Multivalent Compounds for Traumatic Brain Injury Treatment

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Solution Overview

Problem

Current treatments for traumatic brain injury and neurodegenerative conditions are inadequate, with many drug candidates failing to prove efficacy in large clinical studies, highlighting a need for novel therapeutics to address brain damage effectively.

Innovation Solution

Development of novel multivalent compounds of a specific formula, comprising various functional groups and linkers, which can act as pharmaceutically acceptable salts, potentially used in pharmaceutical compositions to treat brain damage, including traumatic brain injury and neurodegenerative conditions, by promoting neurogenesis and providing protective effects against secondary brain injuries.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional drug candidates are used for treating traumatic brain injury, then treatment approaches are available, but efficacy in humans fails to be proven in large clinical studies

Engineering Contradiction:
ImproveefficacyVSAvoidtreatment effectiveness
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies segmentation by dividing the therapeutic approach into multiple functional components within a single molecule: (1) metal ion chelating groups for binding free metals, (2) antioxidant moieties for scavenging reactive oxygen species, and (3) neuroprotective functional groups. This multi-functional segmentation allows the compound to address multiple pathological mechanisms simultaneously, resolving the contradiction between reliability and adaptability by providing a comprehensive treatment approach that has proven effective in preclinical models.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs composite material principles by creating molecules that combine multiple chemical functional groups with distinct therapeutic activities into a single composite structure. The compounds integrate chelating agents, antioxidants, and neuroprotective moieties into unified molecular architectures, enabling simultaneous execution of multiple protective functions. This composite approach has demonstrated reliable neuroprotection in traumatic brain injury models while maintaining the versatility to address diverse pathological mechanisms.

Inventive Principle:
Principle #40Composite materials

2Adaptability or versatility

If novel multivalent compounds are developed to provide comprehensive neuroprotection, then multiple protective functions are achieved, but compound complexity increases

Engineering Contradiction:
Improvemulti-functionalityVSAvoidmolecular complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent directly applies the universality principle by designing compounds that perform multiple therapeutic functions simultaneously. Each molecule is engineered to (1) chelate free metals, (2) scavenge reactive oxygen species, and (3) provide neuroprotection through multiple mechanisms. This multi-functionality allows a single compound to address diverse pathological mechanisms in brain injury, achieving high adaptability while managing complexity through rational molecular design rather than requiring multiple separate agents.

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

Solution Approach 2:

The patent applies merging by combining multiple previously separate therapeutic agents into a single integrated molecule. Instead of administering separate chelating agents, antioxidants, and neuroprotective drugs, the patent merges their essential functional groups into one compound. This consolidation reduces the complexity of multi-drug regimens while maintaining comprehensive neuroprotective coverage, resolving the contradiction between multi-functionality and complexity.

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentEP3201173B1Multivalent compounds for use in the treatment and prevention of brain damage
Publication Date: 2020.10.14 MEDICORTEX FINLAND OY
  • EP3201173B1 patent drawing
  • EP3201173B1 patent drawing
  • EP3201173B1 patent drawing

AI summary

The present invention relates to pounds of general formula (I) and pharmaceutically acceptable salts thereof; wherein R1 - R11, L, Z, Y, and Z are as defined in the claims. The invention also relates to said compounds for use as a medicament and particularly in the treatment of traumatic brain injury.