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发明申请
US20120252743A1 TRYPSIN-LIKE SERINE PROTEASE INHIBITORS, THEIR PREPARATION AND USE AS SELECTIVE INHIBITORS OF THE CLOTTING FACTORS IIA AND XA 有权
TRYPSIN样丝氨酸蛋白酶抑制剂，其制备和用作选择性抑制剂IIA和XA的选择性抑制剂

TRYPSIN-LIKE SERINE PROTEASE INHIBITORS, THEIR PREPARATION AND USE AS SELECTIVE INHIBITORS OF THE CLOTTING FACTORS IIA AND XA
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（中）：

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之间的整数，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。

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