847818-71-7Relevant articles and documents
AMINOPYRIDINE COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF
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Paragraph 0269-0271; 0275-0277, (2021/11/04)
The present invention discloses an aminopyridine compounds, a preparation method and use thereof, particularly the aminopyridine compounds of formula (I), pharmaceutical compositions containing the same, the method for preparing the same and the use thereof in the prophylaxis or treatment of an adenosine A2a receptor related disease.
MAP4K4 INHIBITORS
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Paragraph 00281-00283, (2020/07/05)
This invention relates to compounds that may be useful as inhibitors of Mitogen-activated Protein Kinase Kinase Kinase Kinase-4 (MAP4K4). The invention also relates to the use of these compounds, for example in a method of treatmentof cardiac conditions.In particular, the present invention relates to compounds of formula (I):
Structure-based design and synthesis of 1H-pyrazolo[3,4-d]pyrimidin-4-amino derivatives as Janus kinase 3 inhibitors
Yin, Yuan,Chen, Cheng-Juan,Yu, Ru-Nan,Wang, Zhi-Jian,Zhang, Tian-Tai,Zhang, Da-Yong
, p. 4774 - 4786 (2018/08/24)
Janus kinases (JAKs) regulate various inflammatory and immune responses and are targets for the treatment of inflammatory and immune diseases. Here we report the discovery and optimization of 1H-pyrazolo[3,4-d]pyrimidin-4-amino as covalent JAK3 inhibitors that exploit a unique cysteine (Cys909) residue in JAK3. Our optimization study gave compound 12a, which exhibited potent JAK3 inhibitory activity (IC50 of 6.2 nM) as well as excellent JAK kinase selectivity (>60-fold). In cellular assay, 12a exhibited potent immunomodulating effect on IL-2-stimulated T cell proliferation (IC50 of 9.4 μM). Further, compound 12a showed efficacy in delayed hypersensitivity assay. The data supports the further investigation of these compounds as novel JAKs inhibitors.