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Page 1
Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.
Dineen TA, Weiss MM, Williamson T, Acton P, Babu-Khan S, Bartberger MD, Brown J, Chen K, Cheng Y, Citron M, Croghan MD, Dunn RT 2nd, Esmay J, Graceffa RF, Harried SS, Hickman D, Hitchcock SA, Horne DB, Huang H, Imbeah-Ampiah R, Judd T, Kaller MR, Kreiman CR, La DS, Li V, Lopez P, Louie S, Monenschein H, Nguyen TT, Pennington LD, San Miguel T, Sickmier EA, Vargas HM, Wahl RC, Wen PH, Whittington DA, Wood S, Xue Q, Yang BH, Patel VF, Zhong W. Dineen TA, et al. Among authors: la ds. J Med Chem. 2012 Nov 8;55(21):9025-44. doi: 10.1021/jm300118s. Epub 2012 Apr 18. J Med Chem. 2012. PMID: 22468684
A Potent and Orally Efficacious, Hydroxyethylamine-Based Inhibitor of β-Secretase.
Kaller MR, Harried SS, Albrecht B, Amarante P, Babu-Khan S, Bartberger MD, Brown J, Brown R, Chen K, Cheng Y, Citron M, Croghan MD, Graceffa R, Hickman D, Judd T, Kriemen C, La D, Li V, Lopez P, Luo Y, Masse C, Monenschein H, Nguyen T, Pennington LD, Miguel TS, Sickmier EA, Wahl RC, Weiss MM, Wen PH, Williamson T, Wood S, Xue M, Yang B, Zhang J, Patel V, Zhong W, Hitchcock S. Kaller MR, et al. ACS Med Chem Lett. 2012 Mar 29;3(11):886-91. doi: 10.1021/ml3000148. eCollection 2012 Nov 8. ACS Med Chem Lett. 2012. PMID: 24900403 Free PMC article.
Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis.
La DS, Belzile J, Bready JV, Coxon A, DeMelfi T, Doerr N, Estrada J, Flynn JC, Flynn SR, Graceffa RF, Harriman SP, Larrow JF, Long AM, Martin MW, Morrison MJ, Patel VF, Roveto PM, Wang L, Weiss MM, Whittington DA, Teffera Y, Zhao Z, Polverino AJ, Harmange JC. La DS, et al. J Med Chem. 2008 Mar 27;51(6):1695-705. doi: 10.1021/jm701129j. Epub 2008 Feb 27. J Med Chem. 2008. PMID: 18311900
Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.
Weiss MM, Harmange JC, Polverino AJ, Bauer D, Berry L, Berry V, Borg G, Bready J, Chen D, Choquette D, Coxon A, DeMelfi T, Doerr N, Estrada J, Flynn J, Graceffa RF, Harriman SP, Kaufman S, La DS, Long A, Neervannan S, Patel VF, Potashman M, Regal K, Roveto PM, Schrag ML, Starnes C, Tasker A, Teffera Y, Whittington DA, Zanon R. Weiss MM, et al. Among authors: la ds. J Med Chem. 2008 Mar 27;51(6):1668-80. doi: 10.1021/jm701098w. Epub 2008 Mar 7. J Med Chem. 2008. PMID: 18324759
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.
Harmange JC, Weiss MM, Germain J, Polverino AJ, Borg G, Bready J, Chen D, Choquette D, Coxon A, DeMelfi T, DiPietro L, Doerr N, Estrada J, Flynn J, Graceffa RF, Harriman SP, Kaufman S, La DS, Long A, Martin MW, Neervannan S, Patel VF, Potashman M, Regal K, Roveto PM, Schrag ML, Starnes C, Tasker A, Teffera Y, Wang L, White RD, Whittington DA, Zanon R. Harmange JC, et al. Among authors: la ds. J Med Chem. 2008 Mar 27;51(6):1649-67. doi: 10.1021/jm701097z. Epub 2008 Mar 7. J Med Chem. 2008. PMID: 18324761
Design and preparation of a potent series of hydroxyethylamine containing β-secretase inhibitors that demonstrate robust reduction of central β-amyloid.
Weiss MM, Williamson T, Babu-Khan S, Bartberger MD, Brown J, Chen K, Cheng Y, Citron M, Croghan MD, Dineen TA, Esmay J, Graceffa RF, Harried SS, Hickman D, Hitchcock SA, Horne DB, Huang H, Imbeah-Ampiah R, Judd T, Kaller MR, Kreiman CR, La DS, Li V, Lopez P, Louie S, Monenschein H, Nguyen TT, Pennington LD, Rattan C, San Miguel T, Sickmier EA, Wahl RC, Wen PH, Wood S, Xue Q, Yang BH, Patel VF, Zhong W. Weiss MM, et al. Among authors: la ds. J Med Chem. 2012 Nov 8;55(21):9009-24. doi: 10.1021/jm300119p. Epub 2012 Apr 18. J Med Chem. 2012. PMID: 22468639
Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease.
Huang H, La DS, Cheng AC, Whittington DA, Patel VF, Chen K, Dineen TA, Epstein O, Graceffa R, Hickman D, Kiang YH, Louie S, Luo Y, Wahl RC, Wen PH, Wood S, Fremeau RT Jr. Huang H, et al. Among authors: la ds. J Med Chem. 2012 Nov 8;55(21):9156-69. doi: 10.1021/jm300598e. Epub 2012 Sep 11. J Med Chem. 2012. PMID: 22928914
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities.
Weiss MM, Dineen TA, Marx IE, Altmann S, Boezio A, Bregman H, Chu-Moyer M, DiMauro EF, Feric Bojic E, Foti RS, Gao H, Graceffa R, Gunaydin H, Guzman-Perez A, Huang H, Huang L, Jarosh M, Kornecook T, Kreiman CR, Ligutti J, La DS, Lin MJ, Liu D, Moyer BD, Nguyen HN, Peterson EA, Rose PE, Taborn K, Youngblood BD, Yu V, Fremeau RT Jr. Weiss MM, et al. Among authors: la ds. J Med Chem. 2017 Jul 27;60(14):5969-5989. doi: 10.1021/acs.jmedchem.6b01851. Epub 2017 Apr 20. J Med Chem. 2017. PMID: 28287723
Discovery of triazine-benzimidazoles as selective inhibitors of mTOR.
Peterson EA, Andrews PS, Be X, Boezio AA, Bush TL, Cheng AC, Coats JR, Colletti AE, Copeland KW, DuPont M, Graceffa R, Grubinska B, Harmange JC, Kim JL, Mullady EL, Olivieri P, Schenkel LB, Stanton MK, Teffera Y, Whittington DA, Cai T, La DS. Peterson EA, et al. Among authors: la ds. Bioorg Med Chem Lett. 2011 Apr 1;21(7):2064-70. doi: 10.1016/j.bmcl.2011.02.007. Epub 2011 Feb 12. Bioorg Med Chem Lett. 2011. PMID: 21376583
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement.
Marx IE, Dineen TA, Able J, Bode C, Bregman H, Chu-Moyer M, DiMauro EF, Du B, Foti RS, Fremeau RT Jr, Gao H, Gunaydin H, Hall BE, Huang L, Kornecook T, Kreiman CR, La DS, Ligutti J, Lin MJ, Liu D, McDermott JS, Moyer BD, Peterson EA, Roberts JT, Rose P, Wang J, Youngblood BD, Yu V, Weiss MM. Marx IE, et al. Among authors: la ds. ACS Med Chem Lett. 2016 Sep 21;7(12):1062-1067. doi: 10.1021/acsmedchemlett.6b00243. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994738 Free PMC article.
19 results