Method of phototherapy with antioxidant in case of chronic polypoid rhinosinusitis
SUBSTANCE: laser interstitial thermotherapy of a polipoid tissue in the nasal cavity is preliminarily performed with high-energy laser radiation. A day after the said procedure a 1% solution of emoxipine in a volume up to 1.0 ml is introduced into the polyp stroma. After that, the distal end of a flexible light guide of the light diode therapy apparatus "AFS/S", radiating visible blue radiation with a wavelength of 0.45 mcm, power of radiation of 120 mW, light spot diameter up to 2 cm, is brought to the polyp. After that, the 5-minute long illumination of the polyp is carried out, with the repetition of the entire course daily, for 7 days.
EFFECT: amplification of the emoxipine solution effect on the polypoid tissue of the nose, reduction of recovery terms, and recovery of nasal respiration.
2 tbl, 1 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to pharmaceutical industry, namely to selenium nanocomposites of natural hepatotrophic galactose-containing polysaccharide matrixes, representing water-soluble orange-red powders containing zerovalent selenium (Se0) nanoparticles sized 1-100 nm in the quantitative content of 0.5 - 60 wt %, possessing antioxidant activity for treating and preventing redox-related pathologies, particularly for treating toxic liver damage, to a method for producing and to an antioxidant agent containing the above nanocomposites.
EFFECT: invention provides the targeted agent delivery to liver cells, as well as higher agent accessibility and lower toxic action of selenium.
7 cl, 11 ex, 4 tbl
SUBSTANCE: method involves chelation of ferric (III) ions both in vivo, and in vitro with using 2-ethyl-6-methyl-3-hydroxypyridine succinate (Mexidol) to produce a stable stained complex having a high molecular weight and a complex (organic-inorganic) composition not identified among the known compounds.
EFFECT: high effectiveness of the chelation process and low toxicity of Mexidol that makes it promising for biomedical application.
4 dwg, 3 tbl, 3 ex
SUBSTANCE: invention relates to field of organic chemistry, namely to novel compound - 5(6)-nitro-1-(thietanyl-3)-2-ethoxybenzimidazole, inhibiting peroxidation of lipids.
EFFECT: novel compound, possessing useful biological properties, has been obtained.
2 cl, 1 dwg, 2 ex
SUBSTANCE: invention represents a mixture of two structural isomers: 2,6-di(1,7,7-trimethylbicyclo[2.2.1]hept-2-yl)-4-methylphenol and its diastereomers, and 2-(1,7,7-trimethylbicyclo[2.2.1]hept-2-yl)-6-(2,2,1-trimethylbicyclo[2.2.1]hept-5-yl)-4-methylphenol, and their diastereomers with the ratio of the first and second structural isomer isomers from 60:40 wt % to 95:5 wt %.
EFFECT: extension of the arsenal of means, possessing simultaneously haemorheological, anti-aggregate, anti-thrombogenic, retinoprotecting, endothelium-protecting, neuroprotecting, anti-arrhythmia and anti-ischemic activity, enhancing the cerebral blood flow.
4 dwg, 20 tbl, 6 ex
SUBSTANCE: what is presented is using Histochrom (same as echinochrome A or pentahydroxyethyl naphthoquinone) as an agent able to prevent pulmonary fibrosis developed under cytostatic agents. The invention can be used for the pharmacological prevention and correction of the pulmonary tissue disorders caused by administering the cytostatic agents.
EFFECT: preventing hypertrophy of interalveolar connective tissue in the lungs associated with administering bleomycin.
4 dwg, 1 tbl
SUBSTANCE: drops possessing antiviral and immunomodulatory effects characterised by the fact that they represent a 95% ethanol infusion of wild strawberry leaves and fruit specified in: red raspberry fruit, mountain ash fruit, bilberry fruit, blood-red hawthorn fruit, cinnamon rose fruit; 15-25 mg of the substance in 1 ml of the infusion.
EFFECT: drops possess pronounced antiviral and immunomodulatory effects.
15 tbl, 5 ex
SUBSTANCE: melanin having water-solubility of at least 80% and an paramagnetic centre concentration of at least 8·1017 spin/g is administered orally into the animals having been exposed to the radiation in a dose high enough to cause a spinal radiation injury; melanin is administered after dissolved in distilled water in the effective concentration. Melanin water is used as drinking water for the mice having been exposed to single and fractionated acute radiation, which is able to cause acute radiation disease. Melanin water is taken from the 1st to 30th day following the single radiation, or from the 1st day of the fractionated radiation to the 30th day on completion of the radiation.
EFFECT: higher survival rate, faster recovered haemopoiesis, body weight and orientation and motion activity.
7 tbl, 5 ex
SUBSTANCE: invention provides a composition having antioxidant properties in the form of a tablet, comprising an active agent based on nicotinamide adenine dinucleotide in reduced form (NADH) and inert filling agents, characterised by that the active ingredient is a complex which is a mixture of 10 wt % NADH with 63 wt % vegetable fats, 17 wt % beeswax and 10 wt % chlorophyll, and the inert filling agents are in the form of microcrystalline cellulose, Macrogol 6000, intense sweetener and a food flavourant.
EFFECT: invention provides a new tablet form of NADH.
SUBSTANCE: invention refers to a pharmaceutical composition with anti-ischemic and antioxidant activity in the form of tablets or capsules, and a method for preparing it. The composition contains 4-((3-oxo-3-ethoxypropanoyl)amino)benzoic acid in an amount of 40 to 80 wt %, an amino-containing compound and pharmaceutically acceptable excipients. The amino-containing compound is specified in a group of trometamol, methyl glucamine and L-lysine; 1 mole of 4-((3-oxo-3-ethoxypropanoyl)amino)benzoic acid is accounted for 0.05 to 0.25 mole of the above amino-containing compound. The composition also contains lactose, microcrystalline cellulose, calcium stearate and other pharmaceutically acceptable excipients. According to the method for preparing the composition, taking 4-((3-oxo-3-ethoxypropanoyl)amino)benzoic acid and amino-containing compound in molar ratio 1:0.05 to 1:0.25, pre-mixing, moisturising with a aqueous or alcohol solution of a binding agent, adding pharmaceutically acceptable excipients in such an amount to provide the content of 4-((3-oxo-3-ethoxypropanoyl)amino)benzoic acid from 40 to 80 wt %, granulating the mixture, drying and producing tablets or capsules according to the known technique.
EFFECT: implementing the above application.
6 cl, 7 tbl, 4 ex
SUBSTANCE: claimed is the application of 5(6)-nitro-1-(1,1-dioxothietanyl-3)-2-chlorobenzimidazole of formula (I) , earlier known as the means with broncholytic and spasmolytic activity, as the means, inhibiting peroxide oxidation of lipids.
EFFECT: realisation of the claimed purpose.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to pharmaceutical compositions, in particular to pharmaceutical composition, recovering visual pigment in case of insufficiency of endogenic 11-cis-retinal, which contains effective quantity of retinal derivatives and pharmaceutically acceptable carrier, where retinal derivative is converted into retinal, capable of forming functional complex opsin/retinal, where retinal derivative represents ester of 9-cis-retinyl of formula
ester of 11-cis-retinyl of formula or their combination, where A in each case stands for CH2OR and R represents ester-forming carboxylate radical of monocarboxylic acid C1-C10 or polycarboxylic acid, selected from oxalic acid, succinic acid, malic acid, glutaric acid, adipic acid, pimelic acid, suberic acid, azelaic acid, sebacic acid, citric acid, ketoglutaric acid, fumaric acid, malonic acid and oxalacetic acid, which is substituting group in ester, where 11-cis-retinal insufficiency is caused by mutation in genes, coding proteins RPE65 and LRAT.
EFFECT: invention relates to method of recovering photoreceptor function or attenuation of loss of photoreceptor function; and to application of said retinal derivative for drug manufacturing.
43 cl, 7 dwg, 5 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to novel N-containing heteroaryl derivatives of formula I or II or their pharmaceutically acceptable salts, which possess properties of JAK kinase, in particular JAK3, and can be applied for treating such diseases as asthma and chronic obstructive pulmonary disease (COPD). In formulae A represents carbon and B represents nitrogen or A represents nitrogen and B represents carbon; W represents CH or N; R1 and R2, independently represent hydrogen, C1-4alkyl, halogenC1-4alkyl, -CN; R3 represents C1-4alkyl, R9-C1-4alkyl, Cy1, where Cy1 is optionally substituted with one or several substituents R10; R4 represents hydrogen, C1-4alkyl, R12R7N-C0alkyl, where one of R7 and R12 represents hydrogen, and the other represents C1-4alkyl or group R13, which is selected from C1-5alkyl, Cy2-C0alkyl; R5 represents hydrogen; R6 represents hydrogen, C1-4alkyl, C1-4alkoxyC1-4alkyl, hydroxyC1-4alkyl, R12R7N-C1-4alkyl, R16CO-C0alkyl, Cy1; R7 represents hydrogen or C1-4alkyl; R9 represents halogen, -CN, -CONR7R12, -COR13, CO2R12, -OR12, -SO2R13, -SO2NR7R12, -NR7R12, -NR7COR12; R10 represents C1-4alkyl or R9-C0-4alkyl; R11 represents C1-4alkyl, halogen, -CN, -NR7R14; R12 represents hydrogen or R13; R13 represents C1-5alkyl, hydroxyC1-4alkyl, cyanoC1-4alkyl, Cy2-C0alkyl or R14R7N-C1-4alkyl; where Cy2 is optionally substituted with one or several constituents R11; R14 represents hydrogen or C1-4alkyl; R16 represents C1-4alkyl, halogenC1-4alkyl, C1-4alkoxyC1-4alkyl, hydroxyC1-4alkyl or cyanoC1-4alkyl; Cy1 represents monocyclic carbocyclic unsaturated or saturated ring, selected from C3-C6cycloalkyl, phenyl, or saturated monocyclic 4-6-membered heterocyclic ring, containing from 1 to 2 heteroatoms, selected from N and S, or partially unsaturated 10-membered bicyclic heterocyclic ring, containing oxygen atom as heteroatom, which can be substituted with group R11, where said ring is bound with the remaining part of molecule via any available C atom, and where one or several ring C or S atoms are optionally oxidised with formation of CO or SO2; and Cy2 represents monocyclic carbocyclic unsaturated ring, selected from C3-C6cycloalkyl, or aromatic monocyclic 4-6-membered heterocyclic ring, containing from 1 to 2 heteroatoms, selected from N and S, or unsaturated 10-membered bicyclic heterocyclic ring, containing oxygen atom as heteroatom, which can be substituted with group R11, where said ring is bound with the remaining part of molecule via any available atom C or N.
EFFECT: obtaining novel heteroaryl derivatives.
27 cl, 41 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: claimed invention relates to novel compounds of general formula (A), their stereoisomers or pharmaceutically acceptable salts, possessing ability to inhibit activity of isomerase, taking part in visual cycle. Compounds can be applied for treatment of ophthalmological disease or disorder, such as age-related macular degeneration or Stargardt's macular dystrophy. In general formula (A) Z represents-C(R9)(R10)-C(R1)(R2)-; R1 and R2 each, independently on each other, are selected from hydrogen, halogen, C1-C5alkyl, or -OR6; or R1 and R2 together from oxo; R3 and R4 each, independently on each other, are selected from hydrogen; R6 is selected from a) C5-C15alkyl, optionally substituted with hydroxy, C1-C8alkoxy; or b) C5-C10carbocyclylalkyl, in which carbocycle is 4-, 5-, 6-, 7- or 8-member non-aromatic carbocycle, optionally substituted with hydroxy, halogen or R6CO2-; R9 and R10 each, independently on each other, is selected from hydrogen, halogen, C1-C5alkyl, optionally substituted with hydroxy, or -OR19; or R9 and R10 form oxo; or optionally, R9 and R1 together form direct bond to provide double bond; or optionally, R9 and R1 together form direct bond, and R10 and R2 together form direct bond to provide triple bond; R11 and R12 each, independently on each other, is selected from hydrogen, -C(=O)R23 or -C(NH)NH2, R23 is selected from C1-C8alkyl; R6, R19 and R34 are independently on each other are hydrogen or C1-C8alkyl; each R33 is independently selected from halogen, hydroxyl, C1-C5carboalkoxy, C1-C8alkyl, optionally substituted with hydroxy; and n equals 0 or 1.
EFFECT: compounds inhibit degeneration of retinal cell, in particular neuronal cell, such as photoreceptor cell, in patient's retina.
45 cl, 11 dwg, 11 tbl, 206 ex
SUBSTANCE: method is used to treat a retinal hole with the use of an intravitreal dye. That is ensured by performing a microinvasive vitrectomy. A posterior hyaloid membrane (PHM) is isolated and excised. An irrigation fluid is shut off from the vitreal cavity. A silicone tipped cannula is used to drop a perfluorogranic compound (PFOC) directly on the through macular retinal hole. A PFOC drop diameter makes 1.5-2.0 diameters of the macular hole. Further, an internal limiting membrane (ILM) is coloured with the irrigation fluid shut off. After the membrane is coloured, the ILM is exfoliated by performing a maculorhexis. The PFOC drop is removed. The retina is plugged completely with gas air mixture.
EFFECT: conservation of neuroepithelium and retinal pigment epithelium cells within the macular hole ensured by such relation of the PFOC and macular hole diameters that in turn enables fixing the PFOC within the macular hole reliably.
5 cl, 2 ex
SUBSTANCE: group of inventions relates to medicine, namely to ophthalmology, and can be used for the reduction or inhibition of angiogenesis in an individual, suffering from an eye disease, or a condition, associated with angiogenesis. For this purposethe antagonist TSPAN12 is introduced to the individual. Also claimed is a method of treating the disease or a condition of eyes, associated with undesirable angiogenesis.
EFFECT: group of inventions provides reduction of angiogenesis of vessels of the outer plexiform layer (OPL), connected with the layer of nerve fibres (NFL) of the optic nerve.
30 cl, 13 dwg, 1 tbl, 7 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to the field of organic chemistry, namely to compounds of the general formula I , and its pharmaceutically acceptable salts, where R1, R2 and R3 represent hydrogen, D, E, G, J and L represent CH; n equals to an integer number 1 or 2; W represents oxygen; R4 represents C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkenyl, where the said C1-6alkyl is possibly substituted with one substituent, independently selected from a group, consisting of hydrogen, C1-4alkyl, C3-6cycloalkyl and C3-6cycloalkenyl; Y represents carbonyl; R5 represents C1-6alkyl, C1-6alkoxy or C3-4heteroaryl, which represents a heterocyclic aromatic ring, containing 1-2 heteroatoms, selected from nitrogen and oxygen. The invention also relates to a pharmaceutical composition based on a formula I compound, application of the formula I compound and a method of prevention, treatment of alleviation of a disease, associated with abnormal angiogenesis.
EFFECT: obtained are novel compounds useful in treatment of diseases associated with unregulated angiogenesis, such as cancer, as well as skin and eye diseases.
13 cl, 3 tbl, 11 ex
SUBSTANCE: pharmaceutical composition can additionally contain ethylenediaminotetraacetic acid, polyvinyl pyrrolidone, polyvinyl alcohol, a preserving agent specified in a group: Nipagin, Nipasol, benzoic acid, sodium benzoate, sorbic acid, benzalkonium chloride. As a body-forming base, the composition can contain distilled water, polyethylene oxide 400, polyethylene oxide 4000, polyethylene glycol, propylene glycol, a phosphate buffer, a borate buffer, an acetate-borate buffer depending on a dosage form.
EFFECT: high therapeutic effectiveness, prolonged corneal contact of the preparation which reduces the number of instillations, avoids a risk of side effects and provides good tolerance.
5 cl, 5 ex
SUBSTANCE: invention relates to formula compound or to its pharmaceutically acceptable salt, where R represents COOH or CH2OH. Invention also relates to pharmaceutical composition based on formula I, method of modulating CFTR activity in biological sample, based on application of formula I compound, method of treatment, based on application of formula I compound, set based on formula I compound.
EFFECT: obtained are novel derivatives of quinolin-4-one, useful as CFTR modulators.
18 cl, 1 tbl, 8 ex
SUBSTANCE: invention relates to form A of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl-)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, where said form A is characterised by peak at approximately 7.9 degree, peak at approximately 11.9 degree, peak at approximately 14.4 degree and peak at approximately 15.8 degree in powder X-ray. Invention also relates to pharmaceutical composition and set based on said form A, application of form A, method of CFTR modulation.
EFFECT: obtained is novel form of quinoline derivative, which is modulator of CFTR activity.
12 cl, 3 dwg, 2 tbl, 3 ex
SUBSTANCE: in general formula (I), R1 and R2 that have been taken jointly are a group of formula (II), R3 represents atom of hydrogen or F and R4 represents F; R1, R2, R3 and R4 are connected to 17, 16, 6 and 9 carbon atoms of steroid structure in position α or β; R represents (III) or (IV), and the rest values of radicals are given in the description.
EFFECT: improving use efficiency of compositions for curing of eye diseases, such as diabetic macular edema, diabetic retinopathy, macular degeneration, age-related macular degeneration and other macular and retina diseases.
11 cl, 4 dwg, 5 tbl, 11 ex
SUBSTANCE: device for the endoluminal treatment of a blood vessel comprises a flexible wave guide with a light guide tube. The wave guide has an elongated axis, a proximal end with a connector for optical connection to a laser light source, a distal end placed in the blood vessel and comprising an emitting surface for the emission of light from the light source sideways in relation to the elongated axis of the wave guide onto a surrounding vascular wall segment extending within the angular range. The device is provided with a secondary laser light source, a reflected light reception detector, a laser light transparent cone-shaped primary diffuser (1) with laser light deflection and a secondary diffuser (3) extending the laser light coverage area. The primary diffuser (1) is mounted at an optical output of the wave guide between the emitting surface of the wave guide and a sapphire safety cap (2). The secondary diffuser (3) is mounted between the safety cap (2) and the primary diffuser (1). The device also comprises a detachable sterilised protective sheath (4). The protective sheath (4) is made from heat-shrinkage polytetrafluoroethylene, configured as a tube with an ultrasound contrast insert and mounted on the wave guide over the safety cap (2).
EFFECT: using the invention is expected to improve the quality of blood vessel coagulation, eliminating light guide burning and reducing its friction on the blood vessel.
2 cl, 3 dwg