Quinoline-3-carboxamide Radiotracers for S100A9 Inflammatory Imaging

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Solution Overview

Problem

Current methods for diagnosing inflammatory diseases associated with S100A9 accumulation lack molecular specificity and sensitivity, particularly for early-stage detection and monitoring, and there is a need for alternative compounds suitable for non-invasive imaging modalities like SPECT, PET, optical imaging, and ultrasound.

Innovation Solution

Development of non-peptidic quinoline-3-carboxamide compounds covalently linked to labels such as Cy5.5, 99mTc, and 18F for use in molecular imaging techniques, which specifically bind to S100A9, enabling high molecular sensitivity and specificity for diagnosing and monitoring inflammatory diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If conventional imaging techniques are used, then structural damage can be visualized, but molecular specificity and sensitivity for detecting inflammatory disease activity are insufficient

Engineering Contradiction:
Improvemolecular specificity and sensitivityVSAvoiddetection accuracy of inflammatory disease activity
Core Design Contradiction:
Measurement precisionVSReliability

Solution Approach 1:

The patent introduces S100A9 as a molecular intermediary marker that specifically binds to activated phagocytes at inflammatory sites. The quinoline-3-carboxamide compound acts as a radiolabeled intermediary probe that targets S100A9, enabling indirect but specific detection of inflammatory disease activity with high molecular precision that conventional imaging cannot achieve

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the detection parameter from macroscopic structural visualization to molecular-level S100A9 protein detection. By using radiolabeled quinoline-3-carboxamide compounds with specific binding affinity to S100A9, the system achieves superior measurement precision and sensitivity for inflammatory disease activity compared to conventional structural imaging techniques

Inventive Principle:
Principle #35Parameter changes

2Loss of time

If early-stage inflammatory diseases are detected using conventional methods, then diagnosis is delayed, but current methods lack the sensitivity for early detection

Engineering Contradiction:
Improvediagnosis timingVSAvoiddetection sensitivity for early-stage disease
Core Design Contradiction:
Loss of timeVSMeasurement precision

Solution Approach 1:

The radiolabeled quinoline-3-carboxamide compounds are administered to patients before clinical symptoms of inflammatory disease manifest, enabling preliminary detection of early-stage inflammation through S100A9 accumulation. This preliminary action allows diagnosis at the molecular level before structural changes occur, significantly reducing diagnostic delay

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent replaces conventional mechanical/structural imaging methods with molecular radiotracer-based detection. The radiolabeled compounds substitute for direct structural visualization by targeting molecular biomarkers (S100A9), enabling detection of inflammatory disease activity at the molecular level with much higher sensitivity for early-stage diagnosis

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

3Measurement precision

If non-invasive molecular imaging is performed, then accurate molecular-level detection is achieved, but the complexity of diagnostic procedures increases

Engineering Contradiction:
Improvemolecular-level detection accuracyVSAvoiddiagnostic procedure complexity
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The radiolabeled quinoline-3-carboxamide compounds serve multiple functions: they act as both the targeting molecule (binding to S100A9) and the imaging agent (radiolabel for detection). This multi-functionality simplifies the diagnostic procedure by combining target recognition and signal generation into a single agent, reducing overall system complexity while maintaining high molecular-level detection accuracy

Inventive Principle:
Principle #6Universality (Multi-functionality)

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 allow for accurate detection and monitoring of inflammatory diseases at the molecular level, providing early-stage diagnosis and prognosis, and effectively tracking disease progression and treatment response.

Implementation Method 1

the quinoline-3-carboxamide compound covalently linked to a label specifically binds to S100A9

Methodology Applied
Scientific EffectSpecific binding:

Data Source

PatentUS10350315B2Quinoline-3-carboxamide compounds and their use in diagnosis
Publication Date: 2019.07.16 WESTFAELISCHE WILHELMS-UNIVERSITAET MUENSTER
  • US10350315B2 patent drawing
  • US10350315B2 patent drawing
  • US10350315B2 patent drawing

AI summary

The present application provides quinoline-3-carboxamide compounds covalently linked to a label for use in the diagnosis of an inflammatory disease at local site. The above mentioned compounds can be used to detect or image accumulation of S100A9 in the body of a subject at sites of inflammation, using in vivo non-invasive molecular imaging techniques for the detection of said compounds. Accordingly, labeled quinoline-3-carboxamide compounds can be applied to evaluate the risk of a subject of developing an inflammatory disease and to follow the progress of the disease.