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

Patent · Tue Jun 27 00:00:00 EDT 1995

OSTI ID:87720

Mease, R C; Mausner, L F; Srivastava, S C

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.

• Research Organization: Associated Universities Inc
• DOE Contract Number: AC02-76CH00016
• Assignee: Associated Universities, Inc., Washington, DC (United States)
• Patent Number(s): US 5,428,156/A/
• Application Number: PAN: 8-042,249; CNN: Grant CA-51958
• OSTI ID: 87720
• Resource Relation: Other Information: PBD: 27 Jun 1995
• Country of Publication: United States
• Language: English

Related Subjects

55 BIOLOGY AND MEDICINE
BASIC STUDIES
RADIOPHARMACEUTICALS
CHEMICAL PREPARATION
DIAGNOSTIC USES
THERAPEUTIC USES
SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY
POSITRON COMPUTED TOMOGRAPHY