The development of HEC-866 and its analogues for the treatment of idiopathic pulmonary fibrosis,RSC Medicinal Chemistry

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The development of HEC-866 and its analogues for the treatment of idiopathic pulmonary fibrosis
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2021-6-2 , DOI: 10.1039/d1md00023c
Runfeng Lin ₁ , Zheng Zhang ₁ , Shengtian Cao ₁ , Wen Yang ₁ , Yinglin Zuo ₁ , Xinye Yang ₁ , Jiancun Zhang ₁ , Juan Xu ₁ , Jing Li ₁ , Xiaojun Wang ₁

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Idiopathic pulmonary fibrosis (IPF) is a chronic progressive lung disease with a typical survival time between three to five years. Two drugs, pirfenidone and nintedanib have been approved for the treatment of IPF, but they have limited efficacy. Thus, the development of new drugs to treat IPF is an urgent medical need. In this paper we report the discovery of a series of orally active pyrimidin-4(3H)-one analogs which exhibit potent activity in in vitro assays. Among them, HEC-866 showed promising efficacy in rat IPF models. Since HEC-866 also had good oral bioavailability, a long half-life and favorable long-term safety profiles, it was selected for further clinical evaluation.

中文翻译：

HEC-866及其类似物治疗特发性肺纤维化的进展

特发性肺纤维化 (IPF) 是一种慢性进行性肺病，典型的生存时间在三到五年之间。两种药物吡非尼酮和尼达尼布已被批准用于治疗 IPF，但疗效有限。因此，开发治疗IPF的新药是迫切的医疗需求。在本文中，我们报告了一系列口服活性 pyrimidin-4(3 H )-one 类似物的发现，这些类似物在体外试验中表现出有效的活性。其中，HEC-866 在大鼠 IPF 模型中显示出良好的疗效。由于 HEC-866 还具有良好的口服生物利用度、较长的半衰期和良好的长期安全性，因此被选中进行进一步的临床评估。

更新日期：2021-06-02

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