DE 195 45 107 A 1
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`DE 195 45 107 A1
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`19
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`FEDERAL REPUBLIC
`OF GERMANY
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`12
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` Offenlegungsschrift
` DE 195 45 107 A1
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`43
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`GERMAN
`PATENT OFFICE
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`File reference:
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`195 45 107.4
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`Filing date:
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` 4. 12. 95
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`Date laid open:
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` 5. 6. 97
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`51
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`Int. Cl.6:
`A 61 K 7/42
`A 61K 31/70
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`A 61 K 7/48
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`Applicant:
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`Beiersdorf AG, 20253 Hamburg, DE
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`Inventors:
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`Schönrock, Uwe, Dr., 22844 Norderstedt, DE; Pollet,
`Dieter, Dr., 22523 Hamburg, DE; Schreiner, Volker, Dr.,
`22523 Hamburg, DE; Märker, Uwe, 22085 Hamburg,
`DE; Kruse, Inge, 20146 Hamburg, DE
`
`
`Documents to be taken into consideration in assessing
`patentability:
` DE 34 47 618 C2
` DE 43 23 615 A1
` DE 33 19 282 A1
` DE 26 17 919 A1
` DE-OS 24 01 450
`= US 40 88 756
` FR 26 51 434 A1
` FR 26 49 610 A1
` FR 26 47 342 A1
` FR 26 34 374 A1
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`
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`US 39 37 809
`EP 04 84 199 B1
`EP 02 56 472 A3
`EP 02 56 472 A2
`Derwent Abstract, 84-227814/37 to J5 9134-707-A;
`JP Patents Abstracts of Japan: 63-152309
`A.,C-541,Nov. 8,1988,Vol.12,No.421;
`6- 80564 A.,C-1217,June 27,1994,Vol.18,No.337;
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` Use of adenosine for enhancing cell proliferation in
`human skin.
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`Use of an effective content of adenosine in cosmetic or dermatological preparations
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` The following details have been taken from the documents submitted by the Applicant
`BUNDESDRUCKEREI
`04.97
`
`702 023/445
`
`9/24
`
`L'OREAL USA, INC. EX. 1004
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`- 0 -
`
`

`

`
`
`DESCRIPTION
`
`The present invention relates to the use of adenosine
`
`in cosmetic and dermatological preparations.
`
`5
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`
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`In a separate embodiment, the present invention relates
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`to cosmetic and dermatological preparations for the
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`prevention and therapy of cosmetic or dermatological
`
`skin changes such as, for example, skin aging.
`
`10
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`
`
`The skin ages because of endogenous, genetically
`
`determined influences. Exogenous factors, such as UV-
`
`light and chemical irritants, can have cumulative
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`effects and accelerate the natural aging processes.
`
`15
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`This produces a number of degenerative processes whose
`
`results include the following structural changes and
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`insult in the dermis and epidermis (dermatoheliosis),
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`depending on the magnitude of the influencing factors:
`a) Involution of the microvascular system.
`b) Loosening and formation of wrinkles in part due to
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`20
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`the reduction and cross-linking of collagen and
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`accumulation of glucosaminoglycans (basic substance).
`c) Flattening of the reticular plugs. In conjunction
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`with this is the surface reduction between dermis and
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`25
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`epidermis, through which substances for the nourishment
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`and cleansing of the epidermis are exchanged.
`d) Limited regenerative turnover in the epidermis in
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`conjunction with abnormal formation of the horny layer
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`(hornification) that leads to drying out of the skin.
`e) Abnormal regulation of cell division (proliferation)
`
`30
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`and cell maturation (differentiation) in the epidermis
`
`resulting in atypical cells and polarity loss.
`f) Local hyper-, hypo-, and abnormal pigmentations (age
`
`spots).
`
`35
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`
`
`Accordingly, the present invention relates to products
`
`for the care and prevention of aged skin and for the
`
`therapy of the damage resulting from skin aging, in
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`particular those phenomena listed in a) to f).
`
`- 1 -
`
`

`

`- 2 -
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`It was surprising and unforeseeable by the specialist
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`that for enhancement of cell proliferation in human
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`skin, preferably in cosmetic or dermatological
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`preparations, remedies the drawbacks of the prior art.
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`5
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`
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`In one particular embodiment, the present invention
`
`accordingly relates to the use of adenosine for the
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`care and prevention of aged skin and for the therapy of
`
`the damage resulting from skin aging, in particular
`
`10
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`those phenomena listed in a) to f).
`
`
`
`Adenosine is characterized by the structural formula:
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`15
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`DE-OS 24 01 450 discloses pharmaceutical compositions
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`for the relief of proliferative skin diseases
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`containing an effective adenosine content. Furthermore;
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`several prior art documents are known that deal with
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`the cosmetic or dermatological use of adenosine
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`20
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`phosphates (cyclic adenosine-3'5'-monophosphate = cAMP,
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`adenosine monophosphate = AMP, adenosine diphosphate =
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`ADP, adenosine triphosphate = ATP), for example US
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`patent specification 4,702,913, in which the use of ATP
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`and cAMP as substances enhancing skin moisture is
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`25
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`discussed. The prior art does not, however, provide an
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`indication of the use according to this invention.
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`According to the use as described in the invention,
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`cosmetic or dermatological formulations can be composed
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`30
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`as usual and used for the treatment, care and cleansing
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`of the skin and/or hair, and as a make-up product in
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`

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`- 3 -
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`decorative cosmetics. They contain preferably 0.001% by
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`weight to 10% by weight, but particularly 0.01% by
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`weight to 6% by weight, of the active substance
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`combinations according to the invention relative to the
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`5
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`total weight of the product.
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`For use according to the invention, the cosmetic and
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`dermatological preparations are — applied in sufficient
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`quantity to the skin and/or hair in the manner
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`10
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`conventional for cosmetics.
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`Cosmetic and dermatological preparations can be in
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`various forms for use according to the invention. For
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`example, they can be a solution, a non-aqueous
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`15
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`preparation, a water-in-oil (W/O) or oil-in-water (O/W)
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`emulsion or microemulsion, a multiple emulsion such as
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`a water-in-oil-in-water (W/O/W) emulsion, a gel, a
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`solid stick, a salve or even an aerosol. Adenosine can
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`also be advantageously administered in encapsulated
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`20
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`form according to the invention, for example in
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`collagen matrices and other conventional encapsulation
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`materials, for example as cellulose encapsulations, in
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`gelatins, wax matrices or encapsulated in liposomes. In
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`particular, wax matrices as disclosed in DE-OS 43 08
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`25
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`282 have been shown to be advantageous.
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`The addition of adenosine to aqueous systems or tenside
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`preparations for cleansing the skin and the hair is
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`also possible and advantageous according to the present
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`30
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`invention.
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`In keeping with the use according to the invention,
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`cosmetic and dermatological preparations can contain
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`cosmetic adjuvants as conventionally used in such
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`35
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`preparations, for example preservatives, bactericides,
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`fragrances, anti-foaming agents, dyes, pigments having
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`a
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`coloring
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`effect,
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`thickeners,
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`surfactants,
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`emulsifiers, softening, wetting and/or moisture-
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`retaining substances, fats, oils, waxes or other
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`- 4 -
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`conventional components of a cosmetic or dermatological
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`formulation like alcohols, polyols, polymers, foam
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`stabilizers, electrolytes, organic solvents or silicone
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`derivates.
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`5
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`In particular, adenosine can also be combined with
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`antioxidants.
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`According to the invention, all antioxidants suitable
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`10
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`or
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`usable
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`in
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`cosmetic
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`and/or
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`dermatological
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`applications
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`can
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`be
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`used
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`advantageously
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`as
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`antioxidants.
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`It is advantageous to select the antioxidants from the
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`15
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`group comprised of amino acids (for example; glycine,
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`histidine, tyrosine, tryptophan) and their derivatives,
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`imidazoles (for example, urocanic acid) and their
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`derivatives, peptides such as D,L-carnosine, D-
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`carnosine, L-carnosine and their derivatives (for
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`20
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`example,
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`anserine);
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`carotenoids,
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`carotenes
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`(for
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`example, α-carotene, β-carotene, lycopine) and their
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`derivatives; chlorogenic acid and its derivatives,
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`liponic acid and its derivatives (for example,
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`dihydroliponic acid), aurothioglucose, propylthiouracil
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`25
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`and other thiols (for example, thioredoxin, glutathion,
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`cysteine, cystine, cystamine and their glycosyl-, N-
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`acetyl-, methyl-, ethyl-, propyl-, amyl-, butyl- and
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`lauryl-, palmitoyl-, oleyl-, γ-linoleyl-, cholesteryl-
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`and
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`glyceryl
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`esters)
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`and
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`their
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`salts,
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`30
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`dilaurylthiodipropionate,
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`distearylthiodipropionate,
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`thiodipropionic acid and their derivatives (esters,
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`ethers, peptides, lipids, nucleotides, nucleosides and
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`salts) and sulfoximine compounds (for example,
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`buthionine
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`sulfoximine,
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`homocysteine
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`sulfoximine,
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`35
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`buthionine sulfone, penta-, hexa-, heptathionine
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`sulfoximine) in very low, tolerable doses (for example,
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`pmol to µmol/kg); in addition, (metal) chelators (for
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`example, α-hydroxy fatty acids, palmitic acid, phytinic
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`acid, lactoferrin), α-hydroxy acids (for example,
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`- 5 -
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`citric acid, lactic acid, malic acid), humic acid, bile
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`acid, bile extracts, bilirubin, biliverdin, EDTA, EGTA
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`and their derivatives; unsaturated fatty acids and
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`their derivatives (such as y-linoleic acid, linolic
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`5
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`acid, oleic acid), folic acid and its derivatives,
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`ubiquinone and ubiquinol and their derivatives; vitamin
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`C and its derivatives (for example, ascorbyl palmitate,
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`Mg-ascorbyl phosphate, ascorbyl acetate), tocopherols
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`and derivatives (for example, vitamin E acetate),
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`10
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`vitamin A and derivatives (vitamin A palmitate) and
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`coniferyl benzoate of benzoic resin, rutic acid and its
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`derivatives; butylhydroxytoluene, butylhydroxyanisol,
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`nor-dihydroguaiac resin acid, nordihydroguaiaretic
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`acid, trihydroxybutyrophenone, uric acid and its
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`15
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`derivates, mannose and its derivatives, sesamol,
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`sesamolin, zinc and its derivatives (for example, ZnO,
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`ZnSO4), selenium and its derivatives (for example,
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`selenium methionine), stilbene and its derivatives (for
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`example, stilbene oxide, trans-stilbene oxide) and the
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`20
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`suitable derivatives according to the invention (salts,
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`esters, ethers, sugars, nucleotides, nucleosides,
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`peptides and lipids) of said active substances.
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`
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`The quantity of the abovementioned antioxidants (one or
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`25
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`a plurality of compounds) in the preparations is
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`preferably 0.001 to 30% by weight, particularly
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`preferred 0.05 — 20% by weight, particularly 1-10% by
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`weight, relative to the total weight of the
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`formulation.
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`30
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`
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`In so far as vitamin E and/or its derivatives represent
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`the antioxidant or antioxidants, it is advantageous if
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`their respective concentrations are chosen from the
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`range of 0.001 — 10% by weight relative to the total
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`35
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`weight of the formulation.
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`Insofar as vitamin A or vitamin A derivatives, or
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`carotene or its derivatives are the antioxidant(s), it
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`is advantageous if their respective concentrations are
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`

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`- 6 -
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`chosen from the range of 0.001 — 10% by weight relative
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`to the total weight of the formulation.
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`Emulsions according to the invention are advantageous
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`5
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`and contain, for example, the said fats, oils, waxes
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`and other fatty substances and also water and an
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`emulsifier as is conventionally used for such a
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`formulation.
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`10
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`The lipid phase can be advantageously selected here
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`from the following group of substances:
`— natural, synthetic and/or semi-synthetic oils like
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`triglycerides of capric or caprylic acid, preferably,
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`however, castor oil;
`− fats, waxes and other natural, synthetic and/or semi-
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`15
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`synthetic fatty substances, preferably esters of fatty
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`acids with low-carbon alcohols, for example with
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`isopropanol, propylene glycol or glycerin, or esters of
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`fatty alcohols with low-carbon alkanoic acids or with
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`20
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`fatty acids;
`− silicone
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`oils
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`such
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`as
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`dimethylpolysiloxane,
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`diethylpolysiloxane, diphenylpolysiloxane and mixed
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`forms of same;
`− saturated compounds such as hydrocarbons of natural
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`25
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`or synthetic origin (vaseline, squalane).
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`The aqueous phase of the preparations according to the
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`invention
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`may
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`advantageously
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`contain
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`low-carbon
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`alcohols, diols or polyols and their ethers, preferably
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`30
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`ethanol, isopropanol, propylene glycol, glycerin,
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`ethylene glycol, ethylene glycol monoethyl or monobutyl
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`ether, propylene glycol monomethyl, monoethyl or
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`monobutyl ether, diethylene glycol monomethyl or
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`monoethyl ether and analog products, further low-carbon
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`35
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`alcohols such as ethanol, isopropanol, 1,2-propane
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`diol, glycerin and particularly one or a plurality of
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`thickeners which can be advantageously selected from
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`the group of silicon dioxide, aluminum silicates,
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`polysaccharides or their derivatives such as hyaluronic
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`

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`- 7 -
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`acid, xanthan gums, hydroxypropylmethyl cellulose,
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`particularly advantageously from the polyacrylate
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`group, preferably a polyacrylate from the group of so-
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`called carbopols, for example type 980, 981, 1382,
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`5
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`2984, 5984 carbopols, or even the ETD (easy-to-
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`disperse) 2001, 2020, 2050 types, either singly or in
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`any combinations.
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`In particular, mixtures of the solvents mentioned above
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`10
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`are used. When alcoholic solvents are used, water can
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`be a further component.
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`Emulsions according to the invention are advantageous
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`and contain, for example, the mentioned fats, oils,
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`15
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`waxes and other fatty substances and also water and an
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`emulsifier as is conventionally used for such
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`formulations.
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`Gels according to the invention conventionally contain
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`20
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`low-carbon alcohols, for example ethanol, isopropanol,
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`1,2-propane diol, glycerin and water or one of the
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`above-named oils in the presence of a thickening agent,
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`which in the case of oil-alcohol gels is preferably
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`silicon dioxide or an aluminum silicate, or in the case
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`25
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`of aqueous-alcoholic or alcoholic gels is preferably a
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`polyacrylate.
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`As a propellant for sprayable preparations in aerosol
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`containers
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`according
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`to
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`the
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`invention,
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`the
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`30
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`conventionally
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`known
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`highly-volatile,
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`liquidized
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`propellants, for example hydrocarbons (propane, butane,
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`isobutane) are suitable and can be used alone or in
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`combination with each other. Compressed air can also be
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`used advantageously.
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`35
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`
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`Preparations according to the invention can furthermore
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`advantageously contain substances that absorb UV-rays
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`in the UVB range, whereby the total quantity of filter
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`substances, for example 0.1% by weight to 30% by
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`

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`- 8 -
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`weight, preferably 0.5 to 10% by weight, in particular
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`1.0 to 6.0% by weight relative to the total weight of
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`the preparations, in order to provide cosmetic
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`preparations that protect the hair or the skin against
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`5
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`the entire range of ultraviolet radiation. They can
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`also be used as sun screens for the hair or the skin.
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`
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`If the emulsions according to the invention contain UVB
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`filtering agents, they can be oil-soluble or water-
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`10
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`soluble. Advantageous oil-soluble UVB filters according
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`to the invention include, for example:
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`-
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`3-benzylidene camphor derivatives, preferably 3-
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`(4-methylbenzylidene) camphor, 3-benzylidene camphor;
`—
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`4-amino benzoic acid derivatives, preferably 4-
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`15
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`(dimethylamino)- benzoic acid (2-ethylhexyl) ester, 4-
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`(dimethylamino) benzoic acid amyl ester;
`—
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`cinnamic
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`acid,
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`preferably
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`Esters
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`of
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`4-
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`4-
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`methoxycinnamic
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`acid
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`(2-ethylhexyl)
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`ester,
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`methoxycinnamic acid isopentyl ester;
`—
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`Esters of salicylic acid, preferably salicylic
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`20
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`acid
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`(2-ethylhexyl)
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`ester,
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`salicylic
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`acid
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`(4-
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`isopropylbenzyl) ester, salicylic acid homomenthyl
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`ester;
`−
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`Derivatives of benzophenone, preferably 2-hydroxy-
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`25
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`4-methoxybenzophenone,
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`2-hydroxy-4-methoxy-4'-
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`methylbenzophenone,
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`2,2'-dihydroxy-4-
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`methoxybenzophenone;
`−
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`Esters of benzalmalonic acid, preferably 4-
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`methoxybenzalmalonic acid di(2-ethylhexyl)ester,
`−
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`-2,4,6-trianilino-(p-carbo-2'-ethyl-1'-hexyloxy)-
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`30
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`1,3,5 triazine.
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`Advantageous water-soluble .UVB filters are, for
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`example:
`−
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`Salts of 2-phenylbenzimidazol-5-sulfonic acid such
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`35
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`as its sodium, potassium or its triethanol ammonium
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`salt, and also sulfonic acid itself;
`
`

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`- 9 -
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`−
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`Sulfonic
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`acid
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`derivates
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`of
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`benzophenones,
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`preferably
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`2-hydroxy-4-methoxybenzophenone-5-sulfonic
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`acid and its salts;
`−
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`Sulfonic acid derivatives of 3-benzylidene camphor
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`5
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`such as, for example, 4-(2-oxo-3-bornylidene methyl)
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`benzene sulfonic acid, 2-methyl-5-(2-oxo-3-bornylidene
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`methyl) sulfonic acid and its salts.
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`
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`The list of cited UVB filters that can be used together
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`10
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`with the active substance combinations according to the
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`invention is, of course, not restricted.
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`
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`The subject of the invention is also the use of a
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`combination of adenosine with at least one UVB filter
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`15
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`as an antioxidant, or the use of adenosine with at
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`least one UVB filter as an antioxidant in a cosmetic or
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`dermatological preparation.
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`
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`It can also be advantageous if adenosine is combined
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`20
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`with UVA filters that are conventionally contained in
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`cosmetic preparations. These substances are preferably
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`derivatives of dibenzoyl methane, in particular 1-(4'-
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`tert.-butylpheny1)-3-(4'-methoxyphenyl)
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`propane-1,3-
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`dione and 1-phenyl-3-(4'-isopropylphenyl) propane-1,3-
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`25
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`dione. These combinations or preparations that contain
`
`these combinations, are also the object of the
`
`invention. Those quantities used for the UVB
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`combination can be used.
`
` A
`
` subject of the invention is also the use of a
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`30
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`combination of adenosine with at least one UVA filter
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`as an antioxidant, or the use of a combination of
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`adenosine with at least one UVA filter as an
`
`antioxidant
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`in
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`a
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`cosmetic
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`or
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`dermatological
`
`35
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`preparation.
`
` A
`
` subject of the invention is also the use of a
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`combination of adenosine with at least one UVA filter
`
`and at least one UVB filter as an antioxidant, or the
`
`

`

`- 10 -
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`use of a combination of adenosine with at least one UVA
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`filter and at least one UVB filter as an antioxidant in
`
`a cosmetic or dermatological preparation.
`
`
`
`5
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`Cosmetic and dermatological preparations having an
`
`effective adenosine content can also contain inorganic
`
`pigments that are conventionally used in cosmetics for
`
`the purpose of protecting the skin against UV rays.
`
`These are oxides of titanium, zinc, iron, zirconium,
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`10
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`silicon, manganese, aluminum, cerium and mixtures
`
`thereof as well as alterations in which the oxides are
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`the active substances.
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`
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`Titanium-dioxide-based
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`pigments
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`are
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`particularly
`
`15
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`preferred.
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`
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`The cosmetic and dermatological preparations for the
`
`protection of hair against UV rays pursuant to the
`
`invention, are for example, shampoos, preparations
`
`20
`
`applied when rinsing the hair before or after
`
`shampooing, before or after permanent waving, before or
`
`after dyeing or bleaching the hair, preparations for
`
`blow drying or setting the hair, preparations for
`
`dyeing or bleaching, hairdressing and treatment lotion,
`
`25
`
`hair lacquer, or permanent waving agents.
`
`
`
`The cosmetic and dermatological preparations contain
`
`active
`
`ingredients
`
`and
`
`adjuvants
`
`as
`
`used
`
`in
`
`conventional preparations of this type for hair care
`
`30
`
`and hair treatment. The adjuvants that are used are
`
`preservatives, surfactants, foam inhibiting substances,
`
`thickeners, emulsifiers, fats, oils, waxes, organic
`
`solvents, bactericides, perfumes, dyes or pigments
`
`whose purpose is to color the hair or the cosmetic or
`
`35
`
`dermatological preparation itself, electrolytes, and
`
`substances against oily hair.
`
`
`
`According to the present invention, electrolytes are
`
`understood to be water-soluble alkali metal, ammonia,
`
`

`

`- 11 -
`
`alkaline earth metal (including magnesium) and zinc
`
`salts of inorganic anions and any mixture of such
`
`salts, whereby it must be assured that said salts are
`
`pharmaceutically and cosmetically safe.
`
`5
`
`
`
`The anions according to the invention are preferably
`
`chosen from the group of chlorides, sulfates and
`
`hydrogen sulfates, phosphates, hydrogen phosphates and
`
`linear and cyclic oligophosphates as well as carbonates
`
`10
`
`and hydrogen carbonates.
`
`
`
`Cosmetic preparations as represented by skin cleansing
`
`agents or shampoos preferably contain at least one
`
`anionic,
`
`non-ionic
`
`or
`
`amphoteric
`
`surface-active
`
`15
`
`substance or also a mixture of such substances,
`
`adenosine in aqueous medium and an adjuvant as are
`
`conventionally used therefor. The surface-active
`
`substance or the mixtures of said substances can be
`
`used at a concentration between 1% by weight and 50% by
`
`20
`
`weight in the shampoo.
`
`
`
`If the cosmetic or dermatological preparations are in
`
`the form of a lotion that is rinsed out and applied,
`
`for example before or after bleaching, before or after
`
`25
`
`shampooing, between two shampoo applications, before or
`
`after permanent wave treatment, then aqueous or water-
`
`alcohol solutions are used that may contain surface-
`
`active substances whose concentration can be between
`
`0.1 and 10% by weight, preferably between 0.2 and 5% by
`
`30
`
`weight
`
`
`
`Said cosmetic or dermatological preparations can also
`
`be aerosols having the conventional adjuvants used
`
`therefor.
`
`35
`
`
`
`A cosmetic preparation in the form of a lotion that is
`
`not rinsed out, in particular a hair-setting lotion, a
`
`lotion that is used when blow-drying hair, a
`
`hairdressing and treatment lotion generally is an
`
`

`

`- 12 -
`
`aqueous, alcoholic or water-alcohol solution and
`
`contains at least one cationic, anionic, non-ionic, or
`
`amphoteric polymer, or their mixtures as well as
`
`adenosine in an effective concentration. The quantity
`
`5
`
`of the polymers used is, for example, between 0.1 and
`
`10% by weight, preferably between 0.1 and 3% by weight
`
`
`
`Cosmetic preparations for the treatment and care of
`
`hair that contain adenosine can be non-ionic or anionic
`
`10
`
`type emulsions. Along with water, non-ionic emulsions
`
`contain oils or fatty alcohols that can be also
`
`polyethoxylated or polypropoxylated, for example, or
`
`mixtures comprised of both organic components. Said
`
`emulsions
`
`may
`
`contain
`
`cationic
`
`surface-active
`
`15
`
`substances.
`
`
`
`According to the invention, cosmetic preparations for
`
`the treatment and care of the hair can be gels that,
`
`along with an effective content of adenosine and
`
`20
`
`conventional solvents, preferably contain water,
`
`organic thickening agents such as gum arabic, xanthan
`
`gum, sodium alginate; derivatives of cellulose,
`
`preferably methyl cellulose, hydroxymethyl cellulose,
`
`hydroxyethyl
`
`cellulose,
`
`hydroxypropyl
`
`cellulose,
`
`25
`
`hydroxypropylmethyl cellulose or inorganic thickening
`
`agents such as aluminum silicates such as bentonite, or
`
`a mixture of polyethylene glycol and polyethylene
`
`glycol stearate or distearate. The gel contains the
`
`thickening agent in a quantity e.g. between 0.1 and 30%
`
`30
`
`by weight, and preferably between 0.5 and 15% by
`
`weight.
`
`
`
`Preferably, the quantity of adenosine in a particular
`
`product for the hair is 0.05% by weight to 10% by
`
`35
`
`weight, in particular 0.5% by weight to 5% by weight,
`
`relative to the total weight of the product.
`
`
`
`According to the invention, aqueous cosmetic cleansing
`
`agents or low-water or anhydrous cleansing concentrates
`
`

`

`- 13 -
`
`used for aqueous cleansing can contain anionic, non-
`
`ionic and/or amphoteric tensides, such as:
`−
`
`conventional soaps, for example sodium salts of
`
`fatty acids
`−
`
`alkyl sulfates, alkyl ether sulfates, alkane and
`
`alkylbenzene sulfonates
`−
`
`sulfoacetate
`
`sulfobetaine
`
`sarcosinate
`
`amidosulfobetaine
`
`sulfosuccinate
`
`sulfosuccinic acid mono ester
`
`alkylether carboxylate
`
`protein-fatty acid condensates
`
`alkyl betaine and amidobetaine
`
`fatty acid alkanolamide
`
`polyglycol ether derivatives
`
`−
`
`−
`—
`−
`—
`−
`—
`−
`
`−
`—
`
`
`
`5
`
`10
`
`15
`
`Cosmetic preparations that are cosmetic cleansing
`
`20
`
`preparations for the skin can be in liquid or solid
`
`form. Along with adenosine, they preferably contain at
`
`least one anionic, non-ionic or amphoteric surface-
`
`active substance or mixtures thereof, and one or a
`
`plurality of electrolytes and adjuvants as used
`
`25
`
`conventionally therefor, as desired. The surface-active
`
`substance can be present in the cleansing preparations
`
`at a concentration between 1 and 94% by weight relative
`
`to the total weight of the preparations.
`
`
`
`30
`
`Along with an effective adenosine content, cosmetic
`
`preparations that are shampoos contain preferably at
`
`least one anionic, non-ionic or amphoteric surface-
`
`active substance or mixtures thereof, or possibly an
`
`electrolyte and adjuvant according to the invention as
`
`35
`
`used by conventionally therefor. The surface-active
`
`substance can be in a concentration between 1% by
`
`weight and 94% by weight in the shampoo.
`
`
`
`

`

`- 14 -
`
`In addition to the above-cited tensides, the
`
`compositions according to the invention contain water
`
`and possibly the conventional cosmetic additives such
`
`as
`
`fragrance,
`
`thickeners,
`
`dyes,
`
`deodorants,
`
`5
`
`antimicrobial
`
`substances,
`
`moisturizing
`
`agents,
`
`complexing and sequestration agents, pearl luster
`
`agents, plant extracts, vitamins, active substances,
`
`and the like.
`
`
`
`10
`
`The present invention also includes a cosmetic process
`
`for protection of the skin and hair against oxidative
`
`or photoxidative processes which is characterized in
`
`that a cosmetic agent containing an effective adenosine
`
`concentration is applied in sufficient quantity to the
`
`15
`
`skin or hair.
`
`
`
`The adenosine content in said preparations is
`
`preferably 0.001% by weight to 10% by weight, and
`
`particularly 0.01% by weight to 6% by weight relative
`
`20
`
`to the total weight of the preparations.
`
`
`
`The subject of the invention is also the method for
`
`manufacturing the cosmetic products according to the
`
`invention and is characterized in that adenosine is
`
`25
`
`incorporated
`
`into
`
`cosmetic
`
`and
`
`dermatological
`
`formulations in a manner known per se.
`
`
`
`The following examples are intended to clarify the
`
`present invention but not restrict it. All indications
`
`30
`
`of quantities, portions and percentages, unless
`
`otherwise indicated, refer to the weight and the total
`
`quantity or to the total weight of the preparations.
`
`
`
`
`
`35
`
`Cetearyl alcohol
`
`Example 1
`
`O/W Sunscreen Lotion
`
`Wt. %
`
`2.50
`
`PEG-40 castor oil / sodium cetearyl sulfate
`
`
`
`Caprylic / capric triglyceride
`
`4.00
`
`

`

`- 15 -
`
`Octyl stearate
`
`Octyl methoxycinnamate
`
`Butyl methoxydibenzoyl methane
`
`Cyclodimethicone
`
`Carbomer
`
`NaOH (45%)
`
`Na3 HEDTA
`
`Butylene glycol
`
`Adenosine
`
`Preservative / fragrance
`
`Water, add until
`
`
`
`
`
`Example 2
`
`O/W After-Sun Lotion
`
`Stearic acid
`
`Glyceryl stearate
`
`Isopropyl palmitate
`
`Caprylic / capric triglyceride
`
`Buxus chinensis
`
`Carbomer
`
`NaOH (45%)
`
`Glycerin
`
`Ethanol
`
`Adenosine
`
`Preservative / fragrance
`
`Water, add until
`
`5
`
`
`
`
`
`Example 3
`
`O/W Sun Cream
`
`Stearic acid
`
`Octyl dodecanol
`
`Isopropyl palmitate
`
`Cyclomethicone
`
`Methylbenzylidene camphor
`
`Butyl methoxydibenzoylmethane
`
`Cetyl alcohol
`
`Na3 HEDTA
`
`4.00
`
`5.50
`
`0.70
`
`1.00
`
`0.27
`
`0.22
`
`1.00
`
`5.00
`
`0.10
`
`q.s.
`
`100.00
`
`Wt. %
`
`2.00
`
`1.00
`
`6.00
`
`5.00
`
`2.00
`
`0.20
`
`0.20
`
`5.00
`
`5.00
`
`0.10
`
`q.s.
`
`100.00
`
`Wt. %
`
`3.50
`
`1.00
`
`5.00
`
`4.00
`
`1.00
`
`3.00
`
`1.00
`
`5.00
`
`

`

`- 16 -
`
`NaOH (45%)
`
`Glycerin
`
`Adenosine
`
`Preservative / fragrance
`
`Water, add until
`
`
`
`
`
`Example 4
`
`O/W Cream
`
`Trilaureth-4-phosphate
`
`Cera microcristallina, paraffinum liquidum
`
`Isopropyl palmitate
`
`Cetyl alcohol
`
`Adenosine
`
`Glycerin
`
`Preservative / fragrance
`
`Water, add until
`
`5
`
`
`
`
`
`Example 5
`
`O/W Cream
`
`Glyceryl stearate
`
`Behenyl alcohol
`
`Isopropyl palmitate
`
`Octyl dodecanol
`
`Glycerin
`
`Adenosine
`
`Preservative / fragrance
`
`Water, add until
`
`
`
`
`
`Example 6
`
`O/W Cream
`
`Polyglycery1-3-diisostearate
`
`Paraffin oil
`
`Ceresin
`
`Magnesium stearate
`
`Magnesium sulfate
`
`Adenosine
`
`1.00
`
`0.40
`
`0.10
`
`q.s.
`
`100.00
`
`Wt. %
`
`2.00
`
`5.00
`
`5.00
`
`5.00
`
`0.10
`
`5.00
`
`q.s.
`
`100.00
`
`Wt. %
`
`3.00
`
`5.00
`
`3.00
`
`3.00
`
`5.00
`
`0.10
`
`q.s.
`
`100.00
`
`Wt. %
`
`2.50
`
`15.00
`
`3.00
`
`3.00
`
`0.70
`
`0.10
`
`

`

`- 17 -
`
`Glycerin
`
`Preservative / fragrance
`
`Water, add until
`
`3.00
`
`q.s.
`
`100.00
`
`

`

`- 18 -
`
`PATENT CLAIMS
`
`
`
`1.
`
`The use of adenosine for enhancing cell
`
`proliferation in human skin.
`
`5
`
`
`
`2.
`
`The use of adenosine for combating and relief of
`
`the symptoms of exogenous aging of the skin, preferably
`
`in cosmetic or dermatological preparations.
`
`
`
`10
`
`3.
`
`The use as claimed in claim 1 or 2, characterized
`
`in that the adenosine in cosmetic or dermatological
`
`preparations is present in concentrations of 0.01% by
`
`weight to 10% by weight, but particularly 0.1% by
`
`weight, to 6% by weight, relative in each case to the
`
`15
`
`total weight of the preparations.
`
`

`

`
`
`
`
`German Patent and Trademark Office
`
`The President
`
`
`
`
`
`
`
`Certification
`
`
`
`
`
`
`
`It is hereby confirmed that the attached photocopies correspond to the first publication of
`
`the application that is present in the library of the German Patent and Trademark Office.
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`Munich, September 1, 2017
`
`pp.
`
`
`
`
`
`[signed]
`
`Zellner
`
`File reference: 195 45 107.4
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`- 19 -
`
`

`

`
`
`
`
`
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`
`
`
`
`
`
`
`I, Neil Thomas SIMPKIN BA,
`
`translator to RWS Group Ltd, of Europa House, Chiltern Park, Chiltern Hill, Chalfont St
`
`Peter, Buckinghamshire, United Kingdom, declare;
`
`1.
`
`2.
`
`3.
`
`That I am a citizen of the United Kingdom of Great Britain and Northern Ireland.
`
`That I am well acquainted with the German and English languages.
`
`That the attached is, to the best of my knowledge and belief, a true translation into the
`
`English language of DE19545107.
`
`4.
`
`That I believe that all statements made herein of my own knowledge are true and that
`
`all statements made on information and belief are true; and further that these statements were
`
`made with the knowledge that willful false statements and the like so made are punishable by
`
`fine or imprisonment, or both, under Section 1001 of Title 18 of the United States Code and
`
`that such willful false statements may jeopardize the validity of the patent application in the
`
`United States of America or any patent issuing thereon.
`
`
`
`Date: February 28, 2018
`
`
`
`
`
`N. T. SIMPKIN
`
`For and on behalf of RWS Group Ltd
`
`
`
`
`
`
`
`
`
`
`
`
`- 20 -
`
`