S. T. M. Orr

发表

Novel approach to the lundurine alkaloids: synthesis of the tetracyclic core.

Jianhua Tian, S. Martin, M. Niggemann, 2011, Organic letters.

Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR.

Paolo Vicini, Deepak Dalvie, Chengyi Zhang, 2017, Journal of medicinal chemistry.

Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.

Deepak Dalvie, Michael Zientek, Rose Ann Ferre, 2016, Journal of medicinal chemistry.

Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.

Hao Sun, A. Kalgutkar, R. Obach, 2012, Journal of medicinal chemistry.

Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.

A. Kalgutkar, T. Maurer, J. Warmus, 2015, Journal of medicinal chemistry.

Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor.

L. Michael, T. Goosen, M. Tu, 2013, Bioorganic & medicinal chemistry letters.

Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate.

P. Loria, D. Hepworth, S. Bhattacharya, 2014, ACS medicinal chemistry letters.

Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.

A. Kalgutkar, J. Warmus, D. Hepworth, 2013, ACS medicinal chemistry letters.

Optimization of triazole -based TGR5 agonists towards orally available agents

Bryan M. Li, J. Warmus, D. Hepworth, 2013 .

Small structural changes of the imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitors produce an improved safety profile.

D. Hepworth, T. Goosen, A. Shoieb, 2017, MedChemComm.

Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2).

C. C. Jorgensen, M. Boehm, D. Hepworth, 2015, Journal of medicinal chemistry.

Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195).

Ping Chen, Hong Shen, M. Pairish, 2020, Journal of medicinal chemistry.

Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment.

M. Ammirati, A. Carlo, A. Mathiowetz, 2015, ACS medicinal chemistry letters.

Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists.

P. Loria, D. Hepworth, S. Bhattacharya, 2015, ACS Medicinal Chemistry Letters.

Reactive Metabolite Trapping Studies on Imidazo- and 2-Methylimidazo[2,1-b]thiazole-Based Inverse Agonists of the Ghrelin Receptor

G. S. Walker, A. Kalgutkar, T. Goosen, 2013, Drug Metabolism and Disposition.

Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.

K. Gajiwala, N. Sach, Sherry L. Niessen, 2016, Journal of medicinal chemistry.

Deuterium isotope effects in drug pharmacokinetics II: Substrate-dependence of the reaction mechanism influences outcome for cytochrome P450 cleared drugs

J. Warmus, Hao Sun, A. Vaz, 2018, PloS one.

Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.

A. Kalgutkar, R. Obach, Hao Sun, 2012, Journal of medicinal chemistry.