Peter Herold,Stjepan Jelakovic,Mohammed Daghish,Claudia Reichelt,Alexander Schulze,Andrea Schweinitz,Friedrich-Alexander Ludwig,Adel Rafai Far,Ting Kang
申请号：
US13332900
公开号：
US20120252743A1
申请日:
2011.12.21
申请国别(地区):
US
年份:
2012
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, andR2 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.
