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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: jiang j. J Med Chem. 2013 Jul 25;56(14):5940-8. doi: 10.1021/jm400751p. Epub 2013 Jul 9. J Med Chem. 2013. PMID: 23808489
A potent, nonpeptidyl 1H-quinolone antagonist for the gonadotropin-releasing hormone receptor.
DeVita RJ, Walsh TF, Young JR, Jiang J, Ujjainwalla F, Toupence RB, Parikh M, Huang SX, Fair JA, Goulet MT, Wyvratt MJ, Lo JL, Ren N, Yudkovitz JB, Yang YT, Cheng K, Cui J, Mount G, Rohrer SP, Schaeffer JM, Rhodes L, Drisko JE, McGowan E, MacIntyre DE, Vincent S, Carlin JR, Cameron J, Smith RG. DeVita RJ, et al. Among authors: jiang j. J Med Chem. 2001 Mar 15;44(6):917-22. doi: 10.1021/jm000275p. J Med Chem. 2001. PMID: 11300873
Identification of neutral 4-O-alkyl quinolone nonpeptide GnRH receptor antagonists.
DeVita RJ, Parikh M, Jiang J, Fair JA, Young JR, Walsh TF, Goulet MT, Lo JL, Ren N, Yudkovitz JB, Cui J, Yang YT, Cheng K, Rohrer SP, Wyvratt MJ. DeVita RJ, et al. Among authors: jiang j. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5599-603. doi: 10.1016/j.bmcl.2004.08.056. Bioorg Med Chem Lett. 2004. PMID: 15482932
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. 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
2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists.
Jiang J, Hoang M, Young JR, Chaung D, Eid R, Turner C, Lin P, Tong X, Wang J, Tan C, Feighner S, Palyha O, Hreniuk DL, Pan J, Sailer AW, MacNeil DJ, Howard A, Shearman L, Stribling S, Camacho R, Strack A, Van der Ploeg LH, Goulet MT, DeVita RJ. Jiang J, et al. Bioorg Med Chem Lett. 2006 Oct 15;16(20):5270-4. doi: 10.1016/j.bmcl.2006.08.006. Epub 2006 Aug 17. Bioorg Med Chem Lett. 2006. PMID: 16919456
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. J Med Chem. 2009 May 14;52(9):3039-46. doi: 10.1021/jm8016514. J Med Chem. 2009. PMID: 19354254
Discovery of benzodihydroisofurans as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase inhibitors.
Shen HC, Ding FX, Jiang J, Verras A, Chabin RM, Xu S, Tong X, Chen Q, Xie D, Lassman ME, Bhatt UR, Garcia-Calvo MM, Geissler W, Shen Z, Murphy BA, Gorski JN, Wiltsie J, SinhaRoy R, Hale JJ, Pinto S, Shen DM. Shen HC, et al. Among authors: jiang j. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1550-6. doi: 10.1016/j.bmcl.2012.01.002. Epub 2012 Jan 10. Bioorg Med Chem Lett. 2012. PMID: 22264488
Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold.
Zhu Y, de Jesus RK, Tang H, Walsh SP, Jiang J, Gu X, Teumelsan N, Shahripour A, Pio B, Ding FX, Ha S, Priest BT, Swensen AM, Alonso-Galicia M, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Zhou X, Pai LY, Hampton C, Hernandez M, Owens K, Ehrhart J, Roy S, Kaczorowski GJ, Yang L, Parmee ER, Sullivan K, Garcia ML, Pasternak A. Zhu Y, et al. Among authors: jiang j. Bioorg Med Chem Lett. 2016 Dec 1;26(23):5695-5702. doi: 10.1016/j.bmcl.2016.10.064. Epub 2016 Oct 24. Bioorg Med Chem Lett. 2016. PMID: 27839686
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