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Identification of trans-4-[1-[[7-fluoro-2-(1-methyl-3-indolyl)-6-benzoxazolyl]acetyl]-(4S)-fluoro-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid as a potent, orally active VLA-4 antagonist.
Setoguchi M, Iimura S, Sugimoto Y, Yoneda Y, Chiba J, Watanabe T, Muro F, Iigo Y, Takayama G, Yokoyama M, Taira T, Aonuma M, Takashi T, Nakayama A, Machinaga N. Setoguchi M, et al. Among authors: aonuma m. Bioorg Med Chem. 2012 Feb 1;20(3):1201-12. doi: 10.1016/j.bmc.2011.12.045. Epub 2011 Dec 30. Bioorg Med Chem. 2012. PMID: 22261021
A novel, potent, and orally active VLA-4 antagonist with good aqueous solubility: trans-4-[1-[[2-(5-Fluoro-2-methylphenylamino)-7-fluoro-6-benzoxazolyl]acetyl]-(5S)-[methoxy(methyl)amino]methyl-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid.
Setoguchi M, Iimura S, Sugimoto Y, Yoneda Y, Chiba J, Watanabe T, Muro F, Iigo Y, Takayama G, Yokoyama M, Taira T, Aonuma M, Takashi T, Nakayama A, Machinaga N. Setoguchi M, et al. Among authors: aonuma m. Bioorg Med Chem. 2013 Jan 1;21(1):42-61. doi: 10.1016/j.bmc.2012.11.003. Epub 2012 Nov 10. Bioorg Med Chem. 2013. PMID: 23218775
27 results