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-11858953-B2 优先权日:2018-04-04 标 题:Compositions and methods for synthesis of phosphorylated molecules 发明人:CHAPUT JOHN; LIAO JEN-YU; BALA SAIKAT 权利人:UNIV CALIFORNIA 摘要:The invention provides compositions and methods for synthesis of phosphorylated organic compounds, including nucleoside triphosphates.
专利号:US-9334273-B1 优先权日:2014-03-05 标题:Efficient and stereoselective synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) 发明人:CHU DAVID C K; SINGH UMA S 权利人:UNIV GEORGIA 摘要:The invention provides a new convergent approach for the synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) from a readily available starting material (Vince lactam) in fourteen steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, D -2′-fluoro-6′-methylene cyclopentanol by diazotization, elimination, stereoselective epoxidation, fluorination and oxidative reduction of the Vince lactam in twelve steps is also provided.
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-7125983-B2 优先权日:2000-11-29 标题:L-nucleic acid derivatives and process for the synthesis thereof 发明人:IIZUKA HAJIME; TOGASHI KAZUHIKO; SUZUKI TSUNEJI 权利人:MITSUI CHEMICALS INC 摘要:A novel method has been found to produce 2,2′-anhydro-1-(β-L-arabinofuranosyl)thymine as a novel useful intermediate compound. A novel method has been further found to produce thymidine from 2,2′-anhydro-1-(β-L-arabinofuranosyl)thymine. A novel method has been further found to L-2′-deoxyribose derivatives as a useful synthetic intermediate through L-2,2′-anhydro-5,6-dihydrocyclouridine derivative. According to these methods, synthesis of various L-nucleic acid derivatives, synthesis of which has been difficult till now.
专利号:EP-1543168-B1 优先权日:2002-09-27 标 题:Method for assaying replication of hbv and testing susceptibility to drugs 发明人:DURANTEL DAVID; DURANTEL SANDRA; TREPO CHRISTIAN; ZOULIM FABIEN 权利人:INST NAT SANTE RECH MED 摘要:Measuring the replication capacity of hepatitis B virus (HBV), e.g. HBV in a biological sample, possibly in the presence of a pharmaceutical product, and particularly an antiviral agent, is new. Measuring the replication capacity of hepatitis B virus (HBV), e.g. HBV present in a biological sample, possibly in the presence of a pharmaceutical product, particularly an antiviral agent, comprises: (a) optional extraction of nucleic acids contained in the sample; (b) PCR amplification of HBV nucleic acids using at least 2 primer pairs to obtain at least 2 amplified HBV genomic fragments representing more-than-full-length HBV genome; (c) cloning the fragments obtained into a vector; (d) transfecting or transducing susceptible cells with the vector; (e) culturing the transfected or transduced cells in conditions allowing synthesis of HBV pregenomic RNA (pgRNA) from the cloned HBV DNA; (f) optionally treating the cultured cells with a pharmaceutical product, particularly an antiviral agent; and (g) determining the replication capacity of the HBV, and the effect of any pharmaceutical product used on viral gene expression and/or viral replication. Independent claims are also included for: (1) a polynucleotide useful as primer for HBV amplification, comprising a sequence selected from 21 sequences of 23-42 bp (SEQ ID NO: 1-21) given in the specification; (2) a primer pair for HBV amplification comprising: (a) a forward primer comprising SEQ ID NO: 1-12, and/or a reverse primer comprising SEQ ID NO: 13 or SEQ ID NO: 14; (b) a forward primer comprising SEQ ID NO: 15 and/or 16 or 19, and a reverse primer comprising SEQ ID NO: 17 and/or SEQ ID NO: 18; (c) a forward primer comprising SEQ ID NO: 19, and a reverse primer comprising SEQ ID NO: 17 and/or SEQ ID NO: 18; or (d) a forward primer comprising SEQ ID NO: 20 or 22, and a reverse primer comprising SEQ ID NO: 21 or 23; (3) kits for HBV amplification, comprising a primer pair of (2); (4) a vector comprising a more-than-full length HBV genome as defined above, and a promoter modified in the 5' by the presence of a restriction site in the 5' of the +1 of transcription, where the +1 of transcription of the more-than-full length HBV genome and of the promoter are fused, and the promoter controls the synthesis of a pgRNA from the more-than-full length HBV genome post-cell-transfection; and (5) a baculovirus or cell line comprising the vector. ACTIVITY : Virucide. MECHANISM OF ACTION : None given.
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