871836-51-0Relevant articles and documents
Pyrazolopyridine compound and preparation method thereof
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, (2019/10/29)
The embodiment of the invention discloses a pyrazolopyridine compound and a preparation method thereof. The preparation method includes the steps of: taking 2-chloro-4-amino-3-methylpyridine as the raw materials to prepare a compound shown as formula (III). The preparation method takes 2-chloro-4-amino-3-methylpyridine as the raw materials to prepare 4-chloro-1H-pyrazolo[4, 3-c]pyridine, has the advantages of cheap and easily available raw materials, high reaction activity, mild reaction conditions, simple separation and purification method, high product purity, etc., and can be well applied to industrial production.
Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model
Liang, Jun,Van Abbema, Anne,Balazs, Mercedesz,Barrett, Kathy,Berezhkovsky, Leo,Blair, Wade S.,Chang, Christine,Delarosa, Donnie,DeVoss, Jason,Driscoll, Jim,Eigenbrot, Charles,Goodacre, Simon,Ghilardi, Nico,MacLeod, Calum,Johnson, Adam,Bir Kohli, Pawan,Lai, Yingjie,Lin, Zhonghua,Mantik, Priscilla,Menghrajani, Kapil,Nguyen, Hieu,Peng, Ivan,Sambrone, Amy,Shia, Steven,Smith, Jan,Sohn, Sue,Tsui, Vickie,Ultsch, Mark,Williams, Karen,Wu, Lawren C.,Yang, Wenqian,Zhang, Birong,Magnuson, Steven
, p. 4370 - 4376 (2017/09/12)
Herein we report identification of an imidazopyridine class of potent and selective TYK2 inhibitors, exemplified by prototype 6, through constraint of the rotatable amide bond connecting the pyridine and aryl rings of compound 1. Further optimization led to generation of compound 30 that potently inhibits the TYK2 enzyme and the IL-23 pathway in cells, exhibits selectivity against cellular JAK2 activity, and has good pharmacokinetic properties. In mice, compound 30 demonstrated dose-dependent reduction of IL-17 production in a PK/PD model as well as in an imiquimod-induced psoriasis model. In this efficacy model, the IL-17 decrease was accompanied by a reduction of ear thickness indicating the potential of TYK2 inhibition as a therapeutic approach for psoriasis patients.
HETEROCYCLIC COMPOUND
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, (2015/04/15)
The present invention provides a compound having a superior JAK inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like, or a salt thereof. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.