1,4-Oxazine β‑Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads
Rombouts, Frederik J. R, Tresadern, Gary, Delgado, Oscar, Martínez-Lamenca, Carolina, Van Gool, Michiel, García-Molina, Aránzazu, Alonso de Diego, Sergio A, Oehlrich, Daniel, Prokopcova, Hana, Alonso, José Manuel, Austin, Nigel, Borghys, Herman, Van Brandt, Sven, Surkyn, Michel, De Cleyn, Michel, Vos, Ann, Alexander, Richard, Macdonald, Gregor, Moechars, Dieder, Gijsen, Harrie, Trabanco, Andrés A
Published in Journal of medicinal chemistry (22.10.2015)
Published in Journal of medicinal chemistry (22.10.2015)
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Diazaspirononane Nonsaccharide Inhibitors of O‑GlcNAcase (OGA) for the Treatment of Neurodegenerative Disorders
Martínez-Viturro, Carlos M, Trabanco, Andrés A, Royes, Jordi, Fernández, Elena, Tresadern, Gary, Vega, Juan A, del Cerro, Alcira, Delgado, Francisca, García Molina, Aránzazu, Tovar, Fulgencio, Shaffer, Paul, Ebneth, Andreas, Bretteville, Alexis, Mertens, Liesbeth, Somers, Marijke, Alonso, Jose M, Bartolomé-Nebreda, José M
Published in Journal of medicinal chemistry (25.11.2020)
Published in Journal of medicinal chemistry (25.11.2020)
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Optimization of 1,4-Oxazine β‑Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate
Gijsen, Harrie J. M, Alonso de Diego, Sergio A, De Cleyn, Michel, García-Molina, Aránzazu, Macdonald, Gregor J, Martínez-Lamenca, Carolina, Oehlrich, Daniel, Prokopcova, Hana, Rombouts, Frederik J. R, Surkyn, Michel, Trabanco, Andrés A, Van Brandt, Sven, Van den Bossche, Dries, Van Gool, Michiel, Austin, Nigel, Borghys, Herman, Dhuyvetter, Deborah, Moechars, Diederik
Published in Journal of medicinal chemistry (28.06.2018)
Published in Journal of medicinal chemistry (28.06.2018)
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Scaffold Hopping to Imidazo[1,2‑a]pyrazin-8-one Positive Allosteric Modulators of Metabotropic Glutamate 2 Receptor
de Lucas, Ana I, Vega, Juan A, García Molina, Aránzazu, Linares, María Lourdes, Tresadern, Gary, Lavreysen, Hilde, Oehlrich, Daniel, Trabanco, Andrés A, Cid, José M
Published in ACS omega (07.09.2021)
Published in ACS omega (07.09.2021)
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Correction to Optimization of 1,4-Oxazine β‑Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate
Gijsen, Harrie J. M, Alonso de Diego, Sergio A, De Cleyn, Michel, García-Molina, Aránzazu, Macdonald, Gregor J, Martinez-Lamenca, Carolina, Oehlrich, Daniel, Prokopcova, Hana, Rombouts, Frederik J. R, Surkyn, Michel, Trabanco, Andrés A, Van Brandt, Sven, Van den Bossche, Dries, Van Gool, Michiel, Austin, Nigel, Borghys, Herman, Dhuyvetter, Deborah, Urmaliya, Vijay, Teisman, Ard, Moechars, Diederik
Published in Journal of medicinal chemistry (27.12.2018)
Published in Journal of medicinal chemistry (27.12.2018)
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Spiro-oxindole Piperidines and 3‑(Azetidin-3-yl)‑1H‑benzimidazol-2-ones as mGlu2 Receptor PAMs
de Lucas, Ana Isabel, Vega, Juan Antonio, Matesanz, Encarnación, Linares, María Lourdes, García Molina, Aránzazu, Tresadern, Gary, Lavreysen, Hilde, Trabanco, Andrés A, Cid, José María
Published in ACS medicinal chemistry letters (12.03.2020)
Published in ACS medicinal chemistry letters (12.03.2020)
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Discovery of 6,7-Dihydropyrazolo1,5-apyrazin-4(5H)-one Derivatives as mGluR2 Negative Allosteric Modulators with In Vivo Activity in a Rodent's Model of Cognition
Alonso de Diego, Sergio A, Linares, María Lourdes, García Molina, Aránzazu, de Lucas, Ana Isabel, Del Cerro, Alcira, Alonso, Jose Manuel, Ver Donck, Luc, Cid, Jose María, Trabanco, Andrés A, Van Gool, Michiel
Published in Journal of medicinal chemistry (12.09.2024)
Published in Journal of medicinal chemistry (12.09.2024)
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Journal Article
Discovery of 6,7-Dihydropyrazolo[1,5- a ]pyrazin-4(5 H )-one Derivatives as mGluR 2 Negative Allosteric Modulators with In Vivo Activity in a Rodent’s Model of Cognition
Alonso de Diego, Sergio A., Linares, María Lourdes, García Molina, Aránzazu, de Lucas, Ana Isabel, del Cerro, Alcira, Alonso, Jose Manuel, Ver Donck, Luc, Cid, Jose María, Trabanco, Andrés A., Van Gool, Michiel
Published in Journal of medicinal chemistry (12.09.2024)
Published in Journal of medicinal chemistry (12.09.2024)
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Inhibition of the Alanine-Serine-Cysteine‑1 Transporter by BMS-466442
Torrecillas, Ivan R, Conde-Ceide, Susana, de Lucas, Ana Isabel, Garcı́a Molina, Aránzazu, Trabanco, Andrés A, Lavreysen, Hilde, Pardo, Leonardo, Tresadern, Gary
Published in ACS chemical neuroscience (15.05.2019)
Published in ACS chemical neuroscience (15.05.2019)
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Spiro-oxindole Piperidines and 3-(Azetidin-3-yl)-1 H -benzimidazol-2-ones as mGlu 2 Receptor PAMs
de Lucas, Ana Isabel, Vega, Juan Antonio, Matesanz, Encarnación, Linares, María Lourdes, García Molina, Aránzazu, Tresadern, Gary, Lavreysen, Hilde, Trabanco, Andrés A, Cid, José María
Published in ACS medicinal chemistry letters (12.03.2020)
Published in ACS medicinal chemistry letters (12.03.2020)
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6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglur2 receptors
Trabanco-Suárez, Andrés, Delgado-González, Óscar, Megens, Antonius, Van Gool, Michiel, Decorte, Annelies, Andrés-Gil, José, Macdonald, Gregor, Alonso-De Diego, Sergio-Alvar, García-Molina, Aránzazu, Cid-Núñez, José
Year of Publication 25.06.2021
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Year of Publication 25.06.2021
Patent
Substituted 6,7-dihydropyrazolo[1,5-a]pyrazines as negative allosteric modulators of mGluR2 receptors
Alonso-de Diego, Sergio-Alvar, Delgado-González, Óscar, MacDonald, Gregor James, García-Molina, Aránzazu, Van Gool, Michiel Luc Maria, Andrés-Gil, José Ignacio, Cid-Núñez, José Maria, Decorte, Annelies Marie Antonius, Megens, Antonius Adrianus Hendrikus Petrus, Trabanco-Suárez, Andrés Avelino
Year of Publication 10.03.2020
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Year of Publication 10.03.2020
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SUBSTITUTED 6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZINES AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
Alonso-de Diego, Sergio-Alvar, Delgado-González, Óscar, MacDonald, Gregor James, García-Molina, Aránzazu, Van Gool, Michiel Luc Maria, Andrés-Gil, José Ignacio, Cid-Núñez, José Maria, Decorte, Annelies Marie Antonius, Megens, Antonius Adrianus Hendrikus Petrus, Trabanco-Suárez, Andrés Avelino
Year of Publication 21.02.2019
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Year of Publication 21.02.2019
Patent
6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
Cid-Núnez, José Maria, Decorte, Annelies, Marie, Antonius, Delgado-González, Óscar, MacDonald, Gregor James, Alonso-De Diego, Sergio-Alvar, García-Molina, Aránzazu, Andrés-Gil, José, Ignacio, Van Gool, Michiel Luc Maria, Megens, Antonius Adrianus Hendrikus, Trabanco-Suárez, Andrés Avelino
Year of Publication 06.10.2017
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Year of Publication 06.10.2017
Patent
6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
CID-NÚÑEZ, José Maria, ANDRÉS-GIL, José Ignacio, ALONSO-DE DIEGO, Sergio-Alvar, DELGADO-GONZÁLEZ, Óscar, GARCÍA-MOLINA, Aránzazu, MEGENS, Antonius Adrianus Hendrikus Petrus, MACDONALD, Gregor James, VAN GOOL, Michiel Luc Maria, TRABANCO-SUÁREZ, Andrés Avelino, DECORTE, Annelies Marie Antonius
Year of Publication 20.07.2018
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Year of Publication 20.07.2018
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6,7-DIHYDROPYRAZOLO[1,5-A]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
MACDONALD, GREGOR JAMES, CID-NÚÑEZ, JOSÉ MARIA, DELGADO-GONZÁLEZ, ÓSCAR, GARCÍA-MOLINA, ARÁNZAZU, MEGENS, ANTONIUS ADRIANUS HENDRIKUS PETRUS, DECORTE, ANNELIES MARIE ANTONIUS, ALONSO-DE DIEGO, SERGIO-ALVAR, TRABANCO-SUÁREZ, ANDRÉS AVELINO, ANDRÉS-GIL, JOSÉ IGNACIO, VAN GOOL, MICHIEL LUC MARIA
Year of Publication 31.10.2017
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Year of Publication 31.10.2017
Patent
6,7-DIHYDROPYRAZOLO[1,5-A]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
TRABANCO-SUÁREZ, ANDRÉS, AVELINO, DELGADO-GONZÁLEZ, ÓSCAR, MEGENS, ANTONIUS, ADRIANUS, HENDRIKUS, PETRUS, DECORTE, ANNELIES, MARIE, ANTONIUS, GARCÍA-MOLINA, ARÁNZAZU, CID-NÚÑEZ, JOSÉ, MARIA, VAN GOOL, MICHIEL, LUC, MARIA, ANDRÉS-GIL, JOSÉ, IGNACIO, ALONSO-DE DIEGO, SERGIO-ALVAR, MACDONALD, GREGOR, JAMES
Year of Publication 31.10.2017
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Year of Publication 31.10.2017
Patent
6,7-DIHYDROPYRAZOLO[1,5-A]PYRAZIN-4(5H)-ONFORBINDELSER OG DERES ANVENDELSE SOM NEGATIVE ALLOSTERISKE MODULATORER AF MGLUR2-RECEPTORER
DECORTE, Annelies, Marie, Antonius, TRABANCO-SUÁREZ, Andrés, Avelino, VAN GOOL, Michiel, Luc, Maria, ALONSO-DE DIEGO, Sergio-Alvar, DELGADO-GONZÁLEZ, Óscar, CID-NÚÑEZ, José, Maria, MACDONALD, Gregor, James, GARCÍA-MOLINA, Aránzazu, ANDRÉS-GIL, José, Ignacio, MEGENS, Antonius, Adrianus, Hendrikus, Petrus
Year of Publication 28.08.2017
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Year of Publication 28.08.2017
Patent
6,7-DIHYDROPYRAZOLO[1,5-A]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
GREGOR JAMES MACDONALD, JOSÉ, IGNACIO ANDRÉS-GIL, MICHIEL, LUC, MARIA VAN GOOL, ANDRÉS AVELINO TRABANCO-SUÁREZ, ARÁNZAZU GARCÍA-MOLINA, SERGIO-ALVAR ALONSO-DE DIEGO, JOSÉ, MARIA CID-NÚÑEZ, ÓSCAR DELGADO-GONZÁLEZ, ANNELIES, MARIE, ANTONIUS DECORTE, ANTONIUS ADRIANUS HENDRIKUS PETRUS MEGENS
Year of Publication 16.08.2017
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Year of Publication 16.08.2017
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6,7-DIHYDROPYRAZOLO[1,5-A]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
DECORTE, Annelies, Marie, Antonius, TRABANCO-SUÁREZ, Andrés, Avelino, VAN GOOL, Michiel, Luc, Maria, ALONSO-DE DIEGO, Sergio-Alvar, DELGADO-GONZÁLEZ, Óscar, CID-NÚÑEZ, José, Maria, MACDONALD, Gregor, James, GARCÍA-MOLINA, Aránzazu, ANDRÉS-GIL, José, Ignacio, MEGENS, Antonius, Adrianus, Hendrikus, Petrus
Year of Publication 10.05.2017
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Year of Publication 10.05.2017
Patent