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mGluR2 positive allosteric modulators: a patent review (2009 – present)

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Pages 629-647 | Published online: 02 Mar 2013

Keep up to date with the latest research on this topic with citation updates for this article.

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Andrés A Trabanco, José Manuel Bartolomé & José María Cid. (2019) mGluR2 positive allosteric modulators: an updated patent review (2013–2018). Expert Opinion on Therapeutic Patents 29:7, pages 497-507.
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Sylvain Celanire, Iyassu Sebhat, Juergen Wichmann, Stanislas Mayer, Stephan Schann & Silvia Gatti. (2015) Novel metabotropic glutamate receptor 2/3 antagonists and their therapeutic applications: a patent review (2005 – present). Expert Opinion on Therapeutic Patents 25:1, pages 69-90.
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Articles from other publishers (31)

Si Han Li, Khaled S. Abd-Elrahman & Stephen S.G. Ferguson. (2022) Targeting mGluR2/3 for treatment of neurodegenerative and neuropsychiatric diseases. Pharmacology & Therapeutics 239, pages 108275.
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Ana I. de Lucas, Juan A. Vega, Aránzazu García Molina, María Lourdes Linares, Gary Tresadern, Hilde Lavreysen, Daniel Oehlrich, Andrés A. Trabanco & José M. Cid. (2021) Scaffold Hopping to Imidazo[1,2- a ]pyrazin-8-one Positive Allosteric Modulators of Metabotropic Glutamate 2 Receptor . ACS Omega 6:35, pages 22997-23006.
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Ya-Ting Wang, Xiao-Le Wang, Si-Tong Feng, Nai-Hong Chen, Zhen-Zhen Wang & Yi Zhang. (2021) Novel rapid-acting glutamatergic modulators: Targeting the synaptic plasticity in depression. Pharmacological Research 171, pages 105761.
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Xiaofei Zhang, Zhiwei Xiao, Katsushi Kumata, Tomoteru Yamasaki, Lee Josephson, Ming-Rong Zhang, Lu Wang & Steven H. Liang. 2021. Metabotropic Glutamate Receptor Technologies. Metabotropic Glutamate Receptor Technologies 23 37 .
Tao Chen, Hao Xiong, Jing-Fang Yang, Xiao-Lei Zhu, Ren-Yu Qu & Guang-Fu Yang. (2020) Diaryl Ether: A Privileged Scaffold for Drug and Agrochemical Discovery. Journal of Agricultural and Food Chemistry 68:37, pages 9839-9877.
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Ana Isabel de Lucas, Juan Antonio Vega, Encarnación Matesanz, María Lourdes Linares, Aránzazu García Molina, Gary Tresadern, Hilde Lavreysen, Andrés A. Trabanco & José María Cid. (2019) Spiro-oxindole Piperidines and 3-(Azetidin-3-yl)-1 H -benzimidazol-2-ones as mGlu 2 Receptor PAMs . ACS Medicinal Chemistry Letters 11:3, pages 303-308.
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Laura Pérez-Benito, Claudia Llinas del Torrent, Leonardo Pardo & Gary Tresadern. 2020. From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors. From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors 1 33 .
Youwen Xu & Zizhong Li. (2019) Imaging metabotropic glutamate receptor system: Application of positron emission tomography technology in drug development. Medicinal Research Reviews 39:5, pages 1892-1922.
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Claudia Llinas del Torrent, Laura Pérez-Benito & Gary Tresadern. (2019) Computational Drug Design Applied to the Study of Metabotropic Glutamate Receptors. Molecules 24:6, pages 1098.
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Elizabeth S. Childress, Joshua M. Wieting, Andrew S. Felts, Megan M. Breiner, Madeline F. Long, Vincent B. Luscombe, Alice L. Rodriguez, Hyekyung P. Cho, Anna L. Blobaum, Colleen M. NiswenderKyle A. Emmitte, P. Jeffrey ConnCraig W. Lindsley. (2018) Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu 2 ) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1,5- a ]pyrimidine-5-carboxamide and Thieno[3,2- b ]pyridine-5-carboxamide Cores . Journal of Medicinal Chemistry 62:1, pages 378-384.
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Xiaofei Zhang, Katsushi Kumata, Tomoteru Yamasaki, Ran Cheng, Akiko Hatori, Longle Ma, Yiding Zhang, Lin Xie, Lu Wang, Hye Jin Kang, Douglas J. Sheffler, Nicholas D. P. Cosford, Ming-Rong Zhang & Steven H. Liang. (2017) Synthesis and Preliminary Studies of a Novel Negative Allosteric Modulator, 7-((2,5-Dioxopyrrolidin-1-yl)methyl)-4-(2-fluoro-4-[ 11 C]methoxyphenyl) quinoline-2-carboxamide, for Imaging of Metabotropic Glutamate Receptor 2 . ACS Chemical Neuroscience 8:9, pages 1937-1948.
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Katrina A. Bollinger, Andrew S. Felts, Christopher J. Brassard, Julie L. Engers, Alice L. Rodriguez, Rebecca L. Weiner, Hyekyung P. Cho, Sichen Chang, Michael Bubser, Carrie K. Jones, Anna L. Blobaum, Colleen M. Niswender, P. Jeffrey Conn, Kyle A. Emmitte & Craig W. Lindsley. (2017) Design and Synthesis of mGlu 2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core . ACS Medicinal Chemistry Letters 8:9, pages 919-924.
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Maarten L. J. Doornbos, José María Cid, Jordi Haubrich, Alexandro Nunes, Jasper W. van de Sande, Sophie C. Vermond, Thea Mulder-Krieger, Andrés A. Trabanco, Abdellah Ahnaou, Wilhelmus H. Drinkenburg, Hilde Lavreysen, Laura H. Heitman, Adriaan P. IJzerman & Gary Tresadern. (2017) Discovery and Kinetic Profiling of 7-Aryl-1,2,4-triazolo[4,3- a ]pyridines: Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2 . Journal of Medicinal Chemistry 60:15, pages 6704-6720.
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L. Lundström, C. Bissantz, J. Beck, M. Dellenbach, T.J. Woltering, J. Wichmann & S. Gatti. (2017) Reprint of Pharmacological and molecular characterization of the positive allosteric modulators of metabotropic glutamate receptor 2. Neuropharmacology 115, pages 115-127.
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L. Lundström, C. Bissantz, J. Beck, M. Dellenbach, T.J. Woltering, J. Wichmann & S. Gatti. (2016) Pharmacological and molecular characterization of the positive allosteric modulators of metabotropic glutamate receptor 2. Neuropharmacology 111, pages 253-265.
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A. A. Trabanco, J. M. Cid & G. Tresadern. 2016. Allosterism in Drug Discovery. Allosterism in Drug Discovery 156 174 .
Jose María Cid, Gary Tresadern, Juan Antonio Vega, Ana Isabel de Lucas, Alcira del Cerro, Encarnación Matesanz, María Lourdes Linares, Aránzazu García, Laura Iturrino, Laura Pérez-Benito, Gregor J. Macdonald, Daniel Oehlrich, Hilde Lavreysen, Luc Peeters, Marc Ceusters, Abdellah Ahnaou, Wilhelmus Drinkenburg, Claire Mackie, Marijke Somers & Andrés A. Trabanco. (2016) 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) . Journal of Medicinal Chemistry 59:18, pages 8495-8507.
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Craig W. Lindsley, Kyle A. Emmitte, Corey R. Hopkins, Thomas M. Bridges, Karen J. Gregory, Colleen M. Niswender & P. Jeffrey Conn. (2016) Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors. Chemical Reviews 116:11, pages 6707-6741.
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A. Ahnaou, P. de Boer, H. Lavreysen, H. Huysmans, V. Sinha, L. Raeymaekers, T. Van De Casteele, J.M. Cid, L. Van Nueten, G.J. Macdonald, J.A. Kemp & W.H.I.M. Drinkenburg. (2016) Translational neurophysiological markers for activity of the metabotropic glutamate receptor (mGluR2) modulator JNJ-40411813: Sleep EEG correlates in rodents and healthy men. Neuropharmacology 103, pages 290-305.
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Maarten L J Doornbos, Laura Pérez-Benito, Gary Tresadern, Thea Mulder-Krieger, Ilse Biesmans, Andrés A Trabanco, Jose María Cid, Hilde Lavreysen, Adriaan P IJzerman & Laura H Heitman. (2016) Molecular mechanism of positive allosteric modulation of the metabotropic glutamate receptor 2 by JNJ-46281222. British Journal of Pharmacology 173:3, pages 588-600.
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Mark E. Layton, Alexander J. Reif, Timothy J. Hartingh, Kevin Rodzinak, Vadim Dudkin, Cheng Wang, Ken Arrington, Michael J. KellyIIIIII, Robert M. Garbaccio, Julie A. O’Brien, Brian C. Magliaro, Jason M. Uslaner, Sarah L. Huszar, Kerry L. Fillgrove, Cuyue Tang, Yuhsin Kuo & Marlene A. Jacobson. (2016) Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis. Bioorganic & Medicinal Chemistry Letters 26:4, pages 1260-1264.
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Lorenz Deutschenbaur, Johannes Beck, Anna Kiyhankhadiv, Markus Mühlhauser, Stefan Borgwardt, Marc Walter, Gregor Hasler, Daniel Sollberger & Undine E. Lang. (2016) Role of calcium, glutamate and NMDA in major depression and therapeutic application. Progress in Neuro-Psychopharmacology and Biological Psychiatry 64, pages 325-333.
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Kasper Harpsøe, Vignir Isberg, Benjamin G. Tehan, Dahlia Weiss, Angela Arsova, Fiona H. Marshall, Hans Bräuner-Osborne & David E. Gloriam. (2015) Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors – A Structural Perspective of Ligands and Mutants. Scientific Reports 5:1.
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Oscar Delgado, Francisca Delgado, Juan Antonio Vega & Andrés A. Trabanco. (2015) N-bridged 5,6-bicyclic pyridines: Recent applications in central nervous system disorders. European Journal of Medicinal Chemistry 97, pages 719-731.
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James N. Samson & Albert H. C. Wong. 2015. Drug Discovery for Schizophrenia. Drug Discovery for Schizophrenia 1 27 .
A Farinha, H Lavreysen, L Peeters, B Russo, S Masure, A A Trabanco, J Cid & G Tresadern. (2015) Molecular determinants of positive allosteric modulation of the human metabotropic glutamate receptor 2. British Journal of Pharmacology 172:9, pages 2383-2396.
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Hilde Lavreysen, Abdellah Ahnaou, Wilhelmus Drinkenburg, Xavier Langlois, Claire Mackie, Stefan Pype, Robert Lütjens, Emmanuel Le Poul, Andrés A. Trabanco & José María Cid Nuñez. (2015) Pharmacological and pharmacokinetic properties of JNJ-40411813, a positive allosteric modulator of the mGlu2 receptor. Pharmacology Research & Perspectives 3:1, pages e00096.
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Gary Tresadern, José-Maria Cid & Andrés A. Trabanco. (2014) QSAR design of triazolopyridine mGlu2 receptor positive allosteric modulators. Journal of Molecular Graphics and Modelling 53, pages 82-91.
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José María Cid, Gary Tresadern, Guillaume Duvey, Robert Lütjens, Terry Finn, Jean-Philippe Rocher, Sonia Poli, Juan Antonio Vega, Ana Isabel de Lucas, Encarnación Matesanz, María Lourdes Linares, José Ignacio Andrés, Jesús Alcazar, José Manuel Alonso, Gregor J. Macdonald, Daniel Oehlrich, Hilde Lavreysen, Abdelah Ahnaou, Wilhelmus Drinkenburg, Claire Mackie, Stefan Pype, David Gallacher & Andrés A. Trabanco. (2014) Discovery of 1-Butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1 H )-pyridone (JNJ-40411813): A Novel Positive Allosteric Modulator of the Metabotropic Glutamate 2 Receptor . Journal of Medicinal Chemistry 57:15, pages 6495-6512.
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E. V. Radchenko, D. S. Karlov, V. A. Palyulin & N. S. Zefirov. (2014) Molecular modeling of the transmembrane domain of mGluR2 metabotropic glutamate receptor and the binding site of its positive allosteric modulators. Doklady Biochemistry and Biophysics 454:1, pages 13-16.
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José M. Cid, Andrés A. Trabanco & Hilde Lavreysen. 2015. Small Molecule Therapeutics for Schizophrenia. Small Molecule Therapeutics for Schizophrenia 101 142 .

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