Inhibitors of protein kinases
    71.
    发明授权
    Inhibitors of protein kinases 有权
    蛋白激酶抑制剂

    公开(公告)号:US08258144B2

    公开(公告)日:2012-09-04

    申请号:US12386848

    申请日:2009-04-22

    IPC分类号: C07D487/00 A61K31/519

    摘要: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

    摘要翻译: 本发明涉及式I-II化合物及其药学上可接受的盐,酯和前体药物,它们是syk和/或JAK激酶的抑制剂。 本发明还涉及用于制备这种化合物的中间体,这种化合物的制备,含有这种化合物的药物组合物,抑制性syk和/或JAK激酶活性的方法,抑制血小板聚集的方法以及预防方法 或治疗至少部分通过syk和/或JAK激酶活性介导的许多病症,例如不期望的血栓形成和非霍奇金淋巴瘤。

    Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof
    73.
    再颁专利
    Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof 失效
    含氮杂环化合物及其制备含氮杂环化合物的方法及其中间体

    公开(公告)号:USRE43098E1

    公开(公告)日:2012-01-10

    申请号:US11866275

    申请日:2007-10-02

    摘要: The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.

    摘要翻译: 本发明提供了含氮杂环化合物及其药学上可接受的盐及其制备方法。 这些化合物对抑制这种激酶活性的激酶的磷酸化具有抑制活性。 本发明还提供了可用于该方法的中间体化合物,以及通过该方法生产的最终产物及其盐或前药。 本发明进一步提供了通过抑制激酶的磷酸化来抑制哺乳动物激酶和治疗疾病状态的方法,包括向有需要的患者施用有效量的本发明化合物。

    Compositions and methods for inhibiting TGF-β
    74.
    发明授权
    Compositions and methods for inhibiting TGF-β 失效
    用于抑制TGF-β的组合物和方法

    公开(公告)号:US07943640B2

    公开(公告)日:2011-05-17

    申请号:US11941284

    申请日:2007-11-16

    IPC分类号: A61K31/04

    CPC分类号: C07D401/12 C07D405/14

    摘要: The present invention provides compounds of the formula: and pharmaceutically acceptable isomers, salts, hydrates, solvates, and prodrug derivatives thereof, wherein R1, R6, R7, R8, Pg, and n are those defined herein. The present invention also provides pharmaceutical compositions comprising the same and methods for using the same. In particular, compounds of Formula I are useful in modulating TGF-β activity.

    摘要翻译: 本发明提供下式的化合物及其药学上可接受的异构体,盐,水合物,溶剂合物和前药衍生物,其中R1,R6,R7,R8,Pg和n是本文定义的那些。 本发明还提供了包含该组合物的药物组合物及其使用方法。 特别地,式I化合物可用于调节TGF- 活动。

    PROTEIN KINASE INHIBITORS
    79.
    发明申请
    PROTEIN KINASE INHIBITORS 有权
    蛋白激酶抑制剂

    公开(公告)号:US20090054425A1

    公开(公告)日:2009-02-26

    申请号:US12192034

    申请日:2008-08-14

    CPC分类号: C07D487/04

    摘要: Compounds, particularly compounds having spleen tyrosine kinase (Syk) inhibition activity, having the following structure: or a pharmaceutically acceptable salt thereof, wherein R1 is structure (a), (b), (c) or (d): and Ra, Rb, Rc, R2, R3, R4, R5, R6 and R7 are as defined herein. Methods associated with preparation and use of the same, as well as pharmaceutical compositions containing the same, are also disclosed, as well as uses of the same to treat a condition or disorder mediated by a Syk and/or JAK kinase.

    摘要翻译: 具有以下结构的化合物,特别是具有脾酪氨酸激酶(Syk)抑制活性的化合物或其药学上可接受的盐,其中R 1是结构(a),(b),(c)或(d):和Ra,Rb ,Rc,R2,R3,R4,R5,R6和R7如本文所定义。 还公开了与其制备和使用相关的方法以及含有该组合物的药物组合物,以及其用于治疗由Syk和/或JAK激酶介导的病症或病症的用途。