Hydrolysis-promoting hydrophobic taxane derivatives
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United States of America Patent
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Aug 22, 2000
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N/A
app pub date -
Feb 12, 1999
filing date -
Sep 12, 1995
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Abstract
Provided herein is a taxane having a hydrocarbon attached at the 2' and/or 7 positions, the hydrocarbon's alpha position being occupied by a 'hydrolysis-promoting group' ('HPG'). In one embodiment, the hydrolysis promoting group is stereospecifically attached to the .alpha.-carbon of the hydrophobic taxane. The Substitution of an HPG for the methylene unit ordinarily occupying the alpha position allows for enhanced in vivo hydrolysis of the hydrocarbon-taxane bond, and hence, for enhanced taxane therapeutic activity. Also provided herein are taxane-containing compositions, and methods of administering taxanes to animals, including those afflicted with cancers or inflammatory diseases.
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