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

A   Human necessities(312083)
A61P29                 Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; non-steroidal antiinflammatory drugs (nsaids)(1454)
2-aminopyrasine derivatives as csf-1r kinase inhibitors // 2642777
FIELD: pharmacology.SUBSTANCE: invention relates to a compound that is an amino acid or ester of an amino acid of formula , or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against CSF-1R kinase. In formula (I), ring A is a phenyl group; R1 and R2 independently represent a hydrogen atom, a halogen atom or an unsubstituted C1-4 alkyl; n is 1; X is NH; V is -N=, W is -C(Z)=; Z represents a hydrogen atom, a fluorine atom, a chlorine atom or unsubstituted C1-3 alkyl; ring B is a 1,4-phenylene, 1,3-phenylene or pyridinyl group; [Linker] is a -(CH2)m-X1-(Alk1)x-Y1 group, where m is 0, 1, 2 or 3; x is 0 or 1; Alk1 is an unsubstituted C1-3 alkylene group; X1 and Y1 independently represent a bond, -O-, -S-, -NR7th-, -C(=O) - or -C(=O)NR5-, where R5 is a hydrogen atom or C1-4 alkyl and R7 is a hydrogen atom, unsubstituted C1-4 alkyl or -C(=O)CH3; R is a group of formula or , in which R8 is a -COOH group or an ester group of the formula -(C=O)OR14, where R14 is R15R16R17C-, where any R15 represents a hydrogen atom or C1-3alkyl-(Z1)a-[(C1-C3)alkyl]b-, where a and b are independently 0 or 1, Z1 is -O-, -S- or -NH-, R16 and R17 independently represent a hydrogen atom or C1-3 alkyl- or R15 and R16, taken together with the carbon atom to which they are attached, form a 3-7-membered cycloalkyl ring; and R17 represents a hydrogen atom; where (i) R9 and R10 are side chains of natural amino acids, (ii) one of R9 and R10 represents a hydrogen atom or unsubstituted C1-4 alkyl, and the other is an unsubstituted C1-6 alkyl group or C1-6 alkyl group substituted by a C1-4 alkoxy group, or (iii) R9 and R10, taken together with the carbon atom to which they are attached, form a saturated spiro-cyclobutyl ring; R11 represents a hydrogen atom or an unsubstituted C1-2alkyl group; ring D is a 5- to 7-membered saturated heterocyclyl group with at least one nitrogen atom in the ring. The invention also relates to a pharmaceutical composition, a method of treatment or prevention of diseases or disorders mediated by CSF-1R kinase, as well as application of the said compounds for preparation of a medicament useful for treatment of such diseases.EFFECT: increased application efficiency.18 cl, 59 ex

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

Fusion serpine polypeptides and methods for their application // 2642310
FIELD: biotechnology.SUBSTANCE: invention relates to the field of fusion proteins for serine proteases inhibition, and can be used in medicine. Fusion proteins having at least one human alpha-1 antitrypsin (AAT) polypeptide operably linked to an immunoglobulin Fc polypeptide having an amino acid sequence that is at least 98% identical to the amino acid sequence of SEQ ID NO:6 are obtained.EFFECT: invention allows to obtain a fusion polypeptide capable of effectively inhibiting the activity of serine proteases and thereby alleviating the symptoms of diseases or disorders associated with overexpression or serine protease activity in a subject in need thereof.18 cl, 4 dwg, 4 ex
ethod for endometritis treatment in cows // 2642251
FIELD: veterinary medicine.SUBSTANCE: ozonized autoblood as an immunomodulating and etiotropic agent is infused intramuscularly for four times in increasing-decreasing doses of 50, 75, 100, 75 ml at an interval of 48 hours, after obtaining from a vein, the blood is prepared by mixing in a syringe with 15 mg of sodium citrate and 10 mg of ozone in a ratio of 1:1 for 25 seconds, and Endometramag K is injected intramuscularly in an amount of 100.0 ml at an interval of 48 hours until recovery.EFFECT: increased effectiveness of therapeutic measures in case of endometritis and reduced period of the disease.2 tbl
Biaryl derivatives as agonists gpr120 // 2641003
FIELD: pharmacology.SUBSTANCE: invention relates to diaryl derivatives of the formula 1 , or their pharmaceutically acceptable salts or isomers of formula 1, wherein A and B are independently phenyl or pyridine provided that when B is phenyl, -G-COOR7 is substituted in the para-position of phenyl and, when B is pyridine, -G-COOR7 is substituted in position 3 of pyridine, any of R1-D and R2-E may be absent, D and E are independently carbon, nitrogen, oxygen or sulfur, or represent a direct bond, and any of R1 and R2 may be absent, or R1 is a halogen, C1-C6-alkyl, optionally substituted with halogen, C3-C10-cycloalkyl, C1-C6-alkoxy, C1-C6-alkylamino, C3-C10-heterocycloalkyl or C1-C6-alkyl-C3-C10-heterocycloalkyl, C3-C10-cycloalkyl, optionally substituted by C3-C10-alkylsilanyloxy or hydroxy, C2-C6-alkenyl, C2-C6-alkynyl, C3-C10-heterocycloalkyl, optionally substituted by C1-C6-alkylamino or halogen, C1-C6-alkyl-C3-C10-heterocycloalkyl, phenyl, C3-C9-heteroaryl or C1-C6-alkyl-C5-C6-heteroaryl, R2 is hydrogen, halogen, C1-C6-alkyl, optionally substituted with halogen, C3-C10-cycloalkyl, C1-C6-alkoxy, C1-C6-alkylamino, C3-C10-heterocycloalkyl or C1-C6-alkyl-C3-C10-heterocycloalkyl, C3-C10-cycloalkyl, optionally substituted with C3-C10-alkylsilaniloxy or hydroxy, C2-C6-alkenyl, C2-C6-alkynyl, C3-C10-heterocycloalkyl, optionally substituted with C1-C6-alkylamino or halogen, C1-C6-alkyl-C3-C10-heterocycloalkyl, phenyl, C3-C9-heteroaryl or C1-C6-alkyl-C5-C6-heteroaryl and, when D and E represent nitrogen or carbon, R1 and R2 may represent two or three groups, which may be the same or different, isolated from C1-C6-alkyl or phenyl, G is -J-(CR5C6)p, where J is oxygen or sulfur, R5 and R6 independently represent hydrogen, C1-C6-alkyl or C3-C10-cycloalkyl and R5 and R6, substituted in the one and the same or different carbon atoms, may be bound producing C3-C10-cycloalkyl, R1 and R4 independently from each other may be absent depending on m and n value or independently represent hydrogen, halogen or C1-C6-alkyl, or C1-C6-alkoxy, R7 is hydrogen or C1-C6-alkyl, m and n independently represent an integral number from 0 to 5 and p is an integral number from 2 to 6, where heterocycloalkyl and heteroaryl contain at least one heteroatom, isolated from N, O, and S, to the pharmaceutical composition, containing them, and method of its production.EFFECT: stimulates the formation of GLP-1 in the gastrointestinal tract and improves insulin resistance in the liver or muscles, effective prevention or treatment of diabetes, complications of diabetes, obesity, non-alcoholic fatty hepatosis, steatohepatitis, osteoporosis or inflammation.6 cl, 1 tbl, 279 ex

Antibodies against nerve growth factor and methods for their production and application // 2640254
FIELD: biotechnology.SUBSTANCE: invention relates to a method for production of antibodies suitable for use in cats that are specifically associated with the cat nerve growth factor (NGF) and neutralise the ability of the cat NGF to contact the cat NGF p75 or TrkA receptor and the corresponding antibodies. To implement this method, a donor antibody is obtained from a species other than a cat, the donor antibody having a binding specificity for the target antigen present in cats. Then, each amino acid residue in the sequence of the framework regions of the donor antibody is compared to each amino acid residue present at the corresponding position in the sequence of the framework regions of cat antibodies pool. Then, the identified amino acid residues in the donor antibody are replaced with the amino acid residues present at the corresponding position in the pool of cat antibodies. The resulting antibody does not contain any amino acid foreign at the corresponding position in cats, at any position within the framework regions. This invention also discloses a pharmaceutical composition and a kit containing the said antibodies for treatment of pain in cats, in particular pain associated with arthritis or osteoarthritis immune-mediated rheumatoid arthritis.EFFECT: decrease or loss of antigen-binding activity is avoided.16 cl, 17 dwg, 16 tbl, 11 ex

Antibodies against nerve growth factor and methods for their production and application // 2640252
FIELD: biotechnology.SUBSTANCE: invention relates to a method for production of antibodies suitable for use in horses that are specifically associated with the horse nerve growth factor (NGF) and neutralise the ability of the horse NGF to contact the horse NGF p75 or TrkA receptor and the corresponding antibodies. To implement this method, a donor antibody is obtained from a species other than a horse, the donor antibody having a binding specificity for the target antigen present in horses. Then, each amino acid residue in the sequence of the framework regions of the donor antibody is compared to each amino acid residue present at the corresponding position in the sequence of the framework regions of horse antibodies pool. Then, the identified amino acid residues in the donor antibody are replaced with the amino acid residues present at the corresponding position in the pool of horse antibodies. The resulting antibody does not contain any amino acid foreign at the corresponding position in horses, at any position within the framework regions. This invention also discloses a pharmaceutical composition and a kit containing the said antibodies for the treatment of pain or an NGF-induced tumour in horses.EFFECT: decrease or loss of antigen-binding activity is avoided.12 cl, 11 dwg, 8 tbl, 10 ex

Derivatives of azaindasole or diazaindasole type for pain treatment // 2640046
FIELD: pharmacology.SUBSTANCE: invention relates application of a compound of formula for treatment or prevention of pain associated with at least one Trk protein. The radicals and symbols in formula (I) have the definitions indicated in the claims. The invention also relates to a pharmaceutical composition comprising a compound of formula (I) as an active substance.EFFECT: compound application efficiency increase.15 cl, 6 dwg, 1 tbl, 35 ex
Hetero-aromatic methylic derivative of cyclic amine // 2639869
FIELD: chemistry.SUBSTANCE: invention relates to a compound represented by the formula (IA), where X1 and X2 are the same or different and are a nitrogen atom or a CH group; Y is any structure from the following group of formulas (a); n is 1 or 2; R1 is a hydrogen atom, a halogen atom or a C1-6 alkyl group; R2 is a triazolyl group or a pyrimidinyl group; R3 is a hydrogen atom or a halogen atom; and R4 is a hydrogen atom or a C1-6 an alkyl group; or a pharmaceutically acceptable salt thereof. The invention also relates to a compound represented by the formula (I), where X1 and X2 are the same or different and are a nitrogen atom or a CH group; any one of Y1 and Y2 is a nitrogen atom, and the other is CH; n is 1 or 2; R1 is a hydrogen atom, a halogen atom or a C1-6 alkyl group;R2 is a triazolyl group or a pyrimidinyl group; R3 is a hydrogen atom or a halogen atom; and R4 is a hydrogen atom or a C1-6 alkyl group; or a pharmaceutically acceptable salt thereof. The compounds of the invention are intended for the production of a pharmaceutical composition having antagonistic activity against OX1 and OX2 orexin receptors.EFFECT: hetero-aromatic methyl derivative of cyclic amine, which has antagonistic activity against OX1 and OX2 orexin receptors.9 cl, 6 tbl, 85 ex

Fusion polypeptide containing wap domain and their application methods // 2639526
FIELD: biotechnology.SUBSTANCE: fusion proteins having at least one polypeptide of the human secretory inhibitor of leukocyte proteases (SLPI) operably linked to an immunoglobulin Fc fragment polypeptide having an amino acid sequence that is at least 98% identical to the amino acid sequence of SEQ ID NO:10 are obtained.EFFECT: invention allows to obtain a fusion polypeptide capable of effectively inhibiting the activity of neutrophilic serine proteases and thereby alleviating the symptoms of diseases or disorders associated with overexpression or serine protease activity in a subject in need thereof.15 cl, 4 dwg, 4 ex

Crystalline forms of grapiprant // 2638931
FIELD: pharmacology.SUBSTANCE: invention relates to the crystalline form of grapiprant selected from the group consisting of Form X, Form X2, Form X3, Form F, Form K, Form L, Form M and Form N.EFFECT: new crystalline form of grapiprant, as well as pharmaceutical compositions suitable for treatment of pain, inflammation, arthritis and cancer, and methods to obtain them.8 cl, 13 tbl, 23 dwg, 12 ex

edicinal dosage form, which contains 6'-fluor-(n-methyl-or n,n-dimethyl)-4-phenyl-4,9'-dihydro-3'n-spiro[cyclohexane-1,1'-pyrano[3,4, b]indole]-4-amine for neuropathic pain treatment // 2638818
FIELD: pharmacology.SUBSTANCE: method comprises oral administration of a dosage form containing a pharmacologically active agent according to the general formula wherein R is -H or -CH3, or a physiologically acceptable salt thereof, once a day, to a subject in need thereof. The dosage form provides immediate in vitro release of the pharmacologically active agent, which is contained in a dose of 40 to 190 μg, and the pharmacokinetic parameter tmax is in the range of 4 to 6 hours.EFFECT: good bioavailability and sufficiency of pain relief, high tolerability and safety.12 cl, 5 dwg, 15 tbl, 3 ex

Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods for application // 2638552
FIELD: pharmacology.SUBSTANCE: invention relates to pyrazol-4-yl-heterocyclylcarboxamide compounds of Formula I , including their stereoisomers, tautomers and pharmaceutically acceptable salts, wherein X is a thiazolyl, pyrazinyl, pyridinyl or pyrimidinyl group, R1 and R2 have the meanings indicated in the claims. The compounds of formula I are useful for Pim kinase inhibition and for treatment of disorders such as cancer mediated by Pim kinase. Methods for application of formula I compounds for in vitro, in situ and in vivo diagnosis, prevention or treatment of such diseases in mammalian cells or acssociated pathological conditions are disclosed.EFFECT: increased efficiency of treatment.26 cl, 4 tbl, 528 ex

Derivative cyclic amine and its pharmaceutical application // 2638549
FIELD: pharmacology.SUBSTANCE: invention refers to derivatives if cyclic amine of formula (I), where A is a group, represented by the general formula (IIa), (IIb) or (IIc), where A is a group, provided by the general formula (IIa) or (IIb), R1 represents an alkyl group containing 1 or 2 carbon atoms and optionally substituted by a hydroxyl group, amine group or carboxyl group, R2 represents a hydrogen atom, R3 is a hydrigen atom or alkyl group containing 1 or 2 carbon atoms, R4 is a hydrogen atom or an alkylcarbonyl group, containing 2 carbon atoms, or an alkyl group, containing 1 or 2 carbon atoms and optionally substituted by alkylcarbonylamine group, containing 2 carbon atoms, and n is 1 or 2, in which, when R3 and R4, each independently represent an alkyl group, containing 1 or 2 carbon atoms, R1 represents an alkyl group containing 1 or 2 carbon atoms and substituted by a hydroxyl group, amine group or carboxyl group; and when A is a group, represented by the general formula (IIc), R1 represents an alkyl group, containing 1 carbon atom and substituted by a carboxyl group, R2 represents a hydrogen atom and X represents CH2, O or -NR5 and R5 is an alkyl group, containing 1 carbon atom. Also, the invention relates to a prodrug of the compound of formula (I), pharmaceutical, analgetic agent and therapeutic agent based on compounds of formula (I), or its prodrug.EFFECT: new derivatives of imidazol, useful in the treatment of pain, have been obtained.11 cl, 24 dwg, 5 tbl, 73 ex
Arylcycloalkylamines derivatives neuroprotector (versions), substances with combined neuroprotector, analgetic and antidepressive action, pharmaceutical compositions based thereon // 2637928
FIELD: pharmacology.SUBSTANCE: invention relates to new arylcycloalkylamines of the general formula . In the general formula (I), R1, R2 are H, linear or branched alkyl (C1-C4), linear or branched alkoxy (C1-C4), halogen; Y is -CH2-O-CH2-, - (CH2)n-, where n: 1-3; X is -CO-NH-(CH2)6-, -CO-(CH2)k-, -CH2-NH-(CH2)6-, -CH(CH3)-NH-(CH2)6-, -(CO)p-(CHR5)m, where p, m-: 0, 1, k: 2, 4-7, R5: H, linear alkyl C1-C5; R3, R4 are H, linear alkyl C1-C4, -CH2-C≡CH, -(CH2)2-O-(CH2)2-NH2, cyclopropyl, cyclopropylmethyl; 4-pyridinyl, an amino acid residue of a proteinogenic acyclic or aromatic α-amino acids, γ-aminobutyric acid, ε-aminocaproic acid, β-alanine; -CHR6-CH2-OR7, where R6: H or a linear or branched alkyl C1-C4, benzyl, R7: H, linear alkyl C1-C4, or R3, R4 together with the nitrogen to which they are attached, form a pyrrolidine, 2-(hydroxymethyl) pyrolidine, 4-aminopyridinium ring; G is (C1-C4) carboxylic acid, methanesulfonic acid or a mineral acid or water. As an acyclic or aromatic α-amino acid residue, they contain a proteinogenic α-amino acid residue. As (C1-C4) carboxylic acid, they contain at least one compound from the group consisting of acetic, fumaric, succinic, tartaric, malic and maleic acids. As a mineral acid, they contain at least one compound from the group consisting of hydrochloric, phosphoric, sulfuric acids. The preferred compounds are arylcycloalkylamine derivatives of the general formula , wherein Y: -CH2-O-CH2-, -(CH2)2-. The invention also relates to a pharmaceutical composition which can be a combination of arylcycloalkylamine derivatives and at least one substance from the group comprising levodopa, palmitoyle ethanolamide, N-(2-aminoethyl) palmitamide hydrochloride, rasagiline, risperidone, toloxaton, quetiapine, gamma-aminobutyric acid, sodium valproate, amitriptyline, clomepramine, fluoxetine, paroxetine, sertraline, phenylephrine, dexamethasone, prednisolone. The composition may be in the form of a tablet, capsule, pellet, powder for preparation of a solution for enteral administration, a solution for parenteral administration, a powder for preparation of a solution for parenteral administration.EFFECT: neuroprotective, analgesic and antidepressant action.11 cl, 13 tbl, 96 ex
ethod for production of preparation with anti-inflammatory activity // 2637414
FIELD: pharmacology.SUBSTANCE: method for production of an agent having anti-inflammatory activity, including garden burnet triple extraction with ethyl alcohol, filtering, evaporation, concentration and drying of the alcohol extract, at that, garden burnet herb crushed to a particle size of 2.0 mm is used, extraction is done by 70% alcohol at 90°C at raw materials - extractant ratio of 1:50 within 2 h, at that, this first extraction is performed for 60 minutes, the second and the third - for 30 minutes.EFFECT: increased anti-inflammatory activity of the agent.5 tbl, 2 ex

ethods and applications of inhibitors of proprotein convertase subtilisin/kexin, type 9 (pcsk9) // 2636820
FIELD: medicine.SUBSTANCE: proprotein convertase subtilisin/kexin 9 (PCSK9) is administered to a subject in need thereof, wherein the PCSK9 inhibitor is an antibody or an antigen-binding fragment thereof. Also, PCSK9 application is proposed for manufacture of a medicament for sepsis or septic shockr treatment. A pharmaceutical composition and a commercial package containing the PCSK9 inhibitor.EFFECT: possibility of treatment of a patient with sepsis or septic shock at doses suitable for intensive care.21 cl, 5 dwg, 7 tbl

Drug with anti-inflammatory action // 2636818
FIELD: pharmacology.SUBSTANCE: agent with anti-inflammatory action, representing a polyextract, consisting of dry extracts of sallow thorn fruit, long red pepper fruit, Ural licorice root, broad leaved Echinops roots, dwarf apple fruit taken in a ratio, wt parts: 2:2:1:1:1, obtained in a certain way.EFFECT: drug is effective for treatment and prevention of inflammatory diseases.1 dwg, 4 tbl
Hydrohalogenide of 1-(3,4-dimethoxyphenyl)-2-(7,8-dimethyl-2,3,4,5-tetrahydro-1,3]diazepino[1,2a]benzimidazole-11-yl)ethanone with analgesic and anxiolytic activity // 2636785
FIELD: pharmacology.SUBSTANCE: invention relates to organic chemistry, namely to a hydrohalogenide of 1-(3,4-dimethoxyphenyl)-2-(7,8-dimethyl-2,3,4,5-tetrahydro[1,3]diazepino[1,2-a]benzimidazole-11-yl)ethanone of formula 1 , which has both analgesic and anxiolytic activity.EFFECT: new heterocyclic compound possessing the effective biological properties is obtained.2 cl, 3 tbl, 1 ex

odified antibodies composition, methods of production and application // 2636046
FIELD: medicine, pharmacy.SUBSTANCE: group of invention objects refers to the field of biotechnology. An activated antibody is proposed, comprising a) an antibody or antigen binding fragment (AB), binding to the epidermal growth factor receptor (EGFR); b) masking part (MM), which inhibits the specific AB binding with EGFR in the unsplit state, but does not prevent its binding or compete for binding to EGFR in the split state; c) a split part (CM), which acts as a substrate for the protease; and d) linkers (L1 and L2). The activated antibody in the unsplit state has a structure from N-terminus to C-terminus (MM)-L1-(CM)-L2-(AB) and is activated in the target tissue,localized together with the target and protease for CM. A composition for treatment of tumors, autoimmune diseases or inflammatory diseases or for angiogenesis inhibition; application of the activated antibody for medicament preparation; methods for activated antibody preparation and the isolated nucleic acid molecule comprising the nucleotide sequence of the activated antibody are also described.EFFECT: invention provides more efficient delivery of activated antibodies to the target cells and may find further application in medicine.30 cl, 36 dwg, 60 tbl, 19 ex
Drug based on 5-amino-2,3-dihydrophthalazine-1,4-dione as quick-soluble film for transbuccal introduction // 2635769
FIELD: pharmacology.SUBSTANCE: drug in the form of easily soluble biocompatible film for transbuccal application includes a therapeutically effective amount of pharmacologically active agent, such as a salt of alkaline or alkaline-earth metal 5-amino-2.3-dihydrophthalazine-1.4-dione as a waterless salt or its monohydrate or dihydrate, or their mixtures, mucoadhesive film forming polymer plasticiser and taste flavour, represented by a mixture of β-cyclodextrin or modified β-cyclodextrin with sorbitol when their mass ratio of 4:1-1:2, the content of the specified mixture in the film is 15-40 wt % of the weight of the entire film.EFFECT: increased release speed of the pharmacologically active agent when applying the film, increased transparency, uniformity and stability in storage while retaining elasticity and strength.16 cl, 5 tbl
Preservative-free topical composition, including hyaluronic acid // 2635473
FIELD: pharmacology.SUBSTANCE: invention is a topical composition for stimulation of skin or mucous membranes scarring, containing less than 1 CFU/ml of aerobic flora and free of preservatives, which contains, based on the total weight of the composition: at least 0.1 wt % of hyaluronic acid, a mixture of low molecular weight hyaluronic acid having a molecular weight of 600 to 1,000 kDa, and a high molecular weight hyaluronic acid having a molecular weight of 800 to 1,200 kDa, the said high molecular weight hyaluronic acid has a higher molecular weight than the said low molecular weight hyaluronic acid; at least one agent for skin scarring and water. The invention provides a composition where the high molecular weight hyaluronic acid enhances scarring by its film-forming effect, while the low molecular weight hyaluronic acid, due to its penetrability, enhances composition components penetration into tissues.EFFECT: improved healing properties, improves the epidermis structure and accelerates the differentiation of the granulation tissue.7 cl, 2 ex, 2 tbl

Cycloalkane derivative // 2635354
FIELD: pharmacology.SUBSTANCE: invention provides a compound represented by the formula , or a pharmacologically acceptable salt thereof, where Ar1 and Ar2: a heteroaryl group or an aryl group; R1, R2 and R3: a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group or a cyano group; R4 and R5: a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a hydroxyl group or a C1-C6 alkoxy group; N: an integer between 1 and 3; and the heteroaryl group or aryl group optionally contains one or two groups, independently selected from a halogen atom, a C1-C6 alkyl group, an amino group, and when a heteroaryl group or aryl group contains two such groups, the two groups are the same or different.EFFECT: increased efficiency of treatment.33 cl, 5 dwg, 8 tbl, 179 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

Compositions and methods for treatment of chronic inflammation and inflammatory diseases // 2635188
FIELD: pharmacology.SUBSTANCE: group of inventions refers to an oral pharmaceutical composition with anti-inflammatory activity, to a method for preparation of the said composition, to application of an oral pharmaceutical composition for manufacture of a medicament for treatment of chronic inflammation, to application of an oral pharmaceutical composition for treatment of chronic inflammation, and to a method for treatment of an individual with chronic inflammation. The pharmaceutical composition comprises: a) a non-steroidal anti-inflammatory drug (NSAID), which is a propionic acid derivative that has a log P value greater than 2.0; b) 0.01-15 vol. % of a pharmaceutically acceptable solvent, wherein the solvent is a pharmaceutically acceptable liquid polyethylene glycol polymer; and c) at least 50 vol. % of a pharmaceutically acceptable hydrophobic lipid adjuvant, wherein the pharmaceutically acceptable hydrophobic lipid adjuvant consists of a fatty acid triglyceride, a fatty acid diglyceride and a fatty acid monoglyceride, wherein the pharmaceutical composition is prepared so as to be in a solid state at a temperature of 15°C or lower and has a melting point of 25°C or higher.EFFECT: group of inventions allows the delivery of a therapeutic chemical compound with anti-inflammatory activity so that it more effectively inhibits the anti-inflammatory response, which ultimately increases the effectiveness of chronic inflammation treatment.16 cl, 4 dwg, 7 tbl, 10 ex

New compounds for selective histone deacetylase inhibitors and pharmaceutical composition including such compounds // 2634694
FIELD: pharmacology.SUBSTANCE: invention relates to new compounds of formula I, their optical isomers or pharmaceutically acceptable salts that can be used for treatment of diseases mediated by histone deacetylase. In formula I, A is , Xa and Xb are CH, L1 and L2 independently hydrogen, -F, -Cl, -Br or -I, Q is C(=O), Y is selected from the group consisting of , and , M is C, O or N, l and m are independently 0 or 1, each of Ra1 and Ra2 is independently hydrogen; hydroxy; linear or branched -C1-4-alkyl, etc., n is 0, 1 or 2, Rb is hydrogen; hydroxy; linear or branched -C1-6-alkyl, etc., Z is selected from the group consisting of , etc., where each of Pa and Pb is independently ; hydrogen; hydroxy; linear or branched -C1-4-alkyl, etc., where is selected from phenyl, pyridine, pyrimidine, thiazole, indole, indazole, etc., each of x, y and z is independently 0 or 1, and each of Rg1, Rg2 and Rg3 is selected independently from hydrogen; hydroxy; -C1-3-alkyl, etc. The invention also relates to a pharmaceutical composition comprising compounds of formula I, a method for treatment of diseases mediated by histone deacetylase and application of said compounds for drugs preparation.EFFECT: increased effeciency of compound application.9 cl, 7 dwg, 16 tbl, 173 ex
Analgesic means // 2634618
FIELD: pharmacology.SUBSTANCE: invention relates to an analgesic means in which individual substituted quinoline-4(1H)-ones of general formula 1 their salts or compositions based on them are active substances, and which can be used as an anesthetic to treat humans and animals, where R1 = phenyl unsubstituted or substituted by one substituent selected from alkyl (C1-C4), alkoxy (OC1-OC4), halogen; phenyl substituted by two substituents selected from methyl, ethyl, methoxy, ethoxy or halogen; unsubstituted naphthyl, unsubstituted thienyl or thienyl substituted by one substituent selected from methyl or halogen; unsubstituted furyl, C4-alkyl, OMe; R2+R3 = =O, =NOMe, R4=H, COOMe, COOH; R5= H, Me; R6th= H, Me, OMe, Et, halogen; R7th= H, halogen, CN; R8= H, alkyl (C1-C4), halogen, CN.EFFECT: expansion arsenal of anesthetic means.2 tbl, 7 ex

ethod for preparation of drug with anti-inflammatory action // 2634570
FIELD: pharmacology.SUBSTANCE: methodfor preparation of a drug with an anti-inflammatory action that is a dry extract obtained by three-fold extraction of plant material: pomegranate fruits, cinnamon bark, cardamom fruits, long pepper fruits, ginger root, apple fruits, elecampane roots, coriander fruits, licorice fruits that ground to a particle size of 1 mm and extracted with 50% ethyl alcohol in a raw material:extractant ratio of 1:(14-16), at a temperature of 60°C and constant stirring, with the 1st and 2nd extraction carried out for 60 minutes, the third extraction for 30 minutes, the combined extracts are evaporated to 1/3 of the original volume and purified by separation, the purified extract is doped to 1/5 of the original volume, dried in a vacuum drier at a temperature of 60°C for 8 hours, ground in a propeller-type mill and a preparation with a glycyrrhizic acid content of at least 20% is obtained.EFFECT: means obtained by the above-described method has an increased anti-inflammatory effect.1 dwg, 10 tbl, 3 ex

Aptamer against ngf and its application // 2633510
FIELD: biotechnology.SUBSTANCE: invention relates to an aptamer specifically binding to a nerve growth factor (NGF), and can be used in medicine as an anti-inflammatory or analgesic. The invention allows to obtain an aptamer capable of forming a secondary structure represented by the formula (I), where N is nucleotid selected from the group consisting of A, G, C and U. Each of N14 and N24, N31 and N41, and N39 and N49 forms a Watson-Cric base pair, and the remaining nucleotides of formula (I) are capable of forming a stalk structure.EFFECT: invention provides an aptamer capable of inhibiting NGF activity at IC50 1 nM or less.5 cl, 5 dwg, 5 tbl, 18 ex
edicinal for vaginal application, with antiviral, antimicrobial, antifungal, antiprotozoal, antiinfectious, immunomodulating and antiinflammatory action, as ointment, gel, suppository // 2633056
FIELD: pharmacology.SUBSTANCE: medicament is presented comprising active substances, excipients and a consistently-forming base, characterized by comprising fluconazole, metronidazole, alpha- or beta- or gamma-recombinant interferon as active substances, disodium edetate and boric acid as adjuvants, and substances selected from the group: macrogol 400, macrogol 1500, macrogol 4000, vitepsol, glycerin, cocoa butter, paraffin, lanolin, vaseline, acetylphthalyl, GL type solid fat as a consistently forming base, wherein the drug components are in a specific ratio in g per 1 g of the agent.EFFECT: high therapeutic effect ensures rapid substances entry into the blood.1 cl

Dyetered diaminopyrimidine compounds and pharmaceutical compositions containing such connections // 2632907
FIELD: pharmacology.SUBSTANCE: invention relates to novel deuterated diaminopyrimidines of the general formula (I) and their pharmaceutically acceptable salts. In the general formula (I) R1a, R1b, R1c, R2a, R2b, R2c, R3, R4, R6, R7, R9, R10, R11, R12, R13a, R13b, R13c, R14a, R14b, R14c, R15a, R15b, R15c, R16, R17a, R17b, R18a, R18b, R19a, R19b, R20a and R20b independently hydrogen or deuterium; R5 is hydrogen, deuterium or halogen, R8 Represents a halogen; Provided that at least four of R1a, R1b, R1c, R2a, R2b, R2c, R3, R12, R13a, R13b, R13c, R14a, R14b, R14c, R19a, R19b, R20a or R20b are deuterium. The invention also relates to a process for the preparation of compounds of general formula (I) by reacting compound A6 with compound XV and to intermediates A6 and XV. In this case, in compound A6 R10, R11, R12, R13a, R13b, R13c, R14a, R14b, R14c, R15a, R15b, R15c, R16, R17a, R17b, R18a, R18b, R19a, R19b, R20a or R20b are independently selected from deuterium or hydrogen and at least one of them is deuterium; In compound XV R1a, R1b, R1c, R2a, R2b, R2c, R3, R4, R6, R7, R9 are independently selected from hydrogen or deuterium and at least one of them is deuterium; and R5 is hydrogen, deuterium or halogen; and R8 represents a halogen; X2 is selected from F, Cl, Br, I.EFFECT: compounds have ALK protein kinase inhibitory properties and can be used to treat or prevent cancer, impair cell proliferation, cardiovascular diseases, inflammation, infection, autoimmune diseases, organ transplantation, viral diseases, cardiovascular diseases or metabolic diseases.18 cl, 4 dwg, 1 tbl
Heterocyclic amines and their application // 2632900
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula (III) or a pharmaceutically acceptable salt thereof, wherein W is S; Y is N; X is N; R1 is selected from (a) C1-C6 alkyl optionally substituted with amino, methylamino, dimethylamino, C1-C6 alkoxy or isoindolyl; (B) -NR8R7, -CH2NR7R8, where R7 and R8 are joined to form optionally substituted C3-C7 non-aromatic ring which is pyrrolidine, morpholine, piperazine, piperidine, 1,4-diazepane, azepane, azetidine, 2-azabicyclo[2.2.1]heptane or 2,5-diazabicyclo[2.2.1]heptane and optionally substituted by one or more C1-C6alkyl, C1-C6alkoxy, methoxyethyl, 1-methoxypropane, isopropyloxymethyl, isopropyloxyethyl, -C(O(CH2)-methyl, -C(O)(CH2)-O-isopropyl, C1-C6haloalkyl, -S(O)2-methyl, -S(O)2-isopropyl, oxo, -C(O)(C1-C2)alkyl-N(methyl)2, -C(O)(C2)alkyl-(pyrrolidine), t-butyl-C(O)- or phenyl; or (c) -O-(tetrahydro-2H-pyran); each of R2, R3 and R5 are hydrogen; R4 is selected from C3-C6cycloalkyl, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl and optionally substituted heteroaryl selected from pyridine, pyrazole, pyridazine, pyrimidine. The said heteroaryl is optionally substituted with 1 to 2 substituents selected from C1-C6 alkyl and CN. The invention also relates to specific compounds as defined in the claims. The compounds of the invention are intended for the manufacture of a pharmaceutical composition having an inhibitory activity against an interleukin 1 receptor associated kinase 1 (IRAK-1) and an interleukin 1 receptor associated kinase 4 (IRAK-4). The compounds of the invention are also useful in a method for treatment of a disorder sensitive to inhibition of IRAK-1-mediated signalling.EFFECT: heterocyclic amines having inhibitory activity against an interleukin 1 receptor associated kinase 1 and interleukin 1 receptor associated kinase 4.24 cl, 4 tbl, 431 ex
Amide derivatives as ttx-s blockers // 2632899
FIELD: chemistry.SUBSTANCE: invention relates to the amide derivatives of formula ,where A is selected from the group consisting of phenyl, benzoimidazolyl, dihydroisoquinoline, indole, indazole, pyrazolyl, pyrazinyl, pyridazinyl, pyridyl, chinoline, sochinila and thiazolyl; B is selected from the group consisting of chemical bond, -C1-6alkylene-, -O-C1-6alkylene- and -NR7-; W is hydrogen or C1-6 alkyl; Z represents a nitrogen atom or CH; R1 represents a fluorinated substituent, independently selected from the group consisting of -CF3, -CHF2, -OCF3, -OCHF2, -OCH2CHF2, -OCH2CF3, -OCF2CHF2, -OCF2CF3, -OCH2CH2CF3, -OCH(CH3)CF3, -OCH2C(CH3)F2, -OCH2CF2CHF2, -OCH2CF2CF3, -OCH2CH2OCH2CF3, -NHCH2CF3, -SCF3, -SCH2CF3, -CH2CF3, -C (CH3)2CF3, -CH2CH2CF3, -CH2OCH2CF3, -OCH2CH2OCF3, 4,4-difluoropiperidino and (4-fluorobenzyl) oxy; R2 is independently selected from the group consisting of: (1) hydrogen, (2) halogen, (3) hydroxyl, (4) -On-C1-6 alkyl, where specified alkyl is unsubstituted or substituted by one or more of the substituents independently selected from R7, (7) -On-phenyl or -On-naphthyl, where specified phenyl or naphthyl is unsubstituted or substituted by one or more of the substituents independently selected from R7, and (10) -NR8R9; where n represents 0 or 1; if n=0, a chemical bond is present instead of-On-; p represents 1, 2, 3, or 4; if p is two or more than two, R2 may be the same or different; R3 and R4 independently represent hydrogen or C1-6 alkyl; R5 is independently selected from the group consisting of: (1) hydrogen, (2) halogen, and (3) -On-C1-6 alkyl, where specified alkyl is unsubstituted or substituted by one or more of the substituents independently selected from R7, where n represents 0 or 1; if n=0, a chemical bond is present instead of -On-; q represents 1, 2, or 3; if q is equal to two or more than two, R5 may be the same or different; R6 independently represents hydrogen, C1-6 alkyl, C2-6alkenyl, C3-7 cycloalkyl, phenyl, or heterocyclic group, which is unsubstituted or substituted by one or more of the substituents independently selected from halogen, hydroxyl, C1-6alkyl and -O-C1-6 alkyl; R7 is selected from the group consisting of: (1) hydrogen, (2) halogen, (3) hydroxyl, (4) -(C=O)m-Ol-C1-6 alkyl, where specified alkyl is unsubstituted or substituted by one or more of the substituents independently selected from R10, (9) -(C=O)m-Ol-heterocyclic group, where this heterocyclic group is unsubstituted or substituted by one or more of the substituents independently selected from R10, and (11) -NR8R9, where l=0 or 1 and m=0 or 1; if l=0 or m=0, a chemical bond is present instead of-Ol- or -(C=O)m -, and if l=0 and m=0, a chemical bond is present instead of -(C=O)m-Ol-; R8 and R9independently represent hydrogen or C1-6 alkyl, which is unsubstituted or substituted by one or more of the substituents independently selected from halogen, hydroxyl, C1-6alkyland -O-C1-6 alkyl; or R8 forms a 4-7-membered ring with R9, which may contain a nitrogen atom, an oxygen atom, a sulfur atom, a carbonyl or a double bond, where a 4-7-membered ring is not optionally substituted with 1-6 substituents independently selected from the group consisting of: (1) hydrogen, (2) hydroxyl, (3) halogen, (4) C1-6 alkyl, which is unsubstituted or substituted by one or more of the substituents independently selected from R10, and (6) -O-C1-6 alkyl, which is unsubstituted or substituted by one or more of the substituents independently selected from R10; R10 is independently selected from the group consisting of: (1) hydrogen, (2) hydroxyl, and (3) halogen, which possess activity relative to blocking the potential-dependent sodium channels, such as TTX-S.EFFECT: method for producing amido derivatives is improved.14 cl, 3 tbl

Treatment of malignant and non-malignant diseases with ras antagonists // 2632097
FIELD: pharmacology.SUBSTANCE: group of inventions is a Ras antagonist represented by the formula R1-R2-R3-R4, where: R3 is S; R4 is farnesyl or geranyl-geranyl, wherein geranyl-geranyl has the structure :R2 is a 5-membered heterocyclic ring containing one S heteroatom; R1 is C(=O)R5, CO2M; R5 is hydroxyl; M is a salt forming an organic or inorganic counterion; and R8is hydrogen or C1-C4 alkyl; and pharmaceutically acceptable salts thereof; or R1 is a 5-membered heterocyclic ring containing 2-4 N heteroatoms and R2 is a phenyl ring; or R2 is a 5-membered heterocyclic ring containing three heteroatoms selected from N and S, and R1 is C(=O)R10, and R10 is hydrogen, hydroxyl or C1-C4 alkyloxy. The invention also relates to a method for inhibition of Ras-induced cell proliferation associated with a malignant or non-malignant disease, comprising Ras antagonist administration to a patient.EFFECT: increased efficiency of treatment.20 cl, 9 ex, 7 dwg
Ethyl ether of 2-(((z)-amino((z)-2,4-dioxo-5-(2-oxo-2-phenylethylidene)pirrolidine-3-yliden)methyl)amino)-4,5,6,7-tetrahydrobenzo[b]thiophencarboxylic acid with analgetic activity // 2631649
FIELD: pharmacology.SUBSTANCE: invention relates to 2-(((Z)-amino((Z)-2,4-dioxo-5-(2-oxo-2-phenylethylidene)pyrrolidin-3-ylidene)methyl)amino)-4,5,6,7-tetrahydrobenzo[b]thiophenecarboxylic acid of formula 1 , which has analgesic activity.EFFECT: compound with a high yield is obtained, which has a pronounced analgesic activity, as well as low toxicity.1 tbl, 1 ex

Dosed drug form containing 6-fluoro-(n-methyl- or n,n-dimethyl-)-4-phenyl-4', 9'-dihydro-3'n-spiro[cyclohexane-1,1'-pyrano[3,4,indole]-4-amine for nociceptive pain treatment // 2631481
FIELD: pharmacology.SUBSTANCE: invention relates to the dosed drug form for oral introduction once per day, which contains 6-fluoro-(N-methyl-, or N,N-dimethyl)-4-phenyl-4'-19'-dihydro-3'N-spiro[cyclohexane-1,1'-pyrano[3,4,b]indole]-4-amin or a physiologically acceptable salt thereof, an anionic surfactant, selected from a group consisting of sodium lauryl sulfate, sodium cetyl sulfate, sodium sulfate cetyl stearyl, sodium sulfate stearyl and sodium dioctylsulfosuccinate to treat nociceptive pain.EFFECT: increased efficiency.7 cl, 3 ex, 15 tbl, 5 dwg

Crystalline forms of [(s)-1-carbamoyl-2-(phenylpyrimidin-2-ylamino)ethyl]amide 2-(2-methylaminopyrimidin-4-yl)-1h-indole-5-carbonic acid // 2631320
FIELD: chemistry.SUBSTANCE: invention relates to the novel polymorph 1 ((S)-1-carbamoyl-2-(phenylpyrimidin-2-ylamino)ethyl]amide 2-(2-methylaminopyrimidin-4-yl)-1H-indole-5-carboxylic acid and method for its preparation. Polymorph 1 of the compound has the properties of IkB kinase inhibitors and can be used for the treatment of inflammatory, immunologically or metabolically mediated acute and chronic arthritis, arthropathies, rheumatoid arthritis, degenerative joint diseases, spondylosis, diabetes II type, inflammatory bowel disease, loss of cartilage following joint trauma or a relatively long period of joint immobilization after meniscus or patella injuries or torn ligaments, or diseases of the connective tissue, m algy or disorders of bone metabolism, and also for the treatment of pain, including acute pain and chronic pain. Polymorph 1 has characteristic reflections in a powder X-ray diffraction pattern using CuK-alpha1 radiation in the reflection mode at 2 theta angles (in degrees) of 14.9±0.2, 19.4±0.2, 19.7±0.2, 20.0±0.2, 22.3±0.2, 25.0±0.2. The method of producing polymorph 1 involves heating the polymorph 2 of mentioned compound in a mixture of acetone and water to a temperature of 50 to 60°C, cooling the mixture to a temperature of 20 to 25°C and precipitate precipitation. In this case polymorph 2 has a characteristic x-ray powder reflection using CuK-Alpha1 radiation reflection mode with 2 Theta angles (degrees): 5.8±0.2, 6.7±0.2, 9.3±0.2, 11.2±0.2, 16.5±0.2, 18.1±0.2, 19.4±0.2, 22.1±0.2, as well as indicators of DSC peaks 222.1±1; 248.1±1; 251±1 at heating rate 10°C/minute.EFFECT: polymorphic form 1 is thermodynamically stable, has low hygroscopicity and stability.8 cl, 2 tbl, 5 dwg

Selective inhibitors of cycloxygenase and method for their production // 2631317
FIELD: pharmacology.SUBSTANCE: invention relates to selective inhibitors of the enzyme of cyclooxygenase-2 (COX-2) of the class of substituted 3(2H) -furanones of the general formula and and substituted phenanthro[9,10-b]furan-3(2H)-ones of the general formula , as well as a pharmaceutical composition based thereon. These compounds are effective selective inhibitors of cyclooxygenase-2 (IC50 to 0.004 μg ml, SI to 690).EFFECT: treatment of chronic forms of arthritis, migraine, trauma, skin diseases, inhibition of angiogenesis and inhibition of cell growth in certain cancers such as neuroblastoma, breast, stomach, lung and large intestine cancers.15 cl, 4 tbl, 9 ex, 14 dwg

Cyclosporin analogs molecules modified by 1 and 3 amino acids // 2630690
FIELD: pharmacology.SUBSTANCE: invention relates to cyclosporin-A analogs containing modifications of substituents at amino acids positions 1 and 3, according to the following Formula (I) .EFFECT: compounds have an affinity for cyclophilin, including cyclophilin-A, and reduced immunosuppressive activity compared to cyclosporin-A and its analogs modified only by position 1.22 cl, 1 dwg, 5 tbl, 26 ex

Use of arsenic compounds for pain management and inflammation treatment // 2630574
FIELD: medicine.SUBSTANCE: pharmaceutical composition containing sodium metaarsenite (NaAsO2) in a therapeutically effective amount to reduce pain not associated with cancer in a mammal, and its use in the manufacture of a pharmaceutical composition are proposed.EFFECT: combination of safety benefits, long time staying in blood and wide distribution in tissues.18 cl, 1 tbl, 12 dwg

eans with anti-inflammatory and analgetic action // 2629607
FIELD: pharmacology.SUBSTANCE: means is a complex of flavonoids isolated from the aerial part of the Lychnis chalcedonica L. plant by 5-fold extraction with 70% ethanol at a feedstock:extractant ratio of 1:22.5, followed by extraction with n-butanol, purification of the precipitate from the aqueous fraction by ethyl acetate-ethanol solvent systems at ratios of 5:1 and 3:1.EFFECT: marked anti-inflammatory and analgesic effect.2 dwg, 3 tbl, 2 ex
Nonsteroid anti-inflammatory agent on basis of naproxen with low gastrotoxicity // 2629367
FIELD: pharmacology.SUBSTANCE: invention relates to a new naproxen derivative of the formula (I) , 3-((S)-2-(6-methoxynaphth-2-yl)propanoyloxy)-4.5-bis(((S)-2-(6-methoxynaphth-2-yl)propanoyloxy)methyl)-2-methylpyridinium(S)-2-(6-methoxynaphth-2-yl)propanoate.EFFECT: high anti-inflammatory, analgesic and antipyretic activity, low acute toxicity and gastrotoxicity.7 tbl, 2 ex

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
 
2551315.
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