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    Thrombin Inhibitors
    63.
    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

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

    发明人： Harry Chobanian ,  Tesfaye Biftu ,  Barbara Pio ,  Zhicai Wu

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

    CPC分类号： C07D207/16 ,  C07D207/34 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D417/06

    摘要： 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.

    摘要翻译： 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。

    Substituted 5,6,7,8-tetrahydropyrido[4,3-D]pyrimidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    67.
    发明授权
    Substituted 5,6,7,8-tetrahydropyrido[4,3-D]pyrimidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes 有权
    取代5,6,7,8-四氢吡啶并[4,3-D]嘧啶作为二肽基肽酶-IV抑制剂，用于治疗或预防糖尿病

    公开(公告)号：US07928112B2

    公开(公告)日：2011-04-19

    申请号：US12869869

    申请日：2010-08-27

    申请人： Tesfaye Biftu ,  Ping Chen ,  Danqing Feng ,  Ann E. Weber

    发明人： Tesfaye Biftu ,  Ping Chen ,  Danqing Feng ,  Ann E. Weber

    IPC分类号： A61K31/519

    CPC分类号： C07D487/04 ,  C07D471/04

    摘要： The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

    摘要翻译： 本发明涉及结构式I的新型取代的氨基四氢吡喃，其是二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病，特别是 2型糖尿病 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。