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Title: 211-astatine containing radiotherapeutics for the treatment of cancer

Abstract

Described herein is an alpha-emitting radionuclide, 211At, which has been incorporated into a selective sigma-2 ligand moiety to provide cytotoxic capabilities to a chemical compound. As described herein, a compound of formula (I), wherein R1-R4, m, and n are defined herein, was prepared and utilized in in vitro and in vivo tumor targeting of alpha-emitting sigma-2 ligand in a breast cancer model. In one embodiment, the compound is 5-(211At)—N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2,3-dimethoxybenzamide.

Inventors:
; ; ;
Issue Date:
Research Org.:
Univ. of Pennsylvania, Philadelphia, PA (United States)
Sponsoring Org.:
USDOE Office of Science (SC), Biological and Environmental Research (BER)
OSTI Identifier:
1600218
Patent Number(s):
10457642
Application Number:
15/571,055
Assignee:
The Trustees of the University of Pennsylvania (Philadelphia, PA)
Patent Classifications (CPCs):
A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
G - PHYSICS G21 - NUCLEAR PHYSICS G21H - OBTAINING ENERGY FROM RADIOACTIVE SOURCES
DOE Contract Number:  
SC0012476
Resource Type:
Patent
Resource Relation:
Patent File Date: 04/26/2016
Country of Publication:
United States
Language:
English

Citation Formats

Pryma, Daniel A., Lieberman, Brian P., Makvandi, Mehran, and Mach, Robert H. 211-astatine containing radiotherapeutics for the treatment of cancer. United States: N. p., 2019. Web.
Pryma, Daniel A., Lieberman, Brian P., Makvandi, Mehran, & Mach, Robert H. 211-astatine containing radiotherapeutics for the treatment of cancer. United States.
Pryma, Daniel A., Lieberman, Brian P., Makvandi, Mehran, and Mach, Robert H. Tue . "211-astatine containing radiotherapeutics for the treatment of cancer". United States. https://www.osti.gov/servlets/purl/1600218.
@article{osti_1600218,
title = {211-astatine containing radiotherapeutics for the treatment of cancer},
author = {Pryma, Daniel A. and Lieberman, Brian P. and Makvandi, Mehran and Mach, Robert H.},
abstractNote = {Described herein is an alpha-emitting radionuclide, 211At, which has been incorporated into a selective sigma-2 ligand moiety to provide cytotoxic capabilities to a chemical compound. As described herein, a compound of formula (I), wherein R1-R4, m, and n are defined herein, was prepared and utilized in in vitro and in vivo tumor targeting of alpha-emitting sigma-2 ligand in a breast cancer model. In one embodiment, the compound is 5-(211At)—N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2,3-dimethoxybenzamide.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {2019},
month = {10}
}