Triazole Containing Metal Chelating Agents

Simple SummaryContent extracted from patent full text and abstract with AI.

This patent relates to a new class of metal chelating agents that contain a triazole group and can form stable tricarbonyl complexes with technetium and rhenium. These chelating agents are designed to be easily and efficiently attached (via 'click chemistry') to various biomolecules—such as peptides, proteins, nucleic acids, carbohydrates, or lipids—that accumulate in specific targeted or diseased tissues. The resulting biomolecule-radiometal complexes can be used in both radiodiagnosis (imaging) and radiotherapy (treatment) for a range of diseases, especially cancer.

Use CasesContent extracted from patent full text and abstract with AI.

• Development of new targeted radiotracers for nuclear medicine imaging (e.g., SPECT radiodiagnostics using technetium-99m).
• Preparation of radiolabeled therapeutic agents for oncology (e.g., rhenium-based agents for targeted radiotherapy of tumors).
• Creation of new kits for simple, one-step labeling of biomolecules with medical radionuclides.
• Site-specific radiolabeling of biomolecules (peptides, antibodies, nucleic acids, etc.) for research, diagnostic, or therapeutic applications.
• Labeling of biomolecules that specifically target biomarkers or receptors in diseased tissues, improving accuracy of imaging and therapy.

BenefitsContent extracted from patent full text and abstract with AI.

• Enables simple, robust, and high-yield attachment of radiometals to a wide range of biomolecules without need for complex protecting group strategies.
• Compatible with mild aqueous and organic conditions, preserving the functional integrity of sensitive biomolecules.
• Provides highly stable radiometal complexes, which is crucial for in vivo applications to prevent unwanted release of radionuclides.
• The method uses orthogonal 'click chemistry', enabling simultaneous synthesis and biomolecule attachment, saving time and materials.
• Allows rapid and parallel development of diagnostic and therapeutic agents, accelerating discovery and preclinical screening.
• Ensures excellent in vitro and in vivo stability, high target selectivity, and retention of biological activity of biomolecule conjugates.

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Patent Abstract

New chelating agents as well as their tricarbonyl complexes with technetium and rhenium and the use of these compounds in radiodiagnosis and radiotherapy are described. As a peculiarity of this invention, synthesis and coupling of the chelating systems to (bio)molecules is performed simultaneously. The new chelating agents are coupled to substances that accumulate in the diseased/targeted tissue.