2-Aminomethylphenylamine as a novel scaffold for factor Xa inhibitor

A Mochizuki, T Nagata, H Kanno, M Suzuki…

Index: Mochizuki, Akiyoshi; Nagata, Tsutomu; Kanno, Hideyuki; Suzuki, Makoto; Ohta, Toshiharu Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 5 p. 1623 - 1642

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Citation Number: 11

Abstract

We have been researching orally active factor Xa inhibitor for a long time. We explored the new diamine linker using effective ligands to obtain a new attractive original scaffold 2- aminomethylphenylamine derivative. Compound 1D showed very strong in vitro and in vivo factor Xa inhibitory activity, as well as favorable PK profiles in po administration to monkeys.