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Challenges and Opportunities in the Discovery of New Therapeutics Targeting the Kynurenine Pathway

Journal of medicinal chemistry, 2015-11, Vol.58 (22), p.8762-8782

2015

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An inverse agonist of orphan receptor GPR61 acts by a G protein-competitive allosteric mechanism

Nature communications, 2023-09, Vol.14 (1), p.5938-5938, Article 5938

2023

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Organocatalytic Transfer Hydrogenation of Cyclic Enones

Journal of the American Chemical Society, 2006-10, Vol.128 (39), p.12662-12663

2006

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Discovery and Preclinical Characterization of 1‑Methyl‑3-(4‑methylpyridin‑3‑yl)‑6‑(pyridin‑2‑ylmethoxy)‑1H‑pyrazolo-[3,4‑b]pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator

Journal of medicinal chemistry, 2014-02, Vol.57 (3), p.861-877

2014

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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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Enantioselective Organocatalytic Hydride Reduction

Journal of the American Chemical Society, 2005-01, Vol.127 (1), p.32-33

2005

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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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Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE

Cell chemical biology, 2021-02, Vol.28 (2), p.148-157.e7

2021

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Design and Discovery of 6‑[(3S,4S)‑4-Methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro‑2H‑pyran-4-yl)-1,5-dihydro‑4H‑pyrazolo[3,4‑d]pyrimidin-4-one (PF-04447943), a Selective Brain Penetrant PDE9A Inhibitor for the Treatment of Cognitive Disorders

Journal of medicinal chemistry, 2012-11, Vol.55 (21), p.9045-9054

2012

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An oral SARS-CoV-2 M pro inhibitor clinical candidate for the treatment of COVID-19

Science (American Association for the Advancement of Science), 2021-12, Vol.374 (6575), p.1586-1593

2021

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Quantitative Translational Analysis of Brain Kynurenic Acid Modulation via Irreversible Kynurenine Aminotransferase II Inhibition

Molecular pharmacology, 2018-08, Vol.94 (2), p.823-833

2018

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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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Discovery and Characterization of (R)‑6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1‑c][1,4]oxazin-4(9H)‑one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates

Journal of medicinal chemistry, 2017-09, Vol.60 (18), p.7764-7780

2017

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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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Discovery and Preclinical Characterization of 1-Methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1 H -pyrazolo-[3,4- b ]pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator

Journal of medicinal chemistry, 2014-02, Vol.57 (3), p.861-877

2014

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ChemInform Abstract: Synthesis of ortho-Substituted Nitroaromatics via Improved Negishi Coupling Conditions

ChemInform, 2012-01, Vol.43 (5), p.no-no

2012

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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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Fingolimod (Gilenya): The First Oral Treatment for Multiple Sclerosis

Innovative Drug Synthesis, 2015, p.255-270

2015

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Organocatalytic Transfer Hydrogenation of Cyclic Enones

ChemInform, 2007-01, Vol.38 (5), p.no-no

2007

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Enantioselective Organocatalytic Hydride Reduction

ChemInform, 2005-06, Vol.36 (23), p.no-no

2005

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Challenges and Opportunities in the Discovery of New Therapeutics Targeting the Kynurenine Pathway

An inverse agonist of orphan receptor GPR61 acts by a G protein-competitive allosteric mechanism

Organocatalytic Transfer Hydrogenation of Cyclic Enones

Discovery and Preclinical Characterization of 1‑Methyl‑3-(4‑methylpyridin‑3‑yl)‑6‑(pyridin‑2‑ylmethoxy)‑1H‑pyrazolo-[3,4‑b]pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator

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

Enantioselective Organocatalytic Hydride Reduction

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

Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE

Design and Discovery of 6‑[(3S,4S)‑4-Methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro‑2H‑pyran-4-yl)-1,5-dihydro‑4H‑pyrazolo[3,4‑d]pyrimidin-4-one (PF-04447943), a Selective Brain Penetrant PDE9A Inhibitor for the Treatment of Cognitive Disorders

An oral SARS-CoV-2 M pro inhibitor clinical candidate for the treatment of COVID-19

Quantitative Translational Analysis of Brain Kynurenic Acid Modulation via Irreversible Kynurenine Aminotransferase II Inhibition

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

Discovery and Characterization of (R)‑6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1‑c][1,4]oxazin-4(9H)‑one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates

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

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

Design and Discovery of 6-[(3 S ,4 S )-4-Methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2 H -pyran-4-yl)-1,5-dihydro-4 H -pyrazolo[3,4- d ]pyrimidin-4-one (PF-04447943), a Selective Brain Penetrant PDE9A Inhibitor for the Treatment of Cognitive Disorders

Discovery and Preclinical Characterization of 1-Methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1 H -pyrazolo-[3,4- b ]pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator

ChemInform Abstract: Synthesis of ortho-Substituted Nitroaromatics via Improved Negishi Coupling Conditions

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

Fingolimod (Gilenya): The First Oral Treatment for Multiple Sclerosis

Organocatalytic Transfer Hydrogenation of Cyclic Enones

Enantioselective Organocatalytic Hydride Reduction

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