Styrylpyridine Compounds for Amyloid Plaque Imaging

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Solution Overview

Problem

Current methods for imaging and inhibiting amyloid deposits in the brain, particularly for Alzheimer's disease, face challenges such as the difficulty in noninvasively detecting and quantitating amyloid deposits due to their similar physical properties to normal tissues, and existing imaging techniques like MRI and CT providing disappointing results, with a need for compounds that can cross the blood-brain barrier and effectively inhibit amyloid aggregation.

Innovation Solution

Development of novel styrylpyridine compounds that are radiolabeled for diagnostic imaging and have the ability to inhibit amyloid plaque aggregation, allowing for the visualization of amyloid deposits in the brain and potentially treating Alzheimer's disease by administering these compounds to inhibit amyloid protein aggregation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Difficulty of detecting and measuring

If MRI or CT imaging techniques are used to detect amyloid deposits, then noninvasive imaging is attempted, but the detection precision is poor because amyloid deposits have similar physical properties to normal tissues

Engineering Contradiction:
Improvedetection of amyloid depositsVSAvoidimaging precision
Core Design Contradiction:
Difficulty of detecting and measuringVSMeasurement precision

Solution Approach 1:

The patent changes the detection parameter from physical properties (used in MRI/CT) to biochemical properties by using radiolabeled styrylpyridine compounds that specifically bind to amyloid deposits. This allows detection through radioactive signal emission rather than physical density differences, resolving the contradiction between noninvasive detection and detection precision

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces radiolabeled styrylpyridine compounds as intermediary substances that bind specifically to amyloid deposits. These compounds act as mediators between the imaging system and the amyloid deposits, enabling precise detection through radioactive signal emission while maintaining noninvasive imaging capability

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of operation

If existing imaging compounds are used, then imaging capability is provided, but the compounds cannot effectively cross the blood-brain barrier to reach amyloid deposits in the brain

Engineering Contradiction:
Improveadministration of imaging compoundVSAvoiddelivery to target site
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent modifies the chemical structure parameters of the imaging compounds by using styrylpyridine derivatives with specific lipophilicity and molecular weight characteristics. These parameter changes enable the compounds to cross the blood-brain barrier while maintaining their ability to bind specifically to amyloid deposits, thus resolving the contradiction between ease of administration and reliable target delivery

Inventive Principle:
Principle #35Parameter changes

3Difficulty of detecting and measuring

If conventional imaging methods are used, then noninvasive detection is attempted, but the ability to quantitate amyloid deposits is insufficient

Engineering Contradiction:
Improvenoninvasive detectionVSAvoidquantitation capability
Core Design Contradiction:
Difficulty of detecting and measuringVSMeasurement precision

Solution Approach 1:

The patent employs radiolabeled compounds that emit detectable radioactive signals providing feedback on the amount and distribution of amyloid deposits. The signal intensity is proportional to the concentration of bound compound, enabling quantitative measurement of amyloid burden through imaging techniques while maintaining noninvasive detection

Inventive Principle:
Principle #23Feedback

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 styrylpyridine compounds enable effective imaging of amyloid deposits in the brain, providing a noninvasive diagnostic tool and potential therapeutic option for Alzheimer's disease by specifically binding to amyloid plaques and inhibiting their formation, thereby aiding in the monitoring and treatment of the disease.

Implementation Method 1

radiolabeled styrylpyridine compounds enable effective imaging of amyloid deposits in the brain

Methodology Applied
Scientific EffectRadiolabeling: Radioactive Tracing

Implementation Method 2

styrylpyridine compounds...have the ability to inhibit amyloid plaque aggregation...specifically binding to amyloid plaques and inhibiting their formation

Methodology Applied
Scientific EffectAggregation inhibition: Adsorption

Data Source

PatentEP2363392B1Styrylpyridine derivatives and their use for binding and imaging amyloid plaques
Publication Date: 2017.05.03 THE TRUSTEES OF THE UNIV OF PENNSYLVANIA
  • EP2363392B1 patent drawingFigure 1
  • EP2363392B1 patent drawingFigure 2
  • EP2363392B1 patent drawingFigure 3

AI summary

This invention relates to a method of imaging amyloid deposits and to styrylpyridine compounds, and methods of making radiolabeled styrylpyridine compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.