Specific therapeutic activity of chemical compounds or medicinal preparations (A61P)

A   Human necessities(312083)
A61P              Specific therapeutic activity of chemical compounds or medicinal preparations(25408)
A61P23 - Anaesthetics(281)
A61P33 - Antiparasitic agents(390)
A61P35 - Antineoplastic agents(3496)

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

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
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
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
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

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
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
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
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

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

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
ethod for treatment of alcoholic cardiomyopathy // 2642298
FIELD: medicine.SUBSTANCE: method includes introduction of metabolitotropic cardioprotector represented by (S)-2,6-diaminohexanoic acid 3-methyl-1,2,4-triazolyl-5-thioacetate in a dose of 100 mg/kg a day for 30 days. Invention application allows to increase therapeutic efficiency due to cardioprotective activity and low toxicity of (S)-2,6-diaminohexanoic acid 3-methyl-1,2,4-triazolyl-5-thioacetate.EFFECT: increased efficiency of treatment.2 tbl,1 ex

Hpv chimeric particle // 2642287
FIELD: biotechnology.SUBSTANCE: chimeric virus-like particle (VLP) of human papilloma virus (HPV), and method for its production and extraction, methods for prevention or treatment of HPV infection or cervical cancer, and for induction of an immune response in the patient, including the administration of proposed HPV VLP, as well as the application of the proposed HPV VLP in these methods and in production of pharmaceuticals to implement these methods, are proposed. The proposed chimeric HPV VLPS has a diameter of about 30 nm and contains a chimeric polypeptide HPV 16 L1/L2, which consists of a polypeptide HPV 16 L1, in which the peptide HPV 16 L2 from the amino acid residue 414 is inserted. The peptide contains from 13 to 26 amino acids. The amino acids of the inserted HPV 16 L2 peptide replace the corresponding amino acids of the HPV 16 L1 polypeptide. A method is also provided for the production of said HPV VLP in a plant in which successful assembly of small chimeric HPV VLPs, having a diameter of 30 nm, takes place.EFFECT: proposed group of inventions can be used in medicine for the prevention or treatment of HPV infection or in antitumor therapy for cervical cancer.28 cl, 32 dwg, 11 tbl, 3 ex
ethod for selection of perindopril dosage forpatients with ischemic heart disease on background of arterial hypertension // 2642284
FIELD: medicine.SUBSTANCE: polymorphism of the AGTR2 rs1403543 gene is determined. In case of detection of a homozygous version of GG, perindopril dose is 1.3 times lower than in individuals with allele version AA.EFFECT: increased therapy effectiveness and safety.4 tbl, 3 ex

Cells derived from cardial tissue // 2642282
FIELD: biotechnology.SUBSTANCE: invention relates to a method for improving the contractility of the heart, increasing the capillary density, or reducing myocardial hypertrophy in a patient with a damaged myocardium, which can be used in medicine. This method includes an administration of a purified cell pool, derived from cardial tissue of a human, where these cells do not express telomerase, heavy chain of myosin, CD31, CD45 and CD16 and express GATA4, Nkx2.5, CD105, CD90, CD59 and CD54.EFFECT: invention allows you to effectively improve the contractility of the heart, increase capillary density or reduce myocardial hypertrophy in patients after acute myocardial infarction.16 cl, 39 dwg, 30 tbl, 20 ex

Thrombin-binding molecules of antibodies and their application // 2642276
FIELD: pharmacology.SUBSTANCE: isolated antibody molecule, specifically binding to the thrombin exosite area 1, and an antigen-binding fragment of said antibody, are provided. The use of the antibody molecule in the manufacture of medicaments is considered. A pharmaceutical composition is described as well as a method for treating a thrombin-mediated condition.EFFECT: use in the treatment of diseases associated with thrombin.25 cl, 22 dwg, 4 tbl

Composition for hyperlipidemia treatment containing oxyntomodulin derivative // 2642267
FIELD: biotechnology.SUBSTANCE: oxyntomodulin derivative with SEQ ID NO: 24, 25 or 26 fused to the Fc region of the immunoglobulin via a non-peptidyl polymer that covalently binds the oxyntomodulin derivative and the immunoglobulin Fc region is obtained.EFFECT: invention allows to obtain a conjugate of a oxyntomodulin derivative with a high ability to activate the GLP-1 receptor and a glucagon receptor compared to natural oxyntomodulin and to effectively lower the levels of total cholesterol, low density cholesterol and triglycerides in blood that have been elevated due to a high fat diet and to raise high-density cholesterol levels and high-density cholesterol - low-density cholesterol ratios.13 cl, 10 dwg, 3 tbl, 6 ex

Recombinant chimerical ntbi polypeptide-immunogen with ability to induce neutralizing antibodies to type 1 human immunodeficiency virus and intended for use as component of vaccine against hiv-1 // 2642258
FIELD: medicine.SUBSTANCE: recombinant chimerical polypeptide-immunogen is proposed, including conservative T- and B-cell epitopes of HIV-1 and consecutive peptide fragments of p24, gp41, gp120 proteins, recognizable by wide-neutralizing 10e8, 2F5, VRC01 antibodies.EFFECT: improved HIV-specific immune response due to the inclusion of unique linear conformational epitopes imitators, recognizable by wide-neutralizing antibodies into the polypeptide-immunogen nTBI.6 dwg, 5 ex
Application of composition in medical products or drug manufacture for prevention and treatment of leukopenia caused by radiation and chemotherapy // 2642256
FIELD: pharmacology.SUBSTANCE: invention relates to application of a composition made from raw materials consisting of Radix Panacis Quinquefolii Ganoderma, or Radix Et Rhizoma Ginseng and fermented Cordyceps synesis powder and/or from Cordyceps, taken in a certain amount, in manufacture of medical products or drugs for prevention and treatment of radiation therapy or chemotherapy induced leukopenia in which the composition is obtained by raw materials mixing and extracting them with water and/or alcohol (versions).EFFECT: compositions described above are effective in the manufacture of medical products or drugs for prevention and treatment of radiotherapy or chemotherapy-induced leukopenia.25 cl, 36 tbl, 56 ex
ethod of conservative treatment of osteochondrosis // 2642253
FIELD: medicine.SUBSTANCE: method includes introducing vitamin B12. According to the invention, vitamin B12 is administered with 0.5% novocaine in the interstitial spaces to a depth up to the yellow ligament at a dose of 500 μg/ml.EFFECT: use of the invention makes it possible to accelerate and prolong analgesia by introducing into the depth to the yellow ligament.1 ex
ethod for endometritis treatment in cows // 2642251
FIELD: veterinary medicine.SUBSTANCE: ozonized autoblood as an immunomodulating and etiotropic agent is infused intramuscularly for four times in increasing-decreasing doses of 50, 75, 100, 75 ml at an interval of 48 hours, after obtaining from a vein, the blood is prepared by mixing in a syringe with 15 mg of sodium citrate and 10 mg of ozone in a ratio of 1:1 for 25 seconds, and Endometramag K is injected intramuscularly in an amount of 100.0 ml at an interval of 48 hours until recovery.EFFECT: increased effectiveness of therapeutic measures in case of endometritis and reduced period of the disease.2 tbl
Application of probiotic strain of enterococcus faecium l-3 microorganism for neurodegenerative diseases treatment // 2642246
FIELD: medicine.SUBSTANCE: probiotic strain of Enterococcus faecium L-3 is used. Therapy is carried out by short courses (up to a month) with interruptions under the control of the intestinal microbiota composition and the populations of circulating T cells. In case of exacerbations, traditional therapy with copaxone can be used (the use of a probiotic should be stopped for this period).EFFECT: method allows to increase the effectiveness of treatment by stimulating the production of anti-inflammatory cytokine.5 dwg
Compositions, synthesis and methods for application of phenylcycloalkylmethylamine derivatives // 2642074
FIELD: pharmacology.SUBSTANCE: invention relates to new phenylcycloalkylmethylamine derivatives of structural formula (I), or enantiomers or optically active isomers, or pharmaceutically acceptable salts having affinity for the binding of dopamine (DAT), the carrier of norepinephrine (NET) and the serotonin transporter (SERT). The compounds may find use in treatment and/or prevention of obesity, as well as depression 1. In the structural formula (I) ,n is 1; SP is a spacer, wherein the said spacer is C4 alkylene; X is O or S; R1 and R2 are independently H, C1-6 alkyl, C1-6 alkoxy, halogen; R3 is C1-6 alkyl; R4 is H or C1-6 alkyl; R5 is C1-6 alkyl; and * represents a carbon atom that can be optically active.EFFECT: improved composition properties.12 cl, 1 tbl, 86 ex
N-pyperonyl derivatives of daunorubicine, with antiprofliferative properties // 2642068
FIELD: pharmacology.SUBSTANCE: invention relates to the N-piperonyl derivatives of daunorubicine, which can be used in medicine, of general formula I where R=H, OCH3.EFFECT: new daunorubicine derivatives with antiproliferative properties and relatively low acute toxicity are proposed for cancer treatment, including non-small cell lung cancer, rhabdomyosarcoma, bowel carcinoma, breast adenocarcinoma.2 cl, 1 tbl, 2 ex
Spiro-fused piperidine derivatives for application as inhibitors of external medullar layer potassium channel // 2642066
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of formula I .EFFECT: new compounds of formula I are obtained which are inhibitors of the ROMK channel and which can be used in hypertension treatment.11 cl, 5 tbl, 85 ex
Derivatives of 1-(4,5-dihydroimidazole)-isochromane or 1-(4,5-dihydro)-isothiochromane, which are useful as agonists of alpha2 adrenoreceptors // 2642065
FIELD: chemistry.SUBSTANCE: invention relates to a compound of the formula or a pharmaceutically acceptable salt thereof, wherein X is O or S; R1 is hydroxyhalogen, (C1-C6)alkyl, halogen(C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, cyclo(C3-C6)alkyl, (C1-C6)alkoxy, halogen(C1-C6)alkoxy, hydroxy(C1-C6)alkyl, cyano, (R6)2N-(C=O)-, (C1-C6)alkyl-S-, or furanyl; R2 is H or (C1-C6)alkyl; R3 is H, (C1-C6)alkyl, halogen(C1-C6)alkyl or (C1-C6)alkoxy(C1-C6)alkyl; R4 is H or (C1-C2)alkyl; R5 is H, hydroxy, halogen, (C1-C6)alkyl or (C1-C6)alkoxy; R6 is H; or R1 and R2 form rings together with carbon atoms, to which they are attached, a fused 6- or 7-membered saturated or unsaturated carbocyclic ring. The invention also relates to a pharmaceutical composition based on a compound of formula (I).EFFECT: new isochromane or isothiochromane derivatives, useful as alpha2 adrenoreceptor agonists, have been obtained.10 cl, 1 tbl, 106 ex
 
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