18F-Labeled Radiolabeled Compounds for CH24H Imaging
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Solution Overview
Problem
Current radiotracers for imaging cholesterol 24-hydroxylase (CH24H) enzyme activity lack effective, non-invasive methods for quantitative imaging, particularly for diagnostic and therapeutic applications in neurodegenerative diseases and other conditions associated with CH24H dysfunction.
Innovation Solution
Development of novel radiolabeled compounds represented by the formula (I), which include specific azetidinyl or pyrrolidinyl groups substituted with 18F, used as PET radiotracers for quantitative imaging of CH24H in mammals, allowing for effective imaging and quantification of CH24H occupancy in tissues and the brain.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Measurement precision
If conventional radiotracers are used for imaging CH24H enzyme activity, then imaging capability is provided, but quantitative imaging precision and measurement accuracy are insufficient
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of radiotracers to include specific azetidinyl or pyrrolidinyl groups with 18F labeling at defined positions. These structural parameter changes enable the radiotracers to bind with high affinity and specificity to CH24H enzyme, thereby achieving precise quantitative imaging of enzyme activity in vivo
Solution Approach 2:
The patent replaces conventional imaging methods with PET (positron emission tomography) imaging using 18F-labeled radiotracers. This substitution enables non-invasive quantitative measurement of CH24H enzyme activity in living subjects, providing superior measurement precision compared to traditional methods
2Loss of information
If existing radiotracers are administered for imaging, then diagnostic information is obtained, but the ability to quantify enzyme occupancy and treatment efficacy is limited
Solution Approach 1:
The patent creates radiotracers with dual functionality: they serve both as imaging agents for visualizing CH24H distribution and as quantitative measurement tools for determining enzyme occupancy and treatment efficacy. The 18F-labeled compounds provide comprehensive information including enzyme location, activity level, and response to therapeutic interventions
3Object-affected harmful factors
If non-invasive imaging methods are implemented, then patient comfort and safety are improved, but measurement accuracy and quantification capability are reduced
Solution Approach 1:
The patent replaces invasive biopsy or tissue sampling methods with non-invasive PET imaging using 18F-labeled radiotracers. The radiotracers are administered systemically and accumulate in tissues expressing CH24H enzyme, allowing quantitative measurement of enzyme activity in living subjects without surgical intervention, thereby maintaining both patient safety and measurement accuracy
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
Enables precise and quantitative imaging of CH24H in mammals, facilitating diagnostic and therapeutic applications for neurodegenerative diseases, such as Alzheimer's, Parkinson's, and other conditions by providing a means to quantify enzyme activity and assess treatment efficacy.
Implementation Method 1
Compounds can be labeled with either positron or gamma emitting radionuclides. For imaging, the most commonly used positron emitting (PET) radionuclides are...
Implementation Method 2
the most commonly used positron emitting (PET) radionuclides are 11C, 18F, 15O and 13N
Data Source
Figure 1~2
AI summary
The present invention provides radiolabeled compounds useful as radiotracers for quantitative imaging of CH24H in mammals. The compound of the present invention is represented by the formula (I): wherein each symbol is as defined in the specification.