申请人:Astellas Pharma Inc.
公开号:EP2397479A1
公开(公告)日:2011-12-21
[Object]
A novel and excellent method for preventing or treating rejection in the transplantation of various organs, allergy diseases, autoimmune diseases, hematologic tumor, or the like, based on a PI3Kδ-selective inhibitory action and/or an IL-2 production inhibitory action, and/or a B cell proliferation inhibitory action (including an activation inhibitory action), is provided
[Means for Solution]
It was found that a 3-substituted triazine or 3-substituted pyrimidine derivative exhibits a PI3Kδ-selective inhibitory action, and/or an IL-2 production inhibitory action, and/or a B cell proliferation inhibitory action (including an activation inhibitory action), and can be an agent for preventing or treating rejection in the transplantation of various organs, allergy diseases (asthma, atopic dermatitis, etc.), autoimmune diseases (rheumatoid arthritis, psoriasis, ulcerative colitis, Crohn's disease, systemic lupus erytheznatosus, etc.), hematologic tumor (leukemia etc.), or the like, thereby completing the present invention.
目的
本发明提供了一种基于PI3Kδ选择性抑制作用和/或IL-2产生抑制作用和/或B细胞增殖抑制作用(包括活化抑制作用)的预防或治疗各种器官移植、过敏性疾病、自身免疫性疾病、血液肿瘤或类似疾病的排斥反应的新颖而出色的方法。
[解决方法]
发现一种 3-取代三嗪或 3-取代嘧啶衍生物具有 PI3Kδ 选择性抑制作用,和/或 IL-2 生成抑制作用,和/或 B 细胞增殖抑制作用(包括活化抑制作用),可作为预防或治疗各种器官移植排斥反应、过敏性疾病(哮喘、特应性皮炎等)、自身免疫性疾病(哮喘、特应性皮炎等)的药物。类风湿关节炎、牛皮癣、溃疡性结肠炎、克罗恩病、系统性红斑狼疮等)、血液肿瘤(白血病等)或类似疾病,从而完成本发明。