Radiolabeled-pegylation of ligands for use as imaging agents

A - Human Necessities – 61 – K

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A61K 51/00 (2006.01) A61K 9/14 (2006.01) A61K 36/14 (2006.01)

Patent

CA 2617319

The present invention is directed to a method of using radiolabeled ethylene glycol (n = 1) (EG) or polyethylene glycol (n = from 2 to 10) (PEG) as a labeling group moiety on compounds that can be useful for imaging tissues. Specifically, the EG or PEG moiety preferably contains a radiofluorine (18F), and is covalently bonded to a ligand (L). The L portion of the molecule can be any molecule appropriate for covalently bonding with the radiolabeled EG or PEG moiety and subsequent use as an imaging agent. In particular, the imaging agent is preferably an agent suitable for administering to a mammal and detecting by PET or SPECT imaging.

L'invention porte sur un procédé d'utilisation d'éthylène glycol (n = 1) (EG) ou de polyéthylène glycol (n = de 2 à 10) (PEG) radiomarqué comme fragment d'un groupe d'étiquetage sur des composés qui peuvent être utilisés dans l'imagerie des tissus. En particulier, le fragment EG ou PEG contient de préférence un radiofluor (18F) et est lié par covalence à un ligand (L). La partie L de la molécule peut être n'importe quelle molécule appropriée à la liaison covalente avec le fragment EG ou PEG radiomarqué et pouvant être ensuite utilisée comme agent d'imagerie. Plus particulièrement, l'agent d'imagerie est de préférence un agent apte à être administré à un mammifère et à être détecté par imagerie PET ou SPECT.

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