专利号:US-8785629-B2 优先权日:2009-06-18 标题 :Phosphonates synthons for the synthesis of phosphonates derivatives showing better bioavailability 发明人:AGROFOGLIO LUIGI A; ROY VINCENT; PRADERE UGO 权利人:AGROFOGLIO LUIGI A; ROY VINCENT; PRADERE UGO; CENTRE NAT RECH SCIENT; UNIV ORLEANS 摘要:Synthons for the synthesis of phosphonates prodrugs POM and POC, especially for direct Cross Metathesis.
专利号:US-10155007-B2 优先权日:2014-10-29 标 题:Synthesis method for improved tenofovir disoproxil fumarate using ion-exchange resin and method for preparing oral dissolving film form using the same 发明人:KIM DONG-JIN; KOO CHANG-HUI; CHO IL-HEE; LEE SUNG-BAE; HAN DONG-HOON 权利人:FIRSON 摘要:The present invention relates to a synthesis method of preventing the formation of impurities and byproducts in the synthesis of tenofovir disoproxil fumarate (Teno-DF) used as a medicine for hepatitis B and HIV treatment due to its function to promote bioactivities. In the synthesis method of the present invention, an ion-exchange resin (Dowex 50W hydrogen form, sulfonic acidic cation exchange resin) is used to enhance the yield and purity of the compound. The present invention also relates to a method of preparing an oral dissolving film dosage form in the manufacture of a medicine using the tenofovir compound with high purity obtained by the synthesis method of the present invention as an effective ingredient.
专利号:US-9605019-B2 优先权日:2011-07-19 标 题:Methods for the synthesis of functionalized nucleic acids 发明人:VERDINE GREGORY L; MEENA; IWAMOTO NAOKI; BUTLER DAVID CHARLES DONNELL 权利人:VERDINE GREGORY L; MEENA; IWAMOTO NAOKI; BUTLER DAVID CHARLES DONNELL; WAVE LIFE SCIENCES LTD 摘要:The present application, among other things, provides technologies, e.g., reagents, methods, etc. for preparing oligonucleotides comprising phosphorothiotriesters linkages, e.g., oligonucleotides having the structure of IIIa, IIIb or IIIc. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ia or Ib with a silylating reagent to provide a silyloxyphosphonate, and reacting the silyloxyphosphonate with a thiosulfonate reagent of structure IIa or IIb to provide an oligonucleotide of structure IIIa or IIIb. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ic with a silylating reagent to provide a silyloxyphosphonate, reacting the silyloxyphosphonate with a bis(thiosulfonate) reagent of structure IVc to provide a phosphorothiotriester comprising a thiosulfonate group of structure Vc, and then reacting the phosphorothiotriester comprising a thiosulfonate group of structure Vc with a nucleophile of structure VIc to provide an oligonucleotide of structure IIIc.
专利号:US-2018222936-A1 优先权日:2011-07-19 标 题:Methods for the synthesis of functionalized nucleic acids
专利号:US-9907796-B2 优先权日:2012-10-04 标题:Methods of treating tumoral diseases, or bacterial or viral infections 发明人:DEOKAR RHUSHIKESH CHANDRABHAN; DUGAR SUNDEEP; MAHAJAN DINESH; WERNER MILTON HENRY 权利人:DEOKAR RHUSHIKESH CHANDRABHAN; DUGAR SUNDEEP; MAHAJAN DINESH; WERNER MILTON HENRY; INHIBIKASE THERAPEUTICS INC 摘要:Novel compounds and their synthesis are described. Methods for using these compounds in the prevention or treatment of cancer, a bacterial infection or a viral infection in a subject are also described.
专利号:US-9359376-B2 优先权日:2011-04-08 标题:Substituted methylformyl reagents and method of using same to modify physicochemical and/or pharmacokinetic properties of compounds 发明人:DUGAR SUNDEEP; MAHAJAN DINESH; HOLLINGER FRANK PETER 权利人:DUGAR SUNDEEP; MAHAJAN DINESH; HOLLINGER FRANK PETER; SPHAERA PHARMA PTE LTD 摘要:The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.