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 method...

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Hauptverfasser: JONES, Brian Thomas, MARTINEZ, Luisruben P, PEI, Zhonghua, BECK, Hilary Plake, FLEURY, Melissa, MCSPADDEN, Ethan DeNardo, BARSANTI, Paul A, KNOX, John E, WANG, Chenbo
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Sprache:eng
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Zusammenfassung: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.