As demonstrated in preclinical animal models, the disruption of PI3Kδ expression or its activity leads to a decrease in inflammatory and immune responses. Therefore, inhibition of PI3Kδ may provide an alternative treatment for autoimmune diseases, such as RA, SLE, and respiratory ailments. Herein, we disclose the identification of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent, selective and orally bioavailable PI3Kδ inhibitors. The lead compound demonstrated efficacy in an in vivo mouse KLH model.

中文翻译：

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7-（3-（哌嗪-1-基）苯基）吡咯并[2,1-f] [1,2,4]三嗪-4-胺衍生物的发现作为高效和选择性的PI3Kδ抑制剂

如临床前动物模型所示，PI3Kδ表达或其活性的破坏导致炎症反应和免疫反应降低。因此，抑制PI3Kδ可能为自身免疫性疾病（例如RA，SLE和呼吸系统疾病）提供替代治疗。在这里，我们公开了7-（3-（哌嗪-1-基）苯基）吡咯并[2,1-f] [1,2,4]三嗪-4-胺衍生物的鉴定为高效，选择性和口服生物利用度PI3Kδ抑制剂。铅化合物在体内小鼠KLH模型中显示出功效。