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Page 1
Cyclic sulfamide gamma-secretase inhibitors.
Sparey T, Beher D, Best J, Biba M, Castro JL, Clarke E, Hannam J, Harrison T, Lewis H, Madin A, Shearman M, Sohal B, Tsou N, Welch C, Wrigley J. Sparey T, et al. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4212-6. doi: 10.1016/j.bmcl.2005.06.084. Bioorg Med Chem Lett. 2005. PMID: 16054361
Quantitative measurement of changes in amyloid-beta(40) in the rat brain and cerebrospinal fluid following treatment with the gamma-secretase inhibitor LY-411575 [N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide].
Best JD, Jay MT, Otu F, Ma J, Nadin A, Ellis S, Lewis HD, Pattison C, Reilly M, Harrison T, Shearman MS, Williamson TL, Atack JR. Best JD, et al. Among authors: lewis hd. J Pharmacol Exp Ther. 2005 May;313(2):902-8. doi: 10.1124/jpet.104.081174. Epub 2005 Mar 2. J Pharmacol Exp Ther. 2005. PMID: 15743924
4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.
Churcher I, Beher D, Best JD, Castro JL, Clarke EE, Gentry A, Harrison T, Hitzel L, Kay E, Kerrad S, Lewis HD, Morentin-Gutierrez P, Mortishire-Smith R, Oakley PJ, Reilly M, Shaw DE, Shearman MS, Teall MR, Williams S, Wrigley JD. Churcher I, et al. Among authors: lewis hd. Bioorg Med Chem Lett. 2006 Jan 15;16(2):280-4. doi: 10.1016/j.bmcl.2005.10.009. Epub 2005 Nov 3. Bioorg Med Chem Lett. 2006. PMID: 16275079
The novel gamma secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) reduces amyloid plaque deposition without evidence of notch-related pathology in the Tg2576 mouse.
Best JD, Smith DW, Reilly MA, O'Donnell R, Lewis HD, Ellis S, Wilkie N, Rosahl TW, Laroque PA, Boussiquet-Leroux C, Churcher I, Atack JR, Harrison T, Shearman MS. Best JD, et al. Among authors: lewis hd. J Pharmacol Exp Ther. 2007 Feb;320(2):552-8. doi: 10.1124/jpet.106.114330. Epub 2006 Nov 10. J Pharmacol Exp Ther. 2007. PMID: 17099072
86 results