OA19087A - Medicament and cosmetic composition comprising resorcinol derivatives. - Google Patents

Abstract

The present invention belongs to the fields of pharmaceuticals and cosmetics, and concerns on the one hand a medicament for the inhibition of and refers also on the cosmetic, non-therapeutic use for the treatment of hyperpigmentation, particularly induced by sun light radiation, preferably induced by visible light radiation.

Description

MEDICAMENT COMPRISING RESORCINOL DERIVATIVES

FIELD OF INVENTION

[0001] The present invention belongs to the fields of pharmaceuticals and cosmetics, and 10 concerns on the one hand a médicament for the inhibition of and refers also on the cosmetic, non-therapeutic use for the treatment of hyperpigmentation, particularly induced by sun light radiation, preferably induced by visible light radiation.

STATE OF THE ART

[0002] Many people are concerned with the degree of pigmentation of their skin. For example, people with âge spots or freckles may wish such pigmented spots to be less pronounced. Others may wish to reduce the skin darkening caused by exposure to sunlight or to lighten their natural skin color. Skin may appear lighter or darker than normal in concentrated areas. Such skin pigmentation disorders occur because the body produces too 20 much or too little melanin, which is the pigment produced by mélanocytes in the skin.

[0003] Human skin color is determined primarily by the content of the pigment melanin in the basal epidermis layer. Melanin pigments, which are normally brown to black in color, are formed in the mélanocytes (pigment-producing cells) of the skin, which are transferred to the kératinocytes and give the skin or haïr its color. In mammals, the brown-black 25 eumelanins are primarily formed from hydroxy-substituted aromatic amino acids such as Ltyrosine and L-DOPA, the yellow to red pheomelanins additionally from sulfur-containing molécules (Cosmetics and Toiletries 1996, 111 (5), 43-51). Starting from L-tyrosine, L-3, 4dihydroxyphenylalanine (L-DOPA) is formed by the copper-containing key enzyme tyrosinase and is in turn converted by tyrosinase to dopachrome. By a sériés of steps catalysed by 30 various enzymes, the latter is oxidised to form melanin.

[0004] The skin can become hyperpigmented when too much melanin concentrâtes at one area or portion of the skin due to the rétention time of the melanosomes in the basal layer. Hyperpigmentation can also occur as a resuit of overexposure to the sun or due to divers inflammatory stimuli. Increased melanin production is often referred to as melasma, 35 chloasma or solar lentigenes (âge spots), solar lentigines ephilides (freckles), and pigmented kératoses. Melasma is a general term describing darkening of the skin. Chloasma is generally used to describe skin discolorations caused by hormones. These hormonal changes are usually the resuit of pregnancy, birth control pills or estrogen replacement therapy. Solar lentigenes refer to darkened spots on the skin caused by the sun. These spots are quite 40 common in adults with a long history of unprotected sun exposure. The most common cause of darkened areas of skin, brown spots or areas of discoloration is unprotected sun

exposure, although hyperpigmentation can also be caused by skin damage, such as blemishes, wounds or rashes.

[0005] The prior art discloses ways to treat hyperpigmentation by application of skin lightening agents. Représentative skin lightening agents include hydroquinone and Vitamin 5 C. Such agents typically lighten the skin by inhibiting the activity of tyrosinase enzymes involved in melanogenesis.

[0006] For instance, EP1206241 Al relates to methods of lightening skin, e.g., lightening hyperpigmented régions of skin and of lightening skin by regulating melanin in skin by a composition containing certain oxime compounds.

[0007] WO 2012 020070 Al refers to a skin depigmentation composition comprising a methimazole dérivative, wherein the skin pigmentation disorder is selected from the group consisting of hyperpigmentation, melasma, postinflammatory hyperpigmentation, lentigo, freckles, drug induced hyperpigmentation, light induced hyperpigmentation and chemical induced hyperpigmentation.

[0008] According to Duteil L. et al., Différences in visible light-induced pigmentation according to wavelengths: a clinical and histological study in comparison with UVB exposure, Pigment Cell Melanoma Res. 27; 822-826; 2014 John Wiley & Sons A/S; only few studies hâve been carried oui to study visible light effects on skin pigmentation. Duteil et. al. demonstrates that various wavelengths of the visible part of solar spectrum hâve different 20 effects on skin pigmentation.

[0009] The primary object of the present invention was therefore to provide a composition, and method related thereto, for treating, preventing and/or ameliorating sunlight induced, particularly visible light induced hyperpigmentation of skin areas, particularly of human skin. It is another objection of the present invention to provide a synergistic mixture of active 25 ingrédients for this purpose, and to provide spécial formulations for targeted application of the active ingrédients.

DESCRIPTION OF THE INVENTION

[0010] The subject matter of the invention is a médicament containing at least a resorcinol dérivative of formula (I)

(D in which R stands for an alkyl radical having 3 to 10 carbon atoms or an optionally substituted alkylphenyl radical having 8 to 16 carbon atoms, for use in the treatment, prévention and/or amelioration of hyperpigmentation.

[0011] RESORCINOL DERIVATIVES

[0012] Resorcinol dérivatives of formula (I) are preferabiy compounds of formula (II)

R1

(H), wherein RI is CH3 or H, and

R2 is a C3-C6 aliphatic residue or the C3-C6 aliphatic residue forms together a ring, which is selected from cyclopropane, cyclobutan, cyclopentan, cyclohexan.

[0013] The resorcinol dérivatives of the present invention represent well known compounds that can be obtained in the market. Preferabiy, the compounds are selected from the group 10 consisting of butyl resorcinol, pentyl resorcinol, hexyl resorcinol, heptyl resorcinol, octyl resorcinol, nonyl resorcinol, decylresorcinol, phenylethyl resorcinol, phenylpropyl resorcinol, phenylbutyl resorcinol, phenylhexyl resorcinol, toluoylethyl resorcinol, toluoylpropyl resorcinol, toluoylbutyl resorcinol, toluoylhexyl resorcinol, methoxytoluoylethyl resorcinol, methoxytoluoylpropyl resorcinol, methoxytoluoylbutyl resorcinol, methoxyltoluoylhexyl 15 resorcinol, dimethoxytoluoylethyl resorcinol, dimethoxytoluoylpropyl resorcinol, dimethoxytoluoylbutyl resorcinol, dimethoxytoluoylhexyl resorcinol and their mixtures. The preferred compounds are 4-butyl resorcinol, 4-hexyl resorcinol and phenylethyl resorcinol, most preferred is phenylethyl resorcinol (SymWhite® 377).

[0014] Surprisingly, it has been observed that resorcinol dérivatives as described herein 20 affected the sunlight induced, particularly visible light induced pigmentation of skin areas on which they are applied to, especially in that to prevent, treat and/or ameliorate pigmentation at the area or portion of skin to which they are applied.

[0015] In a preferred embodiment the médicament ofthe present invention is for use in the treatment, prévention and/or amelioration of hyperpigmentation, wherein the 25 hyperpigmentation is induced by the radiation of sunlight, preferabiy with a wavelength in the range from 100 nm to 1500 nm, preferabiy 280 nm to 750 nm, more preferabiy hyperpigmentation which is induced by the radiation of visible light, preferabiy with a wavelength in the range from 380 nm to 750 nm, more preferabiy from 400 nm to 700 nm.

[0016] Therefore, in the sense ofthe présent invention hyperpigmentation is meant to be 30 sunlight induced, more particularly visible light induced hyperpigmentation.

[0017] Advantageously the médicament of the present invention is highly effective to prevent, treat and/or ameliorate hyperpigmentation in the said preferred wavelengths, particularly for radiations in the range from 280 nm to 750 nm, particularly for radiations which lie within the visible light wavelengths from 380 nm to 750 nm.

[0018] In a preferred embodiment, the médicament of the present invention further comprises at least one UV filters, wherein the UV filters are selected from the group consisting of UV-A filters, UV-B filters, and light protection pigments.

[0019] The combination of resorcinol dérivatives of formula (I), respectively (II) with UV filters provides synergistically improved prévention, treatment and/or amelioration of hyperpigmentation and thus improves the performance of resorcinol dérivatives and conventional UV filters in an unexpected manner, especially in case of 4-butyl resorcinol, 4hexyl resorcinol and phenylethyl resorcinol, most preferred in case of phenylethyl resorcinol.

[0020] UV FILTERS

[0021] Mixtures of resorcinol dérivatives of formula (I), respectively (II) and UV filters provide synergistic enhancement of protection of the skin and haïr against the harmful effects of sunlight, and thus is advantageously in the treatment, prévention and/or amelioration of hyperpigmentation of human skin, especially in case of 4-butyl resorcinol, 4hexyl resorcinol and phenylethyl resorcinol, most preferred in case of phenylethyl resorcinol.

[0022] Additionally, the combination of resorcinol dérivatives of formula (I), respectively (II) and UV filters are well tolerated, not causing reddening, bleaching, or tanning of the skin, are non-irritating, do not dry out the skin, do not form a moist, scaly, powdery, or sticky film, and do not chap the skin when applied to the human skin. These UV filters can be UV-A filters, UV-B filters, pigments, or mixtures thereof that are further explained below, especially in case of 4-butyl resorcinol, 4-hexyl resorcinol and phenylethyl resorcinol, most preferred in case of phenylethyl resorcinol.

[0023] UV-A AND UV-B FILTERS

[0024] UV filters are understood to refer, for example, to organic substances that are liquid 25 or crystalline at room température (light filters) and are capable of absorbing ultraviolet radiation and releasing the absorbed energy in the form of long-wave radiation such as heat. Ordinarily, UV filters are contained in amounts of 0.05 wt% to 50 wt% and preferably 0.5 wt% to 40 wt%. UVB filters can be oil-soluble or water-soluble. Examples of suitable oilsoluble substances include:

· 3-benzylidene camphor or 3-benzylidene norcamphor and dérivatives thereof, such as 3-(4-methylbenzylidene)camphor;

• 4-aminobenzoic acid dérivatives, preferably 4-(dimethylamino)benzoic acid-2-ethylhexyl ester, 4-(dimethylamino)benzoic acid-2-octyl ester, and 4-(dimethylamino)benzoic acid amyl ester;

· esters of cinnamic acid, preferably 4-methoxycinnamic acid-2-ethylhexyl ester, 4methoxycinnamîc acid propyl ester, 4-methoxycinnamic acid isoamyl ester, and 2cyano-3,3-phenylcinnamic acid-2-ethylhexyl ester (octocrylene);

• esters of salicylic acid, preferably salicylic acîd-2-ethylhexyl ester, salicylic acid-4isopropyl benzyl ester, and salicylic acid homomenthyl ester;

· benzophenone dérivatives, preferably 2-hydroxy-4-methoxybenzophenone, 2hydroxy-4-methoxy-4'-methylbenzophenone, and 2,2'-dihydroxy-4-methoxybenzophenone;

• esters of benzylmalonic acid, preferably 4-methoxybenzylmalonic acid di-2-ethylhexyl ester;

• triazine dérivatives such as 2,4,6-trianilino-(p-carbo-2'-ethyl·Γ-hexyloxy)-l,3,5triazine and octyl triazone or dioctyl butamidotriazone (Uvasorb® HEB);

· propane- 1,3-diones such as l-(4-tert-butylphenyl)-3-(4'-methoxyphenyl)propane-l,3dione; and • ketotricyclo (5.2.1.0) decane dérivatives.

[0025] Examples of suitable water-soluble substances include:

• 2-phenylbenzimidazole-5-sulfonic acid and alkali, alkaline earth, ammonium, alkylammonium, alkanolammonium, and glucammonium salts thereof;

• lH-benzimidazole-4,6-disulfomc acid, 2,2'-(l,4-phenylene)bis-disodium sait (Neo Heliopan® AP);

• sulfonic acid dérivatives of benzophenones, preferably 2-hydroxy-4methoxybenzophenone-5-sulfonic acid and salts thereof;

· sulfonic acid dérivatives of 3-benzylidene camphor such as 4-(2-oxo-3-bornylidene methyljbenzene sulfonic acid, 2-methyl-5-(2-oxo-3-bornylidene)sulfonic acid, and salts thereof.

[0026] Typical examples of particularly suitable UV-A filters include benzoyl methane dérivatives such as l-(4'-tert-butylphenyl)-3-(4'-methoxyphenyl)propane-l,3-dione, 4-tert20 butyl-4'-methoxy-dibenzoyl methane (Parsol® 1789), 2-(4-diethylamino-2-hydroxybenzoyl)benzoic acid hexyl ester (Uvinul® A Plus), l-phenyl-3-(4'-isopropylphenyl)-propane-l,3dione, as well as enamine compounds. Of course, the UV-A and UV-B filters can also be used in mixtures. Particularly suitable combinations consist of benzoyl methane dérivatives such as 4-tert-butyl-4'-methoxydibenzoyl methane (Parsol® 1789) and 2-cyano-3,325 phenylcinnamic acid-2-ethyl-hexyl ester (octocrylene) in combination with esters of cinnamic acid, preferably 4-methoxycinnamic acid-2-ethylhexyl ester and/or 4-methoxycinnamic acid propyl ester and/or 4-methoxycinnamic acid-isoamyl ester. Such combinations hâve been advantageous combined with water-soluble filters such as 2-phenylbenzimidazole-5-sulfonic acid and alkali, alkaline earth, ammonium, alkylammonium, alkanolammonium, and 30 glucammonium salts thereof.

[0027] In a preferred embodiment the (cosmetic or pharmaceutical) préparation of the présent invention comprises at least an additional UV absorbing substance selected from the group consisting of:

• 3-(4'-trimethylammonium)benzylidenebornan-2-one methyl sulphate · homomenthyl salicylate (Neo Heliopan®HMS) • terephthalylidenedibornanesulphonic acid and salts (Mexoryl®SX) • 3-{4'-suipho)benzylidenebornan-2-one and salts • 2-ethylhexyl 2-cyano-3,3-diphenylacrylate (Neo Heliopan®303) • N-[(2 and 4)-[2-(oxoborn-3-ylidene)methyl]benzyl]acrylamide polymer • 2-ethylhexyl p-methoxycinnamate (Neo Heliopan®AV) • ethyl p-aminobenzoate (25 mol) ethoxylated • isoamyl p-methoxycinnamate (Neo Heliopan®E1000) • 2-phenylbenzimidazole sulfonic acid (Neo Heliopan® Hydro) and its salts • 2,4,6-trianilino(p-carbo-2'-ethylhexyl-r-oxy)-l,3,5-triazine (Uvinul®T150) • phénol,2-(2H-benzotriazol-2-yl)-4-methyl-6-(2-methyl-3(l,3,3,3-tetramethyl-l(trimethylsilyl)oxy)disiloxyanyl)propyl), (Mexoryl®XL) • 4,4'-[(6-[4-(l,l-dimethyl)aminocarbonyl)phenylamino]-l,3,5-triazin-2,4-diyl)diimino]bis(benzoic acid 2-ethylhexyl ester), (Uvasorb® HEB) » 3-(4'-methylbenzylidene)-d,l-camphor (Neo Helipan®MBC) • 2-ethylhexyl salicylate (Neo Helipan®OS) • 2-ethylhexyl 4-dimethylaminobenzoate (Padimate O) • 4-hydroxy-4-methoxybenzophenone - 5-sulfonate (Benzophenone-4, Sulisobenzone) and its salts, • benzylidenemalonate-polysiloxane (Parsol®SLX) • menthyl anthranilate (Neo Heliopan®MA) or mixtures thereof.

[0028] In a preferred embodiment, the (cosmetic or pharmaceutical) préparation of the présent invention comprises resorcinol dérivatives of formula (I), respectively (II) and one, two, three or more UV fîlters, especially preferred hereby is the combination with 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol with the said UV filters, most preferred is phenylethyl resorcinol.

[0029] In a more preferred embodiment the préparation comprises 0.05 wt.% to 0.5 wt.% phenylethyl resorcinol and 0.5 wt.% to 40 wt.% UV filters, and 0.001 wt.% to 98 wt.% additives, wherein ail components sum up to 100 wt.%, based on the total amount of the composition.

[0030] LIGHT PROTECTION PIGMENTS

[0031] In addition to the above-mentioned soluble substances, insoluble light protection pigments, specifically finely-dispersed métal oxides or salts, are also suitable for this purpose. Examples of particuiarly suitable métal oxides are zinc oxide and titanium dioxide, as well as iron, zirconium, silicon, manganèse, aluminum, and cérium oxides and mixtures thereof. Silicates (talc), barium sulfate, or zinc stéarate can be used as examples of suitable salts. The oxides and salts are used in the form of pigments for skin care and skin protection émulsions and décorative cosmetics. In this case, the particles should hâve an average diameter of less than 100 nm, preferably 5 to 50 nm, and particuiarly preferably 15 to 30 nm. They can be spherical in shape, but particles can also be used that are ellipsoid or whose shape is other than spherical The pigments may also be surface-treated, i.e. in a hydrophilized or hydrophobized form. Typical examples are coated titanium dioxides such as titanium dioxide T 805 (Degussa), Eusolex® T2000, Eusolex® T, Eusolex® T-ECO, Eusolex® T-S, Eusolex® T-Aqua, Eusolex® T-45D (ail Merck), and Uvinul TiOz (BASF). Examples of suitable hydrophobie coating agents in this case are primarily silicones, particularly trialkoxyoctyl silane or simethicone. So-called micro- or nanopigments are preferably used in sun 5 protection agents. Micronized zinc oxides such as Z-COTE® or Z-COTE HP1® are preferably used.

[0032] ln a preferred embodiment the light protection pigment is selected from microfine titanium dioxide, Zinc oxide, Microfine zinc oxide. When titanium dioxide is chosen as the light protection pigment, it is advantageous that its total amount ranges from 0.1% to 10.0 10 wt.% of the formulation. When Zinc Oxide is chosen as the light protection pigment it is advantageous that its total amount ranges from 0.1 wt.% to 10.0 wt.% of the formulation and when one or more triazine organic pigment(s) are chosen it is advantageous that its total amount ranges from 0.1% to 10.0 wt.% based on the total amount of the formulation

[0033] In a preferred embodiment, the médicament of the présent invention further 15 comprises at least one skin lightening agent, which is preferably sclareolide.

[0034] The combination of resorcinol dérivatives of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol with skin lightening agent(s) and/or UV filters provide synergistically improved prévention, treatment and/or amelioration of hyperpigmentation and thus 20 improve the performance of resorcinol dérivatives of formula (I), respectively (II), preferably

4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol and conventional skin lightening agents in an unexpected manner, particularly for radiations in the range from 280 nm to 750 nm, particularly for radiations which lie within the visible light wavelengths from 380 nm to 750 nm.

[0035] SKIN LIGHTING AGENTS

[0036] Suitable skin lightening agents for the purposes of the présent invention encompasses sclareolide, kojic acid dérivatives, preferably kojic acid dipalmitate, arbutin, ascorbic acid, ascorbic acid dérivatives, preferably magnésium ascorbyl phosphate, hydroquinone, hydroquinone dérivatives, cyclohexylcarbamates (preferably one or more 30 cyclohexyl carbamates disclosed in WO 2010/122178 and WO 2010/097480), sulfurcontaining molécules, preferably glutathione or cysteine, alpha-hydroxy acids (preferably citric acid, lactic acid, malic acid), salts and esters thereof, N-acetyl tyrosine and dérivatives, undecenoyl phenylalanine, gluconic acid, chromone dérivatives, preferably aloesin, flavonoids, 1-aminoethyl phosphinic acid, thiourea dérivatives, ellagic acid, nicotinamide 35 (niacinamide), zinc salts, preferably zinc chloride or zinc gluconate, thujaplicin and dérivatives, triterpenes, preferably maslinic acid, sterols, preferably ergosterol, benzofuranones, preferably senkyunolide, vinyl guiacol, ethyl guiacol, dionic acids, preferably octodecene dionic acid and/or azelaic acid, inhibitors of nitrogen oxide synthesis, preferably L-nitroarginine and dérivatives thereof, 2,7-dinitroindazole orthiocitrulline, métal 40 chelators (preferably alpha-hydroxy fatty acids, phytic acid, humic acid, bile acid, bile extracts, EDTA, EGTA and dérivatives thereof), retinoids, soy milk and extract, serine protease inhibitors or lipoic acid or other synthetic or natural active ingrédients for skin and haïr lightening, the latter preferably used in the form of an extract from plants, preferably bearberry extract, rice extract, papaya extract, turmeric extract, mulberry extract, 45 bengkoang extract, nutgrass extract, liquorice root extract or constituants concentrated or isolated therefrom, preferably glabridin or licochalcone A, artocarpus extract, extract of rumex and ramulus species, extracts of pine species (pinus), extracts of vitis species or stilbene dérivatives isolated or concentrated therefrom, saxifrage extract, scutelleria extract, grape extract and/or microalgae extract, in particular Tetraselmis suecica Extract.

[0037] Preferred skin lightening agents are sclareolide and kojic acid, beta- and alphaarbutin, hydroquinone, nicotinamide, dioic acid, Mg ascorbyl phosphate and vitamin C and its dérivatives, mulberry extract, Bengkoang extract, papaya extract, turmeric extract, nutgrass extract, licorice extract (containing glycyrrhizin), alpha-hydroxy-acids, 4alkylresorcinols, 4-hydroxyanisole, larixol.

[0038] Particularly preferred is a combination of resorcinol dérivatives of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) with carnosine and/or sclareolide and/or ginger root CO2 extract, which showed the strongest synergistic inhibitory activity towards melanin formation in mélanocytes. The ratio of carnosine or sclareolide or 15 ginger root CO2 extracand phenylethyl resorcinol is preferably from 10:90 to 80:20, more preferred from 20:80 to 50:50. Preferably, in case of a mixture of sclareolide, phenylethyl resorcinol (SymWhite 377®) and ginger root CO2 extract, the ratio of the ginger root CO2 extract to phenylethyl resorcinol is from 10:90 to 80:20, preferably 20:80 to 50:50, in which the synergistic inhibitory activity towards melanin formation in mélanocytes is strong.

Preferred are also préparations comprising resorcinol dérivatives of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) and sclareolide and UV filters.

[0039] SCLAREOLIDE

[0040] Sclareolide (CAS Number 564-20-5)

is a compound prepared by chemical modification or by biotransformation of the labdan type diterpene sclareol. Sclareol is présent in stems, leaves and flowering parts of clary sage 30 (Salvia sclarea L.) and its isolation from this source has been described (US 3,060,172).

According to the présent invention, the source of sclareolide can be derived (extracted) naturally from either species of the Salvia genus, or can be synthetically obtained as substantially pure sclareolide. The substantially pure sclareolide contains according to the présent invention more than 70 percent sclareolide.

[0041] Synonyms for Sclareolide are (3aR,5aS,9aS,9bR)-decahydro- 3a,6,6,9a-tetramethylnaphtha[2,l-b]furan-2(lH)-one; 3a,4,5,5aa,6,7,8,9,9a,9ba- decahydro-3ap,6,6,9aptetramethyl- naphtho[2,l-b]furan-2(lH)-one; [3aR-(3aa,5aB,9aa,9bp)]- decahydro-3a,6,6,9atetramethyl- Naphtho[2,l-b]furan-2(lH)-one; Norambreinolide; (+)-Norambretnolide; (+)5 Sclareolide, (R)-(+)-Sclareolide; 13,14,15,16-Tetranorlabdano-8a,12-lactone;

Norambreinolid.

[0042] Sclareolide is a precursor of ambroxan, a valuable ambergris fragrance used in perfumery. But as sclareolide is used itself as a fragrance material it is often a component of cosmetic formulations.

[0043] The anti-inflammatory activity of sdareol and sclareolide is described in WO 200

230385 A2 (Henkel). The anti-inflammatory activity is proven by an inhibition of 5lipoxygenase as well as cyclooxygenase-1 activity. The use of Sclareolide within a natural combination of five components to treat acné is given in US 2003 ΖΊΉΊΊ (Color Access). The anti-microbial activity of inter alia sclareolide and sclareol is already described in WO 1999

063978 Al (Reynolds) concluding that sclareolide and sclareol are useful to treat acné, dermatitis and indésirable body odour. In WO 2001 074327 A2 (Color Access) the use of inter alia sclareolide as cell différentiation enhancer is disclosed. According to this patent the différentiation enhancers like sclareolide are used to stimulate the production of lipids from epidermal cells, and concurrently increase the lipid content of the barrier. As a use of the described compositions the enhancement and prolongation of self-tanning products is mentioned. Again the strengthening of barrier by the use of sclareolide alone as well as combined with white birch extract is described in WO 2002060381 A2 (Color Access). The use of sclareolide in cosmetic formulations used to enhance the stratum corneum function is described in US 2010 247692 Al (Color Access). The invention WO 2008 155048 Al (Cognis) discloses cosmetic compositions comprising sclareolide alone or combined with hesperidin methyl chalcone. The cosmetic compositions are described to be used for the tanning of skin, the darkening of hair, or the preventing of greying of hair.

[0044] GINGER ROOT CO2 EXTRACT

[0045] Ginger root extracts with a high content of pungent components are well-known for the flavouring of food and beverages. The characterization of ginger root extracts by HPLC, GC and other analytical methods is well-described. The quantification of pungent components like gingerols, shogaols and zingerone is good laboratory practice. But ginger extracts characterized by a high content of pungent components of 42 - 50 % b.w. hâve not 35 been described for cosmetic applications before.

[0046] The water and/or éthanol and/or water/ethanol extracts of ginger root of unknown composition are described as anti-oxidants and anti-aging agents and are often disclosed as the preferred extracts for these applications. The use of these extracts is described inter alia in JP 2009 073777 Al for the improvement of wrinkles, in JP 2000 319189 Al as elastase 40 inhibitors, by Fujimura et al. (Fragrance Journal (2002), 30(6), 38-42) for wrinkle improvement by inhibition of elastase activity. In JP 2007008847 the claimed extract was prepared with 20% éthanol resulting in the concentration of fructosyl dipeptides as active principles.

[0047] For the application to hair and scalp ginger tincture, ginger juice and the above mentioned water and/or éthanol and/or water/ethanol extracts of ginger root are wellknown. As activities for these extracts on hair and scalp inter alia enhanced microcirculation is described. For example, CN 102451128 Al suggests a shampoo claimed to prevent hair loss contains 5% ginger juice. JP 63 091315 Al describes microcirculation enhancing ginger juice in shampoo formations for hair growth stimulation. EP 1281402 81 (Kao) refers to a ginger extract substantially free of gingerols for hair growth inhibition.

[0048] Ginger oil was used as a soothing, relaxing or warming agent in cosmetic formulations in WO 2009 087578 Al (Foamix). But the document did not disclose the composition of the ginger oil. The essential oil of ginger is known for a strong pungent smell and taste due to the volatile constituents and is not comparable to the ginger pungent extract according to the present invention.

[0049] The isolation of the pungent components of ginger is described in different documents. Fickeret al. (Phytotherapy Research (2003), 17(8), 897-902) evaluated the antifungal activity of ginger constituents.

[0050] The évaluation of anti-inflammatory activity of pungent components of ginger was given in different documents, inter alia by Lantz et al. (Phytomedicine (2007), 14(2-3), 123128). Additionally the anti-tumour activity and prolifération inhibitory activity on tumour cells were evaluated by different groups, inter alia by Sang et al. (Journal of Agricultural and Food Chemistry (2009), 57(22), 10645-10650).

[0051] In CN 1840162 Al a ginger root CO2 extract is described without specifying the content of pungent components like gingerols and shogaols. The extract is disclosed as an anti-inflammatory extract. Application examples are tablets, pills and capsules for oral consumption. Examples for topical application on skin are not described.

[0052] Ginger root CO2 extracts that are particularly preferred in combination with resorcinol dérivatives of formula (I), respectîvely (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) in the sense of the present invention contain

(a)	15 to 30	% b.w. [6]-gingerol
(b)	3 to 10	% b.w. [8]-gingero1
(c)	3 to 10	% b.w. [10]-gingerol
(d)	0.5 to 4	% b.w. [6]-shogaol
(e)	0.03 to 1.3	% b.w. [8]-shogaol;
(f)	0.03 to 1	% b.w. [10]-shogaol;
(g)	0.01 to 1	% b.w. zingerone,

on condition that the amount of gingerols sums up to 24 to 50 % b.w. and the amount of shogaols sums up to 0.516 % b.w.

[0053] A first preferred ginger root CO2 extract comprises (a) 25 to 30 % b.w. [6]-gingerol (b) 5 to 10 % b.w. [8]-gingerol (c) 5 to 10 (d) 1.5 to 4 (e) 0.3 to 1.3 % b.w. [10]-gingerol % b.w. [6]-shogaol % b.w. [8]-shogaol;

(f) 0.03 to 1 % b.w. [10]-shogaol;

(g) 0.01 to 1 % b.w. zingerone, on condition that the amount of gingerols sums up to 35 to 50 % b.w. and the amount of shogaols sums up to 1.5 t 6 % b.w. Extracts of this kind are subject to EP 2772245 Al (SYMRISE) which is hereby incorporated by reference with regard to the nature of the extracts and the manner how to obtain them. The product is obtainable under the 10 trademark SymVital® AgeRepair 3040 from Symrise AG, Holzminden (DE).

[0054] A second preferred ginger root CO2 extract comprises
(a)	15 to 25	% b.w. [6]-gingerol
(b)	3 to 5	% b.w. [8]-gingerol
(c)	3to8	% b.w. [10]-gingerol
(d)	0.5 to 3	% b.w. [6]-shogaol
(e)	0.03 to 1	% b.w. [8]-shogaol;
(f)	0.03 to 1	% b.w. [10]-shogaol;
(g)	0.01 to 1	% b.w. zingerone,

on condition that the amount of gingerols sums up to 24 to 35 % b.w. and the amount of 20 shogaols sums up to 0.5 to 5 % b.w.

[0055] CARRIERS

[0056] Both the médicaments and the cosmetic préparations described in the following can contain as component (c) carriers or solvents that are selected from the group selected 25 consisting of water, alcohols, esters, butylène glycol, dipropylene glycol, pentylene glycol,

1,2-hexane diol, caprylyl glycol, decylene glycol, éthanol, ethoxydiglycol, ethyl acetate, glycerol, propanol, isopropanol, macrogols, propyl propylene glycol(2) methyl ether, propyl propylene glycol(3) methyl ether, propylene carbonate, propylene glycol, triethylene glycol, isoparaffin, amyl acetate, amyl benzoate, benzyl acetate, butyl acetate, butylène glycol, 30 butyl lactate, butooctyl benzoate, butooctyl salicylate, C10-C13 alkanes, C14-C17 alkanes,

C11-C15 cycloalkanes, caprylyl butyrate, isoparaffins, diacetin, triacetin dicaprylyl ether, dicaprylyl maleate, and mixtures thereof. Most preferred are glycerol, propylene glycol, butylène glycol, dipropylene glycol, pentylene glycol, 1,2-hexane diol, caprylyl glycol, decylene glycolas compound c) of a médicament préparation of the present invention.

[0057] The matter of the present invention lies on the boundary area between médicaments and cosmetics, particularly as a sun protection agent. Therefore, in the following médicament as well as cosmetic préparations are described.

[0058] MEDICAMENT

[0059] A preferred médicament of the present invention comprises, consists or essentially consists of:

(a) from 0.01 wt.% to 10 wt.%, preferably from 0.02 wt.% to 2 wt.%, particularly preferably from 0.05 wt.% to 1 wt% at least one resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) or a pharmaceutically acceptable sait of resorcinol dérivatives of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol, (b) and at least one compound selected from (bl), (b2) and (b3):

(bl) from 0.05 wt.% to 60 wt.%, preferably 0.1 to 50 wt.%, particularly preferably 0.5 wt.% to 40 wt% of UV filters, (b2) from 0.005 wt.% to 20 wt.%, preferably 0.01 wt.% to 10 wt.% of skin lightening agents, (b3) from 0.0001 wt.% to 30 wt.%, preferably 0.01 wt.% to 10 wt.% of antioxidants, and optionally (c) from 0.2 wt.% to 99 wt.%, preferably from 0.5 wt.% to 20 wt.%, particularly preferably from 1 wt.% to 10 wt.% of carriers, and/or (d) 0.1 wt.% to 90 wt.% further additives, wherein the weight percents ofthe compounds a) to d) are based on the total amount ofthe préparation and the sum of ail compounds add to 100 wt.%.

[0060] The médicament according to the invention preferably contains, respectively essentially consists of components (a) and (bl) in a weight ratio of 0.02:99.98 to 99.5:0.5, particularly 0.04:99.96 to 95:5, and particularly preferably 0.2:99.8 to 75:25. The synergistic effect is most pronounced when the two components are used in a weight ratio of 1:80.

[0061] The médicaments according to the invention preferably contain, respectively essentially consist of components (a) and (b2) in a weight ratio of 0.05:99.95 to 99.95:0.05, and particularly preferably 1:99 to 99:1. The synergistic effect is most pronounced when the two components are used in a weight ratio of 5:1 to 1:5.

[0062] The médicaments according to the invention preferably contain, respectively essentially consist of components (a) and (b3) in a weight ratio of 0.05:99.95 to 99.95:0.05, and particularly preferably 1:99 to 99:1. The synergistic effect is most pronounced when the two components are used in a weight ratio of 5:1 to 1:5.

[0063] Preference is made to a médicament comprising or consisting of or essentially consisting of:

(a) from 0.01 wt.% to 10 wt.%, preferably from 0.02 wt.% to 2 wt.%, particularly preferably from 0.05 wt.% to 1 wt% of at least one resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) or a pharmaceutically acceptable sait of resorcinol dérivatives of formula (I), respectively

(II), preferabiy 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol, and (bl) from 0.05 wt.% to 60 wt.%, preferabiy 0.1 to 50 wt.%, and particularly preferabiy 0.5 wt.% to 40 wt% of UV filters, and (b3) from 0.0001 wt.% to 30 wt.%, preferabiy 0.01 wt.% to 10 wt.% of antioxidants, and (c) from 0.2 wt.% to 99 wt.%, preferabiy from 0.5 wt.% to 20 wt.%, and particularly preferabiy from 1 wt.% to 10 wt.% of carriers selected from the group composed of water, alcohols, esters, butylène glycol, dipropylene glycol, éthanol, ethoxydiglycol, ethyl acetate, glycerol, propanol, isopropanol, macrogols, propyl propylene glycol(2) methyl ether, propyl propylene glycol(3) methyl ether, propylene carbonate, propylene glycol, triethylene glycol, isoparaffin, amyl acetate, amyl benzoate, benzyl acetate, butyl acetate, butylène glycol, butyl lactate, butooctyl benzoate, butooctylsalicylate, C10-C13 alkanes, C14-C17 alkanes, C11-C15 cycloalkanes, caprylyl butyrate, isoparaffins, diacetin, triacetin dicaprylyl ether, dicaprylyl maleate, and 15 mixtures thereof, most preferred are glycerol, propylene glycol, butylène glycol, dipropylene glycol, pentylene glycol, 1,2-hexane diol, caprylyl glycol, decylene glycole, and mixtures thereof, and (d) 0.1 to 90 wt.% further additives, wherein the weight percents ofthe compounds a) to d) are based on the total amount ofthe préparation and the sum of ail compounds add to 100 wt.%.

[0064] A further preferred médicament comprises or consists of or essentially consists of:

(a) from 0.01 wt.% to 10 wt.%, preferabiy from 0.02 wt.% to 2 wt.%, particularly preferabiy from 0.05 wt.% to 1 wt% of at least one resorcinol dérivative of formula (I), 25 respectively (II), preferabiy 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) or a pharmaceutically acceptable sait of resorcinol dérivatives of formula (I), respectively (II), preferabiy 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol, and (bl) from 0.05 wt.% to 60 wt.%, preferabiy 0.1 to 50 wt.%, and particularly preferabiy 0.5 wt.% to 40 wt% of UV filters, and (b2) from 0.005 wt.% to 20 wt.%, preferabiy from 0.01 wt.% to 10 wt.% of skin lightening agents, and (c) from 0.2 wt.% to 99 wt.%, preferabiy from 0.5 wt.% to 20 wt.%, and particularly 35 prefera-bly from 1 wt.% to 10 wt.% of carriers selected from the group composed of wa-ter, alco-hols, esters, butylène glycol, dipropylene glycol, éthanol, ethoxydiglycol, ethyl ace-tate, glycerol, propanol, isopropanol, macrogols, propyl propylene glycol(2) methyl ether, propyl propylene glycol(3) -methyl ether, propylene carbonate, propylene glycol, triethylene glycol, isoparaffin, amyl acetate, amyl benzoate, benzyl 40 acetate, butyl acetate, butylène glycol, butyl lactate, butooctyl benzoate, butooctylsalicylate, C10-C13 alkanes, C14-C17 al-kanes, C11-C15 cycloalkanes, caprylyl butyrate, isoparaffins, diacetin, triacetin dicaprylyl ether, dicaprylyl maleate, and mixtures thereof, most preferred are glycerol, propylene glycol, butylène glycol, dipropylene glycol, pentylene glycol, 1,2-hexane diol, caprylyl glycol, decylene glycole, and mixtures thereof, and (d) 0.1 to 90 wt.% further additives, wherein the weight percent of the compounds a) to d) are based on the total amount of the préparation and the sum of ail compounds add to 100 wt.%.

[0065] A further preferred médicament comprises or consists of or essentially consists of:

(a) from 0.01 wt.% to 10 wt.%, preferably from 0.02 wt.% to 2 wt.%, particularly preferably from 0.05 wt.% to 1 wt% of at least one resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) or a pharmaceutically acceptable sait of resorcinol dérivatives of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol, and (bl) from 0.05 wt.% to 60 wt.%, preferably 0.1 to 50 wt.%, and particularly preferably 0.5 wt.% to 40 wt% of UV filters, wherein the UV filters are UV absorbing substances selected from the group consisting of:

• 3-(4'-trimethylammonium)benzylidenebornan-2-one methyl sulphate • homomenthyl salicylate (Neo Heliopan®HMS) • terephthalylidenedibornanesulphonic acid and salts (Mexoryl®SX) • 3-(4’-sulpho)benzylidenebornan-2-one and salts • 2-ethylhexyl 2-cyano-3,3-diphenylacrylate (Neo Heliopan®303) • N-[(2 and 4)-[2-(oxoborn-3-ylidene)methyl]benzyl]acrylamide polymer • 2-ethylhexyl p-methoxycinnamate (Neo Heliopan®AV) • ethyl p-aminobenzoate (25 mol) ethoxylated • isoamyl p-methoxycinnamate (Neo Heliopan®E1000) • 2-phenylbenzimidazole sulfonic acid (Neo Heliopan® Hydro) and its salts • 2,4,6-trianilino(p-carbo-2^,-ethylhexyl-l'-oxy)-l,3,5-triazine (llvinul®T150) • phénol, 2-(2H-benzotriazol-2-yl)-4-methyl-6-(2-methyl-3(l, 3,3,3-tetramethyl-l(trimethylsilyl)oxy)disiloxyanyl)propyl), (Mexoryl®XL) • 4,4'-[(6-[4-(l,l-dimethyl)aminocarbonyl)phenylamino]-l,3,5-triazin-2,4-diyl)diimino]bis(benzoic acid 2-ethylhexyl ester), (Uvasorb® HEB) • 3-(4'-methylbenzylidene)-d, l-camphor (Neo Helipan®MBC) • 2-ethylhexyl salicylate (Neo Helipan®OS) • 2-ethylhexyl 4-dimethylaminobenzoate (Padimate O) • 4-hydroxy-4-methoxybenzophenone-5-sulfonate (Benzophenone-4,

Sulisobenzone) and its salts, • benzylidenemalonate-polysiloxane(Parsol®SLX) • menthyl anthranilate (Neo Heliopan®MA), and (b2) from 0.005 wt.% to 20 wt.%, preferably from 0.01 wt.% to 10 wt.% of skin lightening agents, preferably selected from kojic acid, beta- and alpha-arbutin, hydroquinone, nicotinamide, dioic acid, Mg ascorbyl phosphate and vitamin C and its dérivatives, mulberry extract, Bengkoang extract, papaya extract, turmeric extract, nutgrass extract, licorice extract (containing glycyrrhizin), alpha-hydroxy-acids, 4alkylresorcinols, 4-hydroxyanisole, sclareolide, larixol; most preferred is sclareolide, (b3) from 0.0001 wt.% to 30 wt.%, preferably 0.01 wt.% to 10 wt.% of antioxidants, preferably selected from amino acids (such as glycine, histidine, tyrosine, tryptophan), imidazoles (such as urocanic acid), carotenoids, carotènes (such as α-carotene, βcarotene, lycopene), chlorogenic acids, liponic acids (such as dihydroliponic acid), aurothioglucose, propylthiouracil and other thiols (such as thioredoxin, glutathione, cysteine, cystine, cystamine and glycosyls thereof, N-acetyl, methyl, ethyl, propyl, amyl, butyl and lauryl, palmitoyl, oleyl , γ-linoleyl , cholesteryl and glyceryl esters), , dilauryl thiodipropionate, distearyl thiodipropionate, thiodipropionic acids and dérivatives thereof (esters, ethers, peptides, Itpids, nucléotides, nucleosides and salts), as well as sulfoximine compounds (such as buthionine sulfoximine, homocystéine sulfoximine, buthionine sulfone, penta, hexa, heptathionine sulfoximine), as well as (métal) chelators (such as α-hydroxy fatty acids, palmitic acid, phytic acid, and lactoferrin), α-hydroxy acids (such as citrie acid, lactic acid, and malic acid), humic acid, gallic acid, gall extracts, bilirubin, biliverdin, EDTA, EGTA and dérivatives thereof, unsaturated fatty acids (such as γ-linolenic acid, linoleic acid, and oleic acid), folie acid and dérivatives thereof, ubiquinone, ubiquinol and dérivatives thereof, Vitamin C and dérivatives thereof (such as ascorbyl palmitate, Mg ascorbyl phosphate, ascorbyl acetate), tocopherols and dérivatives thereof (such as Vitamin E acetate), Vitamin A and dérivatives thereof (vitamin A palmitate), as well as coniferyl benzoate of benzoin, rutic acid and dérivatives thereof, α-glycosylrutin, ferulic acid, furfurylidene glucitol, carnosine, butyl hydroxytoluene, butyl hydroxyanisole, nordihydroguaiac resin acid, nordihydroguaiaretic acid, trihydroxybutyrophenone, uric acid and dérivatives thereof, [6]-Paradol (INCI: Hydroxymethoxyphenyl Decanone), carnosine, L-carnosine, Dcarnosine, D/L-carnosine, carcinine, carcinine*HCl (INCI: decarboxy carnosine* HCl), anserine, D-anserine, L-anserine, as well as L-anserine*HNO3 and mixtures thereof; and (c) from 0.2 wt.% to 99 wt.%, preferably from 0.5 wt.% to 20 wt.%, and particularly preferably from 1 wt.% to 10 wt.% of carriers selected from the group consisting of water, alco-hols, esters, butylène glycol, dipropylene glycol, éthanol, ethoxydiglycol, ethyl acetate, glycerol, propanol, isopropanol, macrogols, propyl propylene glycoi(2) methyl ether, propyl propylene glycol(3) methyl ether, propylene carbonate, propylene glycol, triethylene glycol, isoparaffin, amyl acetate, amyl benzoate, benzyl acetate, butyl acetate, butylène glycol, butyl lactate, butooctyl benzoate, butooctylsalicylate, C10-C13 alkanes, C14-C17 alkanes, C11-C15 cycloalkanes, caprylyl butyrate, isoparaffins, diacetin, triacetin dicaprylyl ether, dicaprylyl maleate, and mixtures thereof, most preferred are glycerol, propylene glycol, butylène glycol,

dipropylene glycol, pentylene glycol, 1,2-hexane diol, caprylyl glycol, decylene glycole, and mixtures thereof; and (d) 0.1 to 90 wt.% further additives, wherein the weight percent ofthe compounds a) to d) are based on the total amount ofthe 5 préparation and the sum of ail compounds add to 100 wt.%.

[0066] A further preferred médicament comprises or consists of or essentially consists of:

(a) from 0.01 wt.% to 10 wt.%, preferably from 0.02 wt.% to 2 wt.%, and particularly preferably from 0.05 wt.% to 1 wt% of at least one resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl 10 resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) or a pharmaceutically acceptable sait of resorcinol dérivatives of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol, and (bl) from 0.05 wt.% to 60 wt.%, preferably 0.1 to 50 wt.%, and particulariy preferably 0.5 15 wt.% to 40 wt% of UV filters, wherein the UV filters are UV absorbing substances selected from the group consisting of:

• 3-(4^l-trimethylammonium)benzylidenebornan-2-one methyl sulphate • homomenthyl salicylate (Neo Heliopan®HMS) • terephthalylidenedibornanesulphonic acid and salts (Mexoryl®SX) · 3-(4'-sulpho)benzylidenebornan-2-one and salts • 2-ethylhexyl 2-cyano-3,3-diphenylacrylate (Neo Heliopan®303) • N-[(2 and 4)-[2-(oxoborn-3-vlidene)methyl]benzyl]acrylamide polymer • 2-ethylhexyl p-methoxycinnamate (Neo Heliopan®AV) • ethyl p-aminobenzoate (25 mol) ethoxylated · isoamyl p-methoxycinnamate (Neo Heliopan®E1000) • 2-phenylbenzimidazole sulfonic acid (Neo Heliopan® Hydro) and its salts • 2,4,6-trianilino(p-carbo-2'-ethylhexyl-l'-oxy)-l,3,5-triazine (Uvinul®T150) • phénol, 2-(2H-benzotriazol-2-yl)-4-methyl-6-(2-methyl-3(l, 3,3,3-tetramethyl-l(trimethylsilyl)oxy)disiloxyanyl)propyl), (Mexoryl®XL) · 4,4'-[(6-[4-(l,l-dimethyl)aminocarbonyl)phenylamino]-l,3,5-triazin-2,4-diyl)diimino]bis(benzoic acid 2-ethylhexyl ester), (Uvasorb® HEB) • 3-(4'-methylbenzylidene)-d,l-camphor (Neo Helipan®IVIBC) • 2-ethylhexyl salicylate (Neo Helipan®OS) • 2-ethylhexyl 4-dimethylaminobenzoate (Padimate O) · 4-hydroxy-4-methoxybenzophenone-5-sulfonate (Benzophenone-4,

Sulisobenzone) and its salts, benzylidenemalonate-polysiloxane(Parsol®SLX) • menthyl anthranilate (Neo Heliopan®MA), and (b2) from 0.005 wt.% to 20 wt.%, preferably from 0.01 wt.% to 10 wt.% of skin lightening agents, preferably selected from kojic acid, , beta- and alpha-arbutin, hydroquinone, nicotinamide, dioic acid, Mg ascorbyl phosphate and vitamin C and its dérivatives, mulberry extract, Bengkoang extract, papaya extract, turmeric extract, nutgrass extract, licorice extract (containing glycyrrhizin), alpha-hydroxy-acids, 4alkylresorcinols, 4-hydroxyanisole, sdareolide, larixol; most preferred is sclareolide; and (b3) from 0.0001 wt.% to 30 wt.%, preferably 0.01 wt.% to 10 wt.% of antioxidants, preferably selected from amino acids (such as glycine, histidine, tyrosine, tryptophan), imidazoles {such as urocanic acid), carotenoids, carotènes (such as α-carotene, βcarotene, lycopene), chlorogenic acids, liponic acids (such as dihydroliponic acid), aurothioglucose, propylthiouracil, dilauryl thiodipropionate, distearyl thiodipropionate, thiodipropionic acids and dérivatives thereof (esters, ethers, peptides, lipids, nucléotides, nucleosides and salts), as well as sulfoximine compounds (such as buthionine sulfoximine, homocystéine sulfoximine, buthionine sulfone, penta, hexa, heptathionine sulfoximine), citric acid, lactic acid, and malle acid), humic acid, gallic acid, gall extracts, bilirubin, biliverdin, EDTA, EGTA γ-linolenic acid, linoleic acid, and oleic acid, folie acid ubiquinone, ubiquinol Vitamin C ascorbyl palmitate, Mg ascorbyl phosphate, ascorbyl acetate), tocopherols Vitamin E acetate, Vitamin A, vitamin A palmitate, α-glycosylrutin, ferulic acid, furfurylidene glucitol, carnosine, butyl hydroxytoluene, butyl hydroxyanisole, nordihydroguaiac resin acid, nordihydroguaiaretic acid, trihydroxybutyrophenone, uric acid and dérivatives thereof, [6]-Paradol (1NCI: Hydroxymethoxyphenyl Decanone), carnosine, L-carnosine, Dcarnosine, D/L-carnosine, carcinine, carcinine*HCI (INCI: decarboxy carnosine* HCl), anserine, D-anserine, L-anserine, as well as L-anserine*HNO3 and mixtures thereof; and (c) from 0.2 wt.% to 99 wt.%, preferably from 0.5 wt.% to 20 wt.%, and particularly prefera-bly from 1 wt.% to 10 wt.% of carriers selected from the group consisting of water, alco-hols, esters, butylène glycol, dipropylene glycol, éthanol, ethoxydiglycol, ethyl acetate, glycerol, propanol, isopropanol, macrogols, propyl propylene glycol(2) methyl ether, propyl propylene glycol(3) methyl ether, propylene carbonate, propylene glycol, triethylene glycol, isoparaffin, amyl acetate, amyl benzoate, benzyl acetate, butyl acetate, butylène glycol, butyl lactate, butooctyl benzoate, butooctylsalicylate, C10-C13 alkanes, C14-C17 alkanes, C11-C15 cycloalkanes, caprylyl butyrate, isoparaffins, diacetin, triacetin dicaprylyl ether, dicaprylyl maleate, and mixtures thereof, most preferred are glycerol, propylene glycol, butylène glycol, dipropylene glycol, pentylene glycol, 1,2-hexane diol, caprylyl glycol, decylene glycole, and mixtures thereof, and (d) 0.05 to 5 wt.% multifunctionals, which are selected from the group consisting of 1,3propanediol, methyl propanediol, 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, 1,2decanediol, 1,5-pentanediol, 1,6-hexanediol, 1,8-octanediol, 1,2-decanediol, ethylhexylglycerin, hexoxy-propan-l,2-diol, heptoxy- propan-l,2-diol, octoxy-propan-

1,2-diol, 3-phenoxy-propan-l,2-diol, 3-benzyloxy-propan-l,2-diol, 3-phenylethyloxypropan-l,2-diol, 3-phenylpropyloxy-propan-l,2-diol, 3-methylbenzyloxy-propan-l,2- η

diol, sorbitan caprylate, triclosan, climbazole, Octopirox (l-hydroxy-4-methyl-6-(2,4,4trimethylpentyl)-2(lH)-pyridone, 2-aminoethanol), chitosan, farnesol, 2-butyloctanoic acid, 2-Benzylheptan-l-ol, glycerol monolaurate, bis(2-pyridylthio)zinc Ι,Γ-dioxide, N,N'-(decane-l,10-diyldipyridin-l-yl-4-ylidene)-dioctan-l-amine dihydrochloride 5 (octenidine dihydrochloride), thymol, eugenol, 4-isopropyl-3-methylphenol, benzyl alcohol, 2-phenyethyl alcohol, 3-phenyl propanol, 2-phenoxyethanol, 1-phenoxypropan-2-ol, 3-phenoxypropanol, benzyloxymethanol, glyceryl caprylate, glyceryl caprate, glyceryl laurate, hydroxyacetophenone, and mixtures thereof, preferably which are selected from 2-pentanediol, 1,2-hexanediol, 1,2-octanediol, 1,2-decanediol, 10 hydroxyacetophenone, and mixtures thereof, wherein the weight percents ofthe compounds a) to d) are based on the total amount ofthe préparation and the sum of ail compounds add to 100 wt.%.

[0067] Most preferred is a médicament comprising or consisting of or essentially consisting of a combination of at least one resorcinol dérivative of formula (I), respectively (II), 15 preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) with at least a further compound (bl), (b2) or (b3) which are preferably selected from ginger root CO2 extract, carnosine, Lcarnosine, D-carnosine, D/L-carnosine, carcinine, carcinine*HCI (INCI: decarboxy carnosine* HCl), anserine, D-anserine, L-anserine, as well as L-anserine*HNO3, sclareolide, larixol. 20 Preferably, two, three or more of the aforementioned compounds are present in a médicament ofthe present invention.

[0068] Most preferred is a binary mixture comprising, consisting or essentially consisting of a resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 25 377®) with ginger root CO2 extract. In such a binary mixture ginger root CO2 extract is preferably present in an amount from 5 % by weight to 80 % by weight, and phenylethyl resorcinol and phenylethyl resorcinol dérivatives preferably present in an amount from 20% by weight to 95% by weight, with the provision that ail actives add together to 100 % by weight.

[0069] Another preferred mixture is a binary mixture comprising, consisting or essentially consisting of a resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) with carnosine, wherein carnosine is preferably present in an amount from 5 % by weight to 80 % by weight, and phenylethyl resorcinol and phenylethyl resorcinol dérivatives are preferably present in an amount from 20% by weight to 95% by weight, with the provision that ail actives add together to 100 % by weight.

[0070] Another preferred mixture is a ternary mixture comprising, consisting or essentially consisting of a resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl 40 resorcinol (SymWhite 377®) with ginger root CO2 extract and sclareolide.

[0071] Preferably ginger root CO2 extract is present in an amount from 5 % by weight to 70 % by weight, wherein sclareolide is preferably present in an amount from 5 % by weight to 70 % by weight, and resorcinol dérivative of formula (I), respectively (II), preferably 4butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) is preferably présent in an amount from 10 % by weight to 90 % by weight in such a ternary mixture, with the provision that ail three compounds add together to 100% by weight.

[0072] Another preferred mixture is a ternary mixture comprising a resorcinol dérivative of 5 formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) and ginger root CO2 extract and carnosine.

[0073] Preferably ginger root CO2 extract is présent in an amount from 5 % by weight to 70 % by weight, wherein the resorcinol dérivative of formula (I), respectively (II), preferably 410 butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) is preferably présent in an amount from 10 % by weight to 90 % by weight and carnosine is preferably présent in an amount from 5 % by weight to 70 % by weight in such a ternary mixture, with the provision that ail three compounds add together to 100% by weight.

[0074] COSMETIC PREPARATIONS

[0075] A preferred cosmetic préparation ofthe présent invention comprises, consists or essentially consists of:

(a) at least a resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) or a pharmaceutically acceptable sait thereof, and at least one compound selected from (bl), (b2) and (b3):

(bl) at least one UV filters, (b2) at least one skin lightening agent, (b3) at least an antioxidant, and at least one compound selected from (cl), (c2) and (c3):

(cl) carriers, .

(c2) oil components (c3) emulsifiers, preferably for use in the treatment, prévention and/or amelioration of hyperpigmentation. [0076] In terms of the UV filters, skin lightening agents, antioxidants and carriers the aforementioned disclosure and preference under médicaments also applies here for the cosmetic préparations and use and are therefore incorporated herewith.

[0077] A preferred cosmetic préparation comprises, consists or essentially consists of (a) from 0.01 wt.% to 10 wt.%, preferably from 0.02 wt.% to 2 wt.%, and particularly preferably from 0.05 wt.% to 1 wt.% of at least one resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) or a cosmetically acceptable sait thereof;

and at least one compound selected from (bl), (b2) and (b3):

(bl) from 0.05 wt.% to 60 wt.%, preferably 0.1 to 50 wt.%, and particularly preferably 0.5 5 wt.% to 40 wt% of UV filters, (b2) from 0.005 wt.% to 20 wt.%, preferably from 0.01 wt.% to 10 wt.% of skin lightening agents, (b3) from 0.0001 wt.% to 30 wt.%, preferably 0.5 wt.% to 20 wt.% of antioxidants, and at least one compound selected from (cl), (c2) and (c3):

(cl) carriers, (c2) oil components, (c3) emulsifiers, wherein the total amount of the compounds (cl) to (c3) sum up together to be lwt.% to 50 wt.%, preferably 5 wt.% to 40wt% relative to the préparation, and wherein the total weight 15 percent of the compounds (a) to (cl to c3) are based on the total amount of the préparation and the sum of ail compounds (a), (b), (c) add to 100 wt.%.

[0078] The préparations according to the invention are preferably in the form of crearris, lotions, gels, pastes, or capsules, and particularly constitute skin care agents, sun protection agents, or haïr care agents.

[0079] It is further preferred that components (a+bl) be présent in an amount of 0.1 wt.% to 40 wt.% relative to the entire composition. In this case, the same preferred weight ratios described above apply.

[0080] It is further preferred that components (a+b2) be présent in an amount of 0.1 wt.% to 10 wt.% relative to the entire composition. In this case, the same preferred weight ratios 25 described above apply.

[0081] It is further preferred that components (a+b3) be présent in an amount of 0.05 wt.% to 10 wt.% relative to the entire composition, ln this case, the same preferred weight ratios described above apply.

[0082] The resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 30 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) is présent in the médicament, respectively cosmetic préparation of use in an active amount to reduce, retard, suppress and/or protect against sunlight induced hyperpigmentation, particularly visible light induced hyperpigmentation.

[0083] The term active amount to reduce, retard and/or suppress hyperpigmentation, 35 respectively to treat, prevent and/or ameliorate hyperpigmentation of skin area, preferably of human skin refers to a mean amount suffirent to cover the région of skin surface where a change in pigmentation is desired, particularly preferably used for radiation wavelengths in the range from 380 nm to 750 nm, more preferably from 400 nm to 700 nm in case of the visible light radiations.

[0084] In a preferred method for cosmetic and/or therapeutic réduction, retardation and/or suppression, respectively treatment, prévention and/or amelioration of hyperpigmentation , the concentration in which resorcinol dérivative of formula (I), respectively (II), preferably 4butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred 5 phenylethyl resorcinol (SymWhite 377®) is used in an active amount according to the invention is in the range from 0.01 wt.% to 10 wt.% preferably in the range from 0.02 wt.% to 2 wt.% and particularly preferentially in the range from 0.05 wt.% to 1 wt.%, in each case based on the total amount of the cosmetic or pharmaceutical product.

[0085] Most preferred is a cosmetic composition comprising a combination of resorcinol 10 dérivatives of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) with at least a further compound (bl), (b2) or (b3) which are preferably selected from ginger root CO2 extract, carnosine, L-carnosine, D-carnosine, D/L-carnosine, carcinine, carcinine*HCI (INCI: decarboxy carnosine* HCl), anserine, D-anserine, L-anserine, as well as L15 anserine*HNO3, sclareolide, larixol. Preferably two, three or more of the aforementioned compounds are présent in a cosmetic composition of the present invention.

[0086] COSMETIC AND PHARMACEUTICAL PREPARATIONS

[0087] Cosmetic and pharmaceutical préparations (médicaments) according to the present invention may include similar additives, such as for example oil bodies or emulsifiers. Therefore, the border between cosmetic and pharmaceutical préparations is in flow and it should be understood that components cited for one application are recommended for the other mutatis-mutandis without literal répétition.

[0088] The cosmetic and médicaments according may comprise typical auxiliaries and further additives as described aforementioned. Typical auxiliaries and further additives are such as mild surfactants, oil components, emulsifiers, pearlizing waxes, consistencyimparting agents, thickeners, superfatting agents, stabilizers, polymers, silicone compounds, fats, waxes, lecithins, phospholipids, moisturizers, biogenic agents, antioxidants, filmforming agents, expanding agents, insect repellents, self-tanning agents, tyrosine inhibitors (depigmenting agents), hydrotropes, solubilizers, preservatives, perfume oils, dyes and the like.

[0089] SURFACTANTS

[0090] Examples of suitable surface-active substances that may be included are anionic, 35 nonionic, cationic and/or amphoteric or zwitterionic surfactants, ordinarily contained in the agents in amounts of approx. 1 to 70, preferably 5 to 50, and particularly 10 to 30 wt%. Typical examples of anionic surfactants include soaps, alkylbenzene sulfonates, alkane sulfonates, olefin sulfonates, alkyl ether sulfonates, glycerol ether sulfonates, α-methyl ester sulfonates, sulfofatty acids, alkyl sulfates, alkylether sulfates, glycerol ether sulfates, fatty 40 acid ether sulfates, hydroxy mixed ether sulfates, monoglyceride (ether) sulfates, fatty acid amide (ether) sulfates, mono- and dialkylsulfosuccinates, mono- and dialkylsulfosuccinamates, sulfotriglycerides, amide soaps, ether carboxylic acids and salts thereof, fatty acid isethionates, fatty acid sarcosinates, fatty acid taurides, N-acylamino acids such as acyl lactylates, acyl tartrates, acyl glutamates, and acyl aspartates, alkyl oligoglycoside sulfates, protein fatty acid condensâtes (particularly wheat-based vegetable products) and alkyl(ether)phosphates. If the anionic surfactants contain polygîycol ether chains, they may show a conventional homolog distribution, but preferably a narrow-range 5 homolog distribution. Typical examples of nonionic surfactants are fatty alcohol polygîycol ethers, alkyl phénol polygîycol ethers, fatty acid polygîycol esters, fatty acid amide polygîycol ethers, fatty amine polygîycol ethers, alkoxylated triglycérides, mixed ethers or mixed formais, optionally partially oxidized alk(en)yl oligoglycosides or glucuronic acid dérivatives, fatty acid N-alkyl glucamides, protein hydrolysates (particularly wheat-based vegetable 10 products), polyol fatty acid esters, sugar esters, sorbitan esters, polysorbates, and amine oxides. If the nonionic surfactants contain polygîycol ether chains, they may show a conventional homolog distribution, but preferably a narrow-range homolog distribution. Typical examples of cationic surfactants are quaternary ammonium compounds such as dimethyl distearyl ammonium chloride, and esterquats, particularly quaternized fatty acid 15 trialkanolamine ester salts. Typical examples of amphoteric or zwitterionic surfactants are alkylbetaines, alkylamidobetaines, aminopropionates, aminoglycinates, imidazolinium betaines, and sulfobetaines. The above-mentioned surfactants are exclusively known compounds. Typical examples of particularly suitable mild surfactants, i.e. those particularly well-tolerated by the skin, are fatty alcohol polylycolether sulfates, monoglyceride sulfates, 20 mono- and/or dialkylsulfosuccinates, fatty acid isethionates, fatty acid sarcosinates, fatty acid taurides, fatty acid glutamates, α-olefin sulfonates, ether carboxylic acids, alkyl oligoglycosides, fatty acid glucamides, alkyl amidobetaines, and amphoacetal and/or protein fatty acid condensâtes, with the latter preferably being based on wheat proteins.

[0091] OIL COMPONENTS

[0092] Suitable oil components are, for example, Guerbet alcohols based on fatty alcohols containing 6 to 18, and preferably 8 to 10 carbon atoms, esters of linear C6-C22 fatty acids with linear or branched C6-C22 fatty alcohols or esters of branched C6-C13 carboxylic acids with linear or branched C6-C22 fatty alcohols, such as myristyl myristate, myristyl palmitate, 30 myristyl stéarate, myristyl isostearate, myristyl oleate, myristyl behenate, myristyl erucate, cetyl myristate, cetyl palmitate, cetyl stéarate, cetyl isostearate, cetyl oleate, cetyl behenate, cetyl erucate, stearyl myristate, stearyl palmitate, stearyl stéarate, stearyl isostearate, stearyl oleate, stearyl behenate, stearyl erucate, isostearyl myristate, isostearyl palmitate, isostearyl stéarate, isostearyl isostearate, isostearyl oleate, isostearyl behenate, isostearyl 35 oleate, oleyl myristate, oleyl palmitate, oleyl stéarate, oleyl isostearate, oleyl oleate, oleyl behenate, oleyl erucate, behenyl myristate, behenyl palmitate, behenyl stéarate, behenyl isostearate, behenyl oleate, behenyl behenate, behenyl erucate, erucyl myristate, erucyl palmitate, erucyl stéarate, erucyl isostearate, erucyl oleate, erucyl behenate and erucyl erucate. Also suitable are esters of linear C6-C22 fatty acids with branched alcohols, 40 particularly 2-ethyl hexanol, esters of Cis-Css-alkyl hydroxycarboxylic acids with linear or branched C6-C22 fatty alcohols, particularly dioctyl malate, esters of linear and/or branched fatty acids with polyhydric alcohols (such as propylene glycol, dimer dioi, or trimer triol) and/or Guerbet alcohols, triglycérides based on C₆-Cio fatty acids, liquid mono-/di/triglyceride mixtures based on Ce-Ci8 fatty acids, esters of C6-C22 fatty alcohols and/or 45 Guerbet alcohols with aromatic carboxylic acids, particularly benzoic acid, esters of C2-C12

dicarboxylic acids with linear or branched alcohols with 1 to 22 carbon atoms or polyols with 2 to 10 carbon atoms and 2 to 6 hydroxyl groups, vegetable oils, branched primary alcohols, substituted cyclohexanes, linear and branched C6-C22 fatty alcohol carbonates such as dicaprylyl carbonate (Cetiol® CC), Guerbet carbonates based on fatty alcohols containing 6 to 5 18, and preferably 8 to 10 carbon atoms, esters of benzoic acid with linear and/or branched

C6-C22-alcohols (such as Finsolv® TN), linear or branched, symmetrical or asymmetrical dialkyl ethers containing 6 to 22 carbon atoms per alkyl group, such as dicaprylyl ether (Cetiol® OE), ring-opening products of epoxidized fatty acid esters with polyols, silicone oils (cyclomethicone, silicon methicones, etc.} and/or aliphatic or naphthenic hydrocarbons such 10 as squalane, squalene, or dialkyl cyclohexane.

[0093] EMULSIFIERS

[0094] Examples of suitable emulsifiers include nonionic surfactants from at least one of the following groups:

· addition products of 2 to 30 mol of ethylene oxide and/or 0 to 5 mol of propylene oxide to linear fatty alcohols with 8 to 22 carbon atoms, to fatty acids with 12 to 22 carbon atoms, to alkyl phénols with 8 to 15 carbon atoms in the alkyl group, as well as alkylamines with 8 to 22 carbon atoms in the alkyl residue;

• alkyl and/or alkenyl oligoglycosides with 8 to 22 carbon atoms the alk(en)yl residue and ethoxylated analogs thereof;

• addition products of 1 to 15 mol of ethylene oxide to castor oil and/or hardened castor oil;

• addition products of 15 to 60 mol of ethylene oxide to castor oil and/or hardened castor oil;

· partial esters of glycerol and/or sorbitan with unsaturated, linear or saturated, branched fatty acids with 12 to 22 carbon atoms and/or hydroxycarboxylic acids with 3 to 18 carbon atoms, as well as adducts thereof with 1 to 30 mol of ethylene oxide;

• partial esters of polyglycerol (average degree of self-condensation 2 to 8), polyethylene glycol (molecular weight 400 to 5000), trimethylolpropane, pentaerythrite, sugar alcohols (such as sorbite), alkyl glycosides (such as methyl glycoside, butyl glycoside, lauryl glycoside), as well as polyglycosides (such as cellulose} with saturated and/or unsaturated, linear or branched fatty acids with 12 to 22 carbon atoms and/or hydroxycarboxylic acids with 3 to 18 carbon atoms, as well as adducts thereof with 1 to 30 mol of ethylene oxide;

· mixed esters of pentaerythrite, fatty acids, citric acid and fatty alcohols and/or mixed esters of fatty acids containing 6 to 22 carbon atoms, methyl glucose and polyols, preferably glycerol or polyglycerol.

• mono, di- and trïalkylphosphates, as well as mono, di- and/or tri-PEG-alkyl phosphates and salts thereof;

· wool wax alcohols;

• polysiloxane/polyalkyl/polyether copolymers or corresponding dérivatives;

• block copolymers such as polyethylene glycol-30 dipolyhydroxystearate;

• polymer emulsifiers, such as Pemulen polymers (TR-1, TR-2) from Goodrich or Cosmedia® SP from Cognis;

• polyalkylene glycols, and · glycerol carbonates.

[0095] In the following, particularly suitable emulsifiers are described in further detail:

[0096] Alkoxylates. The addition products of ethylene oxide and/or propylene oxide to fatty alcohols, fatty acids, alkyl phénols, or castor oil constitute known, commercially available products. These are homolog mixtures whose average degree of alkoxylation corresponds to 10 the ratio of the amounts of ethylene oxide and/or propylene oxide to the substrates with the addition reaction was carried out. Cn/ia-fatty acid mono and diesters of addition products of ethylene oxide to glycerol are known as refatting agents for cosmetic préparations.

[0097] Alkyl and/or alkenyl oligoglycosides. Alkyl and/or alkenyl oligoglycosides and the production and use thereof are known from prior art. In particular they are produced by 15 reacting glucose or oligosaccharides with primary alcohols having 8 to 18 carbon atoms.

With the respect to the glycoside residue, both monoglycosides, in which a cyclic sugar residue is glycosidically bonded to the fatty alcohol, and oligomeric glycosides, preferably having a degree of oligomérization of approx. 8, are suitable. In this case, the degree of oligomérization is an average statistical value based on the usual homolog distribution for 20 such technical products.

[0098] Partial glycerides. Typical examples of suitable partial glycerides are hydroxystearic acid monoglyceride, hydroxystearic acid diglyceride, isostearic acid monoglyceride, isostearic acid diglyceride, oleic acid monoglyceride, oleic acid diglyceride, ricinoleic acid monoglyceride, ricinoleic acid diglyceride, linoleic acid monoglyceride, linoleic acid 25 diglyceride, linolenic acid monoglyceride, linolenic acid diglyceride, erucic acid monoglyceride, erucic acid diglyceride, tartaric acid monoglyceride, tartaric acid diglyceride, citric acid monoglyceride, citric diglyceride, malic acid monoglyceride, malic acid diglyceride, and technical mixtures thereof that can secondarily contain small amounts of triglycérides from the production process. Addition products of 1 to 30, and preferably 5 to 10 mol of 30 ethylene oxide to the above-mentioned partial glycerides are also suitable.

[0099] Sorbitan esters. Examples of suitable sorbitan esters include sorbitan monoisostearate, sorbitan sesquiisostearate, sorbitan diisostearate, sorbitan triisostearate, sorbitan monooleate, sorbitan sesquioleate, sorbitan dioleate, sorbitan trioleate, sorbitan monoerucate, sorbitan sesquierucate, sorbitan dierucate, sorbitan trierucate, sorbitan 35 monoricinoleate, sorbitan sesquiricinoleate, sorbitan diricinoleate, sorbitan triricinoleate, sorbitan monohydroxystearate, sorbitan sesquihydroxystearate, sorbitan dihydroxystearate, sorbitan trihydroxystearate, sorbitan monotartrate, sorbitan sesquitartrate, sorbitan ditartrate, sorbitan tritartrate, sorbitan monocitrate, sorbitan sesquicitrate, sorbitan dicitrate, sorbitan tricitrate, sorbitan monomaleate, sorbitan sesquimaleate, sorbitan 40 dimaleate, sorbitan trimaleate, and technical mixtures thereof. Addition products of 1 to 30 and preferably 5 to 10 mol of ethylene oxide to the above-mentioned sorbitan esters are also suitable.

Ο

[00100] Polyglycerol esters. Typical examples of suitable polyglycerol esters are polyglyceryl-2 dipolyhydroxystearate (Dehymuls® PGPH), polyglyceryl-3-diisostearate (Lameform® TGI), polyglyceryl-4 isostearate (Isolan® Gl 34), polyglyceryl-3 oleate, diisostearoyl polyglyceryl-3 diisostearate (Isolan® PDI), polyglyceryl-3 methylglucose 5 distearate (Tego Care® 450), polyglyceryl-3 beeswax (Cera Bellina®), polyglyceryl-4 caprate (polyglycerol caprate T2010/90), polyglyceryl-3 cetyl ether (Chimexane® NL), polyglyceryl-3 distearate (Cremophor® GS 32), polyglyceryl polyricinoleate (Admul® WOL 1403), polyglyceryl dimerate isostearate, and mixtures thereof. Examples of further suitable polyol esters are mono, di, and triesters, optionally reacted with 1 to 30 mol of ethylene oxide, of 10 trimethylol propane or pentaerythrite with lauric acid, coconut fatty acid, tallow fatty acid, palmitic acid, stearic acid, oleic acid, behenic acid and the like.

[00101] Anionic emulsifiers. Typical anionic emulsifiers are aliphatic fatty acids with 12 to 22 carbon atoms, such as palmitic acid, stearic acid or behenic acid, as well as dicarboxylic acids with 12 to 22 carbon atoms, such as azelaic acid or sebacic acid.

[00102] Amphoteric and cationic emulsifiers. Zwitterionic surfactants can also be used as emulsifiers. Zwitterionic surfactants are surface-active compounds that carry at least one quaternary ammonium group and at least one carboxylate and a sulfonate group in the molécule. Particularly suitable zwitterionic surfactants are the so-called betaines, including N-alkyl-N,N-dimethylammonium glycinates such as coconut alkyl dimethylammonium 20 glycinate, N-acylaminopropyl-N,N-dimethylammonium glycinates such as coconut acylaminopropyldimethyl ammoniumglycinate, and 2-alkyl-3-carboxylmethyl-3hydroxyethylimidazolines containing 8 to 18 carbon atoms in their alkyl or acyl groups, as well as coconut acylaminoethyl hydroxyethyl carboxymethyl glycinate. Particularly preferred is the fatty acid amide dérivative known under the CTFA name cocamidopropyl betaine.

Ampholytic surfactants are also suitable emulsifiers. Ampholytic surfactants are surfaceactive compounds that, in addition to a Cs/is alkyl or acyl group, contain at least one free amino group and at least one -COOH- or -SO3H group in the molécule and are capable of forming inner salts. Examples of suitable ampholytic surfactants include N-alkyl glycines, Nalkyl propionic acids, N-alkyl aminobutyric acids, N-alkyl iminodipropionic acids, N30 hydroxyethyl-N-alkyl amidopropylglycine, N-alkyl taurine, N-alkyl sarcosine, 2-alkyl aminopropionic acids and alkyl aminoacetic acids with approx. 8 to 18 carbon atoms in their alkyl groups. Particularly preferred ampholytic surfactants are N-coconut alkyl aminopropionate, coconut acyl aminoethylaminopropionate, and C12/18 acyl sarcosine. Finally, cationic surfactants are also suitable as emulsifiers, with those of the esterquat type, preferably 35 methyl quaternized difatty acid triethanolamine ester salts, being particularly preferred.

[00103] FATS AND WAXES

[00104] Typical examples of fats are glycerides, i.e. solid or liquid vegetable or animal products consisting essentially of mixed glycerol esters of higher fatty acids; examples of 40 suitable waxes include natural waxes, such as candelilla wax, carnauba wax, Japan wax, esparto grass wax, cork wax, guaruma wax, rice germ oil wax, sugar cane wax, ouricury wax, montan wax, beeswax, shellac wax, spermaceti, lanolin (wool wax), uropygial fat, ceresin, ozocerite (earth wax), petrolatum, paraffin waxes, and microwaxes; chemically modified waxes (hard waxes), such as montan ester waxes, sasol waxes, hydrogenated jojoba waxes, as well as synthetic waxes such as polyalkylene waxes and polyethylene glycol waxes. In addition to the fats, fatlike substances such as lecithins and phospholipids are also suitable as additives. The person skilled in the art understands the term lecithins to refer to glycerophospholipids formed from fatty acids, glycerol, phosphoric acid, and choline by 5 estérification. Lecithins are therefore frequently referred to by specialists as phosphatidyl cholines (PC). Examples of suitable natural lecithins include the kephalins, also referred to as phosphatidic acids, and which are dérivatives of l,2-diacyl-sn-glycerol-3-phosphoric acids. In contrast, phospholipids are ordinarily understood to be mono- and preferabiy diesters of phosphoric acid with glycerol (glycerol phosphates) that are generally classified as fats. In 10 addition, sphingosines or sphingolipids are also suitable.

[00105] Examples of suitable pearlizing waxes include alkylene glycol esters, particularly ethylene glycol distearate; fatty acid alkanolamides, particularly coconut fatty acid diethanolamide; partial glycerides, particularly stearic acid monoglyceride; esters of polyvalent, optionally hydroxy-substituted carboxylic acids with fatty alcohols containing 6 15 to 22 carbon atoms, particularly long-chain esters of tartaric acid; fatty substances such as fatty alcohols, fatty ketones, fatty aldéhydes, fatty ethers, and fatty carbonates that hâve a total of at least 24 carbon atoms, particularly laurone and distearyl ether; fatty acids such as stearic acid, hydroxystearic acid, or behenic acid, ring opening products of olefin epoxides having 12 to 22 carbon atoms with fatty alcohols having 12 to 22 carbon atoms and/or 20 polyols having 2 to 15 carbon atoms and 2 to 10 hydroxyl groups, as well as mixtures thereof.

[00106] COOLANTS

[00107] Codants are compounds that produce a feeling of coolness on the skin. As a rule, 25 these are menthol compounds, which-in addition to the base component menthol itselfcontain substances selected from the group comprising menthol methyl ether, menthone glyceryl acetal (FEMA GRAS 3807), menthone glyceryl ketal (FEMA GRAS 3808), menthyl lactate (FEMA GRAS 3748), menthol ethylene glycol carbonate (FEMA GRAS 3805), menthol propylene glycol carbonate (FEMA GRAS 3806), menthyl-N-ethyloxamate, monomethyl 30 succinate (FEMA GRAS 3810), monomenthyl glutamate (FEMA GRAS 4006), menthoxy-1,2propane diol (FEMA GRAS 3784), menthoxy-2-methyl-l,2-propane dîol (FEMA GRAS 3849), and the methane carboxylic acid esters and amides WS-3, WS-4, WS-5, WS-12, WS-14, and WS-30, as well as mixtures thereof.

[00108] A first important représentative of these substances is monomenthyl succinate 35 (FEMA GRAS 3810). Both the succinate and the analogous monomenthyl glutarate (FEMA

GRAS 4006) constitute important représentatives of monomenthyl esters based on di- and polycarboxylic acids:

O

[00109] Examples of uses of these substances can be found for example in the documents

WO 2003 043431 (Unilever) or EP 1332772 Al (IFF).

[00110] The next important group of preferred menthol compounds within the meaning of the invention comprises carbonate esters of menthol and polyols, including glycols, glycerol, 5 or carbohydrates, such as menthol ethylene glycol carbonate (FEMA GRAS 3805 = Frescolat®

MGC), menthol propylene glycol carbonate (FEMA GRAS 3784 = Frescolat® MPC), menthol 2methyl-l,2-propane diol carbonate (FEMA GRAS 3849) or the corresponding sugar dérivatives. Also preferred are the menthol compounds menthyl lactate (FEMA GRAS 3748 = Frescolat® ML), and particularly menthone glyceryl acetal (FEMA GRAS 3807) or menthone 10 glyceryl ketal (FEMA GRAS 3808), which is marketed under the name Frescolat® MGA, menthyl ethylamide oxalate, which is marketed under the name Frescolat® X-Cool. Among these substances, menthone glyceryl acetal/ketal, menthyl lactate, menthol ethylene glycol carbonate, menthyl ethylamide oxalate or menthol propylene glycol carbonate hâve been found to be particularly advantageous, and are marketed by the Applicant under the names 15 Frescolat® MGA, Frescolat® ML, Frescolat® MGC, Frescolat® X-cool and Frescolat® MPC.

[00111] Menthol compounds having a C-C bond at position 3 and from which a sériés of représentatives can also be used was first developed in the 1970s. These substances are generally referred to as WS types. The base component is a menthol dérivative in which the hydroxyl group has been replaced with a carboxy! group (WS-1). Ail other types of WS, such 20 as the preferred species WS-3, WS-4, WS-5, WS-12, WS-14 and WS-30, are derived from this structure.

[00112] CONSISTENCY-IMPARTING AGENTS AND THICKENERS

[00113] Suitable consistency-imparting agents are primarily fatty alcohols or hydroxy fatty 25 alcohols with 12 to 22, and preferably 16 to 18 carbon atoms, as well as partial glycerides, fatty acids, or hydroxy fatty acids. A combination of these substances with alkyl oligoglycosides and/or fatty acid-N-methylglucamides of the same chain length and/or poîyglyceryl poly-12-hydroxystearates is preferred. Examples of suitable thickeners are aerosil types (hydrophilic silicic acids), polysaccharides, particularly xanthan gum, guar-guar, 30 agar-agar, alginates and tyloses, carboxymethylcellulose and hydroxyethyl- and hydroxypropylcellulose, as well as higher-molecular polyethylene glycol mono- and diesters of fatty acids, polyacrylates (such as Carbopole® and Pemulen products from Goodrich; Synthalene® from Sigma; Keltrol products from Kelco; Sepigel products from Seppic; Salcare products from Allied Colloids) polyacrylamides, polymers, polyvinyl alcohol, and polyvinyl 35 pyrrolidone. Bentonites such as Bentone® Gel VS-5PC (Rheox) hâve also been found to be particularly effective, comprising a mixture of cyclopentasiloxane, disteardimonium hectorite, and propylene carbonate. Also suitable are surfactants such as ethoxylated fatty acid glycerides, esters of fatty acids with polyols such as pentaerythrite or trimethylol propane, fatty alcohol ethoxylates having narrow-range homolog distribution, or alkyl 40 oligoglycosides, as well as electrolytes such as table sait and ammonium chloride.

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[00114] SUPERFATTING AGENTS AND STABILIZERS

[00115] Examples of suitable superfatting agents are substances such as lanolin and lecithin, as well as polyethoxylated or acylated lanolin and lecithin dérivatives, polyol fatty acid esters, monoglycerides, and fatty acid alkanolamides, wherein the latter simultaneously 5 serve as foam stabilizers.

[00116] Métal salts of fatty acids, such as magnésium, aluminum and/or zinc stéarate or ricinoleate, can be used as stabilizers.

[00117] POLYMERS

[00118] Examples of suitable cationic polymers include cationic cellulose dérivatives such as a quaternized hydroxyethylcellulose available under the name Polymer JR 400® from Amerchol, cationic starch, copolymers of diallyl ammonium salts and acrylamides, quaternized vinyl pyrrolidone/vinyl imidazole polymers such as Luviquat® (BASF), condensation products of polyglycols and amines, quaternized collagen polypeptides such as lauryldimonium hydroxypropyl hydrolyzed collagen (Lamequat®L/Grünau), quaternized wheat polypeptides, polyethylene imine, cationic silicone polymers such as amodimethicone, copolymers of adipic acid and dimethylaminohydroxypropyldiethylene triamine (Cartaretine®/Sandoz), copolymers of acryl acid with dimethyl diallyl ammonium chloride (Merquat® 550/Chemviron), polyaminopolyamides and crosslinked water-soluble 20 polymers thereof, cationic chitin dérivatives such as quaternized chitosan, optionally distributed in microcrystalline form, condensation products of dihalogen alkylene such as dibromobutane with bis-dialkylamines such as bis-dimethylamino-l,3-propane, cationic guar-gums such as Jaguar® CBS, Jaguar® C-17, and Jaguar® C-16 from Celanese, and quaternized ammonium sait polymers such as Mirapol® A-15, Mirapol® AD-1, and 25 Mirapol® AZ-1 from Miranol.

[00119] Examples of suitable anionic, zwitterionic, amphoteric, and nonionic polymers include vinyl acetate/crotonic acid copolymers, vinyl pyrrolidone/vinyl acrylate copolymers, vinyl acetate/butyl maleate/isobornyl acrylate copolymers, methylvinyl ether/maleic acid anhydride copolymers and esters thereof, non-crosslinked polyacrylic acids and polyacrylic 30 acids crosslinked with polyols, acrylamidopropyl trimethylammonium chloride/acrylate copolymers, octylacrylamide/methyl methacrylate/tert-butyl aminoethyl methacrylate/2hydroxypropyl méthacrylate copolymers, polyvinyl pyrrolidone, vinyl pyrrolidone/vinyl acetate copolymers, vinyl pyrrolidone/dimethyiaminoethyl methacryiate/vinyl caprolactam terpolymers, and optionally, derivatized cellulose ethers and silicones.

[00120] SILICONE COMPOUNDS

[00121] Suitable silicone compounds are for example dimethyl polysiloxane, methylphenyl polysiloxane, cyclic silicones, as well as amino, fatty acid, alcohol, polyether, epoxy, fluorine, glycoside, and/or alkyl-modified silicone compounds, which can be présent at room 40 température either in liquid or resinous form. Also suitable are simethicones, which are mixtures of dimethicones having an average chain length of 200 to 300 dimethylsiloxane units and hydrogenated silicates.

[00122] MOISTURIZERS

[00123] Moisturizers are used for further optimization of the sensory properties of the composition and for moisture régulation of the skin. At the same time, the cold stability of the préparations according to the invention is increased, particuiarly in the case of émulsions. The moisturizers are ordinarily contained in an amount of 0.1 to 15 wt%, preferably 1 to 10 wt%, and particuiarly preferably 5 to 10 wt%.

[00124] Examples of suitable moisturizers according to the invention include amino acids, pyrrolidone carboxylic acid, lactic acid and salts thereof, lactitol, urea and urea dérivatives, uric acid, glucosamine, créatinine, cleavage products of collagen, chitosan or chitosan sait 10 dérivatives, and particuiarly polyols and polyol dérivatives (such as glycerol, diglycerol, triglycerol, ethylene glycol, propylene glycol, butylène glycol, erythrite, 1,2,6-hexane triol, polyethylene glycols such as PEG-4, PEG-6, PEG-7, PEG-8, PEG-9, PEG-10, PEG-12, PEG-14, PEG-16, PEG-18, and PEG-20), sugar and sugar dérivatives (including fructose, glucose, maltose, maltitol, mannite, inosite, sorbite, sorbityl silane diol, sucrose, trehalose, xylose, 15 xylite, glucuronic acid and salts thereof), ethoxylated sorbite (sorbeth-6, sorbeth-20, sorbeth-30, sorbeth-40), honey and hardened honey, hardened starch hydrolysates, as well as mixtures of hardened wheat protein and PEG-20/acetate copolymer. Preferred suitable moisturizers according to the invention are glycerol, diglycerol, triglycerol, and butylène glycol.

²⁰ .

[00125] BIOGENIC ACTIVE INGREDIENTS AND ANTIOXIDANTS

[00126] Biogenic active ingrédients are understood to be e.g. tocopherol, tocopherol acetate, tocopherol palmitate, ascorbic acid, (deoxy)ribonucleic acid and fragmentation products thereof, β-glucan, retinol, bisabolol, allantoin, phytantriol, panthenol, AHA acids, 25 amino acids, ceramides, pseudoceramides, essential oils, and plant extracts such as Zingiber

Officinale (Ginger) Root Extract, Echinacea Purpurea Extract, prune extract, bambara extract, vitamin complexes, and benzylidene dimethoxydimethylindanone

[00127] Antioxidants interrupt the photochemical reaction chain triggered when UV radiation pénétrâtes the skin. Typical examples of these are amino acids (such as glycine, 30 histïdine, tyrosine, tryptophan) and dérivatives thereof, imidazoles (such as urocanic acid) and dérivatives thereof, carotenoids, carotènes (such as a-carotene, β-carotene, lycopene) and dérivatives thereof, chlorogenic acid and dérivatives thereof, liponic acid and dérivatives thereof (such as dihydroliponic acid), aurothioglucose, propylthiouracil and other thiols (such as thioredoxin, glutathione, cysteine, cystine, cystamine and glycosyls thereof, N35 acetyl, methyl, ethyl, propyl, amyl, butyl and lauryl, palmitoyl, oleyl, y-linoleyl, cholesteryl and glyceryl esters), as well as salts thereof, dilauryl thiodipropionate, distearyl thiodipropionate, thiodipropionic acid and dérivatives thereof (esters, ethers, peptides, lipids, nucléotides, nucleosides and salts), as well as sulfoximine compounds (such as buthionine sulfoximine, homocystéine sulfoximine, buthionine sulfone, penta, hexa, heptathionine 40 sulfoximine) in very low tolerated doses (such as pmol to μηηοΙ/kg), as well as (métal) chelators (such as α-hydroxy fatty acids, palmitic acid, phytic acid, and lactoferrin), ahydroxy acids (such as citric acid, lactic acid, and malic acid), humic acid, gallic acid, gall extracts, bilirubin, biliverdin, EDTA, EGTA and dérivatives thereof, unsaturated fatty acids and dérivatives thereof (such as γ-linolenic acid, linoleic acid, and oleic acid), folie acid and dérivatives thereof, ubiquinone, ubiquinol and dérivatives thereof, Vitamin C and dérivatives thereof (such as ascorbyi palmitate, Mg ascorbyl phosphate, ascorbyl acetate), tocopherols and dérivatives thereof (such as Vitamin E acetate), Vitamin A and dérivatives thereof (vitamin A palmitate), as well as coniferyl benzoate of benzoin, rutic acid and dérivatives 5 thereof, a-glycosylrutin, féru lie acid, furfurylidene glucitol, carnosine, butyl hydroxytoluene, butyl hydroxyanisole, nordihydroguaiac resin acid, nordihydroguaiaretic acid, trihydroxybutyrophenone, uric acid and dérivatives thereof, mannose and dérivatives thereof, superoxide dismutase, zinc and dérivatives thereof (such as ZnO, ZnSCU), sélénium and dérivatives thereof (such as sélénium méthionine), stilbene and dérivatives thereof 10 (such as stilbene oxide, trans-stilbene oxide), and suitable dérivatives of the abovementioned active ingrédients according to the invention (salts, esters, ethers, sugars, nucléotides, nucleosides, peptides, and lipids).

[00128] FILM-FORMING AGENTS, ANTIDANDRUFF AGENTS, AND EXPANDING AGENTS

[00129] Examples of common film-forming agents include chitosan, microcrystalline chitosan, quaternized chitosan, polyvinyl pyrrolidone, vinyl pyrrolidone-vinyl acetate copolymerisates, polymers of the acrylic acid sériés, quaternary cellulose dérivatives, collagen, hyaluronic acid or salts thereof, and similar compounds.

[00130] Examples of suitable antidandruff active ingrédients include piroctone olamine (120 hydroxy-4-methyl-6-(2,4,4-trimethylpentyl)-2-(lH)-pyridinone monoethanolamine sait),

Baypival® (climbazole), Ketoconazol®, (4-acetyl-l-{-4-[2-(2,4-dichlorophenyl) r-2-(lHimidazol-l-ylmethyi)-l,3-dioxylan-c-4-ylmethoxyphenyl}piperazine, kétoconazole, Elubiol, sélénium disulfide, colloïdal sulfur, sulfur polyethylene glycol sorbitan monooleate, sulfur rizinol polyethoxylate, sulfur-tar distillâtes, salicylic acid (or in combination with 25 hexachlorophene), undecylenic acid monoethanolamide suifosuccinate Na sait, Lamepon®

UD (protein-undecylenic acid condensate), zinc pyrithione, aluminum pyrithione, and magnésium pyrithione/dipyrithione magnésium sulfate.

[00131] Examples of suitable expanding agents for aqueous phases are montmorillonite, clay minerai substances, Pemulen, as well as alkyl-modified carbopol products (Goodrich). 30 Further suitable polymers or expanding agents can be seen in the overview of R. Lochhead in

Cosm. Toil. 108, 95 (1993).

[001321 INSECT REPELLENTS

[00133] Examples of suitable insect repellents include N,N-diethyl-m-toluamide, 1,235 pentane diol, or ethyl butyl acetyl aminopropionates. Suitable self-tanning agents indude dihydroxyacetone. Examples of suitable tyrosine inhibitors, which prevent the formation of melanin and are used in depigmentation agents, include arbutin, ferulic acid, kojic acid, eu marie acid, and ascorbic acid (Vitamin C).

Moreover, hydrotropes, such as éthanol, isopropyl alcohol, or polyols can be used in order to improve flow properties; these substances largely correspond to the carriers described at the outset. In this case, suitabie polyols preferably hâve 2 to 15 carbon atoms, and at least two hydroxyl groups. The polyols can also include other functional groups, particularly amino groups, or be modified with nitrogen. Typical examples are

C)

[00134] HYDROTROPES • glycerol;

• alkylene glycols, such as ethylene glycol, diethylene glycol, propylene glycol, butylène glycol, hexylene glycol, as well as polyethylene glycols with an average molecular weight of 100 to 1,000 daltons;

• technical oligoglycerol mixtures having a degree of self-condensation of 1.5 to 10 such as technical diglycerol mixtures with a diglycerol content of 40 to 50 wt%;

• methylol compounds, particularly trimethylol ethane, trimethylol propane, trimethylol butane, pentaerythrite, and dipentaerythrite;

· lower alkyl glycosides, particularly those with 1 to 8 carbon atoms in the alkyl residue, such as methyl and butyl glycoside;

• sugar alcohols with 5 to 12 carbon atoms, such as sorbite or mannite, • sugars with 5 to 12 carbon atoms, such as glucose or saccharose;

• amino sugars, such as glucamine;

· dialcoholamines, such as diethanolamine or 2-amino-l,3-propane diol.

[00135] PRESERVATIVES

[00136] Examples of suitabie preservatives include phenoxyethanol, formaldéhyde solution, parabens, pentane diol, or sorbic acid, as well as the silver complexes known under the 25 name Surfacine® and the additional substance classes listed in Appendix 6, sections A and B ofthe Cosmetics Ordinance.

[00137] Preference is made to preservatives which are selected from the group consisting of o-cymen-5-ol, benzoic acid and para-hydroxybenzoic acid, their esters and salts, Benzyl benzoate, propionic acid and its salts, salicylic acid and its salts, 2,4-hexadienoic acid (sorbic 30 acid) and its salts, levulinic acid and its salts, anisic acid and its salts, perillic acid and Its salts, cinnamic acid and its salts, formaldéhyde and paraformaldéhyde, 4-hydroxy benzaldehyde, ortho-, meta-, and para-anisic aldéhyde, cinnamic aldéhyde, cinnamic alcohol, 2hydroxybiphenyl ether and its salts, 2-zinc-sulfidopyridine N-oxide, inorganic sulfites and bisulfites, sodium iodate, chlorobutanolum, 4-ethylmercury-(ll)5-amino-l,3-bis(235 hydroxybenzoic acid), its salts and esters, dehydracetic acid, formic acid, l,6-bis(4-amidino2-bromophenoxy)-n-hexane and its salts, the sodium sait of ethylmercury-(ll)-thiosalicylic acid, phenylmercury and its salts, 10-undecylenic acid and its salts, 5-amino-l,3-bis(2ethylhexyl)-5-methyl-hexahydropyrimidine, 5-bromo-5-nitro-l,3-dioxane, 2-bromo-2-nitro-

1,3-propanediol, 2,4-dichlorobenzyl alcohol, N-(4-chlorophenyl)-N'-(3,4-dichlorophenyl)40 urea, 4-chloro-m-cresol, 2,4,4'-trichloro-2'-hydroxy-diphenyl ether, 4-chloro-3,5dimethylphenol, l,r-methylene-bis(3-(l-hydroxymethyl-2,4-dioximidazolidin-5-yl)urea), poly-(hexame-thylenedigiianide) hydrochloride, (Benzyloxymethoxy)-methanol hexamethylenetetramine, l-(3-chloroallyl)-3,5,7-triaza-l-azonia-adamantane chloride, l-{4chlorophenoxy)-l-(lH-imidazol-l-yl)-3,3-dimethyl-2-butanone, l,3-bis-(hydroxyme-thyl)-5,5dimethyl-2,4-imidazolidinedione, l,2-dibromo-2,4-dicyanobutane, 2,2'-methylene-bis(65 brom0’4-chlorophenol), bromochlorophene, mixture of 5-chloro-2-methyl-3(2H)isothiazolinone, 2-methyl-3(2H)-isothiazolinone and with magnésium chloride and magnésium nitrate, 2-Octyl-2H-isothiazol-3-one, l,2-benzisothiazol-3(2H)-one, 2-benzyl-4chlorophenol, 3-(4-Chlorphenoxy)-l,2-propanediol (Chlorphenesin), 2-chloroacetamide, chlorhexidine, chlorhexidine acetate, chlorhexidine gluconate, chlorhexidine hydrochloride, 10 N-alkyl(C12-C22)trimethyl-arnmonium bromide and chloride, 4,4-dimethyl-l,3-oxazolidine, N-hydroxymethyl-N-(l,3-di(hydroxymethyl)-2,5-dioxoimidazolidin-4-yl)-N'-hydroxymethylurea, l,6-bis(4-amidino-phenoxy)-n-hexane and its salts, glutaraldehyde, 5-ethyl-laza-3,7-dioxabicydo(3.3.0)octane, 3-(4-chlorophenoxy)-l,2-propanediol, hyamines, alkyl(C8-C18)-dimethyl-benzyl-ammonium chloride, alkyl-(C8-C18)-dimethyl-benzylammonium 15 bromide, alkyl-(C8-C18)-dimethyl-benzyl-ammonium saccharinate, benzyl hemiformal, 3iodo-2-propynyl butylcarbamate, sodium hydroxymethyl-aminoacetate or sodium hydroxymethyl-aminoacetate, imidazolidinylurea, diazolidinylurea, sodium hydroxymethylglycinate, DMDM hydantoin, Tropolone, (Ethylendioxy)dimethanol, 2-Brom-2{brommethyl)pentandinitril, N-(3-Aminopropyl)-N-dodecylpropan-l,3-diamin, α,α',α20 trimethyl-l,3,5-triazine-l,3,5(2H,4H,6H)-triethanol, pyridine-2-thiol-l-oxide, sodium sait,

Tetrahydro-l,3,4,6-tetrakis(hydroxymethyl)imidazo[4,5-d]imidazol-2,5(lH,3H)-dion, 1,3bis(hydroxymethyl) -l-(l,3,4-tris(hydroxymethyl)-2,5-dioxoimidazolidin-4-yl)urea (Diazolidinyl Urea), l,3-Bis(hydroxymethyî)-5,5-dimethylimidazolidine-2,4-dione, 3-Acety!-2hydroxy-6-methyl-4H-pyran-4-one, cetyl pyridium chloride, ethyl-N-alpha-dodecanoyl-L25 arginate hydrochloride, caprylhydroxamic acid, sorbohydroxamic acid, and their mixtures.

[00138] MULTIFUNCTIONALS

[00139] The cosmetic or pharmaceutîcal préparations of the présent invention particularly contain at least one compound of formula (I) or a cosmetically acceptable sait of a 30 compound of formula (I) or a mixture containing two or more of these compounds or the salts thereof in combination with so called multifunctionals which are selected from the group consisting of 1,3-propanediol, methyl propanediol, 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, 1,2-decanediol, 1,5-pentanediol, 1,6-hexanediol, 1,8-octanediol, 1,2decanediol, ethylhexylglycerin, hexoxy-propan-l,2-diol, heptoxy- propan-l,2-diol, octoxy35 propan-l,2-diol, 3-phenoxy-propan-l,2-diol, 3-benzyloxy-propan-l,2-diol, 3-phenylethyloxypropan-l,2-diol, 3-phenylpropyloxy-propan-l,2-diol, 3-methylbenzyloxy-propan-l,2-diol, sorbitan caprylate, triclosan, climbazole, Octopirox (l-hydroxy-4-methyl-6-{2,4,4trimethylpentyl)-2(lH)-pyridone, 2-aminoethanol), chitosan, farnesol, 2-butyloctanoic acid, 2-Benzylheptan-l-ol, glycerol monolaurate, bis(2-pyridylthio)zinc Ι,Γ-dioxide, N,N'-(decane40 l,10-diyldipyridin-l-yl-4-ylidene)-dioctan-l-amine dihydrochloride (octenidine dihydrochloride), thymol, eugenol, 4-isopropyl-3-methylphenol, benzyl alcohol, 2-phenyethyl alcohol, 3-phenyl propanol, 2-phenoxyethanol, l-phenoxy-propan-2-ol, 3-phenoxypropanol, benzyloxymethanol, glyceryl caprylate, glyceryl caprate, glyceryl laurate, hydroxyacetophenone, and mixtures thereof.

[00140] The preferred cosmetic or pharmaceutical préparation of the présent invention, preferably comprises a combination of resorcinol dérivatives of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) with multifunctionals selected from 25 pentanediol, 1,2-hexanediol, 1,2-octanediol, 1,2-decanediol, hydroxyacetophenone, and mixtures thereof. The combination of the resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) with the multifunctionals are especially advantageously for the treatment of sunlight preferably visible light induced 10 hyperpigmentation.

[00141] PERFUME OILS AND FRAGRANCES

[00142] Examples of suitable perfume oils include mixtures of natural and synthetic fragrances. Natural fragrances are flower extracts (lily, lavender, rose, jasmine, neroli, ylang15 ylang), stems and leaves (géranium, patchouli, petitgrain), fruits (anise, coriander, caraway, juniper), fruit peels (bergamot, lemon, orange), roots (nutmeg, angelica, celery, cardamom, costus, iris, calmus), woods (pinewood, sandalwood, guaîac wood, cedarwood, rosewood), herbs and grasses (tarragon, lemon grass, sage, thyme), needles and branches (spruce, fir, pine, dwarf pine), resins and balsams (galbanum, elemi, benzoin, myrrh, olibanum, 20 opoponax). Animal raw materials such as civet and beaver may also be used. Typical synthetic perfume compounds are products of the ester, ether, aldéhyde, ketone, alcohol and hydrocarbon type. Examples of perfume compounds of the ester type are benzyl acetate, phenoxyethyl isobutyrate, p-tert-butyl cyclohexylacetate, linalyl acetate, dimethyl benzyl carbinyl acetate, phenyl ethyl acetate, linalyl benzoate, benzyl formate, ethylmethyl 25 phenyl glycinate, allyl cyclohexyl propionate, styrallyl propionate and benzyl salicylate.

Ethers include benzyl ethyl ether, while aldéhydes include linear alkanals containing 8 to 18 carbon atoms, citral, citronellal, citronellyl oxyacetaldehyde, cyclamen aldéhyde, hydroxycitronellal, lilial and bourgeonal; examples of suitable ketones are the ionones, aisomethylionone, and methyl cedryl ketone. Suitable alcohols are anethol, cîtroneflol, 30 eugenol, isoeugenol, geraniol, linalool, phenylethyl alcohol, and terpineol. The hydrocarbons chiefly include the terpenes and balsams. However, mixtures of different perfume compounds are preferred that produce an agreeable fragrance together. Other suitable perfume oils include essential oils of low volatility that are mostly used as aroma components, such as sage oil, camomile oil, clove oil, melissa oil, mint oil, cinnamon leaf oil, 35 lime-blossom oil, juniper berry oil, vetiver oil, olibanum oil, galbanum oil, ladanum oil, and lavendin oil. Preferably, bergamot oil, dihydromyrcenol, lilial, lyral, citronellol, phenylethyl alcohol, α-hexylcinnamaldehyde, geraniol, benzyl acetone, cyclamen aldéhyde, linalool, boisambrene forte, ambroxan, indole, hedione, sandelice, citrus oil, mandarin oil, orange oil, allyl amyl glycolate, cyclovertal, lavendin oil, clary oil, β-damascone, géranium oil bourbon, 40 cyclohexyl salicylate, Vertofix Coeur, Iso-E-Super, Fixolide NP, evernyl, iraldein gamma, phenylacetic acid, geranyl acetate, benzyl acetate, rose oxide, romillate, irotyl, and floramate are used either individually or in mixtures.

[00143] Examples of suitable fragrances include peppermint oil, spearmint oil, anise oil, star anise oil, caraway oil, eucalyptus oil, fennel oil, citrus oil, wintergreen oil, clove oil, menthol, 45 and the like.

[00144] DYES

[00145] The dyes that can be used are those suitable and approved for cosmetic purposes, such as those listed in the publication Cosmetic Dyes” of the Farbstoffkommission der Deutschen Forschungsgemeinschaft [Dyes Commission of the German Research Foundation], Verlag Chemie, Weinheim, 1984, pp. 81-106. Examples are cochineal red A (C.l. 16255), patent blue V (C.1.42051), indigotin (C.1.73015), chlorophyllin (C.l.75810), quinoline yellow (C.1.47005), titanium dioxide (C.l.77891), indanthrene blue RS (C.l. 69800) and alizarin red (C.l.58000). Luminol can also be included as a luminescent dye. These dyes are ordinarily used in concentrations of 0.001 to 0.1 wt% relative to the entire mixture.

[00146] The total amount of these auxiliaries and additives can be Ito 50, and preferably 5 to 40wt% relative to the agent. The agent can be produced by common cold or hot processes; the phase inversion température mode is preferred.

INDUSTRIAL APPLICATION

[00147] An important aspect ofthe présent invention refers to a non-therapeutical method for treating hyperpigmentation, in sunlight induced, preferably visible light induced hyperpigmentation, comprising the following steps:

(i) providing a preferred (pharmaceutical or cosmetic) composition as described aforementioned comprising a resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®), and (ii) applying said composition to human skin.

[00148] Particularly, the method is preferably directed to ginger root CO2 extract containing, consisting or essentially consisting of

25 (a)	25 to 30	% b.w. [6]-gingerol
(b)	5 to 10	% b.w. [8]-gingerol
(c)	5 to 10	% b.w. [10]-gingerol
(d)	1.5 to 4	% b.w. [6]-shogaol
(e)	0.3 to 1.3	% b.w. [8]-shogaol;
30 (f)	0.03 to 1	% b.w. [10]-shogaol;
(g)	0.01 to 1	% b.w. zingerone,
on	condition that the amount of gingen

surns up to 35 to 50 % b.w. and the amount of shogaols sums up to 1.516 % b.w.

[00149] Preference is made to the method in which the cosmetic/pharmaceutical préparation further comprises, consists or essentially consisting of at least one UV filters, wherein the UV filters are selected from the group consisting of UV-A filters, UV-B filters, and light protection pigments.

[00150] Also preferred is a method in which the cosmetic/pharmaceutical préparation further comprises consists or essentially consisting of at least one skin lightening agent. In a preferred embodiment the préparations are in the form of creams, lotions, gels, pastes or capsules representing skin care or sun protection compositions.

[00151] Preference is also made to a method, wherein resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) is present in an active amount to reduce, retard, suppress and/or protect against sunlight induced, preferably visible light induced hyperpigmentation.

[00152] A further aspect of the present invention is another method of cosmetic, nontherapeutic treatment of a mammal, said method comprising effecting changes in mammalian skin pigmentation, preferably human skin, by administering to said mammal a pigmentation-changing effective amount of resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®).

[00153] Preferably the pigmentation-changing effective amount of the resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) is administered topically.

[00154] Another further aspect of the present invention is a method of reducing, retarding and/or suppressing hyperpigmentation, respectively treating, preventing and/or ameliorating the formation of hyperpigmentation of skin which comprises topically applying a preferred (pharmaceutical or cosmetic) préparation as described aforementioned containing, consisting or essentially consisting of a resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) and further additives to sunlight induced, preferably visible light induced hyperpigmented tissue of a human.

[00155] Optionally, further compounds (bl) from 0.05 wt.% to 60 wt.%, preferably 0.1 wt.% to 50 wt.%, and particularly preferably 0.5 wt.% to 40 wt.% of UV filters, and/or (b2) from 0.005 wt.% to 20 wt.%, preferably 0.01 wt.% to 10 wt.% of skin lightening agents, and/or (b3) from 0.0001 wt.% to 30 wt.%, preferably from 0.01 wt.% to 10 wt.%of antioxidants are 30 present in the present préparations, wherein the weight percent of the compounds a) to d) are based on the total amount of the préparation and the sum of ail compounds add to 100 wt.%, more preferably one of the compounds (bl), (b2) or (b3) is essentially contained in a preferred composition of the present invention. And in a further embodiment compounds (bl) and (b2) are essentially contained in a preferred composition of the present invention.

In another embodiment compounds (bl,) (b2) and (b3) are essentially contained in a preferred composition of the present invention.

[00156] Finally, the invention is directed to the use of resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) for the treatment, prévention 40 and/or amelioration of hyperpigmentation, particularly to reduce, retard, suppress and/or protect against sunlight induced, preferably visible light induced hyperpigmentation.

[00157] A further aspect of the present invention is the use of resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) for reducing, retarding and/or suppressing hyperpigmentation, respectively treating, preventing and/or ameliorating the formation of hyperpigmentation of skin, in which a preferred (pharmaceutical or cosmetic) préparation as described aforementioned that comprises resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl 5 resorcinol or phenylethyl resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) and further additives is topically applied to sunlight induced, preferably visible light induced hyperpigmented tissue of a human.

[00158] Further aspect is the non-therapeutical, cosmetically use of resorcinol dérivatives of formula (I) respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl 10 resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®) for the treatment, prévention and/or amelioration of hyperpigmentation.

[00159] The aforementioned uses herein encompasses the preferred compositions and préparations comprising, consisting or essentially consisting of resorcinol dérivative of formula (I), respectively (II), preferably 4-butyl resorcinol, 4-hexyl resorcinol or phenylethyl 15 resorcinol, and most preferred phenylethyl resorcinol (SymWhite 377®).

EXAMPLES

[00160] EXAMPLE 1

[00161] Human epidermal melanoma cells A375 were cultured in 6-well plates. The cells were exposed to visible light (480 J/cm2) with Hydrosun 750 equipped with KG1 filter. 48 h prior to and past to the irradiation the cells were treated with test compounds in noncytotoxic concentrations. Mélanocytes were lysed in a solution of NaOH. Melanin was quantified by measurement of absorbance at 405 nm and calculation based on a melanin 10 standard curve.

[00162] Table 1

Visible light induced hyperpigmentation in vitro: inhibition vs. visible light induced

Compound	Concentration [%]	Melanin [pg]	Inhibition [%]	Sigii.
Untreated		0.4589 ± 0.0334
Visible light irradiated		0.9731 + 0.1024		###
SymWhite® 377	0.000068	0.5688 ± 0.0793	79	**
0.000210	0.5280 ± 0.0494	86	** *
0.000680	0.4598 ± 0.1024	100	* **
Untreated		1.8632 ±0.1932
Visible light irradiated		2.9248 + 0.1357		###
4-Hexyl resorcinol	0.000005	1.9616 ± 0.2899	91	**
0.000015	1.8407 ± 0.1988	102	** *
0.000050	1.1668 + 0.1312	166	***
Untreated		1.8632 + 0.1932
Visible light irradiated		2.9248 ± 0.1357		###
4-Butyl resorcinol	0.0000316	2.3136 ±0.6518	58	**
0.0001000	1.8593 ± 0.5365	100
0.0003160	0.9849 ± 0.0738	183	***

Significance:

### p<0.001 versus untreated;

* P<0.05 versus visible light irradiated ** PcO.Ol versus visible light irradiated 2Q *** p<q.ooi versus visible light irradiated

[00163] It has been surprisingly shown that SymWhite® 377, 4-hexyl resorcinol and 4-butyl resorcinol significantly inhibit the visible light induced hyperpigmentation.

[00164] EXAMPLE 2

[00165] The below formulations were applied on ex vivo human skin expiants from abdominal surgery of a donor with phototype IV (Fitzpatrick scale). 48 h after the formulations were removed with a cotton pad. Skin expiants were exposed to visible light (480 J/cm2) with Hydrosun 750 equipped with KG1 filter. Formulations were reapplied afterwards. 48 h later skin sections were prepared and melanin was stained by Fontana10 Masson stain. Quantification of melanin was done by image analysis.

[00166] Table3

Formulations applied to ex vivo human skin (ail amounts w/w%)

Phase	Ingrédients	INCI	A	B	C .·'
A.	H2O, demin.	Water (Aqua)	84,75	84,55	84,70
Hydrolite-5	Pentyleneglycol	1,00	1,00	1,00
B.	PCL liquid 100	Cetearyl Octanoate	3,00	3,00	3,00
La nette O	Cetearyl Alcohol	2,00	2,00	2,00
Minerai Oil 5°E	Minerai Oil	3,00	3,00	3,00
Eutanol G PN	Octyldodecanol	4,00	4,00	4,00
Abil 350	Dimethicone	0,50	0,50	0,50
C.	Pemulen TRI	Acrylates/C10-30 Alkyl Acrylate Crosspolymer	0,20	0,20	0,20
Ultrez-21	Acrylates/C10-30 Alkyl Acrylate Crosspolymer	0,05	0,05	0,05
D.	Sodium hydroxid Sol. 10%	Sodium Hydroxide	0,50	0,50	0,50
E.	SymWhite® 377	Phenylethyl Resorcinol	-	0,50	0,20
Hydrolite-5	Pentyleneglycol	1,00	1,00	1,00
	Sum		100,0	100,0	100,0

[00167] Table 4

Melanin formation after visible light irradiation on ex vivo human skin

	% of melanin	Inhibition vs Placebo [%]
untreated	33.22	+	3.7
Placebo	61.68	+	1.7
0.2% SymWhite® 377	42.48	+	2.6	67.5
0.5% SymWhite® 377	25.91	+	1.2	125.7

[00168] The following examples show formulations for various sun protection products that contain the préparations according to the invention. Ail amounts are to be understood as indicating wt%.

[00169] Cosmetic sun protection agent

Components	Amount
Ethylhexyl cinnamic acid	7.50
Benzophenone-3	2.00
Polyglyceryl dimer soyate	0.80
Sorbitan stéarate	1.00
Tocopheryl acetate	0.50
Glyceryl stéarate. PEG-100 Stéarate	3.00
PEG-40. Hydrogenated castor oil	1.00
Titanium dioxide. Aluminum oxide hydrate. Dimethicone/methicone copolymer	3.00
Butyrospermum parkii (shea butter)	1.00
C12-15 alkyl benzoate	6.50
Butylène glycol	5.00
Xanthan gum	0.30
Disodium EDTA	0.10
Allantoin	0.10
Polyacrylamide. C13-14 isoparaffin. Laureth-7	1.00
Pentylene glycol	5.00
4-t-Butyl cyclohexanol	1.00
SymWhite® 377	0.20
Benzylidene Dimethoxydimethylindanone	0.30
Preservatives (methyl, butyl, ethyl, propylparaben, phenoxyethanol)	0.30
Aqua dem.	Ad 100

[00170] Sun protection spray (ali amounts in wt.%)

Components	INCI	A	B	c
Water, demineralized	Water (aqua)	69.00	69.00	69.00
Glycerol	Glycerol	4.00	4.00	4.00
1,3-butylene glycol	Butylène glycol	5.00	5.00	5.00
D-Panthenol	Panthenol	0.50	0.50	0.50
Lara care A-200	Galactoarabinan	0.25	0.25	0.25
Baysilone oil M10	Dimethicone	1.00	1.00	1.00
Edeta BD	Disodium EDTA	0.10	0.10	0.10
Copherol 1250	Tocopheryl acetate	0.50	0.50	0.50
Cetiol OE	Dicaprylyl ether	3.00	3.00	3.00
Neo Heliopan® HMS	Homosalate	5.00	5.00	5.00
Neo Heliopan® AV	Ethylhexyl methoxycinnamate	6.00	6.00	6.00
Neo Heliopan® 357	Butyl methoxydibenzoyl methane	1.00	1.00	1.00
Corapan TQ	Diethylhexylnaphthalate	2.00	2.00	2.00
Alpha Bisabolol	Bisabolol	0.10	0.10	0.10
Pemulen TR-2	Acrylates/C10-30 alkyl acrylate crosspolymer	0.25	0.25	0.25
NaOH 10%	Sodium hydroxide	0.60	0.60	0.60
Perfume oil	Fragrance	0.20	0.20	0.20
Phenoxyethanol	Phenoxyethanol	0.40	0.40	0.40
SymSave® H	Hydroxyacetophenone	0.50	0.50	0.50
Solbrol M	Methyl paraben	0.10	0.10	0.10
Solbrol P	Propylparaben	0.10	0.10	0.10
SymWhite® 377	Phenylethyl Resorcinol	0.20	0.20
4-Hexyi resorcinol	Hexylresorcinol		0.20	0.20
4-Butyl resorcinol	4-Butylresorcinol	0.20		0.20

[00171] Sun protection spray O/W SPF 15-20

Components	INCI	Amount
Dracorin® GOC	Glyceryl oleate citrate. Caprylic/capric triglycéride	2.00
Corapan® TQ	Diethythexyl 2,6-naphthalate	3.00
Neo Heliopan® HMS	Homosalate	7.00
Neo Heliopan® OS	Ethylhexyl salicylate	5.00
Neo Heliopan® 357	Butyl methoxydibenzoyl methane	3.00
Isoadipate	Diisopropyl adipate	6.00
Baysilone® Oil M10	Dimethicone	1.00
Edeta® BD	Disodium EDTA	0.10
Vitamin E acetate	Tocopheryl acetate	0.50
Dragosantol® 100	Bisabolol	0.10
Pemulen® TR-2	Acrylates/C10-30 alkyl acrylate crosspolymer	0.25
Glycerol 99.5 P	Glycerol	4.00
Butylène glycol	Butylène glycol	5.00
Neo Heliopan® hydro (103089). Used as 25% aq. solution neutralized with Biotive® L-Arginine	Phenylbenzimidazole sulfonic acid	8.00
Biotive® L-Arginine	Arginine	0.55
SymWhite 377	Phenylethyl Resorcinol	0.1
Perfume oil	Fragrance	0.40
Sobrol M	Methylparaben	0.30
SymWhite® 377	Phenylethyl Resorcinol	0.20
Water	Water (Aqua)	Ad 100

[00172] Sun protection soft cream W/O SPF 40

Components	INCI	Amount
Dehymuls PGPH	Polyglyceryl-2 dîpolyhydroxystearate	5.00
Copherol 1250	Tocopheryl acetate	0.50
Permulgin 3220	Ozocerite	0.50
Zinc stéarate	Zinc stéarate	0.50
Tegosoft TN	C12-15 alkyl benzoate	10.00
Neo Heliopan® E1000	Isoamyl-p-methoxycinnamate	2.00
Neo Heliopan® 303	Octocrylene	5.00
Neo Heliopan® MBC	4-methylbenzylidene camphor	3.00
Zinc oxide, neutral	Zinc oxide	5.00
EDETA BD	Disodium EDTA	0.10
Glycerol	Glycerol	4.00
Magnésium sulfate	Magnésium sulfate	0.50
Perfume oil PI, P2, P3, or P4	Perfume	0.30
Symdiol® 68	1,2-hexane diol. Caprylyl glycol	0.30
Dragosine	Carnosine	0.10
SymWhite® 377	Phenylethyl Resorcinol	0.10
Water, distilied	Water (aqua)	Add 100

[00173] Sun protection lotion W/O (ail amounts in wt.%)

Components	INCI	A	B	C
Dehymuls PGPH	Polyglyceryl-2 dipolyhydroxystearate	3.00	3.00	3.00
Beeswax 8100	Beeswax	1.00	1.00	1.00
Monomuls 90-0-18	Glyceryl oleate	1.00	1.00	1.00
Zinc stéarate	Zinc stéarate	1.00	1.00	1.00
Cetiol SN	Cetearyi isononanoate	5.00	5.00	5.00
Cetiol OE	Dicaprylyl ether	5.00	5.00	5.00
TegosoftTN	C12-15 alkyl benzoate	4.00	4.00	4.00
Vitamin E	Tocopherol	0.50	0.50	0.50
Neo Heliopan® OS	Ethylhexyl salicylate	5.00	5.00	5.00
Neo Heliopan® AV	Ethylhexyl methoxycinnamate	7.50	7.50	7.50
Uvinul®T150	Ethylhexyl triazone	1.50	1.50	1.50
Trilon BD	Disodium EDTA	0.10	0.10	0.10
Glycerol	Glycerol	5.00	5.00	5.00
Neo Heliopan® AP 10% solution. Neutralized with NaOH	Disodium phenyl dibenzimidazole tetrasulfonate	15.00	15.00	15.00
Perfume oil	Perfume	0.25	0.25	0.25
Alpha bisaboloi	Bisaboloi	0.10	0.10	0.10
SymOcide® PT	Phenoxyethanol. Tropoione	0.25	0.25	0.25
SymWhite® 377	Phenylethyl Resorcinol	0.5
4-Hexyl resorcinol	Hexylresorcinol		0.50
4-Butyl resorcinol	4-Butylresorcinol			1.00
Water, distilled	Water (Aqua)	ad 100	ad 100	ad 100

[00174] After-sun gel

Components	INC*	Amount
SymSol® PF-3	Water (aqua). Pentylene glycol. Sodium lauryl sulfoacetate. Sodium oleoyl sarcosinate. Sodium chloride. Disodium sulfoacetate. Sodium oleate. Sodium sulfate	3.00
Glycerol 99.5 P.	Glycerol	5.00
SymUrban®	Benzylidene dimethoxy dimethylene danone	0.10
Pemuien® TR-2	Acrylates/C10-30 alkyl acrylate crosspolymer	1.00
D-Panthenol 75 W	Panthenol	0.50
SymFinity® 1298	Echinacea purpurea extract	0.10
Extrapone® Pearl GW	Water (aqua). Glycerol. Hydrolyzed pearl. Xanthan gum	1.00
Sodium hydroxide 10% solution	Sodium hydroxide	2.50
Ethanol 96%	Alcohol denat.	15.00
Perfume oil	Perfume	0.20
SymOcide® PS	Phenoxyethanol. 1,2-Hexanediol. Decylene glycol	0.50
SymWhite® 377	Phenylethyl Resorcinol	0.10
Water	Water (aqua)	Ad 100

[00175] Night Recovery Cream

Component	înci λ/J '.; . ;	Amount
Aqua/Water	Aqua	ad 100
SymSave® H	Hydroxyacetophenone	0.5
SymDiol® 68	1,2-Hexanediol	O.S
Caprylyl Glycol
SymVital® AR 3040	Zingiber Officinale (Ginger) Root Extract	0.2
Edeta® BD	Disodium Edta	0.1
Emulsiphos®	Potassium Cetyl Phosphate	2.0
Hydrogenated Palm Glycerides
Mango Butter	Mangifera indica Seed Butter	2.0
SymMollient® S	Cetearyl Nonanoate	1.0
SymWhite® 377	Phenylethyl Resorcinol	0.3
Dragoxat® 89	Ethylhexyl Isononanoate	8.5
La nette® 16	Cetyl Alcohol	2.0
Lanette® 0	Cetearyl Alcohol	4.0
SymRepair® 100	Hexyldecanol	2.0
Bisabolol
Cetylhydroxyproline Palmitamide
Stearic Acid
Brassica Campestrîs (Rapeseed) Sterols
Cetiol® Ultimate	Tridecane	5.0
Undecane
Carbopol® Ultrez 10 Polymer	Carbomer	0.3
Tapioca Pure	Tapioca Starch	2.0
Fragrance	Parfum	0.4
Sodium Hydroxide 10% solution	Aqua	0.4
Sodium Hydroxide
Tocopherol alpha DL	Tocopherol	0.5

[00176] Fresh watering after sun mousse

Component	inci ; 'λ··' ' '.'ν ' .	Amount
Aqua/Water	Aqua	Ad 100
SymSol® PF-3	Aqua	2.0
Pentylene Glycol
Sodium Lauryl Sulfoacetate
Sodium Oleoyl Sarcosinate
Sodium Chloride
Sodium Oleate
Aqua Keep 10SH-NFC	Sodium Acrylates Crosspolymer-2	2.0
SymSave® H	Hydroxyacetophenone	O.S
SymDioi® 68	1,2-Hexanediol	0.5
Caprylyl Glycol
Hydrolite® 5	Pentylene Glycol	3.0
SymWhite® 377	Phenylethyl Resorcinol	0.2
SymGlucan®	Aqua	1.0
Glycerin
1,2-Hexanediol
Caprylyl Glycol
Beta-Glucan
La nette® 0	Cetearyl Alcohol	1.0
SymRepair® 100	Hexyldecanol	1.0
Bisabolol
Cetylhydroxyproline Palmitamide
Stearic Acid
Brassica Campestrîs (Rapeseed) Sterols
SymSitive® 1609	Pentylene Glycol	1.0
4-T-Butylcyclohexanol
Frescolat® Ml	Menthyl Lactate	1.0
SymMollient® S	Cetearyl Nonanoate	2.5
Dragoxat® 89	Ethylhexyl Isononanoate	5.0
Isodragol®	Triisononanoin	3.0

Sym Urban™	Benzylidene Dimethoxydimethylindanone	0.3
Xiameter®	Dimethicone	1.0
Dimethiconol
Fragrance	Parfum	0.3

[00177] Creme gel for face

Comportent	INCI Z' <Z'-: ;'?/Z. /.E	Amount
Aqua/Water	Aqua	ad 100
SymWhite® 377	Phenylethyl Resorcinol	0.15
Sclareolide	Sclareolide	0.10
Glycerin	Glycerin	3.0
Dracorin® Goc	Glyceryl Oleate Citrate ____	0.3
Caprylic/Capric Triglycéride
Jojoba Oil	Simmondsia Chinensis Seed Oil	4.0
Avocado Oil	Persea Gratissima Oil	4.0
Sweet Almond Oil	Prunus Amygdalus Dulcis (Sweet Almond) Oil	4.0
Shea Butter	Butyrospermum Parkii Butter	2.0
Symdecanox Ha	Caprylic/Capric Triglycéride	1.0
Hydroxymethoxyphenyl Decanone
SymWhite® 377	Phenylethyl Resorcinol ________	0.2
Cosmedia Sp		1.2
Symocide® Ps	Phenoxyethanol	1.0
Decylene Glycol
1,2-Hexanediol
Tapioca Pure	Tapioca Starch	1.0

[00178] Creamy fresh body lotion

Component	1NCI - /'	Amount
Emulsiphos®	Potassium Cetyl Phosphate	2.50
Hydrogenated Palm Glycerides
Tegin M	Glyceryl Stéarate	1.20
Pcl-Solid®	Stearyl Heptanoate	2.00
Stearyl Caprylate
Silcare® Silicone 41ml5	Caprylyl Methicone	4.00
Tocopheryl Acetate	Tocopheryl Acetate	0.25
La nette® 16	Cetyl Alcohol __	0.50
PCL-Liquid® 100	Cetearyl Ethyl hexanoate	5.00
Xiameter® Pmx-200 Silicone Fluid lOOcs	Dimethicone	2.00
Symvital® AR 3040	Zingiber Officinale (Ginger) Root Extract	0.10
SymWhite® 377	Phenylethyl Resorcinol	0.20
Tego® Feel Green	Cellulose	1.00
Keltrol® Cg-F	Xanthan Gum	0.30
Extrapone® Watermint P	Aqua	1.00
Propylene Glycol
Glucose
Mentha Aquatica Leaf Extract
Glycerin	Glycerin	4.00
Extrapone®Deep Sea Gw	Aqua	1.00
Glycerin
ThermusThermophillus Ferment
Symwhite Plus®	Caprylic/Capric Triglycérides, Pentylene Glycol, Phenylethyl Resorcinol, Bisabolol, Butyl Methoxydibenzoyl Methane	2.00
Hydrolite® 5	Pentylene Glycol	4.00
Symsave® H	Hydroxyacetoplnenone	0.50
Colour		0.81

Dragosine®	Carnosine	0.10
Frescolat® ML	Menthyl Lactate	0.50
Fragrance	Parfum	0.50
Aqua/Water	Aqua	Ad 100

Dragosine®	Carnosine	0.10
Frescolat® ML	Menthyl Lactate	0.50
Fragrance	Parfum	0.50
Aqua/Water	Aqua	Ad 100

[00179] Eye lotion

Comportent Λ	JNÇL·';LL/ ’-'L' L; 'L.LL:	Amount	Amount
Dracorin® GOC	Glyceryl Oleate Citrate	2.50	2.50
	Caprylic/Capric Triglycéride
Pcl-Liquid® 100	Cetearyl Ethylhexanoate	2.50	2.50
Isodragol®	Triisononanoin	4.00	4.00
Symmollient® S	Cetearyl Nonanoate	1.50	1.50
Xiameter® Pmx-200 Silicone Fluid 350 Cs	Dimethicone	1.00	1.00
Dragosine®	Carnosine	0.10	0.10
Tocopheryl Acetate	Tocopheryl Acetate	0.10	0.10
Carbopol® Etd 2020 Polymer	Acrylates/C10-30 Alkyl Acrylate Crosspolymer	0.15	0.15
Keltrol® Cg-T	Xanthan Gum	0.25	0.25
Symsave® H	Hydroxyacetophenone	0.50	0.50
Symdiol® 68	1,2-Hexanediol	0.50	0.50
	CAPRYLYL GLYCOL
Sodium Hydroxide 10% Sol.	Aqua, Sodium Hydroxide	0.20	0.20
Simulgel Ns	Hydroxyethyl Acrylate/Sodium Acryloyldimethyl Taurate Copolymer	0.60	0.60
SQUALANE
POLYSORBATE 60
Hydroviton® Plus	Aqua, Pentylene Glycol, Glycerin,	2.00	2.00
Fructose, Urea, CitricAcid,
Sodium Hydroxide, Maltose,
Sodium Pca, Sodium Chloride,
Sodium Lactate, Trehalose, Allantoin,
Sodium Hyaluronate, Glucose
SymWhite® 377	Phenylethyl Resorcinol	0.15	0.10
Larixol	Larixol	-	0.10
Symfinity® 1298	Echinacea Purpurea Extract	0.10	0.10
Fragrance	Parfum	0.30	0.30
Aqua/Water	Aqua	ad 100	ad 100

Claims (9)

Claims

1. A médicament containing at least a resorcinol dérivative of formula (I)

in which R stands for an alkyl radical having 3 to 10 carbon atoms or an optionally substituted alkylphenyl radical having 8 to 16 carbon atoms, for use in the treatment, prévention and/or amelioration of hyperpigmentation wherein the hyperpigmentation is induced by the radiation of visible light and/or UVB.

2. The médicament of claim 1, wherein the hyperpigmentation is induced by the radiation of sunlight.

3. The médicament of claim 2, wherein the hyperpigmentation is induced by the radiation of visible light and/or UVB with a wavelength in the range from 100 nm to 1500 nm.

4. The médicament of any preceding claims 1 to 3, wherein the hyperpigmentation is induced by the radiation of visible light and/or UVB with a wavelength in the range from 400 nm to 750 nm.

5. The médicament of any preceding claims 1 to 4, wherein the médicament further comprises at least one UV filter, wherein the UV filters are selected from the group consisting of UV-A filters, UV-B filters, and light protection pigments.

6. The médicament of any preceding claims 1 to 5, wherein the médicament further comprises at least one skin lightening agent.

7. The médicament of any preceding claims 1 to 6, wherein the resorcinol dérivative is present in an active amount to reduce, retard, suppress and/or protect against sunlight.

8. The médicament of any preceding claims 1 to 7, wherein the resorcinol dérivative is present in an active amount to reduce, retard, suppress and/or protect against visible light induced and/or UVB hyperpigmentation.

9. The médicament of claim 1 comprising (a) from 0.01 wt.% to 10 wt.% of at least one resorcinol dérivative of formula (I), (b) and at least one compound selected from (bl), (b2) and (b3):

(bl) from 0.05 wt.% to 60 wt.%, of UV filters, (b2) from 0.005 wt.% to 20 wt.%, of skin lightening agents, (b3) from 0.0001 wt.% to 30 wt.% of antioxidants, and optionally (c) from 0.2 wt.% to 99 wt.% of carriers, and/or (d) 0.1 wt.% to 90 wt.% further additives, wherein the weight percent of each of the compounds a) to d) is based on the total amount of the préparation and the sum of ail compounds adds to 100 wt.%.