Composition for prevention or treatment of chronic obstructive pulmonary diseases containing monoacethyldiglycerol compounds as active ingredient

FIELD: pharmacology.

SUBSTANCE: compounds of this invention reduce the expression level of CXCL-1, TNF-α or MIP-2, and thus do not have the side effects of the currently used therapeutic agents for chronic obstructive pulmonary disease treatment, are non-toxic and have an excellent therapeutic effect, so that they can be useful as a composition for prevention, treatment and reduction of chronic obstructive pulmonary diseaseseverity.

EFFECT: prevention of chronic obstructive pulmonary disease containing monoacetyl diacylglycerin as an active ingredient.

10 cl, 6 ex, 8 tbl

 



 

Same patents:

Crystals // 2556206

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention describes crystals of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulphonyl)acetamide ("compound A"), as a form I of the compound A crystal, which shows diffraction peaks at 9.4 degrees, 9.8 degrees, 17.2 degrees and 19.4 degrees in its power X-ray diffraction spectrum, as a form II of the compound A crystal, which shows diffraction peaks at 9.0 degrees, 12.9 degrees, 20.7 degrees and 22.6 degrees in its power X-ray diffraction spectrum, as a form III of the compound A crystal, which shows diffraction peaks at 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees and 23.5 degrees in its power X-ray diffraction spectrum. There are also described methods for producing the forms I, II and III of the compound A crystal, based pharmaceutical composition and PGI2 receptor agonist agent, an accelerating agent for angiogenic therapy, gene engineering or autoimmune bone marrow transplantation, and an accelerating agent for angiogenesis for peripheral artery recovery or angiogenic therapy on the basis thereof; there are also described a preventive or therapeutic agent for a wide range of diseases and conditions.

EFFECT: preparing the new therapeutic agent for the wide range of diseases and conditions.

11 cl, 6 dwg, 6 tbl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to a novel compound of formula

(I)

or its pharmaceutically acceptable salt, possessing properties of the IKKβ and TNFα inhibitor. The compound can be used with an additional therapeutic agent, selected from vincristine, camptothecin hydrochloride (CPT-11), lefunomid, dexamethasone and TNFα. Preferable are compounds of formula (I), corresponding to 2-{5-chloro-2-[(1R,2R)-2-hydroxycyclopentylamino]pyrimidin-4-yl}-N-cyclopropyl-1H-indole-4-carboxamide and 2-{5-chloro-2-[(1R,2S)-2-hydroxycyclopentylamino]pyrimidin-4-yl}-N-cyclopropyl-1H-indole-4-carboxamide.

EFFECT: compound can be applied in the treatment of inflammatory diseases such as rheumatoid arthritis, chronic obstructive lung disease, bronchial asthma, multiple sclerosis and intestinal inflammatory diseases, or cancer diseases, such as multiple myeloma, colon cancer, pancreas cancer and ovary cancer, by IKKβ inhibition.

30 cl, 4 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to the novel and unexpected application of sulphated hyaluronic acid as a cytokine activity regulator for the prevention and/or treatment of asthma and degenerative joint osteoarthritis, associated with the activation of IL-1, IL-2, IL-6, IL-7, IL-8 and IL-12, the said sulphated hyaluronic acid has a molecular weight from 10000 to 50000 Da, from 150000 to 250000 Da and from 500000 to 750000 Da and where sulphated hyaluronic acid has a sulphation degree equal to 3.

EFFECT: invention provides the extension of an arsenal of means for the prevention and/or treatment of asthma and degenerative joint osteoarthritis.

3 cl, 25 ex, 4 tbl, 12 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to a novel crystalline form of N-[-2[[(2,3-difluorophenyl)methyl]thio]-6-{[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]-1-azatidine-sulphonamide, which has an X-ray powder diffractogram, measured with the application of a wavelength of X-rays of 1.5418 E and containing, at least, one crystalline peak with a value 2-theta (in degrees) 21.0, 28.8 and/or 29.1; or containing, at least, 2 crystalline peaks with a value 2-theta (in degrees) 21.0, 28.8 and/or 29.1; or containing, at least, 3 crystalline peaks with a value 2-theta (in degrees) 21.0, 28.8 and/or 29.1. The said crystalline form can contain additional crystalline peaks with a value 2-theta (in degrees), selected from 12.9 and 18.0, obtained under the said conditions.

EFFECT: crystalline form has the X-ray powder diffractogram, measured with the application of a wavelength of X-rays of 1,5418 E, with the crystalline peaks with a value 2-theta (in degrees) 12,9, 13,1, 18,0, 21,0, 22,5, 25,1, 25,3, 28,8, 29,1 and 30,4, and has melting point (beginning) 152,7°C.

6 cl, 3 dwg, 2 tbl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a citrate of a compound described by formula (II) below, and a pharmaceutical composition containing said citrate.

EFFECT: experimental results of the present inventions prove that said citrate can inhibit activity of phosphodiesterase type 5 and can be used for treating erectile dysfunction, for inhibiting thrombocyte aggregation and treating thrombosis, for reducing pulmonary hypertension and treating cardiovascular diseases, asthma and diabetic gastroparesis.

2 cl

FIELD: medicine.

SUBSTANCE: baseline therapy is accompanied by administering "Enterosgel" 1.5-2 hours prior to or 2 hours after a meal or medication intake in the children aged from 5 to 10 years old in an amount of 15 g 2 times a day, aged from 11 to 15 years old in an amount of 15 g 3 times a day for 7 days; "Qudesan" is administered orally with a meal before noon in age-specific doses: from 5 to 7 years old - 10-16 drops (15-24 mg), from 8 to 15 years old - 16-20 drops (24-30 mg), diluted in a small amount of boiled water or any other beverage of room temperature, once a day for 30 days; "Pantogam" is administered orally 15-20 minutes after a meal in age-specific doses: from 5 to 7 years old - 500 mg 2 times a day, from 8 to 15 years old - 500 mg 3 times a day for 30 days; the combined administration of the above preparations is repeated every 6 months.

EFFECT: method enables reducing the risk of partially controlled forms of bronchial asthma considerably by the pronounced positive synergic effect of the above drug preparations.

4 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and represents using sulphated hyaluronic acid for preparing a therapeutic agent for local administration for treating inflammatory/irritating skin diseases specified in dermatitis, atopic dermatitis, photocontact dermatitis, rash, vitiligo, eczema, psoriasis, all skin irritations related to activation of anti-inflammatory cytokines, such as IL-1, IL-2, IL-7, IL-8, IL-9 and TNF, wherein hyaluronic acid has a molecular weight falling within the ranges of 10000 D to 50000 D, 150000 D to 250000 D and 500000 D to 750000 D, and a sulphatation degree equal to 1.

EFFECT: invention provides stimulating the immune system protein synthesis for eliciting the immune response.

8 cl, 33 ex, 15 dwg, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to medicine and aims at preventing and treating respiratory diseases, disorders or conditions. Implementing a method for preventing or treating the respiratory diseases, disorders or conditions involves administering a therapeutically effective amount of tetomilast and at least one beta2-adrenoreceptor agonist into the patient. According to the other embodiment, tetomilast and at least one beta2-adrenoreceptor agonist are administered together with at least one anti-inflammatory steroid. What is also presented is a pharmaceutical composition containing tetomilast and at least one beta2-adrenoreceptor agonist.

EFFECT: using the declared group of inventions provides the more effective prevention and treatments of respiratory diseases, disorders or conditions.

46 cl, 3 dwg, 6 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: treating bronchial asthma is ensured by superior laryngeal nerve anaesthesia with 0.5% Novocaine mixed with 96° rectified ethyl alcohol for the purpose of bronchial spasmolysis in bronchial asthma.

EFFECT: method enables reducing an episode of bronchial asthma quickly and for long duration by interrupting a flow of pathologic nerve impulses along the superior laryngeal nerve.

2 tbl, 1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula , where: R1, R2, R3, R4, R5 and R6, each independently, denote hydrogen, halogen, cyano, nitro or C1-6alkyl; X denotes O or S; RYa denotes -C(O)R1a, -C(O)OR1a, -C(O)NR1bR1c, -C(S)NR1bR1c, -C(NNO2)NR1bR1c, -S(O)2R1a or -S(O)2NR1bR1c; under the condition that RYa is not -C(O)O-tert-butyl; and each R1a, R1b and R1c independently denotes hydrogen, C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, C6-14aryl, 5-10-member heteroaryl containing one, two or three heteroatoms selected from O, N or S, or morpholinyl; or each pair of R1b and R1c, together with the N atom to which they are bonded, independently forms morpholinyl; under the condition that the compound is not 4-(2-(3,5-dimethylphenoxy)-5-nitrophenylsulphonyl)piperazine-1-carbaldehyde; wherein each alkyl, alkenyl, aryl and 5-10-member heteroaryl, containing one, two or three heteroatoms selected from O, N or S, is optionally substituted with one or more groups, each independently selected from (a) cyano, halogen and nitro; (b) C1-6alkyl, C6-14aryl, furanyl and morpholinyl, each optionally substituted with one or more substitutes Q; (c) -C(O)Ra, -C(O)ORa, -ORa and -SRa, wherein each Q is independently selected from a group consisting of (a) cyano, halogen and nitro; (b) C1-6alkyl and C2-6alkenyl; and (c) -C(O)Re, -C(O)ORe, and -SRe; where each Re, Rf and Rg independently denotes (i) hydrogen; (ii) C1-6alkyl or C2-6alkenyl, which are suitable for modulating CCR3 activity.

EFFECT: obtaining compounds which are suitable for modulating CCR3 activity.

41 cl, 1 tbl, 4 ex

FIELD: veterinary medicine.

SUBSTANCE: complex antibacterial agent for animals, containing a compound from the group of fluoroquinolones and auxiliary substances, characterised in that it additionally comprises a compound from the group of pleuromutilins in an effective amount.

EFFECT: invention is effective against vegetative and spore forms of bacteria, it is harmless, has no allergenic properties, has a stimulating effect on the indices of humoral immune response, and is stable during storage.

6 cl, 9 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of formula , which is a methylhydrofumarate (MHF) prodrug. In formula (I), radicals and symbols have the values specified in the patent claim. The invention also refers to a pharmaceutical composition containing the declared methylhydrofumarate drugs, to using the declared methylhydrofumarate drugs and the pharmaceutical composition containing them, for treating diseases, such as psoriasis, asthma, multiple sclerosis, inflammatory intestinal disease and arthritis, and to a method of treating the above diseases.

EFFECT: higher oral bioavailability and plasma MHF, dimethylfumarate and/or other metabolites.

47 cl, 1 tbl, 54 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical compositions, in particular to pharmaceutical composition, recovering visual pigment in case of insufficiency of endogenic 11-cis-retinal, which contains effective quantity of retinal derivatives and pharmaceutically acceptable carrier, where retinal derivative is converted into retinal, capable of forming functional complex opsin/retinal, where retinal derivative represents ester of 9-cis-retinyl of formula

ester of 11-cis-retinyl of formula or their combination, where A in each case stands for CH2OR and R represents ester-forming carboxylate radical of monocarboxylic acid C1-C10 or polycarboxylic acid, selected from oxalic acid, succinic acid, malic acid, glutaric acid, adipic acid, pimelic acid, suberic acid, azelaic acid, sebacic acid, citric acid, ketoglutaric acid, fumaric acid, malonic acid and oxalacetic acid, which is substituting group in ester, where 11-cis-retinal insufficiency is caused by mutation in genes, coding proteins RPE65 and LRAT.

EFFECT: invention relates to method of recovering photoreceptor function or attenuation of loss of photoreceptor function; and to application of said retinal derivative for drug manufacturing.

43 cl, 7 dwg, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical compositions, in particular to pharmaceutical composition, recovering visual pigment in case of insufficiency of endogenic 11-cis-retinal, which contains effective quantity of retinal derivatives and pharmaceutically acceptable carrier, where retinal derivative is converted into retinal, capable of forming functional complex opsin/retinal, where retinal derivative represents ester of 9-cis-retinyl of formula

ester of 11-cis-retinyl of formula or their combination, where A in each case stands for CH2OR and R represents ester-forming carboxylate radical of monocarboxylic acid C1-C10 or polycarboxylic acid, selected from oxalic acid, succinic acid, malic acid, glutaric acid, adipic acid, pimelic acid, suberic acid, azelaic acid, sebacic acid, citric acid, ketoglutaric acid, fumaric acid, malonic acid and oxalacetic acid, which is substituting group in ester, where 11-cis-retinal insufficiency is caused by mutation in genes, coding proteins RPE65 and LRAT.

EFFECT: invention relates to method of recovering photoreceptor function or attenuation of loss of photoreceptor function; and to application of said retinal derivative for drug manufacturing.

43 cl, 7 dwg, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the pharmaceutical industry, particularly to a composition for treating or preventing the human immunodeficiency virus (HIV) or hepatitis C. The herbal composition used for treating or preventing the patients infected by the HIV or hepatitis C viruses and containing a herbal ingredient with tannin agents and catechin, and a pharmaceutically acceptable carrier; the herbal ingredient is Agrimonia Eupatoria (GAFT) and/or gambier (Uncaria gambir). A method for preparing the herbal composition for treating or preventing the patients infected by the HIV or hepatitis C viruses.

EFFECT: composition is effective for treating or preventing the patients infected by the HIV or hepatitis C viruses.

12 cl, 6 dwg, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and represents a controlled-release preparative form of diacerein administered once a day for treating or autoimmune diseases or their complications. The preparative form contains a core, an active layer, a sustained-release film layer and a delayed-release film layer, wherein the active layer is followed by the sustained-release film, and the delayed-release film layer thereafter. The sustained-release film layer contains ethyl cellulose polymer, povidone, triethylacetate and talc; the delayed-release film layer contains Eudragit polymer, triethylacetate and talc.

EFFECT: reducing the negative side action of diacerein.

18 cl, 23 ex, 33 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmacology and oncology, particularly to a new antitumour agent. Beta-ethyldiphacyl is presented to be used as an agent of an epithelial tumour (carcinoma) inhibition. There is provided to administer Ethyldiphacyl in doses of 15-50 mg/kg both before, and after the tumour grafting; the therapeutic course is up to 2 months after the tumour grafting with administrations following every 6-7 days; or preventive administration is performed 2-24 hours before the tumour grafting.

EFFECT: technical effect consists in prolonging the life of mammals suffering the from the tumour by 30%; the life is not burdened with the disease progression.

4 cl, 1 tbl

FIELD: medicine.

SUBSTANCE: invention refers to medicine and aims at treating the non-alcoholic fatty liver disease. Increasing a transaminase level to three normal values inclusively requires applying essential phospholipids for 2-3 months twice a year that is followed by using statin 10-20 mg in a combination to ursodeoxycholic acid 15-20 mg/kg for 3-6 months. If the transaminase level exceeds three normal values, the treatment is isolated and includes ursodeoxycholic acid 15-20 mg/kg for 3-6 months.

EFFECT: method enables providing the higher clinical effectiveness of the non-alcoholic fatty liver disease.

3 ex

FIELD: medicine.

SUBSTANCE: therapeutically effective amount of ethyl methyl hydroxypyridine succinate and calcium atorvastatin, as well as additives in the form of lactose and magnesium stearate are encapsulated in gelatine. Ethyl methyl hydroxypyridine succinate and magnesium stearate is placed into an inner smaller gelatine capsule inside a main outer gelatine capsule containing atorvastatin, lactose and magnesium strearate. The ingredient ratio in the inner capsule makes, wt %: Ethyl methyl hydroxypyridine succinate 96.2-98.6; magnesium stearate 1.4-3.8, and the ingredient ratio in the outer capsule makes, wt %: calcium atorvastatin 10.0-45.0; lactose 52.0-89.0; magnesium stearate 1.0-3.8.

EFFECT: method enables providing the higher pharmaceutical effectiveness of the preparation and prolonging the shelf-life by preventing atorvastatin degradation.

3 cl, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relates to medicine, in particular to a composition, the application of the composition and a method of treating abuse with substances, causing painful addiction in a subject. The composition contains a carbamoyl compound, or its pharmaceutically acceptable salt, or an ester as an active ingredient and the method includes the introduction of a therapeutically effective quantity of the carbamoyl compound, or its pharmaceutically acceptable salt, or the ester.

EFFECT: composition is used for the treatment of abuse with substances, causing painful addiction in a subject, as well as to an improvement of behaviour associated with the abuse.

14 cl, 1 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical industry, namely represents composition, which contains mixture of particles of hydrophobic silicon dioxide aerogel, which have specific area of surface per weight unit (Sw) in range from 500 to 1500 m2/g and size, expressed in form of volume mean diameter (D[0.5]), in range from 1 to 1500 mcm, and at least one first linear silicone oil, which has viscosity higher than 50 mm2/s, and at least second and third linear silicone oils, and each of them has viscosity lower than or equal 50 mm2/s.

EFFECT: mixture of particles of silicon dioxide aerogel and linear oils provides possibility of obtaining compositions, which provide comfort and smoothness of skin after application and have dullness and "soft focus"-adding properties.

23 cl, 8 ex

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