Pharmaceutically active disubstituted pyridine derivatives
    4.
    发明授权
    Pharmaceutically active disubstituted pyridine derivatives 有权
    药用活性二取代吡啶衍生物

    公开(公告)号:US09242937B2

    公开(公告)日:2016-01-26

    申请号:US14002731

    申请日:2012-03-01

    摘要: The present invention relates to disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted pyridine derivatives as inhibitors for a protein kinase.

    摘要翻译: 本发明涉及二取代的吡啶衍生物和/或其药学上可接受的盐,这些衍生物作为药物活性剂的用途,特别是用于预防和/或治疗感染性疾病,包括机会性疾病,免疫疾病,自身免疫性疾病,心血管疾病 ,细胞增殖性疾病,炎症,勃起功能障碍和中风,以及含有至少一种所述二取代吡啶衍生物和/或其药学上可接受的盐的药物组合物。 此外,本发明涉及所述二取代的吡啶衍生物作为蛋白激酶的抑制剂的用途。

    Pharmaceutically Active Disubstituted Pyridine Derivatives
    5.
    发明申请
    Pharmaceutically Active Disubstituted Pyridine Derivatives 有权
    药学活性二取代吡啶衍生物

    公开(公告)号:US20140296304A1

    公开(公告)日:2014-10-02

    申请号:US14002731

    申请日:2012-03-01

    摘要: The present invention relates to disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted pyridine derivatives as inhibitors for a protein kinase.

    摘要翻译: 本发明涉及二取代的吡啶衍生物和/或其药学上可接受的盐,这些衍生物作为药物活性剂的用途,特别是用于预防和/或治疗感染性疾病,包括机会性疾病,免疫疾病,自身免疫性疾病,心血管疾病 ,细胞增殖性疾病,炎症,勃起功能障碍和中风,以及含有至少一种所述二取代吡啶衍生物和/或其药学上可接受的盐的药物组合物。 此外,本发明涉及所述二取代的吡啶衍生物作为蛋白激酶的抑制剂的用途。

    SUSCEPTIBILITY TO SELECTIVE CDK9 INHIBITORS
    6.
    发明申请
    SUSCEPTIBILITY TO SELECTIVE CDK9 INHIBITORS 审中-公开
    选择性CDK9抑制剂的缺点

    公开(公告)号:US20140287454A1

    公开(公告)日:2014-09-25

    申请号:US14240315

    申请日:2012-08-22

    IPC分类号: G01N33/50

    摘要: The present invention relates to a method of selecting (a) cell(s), (a) tissue(s) or (a) cell culture(s) with susceptibility to a selective CDK9 inhibitor. Also a method for determining the responsiveness of a mammalian tumor cell or cancer cell to treatment with a selective CDK9 inhibitor is described herein. In particular, the present invention provides for an in vitro method for the identification of a responder for or a patient sensitive to a selective CDK9 inhibitor, whereby the patient is suspected to suffer from NUT midline carcinoma (NMC). The present invention also relates to a method of monitoring or predicting the efficacy of a treatment of NUT midline carcinoma (NMC), wherein treatment with a selective CDK9 inhibitor is in particular envisaged. Also the use of a (transgenic) non-human animal or a (transgenic) cell having at least one rearrangement in the NUT gene for screening and/or validation of a medicament for the treatment NUT midline carcinoma (NMC) is described. Furthermore, a kit useful for carrying out the methods described herein as well as an oligo- or polynucleotide capable of detecting rearrangements in the NUT gene are provided.

    摘要翻译: 本发明涉及一种选择(a)对选择性CDK9抑制剂具有易感性的细胞,(a)组织或(a)细胞培养物的方法。 本文还描述了确定哺乳动物肿瘤细胞或癌细胞对用选择性CDK9抑制剂进行治疗的反应性的方法。 特别地,本发明提供了用于鉴定对选择性CDK9抑制剂敏感的患者或患者的体外方法,由此患者怀疑患有NUT中线癌(NMC)。 本发明还涉及监测或预测NUT中线癌(NMC)治疗功效的方法,其中特别设想用选择性CDK9抑制剂进行治疗。 还描述了在NUT基因中具有至少一个重排的(转基因)非人动物或(转基因)细胞用于筛选和/或验证用于治疗NUT中线癌(NMC)的药物的用途。 此外,提供了可用于实施本文所述方法的试剂盒以及能够检测NUT基因重排的寡核苷酸或多核苷酸。