7-MORPHOLINO-L,6-NAPHTHYRIDIN-5-YL DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF USEFUL AS DNA-PK INHIBITOR

The present disclosure provides compounds and methods for inhibiting DNA-dependent protein kinase (DNA-PK). Aspects of the present disclosure also include methods of using the compounds to treat diseases, including, but not limited to, cancer. In certain embodiments, the compounds inhibit DNA-PK and...

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Bibliographische Detailangaben
Hauptverfasser: HSIEH, Tom Han Hsiao, YEE, Leanna, PAQUETTE, Jay John, ARNS, Stephen Paul, OSBORNE, Simon, SMYTH, Elliott, KYLE, Alastair H, MINCHINTON, Andrew I, SHIDMOOSSAVEE, Fahimeh S, HAMBY, Callum, AMBLER, Martin, JAQUITH, James Brian, TAN, Jason Samuel, BAKER, Jennifer H. E, SMILJANIC-HURLEY, Ela
Format: Patent
Sprache:eng ; fre ; ger
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Zusammenfassung:The present disclosure provides compounds and methods for inhibiting DNA-dependent protein kinase (DNA-PK). Aspects of the present disclosure also include methods of using the compounds to treat diseases, including, but not limited to, cancer. In certain embodiments, the compounds inhibit DNA-PK and thus sensitize cancers to therapies such as chemotherapy and radiotherapy. Certain compounds of the present disclosure are in the form of prodrugs that release the DNA-PK inhibitor in hypoxic tissue such as is known to occur in cancers. Aspects of the present disclosure also include methods of using the compounds for repairing a DNA break in a target genomic region or for modifying expression of one or more genes or proteins. Compounds provided are of formula.