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Macrocyclic polyaminocarboxylates for stable radiometal antibody conjugates for therapy, spect and pet imaging

Patent ·
OSTI ID:871006
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.
Research Organization:
ASSOC UNIVERSITIES INC
DOE Contract Number:
AC02-76CH00016
Assignee:
Associated Universities, Inc. (Washington, DC)
Patent Number(s):
US 5639879
Application Number:
08/382,522
OSTI ID:
871006
Country of Publication:
United States
Language:
English

References (2)