40 results about "Adapalene" patented technology

An improved method and preparation for the treatment of acne and hirsutism comprises topically applying an effective amount of a saw palmetto berry extract, and preferably one or more low irritability constituents that enhance penetration of the extract into hair follicle sebaceous glands. The low irritability penetration aid may be selected from the group consisting of adapalene, tretinoin, tretinoin gel microsponges, retinaldehyde, retinol, tazarotene, beta hydroxy acids (salicylic acid), azelaic acid, and alpha hydroxy acids (glycolic acid) as well as polyolprepolymer-2.

An improved method and preparation for the treatment of acne and hirsutism comprises topically applying an effective amount of a saw palmetto berry extract, in combination with two classes of low irritability penetrating agents that enhance penetration of the extract into hair follicles and sebaceous glands. The low irritability penetration agents are selected from the group (A) comedolytics consisting of adapalene, tretinoin, tretinoin gel microsponges, retinaldehyde, retinol, and tazarotene, and (B) keratinolytics consisting of the beta hydroxy acid, salicylic acid, and the alpha hydroxy acid, glycolic acid. Polyolprepolymer-2 may be incorporated into the preparation as well.

Administration of adapalene in a topical medicament to a patient so as to sustain its biological response in the treatment of acne vulgaris, wherein the administration pattern of the topical medicament comprises topically applying onto the afflicted skin area a therapeutically effective amount of adapalene at least once every two days for at least 6 months.

The present invention provides for a method of using adapalene for the maintenance theray of acne vulgaris to prevent acne recurrence or reduce the severity of the acne recurrence.

The invention discloses an externally applied medicine for treating skin disease and application thereof. The medicine consists of an active ingredient and pharmaceutically acceptable auxiliary materials, wherein the active ingredient is a mixture of diflorasone and adapalene, or a mixture of diflorasone and acitretin, or a mixture of diflorasone, adapalene and acitretin. The invention overcomes the defects of poor treatment effect and high side effect of single medication, and the diflorasone and the adapalene or / and the acitretin are compounded to form the compound externally applied medicine. The preparation can be prepared into externally applied formulations in different forms; and due to synergic and complementary effects of medicines, the compound externally applied medicine has high treatment effect, lightens the adverse reaction of the patient in clinical application, has an obvious treatment effect on skin disease, and is easily accepted by the patient.

The present invention relates to an agent for use in selectively killing one or more senescent cells, wherein the agent is selected from the following: a cardiac glycoside or alglycone, a focal adhesion kinase (FAK) inhibitor, an HMG-CoA reductase inhibitor, JFD00244, Cyclosporine, Tyrphostin AG879, Cantharidin, Diphenyleneiodonium chloride, Rottlerin, 2,3-Dimethoxy-1,4-naphthoquinone, LY-367,265,Rotenone, Idarubicin, Dequalintum chloride, Vincristine, Nitazoxanide, Nitrofurazone, Temsirolimus, Eltrombopag, Adapalene, Azacyclonol, Enoxacin and Raltegravir, and pharmaceutically acceptable salts thereof. Another aspect relates to compounds for use in treating or preventing a senescence- associated disease or disorder, and methods relating thereto.

This invention discloses a method for preparing adapalene. The method comprises: (1) reacting halogenated anisole and adamantanol in solvent in the presence of acid at -10-150 deg.C to obtain 2-(1-adamantyl)-4-bromophenyl ether; (2) reacting with magnesium in the presence of iodine, iodide or bromide in ether or a nonpolar solvent to obtain a Grignard reagent; (3) reacting with 6-bromo-2-naphthoate, and hydrolyzing with a base to obtain adapalene. The method has such advantages as high product yield, few side reactions, simple operation, little pollution and low cost, and is suitable for mass production.

A process for preparing adapalene features the hydrolyzing reaction between 6[3-(1-adamantyl)-4methoxyphenyl]-2-methyl naphthanleneformate and one or more of potassium hydroxide, ammonia water and potassium carbonate in polar solvent.

A novel maintenance therapy regime / regimen for the treatment of acne related diseases includes administering an oral antibiotic with a topical fixed-dose combination of a retinoid, such as adapalene, and an anti-bacterial agent, such as benzoyl peroxide.

The present invention relates to stable fixed dose topical formulations comprising an antiacne agent and an antibiotic, which exhibit storage stability at a temperature of about 40° C. and relative humidity of about 75% for a period of at least 3 months. Particularly, the present invention relates to stable fixed dose topical formulations comprising therapeutically effective amounts of (a) adapalene-containing microspheres and (b) clindamycin, a process for their preparation thereof and their use for the treatment of acne.

The present invention relates to a method for treating, reducing or preventing acne. In particular, the present invention relates to methods for reducing the total number, incidence and severity of acne lesions on the skin which includes both inflammatory and non-inflammatory lesions. Further, the invention relates to reducing the incidence and severity of adverse events resulting from topical application of anti-acne agents resulting in improvement of skin tone. The method includes administering a novel and stable topical anti-acne pharmaceutical composition.

The invention discloses an adapalene vesicle and a preparation method thereof, and a preparation containing the adapalene vesicle, and a preparation method thereof, and belongs to the field of pharmaceutical preparations. The adapalene vesicle is prepared from adapalene, a nonionic surfactant and an additive, and is preferably prepared in an external application gel dosage form. According to the present invention, the transdermal adapalene delivery external application preparation has the unique advantages; with the application of the novel vesicle delivery system, the transdermal absorption of drugs can be increased, the clinical treatment effect can be enhanced, and the toxic-side effect during the oral taking can be avoided; and the preparation can be used for treating comedo, papule, pustule and other acne.

The invention discloses vitamin A compound and paeonol condensed derivatives and a preparation method. The vitamin A compound and paeonol condensed derivatives include derivatives in structures I-VII shown as follows; a structure I is ester formed by paeonol and all-trans retinoic acid; a structure II is ester formed by paeonol and 13-cis-retinoic acid; a structure III is ester formed by paeonol and acitretin; a structure IV is ester formed by paeonol and 9-cis-retinoic acid; a structure V is ester formed by paeonol and adapalene; a structure VI is ester formed by paeonol and tazarotene; a structure VII is ester formed by paeonol and bexarotene. By the vitamin A compound and paeonol condensed derivatives and the preparation method, irritation of vitamin A compounds to skin mucosa is relieved; after application to skin, the vitamin A compounds and paeonol are released under the action of hydrolase to dissolve cutin, promote epithelial cell differentiation and the like so as to realize anti-inflammatory and anti-oxidation functions.

An object of the present invention is to provide a medicine that can simply treat and / or prevent a retinal degenerative disease associated with photoreceptor degeneration, including retinitis pigmentosa. The solution is to provide an agent for treating and / or preventing a retinal degenerative disease associated with photoreceptor degeneration, containing a compound having a retinoic acid receptor agonistic activity (for example, tamibarotene, tamibarotene methyl ester, tamibarotene ethyl ester, tazarotene, tazarotenic acid, adapalene, palovarotene, retinol, isotretinoin, alitretinoin, etretinate, acitretin or bexarotene) or a salt thereof.

A topical pharmaceutical composition comprises adapalene or a pharmaceutical acceptable salt thereof and minocycline or a pharmaceutical acceptable salt thereof. The composition is for topical application and used to treat acne.

The present invention relates to a method for treating, reducing or preventing acne. In particular, the present invention relates to methods for reducing the total number, incidence and severity of acne lesions on the skin which includes both inflammatory and non-inflammatory lesions. Further, the invention relates to reducing the incidence and severity of adverse events resulting from topical application of anti-acne agents resulting in improvement of skin tone. The method includes administering a novel and stable topical anti-acne pharmaceutical composition.

The invention provides compositions comprising as active agents benzoyl peroxide (BPO), adapalene and optionally clindamycin phosphate, kits and uses thereof in methods for treating skin surface condition in a subject in need thereof.

The invention relates to the application of tazarotene to preparation of drugs used for treating hepatitis B virus infection, belonging to the technical field of medicine. The identification results of virus transfection and infection cell model tests prove that tazarotene, a tretinoin drug, has strong anti-hepatitis B virus activity, presents long-lasting virus inhibition ability after withdrawal, and is free of cytotoxic effect at corresponding antiviral working concentrations. The invention also discloses that tazarotene has relatively specific activity in interfering with the stability ofcccDNA and inhibiting the transcription of cccDNA, and discloses the anti-hepatitis B virus activity of adapalene which also belongs to tretinoin drugs and is an analogue of tazarotene. The inventionprovides a technical and theoretical foundation for the application of tazarotene and its analogues to clinical anti-hepatitis B virus intervention and for the preparation of novel anti-hepatitis B virus drugs based on tazarotene and its analogues and derivatives.

The invention relates to the technical field of fine chemical engineering, and provides a synthetic method of adapalene. The synthetic method comprises: performing a coupling reaction of 2-methoxycarbonyl-6-naphthyl p-toluenesulfonate or 2-methoxycarbonyl-6-naphthyl dimethylamino sulfamide with bis(4-methoxyl-3-adamantyl phenyl)boric acid under the catalysis of nickel to obtain 6-[3-(1-adamantyl)-4-methoxyl phenyl]-2-methyl naphthoate, and then performing hydrolysis to obtain the adapalene product. The method of the invention substitutes bis(4-methoxyl-3-adamantyl phenyl)boric acid with a mild preparation condition and low price for 4-methoxyl-3-adamantyl phenylboronic acid with high price, and reaches the purpose of reducing raw material cost without using air-sensitive metal organic reagents; the method also partially substitutes cheap N,N'-bisalkyl N-heterocyclic carbene precursor quaternary ammonium halogen salt for organic phosphine ligands, is simple in preparation operation, and has a significantly increased product yield of 58-90%; the production cost is decreased obviously; the generation of 'three wastes' is less; and the method is suitable for industrial scale production.

The invention discloses an external medicament for treating skin diseases and an application thereof. The medicament consists of a pharmaceutically active component and a pharmaceutically-acceptable auxiliary material, wherein the pharmaceutically active component is a mixture of beclomeasone propionate and adapalene, or a mixture of beclomeasone propionate and abamectin A, or a mixture of beclomethasone, adapalene and abamectin A. Due to the adoption of the external medicament, the defects of poor curative effect of single administration and large side effect are overcome, and a compound external medicament is prepared by compounding beclomeasone propionate, adapalene or / and abamectin A. A preparation provided by the invention can be prepared into external dosage forms of different forms; and under the synergic actions and complementary actions of medicaments, the compound external medicament has an enhanced curative effect, untoward effects of patients are reduced in clinical application, the treatment effects on skin diseases are remarkable, and the external medicament is easy to accept for patients.

The present invention relates to stable fixed dose topical formulations comprising an antiacne agent and an antibiotic, which exhibit storage stability at a temperature of about 40° C. and relative humidity of about 75% for a period of at least 3 months. Particularly, the present invention relates to stable fixed dose topical formulations comprising therapeutically effective amounts of (a) adapalene-containing microspheres and (b) clindamycin, a process for their preparation thereof and their use for the treatment of acne.

A method of treating preadolescent acne is described. The method can include administering an effective amount of a pharmaceutical composition that includes a fixed combination of adapalene and benzol peroxide to a preadolescent patient in need thereof.The preadolescent patient can be from age 7 to age 11, and the pharmaceutical composition can include from 0.01% to 2% by weight of adapalene and from 0.1% to 5% by weight by weight of benzol peroxide.Also described, is a composition for use in such a method.

Process for the obtaining of 1-adamantane (tricycle[3.3.1.1 (3,7)]decane) derivatives, or of a pharmaceutically acceptable salt thereof, based on a carboxylation reaction, via metallation, of a precursor compound with an adequate leaving group. It also comprises the preparation of the precursor compound by means of a selective coupling of the corresponding boron, magnesium or zinc derivative with the corresponding disubstitute aromatic derivative. It is especially useful for the obtaining of Adapalene at industrial scale with good yield and high purity.

This invention relates to a new synthesis route and method of adapalene, namely 6-[3-(1-adamanty)-4-methoxy phenyl]-2-naphthoic acid. In a ethers solvent or a non-polar solvent, an organic zincon is generated by reacting 2-(1-adamanty)-4-bromoanisole with a metal zinc. In the presence of a catalyst of niCl2 / DPPE, the organic zincon is reacted with 6-bromo-2-naphthoic acid methyl ether, then the adapalene is obtained after processes of alkaline saponification reaction, water washing, acidifying with hydrochloric acid and recrystallization or the like. The invention has advantages of mild reaction temperature, simple operation, low cost and high yield, so that the yield of each step is more than 90% and the total yield is more than 65%.

The invention discloses an adapalene and vitamin E compound emulsifiable paste and a preparation method thereof. The preparation contains 0.08% to 0.12% of adapalene and 1.0% to 2.0% of vitamin E by weight. The preparation method of the adapalene and vitamin E compound emulsifiable paste includes respectively preparing an oil phase and a water phase, preparing a medicine solution, pouring the oil phase into the water phase, adding the medicine solution into the solution after stirring and cooling, and stirring the mixture evenly to form stable emulsifiable paste. The adapalene and vitamin E compound emulsifiable paste can effectively treat chloasma.

A hyaluronic acid product is comprising a cross-linked hyaluronic acid and one or more cyclodextrin molecules, and further comprising a guest molecule capable of forming a guest-host complex with the aminocyclodextrin molecule acting as a host, wherein the guest molecule is a retinoid, preferably adapalene, or a RAM BA. The hyaluronic acid is cross-linked by ether bonds, and the one or more cyclodextrin molecules are grafted onto the cross-linked hyaluronic acid by amide bonds, preferably using a triazine-based coupling reagent.

The invention provides a method for synthesizing adapalene intermediate 6-bromo-2-naphthoate. The method comprises the following steps: 1), mixing 2-naphthalic acid and an organic solvent uniformly, adding a catalyst, performing stirring, introducing protective gas, controlling pressure at 4-7 atmospheres, controlling the temperature at 130-155 DEG C, maintaining the conditions for 50-70 minutes,then adding dropwise a mixed aqueous solution containing bromide salt and benzenesulfonic acid, adding dropwise an aqueous solution containing only hypobromite, controlling the total dropwise additiontime within 90-150 minutes, heating the system to 165-180 DEG C after dropwise addition, raising pressure to 11-17 atmospheres to continue the reaction for 5-7 hours and ending the reaction; 2) removing solid by filtering while the mixed solution is hot, adding the solid to ice water with weight 3-5 times that of the filtrate, and performing extraction, drying, evaporative concentration for removing a solvent to obtain a product. The method has high yield, and no harmful substances are discharged.

A hyaluronic acid product is comprising a cross-linked hyaluronic acid and one or more cyclodextrin molecules, and further comprising a guest molecule capable of forming a guest-host complex with the aminocyclodextrin molecule acting as a host, wherein the guest molecule is a retinoid, preferably adapalene, or a RAM BA. The hyaluronic acid is cross-linked by ether bonds, and the one or more cyclodextrin molecules are grafted onto the cross-linked hyaluronic acid by amide bonds, preferably using a triazine-based coupling reagent.

The invention discloses an adapalene clindamycin hydrochloride compound gel preparation and a preparation method thereof. The preparation contains 0.08 to 0.12 percent of adapalene and 0.8 to 1.2 percent of clindamycin hydrochloride according to the weight percentage. The preparation method for the adapalene clindamycin hydrochloride compound gel comprises the steps of: preparing a gel matrix, swelling, sterilizing, dissolving the adapalene and the clindamycin hydrochloride into the gel matrix respectively, and using triethanolamine to adjust the pH value to form the steady gel. The product can effectively treat acne.