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    Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors IIa and Xa
    32.
    发明授权
    Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors IIa and Xa 有权
    胰蛋白酶样丝氨酸蛋白酶抑制剂，它们的制备和用作凝血因子IIa和Xa的选择性抑制剂

    公开(公告)号：US08497245B2

    公开(公告)日：2013-07-30

    申请号：US13332900

    申请日：2011-12-21

    申请人： Peter Herold ,  Stjepan Jelakovic ,  Mohammed Daghish ,  Claudia Reichelt ,  Alexander Schulze ,  Andrea Schweinitz ,  Friedrich-Alexander Ludwig ,  Adel Rafai Far ,  Ting Kang

    发明人： Peter Herold ,  Stjepan Jelakovic ,  Mohammed Daghish ,  Claudia Reichelt ,  Alexander Schulze ,  Andrea Schweinitz ,  Friedrich-Alexander Ludwig ,  Adel Rafai Far ,  Ting Kang

    IPC分类号： A61K38/05

    CPC分类号： C07K5/06121 ,  A61K38/00 ,  C07K5/06104 ,  C07K5/06113 ,  C07K5/06191

    摘要： The invention provides methods of making and using compounds of the formula: or a pharmaceutically acceptable salt thereof; wherein n is an integer between 1 and 2 inclusively; m is an integer between 0 and 2 inclusively; X is selected from the group consisting of CH or N; R1 is selected from the group consisting of —CH2NH2, and R2 is selected from the group consisting of —H, —OH, —NH2 and acetyl; R3 is selected from the group consisting of —H, benzyloxycarbonyl and benzylsulfonyl; and R4 is selected from the group consisting of —OH, wherein p is an integer between 0 and 2 inclusively, Y is selected from the group consisting of —O—, —S—, —S(═O)—, —SO2—, methylene, —CH(OH)—, —CH(NH2)—, —CH(CH2—OH)—, —CH(CH2—NH2)— or —N(R6)—, R5 is selected from the group consisting of —H or a simple (C1-C3) alkyl and R6 is selected from the group consisting of —H, a simple (C1-C3) alkyl or a simple (C1-C3) acyl. These compounds are useful as anticoagulant agents as a result of their selective dual inhibition of thrombin and prothrombinase.

    摘要翻译： 本发明提供制备和使用下式的化合物或其药学上可接受的盐的方法： 其中n是1和2之间的整数; m是0和2之间的整数; X选自CH或N; R1选自-CH2NH2，R2选自-H，-OH，-NH2和乙酰基; R3选自-H，苄氧基羰基和苄基磺酰基; 并且R 4选自-OH，其中p是包括0和2的整数，Y选自-O - ， - S - ， - S（= O） - ， - SO 2 - ，亚甲基，-CH（OH） - ， - CH（NH 2） - ， - CH（CH 2 -OH） - ， - CH（CH 2 -NH 2） - 或-N（R 6） - ，R 5选自 -H或简单（C 1 -C 3）烷基，R 6选自-H，简单（C 1 -C 3）烷基或简单（C 1 -C 3）酰基）。 由于它们选择性双重抑制凝血酶和凝血酶原酶，这些化合物可用作抗凝血剂。