Drugs for disorders of the urinary system (A61P13)

A   Human necessities(312083)
A61P13                 Drugs for disorders of the urinary system (diuretics a61p0007100000)(591)
A61P13/04 - For urolithiasis(37)
A61P13/06 - Anti-spasmodics(17)
A61P13/08 - Of the prostate(92)
A61P13/10 - Of the bladder(85)
A61P13/12 - Of the kidneys(187)
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
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
Quinine compounds, method for their production and their medical application // 2641285
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula I or a pharmaceutically acceptable salt or optical isomer thereof, wherein, in formula I, n is selected from 1 to 7, R1 means C3-C7 hydrocarbyl, which may be unsubstituted or optionally substituted by halogen, alkoxy, alkoxycarbonyl, heterocyclyl or aryl; R2 is aryl or heteroaryl containing one or more heteroatoms selected from N, O or S which may be unsubstituted or optionally substituted by one or more substituents of halogen, phenyl, -OR6, -SR6, -NR6R7, -NHCOR6, -CONR6R7, -CN, -NO2, -COOR6, -CF3 or linear or branched C1-C4 hydrocarbyl, R6 and R7 can denote a hydrogen atom or linear or branched C1-C4 hydrocarbyl; R3 is hydroxyl, halogen, alkoxy or acyloxy. Alkoxy or acyloxy may be unsubstituted or optionally substituted by halogen, hydroxyl, alkoxy, hydrocarbyl, alkoxyhydrocarbyl, heterocyclyl or aryl; R4 and R5 may or may not be present, and, independently, can mean, without limitation, a substituent such as halogen, hydroxyl, alkoxy, hydrocarbyl, alkoxyhydrocarbyl, heterocyclyl or aryl when these radicals are present. Y is linear or branched C1-C7 alkyl or - (CH2-O-CH2)m-, which may be optionally substituted by halogen, hydroxyl, alkoxy, alkoxyalkyl, unsaturated hydrocarbyl, cyclic hydrocarbyl or heterocyclyl. M is 1-3; X- means an acid residue or hydroxyl, the said compounds having a selective antagonistic effect on the M1 and M3 receptors subtypes, but insignificantly affect the M2 receptor subtype.EFFECT: compound application efficiency increase.24 cl, 5 tbl, 33 ex

Rectal suppositories for prostate treatment containing lysyl-glutamyl-aspartyl-proline tetrapeptide // 2640931
FIELD: pharmacology.SUBSTANCE: invention describes rectal suppositories for treatment of prostate diseases, particularly chronic prostatitis, including chronic abacterial prostatitis (HAP), prostatic hyperplasia, benign prostatic hyperplasia, and for treatment of pre-and postoperative prostate conditions. Suppositories contain lysyl-glutamyl-aspartyl-proline tetrapeptide (0.0003-0.0010 grams), dimethylsulfoxide (0.014-0.05 g) and a base for suppositories in an amount sufficient to produce a suppository weighing 1.0 g.EFFECT: suppositories are stable during storage and highly effective for treatment of prostate diseases.5 cl, 1 dwg, 3 tbl, 6 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
Phenyl derivative // 2639875
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of the general formula (I) having a high antagonistic activity with respect to human S1P2, and can be used to prepare a drug for treatment of a disease mediated by S1P2, such as a disease caused by vasoconstriction, fibrosis and respiratory disease.EFFECT: compound application efficiency increase.14 cl, 2 tbl, 9 ex
Composition for prevention of urinary tract diseases // 2637650
FIELD: pharmacology.SUBSTANCE: composition for prevention of urinary tract diseases, containing American cranberry (Vaccinium macrocarpon) fruit extract, bearberry (Arctostaphylos uva-ursi) leaves extract, ascorbic acid, taken in a particular quantity.EFFECT: application of the above composition enhances the effectiveness of therapeutic effects, reduces the risk of uncontrolled pharmacokinetic interactions between components, reduces the likelihood of negative side effects, increases availability of biologically active components.2 cl, 1 tbl
ethod for treatment of chronic prostatitis in dogs // 2637632
FIELD: veterinary medicine.SUBSTANCE: method for treatment of chronic prostatitis in dogs includes introduction of antibacterial drug with antibacterial drug injected once a day and represented by 10% solution of ciprofloxacin at a rate of 5 mg/kg, introduced in a therapeutic dose intramuscularly to the rear femoral muscle group, while introducing nicotinic acid 15 minutes before the therapeutic concentrations of the antibacterial drug in the animal blood the rear femoral muscle group in a biological dose of 0.15 mg/kg.EFFECT: achievement of therapeutic concentrations of antibacterial drug in the prostate gland tissues, in parallel with the achievement of such in the serum, shortened system effects of antibacterial drugs on dogs' body in complex treatment and reduced probability of relapse.1 tbl, 4 ex
ethod for chronic bacterial prostatitis treatment // 2636865
FIELD: medicine.SUBSTANCE: catheteris introduced into the urethra. It is directed through the anterior urethra, the external sphincter. Then, through the posterior urethra, passing the posterior sphincter, it is entered into the bladder, where it is bent, thereby introducing the entire length of the catheter. Then, saline solution in a volume of 8-10 ml is injected into the shell cavity from the end of the first catheter layer and thus, the above shell is spread to form a ball, free in the lumen of the urinary bladder. Then the catheter is pulled until resistance appears and thus obturate the internal opening of the urethra. Then, 5 ml of sterile saline solution is injected into the catheter shell cavity, located at the level of the external sphincter, and thus, the specified shell located at the external sphincter is spread as a ball used to hermetically close the distal sphincter of the prostate gland. Then a syringe is used to inject a medicinal mixture under the pressure of the syringe piston through the central tube of the catheter into the prostate. 20 ml of the previously prepared medicinal mixture, prepared as follows: chymopsin or trypsin is diluted in 5 ml of saline, the solution transferred into a sterile graduated test tube or tank with a volume of 25-30 ml, 4 ml of 2% lidocaine, 2 ml of trental (20 mg/ml), 2 ml of dexamethasone (4 mg/ml) and an antibiotic: ceftriaxone - 1.0 gor gentamicin - 2 ml with a concentration of 40 mg/ml, or vidokcin - 0.1 g are added, then the total saline solution is adjusted to 20 ml, is injected into the prostate. Under the pressure of the syringe piston, drugs are injected into the ducts of the prostate gland, then into the acini, thereby impregnating the prostate tissue. Then, 20 minutes after, 2 ml of metrogyl with concentration of 5 mg/ml is introduced and left for another 20-30 minutes in this exposition, and then the catheter is removed emptying the previously disclosed expanding shells, and then 2-4 procedures described above are performed every 3-4 days.EFFECT: method allows to achieve stable remission, shortened treatment time and absence of side effects from prolonged systemic antibacterial treatment.2 dwg, 2 tbl
New tetrahydropyrimidine connection or its salt // 2636310
FIELD: pharmacology.SUBSTANCE: invention relates to a new tetrahydropyridopyrimidine compound of the general formula (I) or a pharmaceutically acceptable salt thereof. The compounds possess an inhibitory activity against the androgen receptor (AR) and can be used to treat a tumour associated with activity (AR). In the general formula ,X is a halogen atom or halogen-C1-3an alkyl group; R is a phenyl group which is substituted by R1 and can also be substituted by R2, or a 5- or 6-membered heteroaryl group which contains 1 to 3 heteroatoms selected from a nitrogen, oxygen or sulfur atom and which is substituted by R1 and can also be substituted by R2; R1 represents a hydrogen atom, a phenyl group, a hydroxy-C1-6alkyl group, hydroxy-C3-7cycloalkyl group,C1-6an alkoxy group which may be substituted by Ra, C3-7 a cycloalkylaminosulfonyl group, a (6-7) membered monocyclic heterocycloalkylsulfonyl group, with two nitrogen atoms or a nitrogen atom and an oxygen atom in the ring; halogen-C1-3alkoxycarbonylamino group, halogen-C1-3alkylcarbonylamino group, a (5-7)membered monocyclic heterocycloalkanecarbonyl group,containing a nitrogen atom in the ring, and substituted with hydroxy-C1-6alkyl group, or - (CH2)n-C(=O)-NHRf; R2 is a hydrogen atom, a halogen atom or a halogen-C1-3an alkyl group; Ra is C1-6alkylpyrazolyl group, a triazolyl group, a tetrazolyl group or a C1-6 alkylsulfonylpiperazinyl group; Rf is halogen-C1-3alkyl group, hydroxy-C1-6alkyl group, hydroxy-C3-7cycloalkyl group, hydroxy-C3-7cycloalkyl-C1-6alkyl group C1-6alkyl group, substituted by Rfa; Rfa is C a 1-6alkylpyrazolyl group, halogen-C1-3alkylthiazolyl group, an oxadiazolyl group or a halogen-C1-3alkyloxadiazolyl group; and n is an integer from 0 to 3.EFFECT: obtaining of a new compound.20 cl, 5 tbl, 63 ex

Composition for treatment of hypertension and/or fibrosis // 2635564
FIELD: pharmacology.SUBSTANCE: invention relates to the compound of the formula (I) or its pharmaceutically acceptable salt. The invention also relates to a pharmaceutical composition having effects that reduce blood pressure and/or antifibrotic effects comprising a compound of the invention or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient. The compound of the invention is intended for therapeutic treatment of hypertension or prehypertension, prophylactic treatment of fibrosis, therapeutic treatment of fibrosis, therapeutic treatment of hypertension and fibrosis, and treatment of prehypertension and fibrosis in a subject.EFFECT: reduces blood pressure, has antifibrotic effects.16 cl, 12 dwg, 3 ex

Preparations of thermo-abrasive hydrogel for application in treatment of utertal disorders // 2635466
FIELD: pharmacology.SUBSTANCE: invention is a composition of a biocompatible, mucoadhesive, thermoreversible hydrogel comprising a botulinum toxin and comprising at least one thermoreversible gelling agent selected from the group consisting of poloxamers, methylcellulose, hydroxypropylmethylcellulose, alginates, pH-controlled gellants, or any combination thereof, And at least one component selected from the group consisting of mucoadhesiveness enhancers and thickeners selected from the group consisting of polycarbophil, poly crosslinked acrylic acid, polymethacrylates, divinyl glycol, polyethylene glycol, polyethylene oxide, copolymer of vinylpyrrolidone and vinyl acetate, cellulose, microcrystalline cellulose, cellulose derivatives, gelatin, starch, starch derivatives, Gum, Dicalcium phosphate, lactose, sucrose, polyvinylpyrrolidone, polyvinyl alcohols, partially hydrolyzed polyvinyl acetate, polysaccharides, waxes, fats, fatty acid derivatives, hyaluronic acid, chitosan, carrageenan, carbomers, eudragit and any combination thereof for use in the treatment of bladder disorders, the treatment comprising applying the composition to the bladder cavity and does not include any step of injecting botulinum toxin into the wall of said bladder.EFFECT: maintaining the stability of botulinum toxin during the instillation process, and after releasing it from the gel, enhancing the effect of botulinum toxin.18 cl, 2 ex, 1 tbl, 3 dwg

eans for kidney fibrosis treatment // 2635460
FIELD: pharmacology.SUBSTANCE: invention relates to a carrier for delivering a substance to extracellular matrix producing cells in the kidney, the carrier consisting of a lipid structure containing a retinoid as a targeting agent, wherein the carrier has the form of a liposome. This invention also relates to a pharmaceutical composition for kidney fibrosis treatment, wherein the said carrier is used, to a method and a kit for its preparation.EFFECT: increased means application effeciency.8 cl, 3 ex, 2 dwg
Drug with spasmolithic, diuretic and lithiolic action // 2635459
FIELD: pharmacology.SUBSTANCE: agent containing belladonna alkaloids, tincture of European madder, magnesium salicylate, a mixture of essential oils with a set of active substances, salicylic acid, linoleic and linolenic acids, ethanol and castor oil is proposed, wherein the substance contains the sum of belladonna alkaloids, recalculated for hyoscyamine as belladonna alkaloids, eucalyptus essential oil, anise essential oil and fennel essential oil as essential oils, and 1,8-cineole eucalyptus essential oil as a biologically active substance with a certain content of the ingredients.EFFECT: pronounced therapeutic effect in pain elimination and excretion of urinary stones, pronounced anti-inflammatory and diuretic effects.3 ex
Drug with litholithic, diuretic and anti-inflammatory action // 2635196
FIELD: pharmacology.SUBSTANCE: preparation containing a tincture of European madder root, magnesium salicylate, essential oils with a set of active substances, ethyl alcohol and vegetable oil is proposed, the composition further comprises a mixture of linoleic and linolenic acids, castor oil as a vegetable oil, eucalyptus essential oil, anise essential oil and fennel essential oil as essential oils, and 1,8-cineole eucalyptus essential oil as a biologically active substance of essential oils a at certain ratio of the composition ingredients.EFFECT: pronounced therapeutic effect in destruction and excretion of urinary stones, pronounced anti-inflammatory and diuretic effects.2 cl, 4 ex
ethod for rehabilitation of children with chronic secondary pyelonephritis // 2634042
FIELD: medicine.SUBSTANCE: at the second stage of rehabilitation, interference therapy is performed with a rhythmically varying frequency of 1-200 Hz, current intensity of 15 mA by the cross-over method to the segmentary-reflex area L2-S1 and the upper third of the front surface of hips. The duration of exposure is 10 minutes, for a course of 8 daily procedures. Also, exercise therapy is performed daily for 20-30 minutes in the morning together with manual massage of the lumbosacral area, for a course of 10 procedures every other day. In addition, sapropel is applied to the lumbar region with a temperature of +38°C, duration of 10-12 minutes, for a course of 8 procedures every other day. Low-mineralized chloride-sulfate magnesium-sodium mineral water, heated to 38-40°C, is administered as 5 ml/kg 3 times a day 40 minutes before meals daily for 21-24 days.EFFECT: normalization of oxidation-reduction processes, correction of immunological disorders, relief of inflammation and improvement of urodynamics and metabolic processes in kidneys, leading to an increase in the terms of remission and prevention of complications.4 tbl, 2 ex
Pyrazole derivative // 2632884
FIELD: pharmacology.SUBSTANCE: in the above formula , A represents a phenyl group which may be unsubstituted or substituted by 1 to 3 Q groups which are identical or different and are selected from the group consisting of a halogen atom, C1-6alkyl, C3-7cycloalkyl, C1-6haloalkyl, phenyl, -O-R2 and -O-C1-6haloalkyl; X and Z are CH and Y is a nitrogen atom; R is a hydrogen atom; R1 is a hydrogen atom and R2 is a hydrogen atom or C1-6alkyl group.EFFECT: compound has an inhibitory effect on xanthine oxidase, is well suited for treatment or prevention of diseases associated with xanthine oxidase such as gout, hyperuricemia, tumor lysis syndrome, stones in the urinary tract, hypertension, dyslipidemia, diabetes, cardiovascular disease, kidney disease, respiratory tract disease, autoimmune diseases, inflammatory bowel disease.10 cl, 7 tbl, 112 ex
New air of fluoridated benzylic acid and its salt // 2632881
FIELD: pharmacology.SUBSTANCE: invention relates to a benzyl ester of formula (I) or a salt thereof: , where R is fluorinated lower alkyl.EFFECT: increase in intraurethral pressure.13 cl, 1 tbl, 6 ex

Orally administrated adsorbent, therapeutic agent for kidney disease and therapeutic agent for liver disease // 2632432
FIELD: pharmacology.SUBSTANCE: orally administered adsorbent containing spherical activated carbon containing at least 0.5 wt % of nitrogen atoms which has a specific surface area determined by the Brunauer-Emmett-Teller method, from 700 to 3000 m2/g, and an average particle size of 0.01 to 1 mm. Therapeutic or prophylactic agent for kidney and kidney disease.EFFECT: high efficiency of method.7 cl, 4 dwg, 1 tbl, 35 ex
etadihol® - liquid and gel nanolartical preparations // 2631600
FIELD: pharmacology.SUBSTANCE: group concerns the water-gel composition of the inverse agonist VDR, which has the water properties, for the treatment of diseases associated with VDR, where the inverse VDR agonist is a polycosanol, the composition contains polycosanol in the form of nanoparticles in a concentration of 0.5-1 wt %, water-soluble polymer - carbopol in a concentration of 0.5-3 wt %, water, the composition is nano-gel. This composition is used to treat skin diseases.EFFECT: prevention of unwanted side effects of vitamin D in the treatment of skin diseases, increasing the therapeutic effect.5 cl, 5 ex, 57 tbl, 15 dwg
Derivatives of 1,2,4-triazine-4-amine // 2625791
FIELD: pharmacology.SUBSTANCE: compounds of Iyd formula possess an inhibitory activity against A1 receptor or A2a receptor. In formula Iyd B represents "CyBB". "CyBB" represents phenyl optionally having one or more substituents R4c. R4b, R4b' and R4c are, in each case independently, a halogen atom. CN. C1-8 alkyl, which optionally bears one or more substituents selected from halogen atoms, OR5a; C3-8 cycloalkyl; Heta; OR8; N (R9f) (R9g); =O; rr2 is 0-1; and ss tt are, in each case independently, 0 or 1, provided that ss and tt can not simultaneously be equal to 0. L1 and L2 are both single bonds; R8 represents, in each case independently, C1-8 alkyl, which optionally bears one or more substituents selected from halogen atoms. Heta represents, independently in each case, 3-6-membered fully saturated heterocyclic ring which contains one or two heteroatoms selected from O and N. R5a, R9f, R9g are H in each case independently; C1-10 alkyl. The invention also relates to individual compounds, to use of a compound, a pharmaceutical composition and a process for preparing a compound of Iyd formula.EFFECT: new compounds with an inhibitory activity against A1 receptor or A2a receptor.12 cl, 7 ex
eans with diuretic activity // 2624851
FIELD: pharmacology.SUBSTANCE: invention is a diuretic agent containing a 0.5% solution of fulvic acids in an amount of 40 ml and manganese oxide in an amount of 0.1 g.EFFECT: invention allows to increase the therapeutic effect and to exclude occurrence of side effects.2 ex

Bacterial strain, capable of oxalate metabolism // 2624033
FIELD: biotechnology.SUBSTANCE: strain of Lactobacillus paracasei spp. Paracasei LPC 09 DSM 24243 bacteria is proposed, which decomposes oxalic acid and/or its salts. The use of a pharmaceutical composition for prevention or therapeutic treatment of hyperoxaluria, urolithiasis, renal failure, cardiopathies, kidney stones, diverticulosis and diverticulitis is proposed. At that, the pharmaceutical composition comprises a bacterial composition comprising a plurality of cells of at least one bacterial strain, wherein at least one bacterial strain is Lactobacillus paracasei spp. paracasei LPC 09 DSM 24243. A food composition comprising a bacterial composition comprising a plurality of cells of at least one bacterial strain, wherein at least one bacterial strain is Lactobacillus paracasei spp. paracasei LPC 09 DSM 24243 is also provided.EFFECT: effective decomposition of oxalic acid or its salt in an amount of more than 60 percent.10 cl, 5 dwg, 2 tbl
Jasmonate application for bladder function disorders treatment // 2623878
FIELD: medicine.SUBSTANCE: invention relates to a method for treatment of non-psychological stress bladder function disorders, which is a bladder hyperactivity. The method involves administration of at least one jasmonate to a mammal in need of treatment, wherein the jasmonate is jasmone or has the structure (I), where n is 0; R1 represents alkoxy; R2 represents O; R3, R4 and R5 represent H; the bond between C9:C10 represents a double bond.EFFECT: invention provides treatment of urinary bladder hyperactivity.4 cl, 1 ex
Inhibitors of nonprilyzine // 2622288
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula , wherein R1 is selected from -OR7 and -NR8R9; R2 is H; X is -C1-9heteroaryl, selected from pyrazole, imidazole, triazole, benzotriazole, furan, tetrazole, pyrazine, thiophene, oxazole, isoxazole, thiazole, oxadiazole, pyridazine, pyridine, pyrimidine, benzoxazole, pyridylimidazole and pyridyltriazole; R3 is absent or is selected from H; Halogen; -C0-5alkylene-OH; -NH2; -C1-6alkyl; -CF3; -C3-7cycloalkyl; -C0-2alkylene-O-C1-6alkyl; -C(O)R20; -C0-1alkylene-COOR21; -C (O) NR22R23; -NHC(O)R24; =O; -NO2; -C(CH3) =N(OH); Phenyl optionally substituted with one or two groups independently selected from halogen, -OH, -CF3, -OCH3, -NHC(O)CH3 and phenyl; Naphthalenyl; Pyridinyl; Pyrazinyl; Pyrazolyl optionally substituted with methyl; Thiophenyl, optionally substituted by methyl or halogen; Furanyl; and -CH2-morpholinyl; and R3, when present, is attached to a carbon atom; R4 is absent or is selected from H; -HE; -C1-6alkyl; -C1-2alkylene-COOR35; -OCH2 O(O)CH (R36)NH2; -OCH2O(O)CH3; -CH2CH(OH)CH2OH; and phenyl or benzyl optionally substituted with 1 to 3 groups selected from halogen, -COOR35, -OCH3, -OCF3 and -SCF3; and R4, when present, is attached to a carbon or nitrogen atom; or R3 and R4 are taken together to form -phenylene-O- (CH2) 1-3- or -phenylene-O-CH2-CHOH-CH2-; A is 0 or 1; R5 is halogen; B is 0 or an integer of 1 to 3; Each R6 is independently selected from halogen, -OH, -CH3 and -OCH3; R7 is selected from H, -C1-8alkyl, -[(CH2)2O]1-3CH3, -C1-6alkylene-OC(O)R10, -C0-6alkylenemorpholinyl, -C1-6alkylene-SO2-C1-6alkyl and the structure of formula (a); R10 is -O-C3-7cycloalkyl; and R32 is -C1-6alkyl; R8 and R9 are H; R20, R21 and R35 are independently selected from H and -C1-6alkyl; R22 and R23 are independently selected from H, -C1-6alkyl, -CH2COOH, -(CH2)2OH, -(CH2)2OCH3, - (CH2)2SO2NH2, -(CH2)2N(CH3)2, -C0-1alkylene-C3-7-cycloalkyl and -(CH2)2-imidazolyl; or R22 and R23 are taken together to form a ring; R24 is selected from -C1-6alkyl; -C0-1alkylene-O-C1-6alkyl; Phenyl optionally substituted by halogen or -OCH3; and pyridinyl; and R36 is -CH (CH3) 2; and wherein the methylene linker on the biphenyl is optionally substituted with one or two -C1-6 alkyl groups; or a pharmaceutically acceptable salt thereof. Compounds of formula (I) are prepared by combining a compound of formula with a compound of formula 2 to provide a compound of formula I; Where P1 is also H. Also, the invention relates to an intermediate of formula 1, wherein P1 is H. The compounds of formula (I) are intended for the preparation of a medicament or pharmaceutical composition having inhibitory activity against non-prolamin (NEP). (a).EFFECT: compounds that have a non-lysine inhibitory enzyme activity.28 cl, 61 tbl, 25 ex

Crystalline form of compound used as a mineralocorticoid receptor antagonist and the method of its production // 2622105
FIELD: chemistry.SUBSTANCE: invention relates to crystalline forms I and II of compound 2-chloro-4-[(3S,3aR)-3-cyclopentyl-7-(4-hydroxy-1-carbonyl)-3,3a, 4.5-tetrahydro-2H-pyrazolo[3.4-f]quinolin-2-yl]benzonitrile of formula (I), used as a mineralocorticoid receptor antagonist. Crystalline forms have characteristic peaks of powder X-ray diffraction pattern specified in the claims. The invention also relates to processes for preparing crystalline forms I and II and the use of the obtained crystal forms in the manufacture of medicaments for the treatment and/or prevention of kidney damage or cardiovascular diseases.EFFECT: obtained crystalline form the compound of formula amorphous form of its superior stability, not only at high temperature and humidity, and light conditions.16 cl, 4 dwg, 4 tbl, 10 ex

Antagonists of trpv1, containing dihydroxy group as substitute, and their use // 2621708
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, in which R1 represents -halo or -CF3; R4 represents -H or -CH3; each of R8 and R9 independently represents -H, -halo, -CH3 or -OCH3, each halo independently represents -F, -Cl, -Br or -I; and m means an integer of 0 or 1; (1) provided that if R4 represents -H, the m means 1; and (2) provided that if R4 represents -H and the carbon atom in the position a of the a-b bond is in (S)-configuration, the methyl group connected to piperazinonyl ring represents a (S)-2-methyl group, a (S)-3-methyl group or a (R)-3-methyl group; (3) provided that if R4 represents -H, the carbon atom in position a of the a-b bond is in (S)-configuration, R8 represents -H and R9 represents -halo, then the methyl group connected to piperazinonyl ring represents a (R)-3-methyl group; (4) provided that if R4 represents -H, the carbon atom in position a of the a-b bond is in (S) configuration, R8 represents -F and R9 represents -F, then the methyl group connected to piperazinonyl ring represents a (S)-2-methyl group or a (S)-3-methyl group; and (5) provided that if R4 represents -CH3, each of the carbon atoms in positions a and c and the a-b bond and the c-d bond is in (S) configuration,R8 represents -H, R9 represents -halo, and m means 1, the methyl group connected to piperazinonyl ring is a (S)-3-methyl group or a (R)-3-methyl group. Invention also relates to a compound of formula (II) or a pharmaceutically acceptable salt thereof, a specific compound of formula (Ia) or a pharmaceutically acceptable salt thereof and / or a co-crystal of fumaric acid. Invention also relates to specific compounds of formula (Ib) or a pharmaceutically acceptable salt thereof. The compounds as per invention are intended to inhibit the function of TRPV1 in a cell and to treat pain, pain associated with osteoarthritis, osteoarthritis, urinary incontinence (UI), ulcer, inflammatory bowel disease (IBD) or irritable bowel syndrome (IBS) in an animal.EFFECT: compounds having an affinity for the receptor TRPV1.38 cl, 11 tbl, 3 dwg, 16 ex
ethod of surgical treatment of patients with purulent pyelonephritis // 2620756
FIELD: medicine.SUBSTANCE: perform video-reteretoneoscopic decapsulation of the kidney with the removal of apostematous foci, sanitation and drainage of the retroperitoneal space. In a day, the renal artery is catheterized for intra-arterial infusion. On the first day, infusion of vasaprostan in a dose of 20 mcg per 20.0 ml of 0.9% sodium chloride solution is carried out. Further for the next four days, infusions of the antibiotic from the group of cephalosporins of the 3rd generation to 50 ml of 0.9% sodium chloride solution in a continuous mode at a rate of 2 ml per hour are carried out.EFFECT: prevention of further spread of purulent-destructive processes in the kidney due to the removal of hypertension and restoration of blood circulation along major arterial highways when the distal blood flow is opened for antibacterial therapy.1 ex, 2 dwg

Lidocain reception diagram for application in long-term treatment of pain in bladder and irritation during urination // 2620032
FIELD: medicine.SUBSTANCE: method for treatment of bladder pain and/or urinary irritation symptoms comprises continuous administration of lidocaine to the patient's bladder during a treatment period of 24 hours or longer in an average therapeutically effective amount of about 10 mg to about 30 mg of lidocaine, based on the free base (FBE, free base equivalent) to achieve a therapeutic effect that persists after the end of the treatment period. A method for treatment of bladder pain and/or urinary irritation symptoms is also proposed, comprising continuous administration of an anesthetic or analgesic agent to the patient's bladder during a treatment period of 24 hours or longer in an amount effective to achieve a therapeutic effect that persists after the end of the treatment period. A method for treatment of bladder pain and/or urinary irritation symptoms is also proposed, comprising continuous administration of an anesthetic or analgesic agent to the patient's bladder during a treatment period of at least 24 hours in an amount effective to achieve a measurable plasma concentration, continuously throughout the treatment period. A device for drug delivery is also proposed to be used for treatment of bladder pain and/or urinary irritation symptoms, comprising an elastic device housing defining the lumen of a reservoir for a drug containing a useful load of lidocaine. The device body is designed to continuously control the release of lidocaine into the patient's bladder over a treatment period of at least 24 hours, with an average amount of about 5 mg to about 30 mg of lidocaine (FBE) per day during the treatment period.EFFECT: inventions provide effective treatment of bladder pain and/or urinary irritation symptoms, while reducing side effects of therapy to provide a lasting therapeutic effect that persists for at least 14 days after the active treatment period due to the proposed intravesical administration regimen.23 cl, 56 dwg, 6 tbl, 3 ex
Capsules for complex treatment of urinary system diseases // 2619736
FIELD: medicine, pharmacy.SUBSTANCE: invention refers to medicine, namely to pharmacy, and concerns the development of tools for complex treatment of urinary system diseases. The means has the form of microgranules, enclosed in a gelatin capsule. The means comprises mebeverine hydrochloride, cowberry extract, cranberry extract, as active ingredients, potato starch and glucose, as well as hydroxyethylcellulose, applied in the form of 0.25% aqueous solution as granulation liquid for microgranules preparation, as auxiliary substances.EFFECT: invention provides improved therapeutic effect and bioavailability of capsules.2 cl, 3 tbl, 3 ex

Crystalline solvates of hydrochloride 6-(piperidin-4-yloxy)-2h-isoquinolin-1-one // 2619129
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, in particular to crystalline dihydrate 6-(piperidin-4-yloxy)-2H-isoquinolin-1-one of formula and a solid pharmaceutical composition thereof.EFFECT: obtained crystalline hydrochloride dihydrate, having better stability and hygroscopicity, which is preferable in obtaining the medicinal product based on it.16 cl, 14 dwg, 1 tbl
Substituted derivatives of 3-thiazolaminepropionic acid and their use as pharmaceuticals // 2617843
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formulas Ia and Ib , in any of its stereoisomeric form or its physiologically acceptable salt, where G R71-O-C(O)-; R1 represents hydrogen; R2 represents hydrogen; R10 represents R11; R11 represents Ar; R30 is selected from the group including a (C3-C7)-cycloalkyl and R32-CuH2u-, where u means an integer chosen from the series containing 0, 1, 2 and 3; R32 represents a phenyl, optionally substituted by one or more identical or different substituents selected from the group comprising a halogen, a (C1-C6)-alkyl, R33 and (C1-C6)- alkyl-O-; R33 is a phenyl optionally substituted by one substitute selected from a halogen; R40 is selected from the group consisting of hydrogen and (C1-C4)-alkyl, or R30 and R40 together represent (CH2)x, where x is an integer selected from the group comprising 2, 3, 4 and 5; R50 is hydrogen; R60 is hydrogen; R71 is hydrogen; Ar, independently of each other Ar group, is selected from the group comprisng a phenyl and an aromatic 5-membered or 6-membered monocyclic heterocycle containing one or two heteroatoms selected from nitrogen and attached via a ring carbon atom, where the phenyl and the heterocycle all are optionally substituted by one or more identical or different substituents selected from the group comprising a halogen, a (C1-C6)-alkyl, (C1-C6) alkyl-O- and CF3; where all the alkyl substituents, independently from each other and independently of any other substituents, are optionally substituted by one or more fluorine atoms. The invention also relates to obtaining the compound of formulas Ia and Ib, or a physiologically acceptable salt thereof, that is prepared by reacting a compound of formula IIa or IIb with the compound. The compound of formulas Ia and Ib or its physiologically acceptable salt is intended for use as a pharmaceutical agent having the inhibitory activity against cathepsin A.EFFECT: substituted derivatives of the 3-thiazoleaminepropionic acid as protease inhibitors of cathepsin A.7 cl, 1 tbl

Vegetable combined cryo-powder based preparations // 2617434
FIELD: pharmacy.SUBSTANCE: vegetable combined preparation with diuretic, and/or antibacterial, and/or litholytic action containing common agrimony grass and dog rose root cryo-powders and auxiliaries.EFFECT: preparation has an effective diuretic, or antibacterial or litholytic action.7 cl, 12 dwg, 11 tbl
Dog treatment method with pyelonephritis and chronic renal insufficiency // 2617390
FIELD: veterinary medicine.SUBSTANCE: method includes injection of antibiotic ceftriaxone at the dose of 20-30 mg/kg of animal body weight intramuscularly once a day, 0.06% sodium hypochlorite solution at the dose of 1.5 ml per kg animal body weight intravenously once a day, physiological saline solution in the dose of 10 ml/kg of the animal body weight intravenously twice a day, 5% solution of cevitamic acid in the amount of 1 ml/30 kg of body weight intravenously twice a day, Essentiale N in the amount of 2.5 ml/30 kg of body weight intravenously 2 times per day during 10 days.EFFECT: method allows to reduce the morphological, functional and metabolic consequences of pyelonephritis disease in dogs with chronic renal insufficiency at the azotemia stage.4 tbl, 1 ex
ethod for correction of innate and adaptive immunity factors dysfunction for chronic renal failure in experiment // 2616213
FIELD: medicine.SUBSTANCE: starting from the 21st day of chronic renal failure simulation, calcium channel blocking amlodipine drug is administered to rats using a pipette at a dose of 0.25 mg/kg per day per animal, for 7 days. Changes in innate and adaptive immunity factors in relation to the performance of laboratory animals who do not receive amlodipine, are recorded. At that, innate immunity cell factors state normalization, phagocytosis and reactive oxygen forms generation ability, intensity of delayed hypersensitivity reaction, increasing of theantibody-forming cells number in the spleen, are established.EFFECT: method application expands information on the chronic renal failure pathogenesis mechanisms, does not require scarce supplies, is available in the research centers practice, is important for calcium channel blockers efficiency analysis for chronic renal failure treatment.2 tbl
Azetidine compounds, compositions and their use as inhibitors of soluble epoxide hydrolase // 2615995
FIELD: chemistry.SUBSTANCE: invention refers to new azetidine derivatives, having soluble epoxide hydrolase (sHE) inhibitor activity. Disclosed are compounds of formula I: R1-L1-A-L2-R2, their stereoisomers and pharmaceutically acceptable salts, where A is selected from a group, consisting of Ia, Ib or Ic, X is N or CH2, Y is N, CH2, CH, L1 is a bond, -C(O)-, -SO2- or -(CH2)0-3-NR3-C(O)-; L2 is a bond, -(CH2)1-3-, -NH-C(O)-NH-, -C(O)-, -SO2- or -(CH2)0-3- NR3-C(O)-; R1 is phenyl, where phenyl is unsubstituted or substituted with one or two R5, 6-member heteroaryl with two nitrogen atoms in ring, where rest of ring atoms are carbon atoms, or adamantyl; R2 is phenyl, -(CH2)1-3-phenyl, where phenyl is unsubstituted or substituted with one or two R5, or 6-member heteroaryl with two nitrogen atoms in ring, where rest of ring atoms are carbon atoms; R3 is hydrogen atom; R4 is a hydrogen atom; R5 is a halogen atom, C1-C6-haloalkyl, C1-C6-haloalkoxy or -C(O)OR4.EFFECT: novel chemical compounds.13 cl, 1 tbl, 21 ex Ia, Ib, Ic
2-pyridyl substituted imidazoles as alk5 and/or alk4 inhibitors // 2612958
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, specifically to a novel 2-pyridyl-substituted imidazole derivative of formula (I), where R1 is phenyl, pyridyl or thienyl, condensed with a structural fragment, which together with two ring members of said phenyl, pyridyl or thienyl forms a 5-6-member aromatic or non-aromatic saturated ring, wherein said ring optionally contains up to two heteroatoms, independently selected from O, N and S, and condensed phenyl ring is optionally substituted with one group, independently selected from halogen, -O-C-1-6alkyl, -C1-6alkyl, -O-(CH2)q-NR4R5, or 5-member heteroaryl containing up to two heteroatoms, independently selected from N; or R1 is phenyl, substituted with one or more groups, independently selected from halogen, -O-C1-6alkyl, -S-C1-6alkyl, -C1-6alkyl, -C1haloalkyl, -CN, -(CH2)p-NR4R5, -(CH2)p-NHCOR4, -(CH2)p-NHCO2R4; -(CH2)p-NHSO2R4 or N-bound 6-member heterocycle, where said heterocycle comprises two heteroatoms, independently selected from O, N, and optionally substituted with C1-6alkyl; R2 is -C1-6alkyl; R3 is H, -(CH2)p-NR4R5, -(CH2)p-CN, -(CH2)p-CO2R4, -(CH2)p-CONR4R5, -(CH2)p-OR4, -(CH2)p-NHCOR4; R4 and R5 independently denote H or -C1-6alkyl; p denotes an integer ranging from 0 to 1; q denotes 2; n denotes an integer ranging from 1 to 2; X is NR7; and R7 is H or -CO-C1-6alkyl. Invention also relates to use of a compound of formula (I), a pharmaceutical composition based on compound of formula (I) and to a method of preventing or treating diseases, based on use of compound of formula (I).EFFECT: technical result is obtaining novel heterocyclic compounds effective in treating or preventing a disease, mediated by ALK5 and/or ALK4 receptors in a mammal.8 cl, 44 ex, 1 tbl

Therapeutic agents for regulating serum phosphorus level // 2612912
FIELD: chemistry.SUBSTANCE: invention relates to chemical-pharmaceutical industry and represents a method of treating chronic kidney disease-mineral and bone disorder (CKD-MBD) in a patient receiving hemodialysis, wherein said method involves administering to patient a composition containing a compound, including Ac-c(C)arrrar-NH2 (SEQ ID NO: 3), and a pharmaceutically acceptable excipient, where composition is administered as intravenous injection during a period beginning approximately 15 minutes before completion of haemodialysis and ending approximately 3 hours after hemodialysis, and where said administering allows to efficiently maintain post-hemodialysis serum phosphorus level below serum phosphorus level prior to hemodialysis during a period, of at least approximately 6 hours after dialysis.EFFECT: invention allows to mitigate post-dialysis rebound of serum phosphorus level.7 cl, 3 dwg, 4 tbl, 2 ex
Substituted dihydropyrazolones for treating cardiovascular and hematologic diseases, use thereof, drug and method of treating and/or preventing // 2611012
FIELD: chemistry; pharmaceutics.SUBSTANCE: present invention relates to use of dihydropyrazolone derivatives of formula (I), in which radicals and symbols are defined in p. 1 of patent claim.EFFECT: making drug for treating and/or preventing cardiac diseases of blood circulation, cardiac failure, anemia, chronic diseases of kidneys and renal failure, as well as medicinal agent containing said dihydropyrazolone derivatives, and method of treating and/or preventing said diseases in human and animals.4 cl, 10 tbl, 180 ex
Substituted amide compounds // 2609021
FIELD: chemistry.SUBSTANCE: invention relates to 2-({[(2-cyano-4-methoxyphenyl)acetyl](3-phenylpropyl)-amino}methyl)-N-(dimethylsulphamoyl)-5-methyl-1,3-thiazol-4-carboxamide or pharmaceutically acceptable salt thereof, which is used as an active ingredient of a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA).EFFECT: compound has excellent LPA receptor antagonist action and can be used as an agent for preventing and/or treating the diseases caused by LPA.7 cl, 138 tbl, 308 ex
ethod of treating haemorrhagic cystitis in cats // 2606910
FIELD: veterinary science.SUBSTANCE: invention relates to veterinary science, namely to method of treating haemorrhagic cystitis in cats. Method involves administering antibacterial preparation into urinary bladder. As antibacterial preparation suspension is used, containing silver nanoparticles, stabilized by submicron particles of titanium dioxide, and synthetic polymer poly-N-vinylpyrrolidone-2 in dose of 2.0 ml once a day for 2–4 days.EFFECT: invention usage allows to reduce length of treatment.1 cl, 3 tbl, 3 ex
ethod of treating detrusor overactivity // 2605624
FIELD: medicine.SUBSTANCE: invention relates to medicine, namely to urology, and concerns treating detrusor overactivity. Method involves cystoscopy with filling bladder with solution of nitrofural with subsequent injection of solution of botulinum toxin type A directly in detrusor in 20-40 injection points. Wherein solution of nitrofural is preliminarily cooled to temperature of 7-10 °C and selected dose of toxin in physiologic saline is introduced with temperature of 4-8 °C, using 0.5-1.0 ml of dissolved toxin for each injection.EFFECT: method provides both prevention of hemorrhage in area of surgical manipulations and prevention of postoperative pain syndrome, requiring no additional economic and physical efforts.1 cl, 2 ex

Amino-substituted 3-heteroaroylamino-propionic acid derivatives and use thereof as pharmaceutical agents // 2605600
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula I in form of any of its stereoisomeric forms, or its physiologically acceptable salt, where A denotes C(R1); D denotes N(R2); E denotes N; G denotes R71-O-C(O)-; R1 is selected from a group consisting of hydrogen and NC-; R2 denotes Ar-CsH2s-, where s denotes an integer 0 or R2 and R11 together denote -C(R18)=C(R19)-; R10 is selected from a group consisting of R11, R12-N(R13)-C(O)- and R14-C(O)- and (C1-C4)-alkyl-S(O)m-; R11 is selected from a group, consisting of hydrogen and R14 or R10 and11 form Het2; R12 and R13 are independently selected from a group, consisting of hydrogen and Ar; R30 is selected from a group, consisting of R31, (C3-C7)-cycloalkyl, R32-CuH2u-, where u denotes an integer selected from a group consisting of 0, 2 and 3; R40 is selected from a group consisting of hydrogen and (C1-C-4)-alkyl; R50 denotes hydrogen; R60 denotes hydrogen or R30 and R50 together denote (CH2)z, optionally substituted with one or more identical or different (C1-C4)-alkyl substitutes, where z denotes an integer selected from a group consisting of 3, 4 and 5; R71 denotes hydrogen; Ar, independently from each other group Ar, is selected from a group consisting of phenyl and aromatic 5-member or 6-member monocyclic heterocycle, which comprises one cyclic heteroatom selected from a group, consisting of nitrogen, oxygen, and is bonded to other part of molecules through a cyclic carbon atom, where phenyl is optionally substituted with one or more identical or different substitutes, selected from a group consisting of halogen, (C1-C6)-alkyl; Het2 denotes a saturated 5-6-member monocyclic heterocycle, which includes cyclic nitrogen atom, through which Het2 is bonded to other part of molecule, and optionally one additional cyclic heteroatom, selected from sulphur, optionally substituted with one or more substitutes, selected from oxo; m independently from each other m denotes 2. Invention also relates to a method of producing a compound of formula I or a physiologically acceptable salt thereof, which includes reacting a compound of formula II with a compound of formula III, where groups A, D, E, G, R10, R11, R30, R40, R50 and R60, in compounds of formulae II and III, are defined as groups in compounds of formula I, and, furthermore, there may be functional groups, which can be in protected form or in form of precursor groups, and group J, which is part of compound of formula II, denotes HO-, (C1-C-4)-alkyl-O- or halogen. Compound of formula I or physiologically acceptable salt thereof are intended for use as a pharmaceutical agent for inhibiting of protease of cathepsin A.EFFECT: technical result is amino-substituted 3-heteroaroylamino-propionic acid derivatives as cathepsin A inhibitor.8 cl, 1 tbl

Neprilysin inhibitors // 2605557
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula I, where R1 is -OR7; R2 is H; X is selected from a pyrazole, triazole, benzotriazole, tetrazole, oxazole, isoxazole, thiazole, pyridazine, pyrimidine and pyridyl triazole; R3 is absent or is selected from H; halogen; -C0-5alkylene-OH; -C1-6alkyl; -C3-7cycloalkyl; -C0-2alkylene-O-C1-6alkyl; -C(O)R20; -C0-1alkylene-COOR21; -C(O)NR22R23; -NHC(O)R24; =O; phenyl, optionally substituted with one or two groups independently selected from halogen, -OCH3, -NHC(O)CH3 and phenyl; naphthalenyl; pyridinyl; pyrazinyl; and R3, when present, is bonded to carbon atom; R4 is selected from H; -OH; -C1-2alkylene-COOR35; -pyridinyl; and phenyl or benzyl, optionally substituted by one or more groups selected from halogen and -OCH3; and R4, when present, is bonded to carbon atom or a nitrogen atom; a equals 0 or a equals 1; and R5 is selected from halogen and -CN; b is equal to 0 or 1, and R6 is selected from Cl, F, -OH, -CH3, -OCH3 and -CF3; or b is equal to 2, and R6 each is independently selected from halogen, -OH, -CH3, or -OCH3, or b is equal to 3, and R6 each is independently selected from halogen or -CH3; R7 is selected from H, -C1-8alkyl, -C1-3alkylene-C6-10aryl, -C0-6alkylene morpholinyl or dioxol-2-one methyl, of formula (a); or a pharmaceutically acceptable salt thereof. Compounds of formula (I) are obtained by condensation of compound of formula 1 with a compound of formula 2, where P1 is H or tert-butoxycarbonyl; and wherein method further includes removal of protective group of compound of formula 1, when P1 is tert-butoxycarbonyl. Also compound of formula (I) is obtained by removing protective group of compound of formula (6) or salt thereof; where R1P is -O-P3, where P3 is methyl. Invention also relates to intermediate compounds of formulae (1) and (6). Compounds of formula (I) are intended for inhibiting neprilysin activity.EFFECT: compounds having neprilysin inhibiting activity.19 cl, 9 ex,(а), ,

Granules with extracts of cranberries, red bilberry madder antidiuretic, antispasmodic and litholytic action // 2605271
FIELD: pharmaceutics.SUBSTANCE: invention refers to pharmaceutical industry, namely to an agent in the form of granules, possessing diuretic, antispasmodic and litholytic action. Agent in the form of granules possessing diuretic, antispasmodic and litholytic action, contains dry extract of rhaponticum madder, dry extract of cranberry and dry extract of bilberry, potato starch, aerosil A-380, glucose, 0.25 % aqueous solution of hydroxyethyl cellulose (HEC), in certain proportions.EFFECT: proposed agent in form of granules has a pronounced diuretic, antispasmodic and litholytic action, possesses fast solubility within 30 seconds, easy and hygienic in use.1 cl, 1 dwg, 3 tbl, 5 ex

Substituted aminobutyric derivatives as neprilysin inhibitors // 2604522
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula I, where R1 denotes -OR7; R2a is selected from -CH2OH, -CH2OP(O)(OH)2 and -CH2OC(O)CH(R37)NH2; or R2a together with R7 forms -CH2O-CR18R19-; R2b is selected from H and -CH3; Z denotes -CH-; X is selected from a pyrazole, imidazole, triazole, benzotriazole, oxazole, isoxazole, pyrimidine, pyridazine, benzimidazole, pyran and triazolo[4,5-b]pyridine; R3 is absent or is selected from H; halogen; -C0-5alkylene-OH; -C-1-6alkyl; -C(O)R20; -C0-1alkylene-COOR21; -C(O)NR22R23; =O; phenyl, optionally substituted with one or two groups, independently selected from halogen; and pyridinyl; R4 is absent or is selected from H; -OH; halogen; -C1-6alkyl; -CH2OC(O)CH(R36)NH2; -CH[CH(CH3)2]-NHC(O)O-C1-6alkyl; and phenyl or benzyl; a = 0; b = 0 or an integer from 1 to 3; each R6 is independently selected from halogen; R7 is selected from H, -C1-8alkyl,-C1-3alkylene-C6-10aryl, [(CH2)2O]1-3CH3, -C1-6alkylene-OC(O)R10, -C1-6alkylene-NR12R13, -C1-6alkylene-C(O)R31, -C0-6alkylenemorpholinyl, -C1-6alkylene-SO2-C1-6alkyl; structural formulae (a1), (a2), (a3) and (a4); R10 is selected from -C1-6alkyl, -O-C1-6alkyl, -C3-7cycloalkyl, -O-C3-7cycloalkyl and -CH[CH(CH3)2]-NH2; and R12 and R13 are independently selected from H, -C1-6alkyl and benzyl, or R12 and R13 together form -(CH2)5- or -(CH2)2O(CH2)2-; R31 is selected from -O-benzyl and -NR12R13; and R32 denotes -C1-6alkyl; R18 and19 are independently selected from H and -C1-6alkyl; R20 is selected from H and -C1-6alkyl; R21 denotes H; R22 and R23 are independently selected from H, -C1-6alkyl, -(CH2)2OCH3 and -C0-1alkylene-C3-7cycloalkyl; or R22 and R23 together form a saturated -C3-5heterocycle, selected from azetidine or pyrrolidine; and optionally containing an oxygen atom in ring; R36 is selected from H, -CH(CH3)2, phenyl and benzyl; and R37 is selected from H and -CH(CH3)2; and where methylene linker on biphenyl can be substituted with one or two -C1-6alkyl groups; or a pharmaceutically acceptable salt thereof. Invention relates to a method of producing a compound of formula I by combining a compound of formula 1 with a compound of formula 2. Invention also relates to an intermediate compound of formula 1, intended for use in synthesis of compound of formula I, where P1 denotes H or tert-butoxycarbonyl; or HCl salt thereof. Compounds of formula I are intended for preparing a pharmaceutical composition, possessing inhibitory activity on neprilysin (NEP).EFFECT: technical result is aminobutyric derivatives as neprilysin (NEP) inhibitor, for treating hypertension, cardiac failure or kidney disease.17 cl, 20 ex, (а1), (а2),(а3) and (а4),

Extended-release formulation for reducing the frequency of urination and method of use thereof // 2603471
FIELD: medicine.SUBSTANCE: group of inventions relates to methods and compositions for inhibiting the contraction of muscles and, in particular, to methods and compositions for inhibiting the contraction of smooth muscles of the urinary bladder. For this purpose, in production of a medicinal agent a pharmaceutical composition containing a first agent is used, namely, acetaminophen in an amount of 5 mg to 2,000 mg, and the second agent which is selected from a group consisting of an antimuscarinic agent, an antidiuretic and a spasmolysant. Besides, in production of a medicinal agent a pharmaceutical composition is used, containing the first component configured to fast release, and the second component configured for prolonged release, where each of said components contains acetaminophen in an amount of 5 mg to 2,000 mg. Pharmaceutical composition for prolonged release is also disclosed, containing acetaminophen in a dose of 5 mg to 2,000 mg, an antidiuretic and a pharmaceutically acceptable carrier.EFFECT: group of inventions provides the effective suppression of smooth muscle contraction of the bladder.28 cl, 9 tbl, 8 ex, 1 dwg

Isolated strains of lactobacillus plantarum dsm mcc1 23881 and lactobacillus gasseri mcc2 dsm 23882 microorganisms, and use thereof // 2603059
FIELD: biotechnology.SUBSTANCE: group of inventions refers to the strains of Lactobacillus plantarum DSM MCC1 23881 and Lactobacillus gasseri MCC2 DSM 23882 microorganisms and use thereof as antioxidant proteolytic ingredients for food product or food additive preparation. Strains generate conjugated linoleic acid (CLA), hydrogen peroxide (H2O2) and nitrogen monoxide (NO). Food products and food additives containing the above strains together or separately, are hypoallergenic, allergy and reduced irritation symptoms of lower urinary tract in males adult individuals, accompanying benign prostatic hyperplasia, and associated with oxidative stress and inflammation. Invention also discloses methods for production of food product or food additive.EFFECT: group of inventions relates to biotechnology and can be used in food industry.13 cl, 6 dwg, 13 tbl, 6 ex

ethods and compositions for treating hyperuricemia and metabolic disorders associated with hyperuricemia // 2603050
FIELD: medicine.SUBSTANCE: group of inventions relates to medicine, pharmacology, pharmaceutics and describes methods and compositions for treating and/or preventing hyperuricemia (HU) or metabolic disorders associated with HU. Such disorders include: acute or chronic gout, its sudden aggravations, gouty arthritis, urate nephrolithiasis, gouty nephropathy. Methods involve administering of therapeutically effective amount of diacerein, rhein or their pharmaceutically acceptable salt, analogue, prodrug or active metabolite. Wherein said compound reduces blood uric acid levels. Therapeutically effective amount of compound can be equivalent to 10-200 mg of diacerein base a day. Methods of treating with said compounds can be used in patients with poor tolerance to anti-inflammatory or urate-lowering agents.EFFECT: group of inventions provides advantages in reducing or preventing HU due to ability of diacerein and its said analogues, salt, prodrug, active metabolite, even in form of single agent therapy to reduce blood uric acid level to normal and below, causing no side effects, refractory to therapy as compared with previously known agents against HU.22 cl, 2 dwg, 2 ex, 2 tbl
Agent for treating chronic inflammatory diseases of urethra and bladder // 2602954
FIELD: pharmaceutics.SUBSTANCE: invention refers to pharmaceutical industry and medicine and represents an agent for treating chronic inflammatory diseases of the urethra and the bladder containing heparin, an analgesic substance and a base, characterized by that it additionally contains dexamethasone, as the analgesic substance - lidocaine, starch-agar gel as the base consisting of starch, agar-agar and purified water and myramistin as a stabilizer of the base, where heparin is contained in the agent in the amount of 22,750-25,500 IU, dexamethasone in the amount of 7.6-8.4 mg, lidocaine 2 % in the amount of 3.8-4.2 ml, starch in the amount of 0.33-0.40 g, agar-agar in the amount of 0.08-0.12 g, myramistin 0.01 % - 4-5 ml and purified water - 45-46 ml.EFFECT: invention provides higher clinical effectiveness in chronic inflammatory diseases of urinary bladder and urethra, prolonged remission, reduced rate of recurrences, effective reduction or reversal of pain syndrome.1 cl, 3 ex
 
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