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Page 1
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: mills sg. J Med Chem. 2000 Mar 23;43(6):1234-41. doi: 10.1021/jm990617v. J Med Chem. 2000. PMID: 10737756
2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist.
Hale JJ, Mills SG, MacCoss M, Shah SK, Qi H, Mathre DJ, Cascieri MA, Sadowski S, Strader CD, MacIntyre DE, Metzger JM. Hale JJ, et al. Among authors: mills sg. J Med Chem. 1996 Apr 26;39(9):1760-2. doi: 10.1021/jm950654w. J Med Chem. 1996. PMID: 8627597 No abstract available.
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: mills sg. J Med Chem. 1998 Nov 5;41(23):4607-14. doi: 10.1021/jm980299k. J Med Chem. 1998. PMID: 9804700
The novel NK1 receptor antagonist MK-0869 (L-754,030) and its water soluble phosphoryl prodrug, L-758,298, inhibit acute and delayed cisplatin-induced emesis in ferrets.
Tattersall FD, Rycroft W, Cumberbatch M, Mason G, Tye S, Williamson DJ, Hale JJ, Mills SG, Finke PE, MacCoss M, Sadowski S, Ber E, Cascieri M, Hill RG, MacIntyre DE, Hargreaves RJ. Tattersall FD, et al. Among authors: mills sg. Neuropharmacology. 2000 Feb 14;39(4):652-63. doi: 10.1016/s0028-3908(99)00172-0. Neuropharmacology. 2000. PMID: 10728886
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanes.
Dorn CP, Finke PE, Oates B, Budhu RJ, Mills SG, MacCoss M, Malkowitz L, Springer MS, Daugherty BL, Gould SL, DeMartino JA, Siciliano SJ, Carella A, Carver G, Holmes K, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Schleif WA, Emini EA. Dorn CP, et al. Among authors: mills sg. Bioorg Med Chem Lett. 2001 Jan 22;11(2):259-64. doi: 10.1016/s0960-894x(00)00637-5. Bioorg Med Chem Lett. 2001. PMID: 11206473
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity.
Hale JJ, Budhu RJ, Holson EB, Finke PE, Oates B, Mills SG, MacCoss M, Gould SL, DeMartino JA, Springer MS, Siciliano S, Malkowitz L, Schleif WA, Hazuda D, Miller M, Kessler J, Danzeisen R, Holmes K, Lineberger J, Carella A, Carver G, Emini E. Hale JJ, et al. Among authors: mills sg. Bioorg Med Chem Lett. 2001 Oct 22;11(20):2741-5. doi: 10.1016/s0960-894x(01)00545-5. Bioorg Med Chem Lett. 2001. PMID: 11591514
Distinct mechanism for antidepressant activity by blockade of central substance P receptors.
Kramer MS, Cutler N, Feighner J, Shrivastava R, Carman J, Sramek JJ, Reines SA, Liu G, Snavely D, Wyatt-Knowles E, Hale JJ, Mills SG, MacCoss M, Swain CJ, Harrison T, Hill RG, Hefti F, Scolnick EM, Cascieri MA, Chicchi GG, Sadowski S, Williams AR, Hewson L, Smith D, Carlson EJ, Hargreaves RJ, Rupniak NM. Kramer MS, et al. Among authors: mills sg. Science. 1998 Sep 11;281(5383):1640-5. doi: 10.1126/science.281.5383.1640. Science. 1998. PMID: 9733503 Clinical Trial.
87 results