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:
Dec. 12, 2017

Filed:

May. 02, 2014
Applicant:

Duke University, Durham, NC (US);

Inventors:

Michael Zalutsky, Chapel Hill, NC (US);

Ganesan Vaidyanathan, Chapel Hill, NC (US);

Assignee:

Duke University, Durham, NC (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K 51/10 (2006.01); C07D 403/12 (2006.01); C07D 207/46 (2006.01); C07D 207/416 (2006.01); C07D 487/04 (2006.01); C07B 59/00 (2006.01); A61K 51/08 (2006.01);
U.S. Cl.
CPC ...
A61K 51/1093 (2013.01); A61K 51/088 (2013.01); A61K 51/1051 (2013.01); C07B 59/002 (2013.01); C07D 207/416 (2013.01); C07D 207/46 (2013.01); C07D 403/12 (2013.01); C07D 487/04 (2013.01);
Abstract

Prosthetic compounds are disclosed that are effective for radiolabeling biomolecules with 18F. Representative biomolecules include antibodies (e.g., monoclonal antibodies (mAbs) and nanobodies (sdAbs)), antibody fragments, and peptides that may have an affinity for particular types of cells, such as cancer cells. The prosthetic compounds effectively address the art-recognized difficulties associated with the retention of radioactivity within the targeted cells, due to internalization of the biomolecule, followed by proteolytic degradation. Representative prosthetic compounds include (i) a succinimidyloxycarbonyl moiety, (ii) a radioactive moiety bearing 18F, and (iii) a charged moiety, i.e., a moiety that is charged under the physiological conditions of the internal cell environment.


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