Protein kinase inhibitors
    61.
    发明授权
    Protein kinase inhibitors 有权
    蛋白激酶抑制剂

    公开(公告)号:US07705004B2

    公开(公告)日:2010-04-27

    申请号:US12192034

    申请日:2008-08-14

    IPC分类号: C07D487/04 A61K31/519

    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。

    COMBINATION THERAPY OF 4-(3-(2H-1,2,3-TRIAZO-2-YL)PHENYLAMINO)-2-((1R,2S)-2-AMINOCYCLOHEXYLAMINO)PYRIMIDINE-5-CARBOXAMIDE AND FLUDARABINE
    66.
    发明申请
    COMBINATION THERAPY OF 4-(3-(2H-1,2,3-TRIAZO-2-YL)PHENYLAMINO)-2-((1R,2S)-2-AMINOCYCLOHEXYLAMINO)PYRIMIDINE-5-CARBOXAMIDE AND FLUDARABINE 审中-公开
    4-(3-(2H-1,2,3-三唑-2-基)苯基氨基)-2 - ((1R,2S)-2-氨基甲酰氧基]氨基] -5-羧酰胺和氟尿嘧啶的组合治疗

    公开(公告)号:US20130252917A1

    公开(公告)日:2013-09-26

    申请号:US13823710

    申请日:2011-09-30

    IPC分类号: A61K31/7076 A61K31/506

    摘要: The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing 4-(3-(2H-1,2,3-triazol-2-yl)phenylamino)-2-(1R,2S)-2-aminocyclohexylamino)pyrimidine-5-carboxamide, or a pharmaceutically acceptable salt thereof, and fludarabine for the treatment of cell proliferative disorders, such as undesired acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL), non-Hodgkin lymphoma (NHL), including diffuse large B cell lymphoma (DLBCL); mantle cell lymphoma, acute lymphocytic leukemia (ALL), follicular lymphoma, Burkitt's lymphoma, small Lymphocytic Lymphoma (SLL) and multiple myeloma.

    摘要翻译: 本发明涉及药物组合物和使用含有4-(3-(2H-1,2,3-三唑-2-基)苯基氨基)-2-(1R,2S)-2-氨基环己基氨基) 嘧啶-5-甲酰胺或其药学上可接受的盐,和氟达拉滨用于治疗细胞增殖性疾病,例如不期望的急性骨髓性白血病(AML),慢性淋巴细胞白血病(CLL),非霍奇金淋巴瘤(NHL),包括弥漫性 大B细胞淋巴瘤(DLBCL); 套细胞淋巴瘤,急性淋巴细胞白血病(ALL),滤泡淋巴瘤,伯基特淋巴瘤,小淋巴细胞淋巴瘤(SLL)和多发性骨髓瘤。

    METHODS OF SYNTHESIZING FACTOR Xa INHIBITORS
    67.
    发明申请
    METHODS OF SYNTHESIZING FACTOR Xa INHIBITORS 有权
    合成因子Xa抑制剂的方法

    公开(公告)号:US20110319627A1

    公开(公告)日:2011-12-29

    申请号:US12969371

    申请日:2010-12-15

    IPC分类号: C07D213/75

    CPC分类号: C07D213/75

    摘要: Described herein are novel methods of preparing a compound of Formula II or a pharmaceutically acceptable salt thereof. In some embodiments, the method is for preparing betrixaban or a pharmaceutically acceptable salt thereof. Also described are compositions comprising substantially pure betrixaban free base or salt thereof.

    摘要翻译: 本文描述了制备式II化合物或其药学上可接受的盐的新方法。 在一些实施方案中,该方法用于制备betrixaban或其药学上可接受的盐。 还描述了包含基本上纯的双倍他卡巴游离碱或其盐的组合物。

    COMPOSITION FOR DOWN-REGULATING PRO-INFLAMMATORY MARKERS
    68.
    发明申请
    COMPOSITION FOR DOWN-REGULATING PRO-INFLAMMATORY MARKERS 审中-公开
    用于下调调控标记的组合物

    公开(公告)号:US20110218172A1

    公开(公告)日:2011-09-08

    申请号:US12768871

    申请日:2010-04-28

    IPC分类号: A61K31/715 A61P29/00

    CPC分类号: A61K31/715

    摘要: The present invention provides a composition for down-regulating pro-inflammatory markers. The composition comprises boswellic acid fraction and polysaccharide faction obtained from Boswellia species at specific concentrations showing enhancement in their activity as compared to boswellic acid fraction and the polysaccharide fraction alone. The invention further comprises use of polysaccharide fraction individually or in combination with boswellic acid fraction for inhibition of PGE2.

    摘要翻译: 本发明提供用于下调促炎症标记物的组合物。 组合物包含从乳香属物种获得的特异性浓度的乳香酸级分和多糖类,其显示出与乳香酸级分和单独的多糖级分相比其活性增强。 本发明还包括单独使用多糖级分或与乳香酸级分组合用于抑制PGE2。

    SALTS AND CRYSTALLINE FORMS OF A FACTOR XA INHIBITOR
    69.
    发明申请
    SALTS AND CRYSTALLINE FORMS OF A FACTOR XA INHIBITOR 有权
    因子XA抑制剂的盐和晶体形式

    公开(公告)号:US20110178135A1

    公开(公告)日:2011-07-21

    申请号:US12970785

    申请日:2010-12-16

    CPC分类号: C07D409/14

    摘要: The present invention provides salts and crystalline forms of the compound 5-chloro-N-((1-(4-(2-oxopyridin-1(2H)-yl)phenyl)-1H-imidazol-4-yl)methyl)thiophene-2-carboxamide, and pharmaceutical compositions and method of use thereof.

    摘要翻译: 本发明提供化合物5-氯-N - ((1-(4-(2-氧代吡啶-1(2H) - 基)苯基)-1H-咪唑-4-基)甲基)噻吩的盐和结晶形式 -2-甲酰胺,以及药物组合物及其使用方法。

    METHODS OF PREPARING FACTOR XA INHIBITORS AND SALTS THEREOF
    70.
    发明申请
    METHODS OF PREPARING FACTOR XA INHIBITORS AND SALTS THEREOF 有权
    制备因子XA抑制剂及其制备方法

    公开(公告)号:US20110152530A1

    公开(公告)日:2011-06-23

    申请号:US12970531

    申请日:2010-12-16

    IPC分类号: C07D401/14

    CPC分类号: C07D409/14

    摘要: The present invention provides for methods of preparing compounds of Formula I or a salt of the compound or a hydrate of the compound or salt thereof that are factor Xa inhibitors. Specifically the present invention provides a method of preparing the compound 5-chloro-N-((1-(4-(2-oxopyridin-1(2H)-yl)phenyl)-1H-imidazol-4-yl)methyl)thiophene-2-carboxamide, or a salt of the compound or a hydrate of the compound or salt thereof.

    摘要翻译: 本发明提供制备式I化合物的方法或其化合物的盐或其化合物或其盐的水合物,其为因子Xa抑制剂。 具体地说,本发明提供一种制备化合物5-氯-N - ((1-(4-(2-氧代吡啶-1(2H) - 基)苯基)-1H-咪唑-4-基)甲基)噻吩 -2-甲酰胺,或化合物的盐或化合物或其盐的水合物。