Polyalkylene Glycol Analgesic Compounds for Pain Management

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Solution Overview

Problem

Current pain management options, such as opioid and non-opioid analgesics, often come with significant side effects and do not adequately address chronic or neuropathic pain without affecting the central nervous system.

Innovation Solution

Development of compounds represented by specific formulas, which can be used alone or in combination with other medications, to treat various types of pain without substantial adverse effects on the central nervous system, including acute and chronic pain, and neuropathic pain.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If opioid or non-opioid analgesics are used to treat pain, then pain relief is achieved, but significant side effects occur and central nervous system is affected

Engineering Contradiction:
Improvepain relief effectivenessVSAvoidside effects and central nervous system impact
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of analgesic compounds through polyalkylene glycol conjugation. This structural modification changes the pharmacokinetic and pharmacodynamic parameters of the drug, enabling effective pain relief while reducing adverse effects on the central nervous system. The polyalkylene glycol chain length and composition can be adjusted to optimize the balance between efficacy and safety.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention uses composite materials by combining the active analgesic compound with polyalkylene glycol polymers. This creates a hybrid molecular structure that integrates the pain-relieving properties of the parent compound with the beneficial properties of the polyalkylene glycol moiety, such as reduced central nervous system penetration and improved safety profile.

Inventive Principle:
Principle #40Composite materials

2Reliability

If existing analgesics are used to treat chronic or neuropathic pain, then some pain relief is achieved, but inadequate treatment occurs without substantial adverse effects on the central nervous system

Engineering Contradiction:
Improvechronic and neuropathic pain treatment effectivenessVSAvoidsuitability for different pain types
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent achieves universality by developing analgesic compounds with broad-spectrum activity against multiple pain types including acute, chronic, and neuropathic pain. The polyalkylene glycol conjugated structures demonstrate multi-functional efficacy, providing reliable pain relief across different pain conditions while maintaining a favorable safety profile without substantial adverse effects on the central nervous system.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Data Source

PatentUS8802734B2Method of treating or preventing pain
Publication Date: 2014.08.12 NOVAREMED LTD
  • US8802734B2 patent drawing
  • US8802734B2 patent drawing
  • US8802734B2 patent drawing

AI summary

Compounds for use in the treatment or prophylaxis of pain, including acute and chronic pain (e.g., nociceptive pain, neuropathic pain, headaches, migraine), represented by general formula I:in which:the dotted line represents a single or a double bond; and R5 and R5′ are independently —H, —OH or —OR6, where R6 is a linear or branched C1-C4 alkyl; X is —CH2O—; Z is —CH2CH2O—, —CH(CH3)CH2O— or —CH2CH(CH3)O—; m is 1; and n is an integer of 1-5. The compounds of the invention are also effective for reducing inflammation and may be used alone or in combination with other analgesics.