Peptide Amide κ-Opioid Agonist for Analgesia

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Solution Overview

Problem

Current opioid drugs, particularly µ opioid receptor agonists, suffer from significant side effects such as tolerance, dependence, and respiratory depression, while non-opioid analgesics like acetaminophen and NSAIDs have limited efficacy and adverse effects, highlighting the need for novel analgesics with high activity and low toxicity.

Innovation Solution

Development of a κ opioid receptor agonist with a novel structure, represented by a specific peptide amide compound, which acts as a κ opioid receptor agonist to provide enhanced analgesic effects with reduced side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If µ opioid receptor drugs are used for pain treatment, then analgesic effect is improved, but side effects such as tolerance, dependence and respiratory depression increase

Engineering Contradiction:

Improveanalgesic effectVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent changes the receptor target parameter from µ opioid receptor to κ opioid receptor, and modifies chemical structure parameters of the ligand molecule. This parameter change allows achieving analgesic effect while reducing harmful side effects associated with µ receptor activation

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates a novel peptide amide compound structure that copies the opioid receptor binding mechanism but with modified molecular architecture. The compound maintains the essential pharmacophore features while introducing structural variations that reduce side effects

Inventive Principle:

Principle #26Copying

2Object-generated harmful factors

If non-opioid analgesics such as acetaminophen and NSAIDs are used, then side effects are reduced, but analgesic efficacy is limited

Engineering Contradiction:

Improveside effectsVSAvoidanalgesic efficacy

Core Design Contradiction:

Object-generated harmful factorsVSReliability

Solution Approach 1:

The patent changes the mechanism of action parameter from non-opioid pathways to κ opioid receptor activation. This parameter change enables the compound to achieve superior analgesic efficacy compared to traditional non-opioid analgesics while maintaining a favorable side effect profile

Inventive Principle:

Principle #35Parameter changes

3Duration of action of stationary object

If traditional opioid drugs are used for long-term pain management, then pain relief is maintained, but treatment cost and recovery cycle increase due to tolerance and dependence

Engineering Contradiction:

Improvepain relief durationVSAvoidrecovery cycle

Core Design Contradiction:

Duration of action of stationary objectVSLoss of time

Solution Approach 1:

The patent changes the receptor selectivity parameter to κ opioid receptor, which inherently reduces the development of tolerance and dependence. This parameter change allows for prolonged pain relief without the progressive loss of efficacy and extended recovery cycles associated with µ opioid receptor drugs

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentEP3656782B1Peptide amide compound and preparation method and medical use thereof

Publication Date: 2021.12.22 SICHUAN HAISCO PHARMA CO LTD

AI summary

The invention provides a peptide amide compound represented by the general general formula (I), a preparation method thereof, and a medical application thereof. The compound has a novel structure, better biological activity, and better analgesic effect.