Prodrug forms of kinase inhibitors and their use in therapy

595206 Disclosed herein are prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the trigger has the structure of Formula IIId whe...

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Bibliographische Detailangaben
Hauptverfasser: HAY MICHAEL PATRICK, LEE HO HUAT, ANDERSON ROBERT FORBES, WILSON WILLIAM ROBERT, ASHOORZADEH AMIR, LU GUO-LIANG, PATTERSON ADAM VORN, SMAILL JEFFREY BRUCE, DENNY WILLIAM ALEXANDER
Format: Patent
Sprache:eng
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Zusammenfassung:595206 Disclosed herein are prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the trigger has the structure of Formula IIId wherein * is a point of attachment, R8 is selected from H and C1-C3 alkyl, and R9 is selected from H and C1-C6 alkyl. The disclosed compounds are useful in treating proliferative diseases such as cancer.