Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents and non-steroidal antiinflammatory drugs (A61P29)

A   Human necessities(308424)
A61P29                 Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; non-steroidal antiinflammatory drugs (nsaids)(1454)

Production and application of bacterial histamine // 2628536
FIELD: medicine.SUBSTANCE: method for selecting a probiotic lactic bacterial strain for use in the local production of histamine in a mammal is provided. A product and composition for the local production of histamine in a mammal containing a lactic acid bacterial strain having an active histidine operon and capable of producing histamine is proposed for use in the treatment and/or prevention of inflammatory conditions.EFFECT: local production of histamine in a mammal by selecting certain strains of lactic acid bacteria.13 cl, 9 dwg, 2 tbl, 5 ex
Tricyclic nitrogen-containing derivatives of imidazo[4,5-c]pyridine, having inhibiting activity in response to hystamine 4 receptor (hh4r) // 2628074
FIELD: pharmacology.SUBSTANCE: invention relates to a heterocyclic compound of formula 1 , or to a racemate, isomer, or pharmaceutically acceptable salt thereof, wherein X1 and X2 are C; each of X3 and X4 is independently C or N, provided that one of X3 and X4 is N; R1 is a saturated 4-9 member mono- or bi-heterocyclyl containing 1-2 heteroatoms (where the heteroatoms are N), where R1 is unsubstituted or substituted by 1 to 3 substituents selected from -NR6R7 and R8; or R1 is selected from -NR6R7 and R8; R2, R3, R4 and R5 may be the same or different; and each is independently selected from -H; -C1-C6alkyl; -C1-C6haloalkyl; -C1 -C6perhaloalkyl; -halogen (-F, -Cl, -Br, -I); -CN; -C1-C6talkoxy; -C1-C6haloalkoxy; -C1-C6perhaloalkoxy; C2alkenyl; -C2-C3alkynyl; -amino; -OH; -nitro (-NO2); -C6-C1aryl; and furan; provided that, when X3 is N, R4 is absent; and when X4 is N, R5 is absent, each of Y1, Y2, Y3, Y4 and Y5 is independently C or a heteroatom (preferably a heteroatom independently selected from N, O and S), provided that at least two of Y1, Y2, Y3, Y4 and Y5 are heteroatoms independently selected from N and O; each of Y2 and Y3 can be independently substituted by R9; Y4 may be substituted with -H or -C1-C6alkyl; each of R6 and R7 is independently selected from -H; -C1-C6alkyl; and -carboxyl (-COOH); R8 is -C1-C6alkyl or -C3cycloalkyl; and R9 is selected from -H; -C1-C6alkyl; and -C3cycloalkyl; wherein the alkyl and heterocyclyl may be independently unsubstituted or substituted by one or more substituents (for example, 1 to 3 substituents) selected from the group consisting of -C1-C4alkyl, -C1-C4alkoxy and -OH. The invention also relates to particular compounds and a pharmaceutical composition based on the said compounds.EFFECT: new heterocyclic compounds useful for human histamine receptor 4 inhibition are obtained.13 cl, 13 tbl, 144 ex
Compounds of pyridazinamide and their use as synthetic syneckinasis inhibitors (syk) // 2627661
FIELD: chemistry.SUBSTANCE: invention relates to novel pyridazinamides of the formula I , where all variable substituents are defined in the claims, and their pharmaceutically acceptable salts, as well as a pharmaceutical composition based on them.EFFECT: compounds of the formula are SYK inhibitors and are useful for the treatment of autoimmune and inflammatory diseases.10 cl, 1 tbl, 43 ex

Anti-inflammatory compositions // 2627451
FIELD: medicine.SUBSTANCE: method for inflammatory condition treatment includes sublingual introduction of interleukin-2 (IL-2) at a dose of 4000 IU to 12000 IU per day, and where the inflammatory condition is selected from arthritis, sinusitis, allergic disorders, psoriasis, acne, inflammatory bowel disease, chronic fatigue syndrome, autoimmune disorders, Sjogren syndrome, prostate gland inflammation, urinary tract inflammation, pancreatitis, vasculitis, diabetes, gout or accompanying state and periodic pain. The group of inventions also concerns the use of interleukin-2 (IL-2) for inflammatory conditions treatment, where the drug is injected sublingually at a dose of 4000 IU to 12000 IU per day.EFFECT: effective treatment with lower doses compared to the currently available systemic delivery.13 cl, 5 ex, 5 dwg, 4 tbl
Pharmaceutical preparation for rheumatological diseases treatment // 2627424
FIELD: pharmacology.SUBSTANCE: pharmaceutical preparation in the form of a solution for use in rheumatological diseases treatment contains a combination comprising sodium diclofenac or naproxen sodium, betamethasone sodium phosphate and hydroxy-cobalamin sulfate as active substances and benzyl alcohol, propylene glycol, sodium metabisulphite and water for injection as auxiliary components. A method for production of the preparation is described as well.EFFECT: stable, effective formulation with analgesic, anti-inflammatory and antineurotic effects.4 cl, 1 tbl, 4 ex
Aza-aryl-1-h-pyrazol-1-yl-sulphonamides // 2627268
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of formula (I) ,in which radicals and characters have values specified in the claims and their versions. The proposed compounds act as potent antagonists of CCR (9) receptor. Animal testing has shown that these compounds are useful for treatment of inflammation, disease with a hallmark for CCR (9). The compounds as a whole are arylsulfamide derivatives and are used in pharmaceutical compositions, methods for treatment of CCR (9) mediated diseases and as a control in assays for identification of CCR (9) antagonists.EFFECT: increased efficiency of compounds application.26 cl, 2 tbl, 33 ex
2-aryl-2,4-dihydroxy-2,5-dihydro-3-heteryl-5-oxo-1h-pyrrol-1-yl-4-methyl benzenesulphanolamides with analgesic activity // 2626650
FIELD: chemistry.SUBSTANCE: invention relates to the field of organic chemistry, namely to the new methylbenzenesulfonamide derivatives of the formula (I) , where X=O, Ar=4-Me-C6H4 (a); X=O, Ar=4-Cl-C6H4 (b); X=NH, Ar=4-Cl-C6H4 (c).EFFECT: new compounds having analgesic activity were obtained.2 tbl, 4 ex
Connections of substituted triazolbronic acid // 2625801
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula (I): , wherein the residues R1, R1' and R1ʺ independently represent hydrogen, alkoxy, halogen or -CF3 group. The residue R2 it represents C1-7alkyl or phenyl, or a pharmaceutically acceptable salt thereof. Also pharmaceutical composition, using the compounds of formula I, and method of treatment are provided.EFFECT: compounds of formula I are inhibitors immunoproteasomal subunit LMP7, and may be useful in the treatment of inflammatory diseases and disorders such as rheumatoid arthritis, lupus and irritable bowel syndrome.13 cl, 1 tbl, 5 ex
Water-based liquid composition with bromfenac possessing preservative effectiveness // 2625755
FIELD: chemistry.SUBSTANCE: invention represents the use of bromfenac or its salt to improve the preservative effectiveness of the water-based liquid composition, comprising (a) bromfenac or its salt and (b) benzalkonium chloride, and c) at least one agent selected from the group consisting of nonionic surfactant and water-soluble polymer. The invention also relates to a method of improving the preservative effectiveness of the aqueous solution described above, which comprises adding of bromfenac or its salt in an amount of 0.1 w/v % to the solution.EFFECT: invention enables to obtain a composition with imroved preservative activity, wherein there are low concentrations of benzalkonium chloride preserving agent.10 cl, 21 tbl, 4 ex
Heterocyclic compounds and their application as glycogen synthase kinase-3 inhibitors // 2623427
FIELD: chemistry.SUBSTANCE: invention relates to a heterocyclic compound of formula , where A represents NRB, where RB represents hydrogen; X1 and X2 represent CR2 and X3, X4, X5 and X6 represent CR3 or CR4, or X1 and X2 represent CR2, X3 represent N, and X4, X5 and X6 represent CR3; Y1, Y2, Y3 and Y4 represent CR4 or CR5 or Y2 represents N, and Y1, Y3 and Y4 represent CR5; provided that no more than one of Y1, Y2, Y3 and Y4 represents CR4; and provided that one of Y1, Y2, Y3 and Y4 represents CR4 or C-CF3, if none of X3, X4, X5 and X6 represents CR4; R1 represents hydrogen; each R2 represents hydrogen; each R3 is independently selected from the group consisting of hydrogen, CN, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy and C1-C6-haloalkoxy; R4 represents a C-linked saturated or partially unsaturated monocyclic 5- or 6-member heterocyclic ring containing one heteroatom selected from O and N, as ring members, wherein the heterocyclic ring optionally has one N-linked substituent R8; R5 is selected from the group consisting of hydrogen, C1-C6-alkyl, C1-C6-haloalkyl and C3-C7-cycloalkyl; and R8 is selected independently on the case from the group consisting of C1-C6-alkyl, C1-C6-haloalkyl and C1-C6-alkoxycarbonyl. The invention also relates to pharmaceutical compositions based on a formula (I) compound, formula (I) compound application, a method of treatment of diseases susceptible to treatment by a compound that modulates the activity of 3β glycogen synthase kinase.EFFECT: new heterocyclic compounds useful for treatment of neurodegenerative disorders or inflammatory diseases are obtained.25 cl, 2 tbl, 70 ex
3-aryl-4a-isopropyl-4an-chromeno[6',7':4,5]furo[3,2-c][1,2]oxazine-8-ones with anti-inflammatory and analgetic activity // 2622768
FIELD: pharmacology.SUBSTANCE: invention relates to 3-aryl-4a-isopropyl-4aN-chromeno[6',7':4,5]furo[3,2-c][1,2]oxazine-8-ones of formula (I).EFFECT: new compounds of the formula with anti-inflammatory and analgesic activity were obtained.2 tbl, 9 ex

N-acylhydrasone derivatives for application as selective inhibitors of t-cells and medicines for lymphoneoplasia treatment // 2622651
FIELD: pharmacology.SUBSTANCE: invention relates to new compounds of formula 1, its (E)-stereoisomer or a pharmaceutically acceptable salt: [Formula 1]. The compounds can be used to prepare pharmaceutical compositions for diseases prevention or treatment, where the disease is a "graft versus host" (GVH) response after organ transplantation or hematopoietic stem cells, multiple sclerosis, rheumatoid arthritis or lymphoneoplasia.EFFECT: new compounds with inhibitory activity against T-cells are obtained.8 cl, 16 tbl, 143 ex, 5 dwg

Compound 8-fluorophthalazine-1(2h)-one as inhibitors of bruton tyrosine kinase // 2622391
FIELD: pharmacology.SUBSTANCE: compounds of 8-fluorophthalazine-1(2H)-ones of formula II are proposed, wherein one of X1, X2 and X3 represent N, and the other symbols have meanings defined in claim 1 of the invention formula, or stereoisomers, gautomers and pharmaceutically acceptable salts thereof. The compounds proposed inhibit the kinase Btk (Bruton tyrosine kinase) and can be used to treat immune disorders, such as inflammation, mediated by kinase Btk.EFFECT: increased efficiency while using the compounds of formula II for the diagnosis and treatment in vitro, in situ and in vivo such disorders in mammalian cells, or associated pathological conditions.25 cl, 8 dwg, 2 tbl, 69 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

Electromagnetic therapeutic device for physiotherapy complete with physiotherapy liquid // 2620907
FIELD: medicine.SUBSTANCE: group of inventions relates to medical equipment, namely to physiotherapy means complete with physiotherapy liquids. Electromagnetic therapy device has a frame and a medical bed. A plurality of upper magnetic heads is fixed to the frame by means of bearings a plurality of lower magnetic heads are installed on the therapeutic bed, each head is connected to a rotary unit and adapted to support a rotational motion independently of each other, wherein the upper magnetic heads are vertically fixed position so that they coincide with vertical positions of the lower magnetic heads and located opposite them. Rotary units provide lower magnetic heads rotation so that they rotate the upper magnetic heads using the magnetic attraction force. A physiotherapy suit with an opening equipped with a waterproof hermetic tap, is located on the bed. The physiotherapy suit is connected to the integrated prefabricated unit through which physiotherapy fluid is delivered, at that, a gasket is installed in the suit, and several natural tourmaline magnetic disks or metal briquettes are placed between the physiotherapy suit and the gasket. Physiotherapy liquid for the therapeutic electromagnetic device comprises a base fluid with Chinese medicine drugs additives, and includes glycerin and olive oil in a ratio of 1:1-1:3.EFFECT: use of inventions allows expansion of the magnetotherapeutic devices range.18 cl, 16 dwg

Hydrocortisone composition with controlled release // 2619869
FIELD: pharmacology.SUBSTANCE: invention relates to a pharmaceutical composition for oral administration, comprising a core containing hydrocortisone and a carrier, and a delayed release polymer layer in contact with the said core. The core contains microcrystalline cellulose in an amount of 75-85% by composition weight. The delayed release polymer is a mixture of a polymer (1) having a composition of poly(methacrylic acid, methyl methacrylate) at a ratio of 1:1, and a polymer (2) having a composition of poly(methacrylic acid, methyl methacrylate) at a ratio of 1:2. Polymers (1) and (2) are presented at a ratio of 1:4 and are taken in an amount of 6-7% by composition weight. Also a method for composition manufacture and its use for treating adrenal insufficiency is described.EFFECT: release of hydrocortisone in accordance with the circadian release of cortisol to reproduce natural cortisol release.39 cl, 7 dwg, 2 tbl, 4 ex
ethod for periodontal diseases treatment for patients with type ii diabetes mellitus // 2619847
FIELD: medicine.SUBSTANCE: for treatment of periodontal disease in patients with type II diabetes mellitus, an anti-inflammatory drug is administered. "Limontar" diluted in an aqueous alkaline medium is used as an anti-inflammatory drug, which is taken one pill 2-4 times a day 10-30 minutes before meals, for 10-14 days.EFFECT: effective treatment of periodontal disease at diabetes mellitus, and a possibility of method application for diabetic patients belonging to different risk groups.3 ex
Bruton's tyrosine kinase inhibitors // 2619465
FIELD: pharmacology.SUBSTANCE: compounds can be used as therapeutically active substances for the treatment of inflammatory and/or autoimmune conditions selected from rheumatoid arthritis and asthma. In formula I A is phenyl, n is 1 or 2, R1 is CH2NHC(=O)R1' or CH2NHC(=O)CH2NHR1', where n is 1. And one R1 is halogen, and the other R1 represents CH2NHC(=O)R1' or CH2N(CH3)C(=O)R1', when n is 2. R1' represents a lower alkoxy group, phenyl, an unsaturated or partially unsaturated 8-9-membered bicyclic heterocycle containing 1-2 heteroatoms in the bicyclic system selected from nitrogen and sulfur, or a 4-6-membered monocyclic heteroaryl with 1-3 heteroatoms selected from nitrogen, oxygen and sulfur, or a 4-5-membered heterocycloalkyl containing oxygen or nitrogen atoms as heteroatoms, optionally substituted by one or more R1". Each radical R1" is an independent lower alkyl, halogen, 3-6-membered cycloalkyl, 4-membered heterocycloalkyl with an oxygen atom as a heteroatom, lower alkyl-4-membered heterocycloalkyl with an oxygen atom as a heteroatom, oxo group, cyano-lower alkyl, hydroxyl-lower alkyl or lower alkoxy group. R2 is H, R3 or R4. R3 represents C(=O)OR3', C(=O)R3' or C(=O)NH(CH2)2R3'. R3' is H, a lower alkyl, 6-membered heterocycloalkyl with 1-2 heteroatoms selected from nitrogen and oxygen, an amino group or OH. R4' is a pyrasolyl possibly substituted with R4'. And R4' is a methyl, CH2-CH2N(CH3)2, CH2C(=O)OCH2CH3, CH2C(=O)OH or CH2CH2OH.EFFECT: increased efficiency of treatment.18 cl, 2 tbl, 51 ex
ethod of prophylaxis of post-traumotomic pain syndrome in oncosurgery // 2619212
FIELD: medicine.SUBSTANCE: for the prevention of post-thoracotomy pain syndrome (hereinafter - PTPS) in oncosurgery a day before the surgery, anticonvulsant pregabalin is administered orally 75 mg 2 times/day and 75 mg 2 hours before the operation. Then, an epidural catheter is performed on the operating table, through which a three-component mixture is infused throughout the operation: ropivacaine 3 mg/ml+fentanyl 4 mcg/ml+epinephrine 2 mcg/ml at a rate of 5-15 ml/h. Induction of anesthesia is intravenously: fentanyl 0.00004±0.00002 mg/kg, ketamine 0.29±0.13 mg, propofol 0.56±0.31 mg/kg, rocuronium bromide 0.68±0.14 mg/kg. Maintenance of anesthesia: sevoflurane inhalation 0.6-1 MAK in an oxygen-air mixture (FiO2 0.3-0.8), fentanyl 0.00004±0.00002 mg/kg/h, ketamine 0.0013±0.0002 mg/kg/hour. 40 minutes before the end of the operation, nefopam is administered with 20 mg IM. In the postoperative period, infusion is performed in the epidural space: ropivacaine 2 mg/ml+fentanyl 4 mcg/ml+epinephrine 2 mcg/ml, injection rate 4-6 ml/h for 2 days. Then, the mixture reduces the concentration of ropivacaine to 0.2% and continues infusion to 5-7 days, at a rate of 4-6 ml/h. At occurrence of the first complaints on painful sensations prescribe nefopam of 20 mg im/m and continue its appointment in a dose of 20 mg 2 times a day for 5 days and lornoxicam 8 mg intravenously - 2 times/day and pregabalin 75 mg orally - 2 times/day for 5 days. In case of ineffectiveness of this therapy, morphine is prescribed 10 mg IM.EFFECT: invention allows to reduce the frequency of development of acute PTPS, its intensity, to reduce the postoperative need for opioid analgesics and to reduce the frequency of development of chronic PTPS.2 ex
Bruton's tyrosine kinase inhibitors // 2618529
FIELD: pharmacy.SUBSTANCE: invention relates to a compound of general formula I, below, or a pharmaceutically acceptable salt thereof. In the formula I compound, X is halogen; Y is H or lower alkyl; R is -R1-R2-R3; R1; R1 is pyridyl; R2 is -C (= O) or is absent; R3 is morpholinyl or pyrrolidinyl, optionally substituted by a lower alkyl. The above compounds are used to modulate OMB activity and treat diseases associated with excessive OMB activity. Furthermore, these compounds are used for treatment of inflammatory and autoimmune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. The invention also relates to the pharmaceutical composition comprising a compound of formula I and at least one carrier, diluent or excipient.EFFECT: increased efficiency of compounds application.20 cl, 2 tbl, 7 ex
Transdermal system containing non-steroidal anti-inflammatory drug // 2618413
FIELD: medicine, pharmacy.SUBSTANCE: invention relates to medicine. A transdermal system is described comprising an adhesive layer composed of a transdermal preparation on a substrate, wherein the transdermal preparation comprises a) 10 to 40 wt % non-aqueous base material based on the total weight of the transdermal preparation, b) 1 to 10 wt % non-steroidal anti-inflammatory drug based on the total weight of the transdermal prepation and c) a polyethylene glycol component consisting of 0.3 to 5 wt % polyethylene glycol of low molecular weight based on the total weight of the transdermal preparation, and from 1 to 10 wt % polyethylene glycol of high molecular weight to based on the total weight of the transdermal preparation.EFFECT: document describes a transdermal system comprising a non-steroidal anti-inflammatory drug.7 cl, 7 tbl, 36 ex
Derivatives of 5-substituted quinazolinone, compositions containing them and methods of application thereof // 2617989
FIELD: pharmaceutics.SUBSTANCE: compounds of formula (I) R1 is halogen atom; (C1-C6) alkyl, optionally substituted with one or more halogen atoms; (C1-C6) alkoxy group, optionally substituted with one or more halogen atoms, or -(CH2)nNHRa, where Ra represents hydrogen atom; -C(O)-(CH2)n-phenyl or -C(O)-(CH2)n-pyridyl, where phenyl is optionally substituted with one or more substitutes of halogen atom; -SCF3; (C1-C6)alkyl, optionally substituted with one or more halogen atoms, or (C1-C6)alkoxy group, optionally substituted with one or more halogen atoms; -C(O)-(C1-C8)alkyl, where alkyl is optionally substituted with one or more halogen atoms; -C(O)-(CH2)n-(C3-C10-cycloalkyl); -C(O)-(CH2)n-NRbRc, where Rb and Rc are hydrogen atoms independently of each other; (C1-C6)alkyl; or phenyl, optionally substituted with one or more substitutes of halogen atom or (C1-C6)alkyl; -C(O)-(CH2)n-O-(C1-C6)alkyl; or -C(O)-(CH2)n-O-(CH2)n-phenyl; R2 is hydrogen atom; OH; phenyl or (C1-C6) alkyl, optionally substituted with one or more halogen atoms; R3 is hydrogen atom; or (C1-C6) alkyl; and n takes values 0, 1 or 2.EFFECT: method is disclosed of treating or controlling diseases or disorders, such as cancer involving administering 5-substituted quinazoline compound of formula (I) or its pharmaceutically acceptable salt, solvate or stereoisomer.32 cl, 59 ex

Diflunisal co-crystalline form // 2617849
FIELD: pharmacology.SUBSTANCE: diflunisal co-crystalline form with isoniazid is disclosed, wherein the molar ratio of diflunisal to isoniazid is 1:1, wherein the cocrystal has an endothermic spike from 148 to 152°C, according to measurement by differential scanning calorimetry, and spikes at 2θ(°) 5.9, 7.5, 8.5, 11.6, 15.1, 18.5, 26.6, according to measurement by powder X-ray diffraction.EFFECT: diflunisal co-crystalline form is obtained, suitable for use in the pharmaceutical industry as a pharmaceutical preparation component, used to relieve pain accompanied by inflammation, and symptomatic treatment of rheumatoid arthritis and osteoarthritis, with increased level of solubility in water by more than 5 times for diflunisal compared with values in pure form.7 dwg, 2 ex

Pyridone and aza-pyridone compounds and methods of use // 2617405
FIELD: chemistry.SUBSTANCE: invention relates to a compound selected from formula I, or its stereoisomers, or pharmaceutically acceptable salts thereof, where R1 is optionally substituted C1-C3 alkyl; R2, R3 and R4 are independently selected from H, F, Cl; R5 is selected from (i) optionally substituted C6-C20 aryl, selected from phenyl; (ii) optionally substituted C5-C20 heteroaryl, selected from pyrazolyl, pyridinyl, pyrimidinyl, tetrahydroisoquinolinyl, 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazinyl, 6,7-dihydro-4H-pyrazolo[5,1-c][1,4]oxazinyl, 4,6,7-trihydropyrazolo[3,2-c][1,4]oxazinyl, 5,6,7,8-tetrahydro-1,6-naphthyridinyl, 2,3-dihydro-1H-isoindolyl, 4,5,6,7-tetrahydrothiazolo[5,4-c]pyridinyl; (iii) optionally substituted -(C6-C20 aryl)-(C3-C20 heterocyclyl), where heterocyclyl is selected from azetidinyl, piperidinyl, morpholino, piperazinyl; (iv) optionally substituted -(C5-C20 heteroaryl)-(C3-C20 heterocyclyl), where heteroaryl is selected from pyridinyl and pyridazinyl and heterocyclyl is selected from azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, 1,4-diazepanyl, 2,6-diazaspiro[3.3]heptanyl, 7,9-diazabicyclo[3.3.1]nonanyl, hexahydropyrrolo[3,4-c]pyrrolyl, morpholino; (v) optionally substituted -(C5-C20 heteroaryl)-(C1-C6 alkyl), where heteroaryl is selected from pirazolyl and pyridinyl; or (vi) optionally substituted -(C5-C20 heteroaryl)-C(=O)-(C3-C20 heterocyclyl), selected from (pyridinyl)-C(=O)-(morpholino); R6 represents H or C1-C3 alkyl; Y1 and Y2 are independently selected from CR6 and N; where C1-C3 alkyl, C3-C20 heterocyclyl, C6-C20 aryl and C5-C20 heteroaryl optionally substituted with one to three groups, independently selected from D, F, Cl, Br, I, -CH3, -CH2CH3, -CH2CH(CH3)2, -CH2OH, -CH2CH2OH, -C(CH3)2OH, -CH2F, -OC(O)CH3, -COCH3, -NHCH3, -N(CH3)2, =O, -OH, -OCH3, -OCH2CH2N(CH3)2, -OP(O)(OH)2, -CH2OCH3, cyclopropyl, azetidinyl, 1-(methylazetidin-3-yl)oxy, N-methyl-N-oxetan-3-ylamino, azetidin-1-ylmethyl, oxetanyl and morpholino; where group (a), formed Z1, Z2, Z3, Z4, Z5, X and NC(O), forms structure, given in claim, and wherein wavy line indicates bonding point. Invention relates to a pharmaceutical composition for treating a condition, mediated by Bruton's tyrosine kinase, containing a compound of formula (I) and a pharmaceutically acceptable carrier, lubricant, a diluent or filler. Compounds of formula (I) are intended for use as a drug for treating cancer, mediated by Bruton's tyrosine kinase.EFFECT: pyridone and aza-pyridone compounds for treating disorders mediated by Bruton's tyrosine kinase (Btk).20 cl, 9 dwg, 4 tbl, 907 ex (а)
Drug with anti-inflammatory activity // 2617123
FIELD: pharmacology.SUBSTANCE: invention relates to a drug having an anti-inflammatory activity and comprising N-(2-hydroxyethyl)-3β-hydroxyurea-12-en-28-amide of formula as an active ingredient.EFFECT: a new effective drug with an anti-inflammatory activity is obtained.2 dwg, 1 tbl, 4 ex
Anti-inflammatory pharmaceutical compositions based on bacterial strain // 2616899
FIELD: pharmacy.SUBSTANCE: pharmaceutical composition exhibiting specific anti-inflammatory activity on experimental dysbiosis model consisting of strains of Bifidobacterium longum GT15, Lactobacillus rhamnosus K32, Enterococcus faecium L-3.EFFECT: increasing the effectiveness of the composition in the treatment of inflammatory bowel disease.18 dwg, 7 tbl, 5 ex

Therapeutic antibodies // 2616881
FIELD: biochemistry.SUBSTANCE: invention relates to biochemistry, namely to antibody specifically binding with second loop of human C5aR.EFFECT: invention provides effective treatment of diseases, for which anti-binding with C5aR is favorable.18 cl, 6 dwg, 10 tbl, 12 ex

ethod for preparing conjugate of hyaluronidase with derivatives of polyethylene piperazine and application of produced conjugate // 2616528
FIELD: pharmacology.SUBSTANCE: group of inventions relates to medicine, namely, to the process of preparing an active conjugate of hyaluronidase enzyme with copolymer using a carbodiimide method or azide method of conjugation, purification, concentration and freeze-drying (or dilution). The copolymer is a water soluble copolymer of N-oxide of 1,4-ethylene piperazine, (N-carboxymethyl)-1,4-ethylene piperazinium or its hydrazide, and 1,4-ethylene piperazine of the general formula: , where n is from 40% to 90% of the total units, m is from 3% to 40% of the total units, n+m+1=100% derived from poly-1,4-ethylene piperazine by oxidation, alkylation and, in the case of an azide method, hydrazinolysis. Also a drug having properties of suppressing hyperplasia of the connective tissue and anti-inflammatory effect is disclosed. It is obtained by one of the embodiments of the method in the form of a suppository, ointment, injection or cosmetic product.EFFECT: increased hyaluronidase activity, degree of conjugation, yield, drug storage stability.15 cl, 10 ex, 3 tbl, 2 dwg

Antiinflammatory pharmaceutical composition for topical use in form of cream with cylaytonum // 2616254
FIELD: pharmacology.SUBSTANCE: invention is an antiinflammatory pharmaceutical composition for topical use in the form of a cream comprising 0.05-2 wt % of cylaytonum as an active component, 30-34 wt % of water, 36-40 wt % of white petrolatum, 4-8 wt % of white beeswax, 16-22 wt % of propylene glycol, 2-6 wt % of phospholipin 90H and 0.005-0.04 wt % of preservative agent.EFFECT: stability at ambient temperature and toxicity reduction.11 cl, 14 tbl, 4 dwg

Hydrochloride of derivative purinona // 2615999
FIELD: chemistry.SUBSTANCE: invention relates to the unknown hydrochloride of 6-amino-9-[(3R)-1-(2-butinoil)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8 and its crystalline form. The compound has the properties of a selective inhibitor of Bruton's tyrosine kinase (Btk) and can be used as an agent for the prophylaxis and / or treatment of diseases associated with Btk involving B-cells and mast cells. Such diseases are allergic, autoimmune, inflammatory, embolic, bone disease or malignancy. The latter may be a non-Hodgkin's lymphoma. Crystals of hydrochloride of 6-amino-9-[(3R)-1-(2-butinoil)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8 have in the powder X-ray diffraction, at least, 2 or more peaks at angles 2θ selected from about 8.11, 8.43, 11.57, 12.73, 13.85, 14.20, 14.67, 14.91, 15.94, 16.64, 18.06, 19.74, 20.42, 21.05, 22.57, 23.21, 23.85 and 24.70 degrees. The hydrochloride crystalline form has an endothermic peak at the temperature of 216°C.EFFECT: said compound has a higher solubility and activity.10 cl, 4 dwg, 6 tbl, 13 ex
ethod for production of pharmaceutical composition with fexofenadine, providing anti-allergic and anti-inflammatory effect // 2614961
FIELD: pharmacy.SUBSTANCE: pharmaceutical composition for fexofenadine gel preparation contains the following auxiliary components: thickener - Carbopol, neutralizing agent - sodium hydroxide 5% solution, glycerin and purified water. First, a hydrophilic base is prepared - carbopol is mixed with glycerol at a ratio of 1:20, with vigorous stirring, purified water is added, and the resulting system is stirred until complete homogenization, fexofenadine is then dissolved in 5% sodium hydroxide solution, the resulting fexofenadine alkaline solution is gradually added to the hydrophilic base with vigorous stirring to obtain a gel composition with a pH of 6.5. The gel is stored at a temperature of 15÷25°C for 2 years, if an increased storage life of the gel composition is required, nipagin or benzalkonium chloride is introduced.EFFECT: fexofenadine gel has a high therapeutic efficacy with minimal side effects, and low cost.1 tbl, 4 ex
Analgesic peptide of sea anemone // 2614759
FIELD: biotechnology.SUBSTANCE: invention relates to biologically active peptide of sea anemone Metridium senile, having the following amino acid sequence H2N-Asnl-Ile2-Ile3-Val4-Gly5-Gly6-Cys7-Ile8-Lys9-Cys10-His11-Val12-Lys13-Asn14-Ala15-Ser16-Gly17-Arg18-Cys19-Val20-Arg21-Ile22-Val23-Gly24-Cys25-Gly26-Val27-Asp28-Lys29-Val30-Pro31-Asp32-Leu33-Phe34-Ser35-COOH. The peptide can be used as a medicament alone or in conjunction with other components to relieve pain conditions in humans and animals stipulated by participation of TRPA1 receptors, as well as for clarification of topology and molecular mechanisms of TRPA1 channels functioning, studying of TRPA1 channels distribution in living organisms, in test systems for detection and testing of new drugs against pain and/or inflammation, TRPA1 receptor agonists and antagonists, or for production of antibodies used for scientific and medical purposes.EFFECT: increase of analgesic effect by inhibiting the functional activity of ion channel TRPA1.10 dwg, 13 ex
Novel efficient inhibitor of kinase 4, associated with interleukin-1 (irak4) // 2613973
FIELD: chemistry.SUBSTANCE: invention relates to a compound of N-(6-((1-((2-ethylpyrimidin-5-yl)methyl)piperidin-4-yl)methyl)pyridin-2-yl)-5-methylthiazol-2-amine or its pharmaceutically acceptable salt, solvate or hydrate. Compound according to invention is intended for preparing a pharmaceutical composition for treating and/or preventing a pathological condition, associated with aberrant activity of IRAK4 kinase. Pharmaceutical composition for treating and/or preventing a pathological condition, associated with aberrant activity of IRAK4 kinase, is characterized by that it contains a therapeutically effective amount of compound according to invention and pharmaceutically acceptable carrier, solvent and/or filler. Pathological condition associated with aberrant activity of IRAK4 kinase is an immune inflammatory disease or oncological disease.EFFECT: technical result is production of N-(6-((1-((2-ethylpyrimidin-5-yl)methyl)piperidin-4-yl)methyl)pyridin-2-yl)-5-methylthiazol-2-amine or its pharmaceutically acceptable salt, solvate or hydrate as a selective IRAK4 kinase inhibitor.13 cl, 10 dwg, 2 tbl

Aminoindane compounds and use thereof in treating pain // 2612959
FIELD: chemistry.SUBSTANCE: invention relates to novel aminoindane compounds of formulae (I) or (II): , where: A is phenyl or a monocyclic aromatic 5- or 6-member ring containing 1 or 2 heteroatoms selected from N and S; R1 and R4 are independently C1-C6 alkyl or CH2CH2OH; or R1 and R4 are combined to form a 4-6-membered carbocyclic or saturated 5- or 6-member monocyclic group containing one additional ring heteroatom, such as O; R2 is independently selected from a group consisting of halogen; R3 is independently selected from a group consisting of halogen and C1-C-6 alkyl; or q equals 2, and two R3 groups are bonded to form a saturated 5- or 6-member monocyclic group containing 1–2 oxygen atoms; m is ranges from 1 to 3; n ranges from 1 to 3; p ranges from 0 to 2; q ranges from 0 to 2; and X- is a halogen, trifluoroacetate, sulphate, etc, as well as methods of producing and using said compounds. Methods involve administering a compound of formula (I) or (II) and a TRPV1 receptor activator.EFFECT: said compounds can find application in treating pain and/or itching.14 cl, 8 tbl, 11 dwg, 59 ex
Dioxino- and oxazin-[2,3-d]pyrimidine compounds as phosphoinositide 3-kinase inhibitors and methods for use thereof // 2612251
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula I , which are used as inhibitors of phosphoinositide 3-kinase (PI3-kinase), having anticancer activity, anti-inflammatory activity or immunoregulatory properties.EFFECT: technical result is obtaining novel compounds of formula I, as well as pharmaceutical compositions based thereon, which can be used for producing a drug for treating cancer, in particular, cerebral cancer.23 cl, 1 tbl, 41 ex
Liposome composition for inflammatory joint diseases relief // 2611998
FIELD: pharmacy.SUBSTANCE: invention is represented by a liposome composition for inflammatory joint diseases relief, comprising dipalmitoylphosphatidylcholine, cholesterol, hydrocortisone acetate, prednisolone hemisuccinate and saline, at that, the components are in a certain ratio, in g.EFFECT: high anti-inflammatory effect and rapid beneficial effect.2 ex
Pharmaceutical ketorolac-based composition in form of nasal spray and method for preparation thereof // 2611659
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutical industry and represents a pharmaceutical composition in form of nasal spray, having analgesic and anti-inflammatory activity, characterized by the fact that it comprises tromethamine ketorolac as an active substance and additives: phenoxyethanol as a antimicrobial preserving agent and antiseptic, poloxamer 407 as a humidifier, disodium edetate as a chelating agent, sodium hydroxide and potassium dihydrogen phosphate as a buffer mixture and a pH regulator and water for injections, wherein ingredients of composition are taken in certain ratio, wt%.EFFECT: invention ensures increased storage life after primary opening up to 20 days, in conditions of a refrigerating chamber, and at room temperature, wider range of nasal sprays, having analgesic and anti-inflammatory activity, as well as storage life of 2 years.2 cl, 7 tbl
Thiazolpyrimidines // 2610840
FIELD: pharmaceutics.SUBSTANCE: invention relates to compound of formula I, where R1 is phenyl optionally including from 1 to 3 of following groups as substitutes: C1-6-haloalkyl, C1-6-alkoxy group, C1-6-alkylsulphonyl or R1'; R1' represents pyrrolidinyl or spiroheterocycloalkyl selected from 8-oxy-3-azabicyclo[3.2.1]octane derivatives or 2-oxy-6-azaspiro[3.3]heptane, each of them optionally contains R1ʺ as substitute; R1ʺ is C1-6-alkyl; B is phenyl, pyridinyl, pyrrolidinyl or piperidinyl; X is OH, C1-6-alkoxy group, NHC(=O)Y, C(=O)NH2, C(=O)NHY, C(=O)X', C(=O)Y, CH2NHY, CH2CH2Y, CF=CHY, CH=CHY, CH2OH, C(=O)NHCH2CH2N(CH3)2 or C(=O)NHCH2CH2Y; X' is OH or C1-6-alkoxy group; Y is heterocycloalkyl, consisting of one ring containing from 5 to 7 ring atoms and containing 1 or 2 N atoms, phenyl or monocyclic or bicyclic heteroaryl containing from 6 to 9 ring atoms, containing at least one aromatic or partially unsaturated ring containing from 5 to 6 ring atoms including 1 or 2 N atoms, each of them optionally contains one or two substitutes Y3; Y3 is hydroxy group, C1-6-alkyl, C1-6-alkoxy group, oxo group, amino group, amide group, C(=O)NH(CH3), C(=O)OH, C(=O)OY4 or heteroaryl, selected from oxadiazolyl or triazolyl, possibly containing one or two C1-6-alkyl groups as substitute, oxo groups or SH; Y4 is C1-6-alkyl; or its pharmaceutically acceptable salts. Invention also relates to pharmaceutical composition with inhibiting activity in relation to splenic tyrosine kinase (SYK), including therapeutically effective amount of compound of formula I, mixed with at least one pharmaceutically acceptable carrier, excipient or thinner.EFFECT: thiazolpyrimidines effective in treating disorders associated with SYK.14 cl, 2 tbl, 68 ex
Use of meadowsweet (filipendula) extracts for treating and preventing chronic pain // 2608442
FIELD: pharmaceutics.SUBSTANCE: present invention relates to pharmaceutical industry, namely to agent for treating chronic pain without recognized organic reasons. Extract of meadowsweet (Filipendula ulmaria) is intended for treating chronic pain without recognized organic causes, wherein extract is obtained by extraction of aboveground parts of meadowsweet (Filipendula ulmaria) with 50–70 % ethanol. Therapeutic agent for treating chronic pain without recognized organic reasons.EFFECT: agents described above are effective for treating chronic pain without recognized organic reasons.2 cl, 2 dwg, 2 ex
Anti-inflammatory composition with prolonged action for treating airway // 2608126
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutical industry and concerns anti-inflammatory composition for treating upper airways. Anti-inflammatory composition for treating upper airway in form of tablets containing echinacea dry extract, evkalimine, colloidal silicon dioxide, sodium stearyl fumarate, dextrose monohydrate, taken in certain amount.EFFECT: composition described above, in form of tablets, has high pharmaceutical activity with respect to treating upper airways, it is stable during storage.1 cl, 1 tbl, 2 ex
Rectal suppositories with analgesic action // 2607661
FIELD: medicine.SUBSTANCE: invention relates to medicine, in particular to drugs, and can be used for production of rectal suppositories for relieving of pain of various origin: postoperative pain, vertebrogenic radicular pain, arthritis, cancer pain, cardialgia, headache, dysmenorrhea, kidney and liver colics. Rectal suppositories proposed by authors have analgesic action and contain preparation of non-steroidal row and base, differing by fact, that preparation of non-steroidal row contains ketorolac and additionally contains amitriptyline, while base contains silicon glicerolates in 3-molar excess of glycerine composition Si(C3H7O3)4⋅3C3H8O3 and polyethylene glycol PEG-4000 with following ratio of components, calculated in g per one suppository: ketorolac 0.021÷0.031, amitriptyline 0.003÷0.008, PEG-4000 1.793÷1.804, silicon glicerolates 0.768÷0.773.EFFECT: production of rectal suppositories.1 cl, 2 tbl, 2 ex

ultiple emulsion // 2607597
FIELD: pharmaceutics.SUBSTANCE: invention refers to pharmaceutical and cosmetic industry and represents multiple emulsion for application of at least one pharmaceutical or cosmetic active substance, which includes external aqueous phase W1, oil phase O, dispersed in external aqueous phase, and inner aqueous phase W2 dispersed in oil phase O, where in inner aqueous phase W2 there is at least one electrolyte, selected from group of alkali and alkali-earth metals halides and sulphates, and at least one hydrophilic active substance, where multiple emulsion is characterized by, that external aqueous phase W1 contains hydrophilic emulsifier, which is ethylene oxide and propylene oxide polymer, oil phase O is formed by triacylglycerols and contains lipophilic emulsifier from dimeticones group, and hydrophilic active substance, which is oligonucleotide having sequence according to SEQ ID No: 1 – SEQ ID No: 148 or SEQ ID No: 150.EFFECT: invention provides high stability, efficient protection of active substances against external effects and protection against microorganisms damages.20 cl, 1 tbl, 3 dwg

New pharmaceutical composition containing nsaid and cyclodextrin // 2607592
FIELD: medicine.SUBSTANCE: invention refers to medicine and consists in liquid composition for treating sore throat, containing 1–5 % wt/vol. of flurbiprofen; 5–10 % wt/vol. of cyclodextrin; up to 5 % wt/vol. of buffer agents and 80–90 % wt/vol. of water.EFFECT: technical result consists in physically and chemically pure stable solution of flurbiprofen of sufficient concentration, solution has no undesirable taste and does not contain alcohol as auxiliary solvent.21 cl, 5 ex, 2 tbl, 5 dwg
Sulfonamide derivative and medicinal use thereof // 2607081
FIELD: chemistry; pharmaceutics.SUBSTANCE: invention relates to novel sulfonamide derivatives of general formula (1) or pharmaceutically acceptable salts thereof, possessing the properties of inhibition integrin α4β7. In general formula (1) (1), A means a group presented by general formula (2-1) or (2-2) , where Arm is a 5- or 6-member aromatic ring, containing 0, 1 or 2 heteroatoms, selected from nitrogen atoms, R1 and R11, each, independently, represents any substitute selected from a hydrogen atom, halogen atom, lower alkyl group, lower alkoxy group, mono- or di-lower alkylamino group, R12, R13 and R14, each, independently, represents any substitute selected from a hydrogen atom, lower alkyl group, lower alkoxy group, amino group, lower alkylamino group, low di(alkyl)amino group or (lower alkylamino)lower alkyl group, R2 and R3, each, independently, represents any substitute selected from a hydrogen atom, lower alkyl group or lower alkoxy group, B is represents any substitute selected from lower alkoxy group, optionally substituted by hydroxyl group, lower alkyl group, mono- or di-lower alkylamino group; C3-C6cyclic alkoxy group and/or 6-member(s) heterocyclic(s) group (groups) with an oxygen atom, sulphur atom or a nitrogen atom as heteroatom, hydroxyl group, R41 is represents a hydrogen atom or lower alkyl group, a, b, c and d, each, independently, represents C-R31, C-R32, C-R33 and C-R34 respectively, but one or two of a, b, c and d, each, can be a nitrogen atom, R31, R32, R33 and R34, each, independently, represents any substitute selected from a hydrogen atom, halogen atom, lower alkyl group, lower alkoxy group, provided that any R31, R32, R33 and R34 represents a halogen atom or lower alkyl group, e, f, g and h, each, independently, represents C-R35, C-R36, C-R37 and C-R38 respectively, however, one or two of e, f, g and h, each, can be a nitrogen atom, R35, R36, R37 and R38, each, independently, represents any substitute selected from a hydrogen atom, lower alkyl group or lower alkoxy group, D represents a phenyl group or a 5 -or 6-member aromatic heterocyclic group, containing a nitrogen atom, an oxygen atom or sulphur atom, optionally containing a substitute(s), selected from a group consisting of hydroxyl groups, lower alkyl groups, lower alkoxy groups, E is a 5- or 6-member heterocyclic group with 1-4 heteroatoms, selected from nitrogen atoms, an oxygen atom and sulphur atom in the cycle, optionally containing a substitute(s), selected from a group consisting of halogen atoms, hydroxyl groups, lower alkyl groups, lower alkoxy groups, amino groups, 4- or 6-member cyclic amino groups, carboxyl groups and lower alkoxy-carbonyl groups; aminocarbonyl group, optionally containing a substitute(s) selected from the group, consisting of hydroxyl groups, lower alkyl groups, lower alkoxy groups, 5- or 6-member heterocyclic groups, containing 1, 2, 3 or 4 heteroatoms, selected from a group consisting of oxygen atoms, sulphur atoms and nitrogen atoms as a component(s) ring atom(s), and substituted by heterocycle of lower alkyl groups, where heterocycle means a 5- or 6-member heterocyclic groups, containing 1, 2, 3 or 4 heteroatoms, selected from group consisting of oxygen atoms, sulphur atoms and nitrogen atoms as a component(s) ring atom(s); hydrogen atom, hydroxyl group, lower alkyl group, lower alkoxy group, amino group, lower alkyl-carbonyl group, lower alkyloxy-carbonyl group or a lower alkylaminoalkilen group, and provided that the lowest alkyl-carbonyl group and the lowest alkyloxycarbonil group can be, each of which, are connected to a phenyl group, presented D, to form condensed ring.EFFECT: compounds can be used for treating or preventing an inflammatory disease, in which the pathological condition associated with indirect by integrins α4β7 adhesion process.15 cl, 2 tbl, 258 ex

Purified extract separated from pseudolysimachion rotundum var subintegrum with high content of active ingredient, its production and composition containing the above extract as an active ingredient to prevent or treat inflammation, allergies and asthma // 2606768
FIELD: pharmaceutics.SUBSTANCE: invention refers to pharmaceutical industry, namely, to the purified extract, broken up using butanol (ATS1) from the Pseudolysimachion rotundum var subintegrum extract. Purified extract broken up using butanol (ATS1) from the Pseudolysimachion rotundum var subintegrum extract, for the prevention and treatment of inflammatory diseases, received in accordance with the method comprising: addition of ethanol to the dried Pseudolysimachion rotundum var subintegrum and carrying out the extraction with cold water; further carrying out the extraction with hot water under reflux with the receipt of the 1st extract at the 1st stage; suspending of said 1st extract in water, adding butanol to said extract, fractionation with obtaining a water layer and butanol layer and the collection of butanol layer with the receipt of purified extract, broken up using butanol (ATS1), under certain conditions, wherein obtain a extract containing verprozid, veratric acid, katalpozid, pikrozid II, izovanilloilkatalpol and 6-O-veratroilkatalpol in certain proportions (versions). A pharmaceutical composition. Functional food product.EFFECT: above described extract Pseudolysimachion rotundum var subintegrum has increased anti-inflammatory effect.4 cl, 15 dwg, 10 tbl, 8 ex

Pharmaceutical composition // 2606510
FIELD: pharmaceutics.SUBSTANCE: present invention relates to compounds of formula (I), in which one of R1a and R1b is hydrogen and the other is methyl; or R1a and R1b together form a cyclopropyl ring; R2 denotes methyl or monofluoromethyl, difluoromethyl or trifluoromethyl; R3 denotes methyl; R4 denotes hydrogen, halogen, monofluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy, monofluoromethoxy, difluoromethoxy or trifluoromethoxy; R5 denotes hydrogen, halogen, monofluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy, monofluoromethoxy, difluoromethoxy or trifluoromethoxy; R6 is hydrogen; R7 means hydrogen; and X denotes oxygen; or pharmaceutically acceptable salts thereof.EFFECT: compound of formula (I) inhibit the transmission of PGE/EP4 signal and can be used for treating autoimmune pathologies, such as rheumatoid arthritis, multiple sclerosis, psoriasis, cancer and other; invention also relates to pharmaceutical compositions containing these compounds, and methods for using them in the case of individuals in need of treatment.50 cl, 2 dwg, 3 tbl, 113 ex
Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as trka kinase inhibitors // 2606131
FIELD: pharmaceutics.SUBSTANCE: invention relates to compounds of formula I given below, or to their stereoisomers, tautomers or pharmaceutically acceptable salts thereof. R1, R2, Ra, Rb, Rc, Rd, X, Y, B, and ring C are as defined by the invention formula. Wherein the Y-B moiety and the NH-C(=X)-NH moiety are in the trans configuration.EFFECT: compounds of formula I are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.56 cl, 31 tbl, 649 ex
ethod of producing anti-inflammatory agent version 4 // 2605285
FIELD: medicine.SUBSTANCE: present invention relates to a method of preparing an anti-inflammatory agent from herbal raw material. Method includes the following: the aboveground part of Geranium albiflorum Ledeb. ((Geranium krylovii Tzvel.) - white-flowered geranium (Krylov's geranium)) is dried and cut into 2-3 mm sized particles; then the extraction is carried out in china-ware for 30-35 minutes while stirring; the extraction uses 60 % ethanol, the mass ratio is 1:20; then the extract is filtered through a paper filter; the filtrate is evaporated to dryness in china-ware at atmospheric pressure and temperature of 55-60 °C.EFFECT: invention extends the range of anti-inflammatory agents.1 cl, 1 ex

Analgesic and anti-inflammatory agent based on 5-butyl-6-hydroxy-2-methyl pyrimidine-4(3h)-one // 2605265
FIELD: medicine.SUBSTANCE: invention refers to medicine and pharmacy and represents analgesic and anti-inflammatory agent, containing 5-butyl-6-hydroxy-2-methylpyrimidine-4(3H)-one as active substance.EFFECT: agent is low-toxic, exhibits considerably higher anti-inflammatory and analgesic activity than preparations of comparison, widely used in medicine.1 cl, 4 ex

Pharmaceutical composition for inflammation and pain and its preparation method (versions) // 2604149
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutical combination and to pharmaceutical composition and, in particular, to combination of analgesic and anti-inflammatory agent, selected from ketorolac and meloxicam, and pharmaceutically acceptable carriers or excipients.EFFECT: present invention also relates to use of said composition for preparation of drug, which can be used for treating pain and inflammation.11 cl, 2 ex, 9 tbl, 8 dwg
 
2550874.
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