Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors

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• 作者：Tsutomu Nagata ; Toshiharu Yoshino ; Noriyasu Haginoya ; Kenji Yoshikawa ; Yumiko Isobe ; Taketoshi Furugohri ; Hideyuki Kanno
• 关键词：Factor Xa inhibitors ; Cycloalkanediamine ; Non-amidine ; Anticoagulant
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 August 2007
• 卷：17
• 期：16
• 页码：4683-4688
• 文件大小：174 K

摘要

This paper describes the synthesis of orally available potent fXa inhibitors 2 and 3 by modification of the piperazine part of lead compound 1. Carbonyl derivative 3 showed potent fXa activity but not sulfonyl derivative 2. Among the compounds synthesized, cyclohexane derivatives 3g and 3h and cycloheptane derivative 3j had potent anticoagulant activity as well as anti-fXa activity. Synthetic study of the optical isomers of 3g demonstrated that (−)-3g had more potent activity.