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Compositions containing endocannabinoid mimetics and anti-inflammatory compounds, methods of preparation and uses thereof

A technology for endocannabinoids and analog compounds, which is applied in the directions of medical preparations containing active ingredients, drug combinations, active ingredients of hydroxyl compounds, etc.

Pending Publication Date: 2022-07-22
PHARMA COSMETIX RES LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although these compounds can be used to affect the endocannabinoid system, some cannabinoids can cause unwanted side effects such as dizziness, ecstasy, and addiction

Method used

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  • Compositions containing endocannabinoid mimetics and anti-inflammatory compounds, methods of preparation and uses thereof
  • Compositions containing endocannabinoid mimetics and anti-inflammatory compounds, methods of preparation and uses thereof
  • Compositions containing endocannabinoid mimetics and anti-inflammatory compounds, methods of preparation and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0218] Some compositions of the invention comprising ECS ​​direct, indirect, related inflammatory pathway and TRP related pathway compounds regulate multiple genes (eg CB1, CB2, FAAH, MAGL, IL1a) significantly better than cannabidiol in fibroblasts , NFKB, PRGS1, TRPM8 and TRPV1) beneficial gene expression (e.g. 54-fold better for CNR1, 33-fold better for CNR2, 15-fold better for MAGL, 10-fold better for TRPM8), indicating that the plants of the invention mimic non-cannabis Cannabinoid compounds favorably modulate ECS more effectively than traditional cannabinoids. See Test Example 1, Compositions 2 and 3.

[0219] In another embodiment, the composition comprises a combination of compounds designed for anti-inflammatory, anti-aging, skin matrix improvement and wound healing selected from direct and indirect endocannabinoid compounds from three Anti-inflammatory compounds for each of the ECS-related anti-inflammatory pathways (nuclear, enzymatic, and cytokines) and the ECS-rel...

Embodiment 3

[0227] Similarly, the compositions of the present invention are in keratinocytes in regulating various genes of skin matrix function, including those for lipid regulation / barrier repair (CERS3, FLG, TLR2), those for inflammatory responses (IL1a, NFKB, MMP1) and structural pathway genes affecting extracellular matrix protein metabolism and cell proliferation, differentiation and apoptosis (COL1A1, ITGB1, JUN, KLF4) regulate beneficial gene expression, superior to cannabidiol in CERS3 , COL1A1, FLG, IL1A, ITGB1, JUN & KLF4, which again demonstrate that the plant-mimetic non-cannabinoid compounds of the present invention are more potent and beneficial in modulating ECS ​​than conventional cannabinoids. See Test Example 3, Composition 8.

[0228]In one embodiment, the composition comprises at least one direct endocannabinoid mimetic compound, wherein the at least one compound is demethoxycurcumin, bisdesmethoxycurcumin, tetrahydroturmeric fenugreek, eugenol, or any combination th...

Embodiment 2

[0424] cell culture : Human skin keratinocyte cultures (or cultures) were obtained by ThermoFisher Scientific (Waltham, MA) or PromoCell GmbH (Heidelberg, Germany). The initial culture was selected from one of the following: C055C, 3C0647 or C12003. Cell lines were derived from the following donors, as follows:

[0425] C055C: Single Adult Donor

[0426] 3C0647: Single Adult Donor, Lightly Pigmented

[0427] C12003: Single Adult Donor

[0428] culture medium : Cells were ready for culture using keratinocyte growth medium from PromoCell GmbH (Heidelberg, Germany) supplemented with bovine pituitary extract 0.004ml / ml, epidermal growth factor (recombinant human) 0.125ng / ml , insulin (recombinant human) 5μg / ml, hydrocortisone 0.33μg / ml, epinephrine 0.39μg / ml, transferrin (recombinant human) 10μg / ml and CaCl 2 0.06mM basal medium. During the 24 hour experimental period, cells were maintained only in basal medium supplemented with test compounds. Store all cultures at 37 °...

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Abstract

Compositions comprising endocannabinoid mimetic compounds of direct, indirect, and related pathways and methods of using the same.

Description

[0001] CROSS-REFERENCE TO RELATED APPLICATIONS [0002] This application claims priority to US Application 62 / 902,291, filed September 18, 2019, which is incorporated herein by reference in its entirety. [0003] Field of Invention [0004] The present invention relates to cosmetic and pharmaceutical compositions intended for human or animal use. [0005] Background of the Invention [0006] The endocannabinoid system (ECS) is a complex biologically evolutionarily conserved homeostatic signaling network composed of receptors, ligands, enzymes, and transporters. Endocannabinoid ligands include endogenously produced lipids that activate two distinct "direct" endocannabinoid receptors, CB1 and CB2. Known examples of such lipid ligands include N-arachidonoylethanolamide [anandamide (AEA)] and 2-arachidonoylglycerol (2-AG). However, other lipids have indirect effects on the ECS system, such as N-palmitoylethanolamide and N-oleoylethanolamide, and other cannabinoid ligands exist, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/12A61K9/08A61K9/10A61P29/00A61P3/02A61Q19/00
CPCA61P29/00A61P3/02A61K9/0014A61Q19/08A61K8/31A61K8/347A61K8/42A61K8/35A61K8/9794A61K8/4973A61K8/9771A61K8/63A61K8/447A61P17/02A61K45/06A61K36/9066A61K31/12A61P17/00A61K31/05A61K31/085A61K31/122A61K31/16A61K31/192A61K31/201A61K31/365A61K36/185A61K36/53A61K36/54A61K36/61
Inventor 约瑟夫·A·刘易斯二世大卫·H·麦克丹尼尔拉维尼亚·波佩斯库
Owner PHARMA COSMETIX RES LLC
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