The Liposome Company, Inc.

Soumendu Bhattacharya

Andrew S Janoff

Imran Ahmad

Eric G Mayhew

Shaukat Ali

J Craig Franklin

Gil Koehane

Provided herein is a taxane having a hydrocarbon attached at the 2&prime; and/or 7 positions, the hydrocarbon's alpha position being occupied by a &ldquo;hydrolysis-promoting group&rdquo; (&ldquo;HPG&rdquo;). In one embodiment, the hydrolysis promoting group is stereospecifically attached to the &agr;-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.

Hydrolysis-promoting hydrophobic taxane derivatives

Provided herein is a taxane having a hydrocarbon attached at the 2&prime; and/or 7 positions, the hydrocarbon's alpha position being occupied by a &ldquo;hydrolysis-promoting group&rdquo; (&ldquo;HPG&rdquo;). In one embodiment, the hydrolysis promoting group is stereospecifically attached to the a-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.

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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Plainsboro, NJ, United States of America

Soumendu Bhattacharya