Radiohalogenation conjugate technology

Chemistry: natural resins or derivatives; peptides or proteins; – Proteins – i.e. – more than 100 amino acid residues – Blood proteins or globulins – e.g. – proteoglycans – platelet...

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530345, 5303911, 5303913, 530405, 530409, 530410, 424 9, 436545, 436547, 436548, C07K 1528, C07K 1702, A61K 4902

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active

053027000

ABSTRACT:
Compounds of the formulae, ##STR1## are provided where L is a linking group of the formula, ##STR2## is --Sn(n--C.sub.4 H.sub.9).sub.3 or --Sn(CH.sub.3).sub.3, HgCl or --N.sub.2.sup.+ ; R is hydrogen, methyl, mono-, di- or oligosaccharide; and R' is methyl. The compounds are site-specifically halogenated or radiohalogenated at the A group and coupled with macromolecules such as monoclonal antibodies, peptides or other proteins.

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patent: 5057301 (1991-10-01), Wilbur et al.
Abstract preparation for The Society of Nuclear Medicine 40th Annual Meeting, Toronto Convention Center Jun. 8-Jun. 11, 1993 by Garg et al.
Manuscript entitled "N-succinimidyl-4-Methyl-3-(Tri-n-Butylstannyl)benzoate:Synthesis and Potential Utility for radioiodination of Monoclonal Antibodies" by Garg et al.
Garg et al., "Labeling Proteins Using Aryl Iodide Acylation Agents: Influence of Meta vs. Para Substitution on In Vivo Stability," Nucl. Med. Biol. vol. 16, No. 7, pp. 669-673, 1989.
Wilbur, et al., "Radioiodinated Iodobenzoyl Conjugates of a Monoclonal Antibody Fab Fragment. In Vivo Comparisons with Chloramine-T-Labeled Fab," Bioconjugate Chem. 1991, 2, 111-116.
Garg et al., "N-Succinimidyl 5-(Trialkylstannyl)-3-Pyridine Carboxylates: A New Class of Reagent for Protein Radioiodination", Bioconjugate Chem., 1991, 2, 50-55.

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