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    MORPHOLINYLBENZOTRIAZINES FOR USE IN CANCER THERAPY
    4.
    发明申请
    MORPHOLINYLBENZOTRIAZINES FOR USE IN CANCER THERAPY 有权
    在癌症治疗中使用的吗啉基苯甲酸

    公开(公告)号：US20140275072A1

    公开(公告)日：2014-09-18

    申请号：US14351773

    申请日：2012-10-30

    Applicant: Merck Patent GmbH

    Inventor： Werner Mederski ,  Thomas Fuchss ,  Ulrich Emde ,  Hans-Peter Buchstaller

    IPC: C07D417/14 ,  C07F7/08 ,  C07F7/10 ,  A61N5/10 ,  C07D401/06 ,  A61K31/5377 ,  C07D401/14 ,  A61K45/06 ,  C07D253/08 ,  C07F7/18

    CPC classification number: C07D417/14 ,  A61K31/5377 ,  A61K45/06 ,  A61N5/10 ,  C07D253/08 ,  C07D401/06 ,  C07D401/14 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04 ,  C07F7/0812 ,  C07F7/10 ,  C07F7/1804

    Abstract: The invention relates to compounds of the formula (I) in which R1, L and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into a salt thereof.

    Abstract translation: 本发明涉及式（I）化合物，其中R 1，L和m具有权利要求中所示的含义，和/或其生理上可接受的盐，互变异构体和立体异构体，包括所有比例的混合物。 式（I）的化合物可用于抑制丝氨酸/苏氨酸蛋白激酶和癌细胞对抗癌剂和/或电离辐射的敏化。 本发明还涉及结合放射治疗和/或抗癌剂的式（I）化合物在癌症，肿瘤，转移或血管生成障碍的预防，治疗或进展控制中的用途。 本发明还涉及通过式（II）和（III）化合物的反应制备式（I）化合物的方法，并且任选地转化式（I）化合物的碱或酸， 加入其盐。

    Morpholinylbenzotriazines for use in cancer therapy
    6.
    发明授权
    Morpholinylbenzotriazines for use in cancer therapy 有权
    用于癌症治疗的吗啉基苯并三嗪

    公开(公告)号：US09187469B2

    公开(公告)日：2015-11-17

    申请号：US14351773

    申请日：2012-10-30

    Applicant: Merck Patent GmbH

    Inventor： Werner Mederski ,  Thomas Fuchss ,  Ulrich Emde ,  Hans-Peter Buchstaller

    IPC: C07D401/06 ,  C07D401/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D253/08 ,  C07F7/18 ,  A61K31/5377 ,  A61K45/06 ,  A61N5/10 ,  C07F7/08 ,  C07F7/10

    CPC classification number: C07D417/14 ,  A61K31/5377 ,  A61K45/06 ,  A61N5/10 ,  C07D253/08 ,  C07D401/06 ,  C07D401/14 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04 ,  C07F7/0812 ,  C07F7/10 ,  C07F7/1804

    Abstract: The invention relates to compounds of the formula (I) in which R1, L and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into a salt thereof.

    Abstract translation: 本发明涉及式（I）化合物，其中R 1，L和m具有权利要求中所示的含义，和/或其生理上可接受的盐，互变异构体和立体异构体，包括所有比例的混合物。 式（I）的化合物可用于抑制丝氨酸/苏氨酸蛋白激酶和癌细胞对抗癌剂和/或电离辐射的敏化。 本发明还涉及结合放射治疗和/或抗癌剂的式（I）化合物在癌症，肿瘤，转移或血管生成障碍的预防，治疗或进展控制中的用途。 本发明还涉及通过式（II）和（III）化合物的反应制备式（I）化合物的方法，并且任选地转化式（I）化合物的碱或酸， 加入其盐。

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