Cage-like bifunctional chelators, copper-64 radiopharmaceuticals and PET imaging using the same

摘要

Disclosed is a class of versatile Sarcophagine based bifunctional chelators (BFCs) containing a hexa-aza cage for labeling with metals having either imaging, therapeutic or contrast applications radiolabeling and one or more linkers (A) and (B). The compounds have the general formula;where A is a functional group selected from group consisting of an amine, a carboxylic acid, an ester, a carbonyl, a thiol, an azide and an alkene, and B is a functional group selected from the group consisting of hydrogen, an amine, a carboxylic acid, and ester, a carbonyl, a thiol, an azide and an alkene. Also disclosed are conjugate of the BFC and a targeting moiety, which may be a peptide or antibody. Also disclosed are metal complexes of the BFC/targeting moiety conjugates that are useful as radiopharmaceuticals, imaging agents or contrast agents.

主权项

1. A chemical composition comprising: wherein A is a carboxylic acid having the formula: and wherein R1, R2, R3, and R4 are independently selected from the group consisting of H, halogen, alkyl, alkoxy or alkene, and a salt or an ester thereof, and B is a functional group selected from the group consisting of hydrogen, and amine, a carboxylic acid, an ester, a carbonyl, a thiol, an azide and alkene.