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Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors.
Yan L, Hale JJ, Lynch CL, Budhu R, Gentry A, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Chrebet G, Bergstrom J, Card D, Rosen H, Mandala SM. Yan L, et al. Bioorg Med Chem Lett. 2004 Oct 4;14(19):4861-6. doi: 10.1016/j.bmcl.2004.07.049. Bioorg Med Chem Lett. 2004. PMID: 15341940
2,5-Disubstituted pyrrolidine carboxylates as potent, orally active sphingosine-1-phosphate (S1P) receptor agonists.
Colandrea VJ, Legiec IE, Huo P, Yan L, Hale JJ, Mills SG, Bergstrom J, Card D, Chebret G, Hajdu R, Keohane CA, Milligan JA, Rosenbach MJ, Shei GJ, Mandala SM. Colandrea VJ, et al. Among authors: yan l. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2905-8. doi: 10.1016/j.bmcl.2006.03.038. Epub 2006 Mar 31. Bioorg Med Chem Lett. 2006. PMID: 16580205
Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P1) receptor.
Vachal P, Toth LM, Hale JJ, Yan L, Mills SG, Chrebet GL, Koehane CA, Hajdu R, Milligan JA, Rosenbach MJ, Mandala S. Vachal P, et al. Among authors: yan l. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3684-7. doi: 10.1016/j.bmcl.2006.04.064. Epub 2006 May 6. Bioorg Med Chem Lett. 2006. PMID: 16682185
Discovery of 3-arylpropionic acids as potent agonists of sphingosine-1-phosphate receptor-1 (S1P1) with high selectivity against all other known S1P receptor subtypes.
Yan L, Huo P, Doherty G, Toth L, Hale JJ, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Chrebet G, Bergstrom J, Card D, Quackenbush E, Wickham A, Mandala SM. Yan L, et al. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3679-83. doi: 10.1016/j.bmcl.2006.04.084. Epub 2006 May 11. Bioorg Med Chem Lett. 2006. PMID: 16697189
Pyrrolidine amides of pyrazolodihydropyrimidines as potent and selective KV1.5 blockers.
Lloyd J, Finlay HJ, Vacarro W, Hyunh T, Kover A, Bhandaru R, Yan L, Atwal K, Conder ML, Jenkins-West T, Shi H, Huang C, Li D, Sun H, Levesque P. Lloyd J, et al. Among authors: yan l. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1436-9. doi: 10.1016/j.bmcl.2009.12.085. Epub 2010 Jan 4. Bioorg Med Chem Lett. 2010. PMID: 20097068
Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.
Yan L, Huo P, Debenham JS, Madsen-Duggan CB, Lao J, Chen RZ, Xiao JC, Shen CP, Stribling DS, Shearman LP, Strack AM, Tsou N, Ball RG, Wang J, Tong X, Bateman TJ, Reddy VB, Fong TM, Hale JJ. Yan L, et al. J Med Chem. 2010 May 27;53(10):4028-37. doi: 10.1021/jm100023j. J Med Chem. 2010. PMID: 20423086
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