Synthesis of macrocyclic polyaminocarboxylates and their use for preparing stable radiometal antibody immunoconjugates for therapy, spect and pet imaging
Patent
·
OSTI ID:869952
- Fairfax, VA
- Stony Brook, NY
- Setauket, NY
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 5428156
- Application Number:
- 08/042,249
- OSTI ID:
- 869952
- Country of Publication:
- United States
- Language:
- English
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acetic acid
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hydrolyzing
imaging
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including
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macrocyclic
macrocyclic compounds
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polyaminocarboxylates
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radiometal
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simple
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synthesis
tetranitrile
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various
various biological