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 409/12 (2006.01) C07D 417/00 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2214320

Novel taxoids of general formula (I), the preparation thereof, and pharmaceutical compositions containing same, are disclosed. In general formula (I), 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 alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl radical; R3 is an aromatic heterocyclic, alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or naphthyl radical; and R4 is an optionally substituted alkoxy, alkenyloxy, alkynyloxy, cycloalkyloxy or cycloalkenyloxy radical. The novel compounds of general formula (I), wherein Z is a radical of general formula (II), have remarkable antitumoral and antineoplastic 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 R1 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, napthyle ou hétérocyclique aromatique, R4 représente un radical alcoxy, alcényloxy, alcynyloxy, cycloalcoyloxy ou cycloalcényloxy éventuellement substitué. 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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