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Direct, Regioselective N‑Alkylation of 1,3-Azoles

Organic letters, 2016-01, Vol.18 (1), p.16-19

2016

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Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity

Journal of medicinal chemistry, 2016-03, Vol.59 (6), p.2794-2809

2016

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Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2

Proceedings of the National Academy of Sciences - PNAS, 2024-02, Vol.121 (6), p.e2317756121

2024

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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, 2017-07, Vol.60 (14), p.5990-6017

2017

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Structure-Based Design of Novel Class II c-Met Inhibitors: 2. SAR and Kinase Selectivity Profiles of the Pyrazolone Series

Journal of medicinal chemistry, 2012-03, Vol.55 (5), p.1868-1897

2012

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Discovery of Potent and Selective 8‑Fluorotriazolopyridine c‑Met Inhibitors

Journal of medicinal chemistry, 2015-03, Vol.58 (5), p.2417-2430

2015

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1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of NaV1.7 inhibition

Bioorganic & medicinal chemistry letters, 2018-06, Vol.28 (11), p.2103-2108

2018

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Asymmetric, Catalytic Synthesis of α-Chiral Amines Using a Novel Bis(phosphine) Monoxide Chiral Ligand

Journal of the American Chemical Society, 2003-11, Vol.125 (47), p.14260-14261

2003

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Catalytic Asymmetric Addition of Diorganozinc Reagents to N-Phosphinoylalkylimines

Proceedings of the National Academy of Sciences - PNAS, 2004-04, Vol.101 (15), p.5405-5410

2004

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The discovery of benzoxazine sulfonamide inhibitors of NaV1.7: Tools that bridge efficacy and target engagement

Bioorganic & medicinal chemistry letters, 2017-08, Vol.27 (15), p.3477-3485

2017

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1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of Na V 1.7 inhibition

Bioorganic & medicinal chemistry letters, 2018-06, Vol.28 (11), p.2103-2108

2018

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Catalytic Enantioselective Addition of Dialkylzinc to N-Diphenylphosphinoylimines. A Practical Synthesis of α-Chiral Amines

Journal of the American Chemical Society, 2003-02, Vol.125 (7), p.1692-1693

2003

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Development of novel azabenzofuran TRPA1 antagonists as in vivo tools

Bioorganic & medicinal chemistry letters, 2014-08, Vol.24 (15), p.3464-3468

2014

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Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors

Bioorganic & medicinal chemistry letters, 2012-08, Vol.22 (15), p.4967-4974

2012

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Evidence for the Structure of the Enantioactive Ligand in the Phosphine-Copper-Catalyzed Addition of Diorganozinc Reagents to Imines

Angewandte Chemie (International ed.), 2004-12, Vol.43 (47), p.6525-6528

2004

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Sulfonamides as Selective Na V 1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity

Journal of medicinal chemistry, 2017-07, Vol.60 (14), p.5990-6017

2017

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Tetraarylphosphonium Salts as Solubility-Control Groups: Phosphonium-Supported Triphenylphosphine and Azodicarboxylate Reagents

Angewandte Chemie (International ed.), 2006-02, Vol.45 (9), p.1415-1420

2006

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Efficient Total Syntheses of (−)-Colombiasin A and (−)-Elisapterosin B: Application of the Cr-Catalyzed Asymmetric Quinone Diels-Alder Reaction

Angewandte Chemie (International ed.), 2005-09, Vol.44 (37), p.6046-6050

2005

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The discovery of benzoxazine sulfonamide inhibitors of Na V 1.7: Tools that bridge efficacy and target engagement

Bioorganic & medicinal chemistry letters, 2017-08, Vol.27 (15), p.3477-3485

2017

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Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors

Bioorganic & medicinal chemistry letters, 2009-11, Vol.19 (22), p.6307-6312

2009

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Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors

Bioorganic & medicinal chemistry letters, 2012-06, Vol.22 (12), p.4089-4093

2012

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Discovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase

Journal of medicinal chemistry, 2008-05, Vol.51 (10), p.2879-2882

2008

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Asymmetric catalytic addition of diorganozinc reagents to imines: Scope and application

Pure and applied chemistry, 2005-07, Vol.77 (7), p.1259-1267

2005

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Direct, Regioselective N‑Alkylation of 1,3-Azoles

Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity

Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity

Structure-Based Design of Novel Class II c-Met Inhibitors: 2. SAR and Kinase Selectivity Profiles of the Pyrazolone Series

Discovery of (R)‑6-(1-(8-Fluoro-6-(1-methyl‑1H‑pyrazol-4-yl)-[1,2,4]triazolo[4,3‑a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)‑one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity

Discovery of Potent and Selective 8‑Fluorotriazolopyridine c‑Met Inhibitors

1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of NaV1.7 inhibition

Asymmetric, Catalytic Synthesis of α-Chiral Amines Using a Novel Bis(phosphine) Monoxide Chiral Ligand

Catalytic Asymmetric Addition of Diorganozinc Reagents to N-Phosphinoylalkylimines

The discovery of benzoxazine sulfonamide inhibitors of NaV1.7: Tools that bridge efficacy and target engagement

1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of Na V 1.7 inhibition

Pharmacological effects of nonselective and subtype-selective nicotinic acetylcholine receptor agonists in animal models of persistent pain

Catalytic Enantioselective Addition of Dialkylzinc to N-Diphenylphosphinoylimines. A Practical Synthesis of α-Chiral Amines

Development of novel azabenzofuran TRPA1 antagonists as in vivo tools

Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors

Evidence for the Structure of the Enantioactive Ligand in the Phosphine-Copper-Catalyzed Addition of Diorganozinc Reagents to Imines

Sulfonamides as Selective Na V 1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity

Tetraarylphosphonium Salts as Solubility-Control Groups: Phosphonium-Supported Triphenylphosphine and Azodicarboxylate Reagents

Efficient Total Syntheses of (−)-Colombiasin A and (−)-Elisapterosin B: Application of the Cr-Catalyzed Asymmetric Quinone Diels-Alder Reaction

The discovery of benzoxazine sulfonamide inhibitors of Na V 1.7: Tools that bridge efficacy and target engagement

Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors

Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors

Discovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase

Asymmetric catalytic addition of diorganozinc reagents to imines: Scope and application

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