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Discovery and Preclinical Profiling of 3‑[4-(Morpholin-4-yl)‑7H‑pyrrolo[2,3‑d]pyrimidin-5-yl]benzonitrile (PF-06447475), a Highly Potent, Selective, Brain Penetrant, and in Vivo Active LRRK2 Kinase Inhibitor

Journal of medicinal chemistry, 2015-01, Vol.58 (1), p.419-432

2015

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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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Identification of Multiple 5‑HT4 Partial Agonist Clinical Candidates for the Treatment of Alzheimer’s Disease

Journal of medicinal chemistry, 2012-11, Vol.55 (21), p.9240-9254

2012

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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, 2024-04

2024

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Scalable, Telescoped Hydrogenolysis–Enzymatic Decarboxylation Process for the Asymmetric Synthesis of (R)‑α-Heteroaryl Propionic Acids

Organic process research & development, 2021-03, Vol.25 (3), p.421-426

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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Two Routes to 4‑Fluorobenzisoxazol-3-one in the Synthesis of a 5‑HT4 Partial Agonist

Organic process research & development, 2016-02, Vol.20 (2), p.233-241

2016

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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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Metabolism of a Serotonin-4 Receptor Partial Agonist 4-{4-[4-Tetrahydrofuran-3-yloxy)-Benzo[d]Isoxazol-3-yloxymethyl]-Piperidin-1-ylmethyl}-Tetrahydropyran-4-ol (TBPT): Identification of an Unusual Pharmacologically Active Cyclized Oxazolidine Metabolite in Human

Journal of pharmaceutical sciences, 2013-09, Vol.102 (9), p.3277-3293

2013

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Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014

The Journal of pharmacology and experimental therapeutics, 2010-07, Vol.334 (1), p.269

2010

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Diamide amino-imidazoles: A novel series of γ-secretase inhibitors for the treatment of Alzheimer’s disease

Bioorganic & medicinal chemistry letters, 2011-05, Vol.21 (9), p.2631-2636

2011

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Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as γ-secretase inhibitors: Discovery of PF-3084014

Bioorganic & medicinal chemistry letters, 2011-05, Vol.21 (9), p.2637-2640

2011

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P2-375: Efficacy of the novel γ-secretase inhibitor, PF-3084014, in reducing Aβ in brain, CSF, and plasma in guinea pigs and Tg2576 mice

Alzheimer's & dementia, 2008-07, Vol.4 (4), p.T482-T483

2008

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Two Routes to 4-Fluorobenzisoxazol-3-one in the Synthesis of a 5-HT 4 Partial Agonist

Organic process research & development, 2016-02, Vol.20 (2), p.233-241

2016

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Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist

Bioorganic & medicinal chemistry letters, 1998-02, Vol.8 (3), p.281-284

1998

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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

Volltextzugriff (PDF)

Identification of Multiple 5-HT 4 Partial Agonist Clinical Candidates for the Treatment of Alzheimer’s Disease

Journal of medicinal chemistry, 2012-11, Vol.55 (21), p.9240-9254

2012

Volltextzugriff (PDF)

Deamination of Quaternary Hydrazinium Halides. A Convenient Synthesis of Tertiary Amines

Synthetic communications, 1982-01, Vol.12 (10), p.801-805

1982

Volltextzugriff (PDF)

Amidrazones. 8. Synthesis of 1,2,4-oxdiazoles by thermolysis of N3-acylamidrazone ylides

Journal of heterocyclic chemistry, 1983-01, Vol.20 (1), p.69-71

1983

Volltextzugriff (PDF)

Amidrazones. 8 . Synthesis of 1,2,4‐oxdiazoles by thermolysis of N 3 ‐acylamidrazone ylides

Journal of heterocyclic chemistry, 1983-01, Vol.20 (1), p.69-71

1983

Volltextzugriff (PDF)

Amidrazones 9. Convenient Syntheses of 1-Alkyl-1-Phenylhydrazines and α,β-Unsaturated Amidrazones Via Base-Promoted Reactions of 1,1-Disubstituted-3-Amino-4,5-Dihydro-1H-Pyrazolium Salts

Synthetic communications, 1986-04, Vol.16 (5), p.585-596

1986

Volltextzugriff (PDF)

Green Roofs as Urban Ecosystems: Ecological Structures, Functions, and Services

Bioscience, 2007-11, Vol.57 (10), p.823-833

2007

Volltextzugriff (PDF)

Phase II clinical trial of metformin as a cancer stem cell-targeting agent in ovarian cancer

JCI insight, 2020-06, Vol.5 (11)

2020

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Discovery and Preclinical Profiling of 3‑[4-(Morpholin-4-yl)‑7H‑pyrrolo[2,3‑d]pyrimidin-5-yl]benzonitrile (PF-06447475), a Highly Potent, Selective, Brain Penetrant, and in Vivo Active LRRK2 Kinase Inhibitor

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

Identification of Multiple 5‑HT4 Partial Agonist Clinical Candidates for the Treatment of Alzheimer’s Disease

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

Scalable, Telescoped Hydrogenolysis–Enzymatic Decarboxylation Process for the Asymmetric Synthesis of (R)‑α-Heteroaryl Propionic Acids

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

Two Routes to 4‑Fluorobenzisoxazol-3-one in the Synthesis of a 5‑HT4 Partial Agonist

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

Metabolism of a Serotonin-4 Receptor Partial Agonist 4-{4-[4-Tetrahydrofuran-3-yloxy)-Benzo[d]Isoxazol-3-yloxymethyl]-Piperidin-1-ylmethyl}-Tetrahydropyran-4-ol (TBPT): Identification of an Unusual Pharmacologically Active Cyclized Oxazolidine Metabolite in Human

Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014

Diamide amino-imidazoles: A novel series of γ-secretase inhibitors for the treatment of Alzheimer’s disease

Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as γ-secretase inhibitors: Discovery of PF-3084014

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

P2-375: Efficacy of the novel γ-secretase inhibitor, PF-3084014, in reducing Aβ in brain, CSF, and plasma in guinea pigs and Tg2576 mice

Two Routes to 4-Fluorobenzisoxazol-3-one in the Synthesis of a 5-HT 4 Partial Agonist

Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist

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

Identification of Multiple 5-HT 4 Partial Agonist Clinical Candidates for the Treatment of Alzheimer’s Disease

Deamination of Quaternary Hydrazinium Halides. A Convenient Synthesis of Tertiary Amines

Amidrazones. 8. Synthesis of 1,2,4-oxdiazoles by thermolysis of N3-acylamidrazone ylides

Amidrazones. 8 . Synthesis of 1,2,4‐oxdiazoles by thermolysis of N 3 ‐acylamidrazone ylides

Amidrazones 9. Convenient Syntheses of 1-Alkyl-1-Phenylhydrazines and α,β-Unsaturated Amidrazones Via Base-Promoted Reactions of 1,1-Disubstituted-3-Amino-4,5-Dihydro-1H-Pyrazolium Salts

Green Roofs as Urban Ecosystems: Ecological Structures, Functions, and Services

Phase II clinical trial of metformin as a cancer stem cell-targeting agent in ovarian cancer

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