- NOVEL 2-PYRIMIDONE ANALOGS AS POTENT ANTIVIRAL AGENTS AGAINST ALPHAVIRUSES
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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
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Paragraph 00413
(2021/10/11)
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- Convenient synthesis of 2-(methylsulfonyl)pyrimidine derivatives
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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.
- Huang, Tong-Hui,Zhou, Shan-Shan,Wu, Xin,An, Lin,Yin, Xiao-Xing
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p. 714 - 720
(2018/02/16)
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- Discovery and Structure Enabled Synthesis of 2,6-Diaminopyrimidin-4-one IRAK4 Inhibitors
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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%).
- 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
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supporting information
p. 942 - 947
(2015/08/24)
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- A simple method for the preparation of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dithione derivatives
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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
- Kobayashi, Kazuhiro,Kuroda, Minami,Tanaka, Noriyuki,Yokoi, Yuki,Kobayashi, Akihiro,Hiyoshi, Hidetaka,Umezu, Kazuto
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p. 1933 - 1939
(2014/08/18)
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- AMINOPYRIMIDINONES AS INTERLEUKIN RECEPTOR-ASSOCIATED KINASE INHIBITORS
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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.
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Page/Page column 38
(2013/05/22)
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- Aminopyrimidinone Cdc7 Kinase Inhibitors
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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.
- 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.
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scheme or table
p. 1940 - 1943
(2012/04/17)
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- Pyrimidinone compounds useful as kinase inhibitors
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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.
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Page/Page column 11-12; 23
(2010/11/27)
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- IMIDAZOLYL PYRIMIDINE DERIVATIVES USEFUL AS IL-8 RECEPTOR MODULATORS
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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;
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- Uracil compounds and use thereof
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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
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- 2-benzyloxy-4-phenoxypyrimidine derivative, processes for producing the derivative and herbicidal composition containing the derivative
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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.
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- Herbicidal composition containing 2-benzyloxypyrimidine derivatives, processes for producing the derivatives and 2-benzyloxypyrimidine derivatives
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A herbicidal composition comprising a herbicidally effective amount of a 2-benzyloxypyrimidine derivative represented by the formula (I): STR1 wherein R1 and R2 are each independently H, a halogen, hydroxyl, C1 -C4 alkyl, C1 -C4 haloalkyl, C3 -C5 alkenyl, C3 -C5 alkynyl, C1 -C4 alkoxy, C1 -C4 haloalkoxy, C3 -C5 alkenyloxy, C3 -C5 alkynyloxy, C1 -C4 alkylthio, or phenyl; n is an integer of 0 to 5; and each X which may be identical or different if n is greater than 1, is a halogen, C1 -C4 alkyl, C1 -C4 haloalkyl, C1 -C4 alkoxy, C1 -C4 alkylthio, C7 -C9 aralkyloxy, phenyl, hydroxymethyl, hydroxycarbonyl, C1 -C4 alkoxycarbonyl, or nitro, and an adjuvant.
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