专利号:WO-2022256490-A9 优先权日:2021-06-03 标题:Improved synthesis of phosphoramidates for the treatment of hepatitis b virus 发明人:LOCKWOOD MARK 权利人:ANTIOS THERAPEUTICS INC 摘要:The synthesis of phosphoramidate prodrugs useful in the treatment of viral infections is disclosed. Specifically, an improved synthesis of phosphoramidate nucleotides useful in the treatment of Hepatitis B virus is disclosed.
专利号:US-12383499-B2 优先权日:2018-01-01 标题:Scale up synthesis of silicasome nanocarriers 发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG 权利人:UNIV CALIFORNIA 摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).
专利号:WO-2024201393-A1 优先权日:2023-03-29 标 题:Methods for the synthesis of nucleoside analogues and nucleosides analogues derived therefrom 发明人:BRITTON ROBERT; Muir Garrett; ANKETELL MATTHEW JAMES; HUXLEY COHAN; BAIKABI SUPING 权利人:UNIV FRASER SIMON 摘要:The present invention relates to methods for the synthesis of nucleoside analogues. More specifically, the present invention relates to methods for the synthesis of C4' substituted nucleoside analogues via the reaction of a soft nucleophile with a halohydrin ketone.
专利号:US-2015376219-A1 优先权日:2014-06-30 标题 :Selective Preparations of Purine Nucleosides and Nucleotides: Reagents and Methods 发明人:ZHONG MINGHONG 权利人:ZHONG MINGHONG 摘要:A process of regiospecific synthesis of N-9 purine nucleoside analogs in either solution or solid phase synthesis is described. The introduction of the sugar moiety or its analogue on to a 6-heteroarylium purine or its mesomeric betaine so that formation of only the N-9 position regioisomers of the purine nucleoside analogs (either D or L enantiomers) is obtained. This regiospecific introduction of the sugar moiety allows the synthesis of purine nucleoside analogs in high yields without formation of the N-7-positional regioisomers, while the 6-heteroaryliums are leaving groups facilitated for nucleophilic displacement. Solid supported 6-heterarylium purine bases can be used for purine based library synthesis and synthesis of nucleotide monophosphates and polyphosphates. Processes for providing novel 6-heteroarylium purines and their corresponding mesomeric betaines for the regiospecific synthesis of N-9 purine nucleoside analogs and nucleotides are described.
专利号:US-2023364078-A1 优先权日:2022-05-12 标题:Method of preparing nanoparticles comprising poorly water soluble drugs for treating hepatitis 发明人:KIM HYUN CHUL; MOON BYOUNG YONG 权利人:EVEX TECH INC 摘要:The present invention provides nanoparticles which contain a poorly water-soluble drug for treating hepatitis, and a method of producing the nanoparticles. More particularly, the present invention provides a method of producing nanoparticles for treating hepatitis, which includes: a first step of preparing a precursor mixture solution for synthesis of nanoparticles which include a drug for treating hepatitis; a second step of extracting the compound under supercritical or subcritical conditions; and a third step of dispersing the same, as well as the nanoparticles including a poorly water-soluble drug for treating hepatitis with improved bioavailability and without organic solvent residue.
专利号:US-10160779-B2 优先权日:2015-06-22 标 题 :Synthesis of phosphoramidates 发明人:SCHÖNE OLGA; WILHELM THORSTEN 权利人:SANDOZ AG 摘要:A process for preparing a compound of formula (I) or a salt thereof, the process comprising providing a compound of formula (III) wherein PG is an inert electron withdrawing hydroxyl protecting group, reacting the compound of formula (III) with a fluorinating agent, obtaining a compound of formula (II) and deprotecting the compound of formula (II).
1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548823/ doi: 10.2147/IDR.S171338. eCollection 2019. Review. 3: Sofosbuvir/velpatasvir/voxilaprevir for hepatitis C. Aust Prescr. 2019 Jun;42(3):108-109. doi: 10.18773/austprescr.2019.033. Epub 2019 Apr 24. Review. 4: Catalli L, Martens SK, Terrault NA, Reeves JD. Novel NS5B Resistance-Associated Substitution Emerges Under Failing Sofosbuvir/Ledipasvir Therapy. Clin Liver Dis (Hoboken). 2019 Mar 29;13(3):74-78. doi: 10.1002/cld.768. eCollection 2019 Mar. Review.
合成参考文献
摘要:European Medicines Agency (EMA), Committee for Medicinal Products for Human Use (CHMP), European Public Assessment Report (EPAR): Sovaldi; p.23 (November 21, 2013). Available from, as of March 17, 2015: 摘要:DHHS/FDA; Electronic Orange Book-Approved Drug Products with Therapeutic Equivalence Evaluations. Available from, as of March 6, 2015: 摘要:European Medicines Agency (EMA), Committee for Medicinal Products for Human Use (CHMP), European Public Assessment Report (EPAR): Sovaldi; p.21-2 (November 21, 2013). Available from, as of March 17, 2015: 摘要:American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 800 摘要:NIH; DailyMed. Current Medication Information for Sovaldi (Sofosbuvir) Tablet, Film Coated (Revised: November 2014). Available from, as of December 31, 2014: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm setid=80beab2c-396e-4a37-a4dc-40fdb62859cf