Pigmentation-regulating compounds 机翻标题: 暂无翻译,请尝试点击翻译按钮。

公开号/公开日
USRE46228 E 2016-12-06 [USRE46228] / 2016-12-06
申请号/申请日
2008US-14175312 / 2008-04-11
发明人
CEBRIÁN PUCHE JUAN;MESSEGUER PEYPOCH ÁNGEL;FERRER MONTIEL ANTONIO VICENTE;ALMIÑANA DOMÉNECH NURIA;CARREÑO SERRAÏMA CRISTINA;
申请人
LIPOTEC;
主分类号
IPC分类号
A61K-008/49A61Q-019/00A61Q-019/02C07D-311/72C07D-405/12C07D-407/12C07D-409/12C07D-495/04
摘要
(USRE46228) The present invention relates to compounds of general formula (I):  <chemistry id="CHEM-US-00001" num="00001"> <img alt="embedded image" file="USRE046228-20161206-C00001.TIF" he="24.47mm" id="EMI-C00001" img-content="chem" img-format="tif" wi="59.35mm"/> </chemistry> wherein X is selected from the group consisting of O or S and R is a linear or branched, saturated or unsaturated aliphatic group with from 2 to 23 carbon atoms (C<sub>2 </sub>to C<sub>23</sub>), or a cyclic group, and which can contain substituents selected from the group consisting of hydroxy, alkoxy, amino, carboxyl, cyano, nitro, alkylsulfonyl or halogen atoms, a method of obtaining them, cosmetic or pharmaceutical compositions containing them and the use thereof for treating, caring for and/or cleaning skin, hair and/or nails, preferably those conditions, disorders or pathologies of the skin, hair and/or nails which require regulating melanogenesis.
机翻摘要
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地址
代理人
代理机构
;
优先权号
2007ES-0001663 2007-06-15 2008US-12440707 2008-04-11 2008US-14175312 2008-04-11 2008US-61037085 2008-03-17 2008WO-ES00230 2008-04-11
主权利要求
(USRE46228) The invention claimed is: 1.  A compound of general formula (I)       or its cosmetically or pharmaceutically acceptable [deleted text: salts] [inserted text: salt], wherein R is a linear or branched, saturated or unsaturated aliphatic group containing 2 to 23 carbon atoms[deleted text: , or a cyclic group,] and which can contain substituents selected from the group consisting of hydroxy, alkoxy, amino, carboxyl, cyano, nitro, alkylsulfonyl or halogen atoms; and X is selected from the group consisting of O and S. 2. A The compound according to claim 1, wherein X is O. 3. The [deleted text: compound] [inserted text: composition ]according to claim [deleted text: 1] [inserted text: 8], wherein R is a saturated or unsaturated aliphatic group, containing 2 to 23 carbon atoms. 4. The compound according to claim [deleted text: 2 or 3] [inserted text: 1], wherein       is selected from the group consisting of tert-butanoyl, hexanoyl, 2-methylhexanoyl, octanoyl, decanoyl, lauroyl, myristoyl, palmitoyl, stearoyl, oleoyl and linoleoyl. 5. The [deleted text: compound] [inserted text: composition ]according to claim [deleted text: 1] [inserted text: 8], wherein R is an alicyclic cyclic group, an aromatic cyclic group or a heterocyclic cyclic group. 6. The [deleted text: compound] [inserted text: composition ]according to [deleted text: claims 2 or 5] [inserted text: claim 8], wherein       is selected from the group consisting of [deleted text:  -- CO -- (CH2)0_6_phenyl] [inserted text:  -- CO -- (CH2)0-6-phenyl], [deleted text:  -- CO -- (CH2)0_6_(1-naphthyl)] [inserted text:  -- CO -- (CH2)0-6-(1-naphthyl)], [deleted text:  -- CO -- (CH2)0_6_(2-naphthyl)] [inserted text:  -- CO -- (CH2)0-6-(2-naphthyl)], [deleted text:  -- CO -- (CH2)0_6_ -- CH(phenyl)2] [inserted text:  -- CO -- (CH2)0-6-CH(phenyl)2],  -- CO-(2-fluorophenyl),  -- CO -- cyclohexyl, [deleted text: c.about.-lipoyl] [inserted text: alpha -lipoyl], L-prolyl, D-prolyl, biotinyl  -- CO-(4-imidazolyl),  -- CO-(2-pyridyl),  -- CO-(2-thienyl),  -- CO-(2-furyl) and  -- CO-(3-furyl). 7. A process of obtaining a compound of general formula (I) or its cosmetically or pharmaceutically acceptable [deleted text: salts] [inserted text: salt ]according to claim 1, wherein 6-hydroxy-7-methoxy -2,2-dimethylchromane is reacted with the compound of general formula (II)   wherein X is selected from the group consisting of O and S;   R is a linear or branched, saturated or unsaturated aliphatic group with from 2 to 23 carbon atoms[deleted text: , or a cyclic group,] and which can contain substituents selected from the group consisting of hydroxy, alkoxy, amino, carboxyl, cyano, nitro, alkylsulfonyl and halogen atoms[deleted text: , or a cyclic group]; and Z is a free OH group[deleted text: , a reactive derivative thereof] or a halogen. 8. A cosmetic or pharmaceutical composition comprising[inserted text: :] a cosmetically or pharmaceutically effective amount of at least one compound of general formula (I)     or its cosmetically or pharmaceutically acceptable [deleted text: salts according to claim 1, comprises] [inserted text: salt, wherein R is a linear or branched, saturated or unsaturated aliphatic group containing 2 to 23 carbon atoms, or a cyclic group, and which can contain substituents selected from the group consisting of hydroxy, alkoxy, amino, carboxyl, cyano, nitro, alkylsulfonyl or halogen atoms; and   X is selected from the group consisting of O and S or its cosmetically or pharmaceutically acceptable salt; and]   at least one cosmetically or pharmaceutically acceptable excipient or adjuvant[inserted text: , and    wherein the compound of general formula (I) or its cosmetically or pharmaceutically acceptable salt is present at from 0.00000001% to 20% by weight of the composition]. 9. The cosmetic or pharmaceutical composition according to claim 8, wherein the compound of general formula (I) or its cosmetically or pharmaceutically acceptable [deleted text: salts] [inserted text: salt ]are incorporated in a cosmetically or pharmaceutically acceptable sustained release system or carrier selected from the group consisting of liposomes, millicapsules, microcapsules, nanocapsules, sponges, vesicles, micelles, millispheres, microspheres, nanospheres, lipospheres, microemulsions, nanoemulsions, milliparticles, microparticles and nanoparticles. 10. The cosmetic or pharmaceutical composition according to claim 8, wherein the compound of general formula (I) or its cosmetically or pharmaceutically acceptable [deleted text: salts] [inserted text: salt ]are adsorbed on a cosmetically or pharmaceutically acceptable organic polymer or solid mineral support selected from the group consisting of talc, bentonite, silica, starch and maltodextrin. 11. The cosmetic or pharmaceutical composition according to claim 8, wherein it has a formulation selected from the group consisting of creams, oil and/or silicone in water emulsions, water in oil and/or silicone emulsions, water/oil or silicone/water type emulsions, oil or silicone/water/oil or silicone type emulsions, oils, milks, balsams, foams, lotions, hydroalcoholic solutions, gels, liniments, serums, soaps, shampoos, ointments, mousses, salves, powders, bars, pencils, sprays or aerosols, capsules, [deleted text: including gelatin capsules,] tablets, [deleted text: including sugar-coated tablets,] powders, granulated forms, chewing gums, solutions, suspensions, emulsions, syrups, jellies and gelatin. 12. The cosmetic or pharmaceutical composition according to claim 8, wherein the compound of general formula (I) or its cosmetically or pharmaceutically acceptable [deleted text: salts] [inserted text: salt ]are incorporated in solid accessories selected from the group consisting of towelettes, hydrogels, adhesive patches, non-adhesive patches and face masks. 13. The cosmetic or pharmaceutical composition according to claim 8, wherein the compound of general formula (I) or its cosmetically or pharmaceutically acceptable [deleted text: salts] [inserted text: salt ]are incorporated in makeup products selected from the group consisting of under eye concealers, makeup bases, makeup removal lotions and makeup removal milks. 14. The cosmetic or pharmaceutical composition according to claim 8, wherein the compound of general formula (I) or its cosmetically or pharmaceutically acceptable [deleted text: salts] [inserted text: salt ]are incorporated in fabrics. 15. The cosmetic or pharmaceutical composition according to claim 8, wherein it further comprises an additional cosmetically or pharmaceutically effective amount of at least one active agent selected from the group consisting of a depigmenting or whitening agent, an anti-stretch mark agent, an anti-wrinkle agent, an antioxidant agent, an anti-glycation agent, an NO-synthase inhibitor, an anti-ageing agent, an agent capable of reducing or eliminating bags under the eyes, an exfoliating agent, emulsifying agents, emollients, organic solvents, liquid propellants, skin conditioners, wetting agents, moisture retaining substances, alpha hydroxy acids, moisturizers, vitamins, pigments or colorants, dyes, gelling polymers, thickeners, surfactants, softeners, an agent stimulating dermal or epidermal molecule synthesis and/or for preventing or inhibiting their degradation, an agent stimulating collagen synthesis, an agent stimulating decorin synthesis, an agent stimulating elastin synthesis, an agent stimulating laminin synthesis, an agent inhibiting collagen degradation, an agent inhibiting elastin degradation, an agent stimulating fibroblast and/or keratinocyte proliferation or for stimulating keratinocyte differentiation, agents stimulating lipid synthesis and synthesis of components of the stratum corneum, agents stimulating glycosaminoglycan synthesis, DNA repair agents, DNA protecting agents, agents stimulating defensin synthesis, agents stimulating chaperone synthesis, anti-pruritus agents, agents for treating sensitive skin, astringent agents, sebum production regulating agents, anti-cellulite agents, agents stimulating lipolysis, agents intended to improve the dermal-epidermal junction, a dermorelaxing agent, a [deleted text: reaffirming] [inserted text: firming ]agent, an anti-atmospheric contamination and/or free radical scavenger, an agent acting on capillary circulation and/or microcirculation, a calming agent, an anti-inflammatory agent, an antimicrobial agent, an antifungal agent, bactericides, an agent acting on cell metabolism, a chelating agent and/or an organic or mineral photoprotective agent active against ultraviolet A and/or B rays, and mixtures thereof. 16. The cosmetic or pharmaceutical composition according to claim 15, wherein the active agent is a desquamating agent selected from the group consisting of alpha hydroxy acids, beta hydroxy acids, urea [deleted text: and derivatives thereof], gentisic acid, cinnamic acid, jasmonic acid [deleted text: and derivatives thereof], oligofucoses, resveratrol, N-acetylglucosamine, Saphorajaponica extract, detergents and enzymes. 17. The cosmetic or pharmaceutical composition according to claim 15, wherein the active agent is an organic or mineral photoprotective agent active against ultraviolet A and/or B rays. 18. The cosmetic or pharmaceutical composition according to claim 15, wherein the active agent is a whitening or depigmenting agent selected from the group consisting of 6-hydroxy-7- methoxy-2,2-dimethylchromane, arbutin and isomers thereof, kojic acid [deleted text: and derivatives thereof], vitamin C [deleted text: and derivatives thereof including][inserted text: , ]6-O-palmitoylascorbic acid, magnesium salt of ascorbic acid-2-phosphate (MAP), sodium salt of ascorbic acid-2-phosphate (NAP), ascorbyl glucoside and ascorbyl tetraisopalmitate (VCIP), retinol [deleted text: and derivatives thereof including][inserted text: , ]tretinoin and isotretinoin, idebenone, hydroxybenzoic acid [deleted text: and derivatives thereof], flavonoids, soy extract, yeast extract, lemon extract, orange extract, ginkgo extract, cucumber extract, geranium extract, bearberry extract, carob bean extract, cinnamon extract, marjoram extract, rosemary extract, clove extract, soluble licorice extract, blackberry leaf extract, niacinamide, liquiritin, resorcinol [deleted text: and derivatives thereof], hydroquinone, alpha -tocopherol, Y-tocopherol, azelaic acid, resveratrol, mercury salts, linoleic acid, alpha -lipoic acid, dihydrolipoic acid, alpha hydroxy acids, beta hydroxy acids, ellagic acid, ferulic acid, cinnamic acid, oleanolic acid, aloesin [deleted text: and derivatives thereof], dithiaoctanediol, gluconic acid, beta- carotene, serine protease inhibitors, [deleted text: including tryptase, trypsin and PAR-2 inhibitors,] diacetylboldine, undecylenoyl phenylalanine, nonapeptide-1, amino ethyl phosphoric acid, Achillea millefolium extract, Alchemilla vulgaris extract, Aloe vera extract, Azadirachta indica extract, Arctostaphylos uva ursi leaf extract, Osmunda japonica extract, Artocarpus incisus extract, Bidens pylosa extract, Brassica napus extract, Broussonetia papyrifera extract, Chlorella vulgaris extract, Cimicifiiga racemosa extract, Emblica officinalis extract, Glycyrrhiza glabra extract, extract of Glycyrrhiza uralensis, Ilex purpurea extract, Ligusticum lucidum extract, Ligusticum wallichii extract, Malva sylvestris extract, Melissa officinalis leaf extract, Mentha piperita leaf extract, Mitracarpus scaber extract, Morinda citrifolia extract, Morus alba extract, Morus bombycis extract, Naringi crenulata extract, Pisum sativum extract, Primula veris extract, Prunus domesticus extract, Pseudostellariae radix extract, Rumex crispus extract, Rumex occidentalis extract, Sapindus mukurossi extract, Saxifraga sarmentosa extract, Scutellaria galericulata extract, Sedum sarmentosum Bunge extract, Stellaria medica extract, Triticum Vulgare extract, Uva ursi extract, Veronica officinalis extract, Withania somnifera extract and leukocyte extract. 19. A method for treating, caring for, or cleaning skin, hair or nails in a subject in need of such treatment comprising applying to said subject a cosmetic or pharmaceutical composition comprising a compound of general formula (I)       or its cosmetically or pharmaceutically acceptable [deleted text: salts according to claim 1] [inserted text: salt, wherein   R is a linear or branched, saturated or unsaturated aliphatic group containing 2 to 23 carbon atoms, or a cyclic group, and which can contain substituents selected from the group consisting of hydroxy, alkoxy, amino, carboxyl, cyano, nitro, alkylsulfonyl or halogen atoms; and   X is selected from the group consisting of O and S]. 20. A method of regulating the pigmentation of the skin, hair or nails in a subject in need of such regulating, comprising applying to said subject a cosmetic or pharmaceutical composition [deleted text: comprising a compound of general formula (I) or its cosmetically or pharmaceutically acceptable salts] according to claim [deleted text: 1] [inserted text: 8]. 21. A method for whitening or lightening the skin in a subject in need of such whitening or lightening comprising applying to said subject a cosmetic or pharmaceutical composition [deleted text: comprising a compound of general formula (I) or its cosmetically or pharmaceutically acceptable salts] according to claim [deleted text: 1] [inserted text: 8]. 22. A method for treating skin pigmentation disorders or pathologies in a subject in need of such treatment, comprising applying to said subject a cosmetic or pharmaceutical composition [deleted text: comprising a compound of general formula (I) or its cosmetically or pharmaceutically acceptable salts] according to claim [deleted text: 1] [inserted text: 8]. 23. A method for reducing or delaying the signs of aging or photoaging in a subject in need of such delaying or reducing, comprising applying to said subject a cosmetic or pharmaceutical composition [deleted text: comprising a compound of general formula (I) or its cosmetically or pharmaceutically acceptable salts] according to claim [deleted text: 1] [inserted text: 8]. 24. A method for photoprotecting skin, hair or nails in a subject in need of such photoprotecting, comprising applying to said subject a cosmetic or pharmaceutical composition comprising a compound of general formula (I) or its cosmetically or pharmaceutically acceptable salts according to claim 1. 25. The method according to any one of claims 19-24 wherein said applying comprises topical or transdermal application of said composition. [inserted text: 26.  The compound according to claim 1, wherein R is CH3(CH2)14 -- .] [inserted text: 27.  The compound according to claim 1, wherein the compound is 7-methoxy-6-palmitoyl-2,2-dimethylchromane.] [inserted text: 28.  A compound of general formula (I)       or its cosmetically or pharmaceutically acceptable salt, wherein R is     and   X is selected from the group consisting of O and S.] [inserted text: 29.  The cosmetic or pharmaceutical composition according to claim 8, wherein the compound of general formula (I) or its cosmetically or pharmaceutically acceptable salt is present at between 0.00001% and 10% by weight of the composition.] [inserted text: 30.  The composition according to claim 3, wherein       is selected from the group consisting of tert-butanoyl, hexanoyl, 2-methylhexanoyl, octanoyl, decanoyl, lauroyl, myristoyl, palmitoyl, stearoyl, oleoyl and linoleoyl.]
法律状态
(USRE46228) LEGAL DETAILS FOR USRE46228  Actual or expected expiration date=2028-09-12    Legal state=ALIVE    Status=GRANTED     Event publication date=2008-04-11  Event code=US/APP  Event indicator=Pos  Event type=Examination events  Application details  Application country=US US14175312  Application date=2008-04-11  Standardized application number=2008US-14175312     Event publication date=2016-12-06  Event code=US/E  Event indicator=Pos  Event type=Event indicating In Force  Reissue  Publication country=US  Publication number=USRE46228  Publication stage Code=E  Publication date=2016-12-06  Standardized publication number=USRE46228
专利类型码
E
国别省市代码
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