Nitrogenous heterocyclic compounds
    71.
    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
    76.
    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))。

    COMBINATION THERAPY WITH 4-(3-(2H-1,2,3-TRIAZOL-2-YL)PHENYLAMINO)-2-((1R,2S)-2-AMINOCYCLOHEXYLAMINO)PYRIMIDINE-5-CARBOXAMIDE
    77.
    发明申请
    COMBINATION THERAPY WITH 4-(3-(2H-1,2,3-TRIAZOL-2-YL)PHENYLAMINO)-2-((1R,2S)-2-AMINOCYCLOHEXYLAMINO)PYRIMIDINE-5-CARBOXAMIDE 审中-公开
    与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)嘧啶-5-羧酰胺

    公开(公告)号:US20130244963A1

    公开(公告)日:2013-09-19

    申请号:US13823699

    申请日:2011-09-30

    摘要: The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing a SYK inhibitor, or a pharmaceutically acceptable salt thereof, and a antineoplastic or antiinflammatory agent for the treatment of inflammatory, autoimmune and cell proliferative diseases, such as allergic reaction, transplant rejection, rheumatoid arthritis (RA), lupus, multiple sclerosis (MS) or psoriasis 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 (SLL), Lymphoma, multiple myeloma, asthma, vasculitis, Idiopathic thrombocytopenic purpura (ITP), Heparin Induced Thrombocytopenia (HIT) and hemolytic anemia.

    摘要翻译: 本发明涉及药物组合物和使用含有SYK抑制剂或其药学上可接受的盐的组合疗法的药物组合物和方法,以及用于治疗炎性,自身免疫性和细胞增殖性疾病如抗过敏反应,移植物的抗肿瘤剂或抗炎剂 排斥反应,类风湿关节炎(RA),狼疮,多发性硬化症(MS)或牛皮癣不需要的急性骨髓性白血病(AML),慢性淋巴细胞性白血病(CLL),非霍奇金淋巴瘤(NHL)(包括弥漫性大B细胞淋巴瘤(DLBCL) ,淋巴细胞淋巴瘤,淋巴细胞淋巴瘤,多发性骨髓瘤,哮喘,血管炎,特发性血小板减少性紫癜(ITP),肝素诱导的血小板减少症(HIT)和溶血性贫血。

    Salts and crystalline forms of a factor Xa inhibitor
    78.
    发明授权
    Salts and crystalline forms of a factor Xa inhibitor 有权
    因子Xa抑制剂的盐和结晶形式

    公开(公告)号:US08530501B2

    公开(公告)日:2013-09-10

    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。