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210 条记录 (耗时 0.03 秒)

    FUNCTIONALIZED THIENO-INDOLE DERIVATIVES FOR THE TREATMENT OF CANCER
    125.
    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.

    6-AMINO-7-BICYCLO-7-DEAZA-PURINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
    127.
    发明公开
    6-AMINO-7-BICYCLO-7-DEAZA-PURINE DERIVATIVES AS PROTEIN KINASE INHIBITORS 审中-公开
    作为蛋白激酶抑制剂的6-氨基-7-二环-7-哒嗪 - 嘌呤衍生物

    公开(公告)号：EP3218378A1

    公开(公告)日：2017-09-20

    申请号：EP15793834.1

    申请日：2015-11-12

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

    发明人： BUFFA, Laura ,  MENICHINCHERI, Maria ,  MOTTO, Ilaria ,  QUARTIERI, Francesca

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00

    摘要： The present invention relates to 6-amino-7-bicyclo-7-deaza-purine derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular RET family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions containing these compounds.

    摘要翻译： 本发明涉及调节蛋白激酶活性的6-氨基-7-双环-7-脱氮嘌呤衍生物，因此可用于治疗由蛋白激酶活性失调引起的疾病，特别是RET家族激酶。 本发明还提供了制备这些化合物的方法，包含这些化合物的药物组合物以及使用含有这些化合物的药物组合物治疗疾病的方法。