Improved imaging agents comprising barbituric acid derivatives

A - Human Necessities – 61 – K

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Details

A61K 31/515 (2006.01) A61K 49/00 (2006.01) A61K 49/04 (2006.01) A61K 51/04 (2006.01)

Patent

CA 2501136

The present invention relates to diagnostic imaging agents for in vivo imaging. The imaging agents comprise a synthetic barbituric acid derivative labelled at the 5-position with an imaging moiety suitable for diagnostic imaging in vivo. The invention also provides pharmaceutical and radiopharmaceutical compositions comprising the imaging agents, together with kits of the preparation of the radiopharmaceuticals. Also described are chelator conjugates of the barbituric acid derivative, which are suitable for the preparation of imaging agents comprising a radioactive or paramagnetic metal ion. The imaging agents are useful for the diagnostic imaging in vivo of various disease states, including atherosclerosis.

La présente invention se rapporte à des agents d'imagerie diagnostique destinés à l'imagerie in vivo. Lesdits agents d'imagerie contiennent un dérivé de l'acide barbiturique synthétique marqué en position 5 avec un groupe caractéristique d'imagerie adapté à l'imagerie diagnostique in vivo. L'invention concerne aussi des compositions pharmaceutiques et radiopharmaceutiques renfermant lesdits agents d'imagerie, ainsi que des trousses permettant la préparation des compositions radiopharmaceutiques. L'invention a également trait à des conjugués chélateurs du dérivé de l'acide barbiturique, qui sont adaptés à la préparation d'agents d'imagerie contenant un ion métallique radioactif ou paramagnétique. Les agents d'imagerie selon l'invention sont utiles pour l'imagerie diagnostique in vivo de divers états pathologiques, notamment l'athérosclérose.

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