Process for making a chelating agent for labeling...

Organic compounds -- part of the class 532-570 series – Organic compounds – Unsubstituted hydrocarbyl chain between the ring and the -c-...

Reexamination Certificate

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C540S470000, C540S476000, C549S470000, C534S010000

Reexamination Certificate

active

06838557

ABSTRACT:
The present invention is directed, in general, to a method for making high yields of functionalized cyclic or acyclic tertiary amine-containing compounds, termed active esters, the functionalized compounds themselves, and diagnostic or therapeutic systems incorporating such compounds. Ester groups are attached to all but one of its Nitrogen atoms of the tertiary amine-containing compound. Therefore, an active agent, in the presence of coupling agent, attaches to the remaining amine via a carboxylate group attached to the amine, to produce high yields of the active ester. The active ester is then combined with a biomolecule, to produce high yields of a bioconjugated product. A metal ion may be chelated to the bioconjugated product to produce a chelating agent for use in either diagnostic or therapeutic applications.

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Yasushi Arano, et al.; “Reassessment of Diethylenetriaminepentaacetic Acid (DTPA) as a Chelating Agent for Indium-111 Labeling of Polypeptides Using a Newly Synthesized Monoreactive DTPA Derivative”; 1996 American Chemical Society, J. Med. Chem. 1996, 39, pp. 3452-3460.
Louis A. Carpino, Hideko Imazumi, Ayman El-Faham, Fernando J, Ferrer, Chongwu Zhang, Yuasub Lee, Bruce M. Foxman, Peter Henklein, Christiane Hanay, Clemens Mugge, Holger Wenschuh, Jana Klose, Michael Beyermann and Michael Bienert: “The Uronium/Guanidinium Peptide Coupling Reagents: Finally the True Uronium Salts”; Angew. Chem. Int. Ed. 2002, 41, No. 3; pp. 442-445.
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