-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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THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA3600 CIVIC CENTER BOULEVARD 9TH FLOOR PHILADELPHIA PA 19104

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  • 2016 Application Filing Year
  • A61K Class
  • 19101 Applications Filed
  • 13019 Patents Issued To-Date
  • 68.16 % Issued To-Date
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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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  • 1 Citation Count
  • A61K Class
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Citation count rangeNumber of patents cited in rangeNumber of patents cited in various citation count ranges11535744839711494311101 - 1011 - 2021 - 3031 - 4041 - 5051 - 6081 - 9091 - 1000500100015002000250030003500400045005000550060006500700075008000850090009500100001050011000115001200012500

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