NOUVEAUX TAXOIDES, LEUR PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT
    3.
    发明公开
    NOUVEAUX TAXOIDES, LEUR PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT 失效
    紫杉醇衍生物,其制备方法和药物组合物

    公开(公告)号:EP0764156A1

    公开(公告)日:1997-03-26

    申请号:EP95922572.0

    申请日:1995-06-07

    摘要: New taxoids having general formula (I), (II), preparation thereof and pharmaceutical compositions containing them. In general formula (I), Ra is hydrogen, hydroxy, alkoxy, acyloxy, alkoxyacetoxy and Rb is hydrogen or Ra and Rb form together with the carbon atom to which they are linked a ketone function; Z is a hydrogen atom or a radical having general formula (II) wherein R1 is an optionally substituted benzoyl radical, thenoyl or furoyl or a radical R2-O-CO- wherein R2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl radical; R3 is an alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, naphtyl or heterocyclic aromatic radical, and R4 and R5, which are the same or different, represent an alkyl, alkenyl, alkynyl, cycoalkyl, cycloalkenyl, bicycloalkyl, aryl, or heterocyclyl radical, R5 not representing a methyl radical. The new products having general formula (I) wherein Z is a radical of general formula (II) have remarkable antitumoral and antileukaemic properties.

    NOUVEAUX TAXOIDES, LEUR PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT
    4.
    发明公开
    NOUVEAUX TAXOIDES, LEUR PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT 失效
    Taxal衍生物,其制备和药物组合物

    公开(公告)号:EP0764154A1

    公开(公告)日:1997-03-26

    申请号:EP95922569.0

    申请日:1995-06-07

    IPC分类号: A61K31 A61P35 C07D305

    CPC分类号: C07D305/14

    摘要: New taxoids having general formula (I), (II) preparation thereof and pharmaceutical compositions containing them. In general formula (I): Ra is hydrogen, hydroxy, alkoxy, acyloxy, alkoxyacetoxy, and Rb is hydrogen or Ra and Rb form together with the carbon atom to which they are linked a ketone function, Z is a hydrogen atom or a radical having general formula (II) wherein R1 is an optionally substituted benzoyl radical, a thenyl or furoyl radical or a radical R2-O-CO- wherein R2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl radical; R3 is an alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, naphtyl or heterocyclic aromatic radical, and R4 and R5, similar or different, represent an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, aryl or heterocyclyl radical, with the condition that R5 does not represent a methyl radical. The new products having general formula (I) wherein Z is a radical having general formula (II) have remarkable antitumoral and antileukaemic properties.