Novel taxoids, preparation thereof and pharmaceutical...

C - Chemistry – Metallurgy – 07 – D

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C07D 305/14 (2006.01) A61K 31/33 (2006.01) C07D 405/00 (2006.01) C07D 407/12 (2006.01) C07D 407/14 (2006.01) C07D 409/00 (2006.01) C07D 417/00 (2006.01)

Patent

CA 2214321

Novel taxoids of general formula (I), the preparation thereof and pharmaceutical compositions containing them are described, wherein Z is a hydrogen atom or a radical of general formula (II), wherein R1 is an optionally substituted benzoyl radical or a radical R2-O-CO- where R2 is an optionally substituted phenyl, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, or heterocyclyl radical, R3 is an aromatic heterocyclic, alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or naphthyl radical, R4 is a substituted alkanoyloxy, alkenoyloxy, alkynoyloxy or cycloalkanoyloxy radical and R5 is an optionally substituted alkoxy radical or a cycloalkyloxy or cycloalkenyloxy radical. The novel products of general formula (I), where Z is a radical of general formula (II), have remarkable anti-tumour and anti-leukemia properties.

Nouveaux taxoïdes de formule générale (I), (voir formule I) leur préparation et les compositions pharmaceutiques qui les contiennent. Dans la formule générale (I), Z représente un atome d'hydrogène ou un radical de formule générale (II), (voir formule II) dans laquelle R, représente un radical benzoyle éventuellement substitué ou un radical R2-O-CO- dans lequel R2 représente un radical alcoyle, alcényle, alcynyle, cycloalcoyle, cycloalcényle, bicycloalcoyle, phényle, éventuellement substitué ou hétérocyclyle, R3 représente un radical alcoyle, alcényle, alcynyle, cycloalcoyle, phényle, naphtyle ou hétérocyclique aromatique, R4 représente un radical alcanoyloxy substitué, alcénoyloxy, alcynoyloxy ou cycloalcanoyloxy, et R5 représente un radical alcoxy éventuellement substitué ou un radical cycloalcoyloxy ou cycloalcényloxy. Les nouveaux produits de formule générale (I), dans laquelle Z représente un radical de formule générale (II), présentent des propriétés antitumorales et antileucémiques remarquables.

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