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WO2024056566A1 - Utilisation d'une composition de thioéthylamine pour le rajeunissement de la peau et effet synergique amélioré lorsqu' elle est combinée à un acide organique et/ou à de l'azabenzène-4-carboxamide - Google Patents

Utilisation d'une composition de thioéthylamine pour le rajeunissement de la peau et effet synergique amélioré lorsqu' elle est combinée à un acide organique et/ou à de l'azabenzène-4-carboxamide Download PDF

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Publication number
WO2024056566A1
WO2024056566A1 PCT/EP2023/074830 EP2023074830W WO2024056566A1 WO 2024056566 A1 WO2024056566 A1 WO 2024056566A1 EP 2023074830 W EP2023074830 W EP 2023074830W WO 2024056566 A1 WO2024056566 A1 WO 2024056566A1
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Prior art keywords
acid
skin
composition
group
azabenzene
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English (en)
Inventor
Behrooz Kasraee
Laure DIRLEWANGER
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/08—Anti-ageing preparations
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/46—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
    • A61K8/4926—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having six membered rings

Definitions

  • the present invention relates to a cosmetic use of a composition comprising thioethylamine along with azabenzene-4-carboxamide and/or an organic acid for skin rejuvenation.
  • the skin is the largest organ in humans and is subject to intrinsic aging and extrinsic aging.
  • Skin aging is a complex biological process influenced by combination of endogenous and exogenous factors.
  • the endogenous factors are typically genetics, cellular metabolism, hormone and metabolic processes, whereas the exogenous factors are typically chronic light exposure, pollution, ionizing radiation, chemicals, toxins.
  • These endogenous and exogenous factors lead to changes in the skin and to the appearance of imperfections therein, such as loss of firmness, wrinkling, roughness and/or sagginess.
  • human skin is often subjected to harsh external conditions, such as excessive sun exposure and general environmental exposures, which over time lead to the anatomic degradation of human skin.
  • GAGs Three primary structural components of the dermis are collagen, elastin and Glycosaminoglycans (GAGs), which have been the subjects of the majority of anti -aging research and efforts for aesthetic-anti-aging strategies pertaining to the skin, which range from “anti-wrinkle creams” to various filling agents.
  • Many of these early treatment methodologies involved the oral administration of vitamin A in the form of the ester of vitamin A, vitamin A palmitate. This approach changed over time to focus on the topical application of vitamin A in its acid form (retinoic acid), which in early reports suggested that vitamin A could potentially retard the effects of aging on the skin.
  • Vitamins have also been used, alone or in combinations, to prevent or reverse skin damage and/or improve the quality of skin in individuals, and in particular, skin damage associated with inflammation due to UV radiation.
  • U.S. Pat. Nos. 5,574,063, 5,545,398, 5,409,693, and 5,376,361 describe the use of fatty acid esters of ascorbic acid (e.g., vitamin C palmitate) or tocotrienol (vitamin E) for the treatment and prevention of skin damage from sun exposure.
  • Hyaluronic acid due to its viscoelastic properties and its capacity to retain water, has also been used in the cosmetic industry to keep skin hydrated, maintain elasticity and treat wrinkles by improving the roughness or even used as a dermal filler.
  • hyaluronic acid is obtained from several sources, such as rooster combs or bacterial extracts and, consequently, these products can contain impurities and need to be characterized thoroughly.
  • desired effects on skin roughness or anti-wrinkle effects appear only after several weeks of treatment (Farwick et al, SOFW Journal, 134(11), 17, 2008; Poetschke et al., MMW Fortschr. Med. 158 (Suppl. 4) (2016 May 25) 1-6).
  • An aspect of the present invention provides a cosmetic method of skin rejuvenation, wherein the method comprises topically applying to an area of the skin of a subject in need thereof a composition comprising
  • an organic acid wherein the organic acid is selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof.
  • Another aspect of the present invention provides a cosmetic method of skin rejuvenation comprising the steps of a) topically applying to an area of the skin of a subject in need thereof a first composition comprising
  • an organic acid wherein the organic acid is selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof
  • a second composition comprising 0.01% to 30% w/w of an azabenzene-4-carboxamide or a salt thereof, c) repeating the steps a) and b) to obtain skin rejuvenation effects.
  • a further aspect of the present invention provides a cosmetic method of skin rejuvenation comprising the steps of a) topically applying to an area of the skin of a subject in need thereof a first composition comprising 0.01% to 30% w/w of thioethylamine, b) topically applying to said area of the skin a second composition comprising 0.01% to 30% w/w of an azabenzene-4-carboxamide or a salt thereof, and 0.1% to 50% w/w of an organic acid, wherein the organic acid is selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof, c) repeating the steps a) and b) to obtain skin rejuvenation effects.
  • a further aspect of the present invention provides a cosmetic combination product comprising a first composition and a second composition for separate topical application, wherein
  • the first composition comprising o 0.01% to 30% w/w of thioethylamine, and o 0.1% to 50% w/w of an organic acid, wherein the organic acid is selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof, and
  • the second composition comprising o 0.01% to 30% w/w of azabenzene-4-carboxamide or a salt thereof.
  • a further aspect of the present invention provides a cosmetic combination product comprising a first composition and a second composition for separate topical application, wherein
  • the first composition comprising o 0.01% to 30% w/w of thioethylamine
  • the second composition comprising o 0.01% to 30% w/w of azabenzene-4-carboxamide or a salt thereof, and o 0.1% to 50% w/w of an organic acid, wherein the organic acid is selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof.
  • the term “at least one” means “one or more” and also encompasses the terms “at least two”, “at least three”, “at least four”, etc.
  • compositions or components thereof so described are suitable for use in contact with skin of a mammal, preferably of human, without undue toxicity, incompatibility, instability, irritability, allergic response, and the like.
  • cosmetic As used herein, the term “cosmetic”, “cosmetic management” or “cosmetic treatment” is non- therapeutic treatment of skin conditions that are not diseases or pathological states.
  • topical refers to the application of the composition of the present invention onto the surface or an area of the skin and/or a portion thereof, such as facial skin, skin on the neck, skin on the arms, skin on the elbows, skin on the hands, skin on the legs, skin on the knees, skin on the male or female genital areas, and skin on the scalp, so that it can display local activity.
  • topical forms embrace cosmetical, and/or dermatological dosage forms which are suitable for external use, so that a direct contact with the skin and/or a portion thereof results.
  • the terms "subject" are well -recognized in the art, and, are used herein to refer to a mammal, and most preferably a human.
  • the subject is a subject in need of skin rejuvenation or a subject presenting signs of skin aging.
  • the term does not denote a particular age or sex. Thus, adult subjects, whether male or female, are intended to be covered.
  • skin rejuvenation and “skin rejuvenation effects” include one or more of the following: reducing the appearance of fine lines and wrinkles; reducing deep wrinkles; enhancing skin elasticity; reducing skin roughness; and producing a younger looking skin.
  • skin rejuvenation includes one or more of the following: anti -wrinkle effects (such as reduction of wrinkle depth, of wrinkle area, of wrinkle volume, of wrinkle number, reduction or prevention of fine lines, improvement in skin roughness), firming effects (such as plumping, anti-sagging, improvement in skin thickness, skin elasticity/suppleness), improving the skin barrier (such as improvement of the skin texture, of the skin moisturization level, reduction of the transepi dermal water loss) as well as decrease in age perception of the subject (either by herself/himself or by another person).
  • anti -wrinkle effects such as reduction of wrinkle depth, of wrinkle area, of wrinkle volume, of wrinkle number, reduction or prevention of fine lines, improvement in skin roughness
  • firming effects such as plumping, anti-sagging, improvement in skin thickness, skin elasticity/suppleness
  • improving the skin barrier such as improvement of the skin texture, of the skin moisturization level, reduction of the transepi dermal water loss
  • smoothing and softening as used herein mean altering the surface of the skin and/or keratinous tissue such that its tactile feel is improved (softening) or reducing the skin relief and eliminate the skin roughness (smoothing).
  • Signs of skin aging include, but are not limited to, all outwardly visible or tactilely perceptible manifestations as well as any other macro or micro effects due to skin aging. Such signs may be induced or caused by intrinsic factors or extrinsic factors, e.g., chronological aging and/or environmental damage.
  • These signs may result from processes that include, but are not limited to, the development of textural discontinuities such as wrinkles and coarse deep wrinkles, skin lines, crevices, bumps, large pores (e.g., associated with adnexal structures such as sweat gland ducts, sebaceous glands, or hair follicles), or unevenness or roughness, loss of skin elasticity (loss and/or inactivation of functional skin elastin), sagging (including puffiness in the eye area and jowls), loss of skin firmness, loss of skin tightness, loss of skin recoil from deformation, hyperkeratinization, elastosis, collagen breakdown, and other histological changes in the stratum comeum, dermis, epidermis, the skin vascular system (e.g., telangiectasia or spider vessels), and underlying tissues, especially those proximate to the skin.
  • textural discontinuities such as wrinkles and coarse deep wrinkles, skin lines, crevices, bumps,
  • thioethylamine in combination with azabenzene-4- carboxamide and/or an organic acid selected from the group consisting of glycolic acid, lactic acid, gluconolactone and/or combination thereof is capable of having anti-wrinkle effects (such as reduction of wrinkle depth, of wrinkle area, of wrinkle volume of wrinkle number, reduction or prevention of fine lines, improvement in skin roughness), firming effects (such as plumping, anti-sagging, improvement in skin thickness, skin elasticity/suppleness), as well as improving the skin barrier (such as improvement of the skin texture, of the skin moisturization level, reduction of the transepidermal water loss) leading in a global skin rejuvenation and thereby decrease in age perception.
  • anti-wrinkle effects such as reduction of wrinkle depth, of wrinkle area, of wrinkle volume of wrinkle number, reduction or prevention of fine lines, improvement in skin roughness
  • firming effects such as plumping, anti-sagging, improvement in skin thickness, skin elasticity/suppleness
  • improving the skin barrier such as improvement of the skin texture
  • an aspect of the present invention provides a cosmetic method of skin rejuvenation, wherein the method comprises topically applying to an area of the skin of a subject in need thereof a composition comprising
  • an organic acid preferably 1% to 30% w/w of an organic acid, wherein the organic acid is selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof,
  • the skin or an area of the skin is at least one of facial skin, skin on the neck, skin on the arms, skin on the hands, skin on the legs and skin on the scalp.
  • the skin rejuvenation consists in reducing the appearance of fine lines and wrinkles, reducing deep wrinkles, enhancing skin elasticity, and/or reducing skin roughness.
  • Fine lines are the start of wrinkles and look like small creases on the skin. Fine lines are closer to the surface of the skin, whereas wrinkles are deeper into the skin.
  • Reducing the appearance of fine lines and wrinkles can be measured by any one of the following methods known in the art: • Visual assessment or clinical a grading done on a scale, by a dermatologist.
  • Reducing deep wrinkles can be assessed by methods known in the art, such as by measuring the depth, the volume, the number, the surface, the spread angles of one or several main wrinkles.
  • Skin elasticity can be measured by methods known in the art, such as by cutometer, by a pinching test, by measuring the displacement of skin pore, skin deformation using unidirectional force, by measuring stress under suction application, or by measuring the velocity of ultrasonic waves through skin tissue.
  • Skin roughness can be measured by method known in the art, such as by digital or analogical dematoscopy method or by 2D or 3D skin image analysis or by replica images.
  • the Applicant has surprisingly found that a combination of thioethylamine, azabenzene-4- carboxamide or a salt thereof and/or an organic acid selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof provides a synergistic effect on skin rejuvenation, while being very well tolerated by human skin.
  • the % w/w of thioethylamine or a salt thereof refers to % w/w of thioethylamine (thioethylamine free base).
  • any particular mass of "thioethylamine or a salt thereof' refers to the mass equivalent of the free base (thioethylamine free base)
  • reference to any particular mass of a specific salt of thioethylamine, such as thioethylamine hydrochloride refers to the mass of the specific salt.
  • azabenzene-4-carboxamide or a salt thereof can be also applied to % w/w of azabenzene-4-carboxamide or a salt thereof, for example reference to any particular mass of "azabenzene-4-carboxamide or a salt thereof' refers to the mass equivalent of the free base (azabenzene-4-carboxamide).
  • thioethylamine is intended here to cover any acceptable salt, ester, solvate, hydrate, prodrug, or any other compound which, upon administration to the patient is capable of providing (directly or indirectly) thioethylamine.
  • the salts of thioethylamine are pharmaceutical acceptable salts, cosmetical acceptable salts, and dermatological acceptable salts.
  • Preferred salts of thioethylamine are hydrochloride, bitartrate, phosphate. Any compound that is a prodrug of thioethylamine is within the scope and spirit of the invention.
  • prodrug is used in its broadest sense and encompasses those derivatives that are converted in vivo to thioethylamine.
  • the prodrug can hydrolyze, oxidize, or otherwise react under biological conditions to provide thioethylamine.
  • prodrugs include, but are not limited to, derivatives and metabolites of thioethylamine that include biohydrolyzable moieties such as biohydrolyzable amides, biohydrolyzable esters, biohydrolyzable carbamates, biohydrolyzable carbonates, biohydrolyzable ureides, and biohydrolyzable phosphate analogues.
  • Prodrugs can typically be prepared using well-known methods, such as those described by Burger in “Medicinal Chemistry and Drug Discovery” 6th ed. (Donald J.
  • thioethylamine referred to herein may be in crystalline or amorphous form either as free compounds or as solvates (e.g. hydrates) and it is intended that all forms are within the scope of the present invention. Methods of solvation are generally known within the art.
  • the salts of the azabenzene-4-carboxamide of the invention are pharmaceutical acceptable salts, cosmetical acceptable salts, and dermatological acceptable salts.
  • pharmaceutically acceptable salts refers to salts that retain the desired biological activity of thioethylamine and azabenzene-4-carboxamide and include pharmaceutically acceptable acid addition salts and base addition salts.
  • Suitable pharmaceutically acceptable acid addition salts of thioethylamine and azabenzene-4- carboxamide may be prepared from an inorganic acid or from an organic acid or can be prepared in situ during the final isolation and purification of thioethylamine and azabenzene-4- carboxamide. Examples of such inorganic acids are hydrochloric, sulfuric, and phosphoric acid.
  • Appropriate organic acids may be selected from aliphatic, cycloaliphatic, aromatic, heterocyclic carboxylic and sulfonic classes of organic acids, examples of which are formic, acetic, propionic, succinic, glycolic, gluconic, lactic, malic, tartaric, citric, fumaric, maleic, alkyl sulfonic, arylsulfonic.
  • Suitable pharmaceutically acceptable base addition salts of azabenzene- 4-carboxamide include metallic salts made from lithium, sodium, potassium, magnesium, calcium, aluminium, and zinc, and organic salts made from organic bases such as choline, diethanolamine, morpholine.
  • organic salts are ammonium salts, quaternary salts such as tetramethylammonium salt; amino acid addition salts such as salts with glycine and arginine. Additional information on pharmaceutically acceptable salts can be found in Remington's Pharmaceutical Sciences, 19th Edition, Mack Publishing Co., Easton, PA 1995. In the case of agents that are solids, it is understood by those skilled in the art that the inventive compounds, agents and salts may exist in different crystalline or polymorphic forms, all of which are intended to be within the scope of the present invention.
  • compositions of the present invention can be prepared by any method known in the art for cosmetic and/or dermatological compositions.
  • the method comprises the simple mixing or blending of the components; though, especially where insoluble or immiscible components are employed higher agitation or homogenization may be necessary to prepare an appropriate composition, e.g., an emulsion or suspension, etc.
  • an appropriate composition e.g., an emulsion or suspension, etc.
  • the pH should range from about be 3.5 to about 8.
  • compositions of the invention are cosmetic compositions further comprising cosmetically acceptable excipients for topical administrations.
  • compositions of the inventions are dermatological compositions further comprising dermatologically acceptable excipients for dermatological administrations.
  • compositions and dermatological compositions according to the invention further comprise one or more cosmetically or dermatologically acceptable excipients, as are used conventionally in such compositions, for example preservatives, antioxidants, bactericides, perfumes, substances for preventing foaming, dyestuffs, pigments which have a colouring effect, thickeners, chelating agents, propellants, surfactant substances, emulsifiers, softening, moisturizing and/or moisture-retaining substances, distilled water, fats, oils, waxes or other conventional constituents of cosmetic or dermatological compositions, such as alcohols, polyols, polymers, foam stabilizers, electrolytes, organic solvents or silicone derivatives.
  • cosmetically or dermatologically acceptable excipients for example preservatives, antioxidants, bactericides, perfumes, substances for preventing foaming, dyestuffs, pigments which have a colouring effect, thickeners, chelating agents, propellants, surfactant substances, emulsifiers, softening
  • the cosmetic compositions, dermatological compositions and cosmetic combination products according to the invention do not contain polystyrenes, such as water-soluble polystyrenes or appropriate salts thereof.
  • the necessary amounts of the cosmetically or dermatologically acceptable excipients can, based on the desired product, easily be chosen by a person skilled in the art.
  • a moisturizing substance may be incorporated into compositions of the invention to maintain hydration or rehydrate the skin.
  • Moisturizers that prevent water from evaporating from the skin by providing a protective coating are called emollients. Additionally, an emollient provides a softening or soothing effect on the skin surface and is generally considered safe for topical use.
  • Preferred emollients include mineral oils, lanolin, petrolatum, capric/caprylic tri glyceraldehydes, cholesterol, silicones such as dimeticone, cyclometicone, almond oil, jojoba oil, avocado oil, castor oil, sesame oil, sunflower oil, coconut oil and grape seed oil, cocoa butter, olive oil, aloe extracts, fatty acids such as oleic and stearic, fatty alcohols such as cetyl and hexadecyl (ENJAY), diisopropyl adipate, hydroxybenzoate esters, benzoic acid esters of Cg-is-alcohols, isonononyl isononanoate, ethers such as polyoxypropylene butyl ethers and polyoxypropylene cetyl ethers, and C12-15- alkyl benzoates, and mixtures thereof.
  • silicones such as dimeticone, cyclometicone, almond oil, jojoba oil
  • Moisturizing substances that bind water, thereby retaining it on the skin surface are called humectants.
  • Suitable humectants can be incorporated into the compositions of the present invention such as glycerin, polypropylene glycol, polyethylene glycol, lactic acid, pyrrolidone carboxylic acid, urea, phospholipids, collagen, elastin, ceramides, lecithin sorbitol, PEG-4, and mixtures thereof.
  • compositions of the invention can also contain the usual alcohols, especially lower alcohols, preferably ethanol and/ or isopropanol, low diols or polyols and their ethers, preferably propyleneglycol, glycerin, ethyleneglycol, ethyleneglycol monoethyl- or monobutylether, propyleneglycol monomethyl- or monoethyl- or -monobutylether, diethyleneglycol monomethyl- or monoethylether and analogue products, polymers, foam stabilizers; electrolytes and especially one or more thickeners.
  • alcohols especially lower alcohols, preferably ethanol and/ or isopropanol
  • low diols or polyols and their ethers preferably propyleneglycol, glycerin, ethyleneglycol, ethyleneglycol monoethyl- or monobutylether, propyleneglycol monomethyl- or monoethyl- or -monobut
  • Thickeners that may be used in the compositions of the invention to assist in making the consistency of a product suitable include carbomer, silicium dioxide, magnesium and/ or aluminium silicates, beeswax, stearic acid, stearyl alcohol polysaccharides and their derivatives such as xanthan gum, hydroxypropyl cellulose, polyacrylamides, acrylate crosspolymers preferably a carbomer, such as Carbopol® of type 980, 981, 1382, 2984, 5984 alone or mixtures thereof.
  • carbomer such as Carbopol® of type 980, 981, 1382, 2984, 5984 alone or mixtures thereof.
  • Suitable stabilizing agents which may be included in the compositions of the invention to stabilize components such as e.g. an emulsifier or a foam builder/ stabilizer include but are not limited to alkali hydroxides such as a sodium and potassium hydroxide; organic bases such as diethanolamine (DEA), triethanolamine (TEA), aminomethyl propanol, and mixtures thereof; amino acids such as arginine and lysine and any combination of any foregoing.
  • alkali hydroxides such as a sodium and potassium hydroxide
  • organic bases such as diethanolamine (DEA), triethanolamine (TEA), aminomethyl propanol, and mixtures thereof
  • amino acids such as arginine and lysine and any combination of any foregoing.
  • compositions of the present invention may also contain filter substances that absorb UV radiation, or sunscreens, wherein the total quantity of filter substances is, for example 0.001 to 30 %, preferably 0.5 to 10 %, based on the total weight of the preparation.
  • the compositions may also serve as sunscreen agents for the skin.
  • Such UV filter substances include, for example, the following: avenobenzene, cinoxate, dioxybenzone, homosalate, menthyl anthranilate, octocrylene, octyl methoxycinnamate, octyl salicylate, oxybenzone, padimate O, phenylbenzimidazole sulfonic acid, sulisobenzone, titanium dioxide, trolamine salicylate, and zinc oxide.
  • compositions of the invention may also include one or more skin penetrants.
  • skin penetrants are additives that, when applied to the skin, have a direct effect on the permeability of the skin barrier: increasing the speed with which and/or the amount by which certain other compounds are able to penetrate into the skin layers.
  • Exemplary organic penetration enhancers include dimethyl sulfoxide; isopropyl myristate; decyl, undecyl or dodecyl alcohol; propylene glycol; polyethylene glycol; C9-11 or C12-15 fatty alcohols; azone; alkyl pyrrolidones; diethoxy glycol (Transcutol); lecithin; etc.
  • Surfactants can also be used as penetration enhancers.
  • compositions of the invention may further comprise at least one anti -wrinkles benefit agent selected from the group comprising coenzyme Q10, sodium hyaluronate, hyaluronic acid, hyaluronic acid fragments, gold particles, peptides (selected from Palmitoyl Tetrapeptide-7, Palmitoyl Oligopeptide, Acetyl Hexapeptide-8, Palmitoyl Tripeptide-5, Palmitoyl pentapeptide-4, Cu-GHK peptide, and dipalmitoyl hydroxyproline), tocopherol, ceramids, retinoids (selected from retinol, retinoic acid, retinyl palmitate, retinal, sodium retinoyl hyaluronate and adapalene), bakuchiol, collagen, resveraterol, heparan sulfate and their analogs, dermatan sulfate and their analogs
  • compositions of the invention may further comprise at least one anti-wrinkles benefit agent selected from the group comprising coenzyme Q10, sodium hyaluronate, hyaluronic acid, gold particles, peptides (selected from Palmitoyl Tetrapeptide-7, Palmitoyl Oligopeptide, Acetyl Hexapeptide-8, Palmitoyl Tripeptide-5, Palmitoyl pentapeptide-4, Cu-GHK peptide, and dipalmitoyl hydroxyproline), tocopherol, ceramids, retinoids (selected from retinol, retinoic acid, retinyl palmitate, retinal, sodium retinoyl hyaluronate and adapalene), bakuchiol, collagen, resveraterol, heparan sulfate, dermatan sulfate, chondroitin sulfate, panthenol, algae extract
  • compositions of the invention may also further include liposomes (unilamellar and/or multilamellar liposomes of any size), niosome, or any encapsulation system (such as microencapsulation, nanoencapsulation, cubosome) in order to facilitate the delivery of any component(s) of the composition to its site of action.
  • liposomes unilamellar and/or multilamellar liposomes of any size
  • niosome or any encapsulation system (such as microencapsulation, nanoencapsulation, cubosome) in order to facilitate the delivery of any component(s) of the composition to its site of action.
  • encapsulation system such as microencapsulation, nanoencapsulation, cubosome
  • the composition consists of • 0.01% to 30% w/w of thioethylamine, preferably 0.1% to 20% w/w of thioethylamine, o 0.01% to 30% w/w of azabenzene-4-carboxamide or a salt thereof, preferably 0.1 to 20% w/w of azabenzene-4-carboxamide or a salt thereof, and/or o 0.1% to 50% w/w of an organic acid, preferably 1% to 30% w/w of an organic acid, wherein the organic acid is selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof,
  • the composition consists of
  • azabenzene-4-carboxamide or a salt thereof 0.1 to 20% w/w of azabenzene-4-carboxamide or a salt thereof, and/or o 0.1% to 50% w/w of an organic acid, preferably 1% to 30% w/w of an organic acid, wherein the organic acid is selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof,
  • compositions comprising thioethylamine in combination with azabenzene-4- carboxamide and/or an organic acid selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof, are for example:
  • anti-wrinkle effects such as reduction of wrinkle depth, of wrinkle number, reduction or prevention of fine lines, improvement in skin roughness
  • compositions comprising thioethylamine in combination with azabenzene-4- carboxamide and/or an organic acid selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof, on the skin structure are for example:
  • thioethylamine in combination with azabenzene-4- carboxamide and/or an organic acid selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof has better, synergistic effects when compared to thioethylamine used alone.
  • compositions of the invention may be cosmetic or dermatologic compositions, and may exist in a wide variety of forms, such as emulsions, suspensions, solutions and the like.
  • the compositions of the invention are in the form of lotions, creams, gels, solutions, sprays, cleansers, powders, ointments, waxes, lipsticks, soaps, shampoos, hydroalcoholic solutions, suspensions, scrubs, saturated pads, skin conditioning agents, and other types of cosmetic compositions.
  • compositions of the invention may be, for example anhydrous preparations, oil-free preparations, emulsions or microemulsions of the type water-in-oil (W/O) or of the type oil-in-water (O/W), multiple emulsions, for example of the type water-in-oil-in-water (W/O/W), solid sticks, or even aerosols.
  • W/O water-in-oil
  • O/W oil-in-water
  • multiple emulsions for example of the type water-in-oil-in-water
  • solid sticks or even aerosols.
  • aerosols aerosols.
  • the preferred forms of the compositions of the invention are gels, lotions, emulsions, powder forms.
  • compositions described herein provide their cosmetic effect in combating skin wrinkles, in skin rejuvenation, and in minor wound repair, at least in part due to their effects on collagen and elastin.
  • compositions of the invention are used for cosmetic skin rejuvenation of human natural healthy skin, i.e. non-therapeutic use, that is not related to treatment of diseases or pathological states of the skin.
  • cosmetic skin rejuvenation relates to anti-wrinkle effects (such as reduction of wrinkle depth of wrinkle area, of wrinkle volume, of wrinkle number, reduction or prevention of fine lines, improvement in skin roughness) firming effects (such as plumping, anti-sagging, improvement in skin thickness, skin elasticity/ suppleness), improving the skin barrier (such as skin texture, skin moisturization level) leading in a global skin rejuvenation (and decrease in age perception).
  • cosmetic skin rejuvenation consists in in reducing the appearance of fine lines and wrinkles, reducing deep wrinkles, enhancing skin elasticity, reducing skin roughness.
  • the method of skin rejuvenation can be used if a subject desires to improve appearance of skin of at least a region of skin for cosmetic reasons.
  • the skin or an area of the skin is at least one of facial skin, skin on the neck, skin on the arms, skin on the elbows, skin on the hands, skin on the legs, skin on the knees, skin on the male or female genital areas, and skin on the scalp.
  • the method of skin rejuvenation of the invention is repeated for number of times sufficient to obtain skin rejuvenation effects and decrease in age perception.
  • the method of skin rejuvenation of the invention can be continued to be applied not every day, not every consecutive day or one to several times a week to maintain the skin rejuvenation results or effects.
  • the compositions are applied to the skin or an area of the skin, preferably human skin.
  • the amount of the composition that is to be applied to the skin depends upon the form of the composition and its mode of application. For example, a spray formulation may be applied so as to provide a light, even coat on the skin.
  • lotions, creams, gels, shampoos and the like are typically applied in an amount to provide a light coating to the treatment area, consistent with the application of topical cosmetic ointments, creams, lotions, and the like.
  • the rate of application is about 20 to 60 ml for the entire body, i.e., for the exposed skin of an "average individual" wearing a swimsuit and standing 1.65 m tall, weighing 68 kg, and having a 0.81 m waist.
  • This translates to an application rate of about 2 mg/cm 2 of skin surface, including hairy or non-hairy skin surface.
  • a typical application rate is 0.5 to 1.0 ml.
  • the amount of composition applied lies in the range of from about 0.1 to about 10 mg/cm 2 , preferably from about 1 to about 3 mg/cm 2 , of skin.
  • compositions of the invention may be applied once or more times per day depending on the activities the particular subject is engaged in. For example, a subject engaging in normal workday activities may wish to apply the compositions twice a day, once in the morning, and once in the evening, in conjunction with normal grooming. On the other hand, if the subject plans outdoor activities such as sunbathing and athletics, the compositions may be applied prior to, and during, such activities, much like a sunscreen composition is applied periodically during the day.
  • the compositions of the present invention may also be applied to the entire body, particularly areas which are not covered by clothing, such as the arms, neck, and lower legs.
  • the invention provides a cosmetic method of skin rejuvenation comprising the steps of a) topically applying to an area of the skin of a subject in need thereof a first composition comprising
  • thioethylamine 0.01% to 99% w/w of thioethylamine, preferably 0.1% to 20% or 0.1% to 30% w/w of thioethylamine, and
  • an organic acid preferably 0.1% to 40% or 0.1% to 50% w/w of an organic acid, wherein the organic acid is selected from the group comprising alpha-hydroxy acid (AHA), beta-hydroxy acid (BHA), poly-hydroxy acid (PHA) and/or combination thereof
  • b) topically applying to said area of the skin a second composition comprising 0.01% to 99% w/w of an azabenzene-carboxamide isomer or a salt thereof, preferably 0.1% to 20% or 0.1% to 30% w/w of an azabenzene-carboxamide isomer or a salt thereof, c) repeating the steps a) and b) to obtain skin rejuvenation effects (endpoint), wherein the azabenzene-carboxamide isomer is selected from the group comprising azabenzene- 4-carboxamide, azabenzene-3-carboxamideand azabenzene-2-carboxamide, alpha-hydroxy acid (AHA) is selected from the group comprising
  • the alpha-hydroxy acid is selected from the group comprising glycolic acid and lactic acid
  • beta-hydroxy acid is selected from the group comprising salicylic acid, beta 5 hydroxybutanoic acid, tropic acid, trethocanic acid and/or combination thereof.
  • the beta-hydroxy acid is salicylic acid
  • poly-hydroxy acid is selected from the group comprising gluconolactone, galactose, ellagic acid, lactobionic acid and/or combination thereof.
  • the poly-hydroxy acid is selected from the group comprising gluconolactone and lactobionic acid.
  • the invention provides a cosmetic method of skin rejuvenation comprising the steps of a) topically applying to an area of the skin of a subject in need thereof a first composition comprising
  • thioethylamine preferably 0.1% to 20% of thioethylamine, and 0.1% to 50% w/w of an organic acid, preferably 1% to 30% of an organic acid, wherein the organic acid is selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof
  • a second composition comprising 0.01% to 30% w/w of an azabenzene-4-carboxamide or a salt thereof, preferably 0.1% to 20% of an azabenzene-4-carboxamide or a salt thereof, c) repeating the steps a) and b) to obtain skin rejuvenation effects (endpoint).
  • the method further comprises removing the first composition by any suitable method before topically applying the second composition.
  • the suitable method is selected from rinsing with water with or without a suitable detergent, removing with any suitable solvent or cleanser, removing with a dry or wet pad, and/or combination thereof
  • the skin rejuvenation consists in reducing the appearance of fine lines and wrinkles, reducing deep wrinkles, enhancing skin elasticity, and/or reducing skin roughness.
  • a suitable detergent is typically a skin cleansing product, such as personal care cleanser, used for example in person washing, selected from bars, liquids, gels, pastes, etc., such as liquid or solid soaps or shampoos.
  • a time period between topical application of the first composition and the topical application of the second composition is few seconds (application of the second composition right after the first one), up to several hours later, such as 1 hour, 2 hours, 3 hours, 4 hours.
  • the second composition is applied right after the application of the first composition or up to 2 hours later.
  • the cosmetic method of skin rejuvenation of the invention is repeated for a time period or number of times sufficient to obtain the desired skin rejuvenation effects (endpoint), such as one week, two weeks, three weeks, four weeks, five weeks, six weeks, seven weeks, eight weeks, 2 months, three months, one year, two years, three years, or more; or such as one to four weeks, one to eight weeks, one week to one year, one week to two years, one week to five years.
  • the cosmetic method skin rejuvenation of the invention is repeated not every day, not every consecutive day or to maintain the skin rejuvenation results or effects, the cosmetic method skin rejuvenation of the invention is repeated one to four times a week.
  • the first composition comprises 0.1% to 20% w/w of thioethylamine or a salt thereof, preferably 0.1% to 20% or 0.1% to 30% w/w of thioethylamine or a salt thereof and 0.1% to 40% w/w of an organic acid, preferably 0.1% to 40% or 0.1% to 50% w/w of an organic acid, wherein the organic acid is selected from the group comprising alpha-hydroxy acid (AHA), beta-hydroxy acid (BHA), poly-hydroxy acid (PHA) and/or combination thereof, and wherein o alpha-hydroxy acid (AHA) is selected from the group comprising glycolic acid, lactic acid, malic acid, tartaric acid, citric acid, mandelic acid and/or combination thereof.
  • AHA alpha-hydroxy acid
  • BHA beta-hydroxy acid
  • PHA poly-hydroxy acid
  • AHA is selected from the group comprising glycolic acid, lactic acid, malic acid, tartaric acid, citric acid, mandelic acid
  • the alpha-hydroxy acid is selected from the group comprising glycolic acid and lactic acid.
  • o beta-hydroxy acid (BHA) is selected from the group comprising salicylic acid, beta 5 hydroxybutanoic acid, tropic acid, trethocanic acid and/or combination thereof.
  • the beta-hydroxy acid is salicylic acid.
  • o poly-hydroxy acid (PHA) is selected from the group comprising gluconolactone, galactose, ellagic acid, lactobionic acid and/or combination thereof.
  • the poly-hydroxy acid is selected from the group comprising gluconolactone and lactobionic acid.
  • the first composition comprises 0.01% to 30% w/w of thioethylamine, preferably 0.1% to 20% or 0.1% to 30% w/w of thioethylamine and 0.1% to 50% w/w of an organic acid, preferably 1% to 30% w/w of an organic acid selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof.
  • the second composition comprises 0.01% to 30% w/w of an azabenzene-carboxamide isomer or a salt thereof, preferably 0.1% to 20% or 0.1% to 30% w/w of an azabenzene-carboxamide isomer or a salt thereof, wherein the azabenzene-carboxamide isomer is selected from the group comprising azabenzene-4-carboxamide, azabenzene-3-carboxamideand azabenzene-2- carb oxami de.
  • the second composition comprises 0.01% to 30% w/w of azabenzene-4-carboxamide or a salt thereof, preferably 0.1% to 20% or 0.1% to 30% w/w of azabenzene-4-carboxamide or a salt thereof.
  • the invention provides a cosmetic method of skin rejuvenation comprising the steps of a) topically applying to an area of the skin of a subject in need thereof a first composition comprising 0.01% to 99% w/w of thioethylamine, preferably 0.1% to 20% or 0.1% to 30% w/w of thioethylamine, b) topically applying to said area of the skin a second composition comprising 0.01% to 99% w/w of an azabenzene-carboxamide isomer or a salt thereof, preferably 0.1% to 20% or 0.1% to 30% w/w of an azabenzene-carboxamide isomer or a salt thereof, and
  • an organic acid preferably 0.1% to 40% or 0.1% to 50% w/w of an organic acid
  • the organic acid is selected from the group comprising alpha-hydroxy acid (AHA), beta-hydroxy acid (BHA), poly-hydroxy acid (PHA) and/or combination thereof
  • the azabenzene-carboxamide isomer is selected from the group comprising azabenzene- 4-carboxamide, azabenzene-3-carboxamideand azabenzene-2-carboxamide
  • alpha-hydroxy acid (AHA) is selected from the group comprising glycolic acid, lactic acid, malic acid, tartaric acid, citric acid, mandelic acid and/or combination thereof.
  • the alpha-hydroxy acid is selected from the group comprising glycolic acid and lactic acid
  • beta-hydroxy acid is selected from the group comprising salicylic acid, beta 5 hydroxybutanoic acid, tropic acid, trethocanic acid and/or combination thereof.
  • the beta-hydroxy acid is salicylic acid
  • poly-hydroxy acid is selected from the group comprising gluconolactone, galactose, ellagic acid, lactobionic acid and/or combination thereof.
  • the poly-hydroxy acid is selected from the group comprising gluconolactone and lactobionic acid.
  • the invention provides a cosmetic method of skin rejuvenation comprising the steps of a) topically applying to an area of the skin of a subject in need thereof a first composition comprising 0.01% to 30% w/w of thioethylamine, preferably 0.1% to 20% w/w of thioethylamine, b) topically applying to said area of the skin a second composition comprising 0.01% to 30% w/w of an azabenzene-4-carboxamide or a salt thereof, preferably
  • an organic acid 0.1% to 50% w/w of an organic acid, preferably 1% to 30% w/w of an organic acid, wherein the organic acid is selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof, c) repeating the steps a) and b) to obtain skin rejuvenation effects (endpoint).
  • the method further comprises removing the first composition by any suitable method before topically applying the second composition.
  • the suitable method is selected from rinsing with water with or without a suitable detergent, removing with any suitable solvent or cleanser, removing with a dry or wet pad, and/or combination thereof
  • the skin rejuvenation consists in reducing the appearance of fine lines and wrinkles, reducing deep wrinkles, enhancing skin elasticity, and/or reducing skin roughness.
  • a suitable detergent is typically a skin cleansing product, such as personal care cleanser, used for example in person washing, selected from bars, liquids, gels, pastes, etc., such as liquid or solid soaps or shampoos.
  • a time period between topical application of the first composition and the topical application of the second composition is few seconds (application of the second composition right after the first one), up to several hours later, such as 1 hour, 2 hours, 3 hours, 4 hours.
  • the second composition is applied right after the application of the first composition or up to 2 hours later.
  • the first composition comprises 0.01% to 30% w/w of thioethylamine, preferably 0.1% to 20% or 0.1% to 30% w/w of thioethylamine.
  • the second composition comprises 0.1% to 20% w/w of an azabenzene-carboxamide isomer or a salt thereof, preferably 0.1% to 20% or 0.1% to 30% w/w of an azabenzene-carboxamide isomer or a salt thereof, and 0.1% to 40% w/w of an organic acid, preferably 0.1% to 40% or 0.1% to 50% w/w of an organic acid, wherein the organic acid is selected from the group comprising alpha-hydroxy acid (AHA), beta-hydroxy acid (BHA), poly-hydroxy acid (PHA) and/or combination thereof, and wherein
  • AHA alpha-hydroxy acid
  • BHA beta-hydroxy acid
  • PHA poly-hydroxy acid
  • the azabenzene-carboxamide isomer is selected from the group comprising azabenzene- 4-carboxamide, azabenzene-3-carboxamideand azabenzene-2-carboxamide, and
  • alpha-hydroxy acid is selected from the group comprising glycolic acid, lactic acid, malic acid, tartaric acid, citric acid, mandelic acid and/or combination thereof.
  • the alpha-hydroxy acid is selected from the group comprising glycolic acid and lactic acid.
  • beta-hydroxy acid is selected from the group comprising salicylic acid, beta 5 hydroxybutanoic acid, tropic acid, trethocanic acid and/or combination thereof.
  • the beta-hydroxy acid is salicylic acid.
  • poly-hydroxy acid is selected from the group comprising gluconolactone, galactose, ellagic acid, lactobionic acid and/or combination thereof.
  • the poly-hydroxy acid is selected from the group comprising gluconolactone and lactobionic acid.
  • the second composition comprises 0.01% to 30% w/w of azabenzene-4-carboxamide or a salt thereof, preferably 0.1% to 20% or 0.1% to 30% w/w of azabenzene-4-carboxamide or a salt thereof, and 0.1% to 50% w/w of an organic acid, preferably 1% to 30% w/w of an organic acid selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof.
  • the first composition and the second composition further comprise at least one cosmetically acceptable excipient.
  • the cosmetic methods of skin rejuvenation of the invention is repeated for the time period sufficient to obtain skin rejuvenation effects
  • the time period can be few days (1 to 7 days), few weeks (1 to 4 weeks or 1 to 8 weeks or 2 to 8 weeks or 4 to 8 weeks), few months (1 to 3 months or 1 to 6 months or 1 to 12 months), few years (1 to 5 years) or a life cosmetic treatment, depending on desired skin rejuvenation effects or results.
  • the methods of the invention can be continued to be applied not every day, not every consecutive day or one to six times a week to maintain the skin rejuvenation results or effects.
  • the cosmetic methods of skin rejuvenation of the invention are repeated (step c) for a number of times sufficient to obtain skin rejuvenation effects or results (endpoint) and/or, after achievement of desired skin rejuvenation results or effects (endpoint), the method of the invention is repeated not every day, not every consecutive day or one to six times a week to maintain the skin rejuvenation results or effects.
  • endpoint chosen in a particular case will vary according to the skin desired appearance, the outcome desired by the subject and other factors.
  • endpoints can be defined subjectively such as, for example when the subject is simply "satisfied" with the results of the cosmetic treatment.
  • the skin rejuvenation effect is surprisingly improved comparing to a composition comprising all threes compounds, namely thioethylamine, an organic acid selected from an alpha-hydroxy acid (AHA), beta-hydroxy acid (BHA) and polyhydroxy acid (PHA), preferably selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof, and an azabenzene-carboxamide isomer or a salt thereof, preferably azabenzene-4- carboxamide or a salt thereof.
  • AHA alpha-hydroxy acid
  • BHA beta-hydroxy acid
  • PHA polyhydroxy acid
  • step a The advantages of the cosmetic methods of skin rejuvenation comprising separate administrations of the first composition comprising thioethylamine (step a) and the second composition comprising an azabenzene-carboxamide isomer or a salt thereof, preferably comprising azabenze-4-carboxamide or a salt thereof, and an organic acid, selected from an alpha-hydroxy acid (AHA), a beta-hydroxy acid (BHA) and a poly-hydroxy acid (PHA), preferably selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof, (step b) are as follows:
  • compositions comprising all threes compounds, namely thioethylamine, an organic acid selected from an alpha-hydroxy acid (AHA), beta-hydroxy acid (BHA) and polyhydroxy acid (PHA), preferably selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof, and an azabenzene-carboxamide isomer or a salt thereof, preferably azabenzene-4- carboxamide or a salt thereof.
  • AHA alpha-hydroxy acid
  • BHA beta-hydroxy acid
  • PHA polyhydroxy acid
  • Another aspect of the present invention provides a cosmetic combination product comprising a first composition and a second composition for separate topical application, wherein
  • thioethylamine 0.01% to 99% w/w of thioethylamine, preferably 0.1% to 20% or 0.1% to 30% w/w of thioethylamine, and
  • an organic acid preferably 0.1% to 40% or 0.1% to 50% w/w of an organic acid
  • the organic acid is selected from the group comprising alpha-hydroxy acid (AHA), beta-hydroxy acid (BHA), poly-hydroxy acid (PHA) and/or combination thereof
  • o alpha-hydroxy acid (AHA) is selected from the group comprising glycolic acid, lactic acid, malic acid, tartaric acid, citric acid, mandelic acid and/or combination thereof.
  • the alpha-hydroxy acid is selected from the group comprising glycolic acid and lactic acid.
  • o beta-hydroxy acid is selected from the group comprising salicylic acid, beta 5 hydroxybutanoic acid, tropic acid, trethocanic acid and/or combination thereof.
  • the beta-hydroxy acid is salicylic acid.
  • o poly-hydroxy acid (PHA) is selected from the group comprising gluconolactone, galactose, ellagic acid, lactobionic acid and/or combination thereof.
  • the poly-hydroxy acid is selected from the group comprising gluconolactone and lactobionic acid.
  • azabenzene-carboxamide isomer 0.01% to 99% w/w of an azabenzene-carboxamide isomer or a salt thereof, preferably 0.1% to 20% or 0.1% to 30% w/w of an azabenzene-carboxamide isomer or a salt thereof, wherein the azabenzene-carboxamide isomer is selected from the group comprising azabenzene-4-carboxamide, azabenzene-3-carboxamideand azabenzene-2-carboxamide.
  • the present invention provides a cosmetic combination product comprising a first composition and a second composition for separate topical application, wherein
  • thioethylamine • 0.01% to 30% w/w of thioethylamine, preferably 0.1% to 20% or 0.1% to 30% w/w of thioethylamine, and • 0.1% to 50% w/w of an organic acid, preferably 1% to 30% w/w of an organic acid selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof, and
  • the first composition and the second composition further comprise at least one cosmetically acceptable excipient.
  • the present invention provides a cosmetic combination product consisting of a first composition and a second composition for separate topical application, wherein
  • an organic acid preferably 1% to 30% w/w of an organic acid selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof,
  • retinoids are selected from the group consisting of retinol, retinoic acid, retinyl palmitate, retinal, sodium retinoyl hyaluronate and adapalene,
  • Tazman pepper is a natural Australian active ingredient extracted from the Colombian pepper berry.
  • Another aspect of the present invention provides a cosmetic combination product comprising a first composition and a second composition for separate topical application, wherein
  • thioethylamine 0.01% to 99% w/w of thioethylamine, preferably 0.1% to 20% or 0.1% to 30% w/w of thioethylamine.
  • azabenzene-carboxamide isomer 0.01% to 99% w/w of an azabenzene-carboxamide isomer or a salt thereof, preferably 0.1% to 20% or 0.1% to 30% w/w of an azabenzene-carboxamide isomer or a salt thereof, wherein the azabenzene-carboxamide isomer is selected from the group comprising azabenzene-4-carboxamide, azabenzene-3-carboxamideand azabenzene-2-carboxamide, and
  • an organic acid preferably 0.1% to 40% or 0.1% to 50% w/w of an organic acid
  • the organic acid is selected from the group comprising alpha-hydroxy acid (AHA), beta-hydroxy acid (BHA), poly-hydroxy acid (PHA) and/or combination thereof
  • o alpha-hydroxy acid (AHA) is selected from the group comprising glycolic acid, lactic acid, malic acid, tartaric acid, citric acid, mandelic acid and/or combination thereof.
  • the alpha-hydroxy acid is selected from the group comprising glycolic acid and lactic acid.
  • o beta-hydroxy acid is selected from the group comprising salicylic acid, beta 5 hydroxybutanoic acid, tropic acid, trethocanic acid and/or combination thereof.
  • the beta-hydroxy acid is salicylic acid.
  • o poly-hydroxy acid (PHA) is selected from the group comprising gluconolactone, galactose, ellagic acid, lactobionic acid and/or combination thereof.
  • the poly-hydroxy acid is selected from the group comprising gluconolactone and lactobionic acid.
  • the present invention provides a cosmetic combination product comprising a first composition and a second composition for separate topical application, wherein
  • the first composition comprising • 0.01% to 30% w/w of thioethyl amine, preferably 0.1% to 20% or 0.1% to 30% w/w of thioethylamine, and
  • an organic acid preferably 1% to 30% w/w of an organic acid selected from the group consisting of glycolic acid, lactic acid, lactobionic acid, gluconolactone and/or combination thereof.
  • the first composition and the second composition further comprise at least one cosmetically acceptable excipient.
  • the present invention provides a cosmetic combination product consisting of a first composition and a second composition for separate topical application, wherein
  • skin anti -wrinkle agents selected from the group comprising peptides, Panthenol, sodium hyaluronate, hyaluronic acid, retinoids, natural moisturizing factors, and sugars selected from Xylitylglucoside, Anhydroxylitol and Xylitol, and
  • retinoids are selected from the group consisting of retinol, retinoic acid, retinyl palmitate, retinal, sodium retinoyl hyaluronate and adapalene.
  • peptides are selected from the group consisting of Palmitoyl Tetrapeptide-7, Palmitoyl Oligopeptide, Acetyl Hexapeptide-8, Palmitoyl Tripeptide-5, Palmitoyl pentapeptide-4, Cu-GHK peptide, and dipalmitoyl hydroxyproline.
  • the natural moisturizing factors are selected from the group consisting of PCA salts, Arginine, Glycine, Alanine, Glutamic Acid, urea and ceramides.
  • the first composition and the second composition are separately topically applied.
  • a time period between topical application of the first composition and the topical application of the second composition is few seconds (application of the second composition right after the first one), up to several hours later, such as 1 hour, 2 hours, 3 hours, 4 hours.
  • the second composition is applied right after the application of the first composition or up to 2 hours later.
  • compositions of the invention are examples of the compositions of the invention.
  • Composition A (emulsion O/W)
  • Composition B (aqueous gel)
  • Composition D (emulsion O/W)
  • Composition E (emulsion O/W)
  • Composition F applied for 30min before being rinsed off
  • composition G applied after composition G as a leave-on
  • Composition H applied for 15min before being rinsed off

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Abstract

La présente invention concerne une utilisation cosmétique d'une composition comprenant de la thioéthylamine conjointement avec de l'azabenzène-4-carboxamide et/ou un acide organique pour le rajeunissement de la peau.
PCT/EP2023/074830 2022-09-12 2023-09-11 Utilisation d'une composition de thioéthylamine pour le rajeunissement de la peau et effet synergique amélioré lorsqu' elle est combinée à un acide organique et/ou à de l'azabenzène-4-carboxamide Ceased WO2024056566A1 (fr)

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Cited By (1)

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WO2025247621A1 (fr) * 2024-05-30 2025-12-04 Beiersdorf Ag Préparation cosmétique pour réduire l'acné fongique

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