Trans-2-decenoic acid derivative for chemotherapy-induced neuropathy

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Current cancer chemotherapy agents often cause peripheral nerve disorders due to their cytotoxic effects, leading to severe side effects such as numbness, pain, and hypersensitivity, with limited effective prophylactic or therapeutic options available, and existing neurotrophic factors like BDNF struggle to cross the blood-brain barrier.

Innovation Solution

A trans-2-decenoic acid derivative or its pharmaceutically acceptable salt, which acts as a neurotrophic factor-like compound, providing analgesic and therapeutic benefits for peripheral nerve disorders by activating the MAP kinase pathway, thereby addressing the limitations of existing treatments.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If anti-cancer agents are administered to treat cancer, then anti-cancer effects are achieved, but peripheral nerve disorders occur as side effects

Engineering Contradiction:

Improveanti-cancer effectVSAvoidperipheral nerve disorder

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces an intermediary substance (amino acid derivative compound) that mediates between the anti-cancer agent and the nervous system. This compound prevents or attenuates the direct harmful interaction between anti-cancer agents and nerve cells, thereby protecting against peripheral nerve disorders while maintaining the anti-cancer effects of the original agents

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent converts the harmful cytotoxic effect of anti-cancer agents on nerve cells into a beneficial protective mechanism. By administering the amino acid derivative compound, the body's natural response to the harmful agent is redirected to produce protective effects, transforming the harmful interaction into a therapeutic outcome that prevents nerve damage

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

2Reliability

If neurotrophic factors like BDNF are used to treat nerve disorders, then neuroprotective effects are achieved, but the compounds cannot cross the blood-brain barrier

Engineering Contradiction:

Improveneuroprotective effectVSAvoidblood-brain barrier penetration

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of neurotrophic factor analogs or related compounds. By changing molecular parameters such as size, charge, and hydrophobicity, the compounds gain the ability to cross the blood-brain barrier while retaining their neuroprotective pharmacological activities

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent substitutes the mechanical approach of directly administering large protein neurotrophic factors (which cannot cross the blood-brain barrier) with small molecule compounds that can penetrate biological barriers. This replacement maintains the desired neuroprotective effect while overcoming the delivery limitation

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

3Ease of operation

If conventional therapies are used for peripheral nerve disorders, then some symptom relief is achieved, but the effectiveness is limited

Engineering Contradiction:

Improvesymptom reliefVSAvoidtherapeutic effectiveness

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent employs a composite therapeutic approach by combining the amino acid derivative compound with existing therapeutic strategies. This composite formulation integrates multiple mechanisms of action, including neuroprotection, anti-inflammatory effects, and symptom management, thereby achieving superior therapeutic effectiveness compared to conventional monotherapies

Inventive Principle:

Principle #40Composite materials

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The compound effectively prevents or treats peripheral nerve disorders induced by cancer chemotherapy agents, offering analgesic action and neuroprotective effects for conditions like dementia, Parkinson's disease, and depression, while also being useful for spinal cord injuries and pain management.

Implementation Method 1

acts as a neurotrophic factor-like compound, providing analgesic and therapeutic benefits for peripheral nerve disorders by activating the MAP kinase pathway

Methodology Applied

Scientific EffectMAP kinase pathway activation:

Data Source

PatentEP2842942B1Trans-2-decenoic acid derivative and drug containing same

Publication Date: 2016.12.07 NIPPON ZOKI PHARMACEUTICAL CO LTD

AI summary

The present invention relates to a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical agent containing the compound as an active ingredient. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt, which is the compound of the present invention, is specifically represented by the general formula (I): wherein X is a substituent such as a 1-pyrrolidyl, a 3-thiazolizyl, or a piperidino, and the compound is highly useful as a pharmaceutical agent, such as a prophylactic or therapeutic agent for a peripheral nerve disorder induced by administration of an anticancer agent, a prophylactic or therapeutic agent for neurodegenerative diseases or mental diseases such as dementia, Alzheimer's diasease, Parkinson's disease, diabetic neuropathy, depression, glaucoma, or autistic disorder spectrum, a therapeutic or repairing agent for spinal cord injury, analgesics against various pain diseases, or the like.