二氟氮杂环庚烷 HBV 衣壳组装调节剂。
Di-fluoro azepane HBV capsid assembly modulators.
机构信息
Janssen Research and Development, 1400 McKean Road, Spring House, PA 19477, United States.
Janssen Pharmaceutica, NV Turnhoutseweg 30, 2340 Beerse, Belgium.
出版信息
Bioorg Med Chem Lett. 2023 Aug 15;92:129350. doi: 10.1016/j.bmcl.2023.129350. Epub 2023 May 27.
The protein that forms the inner shell of the HBV virus, known as the capsid core protein, plays a crucial role in allowing chronic HBV infections to persist. Studies have shown that disrupting the assembly of the capsid can effectively combat the virus, and small molecule drugs that target the HBV capsid assembly modulator (CAM) process have been successful in clinical trials. Herein is described a distinct series of di-fluoro azepane CAMs with exceptional potency, pharmacokinetic, and solubility properties.
HBV 病毒内壳的形成蛋白，即衣壳核心蛋白，在允许慢性 HBV 感染持续存在方面起着关键作用。研究表明，破坏衣壳的组装可以有效地对抗病毒，并且针对 HBV 衣壳组装调节剂 (CAM) 过程的小分子药物在临床试验中已取得成功。本文描述了一系列具有卓越效力、药代动力学和溶解性特性的二氟氮杂环丁烷 CAM。
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