THIADIAZOLYL DERIVATIVES AS DNA POLYMERASE THETA INHIBITORS

Disclosed herein are certain thiadiazolyl derivatives Formula (I):that inhibit DNA Polymerase Theta (Polθ) activity, in particular inhibit Polθ activity by inhibiting ATP dependent helicase domain activity of Polθ. Also, disclosed are pharmaceutical compositions comprising such compounds and methods...

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Bibliographic Details
Main Authors JONES, Brian Thomas, MARTINEZ, Luisruben P, PEI, Zhonghua, BECK, Hilary Plake, FLEURY, Melissa, MCSPADDEN, Ethan DeNardo, BARSANTI, Paul A, KNOX, John E, WANG, Chenbo
Format Patent
LanguageEnglish
French
German
Published 08.11.2023
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:Disclosed herein are certain thiadiazolyl derivatives Formula (I):that inhibit DNA Polymerase Theta (Polθ) activity, in particular inhibit Polθ activity by inhibiting ATP dependent helicase domain activity of Polθ. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Polθ such as cancer, including homologous recombination (HR) deficient cancers.
Bibliography:Application Number: EP20200760608