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Title: Cage-like bifunctional chelators, copper-64 radiopharmaceuticals and PET imaging using the same

Abstract

Disclosed is a class of versatile Sarcophagine based bifunctional chelators (BFCs) containing a hexa-aza cage for labeling with metals having either imaging, therapeutic or contrast applications radiolabeling and one or more linkers (A) and (B). The compounds have the general formula ##STR00001## where A is a functional group selected from group consisting of an amine, a carboxylic acid, an ester, a carbonyl, a thiol, an azide and an alkene, and B is a functional group selected from the group consisting of hydrogen, an amine, a carboxylic acid, and ester, a carbonyl, a thiol, an azide and an alkene. Also disclosed are conjugate of the BFC and a targeting moiety, which may be a peptide or antibody. Also disclosed are metal complexes of the BFC/targeting moiety conjugates that are useful as radiopharmaceuticals, imaging agents or contrast agents.

Inventors:
; ; ;
Issue Date:
Research Org.:
Univ. of Southern California, Los Angeles, CA (United States)
Sponsoring Org.:
USDOE
OSTI Identifier:
1281082
Patent Number(s):
9403875
Application Number:
12/695,125
Assignee:
University of Southern California (Los Angeles, CA)
Patent Classifications (CPCs):
A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61P - SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
Resource Type:
Patent
Resource Relation:
Patent File Date: 2010 Jan 27
Country of Publication:
United States
Language:
English
Subject:
62 RADIOLOGY AND NUCLEAR MEDICINE

Citation Formats

Conti, Peter S., Cai, Hancheng, Li, Zibo, and Liu, Shuanglong. Cage-like bifunctional chelators, copper-64 radiopharmaceuticals and PET imaging using the same. United States: N. p., 2016. Web.
Conti, Peter S., Cai, Hancheng, Li, Zibo, & Liu, Shuanglong. Cage-like bifunctional chelators, copper-64 radiopharmaceuticals and PET imaging using the same. United States.
Conti, Peter S., Cai, Hancheng, Li, Zibo, and Liu, Shuanglong. Tue . "Cage-like bifunctional chelators, copper-64 radiopharmaceuticals and PET imaging using the same". United States. https://www.osti.gov/servlets/purl/1281082.
@article{osti_1281082,
title = {Cage-like bifunctional chelators, copper-64 radiopharmaceuticals and PET imaging using the same},
author = {Conti, Peter S. and Cai, Hancheng and Li, Zibo and Liu, Shuanglong},
abstractNote = {Disclosed is a class of versatile Sarcophagine based bifunctional chelators (BFCs) containing a hexa-aza cage for labeling with metals having either imaging, therapeutic or contrast applications radiolabeling and one or more linkers (A) and (B). The compounds have the general formula ##STR00001## where A is a functional group selected from group consisting of an amine, a carboxylic acid, an ester, a carbonyl, a thiol, an azide and an alkene, and B is a functional group selected from the group consisting of hydrogen, an amine, a carboxylic acid, and ester, a carbonyl, a thiol, an azide and an alkene. Also disclosed are conjugate of the BFC and a targeting moiety, which may be a peptide or antibody. Also disclosed are metal complexes of the BFC/targeting moiety conjugates that are useful as radiopharmaceuticals, imaging agents or contrast agents.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {Tue Aug 02 00:00:00 EDT 2016},
month = {Tue Aug 02 00:00:00 EDT 2016}
}

Works referenced in this record:

Metal radionuclide labeled proteins for diagnosis and therapy
patent, September 1993


MicroPET and Autoradiographic Imaging of Breast Cancer α v -Integrin Expression Using 18 F- and 64 Cu-Labeled RGD Peptide
journal, January 2004


Method for labeling antibodies with a metal ion
patent, October 1991


Metal radionuclide labeled proteins for diagnosis and therapy
patent, December 1992