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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: cascieri ma. J Med Chem. 2000 Mar 23;43(6):1234-41. doi: 10.1021/jm990617v. J Med Chem. 2000. PMID: 10737756
Spirocyclic NK(1) antagonists II: [4.5]-spiroethers.
Williams BJ, Cascieri MA, Chicchi GG, Harrison T, Owens AP, Owen SN, Rupniak NM, Tattersall DF, Williams A, Swain CJ. Williams BJ, et al. Among authors: cascieri ma. Bioorg Med Chem Lett. 2002 Oct 7;12(19):2719-22. doi: 10.1016/s0960-894x(02)00509-7. Bioorg Med Chem Lett. 2002. PMID: 12217362
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. Among authors: cascieri ma. 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: cascieri ma. 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
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. Neuropharmacology. 2000 Feb 14;39(4):652-63. doi: 10.1016/s0028-3908(99)00172-0. Neuropharmacology. 2000. PMID: 10728886
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: cascieri ma. J Med Chem. 1996 Apr 26;39(9):1760-2. doi: 10.1021/jm950654w. J Med Chem. 1996. PMID: 8627597 No abstract available.
N-heteroaryl-2-phenyl-3-(benzyloxy)piperidines: a novel class of potent orally active human NK1 antagonists.
Ladduwahetty T, Baker R, Cascieri MA, Chambers MS, Haworth K, Keown LE, MacIntyre DE, Metzger JM, Owen S, Rycroft W, Sadowski S, Seward EM, Shepheard SL, Swain CJ, Tattersall FD, Watt AP, Williamson DW, Hargreaves RJ. Ladduwahetty T, et al. Among authors: cascieri ma. J Med Chem. 1996 Jul 19;39(15):2907-14. doi: 10.1021/jm9506534. J Med Chem. 1996. PMID: 8709125
135 results