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Title: Synthesis of macrocyclic polyaminocarboxylates and their use for preparing stable radiometal antibody immunoconjugates for therapy, spect and pet imaging

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.
Inventors:
 [1];  [2];  [3]
  1. (Fairfax, VA)
  2. (Stony Brook, NY)
  3. (Setauket, NY)
Issue Date:
OSTI Identifier:
869952
Assignee:
Associated Universities, Inc. (Washington, DC) BNL
Patent Number(s):
US 5428156
Application Number:
08/042,249
Contract Number:
AC02-76CH00016
Research Org:
ASSOC UNIVERSITIES INC
Country of Publication:
United States
Language:
English
Subject:
synthesis; macrocyclic; polyaminocarboxylates; preparing; stable; radiometal; antibody; immunoconjugates; therapy; spect; pet; imaging; simple; method; 10-tetraazacyclododecane; -tetraacetic; acid; 11-tetraazacyclotetradecane; involves; cyanomethylating; form; tetranitrile; hydrolyzing; compounds; functionalized; carboxylates; conjugated; various; biological; molecules; including; monoclonal; antibodies; resulting; labeled; radiometals; radiotherapy; -tetraacetic acid; biological molecules; stable radiometal; radiometal antibody; acetic acid; monoclonal antibodies; pet imaging; various biological; macrocyclic compounds; molecules including; antibody immunoconjugates; simple method; macrocyclic polyaminocarboxylates; /999/