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Page 1
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: jones rm. 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 the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119.
Semple G, Fioravanti B, Pereira G, Calderon I, Uy J, Choi K, Xiong Y, Ren A, Morgan M, Dave V, Thomsen W, Unett DJ, Xing C, Bossie S, Carroll C, Chu ZL, Grottick AJ, Hauser EK, Leonard J, Jones RM. Semple G, et al. Among authors: jones rm. J Med Chem. 2008 Sep 11;51(17):5172-5. doi: 10.1021/jm8006867. Epub 2008 Aug 13. J Med Chem. 2008. PMID: 18698756
GPR119 agonists for the treatment of type 2 diabetes.
Jones RM, Leonard JN, Buzard DJ, Lehmann J. Jones RM, et al. Expert Opin Ther Pat. 2009 Oct;19(10):1339-59. doi: 10.1517/13543770903153878. Expert Opin Ther Pat. 2009. PMID: 19780700 Review.
Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.
Semple G, Ren A, Fioravanti B, Pereira G, Calderon I, Choi K, Xiong Y, Shin YJ, Gharbaoui T, Sage CR, Morgan M, Xing C, Chu ZL, Leonard JN, Grottick AJ, Al-Shamma H, Liang Y, Demarest KT, Jones RM. Semple G, et al. Among authors: jones rm. Bioorg Med Chem Lett. 2011 May 15;21(10):3134-41. doi: 10.1016/j.bmcl.2011.03.007. Epub 2011 Mar 13. Bioorg Med Chem Lett. 2011. PMID: 21444206
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: jones rm. 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
Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile.
Semple G, Lehmann J, Wong A, Ren A, Bruce M, Shin YJ, Sage CR, Morgan M, Chen WC, Sebring K, Chu ZL, Leonard JN, Al-Shamma H, Grottick AJ, Du F, Liang Y, Demarest K, Jones RM. Semple G, et al. Among authors: jones rm. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1750-5. doi: 10.1016/j.bmcl.2011.12.092. Epub 2011 Dec 30. Bioorg Med Chem Lett. 2012. PMID: 22264481
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: jones rm. 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: jones rm. Pharm Pat Anal. 2012 Jul;1(3):285-99. doi: 10.4155/ppa.12.33. Pharm Pat Anal. 2012. PMID: 24236842 Review.
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: jones rm. 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
1,018 results