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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. Among authors: devita rj. J Med Chem. 2013 Jul 25;56(14):5940-8. doi: 10.1021/jm400751p. Epub 2013 Jul 9. J Med Chem. 2013. PMID: 23808489
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: devita rj. 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
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: devita rj. 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
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: devita rj. J Med Chem. 2009 May 14;52(9):3039-46. doi: 10.1021/jm8016514. J Med Chem. 2009. PMID: 19354254
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: devita rj. 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
Fused tricyclic pyrrolizinones that exhibit pseudo-irreversible blockade of the NK1 receptor.
Morriello GJ, Chicchi G, Johnson T, Mills SG, Demartino J, Kurtz M, Tsao KL, Zheng S, Tong X, Carlson E, Townson K, Wheeldon A, Boyce S, Collinson N, Rupniak N, Devita RJ. Morriello GJ, et al. Among authors: devita rj. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5925-32. doi: 10.1016/j.bmcl.2010.07.058. Epub 2010 Jul 19. Bioorg Med Chem Lett. 2010. PMID: 20729082
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: devita rj. 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
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. Among authors: devita rj. 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
Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase.
Liu P, Hamill TG, Chioda M, Chobanian H, Fung S, Guo Y, Chang L, Bakshi R, Hong Q, Dellureficio J, Lin LS, Abbadie C, Alexander J, Jin H, Mandala S, Shiao LL, Li W, Sanabria S, Williams D, Zeng Z, Hajdu R, Jochnowitz N, Rosenbach M, Karanam B, Madeira M, Salituro G, Powell J, Xu L, Terebetski JL, Leone JF, Miller P, Cook J, Holahan M, Joshi A, O'Malley S, Purcell M, Posavec D, Chen TB, Riffel K, Williams M, Hargreaves R, Sullivan KA, Nargund RP, DeVita RJ. Liu P, et al. Among authors: devita rj. ACS Med Chem Lett. 2013 Apr 20;4(6):509-13. doi: 10.1021/ml4000996. eCollection 2013 Jun 13. ACS Med Chem Lett. 2013. PMID: 24900701 Free PMC article.
4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists.
Jiang J, Lin P, Hoang M, Chang L, Tan C, Feighner S, Palyha OC, Hreniuk DL, Pan J, Sailer AW, Morin NR, MacNeil DJ, Howard AD, Van der Ploeg LH, Goulet MT, DeVita RJ. Jiang J, et al. Among authors: devita rj. Bioorg Med Chem Lett. 2006 Oct 15;16(20):5275-9. doi: 10.1016/j.bmcl.2006.08.008. Epub 2006 Aug 17. Bioorg Med Chem Lett. 2006. PMID: 16919453
70 results