Chromanol Compounds for Alzheimer's Plaque Reduction

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Solution Overview

Problem

Current treatments for Alzheimer's disease lack effective compounds that improve memory function and reduce beta-plaque load with minimal or no side effects, and existing antioxidants do not clearly demonstrate memory improvement.

Innovation Solution

Development of chromanol and hydroquinone compounds, specifically the S-enantiomer of SUL-138, which are used to treat Alzheimer's disease, improve memory function, and reduce plaque formation by targeting amyloid-β polymerization.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If existing antioxidants are administered to treat Alzheimer's disease, then oxidative burden in mitochondria is reduced, but clear effect on treating Alzheimer's is not found

Engineering Contradiction:
Improveoxidative burdenVSAvoidtreatment efficacy
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent modifies the chemical structure of conventional antioxidants by introducing specific substituents (R1, R2, R3 groups) to create chromanol and hydroquinone derivatives with enhanced properties. These structural parameter changes improve both antioxidant activity and Alzheimer's treatment efficacy, resolving the contradiction between reducing oxidative burden and achieving reliable treatment effects.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates composite molecular structures combining chromanol/hydroquinone cores with various substituent groups (amino acids, fatty acids, aromatic compounds). This composite approach allows the molecules to simultaneously exhibit antioxidant properties and specific binding affinity to amyloid-β, achieving both oxidative burden reduction and reliable Alzheimer's treatment.

Inventive Principle:
Principle #40Composite materials

2Reliability

If new compounds are developed to improve memory function and reduce plaque load, then treatment efficacy is improved, but side effects may increase

Engineering Contradiction:
Improvetreatment efficacyVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent converts the harmful aggregation of amyloid-β peptides into a beneficial therapeutic target. The chromanol and hydroquinone compounds specifically bind to amyloid-β oligomers and fibrils, converting the harmful plaque formation process into a treatable condition. The compounds' affinity for beta-sheet structures allows them to disrupt plaque formation while maintaining selectivity that minimizes side effects.

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

3Ease of operation

If conventional treatments are used for Alzheimer's disease, then some symptoms are managed, but effective compounds that improve memory function and reduce beta-plaque load with minimal side effects are lacking

Engineering Contradiction:
Improvesymptom managementVSAvoidmemory improvement and plaque reduction
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The chromanol and hydroquinone compounds exhibit multiple therapeutic functions simultaneously: they act as antioxidants, amyloid-β binding agents, and anti-inflammatory agents. This multi-functionality allows a single compound to address multiple aspects of Alzheimer's pathology (oxidative stress, plaque formation, neuroinflammation), providing both symptom management and disease-modifying effects with minimal side effects.

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

Data Source

PatentUS20230052152A1Compounds for treatment of alzheimer's disease
Publication Date: 2023.02.16 SULFATEQ BV
  • US20230052152A1 patent drawing
  • US20230052152A1 patent drawing
  • US20230052152A1 patent drawing

AI summary

The invention relates to certain chromanol, quinone or hydroquinone compounds and derivatives thereof for treatment of Alzheimer's disease and/or for improving memory function and/or reducing plaque load. Specifically, the present invention relates to chromanol compounds chosen from (6-hydroxy-2,5,7,8-tetramethylchroman-2yl)(piperazin-1-5 yl)methanone, ((S)-6-hy-droxy-2,5,7,8-tetramethyl-N-((R)-piperidin-3-yl)chroman-2-carboxamide hydrochloride and S-(6-hydroxy-2,5,7,8-tetramethylchro-man-2-yl)(4-(2-hydroxyethyl)piperazin-1-yl)methanone, and pharmaceutically acceptable salts thereof.