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    FACTOR IXA INHIBITORS
    1.
    发明公开
    FACTOR IXA INHIBITORS 审中-公开
    因子IXA抑制剂

    公开(公告)号：EP2934538A1

    公开(公告)日：2015-10-28

    申请号：EP13873301.9

    申请日：2013-12-16

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

    发明人： SMITH, Cameron, James ,  TAN, John, Qiang ,  ZHANG, Ting ,  BALKOVEC, James ,  GREENLEE, William, John ,  GUO, Liangqin ,  XU, Jiayi ,  CHEN, Yi-heng ,  CHEN, Yili ,  CHACKALAMANNIL, Samuel ,  HIRABAYASHI, Tomokazu ,  NAGASUE, Hiroshi ,  OGAWA, Kouki

    IPC分类号： A61K31/5377 ,  C07D413/12

    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.

    摘要翻译： 本发明提供式（I）（结构表示）的化合物，其中R 1为H或C 1-6烷基，R 2为H或C 1-6烷基或CH 2 OH，R 3为H或C 1-6烷基，且R 4为H或 条件是当R 1，R 2和R 3是H时，R 4是C 1-6烷基，并且当R 1，R 2和R 4是H时，则R 3是C 1-6烷基，并且当R 1，R 3和 R 4是H，R 2是C 1-6烷基或-CH 2 OH，并且当R 2，R 3和R 4是H时，则R 1是C 1-6烷基; A为1）具有1-3个独立地选自N，S和O的杂原子的9-10元双环杂环，该9-10元双环杂环为未取代的或被R5取代且未被取代或被R6取代且未被取代或被NH2取代 或2）未被取代或被R 5取代的未被取代或被R 6取代且未被取代或被-CH 2 NH 2取代的6-9元单环或双环碳环系统; 且B为1）具有1或2个独立地选自N，S或O的杂原子的5-或6-元单环杂环，其未被取代或在碳或氮原子上被R7取代，未被取代或在碳或氮上被取代 原子与R8取代，并且未被取代或在碳或氮原子上被R9取代，或2）具有1,2或3个氮原子的8-或9-元稠合双环杂环，其未被取代或在碳或氮原子上被 R7，并且未被取代或在碳或氮原子上被R8取代; 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的方法。