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Page 1
Tetrahydroindolizinone NK1 antagonists.
Bao J, Lu H, Morriello GJ, Carlson EJ, Wheeldon A, Chicchi GG, Kurtz MM, Tsao KL, Zheng S, Tong X, Mills SG, DeVita RJ. Bao J, et al. Among authors: chicchi gg. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2354-8. doi: 10.1016/j.bmcl.2010.01.120. Epub 2010 Feb 1. Bioorg Med Chem Lett. 2010. PMID: 20188553
Substituted fused bicyclic pyrrolizinones as potent, orally bioavailable hNK1 antagonists.
Morriello GJ, Mills SG, Johnson T, Reibarkh M, Chicchi G, DeMartino J, Kurtz M, Davies P, Tsao KL, Zheng S, Tong X, Carlson E, Townson K, Tattersall FD, Wheeldon A, Boyce S, Collinson N, Rupniak N, Moore S, DeVita RJ. Morriello GJ, et al. Bioorg Med Chem Lett. 2010 Mar 15;20(6):2007-12. doi: 10.1016/j.bmcl.2010.01.065. Epub 2010 Jan 20. Bioorg Med Chem Lett. 2010. PMID: 20153964
2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways.
Kassick AJ, Jiang J, Bunda J, Wilson D, Bao J, Lu H, Lin P, Ball RG, Doss GA, Tong X, Tsao KL, Wang H, Chicchi G, Karanam B, Tschirret-Guth R, Samuel K, Hora DF, Kumar S, Madeira M, Eng W, Hargreaves R, Purcell M, Gantert L, Cook J, DeVita RJ, Mills SG. Kassick AJ, et al. J Med Chem. 2013 Jul 25;56(14):5940-8. doi: 10.1021/jm400751p. Epub 2013 Jul 9. J Med Chem. 2013. PMID: 23808489
4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists II.
Cooper LC, Carlson EJ, Castro JL, Chicchi GG, Dinnell K, Di Salvo J, Elliott JM, Hollingworth GJ, Kurtz MM, Ridgill MP, Rycroft W, Tsao KL, Swain CJ. Cooper LC, et al. Among authors: chicchi gg. Bioorg Med Chem Lett. 2002 Jul 8;12(13):1759-62. doi: 10.1016/s0960-894x(02)00250-0. Bioorg Med Chem Lett. 2002. PMID: 12067555
Novel lactam NK1 antagonists with anti-emetic activity.
Hollingworth GJ, Carlson EJ, Castro JL, Chicchi GG, Clark N, Cooper LC, Dirat O, Salvo JD, Elliott JM, Kilburn R, Kurtz MM, Rycroft W, Tattersall FD, Tsao KL, Swain CJ. Hollingworth GJ, et al. Among authors: chicchi gg. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1197-201. doi: 10.1016/j.bmcl.2005.11.111. Epub 2005 Dec 27. Bioorg Med Chem Lett. 2006. PMID: 16384700
NK1 antagonists based on seven membered lactam scaffolds.
Elliott JM, Carlson EJ, Chicchi GG, Dirat O, Dominguez M, Gerhard U, Jelley R, Jones AB, Kurtz MM, Tsao Kl, Wheeldon A. Elliott JM, et al. Among authors: chicchi gg. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2929-32. doi: 10.1016/j.bmcl.2006.02.080. Epub 2006 Mar 29. Bioorg Med Chem Lett. 2006. PMID: 16574413
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.
Finke PE, Meurer LC, Levorse DA, Mills SG, Maccoss M, Sadowski S, Cascieri MA, Tsao KL, Chicchi GG, Metzger JM, Macintyre DE. Finke PE, et al. Among authors: chicchi gg. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4497-503. doi: 10.1016/j.bmcl.2006.06.035. Epub 2006 Jul 7. Bioorg Med Chem Lett. 2006. PMID: 16824752
75 results