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

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.

Inventors:
 [1];  [2];  [3]
  1. (Fairfax, VA)
  2. (Stony Brook, NY)
  3. (Setauket, NY)
Issue Date:
Research Org.:
ASSOC UNIVERSITIES INC
OSTI Identifier:
871006
Patent Number(s):
5639879
Application Number:
08/382,522
Assignee:
Associated Universities, Inc. (Washington, DC) BNL
DOE Contract Number:  
AC02-76CH00016
Resource Type:
Patent
Country of Publication:
United States
Language:
English
Subject:
macrocyclic; polyaminocarboxylates; stable; radiometal; antibody; conjugates; therapy; spect; pet; imaging; simple; method; synthesis; 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; simple method; macrocyclic polyaminocarboxylates; /999/

Citation Formats

Mease, Ronnie C., Mausner, Leonard F., and Srivastava, Suresh C. Macrocyclic polyaminocarboxylates for stable radiometal antibody conjugates for therapy, spect and pet imaging. United States: N. p., 1997. Web.
Mease, Ronnie C., Mausner, Leonard F., & Srivastava, Suresh C. Macrocyclic polyaminocarboxylates for stable radiometal antibody conjugates for therapy, spect and pet imaging. United States.
Mease, Ronnie C., Mausner, Leonard F., and Srivastava, Suresh C. Tue . "Macrocyclic polyaminocarboxylates for stable radiometal antibody conjugates for therapy, spect and pet imaging". United States. https://www.osti.gov/servlets/purl/871006.
@article{osti_871006,
title = {Macrocyclic polyaminocarboxylates for stable radiometal antibody conjugates for therapy, spect and pet imaging},
author = {Mease, Ronnie C. and Mausner, Leonard F. and Srivastava, Suresh C.},
abstractNote = {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.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {1997},
month = {6}
}

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