1 H-pyrazol-1-yl-thiazoles as inhibitors of lactate dehydrogenase and methods of use thereof

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United States of America Patent

PATENT NO 10954228
APP PUB NO 20190276448A1
SERIAL NO

16313727

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Abstract

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The disclosure provides a compound of the formula (II) and pharmaceutically acceptable salts thereof. The variables, e.g. n, R, R3, R10, X, Y, and Z are defined herein. These compounds act as lactate dehydrogenase inhibitors and are useful for treating cancer and fibrosis. The compounds may be particularly useful for treating forms of cancer in which a metabolic switch from oxidative phosphorylation to glycolysis has occurred. The disclosure also provides pharmaceutical compositions containing a compound of this formula and method for treating patients having cancer, fibrosis, or other conditions in which a metabolic switch from oxidative phosphorylation to glycolysis has occurred.

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Patent Owner(s)

  • THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA; THE UAB RESEARCH FOUNDATION; BOARD OF GOVERNORS OF WAYNE STATE UNIVERSITY AND VANDERBILT UNIVERSITY; NATIONAL INSTITUTES OF HEALTH, UNITED STATES DEPT. OF HEALTH AND HUMAN SERVICES

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Bantukallu, Ganesha Rai Arlington, US 4 32
Brimacombe, Kyle Ryan Brook Park, US 7 10
Christov, Plamen Mount Juliet, US 5 8
Dang, Chi V Penn Valley, US 11 31
Darley-Usmar, Victor M Birmingham, US 3 1
Hall, Matthew Darnestown, US 44 395
Hu, Xin Frederick, US 127 1139
Jadhav, Ajit Chantilly, US 21 63
Jana, Somnath Nashville, US 7 8
Kim, Kwangho Nashville, US 81 287
Maloney, David J Points of Rocks, US 33 477
Moore, William J Hagerstown, US 42 1323
Mott, Bryan T College Park, US 7 14
Neckers, Leonard M Bethesda, US 15 14
Simeonov, Anton Bethesda, US 31 123
Sulikowski, Gary Allen Brentwood, US 5 8
Urban, Daniel Jason Poolesville, US 9 10
Waterson, Alex Gregory Nashville, US 15 48
Yang, Shyh Ming Doylestown, US 11 12

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