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Page 1
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
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
Spirocyclic NK(1) antagonists II: [4.5]-spiroethers.
Williams BJ, Cascieri MA, Chicchi GG, Harrison T, Owens AP, Owen SN, Rupniak NM, Tattersall DF, Williams A, Swain CJ. Williams BJ, et al. Among authors: chicchi gg. Bioorg Med Chem Lett. 2002 Oct 7;12(19):2719-22. doi: 10.1016/s0960-894x(02)00509-7. Bioorg Med Chem Lett. 2002. PMID: 12217362
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
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
Meurer LC, Finke PE, Owens KA, Tsou NN, Ball RG, Mills SG, Maccoss M, Sadowski S, Cascieri MA, Tsao KL, Chicchi GG, Egger LA, Luell S, Metzger JM, Macintyre DE, Rupniak NM, Williams AR, Hargreaves RJ. Meurer LC, et al. Among authors: chicchi gg. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4504-11. doi: 10.1016/j.bmcl.2006.06.044. Epub 2006 Jul 10. Bioorg Med Chem Lett. 2006. PMID: 16831551
Fused bicyclic pyrrolizinones as new scaffolds for human NK1 antagonists.
Morriello GJ, Devita RJ, Mills SG, Young JR, Lin P, Doss G, Chicchi GG, Demartino J, Kurtz MM, Tsao KL, Carlson E, Townson K, Wheeldon A, Boyce S, Collinson N, Rupniak N, Moore S. Morriello GJ, et al. Among authors: chicchi gg. Bioorg Med Chem. 2008 Mar 1;16(5):2156-70. doi: 10.1016/j.bmc.2007.11.081. Epub 2007 Dec 5. Bioorg Med Chem. 2008. PMID: 18248994
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
4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists I.
Elliott JM, Castro JL, Chicchi GG, Cooper LC, Dinnell K, Hollingworth GJ, Ridgill MP, Rycroft W, Kurtz MM, Shaw DE, Swain CJ, Tsao KL, Yang L. Elliott JM, et al. Among authors: chicchi gg. Bioorg Med Chem Lett. 2002 Jul 8;12(13):1755-8. doi: 10.1016/s0960-894x(02)00249-4. Bioorg Med Chem Lett. 2002. PMID: 12067554
75 results