Method for preparing agent showing anti-inflammatory action

FIELD: medicine.

SUBSTANCE: method for preparing an agent showing anti-inflammatory action involves an alkali treatment of terrestrial peat and extraction in the alcohol-chloroform mixture. The terrestrial peat preliminarily ground and dried is milled in the AGO planetary activator before the extraction in the presence of solid alkali and sodium percarbonate for 1 min.

EFFECT: method enables higher antioxidant and anti-inflammatory activity of the terrestrial peat agent by increasing a yield of the extractive biologically active substances.

3 ex

 

The invention relates to medicine, specifically to pharmacology, and relates to a method of obtaining biologically active substances and tools based on them, have anti-inflammatory action.

As anti-inflammatory drugs are widely used synthetic drugs, but they can cause side effects such as nephrotoxicity, ototoxicity, neurotoxicity and allergic reactions.

Means of plant origin contain a wide range of biologically active substances and do not have contraindications and side effects.

Known anti-inflammatory agents and methods for their preparation of plant materials: the leaves of kamalii (Patent No. 2206333), the aboveground part of panzarini woolly (Patent No. 2372934, Patent No. 2160599), leaves of burdock felt (Patent No. 2171680), grass knotweed (Patent No. 2064300), leaves and stems meadowsweet (Patent No. 2210380), leaf willow (Patent No. 2189828), leaves and stems of nettle (Patent No. 2376025). Data anti-inflammatory drugs are similar in scope, but differ in the method of production, which includes the raw material preparation stage: drying, grinding, multi-stage extraction, filtration, evaporation. The end result are alcoholic or aqueous-alcoholic extracts (tinctures) and so these tools have a number against the evidence:

alcoholism and other conditions under which it is contraindicated to receive ethanol. Among other drawbacks, it is possible to note the following: the low concentration of active substances and, therefore, not sufficiently high activity of drugs. List lipid drugs with anti-inflammatory action, is limited to the representatives of this class are not without drawbacks - they have not sufficiently high anti-inflammatory activity, thus expanding the Arsenal of anti-inflammatory drugs and the increased activity of the drugs in this class is the actual problem.

The technical essence is the closest to the proposed method of obtaining funds that have anti-inflammatory action of peat is a method of obtaining biologically active substances from medicinal mud, which consists in the processing of silt sulfide mud cavitation in the pump in the presence of alkali, followed by separation of the complex of water-soluble and lipid biologically

active substances that have a high content of antioxidants (U.S. Pat of the Russian Federation No. 2449801).

The objective of the invention is the increase of antioxidant and anti-inflammatory activity funds of the peat due to the increased yield of extraction of biologically active substances.

This technical re the get query result due to after drying of peat up to 15-20% moisture it is crushed in the presence of alkali and oxidant - percarbonate sodium in planetary ball mills, vibrating, vibratory centrifugal, roller types, enabling acceleration of the acting bodies, for example balls, 300 m/s2. The residence time of the raw material in the treatment zone is 3-5 minutes. Mechanical treatment is carried out in an air environment. The dispersion of peat in the air and in the presence of alkali and oxidant leads to hydrolytic oxidation, contributing to the disruption of intermolecular bonds in supramolecular humic structures, release of lipid molecules and the formation of additional hydroxyl groups. The method allows to increase the output of the lipid extract, its antioxidant and protivovospalitelnoe activity.

Table 1 shows experimental data for the extraction of peat mechanochemical method lipid biologically active substances, increasing their yield and biological activity.

Example 1. Peat, shredded 1 mm and dried to a moisture content of 15-20% wt., placed in a planetary mill type AGO and added in solid form 3% wt. alkali and 3% wt. percarbonate sodium. The machining time in the air is 1 minutes After that peat telepaediatric-chloroform (1:1) in the ratio of sediment: solvent - 1:2. The extraction time is 10 minutes, the Obtained extract was evaporated, removing the solvent, and receive lipid concentrate of biologically active substances. The output of the lipids is of 47.3 g/kg, which is 2.2 times higher than without the use of mechanochemical method (example 8 in table 1), the amount of antioxidants (AO) is equal to 0.29 mol/kg

Example 2. Peat, shredded 1 mm and dried to a moisture content of 15-20% wt., placed in a planetary mill type AGO and added in solid form 3% wt. alkali and 5% wt. percarbonate sodium. The machining time in the air is 1 minutes After that peat is filled with alcohol-chloroform (1:1) in the ratio of sediment:the solvent is 1:2. The extraction time is 10 minutes, the Obtained extract was evaporated, removing the solvent, and receive lipid concentrate of biologically active substances. The output of the lipids is to 49.9 g/kg, the number of AO is equal to 0.37 mol/kg

Example 3. Peat, shredded 1 mm and dried to a moisture content of 15-20% wt., placed in a planetary mill type AGO and added in solid form 5% wt. alkali and 5% wt. percarbonate sodium. The machining time in the air is 1 minutes After that peat is filled with alcohol-chloroform (1:1) in the ratio of sediment: the solvent is 1:2. The extraction time is 10 minutes Received EXT the act evaporated, removing the solvent, and receive lipid concentrate of biologically active substances. The output of the lipids is 59.0 g/kg, the number of AO is equal to 0.46 mol/kg Under these conditions, there is the maximum yield of lipids, different high content of antioxidants.

The increase in machining time up to 3-5 minutes (samples No. 4, No. 7, table 1) leads to poor results, as the outputs of lipids and antioxidant activity. This is due to the fact that during long machining can occur destruction of the lipid molecules.

Anti-inflammatory lipid concentrate of biologically active substances extracted from peat, has been studied in outbred rats. Acute aseptic inflammation in offspring of male rats weighing 200-250 g were caused by the introduction under the plantar aponeurosis of the right hind paw with 0.1 ml of 1% solution carragenin (Winter C.A., and others 1962). The experiment was conducted on 56 outbred albino male rats. Animals were kept on a normal diet in vivarium conditions (8 animals in each experimental group). The study drugs were administered at a dose of 10 mg/kg of 1% starch mucus intragastric an hour before the injection of logogen. The volume of the edematous limb was measured ecometrics after 3 and 4 h after injection of the irritant. About the intensity of inflammation was assessed by mass OTE is and after 3.5 hours, the percentage increase of edema was calculated by the formula (Creenv and others 1971):

The weight of the patient limb - Weight healthy limbs * 100%

The mass of the healthy limb

Administration to rats of 1% solution carragenine led to the development of acute inflammation, weight gain swelling when it was 69%. As a result of studies all investigated drugs possessed anti-inflammatory activity. The degree of inhibition carragenine swelling was reached 31-41% compared with untreated animals (table 2). A more pronounced anti-inflammatory activity possessed lipids peat, obtained by the method described in example No. 3 (table 1).

Thus, therapy of acute aseptic inflammation induced in rats by injection of 1% solution carragenin, lipids peat was significantly successful by increasing their antioxidant activity. Target product, obtained by the proposed method has significant anti-inflammatory activity.

5
Table 1
Experimental data on yield and antioxidant activity of lipids from peat obtained by mechanochemical method
No.The processing time min Supplements, % wt.Lipids, g/kgThe content of antioxidants, mol/kg
NaOHpercarbonate
113347,50,29
2135to 49.90,37
315559,00,46
433535,10,29
535537,00,35
653332,00.36
75532,80,34
8000a 21.50,21
9(PR)55UTS.8,80,35

Table 2
Anti-inflammatory activity of a lipid peat
ExampleWeight reduction of edema, %
135,2
2to 38.3
340,8
831,7
932,2

The method of obtaining funds that have anti-inflammatory action, including the processing of natural material with alkali and extraction of the mixture of the alcohol-chloroform, characterized in that the peat, shredded, vysushennymi humidity 15-20% wt., before the extraction process in the mill planetary type AGO in the presence of 3-5% wt. alkali in solid form and 3-5 wt.%. percarbonate sodium for 1 minutes



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the pharmaceutical industry, namely to a medicated mud composition. The medicated mud composition contains prepared sludge argillaceous deposits of Tambukan Lake, Witepsol W 35, Witepsol H 15, polyethylene glycol 1500, Cremophore RH, as well as carbon-dioxide herbal extracts specified in a group consisting of at least the common willow, sea buckthorn, oak, calendula, licorice, brier, sage and/or carbon-dioxide extract of propolis taken in certain relations.

EFFECT: composition enables extending the range of medicinal agents using therapeutic sludge argillaceous deposits.

10 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the pharmaceutical industry, namely to a treating-preventive mud composition. The treating-preventive mud composition contains preliminarily prepared silt-clayey deposits of lake Tambukan, polyethyleneglycol 4000, polyethyleneglycol 1500, cremophor RH, as well as a carbon dioxide extract of propolis and/or a carbon dioxide vegetable extract, selected from the group, which includes, at least, eucalyptus, dog-rose, hop, laurel, chamomile, licorice and oak, taken in a specified ratio of components.

EFFECT: composition has an increased treating-preventive activity with respect to a patient's organism.

9 ex

Novel application // 2530567

FIELD: medicine.

SUBSTANCE: group of inventions relates to medicine and deals with a preparation for the prevention of an inflammatory disease of the intestine, which represents galactooligosaccharide, which has a degree of polymerisation 3 or higher, selected from the group, consisting of trisaccharides Gal(β 1-6)-Gal(β 1-4)-Glc, Gal(β 1-3)-Gal(β 1-4)-Glc, tetrasaccharide Gal(β 1-6)-Gal(β 1-6)-Gal(β 1-4)-Glc and pentasaccharide Gal(β 1-6)-Gal(β 1-6)-Gal(β 1-6)-Gal(β 1-4)-Glc; application of the claimed galactooligosaccharide for the prevention of the inflammatory disease of the intestine; a method of preventing the inflammatory disease of the intestine, which includes peroral introduction to a mammal of an effective quantity of galactooligosaccharide.

EFFECT: group of inventions provide the powerful anti-inflammatory effect with respect to the inflammatory diseases of the intestine.

10 cl, 9 dwg, 4 ex

FIELD: medicine.

SUBSTANCE: invention refers to immunology and biotechnology. What is presented is a single-domain antibody (VHH) able to bind the cytokine human necrosis factor (TNF), a DNA fragment coding the antibody according to the invention, as well as a method for identifying the human TNF and measuring it in a biological sample.

EFFECT: invention provides the specific block of macrophague-monocytic TNF cells and can find further application in therapy of the diseases associated with an undesired TNF-dependent inflammatory response.

4 cl, 5 ex, 7 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: in general formula A1 stands for CR10R11 or S; A2 stands for CR12R13, C(=O), O, S or S(=O)2; R1 stands for C1-10-alkyl, saturated or unsaturated, branched or non-branched, non-substituted, or monosubstituted, or polysubstituted; C3-10-cycloalkyl or 5- or 6-membered heterocyclyl with the O-atom, each time saturated or unsaturated, non-substituted, or monosubstituted, or polysubstituted; C6-10-aryl or C5-10-heteroaryl with 1-3 heteroatoms, selected from N, O or S, each time non-substituted, or monosubstituted, or polysubstituted; through C1-8-alkyl or C2-8-heteroalkyl bound by the bridge bond C3-10-cycloalkyl, each time saturated, non-substituted, and the alkyl or heteroalkyl chain each time can be branched or non-branched, saturated, non-substituted; or through C1-8-alkyl, bound by the bridge bond aryl or heteroaryl, each time non-substituted, or monosubstituted, or polysubstituted, and the alkyl chain each time can be branched or non-branched, saturated or unsaturated, non-substituted, or monosubstituted, or polysubstituted; R2, R3 and R4 each time independently on each other stand for H; F; Cl; Br; I; methyl; O-C1-6-alkyl or NRaRb, and Ra and Rb together with the nitrogen atom that binds them form heterocyclyl, saturated, non-branched, non-substituted; R5, R6, R7, R8, R10, R11, R12 and R13each time independently on each other stand for H; F; Cl; Br; I; OH or C1-10-alkul; or R5 and R6 or R7 and R11 together with carbon atom(s), that bind(s) them form C3-8-cycloalkyl, each time saturated or non-saturated, non-substituted, or monosubstituted, or polysubstituted; with respective remaining substituents R5, R6, R7, R8, R10, R11, R12 and R13 having the value given above; R9 stands for C3-10-cycloalkyl, saturated, non-substituted; C6-10-aryl or 5- or 6-membered heteroaryl with heteroatom, selected from N and S, each time non-substituted or monosubstituted.

EFFECT: invention relates to substituted nicotinamides of general formula (1), to a medication based on them and their application for treating KCNQ2/3-mediated diseases.

13 cl, 3 tbl, 224 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compound of formula (I) , where ring A is cycloalkane ring with number of members from 3 to 7, benzene ring or monocyclic 5-member or 6-member aromatic heterocyclic ring, containing 1 heteromember of ring, selected from the group, containing N and S, and benzene and heterocyclic rings can optionally have one or two similar or different substituents, selected from the group, containing halogen, HO-, R1-O-, H2N-C(O)- and NC-; Y is selected from the group, containing S, C(R12)=C(R13) and C(R15)=N; Z is selected from the group, containing C(R16); R1, R30, R33, R35, R54 and R55 independently on each other group R1, R30, R33, R35, R54 and R55 are selected from the group, containing (C1-C6)-alkyl, (C2-C6)-alkenyl, (C3-C7)-cycloalkyl and (C3-C7)-cycloalkyl-(C1-C4)-alkyl-, and all of them can optionally have one or more similar or different substituents R70; R3 and R5 represent hydrogen; R4 and R6 are selected independently on each other, from the group, containing hydrogen and , (C1-C4)-alkyl; R12, R13, R15 and R16 are selected independently on each other, from the group, containing hydrogen, halogen and O2N-; R20 is selected from the group, containing hydrogen and (C1-C4)-alkyl; one of the groups R21 and R22 is group of formula II: R24-R23-, and the other of groups R21 and R22 is selected from the group, containing hydrogen, halogen, R30, HO-, R30-O-, R30-S(O)m-, H2N-, R30-NH-, R30-N(R30)-, R30-C(O)- and NC-; R23 is chain, containing from 1 to 5 chain members of which 0 or 1 chain member is heteromember of chain, selected from the group, containing N(R25), O, S, with other chain members being similar or different groups C(R26)(R26), where two adjacent groups can be bound to each other by double bond; R24 is selected from the group, containing hydrogen, R31, R31-O-, R31-NH-, R31-N(R31)-, R31-C(O)-NH-, HO-C(O)- and monocyclic, bicyclic or tricyclic ring with number of members from 5 to 10, which is saturated or non-saturated and contains 0, 1, 2 or 3 similar or different ring heteromembers, selected from the group, containing N, N(R32), O, S, and ring can optionally have on ring carbon atoms one or 2-3 similar or different substituents, selected from the group, containing halogen, R33, R33-O-, R33-S(O)m-, R33-C(O)-NH-, R33-S(O)2-NH-, R33-C(O)-, HO-C(O)-, H2N-C(O)-, R33-NH-C(O)-, R33-N(R33)-S(O)2-, NC-, oxo, phenyl and Het; on condition that total number of C, N, O and S atoms, present in two groups R23 and R24, constitutes not less than 5; R25 is selected from the group, containing hydrogen and (C1-C4)-alkyl; R26, independently on each other group R26, is selected from the group, containing hydrogen, fluorine, (C1-C4)-alkyl and HO-, or two groups R26, together with included into them chain members, form monocyclic ring with number of members 4, which is saturated and contains 1 ring heteromember, selected from the group, containing O; R31 is selected from the group, containing (C1-C6)-alkyl, which can optionally have one substituent R70; R32 is selected independently on each other, from the group, containing hydrogen, R35 and phenyl; R50 is selected from the group, containing R51-O- and R52-N(R53)-; R51 is selected from the group, containing hydrogen and R54; R52 is selected from the group, containing hydrogen; R53 is selected from the group, containing hydrogen; R70 is selected from the group, containing HO-, R71-O-, H2N-, R71-NH-, R71-N(R71)-, R71-C(O)-NH-, HO-C(O)-, H2N-C(O)- and phenyl; R71, independently on each other group R71, is selected from the group, containing (C1-C4)-alkyl; Het, independently on each other group Het, is monocyclic heterocyclic ring with number of members 5, which contains 1 or 2 similar or different ring heteromembers, selected from the group, containing N and S, and ring is saturated or non-saturated and optionally substituted with one or more similar or different substituents, selected from the group, containing (C1-C4)-alkyl; m, independently on each other number m, is integer number, selected from the group, containing 0, 1 and 2; phenyl, independently on each other phenyl group, can optionally have one or more similar or different substituents, selected from the group, containing halogen and (C1-C4)-alkyl.

EFFECT: invention also relates to method of obtaining compound of formula (I) and its application for manufacturing pharmaceutical for inhibiting receptor Edg-2.

17 cl, 14 tbl, 362 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I) , where R1 and R2 have the following values: (i) R1 and R2 together form =O; (ii) R1 and R2 together with carbon atom, which they are bound with, form duoxacycloalkyl; R1 represents hydrogen or halogen; and R2 represents halogen; (iv) R1 represents C1-6alkyl, where alkyl is optionally substituted with cyano, -RxS(O)qRv or -RxNRyRz; and R2 represents hydrogen; (v) R1 represents -OR12 or -NR13R14; and R2 represents hydrogen, deutero or phenyl, which is optionally substituted with halogen; R3 represents hydrogen, halogen, C1-6alkyl, cyano, halogen C1-6alkyl, C3-10cycloalkyl or C1-6alkoxy; R4 and R5 represent hydrogen; R6 is independently selected from halogen, C1-6alkyl, halogenC1-6alkyl, -RxOR18 and -RxS(O)qRv; R7 independently represents halogen or -RxORw; R12 is selected from hydrogen and C1-6alkyl, R13 represents hydrogen; R14 is selected from hydrogen, C3-10cycloalkyl, -C(O)Rv and -C(O)ORw; R18 represents hydrogen, C1-6alkyl, or pyperidinyl, where R18 is optionally substituted with 1-3 Q1 groups, each Q1 is independenly selected from hydroxyl, C1-6alkoxy, C1-6alkoxycarbonyl, carboxyl and morpholinyl; Rx independently represents C1-6alkylene or simple bond; Rv and Rw represent hydrogen or C1-6alkyl; Ry and Rz represent hydrogen; n has value 0-4; p has value 0-5; and each q independently has value 0, 1 or 2. Invention also relates to compounds of formula (II) , where substituents have values, given in the invention formula, to pharmaceutical composition, possessing inhibiting activity with respect to JAK kinases, containing compounds of formula (I) or (II), methods of treating JAK-modulated disease, and application of compounds of formula (I) or (II).

EFFECT: compounds of formula (I) or (II) as inhibitors of JAK kinases.

32 cl, 6 dwg, 2 tbl, 84 ex

FIELD: medicine.

SUBSTANCE: method is implemented by correcting rat's prostatic structural homeostasis in adaptation to low seasonal temperature conditions with the use of dihydroquercetin administered daily in a dose of 5 mg/kg of body weight prior to cooling for four weeks.

EFFECT: developing the method for increasing the adaptive capability of laboratory animal's prostate to low seasonal temperatures.

2 dwg, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new benzene sulphonamide compounds, wherein the compounds are specified in a group of the following compounds, including additive salts with pharmaceutically acceptable acid, additive salts with pharmaceutically acceptable base and enantiomers of these compounds: 1) 3-[(4-but-2-inyloxybenzenesulphonyl)-methylamino]-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 2) (S)-3-(4-but-2-inyloxybenzenesulphonylamino)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 3) (S)-3-(4-benzyloxybenzenesulphonylamino)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 4) (S)-3-[(4-benzyloxybenzenesulphonyl)-methylamino]-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 5) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 6) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(naphthalen-1-ylmethoxy)-benzenesulphonylamino]-propionamide, 7) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-(4-propoxybenzenesulphonylamino)-propionamide, 8) (S)-3-[4-(3-cyanobenzyloxy)-benzenesulphonylamino]-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 9) (S)-3-[4-(4-cyanobenzyloxy)-benzenesulphonylamino]-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 10) benzyl-4-{(S)-1-hydroxycarbamoyl-2-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-entyl}-piperazine-1-carboxylate, 11) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(2-phenylpiperidin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 12) (R)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 13) (S)-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-2-piperazin-1-ylpropionamide, 14) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide hydrochloride, 15) tert-butyl-3-{4-[(S)-2-hydroxycarbamoyl-2-(4-methanesulphonylpiperazin-1-yl)-ethylsulphamoyl]-phenoxymethyl}-2-methylindole-1-carboxylate difluoroacetate, 16) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(quinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 17) (S)-2-(4-benzylpiperazin-1-yl)-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 18) (S)-2-[4-(4-fluorobenzyl)-piperazin-1-yl]-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino-propionamide, 19) (S)-2-(4-ethulpiperazin-1-yl)-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 20) (S)-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-2-[4-(4-trifluoromethylbenzyl)-piperazin-1-yl]-propionamide, 21) (S)-N-hydroxy-2-[4-(4-methylbenzyl)-piperazin-1-yl]-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 22) (S)-3-[4-(benzoisoxazol-3-ylmethoxy)-benzenesulphonylamino]-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 23) (S)-N-hydroxy-2-(4-isobutyrylpiperazin-1-yl)-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 24) (S)-N-hydroxy-2-[4-(2-methylpropane-1-sulphonyl)-piperazin-1-yl]-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 25) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(2-trifluoromethylpyrazolo[1,5-a]pyridin-3-ylmethoxy)-benzenesulphonylamino]-propionamide, 26) (S)-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-2-[4-(propane-2-sulphonyl)-piperazin-1-yl]-propionamide, and 27) (S)-2-(4-benzylpiperazin-1-yl)-N-hydroxy-3-[4-(2-trifluoromethylpyrazolo[1,5-a]pyridin-3-ylmethoxy)-benzenesulphonylamino]-propionamide. The invention also refers to pharmaceutical and cosmetic compositions on the basis of the above compounds possessing TNFα-converting enzyme (TACE) activity.

EFFECT: there are prepared new compounds and compositions on the basis thereof which can be used in medicine and veterinary science for treating rheumatoid arthritis, non-insulin dependent diabetes mellitus, Crohn's disease or inflammatory skin disease.

35 cl, 28 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula (I), wherein A means morpholinyl, 1,4-oxazepamyl, piperidinyl, pyrrolidinyl or azetidinyl which is bound to N; R1 means C1-C6-alkyl group; R2 means bicyclic aryl group specified in 1H-indolyl, 1H-pyrrolo[3,2-b]pyridyl, quinolyl, naphthyl, 1H-pyrrolo[2,3-b]pyridyl, 5H-pyrrolo[3,2-d]pyrimidinyl, 7H-pyrrolo[2,3-d]pyrimidinyl, benzo[b]thiophenyl, imidazo[1,2-a]pyridyl, benzo[b]thiazolyl, 5H-pyrrolol[2,3-b]pyrazinyl and quinoxalinyl which can be substituted by R4; R3 means hydrogen or halogen atom; R4 means C1-C6-alkyl group, C1-C6-halogenalkyl group, OR1A, halogen, -(CH2)aOH, CN, NHCOR1A, SO2R1A or NHSO2R1A; R5 means C1-C6-alkyl group, -(CH2)aOH, -(CH2)aOR1B, halogen or CONH2; provided p is a plural number, R5 can be identical or different, or R5 can be combined with another R5; each of R1A and R1B independently means C1-C6-alkyl group; a is equal to 0, 1 or 2; n is equal to 1 or 2; p is equal to 0, 1, 2, 3, 4 or 5. Besides, the invention refers to intermediate compounds of formulas (IA) and (IB) for preparing the compounds of formula (I), to a preventive or therapeutic agent containing the compounds of formula (I), pharmaceutical compositions, using the compounds of formula (I) and to a method for preventing or treating diseases.

EFFECT: compounds of formula (I) as selective 5-HT2B receptor antagonists.

11 cl, 1 dwg, 18 tbl, 88 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the pharmaceutical industry, namely to a medicated mud composition. The medicated mud composition contains prepared sludge argillaceous deposits of Tambukan Lake, Witepsol W 35, Witepsol H 15, polyethylene glycol 1500, Cremophore RH, as well as carbon-dioxide herbal extracts specified in a group consisting of at least the common willow, sea buckthorn, oak, calendula, licorice, brier, sage and/or carbon-dioxide extract of propolis taken in certain relations.

EFFECT: composition enables extending the range of medicinal agents using therapeutic sludge argillaceous deposits.

10 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the pharmaceutical industry, namely to a treating-preventive mud composition. The treating-preventive mud composition contains preliminarily prepared silt-clayey deposits of lake Tambukan, polyethyleneglycol 4000, polyethyleneglycol 1500, cremophor RH, as well as a carbon dioxide extract of propolis and/or a carbon dioxide vegetable extract, selected from the group, which includes, at least, eucalyptus, dog-rose, hop, laurel, chamomile, licorice and oak, taken in a specified ratio of components.

EFFECT: composition has an increased treating-preventive activity with respect to a patient's organism.

9 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely paediatrics and can be used for treating community-acquired pneumonia in children. That is ensured by prescribing an electrophoresis with an aqueous solution of the natural preparation Relikt-05 on the second day after temperature normalisation with a daily bipolar application of electrodes on the chest at current intensity 2 to 4-5 mA in children aged 3-7 years old and at 5 to 8 mA in children aged 7 and older with underlying drug therapy. The procedure length makes 10 to 15 minutes daily; the therapeutic course is 6-7 procedures.

EFFECT: method enables improving outcome of the integrated therapy in children suffering community-acquired pneumonia by faster resolution of infiltration centres in pulmonary tissue, increasing a neutrophil phagocytic rate and the content of active microelements, activating the endogenous antioxidant and antiradical protection with no complications.

3 ex, 2 tbl

FIELD: medicine.

SUBSTANCE: invention represents a protective coating for removable dentures differing by the fact that the coating is presented by an alcoholic amber varnish.

EFFECT: invention provides preparing a strong and stable coating for dentures possessing an ability to inhibit growth and development of microorganisms, formation of dental plaque in the form of a biofilm.

2 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to gynaecology, reflexotherapy and pelotherapy. A method includes carrying out a course of antibacterial and/or antiviral therapy, which is started on 5-7 day of a menstrual cycle. From 5-7 day of the following menstrual cycle a course of pharmacopuncture is performed by introduction of homeopathic preparations into acupuncture points (AP). On 1, 3, 5, 7, 9, 11 and 13 days of the course Traumel C is introduced into points E36 (2), V31 (2), V32 (2), V33 (2), V34 (2). On 2, 4, 6, 8, 10, 12, 14 days of the course Ovarium compositum is introduced in AP Rp6 (2). Simultaneously with the course of pharmacopuncture or starting from 5-7 day of the following menstrual cycle a course of pelotherapy is carried out. Introduction of gel, based on the Dead Sea mud, is performed rectally for 30 minutes, 1 time per day.

EFFECT: method ensures recovery of the two-phase menstrual cycle due to normalisation of endometrium and vagina biocenosis, improvement of local immune and vegetative status, increases duration of remission.

4 cl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the pharmaceutical industry, namely to a method for preparing the therapeutic mud. The method for preparing the therapeutic mud consists in filling sapropel with sodium hydroxide, heating, cooling and diluting with water, settling, siphonage and filtering; the filtrate is poured into an anode chamber of an electrolytic cell, electrodes of which are made from fine schungite placed into a fine porous non-metallic envelope with a schungite or graphite rod; the rods are attached to the output terminals of a power source; the filtrate electrolysis involves ultrasonic oscillation generation; the filtrate electrolysis is terminated when a target humic concentrate is formed on the surface of the anode and anode chamber; the target concentrate is removed from the surface of the anode and anode chamber and is used as the therapeutic mud.

EFFECT: method described above enables preparing the mud with more pronounced therapeutic and stimulating properties that enables extending the range of using the prepared mud.

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical industry, namely to enterosorbent and method of its obtaining. Enterosorbent based on peat, free from lipids, additionally contains cranberry cake, prebiotic with specified component ratio. Method of obtaining enterosorbent from preliminarily dried sphagnum peat includes extraction of lipids with solvents, mixing with cranberry cake, crushing, mixing with solution of prebiotics - lactulose or lactose and drying.

EFFECT: method makes it possible to extend assortment of natural enterosorbents with improved properties: high enterosorbing capability and prebiotic activity.

2 cl, 1 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: method involves a combination of peloid applications and ultrasonic exposure. Peloid is applied on anterolateral thighs and an anterior abdominal wall. The applications are alternated every second day. Peloid is silt sulphide mud of Melkovodnenskiy deposit. The mud is applied in layer 10 mm thick at temperature 34-36°C. The applications are exposed to ultrasound at frequency 880 kHz in a continuous mode. The applications of the anterior abdominal wall are exposed to ultrasound at intensity 0.2-0.4 Wt/cm2 for 5 - 10 minutes. The anterolateral thighs are exposed to ultrasound at intensity 0.4-0.6 Wt/cm2, for 6-8 minutes for each thigh. Upon the completion of the procedure, the patient is covered with a hydrophobic tissue and left for 10 minutes. The therapeutic course is 10 procedures.

EFFECT: reducing obesity effectively by exposing on the hormonal activity of fat tissue, maintains the results obtained within three months.

2 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely rheumatology, physiotherapy. The method involves drug-induced and drug-free methods of treating. In addition, the area of two affected symmetrical joints is applied with the preparation Biol in a combination with the exposure to high-tone therapy. The length of procedures is 1 to 4-5 to 30 minutes per each joint. Starting from the 4-5th to 8-10th procedure, the length of procedures is 20 minutes per each joint. The procedures are daily. The therapeutic course is 8-10 procedures.

EFFECT: method provides higher therapeutic effectiveness ensured by improved microcirculation, ensured anaesthetic effect, reduced drug-induced load.

1 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely rheumatology, balneotherapy and physiotherapy. The method involves the integrated treatment. There are prescribed sulphide bath with the total hydrogen sulphide concentration of 158 mg/l, the free hydrogen sulphide concentration of 108 mg/l at temperature 36-37°C. The length of the first 2-3 baths is 6-8 minutes. The length is to be increased to 8-12 minutes. The baths are taken within the period of 10.00 to 12.00 every second day. The therapeutic course is 10-12 procedures. On the same days, within the period of 14.00 to 16.00, therapeutic exercises are done, and the climatic and landscape therapy is prescribed. On the days free from taking baths, within the period of 10.00 to 12.00, the EHF therapy is prescribed to cover biologically active points (BAP) at frequency 40-43 GHz. The points G-41, 3E-5 are exposed. The hip osteoarthrosis requires the exposure on the points G-29, G-30. If observing the upper extremity osteoarthrosis, the points 3E-4, Du-4, Du-5, Di-5 are covered. In case of the knee osteoarthrosis, the points M-34, M-35, Le-7, Le-8 are exposed. The length of the exposure covering one BAP makes 5-6 minutes. The total length of the procedure is 20-30 minutes. On the same days within the period of 14.00 to 16.00, high-mineralised average sulphide mud is applied at temperature 38-40°C on the involved joints and respective spinal reflexogenic zones. A single procedure covers not more than 2-3 greater joints. The length of one procedure is 20-25 minutes. The therapeutic course is 8-10 procedures. The total length of the rehabilitation makes 20-24 days.

EFFECT: method prolongs the remission.

2 tbl, 1 dwg, 1 ex

FIELD: medicine, phthisiology.

SUBSTANCE: in early period the preparation "Yantar-antitoks" is used in the dose 0.5 g, 3 times per a day for one month in addition to the conventional antituberculosis therapy. Invention promotes to elimination of symptoms associated with the total intoxication, resorption of focus-infiltration changes, elimination of destructions and ceasing secretion of microorganisms for shorter periods. Invention can be used in treatment of pulmonary tuberculosis.

EFFECT: improved method for treatment.

4 tbl, 1 ex

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