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    FUNCTIONALIZED THIENO-INDOLE DERIVATIVES FOR THE TREATMENT OF CANCER
    29.
    发明公开
    FUNCTIONALIZED THIENO-INDOLE DERIVATIVES FOR THE TREATMENT OF CANCER 有权
    FUNKTIONALISIERTE THIENOINDOLDERIVATE ZUR BEHANDLUNG VON KREBS

    公开(公告)号：EP2836493A1

    公开(公告)日：2015-02-18

    申请号：EP13713180.1

    申请日：2013-03-28

    申请人： Nerviano Medical Sciences S.r.l.

    发明人： BERIA, Italo ,  CARUSO, Michele ,  LUPI, Vittoria ,  ORSINI, Paolo ,  SALSA, Matteo

    IPC分类号： C07D495/04 ,  A61K31/407 ,  A61P35/00

    CPC分类号： A61K47/48338 ,  A61K31/496 ,  A61K45/06 ,  A61K47/65 ,  C07D495/04

    摘要： The invention relates to new functionalized thieno-indole derivatives of formula (I) or (II) which have cytotoxic activity and are useful in treating diseases such as cancer and cellular proliferation disorders. The invention also relates to the use of these functionalized thieno-indole derivatives in the preparation of conjugates. Formula (I) or (II) wherein R1 and R2 taken together form a group (D) or (G): wherein R5 is hydrogen or C1-C4 alkyl; R3 and R4 are independently hydrogen, C1-C4 alkyl or C1-C4 hydroxyalkyl; n is 0, 1 or 2; each of X is independently —O—, —S— or —NR4—; each of Y is independently —CH═ or —N═; R7 and R8 are independently hydrogen, halogen, hydroxy, C1-C4 alkoxy, cyano, —NHCOOR3, —C(NH)NH2 or —NR3R4; A is —O—, —NH— or —CO—; L is null or a conditionally-cleavable moiety; W is null or a self-immolative moiety comprising one or more self-immolative groups; Z is null or a peptidic, non peptidic or hybrid peptidic and non peptidic linker; RM is null or a reactive moiety; R6 is a leaving group; A1 is null or A; L1 is hydrogen or L.

    摘要翻译： 本发明涉及具有细胞毒活性并且可用于治疗疾病如癌症和细胞增殖障碍的式（I）或（II）的新的官能化噻吩并吲哚衍生物。 本发明还涉及这些官能化噻吩并吲哚衍生物在共轭物的制备中的用途。 式（I）或（II）其中R 1和R 2一起形成基团（D）或（G）：其中R 5是氢或C 1 -C 4烷基; R3和R4独立地是氢，C1-C4烷基或C1-C4羟基烷基; n为0,1或2; X各自独立地为-O - ， - S-或-NR 4 - ; Y中的每一个独立地为-CH =或-N =; R 7和R 8独立地是氢，卤素，羟基，C 1 -C 4烷氧基，氰基，-NHCOOR 3，-C（NH）NH 2或-NR 3 R 4; A是-O - ， - NH-或-CO-; L为无效或条件可切割部分; W是无效的或包含一个或多个自褪色基团的自褪色部分; Z是无效或肽，非肽或杂交肽和非肽接头; RM为无效或反应性部分; R6是离职团体; A1为零或A; L1是氢或L.