Radiolabeled mGluR2 Ligands for PET Imaging Precision

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Solution Overview

Problem

There is a need for improved positron emission tomography (PET) radiotracers for imaging the metabotropic glutamate receptor mGluR2, as existing methods lack effectiveness in providing precise and quantitative imaging.

Innovation Solution

Development of specific radiolabeled compounds, such as those described by Formula (I), which are used for imaging mGluR2 receptors in tissues or mammals, utilizing positron-emission tomography, and their corresponding pharmaceutical compositions and methods for preparation and administration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If existing radiotracers are used for imaging mGluR2, then imaging can be performed, but the precision and quantification capability are insufficient

Engineering Contradiction:
Improveimaging precisionVSAvoidquantification reliability
Core Design Contradiction:
Measurement precisionVSReliability

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of radiotracer molecules to optimize their binding affinity and selectivity for mGluR2 receptors. Specific structural parameters such as substituent groups, molecular weight, and functional groups are adjusted to improve imaging precision and quantification reliability simultaneously

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent develops multiple radiotracer compounds based on a core molecular scaffold, creating variations that replicate and improve upon the binding properties of existing tracers. This allows selection of optimal compounds for precise imaging and quantification

Inventive Principle:
Principle #26Copying

2Loss of information

If existing imaging methods are used, then mGluR2 can be visualized, but quantitative assessment is limited

Engineering Contradiction:
Improvequantification informationVSAvoidreceptor quantification precision
Core Design Contradiction:
Loss of informationVSMeasurement precision

Solution Approach 1:

The patent implements feedback mechanisms through standardized imaging protocols and quantitative analysis methods that allow iterative optimization of tracer selection and imaging parameters to maximize both information retention and measurement precision

Inventive Principle:
Principle #23Feedback

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 and quantitative imaging and quantification of mGluR2 receptors, allowing for the assessment of neurological disorders and potential therapeutic mechanisms, including mood disorders and cognitive dysfunctions.

Implementation Method 1

selective, radiolabelled mGluR2 ligands which are useful for imaging and quantifying the metabotropic glutamate receptor mGluR2 in tissues, using positron-emission tomography (PET)

Methodology Applied
Scientific EffectPositron emission: Radioactive Decay

Data Source

PatentEP3226915B1Radiolabelled mglur2 pet ligands
Publication Date: 2019.02.20 JANSSEN PHARMA NV
  • EP3226915B1 patent drawingFigure 1~2
  • EP3226915B1 patent drawingFigure 3~4
  • EP3226915B1 patent drawingFigure 5~6

AI summary

The present invention relates to novel, selective, radiolabelled mGluR2 ligands which are useful for imaging and quantifying the metabotropic glutamate receptor mGluR2 in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a mammal, in vitro or in vivo and to precursors of said compounds.