W. R. Ewing

发表

Eleven amino acid glucagon-like peptide-1 receptor agonists with antidiabetic activity.

K. Constantine, R. Stoffel, B. Koplowitz, 2009, Journal of medicinal chemistry.

Total synthesis and structural investigations of didemnins A, B, and C

B. D. Harris, W. R. Ewing, M. Joullié, 1990 .

In Praise of Remarkably Powerful Centamolecular Therapeutic Agents.

N. Meanwell, W. R. Ewing, 2019, ACS medicinal chemistry letters.

Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics.

W. Humphreys, J. Macor, M. Kowala, 2005, Journal of medicinal chemistry.

To Market, To Market—2010

W. R. Ewing, N. Lonberg, M. Dhar, 2011 .

Modulateurs dihydropyrazoles de gpr40

Z. Gu, W. R. Ewing, Ximao Wu, 2013 .

Site-Selective Functionalization of Methionine Residues via Photoredox Catalysis.

W. R. Ewing, Richard Y.-C. Huang, D. MacMillan, 2020, Journal of the American Chemical Society.

Overcoming the Limitations of γ- and δ-C-H Arylation of Amines through Ligand Development.

Martin D. Eastgate, W. R. Ewing, Zhen Wang, 2018, Journal of the American Chemical Society.

meta-Selective C-H Arylation of Fluoroarenes and Simple Arenes.

K. Yeung, W. R. Ewing, jin-quan yu, 2020, Angewandte Chemie.

meta ‐Selective C−H Arylation of Fluoroarenes and Simple Arenes

K. Yeung, W. R. Ewing, jin-quan yu, 2020, Angewandte Chemie.

Selective C-H Halogenation with a Highly Fluorinated Manganese Porphyrin.

J. Groves, W. R. Ewing, P. Cheng, 2018, Angewandte Chemie.

Nucleophilic (Radio)Fluorination of Redox-Active Esters via Radical-Polar Crossover Enabled by Photoredox Catalysis.

W. R. Ewing, D. Donnelly, A. Doyle, 2020, Journal of the American Chemical Society.

Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode.

David S. Nirschl, Kimberly A. Foster, David S Nirschl, 2017, Journal of medicinal chemistry.

Reduction of Site-Specific CYP3A-Mediated Metabolism for Dual Angiotensin and Endothelin Receptor Antagonists in Various in Vitro Systems and in Cynomolgus Monkeys

W. Humphreys, N. Murugesan, Z. Gu, 2007, Drug Metabolism and Disposition.

Discovery of a potent and novel motilin agonist.

R. Stoffel, Huabin Sun, R. Seethala, 2004, Journal of medicinal chemistry.

Pd(II)-Catalyzed Enantioselective C(sp3)-H Arylation of Cyclobutyl Ketones Using a Chiral Transient Directing Group.

Fan Luo, K. Yeung, W. R. Ewing, 2020, Angewandte Chemie.

Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy.

Michael A. Galella, S. Sheriff, A. Mathur, 2021, Journal of medicinal chemistry.

Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.

P. Lam, S. Sheriff, A. Mathur, 2020, Journal of medicinal chemistry.

Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency.

P. Lam, S. Sheriff, D. Seiffert, 2017, Bioorganic & medicinal chemistry letters.

(D)-2-tert-Butoxycarbonylamino-5,5-difluoro-5-phenyl-pentanoic acid: synthesis and incorporation into the growth hormone secretagogues.

W. Humphreys, R. Seethala, P. Sleph, 2008, Bioorganic & medicinal chemistry letters.

Exploration of structure–activity relationships at the two C-terminal residues of potent 11mer Glucagon-Like Peptide-1 receptor agonist peptides via parallel synthesis

Christopher B. Cooper, B. Koplowitz, C. Mapelli, 2010, Peptides.

Identification of potent 11mer Glucagon-Like Peptide-1 Receptor agonist peptides with novel C-terminal amino acids: Homohomophenylalanine analogs

Christopher B. Cooper, C. Mapelli, V. Lee, 2010, Peptides.

Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies.

K. Behnia, N. Murugesan, Z. Gu, 2011, Bioorganic & medicinal chemistry letters.

Pharmacodynamic activity and antithrombotic efficacy of RPR120844, a novel inhibitor of coagulation factor Xa.

C. Dunwiddie, R. Bentley, A. Spada, 1999, Journal of cardiovascular pharmacology.

RPR120844, a Novel, Specific Inhibitor of Coagulation Factor Xa Inhibits Venous Thrombosis in the Rabbit

C. Dunwiddie, R. Bentley, A. Spada, 1999, Thrombosis and Haemostasis.

Ligand Enabled Pd(II)-Catalyzed γ-C(sp3)-H Lactamization of Native Amides.

M. Poss, K. Yeung, W. R. Ewing, 2021, Journal of the American Chemical Society.

Affinity of fibroblast growth factors for β-cyclodextrin tetradecasulfate

P. B. Weisz, J. Folkman, W. R. Ewing, 1990 .

Ligand-Enabled Pd(II)-Catalyzed C(sp3)-H Lactonization Using Molecular Oxygen as Oxidant.

Martin D. Eastgate, W. R. Ewing, jin-quan yu, 2020, Organic letters.

meta C-H Arylation of Electron-Rich Arenes: Reversing the Conventional Site-Selectivity.

K. Yeung, W. R. Ewing, jin-quan yu, 2019, Journal of the American Chemical Society.

PROGRESS IN THE DESIGN OF INHIBITORS OF COAGULATION FACTOR XA

W. R. Ewing, H. Pauls, P. SpadaAlfred, 1999 .

Aminoisoquinolines: design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA.

C. Dunwiddie, D. Cheney, R. Bentley, 1999, Bioorganic & medicinal chemistry letters.

Crystal structures of human factor Xa complexed with potent inhibitors.

A. Spada, W. R. Ewing, V. Mikol, 2000, Journal of medicinal chemistry.

Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.

D L Cheney, C. Dunwiddie, J. Mason, 1999, Journal of medicinal chemistry.

Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.

R. Bentley, A. Spada, C. Ly, 1999, Bioorganic & medicinal chemistry letters.

Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).

P. Lam, S. Sheriff, A. Mathur, 2017, Journal of medicinal chemistry.

Manganese-Catalyzed Desaturation of N-Acyl Amines and Ethers

Gang Li, J. Groves, Patrick A. Kates, 2019, ACS Catalysis.

The Design of Competitive, Small-molecule Inhibitors of Coagulation Factor Xa

W. R. Ewing, Y. M. Choi-Sledeski, H. Pauls, 2001 .

Ni-Catalyzed Carbon-Carbon Bond-Forming Reductive Amination.

W. R. Ewing, J. Lutz, E. Simmons, 2018, Journal of the American Chemical Society.

Anti-Markovnikov Hydroamination of Unactivated Alkenes with Primary Alkyl Amines.

David C. Miller, W. R. Ewing, R. Knowles, 2019, Journal of the American Chemical Society.

Hemilabile Benzyl Ether Enables γ-C(sp3)-H Carbonylation and Olefination of Alcohols.

W. R. Ewing, jin-quan yu, Keita Tanaka, 2019, Journal of the American Chemical Society.

Decarboxylative alkylation for site-selective bioconjugation of native proteins via oxidation potentials

Chun Liu, William R Ewing, M. Poss, 2017, Nature Chemistry.

Design and synthesis of tetrazole-based growth hormone secretagogue: the SAR studies of the O-benzyl serine side chain.

W. Humphreys, K. Dickinson, R. Seethala, 2008, Bioorganic & medicinal chemistry letters.

Discovery of a tetrazole-based growth hormone secretagogue: 4-(hydroxybutyl)carbamic acid 2-{5-[1-(2-amino-2-methylpropionylamino)-2- benzyloxyethyl]tetrazol-1-yl}ethyl ester (BMS-317180).

W. Humphreys, K. Dickinson, R. Seethala, 2007, Journal of medicinal chemistry.

Writing Your Next Medicinal Chemistry Article: Journal Bibliometrics and Guiding Principles for Industrial Authors.

N. Meanwell, W. R. Ewing, S. Macdonald, 2020, Journal of medicinal chemistry.

Synthetic studies of didemnins. IV: Synthesis of the macrocycle

B. D. Harris, Wen-Ren Li, W. R. Ewing, 1989 .

A tautomeric ligand enables directed C‒H hydroxylation with molecular oxygen

K. Yeung, W. R. Ewing, Zhen Wang, 2021, Science.

Sulfonamidopyrrolidinone factor Xa inhibitors: potency and selectivity enhancements via P-1 and P-4 optimization.

C. Dunwiddie, D. Cheney, R. Bentley, 1999, Journal of medicinal chemistry.

Potent, Orally Bioavailable and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.

P. Lam, S. Sheriff, A. Mathur, 2019, Journal of medicinal chemistry.

Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series.

Ying Wang, Samuel W Gerritz, William R Ewing, 2007, Bioorganic & medicinal chemistry letters.

A Short, Stereocontrolled Synthesis of (—)-Detoxinine

W. R. Ewing, M. Joullié, 1988 .

Control of angiogenesis with synthetic heparin substitutes.

P. B. Weisz, J. Folkman, W. R. Ewing, 1989, Science.

Synthetic studies of the detoxin complex. I. total synthesis of (-) detoxinine

B. D. Harris, W. R. Ewing, M. Joullié, 1986 .

Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).

David S. Taylor, R. Parker, R. Stoffel, 2007, Bioorganic & medicinal chemistry letters.

To Market, To Market—2011

W. R. Ewing, N. Lonberg, M. Dhar, 2012 .

Molecular structures of human factor Xa complexed with ketopiperazine inhibitors: preference for a neutral group in the S1 pocket.

Sébastien Maignan, William R Ewing, A. Spada, 2003, Journal of medicinal chemistry.

Milvexian, an orally bioavailable, small‐molecule, reversible, direct inhibitor of factor XIa: In vitro studies and in vivo evaluation in experimental thrombosis in rabbits

D. Gordon, W. R. Ewing, J. Bozarth, 2021, Journal of thrombosis and haemostasis : JTH.

Potent biphenyl- and 3-phenyl pyridine-based inhibitors of acetyl-CoA carboxylase.

Christopher B. Cooper, M. Poss, R. Seethala, 2009, Bioorganic & medicinal chemistry letters.

β ‐Selective C−H Arylation of Electron‐Deficient Thiophenes, Pyrroles, and Furans

K. Yeung, W. R. Ewing, jin-quan yu, 2020 .

Design and SAR of selective T-type calcium channel antagonists containing a biaryl sulfonamide core.

Daniel L Cheney, William R Ewing, Stephen Swartz, 2008, Bioorganic & medicinal chemistry letters.

Preclinical metabolism and disposition of an orally bioavailable macrocyclic FXIa inhibitor

Y. Shu, W. R. Ewing, J. Luettgen, 2021, Xenobiotica; the fate of foreign compounds in biological systems.

Site-selective tyrosine bioconjugation via photoredox catalysis for native-to-bioorthogonal protein transformation

G. Scholes, Daniel G. Oblinsky, W. R. Ewing, 2021, Nature Chemistry.

Synthetic studies of didemnins. i. revision of the stereochemistry of the hydroxyisovalerylpropionyl (hip) unit.

W. R. Ewing, M. Joullié, K. Bhat, 1986 .

Catalytic Ring Expansions of Cyclic Alcohols Enabled by Proton-Coupled Electron Transfer.

W. R. Ewing, P. Cheng, R. Knowles, 2019, Journal of the American Chemical Society.

Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target activities.

Kimberly A. Foster, Michael A. Galella, J. Barrish, 2023, Bioorganic & medicinal chemistry.

Factor XIa Inhibitors as New Anticoagulants.

D. Seiffert, W. R. Ewing, R. Wexler, 2018, Journal of medicinal chemistry.

Reductions in log P improved protein binding and clearance predictions enabling the prospective design of cannabinoid receptor (CB1) antagonists with desired pharmacokinetic properties.

K. Behnia, N. Murugesan, Z. Gu, 2013, Journal of medicinal chemistry.

Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.

David S Nirschl, P. Lam, S. Sheriff, 2019, Bioorganic & medicinal chemistry letters.