1010120-55-4Relevant articles and documents
Discovery of triazolo [1,5-a] pyridine derivatives as novel JAK1/2 inhibitors
Chen, Dawei,Jiang, Yuyang,Li, Anqi,Liu, Zijian,Lu, Kuan,Wu, Weibin,Xiao, Boren,Yuan, Zigao,Zhai, Xin,Zhang, Cunlong
, (2020)
Small molecule JAK inhibitors have been demonstrated efficacy in rheumatoid arthritis, inflammatory bowel disease, and psoriasis with the approval of several drugs. Aiming to develop potent JAK1/2 inhibitors, two series of triazolo [1,5-a] pyridine derivatives were designed and synthesized by various strategies. The pharmacological results identified the optimized compounds J-4 and J-6, which exerted high potency against JAK1/2, and selectivity over JAK3 in enzyme assays. Furthermore, J-4 and J-6 effectively suppressed proliferation of JAK1/2 high-expression BaF3 cells accompanied with acceptable metabolic stability in liver microsomes. Therefore, J-4 and J-6 might serve as promising JAK1/2 inhibitors for further investigation.
Triazolo pyridine compound and preparation method, medicinal composition and application thereof
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, (2020/05/08)
The invention discloses a triazolo pyridine compound as well as a preparation method, a medicinal composition and application thereof. The compound is selected from a compound shown in a general formula I, or a tautomer, an enantiomer, a diastereoisomer,
JAK INHIBITORS
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Paragraph 0076, (2018/05/03)
Disclosed is a series of JAK inhibitors, which specifically relates to a compound shown in formula (I) or pharmaceutically acceptable salts thereof.