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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: unett dj. 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 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: unett dj. J Med Chem. 2008 Sep 11;51(17):5172-5. doi: 10.1021/jm8006867. Epub 2008 Aug 13. J Med Chem. 2008. PMID: 18698756
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: unett dj. 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: unett dj. 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: unett dj. 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.
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. Among authors: unett dj. 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
Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension.
Tran TA, Kramer B, Shin YJ, Vallar P, Boatman PD, Zou N, Sage CR, Gharbaoui T, Krishnan A, Pal B, Shakya SR, Garrido Montalban A, Adams JW, Ramirez J, Behan DP, Shifrina A, Blackburn A, Leakakos T, Shi Y, Morgan M, Sadeque A, Chen W, Unett DJ, Gaidarov I, Chen X, Chang S, Shu HH, Tung SF, Semple G. Tran TA, et al. Among authors: unett dj. J Med Chem. 2017 Feb 9;60(3):913-927. doi: 10.1021/acs.jmedchem.6b00871. Epub 2017 Jan 19. J Med Chem. 2017. PMID: 28072531
Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain.
Han S, Thoresen L, Jung JK, Zhu X, Thatte J, Solomon M, Gaidarov I, Unett DJ, Yoon WH, Barden J, Sadeque A, Usmani A, Chen C, Semple G, Grottick AJ, Al-Shamma H, Christopher R, Jones RM. Han S, et al. Among authors: unett dj. ACS Med Chem Lett. 2017 Nov 30;8(12):1309-1313. doi: 10.1021/acsmedchemlett.7b00396. eCollection 2017 Dec 14. ACS Med Chem Lett. 2017. PMID: 29259753 Free PMC article.
Discovery of a lead series of potent benzodiazepine 5-HT2C receptor agonists with high selectivity in functional and binding assays.
Ren A, Zhu X, Feichtinger K, Lehman J, Kasem M, Schrader TO, Wong A, Dang H, Le M, Frazer J, Unett DJ, Grottick AJ, Whelan KT, Morgan ME, Sage CR, Semple G. Ren A, et al. Among authors: unett dj. Bioorg Med Chem Lett. 2020 Mar 1;30(5):126929. doi: 10.1016/j.bmcl.2019.126929. Epub 2019 Dec 26. Bioorg Med Chem Lett. 2020. PMID: 31952960
21 results