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    • 86. 发明申请
    • TAXOIDS, PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
    • 紫杉醇,其制备方法及含有其的药物组合物
    • WO1997032869A1
    • 1997-09-12
    • PCT/FR1997000386
    • 1997-03-05
    • RHONE-POULENC RORER S.A.BOUCHARD, HervéBOURZAT, Jean-DominiqueCOMMERCON, Alain
    • RHONE-POULENC RORER S.A.
    • C07D305/14
    • C07D305/14Y02P20/55
    • 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 alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, naphthyl or aromatic heterocyclic radical; R4 is a hydroxy radical or an alkoxy, alkenyloxy, optionally substituted alkynyloxy, alkanoyloxy, alkenoyloxy, alkynyloxy, alkoxyacetyl or alkyloxycarbonyloxy radical, or a cycloalkyloxy, cycloalkenyloxy, arylcarbonyloxy or heterocyclylcarbonyloxy radical; and R5 is an optionally substituted alkoxy radical or a 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.
    • 公开了通式(I)的新型紫杉烷类,其制备方法和含有其的药物组合物。 在通式(I)中,Z是氢原子或通式(II)的基团,其中R 1是任选取代的苯甲酰基或基团R 2 -O-CO-,其中R 2是烷基,烯基,炔基, 环烷基,环烯基,双环烷基,任选取代的苯基或杂环基; R3是烷基,烯基,炔基,环烷基,苯基,萘基或芳族杂环基; R4是羟基或烷氧基,烯氧基,任选取代的炔氧基,烷酰氧基,烯酰氧基,炔氧基,烷氧基乙酰基或烷氧基羰基氧基,或环烷氧基,环烯基氧基,芳基羰基氧基或杂环基羰基氧基; 并且R 5是任选取代的烷氧基或环烷氧基或环烯氧基。 通式(I)的新化合物,其中Z为通式(II)的基团,具有显着的抗肿瘤和抗肿瘤性质。