Novel taxoids, their preparation and pharmaceutical...

C - Chemistry – Metallurgy – 07 – D

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C07D 305/14 (2006.01) A61K 31/33 (2006.01) C07D 405/12 (2006.01) C07D 407/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07F 7/10 (2006.01)

Patent

CA 2175384

Novel taxoids of general formula (I), their preparation and pharmaceutical compositions containing them. In general formula (I), Ar is an aryl, alkyl, alkenyl, cycloalkyl or cycloalkenyl radical; R is a hydrogen atom or an alkanoyl, alkyloxyacetyl or alkyl radical; R¿1? is a benzoyl radical or a radical of formula R¿2?-O-CO-, wherein R¿2? is an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl, heterocyclyl radical and R¿3? is an alkyl, alkenyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted aryl (excepting non-substituted phenyl) or heterocyclyl radical. The novel products of general formula (I) have remarkable antitumor activity.

Nouveaux taxoïdes de formule générale (I), leur préparation et les compositions pharmaceutiques qui les contiennent. Dans la formule générale (I), Ar représente un radical aryle, alcoyle, alcényle, cycloalcoyle ou cycloalcényle; R représente un atome d'hydrogène ou un radical alcanoyle, alcoyloxyacétyle ou alcoyle; R1 représente un radical benzoyle ou un radical de formule R2-O-CO- dans lequel R2 représente un radical alcoyle éventuellement substitué, alcényle, alcynyle, cycloalcoyle, cycloalcényle, bicycloalcoyle, phényle, hétérocyclyle; et R3 représente un radical alcoyle, alcényle, cycloalcoyle, cycloalcényle, bicycloalcoyle, aryle éventuellement substitué (à l'exception de phényle non substitué) ou hétérocyclyle. Les nouveaux produits de formule générale (I) présentent une activité antitumorale remarquable.

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