Thomas A. Dineen

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2005 University of Michigan, Ann Arbor, Ann Arbor, MI 
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William R. Roush grad student 2005 University of Michigan
 (Studies on the intramolecular Diels -Alder reaction: Total synthesis of cochleamycin A and efforts toward the total synthesis of integramycin.)
Andrew G. Myers post-doc 2005-2007 Harvard
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Publications

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Eno MS, Brubaker JD, Campbell JE, et al. (2022) Discovery of BLU-945, a Reversible, Potent, and Wild-Type-Sparing Next-Generation EGFR Mutant Inhibitor for Treatment-Resistant Non-Small-Cell Lung Cancer. Journal of Medicinal Chemistry
Graceffa RF, Boezio AA, Able J, et al. (2017) Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust In Vivo Activity. Journal of Medicinal Chemistry
Weiss MM, Dineen TA, Marx IE, et al. (2017) Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities. Journal of Medicinal Chemistry
Marx IE, Dineen TA, Able J, et al. (2016) Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement. Acs Medicinal Chemistry Letters. 7: 1062-1067
Chen JJ, Liu Q, Yuan C, et al. (2015) Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer's disease. Bioorganic & Medicinal Chemistry Letters. 25: 767-74
Epstein O, Bryan MC, Cheng AC, et al. (2014) Lead optimization and modulation of hERG activity in a series of aminooxazoline xanthene β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors. Journal of Medicinal Chemistry. 57: 9796-810
Dineen TA, Chen K, Cheng AC, et al. (2014) Inhibitors of β-site amyloid precursor protein cleaving enzyme (BACE1): identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine (AMG-8718). Journal of Medicinal Chemistry. 57: 9811-31
Huang H, La DS, Cheng AC, et al. (2012) Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease. Journal of Medicinal Chemistry. 55: 9156-69
Wood S, Wen PH, Zhang J, et al. (2012) Establishing the relationship between in vitro potency, pharmacokinetic, and pharmacodynamic parameters in a series of orally available, hydroxyethylamine-derived β-secretase inhibitors. The Journal of Pharmacology and Experimental Therapeutics. 343: 460-7
Dineen TA, Weiss MM, Williamson T, et al. (2012) Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors. Journal of Medicinal Chemistry. 55: 9025-44
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