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Page 1
Robust Pharmacodynamic Effect of LY3202626, a Central Nervous System Penetrant, Low Dose BACE1 Inhibitor, in Humans and Nonclinical Species.
Willis BA, Lowe SL, Monk SA, Cocke PJ, Aluise CD, Boggs LN, Borders AR, Brier RA, Dean RA, Green SJ, James DE, Jhee SS, Lin Q, Lo AC, May PC, Watson BM, Winneroski LL, Yang Z, Zimmer JA, McKinzie DL, Mergott DJ. Willis BA, et al. Among authors: watson bm. J Alzheimers Dis Rep. 2022 Jan 11;6(1):1-15. doi: 10.3233/ADR-210037. eCollection 2022. J Alzheimers Dis Rep. 2022. PMID: 35243208 Free PMC article.
The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans.
May PC, Willis BA, Lowe SL, Dean RA, Monk SA, Cocke PJ, Audia JE, Boggs LN, Borders AR, Brier RA, Calligaro DO, Day TA, Ereshefsky L, Erickson JA, Gevorkyan H, Gonzales CR, James DE, Jhee SS, Komjathy SF, Li L, Lindstrom TD, Mathes BM, Martényi F, Sheehan SM, Stout SL, Timm DE, Vaught GM, Watson BM, Winneroski LL, Yang Z, Mergott DJ. May PC, et al. Among authors: watson bm. J Neurosci. 2015 Jan 21;35(3):1199-210. doi: 10.1523/JNEUROSCI.4129-14.2015. J Neurosci. 2015. PMID: 25609634 Free PMC article. Clinical Trial.
Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor.
McKinzie DL, Winneroski LL, Green SJ, Hembre EJ, Erickson JA, Willis BA, Monk SA, Aluise CD, Baker TK, Lopez JE, Hendle J, Beck JP, Brier RA, Boggs LN, Borders AR, Cocke PJ, Garcia-Losada P, Lowe SL, Mathes BM, May PC, Porter WJ, Stout SL, Timm DE, Watson BM, Yang Z, Mergott DJ. McKinzie DL, et al. Among authors: watson bm. J Med Chem. 2021 Jun 24;64(12):8076-8100. doi: 10.1021/acs.jmedchem.1c00489. Epub 2021 Jun 3. J Med Chem. 2021. PMID: 34081466
Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor.
May PC, Dean RA, Lowe SL, Martenyi F, Sheehan SM, Boggs LN, Monk SA, Mathes BM, Mergott DJ, Watson BM, Stout SL, Timm DE, Smith Labell E, Gonzales CR, Nakano M, Jhee SS, Yen M, Ereshefsky L, Lindstrom TD, Calligaro DO, Cocke PJ, Greg Hall D, Friedrich S, Citron M, Audia JE. May PC, et al. Among authors: watson bm. J Neurosci. 2011 Nov 16;31(46):16507-16. doi: 10.1523/JNEUROSCI.3647-11.2011. J Neurosci. 2011. PMID: 22090477 Free PMC article. Clinical Trial.
Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.
Winneroski LL, Schiffler MA, Erickson JA, May PC, Monk SA, Timm DE, Audia JE, Beck JP, Boggs LN, Borders AR, Boyer RD, Brier RA, Hudziak KJ, Klimkowski VJ, Garcia Losada P, Mathes BM, Stout SL, Watson BM, Mergott DJ. Winneroski LL, et al. Among authors: watson bm. Bioorg Med Chem. 2015 Jul 1;23(13):3260-8. doi: 10.1016/j.bmc.2015.04.062. Epub 2015 May 6. Bioorg Med Chem. 2015. PMID: 26001341
Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.
Winneroski LL, Erickson JA, Green SJ, Lopez JE, Stout SL, Porter WJ, Timm DE, Audia JE, Barberis M, Beck JP, Boggs LN, Borders AR, Boyer RD, Brier RA, Hembre EJ, Hendle J, Garcia-Losada P, Minguez JM, Mathes BM, May PC, Monk SA, Rankovic Z, Shi Y, Watson BM, Yang Z, Mergott DJ. Winneroski LL, et al. Among authors: watson bm. Bioorg Med Chem. 2020 Jan 1;28(1):115194. doi: 10.1016/j.bmc.2019.115194. Epub 2019 Nov 15. Bioorg Med Chem. 2020. PMID: 31786008
A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6.
Shen Y, Li F, Szewczyk MM, Halabelian L, Chau I, Eram MS, Dela Seña C, Park KS, Meng F, Chen H, Zeng H, Dong A, Wu H, Trush VV, McLeod D, Zepeda-Velázquez CA, Campbell RM, Mader MM, Watson BM, Schapira M, Arrowsmith CH, Al-Awar R, Barsyte-Lovejoy D, Kaniskan HÜ, Brown PJ, Vedadi M, Jin J. Shen Y, et al. Among authors: watson bm. J Med Chem. 2021 Apr 8;64(7):3697-3706. doi: 10.1021/acs.jmedchem.0c02160. Epub 2021 Feb 16. J Med Chem. 2021. PMID: 33591753 Free PMC article.
Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site.
Sheehan SM, Mest HJ, Watson BM, Klimkowski VJ, Timm DE, Cauvin A, Parsons SH, Shi Q, Canada EJ, Wiley MR, Ruehter G, Evers B, Petersen S, Blaszczak LC, Pulley SR, Margolis BJ, Wishart GN, Renson B, Hankotius D, Mohr M, Zechel JC, Michael Kalbfleisch J, Dingess-Hammond EA, Boelke A, Weichert AG. Sheehan SM, et al. Among authors: watson bm. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1765-8. doi: 10.1016/j.bmcl.2006.12.074. Epub 2006 Dec 24. Bioorg Med Chem Lett. 2007. PMID: 17239592
D-phenylglycinol-derived non-covalent factor Xa inhibitors: effect of non-peptidic S4 linkage elements on affinity and anticoagulant activity.
Klimkowski VJ, Watson BM, Wiley MR, Liebeschuetz J, Franciskovich JB, Marimuthu J, Bastian JA, Sall DJ, Smallwood JK, Chirgadze NY, Smith GF, Foster RS, Craft T, Sipes P, Chastain M, Sheehan SM. Klimkowski VJ, et al. Among authors: watson bm. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5801-5. doi: 10.1016/j.bmcl.2007.08.051. Epub 2007 Aug 28. Bioorg Med Chem Lett. 2007. PMID: 17881231
Synthesis and SAR of novel histamine H3 receptor antagonists.
Jesudason CD, Beavers LS, Cramer JW, Dill J, Finley DR, Lindsley CW, Stevens FC, Gadski RA, Oldham SW, Pickard RT, Siedem CS, Sindelar DK, Singh A, Watson BM, Hipskind PA. Jesudason CD, et al. Among authors: watson bm. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3415-8. doi: 10.1016/j.bmcl.2006.04.004. Epub 2006 May 3. Bioorg Med Chem Lett. 2006. PMID: 16677814
80 results