Hydrolysis-promoting hydrophobic taxane derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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Details

510510, 510511, A61K 31337, C07D30514

Patent

active

061073326

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.

REFERENCES:
patent: 5703117 (1997-12-01), Mayhew et al.
McLaughlin, et al., "19-Hydroxybaccatin III, 10-Deacetylcephalomannine, and 10-Deacetyltaxol: New anti-tumor Taxanes from Taxus Wallichiana," J. Nat Prod., 44(3), 312-319, 1981.

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