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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.

Patent No.:

US 10351532 B1

PDFFull Text
Date of Patent:
Jul. 16, 2019

Filed:

Dec. 29, 2015

Small molecule inhibitors of lactate dehydrogenase and methods of use thereof

Applicants:

The United States of America As Represented BY the Secretary, Department of He, Bethesda, MD (US);

Vanderbilt University, Nashville, TN (US);

The Uab Research Foundation, Birmingham, AL (US);

The Trustees of the University of Pennsylvania, Philadelphia, PA (US);

Inventors:

David J. Maloney, Point of Rocks, MD (US);

Alex Gregory Waterson, Nashville, TN (US);

Ganesh Rai Bantukallu, Arlington, VA (US);

Kyle Ryan Brimacombe, Bethesda, MD (US);

Plamen Christov, Nashville, TN (US);

Chi V. Dang, Penn Valley, PA (US);

Victor Darley-Usmar, Brimingham, AL (US);

Xin Hu, Fredrick, MD (US);

Ajit Jadhav, Chantilly, VA (US);

Somnath Jana, Nashville, TN (US);

Kwangho Kim, Nashville, TN (US);

Jennifer L. Kouznetsova, Silver Spring, MD (US);

William J. Moore, Hagerstown, MD (US);

Bryan T. Mott, College Park, MD (US);

Leonard M. Neckers, Bethesda, MD (US);

Anton Simeonov, Bethesda, MD (US);

Gary Allen Sulikowski, Nashville, TN (US);

Daniel Jason Urban, Rockville, MD (US);

Shyh Ming Yang, Doylestown, PA (US);

Assignees:

THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES, Washington, DC (US);

VANDERBILT UNIVERSITY, Nashville, TN (US);

THE UAB RESEARCH FOUNDATION, Birmingham, AL (US);

THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA, Philadelphia, PA (US);

Attorney:

Cantor Colburn LLP

Primary Examiner:

Timothy R Rozof

Int. Cl.
CPC ...
C07D 231/20 (2006.01); C07D 231/38 (2006.01); C07D 401/04 (2006.01); C07D 403/04 (2006.01); C07D 403/06 (2006.01); C07D 409/04 (2006.01); C07D 413/04 (2006.01); C07D 417/04 (2006.01); C07D 417/14 (2006.01); C07D 471/04 (2006.01); C07D 495/04 (2006.01); C07D 495/14 (2006.01); A61K 31/4155 (2006.01); A61K 31/4178 (2006.01); A61K 31/422 (2006.01); A61K 31/427 (2006.01); A61K 31/437 (2006.01); A61K 31/4439 (2006.01); A61K 31/454 (2006.01); A61K 31/496 (2006.01); A61K 31/501 (2006.01); A61K 31/506 (2006.01); A61K 31/519 (2006.01); A61K 31/5355 (2006.01); A61K 31/415 (2006.01); A61K 45/06 (2006.01);
U.S. Cl.
CPC ...
C07D 231/20 (2013.01); A61K 31/415 (2013.01); A61K 31/4155 (2013.01); A61K 31/4178 (2013.01); A61K 31/422 (2013.01); A61K 31/427 (2013.01); A61K 31/437 (2013.01); A61K 31/4439 (2013.01); A61K 31/454 (2013.01); A61K 31/496 (2013.01); A61K 31/501 (2013.01); A61K 31/506 (2013.01); A61K 31/519 (2013.01); A61K 31/5355 (2013.01); A61K 45/06 (2013.01); C07D 231/38 (2013.01); C07D 401/04 (2013.01); C07D 403/04 (2013.01); C07D 403/06 (2013.01); C07D 409/04 (2013.01); C07D 413/04 (2013.01); C07D 417/04 (2013.01); C07D 417/14 (2013.01); C07D 471/04 (2013.01); C07D 495/04 (2013.01); C07D 495/14 (2013.01);
Abstract

Provided is a compound of formula (I), in which Ar, R, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.

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