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Expert Opinion on Therapeutic Patents Volume 24, 2014 - Issue 1
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New developments around histamine H3 receptor antagonists/inverse agonists: a patent review (2010 – present)

Dorota ŁażewskaJagiellonian University Medical College, Department of Technology and Biotechnology of Drugs, Kraków, [email protected]
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Katarzyna Kieć-KononowiczJagiellonian University Medical College, Department of Technology and Biotechnology of Drugs, Kraków, [email protected]
Pages 89-111 | Published online: 17 Oct 2013

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Dorota Łażewska & Katarzyna Kieć-Kononowicz. (2018) Progress in the development of histamine H3 receptor antagonists/inverse agonists: a patent review (2013-2017). Expert Opinion on Therapeutic Patents 28:3, pages 175-196.
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Articles from other publishers (35)

Katarzyna Szczepańska, Tadeusz Karcz, Maria Dichiara, Szczepan Mogilski, Justyna Kalinowska-Tłuścik, Bogusław Pilarski, Arkadiusz Leniak, Wojciech Pietruś, Sabina Podlewska, Katarzyna Popiołek-Barczyk, Laura J. Humphrys, M. Carmen Ruiz-Cantero, David Reiner-Link, Luisa Leitzbach, Dorota Łażewska, Steffen Pockes, Michał Górka, Adam Zmysłowski, Thierry Calmels, Enrique J. Cobos, Agostino Marrazzo, Holger Stark, Andrzej J. Bojarski, Emanuele Amata & Katarzyna Kieć-Kononowicz. (2023) Dual Piperidine-Based Histamine H 3 and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain . Journal of Medicinal Chemistry 66:14, pages 9658-9683.
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Cecília M.S.Q. Aranha, David Reiner-Link, Luisa R. Leitzbach, Flavia B. Lopes, Holger Stark & João Paulo S. Fernandes. (2023) Multitargeting approaches to cognitive impairment: Synthesis of aryl-alkylpiperazines and assessment at cholinesterases, histamine H3 and dopamine D3 receptors. Bioorganic & Medicinal Chemistry 78, pages 117132.
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Justyna Godyń, Paula Zaręba, Dorota Stary, Maria Kaleta, Kamil J. Kuder, Gniewomir Latacz, Szczepan Mogilski, David Reiner-Link, Annika Frank, Agata Doroz-Płonka, Agnieszka Olejarz-Maciej, Sylwia Sudoł-Tałaj, Tobias Nolte, Jadwiga Handzlik, Holger Stark, Anna Więckowska, Barbara Malawska, Katarzyna Kieć-Kononowicz, Dorota Łażewska & Marek Bajda. (2022) Benzophenone Derivatives with Histamine H3 Receptor Affinity and Cholinesterase Inhibitory Potency as Multitarget-Directed Ligands for Possible Therapy of Alzheimer’s Disease. Molecules 28:1, pages 238.
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Anaum Ihsan, Rasheed Ahmad Khera, Javed Iqbal & Muhammad Asgher. (2022) Binding interaction of benzamide derivatives as inhibitors of DNA gyrase and Sec14p using Molegro Virtual Docker based on binding free energy. Zeitschrift für Physikalische Chemie 236:4, pages 561-581.
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Justyna Godyń, Paula Zaręba, Dorota Łażewska, Dorota Stary, David Reiner-Link, Annika Frank, Gniewomir Latacz, Szczepan Mogilski, Maria Kaleta, Agata Doroz-Płonka, Annamaria Lubelska, Ewelina Honkisz-Orzechowska, Agnieszka Olejarz-Maciej, Jadwiga Handzlik, Holger Stark, Katarzyna Kieć-Kononowicz, Barbara Malawska & Marek Bajda. (2021) Cyanobiphenyls: Novel H3 receptor ligands with cholinesterase and MAO B inhibitory activity as multitarget compounds for potential treatment of Alzheimer’s disease. Bioorganic Chemistry 114, pages 105129.
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Xiangqian Li, Xiaowei Li, Fang Liu, Shuo Li & Dayong Shi. (2021) Rational Multitargeted Drug Design Strategy from the Perspective of a Medicinal Chemist. Journal of Medicinal Chemistry 64:15, pages 10581-10605.
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Chenxian Hu, Liu Jiang, Li Tang, Minkui Zhang & Rong Sheng. (2021) Design, synthesis and biological evaluation of 2-styryl-5-hydroxy-4-pyrone derivatives and analogues as multiple functional agents with the potential for the treatment of Alzheimer’s disease. Bioorganic & Medicinal Chemistry 44, pages 116306.
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Katarzyna Szczepańska, Kamil J. Kuder & Katarzyna Kieć-Kononowicz. (2021) Dual-targeting Approach on Histamine H3 and Sigma-1 Receptor Ligands as Promising Pharmacological Tools in the Treatment of CNS-linked Disorders. Current Medicinal Chemistry 28:15, pages 2974-2995.
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Lanchang Gao, Chao Hao, Jiali Chen, Ru Ma, Lu Zheng, Qingkun Wu, Xin Liu, Bi-Feng Liu, Guisen Zhang, Yin Chen & Jian Jin. (2021) Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect. Bioorganic & Medicinal Chemistry Letters 40, pages 127909.
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Minkui Zhang, Li Tang, Liu Jiang, Jun Wei, Yongzhou Hu & Rong Sheng. (2021) Identification of N-phenyl-3-methoxy-4-pyridinones as orally bioavailable H3 receptor antagonists and β-amyloid aggregation inhibitors for the treatment of Alzheimer’s disease. European Journal of Medicinal Chemistry 212, pages 113096.
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Nakisa Ghamari, Siavoush Dastmalchi, Omid Zarei, José‐Antonio Arias‐Montaño, David Reiner, Fulya Ustun‑Alkan, Holger Stark & Maryam Hamzeh‐Mivehroud. (2019) In silico and in vitro studies of two non‐imidazole multiple targeting agents at histamine H 3 receptors and cholinesterase enzymes . Chemical Biology & Drug Design 95:2, pages 279-290.
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Gábor Wágner, Tamara A. M. Mocking, Albert J. Kooistra, Inna Slynko, Péter Ábrányi-Balogh, György M. Keserű, Maikel Wijtmans, Henry F. Vischer, Iwan J. P. de Esch & Rob Leurs. (2019) Covalent Inhibition of the Histamine H3 Receptor. Molecules 24:24, pages 4541.
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István Ledneczki, Zsolt Némethy, Pál Tapolcsányi, János Éles, István Greiner, Eszter Gábor, Balázs Varga, Ottilia Balázs, Viktor Román, György Lévay & Sándor Mahó. (2019) Discovery of novel steroidal histamine H3 receptor antagonists/inverse agonists. Part 2. Versatile steroidal carboxamide derivatives. Bioorganic & Medicinal Chemistry Letters 29:20, pages 126643.
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Katarzyna Szczepańska, Tadeusz Karcz, Agata Siwek, Kamil J. Kuder, Gniewomir Latacz, Marek Bednarski, Małgorzata Szafarz, Stefanie Hagenow, Annamaria Lubelska, Agnieszka Olejarz-Maciej, Michał Sobolewski, Kamil Mika, Magdalena Kotańska, Holger Stark & Katarzyna Kieć-Kononowicz. (2019) Structural modifications and in vitro pharmacological evaluation of 4-pyridyl-piperazine derivatives as an active and selective histamine H3 receptor ligands. Bioorganic Chemistry 91, pages 103071.
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Nakisa Ghamari, Omid Zarei, José-Antonio Arias-Montaño, David Reiner, Siavoush Dastmalchi, Holger Stark & Maryam Hamzeh-Mivehroud. (2019) Histamine H3 receptor antagonists/inverse agonists: Where do they go?. Pharmacology & Therapeutics 200, pages 69-84.
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Katarzyna Szczepańska, Tadeusz Karcz, Szczepan Mogilski, Agata Siwek, Kamil J. Kuder, Gniewomir Latacz, Monika Kubacka, Stefanie Hagenow, Annamaria Lubelska, Agnieszka Olejarz, Magdalena Kotańska, Bassem Sadek, Holger Stark & Katarzyna Kieć-Kononowicz. (2018) Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H3R ligands. European Journal of Medicinal Chemistry 152, pages 223-234.
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Dorota Łażewska, Maria Kaleta, Stefanie Hagenow, Szczepan Mogilski, Gniewomir Latacz, Tadeusz Karcz, Annamaria Lubelska, Ewelina Honkisz, Jadwiga Handzlik, David Reiner, Grzegorz Satała, Barbara Filipek, Holger Stark & Katarzyna Kieć-Kononowicz. (2018) Novel naphthyloxy derivatives – Potent histamine H3 receptor ligands. Synthesis and pharmacological evaluation. Bioorganic & Medicinal Chemistry 26:9, pages 2573-2585.
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Jakub Jończyk, Barbara Malawska & Marek Bajda. (2017) Hybrid approach to structure modeling of the histamine H3 receptor: Multi-level assessment as a tool for model verification. PLOS ONE 12:10, pages e0186108.
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Istvan Ledneczki, Pál Tapolcsányi, Eszter Gábor, János Éles, István Greiner, Éva Schmidt, Zsolt Némethy, Rita Soukupné Kedves, Ottilia Balázs, Viktor Román, György Lévay & Sándor Mahó. (2017) Discovery of novel steroidal histamine H 3 receptor antagonists/inverse agonists. Bioorganic & Medicinal Chemistry Letters 27:19, pages 4525-4530.
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Dorota Łażewska, Maria Kaleta, J. Stephan Schwed, Tadeusz Karcz, Szczepan Mogilski, Gniewomir Latacz, Agnieszka Olejarz, Agata Siwek, Monika Kubacka, Annamaria Lubelska, Ewelina Honkisz, Jadwiga Handzlik, Barbara Filipek, Holger Stark & Katarzyna Kieć-Kononowicz. (2017) Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H3 receptor ligands. Bioorganic & Medicinal Chemistry 25:20, pages 5341-5354.
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Aurore Sors, Fany Panayi, Lionel Bert, Dominique Favale, Olivier Nosjean, Valérie Audinot, Jean-Michel Arrang, Bruno Buisson, Esther Steidl, Jean-Marie Delbos, Tuulia Huhtala, Outi Kontkanen, Anne-Marie Chollet, Patrick Casara & Pierre Lestage. (2017) Mechanistic characterization of S 38093, a novel inverse agonist at histamine H3 receptors. European Journal of Pharmacology 803, pages 11-23.
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Kamil J. Kuder, Dorota Łażewska, Maria Kaleta, Gniewomir Latacz, Tim Kottke, Agnieszka Olejarz, Tadeusz Karcz, Andrzej Fruziński, Katarzyna Szczepańska, Janina Karolak-Wojciechowska, Holger Stark & Katarzyna Kieć-Kononowicz. (2017) Synthesis and biological activity of novel tert -amylphenoxyalkyl (homo)piperidine derivatives as histamine H 3 R ligands. Bioorganic & Medicinal Chemistry 25:10, pages 2701-2712.
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Panayiotis A. Procopiou, Rachael A. Ancliff, Paul M. Gore, Ashley P. Hancock, Simon T. Hodgson, Duncan S. Holmes, Steven P. Keeling, Brian E. Looker, Nigel A. Parr, James E. Rowedder & Robert J. Slack. (2016) The discovery of quinoline based single-ligand human H 1 and H 3 receptor antagonists. Bioorganic & Medicinal Chemistry Letters 26:24, pages 5855-5859.
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Magdalena Dudek, Kamil Kuder, Marcin Kołaczkowski, Adrian Olczyk, Elżbieta Żmudzka, Aleksandra Rak, Marek Bednarski, Karolina Pytka, Jacek Sapa & Katarzyna Kieć-Kononowicz. (2016) H3 histamine receptor antagonist pitolisant reverses some subchronic disturbances induced by olanzapine in mice. Metabolic Brain Disease 31:5, pages 1023-1029.
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Dorota Łażewska, Jakub Jończyk, Marek Bajda, Natalia Szałaj, Anna Więckowska, Dawid Panek, Caitlin Moore, Kamil Kuder, Barbara Malawska & Katarzyna Kieć-Kononowicz. (2016) Cholinesterase inhibitory activity of chlorophenoxy derivatives—Histamine H3 receptor ligands. Bioorganic & Medicinal Chemistry Letters 26:16, pages 4140-4145.
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Armin Zlomuzica, Dorothea Dere, Sonja Binder, Maria Angelica De Souza Silva, Joseph P. Huston & Ekrem Dere. (2016) Neuronal histamine and cognitive symptoms in Alzheimer's disease. Neuropharmacology 106, pages 135-145.
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Rong Sheng, Li Tang, Liu Jiang, Lingjuan Hong, Ying Shi, Naiming Zhou & Yongzhou Hu. (2015) Novel 1-Phenyl-3-hydroxy-4-pyridinone Derivatives as Multifunctional Agents for the Therapy of Alzheimer’s Disease. ACS Chemical Neuroscience 7:1, pages 69-81.
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Ramakrishna Nirogi, Anil Shinde, Vinaykumar Tiriveedhi, Laxman Kota, Sangram Keshari Saraf, Rajesh Kumar Badange, Abdul Rasheed Mohammed, Ramkumar Subramanian, Nageshwararao Muddana, Gopinadh Bhyrapuneni & Renny Abraham. (2016) Benzamide derivatives and their constrained analogs as histamine H 3 receptor antagonists. European Journal of Medicinal Chemistry 108, pages 655-662.
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Kamil Kuder, Dorota Łażewska, Gniewomir Latacz, Johannes Stephan Schwed, Tadeusz Karcz, Holger Stark, Janina Karolak-Wojciechowska & Katarzyna Kieć-Kononowicz. (2016) Chlorophenoxy aminoalkyl derivatives as histamine H3R ligands and antiseizure agents. Bioorganic & Medicinal Chemistry 24:2, pages 53-72.
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B. Sadek, D. Łażewska, S. Hagenow, K. Kieć-Kononowicz & H. Stark. 2016. Histamine Receptors. Histamine Receptors 109 155 .
Meredith Broderick & Christian Guilleminault. 2016. Narcolepsy. Narcolepsy 357 368 .
Eberhard Schlicker & Markus Kathmann. 2017. Histamine and Histamine Receptors in Health and Disease. Histamine and Histamine Receptors in Health and Disease 277 299 .
Amine Bahi, Bassem Sadek, Syed M. Nurulain, Dorota Łażewska & Katarzyna Kieć-Kononowicz. (2015) The novel non-imidazole histamine H3 receptor antagonist DL77 reduces voluntary alcohol intake and ethanol-induced conditioned place preference in mice. Physiology & Behavior 151, pages 189-197.
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Michelle Fidelis Corrêa & João Paulo dos Santos Fernandes. (2015) Histamine H 4 Receptor Ligands: Future Applications and State of Art . Chemical Biology & Drug Design 85:4, pages 461-480.
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Katarina Nikolic, Slavica Filipic, Danica Agbaba & Holger Stark. (2014) Procognitive Properties of Drugs with Single and Multitargeting H 3 Receptor Antagonist Activities . CNS Neuroscience & Therapeutics 20:7, pages 613-623.
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