DERIVES DE 4,9-ETHANO-BANZO(f)ISOINDOLE COMME INHIBITEURS DE FARNESYL TRANSFERASE
    2.
    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

    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.