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547 条记录 (耗时 0.062 秒)

    Pyrazole-derivatives as factor Xa inhibitors
    6.
    发明申请
    Pyrazole-derivatives as factor Xa inhibitors 有权
    吡唑衍生物作为因子Xa抑制剂

    公开(公告)号：US20040204406A1

    公开(公告)日：2004-10-14

    申请号：US10744744

    申请日：2003-12-23

    申请人： AVENTIS PHARMA DEUTSCHLAND GMBH

    发明人： Marc Nazare ,  Volkmar Wehner ,  David W. Will ,  Hans Matter

    IPC分类号： A61K031/541 ,  A61K031/5377 ,  A61K031/496 ,  A61K031/454 ,  A61K031/415

    CPC分类号： C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D417/14

    摘要： The present invention is directed to a compound of formula I, 1 in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is a pharmacologically active compound. It exhibits a strong anti-thrombotic effect and is suitable, for example, for the therapy and prophylaxis of a cardio-vascular disorder like a thromboembolic disease or restenosis. It is a reversible inhibitor of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore is directed to a process for the preparation of the compound of formula I, and pharmaceutical preparation comprising it.

    摘要翻译： 本发明涉及式I化合物，其中R 0; R 1; R 2; R 3; R 4; Q; V，G和M具有以下含义。 式I化合物是药理活性化合物。 它表现出强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可以在其中存在因子Xa和/或因子VIIa的不希望的活性或对于 治疗或预防因素Xa和/或因子VIIa的抑制。 本发明还涉及制备式I化合物的方法和包含其的药物制剂。

    Compositions useful as inhibitors of protein kinases
    8.
    发明申请
    Compositions useful as inhibitors of protein kinases 有权
    可用作蛋白激酶抑制剂的组合物

    公开(公告)号：US20040192682A1

    公开(公告)日：2004-09-30

    申请号：US10772219

    申请日：2004-02-04

    发明人： Jeremy Green ,  Ronald Grey ,  Albert C. Pierce

    IPC分类号： A61K031/541 ,  A61K031/5377 ,  A61K031/503 ,  C07D487/02

    CPC分类号： C07D487/04

    摘要： The present invention provides a compound of formula I: 1 or a pharmaceutically acceptable salt or mixtures thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK mammalian protein kinase, and more particularly inhibitors of GSK-3 mammalian protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.

    摘要翻译： 本发明提供式I化合物或其药学上可接受的盐或其混合物。 这些化合物是蛋白激酶的抑制剂，特别是GSK哺乳动物蛋白激酶的抑制剂，特别是GSK-3哺乳动物蛋白激酶的抑制剂。 本发明还提供包含本发明化合物的药学上可接受的组合物和利用这些化合物和组合物治疗各种蛋白激酶介导的病症的方法。

    Crystalline modifications of 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1 lambda 6-thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide
    9.
    发明申请
    Crystalline modifications of 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1 lambda 6-thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide 有权
    2-（3,5-双 - 三氟甲基 - 苯基）-N- [6-（1,1-二氧代-1λ6 - 硫代吗啉-4-基）-4-（4-氟-2-甲基 - 苯基） - 吡啶-3-基] -N-甲基 - 异丁酰胺

    公开(公告)号：US20040186100A1

    公开(公告)日：2004-09-23

    申请号：US10766122

    申请日：2004-01-27

    发明人： Torsten Hoffmann ,  Fabienne Hoffmann-Emery ,  Sonja Nick ,  Urs Schwitter ,  Pius Waldmeier

    IPC分类号： C07D417/14 ,  A61K031/541

    CPC分类号： C07D213/75

    摘要： The present invention relates to a new crystalline modification of 2-(3,5-bis-trifluoromethyl-phenyl)-N-null6-(1,1-dioxo-1null6-thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-ylnull-N-methyl-isobutyramide characterized by the following X-ray diffraction pattern obtained with a CuKnull, radiation at 2null (2Theta)null4.5, 6.4, 7.5, 7.7, 8.0, 8.2, 10.0, 10.2, 10.9, 11.1, 12.9, 13.4, 14.0, 14.5, 15.1, 15.6, 16.2, 16.5, 17.3, 17.5, 18.0, 18.9, 19.3, 19.5, 19.9, 20.1, 20.6, 21.0, 21.4, 22.7, 23.1 and 23.6 and an infrared spectrum having sharp bands at 2925, 2854, 1637, 1604, 1484, 1395, 1375, 1285, 1230, 1172, 1125, 1082, 999, 943, 893, 868, 860, 782, 705, 684 cmnull1, and wherein the extrapolated melting point (DSC) is 137.2null C.

    摘要翻译： 本发明涉及2-（3,5-双 - 三氟甲基 - 苯基）-N- [6-（1,1-二氧代-1λ6 - 硫代吗啉-4-基）-4- （4-氟-2-甲基 - 苯基） - 吡啶-3-基] -N-甲基 - 异丁酰胺，其特征在于用CuKalpha获得的以下X射线衍射图，在2θ（2θ）= 4.5,6.4,7.5 ，7.7,8.0,8.2,10.0,10.2,10.9,11.1,12.9,13.4,14.0,14.5,15.1,15.6,16.2,16.5,17.3,17.5,18.0,18.9,19.3,19.5,19.9,20.1,20.6,21.0 ，21.4,22.7,23.1和23.6，以及在2925,2854,1637,1604,1484,1395,1375,1285,1230,1172,1125,1028,949,943,893,868,860,825,836,865,836,865,865,836,836,836,836,836,836,836,836,836,863,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,836,816， 782,705,684cm -1，其中外推熔点（DSC）为137.2℃

    Novel fused heteroaromatic compounds as transforming growth factor (TGF) inhibitors
    10.
    发明申请
    Novel fused heteroaromatic compounds as transforming growth factor (TGF) inhibitors 失效
    新型融合杂芳族化合物作为转化生长因子（TGF）抑制剂

    公开(公告)号：US20040176390A1

    公开(公告)日：2004-09-09

    申请号：US10783251

    申请日：2004-02-20

    申请人： Pfizer Inc

    发明人： Laura C. Blumberg ,  Michael J. Munchhof ,  Andrei Shavnya

    IPC分类号： A61K031/541 ,  A61K031/496 ,  A61K031/4439

    CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D513/04

    摘要： Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (nullTGFnull)-null signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.

    摘要翻译： 描述了新颖的融合杂芳族化合物，包括其衍生物，其制备中间体，含有它们的药物组合物及其药物用途。 本发明的化合物是转化生长因子（“TGF”）-β信号通路的有效抑制剂。 它们可用于治疗各种TGF-相关疾病状态，包括例如癌症和纤维化疾病。