Multifunctional Compounds for Neuroprotection via MAO and AChE Inhibition

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Solution Overview

Problem

Current treatments for neurodegenerative diseases like Parkinson's and Alzheimer's are limited, often providing only temporary relief and are associated with significant side effects due to the 'one-drug, one-target' approach, which is insufficient for the complex nature of these diseases.

Innovation Solution

Development of compounds with multiple mechanisms of action that integrate monoamine oxidase inhibition, cholinesterase inhibition, and free radical scavenging capabilities, designed to provide neural protection and treat related diseases more effectively.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If multiple drugs are used in combination therapy to target different pathways, then the treatment effectiveness is improved, but the device complexity and side effects increase

Engineering Contradiction:
Improvetreatment effectivenessVSAvoiddrug combination complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent combines multiple pharmacophores (MAO inhibitor, AChE inhibitor, and free radical scavenger moieties) into a single multifunctional compound molecule. This merging approach integrates the therapeutic actions of multiple drugs into one molecule, achieving synergistic effects while simplifying the treatment regimen and reducing the complexity associated with combination therapy.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention creates a universal compound that performs multiple functions simultaneously: inhibiting monoamine oxidase, inhibiting acetylcholinesterase, and scavenging free radicals. This multi-functional molecule addresses multiple pathological mechanisms of neurodegenerative diseases through a single agent, improving treatment effectiveness without requiring multiple separate medications.

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

2Object-generated harmful factors

If a single drug targets one specific pathway, then the side effects are reduced, but the treatment effectiveness for complex diseases is insufficient

Engineering Contradiction:
Improveside effectsVSAvoidtreatment effectiveness
Core Design Contradiction:
Object-generated harmful factorsVSReliability

Solution Approach 1:

The patent designs a single multifunctional compound that simultaneously targets multiple pathways involved in neurodegenerative diseases: MAO inhibition for neurotransmitter regulation, AChE inhibition for cholinergic enhancement, and free radical scavenging for oxidative stress protection. This multi-functional approach maintains the simplicity of single-drug administration (reducing side effects) while achieving comprehensive disease coverage (improving effectiveness).

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

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

These compounds offer enhanced medical effects with reduced side effects by targeting multiple pathways, potentially leading to more effective prevention and treatment of neurodegenerative diseases and oxidative stress-related conditions.

Implementation Method 1

Monoamine oxidases (MAO) are enzymes to catalyze amines in oxidative deamination reaction of monoamines

Methodology Applied
Scientific EffectOxidative deamination: Oxidation

Implementation Method 2

acetyl cholinesterase inhibitors (AChEI), mainly through reversible inhibition of acetylcholinesterase, may reduce the speed of acetylcholine degradation

Methodology Applied
Scientific EffectEnzymatic hydrolysis: Hydrolysis

Implementation Method 3

antioxidants, such as vitamin E and some other free radical scavengers, can prevent the damage of Aβ to neurons

Methodology Applied
Scientific EffectFree radical scavenging: Oxidation

Data Source

PatentEP3143002B1Compounds with neural protective effect, and preparation and use thereof
Publication Date: 2020.12.02 GUANGZHOU MAGPIE PHARMA
  • EP3143002B1 patent drawingFigure 1~2
  • EP3143002B1 patent drawingFigure 3~4
  • EP3143002B1 patent drawingFigure 5~6

AI summary

The invention generally relates to compounds of formula (I) with neural protective effect, and preparation and uses thereof. The compounds have multiple mechanisms or functions, for example, inhibition of monoamine oxidase and cholinesterase, scavenging of free radicals, and protection of cells such as nerve cells. The compounds can be used for manufacture of medicaments of cell protection, for prevention and/or treatment of monoamine oxidase, cholinesterase and free radicals related diseases, for example, neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease and stroke, and free-radical related diseases such as heart disease, myocardial ischemia, diabetes and other cardiovascular and cerebrovascular diseases.