IRAK4 is a key mediator of innate immunity. There is a high interest in identifying novel IRAK4 inhibitors for the treatment of inflammatory autoimmune diseases. We describe here a highly potent and selective IRAK4 inhibitor (HS271) that exhibited superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties. HS271 displayed robust in vivo anti-inflammatory efficacy as evaluated in rat models of LPS induced TNFα production collagen-induced arthritis.

中文翻译：

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发现和优化的IRAK4抑制剂的有效和选择性吲唑胺系列。

IRAK4是先天免疫的关键介体。鉴定用于治疗炎性自身免疫疾病的新型IRAK4抑制剂引起了高度兴趣。我们在这里描述了一种高效的，选择性的IRAK4抑制剂（HS271），它表现出卓越的酶和细胞活性，以及​​出色的药代动力学特性。如在LPS诱导的TNFα产生胶原诱导的关节炎的大鼠模型中所评估的，HS271显示出强大的体内抗炎功效。