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Page 1
Discovery of novel triazolobenzazepinones as γ-secretase modulators with central Aβ42 lowering in rodents and rhesus monkeys.
Fischer C, Zultanski SL, Zhou H, Methot JL, Shah S, Hayashi I, Hughes BL, Moxham CM, Bays NW, Smotrov N, Hill AD, Pan BS, Wu Z, Moy LY, Tanga F, Kenific C, Cruz JC, Walker D, Bouthillette M, Nikov GN, Deshmukh SV, Jeliazkova-Mecheva VV, Diaz D, Michener MS, Cook JJ, Munoz B, Shearman MS. Fischer C, et al. Among authors: shearman ms. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3488-94. doi: 10.1016/j.bmcl.2015.07.003. Epub 2015 Jul 9. Bioorg Med Chem Lett. 2015. PMID: 26212776
Fluorinated piperidine acetic acids as gamma-secretase modulators.
Stanton MG, Hubbs J, Sloman D, Hamblett C, Andrade P, Angagaw M, Bi G, Black RM, Crispino J, Cruz JC, Fan E, Farris G, Hughes BL, Kenific CM, Middleton RE, Nikov G, Sajonz P, Shah S, Shomer N, Szewczak AA, Tanga F, Tudge MT, Shearman M, Munoz B. Stanton MG, et al. Bioorg Med Chem Lett. 2010 Jan 15;20(2):755-8. doi: 10.1016/j.bmcl.2009.11.034. Epub 2009 Nov 13. Bioorg Med Chem Lett. 2010. PMID: 20005099
Lead optimization of 4,4-biaryl piperidine amides as γ-secretase inhibitors.
Close J, Heidebrecht R Jr, Hendrix J, Li C, Munoz B, Surdi L, Kattar S, Tempest P, Moses P, Geng X, Hughes B, Smotrov N, Moxham C, Chapnick J, Kariv I, Nikov G, Burke JE, Deshmukh S, Jeliazkova-Mecheva V, Leach JK, Diaz D, Xu L, Yang Z, Kwei G, Moy L, Shah S, Tanga F, Kenefic C, Savage D, Shearman M, Ball RG, McNevin MJ, Markarewicz A, Miller T. Close J, et al. Bioorg Med Chem Lett. 2012 May 1;22(9):3203-7. doi: 10.1016/j.bmcl.2012.03.038. Epub 2012 Mar 17. Bioorg Med Chem Lett. 2012. PMID: 22483609
Piperazinyl pyrimidine derivatives as potent gamma-secretase modulators.
Rivkin A, Ahearn SP, Chichetti SM, Kim YR, Li C, Rosenau A, Kattar SD, Jung J, Shah S, Hughes BL, Crispino JL, Middleton RE, Szewczak AA, Munoz B, Shearman MS. Rivkin A, et al. Among authors: shearman ms. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1269-71. doi: 10.1016/j.bmcl.2009.11.101. Epub 2009 Nov 23. Bioorg Med Chem Lett. 2010. PMID: 20022243
Purine derivatives as potent gamma-secretase modulators.
Rivkin A, Ahearn SP, Chichetti SM, Hamblett CL, Garcia Y, Martinez M, Hubbs JL, Reutershan MH, Daniels MH, Siliphaivanh P, Otte KM, Li C, Rosenau A, Surdi LM, Jung J, Hughes BL, Crispino JL, Nikov GN, Middleton RE, Moxham CM, Szewczak AA, Shah S, Moy LY, Kenific CM, Tanga F, Cruz JC, Andrade P, Angagaw MH, Shomer NH, Miller T, Munoz B, Shearman MS. Rivkin A, et al. Among authors: shearman ms. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2279-82. doi: 10.1016/j.bmcl.2010.02.008. Epub 2010 Feb 6. Bioorg Med Chem Lett. 2010. PMID: 20207146
Quinazolinones as γ-secretase modulators.
Fischer C, Shah S, Hughes BL, Nikov GN, Crispino JL, Middleton RE, Szewczak AA, Munoz B, Shearman MS. Fischer C, et al. Among authors: shearman ms. Bioorg Med Chem Lett. 2011 Jan 15;21(2):773-6. doi: 10.1016/j.bmcl.2010.11.111. Epub 2010 Nov 26. Bioorg Med Chem Lett. 2011. PMID: 21190851
Triazoles as γ-secretase modulators.
Fischer C, Zultanski SL, Zhou H, Methot JL, Brown WC, Mampreian DM, Schell AJ, Shah S, Nuthall H, Hughes BL, Smotrov N, Kenific CM, Cruz JC, Walker D, Bouthillette M, Nikov GN, Savage DF, Jeliazkova-Mecheva VV, Diaz D, Szewczak AA, Bays N, Middleton RE, Munoz B, Shearman MS. Fischer C, et al. Among authors: shearman ms. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4083-7. doi: 10.1016/j.bmcl.2011.04.089. Epub 2011 May 4. Bioorg Med Chem Lett. 2011. PMID: 21616665
Triazoloamides as potent γ-secretase modulators with reduced hERG liability.
Fischer C, Zultanski SL, Zhou H, Methot JL, Shah S, Nuthall H, Hughes BL, Smotrov N, Hill A, Szewczak AA, Moxham CM, Bays N, Middleton RE, Munoz B, Shearman MS. Fischer C, et al. Among authors: shearman ms. Bioorg Med Chem Lett. 2012 May 1;22(9):3140-6. doi: 10.1016/j.bmcl.2012.03.054. Epub 2012 Mar 21. Bioorg Med Chem Lett. 2012. PMID: 22497762
Potent benzoazepinone γ-secretase modulators with improved bioavailability.
Methot JL, Fischer C, Li C, Rivkin A, Ahearn SP, Brown WC, Kattar S, Kelley E, Mampreian DM, Schell A, Rosenau A, Zhou H, Ball R, Deshmukh SV, Jeliazkova-Mecheva VV, Diaz D, Moy LY, Kenific CM, Moxham C, Shah S, Nuthall H, Szewczak AA, Hill A, Hughes B, Smotrov N, Munoz B, Miller TA, Shearman MS. Methot JL, et al. Among authors: shearman ms. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3495-500. doi: 10.1016/j.bmcl.2015.06.032. Epub 2015 Jun 15. Bioorg Med Chem Lett. 2015. PMID: 26142947
Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound.
Cook JJ, Wildsmith KR, Gilberto DB, Holahan MA, Kinney GG, Mathers PD, Michener MS, Price EA, Shearman MS, Simon AJ, Wang JX, Wu G, Yarasheski KE, Bateman RJ. Cook JJ, et al. Among authors: shearman ms. J Neurosci. 2010 May 12;30(19):6743-50. doi: 10.1523/JNEUROSCI.1381-10.2010. J Neurosci. 2010. PMID: 20463236 Free PMC article.
120 results