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4,4-Disubstituted piperidine high-affinity NK1 antagonists: structure-activity relationships and in vivo activity.
Stevenson GI, Huscroft I, MacLeod AM, Swain CJ, Cascieri MA, Chicchi GG, Graham MI, Harrison T, Kelleher FJ, Kurtz M, Ladduwahetty T, Merchant KJ, Metzger JM, MacIntyre DE, Sadowski S, Sohal B, Owens AP. Stevenson GI, et al. Among authors: cascieri ma. J Med Chem. 1998 Nov 5;41(23):4623-35. doi: 10.1021/jm980376b. J Med Chem. 1998. PMID: 9804702
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
4,4-Disubstituted piperidines: a new class of NK1 antagonist.
Stevenson GI, MacLeod AM, Huscroft I, Cascieri MA, Sadowski S, Baker R. Stevenson GI, et al. Among authors: cascieri ma. J Med Chem. 1995 Apr 14;38(8):1264-6. doi: 10.1021/jm00008a003. J Med Chem. 1995. PMID: 7731011 No abstract available.
135 results