Drug Development
1,4-diazepane derivative has potent anticoagulant and antithrombotic activity
Published in Blood Weekly, July 29th, 2004
"Factor Xa (fXa) is a serine protease involved in the coagulation cascade, which has received great interest as a potential target for the development of new antithrombotic drugs," scientists in Japan explained.
H. Koshio and colleagues working with Yamanouchi Pharmaceutical Co. Ltd. presented a "series of fXa inhibitors in which the 1,4-diazepane moiety was designed to interact with the S4 aryl-binding domain of the fXa active site."
"Compound 13 (YM-96765) showed potent fXa inhibitory activity (IC50 =6.8 nM) and...
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Source: Blood Weekly (2004-07-29)
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