申请人:Kowa Co., Ltd.
公开号:US06348468B1
公开(公告)日:2002-02-19
This invention relates to pyridazine derivatives represented by the formula (1):
wherein R1 represents a (substituted) aryl group, R2 represents a phenyl group substituted at 4-position by a lower alkoxyl group or a lower alkylthio group, R3 represents 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-1&bgr; production, and are useful as preventives and therapeutics for immune system diseases, inflammatory diseases, ischemic diseases and the like.
这项发明涉及由式(1)表示的吡啶嗪衍生物:
其中R1代表(取代的)芳基,R2代表在4位被低烷氧基或低烷硫基取代的苯基,R3代表低烷氧基、卤代低烷基、低环烷基、(取代的)芳基、(取代的)芳氧基、(取代的)含氮杂环环残基、(取代的)氨基羰基或低烷基羰基,A代表单键、低烷基烯基或低烷烯基,X代表O或S,虚线表示4位和5位之间的碳-碳键为单键或双键,或其盐;以及含有它们作为有效成分的药物。这些化合物对白细胞介素-1β的产生具有出色的抑制活性,并可用作免疫系统疾病、炎症性疾病、缺血性疾病等的预防和治疗药物。