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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: pierce jm. J Med Chem. 2012 Apr 12;55(7):2945-59. doi: 10.1021/jm201542d. Epub 2012 Feb 27. J Med Chem. 2012. PMID: 22364528
The SAR of brain penetration for a series of heteroaryl urea FAAH inhibitors.
Keith JM, Tichenor MS, Apodaca RL, Xiao W, Jones WM, Seierstad M, Pierce JM, Palmer JA, Webb M, Karbarz MJ, Scott BP, Wilson SJ, Wennerholm ML, Rizzolio M, Rynberg R, Chaplan SR, Breitenbucher JG. Keith JM, et al. Among authors: pierce jm. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3109-3114. doi: 10.1016/j.bmcl.2016.05.001. Epub 2016 May 5. Bioorg Med Chem Lett. 2016. PMID: 27189675
1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase.
Keith JM, Hawryluk N, Apodaca RL, Chambers A, Pierce JM, Seierstad M, Palmer JA, Webb M, Karbarz MJ, Scott BP, Wilson SJ, Luo L, Wennerholm ML, Chang L, Rizzolio M, Chaplan SR, Breitenbucher JG. Keith JM, et al. Among authors: pierce jm. Bioorg Med Chem Lett. 2014 Mar 1;24(5):1280-4. doi: 10.1016/j.bmcl.2014.01.064. Epub 2014 Jan 31. Bioorg Med Chem Lett. 2014. PMID: 24513048
Heteroaryl urea inhibitors of fatty acid amide hydrolase: structure-mutagenicity relationships for arylamine metabolites.
Tichenor MS, Keith JM, Jones WM, Pierce JM, Merit J, Hawryluk N, Seierstad M, Palmer JA, Webb M, Karbarz MJ, Wilson SJ, Wennerholm ML, Woestenborghs F, Beerens D, Luo L, Brown SM, Boeck MD, Chaplan SR, Breitenbucher JG. Tichenor MS, et al. Among authors: pierce jm. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7357-62. doi: 10.1016/j.bmcl.2012.10.076. Epub 2012 Oct 22. Bioorg Med Chem Lett. 2012. PMID: 23141911
Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty acid amide hydrolase.
Keith JM, Jones WM, Pierce JM, Seierstad M, Palmer JA, Webb M, Karbarz MJ, Scott BP, Wilson SJ, Luo L, Wennerholm ML, Chang L, Brown SM, Rizzolio M, Rynberg R, Chaplan SR, Breitenbucher JG. Keith JM, et al. Among authors: pierce jm. Bioorg Med Chem Lett. 2014 Feb 1;24(3):737-41. doi: 10.1016/j.bmcl.2013.12.113. Epub 2014 Jan 6. Bioorg Med Chem Lett. 2014. PMID: 24433863
Heteroarylureas with fused bicyclic diamine cores as inhibitors of fatty acid amide hydrolase.
Keith JM, Jones W, Pierce JM, Seierstad M, Palmer JA, Webb M, Karbarz M, Scott BP, Wilson SJ, Luo L, Wennerholm M, Chang L, Rizzolio M, Rynberg R, Chaplan S, Guy Breitenbucher J. Keith JM, et al. Among authors: pierce jm. Bioorg Med Chem Lett. 2020 Oct 15;30(20):127463. doi: 10.1016/j.bmcl.2020.127463. Epub 2020 Aug 9. Bioorg Med Chem Lett. 2020. PMID: 32784090
Identification and structure activity relationships of quinoline tertiary alcohol modulators of RORγt.
Kummer DA, Cummings MD, Abad M, Barbay J, Castro G, Wolin R, Kreutter KD, Maharoof U, Milligan C, Nishimura R, Pierce J, Schalk-Hihi C, Spurlino J, Urbanski M, Venkatesan H, Wang A, Woods C, Xue X, Edwards JP, Fourie AM, Leonard K. Kummer DA, et al. Bioorg Med Chem Lett. 2017 May 1;27(9):2047-2057. doi: 10.1016/j.bmcl.2017.02.044. Epub 2017 Feb 21. Bioorg Med Chem Lett. 2017. PMID: 28318945
6-Substituted quinolines as RORγt inverse agonists.
Barbay JK, Cummings MD, Abad M, Castro G, Kreutter KD, Kummer DA, Maharoof U, Milligan C, Nishimura R, Pierce J, Schalk-Hihi C, Spurlino J, Tanis VM, Urbanski M, Venkatesan H, Wang A, Woods C, Wolin R, Xue X, Edwards JP, Fourie AM, Leonard K. Barbay JK, et al. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5277-5283. doi: 10.1016/j.bmcl.2017.10.027. Epub 2017 Oct 16. Bioorg Med Chem Lett. 2017. PMID: 29079472
Aryl Piperazinyl Ureas as Inhibitors of Fatty Acid Amide Hydrolase (FAAH) in Rat, Dog, and Primate.
Keith JM, Apodaca R, Tichenor M, Xiao W, Jones W, Pierce J, Seierstad M, Palmer J, Webb M, Karbarz M, Scott B, Wilson S, Luo L, Wennerholm M, Chang L, Brown S, Rizzolio M, Rynberg R, Chaplan S, Breitenbucher JG. Keith JM, et al. Among authors: pierce j. ACS Med Chem Lett. 2012 Aug 22;3(10):823-7. doi: 10.1021/ml300186g. eCollection 2012 Oct 11. ACS Med Chem Lett. 2012. PMID: 24900385 Free PMC article.
176 results