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Recent patents in the discovery of small molecule inhibitors of JAK3

Pages 609-623 | Published online: 19 Apr 2010

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

Read on this site (4)

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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Kamonpan Sanachai, Panupong Mahalapbutr, Lueacha Tabtimmai, Supaphorn Seetaha, Tanakorn Kittikool, Sirilata Yotphan, Kiattawee Choowongkomon & Thanyada Rungrotmongkol. (2022) Discovery of JAK2/3 Inhibitors from Quinoxalinone-Containing Compounds. ACS Omega 7:37, pages 33587-33598.
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Yong-Ming Yan, Hong-Jie Zhu, Feng-Jiao Zhou, Zheng-Chao Tu & Yong-Xian Cheng. (2019) Phenolic compounds from the insect Blaps japanensis with inhibitory activities towards cancer cells, COX-2, ROCK1 and JAK3. Tetrahedron 75:8, pages 1029-1033.
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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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S. Dholakia, J.E. Fildes & P.J. Friend. (2017) The use of kinase inhibitors in solid organ transplantation. Transplantation Reviews 31:3, pages 166-171.
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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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Qi Luo, Xiao-Yi Wei, Jing Yang, Jin-Feng Luo, Rui Liang, Zheng-Chao Tu & Yong-Xian Cheng. (2016) Spiro Meroterpenoids from Ganoderma applanatum . Journal of Natural Products 80:1, pages 61-70.
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Yazhou Wang, Wei Huang, Minhang Xin, Pan Chen, Li Gui, Xinge Zhao, Feng Tang, Jia Wang & Fei Liu. (2017) Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors. Bioorganic & Medicinal Chemistry 25:1, pages 75-83.
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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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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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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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Jaebok Choi, Matthew L. Cooper, Bader Alahmari, Julie Ritchey, Lynne Collins, Matthew Holt & John F. DiPersio. (2014) Pharmacologic Blockade of JAK1/JAK2 Reduces GvHD and Preserves the Graft-Versus-Leukemia Effect. PLoS ONE 9:10, pages e109799.
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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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Christophe Legendre. (2013) JAK3 inhibition: what potential for the future?. Transplantation Research 2:S1.
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Sharada Labadie, Kathy Barrett, Wade S. Blair, Christine Chang, Gauri Deshmukh, Charles Eigenbrot, Paul Gibbons, Adam Johnson, Jane R. Kenny, Pawan Bir Kohli, Marya Liimatta, Patrick J. Lupardus, Steven Shia, Micah Steffek, Savita Ubhayakar, Anne van Abbema & Mark Zak. (2013) Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors. Bioorganic & Medicinal Chemistry Letters 23:21, pages 5923-5930.
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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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Saul Jaime-Figueroa, Javier De Vicente, Johannes Hermann, Alam Jahangir, Sue Jin, Andreas Kuglstatter, Stephen M. Lynch, John Menke, Linghao Niu, Vaishali Patel, Ada Shao, Michael Soth, Minh Diem Vu & Calvin Yee. (2013) Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors. Bioorganic & Medicinal Chemistry Letters 23:9, pages 2522-2526.
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Stephen M. Lynch, Javier DeVicente, Johannes C. Hermann, Saul Jaime-Figueroa, Sue Jin, Andreas Kuglstatter, Hongju Li, Allen Lovey, John Menke, Linghao Niu, Vaishali Patel, Douglas Roy, Michael Soth, Sandra Steiner, Parcharee Tivitmahaisoon, Minh Diem Vu & Calvin Yee. (2013) Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome. Bioorganic & Medicinal Chemistry Letters 23:9, pages 2793-2800.
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Christel J. Menet, Luc Van Rompaey & Raphaël Geney. 2013. 153 223 .
Jaebok ChoiEdward D. Ziga, Julie RitcheyLynne Collins, Julie L. Prior, Matthew L. CooperDavid Piwnica-Worms & John F. DiPersio. (2012) IFNγR signaling mediates alloreactive T-cell trafficking and GVHD. Blood 120:19, pages 4093-4103.
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MICHAEL SKYNNER, PHIL JEFFREY, MICHAEL BINKS & MICHAEL WOODROW. 2012. Anti-Inflammatory Drug Discovery. Anti-Inflammatory Drug Discovery 211 254 .
Marina Cetkovic-Cvrlje, Marin Olson & Ketaki Ghate. (2012) Targeting Janus tyrosine kinase 3 (JAK3) with an inhibitor induces secretion of TGF-β by CD4+ T cells. Cellular & Molecular Immunology 9:4, pages 350-360.
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Jinqi Liu & Huseyin Mehmet. (2011) Emerging therapies in the treatment of rheumatoid arthritis. Drug Development Research 72:8, pages 805-816.
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Thorbjørn Krejsgaard, Ulrik Ralfkiaer, Erik Clasen-Linde, Karsten W. Eriksen, Katharina L. Kopp, Charlotte M. Bonefeld, Carsten Geisler, Sally Dabelsteen, Mariusz A. Wasik, Elisabeth Ralfkiaer, Anders Woetmann & Niels Odum. (2011) Malignant Cutaneous T-Cell Lymphoma Cells Express IL-17 Utilizing the Jak3/Stat3 Signaling Pathway. Journal of Investigative Dermatology 131:6, pages 1331-1338.
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Lalgudi S. Harikrishnan, Muthoni G. Kamau, Honghe Wan, Jennifer A. Inghrim, Kurt Zimmermann, Xiaopeng Sang, Harold A. Mastalerz, Walter L. Johnson, Guifen Zhang, Louis J. Lombardo, Michael A. Poss, George L. Trainor, John S. Tokarski, Matthew V. Lorenzi, Dan You, Marco M. Gottardis, Kathy F. Baldwin, Jonathan Lippy, David S. Nirschl, Ruhui Qiu, Arthur V. Miller, Javed Khan, John S. Sack & Ashok V. Purandare. (2011) Pyrrolo[1,2-f]triazines as JAK2 inhibitors: Achieving potency and selectivity for JAK2 over JAK3. Bioorganic & Medicinal Chemistry Letters 21:5, pages 1425-1428.
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Tony Siu, Ekaterina S. Kozina, Joon Jung, Craig Rosenstein, Anjili Mathur, Michael D. Altman, Grace Chan, Lin Xu, Eric Bachman, Jan-Rung Mo, Melaney Bouthillette, Thomas Rush, Christopher J. Dinsmore, C. Gary Marshall & Jonathan R. Young. (2010) The discovery of tricyclic pyridone JAK2 inhibitors. Part 1: Hit to lead. Bioorganic & Medicinal Chemistry Letters 20:24, pages 7421-7425.
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