Medication, possessing anti-inflammatory and regenerating action

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to chemical-pharmaceutical industry, namely to creation of medication, which possesses anti-inflammatory and regenerating action. Medication contains the following ingredients: conifer needle extract, purified oleoresin of cedar or pine, or spruce, or fir, or larch or their mixture in equal proportions, vegetable oil.

EFFECT: medication has increased effectiveness and efficiency and also extends arsenal of medications, which have anti-inflammatory and regenerating action.

7 cl, 9 ex, 2 tbl

 

The invention relates to a tool, which has anti-inflammatory and regenerating effect, with a wide spectrum of action.

Known agents that have anti-inflammatory and regenerating effect, for the treatment of infected and purulent post-traumatic and burn wounds, such drugs as sea buckthorn oil, balsamic liniment on Avissawella, pninat sodium on balsam fir and liniment of syntomycin 1%, ointment, levsin, levomicol, dioxidea ointment, ointment butadiene 10% and other (Mashkovsky PPM Medicines. - M.: Medicine, 1993, 1 and 2 hours, s, 690).

Known ointment "Benin" for the treatment of purulent and infected wounds of various etiologies, including fir oil, propolis, pine resin, spermaceti and the fat penguin, when the mass ratio of the components 3-7:0,5-1,5:0,5-1,5:1,5-2,5:7-15, respectively (RF patent 2058776, CL A61K 9/06, publ. 27.04.96).

The disadvantages of the above ointment is the presence in the formulation of the last spermaceti and fat penguin, accessibility and raw materials are limited. In addition, the drug is used only as an external agent.

Known ointment for the treatment of purulent diseases of skin and osteomyelitis containing wt.%: animal fat 40, pitch 5, the resin of the resin (fir) 12, minced onion 20, the wax 3, propolis 10, sulfur purified 5, sulfate is a single 2,48, soap baby 2,48, mucus bowel chicken 0,04 (RF patent 2135158, CL A61K 9/06, publ. 27.08.99).

The disadvantages of the known ointments are narrow spectrum of therapeutic action, the content of hard-to-reach components and use only as an external tool.

Known external means "Zwar" for the treatment of purulent and infected wounds of various etiologies, containing the following components, wt.%: pine resin (oleoresin of pine or fir) 7,0-8,0; beeswax 6,7-7,3; butter of 6.5-7.5; oil of 6.5-7.5; fat interior (pork or beef or goose, or sheep) 19,0-22,0; propolis 0,5-1,0; bow-turnip - rest (RF patent No. 2139708, CL A61K 9/06, publ. 20.10.99).

A disadvantage of the known ointment is the lack of range of therapeutic actions and presence in the recipe inaccessible components.

Known anti-inflammatory ointment "Picton" (patent RF №2097056, IPC A61K 35/78, publ. 27.11.1997), wt.%: the oleoresin of pine 19,0-21,0; beeswax 16,8-17,5; chalk 10,5-12,0; fatty base - the rest. This tool has insufficient range of therapeutic action and is used only as an external agent.

Known drug wound healing, burns and anti-inflammatory action on the basis of a product of natural origin (RF Patent No. 2111760, IPC A61K 35/78, publ. 27.05.1998,). As the active substance contains a resin neutralino the fir, purified water and emulsifier T-2 in the following ratio, wt.%: resin neutral fir 9-11; emulsifier T-2 9-11; purified water - the rest.

However, this drug has a fairly narrow range of therapeutic actions, contains not only natural remedies and is used only as an external agent.

The closest analogue (prototype) is a tool for the treatment of inflammatory and traumatic diseases of the musculoskeletal system and peripheral nervous system (patent RU 2190389 C1, 10.10.2002)containing the oleoresin of pine or fir, beeswax, propolis and vegetable oil, characterized in that it additionally contains Shilajit, fir oil and sea buckthorn oil in the following ratio, wt.%: the oleoresin of pine or fir 5,0-15,0; beeswax 5,0-15,0; propolis 1,0-3,0; mummy of 0.1-0.3; oil fir 1,0-4,0; sea buckthorn oil 1,0-5,0; vegetable oil - else.

However, this drug has a narrow range of therapeutic actions and is used only as an external agent.

The technical result of the invention is to improve the efficiency, effectiveness, expanding the scope and spectrum of the proposed drug with anti-inflammatory and regenerating action.

Specified-the first result is the creation of tools, it has anti-inflammatory and regenerating effect, representing a balm that contains the extract of pine green, purified resin of cedar or pine, or spruce, or fir, or larch, or a mixture in equal proportions and vegetable oil with the following content, wt.%:

extract pine green1,0-20,0
the purified resin of cedar or pine,
or spruce, or fir, or larch,
or their mixture in equal proportions22,0-30,0
vegetable oilthe rest is up to 100%

In addition, the extract of pine greenery can be an oil extract or an aqueous extract of crushed green fir or pine, or cedar, or fir, or larch, or mixtures thereof:

- mummy in an amount of 0.1-0.5 wt.%;

- propolis in an amount of 0.1-0.5 wt.%;

- essential oil of pine cedar or fir in an amount of 0.01-0.03 wt.%.

The tool may be made in the form of suppositories and ointments for topical use or in the form of capsules for internal use.

Resin, colorless viscous cm is liste substance with a characteristic smell of pine; product life coniferous trees (pine, spruce, cedar, larch, fir). Part g contains: 40-65% diterpene, or resin acids total f-ly C19H29COOH (levopimaric, pimaric, palustria, abietic, dehydroabietylamine and others), 20-35% of monoterpenic hydrocarbons with the General formula C10H16(volatile part J. - α - and β-pinene, Karen, camphene, β-phellandrene, lemon and others), 5-20% Sesqui - and diterpene hydrocarbons and their derivatives (the so-called neutral-VA). The qualitative composition of the resin to t and monoterpenes for J. coniferous trees are mostly the same (J. cedar also contains lambertianic acid), the quantitative composition of them is different and depends on species and tree species, habitat, etc. J. fir contains, in addition, triterpene to you. J. differ significantly from one another on the content and composition of neutral-b (in mass%): J. pine (Pinus silvestris) - 3-4 (pimeyden, pomarina, abietina, abietina, meldegerate and others), in J. Siberian cedar (Pinus sibirica) - 7-10 (cembran, siebren, siembra and others), in J. larch (Larix sibirica, Larix daurica) -18-20 (lyrical, Ericaceae, hapimana, apicobasal, aldehydes, and others), in J. spruce (Picea obovata and others) - 10-12 (noobier, epimanikia and others), in J. fir (Abies sibirica) - 8-12 (monooxide, abitol, noobier and others). J. soluble in diethyl ether, ABSA anole, acetone, worse in gasoline, insoluble in water. The resin is the main raw material for the production of rosin and turpentine.

Oil extract of coniferous greens is an extract of crushed green fir or pine, or cedar, or fir, or larch in vegetable oil.

Aqueous extract of coniferous greens produced by extraction of biologically active substances in a water bath at a temperature of 70-90°C.

Propolis (gr. própolis), bee glue, TGS - dark resinous substance produced by bees to luting gaps and isolation of extraneous objects in the hive. Bees collect propolis on a sticky buds of trees (poplar, alder, birch and others).

Shilajit is a natural blend of organic and inorganic water soluble substance which collects in the crevices of the rocks, hollows, recesses in the form of films, crusts, growths of black, dark brown and brown retinoid masses. Refined and extracted Shilajit is a homogeneous mass of dark brown, elastic consistence, with shiny surface, a peculiar aromatic smell and bitter taste.

The weight of 2-2,5; melting point 80°C; pH of 0.5% solution of 6.7-7, during storage increases to 7.5. Storage mumie gradually calcify due to loss of moisture. Easily soluble in water (1/8), very little dissolve is about 95% alcohol (1/4500) and ether (1/10000). Aqueous solutions of transparent brown color. Includes organic and inorganic parts and contains about 30 macro - and micronutrients, about 10 different oxides of metals, silicate group of silicon dioxide, phosphoric anhydride, various organic substances and acids. A number of diseases, the treatment of which Shilajit gives a special effect: disease of the urinary tract, the treatment of cystitis. Shilajit is able to accelerate the healing of ulcers of various origins, that is perfectly cures diseases of the gastrointestinal tract: gastritis, stomach ulcer. Shilajit is one of the strongest treatments for allergies. Shilajit is one of the best remedies for the treatment of pimples and acne.

This tool is illustrated by the following examples.

Example 1. Tool for internal use, wt.%:

the purified resin of cedar25,0
oil extract pine green1,0
vegetable oilthe rest is up to 100%

Example 2. Tool for internal use, wt.%:

the purified resin of cedar22,0
powder water extract hwain the th green 5,0
vegetable oilthe rest is up to 100%

Example 3. Tool for internal use, wt.%:

the purified resin of cedar, pine, spruce,
fir and larch
in the ratio 1:1:1:1:125,0
powder water extract of pine green10,0
vegetable oilthe rest is up to 100%

Example 4. Tool for internal use, wt.%:

the purified resin fir23,0
powder water extract of pine green15,0
Shilajit0,1
vegetable oilthe rest is up to 100%

Example 5. Tool for internal use, wt.%:

purified rosin pine 22,0
oil extract pine green7,0
essential oil of pine cedar0,01
vegetable oilthe rest is up to 100%

Example 6. Tool for internal use, wt.%:

the purified resin of cedar,
pine, spruce,
fir and larch in the ratio 1:1:1:1:130,0
the mixture of oil extract pine green
powder and aqueous extract of pine green
in the ratio of 1:120,0
propolis0,5
essential oil of pine cedar0,03
vegetable oilthe rest is up to 100%

Example 7. The agent for external use, wt.%:

PTS is placed oleoresin cedar 30,0
oil extract pine green15,0
Shilajit0,1
propolis0,1
essential oil fir needles0,03
vegetable oilthe rest is up to 100

Example 8. The agent for external use, wt.%:

purified rosin pine27,0
oil extract pine green10,0
Shilajit0,1
propolis0,1
essential oil of pine cedar0,01
vegetable oilthe rest is up to 100

Example 9. The agent for external use, wt.%:

purified rosin pine27,0
oil extract pine green 5,0
Shilajit0,1
propolis0,5
essential oil fir needles0,02
vegetable oilthe rest is up to 100

The method of obtaining the proposed drug with anti-inflammatory and regenerating action

Obtain an oil extract. Purified vegetable oil (sunflower or olive, or corn, or flax, or other) is heated to 95°C, add to it with constant stirring chopped green fir or pine, or cedar, or fir, or larch, taken in the ratio by weight of (g), respectively 80-100 g per 1 liter of oil. The oil is cooled to a temperature not lower than 35°C and at this temperature, the extraction is carried out for at least two days, using a vacuum, for example at 0.2 ATM. Temperature extraction oil 15-30°C is selected as the closest to the natural growing conditions of plants in the natural environment, which provides a fermentation raw material without loss of biologically active substances. At the end of the process the mixture is filtered.

Pets maximum size of suspended particles 30 microns. In the extract obtained at 36°C was added when peremeci the years not less than 3 g (for example, 5 g) of camphor. The ratio extract: 1 l of an extract of at least 3 g of camphor. Oil extract is used to produce further proposed drug.

Aqueous extract of coniferous greens produced by extraction of biologically active substances in a water bath at a temperature of 70-90°C. Next, the extract is filtered and distilled water to a residual moisture content of the product is not higher than 2 wt.%. Before the sheet product is crushed, for example, in a ball mill.

The inventive tool is made as follows. Charged to the reactor vegetable oil and heated to a temperature above 80°C under the conditions of the water bath. Further components according to examples 1-9, except essential oils, incubated with stirring on a water bath for 60 minutes. The mixture is gradually cooled to a temperature not higher than 45°C and introduce essential oils. The mixture is cooled to room temperature, stirred and poured into a container.

The above data (tables 1 and 2) on the application of the proposed drug for internal and external use in medicine and veterinary medicine. The analysis of these data confirms the technical result achieved associated with improving the efficiency, effectiveness, expanding the scope and spectrum of the proposed drug, obladaushi what about the anti-inflammatory and regenerating effect, both topical and internal use.

The claimed therapeutic tool can be used as a component of balms, capsules for internal use, and in the form of suppositories, ointment for external use, including cosmetics.

1. The tool, which has anti-inflammatory and regenerating effect, characterized by the fact that it is a balm that contains the extract of pine green, purified resin of cedar or pine, or spruce, or fir, or larch, or a mixture in equal proportions and vegetable oil with the following content, wt.%:

extract pine green1,0-20,0
the purified resin of cedar or pine,
or spruce, or fir, or larch,
or their mixture in equal proportions22,0-30,0
vegetable oilthe rest is up to 100%

2. The tool according to claim 1, where the extract of pine greenery is an oil extract or an aqueous extract of crushed green fir or pine, or cedar, or fir, or larch, or the x in the mixture.

3. The tool according to claim 1 may further comprise a mummy in an amount of 0.1-0.5 wt.%.

4. The tool according to claim 1 may further comprise propolis in an amount of 0.1-0.5 wt.%.

5. The tool according to claim 1 may further comprise an essential oil of pine cedar or fir in an amount of 0.01-0.03 wt.%.

6. The tool according to claim 1 made in the form of suppositories and ointments for external use.

7. The tool according to claim 1 made in the form of capsules for internal use.



 

Same patents:

FIELD: medicine.

SUBSTANCE: invention relates to field of medicine, namely, to therapy and cardiology, and deals with treatment of arterial hypertension. For this purpose into complex of conventional therapy additionally introduced is prostaglandin E2 in form of 0.0008% solution. Prostaglandin is introduced intravenously, starting with rate 50-100 ng/kg/min, increasing rate of introduction each 10 minutes on 20-40 ng/kg/min, bringing rate to 150-300 ng/kg/min during 40-60, minutes. Altogether there are three introductions per a course with 1-2 day intervals between them.

EFFECT: additional introduction of prostaglandin E2 in elaborated doses and regimen ensures efficient normalisation of arterial pressure during long term due to enhance of excretion of prostaglandins by kidneys, expressed vasodilation of vessels of kidneys, heart and brain, as well as normalisation of functional activity of platelets.

6 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I): where: A is a monocyclic or polycyclic aryl or heteroaryl group, where the heteroaryl radical denotes a 5-10-member cyclic system containing at least one heteroaromatic ring and containing at least one heteroatom selected from O, S and N; optionally substituted with one or more substitutes independently selected from a group comprising halogen atoms, C1-4alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-4alkyl, C1-4alkoxy and a hydroxyl group; B is a monocyclic nitrogen-containing heteroaryl group, where the heteroaryl radical denotes a 5-6-member heteroaromatic ring containing at least one heteroatom selected from S and N; optionally substituted with one or more substitutes selected from a group consisting of halogen atoms, C1-4alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-4alkyl, aryl and C1-8alkylthio; either a) R1 is a group of formula: -L-(CR'R")n-G, where L is a binding group selected from a group consisting of a direct bond, -(CO)-, -(CO)NR'- and -SO2-; R' and R" is independently selected from hydrogen atoms; n assumes values from 0 to 1; and G is selected from a group consisting of a hydrogen atom and C1-4alkyl, aryl, heteroaryl, where the heteroaryl radical denotes a 5-6-member heteroaromatic ring containing at least one heteroatom selected from O, S and N; C3-8cycloalkyl and saturated heterocyclic groups, where heterocyclic group denotes a non-aromatic saturated 6-member carbocyclic ring in which one or two carbon atoms are substituted with a N heteroatom; where alkyl, C3-8cycloalkyl, aryl or heteroaryl groups are unsubstituted or substituted with one or more substitutes selected from halogen atoms; and R2 is a group selected from hydrogen atoms, halogen atoms and C1-4alkyl, C2-5alkynyl, C1-4alkoxy, -NH2 and cyano groups, where alkyl and alkynyl groups may be unsubstituted or substituted with one aryl group; or b) R2, R1 and -NH- group to which R1 is bonded form a group selected from groups of formulae and , where: Ra is selected from a hydrogen atom or groups selected from C1-4alkyl, C3-8cycloalkyl, aryl, aryl-C1-4alkyl, heteroaryl, where the heteroaryl radical denotes a 5-6-member heteroaromatic ring containing at least one heteroatom selected from O and N; saturated heterocyclic rings, where the heterocyclic group denotes a non-aromatic saturated 6-member carbocyclic ring in which one carbon atom is substituted with a heteroatom selected from O and N; and C1-4alkylthio; where the aryl or heteroaryl groups are unsubstituted or substituted with one or more groups selected from halogen atoms, cyano group, trifluoromethoxy and carbamoyl; Rb denotes hydrogen; and pharmaceutically acceptable salts thereof and N-oxides; provided that the compound is not selected from N-[6-(1-methyl-1H-indol-3-yl)-5-pyridin-2-ylpyrazin-2-yl]benzamide, N-[3-ethoxycarbonyl-6-(1-methyl-1H-indol-3-yl)-5-pyridin-2-ylpyrazin-2-yl]benzamide, and N-[3-ethoxycarbonyl-6-(1-methyl-1H-indol-3-yl)-5-pyridin-2-ylpyrazin-2-yl]formamide. The invention also relates to a pharmaceutical composition, use of compounds in any of claims 1-20, a method of treating a subject, as well as a composite product.

EFFECT: obtaining novel biologically active compounds having adenosine A2B receptor antagonist activity.

27 cl, 160 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts thereof where R1 and R2 together denote a group selected form groups of formula (III-1): , where R9 denotes 1) a lower alkyl group, optionally substituted with a halogen atom or lower alkoxy group, 2) an aryl group, 3) an aralkyl group, 4) a heteroarylalkyl group, 5) a heteroaryl group, where the aryl, aralkyl, heteroarylalkyl and heteroaryl groups can be substituted with a halogen atom, lower alkyl group, optionally substituted with a lower alkoxy group or 1-3 halogen atoms, lower alkoxy group, optionally substituted with 1-3 halogen atoms, cyano group, hydroxy group, alkylsulphonyl group, cycloalkylsulphonyl group, aryl group, heteroaryl group, alkylaminocarbonyl group, alkanoyl amino group, alkyl amino group or dialkylamino group; R10 denotes a lower alkyl group, optionally substituted with 1-3 halogen atoms, or a lower alkylsulphonyl group; X9-X12 denotes a carbon atom or a nitrogen atom, where the carbon atom can be independently substituted with a lower alkyl group, optionally substituted with a halogen atom or a lower alkoxy group, lower alkoxy group, optionally substituted with a halogen atom, or a cyano group or a halogen atom; R3 denotes a) a group of formula (II-1): (ii-U where R4 and R5, taken together with a nitrogen atom, form a 5- or 6-member monocyclic ring, where the monocyclic ring may contain a substitute in form of a lower alkyl group, m1 equals 3; or b) a group of formula (II-2): , where R6 denotes a lower alkyl group or cycloalkyl group; m2 equals 1 or 2; X1-X4 all denote carbon atoms, or one of X1-X4 denotes a nitrogen atom and the rest denote carbon atoms; and where "heteroaryl" in each case relates to a 5- or 6-member aromatic ring containing 1-3 heteroatoms selected from a nitrogen atom, oxygen atom and a sulphur atom. The invention also relates to a histamine H3 receptor antagonist or inverse agonist, as well as a preventive or medicinal agent.

EFFECT: obtaining novel biologically active compounds, having histamine H3 receptor antagonist or inverse agonist activity.

11 cl, 8 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts thereof where R1 and R2 together denote a group selected form groups of formula (III-1): , where R9 denotes 1) a lower alkyl group, optionally substituted with a halogen atom or lower alkoxy group, 2) an aryl group, 3) an aralkyl group, 4) a heteroarylalkyl group, 5) a heteroaryl group, where the aryl, aralkyl, heteroarylalkyl and heteroaryl groups can be substituted with a halogen atom, lower alkyl group, optionally substituted with a lower alkoxy group or 1-3 halogen atoms, lower alkoxy group, optionally substituted with 1-3 halogen atoms, cyano group, hydroxy group, alkylsulphonyl group, cycloalkylsulphonyl group, aryl group, heteroaryl group, alkylaminocarbonyl group, alkanoyl amino group, alkyl amino group or dialkylamino group; R10 denotes a lower alkyl group, optionally substituted with 1-3 halogen atoms, or a lower alkylsulphonyl group; X9-X12 denotes a carbon atom or a nitrogen atom, where the carbon atom can be independently substituted with a lower alkyl group, optionally substituted with a halogen atom or a lower alkoxy group, lower alkoxy group, optionally substituted with a halogen atom, or a cyano group or a halogen atom; R3 denotes a) a group of formula (II-1): (ii-U where R4 and R5, taken together with a nitrogen atom, form a 5- or 6-member monocyclic ring, where the monocyclic ring may contain a substitute in form of a lower alkyl group, m1 equals 3; or b) a group of formula (II-2): , where R6 denotes a lower alkyl group or cycloalkyl group; m2 equals 1 or 2; X1-X4 all denote carbon atoms, or one of X1-X4 denotes a nitrogen atom and the rest denote carbon atoms; and where "heteroaryl" in each case relates to a 5- or 6-member aromatic ring containing 1-3 heteroatoms selected from a nitrogen atom, oxygen atom and a sulphur atom. The invention also relates to a histamine H3 receptor antagonist or inverse agonist, as well as a preventive or medicinal agent.

EFFECT: obtaining novel biologically active compounds, having histamine H3 receptor antagonist or inverse agonist activity.

11 cl, 8 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts thereof where R1 and R2 together denote a group selected form groups of formula (III-1): , where R9 denotes 1) a lower alkyl group, optionally substituted with a halogen atom or lower alkoxy group, 2) an aryl group, 3) an aralkyl group, 4) a heteroarylalkyl group, 5) a heteroaryl group, where the aryl, aralkyl, heteroarylalkyl and heteroaryl groups can be substituted with a halogen atom, lower alkyl group, optionally substituted with a lower alkoxy group or 1-3 halogen atoms, lower alkoxy group, optionally substituted with 1-3 halogen atoms, cyano group, hydroxy group, alkylsulphonyl group, cycloalkylsulphonyl group, aryl group, heteroaryl group, alkylaminocarbonyl group, alkanoyl amino group, alkyl amino group or dialkylamino group; R10 denotes a lower alkyl group, optionally substituted with 1-3 halogen atoms, or a lower alkylsulphonyl group; X9-X12 denotes a carbon atom or a nitrogen atom, where the carbon atom can be independently substituted with a lower alkyl group, optionally substituted with a halogen atom or a lower alkoxy group, lower alkoxy group, optionally substituted with a halogen atom, or a cyano group or a halogen atom; R3 denotes a) a group of formula (II-1): (ii-U where R4 and R5, taken together with a nitrogen atom, form a 5- or 6-member monocyclic ring, where the monocyclic ring may contain a substitute in form of a lower alkyl group, m1 equals 3; or b) a group of formula (II-2): , where R6 denotes a lower alkyl group or cycloalkyl group; m2 equals 1 or 2; X1-X4 all denote carbon atoms, or one of X1-X4 denotes a nitrogen atom and the rest denote carbon atoms; and where "heteroaryl" in each case relates to a 5- or 6-member aromatic ring containing 1-3 heteroatoms selected from a nitrogen atom, oxygen atom and a sulphur atom. The invention also relates to a histamine H3 receptor antagonist or inverse agonist, as well as a preventive or medicinal agent.

EFFECT: obtaining novel biologically active compounds, having histamine H3 receptor antagonist or inverse agonist activity.

11 cl, 8 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts thereof where R1 and R2 together denote a group selected form groups of formula (III-1): , where R9 denotes 1) a lower alkyl group, optionally substituted with a halogen atom or lower alkoxy group, 2) an aryl group, 3) an aralkyl group, 4) a heteroarylalkyl group, 5) a heteroaryl group, where the aryl, aralkyl, heteroarylalkyl and heteroaryl groups can be substituted with a halogen atom, lower alkyl group, optionally substituted with a lower alkoxy group or 1-3 halogen atoms, lower alkoxy group, optionally substituted with 1-3 halogen atoms, cyano group, hydroxy group, alkylsulphonyl group, cycloalkylsulphonyl group, aryl group, heteroaryl group, alkylaminocarbonyl group, alkanoyl amino group, alkyl amino group or dialkylamino group; R10 denotes a lower alkyl group, optionally substituted with 1-3 halogen atoms, or a lower alkylsulphonyl group; X9-X12 denotes a carbon atom or a nitrogen atom, where the carbon atom can be independently substituted with a lower alkyl group, optionally substituted with a halogen atom or a lower alkoxy group, lower alkoxy group, optionally substituted with a halogen atom, or a cyano group or a halogen atom; R3 denotes a) a group of formula (II-1): (ii-U where R4 and R5, taken together with a nitrogen atom, form a 5- or 6-member monocyclic ring, where the monocyclic ring may contain a substitute in form of a lower alkyl group, m1 equals 3; or b) a group of formula (II-2): , where R6 denotes a lower alkyl group or cycloalkyl group; m2 equals 1 or 2; X1-X4 all denote carbon atoms, or one of X1-X4 denotes a nitrogen atom and the rest denote carbon atoms; and where "heteroaryl" in each case relates to a 5- or 6-member aromatic ring containing 1-3 heteroatoms selected from a nitrogen atom, oxygen atom and a sulphur atom. The invention also relates to a histamine H3 receptor antagonist or inverse agonist, as well as a preventive or medicinal agent.

EFFECT: obtaining novel biologically active compounds, having histamine H3 receptor antagonist or inverse agonist activity.

11 cl, 8 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel prodrugs of biologically active 2,4-pyrimidine diamine compounds with structural formula given below, hydrate, solvate and pharmaceutically acceptable salts thereof. The compounds have properties for inhibiting cascade transmission of a signal from an Fc-receptor, such as FcαRI, FcγRI, FcγRIII and FcεRI, degranulation or Syk kinase activity. Structural formula:

EFFECT: compounds can be used to treat or prevent rheumatoid arthritis and autoimmune diseases.

25 cl, 21 cl, 6 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of general formula (1a-1a), where Va denotes , , ,, WA denotes -O-(C1-6alkylene)-O-, -O- (C2-6alkenylene) O-, -O-(C1-6alkylene)-C(=O)-, -O-(C1-7alkylene) or - (C1-7alkylene)-O-; DA denotes , , , , , , or , EA denotes , , , ,

, m-1 equals 0 or denotes an integer from 1 to 3, w equals 0-5; R5 denotes H, -OH, CH3, C2H5, C3H7, n-C4H9, n-C5H11, n-C6H13, -F, Cl, Br, -OCH3, -OC2H5, -OC3H7, -OC4H9, acetyl, propanoyl, -CF3, -S-CH3; Rz denotes CH3, C2H5, C3H7, C4H9, i-C4H9, -C5H11, -CF3, alkyl, Ph, -OH, -OCH3, -OC2H5, -F, CI, Br, I, acetyl, propanoyl; R11 denotes (1) CH3, C2H5, n-C3H7, i-C3H7, n-C4H9, i-C4H9, fluoro-C4H9, t-C4H9 -C5H11, C6H13, (4)-OH, which can be protected by CH3, C2H5, n-C3H7, i-C3H7, n-C4H9, i-C4H9, fluoro-C4H9, t-C4H9, -C5H11, C6H13, (15) halogen; or pharmaceutically acceptable salt thereof.

EFFECT: compounds have antagonistic effect on the leukotriene receptor, which enables their use as a medicinal agent for preventing or treating leukotriene receptor mediated disease.

10 cl, 8 dwg, 47 tbl, 107 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to phytotherapy. The herbal tea contains haws, motherwort herb, hop cones, peppermint leaves, melilot herb, inula rhizomes and roots, black chokeberry fruits, centaury herb, wild strawberry leaves, melissa herb, green ginger herb, corn stigma and style, mountain ash fruits, caraway fruits in the following proportions 1:1:1:0.5:2:1:1:1:1:2:1:1:1:1 respectively.

EFFECT: use of the invention provides extended range of herbal drugs with an evident therapeutic effect for prevention and treatment of chronic heart disease.

5 ex, 3 dwg, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry, namely to creation of a white turpentine emulsion with a herbal extract showing bracing, tonic and rejuvenating action, containing gum turpentine, baby soap or an emulsifier, camphor spirit, salicylic acid, a water-propyleneglycol herbal extract taken in equal proportions and demineralised water.

EFFECT: various versions of the white turpentine emulsion can be used for prevention and treatment of the locomotor apparatus, cardiovascular system, metabolic disorders (weight reduction and cellulitis).

3 cl

FIELD: chemistry.

SUBSTANCE: in formula (I) Cy1 is a 6-member heterocyclyl containing N as a heteroatom, a 5,6-member monocyclic or 9,10-member bicyclic heteroaryl containing 1-3 heteroatoms selected from N, S and O, phenyl or phenyl condensed with a 5-member heterocycle containing O as a heteroatom, each optionally having 1-3 identical or different substituting Cy1 groups which are: (C1-C6)-acyl, cyano, carboxy, hydroxy, (C1-C6)alkylsulphonyl, (C3-C6)-cycloalkyl, a 6-member heterocyclyl containing 1-2 heteroatoms selected from O and N, phenyl, a 5-member heteroaryl containing 1-3 heteroatoms selected from N, S and O, Y1Y2N-, Y1Y2NC(=O)-, Y1Y2NSO2-, (C1-C6)-alkyl-SO2-N(R5)-C(=O)-, R6-C(=O)-N(R5)-, R7-NH-C(=O)-NH-; (C1-C6)-alkoxycarbonyl; (C1-C6)-alkyl, which optionally contains 1-3 identical or different substitutes which are halogen, carboxy, cyano, hydroxy, Y1Y2N-, Y1Y2N-C(=O)-, R6-C(=O)-N(R5)-, R8-SO2-N(R5)-C(=O)-, 5-member heterocyclyl, containing N as a heteroatom, 5-member heteroaryl containing 1-3 heteroatoms selected from N and O; or (C1-C6)-alkoxycarbonyl; as well as (C1-C6)-alkoxy which optionally have 1-3 identical or different substitutes which are carboxy, (C1-C6)-alkoxycarbonyl, cyano, 3-member heterocyclyl containing O as a heteroatom, or 5-member heteroaryl containing 1-3 heteroatoms selected from N and O; where phenyl or heteroaryl fragments in the substituting Cy1 groups optionally and independently have substitutes represented by hydroxy, (C1-C6)-alkyl, (C1-C6)-alkoxy, carboxy, (C1-C6)-alkoxycarbonyl or R8-SO2-N(R5)-C(=O)-; and where cycloalkyl fragments in the substituting Cy1 groups which optionally and independently have substitutes represented by (C1-C6)-alkoxy, carboxy; Cy2 is a 9-member cycloalkenyl, phenyl, 5,6-member monocyclic or 9,10-member bicyclic heteroaryl containing 1-3 heteratoms selected from N, S and O, or phenyl condensed with a 5,6-member heterocycle containing 1-2 heteroatoms selected from N and O, each independently and optionally having 1-3 identical or different substitutes represented by (C1-C6)-alkoxy, (C1-C3)-alkyl, hydroxy, halogen, halogen-(C1-C6)-alkoxy, nitro, Y1Y2N-; L1 is an alkylene with a straight or branched chain containing 1-6 carbon atoms, optionally substituted carboxy; or L1 is -CH2-(C1-C5)halogenalkylene; L2 is a bond, -O- or -CH2-O-. Other values of radicals are given in the formula of invention.

EFFECT: novel compounds have prostaglandin D2 receptor antagonist properties, can be used in treating primarily allergic disorders such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma, food allergy and other diseases.

39 cl, 1 tbl, 99 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to application in an effective amount and to new nicotine receptor agonists described by general formula (i) or (ii) for treating inflammatory diseases chosen from a group including asthma, chronic obstructive pulmonary disease (COPD), interstitial pulmonary tissue fibrosis (IPF), sarcoidosis, hypersensitivity pneumonitis (HP), chronic hypersensitivity pneumonitis and bronchiolitis obliterans organising pneumonia (BOOP). The compounds (i) and compounds (ii) relate to formulae (i) (ii) where in formula (i) R1 and R2 independently mean alkyl with 1-10 carbon atoms; Xa means CH or N; Ya means one or more substitutes chosen from hydrogen, halogen, cyano, hydroxyl, alkyl with 1-10 carbon atoms optionally substituted with one or more halogen atoms, and alkoxy with 1-10 carbon atoms; n means an integer 0 or 2; J means a counterion representing a compound for maintaining electric neutrality, e.g., halogen, sulphate, sulphonate; in formula (ii) R3 is chosen from or Xb means N or N+-R10; R4 means one or more substitutes chosen from hydrogen, halogen; each R10, R11 and R12 independently means alkyl with 1-10 carbon atoms; provided the presence of the counterion when Xb means N+-R10.

EFFECT: use of nicotine receptor agonists in the effective amount for treating inflammatory diseases.

26 cl, 40 dwg, 3 tbl, 38 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine and concerns cat allergen fused proteins and application thereof. Substance of the invention involves a compositions containing a virus-like particle (VLP) or a viral particle and at least, one antigen, first of all at least, one cat antigen, and more specifically at least one cat antigen which is human allergen. In specific versions of the invention, said antigen represents cat antigen Fel d1 or its fragment covalently bound with the VLP.

EFFECT: invention can be applied for preparing vaccines first of all aimed at treatment and/or prevention of cat dander allergy and other cat antigens and allergens responses.

25 cl, 20 ex, 5 tbl, 4 dwg

FIELD: medicine.

SUBSTANCE: daily in morning hours nasal passages are washed with physiological solution, 10% oil solution of vitamin E in dose 3 drops into each passage is dropped into both nasal passages. After 2 hours transcutaneous impact with constant magnetic field and low-intensity laser irradiation with power 30-80 mW, wavelength 0.85-0.89 mcm, pulse repetition rate 50-80 Hz is carried out on region of projection of thymus, maxillary sinuses, submandibular lymph nodes, spinous process of the third cervical vertebra, mastoid process. Time of impact is 60 seconds per each region. Ozonised olive oil is dropped into each nasal passage in dose 3 drops. After that, by means of light-conducting nozzle performed is impact on anterior parts of inferior nasal conchas with pulse red irradiation with wavelength 0.63-0.65 mcm, pulse power of irradiation at outlet not less than 5 W, pulse repetition rate 50-80 Hz, frequency of light diode modulation - 4-8 Hz. Impact time is 60-120 seconds. Total treatment course is 7 days with 4 month interval, 3 times per year. During the first interval between courses bacterial immunomodulator IRS-19 is introduced in age dose in therapeutic regimen. During the second interval antihomotoxic therapy with drugs Luffel and Lymphomyosot is administered.

EFFECT: method makes it possible to increase treatment efficiency, reduce frequency of disease recurrences, reduce medication load in case of allergic rhinites, which usually require long treatment.

2 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: invention refers to producing versions of group I Poaceae (holy grass) allergen, also can be used either for specific immunotherapy (hyposensitisation) of patients with grass pollen allergy, or for preventive immunotherapy of grass pollen allergies. The produced versions are characterised by Cys41 Ser, Cys57Ser, Cys69Ser, Cys72Ser, Cys77Ser, Cys83Ser and Cysl39Ser substitutes in a Phi p1 mature protein sequence. Also, a structure of the allergen versions can be presented with no fragments relevant to amino acid residues 1-6, 1-30, 92-104, 115-119, 175-185 and 213-220 or 1-6, 115-119 and 213-220 as a part of a primary sequence of Phi p1 mature protein.

EFFECT: invention allows producing a version of group I Poaceae allergen characterised lower IgE responsiveness as compared with common wild allergen and substantially maintained responsiveness to T-lymphocytes.

8 cl, 9 dwg, 2 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to application of N-acyl derivatives of amino acids of general formula

, where n equals 2 or 3 and their pharmaceutically acceptable salts as anti-allergic, anti-inflammatory and anti-anaphylactic medications.

EFFECT: obtaining pharmaceutical composition for treatment of allergic and inflammatory diseases, for instance such as bronchial asthma, allergic rhinitis, pollinosis, psoriasis.

11 cl, 12 tbl, 19 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of general formula (III): , in which D is a benzene ring, 2-pyridone ring, pyridine ring, benzoxalone ring, benzoxadinone ring or benzimidazole ring; R1 denotes carboxy or hydroxy; R2 independently denotes a halogen atom; alkyl optionally substituted with a halogen atom, aryl or alkylamine; alkynyl, optionally substituted alkoxy; hydroxy; carboxy; alkoxy optionally substituted with phenyl, aromatic heterocyclic ring which denotes a 5-6-member aromatic monocyclic carbocyclic ring containing one or two heteroatoms, independently selected from oxygen and nitrogen atoms; alkylsulphonyl; aryloxy; amino optionally substituted with alkyl; acyl optionally substituted with alkyl or alkyloxy; alkyloxycarbonyl; alkanesulphonyl; arylsulphonyl or alkylcarbamoyl; carbamoyl optionally substituted with alkyl, phenyl, cycloalkyl, acetyl, alkanesulphonyl, heteroarylalkyl, cycloalkylalkyl, heteroaryl which denotes a 5-6-member aromatic monocyclic ring containing one or three heteroatoms independently selected from oxygen and nitrogen atoms, and which is optionally substituted with alkyl or cycloalkyl; acylcyano; nitro, aryl; heteroaryl which denotes a 5-6-member aromatic ring containing one or more heteroatoms independently selected from oxygen, sulphur and nitrogen atoms, and which is optionally substituted with alkyl; alkylsulphonyl; morpholinylsulphonyl; non-aromatic heterocyclic group which denotes a 5-6-member non-aromatic heterocyclic ring containing one or more nitrogen atoms and optionally an oxygen and/or sulphur atom; R3 denotes C1-C6alkyloxy, C1-C6alkylthio; R4 denotes a halogen atom or alkyloxy; R5 denotes alkyl; M denotes sulphonyl; L3 independently denotes alkylene optionally containing one oxygen or nitrogen atom, alkenylene, or -N(R7)-; R7 independently denotes a hydrogen atom, alkyl; Y denotes a single bond or CO; Z denotes CH or N; n equals 0 or 1; p equals 0, 1, or 2; q equals 0 or 1; provided that R1 does not denote carboxy when ring D is a benzene ring, -L3- denotes -(O-alkylene)- and the substitution position of L3 and Y is an ortho-position in ring D; to pharmaceutically acceptable salts thereof. The invention also relates to compounds of formula (IV), a pharmaceutical composition, a method of treating diseases associated with the DP receptor, use of compounds in any of the claims 1-17, as well as compounds of general formula (V).

EFFECT: obtaining novel biologically active compounds having DP receptor antagonist activity.

30 cl, 8 ex, 62 tbl

Infant food // 2404785

FIELD: food industry.

SUBSTANCE: invention relates to food and pharmaceutical industry. Infant food composition, containing protein, fats, carbohydrates, nucleotides, nucleosides and nonprotein negatively charged polygalacturonic acid taken at in certain amounts. Application of composition for production of composition for infant feeding. Application of nutrient composition to produce composition for treatment and/or prophylactics of inflammatory disease, diarrhea, eczema and/or atopic dermatitis of a baby.

EFFECT: nutrient composition efficiently imitates protective action of human milk, in particular, against allergies and infections.

9 cl, 4 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds selected from a group comprising 2,3,4,9-tetrahydro-1H-carbazoles of formula I

,

where R1, R2, R3 and R4 independently denote hydrogen, alkyl, alkoxy, halogen, nitro, cyano, trifluoromethyl or formyl, R5 denotes hydrogen, alkyl or -CF3, R6 denotes alkoxy, arylalkoxy, selected from benzyloxy and 1-phenylethoxy, or -NR7R8, R7 and R8 independently denote hydrogen, alkyl, cyanoalkyl, alkenyl, where alkenyl is ethenyl, 2-propenyl, 2-methyl-2-propenyl, 3-butenyl, 4-pentenyl or 5-hexenyl; aryl, where aryl is a phenyl or naphthyl radical, where said radicals can optionally be monosubstituted with a halogen, alkyl, alkoxy, -CF3, -OCF3, phenylalkyl or phenylcarbonyl; or disubstituted with a substitute independently selected from halogen, alkoxy and phenyl; arylalkyl, where arylalkyl is phenylalkyl, where the alkyl group can optionally be substituted with phenyl; phenylalkyl, where the phenyl ring can optionally be substituted with methylenedioxy; phenylalkyl which is disubstituted with a halogen; phenylalkyl which is monosubstituted with a halogen, -CF3, -OCHF2, alkyl or alkylsulfanyl; or naphthylalkyl; phenylcarbonyl; cycloalkyl, where cycloalkyl is a cyclopentyl or cyclohexyl radical, where said radicals can optionally be substituted with a condensed benzene ring; pyridylalkyl; thienylalkyl; or R7 and R8 together with a nitrogen atom to which they are bonded form a heterocyclic 5-, 6-, 7- or 8-member ring system containing 1-3 heteroatoms selected from nitrogen, oxygen and sulphur atoms, wherein said cyclic system can optionally be substituted with (1) one or two condensed benzene rings, where the benzene rings are unsubstituted or substituted with one or two substitutes independently selected from a group comprising C1-C4alkyl, C1-C4alkoxy, halogen, -CF3 and -OCF3; (2) unsubstituted phenyl ring, (3) mono- or disubstituted phenyl ring, where the substitutes are independently selected from a group comprising halogen, C1-C4alkyl, C1-C4alkoxy, -CF3 and -OCF3; or (4) phenylalkyl, where the alkyl group is substituted with phenyl; where the term "alkyl", separately or in any combination, denotes a saturated straight or branched hydrocarbon chain containing 1-7 carbon atoms; where the said alkyl group is unsubstituted unless stated otherwise; or to pharmaceutically acceptable salts thereof. Invention also relates to a pharmaceutical composition and to use of compounds in claim 1.

EFFECT: obtaining novel biologically active compounds having CRTH2 receptor antagonist activity.

13 cl, 5 tbl

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to allergology, and can be applied for treatment of allergic rhinitis of domestic etiology. For this purpose in treatment included is allergen-specific immunotherapy with sublingual introduction of cause-significant allergen. Simultaneously hirudotherapy with application of medical leech on skin in region of oral cavity bottom projection is carried out. Procedures are carried out 2 times per week, starting from 0.1 ml 10-6 degree of dissolving of cause-significant allergen and bringing up to 0.5 ml of undissolved allergen, which after that is introduced 1 time per 2 weeks during 3 years.

EFFECT: invention allows to increase treatment efficiency due to increase of cause-significant allergen penetration into system of organs of mucosal immunity of upper airways.

1 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to psychiatry and gynecology, and can be used in treatment of endometriosis in women with anxiety-and-depressive disorders. For this purpose one month after performing laparoscopy at the background of drug hormonal treatment during 6 months phenotropil in dose 100 mg/day is additionally administered for 90 days.

EFFECT: administration of phenotropil in said dose and introduction regimen makes it possible to reduce anxiety-and-depressive symptoms, and has positive impact on functional state of immune and vegetative nervous system.

4 tbl, 3 ex

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