Gemcitabine derivatives

C - Chemistry – Metallurgy – 07 – H

Patent

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Details

C07H 19/073 (2006.01) A61K 31/70 (2006.01) C07H 19/06 (2006.01)

Patent

CA 2278056

The invention provides Gemcitabine esters or amides in which the 3'- and/or 5'- OH group and/or the N4-amino group is derivatised with a C18- and/or C20- saturated or mono-unsaturated aryl group, preferably an acyl group selected from oleoyl, elaidoyl, cis-icosenoyl and trans-eicosenoyl. The Gemcitabine esters and amides are useful as anti- cancer and anti-viral agents.

L'invention concerne des esters ou des amides de gemcitabine, dans lesquels le groupe 3'- et/ou 5'-OH et/ou le groupe N<4>-amino est dérivé à l'aide d'un groupe acyle C18 et/ou C20 saturé ou monosaturé, de préférence un groupe acyle choisi parmi oléoyle, élaidoyle, cis-éicosénoyle et trans-éicosénoyle. Les esters et amides de Gemcitabine sont utiles en tant qu'agents anticancéreux et antiviraux.

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