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1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia.
Vachal P, Miao S, Pierce JM, Guiadeen D, Colandrea VJ, Wyvratt MJ, Salowe SP, Sonatore LM, Milligan JA, Hajdu R, Gollapudi A, Keohane CA, Lingham RB, Mandala SM, DeMartino JA, Tong X, Wolff M, Steinhuebel D, Kieczykowski GR, Fleitz FJ, Chapman K, Athanasopoulos J, Adam G, Akyuz CD, Jena DK, Lusen JW, Meng J, Stein BD, Xia L, Sherer EC, Hale JJ. Vachal P, et al. Among authors: lingham rb. J Med Chem. 2012 Apr 12;55(7):2945-59. doi: 10.1021/jm201542d. Epub 2012 Feb 27. J Med Chem. 2012. PMID: 22364528
Discovery of N-[Bis(4-methoxyphenyl)methyl]-4-hydroxy-2-(pyridazin-3-yl)pyrimidine-5-carboxamide (MK-8617), an Orally Active Pan-Inhibitor of Hypoxia-Inducible Factor Prolyl Hydroxylase 1-3 (HIF PHD1-3) for the Treatment of Anemia.
Debenham JS, Madsen-Duggan C, Clements MJ, Walsh TF, Kuethe JT, Reibarkh M, Salowe SP, Sonatore LM, Hajdu R, Milligan JA, Visco DM, Zhou D, Lingham RB, Stickens D, DeMartino JA, Tong X, Wolff M, Pang J, Miller RR, Sherer EC, Hale JJ. Debenham JS, et al. Among authors: lingham rb. J Med Chem. 2016 Dec 22;59(24):11039-11049. doi: 10.1021/acs.jmedchem.6b01242. Epub 2016 Nov 30. J Med Chem. 2016. PMID: 28002958
Discovery of N-{N-[(3-cyanobenzene) sulfonyl]-4(R)-(3,3-difluoropiperidin-1-yl)-(l)-prolyl}-4-[(3',5'-dichloro-isonicotinoyl) amino]-(l)-phenylalanine (MK-0617), a highly potent and orally active VLA-4 antagonist.
Venkatraman S, Lebsack AD, Alves K, Gardner MF, James J, Lingham RB, Maniar S, Mumford RA, Si Q, Stock N, Treonze KM, Wang B, Zunic J, Munoz B. Venkatraman S, et al. Among authors: lingham rb. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5803-6. doi: 10.1016/j.bmcl.2009.07.111. Epub 2009 Jul 28. Bioorg Med Chem Lett. 2009. PMID: 19713111
Heterocycle-substituted proline dipeptides as potent VLA-4 antagonists.
Reger TS, Zunic J, Stock N, Wang B, Smith ND, Munoz B, Green MD, Gardner MF, James JP, Chen W, Alves K, Si Q, Treonze KM, Lingham RB, Mumford RA. Reger TS, et al. Among authors: lingham rb. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1173-6. doi: 10.1016/j.bmcl.2009.12.009. Epub 2009 Dec 4. Bioorg Med Chem Lett. 2010. PMID: 20022493
Influence of acid surrogates toward potency of VLA-4 antagonist.
Venkatraman S, Lim J, Cramer M, Gardner MF, James J, Alves K, Lingham RB, Mumford RA, Munoz B. Venkatraman S, et al. Among authors: lingham rb. Bioorg Med Chem Lett. 2005 Sep 15;15(18):4053-6. doi: 10.1016/j.bmcl.2005.06.034. Bioorg Med Chem Lett. 2005. PMID: 16039122
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