Preparations for medical, dental, or toilet purposes (A61K)

A   Human necessities(312083)
A61K              Preparations for medical, dental, or toilet purposes (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms a61j0003000000; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles a61l)(51170)
A61K7 - (2074)
A61K37 - (206)
A61K43 - (6)

Liposomal suspensions stabiliser // 2642786
FIELD: pharmacology.SUBSTANCE: conjugate of the invention is a compound of formula (C6O4H9NH2)m(C6O4H9NHX)n, wherein the remainder of the polyethylene glycol derivative, which is a monomethoxy-PEG succinate acts as a substituent on the amino group X, the molecular weight of chitosan used to prepare the conjugate is 15 to 120,000 daltons, am and n are the number of units in the molecule, where m/n is 6 to 19. The proposed method involves preparation of a solution of N-hydroxysuccinimide ester of PEG-hemisuccinate in dimethylformamide or dimethylsulfoxide, mixing of the solution prepared with an acidic solution of chitosan with a molecular weight of 15-120 kDa, and adjustment of the resulting mixture to a pH of 7.5-8.0, followed by purification by dialysis against buffer solution.EFFECT: new substance effective for liposomal suspensions stabilization is disclosed, and an effective method for its preparation.3 cl, 3 dwg, 4 ex

Fluorine-9-methyl-β-carbolines // 2642785
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of the general formula (I) , where R1 is -F, and R2 is -H or -F, or R1 is -H, and R2 is -F; which can be used as a medicine for treatment of diseases and/or injuries of the inner ear.EFFECT: increased efficiency of compounds.10 cl, 30 dwg, 1 tbl, 9 ex
Forzicyaside sulfate and its derivatives, method for its production and its application // 2642784
FIELD: pharmacology.SUBSTANCE: invention relates to forzicyaside sulfate and its derivative represented by the following formula , wherein R is Na+, K+ or NH+, and a method for their preparation, as well as an antiviral drug based on them and its use.EFFECT: increased efficiency of agents.10 cl, 9 tbl, 2 dwg
New benzoazepine derivative and its medical application // 2642783
FIELD: pharmacology.SUBSTANCE: invention relates to a new benzoazepine derivative of formula (I) or a pharmacologically acceptable salt thereof, wherein R1 represents a hydroxyl group, a lower alkoxy group or , where A is absent or a lower alkylene group which may be substituted by a lower alkyl group; R6 represents a hydrogen atom or a lower alkyl group; R7 represents a hydrogen atom, a hydroxyl group, a five-membered aromatic heterocyclic group containing 3 heteroatoms selected from nitrogen and oxygen which may be substituted by a lower alkyl group, a five-membered non-aromatic heterocyclic group containing one nitrogen atom which may be substituted by an oxo group or a carbamoyl group , which may be substituted by a lower alkyl group; R2 represents a hydrogen atom or a lower alkyl group; R3 is a lower alkyl group which may be substituted by 1 to 3 fluorine atoms or a halogen atom; R4 represents a lower alkoxy group which may be substituted by 1 to 3 halogen atoms, a five-membered aromatic monocyclic heterocyclic group or a five-membered non-aromatic monocyclic heterocyclic group (provided that each of these heterocyclic groups contains one nitrogen atom, two nitrogen atoms or one nitrogen atom and one oxygen atom in the ring, and may contain a lower alkyl group); and R5 represents a hydrogen atom, a lower alkyl group or a halogen atom. The invention also relates to a pharmaceutical composition based on a compound of the formula and intermediates of the formulas and .EFFECT: new benzoazepine derivatives having V2 receptor agonist activity are obtained.14 cl, 12 tbl, 128 ex
Comt inhibitors // 2642779
FIELD: pharmacology.SUBSTANCE: invention relates to new compounds of the formula (I) and their pharmaceutically acceptable salts which have the properties of a catechol-O-methyltransferase (COMT) inhibitor. In the compound of the formula (I) , where R1 is hydrogen, methyl, Br, F or Cl; R2 is hydrogen, lower alkyl, Br, I, C3-6cycloalkyl, C(O)O-lower alkyl, C(O)NH-lower alkyl substituted by halogen, C(O)(morpholine) or is 3,4-dihydronaphthalen-2-yl optionally substituted by lower alkyl, 1,2,3,4-tetrahydronaphthalen-2-yl, 2,3-dihydrobenzofuran-6-yl, 1-methyl-2,3-dihydro-1H-indolin-5-yl, 1-methylindolin-5-yl, tetrahydropyran-4-yl, 3,6-dihydro-2H-pyran-4-yl, 2-isopropyl-1,2,3-tetrahydroisoquinolin-5-yl, 2,3-dihydro- dimethyl[1,4]dioxin-6-yl, benzo[1,3]-dioxol-5-yl, 1,2,3,4-tetrahydroisoquinolin-7-yl optionally substituted by lower alkyl, cyclohexenyl, morpholinyl, 4-methylpiperazinyl, naphthalen-1-yl, naphtalen-2-yl, or represents (CHR)n-phenyl optionally substituted by one to five substituents R4, where R4 is F, Cl, CN, CH2-CN, lower alkyl, hydroxy, lower alkyl, substituted hydroxy, lower alkoxy, (CH2)1.2-lower alkoxy, S-lower alkyl, (CH2)1.2-S-lower alkyl, -CH2)1.2-S (O)2-lower alkyl, -S(O)2-lower alkyl, -S(O)2-di-lower alkylamino, -S(O)2-piperidinyl, lower alkyl substituted by halogen, -N=N-phenyl, di-lower alkylamino, (CH2)1.2-di-lower alkylamino, (CH2)2-NH-lower alkyl, NHC(O)-lower alkyl, lower alkoxy substituted by halogen, CH(CH3) C(O)O-lower alkyl, O-phenyl, O-benzyl, phenyl, optionally substituted CF3, SF5, benzyl, C(O)-lower alkyl, C(O)-phenyl, C(O)-morpholinyl, C(O)-4-methylpiperazinyl, C(O)-di-oxothiomorpholinyl, C(O)-piperidinyl, optionally substituted by F, C(O)-NH-(CH2)2-morpholinyl, C(O)-NR-(CH2)2-NR2, C(O)-N-di-lower alkyl, CH2-O-(CH2)2-4-methylpiperazinyl, CH2-O-(CH2)2-di-alkylamino, CH2-O-(CH2)2-pyrrolidinyl, CH2-O-(CH2)2-morpholinyl, CH2-O-(CH2)2-piperidinyl optionally substituted by lower alkyl substituted by halogen or lower alkyl, (CH2)3,4-pyrrolidinyl, (CH2)2,3-di-lower alkylamino, morpholinyl, CH2-morpholinyl, CH2-piperazine substituted by lower alkyl, -S(O)2-piperazine substituted by lower alkyl, CH2-O-C(O)-piperazine substituted by lower alkyl, pyrazolyl or (CH2)1,2-lower alkoxy; R is hydrogen, lower alkyl or hydroxyl; n is 0, 1, 2, or 3; or R2 is C(O)-phenyl optionally substituted by lower alkyl; or is -O-phenyl optionally substituted by F; or is CH=CH-phenyl optionally substituted by lower alkyl; or is C≡C-phenyl; or R2 is a heteroaryl selected from the group consisting of pyrazolyl, thiazolyl, pyridinyl, pyrimidinyl, imidazolyl, isoxazolyl, isothiazolyl, thiophenyl, 1-thia-3,4-diazolyl, imidazo[1,2-a]pyridinyl, indazolyl, quinolinyl or isoquinolinyl, and the said groups are optionally substituted by R5, where R5 is halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, hydroxy, (CH2)1.2-lower alkoxy, CH2-di-lower alkylamino, di-lower alkylamino, morpholinyl, piperazinyl, pyrrolidin-1-yl, C(O)-piperidinyl, C(O)-4-methylpiperazinyl, phenyl optionally substituted by halogen, pyridinyl, S(O)2N(CH3)2, C(O)O-lower alkyl, NHC(O)-lower alkyl, or is C(O)-heteroaryl selected from pyridinyl and thiophenyl, where heteroaryl groups are optionally substituted by lower alkyl, n is 0, 1, 2 or 3; R3 is hydrogen, methyl, Br, F, Cl, CF3, nitro, amino, cyano, NHC(O)-phenyl, or is 1-methyl-1,2,3,6-tetrahydropyridinyl, or is pyridinyl optionally substituted by methyl or morpholinyl, or is phenyl optionally substituted by methyl , SO2CH3, CF3, CN, F or C(O)N (di-lower alkyl).EFFECT: compounds can be used to treat Parkinson's disease, depression, cognitive impairment and motor symptoms, resistant depression, cognitive impairment, mood and negative symptoms of schizophrenia.16 cl, 2 tbl, 256 ex
2-aminopyrasine derivatives as csf-1r kinase inhibitors // 2642777
FIELD: pharmacology.SUBSTANCE: invention relates to a compound that is an amino acid or ester of an amino acid of formula , or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against CSF-1R kinase. In formula (I), ring A is a phenyl group; R1 and R2 independently represent a hydrogen atom, a halogen atom or an unsubstituted C1-4 alkyl; n is 1; X is NH; V is -N=, W is -C(Z)=; Z represents a hydrogen atom, a fluorine atom, a chlorine atom or unsubstituted C1-3 alkyl; ring B is a 1,4-phenylene, 1,3-phenylene or pyridinyl group; [Linker] is a -(CH2)m-X1-(Alk1)x-Y1 group, where m is 0, 1, 2 or 3; x is 0 or 1; Alk1 is an unsubstituted C1-3 alkylene group; X1 and Y1 independently represent a bond, -O-, -S-, -NR7th-, -C(=O) - or -C(=O)NR5-, where R5 is a hydrogen atom or C1-4 alkyl and R7 is a hydrogen atom, unsubstituted C1-4 alkyl or -C(=O)CH3; R is a group of formula or , in which R8 is a -COOH group or an ester group of the formula -(C=O)OR14, where R14 is R15R16R17C-, where any R15 represents a hydrogen atom or C1-3alkyl-(Z1)a-[(C1-C3)alkyl]b-, where a and b are independently 0 or 1, Z1 is -O-, -S- or -NH-, R16 and R17 independently represent a hydrogen atom or C1-3 alkyl- or R15 and R16, taken together with the carbon atom to which they are attached, form a 3-7-membered cycloalkyl ring; and R17 represents a hydrogen atom; where (i) R9 and R10 are side chains of natural amino acids, (ii) one of R9 and R10 represents a hydrogen atom or unsubstituted C1-4 alkyl, and the other is an unsubstituted C1-6 alkyl group or C1-6 alkyl group substituted by a C1-4 alkoxy group, or (iii) R9 and R10, taken together with the carbon atom to which they are attached, form a saturated spiro-cyclobutyl ring; R11 represents a hydrogen atom or an unsubstituted C1-2alkyl group; ring D is a 5- to 7-membered saturated heterocyclyl group with at least one nitrogen atom in the ring. The invention also relates to a pharmaceutical composition, a method of treatment or prevention of diseases or disorders mediated by CSF-1R kinase, as well as application of the said compounds for preparation of a medicament useful for treatment of such diseases.EFFECT: increased application efficiency.18 cl, 59 ex
ethod for increase of organism resistance to combined toxic action of nanoparticles of copper, zinc and lead oxides // 2642674
FIELD: medicine.SUBSTANCE: method for reduction of the adverse effects of combined effects of copper (CuO), zinc (ZnO) and lead (PbO) oxides nanoparticles on organism in risk groups covering individuals exposed to such effects under production conditions. Method includes prescription of a complex of biologically active drugs: glutaminic acid, glycine, N-acetylcysteine, pectin enterosorbent, fish oil preparation rich in unesterified omega-3 fatty acids, Vitamins A, C, D3, E, selenium, iron and iodized preparations. This complex is taken by repeated courses 1-2 times a year for 4-6 weeks daily at doses providing daily intake of 300 mg of glycine, 600 mg of cysteine, 4 g of glutaminic acid, 25 ml of fish oil with 12-15% content of polyunsaturated omega-3 fatty acids, 4-5 grams of pectin, as well as selenium, iron, iodine and these vitamins in doses that provide the normal physiological needs of the organism.EFFECT: reduction of all three metals in the blood, improved elimination function of the liver and kidneys, reduced integral signs of chronic intoxication, including signs of neurotoxicity, and genotoxic combined action of copper, zinc and lead oxides nanoparticles on the body.6 tbl
Composition for increasing operability and physical durability // 2642673
FIELD: food industry; pharmaceutical industry.SUBSTANCE: invention relates to the pharmaceutical and food industries and is a composition for improving working capacity and physical endurance comprising vitamin A, vitamin E and succinic acid, characterized in that it further comprises dry guarana extract and a chocolate mass, the components in the composition being in a certain ratio, in mass %.EFFECT: invention provides good taste qualities, a convenient form for reception, and also provides for a short time increase in efficiency and physical endurance by taking a complex of active substances optimally selected and in an amount sufficient to achieve maximum effect.1 cl, 3 ex, 2 tbl

Inhibitor of hyaluronic acid decomposition including rosemary extract and retinol acetate // 2642672
FIELD: pharmacology.SUBSTANCE: hyaluronidase inhibitor includes rosemary extract and retinol acetate in the following ratio: 0.01 - 5 wt % parts of retinol acetate per 1 wt % part of rosemary extract. Means for external use on the skin to alleviate or prevent skin problems selected from the group consisting of skin aging, wrinkled skin, rough skin, dry and rough skin, acne and atopic dermatitis, including a hyaluronidase inhibitor. The cosmetic treatment method includes rosemary extract and retinol acetate application to the subject suffering from a decrease in the hyaluronic acid level, in the following proportion: 0.01-5 wt parts of retinol acetate per 1 wt % part of rosemary extract.EFFECT: agent has a synergistic activity of hyaluronidase inhibition.3 cl, 1 dwg
Packaged product of solid preparation containing 5-hydroxy-1h-imidazole-4-carboxamide, or its salt, or its hydrate // 2642670
FIELD: medicine.SUBSTANCE: invention relates to a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or its salt, or its hydrate and a medium regulating agent, as well as a method for solid preparation stabilizing. The packaged product of the present invention is characterized by the colour differences of the solid preparation being no more than 3, when evaluating the solid preparation surface before and after storage for 3 months under conditions of 40°C and relative humidity of 75%, or for four weeks under conditions of 60°C.EFFECT: invention provides a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or its salt, or its hydrate, with excellent stability of solid preparation during storage.6 cl, 1 tbl, 15 ex
ethod for treatment of recurrent vulvovaginal candidiasis // 2642666
FIELD: medicine.SUBSTANCE: immunomodulatory therapy is administered by local action on the cervico-vaginal area with a drug containing sodium aminodihydrophthalazinedione, represented by the rectal suppositories Galavit, by introduction into the cervico-vaginal zone in successive doses of 100 mg overnight in three steps: the first preparatory phase of recovery of functional metabolic activity of cervical secret neutrophilic granulocytes by stimulation of their microbicidal activity by daily administration of the said drug with a course of 5 doses, one dose per day; the second stage of normalization of the monocyte-macrophagal system in the cervico-vaginal zone by enhancing phagocytosis using this drug with a course of 5 doses at a single dose with 48 hours pauses between them; the third stage of formation of a stable immune response in the cervico-vaginal zone at the local level by introduction of this drug with a course of 10 doses at a single dose with 72 hours pauses, and administration of a systemic antimycotic, which is itraconazole administered orally at a dose of 200 mg 1 dose daily, is performed at the third stage, starting with the administration of the 15th dose of Galavit.EFFECT: normalization of the local immune status, with preservation of a full-fledged immune response in the long-term period, a stable immunity is provided, with a reduction in the number of relapses and a reduction in the duration of treatment.3 cl, 2 tbl, 2 ex

Polymeric protein microparticles // 2642664
FIELD: pharmacology.SUBSTANCE: microparticles containing a core of therapeutic protein and a top layer of biocompatible and biodegradable polymer, and methods for production and application of these microparticles are proposed. The prolonged release of the therapeutic protein from the microparticles into saline is demonstrated over an extended period of time.EFFECT: group of inventions allows to expand the arsenal of available pharmaceuticals.18 cl, 3 dwg, 7 tbl, 9 ex

Compositions of long-term action insulins // 2642662
FIELD: pharmacology.SUBSTANCE: group of inventions refers to an aqueous pharmaceutical composition containing 270-330 U/ml of glargine insulin [equimolar to 270-330 IU of human insulin], wherein the composition containing 300 U/ml of glargine insulin is excluded, for treatment of type I and II diabetes.EFFECT: application of these inventions allows to provide a basal insulin reserve within 24 hours after a subcutaneous injection of a single dose.16 cl, 9 dwg, 12 tbl, 18 ex
Tint dye for hair on foaming basis // 2642655
FIELD: cosmetology.SUBSTANCE: dye includes henna, or colourless henna, or basma, or their mixture in an amount of 0.1-55 wt % as a filler; propylene glycol, glycerine, or their mixture in an amonur of 0.1-30 wt % as a solvent; a mixture of DEA cocaminde, betaine cocoamidopropyl, sodium lauryl ether sulphate, sodium lauryl sarkosinate, sodium cocosulfate, ammonium lauryl sarkosinate in an amount of 0.1-10 wt % as surfactants; direct non-ionic nitro dyes, main direct cationic dyes, acidic direct anionic dyes or their mixture in an amount of 0.1-7 wt % as a dye; preservatives in an amount of 0.1-1 wt %; functional additives in an amount of 0.1-10 wt % and water in an amount up to 100 wt %.EFFECT: homogeneous and uniform colouring, shading of grey hair.3 cl, 6 ex

Concentrated therapeutic phospholipide compositions // 2642653
FIELD: pharmacology.SUBSTANCE: composition for treatment or prevention of cardiometabolic disorders, a metabolic syndrome, neurodegenerative disorders comprises a concentrated therapeutic phospholipid extract comprising compounds of Formula I wherein the total amount of the phospholipid compounds of Formula I from the extract is in a concentration of 60 wt % to 90 wt % of the total weight of the composition and the extract includes astaxanthin; to a capsule containing a concentrated therapeutic extract of krill oil that contains the phospholipid compounds of Formula I and the extract includes astaxanthin; to application of a composition that includes a concentrated therapeutic phospholipid extract containing compounds of Formula I for preparation of therapeutic compositions for serum triglyceride levels lowering; to application of a concentrated therapeutic phospholipid extract that contains compounds of Formula I for preparation of pharmaceutical compositions for treatment of cardiovascular diseases.EFFECT: increased mass percentage of phospholipids in the composition.20 cl, 35 dwg, 2 tbl, 7 ex

Cosmetic application of harungana madagascariensis extract // 2642652
FIELD: cosmetology.SUBSTANCE: invention relates to cosmetology and is application of a cosmetic composition containing at least an aqueous extract of Harungana madagascariensis leaves and one or more formulation agents or additives selected from emollients, dyes, film formers, surfactants, fragrances, preservatives, emulsifiers, oils, glycols, UV filters and vitamins, to enhance collagen synthesis.EFFECT: invention protects the skin from aging, promotes collagen synthesis and protects skin proteins against glycation.7 cl, 2 dwg
Combination of growth factors, cytokines, antibacterial/antiviral factors, stem cells factors, c3a/s4a complement proteins, immunoglobulins and chemotactic factors // 2642650
FIELD: pharmacology.SUBSTANCE: combination of cytokines, growth factors, chemotactic factors, stem cell factors, protein complement, immunoglobulins and antibacterial/antiviral factors, taken in a specific ratio and with a specific components composition for treatment of diseases, requiring reconstruction and regeneration of tissues. A pharmaceutical composition for treatment of diseases requiring restoration and regeneration of tissues.EFFECT: combination described above and the pharmaceutical composition can effectively regenerate and restore tissues.9 cl, 2 dwg, 11 tbl, 9 ex
ethod of treating inflammatory periodontal and oral mucosal diseases // 2642648
FIELD: medicine.SUBSTANCE: method of treating inflammatory periodontal and oral mucosal diseases include the elimination of acute and inflammatory processes in the acute stage, elimination of supragingival and subgingival dental deposits, surgical and orthopedic intervention if there is evidence; oral irrigation with ozonated mineral water, optionally hydromassage, irrigation, instillation and irrigation on disease sites of periodontal tissue and oral mucosa is held with 3.5-2.5% solution of bentonite in warmed up to 38-42° C ozonized mineral water for 15-30 minutes daily for 10-14 days and it is taken inside twice a day in small sips to 100-150 ml for 14-21 days. Mineral water is used as mineral water, having the following composition: total mineralization - 1.9-2.5 g/dm3, hydrogen carbonate ions - 740-950 mg/dm3, sulfate ions - 90-140 mg/dm3, chloride ions - 500-600 mg/dm3, calcium ions - no more than 15 mg/dm3; magnesium ions - no more than 10 mg/dm3; ions of sodium and potassium - 600-800 mg/dm3, strontium - no more than 25.00 mg/dm3, chromium - not more than 0.50 mg/dm3, zinc - no more than 5.00 mg/dm3, lead - no more than 0.10 mg/dm3, mercury - not more than 0.02 mg/dm3, selenium - not more than 0.05 mg/dm3, vanadium - no more than 0.40 mg/dm3, copper - not more than 1.00 mg/dm3, cadmium - not more than 0.01 mg/dm3, nitrates - not more than 50.00 mg/dm3, nitrites - not more than 2.00 mg/dm3, fluorine - not more than 10.00 mg/dm3, arsenic - no more than 1.50 mg/dm3, phenols - not more than 0.10 mg/dm3, uranium - not more than 1.80 mg/dm3, radium - no more than 5.2×10-7 mg/dm3, organic substances in terms of carbon - 5.00-30.00 mg/dm3. In particular, mineral water can be used from the source of the resort of Saki, the Republic of Crimea, mineral water from the source of the resort of Loutraki, Greece, mineral water from the resort's source in Evpatoria, the Republic of Crimea. Montmorillonite clay Kudrinsky deposit, the Republic of Crimea can be used as bentonite.EFFECT: effective treatment, reducing the risk of recurrence of inflammatory periodontal diseases and conditions after invasive interventions of the oral mucosa.5 cl, 3 ex

Disposable system for sterile obtaining of lipids and nucleic acids particles // 2642640
FIELD: pharmacology.SUBSTANCE: group of inventions discloses a system for sterile obtaining of lipids and nucleic acids nanoparticles and method for sterile obtaining of lipids and nucleic acids nanoparticles.EFFECT: group of inventions allows to obtain uniform lipid and nucleic acid particles by simple steps, reproducible and under aseptic conditions, and can be used to deliver this class of therapeutic molecules to target cells.23 cl, 13 tbl, 7 ex, 1 dwg
Processing of fish population by lufenuron // 2642637
FIELD: veterinary medicine.SUBSTANCE: drug is applied by oral administration of daily doses of 1 lufenuron to 30 mg/kg of fish biomass within a period of 3 to 14 days, while the total number of lufenuron used during the specified interval of time is from 7 up to 350 mg/kg of fish biomass.EFFECT: invention is suitable for treating salmon and provides continued effective protection against sea lice in the sea.10 cl, 6 tbl, 2 ex

Improved synergic antidiabetic compositions // 2642633
FIELD: pharmacology.SUBSTANCE: composition comprising inulin with a degree of polymerization (DP) below about 25, and a sulfonylurea and/or a derivative thereof, or a combination thereof, wherein the composition is synergic when used to treat or delay the onset of type 2 diabetes, and wherein the composition contains 5 mg to 50 g of inulin and 0.5 mg to 2000 mg of sulfonylurea and/or a derivative thereof, or a combination thereof. A method for treatment or delaying of the onset of type 2 diabetes. A method for treatment of hyperglycemia associated with type 2 diabetes. A method for prevention of development or alleviation of a side effect in a subject having type 2 diabetes treated with sulfonylurea and/or a derivative thereof or a combination thereof, wherein the side effect arises or is aggravated by treatment with sulfonylurea and/or a derivative thereof or a combination thereof. A method for prevention of development or alleviation of a pathological condition in a subject having type 2 diabetes or hyperglycemia associated with type 2 diabetes. A method for treatment or delaying of the onset of type 2 diabetes or treatment of hyperglycemia in a subject with type 2 diabetes.EFFECT: composition is effective for treatment or delaying of the onset of type 2 diabetes and acts synergistically.22 cl, 13 dwg, 13 tbl, 12 ex
Composition for prevention or treatment of chronic obstructive pulmonary diseases containing monoacethyldiglycerol compounds as active ingredient // 2642631
FIELD: pharmacology.SUBSTANCE: compounds of this invention reduce the expression level of CXCL-1, TNF-α or MIP-2, and thus do not have the side effects of the currently used therapeutic agents for chronic obstructive pulmonary disease treatment, are non-toxic and have an excellent therapeutic effect, so that they can be useful as a composition for prevention, treatment and reduction of chronic obstructive pulmonary diseaseseverity.EFFECT: prevention of chronic obstructive pulmonary disease containing monoacetyl diacylglycerin as an active ingredient.10 cl, 6 ex, 8 tbl

Boron-containing small molecules as anti-inflammatory agents // 2642628
FIELD: pharmacology.SUBSTANCE: invention relates to application of 5-(4-cyanophenoxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaborol, or its pharmaceutically acceptable salts for manufacture of a drug to treat or prevent diseases associated with inflammation, selected from acne and lupus in humans.EFFECT: application of this substance allows to treat skin diseases associated with an autoimmune component.3 dwg, 20 ex

Compositions and methods for inhibition of cellular adhesion or direction of diagnostic or therapeutic agents to rgd binding sites // 2642625
FIELD: pharmacology.SUBSTANCE: group of inventions concerns a peptide containing the glycine-arginine-glycine-cysteic acid-threonine-proline sequence, which inhibits cell adhesion to RGD binding sites. A composition, and a method for vitreoretinal disease treatment, and a method for stimulation of vitreolysis, dilation of the vitreous or vitreoretinal detachment are also described.EFFECT: group of inventions provides treatment of retinal diseases or simplified removal of the vitreous body during vitrectomy.10 cl, 6 ex, 5 dwg, 2 tbl
Pharmaceutical composition // 2642624
FIELD: pharmacology.SUBSTANCE: version 1 of the composition contains maleate indacaterol in an amount of 20-1200 μg in combination with fluticasone furoate in an amount of 0.5-800 μg or ciclesonide in an amount of 20-800 μg, lactose and optionally one or more pharmaceutically acceptable excipients. Version 2 of the composition contains maleate indacaterol in an amount of 20-1200 μg in combination with fluticasone furoate in an amount of 0.5-800 μg and tiotropium in an amount of 2.25-30 μg, lactose and optionally one or more pharmaceutically acceptable excipients. The composition is in a form suitable for administration once a day.EFFECT: composition according to the invention simplifies the mode of drug administration in the treatment of respiratory, inflammatory or obstructive airway diseases.2 cl, 49 ex
Stable compositions containing metal ion // 2642620
FIELD: chemistry.SUBSTANCE: proposed oral care composition includes: a) one or more pyrophosphates, wherein the total concentration of pyrophosphates in the composition is from 0.9 wt % up to 1.1 wt % in terms of the composition weight; b) one or more thickening gums, wherein the total concentration of thickening gums in the composition is from 1.25 wt % to 1.6 wt % in terms of the composition weight; and c) a source of zinc ions, which is a mixture of zinc oxide and zinc citrate, the ratio of the amount of pyrophosphate to the amount of thickening gums is less than 0.8. It is also proposed to use a combination of one or more pyrophosphates with one or more thickening gums to reduce or prevent the phase separation in the oral care composition under subclauses 1-15.EFFECT: use of the above pyrophosphate combination with thickening gums provides improved stability of the composition with respect to phase separation while maintaining an acceptable taste and mouth feel when using a composition containing a source of zinc ions.16 cl, 2 tbl
Complex preparation for treatment of acute and chronic otites of parasitary, bacterial and fungical origin in dogs, cats, fur-bearing animals and rabbits // 2642617
FIELD: veterinary science.SUBSTANCE: this invention relates to veterinary medicine and can be used in the treatment of acute and chronic otitis of parasitic, bacterial and fungal origin in dogs, cats, fur-bearing animals and rabbits. Complex preparation in the form of eardrops contains levofloxacin, clotrimazole, dexamethasone, moxidectin, and also targeted additives.EFFECT: invention provides 100 % therapeutic efficacy for parasitizing of ear mites and 98–100 % efficacy for otites of bacterial and/or fungal etiology.1 cl, 4 ex
Oral care composition // 2642614
FIELD: pharmacology.SUBSTANCE: oral care composition comprising an orally acceptable carrier, a fluoride ion representing amine fluoride and a buffer having pKa less than 7.0. The buffer contains an aqueous solution of an acid and a salt of this acid where the acid is selected from succinic acid, malic acid, and combinations thereof; pH of the composition for oral administration is 4.2-4.8; the composition has an acid number greater than 6; amine fluoride is olaflur (N-octadecyltrimethylenediamine-N,N,N'-tris(2-ethanol)dihydrofluoride). Methods for application of the above composition, namely the method for fluoride ions delivery to the mouth of a mammal, a method for reduction of cavities formation in the teeth of mammals and a method for teeth remineralization in a mammal. Composition contents comprising the buffer can counteract the buffering effect of saliva and maintain the pH of the composition at a slightly acidic level during composition application.EFFECT: improved absorption of fluoride from the composition in damages caused by caries, and increased remineralization potential compared to toothpastes corresponding to the current state of art in the field.14 cl, 3 tbl
Complexes based on chondroitin for cutaneous absorption // 2642612
FIELD: pharmacology.SUBSTANCE: invention is a transdermal delivery composition comprising non-covalent complexes between non-sulphated chondroitin having a molecular weight of 5 to 100 kDa determined by exclusion chromatography and active ingredients selected from diclofenac or its salts and ketorolac or its salts.EFFECT: invention provides passage through the stratum corneum of the skin, penetration into the epidermis, through the mucous membrane, as well as delayed release of the active components.4 cl, 11 tbl, 7 ex

Composition and method for treatment of eye disease assiciated with nucleic acids // 2642609
FIELD: medicine.SUBSTANCE: composition for treatment of dry eyes syndrome associated with nucleic acids, which develops as a result of nucleic acids formation/generation together with formation of eye mucoid films and/or biofilms, contains deoxyribonuclease I (DNAase I) and ophthalmologic auxiliary substance, and does not contain antibiotics. The composition is applied to the eye surface to remove the nucleic acid from the eye surface. Also, a method for treatment of the said dry eyes syndrome is provided, comprising administration of the said composition to the eye in an effective amount.EFFECT: application of the group of inventions improves treatment of the dry eyes syndrome associated with nucleic acids, which develops as a result of formation, generation of nucleic acids together with formation of eye mucoid films or biofilms.13 cl, 16 dwg, 7 ex

System delivery and regulated expression of paracrine genes for treatment of cardiovascular and other diseases // 2642605
FIELD: medicine.SUBSTANCE: group of inventions can be used to treat heart failure with congestive heart failure (CHF), diabetes or prediabetes in vivo in a patient in need thereof. To this end, a vector is administered to a subject comprising a nucleic acid encoding a paracrine polypeptide or a peptide selected from the group consisting of cardiotonic peptide, urocortin-2 (UCn-2), urocortin-1 (UCn-1), urocortin-3 (UCn-3), brain natriuretic peptide and prostacyclin synthase, wherein the said nucleic acid encoding a paracrine polypeptide or peptide is operably linked to a promoter, wherein the vector is an adeno-associated virus (AAV), and wherein the paracrine polypeptide or peptide is expressed in a cell.EFFECT: group of inventions provides treatment or improvement of CHF, diabetes or prediabetes in a patient.24 cl, 20 dwg, 3 tbl
eans for correction of psychoemotical status of organism based on astragalus herbs extract // 2642595
FIELD: pharmacology.SUBSTANCE: means for correction of the psychoemotional status of the organism, with antistress, antidepressant, anxiolytic and nootropic action, which is an aqueous or hydroalcoholic extract of Astragalus vulpinus Willd., containing flavonoids, ascorbic acid, saponins and tannins in a certain quantity.EFFECT: drug has a pronounced anti-stress, antidepressant, anxiolytic and nootropic effect, restores psychoemotional state of the organism.5 ex

Herbs-containing composition // 2642591
FIELD: pharmacology.SUBSTANCE: application of a combination of the following four components of plant origin: milkwort root; astragalus root; lovage root; and Angelica Sinensis root, in the manufacture of a medicament for treatment of a disease or disorder selected from the group consisting of stroke, neurological disorder or ischemia, or for neuroconditioning for prophylactic induction of cerebral tolerance to an ischemic, epileptic or other damaging event. A kit for application in a method for treatment of a disease or disorder selected from the group consisting of stroke, neurological disorder or ischemia, or for neuroconditioning for prophylactic induction of cerebral tolerance to an ischemic, epileptic or other damaging event. A composition for use in treatment of a disease or disorder selected from the group consisting of stroke, neurologic disorder, ischemia, or for neuroconditioning to ensure brain tolerance to an ischemic, epileptic or other damaging event.EFFECT: agents are effective for treatment of a disease or disorder selected from the group consisting of stroke, neurological disorder or ischemia, or for neuroconditioning for prophylactic induction of cerebral tolerance to an ischemic, epileptic or other damaging event.22 cl, 6 dwg, 3 ex
ultifunctional quinoline derivatives as antineurodegenerative agents // 2642466
FIELD: chemistry.SUBSTANCE: invention relates to a hydroxy-derived quinoline of the formula (I) or to a pharmaceutically acceptable salt thereof, (I) wherein R1 is hydrogen, (C1-C3)alkyl, (C1)alkylene(C3)cycloalkyl, (C1)haloalkyl or (C1)alkylene(C6)aryl; R2 is hydrogen or halogen; R3 is hydrogen, halogen, (C1)alkyl or (C1)alkoxy; R4 is hydrogen, halogen, (C1)alkyl, (C1)alkoxy or (C1)haloalkyl; R5 and R6 are hydrogen; and R7 is (C9-C15)alkanol, (C1)alkylenepiperazinyl(C1-C2)alkanol, (C1-C8)alkylenepiperazinyl (C1-C2)alkyl, (C10-C13)alkylene OCOCH3, (C1)alkylene(C1)alkylamino(C3)alkynyl, (C1)alkyleneamino(C8)alkanol or (C1)alkyleneamino(C6)alkanol(C1)alkylene(8-methoxyquinolin-2-yl); or (II), where R1, R2, R3, R4 and R6 each is as described in (I) above; R5 is (C11-C12)alkanol, and R7 is hydrogen. The invention also relates to a pharmaceutical composition based on the formula (I) compounds, a method for treatment of Alzheimer's disease, traumatic brain injury and/or damage to the spinal cord and a method for improvement of the ability of learning and/or memory in a patient suffering from Alzheimer's disease, based on the formula (I) compound.EFFECT: new hydroxy derivatives of quinoline have been obtained that have useful biological properties.13 cl, 13 dwg, 9 ex
Cyclopropane carboxylate ethers of purine analogues // 2642463
FIELD: pharmacology.SUBSTANCE: invention relates to new cyclopropane carboxylate esters of purine analogues of the formula (T) or pharmaceutically acceptable salts thereof, which can be used for treatment of herpesvirus infections. Herpesvirus infection is an infection caused by the herpes simplex virus, infection of herpes zoster, or cytomegalovirus infection. In the compound of the formula (T) each Rx and Rz is independently hydrogen or (C1-C6)alkyl, or Rx is hydrogen and Rz is (C1-C6)alkyl, or Rx is (C1-C6)alkyl and Rz is hydrogen; and Ry is (C1-C6)alkyl, halo (C1-C6)alkyl, C6aryl, haloC6aryl or (C4-C5)heteroaryl with one heteroatom selected from nitrogen and oxygen in the ring.EFFECT: increased efficiency of compounds application.7 cl, 5 dwg, 3 tbl, 16 ex
Obtaining of ioforminol - radio-opaque agent // 2642436
FIELD: chemistry.SUBSTANCE: invention refers to a method of obtaining a compound (1) used as a contrast agent for carrying out radiological studies, from the compound (3). In the compound (3), each X individually represents hydrogen, a formyl group (-CO-H) or an acetyl group (-CO-CH3). The method includes a base-activated in situ hydrolysis of the protecting groups (-OX) of the compound (3), comprising the following successive steps: i) suspending the compound (3) in water; ii) adjusting the pH of the solution obtained in step i) to a value between 10.0 and 12.5.EFFECT: method makes it possible to shorten the reaction time and increase the yield of the compound.6 cl, 1 ex

7-(4-methoxyphenyl)-5-phenyl-4,5-dihydro-[1,2,4]triazolo[1,5-a]pyrimidine as activator of glucokinase and inhibitor of dipeptidyl peptidase of type 4 and method of its production // 2642432
FIELD: chemistry.SUBSTANCE: invention relates to 7-(4-methoxyphenyl)-5-phenyl-4,5-dihydro-[1,2,4]triazolo [1,5-a]pyrimidine as an activator of glucokinase and an inhibitor of dipeptidyl peptidase of type 4: . The invention also relates to the method of its production.EFFECT: new compound is produced that can be used as an activator of glucokinase and an inhibitor of dipeptidyl peptidase of type 4.2 cl, 3 dwg, 3 ex
Amide derivatives as grp119 agonists // 2642429
FIELD: pharmacology.SUBSTANCE: invention relates to an amide derivative of the following formula 1, its stereoisomers or its pharmaceutically acceptable salts of formula 1, wherein X1, X2, X3, X4, X5, X6, X7 and X8 each independently is C or N; R1 is -F or -C1-3-perfluorinated alkyl; R2 and R3 each is independently selected from the group consisting of halogen, -C1-5-alkyl and C3-6-cycloalkyl, wherein -C1-5-alkyl and C3-6cycloalkyl independently of one another may be unsubstituted or substituted by halogen, -CN, -OC1-5-alkyl or-C1-5-alkyl, or R2 and R3 together with the carbon atom to which they are attached, can form C3-6-cycloalkyl, where C3-6cycloalkyl may be unsubstituted or substituted by halogen, -OC1-5-alkyl or -C1-5-alkyl; R4 and R5 each independently is H, halogen or -C1-5-alkyl; R6 and R7 each independently is H, halogen, -C1-5-alkyl or -CN; R8 means methyl; R9 means H, halogen or OH; and m is 1 or 2. The invention also relates to individual compounds and to a pharmaceutical composition.EFFECT: new compounds of formula 1 are obtained that have the properties of GPR119 agonists, which can be used in diabetes mellitus treatment.7 cl, 15 tbl
N-aryl-4-(5-nitrofuran-2-yl)-pyrimidine-5-amines with antibacterial activity and method for their obtaining // 2642428
FIELD: pharmacology.SUBSTANCE: invention relates to new N-aryl-4-(5-nitrofuran-2-yl)-pyrimidine-5-amines of general formula I , where a: R1=R2=R3=H; b: R2=CH3, R1=R3=H; c: R2= OCH3, R1=R3=H; d: R1=R2=R3=OCH3 and a method for their preparation, in which 5-bromo-4-(5-nitrofuran-2-yl)pyrimidine (6) is mixed with the corresponding arylamine taken in 1.5 times excess, palladium (II) acetate and 1,1'-bis (diphenylphosphino)ferracene taken in catalytic amounts and potassium phosphate taken in 2.5-fold excess, the resulting mixture is dissolved in degassed 1,4-dioxane and heated at 85°C with vigorous stirring for at least 15 hours, followed by solvent distillation on a rotary evaporator under reduced pressure, and the resulting residue is subjected to chromatographic separation on a silica gel column with a ratio of ethyl acetate: hexane components of 1:3 in the eluent.EFFECT: highly effective method is proposed for the preparation of a compound that has a broad spectrum of antibacterial activity against coccal infections caused by gonococci or staphylococcus aureus, as well as purulent inflammatory infectious diseases of skin and mucous membranes caused by staphylococci and streptococci.2 cl, 1 tbl, 4 ex
1-ethyl-6-fluoro-4-oxo-7-(8-ethoxy-2-oxo-2h-chromen-3-yl)-1,4-dihydroquinoline-3-carboxylic acid with anti-tubercular activity // 2642426
FIELD: pharmacology.SUBSTANCE: invention relates to a fluoroquinolone carboxylic acid derivative, namely 1-ethyl-6-fluoro-4-oxo-7-(8-ethoxy-2-oxo-2H-chromen-3-yl)-1,4-dihydroquinoline-3 carboxylic acid of formula .EFFECT: high antitubercular activity, including that with respect to strains of mycobacteria with multiple drug resistance.2 tbl, 1 ex

Probiotic strains for treatment and/or prevention of diarrhea // 2642320
FIELD: biotechnology.SUBSTANCE: method for selection of a probiotic Bacillus strain, which includes assessment of the impact of the test strain on CFTR protein expression or NHE3 protein expression; Bacillus subtilis probiotic strain reducing CFTR protein expression and/or increasing NHE3 protein expression, deposited in the CNCM under accession number I-2745; cells obtained by cultivation of probiotic Bacillus strain, and a composition containing the effective number of cells for use in treatment and/or prevention of diarrhea.EFFECT: regulation of water absorption in the colon in the treatment and/or prevention of diarrhea.21 cl, 6 dwg, 2 ex
ethod for production of vaccine against brucellosis of small cattle // 2642316
FIELD: biotechnology.SUBSTANCE: method for production of vaccine against the brucellosis of small cattle provides seeding and growing strain of Brucella melitensis Rev-1 on a nutritional medium, containing pancreatic digest of casein of a high decomposition degree, yeast extract, sodium chloride, glucose, glycerol, and agar-agar in the specified component ratio within 72 hours at 37°C. The grown vaccine culture is washed from the surface of the agar by a drying medium and brought to a concentration of 80-140 billion m.c. per 1 ml. It is checked for purity and dissociation, packed in ampoules and subjected to freeze-drying.EFFECT: increase in the yield of Brucella melitensis Rev-1 strain in the S-form.1 tbl, 1 ex
ethod for prevention and treatment of dangerous neuroviral infections // 2642312
FIELD: medicine.SUBSTANCE: for treatment of dangerous neuroviral infections, mice are injected with Moliksan® in a single dose of 20.0 mg/kg of body weight immediately after infection and after 24, 48, 72 hours.EFFECT: increased effectiveness of combating diseases caused by pathogens of dangerous neuroviral infections.6 tbl

Fusion serpine polypeptides and methods for their application // 2642310
FIELD: biotechnology.SUBSTANCE: invention relates to the field of fusion proteins for serine proteases inhibition, and can be used in medicine. Fusion proteins having at least one human alpha-1 antitrypsin (AAT) polypeptide operably linked to an immunoglobulin Fc polypeptide having an amino acid sequence that is at least 98% identical to the amino acid sequence of SEQ ID NO:6 are obtained.EFFECT: invention allows to obtain a fusion polypeptide capable of effectively inhibiting the activity of serine proteases and thereby alleviating the symptoms of diseases or disorders associated with overexpression or serine protease activity in a subject in need thereof.18 cl, 4 dwg, 4 ex
Application of phototrophic bacteria rhodobacter capsulatus pg lipopolisaccharide as factor affecting differentiation activity of 1alfa,25-dihydroxyvitamin d3 // 2642309
FIELD: biotechnology.SUBSTANCE: application of physiological lipopolysaccharide produced by the strain of the phototrophic bacterium Rhodobacter capsulatus VKM IBPM RAS B-2381D as a non-toxic factor enhancing the differentiating activity of 1α,25-dihydroxyvitamin D3 when monocytic-like cells are differentiated into monocytes, is proposed.EFFECT: invention can be used to further differentiate promonocytes and monocytes in clinical and experimental medicine and in development of drugs, in particular for oncology.2 dwg, 1 tbl

Cancer treatment using targeted antibodies in vivo // 2642305
FIELD: biotechnology.SUBSTANCE: antibody binding to claudine 6 (CLDN6) and inhibiting tumor growth in vivo is claimed. The antibody can be used as part of a pharmaceutical composition, in a method for treatment of tumor related to cells expressing CLDN6. The invention also relates to hybridomas producing antibodies to CLDN6 deposited under the accession numbers DSM ACC3059 (GT512muMAB 36A), DSM ACC3058 (GT512muMAB 27A), DSM ACC3057 (GT512muMAB 5F2D2).EFFECT: invention effectively inhibits the growth of CLDN6-positive germ cell tumors, improves survival and prolongs life of patients with tumors.17 cl, 18 dwg, 5 ex
Combined administration of gdf traps and erythropoetin receptor activators for increasing content of erythrocytes // 2642302
FIELD: biotechnology.SUBSTANCE: method of treatment comprises of administration to the patient of an isolated polypeptide including the amino acid sequence of SEQ ID NO: 28.EFFECT: invention makes it possible to effectively increase the contents of erythrocytes in patients.17 cl, 22 dwg, 19 ex
Probiotic bacterial strain for obtaining nutrient composition improving sleep nature // 2642301
FIELD: biotechnology.SUBSTANCE: invention relates to application of a probiotic bacterial strain Lactobacillus reuteri DSM 17938 and/or Bifidobacterium longum ATCC BAA-999 in the manufacture of a nutritional composition for a subject. At that, the REM (REM+NREM) % ratio decreases by at least 8% compared to the subject that did not take such a nutritional composition, where REM is active sleep duration (minutes), and NREM is slow sleep duration (minutes).EFFECT: invention provides normalization of the sleep nature and improves the quality of sleep.12 cl, 2 dwg, 6 tbl, 4 ex

Immunotherapeutic compositions on the basis of yeast-muc1 and methods of their use // 2642300
FIELD: biotechnology.SUBSTANCE: fusion protein is produced which contains the MUC1 antigen having an amino acid sequence that is at least 85% identical to the sequence of SEQ ID NO: 25 or at least 95% identical to the positions 92-566 of the sequence of SEQ ID NO: 25, and where MUC1 antigen contains 2, 3, 4, 5, 6, 7, 8, 9, 10 or 11 of the following amino acids L184, Y232, L233, V240, V241, L242, Y483, V497, L335, F536 and Y551.EFFECT: invention allows to effectively treat Mucin-1-expressing carcinomas, and also to prevent their metastatic progression.14 cl, 3 dwg, 5 tbl, 10 ex

P53 peptidomimetic macrocycles // 2642299
FIELD: biotechnology.SUBSTANCE: stable cross-linked p53 peptidomimetic macrocycle, a method for its preparation and its use are proposed. The p53 peptidomimetic macrocycle has a structure represented in the formula, and interferes with binding of p53 to MDM2 and/or p53 to MDMX. The P53 peptidomimetic macrocycle can be used to prepare pharmaceutical compositions for treatment of cancer characterized by undesirably low or low p53 activity and/or for the treatment of cancer characterized by undesirably high levels of MDM2 or MDMX activity.EFFECT: proposed cross-linked p53 macrocycle has cell permeability that is at least twice as high as that of the corresponding macrocycle without cross-links.50 cl, 7 dwg, 9 tbl, 22 ex
 
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