Hydrophobic taxane derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 305/14 (2006.01) A61K 9/127 (2006.01) A61K 31/335 (2006.01) A61K 31/665 (2006.01) C07F 9/655 (2006.01)

Patent

CA 2209001

This invention provides a taxane derivative of formula (I), wherein a hydrophobic organic moiety is attached to a taxane. R and R1 is each independently H or a hydrophobic organic moiety, as long as at least one of R and R1 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.

L'invention porte sur un dérivé du taxane de formule générale (I) dans laquelle un fragment organique hydrophobe est attaché à un taxane, R et R<1> sont chacun H ou un fragment organique hydrophobe sous réserve que R ou R<1> ne soit pas H. La fixation d'un fragment organique hydrophobe sur un taxane en vue de l'obtention d'un dérivé du taxane stabilise sensiblement l'association du dérivé avec un lipide, notamment liposomique, porteur du plasma d'animaux auxquels l'association dérivé/porteur est administrée. L'invention porte également sur une composition contenant ledit dérivé du taxane et un milieu pharmacocompatible, ledit milieu contenant de préférence un porteur lipidique et le dérivé étant associé au porteur. Elle porte en outre sur un procédé d'administration de dérivés du taxane à des animaux, par exemple à des animaux souffrant de cancers.

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