Imaging agents comprising caspase-3 inhibitors

Details Imaging agents comprising caspase-3 inhibitors Imaging agents comprising caspase-3 inhibitors

A - Human Necessities

61

K

A61K 51/00 (2006.01) A61K 49/00 (2006.01) A61K 49/06 (2006.01) A61K 49/08 (2006.01) A61K 49/10 (2006.01) A61K 49/12 (2006.01) A61K 49/14 (2006.01) A61K 51/02 (2006.01) A61K 51/04 (2006.01) A61K 51/06 (2006.01) A61K 51/08 (2006.01)

Patent

CA 2547236

The present invention relates to diagnostic imaging agents for in vivo imaging. The imaging agents comprise a synthetic caspase-3 inhibitor labelled 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 for the preparation of the radiopharmaceuticals. Also described are chelator conjugates of the caspase-3 inhibitor, 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 and or therapy monitoring in vivo of various disease states where caspase-3 is involved.

L'invention concerne des agents d'imagerie diagnostique destinés à l'imagerie in vivo. Ces agents comprennent un inhibiteur de caspase-3 synthétique marqué avec un groupe caractéristique d'imagerie approprié pour l'imagerie diagnostique in vivo. L'invention concerne également des compositions pharmaceutiques et radiopharmaceutiques renfermant ces agents d'imagerie, ainsi que des trousses permettant la préparation des compostions radiopharmaceutiques. Elle concerne en outre des conjugués chélateurs de l'inhibiteur de caspase-3 appropriés pour la préparation d'agents d'imagerie comprenant un ion métallique radioactif ou paramagnétique. Les agents d'imagerie sont utiles pour l'imagerie diagnostique et/ou la surveillance thérapeutique in vivo de divers états pathologiques impliquant caspase-3.

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