Labeled inhibitors of prostate specific membrane antigen...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 213/38 (2006.01) A61K 51/04 (2006.01)

Patent

CA 2694266

The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. Various 99mTc/Re-labeled compounds were prepared by attaching known Tc/Re chelating agents to an amino--functionalized PSMA inhibitor with or without a variable length linker moiety. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+ PC3 PIP tumors.

La présente invention concerne l'antigène membranaire spécifique de la prostate (PSMA) qui est de plus en plus souvent considéré comme cible viable pour l'imagerie et la thérapie du cancer. Divers composés 99mTc/ à nouveau marqués ont été préparés par la liaison d'agents chélateurs Tc/Re connus avec un inhibiteur du PSMA amino-fonctionnalisé, avec ou sans un groupement lieur de longueur variable. La biodistribution ex vivo et l'imagerie ex vivo ont mis en évidence le degré de liaison spécifique avec des tumeurs PSMA+ PC3 PIP fabriquées par génie génétique.

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