Tau Imaging Compounds With BBB Penetration and Specific Binding
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Solution Overview
Problem
Current imaging agents fail to specifically bind to tau proteins that accumulate in the brain, particularly in Alzheimer's disease and non-Alzheimer's tauopathies, limiting the ability to visualize tau pathologies in vivo.
Innovation Solution
Development of novel compounds with a basic structure of specific length ranging from 13 to 19 Å that exhibit affinity to tau aggregates, allowing specific binding and imaging of tau proteins in the brain.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing imaging agents are used, then imaging capability is provided, but specific binding to tau proteins is not achieved
Solution Approach 1:
The patent applies parameter changes by modifying the molecular structure of imaging agents, specifically adjusting the basic structure length to 13-19 Å and optimizing functional group configurations, to achieve specific binding to tau proteins while maintaining imaging capability
Solution Approach 2:
The patent implements local quality by designing compounds with specific functional groups positioned at particular locations within the molecular structure, enabling selective interaction with tau protein aggregates while the rest of the molecule provides imaging functionality
2Reliability
If compounds with specific basic structure length (13-19 Å) are developed, then specific binding to tau aggregates is achieved, but compound design complexity increases
Solution Approach 1:
The patent establishes a specific parameter range (13-19 Å) for the basic structure length, providing a clear design guideline that simplifies the compound development process while ensuring specific binding affinity to tau aggregates
3Speed
If rapid passage through blood-brain barrier is achieved, then imaging speed is improved, but compound stability may be reduced
Solution Approach 1:
The patent optimizes molecular parameters including size, lipophilicity, and functional group composition to enable rapid blood-brain barrier penetration while maintaining sufficient stability for in vivo imaging applications
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 compounds can effectively bind to tau aggregates, enabling accurate imaging of tau proteins in the brain, with rapid passage through the blood-brain barrier and minimal impact on the human body, and offer dual imaging capabilities through fluorescence and radioactivity.
Implementation Method 1
compounds having a basic structure of specific length ranging from 13 to 19 Å exhibit affinity to tau aggregates in living organisms
Implementation Method 2
After being administered in mammals, the compounds of the present invention can quickly pass the blood brain barrier
Implementation Method 3
the compounds of the present invention have fluorescence properties, so that the compounds of the present invention, when labeled with a radioactive isotope, are capable of double imaging
Implementation Method 4
one or more atoms are a radioisotope of the atom(s)
Data Source
AI summary
The present invention provides a compound represented by the following formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof:wherein:R1 and R2 are each separately selected from the group consisting of hydrogen, alkyl, alkenyl, acyl, and hydroxyalkyl;R3 is hydrogen or halogen;ring A is a benzene ring or a pyridine ring;ring B is selected from the group consisting of the following formulas (i), (ii), (iii), and (iv):in the formula (ii), Ra is alkyl;R4 and R5 are each separately selected from the group consisting of hydrogen, hydroxy, alkoxy, haloalkoxy, halohydroxyalkoxy, and aminoalkyl; andrepresents a double bond or a triple bond. The above compound can be used as a molecular probe for imaging tau proteins that accumulate in the brain.