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Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists

Bioorganic & medicinal chemistry letters, 2009-05, Vol.19 (9), p.2400-2403

2009

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Discovery of Clinical Candidate 4‑[2-(5-Amino‑1H‑pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro‑N‑1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7

Journal of medicinal chemistry, 2017-08, Vol.60 (16), p.7029-7042

2017

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Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes

Bioorganic & medicinal chemistry letters, 2017-11, Vol.27 (21), p.4805-4811

2017

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One-Pot Synthesis of α‑Branched N‑Acylamines via Titanium-Mediated Condensation of Amides, Aldehydes, and Organometallics

Organic letters, 2017-03, Vol.19 (5), p.1064-1067

2017

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PF-04859989 as a template for structure-based drug design: Identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency

Bioorganic & medicinal chemistry letters, 2013-04, Vol.23 (7), p.1961-1966

2013

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Diastereoselective Synthesis of β‑Heteroaryl syn-α-Methyl-β-Amino Acid Derivatives via a Double Chiral Auxiliary Approach

Organic letters, 2013-02, Vol.15 (3), p.562-565

2013

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Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of Na V 1.7

Journal of medicinal chemistry, 2017-08, Vol.60 (16), p.7029-7042

2017

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Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia

ACS medicinal chemistry letters, 2012-03, Vol.3 (3), p.187-192

2012

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A General Strategy for the Synthesis of Cyclic N-Aryl Hydroxamic Acids via Partial Nitro Group Reduction

Journal of organic chemistry, 2011-05, Vol.76 (9), p.3484-3497

2011

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Synthesis of ortho-substituted nitroaromatics via improved Negishi coupling conditions

Tetrahedron letters, 2011-10, Vol.52 (41), p.5211-5213

2011

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Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions

ACS medicinal chemistry letters, 2013-01, Vol.4 (1), p.37-40

2013

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Development of a scalable synthetic route towards a 2,2,6-trisubstituted chiral morpholine via stereoselective hydroalkoxylation

Tetrahedron letters, 2018-05, Vol.59 (19), p.1808-1812

2018

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Short-acting 5-(trifluoromethyl)pyrido[4,3- d]pyrimidin-4(3 H)-one derivatives as orally-active calcium-sensing receptor antagonists

Bioorganic & medicinal chemistry letters, 2009-08, Vol.19 (16), p.4555-4559

2009

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A Second-Generation Oral SARS-CoV‑2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19

Journal of medicinal chemistry, 2024-08, Vol.67 (16), p.13550-13571

2024

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Identification of Tricyclic Analogs Related to Ellagic Acid as Potent/Selective Tyrosine Protein Kinase Inhibitors

Journal of medicinal chemistry, 1994-07, Vol.37 (14), p.2224-2231

1994

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Benzyloxazolidine-2,4-diones as potent hypoglycemic agents

Journal of medicinal chemistry, 1991-05, Vol.34 (5), p.1538-1544

1991

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Chemically-enabled synthesis of 1,2,3,4-tetrahydroisoquinolin-1-ones

Tetrahedron letters, 2009-05, Vol.50 (18), p.2140-2143

2009

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Discovery of hydroxamate bioisosteres as KAT II inhibitors with improved oral bioavailability and pharmacokinetics

MedChemComm, 2013, Vol.4 (1), p.125-129

2013

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Highly potent and selective Na V 1.7 inhibitors for use as intravenous agents and chemical probes

Bioorganic & medicinal chemistry letters, 2017-11, Vol.27 (21), p.4805

2017

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Synthesis of t-boc-4-dimethylphosphonomethyl-L-phenylalanine

Synlett, 1994-04 (4), p.293-294

1994

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Synthesis of t -Boc-4-Dimethylphosphonomethyl-L-Phenylalanine 1

Synlett, 1994, Vol.1994 (4), p.293-294

1994

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Synthesis of t-Boc-4-Dimethylphosphonomethyl-L-Phenylalanine1

Synlett, 1994, Vol.1994 (4), p.293-294

1994

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ChemInform Abstract: Diastereoselective Synthesis of [beta]-Heteroaryl syn-[alpha]-Methyl-[beta]-amino Acid Derivatives via a Double Chiral Auxiliary Approach

ChemInform, 2013-06, Vol.44 (26), p.no

2013

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Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists

Discovery of Clinical Candidate 4‑[2-(5-Amino‑1H‑pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro‑N‑1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7

Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes

One-Pot Synthesis of α‑Branched N‑Acylamines via Titanium-Mediated Condensation of Amides, Aldehydes, and Organometallics

PF-04859989 as a template for structure-based drug design: Identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency

Diastereoselective Synthesis of β‑Heteroaryl syn-α-Methyl-β-Amino Acid Derivatives via a Double Chiral Auxiliary Approach

Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of Na V 1.7

Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia

A General Strategy for the Synthesis of Cyclic N-Aryl Hydroxamic Acids via Partial Nitro Group Reduction

Synthesis of ortho-substituted nitroaromatics via improved Negishi coupling conditions

Discovery Tactics To Mitigate Toxicity Risks Due to Reactive Metabolite Formation with 2-(2-Hydroxyaryl)-5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3H)-one Derivatives, Potent Calcium-Sensing Receptor Antagonists and Clinical Candidate(s) for the Treatment of Osteoporosis

Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions

Development of a scalable synthetic route towards a 2,2,6-trisubstituted chiral morpholine via stereoselective hydroalkoxylation

Short-acting 5-(trifluoromethyl)pyrido[4,3- d]pyrimidin-4(3 H)-one derivatives as orally-active calcium-sensing receptor antagonists

A Second-Generation Oral SARS-CoV‑2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19

Identification of Tricyclic Analogs Related to Ellagic Acid as Potent/Selective Tyrosine Protein Kinase Inhibitors

Benzyloxazolidine-2,4-diones as potent hypoglycemic agents

Chemically-enabled synthesis of 1,2,3,4-tetrahydroisoquinolin-1-ones

Discovery of hydroxamate bioisosteres as KAT II inhibitors with improved oral bioavailability and pharmacokinetics

Highly potent and selective Na V 1.7 inhibitors for use as intravenous agents and chemical probes

Synthesis of t-boc-4-dimethylphosphonomethyl-L-phenylalanine

Synthesis of t -Boc-4-Dimethylphosphonomethyl-L-Phenylalanine 1

Synthesis of t-Boc-4-Dimethylphosphonomethyl-L-Phenylalanine1

ChemInform Abstract: Diastereoselective Synthesis of [beta]-Heteroaryl syn-[alpha]-Methyl-[beta]-amino Acid Derivatives via a Double Chiral Auxiliary Approach

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