Having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole (A61K31/41)

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
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
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
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
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
4-amino-3-methoxymethyl-5-phenyl-1h-pyrazole // 2642060
FIELD: pharmacology.SUBSTANCE: invention relates to preparation of new 4-amino-3-methoxymethyl-5-phenyl-1H-pyrazole previously not described. 4-amino-3-methylamide-5-phenyl-1H-pyrazole that has the following equation, derived from cycloaromatization of isonitrosodiketone and restoration of a new, not previously described intermediate - 4-nitroso-3-methylamide-5-phenyl-1H-pyrazole. The resulting target compound shows high antibacterial activity against E. coli (Escherichia coli strain ATCC 25822, sensitive to antibiotics) that allows its use in pharmacology to create antibacterial drugs. .EFFECT: increased efficiency of compounds application.2 ex
Polycyclic compounds and methods for their use // 2641648
FIELD: pharmacology.SUBSTANCE: invention relates to a compound having the formula or a pharmaceutically acceptable salt or stereoisomer thereof. In the formula (IVa): (i) R1 and R3 together with the atoms to which they are attached form an optionally substituted 3-20 membered heterocyclyl and R4 is hydrogen; or (ii) R3 and R4 together form a double bond and together with R1 and the atoms to which they are attached form an optionally substituted 5-20 membered heteroaryl; R2 is hydrogen, C1-6alkyl or absent; R5 is hydrogen; R6 and R7 are hydrogen; m is 0; n is 1; and wherein heterocyclyl or heteroaryl may be substituted by one or more substituents selected from C1-6alkyl. And heterocyclyl is a monocyclic or polycyclic ring system, which contains at least one non-aromatic ring containing one or more heteroatoms, selected from N, and the rest of the ring atoms are carbon atoms, heteroaryl is a monocyclic or polycyclic ring system, which contains at least one aromatic ring containing one or more heteroatoms, independently selected from S and N. A pharmaceutical composition and a method for neurological disorder treatment are also proposed.EFFECT: compound of the formula is used to treat neurological disorders.31 cl, 2 tbl
Agent for pyoinflammatory processes in soft tissues and mucous membranes // 2641095
FIELD: pharmacology.SUBSTANCE: invention is an agent for treatment of pyoinflammatory processes in soft tissues and mucous membranes in the form of a film that contains benzalkonium chloride, metronidazole, lidocaine hydrochloride, dimethyl sulfoxide, glycerol, sodium salt of carboxymethylcellulose and 5% solution of aminocaproic acid, with components in the agent being in a specific ratio of mass fractions.EFFECT: creation of an effective agent in the form of a film possessing antimicrobial, sorption, analgesic, wound healing and haemostatic action.4 tbl

eans and methods for cancer treatment and/or prevention depending on natural ahr ligand // 2640913
FIELD: medicine.SUBSTANCE: group relates to the treatment and/or prevention of cancer, dependent on the natural AHR ligand. To this end, a therapeutically effective amount of an arylhydrocarbon receptor (AHR) inhibitor is administered.EFFECT: possibility of effective treatment or prevention of a brain tumour, the pathogenesis of which is justified by unbalanced production of kynurenin.15 cl, 24 dwg, 4 ex

Combination treatment of cancer // 2640485
FIELD: pharmacology.SUBSTANCE: proposed: a combination for application as a drug for cancer treatment, containing: (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363) or a salt thereof with an androgen receptor signal modulator selected from 4-{3-[4-cyano-3-(trifluoromethyl)-phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl}-2-fluoro-N-methylbenzamide (MDV-3100) and N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)-sulfonyl]-2-hydroxy-2-methylpropanamide (bicalutamide) or a salt thereof, a set of these components for application in cancer treatment (versions).EFFECT: greater inhibition of tumour growth by combining the said compound against monotherapy of castration-resistant prostate cancer, the combination showed good tolerability.9 cl, 3 dwg, 1 tbl
Supramolecular complex of triclabendazole for treatment of animals in case of fascioliasis // 2640482
FIELD: veterinary medicine.SUBSTANCE: method comprises enteral administration of a supramolecular complex of triclabendazole and arabinogalactan in a ratio of 1:10 in the form of a powder of 0.1 to 10 microns in size, where the animals are received the complex in the form of an aqueous solution or in a dry mixture with food at a dose of 1-2 mg/kg.EFFECT: increased anthelmintic efficacy.4 ex, 4 tbl

Cystathionine-g-lyase (cse) inhibitors // 2640418
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the Formula (I) or their pharmaceutically acceptable salts inhibiting the activity of cystathionine-gamma-lyase (CSE). In Formula (I) A is or -CONHSO2R4, where R4 is independently unsubstituted alkyl or unsubstituted aryl; X is CR1 or N; R1 is H; each R2 and R3 is H. The invention also relates to a pharmaceutical composition comprising the said compounds and a method for treatment or prevention of various diseases associated with CSE activity.EFFECT: increased efficiency of the composition and treatment method.13 cl, 11 dwg, 2 tbl, 17 ex
Bicyclic compound // 2640416
FIELD: pharmacology.SUBSTANCE: in the general formula (1) (1), A is an unbranched C1-C3 alkylene group, wherein one methylene group is optionally substituted with O or S; n is an integer from 3 to 5; each of X1 and X2 is independently CH or N; each of W1 and W2 is independently a carboxyl group or W1 is a carboxyl group and W2 is a tetrazolyl group; V is a linear or branched C1-C8 alkylene group in which one methylene group is optionally substituted by O or S; R is a group selected from the following , , where R1, R2, R3, R4 and R5 is a hydrogen atom, a halogen atom, a C1-C6 alkyl group which may have a substituent group, a C1-C6 alkoxy group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkoxy group, a halogen C1-C4 alkyl group, a halogen C1-C4 vinyl group which may have a substituent group, an ethynyl group which may have a substituent group, a phenyl group which may have a substituent group on the aromatic ring, a phenoxy group which may have a substituent group on the aromatic ring, a benzyl group, which may have a substituent group on the benzene ring, a phenethyl group which may have a substituent group on the benzene ring, a benzyloxy group which may have a substituent group on the benzene ring, a benzylsulfanyl group which may have a substituent group on the benzene ring, a benzylamino group which may have a substituent group on the benzene ring, a phenyloxymethyl group which may have a substituent group on the benzene ring, a phenylsulfanylmethyl group which may contain a substituent group on the benzene ring, or a phenylaminomethyl group which may have a substituent group on the benzene ring, wherein the substituent group is indicated in the claims, m is an integer of 1 or 2 and each of Y1 and Y2 independently represents methylene, O or S, provided that they both do not represent S.EFFECT: compounds can be used to prevent or treat disorders associated with soluble guanylate cyclase, such as hypertension, pulmonary hypertension, heart failure, endothelial dysfunction, atherosclerosis, peripheral vascular disease, angina pectoris, thrombosis, myocardial infarction, erectile dysfunction or impaired renal function.9 cl, 41 tbl, 213 ex

Composition inhibiting telomerase // 2639819
FIELD: chemistry.SUBSTANCE: composition includes a block-copolymer of polyoxyethylene and polyoxypropylene, as well as a coordination compound of the imidizole-4-one derivative inhibiting telomerase, of the general formula .Herewith the coordination compound of the imidazol-4-one derivative is contained in an amount of 5 to 60 wt %, the block-copolymer is the rest.EFFECT: invention provides a greater effect of telomerase inhibition by increasing the solubility of coordination compounds of the imidazol-4-one derivatives.9 cl, 3 dwg, 2 tbl, 1 ex

Pharmaceutical composition containing biotin and method for its production // 2639488
FIELD: pharmacology.SUBSTANCE: group of inventions refers to pharmaceutical compositions for polyneuropathy prevention and treatment as a solid dosage form with extended release, comprising Biotin - 40-60 wt % as an active agent, as well as Methocel K100 LV - 14-21 wt %, Methocel K4M - 5-10 wt %, microcrystalline cellulose (MCC) - 7-18 wt %, copovidone - 1.5-3 wt %, colloidal silicon dioxide - 0.4-1 wt % and a pharmaceutically acceptable stearic acid salt - 0.6-1 wt %, as well as to a method for its production, according to which Biotin, Methocel K4M, Methocel K100 LV, MCC and copovidone are sieved and mixed until homogeneous, stearic acid salt, colloidal silicon dioxide are mixed, the mixture is compacted by rolling, colloidal silicon dioxide is added and mixed together with pre-compacted grains, followed by addition of stearic acid salt, stirring and formation a solid dosage form.EFFECT: creation of a new medicinal composition with high technological properties, high stability and reproducible kinetics of active agent release.9 cl, 8 ex, 5 tbl, 1 dwg
Oxothioimidazoline derivatives, methods for their production and application in medicine as androgen receptor inhibitors // 2639145
FIELD: pharmacology.SUBSTANCE: invention relates to an oxothioimidazoline derivative of the formula or to its mesomer, racemate, enantiomer, diastereomer, or a mixture thereof, wherein A is -CR' or N; R' is hydrogen or halogen; Z1 and Z2 each independently represents methyl; R1 and R2 each is independently selected from the group consisting of S or O; R3 is selected from the group consisting of C1-C3-alkyl, heterocyclyl selected from tetrahydrofuran, tetrahydropyran, piperidine, dioxo-tetrahydrothiopyran, azetidine, pyrrolidine, oxetane; C6-aryl and -S(O)mR6; when R3 is selected from heterocyclyl selected from tetrahydrofuran, tetrahydropyran, piperidine, dioxo-tetrahydrothiopyran, azetidine, pyrrolidine, oxetane; or C6-aryl, each of the heterocyclyl and aryl is optionally substituted by one or more groups selected from the group consisting of C1-alkyl, -OR6, -C(O)NR7R8, -S (O)mR6 and -C(O)R6; when R3 is C1-C3alkyl, alkyl is substituted by one or more groups selected from the group consisting of halogen, cyano, amino, C3-cycloalkyl, tetrahydrofuran, -OR6, -C(O)NR7R8, -S(O)mR6 and -C(O)OR6, wherein the cycloalkyl is optionally substituted by one group selected from cyano, amino, -OR6, -C(O)NR7R8 and -C(O)OR6; R4 and R5 are each independently selected from the group consisting of cyano, C1-alkyl, halogen and -CF3; R6 is hydrogen, C1-alkyl or -CF3; R7 and R8 are each independently selected from the group consisting of hydrogen and C1-alkyl, and m is 2. The invention also relates to intermediates, a process for preparation of a compound of formula (I), a pharmaceutical composition based on the compound of formula (I) and its application.EFFECT: new oxothiohydantoin derivatives, useful for treatment of androgen receptor mediated diseases.18 cl, 51 ex

Diaryl hydantoins // 2638833
FIELD: biotechnology.SUBSTANCE: invention relates to organic chemistry, namely to a new heterocyclic compound [RD93], which may be useful for treatment of hormone-refractory prostate cancer, benign prostatic hyperplasia, breast cancer and ovarian cancer.EFFECT: new heterocyclic compound with useful biological properties is obtained.6 cl, 41 dwg, 11 tbl, 61 ex
Veterinary method for noise aversion reduction // 2638804
FIELD: veterinarymedicine.SUBSTANCE: animal receives an effective amount of dexmedetomidine, medetomidine or a pharmacologically acceptable salt thereof, for example in the form of an oromucosal gel. Also, application of dexmedetomidine, medetomidine or a pharmaceutically acceptable salt thereof for the manufacture of a drug for reduction of noise aversion in animals is proposed.EFFECT: decreased noise aversion in dogs.11 cl, 1 tbl, 3 ex
Biotin tablets with delayed release and method for obtaining thereof // 2638803
FIELD: pharmacology.SUBSTANCE: invention is a pharmaceutical composition in the form of a pill that contains biotin as an active ingredient with a delayed release, and excipients, containing the following components, wt %: biotin 50-60, stabiliser 15-21, emulsifier 6-10, thickener 16.5-17, binder 1.5-3, debonder 0.4-1, lubricant 0.6-1.EFFECT: invention provides controlled release of the pharmaceutical composition of biotin in the presence of stable technological properties and stability.3 cl, 1 tbl, 5 ex
ethod for treatment of olfactory dysfunction in patients with acute rhinosinusitis // 2638688
FIELD: medicine.SUBSTANCE: method includes application of local decongestants, irrigation, anti-inflammatory and mucolytic therapy. After acute manifestations of the disease subside, multichannel electrical stimulation is performed on the areas of the chewing muscles, nose wings muscles, the circular muscle of the mouth and the trapezium from both sides. Electrical stimulation is carried out by bipolar-pulse current with a trapezoidal envelope by a premise and a pause of 2 s, with a frequency of 20-120 MHz, current strength to low vibration of muscles under the electrodes. Exposure duration is 10-15 minutes. After this, a leech is placed on the lateral wall of the nose vestibule on one side for 10-12 minutes. The course of physiotherapeutic treatment is 4-5 combined weekly procedures.EFFECT: increased effectiveness of olfactory dysfunction treatment in patients with acute rhinosinusitis due to a multifactorial sequential action on all segments of the olfactory analyzer and the autonomic nervous system.1 ex

Derivative cyclic amine and its pharmaceutical application // 2638549
FIELD: pharmacology.SUBSTANCE: invention refers to derivatives if cyclic amine of formula (I), where A is a group, represented by the general formula (IIa), (IIb) or (IIc), where A is a group, provided by the general formula (IIa) or (IIb), R1 represents an alkyl group containing 1 or 2 carbon atoms and optionally substituted by a hydroxyl group, amine group or carboxyl group, R2 represents a hydrogen atom, R3 is a hydrigen atom or alkyl group containing 1 or 2 carbon atoms, R4 is a hydrogen atom or an alkylcarbonyl group, containing 2 carbon atoms, or an alkyl group, containing 1 or 2 carbon atoms and optionally substituted by alkylcarbonylamine group, containing 2 carbon atoms, and n is 1 or 2, in which, when R3 and R4, each independently represent an alkyl group, containing 1 or 2 carbon atoms, R1 represents an alkyl group containing 1 or 2 carbon atoms and substituted by a hydroxyl group, amine group or carboxyl group; and when A is a group, represented by the general formula (IIc), R1 represents an alkyl group, containing 1 carbon atom and substituted by a carboxyl group, R2 represents a hydrogen atom and X represents CH2, O or -NR5 and R5 is an alkyl group, containing 1 carbon atom. Also, the invention relates to a prodrug of the compound of formula (I), pharmaceutical, analgetic agent and therapeutic agent based on compounds of formula (I), or its prodrug.EFFECT: new derivatives of imidazol, useful in the treatment of pain, have been obtained.11 cl, 24 dwg, 5 tbl, 73 ex
Enzymes inhibition // 2638537
FIELD: pharmacology.SUBSTANCE: invention relates to the compound of the formula or its pharmaceutically acceptable salt. In the formula (I) R1 represents -CN; R2 is selected from (C1-C4)haloalkyl, (C1-C4)haloalkoxy; W represents the (i) 5-membered heteroaryl ring, where two or three ring-atoms represent the hetero-atom N, optionally substituted by one group, which is selected from the (C1-C4) alkyl, the group -NHR18, and from the group -COOR28; or (iii) phenyl group; R3 represents the group -CH2-R23; R5 represents the hydrogen; R6 represents the hydrogen; A1 represents the group -CR7=; A2 represents the group =CR8- or the group =N-; A3--A4 represents the group, which is selected from the group -CR4=N-, the group -CR4=CR9- and the group NR17-CO-; R4 represents the group, which is selected from the hydrogen, the (C1-C4) alkyl, -NR10R11, -NHCOR12, -NHCOO-R13, -NHCONR27-R14, the (C1-C4)alkoxy, -NH(CH2)n-SO2(C1-C4)alkyl, -(NH)q(CH2)n-(C6H4)-SO2(C1-C4)alkyl, -NHSO2(C1-C4) alkyl and -(NH)r(CH2)nCONR15R16; the other chemical groups value is indicated in the invention formula. The invention also relates to the pharmaceutical composition and to the method of the disease or state treatment, where HNE is implicated.EFFECT: there are new compounds of the formula that offer the inhibitors' properties of the human neutrophil elastase.14 cl, 97 ex
ethod of increasing medical efficiency for cattle pyroplasmosis with neozidin-m in association with laserpuncture // 2638444
FIELD: veterinary medicine.SUBSTANCE: Neozidin-M is injected in association with irradiation with a semiconductor infrared pulsed laser of biological active spots with numbers 8, 9, 13, 17 and 22 according to the atlas written by Kazeev G.V. The laser is operated by the "Uzor" apparatus with a length of 890 nm with a pulse frequency of 1000, 1500 and 2000 Hz, in exposure of 0.5; 1.0; 1.5; 2.0 and 2.5 minutes after diagnosis and every 24 hours during the course of treatment.EFFECT: method provides high therapeutic activity of the disease treatment due to additional biostimulating effect.3 tbl, 1 dwg
ethod for increast of therapeutic efficiency of diminasin-70 in case of cattle pyroplasmosis // 2638433
FIELD: veterinary medicine.SUBSTANCE: invention can be used to increase the therapeutic efficacy of Diminazene-70 in case of cattle pyroplasmosis. For this purpose, the "Diminazene-70" preparation is administered in combination with irradiation of biologically active points 8, 9, 13, 17 and 22 according to the Kazeev G.V. atlas with a semiconductor infrared pulsed laser. Laser irradiation is carried out from the "Uzor" apparatus with a length of 890 nm, pulse frequency of 1000, 1500 and 2000 Hz, in exposures of 0.5; 1.0; 1.5; 2.0 and 2.5 minutes after diagnosis and every 24 hours during the treatment period.EFFECT: high therapeutic activity due to additional biostimulating effect.1 dwg, 3 tbl
ethod of increasing medical efficiency for cattle pyroplasmosis with pyro-stop medication in association with laserpuncture // 2638431
FIELD: veterinary medicine.SUBSTANCE: PYRO-STOP medication is injected in association with irradiation with a semiconductor infrared pulsed laser of biological active spots with numbers 8, 9, 13, 17 and 22 according to the atlas written by Kazeev G.V. The laser is operated by the "Uzor" apparatus with a length of 890 nm with a pulse frequency of 1000, 1500 and 2000 Hz, in exposure of 0.5; 1.0; 1.5; 2.0 and 2.5 minutes after diagnosis and every 24 hours during the course of treatment.EFFECT: increase of medical efficiency for cattle pyroplasmosis, high therapeutic activity due to additional biostimulating effect.3 tbl, 1 dwg
ethod for treatment of teeth hyperesthesia in patients on background of somatic diseases // 2638293
FIELD: medicine.SUBSTANCE: after a professional hygienic cleaning of teeth, 1.0-2.0 ml of "R.O.C.S® Medical Minerals" gel is applied on all surfaces of the teeth enamel with a circular brush. After that, 1.0-1.5 ml of "Gialudent gel" No.3 is applied to the mucous membrane of the teeth gums, isolated from saliva, with a disposable application syringe. Laser therapy is carried out by a laser semiconductor dental therapeutical device "Optodan" with a periodontal nozzle, in frequency mode II, with exposure of 1 minute per 4 fields of the left and right halves of both jaws, no more than 4 minutes for 1 procedure. The therapeutic course makes 7-10 daily procedures. Additionally, a vitamin-mineral complex of chewable tablets "R.O.C.S Medical" is administered 1 tablet 3 times a day for 30 days.EFFECT: decreased prevalence, intensity of tooth hyperesthesia and caries intensity, increased enamel resistance with long-term and persistent effect of remineralization and stabilization of enamel zones demineralization.3 tbl, 6 ex
Triazolcarboxamide derivatives // 2637938
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the formula I. In formula IR1 is phenyl or pyridinyl optionally substituted by halogen, lower alkyl, lower alkoxy, lower alkyl, substituted halogen, and lower alkoxy substituted by halogen; X1 is -N = or CH; X2 is a CR2 or =N-; X3 is -N= or CH; provided that only two of X1, X2 or X3 are nitrogen; where is a triazole group selected from , or ; R2 is hydrogen or lower alkyl; Z is a bond, -O- or -CH2-. The compounds of the invention possess affinity for the receptors associated with trace amines (TAAR). The invention also relates to pharmaceutical compositions and to application of a compound for drug manufacture.EFFECT: new compounds of formula I are obtained that have a high affinity for the receptors associated with trace amines, especially TAAR1.12 cl, 1 tbl, 36 ex
New eye droplets for conservative treatment and prevention of the age-related nuclear cataract // 2637875
FIELD: pharmacology.SUBSTANCE: eye droplets for prevention and treatment of age-related nuclear cataract contain the following components: sodium chloride - 4.1 mg, sodium dihydrogen phosphate (monohydrate) - 4.6 mg, sodium hydrophosphate (ahydrous) - 4.74 mg, benzalkonium chloride - 0.2 mg, ondansetron hydrochloride dihydrate - 0.002-0.2 mg and water for injection - 1.0 ml.EFFECT: application of the invention provides highly effective eye droplets for the conservative treatment and prevention of age-related nuclear cataract, taking into account the pathogenetically substantiated need for a differentiated approach to treatment of different types of age-related cataract.1 tbl, 3 ex
ethod for prevention of early postoperative cognitive dysfunction in patients with digestive organs pathology // 2636867
FIELD: medicine.SUBSTANCE: preliminary study of the cognitive and psychological status of the patient is performed. Combined anaesthesia is performed, including inhalation endotracheal sevoflurane anaesthesia and prolonged epidural analgesia. In this case, when a patient is diagnosed with initial cognitive impairment, chronic pain syndrome, anxiety and depression, a potentized anaesthetic with sevoflurane at a dose of 1.8-2.0% in oxygen is performed in the preoperative period. Immediately after trachea intubation, micro-jet infusion of dexmedetomidine is added at a dose of 0.4-0.8 mcg/kg/h, which is continued until suturing of the postoperative wound begins. The bispectral index of the electroencephalogram during the operation is maintained in the range of 40-60%.EFFECT: method allows to increase the effectiveness of prevention of early POCD development in patient subject to surgery due to GIT cancer, to reduce the opioids dose, to exclude the risk of application of excessively high doses of anaesthesia drugs.2 ex
Combined drug for primary neuroprotection // 2636616
FIELD: pharmacology.SUBSTANCE: drug containing glycine and thiotriazoline is presented.EFFECT: high primary neuroprotective activity due to mutually reinforcing action, which are part of the preparations, and a wide range of biological effects.3 cl, 4 tbl
Substituted pyrrolidines as xia factor inhibitors for thromboembolic diseases treatment // 2636050
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the general formula , their pharmaceutically acceptable salts, pharmaceutical compositions containing the said compounds.EFFECT: compounds of general formula I are XIa factor inhibitors and are suitable for thromboembolic diseases prevention or treatment.22 cl, 1 tbl, 115 ex
Imidzol derivative condensed heterocycle having active ampk effect // 2635662
FIELD: chemistry.SUBSTANCE: invention relates to a heterocyclic compound of the formula (I), or a pharmaceutically acceptable salt thereof, wherein the group represented by the formula is a group represented by the formula: ; R1, in each case, independently, is halogen, unsubstituted alkyl, substituted alkenyl, substituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclyl, or substituted amino; wherein the said radical values are disclosed in the invention formula; m is an integer of 2 or 3; R2 is hydrogen; X is -O-; and Y is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; where the said values of the radical are disclosed in the invention formula. The invention also relates to the pharmaceutical composition based on a compound of theformula (I) and the method of preventing or treating diabetes based on the compound use of the formula (I). .EFFECT: new compounds have been produced that have an activating effect on adenosine monophosphate-activated protein kinase.18 cl, 87 tbl, 24 ex
ethod for prevention of agitation syndrome in children with oncological pathology // 2635532
FIELD: medicine.SUBSTANCE: methodincludes single intranasal injection of dexmedetomidine at a dose of 2 mcg/kg prior to anesthesia with sevoflurane on a semi-open contour with maintained spontaneous breathing. Application of the invention makes it possible to achieve pre-anesthesia sedation level R3-R5 on the Ramsey scale without respiratory depression, development of analgesic effect.EFFECT: decrease in MAC of sevoflurane, prolongation of postnarvic sleep, a decrease in intracranial pressure, level of cerebral blood flow, and brain oxygen consumption.2 tbl, 2 ex

Stable anti-inflammatory solutions for injection // 2635521
FIELD: pharmacology.SUBSTANCE: liquid pharmaceutical solution for injection contains ketoprofen, amitriptyline, oxymetazoline, polyol, Na citrate and water. The polyol is selected from polyethylene glycol, propylene glycol, glycofurol and diethylene glycol monomethyl ether. The pharmaceutical solution has a pH of 4.5 to 7.0.EFFECT: injection solution of the invention is stable for 6 months when stored at a temperature between 2 and 30 degrees.11 cl, 7 dwg, 3 tbl, 8 ex
New photographic system // 2635512
FIELD: pharmacology.SUBSTANCE: invention is a photoprotective composition consisting of only 3 or 4 solar filters comprising: one or two UV-A filters to achieve a critical wavelength of >370 nm selected from the following: 5,6,5',6'-tetraphenyl-3,3'-(1,4-phenylene)-bis[1,2,4]triazine, 1,1'-(1,4-piperazinediyl)bis[1-[2-[4-(diethylamino)-2-hydroxybenzoyl]-phenyl]-methanone, butyl methoxydibenzoylmethane (BMDBM) in an amount of less than 2 wt %, based on the total weight of mentioned composition, hexyl-2-[4-(diethylamino)-2-hydroxybenzoyl] benzoate; Subject to the mandatory presence of 5,6,5',6'-tetraphenyl-3,3'-(1,4-phenylene)-bis[1,2,4]triazine. Also included in the composition are 2,4-bis[4-(2-ethylhexyloxy)-2-hydroxyphenyl]-6-(4-methoxyphenyl)-1,3,5-triazine (BEMT), one or two filters selected among UV-B filters, provided that the solar filters do not include octocrylene, para-aminobenzoic acid (PABA) and ethylhexyl methoxy cinnamate.EFFECT: invention can significantly increase the sunscreen factor SPF, photostability, stability in relation to light, air, moisture and temperature of the composition.22 cl, 7 tbl, 4 ex
Preservative-free topical composition, including hyaluronic acid // 2635473
FIELD: pharmacology.SUBSTANCE: invention is a topical composition for stimulation of skin or mucous membranes scarring, containing less than 1 CFU/ml of aerobic flora and free of preservatives, which contains, based on the total weight of the composition: at least 0.1 wt % of hyaluronic acid, a mixture of low molecular weight hyaluronic acid having a molecular weight of 600 to 1,000 kDa, and a high molecular weight hyaluronic acid having a molecular weight of 800 to 1,200 kDa, the said high molecular weight hyaluronic acid has a higher molecular weight than the said low molecular weight hyaluronic acid; at least one agent for skin scarring and water. The invention provides a composition where the high molecular weight hyaluronic acid enhances scarring by its film-forming effect, while the low molecular weight hyaluronic acid, due to its penetrability, enhances composition components penetration into tissues.EFFECT: improved healing properties, improves the epidermis structure and accelerates the differentiation of the granulation tissue.7 cl, 2 ex, 2 tbl

Halides of 1-(4-tert-butylphenyl)-2-{3-[2-(4-fluoro-phenoxy)ethyl]-2-methyl-3h-benzimidazole-1-yl}ethanone with property of rupture cross-linkers of glycated proteins // 2635112
FIELD: chemistry.SUBSTANCE: halides of the formula 1 are described, possessing the property of rupture cross-linkers of glycated proteins.EFFECT: new halides that have beneficial biological properties.4 cl, 2 dwg, 1 tbl

Parasiticide compositions containing several active agents, methods and their applications // 2633751
FIELD: veterinary medicine.SUBSTANCE: group of inventions relates to a veterinary composition for punctual external application to treat or prevent parasitic infections or invasions in an animal. The composition comprises: (a) a combination of four active agents comprising i. two topically active agents, where one of the topically active agents is fipronil, and the other is a regulator of insect growth; and ii. two systemically active agents where one of the systemically active agents is praziquantel and the second is an avermectin or milbemycin active agent; and (b) a pharmaceutically acceptable carrier comprising glycerolformal, dimethyl isosorbide or a combination thereof. A method for treatment or prevention of parasitic invasions or infections in an animal is also provided.EFFECT: group of inventions ensures destruction, control and prevention of parasitic infections and invasions in an animal.21 cl, 1 dwg, 7 tbl, 5 ex

Treatment of inflammatory damages in case of rosazea using ivermectin // 2633481
FIELD: pharmacology.SUBSTANCE: invention is a method for inflammatory damages treatment in case of rosacea in a subject in need thereof, comprising topical administration of a pharmaceutical composition containing 0.5% to 1.5% by weight of ivermectin and a pharmaceutically acceptable carrier once a day to the skin area affected by inflammatory damages at rosacea, where, 2 weeks after the initial administration of the pharmaceutical composition, a significant reduction in the amount of inflammatory damages is observed.EFFECT: significant reduction in the number of inflammatory damages at rosacea two weeks after the initial application, more effective treatment, statistically significant remission and reduced adverse skin reactions.15 cl, 5 ex, 8 tbl, 13 dwg
ethod for operative hemostasis in acute hardly accessible epidural bleedings from damaged veins, fractures of cranial vault and base and subsequent postoperative supervision // 2633299
FIELD: medicine.SUBSTANCE: epidural hematoma is removed, then the dura mater is pierced and liquid is injected thereunder. At that, a puncture with an insulin needle is performed at an angle of approximately 30-40 degrees to the shell surface, its outer sheet is pierced, then the needle tip is slightly raised. The raised area is grasped with an anatomic tweezers and the insulin needle is further injected under the shell. Physiological solution containing 1-2 ml of cyanocobalamin is then injected into the subdural space in a volume sufficient to completely expand the dura mater and tightly adhere to the edges of the bone defect. Then the insulin needle is removed and an epidural catheter is installed through the hole in the dura mater, the height of the liquid column in which indicates the liquid level under the shell. When the shell stress on the catheter is relaxed, an additional volume of physiological solution containing cyanocobalamin is injected.EFFECT: reduced frequency of hemorrhagic complications decreases, reduced operating injury of skull bones decreases, prevention of the development of the trepanized patients syndrome, minimized risk of hematoma recurrence and the best conditions for subsequent skull plasty are provided, while the hard shell is adapted to the edge of the bone defect.1 ex

Papulopustular rosacea treatment by ivermectin // 2633076
FIELD: pharmacology.SUBSTANCE: invention is a method for treatment of papulopustular rosacea in a subject in need thereof, comprising topical application of a therapeutically effective amount of a pharmaceutical composition comprising ivermectin and a pharmaceutically acceptable carrier, once a day, to a region of skin afflicted with papulopustular rosacea, wherein the treatment results in a significant reduction in the number of inflammatory foci within 2 weeks after the initial application of the pharmaceutical composition.EFFECT: significant reduction in the number of inflammatory foci two weeks after the initial application without joint application of another active agent, more effective treatment, and a longer remission, a reduction in adverse skin reactions.16 cl, 12 dwg, 7 tbl, 4 ex
Preparation for application of aspartate and vitamin b12 or biotine for ketone bodies regulation // 2633071
FIELD: pharmacology.SUBSTANCE: compositions (versions) for enteral use for treatment and/or prevention of disturbed ketone and lactate metabolism, i.e. increased concentrations of ketone bodies, lactate and/or other organic acids of a mammal suffering from hyperglycemia after fasting or after eating, resistance to insulin or diabetes, comprising 12-40 wt % of aspartate equivalents in the protein fraction of vegetable and animal proteins in combination with vitamin B12.EFFECT: improved glucose and insulin response in blood, and restoration of the glucose and fatty acid metabolism balance.19 cl, 2 tbl, 4 ex
edicinal for vaginal application, with antiviral, antimicrobial, antifungal, antiprotozoal, antiinfectious, immunomodulating and antiinflammatory action, as ointment, gel, suppository // 2633056
FIELD: pharmacology.SUBSTANCE: medicament is presented comprising active substances, excipients and a consistently-forming base, characterized by comprising fluconazole, metronidazole, alpha- or beta- or gamma-recombinant interferon as active substances, disodium edetate and boric acid as adjuvants, and substances selected from the group: macrogol 400, macrogol 1500, macrogol 4000, vitepsol, glycerin, cocoa butter, paraffin, lanolin, vaseline, acetylphthalyl, GL type solid fat as a consistently forming base, wherein the drug components are in a specific ratio in g per 1 g of the agent.EFFECT: high therapeutic effect ensures rapid substances entry into the blood.1 cl
Gel pharmaceutical composition for blepharitis treatment // 2633054
FIELD: pharmacology.SUBSTANCE: invention is a pharmaceutical composition comprising recombinant interferon, metronidazole, fluconazole, boric acid and a consistently forming base, characterized by further comprising hyaluronic acid or sodium hyaluronate, the components in the composition being in a certain ratio %.EFFECT: increased therapeutic effect by expanding the drug spectrum, including complex anti-inflammatory, antifungal, antibacterial, antiviral, acaricidal and anti-allergic action, as well as due to the prolonged treatment effect of the drug.2 cl, 10 ex
New inhibitors of serine-threonine kinases, including for treatment of oncological diseases and tuberculosis // 2633032
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the general formula or n=0-2; A is independently selected and is a 5-7-membered aromatic heterocycle containing 1-2 N atoms and 0-1 S atom; A contains 0-2 R substituents; R is independently selected and represents methyl or ethyl; B is independently selected and represents phenyl, 5-6-membered heteroaryl cycle containing 0-2 N atoms and 0-1 S atom, or 5-6-membered cycloalkyl containing 0-2 N atoms and 0-1 S atom; B contains 0-3 R1 substituents; C is independently selected and represents phenyl, -NH2, -NH-C1-3-alkyl, -NH (C1-3-alkyl) C1-3-alkyl, a 5-6-membered heteroaryl cycle containing 0-2 N atoms and 0-1 S atom, or a 5-6-membered cycloalkyl containing 0-2 N atoms and 0-1 S atom; C contains 0-3 R1 substituents; R1 is independently selected and represents -C1-6-alkyl, halogen, phenyl, -C5-7-heteroaryl containing 1-2 N atoms and 0-1 S atom, -COOH, -CONH2, -NH2 or -NHR2; R2 is independently selected and represents -C1-6-alkyl, -C (O) -C1-8-alkyl; the linker X is independently selected and is -CH2-, -C(=O)-CH2- or -CH2-O-group; the linker Q is independently selected and represents -NH- or -NH-C(O) -group; the Y linker is independently selected and represents -O-(CH2) m or -C(O)-NH-(CH2)m, where m=1-3; Z is independently selected and represents -CH2- group or an oxygen atom.EFFECT: compounds are prospective for use in the therapy of diseases associated with the activity of serine-threonine kinases.13 cl, 2 tbl, 16 ex
Heterocyclic derivative and pharmaceutical means // 2632908
FIELD: pharmacology.SUBSTANCE: invention relates to a heterocyclic derivative or a pharmaceutically acceptable salt thereof, of the general formula , wherein ring A is a group represented by the general formulas , or , where X1 is NH, NC1-6alkyl or O; A1 is hydrogen; A2 is i) hydrogen; ii) halogen; iii) C1-6alkyl optionally substituted by one to three groups selected from a group consisting of halogen, amino, mono(C1-6alkyl)amino, di(C1-6alkyl)amino, carbamoyl, mono(C1-6alkyl)aminocarbonyl, di(C1-6alkyl)aminocarbonyl, saturated cyclic aminocarbonyl, wherein the "saturated cyclic amino group" of the "saturated cyclic aminocarbonyl" part is 1-pyrrolidinyl, C1-6alkoxy and C1-6alkoxy-C1-6alkoxy; iv) C3-6cycloalkyl, optionally substituted by C1-6alkyl optionally substituted by one to three halogens; vi) a 4 to 5-membered saturated heterocyclic group containing one nitrogen or oxygen atom in the ring, optionally substituted by C1-6alkyl, (C1-6alkyloxy)carbonyl, (C1-6alkyl)carbonyl or hydroxy; (vii) C1-6alkylthio; (viii) C1-6alkylsulfonyl; ix) C1-6alkylsulfinyl; x) -NR3R4, where R3 and R4 are the same or different groups selected from a) hydrogen, b) optionally substituted C1-6alkyl, or c) C3-6cycloalkyl; or xi) saturated cyclic amino, wherein the "saturated cyclic amino" is piperidino, 1-piperazinyl or 4-morpholino, optionally substituted by C1-6alkyl, amino, mono(C1-6alkyl)amino, di(C1-6alkyl)amino, C1-6alkoxy or hydroxyl; R1 is phenyl, benzyl, naphthyl, C3-6cycloalkyl, C3-6cycloalkylmethyl, heteroaryl wherein heteroaryl is benzothiadiazolyl, benzothiazolyl, indolyl, 1,1-dioxobenzothiophenyl, quinolyl or 1,3-benzoxazol-2-yl, 1,2,3,4-tetrahydronaphthalen-5-yl, 1,2, 3,4-tetrahydronaphthalen-6-yl, 2,3-dihydro-1H-inden-4-yl, 2,3-dihydro-1H-inden-5-yl or C1-6alkyl, wherein the said phenyl, benzyl, cycloalkyl, cycloalkylmethyl and heteroaryl are optionally substituted; R2 is phenyl or pyridyl, wherein the said phenyl and pyridyl are optionally substituted. The invention also relates to a pharmaceutical composition and to an agent having the ability to inhibit mPGES-1 comprising a compound selected from the group consisting of a heterocyclic derivative of formula 1 and a pharmaceutically acceptable salt thereof as an active ingredient.EFFECT: heterocyclic derivatives possessing the inhibitory activity of mPGES-1.10 cl, 18 tbl, 257 ex
eans for inhibition of metastasis in lungs // 2632703
FIELD: medicine.SUBSTANCE: use of 2-(3,4-dihydroxyphenyl)-9-diethylaminoethylimidazo[1,2-a]benzimidazole(enoxifol) dihydrobromide as an agent for metastases inhibition is proposed.EFFECT: reduced frequency of development and the number of metastases, with a level of toxicity similar to mexidol, more pronounced antimetastatic activity.2 cl, 1 tbl
N-(acetylsalicyloyl)pyrazol with cerebroprotector action in case of cerebral circulation insufficiency // 2632005
FIELD: pharmacology.SUBSTANCE: invention can be used to obtain effective cerebroprotective agents based on pyrazole and 2-acetoxybenzoic acid (acetylsalicylic acid, aspirin). A pyrazole derivative with the formula given below is proposed. .EFFECT: derivative has a cerebroprotective effect, effectively and in small doses improves cerebral circulation in the model of one-stage irreversible bilateral occlusion of common carotid arteries, surpasses the action of pyracetam.3 tbl, 2 ex
ethod of medically induced support of patients during implementation of osteoplastic operations // 2631416
FIELD: medicine.SUBSTANCE: seven days prior to the operation and within three weeks after the operation, the patient is administered the drug Trental in tablets at a dose of 100 to 400 mg and the drug Actovegin by 1 pill up to three times a day. As an antibacterial agent on the day of the operation and within six days after it, Klacid SR is administered at a dose of 500 mg by 1 tablet 2 times a day. From the first day after the operation until the removal of the sutures, Zyrtec is administered at a dose of 10 mg by 1 tablet per day. For anesthesia, the patient is administered a selective COX-2 inhibitor by 1 tablet after a meal. From the first day after the operation until the removal of the sutures, PerioKin gel is topically applied to the patient's surgery area 2-3 times a day. Within three weeks after the operation, ultraviolet gum irradiation and local laser therapy are performed, alternating these physiotherapeutic procedures daily. From the third day after the operation, paste and rinse after toothbrushing KIN® GINGIVAL ALPHANTA are used 2-3 times a day after a meal. 3 weeks after the operation Osteogenon drug is administered by 1 tablet twice a day and Chlorophyll Forte GP drug is administered by 1 capsule 1 time per day.EFFECT: improvement of microcirculation and trophism of tissues in the operated zone, creation of optimal conditions for reparative osteogenesis in the field of plastic and wound healing, prevention of postoperative complications concerning soft tissues.1 ex
 
2551385.
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