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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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
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creator 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
description 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.
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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. 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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
title Prodrug forms of kinase inhibitors and their use in therapy
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