59 results about "Elastase inhibitor" patented technology

The present invention relates to the use of an elastase inhibitor, preferably fahsin for the treatment or prevention of emphysema, COPD or lung cancer. The elastase inhibitor is preferably administered through inhalation, preferably thorough inhalation of tobacco smoke. The invention also comprises smoking articles comprising such an elastase inhibitor.

The invention discloses a radix gentianae extract and a preparation method and application thereof. The preparation method of the radix gentianae extract comprises the following steps that 1, radix gentianae and a solvent are mixed, extracted and filtered, pressure is reduced, the solvent is removed, and the radix gentianae extract is obtained; 2, the radix gentianae extract is dissolved in water, sampled to a resin filling column andeluted through water and an ethanol solution in sequence, eluent is collected, pressure is reduced, ethyl alcohol and water are removed, and the radix gentianae extract is obtained. The preparation method of the radix gentianae extract is simple, and the obtained radix gentianae extract can be applied as tyrosinase inhibitor, elastinase inhibitor, antioxidant active agent and anti-aging active agent, preferentially applied in preparation of skin care products or cosmetics.

treating method for hair growth inhibition, which comprises administering (A) the extract of a plant of the family Juniperus or a malt. In addition, the present invention relates to a dermatologic composition for external use, which comprises (B) an elastase inhibitor or neutral endopeptidase inhibitor, and the above-described component (A) and / or (C) at least one proteolytic enzyme selected from the group consisting of papain, trypsin, chymotrypsin, pepsin, bromelain, ficin and pancreatin.

Azlactone Compound (2) is reacted with Amidine Compound (3) to give Pyrimidine Compound (1) which is useful as an intermediate for the production of enzyme inhibitors (e.g., elastase inhibitor, chymase inhibitor etc.): wherein each symbol is as defined in the specification.

The present invention relates to an elastase inhibitor containing, as an active ingredient, a protein hydrolysate (with soybean protein hydrolysate and almond protein hydrolysate being excluded). According to the present invention, there can be provided pharmaceuticals and cosmetics which exhibit inhibitory effect against the growth of body hair, and skin aging preventing effect by restoring elasticity and tonicity of the skin and reducing wrinkles.

The present invention provides a fibrinogen-based tissue adhesive which contains an elastase inhibitor.

The present invention relates to a heterocyclic compound of the following formula (I-a), its ester, or a salt thereof, and a human neutrophilic elastase inhibitor containing the same as the active ingredient, etc.wherein A and B are the same or different and each is a lower alkylene group being optionally substituted by an oxo group, D is a heteromonocyclic or heterobicyclic group being optionally substituted by an oxo group, R<1 >and R<2 >are the same or different and each is a lower alkyl group, R<3 >and R<4 >are different from each other, and each is a hydrogen atom or a hydroxy group, or both combine together to form an oxo group, and R<5 >is 2-benzoxazolyl, trifluoromethyl, benzylamino-carbonyl, etc.

The invention relates to an efficient composite system for preventing stretch marks and application of the system in cosmetics. The composite system is prepared from micro-molecular sodium hyaluronate, chondroitin sulfate, a fibrous protein polypeptide composite, amino acids, an ascorbic acid derivative, an elastase inhibitor, a fibroblast accelerator, a moisturizing and conditioning agent and a matrix. Based on the pathogenesis of the stretch marks, the stretch marks are comprehensively effectively prevented from the aspects of maintenance of an acellular dermal matrix environment, pathological inhibition or remission and nourishing and maintenance of skin. Besides, the efficient composite system can be used in lotion, cream, gel and various cosmetics, and the efficient composite system is safe, free of irritation and suitable for products for pregnant women.

The invention is directed to methods of converting a carboxylic acid group in a compound, via a redox active ester, to a corresponding boronic ester by treatment with bis(pinacolato)diboron-alkyllithium complex in the presence of a ligand, a Ni(ll) salt or a copper salt, and an Mg(ll) salt, in the presence of an alkyllithium or a lithium hydroxide or alkoxide salt. The product pinacolato boronateester can be cleaved to provide a boronic acid. The invention is also directed to methods of preparing various compounds of medical value comprising boronic acid groups, and to novel boronic-acid containing compounds of medicinal value, including an atorvastatin boronic acid analog, a vancomycin aglycone boronic acid analog, and boronic acid containing elastase inhibitors mCBK319, mCBK320, mCBK323, and RPX-7009.

The invention discloses skin lotion and a preparation method thereof. The skin lotion is prepared from the following components by weight: (1) 30 to 60 parts of honeysuckles, (2) 20 to 50 parts of radix isatidis, (3) 10 to 20 parts of scutellaria baicalensis, (4) 5 to 10 parts of cordate houttuynia, (5) 1 to 3 parts of sodium chloride, (6) 1 to 3 parts of mint oil, (7) 2 to 10 parts of collagen, (8) 2 to 5 parts of a collagenase inhibitor, (9) 2 to 5 parts of an elastase inhibitor, and 300 to 500 parts of deionized water. The skin lotion has the effects of whitening and moistening the skin andkilling germs on the skin, goes green and is environmentally friendly.

The invention discloses a skin tightening composition. The skin tightening composition comprises antioxidants, humectants and elastase inhibitors. The elastase inhibitors mainly comprise one or more types of rhizoma polygoni cuspidati extract, ramulus et folium picrasmae alkaloid and anthocyanin. The skin tightening composition has the advantages that oxidative injury of skin can be reduced by theadded antioxidants, and senility of the skin can be delayed by the added antioxidants; water can be replenished by the added humectants, and water retention barriers further can be formed on the surface of the skin by the added humectants; the skin can be effectively tightened by the added elastase inhibitors, and accordingly elasticity of the skin can be improved; synergistic effects can be realized by components in the skin tightening composition, accordingly, good effects of tightening the skin can be realized, and cosmetics can have good skin tightening and antioxidant functions if the skin tightening composition is applied to the cosmetics.

The present invention relates to an elastase inhibitor containing, as an active ingredient, a protein hydrolysate (with soybean protein hydrolysate and almond protein hydrolysate being excluded). According to the present invention, there can be provided pharmaceuticals and cosmetics which exhibit inhibitory effect against the growth of body hair, and skin aging preventing effect by restoring elasticity and tonicity of the skin and reducing wrinkles.

An arctigenin derivative used for anti-aging treatment, including protection of the skin from the sun and recovery of skin elasticity. A variety of fatty acid ester derivatives, alcohol ether derivatives and alkylated derivatives are used as the arctigenin derivatives. Agents for controlling ET-1 production, elastase inhibitors, and anti-inflammatory agents are prepared. Such arctigenin derivatives are particularly useful as an external agent for the skin, such as an anti-inflammatory external agent, a sunscreen external agent, or an external agent for recovering elasticity.

An elastase inhibitor contains raspberry extract and hydroxyproline as active ingredients, and optionally contains yeast extract.

The invention discloses an anti-aging and skin-tendering combined liquid and a preparation method thereof. The combined liquid comprises purified water, a matrix metalloproteinase inhibitor, an elastase inhibitor, a non-enzymatic glycosylation inhibitor, an active factor, a free radical scavenger, a humectant, an emulsifier, a buffer agent, a suspending aid, a chelating agent, a bacteriostatic agent and a stabilizer. Starting from six aspects of scavenging free radicals, repairing a barrier function of skin, supplying energy, improving cell viability, recovering a skin tissue structure, recovering a nerve-immune-endocrine system and the like, the purpose of recovering and perfecting normal skin cells and a skin tissue ecological system is achieved, a skin self-repairing mechanism is started, skin injury healing is promoted, and therefore, efficient, safe and durable anti-aging and repairing effects are achieved.

The invention discloses a limonium sinense(Girard)O.Kuntze extract and a preparation method and application thereof. The preparation method of the limonium sinense(Girard)O.Kuntze extract comprises the following steps that 1, limonium sinense(Girard)O.Kuntze is mixed with a solvent, extraction and filtration are conducted, the solvent is removed through pressure reduction, and a limonium sinense(Girard)O.Kuntze crude extract is obtained; 2, after the limonium sinense(Girard)O.Kuntze crude extract is dissolved in water and then loaded on a resin packed column, elution is conducted with water and an ethanol solution in sequence, eluents are collected respectively, ethanol and the water are removed through pressure reduction, and the limonium sinense(Girard)O.Kuntze extract is obtained. The preparation method of the limonium sinense(Girard)O.Kuntze extract is simple, the obtained limonium sinense(Girard)O.Kuntze extract can be applied to serve as a tyrosinase inhibitor, an elastic protease inhibitor, an antioxidant activator and an anti-ageing activator; preferably, application of the limonium sinense(Girard)O.Kuntze extract in preparing skin care products or cosmetics is achieved.

The invention relates to the use of deuterium oxide (D2O) as an elastase inhibitor and especially as an inhibitor of the human neutrophil elastase (HNE). The invention also relates to the use of deuterium oxide for the prophylaxis and / or treatment of HNE-related diseases.

The present invention relates to a treating method for hair growth inhibition, which comprises administering (A) the extract of a plant of the family Juniperus or a malt. In addition, the present invention relates to a dermatologic composition for external use, which comprises (B) an elastase inhibitor or neutral endopeptidase inhibitor, and the above-described component (A) and / or (C) at least one proteolytic enzyme selected from the group consisting of papain, trypsin, chymotrypsin, pepsin, bromelain, ficin and pancreatin.

The invention provides anelastase inhibitor for use in the promotion of muscle regeneration in the treatment of a myopathy, as well as a method for promoting muscle regeneration in a subject with a myopathy, the method comprising providing the subject with a therapeutically effective amount of an elastase inhibitor. Further provided is a pharmaceutical composition comprising anelastase inhibitor for use in the promotion of muscle regeneration in the treatment of a myopathy. Elastase inhibitors may have a protective effect on muscle progenitor cells and their regenerative potential, which aids muscle cell regeneration. By protecting regenerative potential of muscle progenitor cells, elastase inhibitors enable or enhance the grown of new or existing muscle fibres.

The present disclosure is directed to methods of treatment, including treatment of a myopathy by administering to a subject in need thereof an elastase inhibitor in combination with a glucocorticoid. The present disclosure is also directed to pharmaceutical compositions that include an elastase inhibitor that can be used in such treatment.

The invention provides a prodrug of an elastase inhibitor and application of the prodrug. The prodrug of the elastase inhibitor is a compound with a structure shown in a formula I defined in the description or pharmaceutically acceptable salt, ester, isomer, solvate, prodrug or isotope label of the compound. Compared with a compound 52 (control) in the patent WO2018175173A1, the prodrug compound of the elastase inhibitor has the advantages of high lung exposure and long half-life period. The prodrug compound provided by the invention greatly improves the concentration and residence time of an active compound (control) in the lung, and has a remarkable improvement in the aspect of in-vivo PK compared with the control.

The invention relates to the field of medicines, in particular to a preparation method of an elastase inhibitor compound. The preparation method comprises the step of reacting a compound 10 in the presence of a boronizing reagent, an acidifying reagent and a reaction solvent to obtain the elastase inhibitor compound as shown in the formula (I). The method is environment-friendly, simple and convenient to operate, efficient, mild in reaction condition, easy to control the operation, safe, reliable, low in cost and good in economic benefit. Meanwhile, the preparation method is high in reaction yield, the obtained product is high in purity, and the preparation method is suitable for industrial production. # imgabs0 #

The invention relates to the use of an essential oil of white fir tree (Abies alba) branches as an elastase inhibitor for combating the signs of skin ageing, in particular for limiting and / or reducing the degradation of elastic skin fibers, the loosening of skin and / or the loss of elasticity of the skin and / or the appearance of wrinkles.

The invention discloses a recombinant protein, which consists of a transdermal peptide connected to fibronectin through a connecting peptide to form a recombinant transdermal fibronectin, and then carries out E174D and P292G site mutations on the amino acid sequence of the recombinant transdermal fibronectin to obtain a recombinant transdermal fibronectin. A fibronectin mutant, the amino acid sequence of the recombinant transdermal fibronectin mutant is shown in SEQ ID No.1, and the flexible end of the recombinant transdermal fibronectin mutant is connected to an elastase inhibitor by a connecting peptide Peptides are constructed. The recombinant protein provided by the invention has better stability and guaranteed efficacy, is easy to prepare and has low cost, and greatly expands the application of fibronectin and collagenase inhibitory peptides in cosmetics.

This invention belongs to the pharmaceutical field and relates to an elastase inhibitor and its application in disease treatment. Specifically, it relates to a compound of formula (I), a pharmaceutical composition comprising compound (I), and its application in disease treatment. The compound of formula (I) of this invention has an inhibitory effect on elastase and can be used to treat or prevent diseases caused by the action of elastase, including systemic inflammatory response syndrome (SIRS) with acute lung injury (ALI) / acute respiratory distress syndrome (ARDS).

To provide compounds that are obtained from extract of natural origin and have radical erasing action, hyaluronidase activity inhibitory action, PGE2 production inhibitory action, tyrosinase activity inhibitory action, elastase activity inhibitory action, collagen type I production promoting action and dermal papilla cell proliferation promoting action.SOLUTION: The present invention provides a ketone compound represented by the formula (1).SELECTED DRAWING: None

The present disclosure relates to the compound of an elastase inhibitor having the structure of Formula (I), the crystal form of the said inhibitor and its preparation method, the amorphous form of the said inhibitor and its preparation method and applications of these. The preparation method in present disclosure has advantages in simplicity, good repeatability, strong drug induction ability, high in-vivo exposure, long pharmacokinetic elimination half-life and high safety. The crystal form or amorphous form of present compound has beneficial effects such as high solubility and good stability. The preparation methods for the crystal form or amorphous form of the present compound are simple, easy to control and have a good reproducibility in the crystallization process.

The present disclosure relates to a process for preparing an elastase inhibitor compound. The process is: friendly to the environment, simple in operation, highly efficient, mild in reaction conditions, easy to control in operation, safe and reliable, low-cost and good in economic benefits. Meanwhile, the process provided in present disclosure offers a high reaction yield and a high purity for the obtained product, thus being suitable for industrial production.