COMPOSITION FOR DOWN-REGULATING PRO-INFLAMMATORY MARKERS
    61.
    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
    62.
    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
    63.
    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。

    Factor Xa inhibitors
    64.
    发明授权
    Factor Xa inhibitors 有权
    因子Xa抑制剂

    公开(公告)号:US07767697B2

    公开(公告)日:2010-08-03

    申请号:US12166944

    申请日:2008-07-02

    IPC分类号: A61K31/4412 C07D401/14

    摘要: The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.

    摘要翻译: 本发明涉及作为因子Xa抑制剂的式(I)化合物及其药学上可接受的盐,酯和前药。 本发明还涉及用于制备这种化合物的中间体,含有这种化合物的药物组合物,预防或治疗许多不希望的血栓形成特征的病症的方法和抑制血液样品凝固的方法。

    COMPOSITIONS AND METHODS FOR INHIBITING TGF-BETA
    65.
    发明申请
    COMPOSITIONS AND METHODS FOR INHIBITING TGF-BETA 失效
    用于抑制TGF-β的组合物和方法

    公开(公告)号:US20080108656A1

    公开(公告)日:2008-05-08

    申请号:US11941284

    申请日:2007-11-16

    IPC分类号: A61K31/47 C07D215/38 A61P9/00

    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R 1,R 6,R 6, 7,R 8,P g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-β活性。

    Nitrogenous heterocyclic compounds
    66.
    发明申请
    Nitrogenous heterocyclic compounds 审中-公开
    含氮杂环化合物

    公开(公告)号:US20060063770A1

    公开(公告)日:2006-03-23

    申请号:US11200456

    申请日:2005-08-08

    IPC分类号: A61K31/517

    摘要: The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

    摘要翻译: 本发明涉及对抑制这种激酶活性的激酶磷酸化具有抑制活性的含氮杂环化合物及其药学上可接受的盐。 本发明还涉及通过抑制激酶的磷酸化来抑制哺乳动物的激酶和治疗疾病状态的方法。 在一个特定方面,本发明提供了抑制PDGF受体的磷酸化以阻止异常细胞生长和细胞游动的含氮杂环化合物及其药学上可接受的盐,以及预防或治疗细胞增殖性疾病如动脉硬化,血管 重建,癌症和肾小球硬化症。

    Anti-obesity potential of Calebin A
    69.
    发明申请
    Anti-obesity potential of Calebin A 有权
    Calebin A的抗肥胖潜力

    公开(公告)号:US20140249219A1

    公开(公告)日:2014-09-04

    申请号:US14274096

    申请日:2014-05-09

    IPC分类号: A61K31/216

    摘要: The present invention discloses the potential of Calebin A in inhibiting adipogenesis and applications thereof in obesity management. The present invention elucidates the potential of Calebin A to favorably modulate biochemical markers associated with obesity. Notable biomodulatory properties of Calebin A include inhibiting leptin production, increasing adiponectin expression and inhibiting local (adipocyte) and systemic inflammation caused by pro-inflammatory cytokines Tumor Necrosis Factor (TNF-α), Interleukin-6 (IL-6) and Interleukin-1 (IL-1β).

    摘要翻译: 本发明公开了Calebin A在肥胖管理中抑制脂肪形成及其应用的潜力。 本发明阐明了Calebin A有利地调节与肥胖相关的生化标志物的潜力。 Calebin A的显着生物学特性包括抑制瘦素生成,增加脂联素表达和抑制局部(脂肪细胞)和由促炎细胞因子肿瘤坏死因子(TNF-α),白细胞介素-6(IL-6)和白介素-1 (IL-1&bgr))。

    OXYPYRIMIDINES AS SYK MODULATORS
    70.
    发明申请
    OXYPYRIMIDINES AS SYK MODULATORS 审中-公开
    氧化亚胺作为SYK调节剂

    公开(公告)号:US20130317029A1

    公开(公告)日:2013-11-28

    申请号:US13882958

    申请日:2011-11-01

    摘要: The present invention is directed to compounds of formula (I) and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which arc inhibitor of Syk 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 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 kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

    摘要翻译: 本发明涉及其抑制Syk激酶的式(I)化合物及其互变异构体或其药学上可接受的盐,酯和前药。 本发明还涉及用于制备这些化合物的中间体,这种化合物的制备,含有这种化合物的药物组合物,抑制Syk激酶活性的方法,抑制血小板聚集的方法,以及预防或治疗数字的方法 至少部分地由Syk激酶活性介导的病症,例如不期望的血栓形成和非霍奇金淋巴瘤。