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A technology of glycopeptides and mixtures, applied in the field of glycopeptides that increase lipid synthesis, can solve the problems of causing inflammatory response and being expensive
Pending Publication Date: 2022-04-12
TFCHEM
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However, the technique currently used is expensive, can cause an inflammatory response, and requires multiple redoing to achieve a satisfactory result
Method used
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[0171] The following abbreviations are used in the examples:
[0172] DCE: dichloroethane
[0173] DCM: dichloromethane
[0174] DIEA: N,N-Diisopropylethylamine
[0175] NMR: nuclear magnetic resonance
[0176] PTFE: Polytetrafluoroethylene
[0177] THF: Tetrahydrofuran
[0178] 1. Synthesis of compounds according to the invention
[0179] Compounds 1-3 were prepared as reported in WO2015 / 140178, in the form of their hydrochloride salts. The base form was obtained according to the following scheme:
[0180] Will IRA-67 (pre-washed with water, 17.0g) was added Hydrochloride (12.3mmol, 1eq) in water (325mL). The solution was stirred at room temperature for 1 hour and 30 minutes. The pH of the solution was measured (pH=7.0) and the mixture was filtered (0.2 μm, HPTFE). The filtrate was then lyophilized to give compound 1-3 base form .
[0181] according to Image 6 The synthetic scheme shown produced compounds 4-5. The synthetic scheme is detailed as follows:
[...
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Abstract
The present invention relates to glycopeptides of the following formula I: or a tautomer, stereoisomer or a mixture of stereoisomers in any proportion, in particular a mixture of enantiomers, in particular a racemic mixture, and / or a physiologically acceptable salt and / or solvate thereof, where:-n represents an integer from 1 to 6,-m represents 0 or 1,-p represents 0 or 1,-R represents H, F, CH3, CH2F or CH2OH, and / or a pharmaceutically acceptable salt and / or solvate thereof. -R1, R2, and R3 independently of each other represent H, F, or OH,-R4 represents hydrogen, halogen, or OH,-R6 and R7 independently of each other represent hydrogen, (C1-C6) alkyl, aryl, or aryl-(C1-C6) alkyl, and-R8 represents H or CO-(C1-C20) alkyl, used for plumping and / or plumping and / or densifying and / or filling wrinkles and / or moisturizing and / or restoring lipids of skin or hair and / or stimulating hair growth and / or for treating skin dryness and / or atopic dermatitis and / or atopic eczema and / or scurf due to its ability to increase lipid synthesis diseases.
Description
technical field [0001] The present invention relates to the use of glycopeptide derivatives for cosmetic or dermatological applications, in particular for plumping ( ) and / or plumping and / or densifying the skin, and / or filling wrinkles and / or making the skin or hair moisturizing and / or lipid restoration of the skin or hair and / or stimulation of hair growth and / or for the treatment of dry skin and / or atopic dermatitis and / or eczema and / or psoriasis. Background technique [0002] Loss of skin elasticity and degeneration of fatty tissue with aging has undesired and pronounced effects on the body (hands, feet, buttocks, breasts, face) and especially on the face: appearance of fine lines and wrinkles, loss of skin volume around the eyes and sunken cheeks. To reshape the body, fill expression lines and wrinkles, and plump the skin, surgical fat injection (fat grafting or lipofilling) has been developed, which consists in reinjecting fat removed from fat-rich areas of the body, R...
Claims
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