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Orally active factor Xa inhibitor: synthesis and biological activity of masked amidines as prodrugs of novel 1,4-diazepane derivatives.
Koshio H, Hirayama F, Ishihara T, Kaizawa H, Shigenaga T, Taniuchi Y, Sato K, Moritani Y, Iwatsuki Y, Uemura T, Kaku S, Kawasaki T, Matsumoto Y, Sakamoto S, Tsukamoto S. Koshio H, et al. Among authors: shigenaga t. Bioorg Med Chem. 2004 Oct 15;12(20):5415-26. doi: 10.1016/j.bmc.2004.07.046. Bioorg Med Chem. 2004. PMID: 15388168
Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor.
Hirayama F, Koshio H, Ishihara T, Hachiya S, Sugasawa K, Koga Y, Seki N, Shiraki R, Shigenaga T, Iwatsuki Y, Moritani Y, Mori K, Kadokura T, Kawasaki T, Matsumoto Y, Sakamoto S, Tsukamoto S. Hirayama F, et al. Among authors: shigenaga t. J Med Chem. 2011 Dec 8;54(23):8051-65. doi: 10.1021/jm200868m. Epub 2011 Nov 11. J Med Chem. 2011. PMID: 21995444
Design, synthesis and biological activity of selective and orally available TF/FVIIa complex inhibitors containing non-amidine P1 ligands.
Miura M, Seki N, Koike T, Ishihara T, Niimi T, Hirayama F, Shigenaga T, Sakai-Moritani Y, Tagawa A, Kawasaki T, Sakamoto S, Okada M, Ohta M, Tsukamoto S. Miura M, et al. Among authors: shigenaga t. Bioorg Med Chem. 2007 Jan 1;15(1):160-73. doi: 10.1016/j.bmc.2006.09.071. Epub 2006 Oct 4. Bioorg Med Chem. 2007. PMID: 17064913
Potent and selective TF/FVIIa inhibitors containing a neutral P1 ligand.
Miura M, Seki N, Koike T, Ishihara T, Niimi T, Hirayama F, Shigenaga T, Sakai-Moritani Y, Kawasaki T, Sakamoto S, Okada M, Ohta M, Tsukamoto S. Miura M, et al. Among authors: shigenaga t. Bioorg Med Chem. 2006 Dec 1;14(23):7688-705. doi: 10.1016/j.bmc.2006.08.010. Epub 2006 Aug 30. Bioorg Med Chem. 2006. PMID: 16942884
43 results