892408-42-3Relevant articles and documents
Discovery of Pyridazinone and Pyrazolo[1,5- a]pyridine Inhibitors of C-Terminal Src Kinase
O'Malley, Daniel P.,Ahuja, Vijay,Fink, Brian,Cao, Carolyn,Wang, Cindy,Swanson, Jesse,Wee, Susan,Gavai, Ashvinikumar V.,Tokarski, John,Critton, David,Paiva, Anthony A.,Johnson, Benjamin M.,Szapiel, Nicolas,Xie, Dianlin
, p. 1486 - 1491 (2019)
C-terminal Src kinase (CSK) functions as a negative regulator of T cell activation through inhibitory phosphorylation of LCK, so inhibitors of CSK are of interest as potential immuno-oncology agents. Screening of an internal kinase inhibitor collection identified pyridazinone lead 1, and a series of modifications led to optimized compound 13. Compound 13 showed potent activity in biochemical and cellular assays in vitro and demonstrated the ability to increase T cell proliferation induced by T cell receptor signaling. Compound 13 gave extended exposure in mice upon oral dosing and produced a functional response (decrease in LCK phosphorylation) in mouse spleens at 6 h post dose.
COMPOUNDS AND USES THEREOF
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Page/Page column 160, (2021/08/06)
The present disclosure features compounds and methods useful for the treatment of BAF complex-related disorders.
Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3-Oxo-3,4-dihydro-2 H-benzo[ b][1,4]oxazin-6-yl Moiety
Ikeda, Shuhei,Sugiyama, Hideyuki,Tokuhara, Hidekazu,Murakami, Masataka,Nakamura, Minoru,Oguro, Yuya,Aida, Jumpei,Morishita, Nao,Sogabe, Satoshi,Dougan, Douglas R.,Gay, Sean C.,Qin, Ling,Arimura, Naoto,Takahashi, Yasuko,Sasaki, Masako,Kamada, Yusuke,Aoyama, Kazunobu,Kimoto, Kouya,Kamata, Makoto
, p. 11014 - 11044 (2021/08/24)
The therapeutic potential of monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases has attracted attention worldwide. However, the availability of reversible-type inhibitor is still limited to clarify the pharmacological eff
