46 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 neutrophilic granulocyte elastase inhibitor of which the active ingredient is a compound with a pentacyclic triterpene structure. The inhibitor can be used for preparing a medicament or health-care food for treating or preventing diseases with neutrophilic granulocyte elastase as an action way. The diseases with the neutrophilic granulocyte elastase as an action way include acute lung injury, acute respiratory distress syndrome, systemic inflammatory response syndrome and cystic fibrosis diseases. As the active ingredient of the neutrophilic granulocyte elastase inhibitor disclosed by the invention, the compound with the pentacyclic triterpene structure can be extracted and separated from a natural product or can be prepared from a natural product through chemical synthesis, and has the advantages of being wide in sources, safe and effective.

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 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.

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 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 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 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.

An object of the present invention is to provide hyaluronidase inhibitors, collagenase inhibitors, elastase inhibitors, MMP-1 production suppressors, and collagen synthesis promoters that contain as an active component one or more pigment compounds that are obtained as extracted from plants of the family Rosaceae, as well as agents for cutaneous application, skin cosmetics, and quasi-drugs that contain such pigment compounds. The present invention provides hyaluronidase inhibitors, collagenase inhibitors, elastase inhibitors, MMP-1 production suppressors, collagen synthesis promoters, agents for cutaneous application, skin cosmetics, and quasi-drugs that contain one or more compounds in a class of rosacyanins or one or more compounds in a class of rosadelphins as an active component.

Compositions and methods are provided for the treatment of IL-17-type inflammatory demyelinating diseases with inhibitors of granulocyte function, e.g. elastase inhibitors. Diseases of interest include multiple sclerosis, neuromyelitis optica, animal models of such diseases, etc. In some embodiments pharmaceutical formulations comprising an elastase inhibitor in an effective dose for treatment of IL-17-type inflammatory demyelinating disease and a pharmaceutically acceptable excipient are provided. Patients may be classified into subtypes prior to treatment, which subtypes are informative of the patient's need for therapy and responsiveness to a therapy of interest.

The invention belongs to the technical field of medicines, and particularly relates to application of a jasminum grandiflorum extract or active ingredients thereof in preparation of an elastase inhibitor, and the jasminum grandiflorum extract is an ethyl acetate layer extract of jasminum grandiflorum; and the effective ingredients of the jasminum jasminoides extract comprise oleuropein and hydroxytyrosol. The oleuropein, the hydroxytyrosol or the jasminum grandiflorum extract all have an effect of inhibiting activity of elastase, skin aging, emphysema and other diseases caused by overexpression of the elastase are avoided, and when the oleuropein and the hydroxytyrosol which are equal in molar concentration are mixed in an isovolumetric mode, an inhibiting effect on elastase is higher. Therefore, the oleuropein, hydroxytyrosol or jasminum grandiflorum extract provides a new choice for improving skin aging or treating chronic complications of emphysema.