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    Factor IXa inhibitors
    1.
    发明授权
    Factor IXa inhibitors 有权

    公开(公告)号：US09708308B2

    公开(公告)日：2017-07-18

    申请号：US14652237

    申请日：2013-12-16

    申请人： Merck Sharp & Dohme Corp. ,  Mochida Pharmaceutical Co., Ltd.

    发明人： Cameron James Smith ,  John Qiang Tan ,  Ting Zhang ,  James Balkovec ,  William John Greenlee ,  Liangqin Guo ,  Yi-Heng Chen ,  Yili Chen ,  Jiayi Xu ,  Samuel Chackalamannil ,  Tomokazu Hirabayashi ,  Hiroshi Nagasue ,  Kouki Ogawa

    IPC分类号： C07D471/04 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D498/04

    CPC分类号： C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

    摘要： The present invention provides a compound of Formula (I) wherein R1 is H or C1-6 alkyl, R2, is H or C1-6 alkyl or CH2OH, R3 is H or C1-6 alkyl, and R4 is H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, then R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl or —CH2OH, and when R2, R3, and R4 are H, then R1 is C1-6 alkyl; A is 1) a 9-10 membered bicyclic heterocycle having 1-3 heteroatoms independently selected from N, S and O, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with R5 and unsubstituted or substituted with R6 and unsubstituted or substituted with NH2, or 2) a 6-9 membered monocyclic or bicyclic carbocyclic ring system unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with —CH2NH2; and B is 1) a 5- or 6-membered monocyclic heterocycle having 1 or 2 heteroatoms independently selected from N, S or O, which is unsubstituted or substituted on a carbon or nitrogen atom with R7, unsubstituted or substituted on a carbon or nitrogen atom with R8, and unsubstituted or substituted on a carbon or nitrogen atom with R9, or 2) an 8- or 9-membered fused bicyclic heterocycle having 1, 2 or 3 nitrogen atoms which is unsubstituted or substituted on a carbon or nitrogen atom with R7, and unsubstituted or substituted on a carbon or nitrogen atom with R8; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses.

    Factor IXa Inhibitors
    4.
    发明申请
    Factor IXa Inhibitors 有权
    因子IXa抑制剂

    公开(公告)号：US20150329562A1

    公开(公告)日：2015-11-19

    申请号：US14652174

    申请日：2013-12-16

    申请人： MERCK SHARP & DOHME CORP.

    发明人： Cameron James Smith ,  John Qiang Tan ,  Ting Zhang ,  James Balkovec ,  William John Greenlee ,  Liangqin Guo ,  Yi-Heng Chen ,  Yili Chen ,  Samuel Chackalamannil ,  Tomokazu Hirabayashi ,  Mika Sekioka

    IPC分类号： C07D513/04 ,  C07D413/14

    CPC分类号： C07D413/14 ,  C07D413/12 ,  C07D513/04

    摘要： The present invention provides a compound of Formula (I) wherein R1, R2, R3 and R4 are independently H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl, and when R2, R3, and R4 are H, R is C1-6 alkyl; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.

    摘要翻译： 本发明提供式（I）的化合物，其中R 1，R 2，R 3和R 4独立地为H或C 1-6烷基，条件是当R 1，R 2和R 3为H时，R 4为C 1-6烷基， 中，R 2和R 4为H，R 3为C 1-6烷基，当R 1，R 3和R 4为H时，R 2为C 1-6烷基，当R 2，R 3和R 4为H时，R为C 1-6烷基 ; 和包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维化改变的方法。