- A 1/10 water ribavirin compounds and pharmaceutical compositions thereof (by machine translation)
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The invention discloses a 1/10 water ribavirin compounds and pharmaceutical compositions thereof, per mole of ribavirin compounds containing 1/10 mole water. Its infrared spectrum in the wave number is 3451.8 ± 2 cm- 1 , 3347.5 ± 2 cm- 1 , 2857.1 ± 2 cm- 1 , 1663.3 ± 2 cm- 1 , 1502.8 ± 2 cm- 1 , 1438.4 ± 2 cm- 1 , 1336.8 ± 2 cm- 1 , 1281.8 ± 2 cm- 1 , 1070.3 ± 2 cm- 1 , 892.8 ± 2 cm- 1 , 773.3 ± 2 cm- 1 , 672.0 ± 2 cm- 1 There is a characteristic absorption peak. The invention through crystallization of the ribavirin impact factors study and research of different crystallization solvent system, to prepare high purity, good stability 1/10 water RBV compound, and by this invention stated 1/10 water RBV compound preparation has good stability of the pharmaceutical composition. (by machine translation)
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- Ribavirin compound containing one-twentieth water
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The invention discloses a ribavirin compound containing one-twentieth water. Each mole of the ribavirin compound contains one-twentieth mole of water. After a crude ribavirin product is dissolved in water, the temperature and pH of a solution are controlled, and crystallization is carried out in an acetonitrile aqueous solvent to obtain the ribavirin compound containing one-twentieth water. The prepared product has high purity and stability and a higher application value.
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Paragraph 0047; 0050; 0051
(2019/01/23)
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- Preparation of L-ribavirin (by machine translation)
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The invention provides a method for the preparation of ribavirin, to inosine as raw materials, after acetylation, condensation, aminolysis step to obtain the target product, the alkali in the acylation reaction of aluminum trichloride as a catalyst is conducted under the condition of, said condensation is in the NaI is conducted under the conditions of the catalyst, the aminolysis in methanol of existence of the sodium is conducted under the condition of. The method improves the acetylation efficiency, improves the yield of target product purity, shortens the reaction time, more easy to operate, is very suitable for industrial application. (by machine translation)
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Paragraph 0023; 0035
(2018/04/03)
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- Structural effects on the phosphorylation of 3-substituted 1-β-d-ribofuranosyl-1,2,4-triazoles by human adenosine kinase
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The conversion of ribavirin to the monophosphate by adenosine kinase is the rate-limiting step in activation of this broad spectrum antiviral drug. Variation of the 3-substituents in a series of bioisosteric and homologated 1-β-d-ribofuranosyl-1,2,4-triazoles has marked effects on activity with the human adenosine kinase, and analysis of computational descriptors and binding models offers insight for the design of novel substrates.
- Kumarapperuma, Sidath C.,Sun, Yanjie,Jeselnik, Marjan,Chung, Kiwon,Parker, William B.,Jonsson, Colleen B.,Arterburn, Jeffrey B.
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p. 3203 - 3207
(2008/02/03)
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- Synthesis of Azole Nucleoside 5′-Monophosphate Mimics (P1Ms) and Their Inhibitory Properties of IMP Dehydrogenases
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IMPDH inhibitors have potential antimicrobial, anticancer and immunomodulatory effects. Nucleoside inhibitors of IMPDH exert their inhibitory effects via nucleoside 5′-MPs. Conversion of nucleoside analogs to NMPs by cellular nucleoside kinases is not ass
- Wang, Guangyi,Sakthivel, Kandasamy,Rajappan, Vasanthakumar,Bruice, Thomas W.,Tucker, Kathleen,Fagan, Patrick,Brooks, Jennifer L.,Hurd, Tiffany,Leeds, Janet M.,Cook, P. Dan
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p. 317 - 337
(2007/10/03)
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- Process for the preparation of ribavirin
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A process for the preparation of ribavirin on an industrial scale is described which comprises the reaction of glycosylation of 3-substituted triazoles in the presence of a Lewis acid. Said process comprises:a) the reaction of a triazole of the formula with a protected ribofuranose of the formulab) the removal of the Pg groups and, optionally, the conversion into a carhoxyamide group of the R2 group of the compound obtained of the formula
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Page/Page column 6
(2008/06/13)
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- 1,2,4-Triazole nucleosides
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As antiviral agents and intermediates therefor, 3-substituted 1-(β-D-glycosyl)-1,2,4-triazoles, O-acylated analogs thereof, and 5'- and 3',5'-cyclic phosphates of the triazole nucleosides, "glycosyl" being .[.a pentofuranosyl moiety, preferably one whose 2'-oxygen is trans to the triazole aglycon, e.g., xylofuranosyl,.]. ribofuranosyl, .[.2-0-methylribofuranosyl, etc.,.]. the triazole aglycon being 3-substituted with cyano, methylcarboxylate, carboxamidoxime, carboxamido-, thiocarboxamido, or carboxamidine. Preparation of these nucleosides is by silylation of the substituted triazole followed by glycosylation with the appropriate blocked glycosyl halide. Alternatively, acid-catalyzed fusion of the requisite 1,2,4-triazole with an O-acylated pentofuranose yields the nucleosides.
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