- Pyridazine compounds and compositions containing the same
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This invention relates to pyridazine derivatives represented by the formula (1): wherein R1represents a (substituted) aryl group, R2represents a phenyl group substituted at 4-position by a lower alkoxyl group or a lower alkylthio group, R3represents a lower alkoxyl group, a halogenated lower alkyl group, a lower cycloalkyl group, a (subsituted) aryl group, a (substituted) aryloxy group, a (substituted) nitrogen-containing heterocyclic ring residue, a (substituted) aminocarbonyl group or a lower alkylcarbonyl group, A represents a single bond, a lower alkylene group or a lower alkenylene group, X represents O or S, and the dashed line indicates that the carbon-carbon bond between the 4-position and the 5-position is a single bond or a double bond, or salts thereof; and also to medicines containing them as effective ingredients. These compounds have excellent inhibitory activity against interleukin-1β production, and are useful as preventives and therapeutics for immune system diseases, inflammatory diseases, ischemic diseases and the like.
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Page column 24
(2008/06/13)
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- Synthesis and bioactivities of novel 5,6-Bis(4-methoxyphenyl)-2H-pyridazin-3-one derivatives: Inhibitors of interleukin-1 beta (IL-1β) production
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New 5,6-bis(4-methoxyphenyl)-2H-pyridazin-3-one derivatives were prepared, and their abilities to inhibit IL-1β production were evaluated. Some compounds showed potent inhibitory activity against IL-1β production in HL-60 cells stimulated with lipopolysaccharide (LPS). The synthesis and structure-activity relationships of these compounds are described.
- Matsuda, Takayuki,Aoki, Taro,Koshi, Tomoyuki,Ohkuchi, Masao,Shigyo, Hiromichi
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p. 2373 - 2375
(2007/10/03)
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