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. 14, 2018

Filed:

Mar. 14, 2014
Applicant:

The United States of America, As Represented BY the Secretary, Department of Health & Human Services, Washington, DC (US);

Inventors:

Wenjian Qian, Frederick, MD (US);

Jung Eun Park, Bethesda, MD (US);

Christopher C. Lai, Ellicott City, MD (US);

James A. Kelley, Silver Spring, MD (US);

Kyung S. Lee, Gaithersburg, MD (US);

Terrence R. Burke, Jr., Bethesda, MD (US);

Attorneys:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K 38/00 (2006.01); C07K 7/06 (2006.01); C12N 9/12 (2006.01); C07F 9/141 (2006.01); C07F 9/40 (2006.01); C07K 1/06 (2006.01);
U.S. Cl.
CPC ...
C07K 7/06 (2013.01); A61K 38/005 (2013.01); C07F 9/1411 (2013.01); C07F 9/4071 (2013.01); C07K 1/061 (2013.01); C12N 9/1205 (2013.01); C07K 2319/21 (2013.01); C07K 2319/50 (2013.01);
Abstract

The invention provides novel compounds that may serve as anticancer therapeutics. The compounds of the invention bind to polo-like kinases through the polo-box domain. In certain embodiments, the compounds of the invention are POM-protected peptide derivatives. The use of cationic bis-alkyl his residues in combination with a mono POM-protected phophoryl group results in a peptide possessing an overall neutral charge. The peptide derivatives of the invention have achieved both good efficacy and an enhanced bioavailability. The invention also provides methods of use, compositions, and kits thereof. Further, the invention provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.


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