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Page 1
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
Hale JJ, Lynch CL, Neway W, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Parent SA, Chrebet G, Bergstrom J, Card D, Ferrer M, Hodder P, Strulovici B, Rosen H, Mandala S. Hale JJ, et al. J Med Chem. 2004 Dec 30;47(27):6662-5. doi: 10.1021/jm0492507. J Med Chem. 2004. PMID: 15615513
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds.
Shen DM, Shu M, Willoughby CA, Shah S, Lynch CL, Hale JJ, Mills SG, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Lyons K, Pivnichny JV, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA. Shen DM, et al. Among authors: hale jj. Bioorg Med Chem Lett. 2004 Feb 23;14(4):941-5. doi: 10.1016/j.bmcl.2003.12.005. Bioorg Med Chem Lett. 2004. PMID: 15012998
Selecting against S1P3 enhances the acute cardiovascular tolerability of 3-(N-benzyl)aminopropylphosphonic acid S1P receptor agonists.
Hale JJ, Doherty G, Toth L, Mills SG, Hajdu R, Keohane CA, Rosenbach M, Milligan J, Shei GJ, Chrebet G, Bergstrom J, Card D, Forrest M, Sun SY, West S, Xie H, Nomura N, Rosen H, Mandala S. Hale JJ, et al. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3501-5. doi: 10.1016/j.bmcl.2004.04.070. Bioorg Med Chem Lett. 2004. PMID: 15177461
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. Among authors: hale jj. 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
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: hale jj. J Med Chem. 2005 Oct 6;48(20):6169-73. doi: 10.1021/jm0503244. J Med Chem. 2005. PMID: 16190743
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: hale jj. 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
93 results