Pentacyclic compound

C - Chemistry – Metallurgy – 07 – D

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C07D 493/08 (2006.01) C07D 305/14 (2006.01) C07D 519/00 (2006.01)

Patent

CA 2219675

The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1). (see formula I) [In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group -O-R31, an acyloxy group or a group -O-CO-R31, (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group]

La présente invention concerne des composés représentés par la formule générale (I), ayant un effet antitumoral, et leurs sels. Dans ladite formule générale, R<1> représente phényle, R<2> représente alkyle, alcényle, alkynyle, cycloalkyle ou alcoxy; R<3> représente hydrogène, hydroxy, halogéno, alcoxy, -O-R<31>, alcyloxy ou -O-CO-R<31> (où R<31> représente alkylamino, alcényle, alkynyle, cycloalkyle, aryle ou un hétérocycle); R<4> et R<5> représentent chacun hydrogène, alkyle, alcényle, alkynyle, aryle ou un hétérocyle; Z<1> représente hydrogène, hydroxy, halogéno ou alkyle; Z<2> représente hydrogène, hydroxy, halogéno ou alkyle; et Z<3> représente alkyle, alcényle, alkynyle, cycloalkyle, aryle ou un hétérocycle.

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