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Bifunctional chelating agent for the design and development of site specific radiopharmaceuticals and biomolecule conjugation strategy

United States Patent

6,635,235
October 21, 2003
View the Complete Patent at the US Patent & Trademark Office
There is provided a method of labeling a biomolecule with a transition metal or radiometal in a site specific manner to produce a diagnostic or therapeutic pharmaceutical compound by synthesizing a P.sub.2 N.sub.2 -bifunctional chelating agent intermediate, complexing the intermediate with a radio metal or a transition metal, and covalently linking the resulting metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. Also provided is a method of synthesizing the --PR.sub.2 containing biomolecules by synthesizing a P.sub.2 N.sub.2 -bifunctional chelating agent intermediate, complexing the intermediate with a radiometal or a transition metal, and covalently linking the resulting radio metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. There is provided a therapeutic or diagnostic agent comprising a --PR.sub.2 containing biomolecule.
Katti; Kattesh V. (Colubmia, MO), Prabhu; Kandikere R. (Bangalore, IN), Gali; Hariprasad (Columbia, MO), Pillarsetty; Nagavara Kishore (Columbia, MO), Volkert; Wynn A. (Columbia, MO)
The Curators of the University of Missouri (Columbia, MO)
09/ 602,487
June 23, 2000
GRANT INFORMATION Research in this application was supported in part by a grant from the Department of Energy (DEFG02-89ER60875). The government has certain rights in the invention. Research in this application was also supported in part by a grant from DuPont Pharmaceuticals (C-5-35122; and C-5-31488).