ROS PET Probe Compound With Low DNA Intercalation
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Solution Overview
Problem
Existing PET probes for diagnosing neurodegenerative diseases like Parkinson's and Alzheimer's focus on abnormal protein accumulation, which does not necessarily reflect disease symptoms, leading to late diagnosis and ineffective treatment.
Innovation Solution
Development of a compound represented by General Formula (1) or its salt, which can detect reactive oxygen species (ROS) with high sensitivity and minimal DNA intercalation, allowing for early and accurate diagnosis of neurodegenerative diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Measurement precision
If PET probes are used to measure accumulated abnormal proteins for diagnosing neurodegenerative diseases, then diagnosis can be performed, but the diagnosis is too late and does not necessarily reflect disease symptoms
Solution Approach 1:
The patent applies preliminary action by detecting ROS production before abnormal protein accumulation becomes clinically significant. The probe detects ROS at early stages of neurodegenerative disease, enabling diagnosis before symptoms manifest and before protein accumulation reaches problematic levels, thus resolving the timing issue.
Solution Approach 2:
The patent uses ROS as an intermediary marker to indirectly assess early disease stages. Instead of directly measuring abnormal proteins which accumulate late, the probe detects ROS production which occurs early and correlates with disease progression, providing an intermediate measurement that predicts future protein accumulation.
2Measurement precision
If existing PET probes are used to detect abnormal protein accumulation, then protein aggregation can be measured, but the measurement does not reflect disease symptoms and treatment effectiveness
Solution Approach 1:
The patent introduces ROS as an intermediary biological marker that correlates with both early disease stages and symptom progression. ROS production serves as a mediator between cellular stress mechanisms and clinical manifestations, providing measurement information that actually reflects disease severity and treatment response.
Solution Approach 2:
The patent changes the detection parameter from static protein accumulation to dynamic ROS production rates. This parameter change enables measurement of active disease processes rather than just accumulated damage, providing information that correlates with symptom progression and treatment effectiveness.
3Measurement precision
If a compound is designed to detect ROS with high sensitivity, then early disease detection is enabled, but the compound may intercalate into DNA causing mutagenicity
Solution Approach 1:
The patent modifies the molecular structure parameters of the probe compound to achieve high ROS detection sensitivity while minimizing DNA intercalation. By adjusting structural parameters such as the hydrophobicity and molecular geometry, the probe achieves effective ROS detection without the harmful side effect of DNA binding.
Solution Approach 2:
The patent applies local quality by designing the probe to have specific regional properties - the molecule is structured to interact selectively with ROS in the local cellular environment without having affinity for DNA. The local chemical properties are optimized for ROS detection while avoiding global harmful interactions with genetic material.
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 compound enables early detection of ROS, facilitating earlier and more accurate diagnosis and treatment of neurodegenerative diseases by quantifying ROS production in the brain.
Implementation Method 1
a small percentage of oxygen taken into a living body is changed to reactive oxygen species (ROS) such as superoxide anions, hydroxyl radicals, or hydrogen peroxide
Data Source
AI summary
The present invention relates to a compound represented by the following General Formula (1) or a salt thereof.In General Formula (1), R1, R2, R3 and R4 each independently represent a hydrogen atom, a linear or branched alkyl group which may have a substituent or the like. R1 and R2 may be bonded to each other to form a ring. R3 and R4 may be bonded to each other to form a ring. R1 and/or R2 may be bonded to a 6-membered ring to which —NR1R2 is bonded to form a ring. R3 and/or R4 may be bonded to a 6-membered ring to which —NR3R4 is bonded to form a ring. R5 represents —11CH3, a linear or branched alkyl group which may have a substituent or the like. R6 represents —F, —18F or the like. X, Y and Z each independently represent a carbon atom, an oxygen atom or the like. n is 0 or 1.