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Recent developments on JAK2 inhibitors: a patent review

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Pages 471-495 | Published online: 08 Mar 2010

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

Read on this site (5)

Ramesh Itteboina, Srilata Ballu, Sree Kanth Sivan & Vijjulatha Manga. (2018) Molecular docking, 3D-QSAR, molecular dynamics, synthesis and anticancer activity of tyrosine kinase 2 (TYK 2) inhibitors. Journal of Receptors and Signal Transduction 38:5-6, pages 462-474.
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Ramesh Itteboina, Srilata Ballu, Sree Kanth Sivan & Vijjulatha Manga. (2017) Molecular modeling-driven approach for identification of Janus kinase 1 inhibitors through 3D-QSAR, docking and molecular dynamics simulations. Journal of Receptors and Signal Transduction 37:5, pages 453-469.
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Peter Norman. (2014) Evaluation of WO2013125543, WO2013146963 and EP2634185: the first Tyk2 inhibitors from Takeda and Sareum. Expert Opinion on Therapeutic Patents 24:3, pages 361-368.
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Brian W Dymock & Cheng Shang See. (2013) Inhibitors of JAK2 and JAK3: an update on the patent literature 2010 – 2012. Expert Opinion on Therapeutic Patents 23:4, pages 449-501.
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Peter Norman. (2012) Selective JAK1 inhibitor and selective Tyk2 inhibitor patents. Expert Opinion on Therapeutic Patents 22:10, pages 1233-1249.
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Articles from other publishers (26)

Nguyen Thi Mai, Ngo Thi Lan, Thien Y. Vu, Nguyen Thanh Tung & Huong Thi Thu Phung. (2022) A computationally affordable approach for accurate prediction of the binding affinity of JAK2 inhibitors. Journal of Molecular Modeling 28:6.
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Syeda Rehana Zia. (2021) Role of water in the determination of protonation states of titratable residues. Journal of Molecular Modeling 27:2.
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Emad M. Gad, Mohamed S. Nafie, Elsayed H. Eltamany, Magdy S. A. G. Hammad, Assem Barakat & Ahmed T. A. Boraei. (2020) Discovery of New Apoptosis-Inducing Agents for Breast Cancer Based on Ethyl 2-Amino-4,5,6,7-Tetra Hydrobenzo[b]Thiophene-3-Carboxylate: Synthesis, In Vitro, and In Vivo Activity Evaluation. Molecules 25:11, pages 2523.
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Seketoulie Keretsu, Swapnil Pandurang Bhujbal & Seung Joo Cho. (2020) Computational Study of Pyrimidin‐2‐Aminopyrazol‐Hydroxamate‐based JAK2 Inhibitors for the Treatment of Myeloproliferative Neoplasms . Bulletin of the Korean Chemical Society 41:5, pages 542-551.
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Addila Abu Bakar, Muhammad Akhtar, Norlaily Mohd Ali, Swee Yeap, Ching Quah, Wan-Sin Loh, Noorjahan Alitheen, Seema Zareen, Zaheer Ul-Haq & Syed Shah. (2018) Design, Synthesis and Docking Studies of Flavokawain B Type Chalcones and Their Cytotoxic Effects on MCF-7 and MDA-MB-231 Cell Lines. Molecules 23:3, pages 616.
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Hiroaki Yamagishi, Takayuki Inoue, Yutaka Nakajima, Jun Maeda, Hiroaki Tominaga, Hiroyuki Usuda, Takeshi Hondo, Ayako Moritomo, Fumihiro Nakamori, Misato Ito, Koji Nakamura, Hiroki Morio, Yasuyuki Higashi, Masamichi Inami & Shohei Shirakami. (2017) Discovery of tricyclic dipyrrolopyridine derivatives as novel JAK inhibitors. Bioorganic & Medicinal Chemistry 25:20, pages 5311-5326.
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Tingfang Wang, Xiaofei Liu, Meixi Hao, Jianan Qiao, Caoyun Ju, Lingjing Xue & Can Zhang. (2016) Design, synthesis and evaluation of pyrrolo[2,3-d]pyrimidine-phenylamide hybrids as potent Janus kinase 2 inhibitors. Bioorganic & Medicinal Chemistry Letters 26:12, pages 2936-2941.
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Hiroaki Yamagishi, Shohei Shirakami, Yutaka Nakajima, Akira Tanaka, Fumie Takahashi, Hisao Hamaguchi, Keiko Hatanaka, Ayako Moritomo, Masamichi Inami, Yasuyuki Higashi & Takayuki Inoue. (2015) Discovery of 3,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2(1H)-one derivatives as novel JAK inhibitors. Bioorganic & Medicinal Chemistry 23:15, pages 4846-4859.
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Maria Gabriella Brasca, Paola Gnocchi, Marcella Nesi, Nadia Amboldi, Nilla Avanzi, Jay Bertrand, Simona Bindi, Giulia Canevari, Daniele Casero, Marina Ciomei, Nicoletta Colombo, Sabrina Cribioli, Gabriele Fachin, Eduard R. Felder, Arturo Galvani, Antonella Isacchi, Ilaria Motto, Achille Panzeri & Daniele Donati. (2015) Novel pyrrole carboxamide inhibitors of JAK2 as potential treatment of myeloproliferative disorders. Bioorganic & Medicinal Chemistry 23:10, pages 2387-2407.
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Maria Gabriella Brasca, Marcella Nesi, Nilla Avanzi, Dario Ballinari, Tiziano Bandiera, Jay Bertrand, Simona Bindi, Giulia Canevari, Davide Carenzi, Daniele Casero, Lucio Ceriani, Marina Ciomei, Alessandra Cirla, Maristella Colombo, Sabrina Cribioli, Cinzia Cristiani, Franco Della Vedova, Gabriele Fachin, Marina Fasolini, Eduard R. Felder, Arturo Galvani, Antonella Isacchi, Danilo Mirizzi, Ilaria Motto, Achille Panzeri, Enrico Pesenti, Paola Vianello, Paola Gnocchi & Daniele Donati. (2014) Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors. Bioorganic & Medicinal Chemistry 22:17, pages 4998-5012.
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Brian W Dymock, Eugene Guorong Yang, Yuyi Chu-Farseeva & Lianbin Yao. (2014) Selective JAK inhibitors. Future Medicinal Chemistry 6:12, pages 1439-1471.
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Qibin Su, Stephanos Ioannidis, Claudio Chuaqui, Lynsie Almeida, Marat Alimzhanov, Geraldine Bebernitz, Kirsten Bell, Michael Block, Tina Howard, Shan Huang, Dennis Huszar, Jon A. Read, Caroline Rivard Costa, Jie Shi, Mei Su, Minwei Ye & Michael Zinda. (2013) Discovery of 1-Methyl-1 H -imidazole Derivatives as Potent Jak2 Inhibitors . Journal of Medicinal Chemistry 57:1, pages 144-158.
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Min-Yi Li, Yan Tian, Li Shen, Ralf Buettner, Hong-Zhi Li, Lucy Liu, Yate-Ching Yuan, Qiang Xiao, Jun Wu & Richard Jove. (2013) 3-O-methylthespesilactam, a new small-molecule anticancer pan-JAK inhibitor against A2058 human melanoma cells. Biochemical Pharmacology 86:10, pages 1411-1418.
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Michael Siu, Richard Pastor, Wendy Liu, Kathy Barrett, Megan Berry, Wade S. Blair, Christine Chang, Jacob Z. Chen, Charles Eigenbrot, Nico Ghilardi, Paul Gibbons, Haiying He, Christopher A. Hurley, Jane R. Kenny, S. Cyrus Khojasteh, Hoa Le, Leslie Lee, Joseph P. Lyssikatos, Steve Magnuson, Rebecca Pulk, Vickie Tsui, Mark Ultsch, Yisong Xiao, Bing-yan Zhu & Deepak Sampath. (2013) 2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors. Bioorganic & Medicinal Chemistry Letters 23:17, pages 5014-5021.
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Christopher A. Hurley, Wade S. Blair, Richard J. Bull, Christine Chang, Peter H. Crackett, Gauri Deshmukh, Hazel J. Dyke, Rina Fong, Nico Ghilardi, Paul Gibbons, Peter R. Hewitt, Adam Johnson, Tony Johnson, Jane R. Kenny, Pawan Bir Kohli, Janusz J. Kulagowski, Marya Liimatta, Patrick J. Lupardus, Robert J. Maxey, Rohan Mendonca, Raman Narukulla, Rebecca Pulk, Savita Ubhayakar, Anne van Abbema, Stuart I. Ward, Bohdan Waszkowycz & Mark Zak. (2013) Novel triazolo-pyrrolopyridines as inhibitors of Janus kinase 1. Bioorganic & Medicinal Chemistry Letters 23:12, pages 3592-3598.
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MICHAEL SKYNNER, PHIL JEFFREY, MICHAEL BINKS & MICHAEL WOODROW. 2012. Anti-Inflammatory Drug Discovery. Anti-Inflammatory Drug Discovery 211 254 .
Anthony D. William, Angeline C.-H. Lee, Anders Poulsen, Kee Chuan Goh, Babita Madan, Stefan Hart, Evelyn Tan, Haishan Wang, Harish Nagaraj, Dizhong Chen, Chai Ping Lee, Eric T. Sun, Ramesh Jayaraman, Mohammad Khalid Pasha, Kantharaj Ethirajulu, Jeanette M. Wood & Brian W. Dymock. (2012) Discovery of the Macrocycle (9 E )-15-(2-(Pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a Potent Inhibitor of Janus Kinase 2/Fms-LikeTyrosine Kinase-3 (JAK2/FLT3) for the Treatment of Rheumatoid Arthritis . Journal of Medicinal Chemistry 55:6, pages 2623-2640.
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Oliver Weigert, Andrew A. Lane, Liat Bird, Nadja Kopp, Bjoern Chapuy, Diederik van Bodegom, Angela V. Toms, Sachie Marubayashi, Amanda L. Christie, Michael McKeown, Ronald M. Paranal, James E. Bradner, Akinori Yoda, Christoph Gaul, Eric Vangrevelinghe, Vincent Romanet, Masato Murakami, Ralph Tiedt, Nicolas Ebel, Emeline Evrot, Alain De Pover, Catherine H. Régnier, Dirk Erdmann, Francesco Hofmann, Michael J. Eck, Stephen E. Sallan, Ross L. Levine, Andrew L. Kung, Fabienne Baffert, Thomas Radimerski & David M. Weinstock. (2012) Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition. Journal of Experimental Medicine 209:2, pages 259-273.
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Emilie-Fleur GautierMuriel PicardCamille LaurentCaroline MartyJean-Luc VillevalCécile DemurFrançois DelhommeauElizabeth HexnerStéphane GiraudierNicolas Bonnevialle, Bernard Ducommun, Christian RécherGuy LaurentStéphane ManentiVéronique Mansat-De Mas. (2012) The cell cycle regulator CDC25A is a target for JAK2V617F oncogene. Blood 119:5, pages 1190-1199.
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Rebekah Baskin, Meghanath Gali, Sung O. Park, Zhizhuang Joe Zhao, György M. Keserű, Kirpal S. Bisht & Peter P. Sayeski. (2012) Identification of novel SAR properties of the Jak2 small molecule inhibitor G6: Significance of the para-hydroxyl orientation. Bioorganic & Medicinal Chemistry Letters 22:3, pages 1402-1407.
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Linda R. Weinberg, Mark S. Albom, Thelma S. Angeles, Henry J. Breslin, Diane E. Gingrich, Zeqi Huang, Joseph G. Lisko, Jennifer L. Mason, Karen L. Milkiewicz, Tho V. Thieu, Ted L. Underiner, Gregory J. Wells, Kevin J. Wells-Knecht & Bruce D. Dorsey. (2011) 2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: Modification of target structure to minimize reactive metabolite formation. Bioorganic & Medicinal Chemistry Letters 21:24, pages 7325-7330.
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Cui‐Juan Qian, Jun Yao & Jian‐Min Si. (2011) Nuclear JAK2: Form and Function in Cancer. The Anatomical Record 294:9, pages 1446-1459.
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Anthony D. William, Angeline C.-H. Lee, Stéphanie Blanchard, Anders Poulsen, Ee Ling Teo, Harish Nagaraj, Evelyn Tan, Dizhong Chen, Meredith Williams, Eric T. Sun, Kee Chuan Goh, Wai Chung Ong, Siok Kun Goh, Stefan Hart, Ramesh Jayaraman, Mohammed Khalid Pasha, Kantharaj Ethirajulu, Jeanette M. Wood & Brian W. Dymock. (2011) Discovery of the Macrocycle 11-(2-Pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a Potent Janus Kinase 2/Fms-Like Tyrosine Kinase-3 (JAK2/FLT3) Inhibitor for the Treatment of Myelofibrosis and Lymphoma. Journal of Medicinal Chemistry 54:13, pages 4638-4658.
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Tao Wang, Stephanos Ioannidis, Lynsie Almeida, Michael H. Block, Audrey M. Davies, Michelle L. Lamb, David A. Scott, Mei Su, Hai-Jun Zhang, Marat Alimzhanov, Geraldine Bebernitz, Kirsten Bell & Michael Zinda. (2011) In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors. Bioorganic & Medicinal Chemistry Letters 21:10, pages 2958-2961.
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Zohreh Hosseinzadeh, Shefalee K. Bhavsar, Mentor Sopjani, Ioana Alesutan, Ambrish Saxena, Miribane Dërmaku-Sopjani & Florian Lang. (2011) Regulation of the Glutamate Transporters by JAK2. Cellular Physiology and Biochemistry 28:4, pages 693-702.
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Kavitha Gnanasambandan, Andrew Magis & Peter P. Sayeski. (2010) The Constitutive Activation of Jak2-V617F Is Mediated by a π Stacking Mechanism Involving Phenylalanines 595 and 617. Biochemistry 49:46, pages 9972-9984.
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