overview

Problem

The use of opioids for chronic pain management is associated with risks of opioid-induced depression, hyperalgesia, non-medical use, addiction, overdose, and adverse health events, particularly in patients with prolonged treatment, necessitating a need for non-opioid adjunctive medications that can reduce opioid doses and duration of treatment.

Innovation Solution

Administering (1R,5S)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane, in free or pharmaceutically acceptable salt form, in conjunction with opioids to achieve an opioid-sparing effect, reduce peak daily doses, prevent dose escalation, facilitate tapering, and manage opioid-induced adverse effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If opioids are used for chronic pain management, then pain relief is achieved, but risks of addiction, overdose, and adverse health events increase

Engineering Contradiction:

Improvepain relief effectivenessVSAvoidopioid-related adverse events

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces (1R,5S)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane as a non-opioid adjunctive medication that acts as an intermediary agent. This compound enhances opioid analgesic effects while reducing the required opioid dose, thereby maintaining pain relief effectiveness while minimizing opioid-related adverse events including addiction and overdose risks

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the dosage parameter of opioids by using adjunctive (1R,5S)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane to reduce the effective opioid dose by at least 10-50% or more. This parameter change maintains therapeutic pain relief while reducing exposure to harmful opioid effects

Inventive Principle:

Principle #35Parameter changes

2Reliability

If opioid dose and duration are increased to manage chronic pain, then pain control is improved, but development of opioid use disorder and tolerance increases

Engineering Contradiction:

Improvepain control effectivenessVSAvoidopioid use disorder and tolerance

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The non-opioid adjunctive medication (1R,5S)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane serves as a mediator that allows effective pain control without requiring increased opioid doses. It blocks opioid receptors and reduces opioid metabolism, thereby preventing tolerance development and opioid use disorder while maintaining analgesic effectiveness

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent applies preliminary anti-action by using (1R,5S)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane to preemptively block the development of opioid tolerance and use disorder. The adjunctive medication is administered concurrently with opioids to prevent these harmful effects before they develop, rather than treating them after onset

Inventive Principle:

Principle #9Preliminary anti-action

3Duration of action of stationary object

If opioid treatment is continued for prolonged periods, then chronic pain management is maintained, but negative gastrointestinal effects and other adverse effects are exacerbated

Engineering Contradiction:

Improveduration of opioid treatmentVSAvoidgastrointestinal effects and adverse events

Core Design Contradiction:

Duration of action of stationary objectVSObject-generated harmful factors

Solution Approach 1:

The adjunctive medication (1R,5S)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane acts as a protective intermediary that allows prolonged opioid treatment to be maintained while reducing adverse effects. It achieves this by reducing the required opioid dose and blocking opioid receptors in the gastrointestinal tract, thereby preventing opioid-induced constipation and other GI effects during long-term treatment

Inventive Principle:

Principle #24Intermediary (Mediator)

Data Source

PatentUS12257233B2Methods

Publication Date: 2025.03.25 ETHISMOS RESEARCH INC

AI summary

Provided are methods of using (1R,5S)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane, in free or pharmaceutically acceptable salt form.