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Patented PDE10A inhibitors: novel compounds since 2007

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Pages 1715-1725 | Published online: 26 Nov 2009

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Jan Kehler. (2013) Phosphodiesterase 10A inhibitors: a 2009 – 2012 patent update. Expert Opinion on Therapeutic Patents 23:1, pages 31-45.
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Articles from other publishers (41)

Harsh S. Amin, Palak K. Parikh & Manjunath D. Ghate. (2021) Medicinal chemistry strategies for the development of phosphodiesterase 10A (PDE10A) inhibitors - An update of recent progress. European Journal of Medicinal Chemistry 214, pages 113155.
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Artur Świerczek, Agnieszka Jankowska, Grażyna Chłoń-Rzepa, Maciej Pawłowski & Elżbieta Wyska. (2019) Advances in the Discovery of PDE10A Inhibitors for CNS-Related Disorders. Part 2: Focus on Schizophrenia. Current Drug Targets 20:16, pages 1652-1669.
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Hervé Geneste, Karla Drescher, Clarissa Jakob, Loïc Laplanche, Michael Ochse & Maricel Torrent. (2019) Novel, potent, selective, and brain penetrant phosphodiesterase 10A inhibitors. Bioorganic & Medicinal Chemistry Letters 29:3, pages 406-412.
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Elham Gholami Rostami & Mohammad H. Fatemi. (2018) Comparative molecular field analysis and hologram quantitative structure activity relationship studies of pyrimidine series as potent phosphodiesterase 10A inhibitors. Journal of the Chinese Chemical Society 65:11, pages 1293-1306.
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Rafał Moszczyński-Pętkowski, Jakub Majer, Małgorzata Borkowska, Łukasz Bojarski, Sylwia Janowska, Mikołaj Matłoka, Filip Stefaniak, Damian Smuga, Katarzyna Bazydło, Krzysztof Dubiel & Maciej Wieczorek. (2018) Synthesis and characterization of novel classes of PDE10A inhibitors - 1H-1,3-benzodiazoles and imidazo[1,2-a]pyrimidines. European Journal of Medicinal Chemistry 155, pages 96-116.
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Takashi Sasaki, Jun Kotera & Kenji Omori. 2018. Encyclopedia of Signaling Molecules. Encyclopedia of Signaling Molecules 3957 3961 .
Luca Codutti, Manuela Grimaldi & Teresa Carlomagno. (2017) Structure-Based Design of Scaffolds Targeting PDE10A by INPHARMA-NMR. Journal of Chemical Information and Modeling 57:6, pages 1488-1498.
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J. Kehler. 2017. Comprehensive Medicinal Chemistry III. Comprehensive Medicinal Chemistry III 384 407 .
Gretchen L. Snyder & Kimberly E. Vanover. 2017. Phosphodiesterases: CNS Functions and Diseases. Phosphodiesterases: CNS Functions and Diseases 385 409 .
Susann Schröder, Barbara Wenzel, Winnie Deuther-Conrad, Matthias Scheunemann & Peter Brust. (2016) Novel Radioligands for Cyclic Nucleotide Phosphodiesterase Imaging with Positron Emission Tomography: An Update on Developments Since 2012. Molecules 21:5, pages 650.
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Sally Wagner, Matthias Scheunemann, Karolin Dipper, Ute Egerland, Norbert Hoefgen, Jörg Steinbach & Peter Brust. (2016) Development of highly potent phosphodiesterase 10A (PDE10A) inhibitors: Synthesis and in vitro evaluation of 1,8-dipyridinyl- and 1-pyridinyl-substituted imidazo[1,5-a]quinoxalines. European Journal of Medicinal Chemistry 107, pages 97-108.
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Erik Rosendahl Kjellgren, Oliver Emil Skytte Glue, Peter Reinholdt, Julie Egeskov Meyer, Jacob Kongsted & Vasanthanathan Poongavanam. (2015) A comparative study of binding affinities for 6,7-dimethoxy-4-pyrrolidylquinazolines as phosphodiesterase 10A inhibitors using the linear interaction energy method. Journal of Molecular Graphics and Modelling 61, pages 44-52.
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Alexandru Vlasceanu, Mikkel Jessing & John Paul Kilburn. (2015) BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors. Bioorganic & Medicinal Chemistry 23:15, pages 4453-4461.
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José-Manuel Bartolomé-Nebreda, Susana Conde-Ceide & María García. (2015) Phosphodiesterase 10A inhibitors: analysis of US/EP patents granted since 2012. Pharmaceutical Patent Analyst 4:3, pages 161-186.
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Jan Kehler, John Paul Kilburn, Sergio Estrada, Søren Rahn Christensen, Anders Wall, Alf Thibblin, Mark Lubberink, Christoffer Bundgaard, Lise Tøttrup Brennum, Björn Steiniger-Brach, Claus Tornby Christoffersen, Stine Timmermann, Mads Kreilgaard, Gunnar Antoni, Benny Bang-Andersen & Jacob Nielsen. (2014) Discovery and Development of 11 C-Lu AE92686 as a Radioligand for PET Imaging of Phosphodiesterase10A in the Brain . Journal of Nuclear Medicine 55:9, pages 1513-1518.
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Antonio Dore, Battistina Asproni, Alessia Scampuddu, Gerard Aime Pinna, Claus Tornby Christoffersen, Morten Langgård & Jan Kehler. (2014) Synthesis and SAR study of novel tricyclic pyrazoles as potent phosphodiesterase 10A inhibitors. European Journal of Medicinal Chemistry 84, pages 181-193.
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Anton A. H. P. Megens, Herman M. R. Hendrickx, Michel M. A. Mahieu, Annemie L. Y. Wellens, Peter Boer & Greet Vanhoof. (2014) PDE 10A inhibitors stimulate or suppress motor behavior dependent on the relative activation state of the direct and indirect striatal output pathways . Pharmacology Research & Perspectives 2:4.
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Gregor Schwan, Ghadir Barbar Asskar, Norbert Höfgen, Lenka Kubicova, Uta Funke, Ute Egerland, Michael Zahn, Karen Nieber, Matthias Scheunemann, Norbert Sträter, Peter Brust & Detlef Briel. (2014) Fluorine-Containing 6,7-Dialkoxybiaryl-Based Inhibitors for Phosphodiesterase 10 A: Synthesis and in vitro Evaluation of Inhibitory Potency, Selectivity, and Metabolism. ChemMedChem 9:7, pages 1476-1487.
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Erik I. Charych & Nicholas J. Brandon. 2014. Cyclic-Nucleotide Phosphodiesterases In The Central Nervous System. Cyclic-Nucleotide Phosphodiesterases In The Central Nervous System 247 268 .
Frank S. Menniti, Niels Plath, Niels Svenstrup & Christopher J. Schmidt. 2014. Cyclic-Nucleotide Phosphodiesterases In The Central Nervous System. Cyclic-Nucleotide Phosphodiesterases In The Central Nervous System 77 114 .
Sanjib Das, Rajendra L. Harde, Dnyaneshwar E. Shelke, Neelima Khairatkar-Joshi, Malini Bajpai, Ratika S. Sapalya, Harshada V. Surve, Girish S. Gudi, Rambabu Pattem, Dayanidhi B. Behera, Satyawan B. Jadhav & Abraham Thomas. (2014) Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: Part I. Bioorganic & Medicinal Chemistry Letters 24:9, pages 2073-2078.
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Thomas A. Chappie & Patrick Verhoest. 2014. Phosphodiesterases and Their Inhibitors. Phosphodiesterases and Their Inhibitors 65 82 .
Anton A. H. P. Megens, Herman M. R. Hendrickx, Koen A. Hens, Ineke Fonteyn, Xavier Langlois, Ilse Lenaerts, Marijke V. F. Somers, Peter de Boer & Greet Vanhoof. (2014) Pharmacology of JNJ-42314415, a Centrally Active Phosphodiesterase 10A (PDE10A) Inhibitor: A Comparison of PDE10A Inhibitors with D 2 Receptor Blockers as Potential Antipsychotic Drugs . Journal of Pharmacology and Experimental Therapeutics 349:1, pages 138-154.
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S Natesan, S Ashworth, J Nielsen, S-P Tang, C Salinas, S Kealey, J B Lauridsen, T B Stensbøl, R N Gunn, E A Rabiner & S Kapur. (2014) Effect of chronic antipsychotic treatment on striatal phosphodiesterase 10A levels: a [11C]MP-10 PET rodent imaging study with ex vivo confirmation. Translational Psychiatry 4:4, pages e376-e376.
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John Paul Kilburn, Jan Kehler, Morten Langgård, Mette N. Erichsen, Sebastian Leth-Petersen, Mogens Larsen, Claus Tornby Christoffersen & Jacob Nielsen. (2013) N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors. Bioorganic & Medicinal Chemistry 21:19, pages 6053-6062.
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Junfeng Li, Hongjun Jin, Haiying Zhou, Justin Rothfuss & Zhude Tu. (2013) Synthesis and in vitro biological evaluation of pyrazole group-containing analogues for PDE10A. MedChemComm 4:2, pages 443.
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S Miyamoto, N Miyake, L F Jarskog, W W Fleischhacker & J A Lieberman. (2012) Pharmacological treatment of schizophrenia: a critical review of the pharmacology and clinical effects of current and future therapeutic agents. Molecular Psychiatry 17:12, pages 1206-1227.
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Thomas A. Chappie, Christopher J. Helal & Xinjun Hou. (2012) Current Landscape of Phosphodiesterase 10A (PDE10A) Inhibition. Journal of Medicinal Chemistry 55:17, pages 7299-7331.
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Judith A. Siuciak & William J. Pitts. 2012. Targets and Emerging Therapies for Schizophrenia. Targets and Emerging Therapies for Schizophrenia 85 113 .
Udo Bauer, Fabrizio Giordanetto, Martin Bauer, Gavin O’Mahony, Kjell E. Johansson, Wolfgang Knecht, Judith Hartleib-Geschwindner, Eva Töppner Carlsson & Cristofer Enroth. (2012) Discovery of 4-hydroxy-1,6-naphthyridine-3-carbonitrile derivatives as novel PDE10A inhibitors. Bioorganic & Medicinal Chemistry Letters 22:5, pages 1944-1948.
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Uta Funke, Winnie Deuther-Conrad, Gregor Schwan, Aurélie Maisonial, Matthias Scheunemann, Steffen Fischer, Achim Hiller, Detlef Briel & Peter Brust. (2012) Radiosynthesis and Radiotracer Properties of a 7-(2-[18F]Fluoroethoxy)-6-methoxypyrrolidinylquinazoline for Imaging of Phosphodiesterase 10A with PET. Pharmaceuticals 5:2, pages 169-188.
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William T. McElroy, Zheng Tan, Kallol Basu, Shu-Wei Yang, Jennifer Smotryski, Ginny D. Ho, Deen Tulshian, William J. Greenlee, Deborra Mullins, Mario Guzzi, Xiaoping Zhang, Carina Bleickardt & Robert Hodgson. (2012) Pyrazoloquinolines as PDE10A inhibitors: Discovery of a tool compound. Bioorganic & Medicinal Chemistry Letters 22:3, pages 1335-1339.
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Shu-Wei Yang, Jennifer Smotryski, William T. McElroy, Zheng Tan, Ginny Ho, Deen Tulshian, William J. Greenlee, Mario Guzzi, Xiaoping Zhang, Deborra Mullins, Li Xiao, Alan Hruza, Tze-Ming Chan, Diane Rindgen, Carina Bleickardt & Robert Hodgson. (2012) Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia. Bioorganic & Medicinal Chemistry Letters 22:1, pages 235-239.
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Dominique M. Donato, Steven K. Hanks, Kenneth A. Jacobson, M. P. Suresh Jayasekara, Zhan-Guo Gao, Francesca Deflorian, John Papaconstantinou, Ching-Chyuan Hsieh, James H. DeFord, Krassimira Alexieva-Botcheva, Carl W. Anderson, Sheng-Wei Yang, Yuan-Hao Hsu, Linya You, Xiang-Jiao Yang, Miles D. Houslay, Joanna E. Gawecka, Joe W. Ramos, Maria Aparecida Nagai, Jonathan H. Clarke, Robin F. Irvine, Su Jun Lim, Willis X. Li, Sujeet Kumar, Ponniah Selvakumar, Rajendra K. Sharma, Takashi Sasaki, Jun Kotera, Kenji Omori, Lomon So, David A. Fruman, Makoto Murakami, Julian Gomez-Cambronero, Karen M. Henkels, Christopher T. Cottage, Balaji Sundararaman, Shabana Din, Nirmala Hariharan, Mark A. Sussman, Dana Onica, David W. Litchfield, Peter Storz, Anthony John Sadler, Emanuel E. Strehler, Daryl L. Goad, Michael A. Grillo, Peter Koulen, Hisashi Tatebe, Kazuhiro Shiozaki, Giorgio Iotti, Francesco Blasi, Daisuke Urano, Hiroshi Itoh, Rafael Linden, Vilma R. Martins, Marco A. M. Prado, Lai N. Chan, Fuyuhiko Tamanoi, Amanda Harvey, Mingyao Liu, Melissa Rodriguez, Nicholas R. Leslie, Laura Spinelli, Georgios Zilidis, Nimmi R. Weerasinghe, Priyanka Tibarewal, Laura M. Westrate, Jeffrey P. MacKeigan, Ari Elson, Liat Rousso-Noori, Timothy J. Bauler, Philip D. King, Marina Tiemi Shio & Martin Olivier. 2012. Encyclopedia of Signaling Molecules. Encyclopedia of Signaling Molecules 1388 1392 .
Zhanbin Zhang, Xiaoxia Lu, Jinbin Xu, Justin Rothfuss, Robert H. Mach & Zhude Tu. (2011) Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A. European Journal of Medicinal Chemistry 46:9, pages 3986-3995.
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Jan Kehler, Andreas Ritzen, Morten Langgård, Sebastian Leth Petersen, Mohamed M. Farah, Christoffer Bundgaard, Claus Tornby Christoffersen, Jacob Nielsen & John Paul Kilburn. (2011) Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors. Bioorganic & Medicinal Chemistry Letters 21:12, pages 3738-3742.
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Kanako Itoh, Tamaki Ishima, Jan Kehler & Kenji Hashimoto. (2011) Potentiation of NGF-induced neurite outgrowth in PC12 cells by papaverine: Role played by PLC-γ, IP3 receptors. Brain Research 1377, pages 32-40.
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Zhude Tu, Jinda Fan, Shihong Li, Lynne A. Jones, Jinquan Cui, Prashanth K. Padakanti, Jinbin Xu, Dexing Zeng, Kooresh I. Shoghi, Joel S. Perlmutter & Robert H. Mach. (2011) Radiosynthesis and in vivo evaluation of [11C]MP-10 as a PET probe for imaging PDE10A in rodent and non-human primate brain. Bioorganic & Medicinal Chemistry 19:5, pages 1666-1673.
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Battistina Asproni, Gabriele Murineddu, Amedeo Pau, Gérard A. Pinna, Morten Langgård, Claus Tornby Christoffersen, Jacob Nielsen & Jan Kehler. (2011) Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5-c]quinazolines as potent phosphodiesterase 10A inhibitors. Bioorganic & Medicinal Chemistry 19:1, pages 642-649.
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Nicholas J Bray, F Markus Leweke, Shitij Kapur & Andreas Meyer-Lindenberg. (2010) The neurobiology of schizophrenia: new leads and avenues for treatment. Current Opinion in Neurobiology 20:6, pages 810-815.
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Carmela Giampà, Daunia Laurenti, Serenella Anzilotti, Giorgio Bernardi, Frank S. Menniti & Francesca Romana Fusco. (2010) Inhibition of the Striatal Specific Phosphodiesterase PDE10A Ameliorates Striatal and Cortical Pathology in R6/2 Mouse Model of Huntington's Disease. PLoS ONE 5:10, pages e13417.
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