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Page 1
Discovery of 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalen-4-carboxamides as potent and selective CB2 receptor agonists.
Han S, Thoresen L, Zhu X, Narayanan S, Jung JK, Strah-Pleynet S, Decaire M, Choi K, Xiong Y, Yue D, Semple G, Thatte J, Solomon M, Fu L, Whelan K, Al-Shamma H, Gatlin J, Chen R, Dang H, Pride C, Gaidarov I, Unett DJ, Behan DP, Sadeque A, Usmani KA, Chen C, Edwards J, Morgan M, Jones RM. Han S, et al. Among authors: edwards j. Bioorg Med Chem Lett. 2015 Jan 15;25(2):322-6. doi: 10.1016/j.bmcl.2014.11.040. Epub 2014 Nov 26. Bioorg Med Chem Lett. 2015. PMID: 25488844
Discovery and characterization of potent and selective 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acids as S1P₁ agonists.
Buzard D, Han S, Thoresen L, Moody J, Lopez L, Kawasaki A, Schrader T, Sage C, Gao Y, Edwards J, Barden J, Thatte J, Fu L, Solomon M, Liu L, Al-Shamma H, Gatlin J, Le M, Xing C, Espinola S, Jones RM. Buzard D, et al. Among authors: edwards j. Bioorg Med Chem Lett. 2011 Oct 1;21(19):6013-8. doi: 10.1016/j.bmcl.2011.05.110. Epub 2011 Jun 6. Bioorg Med Chem Lett. 2011. PMID: 21852130
Fused tricyclic indoles as S1P₁ agonists with robust efficacy in animal models of autoimmune disease.
Buzard DJ, Han S, Lopez L, Kawasaki A, Moody J, Thoresen L, Ullman B, Lehmann J, Calderon I, Zhu X, Gharbaoui T, Sengupta D, Krishnan A, Gao Y, Edwards J, Barden J, Morgan M, Usmani K, Chen C, Sadeque A, Thatte J, Solomon M, Fu L, Whelan K, Liu L, Al-Shamma H, Gatlin J, Le M, Xing C, Espinola S, Jones RM. Buzard DJ, et al. Among authors: edwards j. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4404-9. doi: 10.1016/j.bmcl.2012.04.129. Epub 2012 May 7. Bioorg Med Chem Lett. 2012. PMID: 22633692
Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.
Buzard DJ, Kim SH, Lopez L, Kawasaki A, Zhu X, Moody J, Thoresen L, Calderon I, Ullman B, Han S, Lehmann J, Gharbaoui T, Sengupta D, Calvano L, Montalban AG, Ma YA, Sage C, Gao Y, Semple G, Edwards J, Barden J, Morgan M, Chen W, Usmani K, Chen C, Sadeque A, Christopher RJ, Thatte J, Fu L, Solomon M, Mills D, Whelan K, Al-Shamma H, Gatlin J, Le M, Gaidarov I, Anthony T, Unett DJ, Blackburn A, Rueter J, Stirn S, Behan DP, Jones RM. Buzard DJ, et al. Among authors: edwards j. ACS Med Chem Lett. 2014 Nov 4;5(12):1313-7. doi: 10.1021/ml500389m. eCollection 2014 Dec 11. ACS Med Chem Lett. 2014. PMID: 25516790 Free PMC article.
(7-Benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic Acids as S1P1 Functional Antagonists.
Buzard DJ, Lopez L, Moody J, Kawasaki A, Schrader TO, Kasem M, Johnson B, Zhu X, Thoresen L, Kim SH, Gharbaoui T, Sengupta D, Calvano L, Krishnan A, Gao Y, Semple G, Edwards J, Barden J, Morgan M, Usmani K, Chen C, Sadeque A, Chen W, Christopher RJ, Thatte J, Fu L, Solomon M, Whelan K, Al-Shamma H, Gatlin J, Gaidarov I, Anthony T, Le M, Unett DJ, Stirn S, Blackburn A, Behan DP, Jones RM. Buzard DJ, et al. Among authors: edwards j. ACS Med Chem Lett. 2014 Nov 25;5(12):1334-9. doi: 10.1021/ml500422m. eCollection 2014 Dec 11. ACS Med Chem Lett. 2014. PMID: 25516794 Free PMC article.
Design and synthesis of new tricyclic indoles as potent modulators of the S1P1 receptor.
Buzard DJ, Schrader TO, Zhu X, Lehmann J, Johnson B, Kasem M, Kim SH, Kawasaki A, Lopez L, Moody J, Han S, Gao Y, Edwards J, Barden J, Thatte J, Gatlin J, Jones RM. Buzard DJ, et al. Among authors: edwards j. Bioorg Med Chem Lett. 2015 Feb 1;25(3):659-63. doi: 10.1016/j.bmcl.2014.11.089. Epub 2014 Dec 9. Bioorg Med Chem Lett. 2015. PMID: 25532755
A new family of H3 receptor antagonists based on the natural product Conessine.
Santora VJ, Covel JA, Hayashi R, Hofilena BJ, Ibarra JB, Pulley MD, Weinhouse MI, Sengupta D, Duffield JJ, Semple G, Webb RR, Sage C, Ren A, Pereira G, Knudsen J, Edwards JE, Suarez M, Frazer J, Thomsen W, Hauser E, Whelan K, Grottick AJ. Santora VJ, et al. Among authors: edwards je. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1490-4. doi: 10.1016/j.bmcl.2007.12.059. Epub 2007 Dec 25. Bioorg Med Chem Lett. 2008. PMID: 18194865
Novel H3 receptor antagonists with improved pharmacokinetic profiles.
Santora VJ, Covel JA, Hayashi R, Hofilena BJ, Ibarra JB, Pulley MD, Weinhouse MI, Semple G, Ren A, Pereira G, Edwards JE, Suarez M, Frazer J, Thomsen W, Hauser E, Lorea J, Grottick AJ. Santora VJ, et al. Among authors: edwards je. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4133-6. doi: 10.1016/j.bmcl.2008.05.086. Epub 2008 May 24. Bioorg Med Chem Lett. 2008. PMID: 18554904
APD791, 3-methoxy-n-(3-(1-methyl-1h-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide, a novel 5-hydroxytryptamine 2A receptor antagonist: pharmacological profile, pharmacokinetics, platelet activity and vascular biology.
Adams JW, Ramirez J, Shi Y, Thomsen W, Frazer J, Morgan M, Edwards JE, Chen W, Teegarden BR, Xiong Y, Al-Shamma H, Behan DP, Connolly DT. Adams JW, et al. Among authors: edwards je. J Pharmacol Exp Ther. 2009 Oct;331(1):96-103. doi: 10.1124/jpet.109.153189. Epub 2009 Jul 23. J Pharmacol Exp Ther. 2009. PMID: 19628629
Design and evaluation of novel biphenyl sulfonamide derivatives with potent histamine H(3) receptor inverse agonist activity.
Covel JA, Santora VJ, Smith JM, Hayashi R, Gallardo C, Weinhouse MI, Ibarra JB, Schultz JA, Park DM, Estrada SA, Hofilena BJ, Pulley MD, Smith BM, Ren A, Suarez M, Frazer J, Edwards J, Hauser EK, Lorea J, Semple G, Grottick AJ. Covel JA, et al. Among authors: edwards j. J Med Chem. 2009 Sep 24;52(18):5603-11. doi: 10.1021/jm900857n. J Med Chem. 2009. PMID: 19722526
7,007 results