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

Abstract

A simple method for the synthesis of 1,4,7,10-tetraazacyclododecane N,N{prime}N{double_prime},N{prime}{double_prime}-tetraacetic acid and 1,4,8,11-tetraazacyclotetradecane N,N{prime},N{double_prime},N{prime}{double_prime}-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. 4 figs.

Inventors:
; ;
Issue Date:
Research Org.:
Associated Universities Inc
OSTI Identifier:
87720
Patent Number(s):
5428156
Application Number:
PAN: 8-042,249; CNN: Grant CA-51958
Assignee:
Associated Universities, Inc., Washington, DC (United States)
DOE Contract Number:  
AC02-76CH00016
Resource Type:
Patent
Resource Relation:
Other Information: PBD: 27 Jun 1995
Country of Publication:
United States
Language:
English
Subject:
55 BIOLOGY AND MEDICINE, BASIC STUDIES; RADIOPHARMACEUTICALS; CHEMICAL PREPARATION; DIAGNOSTIC USES; THERAPEUTIC USES; SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY; POSITRON COMPUTED TOMOGRAPHY

Citation Formats

Mease, R C, Mausner, L F, and Srivastava, S C. Synthesis of macrocyclic polyaminocarboxylates and their use for preparing stable radiometal antibody immunoconjugates for therapy, SPECT and PET imaging. United States: N. p., 1995. Web.
Mease, R C, Mausner, L F, & Srivastava, S C. Synthesis of macrocyclic polyaminocarboxylates and their use for preparing stable radiometal antibody immunoconjugates for therapy, SPECT and PET imaging. United States.
Mease, R C, Mausner, L F, and Srivastava, S C. Tue . "Synthesis of macrocyclic polyaminocarboxylates and their use for preparing stable radiometal antibody immunoconjugates for therapy, SPECT and PET imaging". United States.
@article{osti_87720,
title = {Synthesis of macrocyclic polyaminocarboxylates and their use for preparing stable radiometal antibody immunoconjugates for therapy, SPECT and PET imaging},
author = {Mease, R C and Mausner, L F and Srivastava, S C},
abstractNote = {A simple method for the synthesis of 1,4,7,10-tetraazacyclododecane N,N{prime}N{double_prime},N{prime}{double_prime}-tetraacetic acid and 1,4,8,11-tetraazacyclotetradecane N,N{prime},N{double_prime},N{prime}{double_prime}-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. 4 figs.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {1995},
month = {6}
}