Alpha-Synuclein PET Tracers for Selective Aggregate Imaging
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Solution Overview
Problem
Current diagnostic methods for alpha-synuclein-related diseases, such as Parkinson's disease, lack effective imaging agents that can selectively bind to pathological alpha-synuclein aggregates, leading to inaccurate diagnoses and limited treatment options.
Innovation Solution
Development of novel compounds, including those of formula (I) and its subformulae, which exhibit high affinity and selectivity for alpha-synuclein aggregates, allowing for positron emission tomography (PET) imaging to detect and quantify Lewy bodies and neurites.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Measurement precision
If current diagnostic methods are used for alpha-synuclein-related diseases, then diagnosis can be performed, but diagnostic accuracy is low and imaging agents cannot selectively bind to pathological alpha-synuclein aggregates
Solution Approach 1:
The patent modifies molecular parameters of imaging agents by introducing specific chemical groups (aryl, heteroaryl, cycloalkyl, heterocyclyl) and adjusting substituent patterns to optimize binding affinity and selectivity for alpha-synuclein aggregates, thereby improving both diagnostic accuracy and binding reliability
Solution Approach 2:
The patent creates composite molecular structures combining multiple structural motifs (aryl-heteroaryl-cycloalkyl-heterocyclyl combinations) with specific substituent patterns to achieve enhanced selectivity and affinity for pathological alpha-synuclein aggregates, resolving the contradiction between measurement precision and binding reliability
2Measurement precision
If novel compounds with high affinity for alpha-synuclein aggregates are developed, then imaging precision is improved, but compound complexity increases
Solution Approach 1:
The patent divides the imaging compound into distinct modular segments (aryl group, heteroaryl group, cycloalkyl group, heterocyclyl group, and substituent groups) that can be independently optimized and combined, allowing high imaging precision to be achieved through systematic assembly of functional modules rather than through undifferentiated complexity
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
These compounds enable precise in vivo imaging of alpha-synuclein aggregates, facilitating early detection, monitoring disease progression, and predicting treatment responsiveness, thereby improving diagnostic accuracy and therapeutic development.
Implementation Method 1
novel compounds, including those of formula (I) and its subformulae, which exhibit high affinity and selectivity for alpha-synuclein aggregates
Implementation Method 2
detectably labelled compound... that can be employed in the imaging of alpha-synuclein aggregates... positron emission tomography (PET) imaging
Data Source
AI summary
The present invention relates to novel compounds of formula (I), or a detectably labelled compound, stereoisomer, racemic mixture, pharmaceutically acceptable salt, hydrate, or solvate thereof, that can be employed in the imaging of alpha-synuclein aggregates and determining an amount thereof. Furthermore, the compounds can be used for diagnosing a disease, disorder or abnormality associated with an alpha-synuclein aggregates, including, but not limited to, Lewy bodies and/or Lewy neurites (such as Parkinson's disease), determining a predisposition to such a disease, disorder or abnormality, prognosing such a disease, disorder or abnormality, monitoring the evolution of the disease in a patient suffering from such a disease, disorder or abnormality, monitoring the progression of such a disease, disorder or abnormality and predicting responsiveness of a patient suffering from such a disease, disorder or abnormality to a treatment thereof.