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    CERTAIN IMIDAZO[1,2-A]PYRAZIN-8-YLAMINES AND METHOD OF INHIBITION OF BRUTON'S TYROSINE KINASE BY SUCH COMPOUNDS
    43.
    发明申请
    CERTAIN IMIDAZO[1,2-A]PYRAZIN-8-YLAMINES AND METHOD OF INHIBITION OF BRUTON'S TYROSINE KINASE BY SUCH COMPOUNDS 审中-公开
    某些咪唑并[1,2-A]吡嗪-8-胺和这种化合物抑制BRUTON的酪氨酸激酶的方法

    公开(公告)号：US20110177011A1

    公开(公告)日：2011-07-21

    申请号：US12018573

    申请日：2008-01-23

    申请人： Kevin S. Currie ,  Robert W. DeSimone ,  Scott A. Mitchell ,  Douglas A. Pippin ,  James W. Darrow ,  Xiaobing Qian ,  Mark Velleca ,  Dapeng Qian

    发明人： Kevin S. Currie ,  Robert W. DeSimone ,  Scott A. Mitchell ,  Douglas A. Pippin ,  James W. Darrow ,  Xiaobing Qian ,  Mark Velleca ,  Dapeng Qian

    IPC分类号： A61K31/551 ,  A61K31/4985 ,  A61K31/5355 ,  A61K9/12 ,  A61P29/00 ,  A61P35/00

    CPC分类号： C07D487/04

    摘要： Compounds of Formula I-a and all pharmaceutically-acceptable forms thereof, are described herein.The variables R1, R2, R3, Z1, Q, and A shown in Formula I-a are defined herein.Pharmaceutical compositions containing one or more compounds of Formula I-a, 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-a 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 and domesticated companion animals, suffering from a disease responsive to inhibition of kinase activity.Methods of treatment include administering a compound of Formula I-a as a single active agent or administering a compound of Formula I-a 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-a 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： 本文描述式I-a化合物及其所有药学上可接受的形式。 式I-a中所示的变量R1，R2，R3，Z1，Q和A在本文中定义。 本文提供了含有一种或多种式I-a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减少疾病体征或症状的式I-a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，包括患有对抑制激酶活性有响应的疾病的家畜和驯养的伴侣动物的方法。 治疗方法包括施用式I-a化合物作为单一活性剂或给予式I-a的化合物与一种或多种其它治疗剂的组合。 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Ia化合物或其形式接触的方法， 样品中没有Btk。

    Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of kinase activity
    46.
    发明授权
    Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of kinase activity 有权

    公开(公告)号：US07189723B2

    公开(公告)日：2007-03-13

    申请号：US10776002

    申请日：2004-02-10

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

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

    IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  C07D47/00

    CPC分类号： C07D487/04

    摘要： This invention pertains to compounds of Formula I: and all pharmaceutically-acceptable forms thereof. The variables R1, R2, R3, Z1, Z2, W, and X shown in Formula I are defined herein.The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents.The invention further comprises methods of treating patients suffering from certain diseases and disorders responsive to EphB4 kinase modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These diseases include cancer, including of breast neoplasma, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Thus methods of treatment include administering a sufficient amount of a compound or salt of the invention to decrease the symptoms or slow the progression of these diseases or disorders.The invention also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an disease or disorder responsive to EphB4 modulation.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.The invention also includes a method for determining the presence of EphB4 kinase in a sample, comprising contacting the sample with a compound of Formula I, or form thereof, and the detecting the amount of compound or form bound to EphB4 kinase, and therefrom determining the presence or absence of EphB4 kinase in the sample.

    Certain 6, 8-(heteroaryl or aryl) disubstituted imidazo[1,2-a]pyrazines as modulators of Hsp90 complex activity
    47.
    发明授权
    Certain 6, 8-(heteroaryl or aryl) disubstituted imidazo[1,2-a]pyrazines as modulators of Hsp90 complex activity 有权

    公开(公告)号：US07160885B2

    公开(公告)日：2007-01-09

    申请号：US10776631

    申请日：2004-02-10

    申请人： Kevin S. Currie ,  Robert W. DeSimone ,  Douglas A. Pippin ,  James W. Darrow ,  Scott A. Mitchell

    发明人： Kevin S. Currie ,  Robert W. DeSimone ,  Douglas A. Pippin ,  James W. Darrow ,  Scott A. Mitchell

    IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  C07D471/00

    CPC分类号： C07D487/04

    摘要： This invention pertains to compounds of Formula I: and the pharmaceutically-acceptable forms thereof. The variables R1, R2, R3, Z1, Z2, W, and X shown in Formula I are defined herein.The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents.The invention further comprises methods of treating patients suffering from certain diseases and disorders responsive to Hsp90 complex modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These diseases include cancer, including chronic myeloid leukemia, melanoma, breast, ovarian, brain, thyroid, colorectal, prostate, and bladder cancer, heart disease, stroke, autoimmune/inflammatory diseases, and neurodegenerative diseases. Thus methods of treatment include administering a sufficient amount of a compound of Formula I or form thereof to decrease the symptoms or slow the progression of these diseases or disorders.The invention also encompasses methods of treating non-human patients, including livestock and domesticated companion animals, suffering from a disease or disorder responsive to Hsp90 complex modulation.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.The invention also includes a method for determining the presence of certain kinases or Hsp90 complex in a sample, comprising contacting the sample with a compound of Formula I or form thereof, and detecting Hsp9O complex activity in the sample.