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    Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
    2.
    发明授权
    Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds 有权
    某些咪唑并[1,2-a]吡嗪-8-基胺和这种化合物抑制布鲁顿酪氨酸激酶的方法

    公开(公告)号：US07405295B2

    公开(公告)日：2008-07-29

    申请号：US10861791

    申请日：2004-06-04

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

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

    IPC: C07D417/00 ,  C07D413/00 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00 ,  C07D497/00

    CPC classification number: C07D487/04

    Abstract: 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.

    Abstract translation: 本文描述式I-a化合物及其所有药学上可接受的形式。 式Ia中所示的变量R 1，R 2，R 3，Z 1，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。

    Aminoalkyl substituted 5,6,7,8-tetrahydro-9H-pyridino [2, 3-B] indole and 5,6,7,8-tetrahydro-9H-pyrimidino [4, 5-B] indole derivatives: CRF1 specific ligands
    7.
    发明授权
    Aminoalkyl substituted 5,6,7,8-tetrahydro-9H-pyridino [2, 3-B] indole and 5,6,7,8-tetrahydro-9H-pyrimidino [4, 5-B] indole derivatives: CRF1 specific ligands 失效
    氨基烷基取代的5,6,7,8-四氢-9H-吡啶并[2,3-B]吲哚和5,6,7,8-四氢-9H-嘧啶并[4,5-B]吲哚衍生物：CRF1特异性配体

    公开(公告)号：US06291473B1

    公开(公告)日：2001-09-18

    申请号：US09283723

    申请日：1999-04-01

    Applicant: Raymond F. Horvath ,  James W. Darrow ,  George D. Maynard

    Inventor： Raymond F. Horvath ,  James W. Darrow ,  George D. Maynard

    IPC: A61K31405

    CPC classification number: C07D471/04 ,  C07D487/04

    Abstract: Disclosed are compounds of the formula: wherein Ar, R1, W, X and m are substituents as defined herein. These compounds are modulators of CRF receptors and are therefore useful for treating affective disorder, anxiety, depression, headache, irritable bowel syndrome, post-traumatic stress disorder, supranuclear palsy, immune suppression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa or other feeding disorder, drug addiction, drug or alcohol withdrawal symptoms, inflammatory diseases, cardiovascular or heart-related diseases, fertility problems, human immunodeficiency virus infections, hemorrhagic stress, obesity, infertility, head and spinal cord traumas, epilepsy, stroke, ulcers, amyotrophic lateral sclerosis, hypoglycemia or a disorder the treatment of which can be effected or facilitated by antagonizing CRF, including but not limited to disorders induced or facilitated by CRF, in mammals, comprising: administering to the mammal a therapeutically effective amount of a compound of Formula I.

    Abstract translation: 公开了下式的化合物：其中Ar，R 1，W，X和m是如本文所定义的取代基。这些化合物是CRF受体的调节剂，因此可用于治疗情感障碍，焦虑症，抑郁症，头痛，肠易激综合征， 创伤性应激障碍，核上性麻痹，免疫抑制，阿尔茨海默病，胃肠道疾病，神经性厌食症或其他进食障碍，药物成瘾，药物或酒精戒断症状，​​炎症性疾病，心血管或心脏相关疾病，生育问题，人类免疫缺陷病毒感染， 出血性压力，肥胖症，不育症，头部和脊髓创伤，癫痫，中风，溃疡，肌萎缩性侧索硬化，低血糖或疾病，其治疗可以通过拮抗CRF来实现或促进，包括但不限于由 CRF，在哺乳动物中，包括：向哺乳动物施用治疗有效量的ac 一级方程式

    Certain substituted imidazo[1,2-a]pyrazines, as modulators of kinase activity
    10.
    发明授权
    Certain substituted imidazo[1,2-a]pyrazines, as modulators of kinase activity 有权
    某些取代的咪唑并[1,2-a]吡嗪，作为激酶活性的调节剂

    公开(公告)号：US07259164B2

    公开(公告)日：2007-08-21

    申请号：US10915696

    申请日：2004-08-11

    Applicant: Scott A. Mitchell ,  Robert W. DeSimone ,  James W. Darrow ,  Douglas A. Pippin ,  M. Diana Danca

    Inventor： Scott A. Mitchell ,  Robert W. DeSimone ,  James W. Darrow ,  Douglas A. Pippin ,  M. Diana Danca

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

    CPC classification number: C07D487/04

    Abstract: Certain substituted imidazo[1,2-a]pyrazines and the pharmaceutically acceptable salts thereof, are provided herein. Pharmaceutical compositions containing one or more compound of Formula I, or a pharmaceutically acceptable salt of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents, are also provided herein. 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 are disclosed.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 agents.A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with a compound of Formula I under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.

    Abstract translation: 本文提供了某些取代的咪唑并[1,2-a]吡嗪及其药学上可接受的盐。 本文还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盐以及一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。 公开了治疗患有某些对EphB4激酶调节作用的疾病和病症的患者的方法，其包括给予这样的患者一定量的有效降低疾病或病症体征或症状的式I化合物。 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联合给药。 一种用于确定样品中血管生成激酶存在或不存在的方法，包括在允许检测血管生成激酶活性，检测血管生成激酶活性水平的条件下将样品与式I化合物接触 确定样品中存在或不存在血管生成激酶。

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