46 results about "Endothelin Antagonists" patented technology

A compound of the formula (I):or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, a method of antagonizing endothelin, methods for the inhibition of bone metastases, methods for the prevention of growth of new metastases, methods for the inhibition of bone turnover, and methods for the prevention of bone loss in patients, including cancer patients, using an endothelin ET-A receptor antagonist.

Provided are devices and methods for treating or preventing smooth muscle cell proliferation caused by endothelin-mediated conditions. In particular, a medical device comprising a structure which is implantable within a body lumen and means on or within the structure for releasing an endothelin (A) receptor antagonist at a rate effective to inhibit smooth muscle cell proliferation. The device can be, for example, an expansible stent or a graft, and the means can include a matrix coating, wherein the endothelin (A) receptor antagonist can be dispersed within the coating or disposed directly on the structure and under the matrix. The methods and devices of this invention can be used to decrease the incidence of restenosis as well as other thromboembolic complications resulting from implantation of medical devices.

Aliquots of extracts from ethnopharmacological plants that have activity against the effects of sarafotoxins present in snake venom are isolated and identified as antagonists of endothelin using a fluorescence-based assay. A process is provided for the identification of an antagonist of an endothelin selected from the group consisting of endothelin-1, endothelin-2, endothelin-3 and mixtures thereof. The process comprises extraction of ethnopharmacological plants with a solvent followed by evaporation of the solvent to form an aliquot containing at least one component of the extract, optionally purifying and isolating one or more component by chromatography, and subjecting the aliquot or purified component to a competitive fluorescent binding assay using biotinylated endothelin-1, wherein the plants having activity against the effects of one or more sarafotoxins present in snake venom.

The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one nitric oxide enhancing group, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and / or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia. The cardiovascular compounds are angiotensin II antagonists, aldosterone antagonists, endothelin antagonists, hydralazine compounds, neutral endopeptidase inhibitors and renin inhibitors. The nitric oxide enhancing groups are nitroxides and / or heterocyclic nitric oxide donors.

A method for recognizing and evaluating the presence and function of GnRH receptors on tumor cells originating in the brain and / or nervous system and / or the meninges and / or reactive neuroglia cells and / or primitive neuroectodermal tumor cells and / or on Kaposi sarcoma is provided. Furthermore a method for reducing degenerate GnRH-positive tumor cells and / or for decreasing cellular replication of the above GnRH-positive tumor cells comprising administering to a cell or to a subject a replication decreasing amount of a GnRH agonist and / or GnRH antagonist and / or an erythropoietin agonist, and / or a thrombopoietin agonist, and / or a endothelin antagonist and / or a gonadotropin inhibiting hormone agonist is also provided. Furthermore, a diagnostic kit for detecting GnRH receptors on tumor cells according to the present methods is disclosed.

The invention relates to a composition for whitening and brightening skin and an application of the composition for whitening and brightening skin to cosmetics. The composition comprises the followingcomponents of a glabridin carrier, hydroxyethylpiperazine ethane sulfonic acid (HEPES), an endothelin antagonist and plant composite essence. The composition for whitening and brightening skin can effectively restrain tyrosinase activity, restrain melanocyte disintegration, eliminate free radicals, soften cutin, improve skin withstanding capacity and the like; a glabridin carrier technique and plant fresh and living ingredients coexist, powerful efficacy of whitening skin and lightening freckles of the endothelin antagonist is used for cooperation, in the presence of the HEPES, synergistic interaction is achieved, and excellent efficacy of whitening skin and brightening skin can be achieved.

The present invention relates, in general to treatment of pain comprising administering an alpha-2 adrenergic agonist and an endothelin antagonist, wherein administration of the agents acts as an analgesic and ameliorates pain in a subject.

A method for recognizing and evaluating the presence and function of GnRH receptors on tumor cells including those originating in the brain and / or nervous system and / or the meninges and / or reactive neuroglia cells and / or primitive neuroectodermal tumor cells and / or on Kaposi sarcoma is provided. Furthermore, a method for reducing degenerate GnRH-positive tumor cells and / or for decreasing cellular replication of the above GnRH-positive tumor cells comprising administering to a cell or to a subject a replication decreasing amount of a GnRH agonist and / or GnRH antagonist and / or an erythropoietin agonist, and / or a thrombopoietin agonist, and / or a endothelin antagonist and / or a gonadotropin inhibiting hormone agonist is also provided. Furthermore, a diagnostic kit for detecting GnRH receptors on tumor cells according to the present methods is disclosed.

The invention discloses skin whitening and freckle removing composition and an application thereof. The composition comprises forchlorfenuron and a whitening agent, wherein the whitening agent adoptsa tyrosinase activity inhibitor, a tyrosinase saccharification inhibitor, a tyrosinase decomposition agent, a melanocyte toxicity agent, a melanin transport blocking agent, a sunscreen agent, a reducing agent, a chemical stripping agent and an endothelin antagonist or a free radical scavenger. The composition can remove wrinkles and freckles, prevent water loss and keep skin moist, and has the functions of whitening the skin, removing freckles and wrinkles, preserving moisture and the like. Compared with the prior art, the composition is safe to use, simple and convenient to manufacture and suitable for industrial mass production.

The present invention relates, in general to treatment of pain comprising administering an alpha-2 adrenergic agonist and an endothelin antagonist, wherein administration of the agents acts as an analgesic and ameliorates pain in a subject.

The invention discloses a fat-soluble glabridin compound whitening agent and application of the agent in cosmetics. The compound whitening agent is prepared from the following active ingredients in byweight percent: 30-50 percent of glycyrrhiza glabra extract, 10-30 percent of tetrahydroxychalcone, 10-30 percent of ubiquinone and 10-30 percent of an endothelin antagonist. The compound whitening agent has main whitening action mechanisms of inhibiting the activity of tyrosinase, inhibiting the activity of DOPA chrome tautomerase and obstructing indole-5,6-quinone polymerization, so that melanogenesis can be obstructed, differentiation of melanophores can be reduced, and the aims of whitening skin, lightening spots and improving dark skin color can be achieved. The compound whitening agenthas a simple and practical formula and a good whitening and spot-lightening effect, is environmentally friendly and safe since natural products are adopted, is mild and nonirritant in use, and can overcome the defect in an existing whitening agent.

The invention discloses a blood vessel ice-crystal-free cryopreservation solution and a blood vessel preservation method. The blood vessel ice-crystal-free cryopreservation solution comprises 1.0-6.0mol / L of glycerol, 1.0-7.0 mol / L of formamide, 0.1-2.5 mol / L of polyvinylpyrrolidone and a component X; wherein the component X is one or more of a component A, a component B and a component C; wherein the component A is an NO donor, the component B is an endothelin inhibitor or an endothelin antagonist, and the component C is an anti-apoptotic agent. According to the preserving fluid disclosed bythe invention, the preserving effect on the vascular function is improved, especially for vascular smooth muscle cells and endothelial cells which are most easily subjected to cryopreservation injury; the vascular smooth muscle cell and the endothelial cell can be effectively protected, the function of effectively protecting the vascular smooth muscle cell and the endothelial cell is achieved; inaddition, the long-term patency rate after vascular transplantation is increased, and the success rate of clinical vascular transplantation is greatly guaranteed.

The invention relates to the fields of medicaments for treating blood pressure diseases and particularly relates to pyridine ring-substituted alpha-hydroxycarboxylic acid derivatives of a general formula I, preparation method thereof, medicinal compositions having the same and use thereof as an endothelin antagonist in the preparation of medicaments for treating hypertension and pulmonary hypertension, wherein groups are defined in the description.

The invention discloses a water-replenishing and moisturizing sunscreen, which is made of the following raw materials in parts by mass: 7-9 parts of glycerin stearate, 6-10 parts of shea butter, and 3-parts of polydimethylsiloxane 6 parts, 6‑8 parts of active raspberry polyphenols, 5‑7 parts of olive oil, 6‑9 parts of tetrandrine, 7‑11 parts of chitin, 5‑7 parts of menthol, 3‑5 parts of dihydroxyacetone, 8‑12 parts of polyoxyethylene sorbitan monostearate, 6‑10 parts of titanium dioxide, 4‑8 parts of aloe extract, 11‑14 parts of zinc oxide particles, 6‑7 parts of collagen, endothelin antagonist 4‑5 parts, 5‑7 parts of cinnamic acid, 6‑9 parts of isopropyl palmitate, 7‑9 parts of lanolin, and the rest is water. The invention has good sun protection effect, can lock the moisture on the skin, can moisturize and maintain the skin, and prevents aging, wrinkles and stains.

A method and solution for perioperatively inhibiting a variety of pain, inflammation, spasm and restenosis processes resulting from cardiovascular or general vascular therapeutic and diagnostic procedures. The solution preferably includes multiple pain and inflammation inhibitory agents and spasm inhibitory agents at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. Specific preferred embodiments of the solution of the present invention for use in cardiovascular and general vascular procedures also include anti-restenosis agents. The solution is introduced luminally to continuously irrigate an arterial site during an operative / interventional or diagnostic procedure for preemptive inhibition of pain and inflammation, vascular and non-vascular smooth muscle spasm, and restenosis while avoiding undesirable side effects associated with oral, intramuscular, subcutaneous or intravenous application of larger doses of the agents. One preferred solution to inhibit pain, inflammation, vasospasm and restenosis includes a serotonin2 antagonist, a cyclooxygenase inhibitor, an endothelin antagonist, an ATP-sensitive K<+> channel antagonist, a Ca<2+> channel antagonist, a nitric oxide donor, an anti-thrombin agent, a glycoprotein IIb / IIIa receptor blocker, a PKC inhibitor and a protein tyrosine kinase inhibitor.

The invention discloses a preparation method for a pearl shell whitening factor. The preparation method comprises the following steps: 1) crushing clamshells, and conducting screening to obtain small-particle clamshell powder; 2) mixing the clamshell powder with an aqueous weak acid solution, conducting stirring and decomposing, and separating out a solid, namely crude protein; 3) cleaning the crude protein with deionized water, mixing the cleaned crude protein with a buffer solution having a pH value of 6.0-7.5, treating the mixed solution for 20-40 minutes at an ultrahigh pressure of 100-200Mpa and a temperature of 40-80 DEG C, and subjecting the mixed solution and protease to mixing and reacting for 2-7 hours at a temperature of 40-60 DEG C under ultrasonic conditions; 4) carrying outstirring for 20-50 minutes at 85-100 DEG C for enzyme deactivation, and performing filter pressing through a filter membrane to obtain a sterile filtrate; 5) mixing a freeze-drying protective agent with the filtrate, conducting pre-freezing, and then performing freeze-drying in a vacuum freeze-drying bin for 12-20 hours so as to finally obtain freeze-dried powder with a moisture content of 2-5%. The invention also discloses application of the pearl shell whitening factor obtained by the method in preparation of an endothelin antagonist. The preparation method is simple in process, and the obtained pearl shell whitening factor is obvious in whitening effect.

The invention describes novel nitrosated and / or nitrosylated cardiovascular compounds or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and / or nitrosylated cardiovascular compound, and, optionally, at least one nitric oxide donor and / or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one cardiovascular compound of the invention, that is optionally nitrosated and / or nitrosylated, and, optionally, at least one nitric oxide donor compound and / or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; and (k) treating nephropathy. The nitrosated and / or nitrosylated cardiovascular compounds are preferably nitrosated and / or nitrosylated aldosterone antagonists, nitrosated and / or nitrosylated angiotensin II antagonists, nitrosated and / or nitrosylated calcium channel blockers, nitrosated and / or nitrosylated endothelin antagonists, nitrosated and / or nitrosylated hydralazine compounds, nitrosated and / or nitrosylated neutral endopeptidase inhibitors and nitrosated and / or nitrosylated renin inhibitors.

The invention discloses a skin care wet tissue additive solution with whitening and moistening functions and relates to the technical field of skin care wet tissue production. The skin care wet tissue additive solution is prepared from the following raw materials in percentage by mass: 25-35% of a raspberry fruit extract, 15-30% of a felwort extract, 10-20% of a lemon extract, 10-15% of a radix puerariae extract, 5-10% of a radix angelicae extract, 5-8% of arbutin, 5-7% of kojic acid, 3-6% of an endothelin antagonist, 3-6% of ascorbic acid magnesium phosphate, 3-5% of almond powder, 2.5-4.5% of pearl powder, 2-4% of pineapple ferment, 1.5-3% of papaya enzyme, 2-3.5% of hydrolate, 1.5-2.5% of linoleic acid and 0.3-0.5% of a preservative. The wet tissue additive solution prepared by using natural plant ingredients as the main raw materials is mild to the skin, has no irritation or side effect and can be well absorbed by the skin. Meanwhile, the wet tissue additive solution has the double functions of whitening and moistening and fully nourishes the skin.

The invention discloses a moisturizing sun cream. The moisturizing sun cream is prepared from the raw materials in parts by weight: 2-6 parts of dioxyacetone, 3-6 parts of polyoxyethylene 20 sorbitan monostearate, 4-12 parts of ultrafine titanium dioxide, 2-5 parts of stearic acid, 10-20 parts of aloe powder, 3-6 parts of endothelin antagonists, 4-8 parts of cinnamic acid, 10-20 parts of octyl salicylate, 15-25 parts of hydroxyethyl cellulose, 8-16 parts of isononyl isononanoate, 7-14 parts of cyclomethicone, 6-12 parts of cetyl dimethicone, 3-9 parts of glycerin monostearate, 2-4 parts of triethanolamine and 20-50 parts of deionized water. The invention provides the moisturizing sun cream which has the function of preventing ultraviolet rays and sunshine and also has the actions of skin moistening, moisturizing, skin injury repairing and skin moisture replenishing.

The invention provides a skin care spray with skin-whitening, spot-fading, and acne-removing functions. The skin care spray is mainly composed of following components in percentage by weight: 2 to 6%of vitamin C, 5 to 8% of pearl powder, 4 to 10% of plant extract, 10 to 30% of aloe, 3 to 10% of endothelin antagonist, 0.05 to 2% of hyaluronic acid, 0.5 to 1.5% of salicylic acid, 5 to 10% of lavender essential oil, 20 to 35% of deionized water, and 20 to 30% of skincare product auxiliary matrix. The skin care spray is mild and nonirritant, is suitable for various skins, has skin-whitening, spot-fading, and acne-removing functions, and makes skin become smooth, lustrous and elastic for a long term.

The invention provides a phenoxy phenylacetic acid endothelin antagonist shown in a formula (I) or a pharmaceutically acceptable salt thereof, and also provides a preparation method of the benzene oxygen phenylacetic acid endothelin antagonist or the pharmaceutically acceptable salt thereof, and an application thereof in preparation of a medicament for treating cardiovascular and cerebrovascular diseases, tumors, diabetes mellitus, nephrosis, asthma or hyperthyroidism.

The invention relates to a combination consisting of endothelin-antagonists and beta receptor blocking agents. Said combination is suitable for the treatment of diseases.

The invention provides methods of treating and / or preventing vascular diseases characterized by nitric oxide insufficiency by administering a therapeutically effective amount of at least one nitrosated angiotensin-converting enzyme inhibitor, nitrosated beta-adrenergic blocker, nitrosated cholesterol reducer, nitrosated calcium channel blocker, nitrosated endothelin antagonist, nitrosated angiotensin II receptor antagonist, nitrosated renin inhibitor, and optionally at least one compound used to treat cardiovascular diseases and / or at least one antioxidant, or a pharmaceutically acceptable salt thereof, and / or at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase may preferably be isosorbide dinitrate and / or isosorbide mononitrate. The vascular diseases characterized by nitric oxide insufficiency include a cardiovascular disease and a disease resulting from oxidative stress.