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    • 7. 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
    • 8. 发明申请
    • BENZOIMIDAZOLE DERIVATIVES AS SIRTUIN (SIR) MODULATING COMPOUNDS
    • 苯并咪唑衍生物作为SIRTUIN(SIR)调节化合物
    • WO2008073451A8
    • 2008-12-11
    • PCT/US2007025391
    • 2007-12-11
    • SIRTRIS PHARMACEUTICALS INCBEMIS JEANVU CHI BNUNES JOSEPH JARMISTEAD DAVID
    • BEMIS JEANVU CHI BNUNES JOSEPH JARMISTEAD DAVID
    • C07D417/14A61K31/429C07D417/04
    • C07D513/04
    • A. Provided herein are novel sirtuin-modulating compounds of formula (I) and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent ( I ), wherein: one of R1 R2 R3 or R4 is selected from a 5- to 6-membered heteroaryl comprising 1 to 3 heteroatoms 'independently selected from N, O or S, wherein said heteroaryl is optionally benzofused or optionally fused to a second 5- to 6-membered heteroaryl comprising 1 to 3 heteroatoms independently selected from N, O or S and is bound to the rest of the compound via a carbon ring atom, wherein said heteroaryl is optionally substituted on a single carbon ring atom with a substituent selected from a solubilizing group, or a C1-C4 straight or branched alkyl.
    • A.本文提供的是式(I)的新型沉默调节蛋白的调节性化合物及其使用方法。 沉默调节蛋白的调节化合物可用于增加细胞的寿命,以及治疗和/或预防各种各样的疾病和病症,包括例如与老化或紧张相关的疾病或病症,糖尿病,肥胖症,神经变性疾病, 心血管疾病,血液凝固障碍,炎症,癌症和/或潮红以及将受益于增加的线粒体活性的疾病或病症。 还提供了包含与另一种治疗剂(I)组合的沉默调节蛋白的调节性化合物的组合物,其中:R 1 R 2 R 3或R 4中的一个选自包含1至3个独立地选自N ,O或S,其中所述杂芳基任选地被苯并稠合或任选地与包含1至3个独立地选自N,O或S的杂原子的第二个5-至6-元杂芳基稠合,并且经由碳环与化合物的其余部分结合 原子,其中所述杂芳基任选地在单个碳环原子上具有选自增溶基团或C 1 -C 4直链或支链烷基的取代基取代。