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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. 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
Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation.
Semple G, Tran TA, Kramer B, Hsu D, Han S, Choi J, Vallar P, Casper MD, Zou N, Hauser EK, Thomsen W, Whelan K, Sengupta D, Morgan M, Sekiguchi Y, Kanuma K, Chaki S, Grottick AJ. Semple G, et al. Among authors: han s. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6166-71. doi: 10.1016/j.bmcl.2009.09.003. Epub 2009 Sep 6. Bioorg Med Chem Lett. 2009. PMID: 19773162
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: han s. 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: han s. 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
GPR119 agonists 2009-2011.
Buzard DJ, Lehmann J, Han S, Jones RM. Buzard DJ, et al. Among authors: han s. Pharm Pat Anal. 2012 Jul;1(3):285-99. doi: 10.4155/ppa.12.33. Pharm Pat Anal. 2012. PMID: 24236842 Free article. Review.
Discovery and optimization of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists.
Buzard DJ, Kim SH, Lehmann J, Han S, Calderon I, Wong A, Kawasaki A, Narayanan S, Bhat R, Gharbaoui T, Lopez L, Yue D, Whelan K, Al-Shamma H, Unett DJ, Shu HH, Tung SF, Chang S, Chuang CF, Morgan M, Sadeque A, Chu ZL, Leonard JN, Jones RM. Buzard DJ, et al. Among authors: han s. Bioorg Med Chem Lett. 2014 Sep 1;24(17):4332-5. doi: 10.1016/j.bmcl.2014.06.071. Epub 2014 Jul 3. Bioorg Med Chem Lett. 2014. PMID: 25088191
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: han s. 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.
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: han s. 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
Discovery of a novel trans-1,4-dioxycyclohexane GPR119 agonist series.
Han S, Narayanan S, Kim SH, Calderon I, Zhu X, Kawasaki A, Yue D, Lehmann J, Wong A, Buzard DJ, Semple G, Carroll C, Chu ZL, Al-Sharmma H, Shu HH, Tung SF, Unett DJ, Behan DP, Yoon WH, Morgan M, Usmani KA, Chen C, Sadeque A, Leonard JN, Jones RM. Han S, et al. Bioorg Med Chem Lett. 2015 Aug 1;25(15):3034-8. doi: 10.1016/j.bmcl.2015.04.102. Epub 2015 May 23. Bioorg Med Chem Lett. 2015. PMID: 26048791
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