-astatine containing radiotherapeutics for the treatment of cancer

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United States of America Patent

PATENT NO 10457642
APP PUB NO 20180162818A1
SERIAL NO

15571055

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Abstract

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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.

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Patent OwnerAddress
THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA1ST FLOOR GARDNER STEEL CONFERENCE CENTER 130 THACKERAY AVENUE PITTSBURGH PA 15260

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Lieberman, Brian P Philadelphia, US 1 1
Mach, Robert H Wallingford, US 24 114
Makvandi, Mehran Philadelphia, US 3 3
Pryma, Daniel A Bryn Mawr, US 2 1

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