Results 261 to 270 of about 74,157 (302)

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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Oral Janus kinase inhibitors for atopic dermatitis

Annals of Allergy, Asthma & Immunology, 2023
Atopic dermatitis (AD) is one of the most common inflammatory skin conditions. The pathogenesis of AD involves skin barrier disruption and immune activation of T-helper (TH)2 and TH22 and varying degrees of TH1 and TH17 activation in various patient subtypes.
Daniela, Mikhaylov, Benjamin, Ungar, Yael, Renert-Yuval, Emma, Guttman-Yassky   +3 more
openaire   +2 more sources

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 Kinase Inhibitors: A Review of Their Application in the Vitiligo

Mini-Reviews in Medicinal Chemistry, 2021
Abstract: The small-molecular inhibitors targeted JAks (JAK inhibitors), could modulate the cytokines-mediated signaling via JAK-STAT pathway, which plays a important role in immune regulation and cell proliferation. The JAK inhibitors are previously designed and synthesized to treat diseases involved with hematologic and immune system.
Chao, Niu, Hunjun, Xie, Haji Akber, Aisa
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[Pharmacology of Janus kinase inhibitors].

Der Hautarzt; Zeitschrift fur Dermatologie, Venerologie, und verwandte Gebiete, 2019
Modern dermatotherapy is dominated by the development of various biologicals and small molecules. Janus kinase inhibitors (JAKi) form a novel class of small molecular synthetic compounds inhibiting the intracellular signal transduction of cytokine receptors. Cytokines are key mediators in the pathophysiology of numerous inflammatory skin diseases. Many
F, Solimani, F J, Hilke, K, Ghoreschi
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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
openaire   +1 more source

Janus kinases inhibitors for treating patients with rhupus

Joint Bone Spine, 2020
HIGHLIGHTS • baricitinib and tofacitinib are effective in patients with Rhupus • JAK inhibitors are an alternative option in patients with refractory SLE • JAK inhibitors have a steroid-sparing effect in patients with ...
Garufi C., Mancuso S., Spinelli F. R., Truglia S., Ceccarelli F., Alessandri C., Conti F.   +6 more
openaire   +2 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

[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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Inhibitors of the Janus Kinases

Journal of Clinical Gastroenterology, 2019
Background: The treatment of ulcerative colitis (UC) is based on conventional therapies (aminosalicylates, corticosteroids, and immunosuppressants) and when these are ineffective, biologic drugs. However, in a substantial portion of patients undergoing treatment with biologic agents there is primary or secondary loss of ...
Elisabetta, Antonelli, Gabriele, Torti, Gabrio, Bassotti   +2 more
openaire   +2 more sources