专利号:US-2025188022-A1 优先权日:2022-02-07 标 题 :Process for the preparation of nafamostat, camostat and their derivatives 发明人:AHMED RIYAZ; KUMAR GULSHAN; MAHAJAN SHEENA; Verma Praveen Kumar; CHAM PANKAJ SINGH; KUMAR AMIT; AHMED QAZI NAVEED; REDDY DUMBALA SRINIVASA; SHANKAR RAVI; SINGH PARVINDER PAL 权利人:COUNCIL SCIENT IND RES 摘要:The invention provides a novel, economical and practical route for the synthesis of an ester from acid and alcoholic functionalities using Trihalotriazine as coupling agent. Specifically, the invention provides a novel, economical and practical route for the preparation of Nafamostat and Camostat. Synthesis of p-guanidinobenzoic acid (Al) was also achieved from thiourea and p-aminobenzoic acid by using trihalotriazine as coupling reagent.
专利号:US-2024002405-A1 优先权日:2022-06-01 标题 :Antimicrobial compounds, synthesis methods, and uses thereof 发明人:VERMA RAJNI; DONAVALLI KRISHNA MOHAN; ZAID GENE H 权利人:ANKH LIFE SCIENCES LTD 摘要:Fused tricyclic compounds and novel methods of synthesizing, using, and/or administering the same. Methods of inhibiting microbial activity and/or treating a microbial infection with fused tricyclic compounds, bicyclic compounds, and other polycyclic compounds. The treatment of subjects suffering from a microbial infection comprises the step of administering to the subject one or more fused tricyclic compounds, bicyclic compounds, and other polycyclic compounds or a composition comprising one or more fused tricyclic compounds, bicyclic compounds, and other polycyclic compounds.
1: Hoffmann M, Hofmann-Winkler H, Smith JC, Krüger N, Sørensen LK, Søgaard OS, Hasselstrøm JB, Winkler M, Hempel T, Raich L, Olsson S, Yamazoe T, Yamatsuta K, Mizuno H, Ludwig S, Noé F, Sheltzer JM, Kjolby M, Pöhlmann S. Camostat mesylate inhibits SARS-CoV-2 activation by TMPRSS2-related proteases and its metabolite GBPA exerts antiviral activity. bioRxiv [Preprint]. 2020 Aug 5:2020.08.05.237651. doi: 10.1101/2020.08.05.237651. 2: Bittmann S, Weissenstein A, Villalon G, Moschuring-Alieva E, Luchter E. Simultaneous Treatment of COVID-19 With Serine Protease Inhibitor Camostat and/or Cathepsin L Inhibitor? J Clin Med Res. 2020 May;12(5):320-322. doi: 10.14740/jocmr4161. Epub 2020 May 8.
合成参考文献
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