89466-42-2Relevant articles and documents
NOVEL 2-PYRIMIDONE ANALOGS AS POTENT ANTIVIRAL AGENTS AGAINST ALPHAVIRUSES
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Paragraph 00413, (2021/10/11)
The present disclosure is concerned with 2-pyrimidone compounds that are capable of inhibiting a viral infection and methods of treating alphavirus viral infections such as, for example, chikungunya, Eastern equine encephalitis (EEEV), Western equine ence
Discovery and Structure Enabled Synthesis of 2,6-Diaminopyrimidin-4-one IRAK4 Inhibitors
Seganish, W. Michael,Fischmann, Thierry O.,Sherborne, Brad,Matasi, Julius,Lavey, Brian,McElroy, William T.,Tulshian, Deen,Tata, James,Sondey, Christopher,Garlisi, Charles G.,Devito, Kristine,Fossetta, James,Lundell, Daniel,Niu, Xiaoda
supporting information, p. 942 - 947 (2015/08/24)
We report the identification and synthesis of a series of aminopyrimidin-4-one IRAK4 inhibitors. Through high throughput screening, an aminopyrimidine hit was identified and modified via structure enabled design to generate a new, potent, and kinase selective pyrimidin-4-one chemotype. This chemotype is exemplified by compound 16, which has potent IRAK4 inhibition activity (IC50 = 27 nM) and excellent kinase selectivity (>100-fold against 99% of 111 tested kinases), and compound 31, which displays potent IRAK4 activity (IC50 = 93 nM) and good rat bioavailability (F = 42%).
AMINOPYRIMIDINONES AS INTERLEUKIN RECEPTOR-ASSOCIATED KINASE INHIBITORS
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Page/Page column 38, (2013/05/22)
This invention relates to aminopyrimidinone compounds of Formula (I) that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment or prevention of inflammatory diseases, including rheumatoid arthritis and inflammatory bowel disease.
