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5-hydroxytryptamine subtype 6 receptor modulators: a patent survey

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Pages 1171-1196 | Published online: 18 Aug 2010

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Gabriel C Léger & Fadi Massoud. (2013) Novel disease-modifying therapeutics for the treatment of Alzheimer’s disease. Expert Review of Clinical Pharmacology 6:4, pages 423-442.
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Alexandre V Ivachtchenko, Yan A Ivanenkov & Andrey V Skorenko. (2012) 5-HT6 receptor modulators: a patent update. Part 2. Diversity in heterocyclic scaffolds. Expert Opinion on Therapeutic Patents 22:10, pages 1123-1168.
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Alexandre V Ivachtchenko & Yan A Ivanenkov. (2012) 5HT6 receptor antagonists: a patent update. Part 1. Sulfonyl derivatives. Expert Opinion on Therapeutic Patents 22:8, pages 917-964.
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Articles from other publishers (23)

Hilda Ferrero, Maite Solas, Paul T. Francis & Maria J. Ramirez. (2016) Serotonin 5-HT6 Receptor Antagonists in Alzheimer’s Disease: Therapeutic Rationale and Current Development Status. CNS Drugs 31:1, pages 19-32.
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Alexandre V. Ivachtchenko, Yan Lavrovsky & Ilya Okun. (2016) AVN-101: A Multi-Target Drug Candidate for the Treatment of CNS Disorders. Journal of Alzheimer's Disease 53:2, pages 583-620.
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Paweł Zajdel, Krzysztof Marciniec, Grzegorz Satała, Vittorio Canale, Tomasz Kos, Anna Partyka, Magdalena Jastrzębska-Więsek, Anna Wesołowska, Agnieszka Basińska-Ziobroń, Jacek Wójcikowski, Władysława A. Daniel, Andrzej J. Bojarski & Piotr Popik. (2016) N 1-Azinylsulfonyl-1 H -indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties . ACS Medicinal Chemistry Letters 7:6, pages 618-622.
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Christel A.S. Bergström, William N. Charman & Christopher J.H. Porter. (2016) Computational prediction of formulation strategies for beyond-rule-of-5 compounds. Advanced Drug Delivery Reviews 101, pages 6-21.
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Yan A. Ivanenkov, Mark S. Veselov, Nina V. Chufarova, Alexander G. Majouga, Anna A. Kudryavceva & Alexandre V. Ivachtchenko. (2015) Non-dopamine receptor ligands for the treatment of Parkinson’s disease. Insight into the related chemical/property space. Molecular Diversity 20:1, pages 345-365.
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Alexandre G. Dayer, Moritz Jacobshagen, Séverine Chaumont-Dubel & Philippe Marin. (2015) 5-HT 6 Receptor: A New Player Controlling the Development of Neural Circuits . ACS Chemical Neuroscience 6:7, pages 951-960.
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Faisal Hayat, Ambily Nath Indu Viswanath, Ae Nim Pae, Hyewhon Rhim, Woo-Kyu Park & Hea-Young Park Choo. (2015) Synthesis and biological evaluation of 4-nitroindole derivatives as 5-HT2A receptor antagonists. Bioorganic & Medicinal Chemistry 23:6, pages 1313-1320.
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A. V. Ivachtchenko, E. S. Golovina, M. G. Kadieva, O. D. Mitkin & I. M. Okun. (2015) Antagonists of Serotonin 5-HT6 Receptors. VI. Substituted 3-(Phenylsulfonyl)Quinolines, Synthesis and Structure–Activity Relationships. Pharmaceutical Chemistry Journal 48:10, pages 646-660.
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A V Ivachtchenko. (2014) Sulfonyl-containing modulators of serotonin 5-HT 6 receptors and their pharmacophore models . Russian Chemical Reviews 83:5, pages 439-473.
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Maria J. Ramirez, Mitchell K. P. Lai, Rosa M. Tordera & Paul T. Francis. (2014) Serotonergic Therapies for Cognitive Symptoms in Alzheimer’s Disease: Rationale and Current Status. Drugs 74:7, pages 729-736.
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Bart A. Ellenbroek & Andrea M. Cesura. 2015. Small Molecule Therapeutics for Schizophrenia. Small Molecule Therapeutics for Schizophrenia 1 49 .
Alexandre Ivachtchenko, Elena Golovina, Madina Kadieva, Oleg Mitkin, Sergei Tkachenko & Ilya Okun. (2013) Synthesis of substituted diphenyl sulfones and their structure–activity relationship with the antagonism of 5-НТ6 receptors. Bioorganic & Medicinal Chemistry 21:15, pages 4614-4627.
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María Javier Ramírez. (2013) 5-HT6 receptors and Alzheimer's disease. Alzheimer's Research & Therapy 5:2.
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Philippe Marin, Julie Meffre & Joël Bockaert. (2013) mTOR. médecine/sciences 29:1, pages 28-30.
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A. V. Ivashchenko, E. S. Golovina, M. G. Kadieva, V. M. Kysil, O. D. Mitkin & I. M. Okun. (2012) Antagonists of serotonin 5-HT6 receptors. III. Pyridine-substituted 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrimidines: synthesis and structure – activity relationship. Pharmaceutical Chemistry Journal 46:7, pages 406-410.
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A. V. Ivachtchenko, E. S. Golovina, M. G. Kadieva, V. M. Kysil, O. D. Mitkin & I. M. Okun. (2012) Serotonin 5-HT6 receptor antagonists. II. Synthesis and structure—activity relationship of 3-arylsulfonyl-2-methylthiopyrazolo[1,5-a]pyrimidines with substituents containing an amine in the 6-position. Pharmaceutical Chemistry Journal 46:6, pages 337-345.
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Alexandre V. Ivachtchenko, Elena S. Golovina, Madina G. Kadieva, Volodymyr M. Kysil, Oleg D. Mitkin, Anton A. Vorobiev & Ilya Okun. (2012) Antagonists of 5-HT6 receptors. Substituted 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[3,4-e]pyrimidines and 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[4,3-d]pyrimidines—Synthesis and ‘structure–activity’ relationship. Bioorganic & Medicinal Chemistry Letters 22:13, pages 4273-4280.
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Rabindranath Tripathy, Robert J. McHugh, Edward R. Bacon, Joseph M. Salvino, George C. Morton, Lisa D. Aimone, Zeck Huang, Joanne R. Mathiasen, Amy DiCamillo, Mark J. Huffman, Beth A. McKenna, Karla Kopec, Lily D. Lu, Jie Qian, Thelma S. Angeles, Thomas Connors, Chrysanthe Spais, Beverly Holskin, Emir Duzic, Hervé Schaffhauser & Gerard C. Rossé. (2012) Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: Identification of a potent and selective 5-HT6 receptor antagonist showing activity in rat social recognition test. Bioorganic & Medicinal Chemistry Letters 22:3, pages 1421-1426.
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Simon D. Brandt, Ruchanok Tearavarich, Nicola Dempster, Nicholas V. Cozzi & Paul F. Daley. (2012) Synthesis and characterization of 5‐methoxy‐2‐methyl‐ N , N ‐dialkylated tryptamines . Drug Testing and Analysis 4:1, pages 24-32.
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Alexandre V. Ivachtchenko, Elena S. Golovina, Madina G. Kadieva, Volodymyr M. Kysil, Oleg D. Mitkin, Sergey E. Tkachenko & Ilya M. Okun. (2011) Synthesis and Structure–Activity Relationship (SAR) of (5,7-Disubstituted 3-phenylsulfonyl-pyrazolo[1,5- a ]pyrimidin-2-yl)-methylamines as Potent Serotonin 5-HT 6 Receptor (5-HT 6 R) Antagonists . Journal of Medicinal Chemistry 54:23, pages 8161-8173.
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Ramakrishna Nirogi, Adireddy Dwarampudi, Ramasastry Kambhampati, Venugopalarao Bhatta, Laxman Kota, Anil Shinde, Rajesh Badange, Pradeep Jayarajan, Gopinadh Bhyrapuneni & P.K. Dubey. (2011) Rigidized 1-aryl sulfonyl tryptamines: Synthesis and pharmacological evaluation as 5-HT6 receptor ligands. Bioorganic & Medicinal Chemistry Letters 21:15, pages 4577-4580.
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Xabier Codony, Jose Miguel Vela & Maria Javier Ramírez. (2011) 5-HT6 receptor and cognition. Current Opinion in Pharmacology 11:1, pages 94-100.
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Alfredo Meneses, Georgina Pérez-García, T. Ponce-Lopez & Carlos Castillo. 2011. International Review of Neurobiology Volume 96. International Review of Neurobiology Volume 96 27 47 .

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