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Page 1
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: machinaga n. 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
Identification of 4-[1-[3-chloro-4-[N'-(5-fluoro-2-methylphenyl)ureido]phenylacetyl]-(4S)-fluoro-(2S)-pyrrolidinylmethoxy]benzoic acid as a potent, orally active VLA-4 antagonist.
Muro F, Iimura S, Yoneda Y, Chiba J, Watanabe T, Setoguchi M, Iigou Y, Takayama G, Yokoyama M, Takashi T, Nakayama A, Machinaga N. Muro F, et al. Among authors: machinaga n. Bioorg Med Chem. 2008 Dec 1;16(23):9991-10000. doi: 10.1016/j.bmc.2008.10.020. Epub 2008 Oct 12. Bioorg Med Chem. 2008. PMID: 18952443
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: machinaga n. 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
Synthesis, biological evaluation, and pharmacokinetic study of prolyl-1-piperazinylacetic acid and prolyl-4-piperidinylacetic acid derivatives as VLA-4 antagonists.
Chiba J, Takayama G, Takashi T, Yokoyama M, Nakayama A, Baldwin JJ, McDonald E, Moriarty KJ, Sarko CR, Saionz KW, Swanson R, Hussain Z, Wong A, Machinaga N. Chiba J, et al. Among authors: machinaga n. Bioorg Med Chem. 2006 Apr 15;14(8):2725-46. doi: 10.1016/j.bmc.2005.11.058. Epub 2005 Dec 27. Bioorg Med Chem. 2006. PMID: 16377201
18 results