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    Thrombin Inhibitors
    32.
    发明申请
    Thrombin Inhibitors 有权
    凝血酶抑制剂

    公开(公告)号：US20150315141A1

    公开(公告)日：2015-11-05

    申请号：US14443470

    申请日：2013-11-15

    Applicant: Harry CHOBANIAN ,  Tesfaye BIFTU ,  Barbara PIO ,  Zhicai WU ,  MERCK SHARP & DOHME CORP.

    Inventor： Harry Chobanian ,  Tesfaye Biftu ,  Barbara Pio ,  Zhicai Wu

    IPC: C07D207/16 ,  C07D401/14 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D207/34 ,  C07D401/06

    CPC classification number: C07D207/16 ,  C07D207/34 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D417/06

    Abstract: Compounds of the invention, which may be useful in inhibiting thrombin and associated thrombotic occlusions, have the following structure: or a pharmaceutically acceptable salt thereof, wherein m is 0 or 1; R is a heterocycle, —(CR8R9)1-2NH2, or —(CR8R9)1-2OH, wherein R8 and R9, each time in which they occur, are independently H, C1-6 alkyl, —CH2F, —CHF2, CF3 or —CH2OH; W is a) —CHR1R2, where R1 is —C(CH3)3, and R2 is —(CH2)1-2OH, b) a 5- or 6-membered unsubstituted or substituted heterocycle having 1 or 2 heteroatoms selected from N and O, wherein substituted heterocycle is substituted with R3, c) a 9- or 10-membered unsubstituted or substituted heterocycle having 1 or 2 heteroatoms selected from N, O and S, wherein substituted heterocycle is mono-substituted with R3, or disubstituted with R3 and R4, or d) a 3-, 4-, or 5-membered carbocyclic ring which is unsubstituted, mono-substituted with R3, di-substituted with R3 and R4, or tri-substituted with R3, R4 and R5; R3 is —CF3, —COOH, —COOR7, —C(O)R6, —CH(OH)R6, —CH2R6, R6, =O, halogen, R7, —OH, —NH2, or —NHSO2R7; and R10 is H or C1-6 alkyl.

    Abstract translation: 可用于抑制凝血酶和相关血栓闭塞的本发明化合物具有以下结构：或其药学上可接受的盐，其中m为0或1; R是杂环， - （CR 8 R 9）1-2 NH 2或 - （CR 8 R 9）1-2 OH，其中R 8和R 9各自独立地为H，C 1-6烷基，-CH 2 F，-CHF 2，CF 3 或-CH 2 OH; W是a）-CHR 1 R 2，其中R 1是-C（CH 3）3，并且R 2是 - （CH 2）1-2 OH，b）具有1或2个选自N的杂原子的5或6元未取代或取代的杂环， O，其中取代的杂环被R 3取代，c）具有1或2个选自N，O和S的杂原子的9或10元未取代或取代的杂环，其中取代的杂环被R 3单取代或被R 3二取代 和R 4，或d）未被取代的，被R 3和R 4二取代或被R3，R4和R5三取代的R3单取代的3-，4-或5-元碳环; R3是-CF3，-COOH，-COOR7，-C（O）R6，-CH（OH）R6，-CH2R6，R6，= O，卤素，R7，-OH，-NH2或-NHSO2R7; R 10为H或C 1-6烷基。

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