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    NEW ALKYLATING AGENTS
    4.
    发明公开
    NEW ALKYLATING AGENTS 审中-公开
    NEUE ALKYLIERUNGSMITTEL

    公开(公告)号：EP2836494A1

    公开(公告)日：2015-02-18

    申请号：EP13715931.5

    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 ,  PANZERI, Achille

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

    CPC分类号： A61K31/407 ,  A61K31/496 ,  A61K38/05 ,  A61K38/06 ,  A61K45/06 ,  A61K47/545 ,  C07D495/04 ,  C07K5/06017 ,  C07K5/0804

    摘要： The present invention relates to a novel class of alkylating agents comprising a thieno-indole moiety linked to a DNA-binding moiety, which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds or the pharmaceutical composition containing them. The invention also relates to the use of this novel class of alkylating agents in the preparation of conjugates.

    摘要翻译： 本发明涉及一类新颖的烷化剂，其包含与DNA结合部分连接的噻吩并吲哚部分，其具有细胞毒活性，并且可用于治疗疾病如癌症，细胞增殖病症和病毒感染。 本发明还提供了制备这些化合物的方法，包含它们的药物组合物以及利用这些化合物治疗疾病的方法或含有它们的药物组合物。 本发明还涉及这种新型烷基化剂在制备缀合物中的用途。

    FUNCTIONALIZED THIENO-INDOLE DERIVATIVES FOR THE TREATMENT OF CANCER
    10.
    发明授权
    FUNCTIONALIZED THIENO-INDOLE DERIVATIVES FOR THE TREATMENT OF CANCER 有权

    公开(公告)号：EP2836493B1

    公开(公告)日：2018-06-20

    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： A61K45/06 ,  A61K31/496 ,  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.