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Electrophilically enhanced phenolic compounds for treating inflammatory related diseases and disorders

A compound and disease technology, applied to metabolic diseases, nervous system diseases, cardiovascular system diseases, etc.

Pending Publication Date: 2019-03-15
GLOBAL BIOLIFE INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Fewer units lead to lag effects

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  • Electrophilically enhanced phenolic compounds for treating inflammatory related diseases and disorders
  • Electrophilically enhanced phenolic compounds for treating inflammatory related diseases and disorders
  • Electrophilically enhanced phenolic compounds for treating inflammatory related diseases and disorders

Examples

Experimental program
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Embodiment 1

[0093] According to the present disclosure, one or more flavonoids, such as, for example, myricetin, are chlorinated. The compounds may be taken alone, or may be combined in a single dosage form, for example, as capsules, liquid solutions or suspensions, syrups, tablets, powders, and controlled release dosage forms.

[0094] In a preferred embodiment, 1 to 1000 mg of the chlorinated flavonoid is administered orally in capsule form.

Embodiment 2

[0096] Chlorinated flavonoids according to the present disclosure can be administered to various mammalian species in need of such treatment, such as domestic animals, horses, cows, sheep, pigs, dogs, cats, humans, and the like.

[0097] The following example is entitled "Non-GLP Assessment of Antiviral Activity of a Test Compound Against Rhinovirus 14".

[0098] The test product was prepared as follows: 0.312 g of the test product was dissolved in 10 mL of DMSO to obtain a test product at a concentration of 100 mM; in maintenance medium, a 1 / 1000 dilution of 100 μM test product was prepared to obtain a concentration of 100 uM; Gradation factor of , serial dilutions were performed in maintenance medium. The cytotoxicity of 1 / 1000 dilution of DMSO in culture medium was evaluated. A total of eight different concentrations of the test product were evaluated for their antiviral properties against rhinovirus type 14 strain 1059 (ATCC #VR-284). Post-infection and pre-infection ant...

Embodiment 3

[0142] Analysis of Equivir against influenza virus and dengue virus

[0143] The following examples and experiments have the following objectives:

[0144] In the CPE trial, the antiviral activity of Equivir was determined against three influenza A viruses:

[0145] —A / TX / 36 / 91(H1N1)

[0146] —A / Perth / 265 / 09 (H1N1) and

[0147] —A / HK / 1 / 68(H3N2);

[0148] Determination of cytotoxicity in day 7 MDCK cells;

[0149] Determining the antiviral activity of anti-DENV-2 New Guinea C in dendritic cells (yield reduction assay); and

[0150] Determine the cytokine profile (IFN-γ, IL-1β, IL-2, IL-4, IL-6, IL-8, IL-10, IL-12p70, IL-13 and TNF -α) (MSD).

[0151] Table 9: Potency Overview

[0152] EC50[μM]

[0153]

[0154] Data affecting viruses in MDCK cells.

[0155] Data related to influenza virus in MDCK cells are shown in Figure 4-8 middle.

[0156] CPE-based EC50 assay.

[0157] The following experiments were performed as follows:

[0158] Cells were seeded in 96-wel...

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Abstract

A therapeutic compound has a modified phenolic compound of the general formula (I) wherein at least one of R, R1, R2, R3, and R4 is an electrophilic group chosen fromhalogen, aldehyde, haloalkane, alkene, butyryl, flurophenol, sulfonamide, flurophenol sulfoxide and the remaining R, R1, R2, R3, and R4 is are each independently hydrogen, a hydroxyl group, an alkoxy group, a rutinosyl group, a carboxyl group, chromone, benzopyran, a rhamnosyl group, a substituted alkoxy group or a substituted acyloxy group wherein the substituent is chosen from hydroxyl, alkoxy, aryloxy, phenyl, halogen, and amido group. The compound can be used in a therapeutic treatment of inflammatory related diseases and condition.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of US Nonprovisional Patent Application Serial No. 15 / 156,021, filed May 16, 2016, which is incorporated herein by reference. technical field [0003] The present invention relates to electrophilic enhanced phenolic compounds, including but not limited to flavonoid compounds, and the use of these compounds in the treatment of various disorders, including those having an inflammatory association, including inflammatory-associated diseases and disorders. Background technique [0004] The metabolic and enzymatic systems of organisms have evolved to absorb phenolic compounds, phenolic acids, and flavonoids readily available in the environment from plant food sources into relevant biochemical pathways for each major metabolic system. Flavonoids not only have physiological effects on many metabolic systems, but they are an intrinsic part of the proper functioning of such systems. As part ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P31/14A61K38/21
CPCA61K31/352A61K31/7048A61K31/4525A61P31/12A61P31/16A61P31/04A61P3/00A61P9/00A61P25/00A61P29/00A61P35/00A61P3/10Y02A50/30A61K2300/00A61K9/00
Inventor D·L·汤姆森
Owner GLOBAL BIOLIFE INC
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