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

Patent ·
OSTI ID:869952
 [1];  [2];  [3]
  1. Fairfax, VA
  2. Stony Brook, NY
  3. Setauket, NY
+ Show Author Affiliations

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:
Associated Universities, Inc., Upton, NY (United States)
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

References (11)

Investigations of N-linked macrocycles for 111in and 90Y labeling of proteins journal February 1992
Synthesis of nonionic gadolinium chelates useful as contrast agents for magnetic resonance imaging: 1,4,7-tris(carboxymethyl)-10-substituted-1,4,7,10-tetraazacyclododecanes and their corresponding gadolinium chelates journal March 1991
The peptide way to macrocyclic bifunctional chelating agents: synthesis of 2-(p-nitrobenzyl)-1,4,7,10-tetraazacyclododecane-N,N',N",N'''-tetraacetic acid and study of its yttrium(III) complex journal August 1988
Gd(DOTA): An alternative to Gd(DTPA) as aT1,2 relaxation agent for NMR imaging or spectroscopy journal October 1986
Copper chelates as probes of biological systems: Stable copper complexes with a macrocyclic bifunctional chelating agent journal July 1985
Synthesis of a kinetically stable yttrium-90 labelled macrocycle–antibody conjugate journal January 1989
Preparation and characterization of paramagnetic polychelates and their protein conjugates journal January 1990
Nuclear magnetic resonance spectroscopy of lanthanide complexes with a tetraacetic tetraaza macrocycle. Unusual conformation properties journal May 1980
Simplified method for conjugating macrocyclic bifunctional chelating agents to antibodies via 2-iminothiolane journal May 1990
Newer approaches to the radiolabeling of monoclonal antibodies by use of metal chelates journal January 1991
An efficient method for labelling antibodies with 111 In journal January 1984

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Related Subjects

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/