Novel pyridazine derivatives and drugs containing the same...

C - Chemistry – Metallurgy – 07 – D

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C07D 237/04 (2006.01) A61K 31/50 (2006.01) C07D 213/00 (2006.01) C07D 237/00 (2006.01) C07D 237/14 (2006.01) C07D 237/18 (2006.01) C07D 401/04 (2006.01)

Patent

CA 2307111

Pyridazine derivatives represented by general formula (1) or salts thereof; and drugs containing the same as the active ingredient: wherein R1 is (substituted) aryl; R2 is phenyl substituted with lower alkoxy, lower alkylthio or the like at the position 4; R3 is H, lower alkoxy, lower haloalkyl, lower cycloalkyl, (substituted) aryl, (substituted) aryloxy, (substituted) nitrogenous heterocyclic residue, (substituted) aminocarbonyl or lower alkyl--carbonyl; A is a single bond, lower alkylene or lower alkenylene; X is O or S; and the broken line between the carbon atoms at the positions 4 and 5 represents a single or double bond. These compounds exhibit excellent inhibitory activity against the production of interleukin 1.beta., thus being useful as preventive and therapeutic drugs for immunologic diseases, inflammatory diseases, ischemic diseases and so on.

Cette invention se rapporte à des dérivés de pyridazine représentés par la formule générale (1) ou à des sels de ces dérivés; et à des médicaments contenant ces composés comme principe actif. Dans cette formule, R<1> représente aryle (substitué); R<2> représente phényle substitué par alcoxy inférieur, alkylthio inférieur ou similaire à la position 4; R<3> représente H, alcoxy inférieur, haloalkyle inférieur, cycloalkyle inférieur, aryle (substitué), aryloxy (substitué), un reste hétérocyclique azoté (substitué), aminocarbonyle (substitué) ou alkyle-carbonyle inférieur; A représente une liaison simple, alkylène inférieur ou alcénylène inférieur; X représente O ou S, et la ligne en pointillé entre les atomes de carbone aux positions 4 et 5 représente une liaison simple ou double. Ces composés ont une excellente action inhibitrice contre la production de l'interleukine 1 beta , ce qui les rend utiles comme médicaments préventifs et thérapeutiques contre les maladies immunologiques, les maladies inflammatoires, les maladies ischémiques, etc.

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