1204333-58-3Relevant articles and documents
PROCESS FOR PREPARING 1-[(3R,4S)-4-CYANOTETRAHYDROPYRAN-3-YL]-3-[(2-FLUORO-6-METHOXY-4-PYRIDYL)AMINO]P YRAZOLE-4-CARBOXAMIDE
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Page/Page column 22-23, (2020/07/07)
The application relates to processes for the preparation of 1-[(3R,4S) -4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl) amino]pyrazole-4-carboxamide (I) which include (i) a synthesis for bromo and iodo pyridine intermediates, (ii) a synthesis of a pyrazole ester intermediate which can be obtained in enantiopure form and (iii) the combination of these intermediates into compound (I).
Identification of Potent and Selective RIPK2 Inhibitors for the Treatment of Inflammatory Diseases
He, Xiaohui,Da Ros, Sara,Nelson, John,Zhu, Xuefeng,Jiang, Tao,Okram, Barun,Jiang, Songchun,Michellys, Pierre-Yves,Iskandar, Maya,Espinola, Sheryll,Jia, Yong,Bursulaya, Badry,Kreusch, Andreas,Gao, Mu-Yun,Spraggon, Glen,Baaten, Janine,Clemmer, Leah,Meeusen, Shelly,Huang, David,Hill, Robert,Nguyen-Tran, Van,Fathman, John,Liu, Bo,Tuntland, Tove,Gordon, Perry,Hollenbeck, Thomas,Ng, Kenneth,Shi, Jian,Bordone, Laura,Liu, Hong
supporting information, p. 1048 - 1053 (2017/10/18)
NOD2 (nucleotide-binding oligomerization domain-containing protein 2) is an internal pattern recognition receptor that recognizes bacterial peptidoglycan and stimulates host immune responses. Dysfunction of NOD2 pathway has been associated with a number of autoinflammatory disorders. To date, direct inhibitors of NOD2 have not been described due to technical challenges of targeting the oligomeric protein complex. Receptor interacting protein kinase 2 (RIPK2) is an intracellular serine/threonine/tyrosine kinase, a key signaling partner, and an obligate kinase for NOD2. As such, RIPK2 represents an attractive target to probe the pathological roles of NOD2 pathway. To search for selective RIPK2 inhibitors, we employed virtual library screening (VLS) and structure based design that eventually led to a potent and selective RIPK2 inhibitor 8 with excellent oral bioavailability, which was used to evaluate the effects of inhibition of RIPK2 in various in vitro assays and ex vivo and in vivo pharmacodynamic models.
Fluorine-controlled C-H borylation of arenes catalyzed by a PSiN-pincer platinum complex
Takaya, Jun,Ito, Shisei,Nomoto, Hironori,Saito, Narumasa,Kirai, Naohiro,Iwasawa, Nobuharu
supporting information, p. 17662 - 17665 (2015/12/18)
An efficient, regioselective synthesis of fluorine-substituted arylboronic esters was achieved through fluorine-controlled C-H borylation of arenes with diboron catalyzed by a PSiN-platinum complex. The promising utility of the PSiN-platinum catalyst and its unique regioselectivity were demonstrated for the first time, which would complement the well-developed Ir-catalyzed C-H borylation.