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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: hargreaves r. 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: hargreaves 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
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: hargreaves r. J Med Chem. 2009 May 14;52(9):3039-46. doi: 10.1021/jm8016514. J Med Chem. 2009. PMID: 19354254
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
Hale JJ, Mills SG, MacCoss M, Dorn CP, Finke PE, Budhu RJ, Reamer RA, Huskey SE, Luffer-Atlas D, Dean BJ, McGowan EM, Feeney WP, Chiu SH, Cascieri MA, Chicchi GG, Kurtz MM, Sadowski S, Ber E, Tattersall FD, Rupniak NM, Williams AR, Rycroft W, Hargreaves R, Metzger JM, MacIntyre DE. Hale JJ, et al. Among authors: hargreaves r. J Med Chem. 2000 Mar 23;43(6):1234-41. doi: 10.1021/jm990617v. J Med Chem. 2000. PMID: 10737756
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
Hale JJ, Mills SG, MacCoss M, Finke PE, Cascieri MA, Sadowski S, Ber E, Chicchi GG, Kurtz M, Metzger J, Eiermann G, Tsou NN, Tattersall FD, Rupniak NM, Williams AR, Rycroft W, Hargreaves R, MacIntyre DE. Hale JJ, et al. Among authors: hargreaves r. J Med Chem. 1998 Nov 5;41(23):4607-14. doi: 10.1021/jm980299k. J Med Chem. 1998. PMID: 9804700
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: hargreaves rj. 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
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: hargreaves r. 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.
Brain penetration of aprepitant, a substance P receptor antagonist, in ferrets.
Huskey SE, Dean BJ, Bakhtiar R, Sanchez RI, Tattersall FD, Rycroft W, Hargreaves R, Watt AP, Chicchi GG, Keohane C, Hora DF, Chiu SH. Huskey SE, et al. Among authors: hargreaves r. Drug Metab Dispos. 2003 Jun;31(6):785-91. doi: 10.1124/dmd.31.6.785. Drug Metab Dispos. 2003. PMID: 12756213
[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
Bell IM, Gallicchio SN, Stump CA, Bruno JG, Fan H, Gantert LT, Hostetler ED, Kemmerer AL, McWherter M, Moore EL, Mosser SD, Purcell ML, Riffel K, Salvatore CA, Sanabria-Bohórquez S, Staas DD, White RB, Williams M, Zartman CB, Cook JJ, Hargreaves RJ, Kane SA, Graham SL, Selnick HG. Bell IM, et al. ACS Med Chem Lett. 2013 Jul 18;4(9):863-8. doi: 10.1021/ml400199p. eCollection 2013 Sep 12. ACS Med Chem Lett. 2013. PMID: 24900761 Free PMC article.
Discovery of N-{(1S,2S)-2-(3-cyanophenyl)- 3-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylpropyl}- 2-methyl-2-[(5-methylpyridin-2-yl)oxy]propanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use.
Liu P, Lin LS, Hamill TG, Jewell JP, Lanza TJ Jr, Gibson RE, Krause SM, Ryan C, Eng W, Sanabria S, Tong X, Wang J, Levorse DA, Owens KA, Fong TM, Shen CP, Lao J, Kumar S, Yin W, Payack JF, Springfield SA, Hargreaves R, Burns HD, Goulet MT, Hagmann WK. Liu P, et al. Among authors: hargreaves r. J Med Chem. 2007 Jul 26;50(15):3427-30. doi: 10.1021/jm070131b. Epub 2007 Jul 3. J Med Chem. 2007. PMID: 17608398
306 results