申请人:SANDOZ LTD.
公开号:EP0606044A1
公开(公告)日:1994-07-13
Novel compounds of formula I
wherein R₄, R₅, R₆, -a-b-, c, -d-e- and -f-g- are as defined are cytokine release inhibitors and IL-1 antagonists and are thus indicated for treatment of disorders with an aetiology associated with or comprising excessive cytokine release, particularly IL-1β release, including a wide variety of inflammatory states and diseases such as RA, osteoarthritis, septic shock, psoriasis, atherosclerosis, inflammatory bowel disease, Crohn's disease and asthma. Related known compounds Zearalenone and radicicol and derivatives thereof have also been found to have cytokine release inhibitor properties and have similar pharmaceutical applications.
化合物的式子为I,其中R₄、R₅、R₆、-a-b-、c、-d-e-和-f-g-的定义如下,它们是细胞因子释放抑制剂和IL-1受体拮抗剂,因此适用于治疗与细胞因子过度释放相关的病因学或包括过度释放IL-1β的疾病,特别是包括各种炎症状态和疾病,如RA、骨关节炎、脓毒症、银屑病、动脉粥样硬化、炎症性肠病、克罗恩病和哮喘。相关的已知化合物Zearalenone和radicicol及其衍生物也被发现具有细胞因子释放抑制剂的特性,并具有类似的药物应用。