Benzodiazepine Derivative Multi-Target Ligand Neurodegeneration

Solution Overview

Problem

Current treatments for neurodegenerative diseases such as Alzheimer's, Parkinson's, and neuropathic pain are inadequate, with existing medications providing temporary relief but not preventing disease progression, and are complicated by multiple-drug regimens that are challenging for elderly patients and caregivers due to pharmacokinetic and pharmacodynamic interactions.

Innovation Solution

Development of a multi-target-directed ligand, JM-20, a benzodiazepine derivative that acts on multiple pharmacological targets, potentially offering improved efficacy and safety by simplifying therapeutic regimens and reducing drug interactions, which can be administered in various forms including tablets, solutions, and transdermal patches.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If multiple drugs are administered to treat neurodegenerative diseases, then therapeutic coverage is improved, but treatment complexity and drug interactions increase

Engineering Contradiction:
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent combines multiple therapeutic functions into a single multi-target-directed ligand (MTDL) that can simultaneously act on multiple pharmacological targets (e.g., acetylcholinesterase, butyrylcholinesterase, NMDA receptors, mitochondrial complex I). This merging approach maintains comprehensive therapeutic coverage while eliminating the complexity of administering multiple separate drugs and avoiding drug-drug interactions.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention creates a universal compound with multi-functional activity that can treat multiple aspects of neurodegenerative diseases simultaneously. The MTDL is designed to interact with multiple targets involved in disease pathogenesis, providing broad therapeutic coverage through a single agent rather than requiring multiple specialized drugs.

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

2Reliability

If multiple drugs are administered to treat neurodegenerative diseases, then therapeutic coverage is improved, but pharmacokinetic and pharmacodynamic interactions increase

Engineering Contradiction:
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

By merging multiple therapeutic functions into a single compound, the patent eliminates pharmacokinetic interactions (absorption, distribution, metabolism, excretion between drugs) and pharmacodynamic interactions (additive or synergistic effects between drugs) that would occur with multiple medication regimens.

Inventive Principle:
Principle #5Merging (Combining)

3Ease of operation

If simplified treatment regimens are used, then compliance is improved, but therapeutic coverage may be reduced

Engineering Contradiction:
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The multi-target-directed ligand provides simplified treatment (single drug regimen) while maintaining comprehensive therapeutic coverage by acting on multiple disease-relevant targets simultaneously, thus resolving the trade-off between compliance and effectiveness.

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

Data Source

PatentEP3470414B1Benzodiazepine derivative with activity on the central nervous and vascular systems
Publication Date: 2021.10.13
  • EP3470414B1 patent drawingFigure 1~2
  • EP3470414B1 patent drawingFigure 3~5
  • EP3470414B1 patent drawingFigure 6

AI summary

Formula III compound, its products and pharmaceutical compositions containing them for the treatment of central nervous and vascular system diseases, particularly neurodegenerative disorders with cognitive deterioration, diseases associated with oxidative stress, diseases taking in mitochondrial dysfunction, Parkinson's disease and neuropathic pain, as well as the pathological processes associated with aging.