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    Certain imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof
    3.
    发明申请
    Certain imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof 审中-公开
    某些咪唑并[1,2-a]吡嗪-8-基胺，制备方法及其使用方法

    公开(公告)号：US20050288295A1

    公开(公告)日：2005-12-29

    申请号：US10985023

    申请日：2004-11-10

    申请人： Kevin Currie ,  Robert DeSimone ,  Douglas Pippin ,  James Darrow ,  Scott Mitchell

    发明人： Kevin Currie ,  Robert DeSimone ,  Douglas Pippin ,  James Darrow ,  Scott Mitchell

    IPC分类号： A61K31/498 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable pharmaceutically acceptable salts, hydrates, solvates, crystal forms, diastereomers, and prodrugs thereof. Methods of treating or preventing disorders in which aberrant kinase activity is implicated, pharmaceutically compositions, and methods for detecting the presence kinases in cells or biological preparations and for identifying kinases of therapeutic interest.

    摘要翻译： 至少一种选自式1化合物的化学实体及其药学上可接受的药学上可接受的盐，水合物，溶剂化物，晶型，非对映异构体和前药。 治疗或预防涉及异常激酶活性的病症的方法，药物组合物和用于检测细胞或生物制剂中存在的激酶以及鉴定治疗感兴趣的激酶的方法。

    Substituted ring-fused imidazole derivative: GABAA receptors ligands
    6.
    发明授权
    Substituted ring-fused imidazole derivative: GABAA receptors ligands 失效
    取代的环稠合咪唑衍生物：GABA A受体配体

    公开(公告)号：US06916827B2

    公开(公告)日：2005-07-12

    申请号：US10438496

    申请日：2003-05-15

    申请人： George D. Maynard ,  Jun Yuan ,  George P. Luke ,  Kevin Currie

    发明人： George D. Maynard ,  Jun Yuan ,  George P. Luke ,  Kevin Currie

    IPC分类号： A61P25/00 ,  C07D471/04 ,  A61K31/437 ,  A61K31/4184 ,  A61K31/506 ,  C07D403/06

    CPC分类号： C07D471/04

    摘要： Substituted ring-fused imidazole derivatives that bind to GABAA receptors are provided. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).

    摘要翻译： 提供了与GABA A A受体结合的取代的环稠合咪唑衍生物。 这样的化合物可用于在体内或体外调节配体与GABA A A受体的结合，并且特别可用于治疗人类中的各种中枢神经系统（CNS）紊乱，驯养伴侣动物 和牲畜。 本文提供的化合物可以单独施用或与一种或多种其它CNS剂组合施用，以增强其它CNS剂的作用。 还提供了用于治疗这种病症的药物组合物和方法，以及使用这种配体检测GABA A受体的方法（例如，受体定位研究）。

    Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of bruton's tyrosine kinase by such compounds
    7.
    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 有权
    某些杂环取代的咪唑并[1,2-A]吡嗪-8-基胺和这种化合物抑制布鲁特酪氨酸激酶的方法

    公开(公告)号：US20050101604A1

    公开(公告)日：2005-05-12

    申请号：US10883646

    申请日：2004-06-30

    申请人： Kevin Currie ,  Robert DeSimone ,  Scott Mitchell ,  Douglas Pippin

    发明人： Kevin Currie ,  Robert DeSimone ,  Scott Mitchell ,  Douglas Pippin

    IPC分类号： C07D487/04 ,  A61K31/498 ,  C07D487/02

    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 and 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，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。

    Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton's tyrosine kinase by such compounds
    8.
    发明申请
    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特酪氨酸激酶的方法

    公开(公告)号：US20050090499A1

    公开(公告)日：2005-04-28

    申请号：US10861791

    申请日：2004-06-04

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

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

    IPC分类号： A61K31/498 ,  A61P37/02 ,  C07D487/04 ,  C07D519/00

    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。 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 imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof
    9.
    发明申请
    Certain imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof 审中-公开
    某些咪唑并[1,2-a]吡嗪-8-基胺，制备方法及其使用方法

    公开(公告)号：US20060178367A1

    公开(公告)日：2006-08-10

    申请号：US11270837

    申请日：2005-11-10

    申请人： Kevin Currie ,  Jeffrey Kropf ,  James Darrow ,  Robert Desimone

    发明人： Kevin Currie ,  Jeffrey Kropf ,  James Darrow ,  Robert Desimone

    IPC分类号： A61K31/53 ,  A61K31/498 ,  C07D487/04 ,  A61K31/506 ,  A61K31/501

    CPC分类号： C07D487/04

    摘要： Chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, are described herein. Pharmaceutical compositions comprising at least one chemical entity of Formula 1, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell proliferation are described. Methods for determining the presence of Btk in a sample are described.

    摘要翻译： 本文描述了选自式1化合物的化学实体及其可药用盐，溶剂合物，结晶形式，螯合物，非共价复合物，前药及其混合物。 描述了包含至少一种式1的化学实体的药物组合物，以及选自载体佐剂和赋形剂的至少一种药学上可接受的载体。 描述了治疗患有某些对抑制Btk活性和/或B细胞增殖有响应的疾病的方法。 描述了确定样品中Btk的存在的方法。