89466-42-2Relevant academic research and scientific papers
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
Convenient synthesis of 2-(methylsulfonyl)pyrimidine derivatives
Huang, Tong-Hui,Zhou, Shan-Shan,Wu, Xin,An, Lin,Yin, Xiao-Xing
supporting information, p. 714 - 720 (2018/02/16)
An efficient and convenient approach for the preparation of functionalized 2-(methylsulfonyl)pyrimidine derivatives has been developed through cyclic condensation of malonate derivatives with S-methylisothiouronium sulfate followed by derivation and oxidation in water–acetone mixture using oxone as the oxidant. This synthetic strategy provides an efficient and environmentally friendly approach for easy access to 2-(methylsulfonyl)pyrimidine derivatives with considerable yields.
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%).
A simple method for the preparation of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dithione derivatives
Kobayashi, Kazuhiro,Kuroda, Minami,Tanaka, Noriyuki,Yokoi, Yuki,Kobayashi, Akihiro,Hiyoshi, Hidetaka,Umezu, Kazuto
, p. 1933 - 1939 (2014/08/18)
A facile and efficient two-step sequence for the preparation of 1,3-disubstituted pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dithiones starting with 4-chloro-6-methoxy-2-(methylsulfanyl)pyrimidine has been developed. Thus, the reaction of 4-chloro-5-lithio-6-me
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.
Aminopyrimidinone Cdc7 Kinase Inhibitors
Woods, Keith W.,Lai, Chunqiu,Miyashiro, Julie M.,Tong, Yunsong,Florjancic, Alan S.,Han, Edward K.,Soni, Niru,Shi, Yan,Lasko, Loren,Leverson, Joel D.,Johnson, Eric F.,Shoemaker, Alexander R.,Penning, Thomas D.
scheme or table, p. 1940 - 1943 (2012/04/17)
We have investigated the SAR of a series of pyrimidinone-containing Cdc7 kinase inhibitors. A wide range of amine substitutions give potent compounds with activities (Ki) less than 1 nM. Kinase selectivity is reasonable and cytotoxicity corresponds to inhibition of MCM2 phosphorylation.
Pyrimidinone compounds useful as kinase inhibitors
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Page/Page column 11-12; 23, (2010/11/27)
This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 proteins.
IMIDAZOLYL PYRIMIDINE DERIVATIVES USEFUL AS IL-8 RECEPTOR MODULATORS
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Page 25, (2010/02/07)
The invention relates to compounds of the formula I, wherein R1, R2, R3 and R4 are each independently selected from H, (1-4C)alkyl, (1-4C)alkoxy, trifluoromethyl, trifluoromethoxy, halogen, amino, sulfonamide, cyano, OH and nitro; R5 is H or (1-6C)alkyl;
Uracil compounds and use thereof
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, (2008/06/13)
The present invention relates to an uracil compound of the formula [I]: [wherein, Q—R3represents a R3-substituted group of a 5-membered or 6-membered heterocyclic ring having one or two nitrogen selected from the group consisting of
2-benzyloxy-4-phenoxypyrimidine derivative, processes for producing the derivative and herbicidal composition containing the derivative
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, (2008/06/13)
A 2-benzyloxy-4-phenoxypyrimidine derivative represented by the formula (I): STR1 wherein R1 represents hydrogen, a halogen, C1 -C4 alkyl, C1 -C4 haloalkyl, C1 -C4 alkoxy, C1 -C4 haloalkoxy, C3 -C5 alkenyloxy, C1 -C4 alkylthio, C1 -C4 haloalkylthio, cyano, or phenyl; each X, which may be identical or different if n is greater than 1, represents a halogen, C1 -C4 alkyl, C1 -C4 haloalkyl, or C1 -C4 alkoxy; each Y, which may be identical or different if m is greater than 1, represents a halogen, C1 -C4 alkyl, C1 -C4 haloalkyl, C1 -C4 alkoxy, C1 -C4 haloalkoxy, C1 -C4 alkylthio, or C1 -C4 haloalkylthio; and n and m each independently represent an integer of 0 to 5, which is useful as a herbicide.
