Macrocyclic polyaminocarboxylates for stable radiometal antibody conjugates for therapy, spect and pet imaging
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United States of America Patent
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Jun 17, 1997
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Feb 2, 1995
filing date -
Apr 2, 1993
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Abstract
A simple method for the synthesis of 1,4,7, 10-tetraazacyclododecane N,N'N',N''-tetraacetic acid and 1,4,8,11-tetraazacyclotetradecane N,N',N',N''-tetraacetic acid involves cyanomethylating 1,4,7, 10-tetraazacyclododecane or 1,4,8,11-tetraazacyclotetradecane to form a tetranitrile and hydrolyzing the tetranitrile. These macrocyclic compounds are functionalized through one of the carboxylates and then conjugated to various biological molecules including monoclonal antibodies. The resulting conjugated molecules are labeled with radiometals for SPECT and PET imaging and for radiotherapy.
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