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A unique industrial-academic collaboration towards the next generation of schizophrenia therapeutics

Current topics in medicinal chemistry, 2014-02, Vol.14 (3), p.304

2014

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Molecular properties affecting fast dissociation from the D₂ receptor

Bioorganic & medicinal chemistry, 2011-04, Vol.19 (7), p.2231-2241

2011

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Discovery of a Potent, Selective, and Orally Active Phosphodiesterase 10A Inhibitor for the Potential Treatment of Schizophrenia

Journal of medicinal chemistry, 2014-05, Vol.57 (10), p.4196-4212

2014

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[1,2,4]Triazolo[1,5‑a]pyrimidine Phosphodiesterase 2A Inhibitors: Structure and Free-Energy Perturbation-Guided Exploration

Journal of medicinal chemistry, 2020-11, Vol.63 (21), p.12887-12910

2020

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Optimization of 1,4-Oxazine β‑Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate

Journal of medicinal chemistry, 2018-06, Vol.61 (12), p.5292-5303

2018

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Pharmacological characterization of JNJ-40068782, a new potent, selective, and systemically active positive allosteric modulator of the mGlu2 receptor and its radioligand [3H]JNJ-40068782

The Journal of pharmacology and experimental therapeutics, 2013-09, Vol.346 (3), p.514

2013

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Imidazo[1,2-a]pyridines: Orally Active Positive Allosteric Modulators of the Metabotropic Glutamate 2 Receptor

Journal of medicinal chemistry, 2012-03, Vol.55 (6), p.2688-2701

2012

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A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo

ACS medicinal chemistry letters, 2022-01, Vol.13 (1), p.76-83

2022

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Scaffold hopping from pyridones to imidazo[1,2- a]pyridines. New positive allosteric modulators of metabotropic glutamate 2 receptor

Bioorganic & medicinal chemistry letters, 2010, Vol.20 (1), p.175-179

2010

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Energy: Oilman at the peak

Nature (London), 2016-04, Vol.532 (7597), p.31-32

Macdonald, Gregor

2016

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Correction to Optimization of 1,4-Oxazine β‑Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate

Journal of medicinal chemistry, 2018-12, Vol.61 (24), p.11415-11415

2018

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Rational design and synthesis of aminopiperazinones as β-secretase (BACE) inhibitors

Bioorganic & medicinal chemistry letters, 2011-12, Vol.21 (24), p.7255-7260

2011

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1,3,5‐Trisubstituted Pyrazoles as Potent Negative Allosteric Modulators of the mGlu2/3 Receptors

ChemMedChem, 2017-06, Vol.12 (12), p.905-912

2017

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Identification of a Novel Orally Bioavailable Phosphodiesterase 10A (PDE10A) Inhibitor with Efficacy in Animal Models of Schizophrenia

Journal of medicinal chemistry, 2015-01, Vol.58 (2), p.978-993

2015

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1,3,5-Trisubstituted Pyrazoles as Potent Negative Allosteric Modulators of the mGlu 2/3 Receptors

ChemMedChem, 2017-06, Vol.12 (12), p.905-912

2017

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Heterotropic activation of the midazolam hydroxylase activity of CYP3A by a positive allosteric modulator of mGlu5: in vitro to in vivo translation and potential impact on clinically relevant drug-drug interactions

Drug metabolism and disposition, 2013-12, Vol.41 (12), p.2066

2013

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Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound

Bioorganic & medicinal chemistry letters, 2015-09, Vol.25 (17), p.3515-3519

2015

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A unique industrial-academic collaboration towards the next generation of schizophrenia therapeutics

Discovery of 3‑Cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8-trifluoromethyl[1,2,4]triazolo[4,3‑a]pyridine (JNJ-42153605): A Positive Allosteric Modulator of the Metabotropic Glutamate 2 Receptor

Discovery of 8‑Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3‑a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM)

Molecular properties affecting fast dissociation from the D₂ receptor

Discovery of a Potent, Selective, and Orally Active Phosphodiesterase 10A Inhibitor for the Potential Treatment of Schizophrenia

[1,2,4]Triazolo[1,5‑a]pyrimidine Phosphodiesterase 2A Inhibitors: Structure and Free-Energy Perturbation-Guided Exploration

Discovery of 1‑Butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)‑pyridone (JNJ-40411813): A Novel Positive Allosteric Modulator of the Metabotropic Glutamate 2 Receptor

Optimization of 1,4-Oxazine β‑Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate

Pharmacological characterization of JNJ-40068782, a new potent, selective, and systemically active positive allosteric modulator of the mGlu2 receptor and its radioligand [3H]JNJ-40068782

Imidazo[1,2-a]pyridines: Orally Active Positive Allosteric Modulators of the Metabotropic Glutamate 2 Receptor

A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo

Scaffold hopping from pyridones to imidazo[1,2- a]pyridines. New positive allosteric modulators of metabotropic glutamate 2 receptor

Energy: Oilman at the peak

Correction to Optimization of 1,4-Oxazine β‑Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate

Rational design and synthesis of aminopiperazinones as β-secretase (BACE) inhibitors

1,3,5‐Trisubstituted Pyrazoles as Potent Negative Allosteric Modulators of the mGlu2/3 Receptors

Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia

Identification of a Novel Orally Bioavailable Phosphodiesterase 10A (PDE10A) Inhibitor with Efficacy in Animal Models of Schizophrenia

Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents

1,3,5-Trisubstituted Pyrazoles as Potent Negative Allosteric Modulators of the mGlu 2/3 Receptors

Discovery of 1,4-Disubstituted 3-Cyano-2-pyridones: A New Class of Positive Allosteric Modulators of the Metabotropic Glutamate 2 Receptor

Heterotropic activation of the midazolam hydroxylase activity of CYP3A by a positive allosteric modulator of mGlu5: in vitro to in vivo translation and potential impact on clinically relevant drug-drug interactions

Dihydrothiazolopyridone Derivatives as a Novel Family of Positive Allosteric Modulators of the Metabotropic Glutamate 5 (mGlu5) Receptor

Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound

Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia

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