WO2023048528A1 - Composition pharmaceutique comprenant un inhibiteur d'inflammasome en tant que principe actif pour la prévention, le soulagement ou le traitement de la dermatite atopique - Google Patents
Composition pharmaceutique comprenant un inhibiteur d'inflammasome en tant que principe actif pour la prévention, le soulagement ou le traitement de la dermatite atopique Download PDFInfo
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- WO2023048528A1 WO2023048528A1 PCT/KR2022/014366 KR2022014366W WO2023048528A1 WO 2023048528 A1 WO2023048528 A1 WO 2023048528A1 KR 2022014366 W KR2022014366 W KR 2022014366W WO 2023048528 A1 WO2023048528 A1 WO 2023048528A1
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- Prior art keywords
- atopic dermatitis
- formula
- preventing
- improving
- composition
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- 229960005078 sorbitan sesquioleate Drugs 0.000 description 1
- 235000020712 soy bean extract Nutrition 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 125000004079 stearyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
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- 208000004371 toothache Diseases 0.000 description 1
- 229940078499 tricalcium phosphate Drugs 0.000 description 1
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- 229910000391 tricalcium phosphate Inorganic materials 0.000 description 1
- 229950000088 upadacitinib Drugs 0.000 description 1
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- 235000019165 vitamin E Nutrition 0.000 description 1
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Images
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/63—Steroids; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
Definitions
- the present invention relates to a pharmaceutical composition for preventing, improving or treating atopic dermatitis, containing a novel inflammatory complex inhibitor as an active ingredient.
- Atopic diseases include asthma, allergic rhinitis, and allergic conjunctivitis in addition to atopic dermatitis.
- asthma allergic rhinitis
- allergic conjunctivitis in addition to atopic dermatitis.
- the incidence of atopic dermatitis is rapidly increasing worldwide due to the increase in environmental pollutants, and the prevalence of atopic dermatitis reaches 20% of the total population.
- Patients with atopic dermatitis have a reduced quality of life due to restrictions in their daily life, and socially, the economic burden of treatment is increasing. Therefore, there is an urgent need for atopic treatment management measures.
- Atopic dermatitis is a recurrent chronic skin disease accompanied by severe itching that usually starts in infancy or childhood and is a very common skin disease accompanied by a family history. Symptoms begin in infancy and infancy, especially around the age of 2 months, of which about 50% occur before the age of 2 years, most of which appear before the age of 5 years, whereas first symptoms appear in adults are very rare. . In some patients, symptoms are alleviated or cured spontaneously with growth, and more than half of patients with infancy symptoms improve before the age of 2 years. The shape and distribution of skin lesions are characteristic, accompanied by pruritus (pruritus), dry skin, and characteristic eczema.
- Atopy usually involves an allergic reaction.
- atopic dermatitis is not only a skin disease, but also a signal of an allergic march such as allergic asthma and rhinitis.
- a suitable treatment drug that can cure it completely has not been developed.
- steroids, PDE4 inhibitors, JAK inhibitors, and antibody treatments are used as treatments for atopic dermatitis.
- Anti-inflammatory analgesics and steroid-based immunosuppressants are mainly used to alleviate inflammation and immune response.
- Elidel (pimecrolimus) cream and Protopic (tacrolimus, FK506) ointment which are non-steroidal immunomodulatory agents, were developed as agents that can replace steroid ointments, and when applied for a long time, there are no side effects seen with existing steroid ointments, It is often used for sensitive skin such as the neck and has grown rapidly to 30% of the entire atopic dermatitis market.
- the risk of cancer induction of calcineurin inhibitors has been raised, and sales are declining as only low concentration use is recognized for patients under the age of 16, and low concentration use is not recognized for children under 2 years of age. .
- Dupicent is only covered by insurance for the treatment of patients who do not respond to steroids, calcineurin inhibitors, Eucrisa, and systemic treatments.
- patients' access to Dupicent treatment is very limited.
- antihistamines and, in severe cases, taking short-term adrenocortical hormones and applying external agents, and skin UV treatment or interferon treatment are being implemented.
- skin UV treatment or interferon treatment are being implemented.
- most cases only temporary improvement is induced, and atopic dermatitis recurs when the medication is stopped. Therefore, most patients with atopic dermatitis still urgent need the development of therapeutic and preventive drugs with fewer side effects than conventional treatments and high efficacy.
- composition containing a deoxycholic acid derivative compound of Formula 1 has a significant effect on treating atopic dermatitis and proposes it as a pharmaceutical component for preventing, treating, and improving atopic dermatitis.
- An object of the present invention is to provide a composition for preventing, improving or treating atopic dermatitis, comprising a deoxycholic acid derivative compound of Formula 1 as an active ingredient, or a pharmaceutically acceptable salt or solvate thereof.
- Another object of the present invention is to provide a method for preventing, improving or treating atopic dermatitis comprising administering the pharmaceutical composition to a subject.
- Another object of the present invention is to provide the use of the pharmaceutical composition for use in preventing, improving or treating atopic dermatitis.
- the present invention provides a pharmaceutical composition for preventing, improving or treating atopic dermatitis, containing a deoxycholic acid derivative compound of Formula 1 below, or a pharmaceutically acceptable salt or solvate thereof as an active ingredient.
- the compound of Formula 1 may have an isomeric form as shown in Formula 2 below.
- the compound of Formula 1 may be in the form of a salt selected from the group consisting of alkali metal salts, inorganic acid salts, organic acid salts, alkaline earth metal salts, and ammonium salts, but is not limited thereto.
- the compound of Formula 1 may be a sodium salt, and may be a compound of Formula 3 below.
- the compound of Formula 3 may have an isomeric form as shown in Formula 4 below.
- the pharmaceutical composition may be formulated in the form of oral preparations, injection preparations or external preparations, but is not limited thereto.
- pharmaceutically acceptable additives may be further included therein.
- the oral preparation may be formulated into a dosage form selected from the group consisting of tablets, granules, pills, powders, capsules and solutions, but is not limited thereto.
- the composition for external application may be formulated into a formulation selected from the group consisting of creams, gels, ointments, emulsions, suspensions, sprays, and transdermal delivery patches, but is not limited thereto.
- the external preparation may be applied in an amount of 0.01 to 50 mg per day.
- a cosmetic composition for preventing or improving atopic dermatitis containing a compound having the structure of Formula 1 below, a pharmaceutically acceptable salt thereof, or a solvate thereof as an active ingredient is provided.
- the cosmetic composition is a soap for atopy, cleansing foam, cleansing cream, cleansing water, bath agent, skin lotion, skin softener, skin toner, lotion, cream, essence, astringent, emulsion, gel, lipstick, spray , Shampoo, rinse, treatment, body cleanser, pack, massage agent, face powder, compact, foundation, two-way cake and may be prepared in one or more formulations selected from the group consisting of a makeup base, but is not limited thereto.
- compositions for preventing, improving or treating atopic dermatitis in animals other than humans containing a compound having the structure of Formula 1, a pharmaceutically acceptable salt thereof, or a solvate thereof as an active ingredient Provided.
- the deoxycholic acid derivative compound of Formula 1, or a pharmaceutically acceptable salt or solvate thereof is administered in an amount of 0.001 mg to 1000 mg/day to an individual in need of prevention, improvement, or treatment of atopic dermatitis. , or an amount of 0.001 mg to 100 mg/day, or an amount of 0.01 mg to 10 mg/day may be administered to a warm-blooded animal weighing 75 kg to prevent, ameliorate, or treat atopic dermatitis.
- the dosage of the deoxycholic acid derivative compound of Formula 1 or its pharmaceutically acceptable salt or solvate for use in the present invention depends on various factors, such as the effectiveness and duration of action of the active ingredient, the mode of administration, the sex of the warm-blooded animal, It may vary depending on individual conditions such as age, weight, and the severity of other diseases.
- a specific administration route and dosage may be selected by a doctor/veterinarian in charge according to conditions such as the characteristics of the subject to be administered, that is, age, weight, disease state, and physical condition.
- the administration route of the composition may be administered through any general route as long as it can reach the target tissue.
- the composition of the present invention may be administered orally, intraperitoneally, intravenously, intramuscularly, subcutaneously, intradermally, intranasally, pulmonaryly, or intrarectally, but is not limited thereto.
- the composition may be administered by any device capable of transporting an active substance to a target cell.
- pharmaceutical preparations for oral administration may be presented in dosage unit form such as, for example, dragees, tablets, pills, powders, granules or capsules, and in ampoules. They are prepared by methods known per se, for example by conventional mixing, granulation, confectioning, dissolving or lyophilization methods.
- pharmaceutical preparations for oral administration are prepared by mixing the active ingredient with a solid carrier, granulating the mixture, and formulating the mixture or granules into tablets or dragees, after adding suitable excipients, if desired. It can be.
- Suitable carriers include in particular fillers such as sugars, for example lactose, saccharose, mannitol or sorbitol, cellulosic agents and/or calcium phosphates, for example tricalcium phosphate or calcium hydrogen phosphate, and binders, such as for example corn, Starch paste using wheat, rice or potato starch, gelatin, tragacanth, methylcellulose and/or polyvinylpyrrolidone and, if necessary, disintegrants such as the aforementioned starches, carboxymethyl starch, crosslinked polyvinylpyrrolidone money, agar or alginic acid or a salt thereof such as sodium alginate.
- fillers such as sugars, for example lactose, saccharose, mannitol or sorbitol, cellulosic agents and/or calcium phosphates, for example tricalcium phosphate or calcium hydrogen phosphate
- binders such as for example corn, Starch paste using wheat, rice or potato starch
- Additives are in particular flow-regulating agents and lubricants, for example silicic acid, talc, stearic acid or salts thereof, such as magnesium or calcium stearate, and/or polyethylene glycol.
- Concentrated sugar solutions which provide dragee cores with suitable coatings which can be resistant to gastric juices, and which optionally contain gum arabic, talc, polyvinylpyrrolidone, polyethylene glycols and/or titanium dioxide in suitable organic solvents or solvent mixtures;
- a lacquer solution may be used, or, to form a coating resistant to gastric fluid, a solution of a suitable cellulosic agent such as acetylcellulose phthalate or hydroxypropylmethylcellulose phthalate may be used.
- Other orally administrable pharmaceutical preparations include capsules, dry-filled capsules made of gelatin, and soft, sealed capsules made of gelatin and a plasticizer, such as glycerol or sorbitol.
- Dry-filled capsules contain the active ingredients in the form of particles, for example in admixture with fillers such as lactose, binders such as starches, and/or lubricants such as talc or magnesium stearate and, if appropriate, stabilizers. You may.
- the active ingredient is dissolved or suspended in a suitable liquid, such as fatty oil, paraffin oil or liquid polyethylene glycol, to which stabilizers may be added.
- Formulations for parenteral administration include sterilized aqueous solutions, non-aqueous solvents, suspensions, emulsions, freeze-dried formulations, and suppositories.
- Parenteral preparations can be injectable solutions effective in several ways, such as intravenous, intraarterial, intramuscular, intraperitoneal, intranasal, intradermal, subcutaneous, preferably intravenous.
- Such liquids are preferably isotonic aqueous solutions or suspensions which may be prepared prior to use from lyophilized preparations containing the active ingredient alone or together with a pharmaceutically acceptable carrier.
- the pharmaceutical preparations may be sterile and/or may contain additives such as preservatives, stabilizers, wetting and/or emulsifying agents, solubilizing agents, salts to adjust osmotic pressure and/or buffers.
- propylene glycol polyethylene glycol
- vegetable oils such as olive oil
- injectable esters such as ethyl oleate
- a base for the suppository witepsol, macrogol, tween 61, cacao butter, laurin paper, glycerogelatin, and the like may be used.
- the deoxycholic acid derivative compound of Formula 1 according to the present invention is administered in combination/combination with other drugs for the prevention, improvement, or treatment of atopic dermatitis. It can be. Therefore, the present invention also includes a method for treating atopic patients, including combination therapy with the deoxycholic acid derivative compound of Formula 1, a pharmaceutically acceptable salt or solvate thereof, and different agents for preventing/treating atopic dermatitis.
- an external preparation for preventing, improving or treating atopic dermatitis containing the deoxycholic acid derivative compound of Formula 1 or a pharmaceutically acceptable salt or solvate thereof as an active ingredient is provided.
- the composition for external application may be selected from the group consisting of creams, gels, ointments, emulsions, suspensions, sprays, and transdermal delivery patches, but is not limited thereto.
- the external preparation may be applied in an amount of 0.01 to 50 mg per day, specifically 0.1 to 20 mg per day, 1 to several times a day, specifically 1 It can be applied 1 to 3 times a day. It can be applied until the symptoms of atopic dermatitis get better.
- a cosmetic composition for preventing or improving atopic dermatitis containing a deoxycholic acid derivative compound of Formula 1 or a pharmaceutically acceptable salt or solvate thereof as an active ingredient is provided.
- the cosmetic composition is a soap for atopy, cleansing foam, cleansing cream, cleansing water, bath agent, skin lotion, skin softener, skin toner, lotion, cream, essence, astringent, emulsion, gel, lipstick, Sprays, shampoos, rinses, treatments, body cleansers, packs, massages, face powders, compacts, foundations, two-way cakes, and makeup bases may be prepared in any one or more formulations selected from, but are not limited thereto.
- the cosmetic composition may be commercialized as a formulation selected from the group consisting of soap for atopy, cleansing foam, cleansing cream, cleansing water and bathing agent.
- the formulation of the present invention is a paste, cream or gel, animal oil, vegetable oil, wax, paraffin, starch, tragacanth, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide are used as carrier components. It can be.
- lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component, and in particular, in the case of a spray, additional chlorofluorohydrocarbon, propane / May contain a propellant such as butane or dimethyl ether.
- a solvent, solubilizing agent or emulsifying agent is used as a carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1 ,3-butyl glycol oil, fatty acid esters of glycerol, polyethylene glycol or sorbitan.
- the formulation of the present invention is a suspension
- a liquid diluent such as water, ethanol or propylene glycol
- a suspending agent such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, microcrystals Star cellulose, aluminum metahydroxide, bentonite, agar or tragacanth and the like may be used.
- the formulation of the present invention is surfactant-containing cleansing
- carrier components aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, methyl taurate, sarcosinate, fatty acid amide Ether sulfates, alkylamidobetaines, fatty alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, lanolin derivatives, or ethoxylated glycerol fatty acid esters may be used.
- solvate is a form formed by adding a solvent to a compound, and includes monohydrate, dihydrate, and the like.
- atopic dermatitis is used in the meaning of including all diseases classified as atopic dermatitis in the art regardless of the direct or indirect cause of its occurrence. Atopic dermatitis usually refers to the time of onset or the subject of the invention.
- atopic dermatitis is defined to include all types of atopic dermatitis.
- atopic dermatitis means a state in which the infected part of the skin is changed by atopic dermatitis, and this state includes both a state considered as a skin disease and a state not considered as a skin disease.
- treatment includes complete cure of atopic dermatitis symptoms as well as partial cure, improvement, and relief of atopic dermatitis symptoms as a result of applying the pharmaceutical composition of the present invention to the atopic dermatitis site.
- prevention means preventing the symptoms of atopic dermatitis from occurring in advance by applying the pharmaceutical composition of the present invention to the skin, particularly atopic dermatitis, to suppress or block the symptoms of atopic dermatitis on the skin.
- “improvement” is meant to include alleviation, prevention or treatment of symptoms.
- active ingredient means a component that exhibits activity alone or exhibits activity together with a carrier (carrier) that itself has no activity.
- the pharmaceutical composition of the present invention is administered in a pharmaceutically effective amount.
- pharmaceutically effective amount means an amount sufficient to treat a disease with a reasonable benefit / risk ratio applicable to medical treatment or improvement, and the effective dose level is subject type and severity, age, sex, drug activity, drug sensitivity, administration time, route of administration and excretion rate, duration of treatment, factors including drugs used concurrently, and other factors well known in the medical field.
- the term "individual” refers to all animals, including humans, who have already developed or can develop atopic disease, and the deoxycholic acid derivative compound of Formula 1 according to the present invention, a pharmaceutically acceptable salt or solvent thereof
- the disease can be effectively prevented, improved or treated.
- the present invention provides a method for preventing, improving or treating atopic dermatitis comprising administering the pharmaceutical composition to a subject.
- the present invention provides the use of the pharmaceutical composition for use in preventing, improving or treating atopic dermatitis.
- composition containing the deoxycholic acid derivative compound of Formula 1 according to the present invention and a pharmaceutically acceptable salt or solvate thereof exhibits excellent effects in treating and improving atopic dermatitis.
- FIG. 1 is a schematic diagram of an experimental schedule for evaluating the effectiveness of a compound (HY303) according to an embodiment of the present invention in a mouse model of atopic dermatitis induced by MC903.
- Figure 2 is a diagram showing an image of a mouse ear lesion site when a compound (HY303) according to an embodiment of the present invention is topically or orally administered in an atopic dermatitis mouse model induced by MC903.
- Figure 3 is a diagram showing the results of measuring the thickness of the ear when the compound (HY303) according to an embodiment of the present invention was administered topically or orally to each atopic dermatitis-induced mouse model.
- FIG. 4 is a diagram showing clinical score results when a compound (HY303) according to an embodiment of the present invention is administered topically or orally to an atopic dermatitis-induced animal model.
- Figure 5 is a diagram and graph showing the results of measuring the thickness of the epidermis and dermis of the mouse ear when the compound (HY303) according to an embodiment of the present invention was administered topically or orally in an atopic dermatitis mouse model induced by MC903.
- the present invention relates to a pharmaceutical composition for preventing, improving or treating atopic dermatitis, including a composition containing a deoxycholic acid derivative compound of Formula 1, or a pharmaceutically acceptable salt or solvate thereof.
- HY303 in 1% hyaluronic acid (HA) gel was prepared according to the composition shown in Table 1 and used for topical treatment.
- HY303 represents the sodium salt of a deoxycholic acid derivative compound according to Formula 1, and the compound of Formula 3 (2-([3 ⁇ ,12 ⁇ -dihydroxy-24-oxo-5 ⁇ -cholan-24-yl] It is the sodium salt of amino)benzensulfonic acid (2-([3 ⁇ ,12 ⁇ -Dihydroxy-24-oxo-5 ⁇ -cholan-24-yl]amino)benzensulfonic acid sodium salt).
- HY303 in 0.5% CMC was prepared by dissolving 500mg carboxymethylcellulose (CMC) in 100mL of distilled water to prepare 0.5% CMC, and then adding 100mg HY303 to 80mL of 0.5% CMC to prepare 1.25mg/ml HY303.
- CMC carboxymethylcellulose
- 200 ⁇ l of 1.25 mg/ml HY303 (calculated as 25 g of mouse weight) was used for oral treatment in mice of the 10 mg/kg HY303 group.
- MC903 (Sigma, C4369-10MG) for inducing atopic dermatitis on the skin of mice was dissolved in 100% ethanol (Merck, CAS-No. 64-17-5) to prepare 1 nM MC903 1mL, 10 ⁇ L was applied to both ears.
- Atopic dermatitis was induced by applying the same amount of MC903 to cover both ears of Balb/C mice.
- HY303 was topically and orally administered to an atopic dermatitis-induced mouse model.
- Each processing schedule and method are as shown in FIG. After installing the cage the day before the experiment, mice were placed in the cage and experimental groups were set as follows.
- mice were labeled with a marker pen either at the ear-punch or at the tail.
- 10 ⁇ L of MC903 was applied to both sides (inner and outer) of the ears of Balb/C mice using a pipette according to the schedule shown in FIG. 1 .
- the same amount of MC903 was applied to the entire ear in all mice.
- the MC903 solution was not applied twice to one area, and the mouse ears were observed until the MC903 was completely dry.
- the experiment period may take more than 10 days depending on the degree of recovery of the thickness of the ear. Ear thickness and weight were measured on the 1st, 3rd, 5th, 7th, and 11th days, and images of the lesion area were collected.
- the MC903 group was 265.00 ⁇ 6.52 ⁇ m, 43.33 ⁇ m thicker than the control group, 221.67 ⁇ 1.67 ⁇ m, and the 0.5% HY303 group was 227.00 ⁇ 4.90 ⁇ m, compared to the MC903 group. It was confirmed that it decreased by 38.00 ⁇ m.
- the MC903 group Upon oral administration, the MC903 group was 290.00 ⁇ 13.04 ⁇ m, 68.33 ⁇ m thicker than the control group 221.67 ⁇ 1.67 ⁇ m, and the 10 mpk HY303 group was 258.00 ⁇ 7.18 ⁇ m, a decrease of 32.00 ⁇ m compared to the MC903 group (FIG. 3).
- the clinical score was also confirmed to decrease by 0.13 compared to the MC903 group from 1.00 ⁇ 0.05 in the MC903 group to 0.87 ⁇ 0.03 in the 0.5% HY303 group.
- the MC903 group decreased by 0.12 compared to the MC903 group from 1.22 ⁇ 0.04 to 10 mpk HY303 group 1.10 ⁇ 0.04 (FIG. 4).
- the epithelial thickness of the MC903 group was 23.40 ⁇ 1.00 ⁇ m, 7.60 ⁇ m thicker than the control group’s 15.80 ⁇ 0.66 ⁇ m, and the 0.5% HY303 group was 20.10 ⁇ 1.08 ⁇ m, a decrease of 3.30 ⁇ m compared to the MC903 group.
- the MC903 group was 189.00 ⁇ 8.22 ⁇ m, 65.17 ⁇ m thicker than the control group 123.84 ⁇ 4.58 ⁇ m, and the 0.5% HY303 group was 145.88 ⁇ 7.74 ⁇ m, a decrease of 43.13 ⁇ m compared to the MC903 group (FIG. 5).
- Deoxycholic acid derivative compound of Formula 1 10 mg of a pharmaceutically acceptable salt thereof or a solvate thereof
- the powder After powdering and mixing the above ingredients, the powder is prepared by filling in an airtight bag.
- Deoxycholic acid derivative compound of Formula 1 a pharmaceutically acceptable salt thereof or a solvate thereof 10 mg
- Tablets are prepared by mixing the above ingredients according to a conventional tablet manufacturing method and then tableting them.
- Deoxycholic acid derivative compound of Formula 1 a pharmaceutically acceptable salt thereof or a solvate thereof 10 mg
- the capsule preparation is prepared by filling a gelatin capsule.
- Deoxycholic acid derivative compound of Formula 1 a pharmaceutically acceptable salt thereof or a solvate thereof 10 mg
- Deoxycholic acid derivative compound of Formula 1 a pharmaceutically acceptable salt thereof or a solvate thereof 10 mg
- Deoxycholic acid derivative compound of Formula 1 a pharmaceutically acceptable salt thereof or a solvate thereof 10 mg
- Deoxycholic acid derivative compound of Formula 1 a pharmaceutically acceptable salt thereof or a solvate thereof 10 mg
- Deoxycholic acid derivative compound of Formula 1 a pharmaceutically acceptable salt thereof or a solvate thereof 0.001
- Deoxycholic acid derivative compound of Formula 1 a pharmaceutically acceptable salt thereof or a solvate thereof 0.001
- Deoxycholic acid derivative compound of Formula 1 a pharmaceutically acceptable salt thereof or a solvate thereof 0.001
- Deoxycholic acid derivative compound of Formula 1 a pharmaceutically acceptable salt thereof or a solvate thereof 0.001
- Deoxycholic acid derivative compound of Formula 1 a pharmaceutically acceptable salt thereof or a solvate thereof 0.001
- Deoxycholic acid derivative compound of Formula 1 a pharmaceutically acceptable salt thereof or a solvate thereof 0.001
- Deoxycholic acid derivative compound of Formula 1 a pharmaceutically acceptable salt thereof or a solvate thereof 0.001
- Deoxycholic acid derivative compound of Formula 1 a pharmaceutically acceptable salt thereof or a solvate thereof 0.001
- Deoxycholic acid derivative compound of Formula 1 a pharmaceutically acceptable salt thereof or a solvate thereof 0.001
- Deoxycholic acid derivative compound of Formula 1 a pharmaceutically acceptable salt thereof or a solvate thereof 0.001
- a powder pact is prepared using the above ingredients according to a conventional method in the cosmetics manufacturing field for preparing a powder pact.
- Deoxycholic acid derivative compound of Formula 1 a pharmaceutically acceptable salt thereof or a solvate thereof 0.001
- the compound of the present invention can provide a pharmaceutical composition for preventing, improving or treating atopic dermatitis, and thus can be usefully used in the field of medicine.
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Abstract
La présente invention concerne une composition comprenant un nouvel inhibiteur d'inflammasome en tant que principe actif pour la prévention, le soulagement ou le traitement de la dermatite atopique.
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Citations (4)
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WO2003029268A1 (fr) * | 2001-10-03 | 2003-04-10 | Merck & Co., Inc. | Androstane 17-beta-carboxamides en tant que modulateurs de recepteurs d'androgenes |
US20080166301A1 (en) * | 2000-06-22 | 2008-07-10 | Hanson Robert N | Steroidal antiestrogens and antiandrogens and uses thereof |
US20140045808A1 (en) * | 2012-08-13 | 2014-02-13 | of Nevada, Las Vegas | Reducing Risk of Contracting Clostridium-Difficile Associated Disease |
KR20180100703A (ko) * | 2016-01-28 | 2018-09-11 | 치아타이 티안큉 파마수티컬 그룹 주식회사 | 스테로이드 유도체 fxr 작용체 |
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KR101452864B1 (ko) | 2011-11-17 | 2014-11-04 | 서울대학교산학협력단 | Gpcr19 경로의 활성화에 의한 골수 유래 면역 조절 세포 및 면역 조절 b 림프구의 체내외 증폭 |
KR101548955B1 (ko) | 2013-08-26 | 2015-09-02 | (주)샤페론 | Gpcr19 작용제를 유효성분으로 함유하는 아토피 예방 또는 치료용 조성물 |
KR101998402B1 (ko) | 2014-09-22 | 2019-07-10 | (주)샤페론 | Gpcr19 작용제를 유효성분으로 함유하는 아토피 예방 또는 치료용 조성물 |
-
2022
- 2022-09-26 WO PCT/KR2022/014366 patent/WO2023048528A1/fr unknown
- 2022-09-26 KR KR1020220121782A patent/KR20230043774A/ko unknown
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KR20180100703A (ko) * | 2016-01-28 | 2018-09-11 | 치아타이 티안큉 파마수티컬 그룹 주식회사 | 스테로이드 유도체 fxr 작용체 |
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