- PROMOIETY STRATEGY TO ENHANCE DRUG ACTIVITY
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Various nucleoside phosphate and phosphonate analogues are provided for treatment of viral infections. Methods of preparing the analogues, pharmaceutical compositions containing the analogues, and methods of using the analogues as antiviral compounds, especially against adenoviruses, coronaviruses, and varicella zoster viruses, are also provided.
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Paragraph 0045
(2022/03/02)
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- FATTY ACYL AND FATTY ETHER CONJUGATES OF REMDESIVIR AND ITS ACTIVE METABOLITES AS ANTIVIRALS
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Antiviral compounds, pharmaceutical compositions containing the same, and methods of treating viral infections or medical disorders resulting from viral infections are disclosed.
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- METHODS OF PREPARING 1'-CYANO NUCLEOSIDES
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The present disclosure generally describes methods of preparing l'-cyano nucleosides, such as a compound of Formula (I). For example, the compound of Formula (I) can be prepared from a compound of Formula (Il-a) in a flow reactor.
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- N-protected heterocyclic compound, preparation method thereof and method for preparing C-nucleoside derivative by using N-protected heterocyclic compound
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The invention provides an N-protected heterocyclic compound, a preparation method thereof and a method for preparing a C-nucleoside derivative by using the N-protected heterocyclic compound. Specifically, the invention provides a method for preparing the C-nucleoside derivative by using a heterocyclic compound protected by N-carbobenzoxy or N-tert-butyloxycarboryl. According to the method, halogenation is not needed, temporary amino protection is not needed, protons of the heterocyclic compound are removed by directly using an organic lithium or organic magnesium compound, and addition with ribose lactone is carried out. According to the method, the synthesis route of the C-nucleoside derivative is shortened, and the yield of the reaction of the heterocyclic compound and the ribose lactone is remarkably improved under the condition that no halogen atom is used as a substituent group.
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- ISOMORPHS OF REMDESIVIR AND METHODS FOR SYNTHESIS OF SAME
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A new isoform of 2-ethylbutyl (2S)-2-[[[(2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3/4-dihydroxyoxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate (Remdesivir) having increased water solubility is disclosed, along with methods
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Paragraph 0086
(2021/06/04)
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- Method for preparing retegravir by using micro-channel reactor
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The invention discloses a method for synthesizing retegravir by using a micro-channel reactor, which realizes continuous flow synthesis of retegravir by using a scale effect of a micro-flow field technology and using a novel micro-channel reactor to repla
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- Crystal form of nucleoside compound and preparation method thereof
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The invention provides a crystal form of a nucleoside compound and a preparation method thereof, wherein the crystal form comprises a crystal form I. Crystal form . The crystal form is small in particle size, high in crystallinity and good in physical and chemical stability. The preparation method of the crystal form is simple to operate and high in repeatability.
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Paragraph 0082
(2021/11/27)
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- Nucleoside compound for treating virus infection and application thereof
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The invention discloses a nucleoside compound for treating coronavirus infection and a prodrug thereof, a compound shown in a formula I, the prodrug and/or pharmaceutically acceptable salt thereof, and a composition and application thereof. The compound and the composition have the application of preventing, relieving or treating coronavirus infection, or replication or reproduction of homologous variant viruses of the coronavirus infection, and cytopathic effects generated by the coronavirus infection or the replication or reproduction of the homologous variant viruses of the coronavirus infection.
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Paragraph 0172-0175
(2021/12/07)
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- Method for preparing Remdesivir key intermediate by using novel micro-channel reactor
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The invention discloses a method for preparing a Remdesivir key intermediate by using a novel micro-channel reactor, which comprises the steps of simultaneously pumping a material I and a material IIinto the micro-channel reactor, conveying into a reaction module, reacting, collecting the reaction solution flowing out of the outlet of the micro-channel reactor, and carrying out after-treatment toobtain (3aR,4R,6R,6aR)-4-(4-aminopyrrolo[2, 1-f][1,2,3]triazine-7-yl)-6-(hydroxymethyl)-2,2-dimethyl tetrahydrofuran[3,4-d] dioxazole-4-nitrile. The micro-channel reactor provided by the invention has the characteristics of low price, convenience in transportation and cleaning, high mass and heat transfer efficiency, easiness in industrial amplification and the like. The micro-channel reaction technology adopted by the invention can effectively shorten the reaction time, save the cost, can continuously produce the target product with stable quality, and is suitable for preparing the Remdesivir intermediate.
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Paragraph 0037-0086
(2021/01/29)
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- Preparation method of high-purity Remdesivir
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The invention belongs to the field of medicinal chemistry, and particularly relates to a preparation method of a compound Remdesivir as shown in a formula I defined in the description. The method is simple and convenient to operate, mild in reaction condi
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Paragraph 0031-0035
(2021/06/23)
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- Application of nucleoside analogue or combined preparation containing nucleoside analogue in virus resistance
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The invention relates to an application of nucleoside analogs in virus resistance. Specifically, the invention relates to the use of nucleoside analogs and pharmaceutical compositions thereof as (a) inhibitors for inhibiting the replication of coronavirus, influenza virus, respiratory syncytial virus, flaviviridae virus, filoviridae virus and/or porcine epidemic diarrhea virus (PEDV); and/or (b) medicines for treating and/or preventing and relieving related diseases caused by infection of coronavirus, influenza virus, respiratory syncytial virus, flaviviridae virus, filoviridae virus and/or porcine epidemic diarrhea virus (PEDV). The nucleoside analogue disclosed by the invention can be used for treating and/or preventing and relieving related diseases such as respiratory tract infection, pneumonia (COVID-19) and the like caused by 2019 novel coronavirus infection.
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Paragraph 0315-0318
(2021/05/12)
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- Novel method for recovering nucleoside phosphoramidate medicine mother liquor
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The invention relates to a novel method for recovering nucleoside phosphoramidate medicine mother liquor, and belongs to the field of chemical synthesis. The method comprises the following steps: carrying out hydrolysis reaction on nucleoside phosphoramidate drug mother liquor in the presence of an alkaline reagent, and then standing for layering to respectively obtain an organic phase and a waterphase; concentrating the obtained organic phase under reduced pressure, recovering pyrrolizine compounds, adding an acidic reagent into the water phase to react to obtain a mixed solution containingpentafluorophenol, phenol and L-alanine, extracting the mixed solution by adopting an organic solvent, and finally respectively recovering pentafluorophenol, phenol and L-alanine by adopting a distillation mode. The scheme is of great significance to the recycling of the mother liquor in the industry.
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Paragraph 0030; 0042-0047
(2020/07/02)
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- METHODS FOR TREATING ARENAVIRIDAE AND CORONAVIRIDAE VIRUS INFECTIONS
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Provided are methods for treating Arenaviridae and Coronaviridae virus infections by administering nucleosides and prodrugs thereof, of Formula I: wherein the 1′ position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Lassa virus and Junin virus infections.
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- METHODS FOR TREATING FLAVIVIRIDAE VIRUS INFECTIONS
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Provided are methods for treating Flaviviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I:, wherein the 1' position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Zika virus infections.
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Paragraph 0261
(2017/11/15)
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- METHODS FOR TREATING FILOVIRIDAE VIRUS INFECTIONS
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Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae vims infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula (IV): The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
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