THIADIAZOLYL DERIVATIVES AS DNA POLYMERASE THETA INHIBITORS AND USES THEREOF

THIADIAZOLYL DERIVATIVES AS DNA POLYMERASE THETA INHIBITORS AND USES THEREOF

Disclosed herein are compounds of Formula (I): (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 an...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: BOTYANSZKI, Janos, MASKEY, Reeja, FISCHER, Marcus Michael, ADAMS, Nicholas, DUFFY, Kevin, WANG, Chenbo
Format: Patent
Sprache:eng
Schlagworte:
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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Beschreibung
Zusammenfassung:Disclosed herein are compounds of Formula (I): (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. Further disclosed herein are methods of using compounds of Formula (I) or Formula (II) that inhibit DNA Polymerase Theta (Polθ) activity in combination with a Poly ADP Ribose Polymerase (PARP) inhibitor. (II)