Chia C S Brian, See Yi Yang
Experimental Drug Development Centre, 10 Biopolis Road, Chromos #08-01, Singapore 138670, Singapore.
ACS Med Chem Lett. 2022 May 27;13(6):875-876. doi: 10.1021/acsmedchemlett.2c00136. eCollection 2022 Jun 9.
COVID-19 is a highly infectious disease caused by the SARS-CoV-2 coronavirus. It rapidly escalated into a global pandemic, causing more than 6 million fatalities by March 2022, a little over 2 years since its emergence in December 2019. The first peptidomimetic coronavirus main protease inhibitor, nirmatrelvir, was granted Emergency Use Authorization by the U.S. FDA on Dec 22, 2021. Less than a month after its patent application, Hoffmann La-Roche scientists filed a patent application describing azadipeptide peptidomimetic inhibitors (WO 2022/043374 A1). This patent highlight reveals the structure-activity relationship of key azadipeptide inhibitors described in the patent.
新冠病毒病（COVID-19）是一种由严重急性呼吸综合征冠状病毒2（SARS-CoV-2）引起的高传染性疾病。它迅速升级为全球大流行，自2019年12月出现至2022年3月，已造成600多万人死亡，时间跨度略超两年。首个拟肽类冠状病毒主蛋白酶抑制剂奈玛特韦于2021年12月22日获得美国食品药品监督管理局（FDA）的紧急使用授权。在其专利申请不到一个月后，罗氏公司的科学家提交了一份描述氮杂二肽拟肽抑制剂的专利申请（WO 2022/043374 A1）。本专利亮点揭示了该专利中所述关键氮杂二肽抑制剂的构效关系。
