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Page 1
The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists.
Lin LS, Kopka IE, Mumford RA, Magriotis PA, Lanza T Jr, Durette PL, Kamenecka T, Young DN, de Laszlo SE, McCauley E, Riper GV, Kidambi U, Egger LA, Tong X, Lyons K, Vincent S, Stearns R, Colletti A, Teffera Y, Fenyk-Melody J, Schmidt JA, MacCoss M, Hagmann WK. Lin LS, et al. Among authors: stearns r. Bioorg Med Chem Lett. 2002 Feb 25;12(4):611-4. doi: 10.1016/s0960-894x(01)00818-6. Bioorg Med Chem Lett. 2002. PMID: 11844683
Substituted N-(3,5-dichlorobenzenesulfonyl)-L-prolyl-phenylalanine analogues as potent VLA-4 antagonists.
Kopka IE, Young DN, Lin LS, Mumford RA, Magriotis PA, MacCoss M, Mills SG, Van Riper G, McCauley E, Egger LE, Kidambi U, Schmidt JA, Lyons K, Stearns R, Vincent S, Colletti A, Wang Z, Tong S, Wang J, Zheng S, Owens K, Levorse D, Hagmann WK. Kopka IE, et al. Among authors: stearns r. Bioorg Med Chem Lett. 2002 Feb 25;12(4):637-40. doi: 10.1016/s0960-894x(01)00821-6. Bioorg Med Chem Lett. 2002. PMID: 11844689
Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists.
Kopka IE, Lin LS, Mumford RA, Lanza T Jr, Magriotis PA, Young D, DeLaszlo SE, MacCoss M, Mills SG, Van Riper G, McCauley E, Lyons K, Vincent S, Egger LA, Kidambi U, Stearns R, Colletti A, Teffera Y, Tong S, Owens K, Levorse D, Schmidt JA, Hagmann WK. Kopka IE, et al. Among authors: stearns r. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2415-8. doi: 10.1016/s0960-894x(02)00460-2. Bioorg Med Chem Lett. 2002. PMID: 12161146
Amidines as amide bond replacements in VLA-4 antagonists.
Kamenecka TM, Park YJ, Lin LS, de Laszlo S, McCauley ED, Van Riper G, Egger L, Kidambi U, Mumford RA, Tong S, Tang W, Colletti A, Teffera Y, Stearns R, MacCoss M, Schmidt JA, Hagmann WK. Kamenecka TM, et al. Among authors: stearns r. Bioorg Med Chem Lett. 2004 May 3;14(9):2323-6. doi: 10.1016/j.bmcl.2004.01.100. Bioorg Med Chem Lett. 2004. PMID: 15081033
The discovery of sulfonylated dipeptides as potent VLA-4 antagonists.
Hagmann WK, Durette PL, Lanza T, Kevin NJ, de Laszlo SE, Kopka IE, Young D, Magriotis PA, Li B, Lin LS, Yang G, Kamenecka T, Chang LL, Wilson J, MacCoss M, Mills SG, Van Riper G, McCauley E, Egger LA, Kidambi U, Lyons K, Vincent S, Stearns R, Colletti A, Teffera J, Tong S, Fenyk-Melody J, Owens K, Levorse D, Kim P, Schmidt JA, Mumford RA. Hagmann WK, et al. Among authors: stearns r. Bioorg Med Chem Lett. 2001 Oct 22;11(20):2709-13. doi: 10.1016/s0960-894x(01)00544-3. Bioorg Med Chem Lett. 2001. PMID: 11591507
Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist.
Hong Q, Bakshi RK, Palucki BL, Park MK, Ye Z, He S, Pollard PG, Sebhat IK, Liu J, Guo L, Cashen DE, Martin WJ, Weinberg DH, MacNeil T, Tang R, Tamvakopoulos C, Peng Q, Miller RR, Stearns RA, Chen HY, Chen AS, Strack AM, Fong TM, MacIntyre DE, Wyvratt MJ, Nargund RP. Hong Q, et al. Among authors: stearns ra. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2330-4. doi: 10.1016/j.bmcl.2011.02.090. Epub 2011 Mar 1. Bioorg Med Chem Lett. 2011. PMID: 21439820
Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.
He S, Ye Z, Dobbelaar PH, Sebhat IK, Guo L, Liu J, Jian T, Lai Y, Franklin CL, Bakshi RK, Dellureficio JP, Hong Q, Tsou NN, Ball RG, Cashen DE, Martin WJ, Weinberg DH, Macneil T, Tang R, Tamvakopoulos C, Peng Q, Miller RR, Stearns RA, Chen HY, Chen AS, Strack AM, Fong TM, Macintyre DE, Wyvratt MJ Jr, Nargund RP. He S, et al. Among authors: stearns ra. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2106-10. doi: 10.1016/j.bmcl.2010.02.058. Epub 2010 Feb 19. Bioorg Med Chem Lett. 2010. PMID: 20207541
Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.
Feng DD, Biftu T, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Strader CD, Tota L, Wyvratt MJ, Fisher MH, Weber AE. Feng DD, et al. Among authors: stearns ra. Bioorg Med Chem Lett. 2000 Jul 3;10(13):1427-9. doi: 10.1016/s0960-894x(00)00267-5. Bioorg Med Chem Lett. 2000. PMID: 10888324
247 results