TRYPSIN LIKE SERINE PROTEASE INHIBITORS THEIR PREPARATION AND USE AS SELECTIVE INHIBITORS OF THE CLOTTING FACTORS IIA AND XA

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专利权人:

发明人:

HEROLD PETER,JELAKOVIC STJEPAN,DAGHISH MOHAMMED,REICHELT CLAUDIA,SCHULZE ALEXANDER,SCHWEINITZ ANDREA,LUDWIG Friedrich Alexander,FAR ADEL RAFAI,KANG TING

申请号：

IN4744/CHENP/2013

公开号：

IN2013CN04744A

申请日:

2013.06.19

申请国别(地区):

IN

年份:

2014

代理人:

摘要：

122223422222651313The invention provides methods of making and using compounds of the formula (I) 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 R is selected from the group consisting of CHNH and (Formula (II)) R is selected from the group consisting of H OH NH and acetyl R is selected from the group consisting of H benzyloxycarbonyl and benzyisulfonyland R is selected from the group consisting of OH (Formulae (III) (IV) (V) (VI)) wherein p is an integer between 0 and 2 inclusively Y is selected from the group consisting of 0 S S(=0) S0 methylene CH(OH) CH(NH) CH(CH OH) CH(CH NH) or N(R) R 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 (C C) alkyl or a simple (C C) acyl. These compounds are useful as anticoagulant agents as a result of their selective dual inhibition of thrombin and prothrombinase.

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