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Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.
Jiang J, Bunda JL, Doss GA, Chicchi GG, Kurtz MM, Tsao KL, Tong X, Zheng S, Upthagrove A, Samuel K, Tschirret-Guth R, Kumar S, Wheeldon A, Carlson EJ, Hargreaves R, Burns D, Hamill T, Ryan C, Krause SM, Eng W, DeVita RJ, Mills SG. Jiang J, et al. Among authors: kurtz mm. J Med Chem. 2009 May 14;52(9):3039-46. doi: 10.1021/jm8016514. J Med Chem. 2009. PMID: 19354254
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
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: kurtz mm. 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: kurtz mm. 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: kurtz mm. 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
The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine.
Lin P, Chang L, Devita RJ, Young JR, Eid R, Tong X, Zheng S, Ball RG, Tsou NN, Chicchi GG, Kurtz MM, Tsao KL, Wheeldon A, Carlson EJ, Eng W, Burns HD, Hargreaves RJ, Mills SG. Lin P, et al. Among authors: kurtz mm. Bioorg Med Chem Lett. 2007 Sep 15;17(18):5191-8. doi: 10.1016/j.bmcl.2007.06.085. Epub 2007 Jul 4. Bioorg Med Chem Lett. 2007. PMID: 17637506
Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.
Young JR, Eid R, Turner C, DeVita RJ, Kurtz MM, Tsao KL, Chicchi GG, Wheeldon A, Carlson E, Mills SG. Young JR, et al. Among authors: kurtz mm. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5310-5. doi: 10.1016/j.bmcl.2007.08.028. Epub 2007 Aug 16. Bioorg Med Chem Lett. 2007. PMID: 17723300
99 results