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    BIARYLMETHYL INDOLINES, INDOLES AND TETRAHYDROQUINOLINES, USEFUL AS SERINE PROTEASE INHIBITORS
    8.
    发明公开
    BIARYLMETHYL INDOLINES, INDOLES AND TETRAHYDROQUINOLINES, USEFUL AS SERINE PROTEASE INHIBITORS 审中-公开
    二芳基甲基吲哚啉，吲哚和四氢喹啉，可用作丝氨酸蛋白酶抑制剂

    公开(公告)号：EP1633716A2

    公开(公告)日：2006-03-15

    申请号：EP04750251.3

    申请日：2004-04-15

    申请人： Bristol-Myers Squibb Company

    发明人： SMALLHEER, Joanne, M. ,  QUAN, Mimi, L. ,  WANG, Shuaige ,  BISACCHI, Gregory, S.

    IPC分类号： C07D215/00

    CPC分类号： C07D209/08 ,  C07D209/22

    摘要： The present invention provides compounds of Formula (I) or a stereoisomer or pharmaceutically acceptable salt or hydrate form thereof, wherein the variables A, B, L1, L2, X1, X2, X3, X4 and W are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

    摘要翻译： 本发明提供式（I）的化合物或其立体异构体或药学上可接受的盐或水合物形式，其中变量A，B，L1，L2，X1，X2，X3，X4和W如本文所定义。 式（I）化合物可用作凝血级联和/或接触活化系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。 具体而言，它涉及选择性因子XIa抑制剂的化合物。 本发明还涉及包含这些化合物的药物组合物以及使用该组合物治疗血栓栓塞性和/或炎症性疾病的方法。

    1, 4, 5, 6-TETRAHYDROPYRAZOLO- 3, 4-C]-PYRID IN-7-ONES AS FACTOR XA INHIBITORS
    9.
    发明公开
    1, 4, 5, 6-TETRAHYDROPYRAZOLO- 3, 4-C]-PYRID IN-7-ONES AS FACTOR XA INHIBITORS 审中-公开
    作为因子XA抑制剂的1,4,5,6-四氢吡唑-3,4-C] - 吡啶-7-酮

    公开(公告)号：EP1379245A1

    公开(公告)日：2004-01-14

    申请号：EP02723904.5

    申请日：2002-04-17

    申请人： BRISTOL-MYERS SQUIBB COMPANY

    发明人： PINTO, Donald, J. ,  GALEMMO, Robert, J. ,  ORWAT, Michael, J. ,  QUAN, Mimi, L.

    IPC分类号： A61K31/44 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： The present application describes 1, 4, 5, 6-tetrahydropyrazolo-[3, 4-c]-pyridin-7-ones of the following formula or pharmaceutically acceptable salt forms thereof: wherein ring Rb is 3-amido or 4-methoxy, Ra can be cyano, trifluoromethyl, or amido, and R can be a substituted phenyl, a substituted imidazolyl, or a substituted pyridine. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

    摘要翻译： 本申请描述了下式的1,4,5,6-四氢吡唑并[3,4-c]吡啶-7-酮或其药学上可接受的盐形式：其中环Rb为3-酰氨基或4-甲氧基， Ra可以是氰基，三氟甲基或酰氨基，并且R可以是取代的苯基，取代的咪唑基或取代的吡啶。 本发明化合物可用作胰蛋白酶样丝氨酸蛋白酶，特别是Xa因子的抑制剂。