Results 261 to 270 of about 80,577 (303)
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Investigational Janus kinase inhibitors

Expert Opinion on Investigational Drugs, 2013
Dysregulation of the Janus kinase-signal transducer and activator of transcription (JAK-STAT) pathway is central to the pathophysiology of myeloproliferative neoplasms (MPN). Small molecule inhibitors of JAK family members are currently under investigation for the treatment of MPN.
Constantine S, Tam, Srdan, Verstovsek
openaire   +2 more sources

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   +24 more
openaire   +2 more sources

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
openaire   +1 more source

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
openaire   +2 more sources

Janus kinase-1 and Janus kinase-2 inhibitors for treating myelofibrosis

2013
This is the protocol for a review and there is no abstract. The objectives are as follows: To determine the clinical efficacy and safety of JAK1 and JAK2 inhibitors for treating MF generated by hematologic or non-hematologic conditions. © 2013 The Cochrane Collaboration.
Martí-Carvajal A.J.   +3 more
openaire   +2 more sources

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
openaire   +1 more source

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   +6 more
openaire   +2 more sources

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.   +22 more
openaire   +5 more sources

[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 ...
openaire   +1 more source

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   +10 more
openaire   +2 more sources

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