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    Certain Heterocyclic Substituted Imidazo[1,2-A]Pyrazin-8-Ylamines And Methods Of Inhibition Of Bruton's Tyrosine Kinase By Such Compounds
    4.
    发明申请
    Certain Heterocyclic Substituted Imidazo[1,2-A]Pyrazin-8-Ylamines And Methods Of Inhibition Of Bruton's Tyrosine Kinase By Such Compounds 审中-公开
    某些杂环取代的咪唑并[1,2-A]吡嗪-8-胺和这些化合物抑制布鲁特酪氨酸激酶的方法

    公开(公告)号：US20080182849A1

    公开(公告)日：2008-07-31

    申请号：US12055514

    申请日：2008-03-26

    申请人： Kevin S. CURRIE ,  Robert W. DeSimone ,  Scott A. Mitchell ,  Douglas A. Pippin

    发明人： Kevin S. CURRIE ,  Robert W. DeSimone ,  Scott A. Mitchell ,  Douglas A. Pippin

    IPC分类号： A61K31/4985

    CPC分类号： C07D487/04

    摘要： Compounds of Formula I and all pharmaceutically acceptable forms thereof, are described herein.The variables R1, R2, R3, Z2, and Q, shown in Formula I are defined herein.Pharmaceutical compositions containing one or more compounds of Formula I, or a pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein.Methods of treating patients suffering from certain diseases responsive to inhibition of tyrosine kinase activity are also given. In certain embodiments the diseases are responsive to inhibition of Btk activity and/or B-cell proliferation. Such methods comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These diseases include cancer, an autoimmune and/or inflammatory disease, or an acute inflammatory reaction. Thus methods of treatment include administering a sufficient amount of a compound or salt as provided herein to decrease the symptoms or slow the progression of these diseases.Other embodiments include methods of treating other animals, including livestock aid domesticated companion animals, suffering from a disease responsive to inhibition of kinase activity.Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with one or more other therapeutic agent.A method for determining the presence of Btk in a sample, comprising contacting the sample with a compound or form thereof of Formula I under conditions that permit detection of Btk activity, detecting a level of Btk activity in the sample, and therefrom determining the presence or absence of Btk in the sample.

    摘要翻译： 本文描述了式I化合物及其所有药学上可接受的形式。 式I中所示的R 1，R 2，R 3，R 3，Z 2和Q的变量是 本文定义。 本文提供了含有一种或多种式I化合物或这些化合物的药学上可接受的形式的药物组合物和一种或多种药学上可接受的载体，赋形剂或稀释剂。 还给出了治疗患有某些对抑制酪氨酸激酶活性有响应的疾病的患者的方法。 在某些实施方案中，疾病对Btk活性和/或B细胞增殖的抑制有反应。 这样的方法包括向这样的患者施用一定量的有效降低疾病体征或症状的式I化合物。 这些疾病包括癌症，自身免疫和/或炎性疾病或急性炎症反应。 因此，治疗方法包括施用足够量的本文提供的化合物或盐以减少症状或减缓这些疾病的进展。 其他实施方案包括治疗其它动物的方法，包括家畜帮助驯化的伴侣动物，患有对抑制激酶活性有反应作用的疾病。 治疗方法包括给予式I化合物作为单一活性剂或将一种式I化合物与一种或多种其它治疗剂组合施用。 一种用于确定样品中Btk的存在的方法，包括在允许检测Btk活性，检测样品中Btk活性水平的条件下使样品与式I化合物或其形式接触的方法， 样品中没有Btk。