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

United States Patent

August 2, 2016
View the Complete Patent at the US Patent & Trademark Office
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 ##STR00001## 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.
Conti; Peter S. (Pasadena, CA), Cai; Hancheng (Alhambra, CA), Li; Zibo (Logan, UT), Liu; Shuanglong (Alhambra, CA)
12/ 695,125
January 27, 2010
STATEMENT REGARDING FEDERALLY SPONSORED RESEARCH AND DEVELOPMENT This work was supported by research grant from the Department of Energy. The government has certain rights in the invention.