Isavuconazole Hydrobromide置于碳酸氢钠体系中,用 二氯甲烷,水 用作溶剂,以18.5 G的收率获得艾沙康唑 参考文献: Novel Stable Polymorphs Of Isavuconazole Or Its Salt Thereof[fr] Nouveaux Polymorphes Stables D'Isavuconazole Ou De Son Sel 标题: Novel Stable Polymorphs Of Isavuconazole Or Its Salt Thereof[fr] Nouveaux Polymorphes Stables D'Isavuconazole Ou De Son Sel 摘要:本发明涉及伊沙庫唑或其盐的新型稳定多晶形态,通过HPLC测量时纯度超过90%.具体来说,本发明涉及制备伊沙庫唑基固体非晶态和结晶形式的方法.在另一实施方式中,本发明涉及伊沙庫唑盐的结晶形式,以及2-(2,5-二氟苯基)-1-[1,2,4]三唑-1-基丁烷-2,3-二醇的盐.
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:US-2024336559-A1 优先权日:2021-10-06 标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids 发明人:OJIMA IWAO; HARANAHALLI KRUPANANDAN; DEL POETA MAURIZIO; GARG ASHNA 权利人:UNIV NEW YORK STATE RES FOUND 摘要:The present invention provides a compound having the structure: n n n n n n n n n n n n wherein n R 3 , R 4 , R 5 , R 6 , and R 7 are each independently, H, halogen, CN, —CF 3 , —OCF 3 , —NO 2 , alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycle, —OH, —OAc, —OR 13 , —COR 13 , —CH 2 OR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ; n R 9 , R 10 , R 11 , and R 12 are each independently, H, CN, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, —OAc, —COR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ;n wherein each occurrence of R 13 is independently alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 14 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 15 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, n n wherein when R 14 is methyl, R 15 is not methyl; n wherein at least one of R 9 , R 10 , R 11 , and R 12 is not H; n wherein at least one of R 3 , R 4 , R 5 , R 6 , and R 7 is not H.
专利号:US-10443047-B2 优先权日:2014-05-01 标题 :Increasing cellular lipid production by increasing the activity of diacylglycerol acyltransferase and decreasing the activity of triacylglycerol lipase 发明人:TSAKRAKLIDES VASILIKI; BREVNOVA ELENA E 权利人:NOVOGY INC 摘要:Disclosed are methods and compositions for increasing the triacylglycerol content of a cell by up-regulating diacylglycerol acyltransferase and down-regulating triacylglycerol lipase. In some embodiments, a DGA1 protein is expressed and a native TGL3 gene is knocked out, thereby increasing the synthesis of triacylglycerol and decreasing its consumption, respectively.
专利号:US-12325678-B2 优先权日:2017-06-16 标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids 发明人:OJIMA IWAO; DEL POETA MAURIZIO; LAZZARINI CRISTINA; HARANAHALLI KRUPANANDAN; SUN YI 权利人:UNIV NEW YORK STATE RES FOUND 摘要:The present invention provides a compound having the structure: n nand use of the compound for inhibiting the growth of or killing.
专利号:US-2023364251-A1 优先权日:2020-08-06 标 题:Methods for the synthesis of protein-drug conjugates 发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL 权利人:CIDARA THERAPEUTICS INC 摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.
专利号:US-9051282-B2 优先权日:2011-12-16 标 题:Methods for triazole synthesis 发明人:HENDERSON WILLIAM H; RICHARDSON JOHN 权利人:CHEMTREAT INC 摘要:Disclosed are methods of synthesizing triazoles that avoids the use of concentrated acids in favor of carbonic acid generated from CO 2 that can be practiced at ambient and/or elevated temperature and/or atmospheric and/or elevated pressures. The disclosed methods also provide a way of synthesizing triazole products that are sufficiently pure and/or of sufficient concentration whereby the reaction product(s) may not require purification or other treatment before being used in, for example, formulating water treatment compositions that will tend to suppress corrosion or as an intermediate product in a more complex synthesis.
1: Regella VRPS, Subramanian VC, Bhetanabhotla SS. Identification and structural characterization of four novel degradation products and a process impurity of isavuconazonium sulfate for injection formulation bulk by LC-ESI-QTOF-MS/MS. Eur J Mass Spectrom (Chichester). 2019 Nov 10:1469066719884402. doi: 10.1177/1469066719884402. [Epub ahead of print] Available from http://www.ncbi.nlm.nih.gov/books/NBK548643/ doi: 10.1186/s12941-019-0311-3. 4: Adamsick ML, Elshaboury RH, Gift T, Mansour MK, Kotton CN, Gandhi RG. Therapeutic drug concentrations of isavuconazole following the administration of isavuconazonium sulfate capsules via gastro-jejunum tube: A case report. Transpl Infect Dis. 2019 Apr;21(2):e13048. doi: 10.1111/tid.13048. Epub 2019 Jan 29. doi: 10.1016/j.diagmicrobio.2018.04.005. Epub 2018 Apr 13. pii: e01292-17. doi: 10.1128/AAC.01292-17. Print 2017 Dec.
合成参考文献
参考文献:10.2147/clep.s12502 摘要:Kriengkauykiat J, Ito JI, Dadwal SS. Epidemiology and treatment approaches in management of invasive fungal infections. Clin Epidemiol. 2011;3():175–91.