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    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
    TEXOL衍生物，其制备和药物组合物

    公开(公告)号：EP0788492A1

    公开(公告)日：1997-08-13

    申请号：EP95935998.0

    申请日：1995-10-23

    申请人： RHONE-POULENC RORER S.A.

    发明人： BOUCHARD, Hervé ,  BOURZAT, Jean-Dominique ,  COMMER ON, Alain ,  TERRIER, Corinne ,  ZUCCO, Martine

    IPC分类号： A61K31 ,  A61P35 ,  C07D305

    CPC分类号： C07D305/14

    摘要： Novel taxoids of general formulas (I) and (II), preparation thereof, and pharmaceutical compositions containing same. In general formula (I), Ra is hydrogen, hydroxy, alkoxy, acyloxy or alkoxyacetoxy and Rb is hydrogen, or Ra and Rb, taken together with the carbon atom to which they are attached, form a ketone function; Z is a hydrogen atom or a radical of general formula (II), wherein R1 is an optionally substituted benzoyl, thenoyl or furoyl 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; R4 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, aryl or heterocyclyl radical; and R5 is an optionally substituted cycloalkenyl, alkyl, alkenyl, alkynyl or cycloalkyl radical. The novel products of general formula (I), wherein Z is a radical of general formula (II), have remarkable antitumoral and antineoplastic properties.

    DERIVES DE 4,9-ETHANO-BANZO(f)ISOINDOLE COMME INHIBITEURS DE FARNESYL TRANSFERASE
    4.
    发明公开
    DERIVES DE 4,9-ETHANO-BANZO(f)ISOINDOLE COMME INHIBITEURS DE FARNESYL TRANSFERASE 失效
    4,9-乙烯基（F）葡萄糖醛酸转运酶抑制剂

    公开(公告)号：EP0839133A1

    公开(公告)日：1998-05-06

    申请号：EP96924952.0

    申请日：1996-07-08

    申请人： RHONE-POULENC RORER S.A.

    发明人： COMMERCON, Alain ,  LEBRUN, Alain ,  MAILLIET, Patrick ,  PEYRONEL, Jean-François ,  SOUNIGO, Fabienne ,  TRUCHON, Alain ,  ZUCCO, Martine

    IPC分类号： C07D409 ,  A61K31 ,  A61P35 ,  A61P43 ,  C07D209 ,  C07D277 ,  C07D417 ,  C07F9

    CPC分类号： C07D209/72 ,  C07F9/5728

    摘要： Novel products of general formula (I), preparation thereof and pharmaceutical compositions containing said products are disclosed. In general formula (I), R is a radical of general formula -(CH2)m-X1-(CH2)n-Z, where X1 is a simple bond or O or S, n is 0 or 1 and n is 0, 1 or 2, the CH2 radicals being optionally substituted by carboxy, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, amino, alkylamino or dialkylamino, and Z is carboxy, COOR4, where R4 is alkyl, or CON(R5)(R6), where R5 is hydrogen or alkyl and R6 is hydrogen or optionally substituted alkyl, or else R5 is hydrogen or alkyl and R6 is hydroxy, optionally substituted alkyloxy or amino, or PO(OR7)2, where R7 is hydrogen or alkyl; or a radical -NH-CO-T where T is hydrogen or optionally substituted alkyl; or else a radical (a); R1 and R2 are hydrogen or halogen or optionally substituted alkyloxy or alkyl, or else R1 and R2 in ortho positions form a heterocyclic ring containing 1 or 2 optionally substituted heteroatoms, or R1 is hydrogen or halogen or optionally substituted alkyloxy or alkyl, and R2 is thioalkyl; R3 is hydrogen or halogen or alkyl, alkenyl, alkyloxy, alkylthio, carboxy or alkyloxycarbonyl; X is O or S or -NH-, -CO-, methylene, ethylene, alkylidene or 1,1-cycloalkyl; and Y is O or S. The novel products of general formula (I) are farnesyl transferase inhibitors having remarkable antitumoral and antineoplastic properties.

    NOUVEAUX TAXOIDES, LEUR PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT
    5.
    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

    申请人： RHONE-POULENC RORER S.A.

    发明人： BOUCHARD, Hervé ,  BOURZAT, Jean-Dominique ,  COMMER ON, Alain ,  TERRIER, Corinne ,  ZUCCO, Martine

    IPC分类号： A61K31 ,  A61P35 ,  C07D305 ,  C07D407 ,  C07D409 ,  C07D417

    CPC分类号： C07D407/12 ,  C07D305/14 ,  C07D409/12 ,  C07D417/12

    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
    6.
    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

    申请人： RHONE-POULENC RORER S.A.

    发明人： BOUCHARD, Hervé ,  BOURZAT, Jean-Dominique ,  COMMERCON, Alain ,  TERRIER, Corinne ,  ZUCCO, Martine

    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.