Results 261 to 270 of about 117,631 (302)

Mapping the kinase domain of janus kinase 3

Bioorganic & Medicinal Chemistry Letters, 2003
The utilization and impact of parallel synthesis on lead exploration around initial hit oxindole (1) are described. The emergent SAR, analogue design and functional impact will also be detailed.
Christopher, Adams, David J, Aldous, Shelley, Amendola, Paul, Bamborough, Colin, Bright, Sarah, Crowe, Paul, Eastwood, Garry, Fenton, Martyn, Foster, Trevor K P, Harrison, Sue, King, Justine, Lai, Christopher, Lawrence, Jean-Philippe, Letallec, Clive, McCarthy, Neil, Moorcroft, Kenneth, Page, Sudha, Rao, Jane, Redford, Shazia, Sadiq, Keith, Smith, John E, Souness, Sukanthini, Thurairatnam, Mark, Vine, Barry, Wyman   +24 more
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Janus-Kinase-Hemmer

Zeitschrift für Rheumatologie, 2012
Die Janus-Kinase-Inhibitoren stellen einen neuen therapeutischen Ansatz in der Behandlung der rheumatoiden Arthritis dar. In Phase-II- und -III-Studien zu Tofacitinib zeigte sich eine gute klinische Wirksamkeit mit einem ACR (American College of Rheumatology)-20-Ansprechen von > 50% sowohl fur die Mono- als auch die Kombinationstherapie mit Methotrexat.
E. Ostermeier, P. Roll, H.-P. Tony
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Janus kinase inhibitors: efficacy and safety

Current Opinion in Rheumatology, 2023
Purpose of review Janus kinase inhibitors (JAKi) have been available for the treatment of rheumatoid arthritis (RA) since 2012 and are indicated for patients with active disease despite csDMARD therapy. Efficacy and safety, as demonstrated in the clinical trials, was similar to biologics. A recent post marketing trial suggested
Stanley, Cohen, Virginia, Reddy
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Janus kinases and their role in growth and disease

Life Sciences, 1999
Janus kinases (JAK) play a crucial role in the initial steps of cytokine signaling. Each of the four members (JAK1, JAK2, JAK3, TYK2) of this non-receptor tyrosine kinase family is indispensable for the effects of distinct cytokines. Moreover, recent reports have added to our knowledge on their highly specific functions: JAK3 knockout mice and JAK3 ...
M, Aringer, A, Cheng, J W, Nelson, M, Chen, C, Sudarshan, Y J, Zhou, J J, O'Shea   +6 more
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Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs)

Bioorganic & Medicinal Chemistry Letters, 2009
A series of phenylaminopyrimidines has been identified as inhibitors of Janus kinases (JAKs). Development of this initial series led to the potent JAK2/JAK1 inhibitor CYT387 (N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-benzamide). Details of synthesis and SAR studies of these compounds are reported.
Burns, Christopher J., Bourke, David G., Andrau, Laura, Bu, Xianyong, Charman, Susan A., Donohue, Andrew C., Fantino, Emmanuelle, Farrugia, Michelle, Feutrill, John T., Joffe, Max, Kling, Marcel R., Kurek, Margarita, Nero, Tracy L., Nguyen, Thao, Palmer, James T., Phillips, Ian, Shackleford, David M, Sikanyika, Harrison, Styles, Michelle, Su, Stephen, Treutlein, Herbert, Zeng, Jun, Wilks, Andrew F.   +22 more
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Janus Kinase Inhibitors

2017
To control gene expression, cytokines and other extracellular molecules utilize the Janus kinase (JAK) and signal transducers and activators of transcription (STAT). Dysregulation of the JAK-STAT pathway has been implicated in a myriad of inflammatory and hematologic disorders.
Andrew Kim, Bruce Strober
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[Janus kinase inhibitors].

Zeitschrift fur Rheumatologie, 2022
In 2017 the first Janus kinase (JAK) inhibitors were approved for the treatment of rheumatoid arthritis in Germany. The mode of action of JAK inhibitors differs from biologicals, as multiple cytokines are inhibited. In comparison with the treatment with biologicals, JAK inhibitors have the advantage of oral application, three of the four currently ...
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[Janus kinase inhibitors].

Zeitschrift fur Rheumatologie, 2013
Janus protein tyrosine kinase (JAK) inhibitors are new therapeutic targets in the treatment of rheumatoid arthritis. Tofacitinib has shown good clinical efficacy in phase II and III studies with American College of Rheumatology (ACR) 20 response rates over 50% for monotherapy and in combination with methotrexate (MTX).
E, Ostermeier, P, Roll, H-P, Tony
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Dehydrocrenatidine Is a Novel Janus Kinase Inhibitor

Molecular Pharmacology, 2015
Janus kinase (JAK) 2 plays a pivotal role in the tumorigenesis of signal transducers and activators of transcription (STAT) 3 constitutively activated solid tumors. JAK2 mutations are involved in the pathogenesis of various types of hematopoietic disorders, such as myeloproliferative disorders, polycythemia vera, essential thrombocythemia, and primary ...
Jing, Zhang, Ning, Zhu, Yuping, Du, Qifeng, Bai, Xing, Chen, Jing, Nan, Xiaodong, Qin, Xinxin, Zhang, Jianwen, Hou, Qin, Wang, Jinbo, Yang   +10 more
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Janus Activated Kinase inhibition in Myelofibrosis

Indian Journal of Cancer, 2012
Janus Activated Kinase (JAK) 2 plays an important role in the pathogenesis of myelofibrosis (MF). Ruxolitinib (INCB018424, Jakafi) is a potent dual JAK1 and JAK2 inhibitor. In November 2011, it became approved by the US FDA for the treatment of intermediate or high-risk MF.
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