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TRYPSIN-LIKE SERINE PROTEASE INHIBITORS, THEIR PREPARATION AND USE AS SELECTIVE INHIBITORS OF THE CLOTTING FACTORS IIA AND XA
专利权人:
发明人:
申请号:
EP11850640.1
公开号:
EP2655399A1
申请日:
2011.12.21
申请国别(地区):
EP
年份:
2013
代理人:
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.
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