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4 '-halogen-containing nucleotide and nucleoside therapeutic compositions and uses related thereto

A composition and compound technology, applied in the directions of medical preparations containing active ingredients, applications, sugar derivatives, etc.

Pending Publication Date: 2022-08-05
EMORY UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are serious concerns about the use of aerosol-delivered virulent strains of the VEE virus as bioweapons against warfighters

Method used

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  • 4 '-halogen-containing nucleotide and nucleoside therapeutic compositions and uses related thereto
  • 4 '-halogen-containing nucleotide and nucleoside therapeutic compositions and uses related thereto
  • 4 '-halogen-containing nucleotide and nucleoside therapeutic compositions and uses related thereto

Examples

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example 1

[1894] Conjugated preparation

[1895] Monophosphate and diphosphate prodrugs have been prepared by several groups. See Jessen et al, "Bioreversible Protection of Nucleoside Diphosphates", Angewandte Chemie-International Edition English 2008, 47(45), 8719-8722, vol. The aforementioned references are hereby incorporated by reference. To prevent cleavage of the P-O-P anhydride bond, a rapidly cleaving side group (eg, bis-(4-acyloxybenzyl)-nucleoside diphosphate (BAB-NDP), which is deacylated by endogenous esterases) A negative charge is created on the diphosphate. See also Routledge et al, "Synthesis, Bioactivation and Anti-HIV Activity of 4-Acyloxybenzyl- bis(nucleosid-5'-yl) Phosphates)", "Nucleosides & Nucleotides" 1995, 14(7), 1545-1558 and Meier et al., "2',3'-dideoxy-2 Comparative study of bis(benzyl)phosphate triesters of ',3'-didehydrothymidine (d4T) and cycloSal-d4TMP--hydrolysis, mechanistic insights and anti-HIV activity (Comparative study of bis(benzyl)phosphate ...

example 2

[1899] General procedure for base coupling

[1900] The persilylation was prepared in a round bottom flask containing dry nucleobase (15.5 mmol), chlorotrimethylsilane (12.21 mmol) and bis(trimethylsilyl)amine (222 mmol) under nitrogen nucleobase. The mixture was refluxed overnight (16 hours) with stirring until all solids had dissolved. The mixture was cooled to room temperature and volatiles were removed by rotary evaporation followed by high vacuum to give the persilylated nucleobase. This compound was used immediately in the next step.

[1901] The freshly prepared persilylated nucleobase (15.50 mmol) was dissolved in 1,2-dichloroethane (50 mL) or chlorobenzene (50 mL) with stirring at room temperature under nitrogen. A solution of β-D-ribofuranose 1,2,3,5-tetraacetate (7.75 mmol) in 1,2-dichloroethane (50 mL) or chlorobenzene (50 mL) was added all in one portion to the into the stirred mixture.

[1902] To this mixture was added SnCl dropwise via syringe 4 (11.63 mm...

example 3

[1904] General Cytosine Analog Conjugation

[1905] in N 2 down, when fitted with N 4 - Bis(trimethylsilyl)amine (8.45 mmol) and ammonium sulfate (0.02 mmol) were added to a flask of benzoyl-protected cytosine analog (0.793 mmol). The flask was heated at reflux for 2 hours, and after cooling to room temperature, the solvent was removed in vacuo and further dried under high vacuum for 1 hour. The residue was dissolved in dry chlorobenzene (10 ml) and β-D- or β-L-ribofuranose 1,2,3,5-tetraacetate (0.53 mmol) was added. Then, SnCl was added dropwise 4 (0.27ml, 2.3mmol). After stirring at room temperature for 1 hour, it was heated to 60°C overnight. After cooling to 0°C, solid sodium bicarbonate (0.85 g) was added followed by EtOAc (5 mL). It was allowed to stir for 15 minutes, and then water (0.5 mL) was added slowly. The insoluble material was filtered off and washed with more EtOAc (2.5 mL). The filtrate was washed once with water, once with brine, and dried (Na 2 SO ...

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Abstract

Halogen-containing nucleotide and nucleoside therapeutic compositions and related uses thereof are disclosed. In certain embodiments, the disclosure relates to the treatment or prevention of viral infections. Such viral infections may comprise a tapiviridae, a bunyaviridae, an arenaviridae, a coronaviridae, a flaviviridae, a picornaviridae, eastern equine encephalitis, western equine encephalitis, and Venezuela equine encephalitis (EEE, WEE, and VEE, respectively), Chikungunya fever (CHIK), Ebola, influenza, RSV, and Zika viral infections.

Description

[0001] CROSS-REFERENCE TO RELATED APPLICATIONS [0002] This application claims the benefit of priority from US Provisional Application No. 62 / 912,165, filed October 8, 2019, which is incorporated herein by reference in its entirety. [0003] Statement of Government Support [0004] This invention was made with government support under Contract Nos. HDTRA1-13-C-0072 and HDTRA1-15-C-0075 awarded by the Department of Defense (DTRA) and Grant No. HHSN272201500008C awarded by the National Institutes of Health carried out below. The government has certain rights in this invention. technical field [0005] The present disclosure relates to halogen-containing nucleotide and nucleoside therapeutic compositions and related uses thereof. In certain embodiments, the present disclosure relates to the treatment or prevention of viral infections, such as togaviridae, bunyaviridae, arenaviridae, coronaviridae, flaviviridae, picornaviruses family (picornaviridae), Eastern Equine Enceph...

Claims

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Application Information

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IPC IPC(8): A01N43/04A61K31/495A61K31/706A61P31/12
CPCC07H19/06C07H19/067A61K31/7068Y02A50/30A61K31/7072A61P31/14A61P31/12A61K45/06
Inventor 乔治·R·佩因特大卫·佩里曼格雷戈里·R·布鲁姆林
Owner EMORY UNIVERSITY
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