N-(5-Chloro-2-(hydroxymethyl)-N-alkyl-arylsulfonamides as γ-secretase inhibitors

Bioorganic & Medicinal Chemistry Letters - Tập 17 - Trang 4432-4436 - 2007
Michael F. Parker1, Donna M. Barten2, Carl P. Bergstrom1, Joanne J. Bronson1, Jason A. Corsa2, Milind S. Deshpande1, Kevin M. Felsenstein2, Valerie L. Guss2, Steven B. Hansel3, Graham Johnson1, Daniel J. Keavy1, Wai Y. Lau1, Jeremy Mock1, C.V.C. Prasad1, Craig T. Polson2, Charles P. Sloan1, David W. Smith1, Owen B. Wallace1, Henry H. Wang1, Andrew Williams1
1Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA
2Department of Neuroscience Biology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA
3Department of Drug Metabolism and Pharmacokinetics, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA

Tài liệu tham khảo

Clark, 2003, Ann. Intern. Med., 138, 400, 10.7326/0003-4819-138-5-200303040-00010 Hardy, 1992, Science, 256, 184, 10.1126/science.1566067 Olson, 2001, Curr. Opin. Drug. Disc. Dev., 4, 390 Walsh, 2002, Nature, 416, 535, 10.1038/416535a Selkow, 1988, Proc. Natl. Acad. Sci. U.S.A., 85, 7341, 10.1073/pnas.85.19.7341 Esler, 2001, Science, 293, 1449, 10.1126/science.1064638 Transfected H4 (human neuroglioma) cells stably expressing APP constructs were used to evaluate compounds. The Aβ produced was detected by an ELISA. See Smith, D. W.; Munoz, B.; Srinirvasan, K.; Bergstrom, C. P.; Chaturvedula, P. V.; Deshpande, M. S.; Keavy, D. J.; Lau, W. Y.; Parker, M. F.; Sloan, C. P.; Wallace, O. B.; Wang, H. H. WO 0050391. Smith, D. W.; Munoz, B.; Anderson, J.; Arruda, J.; Barten, D.; Baskin, P.; Bergstrom, C.; Corsa, J.; Felsenstein, K.; Guss, V.; Holtz, G.; Hu, Y.; Kounnas, M.; Lau, W.; Loo, A.; Noonan, J.; Parker, M.; Polson, C.; Roberts, S.; Roope, J.; Sloan, C.; Srinivasan, K.; Tomlinson, R.; Tran, T.; Wagner, S.; Wallace, O.; Wang, B.; Wang, R.; Wong, J.; Yang, F. Abstracts of Papers, 228th ACS National Meeting, Philadelphia, PA, United States, August 22–26, 2004, MEDI-337, AN 2004:658199. Roberts, S. B.; Hendrick, J. P.; Vinitsky, A.; Lewis, M.; Smith, D. W.; Pak, R. Isolation of a functionally active γ-secretase presenilin 1 complex and fluorescence assay for γ-secretase activity and inhibitors. PCT Int. Appl. WO01/75435A2. Zhang, 2001, Biochemistry, 40, 5049, 10.1021/bi0028800 Barten, 2005, J. Pharmacol. Exp. Ther., 312, 635, 10.1124/jpet.104.075408