The discovery of YM-60828: a potent, selective and orally-bioavailable factor Xa inhibitor

…, Y Sakai-Moritani, T Kawasaki, Y Matsumoto…

Index: Hirayama, Fukushi; Koshio, Hiroyuki; Katayama, Naoko; Kurihara, Hiroyuki; Taniuchi, Yuta; Sato, Kazuo; Hisamichi, Nami; Sakai-Moritani, Yumiko; Kawasaki, Tomihisa; Matsumoto, Yuzo; Yanagisawa, Isao Bioorganic and medicinal chemistry, 2002 , vol. 10, # 5 p. 1509 - 1523

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Citation Number: 45

Abstract

Since Factor Xa (FXa) is well known to play a central role in thrombosis and hemostasis, inhibition of FXa is an attractive target for antithrombotic strategies. As a part of our investigation of a non-peptide, orally available FXa inhibitor, we found that a series of N-[(7- amidino-2-naphthyl) methyl] aniline derivatives possessed potent and selective inhibitory activities. Structure–activity relationship (SAR) of the substituent (R1) on the central aniline ...