175358-01-7Relevant articles and documents
Fragment-based drug discovery of potent and selective MKK3/6 inhibitors
Adams, Mark,Kobayashi, Toshitake,Lawson, J. David,Saitoh, Morihisa,Shimokawa, Kenichiro,Bigi, Simone V.,Hixon, Mark S.,Smith, Christopher R.,Tatamiya, Takayuki,Goto, Masayuki,Russo, Joseph,Grimshaw, Charles E.,Swann, Steven
, p. 1086 - 1089 (2016)
The MAPK signaling cascade, comprised of several linear and intersecting pathways, propagates signaling into the nucleus resulting in cytokine and chemokine release. The Map Kinase Kinase isoforms 3 and 6 (MKK3 and MKK6) are responsible for the phosphorylation and activation of p38, and are hypothesized to play a key role in regulating this pathway without the redundancy seen in downstream effectors. Using FBDD, we have discovered efficient and selective inhibitors of MKK3 and MKK6 that can serve as tool molecules to help further understand the role of these kinases in MAPK signaling, and the potential impact of inhibiting kinases upstream of p38.
NITROGEN HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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, (2021/06/26)
The present disclosure relates to compounds of formula (I): and pharmaceutically acceptable salts and stereoisomers thereof. The present disclosure also relates to methods of preparing the compounds, compositions comprising the compounds, and methods of using the compounds as inhibitors of receptor tyrosine kinases, in particular oncogenic mutants of ErbB-receptors e.g. in the treatment of cancer.
4, 6-disubstituted pyridine [3, 2-d] pyrimidine compound as well as preparation and application thereof
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, (2020/04/02)
The invention belongs to the technical field of medicines. The invention relates to the field of pharmaceutical chemistry, in particular to a 4, 6-disubstituted pyridine [3, 2-d] pyrimidine compound and pharmaceutically acceptable salt thereof, a preparation method of the compound, a pharmaceutical composition taking the compound as an active ingredient, and application of the compound in preparation of an MNK inhibitor and drugs for treating and/or preventing various cancers and/or metabolic diseases. The present invention relates to compounds represented by formulas I, II, III or IV, and pharmaceutically acceptable salts, hydrates, solvates and metabolites thereof, wherein the variables are described in the claims and the description.