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    • 4. 发明申请
    • 6-ARYL-IMIDAZ0[L, 2-A] PYRAZINE DERIVATIVES, METHOD OF MAKING, AND METHOD OF USE THEREOF
    • 6-ARYL-IMIDAZO [L,2-A]吡嗪衍生物,制备方法及其使用方法
    • WO2009102468A1
    • 2009-08-20
    • PCT/US2009/000919
    • 2009-02-12
    • CGI PHARMACEUTICALS, INC.MITCHELL, Scott A.CURRIE, Kevin S.BLOMGREN, Peter A.ARMISTEAD, David M.RAKER, Joseph
    • MITCHELL, Scott A.CURRIE, Kevin S.BLOMGREN, Peter A.ARMISTEAD, David M.RAKER, Joseph
    • C07D487/04A61K31/4985A61P37/00
    • C07D487/04
    • Certain chemical entities chosen from compounds represented by Formula I and pharmaceutically acceptable salts and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer (e.g., B -cell lymphoma and leukemia), autoimmune diseases, inflammatory diseases, acute inflammatory reactions, and allergic disorders. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for determining the presence or absence of Syk kinase in a sample. Formula I
    • 在本文中提供了选自由式I表示的化合物的某些化学实体及其药学上可接受的盐及其混合物。 包含至少一种化学实体和一种或多种药学上可接受的载体的药物组合物。 公开了治疗患有对抑制Syk活性有反应的某些疾病和病症的患者的方法,所述方法包括向所述患者施用一定量的至少一种有效减少疾病或病症体征或症状的化学实​​体。 这些疾病包括癌症(例如,B细胞淋巴瘤和白血病),自身免疫疾病,炎性疾病,急性炎症反应和过敏性疾病。 治疗方法包括给予至少一种化学实体作为单一活性剂或与一种或多种其它治疗剂组合施用至少一种化学实体。 还提供了用于确定样品中Syk激酶的存在或不存在的方法。 一级方程式
    • 10. 发明申请
    • SUBSTITUTED IMIDAZO[1,2-A]PYRAZINES AS MODULATORS OF KINASE ACTIVITY
    • 取代的咪唑并[1,2-a]吡嗪类化合物作为激酶活性的调节剂
    • WO2005019220A9
    • 2005-06-02
    • PCT/US2004025884
    • 2004-08-11
    • CELLULAR GENOMICS INCMITCHELL SCOTT ADESIMONE ROBERT WDARROW JAMES WPIPPIN DOUGLAS ADANCA M DIANA
    • MITCHELL SCOTT ADESIMONE ROBERT WDARROW JAMES WPIPPIN DOUGLAS ADANCA M DIANA
    • A61K31/498A61P35/00C07D487/04A61K31/4985
    • C07D487/04
    • 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. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Thus methods of treatment include administering a sufficient amount of a compound of the invention to decrease the symptoms or slow the progression of these diseases or disorders. 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.
    • 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。 公开了治疗患有对EphB4激酶调节有响应的某些疾病和病症的患者的方法,其包括向所述患者施用有效减少疾病或病症的体征或症状的量的式I化合物。 这些疾病包括癌症,包括乳腺瘤,子宫内膜癌,结肠癌和颈部鳞状细胞癌。 因此治疗方法包括给予足够量的本发明化合物以减轻这些疾病或病症的症状或减缓其进展。 治疗方法包括施用式I化合物作为单一活性剂或将式I化合物与一种或多种其他治疗剂组合施用。 用于确定样品中血管生成激酶的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使样品与式I化合物接触,并由此 确定样品中血管生成激酶的存在或不存在。