α-Synuclein Aggregate Binder Composition for Selective Brain Imaging

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Solution Overview

Problem

Existing imaging agents, such as [11C]BF-227, have insufficient binding affinity and low selectivity for α-synuclein aggregates, limiting their effectiveness in diagnosing diseases like Parkinson's disease and multiple system atrophy, and lack the ability to differentiate between α-synuclein and other protein aggregates.

Innovation Solution

Development of a novel compound with specific structure, represented by formulae (I) and (II), which exhibits high binding selectivity to α-synuclein aggregates, allowing for both optical and radiological imaging.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If [11C]BF-227 is used as a PET probe for imaging α-synuclein aggregates, then imaging capability is provided, but binding affinity and selectivity are insufficient leading to nonspecific accumulation

Engineering Contradiction:

Improveimaging capabilityVSAvoidbinding selectivity

Core Design Contradiction:

Measurement precisionVSReliability

Solution Approach 1:

The patent modifies molecular parameters of imaging agents by introducing specific chemical groups (benzothiazole, pyridine, fluorine atoms) and adjusting molecular weight and hydrophobicity to optimize binding affinity and selectivity for α-synuclein aggregates while reducing nonspecific accumulation in the brain

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates composite imaging agents combining multiple functional moieties (benzothiazole ring, pyridine ring, fluorine-containing groups) into a single molecular structure that simultaneously achieves high binding affinity, selectivity for α-synuclein, and reduced nonspecific brain accumulation

Inventive Principle:

Principle #40Composite materials

2Measurement precision

If existing imaging agents are used, then detection of α-synuclein aggregates is possible, but binding affinity is insufficient limiting diagnostic effectiveness

Engineering Contradiction:

Improvedetection capabilityVSAvoidbinding affinity

Core Design Contradiction:

Measurement precisionVSQuantity of substance

Solution Approach 1:

The patent systematically optimizes molecular parameters including adding aromatic rings (benzothiazole, pyridine) to increase molecular weight to optimal range (300-500 Da), introducing fluorine atoms for PET imaging, and adjusting hydrophobicity to enhance binding affinity by several-fold compared to existing agents

Inventive Principle:

Principle #35Parameter changes

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 novel compound enables accurate visualization of α-synuclein aggregates in vivo, facilitating early disease diagnosis and assessment of therapeutic agents targeting these aggregates.

Implementation Method 1

composition for optical imaging of α-synuclein aggregates

Methodology Applied

Scientific EffectFluorescence: Fluorescence

Implementation Method 2

composition for radiological imaging of α-synuclein aggregates

Methodology Applied

Scientific EffectRadioactive tracing: Radioactive Tracing

Data Source

PatentUS12630544B2Compound, α-synuclein aggregate binder, and use thereof

Publication Date: 2026.05.19 EISAI R&D MANAGEMENT CO LTD

AI summary

An embodiment of the present invention relates to a compound represented by formula (I) or (II), a pharmaceutically acceptable salt thereof, or a solvate thereof.