FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to derivatives of pyridazine represented by the following formula (I): wherein R1 means C1-C6-alkoxyl group, C1-C6-alkylthio-group or halogen atom; R2 means hydrogen atom, C1-C6-alkoxyl group, C1-C6-alkyl-thio-group or halogen atom; R3 means linear or branched C1-C6-alkyl or C2-C9-alkenyl group that can be substituted with hydroxy-group, halogen atom, cyano-group, C3-C6-cycloalkyl group or phenyl or pyridyl group that can comprise one-three substituents taken among halogen atom, nitro-group, amino-group that can be substituted with C1-C6-alkyl group, hydroxyl-C1-C6-alkyl group, pyridyl-C1-C6-alkyl group or C1-C6-alkylthiophenyl group; R4 means carboxyl group, C1-C6-alkoxycarbonyl group, carbamoyl or C1-C6-alkylthiocarbamoyl group that can be substituted with C1-C6-alkyl group, phenyl group, pyridyl group, phenyl-C1-C6-alkyl group or pyridyl-C1-C6-alkyl group, amino-group that can be substituted with C1-C6-alkoxycarbonyl group, phenyl-C1-C6-alkoxycarbonyl group, C1-C6-alkylthiophenyl-C1-C6-alkoxycarbonyl group, C1-C5-acyl group, C1-C6-alkyl group, phenyl-C1-C6-alkyl group, pyridyl-C1-C6-alkyl group or C1-C6/ -alkylsulfonyl group; or ureido-group that can be substituted with C1-C6-alkyl group; and dotted line indicates that the bond carbon-carbon between position 4 and position 5 is a simple bond or double bond; or its salt. Compounds of the formula (I) elicit inhibitory activity against producing interleukin-1β and can be used as an active component of medicinal agent for prophylaxis and treatment of rheumatism or arthritis. Invention relates also to medicinal agent eliciting above indicated activity and method for treatment of disease caused by stimulation of producing interleukin-1β, such as rheumatism or arthritis. EFFECT: valuable medicinal properties of compounds. 10 cl, 3 tbl, 130 ex
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Authors
Dates
2004-01-20—Published
1999-02-26—Filed