2096-21-1Relevant academic research and scientific papers
CYCLOALKANE-1,3-DIAMINE DERIVATIVE
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Paragraph 1399-1402, (2021/09/03)
The present invention provides a compound or a pharmaceutically acceptable salt thereof having an inhibitory action on the interaction between menin and an MLL protein. The compound represented by the formula (1) or a pharmaceutically acceptable salt thereof. wherein, in the formula (1), the dotted circle, R1, R2, R3, R4, R5, R6, R7, R8, Ring Q1, W, m and n are each as defined in the description.
Phenyl substituted 4-hydroxypyridazin-3(2 H)-ones and 5-hydroxypyrimidin-4(3 H)-ones: Inhibitors of influenza a endonuclease
Sagong, Hye Yeon,Bauman, Joseph D.,Patel, Disha,Das, Kalyan,Arnold, Eddy,Lavoie, Edmond J.
, p. 8086 - 8098 (2014/12/10)
Seasonal and pandemic influenza outbreaks remain a major human health problem. Inhibition of the endonuclease activity of influenza RNA-dependent RNA polymerase is attractive for the development of new agents for the treatment of influenza infection. Our earlier studies identified a series of 5- and 6-phenyl substituted 3-hydroxypyridin-2(1H)-ones that were effective inhibitors of influenza endonuclease. These agents identified as bimetal chelating ligands binding to the active site of the enzyme. In the present study, several aza analogues of these phenyl substituted 3-hydroxypyridin-2(1H)-one compounds were synthesized and evaluated for their ability to inhibit the endonuclease activity. In contrast to the 4-aza analogue of 6-(4-fluorophenyl)-3-hydroxypyridin-2(1H)-one, the 5-aza analogue (5-hydroxy-2-(4-fluorophenyl)pyrimidin-4(3H)-one) did exhibit significant activity as an endonuclease inhibitor. The 6-aza analogue of 5-(4-fluorophenyl)-3-hydroxypyridin-2(1H)-one (6-(4-fluorophenyl)-4-hydroxypyridazin-3(2H)-one) also retained modest activity as an inhibitor. Several varied 6-phenyl-4-hydroxypyridazin-3(2H)-ones and 2-phenyl-5-hydroxypyrimidin-4(3H)-ones were synthesized and evaluated as endonuclease inhibitors. The SAR observed for these aza analogues are consistent with those previously observed with various phenyl substituted 3-hydroxypyridin-2(1H)-ones.
THERAPEUTIC HYDROXYPYRIDINONES, HYDROXYPYRIMIDINONES AND HYDROXYPYRIDAZINONES
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Page/Page column 73, (2014/04/03)
The invention provides compounds of formula (I): and salts and prodrugs thereof wherein R4, X1 and X2 have any of the meanings defined in the specification, as well as pharmaceutical compositions comprising the compounds or salts and methods for their use in therapy. The compounds have useful antiviral properties.
Studies on Syntheses and Reactions of Methoxypyridazines. II. Methoxylation of 3,4,6-Trichloropyridazine
Nagashima, Hiromu,Ukai, Kiyoshi,Oda, Hirohisa,Masaki, Yukio,Kaji, Kenji
, p. 350 - 356 (2007/10/02)
Methoxylation of 3,4,6-trichloropyridazine (1) with sodium methoxide was investigated in detail.Dimethoxylation of 1 afforded 6-chloro-3,4-dimethoxypyridazine (5) and a molecular complex (M) which is composed of 5 and 3-chloro-4,6-dimethoxypyridazine (6) in a ratio of 1:1.The nature of the complex (M) was examined by thermal and X-ray analyses.The molecular complex (M) was also obtained by monomethoxylation of 3,6-dichloro-4-methoxypyridazine (3) with sodium methoxide. Keywords --- 3,4,6-trichloropyridazine; methoxylation; pyridazinone; dimethoxymonochloropyridazine; trimethoxypyridazine; molecular complex; thermal analysis; X-ray analysis
