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63921-23-3Relevant articles and documents
Discovery and Biological Evaluation of N-Methyl-pyrrolo[2,3- b]pyridine-5-carboxamide Derivatives as JAK1-Selective Inhibitors
Park, Eunsun,Lee, Sun Joo,Moon, Heegyum,Park, Jongmi,Jeon, Hyeonho,Hwang, Ji Sun,Hwang, Hayoung,Hong, Ki Bum,Han, Seung-Hee,Choi, Sun,Kang, Soosung
, p. 958 - 979 (2021/02/01)
Janus kinase 1 (JAK1) plays a key role in most cytokine-mediated inflammatory and autoimmune responses through JAK/STAT signaling; thus, JAK1 inhibition is a promising therapeutic strategy for several diseases. Analysis of the binding modes of current JAK inhibitors to JAK isoforms allowed the design of N-alkyl-substituted 1-H-pyrrolo[2,3-b] pyridine carboxamide as a JAK1-selective scaffold, and the synthesis of various methyl amide derivatives provided 4-((cis-1-(4-chlorobenzyl)-2-methylpiperidin-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide (31g) as a potent JAK1-selective inhibitor. In particular, the (S,S)-enantiomer of 31g (38a) exhibited excellent potency for JAK1 and selectivity over JAK2, JAK3, and TYK2. On investigating the effect of 31g on hepatic fibrosis, it was found that it reduces the proliferation and fibrogenic gene expression of TGF-β-induced hepatic stellate cells (HSCs). Specifically, 31g significantly inhibited TGF-β-induced migration of HSCs at 0.25 μM in wound-healing assays.
WNT PATHWAY MODULATORS
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Paragraph 0247 - 0249, (2015/07/07)
The present invention relates to dihydropyrazolo[l,5-a]pyrimidine compounds of formula I, defined herein, as WNT pathways modulators, processes for making them, and pharmaceutical compositions comprising them. Methods of treatment of conditions mediated by WNT pathway signalling including cancer, fibrosis, stem cell and diabetic retinopathy, rheumatoid arthritis, psoriasis and myocardial infarction, comprising the compounds of formula I are also provided.
Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses
Tang, Guozhi,Kertesz, Denis J.,Yang, Minmin,Lin, Xianfeng,Wang, Zhanguo,Li, Wentao,Qiu, Zongxing,Chen, Junli,Mei, Jianghua,Chen, Li,Mirzadegan, Taraneh,Harris, Seth F.,Villase?or, Armando G.,Fretland, Jennifer,Fitch, William L.,Hang, Julie Qi,Heilek, Gabrielle,Klumpp, Klaus
scheme or table, p. 6020 - 6023 (2010/11/05)
Further investigation of the recently reported piperidine-4-yl- aminopyrimidine class of non-nucleoside reverse transcriptase inhibitors (NNRTIs) has been carried out. Thus, preparation of a series of N-phenyl piperidine analogs resulted in the identification of 3-carboxamides as a particularly active series. Analogs such as 28 and 40 are very potent versus wild-type HIV-1 and a broad range of NNRTI-resistant mutant viruses. Synthesis, structure-activity relationship (SAR), clearance data, and crystallographic evidence for the binding motif are discussed.