Cannabinoid Receptor Modulator Formula Ia for Pain Management

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for pain management, particularly for conditions like osteoarthritis and cancer-related pain, often rely on opioids and NSAIDs, which can have limitations in efficacy and are associated with side effects, and there is a need for alternative analgesic agents that can provide effective pain relief without these drawbacks.

Innovation Solution

A composition comprising a compound of Formula Ia or its pharmaceutically acceptable salt, solvate, hydrate, and N-oxide, combined with known analgesic, antidiabetic, osteoarthritis, and anticancer agents, is administered to provide therapeutically effective pain management by modulating cannabinoid receptors, thereby addressing both acute and chronic pain conditions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If opioids and NSAIDs are used for pain management, then pain relief efficacy is improved, but side effects increase

Engineering Contradiction:
Improvepain relief efficacyVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent segments the pain management approach by introducing a novel cannabinoid receptor modulator (Formula Ia) that acts through a different mechanism than traditional opioids and NSAIDs. This segmentation allows for effective pain relief through CB1 and CB2 receptor modulation while avoiding the side effect profile of conventional analgesics.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs a composite pharmaceutical composition combining the cannabinoid receptor modulator of Formula Ia with other therapeutic agents. This composite approach leverages the unique mechanism of action of the cannabinoid modulator to achieve synergistic pain relief while minimizing the harmful effects associated with single-agent therapy.

Inventive Principle:
Principle #40Composite materials

2Reliability

If higher doses of individual drugs are used to improve pain relief, then efficacy is improved, but side effects increase

Engineering Contradiction:
Improvepain relief efficacyVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent merges the cannabinoid receptor modulator of Formula Ia with known analgesic and anti-inflammatory agents in a combination therapy. This merging allows for effective pain management at lower doses of each individual component, thereby reducing the side effects that would occur with higher doses of single agents.

Inventive Principle:
Principle #5Merging (Combining)

3Object-generated harmful factors

If alternative analgesic agents are developed, then side effects are reduced, but efficacy may be compromised

Engineering Contradiction:
Improveside effectsVSAvoidpain relief efficacy
Core Design Contradiction:
Object-generated harmful factorsVSReliability

Solution Approach 1:

The patent utilizes parameter changes by modifying the chemical structure of cannabinoid receptor ligands (Formula Ia with various R1-R9 substituents) to optimize both efficacy and safety profile. The structural variations allow for fine-tuning of receptor binding affinity and selectivity, achieving effective pain relief with reduced side effects.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS11771695B2Cannabinoid receptor modulators
Publication Date: 2023.10.03 ARENA PHARMACEUTICALS INC
  • US11771695B2 patent drawing
  • US11771695B2 patent drawing
  • US11771695B2 patent drawing

AI summary

Provided are certain methods useful in the treatment of pain comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;