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Table representation of search results timeline featuring number of search results per year.

Year Number of Results
1992 2
1993 1
1997 1
1999 2
2004 2
2007 1
2008 2
2010 2
2012 3
2014 1
2016 4
2017 1
2018 1
2019 1
2021 0
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23 results
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Page 1
The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients.
Kennedy ME, Stamford AW, Chen X, Cox K, Cumming JN, Dockendorf MF, Egan M, Ereshefsky L, Hodgson RA, Hyde LA, Jhee S, Kleijn HJ, Kuvelkar R, Li W, Mattson BA, Mei H, Palcza J, Scott JD, Tanen M, Troyer MD, Tseng JL, Stone JA, Parker EM, Forman MS. Kennedy ME, et al. Among authors: kuvelkar r. Sci Transl Med. 2016 Nov 2;8(363):363ra150. doi: 10.1126/scitranslmed.aad9704. Sci Transl Med. 2016. PMID: 27807285
Discovery of potent iminoheterocycle BACE1 inhibitors.
Caldwell JP, Mazzola RD, Durkin J, Chen J, Chen X, Favreau L, Kennedy M, Kuvelkar R, Lee J, McHugh N, McKittrick B, Orth P, Stamford A, Strickland C, Voigt J, Wang L, Zhang L, Zhang Q, Zhu Z. Caldwell JP, et al. Among authors: kuvelkar r. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5455-9. doi: 10.1016/j.bmcl.2014.10.006. Epub 2014 Oct 23. Bioorg Med Chem Lett. 2014. PMID: 25455483
Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety.
Mandal M, Mitra K, Grotz D, Lin X, Palamanda J, Kumari P, Buevich A, Caldwell JP, Chen X, Cox K, Favreau L, Hyde L, Kennedy ME, Kuvelkar R, Liu X, Mazzola RD, Parker E, Rindgen D, Sherer E, Wang H, Zhu Z, Stamford AW, Cumming JN. Mandal M, et al. Among authors: kuvelkar r. J Med Chem. 2018 Dec 13;61(23):10700-10708. doi: 10.1021/acs.jmedchem.8b01326. Epub 2018 Nov 15. J Med Chem. 2018. PMID: 30388368
TarO-specific inhibitors of wall teichoic acid biosynthesis restore β-lactam efficacy against methicillin-resistant staphylococci.
Lee SH, Wang H, Labroli M, Koseoglu S, Zuck P, Mayhood T, Gill C, Mann P, Sher X, Ha S, Yang SW, Mandal M, Yang C, Liang L, Tan Z, Tawa P, Hou Y, Kuvelkar R, DeVito K, Wen X, Xiao J, Batchlett M, Balibar CJ, Liu J, Xiao J, Murgolo N, Garlisi CG, Sheth PR, Flattery A, Su J, Tan C, Roemer T. Lee SH, et al. Among authors: kuvelkar r. Sci Transl Med. 2016 Mar 9;8(329):329ra32. doi: 10.1126/scitranslmed.aad7364. Sci Transl Med. 2016. PMID: 26962156
Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity.
Scott JD, DeMong DE, Greshock TJ, Basu K, Dai X, Harris J, Hruza A, Li SW, Lin SI, Liu H, Macala MK, Hu Z, Mei H, Zhang H, Walsh P, Poirier M, Shi ZC, Xiao L, Agnihotri G, Baptista MA, Columbus J, Fell MJ, Hyde LA, Kuvelkar R, Lin Y, Mirescu C, Morrow JA, Yin Z, Zhang X, Zhou X, Chang RK, Embrey MW, Sanders JM, Tiscia HE, Drolet RE, Kern JT, Sur SM, Renger JJ, Bilodeau MT, Kennedy ME, Parker EM, Stamford AW, Nargund R, McCauley JA, Miller MW. Scott JD, et al. Among authors: kuvelkar r. J Med Chem. 2017 Apr 13;60(7):2983-2992. doi: 10.1021/acs.jmedchem.7b00045. Epub 2017 Mar 16. J Med Chem. 2017. PMID: 28245354
Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.
Cumming J, Babu S, Huang Y, Carrol C, Chen X, Favreau L, Greenlee W, Guo T, Kennedy M, Kuvelkar R, Le T, Li G, McHugh N, Orth P, Ozgur L, Parker E, Saionz K, Stamford A, Strickland C, Tadesse D, Voigt J, Zhang L, Zhang Q. Cumming J, et al. Among authors: kuvelkar r. Bioorg Med Chem Lett. 2010 May 1;20(9):2837-42. doi: 10.1016/j.bmcl.2010.03.050. Epub 2010 Mar 12. Bioorg Med Chem Lett. 2010. PMID: 20347593
Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates.
Mandal M, Wu Y, Misiaszek J, Li G, Buevich A, Caldwell JP, Liu X, Mazzola RD, Orth P, Strickland C, Voigt J, Wang H, Zhu Z, Chen X, Grzelak M, Hyde LA, Kuvelkar R, Leach PT, Terracina G, Zhang L, Zhang Q, Michener MS, Smith B, Cox K, Grotz D, Favreau L, Mitra K, Kazakevich I, McKittrick BA, Greenlee W, Kennedy ME, Parker EM, Cumming JN, Stamford AW. Mandal M, et al. Among authors: kuvelkar r. J Med Chem. 2016 Apr 14;59(7):3231-48. doi: 10.1021/acs.jmedchem.5b01995. Epub 2016 Mar 22. J Med Chem. 2016. PMID: 26937601
Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)-A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer's Disease.
Scott JD, Li SW, Brunskill AP, Chen X, Cox K, Cumming JN, Forman M, Gilbert EJ, Hodgson RA, Hyde LA, Jiang Q, Iserloh U, Kazakevich I, Kuvelkar R, Mei H, Meredith J, Misiaszek J, Orth P, Rossiter LM, Slater M, Stone J, Strickland CO, Voigt JH, Wang G, Wang H, Wu Y, Greenlee WJ, Parker EM, Kennedy ME, Stamford AW. Scott JD, et al. Among authors: kuvelkar r. J Med Chem. 2016 Dec 8;59(23):10435-10450. doi: 10.1021/acs.jmedchem.6b00307. Epub 2016 Nov 18. J Med Chem. 2016. PMID: 27933948
Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS Aβ Reduction.
Stamford AW, Scott JD, Li SW, Babu S, Tadesse D, Hunter R, Wu Y, Misiaszek J, Cumming JN, Gilbert EJ, Huang C, McKittrick BA, Hong L, Guo T, Zhu Z, Strickland C, Orth P, Voigt JH, Kennedy ME, Chen X, Kuvelkar R, Hodgson R, Hyde LA, Cox K, Favreau L, Parker EM, Greenlee WJ. Stamford AW, et al. Among authors: kuvelkar r. ACS Med Chem Lett. 2012 Nov 8;3(11):897-902. doi: 10.1021/ml3001165. Epub 2012 Jul 12. ACS Med Chem Lett. 2012. PMID: 23412139 Free PMC article.
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