Synthesis of hydrophobic taxane derivatives

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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549511, C07D30514

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active

059395672

ABSTRACT:
This invention provides a taxane derivative of the formula: ##STR1## wherein a hydrophobic organic moiety is attached to a taxane. R and R.sup.1 is each indepently H or a hydrophobic organic moiety, as long as at least one of R and R.sup.1 is not H. Attachment of a hydrophobic organic moiety to the taxane so as to obtain a taxane derivative generally stabilizes the association of the derivative with a lipid, including a liposomal lipid, carrier in the plasma of animals to which the derivative-carrier association is administered. Also provided herein is a composition containing the taxane derivative and a pharmaceutically acceptable medium; desirably, the medium also contains a lipid carrier, and the derivative is associated with the carrier. Further provided herein is a method of administering taxane derivatives to animals, for example, animals afflicted with cancers.

REFERENCES:
patent: 4960790 (1990-10-01), Stella et al.
patent: 5015744 (1991-05-01), Holton
patent: 5200534 (1993-04-01), Rao
patent: 5534499 (1996-07-01), Ansell
Borman, "Scientists Mobilize to Increase Supply of Anticancer Drug Taxol", Chemical & Engineering News, Sep. 2, 1991, 11-18.
Edgington, et al., "Taxol, Out of the Woods", Biotechnology, 9:933-938 (Oct. 1991).
Holton, et al., "First Total Synthesis of Taxol. 1. Functionalization of the B Ring", J. Am. Chem. Sos. 116:1597-1600, (1994).
Nicolau, "Design, sysnthesis and biological activity of protaxols", Nature, 364, 464-466, 1993.
Nicolau, et al., "Total Synthesis of Taxol", Nature, 367:630-634 (1994).
Rizzo, et al., "Analysis of anitcancer drugs in biological fluids: determination of taxol with application to clainical pharmacokinetics", J. Pharma. & Biomed. Anal. 8(2): 159 (1990).
Schiff, et al., "Promotion of microtubule assembly in vitro by taxol", Nature 277:665 (1979).
Schiff, "Taxol stabilizes microtubules in mouse fibroblast cells", Proc. Natl. Acad. Sci. USA, 77(3):1561-1565, 1980.
Suffness and Cordel, "Antitutmor Alkloids," in: The Alkaloids, Volume XXI, Academic Press, New York, pp. 5-18 (1985).

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