Small technetium-99m and rhenium labeled agents and methods...

C - Chemistry – Metallurgy – 07 – C

Patent

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Details

C07C 323/41 (2006.01) A61K 51/04 (2006.01) C07D 295/12 (2006.01) C07D 295/13 (2006.01) C07K 5/06 (2006.01)

Patent

CA 2407592

The present invention relates to compounds of formula (1) (where the variables R A, R B, R c and n are as defined in the claims) and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tumors, e.g., carcinomas, melanomas and other tumors. In another embodiment, the invention relates to methods of imaging tumors using radiolabelled metal complexes. Preferred radiolabelled complexes for imaging tumors include technetium and rhenium complexes. The high tumor uptake and significant tumour/nontumour ratios of the technetium complexes of the invention indicated that such small technetium-99m-based molecular probes can be developed as in-vivo diagnostic agents for melanoma and its metastases. In yet another embodiment, the invention relates to methods for treatment of tumours using a radiolabelled metal complex as a radiopharmaceutical agent to treat the tumor.

L'invention concerne des composés et des complexes de technétium et de rhénium de ceux-ci, convenant à l'imagerie ou au traitement thérapeutique de tumeurs, dont, par exemple, des carcinomes, des mélanomes et d'autres tumeurs. Dans un autre mode de réalisation, l'invention se rapporte à des procédés d'imagerie de tumeurs au moyen de complexes métalliques radiomarqués. Les complexes radiomarqués préférés pour l'imagerie de tumeurs comprennent des complexes de technétium et de rhénium. L'absorption élevée des tumeurs et les rapports tumeurs/non tumeurs élevés des complexes de technétium de l'invention indiquent que des sondes moléculaires à base de technétium 99m, de petite taille moléculaire, peuvent être mises au point en tant qu'agents diagnostiques in-vivo pour le mélanome et ses métastases. Dans encore un autre mode de réalisation, l'invention se rapporte à des procédés de traitement de tumeurs au moyen d'un complexe métallique radiomarqué en tant qu'agent radiopharmaceutique, pour le traitement de la tumeur.

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