Hydrolysis-promoting hydrophobic taxane derivatives

Details Hydrolysis-promoting hydrophobic taxane derivatives Hydrolysis-promoting hydrophobic taxane derivatives

1996-09-12

1997-12-30

Trinh, Ba K.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

549510, 549511, A61K 31335, C07D30514

Patent

active

057031177

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"). 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.

REFERENCES:
patent: 5580899 (1996-12-01), Mayhew et al.

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