Macrocyclic polyaminocarboxylates for stable radiometal antibody conjugates for therapy, SPECT and PET imaging

Patent · Tue Jun 17 00:00:00 EDT 1997

OSTI ID:512425

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
• Sponsoring Organization: USDOE, Washington, DC (United States); National Insts. of Health, Bethesda, MD (United States)
• DOE Contract Number: AC02-76CH00016
• Assignee: Associated Universities, Inc., Washington, DC (United States)
• Patent Number(s): US 5,639,879/A/
• Application Number: PAN: 8-382,522; CNN: Grant CA-51958; TRN: 97:013495
• OSTI ID: 512425
• Resource Relation: Other Information: PBD: 17 Jun 1997
• Country of Publication: United States
• Language: English

Related Subjects

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