Small molecule inhibitors of lactate dehydrogenase and methods of use thereof

US10961200B2 · kind B2 · utility

Assignees

• The United States of America, as represented by the Secretary, Department of Health and Human Services · US
• VANDERBILT UNIVERSITY · US
• THE UAB RESEARCH FOUNDATION · US
• The Trustees of the University of Pennsylvania · US

Inventors

• David J. Maloney · Point of Rocks, US
• Alex G. Waterson · Durham, US
• Ganesh Rai Bantukallu · Arlington, US
• Kyle Ryan Brimacombe · Bethesda, US
• Plamen P. Christov · Mount Juliet, US
• Chi V. Dang · Penn Valley, US
• Victor Darley-Usmar · Birmingham, US
• Xin Hu · Chestertown, US
• Ajit Jadhav · Chantilly, US
• Somnath Jana · Nashville, US
• Kwangho Kim · Nashville, US
• Jennifer L. Kouznetsova · Silver Spring, US
• William J. Moore · Hagerstown, US
• Bryan T. Mott · College Park, US
• Leonard M. Neckers · Bethesda, US
• Anton Simeonov · Rockville, US
• Gary A. Sulikowski · Brentwood, US
• Daniel Jason Urban · Rockville, US
• Shyh-Ming Yang · Doylestown, US

Key dates

• Filing date: Jun 28, 2019
• Grant date: Mar 30, 2021
• Expiry date: Jun 28, 2039

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D495/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Provided is a compound of formula (I) in which Ar1, R1, 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.