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Page 1
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: finke pe. 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 1: discovery and initial SAR.
Finke PE, Meurer LC, Levorse DA, Mills SG, Maccoss M, Sadowski S, Cascieri MA, Tsao KL, Chicchi GG, Metzger JM, Macintyre DE. Finke PE, et al. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4497-503. doi: 10.1016/j.bmcl.2006.06.035. Epub 2006 Jul 7. Bioorg Med Chem Lett. 2006. PMID: 16824752
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: finke pe. 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
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: finke pe. J Med Chem. 2000 Mar 23;43(6):1234-41. doi: 10.1021/jm990617v. J Med Chem. 2000. PMID: 10737756
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: finke pe. 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
Syntheses and biological evaluation of 5-(piperidin-1-yl)-3-phenyl-pentylsulfones as CCR5 antagonists.
Shankaran K, Donnelly KL, Shah SK, Caldwell CG, Chen P, Finke PE, Oates B, MacCoss M, Mills SG, DeMartino JA, Gould SL, Malkowitz L, Siciliano SJ, Springer MS, Kwei G, Carella A, Carver G, Danzeisen R, Hazuda D, Holmes K, Kessler J, Lineberger J, Miller MD, Emini EA, Schleif WA. Shankaran K, et al. Among authors: finke pe. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3589-93. doi: 10.1016/j.bmcl.2004.03.112. Bioorg Med Chem Lett. 2004. PMID: 15177481
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: finke pe. 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: finke pe. 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
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure-activity relationships for substituted 2-Aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes.
Finke PE, Meurer LC, Oates B, 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. Finke PE, et al. Bioorg Med Chem Lett. 2001 Jan 22;11(2):265-70. doi: 10.1016/s0960-894x(00)00639-9. Bioorg Med Chem Lett. 2001. PMID: 11206474
44 results