cosmetic

Abstract

A cosmetic according to the present invention contains (a) a pyrimidyl pyrazole compound represented by general formula (1) or a pharmacologically acceptable salt thereof, (b) a nonionic surfactant that has an HLB of 2–5, and (c) a nonionic surfactant that has an HLB of 9–18, the (a) component content being 0.05–1.5 mass%. (In general formula (1), R1, R3, R4, and R6 each independently indicate a C1–3 alkyl group, and R2 and R5 each independently indicate a hydrogen atom or a C1–3 alkyl group.)

Description

cosmetics

[0001] The present invention relates to a cosmetic preparation.

[0002] Cream bases containing polyethylene glycol stearate (PEG) have a high hardness, yet they blend well with the skin upon application and have a characteristic feel that does not leave a sticky feeling after application. They also have the advantageous properties of spreading lightly on the skin, being non-sticky, refreshing, having excellent penetration, and excellent stability over time.

[0003] For example, there is a demand for cosmetics that spread easily on the skin, are not sticky, have an excellent refreshing feel, have a texture that feels as if the cosmetics stick to the skin when applied (fit feeling), and have an excellent feeling that the active ingredients penetrate the skin (penetration feeling). In response to this demand, an oil-in-water emulsion skin cosmetic has been reported that contains (A) a nonionic surfactant having an HLB of 9 to 18, (B) a nonionic surfactant having an HLB of 2 to 5, (C) a homopolymer or copolymer of 2-acrylamido-2-methylpropanesulfonic acid, and (D) an ester oil having an IOB value of 0.2 to 0.6 (see, for example, Patent Document 1).

[0004] Japanese Patent Application Laid-Open No. 2005-320263

[0005] However, it was found that when a thickener is blended into a cream base containing PEG stearate to improve high-temperature stability, there are problems such as a slippery feeling during application and stickiness after application.

[0006] An object of one embodiment of the present invention is to provide a cosmetic that is quick to blend during application, has a reduced sticky feeling after application, and is excellent in feel when used.

[0007] Hereinafter, embodiments of the present invention will be described in detail. Note that the embodiments are not limited by the following description and can be modified as appropriate within the scope of the present invention. Furthermore, in this specification, unless otherwise specified, the term "to" indicating a range of values ​​means that the values ​​before and after it are included as the lower and upper limits.

[0008] One embodiment of the cosmetic of the present invention as a means for solving the above-mentioned problems comprises (a) a pyrimidylpyrazole compound represented by the following general formula (1) or a pharmacologically acceptable salt thereof, (b) a nonionic surfactant having an HLB of 2 to 5, and (c) a nonionic surfactant having an HLB of 9 to 18, wherein the content of component (a) is 0.05% by mass or more and 1.5% by mass or less:

[0009] (In the general formula (1), R １ , R ３ , R ４ , and R ６ each independently represents an alkyl group having 1 to 3 carbon atoms; R ２ and R ５ each independently represents a hydrogen atom or an alkyl group having 1 to 3 carbon atoms.

[0010] According to one embodiment of the present invention, it is possible to provide a cosmetic that is quick to blend during application, has a reduced sticky feeling after application, and is excellent in feel when used.

[0011] (Cosmetic Preparation) The cosmetic preparation of the present embodiment contains (a) a pyrimidylpyrazole compound represented by the following general formula (1) or a pharmacologically acceptable salt thereof, (b) a nonionic surfactant having an HLB of 2 to 5, and (c) a nonionic surfactant having an HLB of 9 to 18, and may further contain other ingredients as necessary.

[0012] The content of the component (a) is 0.05% by mass or more and 1.5% by mass or less.

[0013] (In the general formula (1), R １ , R ３ , R ４ , and R ６ each independently represents an alkyl group having 1 to 3 carbon atoms; R ２ and R ５ each independently represents a hydrogen atom or an alkyl group having 1 to 3 carbon atoms.

[0014] <(a) Pyrimidylpyrazole compound represented by general formula (1) or a pharmacologically acceptable salt thereof> The pyrimidylpyrazole compound represented by general formula (1) or a pharmacologically acceptable salt thereof (hereinafter, sometimes referred to as "component (a)") has very low cytotoxicity.

[0015] In general formula (1), R １ , R ３ , R ４ , and R ６ Each independently represents an alkyl group having 1 to 3 carbon atoms. １ , R ３ , R ４ , and R ６ The "C1-C3 alkyl group" is a linear, branched, or cyclic saturated hydrocarbon group having 1 to 3 carbon atoms. １ , R ３ , R ４ , and R ６ may be different alkyl groups having 1 to 3 carbon atoms, or may be the same alkyl group having 1 to 3 carbon atoms.

[0016] R １ , R ３ , R ４ , and R ６ Examples of the alkyl group having 1 to 3 carbon atoms represented by R include a methyl group, an ethyl group, an n-propyl group, an isopropyl group, and a cyclopropyl group. １ , R ３ , R ４ , and R ６ The alkyl group having 1 to 3 carbon atoms represented by is preferably a methyl group or an ethyl group, more preferably a methyl group.

[0017] In general formula (1), R ２ and R ５ Each independently represents a hydrogen atom or an alkyl group having 1 to 3 carbon atoms. ２ and R ５The "C1-C3 alkyl group" is a linear, branched, or cyclic saturated hydrocarbon group having 1 to 3 carbon atoms. ２ and R ５ may be different hydrogen atoms or alkyl groups having 1 to 3 carbon atoms, or may be the same hydrogen atom or alkyl groups having 1 to 3 carbon atoms.

[0018] R ２ and R ５ Examples of the alkyl group having 1 to 3 carbon atoms represented by R include a methyl group, an ethyl group, an n-propyl group, an isopropyl group, and a cyclopropyl group. ２ and R ５ is preferably a hydrogen atom.

[0019] Examples of the pharmacologically acceptable salt of the pyrimidylpyrazole compound represented by general formula (1) include inorganic acid salts such as hydrochloride, hydrobromide, sulfate, and phosphate; and organic acid salts such as acetate, propionate, citrate, lactate, oxalate, maleate, fumarate, succinate, tartrate, and methanesulfonate.

[0020] The pyrimidylpyrazole compound represented by the general formula (1) or a pharmacologically acceptable salt thereof includes R １ , R ３ , R ４ , and R ６ is a methyl group, and R ２ and R ５ is a hydrogen atom, 2-(3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine hydrochloride (also referred to as "dimethylpyrazolyldimethylpyrimidine hydrochloride") is particularly preferred.

[0021] The pyrimidylpyrazole compound represented by the general formula (1) may be synthesized by a known method or may be a commercially available product.

[0022] Representative synthesis examples of the pyrimidylpyrazole compound represented by general formula (1) are described below, but the synthesis examples are not limited thereto. Examples of synthesis examples of the pyrimidylpyrazole compound represented by general formula (1) include a synthesis method using the reaction shown in Scheme 1 below. The reaction shown in Scheme 1 below can be carried out in accordance with the methods described in, for example, JP-A-62-000404, Dharmpal S. Dodd et al., Tetrahedron Letters, Volume 45, Issue 22, 2004, pp. 4265-4267, Gazzetta Chemica Italiana, Vol. 93, Parte I, 1963, p. 100, etc.

[0023]

[0024] In Scheme 1, the reaction of the hydrazine compound represented by the general formula (2) with the 1,3-dicarbonyl compound represented by the general formula (3a) or the 1-sulfonyl-3-carbonyl compound represented by the general formula (3b) can be carried out in a suitable solvent such as methanol, in the presence of an acid catalyst such as hydrochloric acid or acetic acid, and with heating as necessary.

[0025] The pharmacologically acceptable salt of the pyrimidylpyrazole compound represented by general formula (1) may be appropriately synthesized by a known method, or may be a commercially available product.An example of the synthesis of the pharmacologically acceptable salt of the pyrimidylpyrazole compound represented by general formula (1) includes a method of converting the pyrimidylpyrazole compound represented by general formula (1) into an acid addition salt appropriately selected from known methods.The acid used in the method of converting into an acid addition salt includes, for example, inorganic acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, phosphoric acid, etc.; organic acids such as acetic acid, propionic acid, citric acid, lactic acid, oxalic acid, maleic acid, fumaric acid, succinic acid, tartaric acid, methanesulfonic acid, etc.

[0026] The hydrazine compound represented by general formula (2) used as a starting material in Scheme 1 may be synthesized by a known method or may be a commercially available product. An example of a synthesis of the hydrazine compound represented by general formula (2) is a synthesis method using the reaction shown in Scheme 2 below. The reaction shown in Scheme 2 below can be carried out, for example, in accordance with the method described in JP-A-8-208620.

[0027]

[0028] The hydrazine compound represented by general formula (2) used as a starting material in Scheme 1 can also be synthesized from a pyrimidine compound represented by general formula (5) having a leaving group Z by the reaction shown in Scheme 3 below. Examples of the leaving group Z in the pyrimidine compound represented by general formula (5) include halogen. The reaction shown in Scheme 3 below can be carried out, for example, as described in Takeo Naito et al., Chemical and Pharmaceutical Bulletin, 1969, Vol. 17, No. 7, pp. 1467-1478; Kaname Takagi et al., Chemical and Pharmaceutical Bulletin, 1963, Vol. 11, No. 11, pp. 1382-1388; and Kenzo Shirakawa, Pharmaceutical Journal, 1953, Vol. 73, No. 6, p. This can be carried out in accordance with the method described in, for example, J. Am. Chem. Soc. 2002, 635-639.

[0029]

[0030] Other compounds used in the reactions of Schemes 1 to 3 may be synthesized by known methods or may be commercially available products.

[0031] In the reactions of Schemes 1 to 3, when a functional group is present in the molecule and this functional group interferes with or is likely to interfere with the reaction, it is preferable to use an appropriate protecting group to efficiently proceed with the reaction. The protecting group can be used, for example, in accordance with the method described in Greene's Protective Groups in Organic Synthesis by Theodora W. Greene and Peter G. M. Wuts.

[0032] In the reactions of Schemes 1 to 3, when isomers such as conformational isomers, geometric isomers, or optical isomers exist, they can be obtained as pure isomers or geometric isomers by appropriately selecting raw materials and reaction conditions and performing separation procedures. The pyrimidylpyrazole compound represented by general formula (1) or a pharmacologically acceptable salt thereof also includes pure isomers and mixtures thereof.

[0033] The content of component (a) is from 0.05% to 1.5% by mass, preferably from 0.1% to 1.5% by mass, more preferably from 0.5% to 1.5% by mass, and even more preferably from 0.5% to 1% by mass, relative to the total mass of the cosmetic. When the content of component (a) is from 0.05% to 1.5% by mass, the quickness of absorption during application can be suitably improved and the sticky feeling after application can be reduced.

[0034] <(b) Nonionic Surfactant with HLB of 9 to 18> The nonionic surfactant with HLB of 9 to 18 (hereinafter, may be referred to as "component (b)") is a nonionic surfactant having an HLB value (hydrophile-lipophile balance value) of 9 or more and 18 or less.

[0035] The component (b) is not particularly limited and can be appropriately selected depending on the purpose. Examples include polyglycerin fatty acid esters, polyoxyethylene glycerin fatty acid esters, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene sorbit fatty acid esters, polyoxyethylene lanolin / lanolin alcohol / beeswax derivatives, polyoxyethylene castor oil / hardened castor oils, polyoxyethylene sterol / hydrogenated sterols, polyoxyethylene alkyl ethers, polyoxyethylene polyoxypropylene alkyl ethers, polyethylene glycol fatty acid esters, and polyoxyethylene glyceryl isostearate.

[0036] The component (b) may be used alone or in combination of two or more. In particular, from the viewpoint of stability, when a nonionic surfactant having an HLB of 9.0 to 10.0 is used, it is preferable to use it in combination with a nonionic surfactant having an HLB of 15.0 or more.

[0037] Examples of polyglycerin fatty acid esters include hexaglyceryl monolaurate (HLB 14.5), hexaglyceryl monomyristate (HLB 11.0), hexaglyceryl monostearate (HLB 9.0), hexaglyceryl monooleate (HLB 9.0), decaglyceryl monolaurate (HLB 15.5), decaglyceryl monomyristate (HLB 14.0), decaglyceryl monostearate (HLB 12.0), decaglyceryl monoisostearate (HLB 12.0), decaglyceryl monooleate (HLB 12.0), decaglyceryl distearate (HLB 9.5), and decaglyceryl diisostearate (HLB 10.0). Here, the numbers in parentheses indicate the HLB value.

[0038] Examples of polyoxyethylene glycerin fatty acid esters include polyoxyethylene (hereinafter abbreviated as POE) (5) glyceryl monostearate (HLB 9.5), POE (15) glyceryl monostearate (HLB 13.5), POE (5) glyceryl monooleate (HLB 9.5), and POE (15) glyceryl monooleate (HLB 14.5).

[0039] Examples of polyoxyethylene sorbitan fatty acid esters include mono-coconut oil fatty acid POE (20) sorbitan (HLB 16.9), monopalmitic acid POE (20) sorbitan (HLB 15.6), monostearate POE (20) sorbitan (HLB 14.9), monostearate POE (6) sorbitan (HLB 9.5), tristearate POE (20) sorbitan (HLB 10.5), monoisostearate POE (20) sorbitan (HLB 15.0), monooleic acid POE (20) sorbitan (HLB 15.0), monooleic acid POE (6) sorbitan (HLB 10.0), trioleic acid POE (20) sorbitan (HLB 11.0), and the like.

[0040] Examples of polyoxyethylene sorbitol fatty acid esters include POE(6) sorbitol monolaurate (HLB 15.5), POE(60) sorbitol tetrastearate (HLB 13.0), POE(30) sorbitol tetraoleate (HLB 11.5), POE(40) sorbitol tetraoleate (HLB 12.5), and POE(60) sorbitol tetraoleate (HLB 14.0).

[0041] Examples of polyoxyethylene lanolin, lanolin alcohol, and beeswax derivatives include POE (10) lanolin (HLB 12.0), POE (20) lanolin (HLB 13.0), POE (30) lanolin (HLB 15.0), POE (5) lanolin alcohol (HLB 12.5), POE (10) lanolin alcohol (HLB 15.5), POE (20) lanolin alcohol (HLB 16.0), POE (40) lanolin alcohol (HLB 17.0), and POE (20) sorbitol beeswax (HLB 9.5).

[0042] Examples of polyoxyethylene castor oils and hydrogenated castor oils include POE (20) castor oil (HLB 10.5), POE (40) castor oil (HLB 12.5), POE (50) castor oil (HLB 14.0), POE (60) castor oil (HLB 14.0), POE (20) hydrogenated castor oil (HLB 10.5), POE (30) hydrogenated castor oil (HLB 11.0), POE (40) hydrogenated castor oil (HLB 13.5), POE (60) hydrogenated castor oil (HLB 14.0), POE (80) hydrogenated castor oil (HLB 16.5), and POE (40) hydrogenated castor oil (100) hydrogenated castor oil (HLB 16.5).

[0043] Examples of polyoxyethylene sterols and hydrogenated sterols include POE(5) phytosterol (HLB 9.5), POE(10) phytosterol (HLB 12.5), POE(20) phytosterol (HLB 15.5), POE(30) phytosterol (HLB 18.0), POE(25) phytostanol (HLB 14.5), and POE(30) cholestanol (HLB 17.0).

[0044] Examples of polyoxyethylene alkyl ethers include polyoxyethylene lauryl ethers such as POE (2) lauryl ether (HLB 9.5), POE (4.2) lauryl ether (HLB 11.5), and POE (9) lauryl ether (HLB 14.5); polyoxyethylene cetyl ethers such as POE (5.5) cetyl ether (HLB 10.5), POE (7) cetyl ether (HLB 11.5), POE (10) cetyl ether (HLB 13.5), POE (15) cetyl ether (HLB 15.5), POE (20) cetyl ether (HLB 17.0), and POE (23) cetyl ether (HLB 18.0); Polyoxyethylene stearyl ethers such as POE (4) stearyl ether (HLB 9.0) and POE (20) stearyl ether (HLB 18.0); Polyoxyethylene oleyl ethers such as POE (7) oleyl ether (HLB 10.5), POE (10) oleyl ether (HLB 14.5), POE (15) oleyl ether (HLB 16.0), POE (20) oleyl ether (HLB 17.0), and POE (50) oleyl ether (HLB 18.0); Polyoxyethylene behenyl ethers such as POE (10) behenyl ether (HLB 10.0), POE (20) behenyl ether (HLB 16.5), and POE (30) behenyl ether (HLB 18.0); POE (2) (C12-15) alkyl ether (HLB 9.0), POE (4) (C12-15) alkyl ether (HLB 10.5), POE (10) (C12-15) alkyl ether (HLB 15.5), POE (5) secondary alkyl ether (HLB 10.5), POE (7) secondary alkyl ether (HLB 12.0), POE (9) alkyl ether (HLB 13.5), POE (12) alkyl ether (HLB 14.5); and the like.

[0045] Examples of polyoxyethylene polyoxypropylene alkyl ethers include polyoxyethylene (hereinafter abbreviated as POE) (1) polyoxypropylene (hereinafter abbreviated as POP) (4) cetyl ether (HLB 9.5), POE (10) POP (4) cetyl ether (HLB 10.5), POE (20) POP (8) cetyl ether (HLB 12.5), POE (20) POP (6) decyl tetradecyl ether (HLB 11.0), and POE (30) POP (6) decyl tetradecyl ether (HLB 12.0).

[0046] Examples of polyethylene glycol fatty acid esters include polyethylene glycol monolaurate (hereinafter abbreviated as PEG) (10) (HLB 12.5), PEG monostearate (10) (HLB 11.0), PEG monostearate (25) (HLB 15.0), PEG monostearate (40) (HLB 17.5), PEG monostearate (45) (HLB 18.0), PEG monostearate (55) (HLB 18.0), PEG monooleate (10) (HLB 11.0), PEG distearate (HLB 16.5), and PEG diisostearate (HLB 9.5).

[0047] Examples of polyoxyethylene glyceryl isostearate include PEG (8) glyceryl isostearate (HLB 10.0), PEG (10) glyceryl isostearate (HLB 10.0), PEG (15) glyceryl isostearate (HLB 12.0), PEG (20) glyceryl isostearate (HLB 13.0), PEG (25) glyceryl isostearate (HLB 14.0), PEG glyceryl (30) isostearate (HLB 15.0), PEG (40) glyceryl isostearate (HLB 15.0), PEG (50) glyceryl isostearate (HLB 16.0), and PEG (60) glyceryl isostearate (HLB 16.0).

[0048] In one embodiment of component (b), from the viewpoint of usability (skin compatibility), it is preferable to include a combination of polyethylene glycol (40) monostearate (HLB 17.5) and polyoxyethylene (20) sorbitan monostearate (HLB 14.9, also known as polysorbate 60).

[0049] The content of component (b) is not particularly limited and can be selected appropriately depending on the purpose, but is preferably 0.5% by mass to 5.0% by mass, and more preferably 0.5% by mass to 2.0% by mass, relative to the total mass of the cosmetic. If the content of component (b) is less than 0.5% by mass, the system may become unstable, and if it exceeds 5.0% by mass, the effect is not enhanced and stickiness may occur.

[0050] <(c) Nonionic Surfactant with HLB of 2 to 5> The nonionic surfactant with HLB of 2 to 5 (hereinafter, sometimes referred to as "component (c)") is a nonionic surfactant having an HLB value of 2 or more and 5 or less.

[0051] The component (c) is not particularly limited and can be appropriately selected depending on the purpose. Examples thereof include POE (2) stearyl ether (HLB 4.0), self-emulsifying propylene glycol monostearate (HLB 4.0), glyceryl myristate (HLB 3.5), glyceryl monostearate (HLB 4.0), self-emulsifying glyceryl monostearate (HLB 4.0 to 5.0), glyceryl monoisostearate (HLB 4.0), glyceryl monooleate (HLB 2.5), hexaglyceryl tristearate (HLB 2.5), decaglyceryl pentastearate (HLB 3.5), and deca pentaisostearate. Glyceryl (HLB 3.5), decaglyceryl pentaoleate (HLB 3.5), sorbitan monostearate (HLB 4.7), sorbitan tristearate (HLB 2.1), sorbitan monoisostearate (HLB 5.0), sorbitan sesquiisostearate (HLB 4.5), sorbitan monooleate (HLB 4.3), POE (6) sorbit hexastearate (HLB 3.0), POE (3) castor oil (HLB 3.0), PEG (2) monostearate (HLB 4.0), ethylene glycol monostearate (HLB 3.5), PEG (2) stearate (HLB 4.5), and the like.

[0052] The component (c) may be used alone or in combination of two or more. Among these, from the viewpoint of the feel when used (compatibility with the skin), it is preferable to include sorbitan tristearate (HLB 2.1), and it is preferable to include a combination of sorbitan tristearate and glyceryl stearate (glyceryl monostearate, self-emulsifying glyceryl monostearate, etc.).

[0053] The content of component (c) is not particularly limited and can be selected appropriately depending on the purpose, but is preferably 0.1% by mass to 5.0% by mass, and more preferably 0.1% by mass to 2.0% by mass, relative to the total mass of the cosmetic. If the content of component (c) is less than 0.1% by mass, the feeling of penetration may not be achieved, and if it exceeds 5.0% by mass, the stability of the system may be reduced.

[0054] <(d) Higher Alcohol> It is preferable that the cosmetic preparation of the present embodiment further contains (d) a higher alcohol (hereinafter, may be referred to as “component (d)”), from the viewpoint of stabilizing the emulsion and / or imparting a rich feel to the preparation.

[0055] The component (d) is not particularly limited and can be appropriately selected depending on the purpose. Examples thereof include straight-chain alcohols such as lauryl alcohol, cetyl alcohol, stearyl alcohol, behenyl alcohol, myristyl alcohol, oleyl alcohol, and cetostearyl alcohol; and branched-chain alcohols such as lanolin alcohol, cholesterol, phytosterol, hexyldodecanol, isostearyl alcohol, and octyldodecanol.

[0056] The content of component (d) is not particularly limited and can be selected appropriately depending on the purpose, but is preferably 0.1% by mass to 5.0% by mass, and more preferably 0.1% by mass to 2.0% by mass, relative to the total mass of the cosmetic. If the content of component (d) exceeds 5.0% by mass, the stability of the system may deteriorate.

[0057] <(e) Thickener> The cosmetic preparation of the present embodiment preferably further comprises a (e) thickener (hereinafter, sometimes referred to as "component (e)"). As described above, when a thickener is blended into a cream base containing PEG stearate to improve high-temperature stability, problems arise in that the base may feel slippery during application and sticky after application. However, the cosmetic preparation of the present embodiment, which contains components (a), (b), and (c), can solve these problems, improve the speed of absorption during application, reduce the sticky feeling after application, and provide a cosmetic preparation that is excellent in feel when used.

[0058] The component (e) is not particularly limited and can be appropriately selected depending on the purpose, and examples thereof include plant-based polymers, animal-based polymers, microbial-based polymers, starch-based polymers, cellulose-based polymers, alginic acid-based polymers, vinyl-based polymers, acrylic-based polymers, inorganic water-soluble polymers, etc. The component (e) may be used alone or in combination of two or more types.

[0059] Examples of plant-derived polymers include gum arabic, tragacanth gum, galactan, guar gum, carob gum, karaya gum, gellan gum, carrageenan, pectin, and agar.

[0060] Examples of animal-derived polymers include collagen, casein, albumin, and gelatin.

[0061] Examples of microbial polymers include xanthan gum, dextran, succinoglucan, and pullulan.

[0062] Examples of starch-based polymers include vegetable starches such as those from corn, wheat, potato, and rice; carboxymethyl starch; and methylhydroxypropyl starch.

[0063] Examples of the cellulose polymer include methyl cellulose, nitrocellulose, ethyl cellulose, methylhydroxypropyl cellulose, hydroxyethyl cellulose, sodium cellulose sulfate, hydroxypropyl cellulose, sodium carboxymethyl cellulose, and crystalline cellulose.

[0064] Examples of alginic acid polymers include sodium alginate and propylene glycol alginate.

[0065] Examples of vinyl polymers include polyvinyl alcohol, polyvinyl acetate, polyvinyl methyl ether, polyvinylpyrrolidone, copolymers of vinylpyrrolidone and vinyl acetate, and carboxyvinyl polymers.

[0066] Examples of acrylic polymers include sodium polyacrylate, polyethyl acrylate, alkanolamine polyacrylate, (dimethylacrylamide / sodium acryloyldimethyltaurate) crosspolymer, copolymer of alkyl methacrylate and dimethylaminoethyl methacrylate, poly(2-acrylamido-2-methylpropanesulfonic acid), and poly(methacryloyloxytrimethylammonium).

[0067] Examples of inorganic water-soluble polymers include polyethyleneimine, cationic polymers, bentonite, aluminum magnesium silicate, laponite, hectorite, and silicic anhydride.

[0068] The content of component (e) is not particularly limited and can be selected appropriately depending on the purpose, but is preferably 0.1% by mass to 2.0% by mass, and more preferably 0.1% by mass to 1.0% by mass, relative to the total mass of the cosmetic. If the content of component (e) exceeds 2.0% by mass, the quickness of absorption during application may decrease, and the effect of reducing stickiness after application may not be obtained.

[0069] The content of component (e) is not particularly limited and can be selected appropriately depending on the purpose, but in order to achieve an excellent feel in use, allowing the user to sense the thickness during application even when a salt-type drug is used, and to maintain a good, smooth, lotion-like feel during use, the content is preferably from 0.03% to 0.2% by mass, more preferably from 0.05% to 0.2% by mass, and even more preferably from 0.08% to 0.2% by mass, relative to the total amount of the cosmetic. If the content is less than 0.03% by mass, the user may not sense a sufficient thickness during application, and if the content exceeds 0.2% by mass, the viscosity may be too high, resulting in a poor feel during use.

[0070] <Water> The amount of water contained in the cosmetic of the present embodiment is not particularly limited and can be selected appropriately depending on the purpose, but is preferably 30% by mass or more and 90% by mass or less, and more preferably 40% by mass or more and 80% by mass or less, relative to the total amount of the cosmetic.

[0071] <Other Components> In addition to the essential components (a) to (c) and the optional components (d) and (e), the cosmetic of the present embodiment may contain optional components that are blended into known cosmetic compositions as other components.

[0072] The other components are not particularly limited, and known cosmetic components can be appropriately selected depending on the purpose. Examples include drugs other than component (a), surfactants other than components (b) to (c), oils, moisturizers, alcohols having 6 or less carbon atoms, neutralizing agents, preservatives, chelating agents, stabilizers, ultraviolet absorbers, pigments, etc.

[0073] Drugs include drugs other than component (a), such as salt-type drugs, vitamins, plant extracts, anti-inflammatory agents, and whitening agents.

[0074] -Surfactant- Examples of surfactants include anionic surfactants, cationic surfactants, nonionic surfactants other than components (b) to (c), and amphoteric surfactants.

[0075] Examples of anionic surfactants include fatty acid soaps such as sodium laurate and sodium palmitate; higher alkyl sulfates such as sodium lauryl sulfate and potassium lauryl sulfate; alkyl ether sulfates such as polyoxyethylene triethanolamine lauryl sulfate and sodium polyoxyethylene lauryl sulfate; N-acyl sarcosinates such as sodium lauroyl sarcosinate; higher fatty acid amide sulfonates such as sodium N-myristoyl-N-methyl taurate, sodium N-stearoyl-N-methyl taurate, sodium coconut oil fatty acid methyl tauride, and sodium lauryl methyl tauride; phosphate salts such as sodium polyoxyethylene oleyl ether phosphate and sodium polyoxyethylene stearyl ether phosphate; sodium di-2-ethylhexyl sulfosuccinate and monolauroyl monoethanolamide polyoxyethylene. alkylbenzenesulfonates such as sodium diethylene sulfosuccinate and sodium lauryl polypropylene glycol sulfosuccinate; N-acylglutamic acids such as monosodium N-lauroyl glutamate and disodium N-stearoyl glutamate; higher fatty acid ester sulfates such as hydrogenated coconut oil fatty acid glycerin sodium sulfate; polyoxyethylene alkyl ether carboxylates, α-olefin sulfonates, higher fatty acid ester sulfonates, secondary alcohol sulfates, higher fatty acid alkylolamide sulfates, sodium lauroyl monoethanolamide succinate, N-palmitoyl aspartic acid, ditriethanolamine, and coconut oil fatty acid collagen hydrolyzed alkali salts.

[0076] Examples of cationic surfactants include alkyltrimethylammonium salts such as stearyltrimethylammonium chloride and lauryltrimethylammonium chloride; dialkyldimethylammonium salts such as distearyldimethylammonium chloride; alkylpyridinium salts such as poly(N,N'-dimethyl-3,5-methylenepiperidinium chloride) and cetylpyridinium chloride; alkyl quaternary ammonium salts, alkyldimethylbenzylammonium salts, alkylisoquinolinium salts, dialkylmorphonium salts, polyoxyethylene alkylamines, alkylamine salts, polyamine fatty acid derivatives, amyl alcohol fatty acid derivatives, benzalkonium chloride, benzethonium chloride, cationic polymers, and β-N-N-dimethyl-N-ethylammonioethyl acrylate vinylpyrrolidone chloride copolymers.

[0077] Examples of amphoteric surfactants include imidazoline-based amphoteric surfactants such as 2-undecyl-N,N,N-(hydroxyethylcarboxymethyl)-2-imidazoline sodium and 2-cocoyl-2-imidazolinium hydroxide-1-carboxyethyloxy disodium salt; and betaine-based amphoteric surfactants such as 2-heptadecyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, lauryldimethylaminoacetic acid betaine, alkyl betaine, amido betaine, and sulfobetaine.

[0078] -Oil- There are no particular limitations on the oil, and known cosmetic ingredients can be appropriately selected depending on the purpose, and examples include ester oil, hydrocarbon oil, silicone oil, higher fatty acid, alkyl glyceryl ether, liquid oil, solid oil, semi-solid oil, oil-soluble drug, etc. These may be used alone or in combination of two or more.

[0079] Examples of ester oils include octyl octanoate, nonyl nonanoate, cetyl octanoate, isopropyl myristate, octyldodecyl myristate, isopropyl palmitate, ethylhexyl palmitate, butyl stearate, hexyl laurate, myristyl myristate, decyl oleate, hexyldecyl dimethyloctanoate, cetyl lactate, myristyl lactate, lanolin acetate, isocetyl stearate, isocetyl isostearate, 12-hydroxystearyl alcohol, and the like. Cholesteryl phosphate, ethylene glycol di-2-ethylhexanoate, dipentaerythritol fatty acid ester, N-alkyl glycol monoisostearate, neopentyl glycol dicaprate, tripropylene glycol pivalate, diisostearyl malate, glycerin di-2-heptylundecanoate, glycerin diisostearate, trimethylolpropane tri-2-ethylhexanoate, trimethylolpropane triisostearate, tetraethylhexane Pentaerythrityl Tri-2-Ethylhexanoate (Triethylhexanoin), Glyceryl Trioctanoate, Glyceryl Triisopalmitate, Trimethylolpropane Triisostearate, Cetyl 2-Ethylhexanoate-2-Ethylhexyl Palmitate, Glyceryl Trimyristate, Tri-2-Heptylundecanoic Acid Glyceride, Castor Oil Fatty Acid Methyl Ester, Oleyl Oleate, Acetoglyceride, 2-Heptylundecyl Palmitate Examples of suitable oils include 2-hexyldecyl palmitate, 2-hexyldecyl palmitate, 2-hexyldecyl adip ...

[0080] Examples of hydrocarbon oils include isododecane, isohexadecane, isoparaffin, mineral oil (liquid paraffin), ozokerite, squalane, pristane, paraffin, ceresin, squalene, petrolatum, microcrystalline wax, and hydrogenated polydecene.

[0081] Examples of silicone oils include chain polysiloxanes such as dimethicone, diphenylsiloxyphenyl trimethicone, and diphenylpolysiloxane; cyclic polysiloxanes such as octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, and dodecamethylcyclohexasiloxane; silicone resins that form a three-dimensional network structure; silicone rubber; various modified polysiloxanes such as amino-modified polysiloxane, polyether-modified polysiloxane, alkyl-modified polysiloxane, and fluorine-modified polysiloxane; and acrylic silicones.

[0082] Examples of higher fatty acids include lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, oleic acid, undecylenic acid, tall acid, isostearic acid, linoleic acid, linolenic acid, eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA).

[0083] Examples of alkyl glyceryl ethers include batyl alcohol and chimyl alcohol.

[0084] Examples of liquid oils include avocado oil, camellia oil, macadamia nut oil, corn oil, olive oil, rapeseed oil, sesame oil, persic oil, wheat germ oil, camellia oil, castor oil, linseed oil, safflower oil, cottonseed oil, perilla oil, soybean oil, peanut oil, tea seed oil, kaya oil, rice bran oil, Chinese tung oil, Japanese tung oil, jojoba oil, germ oil, and triglycerin.

[0085] Examples of solid oils include cacao butter, coconut oil, hardened coconut oil, palm oil, palm kernel oil, hydrogenated palm oil, Japan wax kernel oil, hardened oil, and Japan wax.

[0086] Examples of semi-solid oils include shea butter, partially hydrogenated coconut oil, and partially hydrogenated jojoba oil.

[0087] - Moisturizers - Moisturizers can enhance the moisturizing and hydrating effects of the skin.

[0088] Examples of moisturizing agents include glycerin (dynamite glycerin), 1,3-butylene glycol, propylene glycol, dipropylene glycol, erythritol, maltitol, polyoxyethylene polyoxypropylene alkyl ether, acetylated hyaluronic acid and salts thereof.

[0089] Alcohols Having 6 or Less Carbon Atoms Examples of alcohols having 6 or less carbon atoms include ethanol, propanol, isopropanol, isobutyl alcohol, and t-butyl alcohol.

[0090] Neutralizing Agent Examples of neutralizing agents include potassium hydroxide, sodium hydroxide, triethanolamine, sodium carbonate, lactic acid, citric acid, sodium citrate, glycolic acid, succinic acid, tartaric acid, malic acid, sodium hydrogen carbonate, and ammonium hydrogen carbonate.

[0091] - Preservatives - Examples of preservatives include benzoic acid, salicylic acid, paraoxybenzoic acid esters (methylparaben, ethylparaben, butylparaben, etc.), sorbic acid, parachlormetacresol, hexachlorophene, benzalkonium chloride, chlorhexidine chloride, trichlorocarbanilide, photosensitizers, and phenoxyethanol.

[0092] —Chelating Agent— Examples of chelating agents include citramalic acid, agaric acid, glyceric acid, shikimic acid, hinokitiol, gallic acid, tannic acid, caffeic acid, ethylenediamine-N,N,N′,N′-tetraacetic acid trisodium salt trihydrate (EDTA-3Na), ethylene glycol diamine tetraacetic acid, diethylenetriamine pentaacetic acid, phytic acid, polyphosphoric acid, metaphosphoric acid, analogs thereof, alkali metal salts thereof, and carboxylic acid esters thereof.

[0093] -Stabilizer- Examples of stabilizers include sodium pyrosulfite, ascorbic acid, α-tocopherol, and carotenoids.

[0094] -Ultraviolet Absorber- Examples of the ultraviolet absorber include benzoic acid-based ultraviolet absorbers such as para-aminobenzoic acid; anthranilic acid-based ultraviolet absorbers such as methyl anthranilate; salicylic acid-based ultraviolet absorbers such as octyl salicylate; cinnamic acid-based ultraviolet absorbers such as isopropyl paramethoxycinnamate and octyl paramethoxycinnamate; ultraviolet absorbers such as urocanic acid and ethyl urocanate, benzophenone-based ultraviolet absorbers such as 2-hydroxy-4-methoxybenzophenone and dihydroxybenzophenone, benzotriazole-based ultraviolet absorbers, and 2-phenylbenzimidazole-5-sulfonic acid.

[0095] Pigments Examples of pigments include inorganic pigments, organic pigments, pearl pigments, and metal powder pigments.

[0096] [Viscosity] The viscosity of the cosmetic is not particularly limited, and known cosmetic ingredients can be appropriately selected depending on the purpose. The viscosity at 25°C is preferably 1,000 mPa·s or more, more preferably 5,000 mPa·s or more, and even more preferably 10,000 mPa·s or more.

[0097] The viscosity of the cosmetic can be measured, for example, using a viscosity measuring device (VISCOMETER TVB-15, Toki Sangyo Co., Ltd.) with a No. 2 probe at 30° C. and a rotation speed of 12 rpm.

[0098] [Dosage Form] The dosage form of the cosmetic according to one embodiment is not particularly limited and can be appropriately selected depending on the purpose, but is preferably a liquid cosmetic, more preferably a liquid emulsion cosmetic, even more preferably an oil-in-water emulsion, and particularly preferably an oil-in-water emulsion cosmetic.

[0099] The product form of the cosmetic according to one embodiment is not particularly limited and can be appropriately selected depending on the purpose, and examples thereof include cosmetics intended for skin care such as lotion, emulsion, serum, cream, etc.; sunscreen bases; suntan bases; cleansing bases, etc. Among these, the product form of the cosmetic according to one embodiment is preferably used as a cosmetic such as a cream, emulsion, serum, etc., because these have excellent quick absorption during application and reduce stickiness after application.

[0100] [Method for producing cosmetic preparations] The method for producing a cosmetic preparation according to an embodiment is not particularly limited, and the cosmetic preparation can be produced according to a method typically used for cosmetics, preferably liquid cosmetics. As a specific example of a method for producing a cosmetic preparation according to an embodiment, the cosmetic preparation can be obtained by a conventional method, such as preparing an oil layer component and an aqueous layer component in advance, and emulsifying the oil layer component by gradually adding the oil layer component to the prepared aqueous layer and mixing or stirring the components.

[0101] The present invention will be described in more detail below based on examples, but the present invention is not limited to the following examples. In the description of these examples, percentages (% and parts) indicate "mass %" relative to the total mass of the cosmetic unless otherwise specified, and all values ​​are converted into pure contents.

[0102] Example 1 A cosmetic composition was prepared according to the formulation shown in Table 1 below.

[0103] Specifically, first, components (a) and (e), as well as any other water-soluble components, were dissolved in water to prepare an aqueous phase. Next, components (b), (c), and (d), as well as any other water-insoluble components, were uniformly mixed and dissolved to prepare an oil phase. Finally, the oil phase was gradually added to the aqueous phase while stirring, thereby preparing the lotion of Example 1.

[0104] Comparative Example 1 A cosmetic of Comparative Example 1 was prepared in the same manner as in Example 1, except that the essential component (a) was omitted as shown in Table 1.

[0105] (Comparative Example 2) A cosmetic of Comparative Example 2 was prepared in the same manner as in Example 1, except that the content of component (a) in Example 1 was changed from 0.1% by mass to 2% by mass, as shown in Table 1.

[0106] (Comparative Examples 3 to 4) Cosmetics of Comparative Examples 3 and 4 were prepared in the same manner as in Example 1, except that the essential components (b) and (c) were omitted as shown in Table 1.

[0107] Examples 2 and 3 Cosmetics of Examples 2 and 3 were prepared in the same manner as in Example 1, except that the formulations shown in Table 1 were used.

[0108] The prepared cosmetics were evaluated for "quickness of absorption during application" and "non-stickiness after application" as follows. The results are shown in Table 1.

[0109] <Speed ​​of absorption during application> A sensory evaluation was performed to determine whether the prepared cosmetic was absorbed quickly when applied to the skin, using the following procedure and evaluation criteria as follows. - Sensory evaluation - Three expert panelists applied the prepared cosmetic to the back of their hands at room temperature (25°C ± 5°C), and evaluated the feel when used with the cosmetic of Comparative Example 1 as the standard (STD). Evaluation criteria unanimous by the three expert panelists were used for the evaluation. - Evaluation criteria - A: The cosmetic absorbed more quickly than the STD B: The cosmetic absorbed slightly faster than the STD C: The cosmetic absorbed slightly faster than the STD D: The cosmetic absorbed equally quickly or no faster than the STD

[0110] <Non-sticky feeling after application> When the prepared cosmetic preparations were applied to the skin, a sensory evaluation of whether or not the cosmetic preparations felt non-sticky after application was performed using the procedure described below, and the evaluation was based on the following evaluation criteria. -Evaluation criteria- A: Compared to the STD, the cosmetic preparations felt less sticky after application. B: Compared to the STD, the cosmetic preparations felt slightly less sticky after application. C: Compared to the STD, the cosmetic preparations felt slightly less sticky after application. D: Compared to the STD, the cosmetic preparations felt the same non-sticky feeling after application, or the cosmetic preparations felt sticky after application.

[0111]

[0112] As shown in Table 1, it was found that the cosmetics of Examples 1 to 3, by containing all of the components (a) to (c), improved the quickness of absorption during application, reduced the sticky feeling after application, and provided an excellent feel when used.

[0113] On the other hand, when any of the components (a) to (c) was not included (Comparative Examples 1, 3 to 4), it was not possible to ensure either the quick absorption during application or the absence of a sticky feeling after application.

[0114] The components used in Table 1 are as follows:

[0115]

[0116] The component (a) 2-(3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine hydrochloride (dimethylpyrazolyldimethylpyrimidine hydrochloride) used in the examples and comparative examples is a compound represented by the following structural formula (1), which was produced by the method described in Japanese Patent No. 4586108.

[0117]

[0118] The present invention provides a compound comprising: (a) a pyrimidylpyrazole compound represented by the following general formula (1) or a pharmacologically acceptable salt thereof;

[0119] (In the general formula (1), R １ , R ３ , R ４ , and R ６ each independently represents an alkyl group having 1 to 3 carbon atoms; R ２ and R ５ each independently represents a hydrogen atom or an alkyl group having 1 to 3 carbon atoms.) (b) a nonionic surfactant having an HLB of 9 to 18, and (c) a nonionic surfactant having an HLB of 2 to 5, wherein the content of the component (a) is 0.05% by mass or more and 1.5% by mass or less. <2> A cosmetic preparation comprising R in the general formula (1) ２ and R ５<3> The cosmetic according to <1>, wherein R in the general formula (1) is a hydrogen atom. １ , R ３ , R ４ , and R ６ is a methyl group. <4> The cosmetic preparation according to any one of <1> to <3>, wherein the component (b) comprises a combination of polyethylene glycol (40) monostearate and polyoxyethylene (20) sorbitan monostearate. <5> The cosmetic preparation according to any one of <1> to <4>, wherein the component (c) comprises a combination of sorbitan tristearate and glyceryl stearate. <6> The cosmetic preparation according to any one of <1> to <5>, further comprising (d) a higher alcohol. <7> The cosmetic preparation according to any one of <1> to <6>, further comprising (e) a thickener. <8> The cosmetic preparation according to any one of <1> to <7>, wherein the content of the component (b) is 0.5% by mass or more and 5.0% by mass or less. <9> The cosmetic preparation according to any one of <1> to <8>, wherein the content of the component (c) is 0.1% by mass or more and 5.0% by mass or less.

[0120] Although the present invention has been described above based on specific embodiments and examples, these embodiments and examples are presented only as examples, and the present invention is not limited to the above embodiments and examples. Various changes, modifications, substitutions, deletions, additions, combinations, etc. are possible within the scope of the disclosure of the present invention.

[0121] This application claims priority based on Japanese Patent Application No. 2023-218440, filed on December 25, 2023, the entire contents of which are incorporated herein by reference.

Claims

1. (a) A pyrimidylpyrazole compound represented by the following general formula (1) or a pharmacologically acceptable salt thereof, (In the general formula (1), R １ , R ３ , R ４ , and R ６ each independently represent an alkyl group having 1 to 3 carbon atoms, and R ２ and R ５ each independently represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms.) (b) A nonionic surfactant having an HLB of 9 to 18, and (c) A nonionic surfactant having an HLB of 2 to 5, and a cosmetic characterized in that the content of the component (a) is 0.05% by mass or more and 1.5% by mass or less.

2. R in the general formula (1) ２ and R ５ are hydrogen atoms, and the cosmetic according to claim 1.

3. R in the general formula (1) １ , R ３ , R ４ , and R ６ are methyl groups, and the cosmetic according to claim 1.

4. The cosmetic according to claim 1, wherein the component (b) contains a combination of polyethylene glycol (40) monostearate and polyoxyethylene (20) sorbitan monostearate.

5. The cosmetic according to claim 1, wherein the component (c) contains a combination of sorbitan tristearate and glyceryl stearate.

6. The cosmetic according to claim 1, further comprising (d) a higher alcohol.

7. The cosmetic according to claim 1, further comprising (e) a thickener.

8. The cosmetic according to claim 1, wherein the content of the component (b) is 0.5% by mass or more and 5.0% by mass or less.

9. The cosmetic according to claim 1, wherein the content of the component (c) is 0.1% by mass or more and 5.0% by mass or less.

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