The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Aug. 12, 2025

Filed:

Jun. 27, 2022
Applicants:

Hampton University, Hampton, VA (US);

University of Virginia Patent Foundation, Charlottesville, VA (US);

Inventors:

Tyvin A. Rich, Charlottesville, VA (US);

Dongfeng Pan, Charlottesville, VA (US);

Mahendra D. Chordia, Charlottesville, VA (US);

Assignees:

UNIVERSITY OF VIRGINIA PATENT FOUNDATION, Charlottesville, VA (US);

HAMPTON UNIVERSITY, Hampton, VA (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07H 19/073 (2006.01); A61K 31/7072 (2006.01); A61N 5/10 (2006.01); A61P 35/00 (2006.01); C07B 59/00 (2006.01);
U.S. Cl.
CPC ...
C07H 19/073 (2013.01); A61K 31/7072 (2013.01); A61N 5/10 (2013.01); A61P 35/00 (2018.01); C07B 59/005 (2013.01); A61N 2005/1087 (2013.01);
Abstract

The present application provides compositions and methods for preparing and using 'heavy' nucleotide derivatives of thymidine or uridine by replacing the oxygen atom attached to one or more of positions with non-radioactive oxygen-18 (O), administering it to a subject to target a tumor including incorporation into tumor cell DNA, and then treating the tumor with proton beam therapy to transmutate theO toF, resulting in a break of the new fluorine-phosphorous bond. This chemical event destabilizes ribose-phosphate DNA back-bone and base pairing thus produce single- and double strand breaks, clusters lesions that can lead to irreparable DNA damage and enhanced tumor cell killing. The atomic, chemical, and physical aspects result in the use of lower radiation doses and significantly alter acute and late morbidity of radiotherapy. Heavy thymidine and heavy uridine derivatives labeled withO have been made and tested.


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