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832 results

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Page 1
Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3.
Li Z, Chen W, Hale JJ, Lynch CL, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Chrebet G, Parent SA, Bergstrom J, Card D, Forrest M, Quackenbush EJ, Wickham LA, Vargas H, Evans RM, Rosen H, Mandala S. Li Z, et al. Among authors: vargas h. J Med Chem. 2005 Oct 6;48(20):6169-73. doi: 10.1021/jm0503244. J Med Chem. 2005. PMID: 16190743
Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.
Shipe WD, Barrow JC, Yang ZQ, Lindsley CW, Yang FV, Schlegel KA, Shu Y, Rittle KE, Bock MG, Hartman GD, Tang C, Ballard JE, Kuo Y, Adarayan ED, Prueksaritanont T, Zrada MM, Uebele VN, Nuss CE, Connolly TM, Doran SM, Fox SV, Kraus RL, Marino MJ, Graufelds VK, Vargas HM, Bunting PB, Hasbun-Manning M, Evans RM, Koblan KS, Renger JJ. Shipe WD, et al. J Med Chem. 2008 Jul 10;51(13):3692-5. doi: 10.1021/jm800419w. Epub 2008 Jun 10. J Med Chem. 2008. PMID: 18540666
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.
Yang ZQ, Barrow JC, Shipe WD, Schlegel KA, Shu Y, Yang FV, Lindsley CW, Rittle KE, Bock MG, Hartman GD, Uebele VN, Nuss CE, Fox SV, Kraus RL, Doran SM, Connolly TM, Tang C, Ballard JE, Kuo Y, Adarayan ED, Prueksaritanont T, Zrada MM, Marino MJ, Graufelds VK, DiLella AG, Reynolds IJ, Vargas HM, Bunting PB, Woltmann RF, Magee MM, Koblan KS, Renger JJ. Yang ZQ, et al. J Med Chem. 2008 Oct 23;51(20):6471-7. doi: 10.1021/jm800830n. Epub 2008 Sep 26. J Med Chem. 2008. PMID: 18817368
Benzofuran Derivatives as Potent, Orally Active S1P1 Receptor Agonists: A Preclinical Lead Molecule for MS.
Saha AK, Yu X, Lin J, Lobera M, Sharadendu A, Chereku S, Schutz N, Segal D, Marantz Y, McCauley D, Middleton S, Siu J, Bürli RW, Buys J, Horner M, Salyers K, Schrag M, Vargas HM, Xu Y, McElvain M, Xu H. Saha AK, et al. Among authors: vargas hm. ACS Med Chem Lett. 2010 Nov 9;2(2):97-101. doi: 10.1021/ml100227q. eCollection 2011 Feb 10. ACS Med Chem Lett. 2010. PMID: 24900286 Free PMC article.
Discovery of a Potent, S1P3-Sparing Benzothiazole Agonist of Sphingosine-1-Phosphate Receptor 1 (S1P1).
Lanman BA, Cee VJ, Cheruku SR, Frohn M, Golden J, Lin J, Lobera M, Marantz Y, Muller KM, Neira SC, Pickrell AJ, Rivenzon-Segal D, Schutz N, Sharadendu A, Yu X, Zhang Z, Buys J, Fiorino M, Gore A, Horner M, Itano A, McElvain M, Middleton S, Schrag M, Vargas HM, Xu H, Xu Y, Zhang X, Siu J, Bürli RW. Lanman BA, et al. Among authors: vargas hm. ACS Med Chem Lett. 2010 Nov 9;2(2):102-6. doi: 10.1021/ml100228m. eCollection 2011 Feb 10. ACS Med Chem Lett. 2010. PMID: 24900287 Free PMC article.
4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia.
Fish LR, Gilligan MT, Humphries AC, Ivarsson M, Ladduwahetty T, Merchant KJ, O'Connor D, Patel S, Philipps E, Vargas HM, Hutson PH, MacLeod AM. Fish LR, et al. Among authors: vargas hm. Bioorg Med Chem Lett. 2005 Aug 15;15(16):3665-9. doi: 10.1016/j.bmcl.2005.05.104. Bioorg Med Chem Lett. 2005. PMID: 15993598
Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.
Dineen TA, Weiss MM, Williamson T, Acton P, Babu-Khan S, Bartberger MD, Brown J, Chen K, Cheng Y, Citron M, Croghan MD, Dunn RT 2nd, Esmay J, Graceffa RF, Harried SS, Hickman D, Hitchcock SA, Horne DB, Huang H, Imbeah-Ampiah R, Judd T, Kaller MR, Kreiman CR, La DS, Li V, Lopez P, Louie S, Monenschein H, Nguyen TT, Pennington LD, San Miguel T, Sickmier EA, Vargas HM, Wahl RC, Wen PH, Whittington DA, Wood S, Xue Q, Yang BH, Patel VF, Zhong W. Dineen TA, et al. Among authors: vargas hm. J Med Chem. 2012 Nov 8;55(21):9025-44. doi: 10.1021/jm300118s. Epub 2012 Apr 18. J Med Chem. 2012. PMID: 22468684
Discovery of AMG 369, a Thiazolo[5,4-b]pyridine Agonist of S1P1 and S1P5.
Cee VJ, Frohn M, Lanman BA, Golden J, Muller K, Neira S, Pickrell A, Arnett H, Buys J, Gore A, Fiorino M, Horner M, Itano A, Lee MR, McElvain M, Middleton S, Schrag M, Rivenzon-Segal D, Vargas HM, Xu H, Xu Y, Zhang X, Siu J, Wong M, Bürli RW. Cee VJ, et al. Among authors: vargas hm. ACS Med Chem Lett. 2010 Dec 29;2(2):107-12. doi: 10.1021/ml100306h. eCollection 2011 Feb 10. ACS Med Chem Lett. 2010. PMID: 24900288 Free PMC article.
832 results