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

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 parti...

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Main Authors Maloney, David J, Mott, Bryan T, Christov, Plamen, Urban, Daniel Jason, Dang, Chi V, Simeonov, Anton, Jana, Somnath, Yang, Shyh Ming, Jadhav, Ajit, Moore, William J, Bantukallu, Ganesha Rai, Darley-Usmar, Victor M, Kim, Kwangho, Hall, Matthew, Sulikowski, Gary Allen, Brimacombe, Kyle Ryan, Hu, Xin, Neckers, Leonard M, Waterson, Alex Gregory
Format Patent
LanguageEnglish
Published 23.03.2021
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary: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.
Bibliography:Application Number: US201716313727