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Selective JAK1 inhibitor and selective Tyk2 inhibitor patents

, MBA PhD
Pages 1233-1249 | Published online: 13 Sep 2012

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Xingrui He, Xiabin Chen, Hancheng Zhang, Tian Xie & Xiang-Yang Ye. (2019) Selective Tyk2 inhibitors as potential therapeutic agents: a patent review (2015–2018). Expert Opinion on Therapeutic Patents 29:2, pages 137-149.
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Barry J Sheane & Vinod Chandran. (2014) Investigational drugs for treating psoriatic arthritis. Expert Opinion on Investigational Drugs 23:7, pages 1001-1016.
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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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Articles from other publishers (29)

Kuojun Zhang, Ke Ye, He Tang, Zhihao Qi, Tianyu Wang, Jie Mao, Xiangyu Zhang & Sheng Jiang. (2023) Development and Therapeutic Implications of Tyrosine Kinase 2 Inhibitors. Journal of Medicinal Chemistry 66:7, pages 4378-4416.
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Sarveswara Rao Vangala, Navneet Bung, Sowmya Ramaswamy Krishnan & Arijit Roy. (2022) An interpretable machine learning model for selectivity of small-molecules against homologous protein family. Future Medicinal Chemistry 14:20, pages 1441-1453.
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Mengyuan Li, Yu Yan, Xinxin Zhang, Yidan Zhang, Xiaohan Xu, Lei Zhang, Liangliang Lu, Jie Wang, Yazhuo Zhang, Qiaoling Song & Chenyang Zhao. (2021) Scaffold compound L971 exhibits anti‐inflammatory activities through inhibition of JAK/STAT and NFκB signalling pathways. Journal of Cellular and Molecular Medicine 25:13, pages 6333-6347.
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Chilakamarti V. Ramana & Bikul Das. (2021) Profiling transcription factor sub-networks in type I interferon signaling and in response to SARS-CoV-2 infection. Computational and Mathematical Biophysics 9:1, pages 273-288.
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Elham Y. Al-Barghouthy, Areej Abuhammad & Mutasem O. Taha. (2019) QSAR-guided pharmacophore modeling and subsequent virtual screening identify novel TYK2 inhibitor. Medicinal Chemistry Research 28:9, pages 1368-1387.
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Ana Martinez & Carmen Gil. 2019. Emerging Drugs and Targets for Multiple Sclerosis. Emerging Drugs and Targets for Multiple Sclerosis 170 196 .
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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Atli Thorarensen, Martin E. Dowty, Mary Ellen Banker, Brian Juba, Jason Jussif, Tsung Lin, Fabien Vincent, Robert M. Czerwinski, Agustin Casimiro-Garcia, Ray Unwalla, John I. Trujillo, Sidney Liang, Paul Balbo, Ye Che, Adam M. Gilbert, Matthew F. Brown, Matthew Hayward, Justin Montgomery, Louis Leung, Xin Yang, Sarah Soucy, Martin Hegen, Jotham Coe, Jonathan Langille, Felix Vajdos, Jill Chrencik & Jean-Baptiste Telliez. (2017) Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2 S ,5 R )-5-((7 H -Pyrrolo[2,3- d ]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans . Journal of Medicinal Chemistry 60:5, pages 1971-1993.
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Qunhao Hou, Ruiyue Gong, Xiancheng Liu, Huiling Mao, Xiaowen Xu, Dan Liu, Zao Dai, Haizhou Wang, Binhua Wang & Chengyu Hu. (2017) Poly I:C facilitates the phosphorylation of Ctenopharyngodon idellus type I IFN receptor subunits and JAK kinase. Fish & Shellfish Immunology 60, pages 13-20.
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Róbert Kiss, Dávid Bajusz, Rebekah Baskin, Katalin Tóth, Katalin Monostory, Peter P. Sayeski & György M. Keserű. (2016) Identification of 8-Hydroxyquinoline Derivatives Active Against Somatic V658F Mutant JAK1-Dependent Cells. Archiv der Pharmazie 349:12, pages 925-933.
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Wei Zhang, Jianzong Li, Zhixin Huang, Haiyang Wang, Hao Luo, Xin Wang, Nan Zhou, Chuanfang Wu & Jinku Bao. (2016) Computer-aided identification of potential TYK2 inhibitors from drug database. Journal of Molecular Structure 1122, pages 309-317.
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Yutaka Nakajima, Naohiro Aoyama, Fumie Takahashi, Hiroshi Sasaki, Keiko Hatanaka, Ayako Moritomo, Masamichi Inami, Misato Ito, Koji Nakamura, Fumihiro Nakamori, Takayuki Inoue & Shohei Shirakami. (2016) Design, synthesis, and evaluation of 4,6-diaminonicotinamide derivatives as novel and potent immunomodulators targeting JAK3. Bioorganic & Medicinal Chemistry 24:19, pages 4711-4722.
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Takatoshi Yogo, Hiroyuki Nagamiya, Masaki Seto, Satoshi Sasaki, Huang Shih-Chung, Yusuke Ohba, Norihito Tokunaga, Gil Nam Lee, Chul Yun Rhim, Cheol Hwan Yoon, Suk Young Cho, Robert Skene, Syunsuke Yamamoto, Yousuke Satou, Masako Kuno, Takahiro Miyazaki, Hideyuki Nakagawa, Atsutoshi Okabe, Shogo Marui, Kazuyoshi Aso & Masato Yoshida. (2016) Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4 H -pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 Inhibitors . Journal of Medicinal Chemistry 59:2, pages 733-749.
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Woo Dae Jang, Jun-Tae Kim, Hoon Young Son, Seung Yeon Park, Young Sik Cho, Tae-sung Koo, Hyuk Lee & Nam Sook Kang. (2015) Discovery of Tyk2 inhibitors via the virtual site-directed fragment-based drug design. Bioorganic & Medicinal Chemistry Letters 25:18, pages 3947-3952.
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Yutaka Nakajima, Takayuki Inoue, Kazuo Nakai, Koichiro Mukoyoshi, Hisao Hamaguchi, Keiko Hatanaka, Hiroshi Sasaki, Akira Tanaka, Fumie Takahashi, Shigeki Kunikawa, Hiroyuki Usuda, Ayako Moritomo, Yasuyuki Higashi, Masamichi Inami & Shohei Shirakami. (2015) Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3. Bioorganic & Medicinal Chemistry 23:15, pages 4871-4883.
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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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John S. Tokarski, Adriana Zupa-Fernandez, Jeffrey A. Tredup, Kristen Pike, ChiehYing Chang, Dianlin Xie, Lihong Cheng, Donna Pedicord, Jodi Muckelbauer, Stephen R. Johnson, Sophie Wu, Suzanne C. Edavettal, Yang Hong, Mark R. Witmer, Lisa L. Elkin, Yuval Blat, William J. Pitts, David S. Weinstein & James R. Burke. (2015) Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain. Journal of Biological Chemistry 290:17, pages 11061-11074.
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Christel J Menet, Oscar Mammoliti & Miriam López-Ramos. (2015) Progress toward JAK1-selective inhibitors. Future Medicinal Chemistry 7:2, pages 203-235.
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Yutaka NakajimaTakashi TojoMasataka MoritaKeiko HatanakaShohei ShirakamiAkira TanakaHiroshi SasakiKazuo NakaiKoichiro MukoyoshiHisao HamaguchiFumie TakahashiAyako MoritomoYasuyuki HigashiTakayuki Inoue. (2015) Synthesis and Evaluation of 1<i>H</i>-Pyrrolo[2,3-<i>b</i>]pyridine Derivatives as Novel Immunomodulators Targeting Janus Kinase 3. CHEMICAL & PHARMACEUTICAL BULLETIN Chemical and Pharmaceutical Bulletin 63:5, pages 341-353.
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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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Atli Thorarensen, Mary Ellen Banker, Andrew Fensome, Jean-Baptiste Telliez, Brian Juba, Fabien Vincent, Robert M. Czerwinski & Agustin Casimiro-Garcia. (2014) ATP-Mediated Kinome Selectivity: The Missing Link in Understanding the Contribution of Individual JAK Kinase Isoforms to Cellular Signaling. ACS Chemical Biology 9:7, pages 1552-1558.
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Christel J Menet. (2014) Toward selective TYK2 inhibitors as therapeutic agents for the treatment of inflammatory diseases. Pharmaceutical Patent Analyst 3:4, pages 449-466.
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James D. Clark, Mark E. Flanagan & Jean-Baptiste Telliez. (2014) Discovery and Development of Janus Kinase (JAK) Inhibitors for Inflammatory Diseases. Journal of Medicinal Chemistry 57:12, pages 5023-5038.
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Raimund M. Vielnascher, Eva Hainzl, Nicole R. Leitner, Michael Rammerstorfer, David Popp, Agnieszka Witalisz, Rita Rom, Marina Karaghiosoff, Thomas Kolbe, Simone Müller, Thomas Rülicke, Caroline Lassnig, Birgit Strobl & Mathias Müller. (2014) Conditional ablation of TYK2 in immunity to viral infection and tumor surveillance. Transgenic Research 23:3, pages 519-529.
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Eva Salgado, Jose R Maneiro, Loreto Carmona & Juan J Gomez-Reino. (2014) Safety profile of protein kinase inhibitors in rheumatoid arthritis: systematic review and meta-analysis. Annals of the Rheumatic Diseases 73:5, pages 871-882.
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Charles J Malemud. (2014) Protein kinase small molecule inhibitors for rheumatoid arthritis: Medicinal chemistry/clinical perspectives. World Journal of Orthopedics 5:4, pages 496.
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Soumya D. Chakravarty, Poulikos I. Poulikakos, Lionel B. Ivashkiv, Jane E. Salmon & George D. Kalliolias. (2013) Kinase inhibitors: A new tool for the treatment of rheumatoid arthritis. Clinical Immunology 148:1, pages 66-78.
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Lorena Fontan & Ari Melnick. (2013) Discovering What Makes STAT Signaling TYK in T-ALL. Cancer Discovery 3:5, pages 494-496.
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Hae-Rim Kim. (2013) Phosphoinositide 3-kinase (PI3K) as a New Therapeutic Target for Rheumatoid Arthritis. Journal of Rheumatic Diseases 20:2, pages 74.
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