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Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes.
Xiong Y, Guo J, Candelore MR, Liang R, Miller C, Dallas-Yang Q, Jiang G, McCann PE, Qureshi SA, Tong X, Xu SS, Shang J, Vincent SH, Tota LM, Wright MJ, Yang X, Zhang BB, Tata JR, Parmee ER. Xiong Y, et al. Among authors: vincent sh. J Med Chem. 2012 Jul 12;55(13):6137-48. doi: 10.1021/jm300579z. Epub 2012 Jun 28. J Med Chem. 2012. PMID: 22708876
Discovery of cyclic guanidines as potent, orally active, human glucagon receptor antagonists.
Sinz C, Chang J, Lins AR, Brady E, Candelore M, Dallas-Yang Q, Ding V, Jiang G, Lin Z, Mock S, Qureshi S, Salituro G, Saperstein R, Shang J, Szalkowski D, Tota L, Vincent S, Wright M, Xu S, Yang X, Zhang B, Tata J, Kim R, Parmee E. Sinz C, et al. Bioorg Med Chem Lett. 2011 Dec 1;21(23):7131-6. doi: 10.1016/j.bmcl.2011.09.085. Epub 2011 Sep 29. Bioorg Med Chem Lett. 2011. PMID: 22001094
Discovery of N-aryl-2-acylindole human glucagon receptor antagonists.
Sinz C, Bittner A, Brady E, Candelore M, Dallas-Yang Q, Ding V, Jiang G, Lin Z, Qureshi S, Salituro G, Saperstein R, Shang J, Szalkowski D, Tota L, Vincent S, Wright M, Xu S, Yang X, Zhang B, Tata J, Kim R, Parmee ER. Sinz C, et al. Bioorg Med Chem Lett. 2011 Dec 1;21(23):7124-30. doi: 10.1016/j.bmcl.2011.09.105. Epub 2011 Oct 5. Bioorg Med Chem Lett. 2011. PMID: 22030028
Discovery of N-{N-[(3-cyanophenyl)sulfonyl]-4(R)-cyclobutylamino-(L)-prolyl}-4-[(3',5'-dichloroisonicotinoyl) amino]-(L)-phenylalanine (MK-0668), an extremely potent and orally active antagonist of very late antigen-4.
Lin LS, Lanza T, Jewell JP, Liu P, Jones C, Kieczykowski GR, Treonze K, Si Q, Manior S, Koo G, Tong X, Wang J, Schuelke A, Pivnichny J, Wang R, Raab C, Vincent S, Davies P, Maccoss M, Mumford RA, Hagmann WK. Lin LS, et al. J Med Chem. 2009 Jun 11;52(11):3449-52. doi: 10.1021/jm900257b. J Med Chem. 2009. PMID: 19441819
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. 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
A potent, nonpeptidyl 1H-quinolone antagonist for the gonadotropin-releasing hormone receptor.
DeVita RJ, Walsh TF, Young JR, Jiang J, Ujjainwalla F, Toupence RB, Parikh M, Huang SX, Fair JA, Goulet MT, Wyvratt MJ, Lo JL, Ren N, Yudkovitz JB, Yang YT, Cheng K, Cui J, Mount G, Rohrer SP, Schaeffer JM, Rhodes L, Drisko JE, McGowan E, MacIntyre DE, Vincent S, Carlin JR, Cameron J, Smith RG. DeVita RJ, et al. J Med Chem. 2001 Mar 15;44(6):917-22. doi: 10.1021/jm000275p. J Med Chem. 2001. PMID: 11300873
Highly constrained bicyclic VLA-4 antagonists.
Chang LL, Truong Q, Doss GA, MacCoss M, Lyons K, McCauley E, Mumford R, Forrest G, Vincent S, Schmidt JA, Hagmann WK. Chang LL, et al. Bioorg Med Chem Lett. 2007 Feb 1;17(3):597-601. doi: 10.1016/j.bmcl.2006.11.011. Epub 2006 Nov 7. Bioorg Med Chem Lett. 2007. PMID: 17118652
Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity.
Ashton WT, Sisco RM, Kieczykowski GR, Yang YT, Yudkovitz JB, Cui J, Mount GR, Ren RN, Wu TJ, Shen X, Lyons KA, Mao AH, Carlin JR, Karanam BV, Vincent SH, Cheng K, Goulet MT. Ashton WT, et al. Among authors: vincent sh. Bioorg Med Chem Lett. 2001 Oct 8;11(19):2597-602. doi: 10.1016/s0960-894x(01)00512-1. Bioorg Med Chem Lett. 2001. PMID: 11551758
81 results