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Page 1
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: taira t. 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
4-(Pyrrolidinyl)methoxybenzoic acid derivatives as a potent, orally active VLA-4 antagonist.
Chiba J, Iimura S, Yoneda Y, Sugimoto Y, Horiuchi T, Muro F, Ochiai Y, Ogasawara T, Tsubokawa M, Iigou Y, Takayama G, Taira T, Takata Y, Yokoyama M, Takashi T, Nakayama A, Machinaga N. Chiba J, et al. Among authors: taira t. Chem Pharm Bull (Tokyo). 2006 Nov;54(11):1515-29. doi: 10.1248/cpb.54.1515. Chem Pharm Bull (Tokyo). 2006. PMID: 17077548 Free article.
Discovery of trans-4-[1-[[2,5-Dichloro-4-(1-methyl-3-indolylcarboxamido)phenyl]acetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid: an orally active, selective very late antigen-4 antagonist.
Muro F, Iimura S, Sugimoto Y, Yoneda Y, Chiba J, Watanabe T, Setoguchi M, Iigou Y, Matsumoto K, Satoh A, Takayama G, Taira T, Yokoyama M, Takashi T, Nakayama A, Machinaga N. Muro F, et al. Among authors: taira t. J Med Chem. 2009 Dec 24;52(24):7974-92. doi: 10.1021/jm901154c. J Med Chem. 2009. PMID: 19891440
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: taira t. 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
Highly potent, orally active novel small-molecule HPK1 inhibitor DS21150768 induces anti-tumor responses in multiple syngeneic tumor mouse models.
Setsu G, Goto M, Ito K, Taira T, Miyamoto M, Watanabe T, Taniguchi T, Umezaki Y, Nakazawa Y, Uesugi S, Mori K, Horiuchi T, Obuchi W, Minami M, Shimada T, Wada C, Yoshida T, Higuchi S. Setsu G, et al. Among authors: taira t. Eur J Pharmacol. 2023 Dec 15;961:176184. doi: 10.1016/j.ejphar.2023.176184. Epub 2023 Nov 8. Eur J Pharmacol. 2023. PMID: 37944847
DS-1205b, a novel selective inhibitor of AXL kinase, blocks resistance to EGFR-tyrosine kinase inhibitors in a non-small cell lung cancer xenograft model.
Jimbo T, Hatanaka M, Komatsu T, Taira T, Kumazawa K, Maeda N, Suzuki T, Ota M, Haginoya N, Isoyama T, Fujiwara K. Jimbo T, et al. Among authors: taira t. Oncotarget. 2019 Aug 27;10(50):5152-5167. doi: 10.18632/oncotarget.27114. eCollection 2019 Aug 27. Oncotarget. 2019. PMID: 31497246 Free PMC article.
910 results