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Page 1
Discovery of N-[Bis(4-methoxyphenyl)methyl]-4-hydroxy-2-(pyridazin-3-yl)pyrimidine-5-carboxamide (MK-8617), an Orally Active Pan-Inhibitor of Hypoxia-Inducible Factor Prolyl Hydroxylase 1-3 (HIF PHD1-3) for the Treatment of Anemia.
Debenham JS, Madsen-Duggan C, Clements MJ, Walsh TF, Kuethe JT, Reibarkh M, Salowe SP, Sonatore LM, Hajdu R, Milligan JA, Visco DM, Zhou D, Lingham RB, Stickens D, DeMartino JA, Tong X, Wolff M, Pang J, Miller RR, Sherer EC, Hale JJ. Debenham JS, et al. Among authors: sonatore lm. J Med Chem. 2016 Dec 22;59(24):11039-11049. doi: 10.1021/acs.jmedchem.6b01242. Epub 2016 Nov 30. J Med Chem. 2016. PMID: 28002958
1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia.
Vachal P, Miao S, Pierce JM, Guiadeen D, Colandrea VJ, Wyvratt MJ, Salowe SP, Sonatore LM, Milligan JA, Hajdu R, Gollapudi A, Keohane CA, Lingham RB, Mandala SM, DeMartino JA, Tong X, Wolff M, Steinhuebel D, Kieczykowski GR, Fleitz FJ, Chapman K, Athanasopoulos J, Adam G, Akyuz CD, Jena DK, Lusen JW, Meng J, Stein BD, Xia L, Sherer EC, Hale JJ. Vachal P, et al. Among authors: sonatore lm. J Med Chem. 2012 Apr 12;55(7):2945-59. doi: 10.1021/jm201542d. Epub 2012 Feb 27. J Med Chem. 2012. PMID: 22364528
Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors.
Cernak T, Gesmundo NJ, Dykstra K, Yu Y, Wu Z, Shi ZC, Vachal P, Sperbeck D, He S, Murphy BA, Sonatore L, Williams S, Madeira M, Verras A, Reiter M, Lee CH, Cuff J, Sherer EC, Kuethe J, Goble S, Perrotto N, Pinto S, Shen DM, Nargund R, Balkovec J, DeVita RJ, Dreher SD. Cernak T, et al. J Med Chem. 2017 May 11;60(9):3594-3605. doi: 10.1021/acs.jmedchem.6b01543. Epub 2017 Mar 2. J Med Chem. 2017. PMID: 28252959
Rapid development of two factor IXa inhibitors from hit to lead.
Parker DL Jr, Walsh S, Li B, Kim E, Sharipour A, Smith C, Chen YH, Berger R, Harper B, Zhang T, Park M, Shu M, Wu J, Xu J, Dewnani S, Sherer EC, Hruza A, Reichert P, Geissler W, Sonatore L, Ellsworth K, Balkovec J, Greenlee W, Wood HB. Parker DL Jr, et al. Bioorg Med Chem Lett. 2015 Jun 1;25(11):2321-5. doi: 10.1016/j.bmcl.2015.04.025. Epub 2015 Apr 13. Bioorg Med Chem Lett. 2015. PMID: 25937013
Disubstituted pyrimidines as Lck inhibitors.
Hunt JA, Beresis RT, Goulet JL, Holmes MA, Hong XJ, Kovacs E, Mills SG, Ruzek RD, Wong F, Hermes JD, Park YW, Salowe SP, Sonatore LM, Wu L, Woods A, Zaller DM, Sinclair PJ. Hunt JA, et al. Among authors: sonatore lm. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5440-3. doi: 10.1016/j.bmcl.2009.07.102. Epub 2009 Jul 25. Bioorg Med Chem Lett. 2009. PMID: 19674899
Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety.
He S, Hong Q, Lai Z, Yang DX, Ting PC, Kuethe JT, Cernak TA, Dykstra KD, Sperbeck DM, Wu Z, Yu Y, Yang GX, Jian T, Liu J, Guiadeen D, Krikorian AD, Sonatore LM, Wiltsie J, Liu J, Gorski JN, Chung CC, Gibson JT, Lisnock J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, Pinto S, Nargund RP, DeVita RJ. He S, et al. Among authors: sonatore lm. ACS Med Chem Lett. 2014 Sep 8;5(10):1082-7. doi: 10.1021/ml5003426. eCollection 2014 Oct 9. ACS Med Chem Lett. 2014. PMID: 25349648 Free PMC article.
Development of a novel class of potent and selective FIXa inhibitors.
Zhang T, Andre P, Bateman TJ, Chen YH, Desai K, Ellsworth K, Geissler WM, Guo L, Hruza A, Jian T, Meng D, Parker DL Jr, Qian X, Reichert P, Sherer EC, Shu M, Smith CJ, Sonatore LM, Tschirret-Guth R, Nolting AF, Orr R, Campeau LC, Araki K, Nishimura T, Sakurada I, Wood HB. Zhang T, et al. Among authors: sonatore lm. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4945-4949. doi: 10.1016/j.bmcl.2015.04.057. Epub 2015 Apr 29. Bioorg Med Chem Lett. 2015. PMID: 25978966
Development of a novel tricyclic class of potent and selective FIXa inhibitors.
Meng D, Andre P, Bateman TJ, Berger R, Chen YH, Desai K, Dewnani S, Ellsworth K, Feng D, Geissler WM, Guo L, Hruza A, Jian T, Li H, Metzger J, Parker DL, Reichert P, Sherer EC, Smith CJ, Sonatore LM, Tschirret-Guth R, Wu J, Xu J, Zhang T, Campeau LC, Orr R, Poirier M, McCabe-Dunn J, Araki K, Nishimura T, Sakurada I, Hirabayashi T, Wood HB. Meng D, et al. Among authors: sonatore lm. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5437-43. doi: 10.1016/j.bmcl.2015.07.078. Epub 2015 Jul 31. Bioorg Med Chem Lett. 2015. PMID: 26318999
Definitive Metabolite Identification Coupled with Automated Ligand Identification System (ALIS) Technology: A Novel Approach to Uncover Structure-Activity Relationships and Guide Drug Design in a Factor IXa Inhibitor Program.
Zhang T, Liu Y, Yang X, Martin GE, Yao H, Shang J, Bugianesi RM, Ellsworth KP, Sonatore LM, Nizner P, Sherer EC, Hill SE, Knemeyer IW, Geissler WM, Dandliker PJ, Helmy R, Wood HB. Zhang T, et al. Among authors: sonatore lm. J Med Chem. 2016 Mar 10;59(5):1818-29. doi: 10.1021/acs.jmedchem.5b01293. Epub 2016 Feb 22. J Med Chem. 2016. PMID: 26871940
Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety.
He S, Lai Z, Hong Q, Shang J, Reibarkh M, Kuethe JT, Liu J, Guiadeen D, Krikorian AD, Cernak TA, Dykstra KD, Sperbeck DM, Wu Z, Yu Y, Yang GX, Jian T, Verras A, Sonatore LM, Wiltsie J, Chung CC, Murphy BA, Gorski JN, Liu J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, Pinto S, Nargund RP, DeVita RJ. He S, et al. Among authors: sonatore lm. Bioorg Med Chem Lett. 2019 May 15;29(10):1182-1186. doi: 10.1016/j.bmcl.2019.03.025. Epub 2019 Mar 21. Bioorg Med Chem Lett. 2019. PMID: 30926247
20 results