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![Novel crystalline forms of n-[-2[[(2,3-difluorophenyl)methyl]thio]-6-{[(1r,2s)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]-1-azatidine-sulphonamide](http://img.russianpatents.com/img_data/1202/12027164-s.gif)
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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. |
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Compound possessing inhibitory action on phosphodiesterase type 5, and method for preparing it Present invention refers to a citrate of a compound described by formula (II) below, and a pharmaceutical composition containing said citrate. |
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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. |
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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. |
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Methods of using thiazol derivatives 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. |
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Method of treating bronchial asthma 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. |
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Arylsulphonamide ccr3 antagonists 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. |
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Group of inventions refers to organic chemistry, namely to a compound of formula I and to their pharmaceutically acceptable salt or their ester, wherein W means C(H)2, C(H)2-C(H)2 or C(H)(CH3); X is specified in a group consisting of: (1) O, (2) N(H), (4) S, (5) S(O) and (6) S(O)2; Y means carbon or nitrogen; R1 is specified in a group consisting of: (1) hydrogen, (2) halogen, (3) methyl optionally substituted by fluorine, (4) C1-7alkoxygroup optionally substituted by fluorine, (5) cyano group and (6) C1-7alkylsulphonyl; R2 means hydrogen, fluorine, chlorine or C1-7alkoxygroup; R3 means hydrogen, fluorine, chlorine, bromine or methyl; R4 is specified in a group consisting of: (1) hydrogen, (2) halogen, (3) C1-7alkyl optionally substituted by fluorine, (4) C3-7cycloalkyl, and (5) ethenyl; R5 and R6 are independently from each other specified in a group consisting of: (1) hydrogen, (2) halogen, (3) C1-7alkyl, (4) cyanogroup and (5) C3-7cycloalkyl; R7 means cyano group or S(O)2-R8, wherein R8 is specified in a group consisting of: (1) C1-7alkyl, (2) C3-7cycloalkyl, (4) C1-7alkylamino group, (5) C1-7dialkylamino group, (6) lower heterocycloalkyl optionally substituted by halogen, C1-7alkyl, or C1-7alkoxycarbonyl and (7) 2-oxa-6-azaspiro[3.3]hept-6-yl, wherein lower heterocycloalkyl means a saturated or partially unsaturated non-aromatic ring fragment containing 3 to 7 atoms bound together to form a ring structure, wherein one, two or three ring atoms are heteroatoms, whereas the rest ring atoms are carbon atoms; and pharmaceutically acceptable esters represent methyl and ethyl acid esters of formula I acceptable as prodrugs. The invention also refers to a pharmaceutical composition based on the compound of formula . |
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Substituted isoquinolines and isoquinolinones as rho-kinase inhibitors Invention refers to substituted isoquinolines and isoquinolinones of formula (I) and to their stereoisomer and/or tautomer forms and/or pharmaceutically acceptable salts, wherein R1 is H, OH or NH2; R3 is H; R4 is H, halogen or (C1-C6)alkylene-R'; R5 is H, halogen, (C1-C6)alkyl; R7 is H, halogen, (C1-C6)alkyl, O-(C1-C6)alkyl; R8 is H; R6 is absent; or is one of (C1-C4)alkylene related to a cycloalkyl ring related to a cycloalkyl ring, wherein (C1-C4)alkylene forms a second bond to another carbon atom of the cycloalkyl ring to form a bicyclic ring system, R10 is H, phenyl, or pyridine, wherein phenyl is unsubstituted or substituted; R11 is H, (C1-C6)alkyl; or R11 and R12 together with the carbon atom to which they are attached form (C3)cycloalkyl; R12 is (C1-C6)alkyl, (C3-C8)cycloalkyl or phenyl; or R12 is H, provided r=2 and another R12 is other than H; or R11 and R12 together with the carbon atom to which they are attached form (C3)cycloalkyl; R13 and R14 are independently H, (C1-C6)alkyl, (C1-C6)alkylene-R', C(O)O-(C1-C6)alkyl, n is equal to 0; m is equal to 1 or 2; s is equal to 1 or 2; r is equal to 1 or 2; L is O, NH; R' is (C3-C8)cycloalkyl, (C6-C10)aryl; wherein in R11 and R12 residues, alkyl is unsubstituted or optionally substituted by one OCH3; wherein in R11 and R12 residues, alkyl is unsubstituted or optionally substituted by one or more halogens; wherein in R10 and R12 residues, (C6-C10)aryl is unsubstituted or optionally substituted by one or two groups optionally specified in halogen, CN, (C1-C6)alkyl, O-(C1-C6)alkyl, SO2-(C1-C6)alkyl, CF3 and OCF3. Also, the invention refers to using a compound of formula (I). |
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Combined aerosol preparation for treating respiratory diseases As active ingredients, a formulation contains fenoterol hydrobromide and ipratropium bromide monohydrate; the excipients are absolute ethanol, triethylcitrate, propellant 1,1,1,4 tetrafluoroethane (HFA-134a) and/or 1,1,1,2,3,3,3-heptafluoropropane (HFA-227ea) and a pharmaceutically acceptable acid specified in hydrochloric, orthophosphoric and citric acids. |
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2,5-disubstituted arylsulphonamide ccr3 antagonists Invention relates to compounds of formula I, possessing a modulating action with respect to the CC chemokine receptor 3 (CCR3), a based on them pharmaceutical composition, versions of treatment methods and a method of controlling the CCR3 activity. In the general formula I R1 and R2 represent halogen or C1-6alkyl; R3 represents cyano or nitro; R4 represents or ; R5 represents oxo; C1-6alkyl, optionally substituted with halogen atoms; or C(O)OR1a; X represents O or S; Y represents -O-, -S-, -N(R1a)-, -C(R1a)(R1d)- or -C(R1a)(NR1bR1c)-; m represents an integer number from 0 to 2; n represents 1; p represents an integer number from 0 to 2; r represents 1 or 2; and each R1a, R1b, R1c and R1d represents (a) hydrogen; (b) C3-7cycloalkyl; or (c) C1-6alkyl, optionally substituted with hydroxyl, or each pair R1b and R1c together with a N atom, which they are bound to, form imidazoimidazolyl, substituted with oxo, butyl or chlorine, or heterocycle, containing 5 or 6 atoms in a cycle. |
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Invention relates to bi- and polycyclic substituted isoquinoline and isoquinolinones of formula (I), or to its stereoisomeric and/or tautomeric forms and/or to its pharmaceutically acceptable salts, where R1 represents OH; R3, R4, R5 and R8 represents H; R7 represents halogen or (C1-C6) alkyl; R6 represents one (C1-C4)alkylene, bound to a cycloalkyl ring, in which (C1-C4)alkylene forms the second bond with the other carbon atom of the cycloalkyl ring with the formation of a bicyclic ring system, where in the bicyclic ring system one carbon atom is substituted with a group, independently selected from O, S or SO2; and if m and s equal 2 or m equals 3 and s equals 1, R6 represents a group CH2-CH-(CH2)2, which via one group CH2 is bound to the cycloalkyl ring, and two other CH2 groups are bound to different carbon atoms of the cycloalkyl ring, and if m equals 3 and s equals 3, R6 represents two methylene groups, bound to different carbon atoms of the cycloalkyl ring, where the methylene groups or group CH2-CH-(CH2)2 are bound to the carbon atoms of the cycloalkyl ring and form an adamantane system of formula (XX) , where L can be bound to any secondary or tertiary carbon atom, or R6 together with R11 and an N atom form (C5) heterocycloalkyl, bound with the cycloalkyl residue in the form of a spirocyclic ring system, where the bicyclic ring system, or the adamantane system, or a ring system, containing (C5) heterocycloalkyl, represent non-substituted or optionally substituted with substituent R9; R9 represents (C1-C6)alkyl, (C2-C6)alkenyl, (C6)aryl or cyclopropyl R11 and R12 independently on each other represent H or (C1-C6)alkylene-(C6)aryl; n equals 0 or 1; m equals 2 or 3; s equals 1, 2 or 3; L represents O; its stereoisomeric and/or tautomeric forms and/or its pharmaceutically acceptable salts. The invention also relates to the application of a formula (I) compound. |
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Invention relates to compounds of general formula (I), possessing an activity with respect to cytokines, versions of based on them pharmaceutical compositions and their application. Formula (I) compounds can be applied for treatment or prevention asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis or gouty arthritis. In general formula (I) L is selected from the group, consisting of -C(O)-, -CH2-, Ar1 represents a mono-, di- or trisubstituted phenyl ring, where substituents are independently selected from the group, consisting of a halogen and -C1-4alkyl; Ar2 represents an optionally substituted thiadiazolyl ring, where the substituent represents -C1-4alkyl, -C3-5cycloalkyl, -methylcyclopropyl, phenyl or a 5- or 6-membered monocyclic heteroaromatic ring or a bicyclic heteroaromatic ring with 9 or 10 atoms, with the said heteroaromatic ring containing 1, 2 or 3 heteroatoms, selected from the group, consisting of S, O and N, where the said phenyl or heteroaromatic ring is optionally mono- or disubstituted with substituents, independently selected from the group, consisting of a halogen, -C1-6alkyl, optionally substituted with 1-4 fluorine atoms, -O-C1-6alkyl, -CF3 and oxo. |
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6-substituted isoquinolines and isoquinolinones effective as rho-kinase inhibitors Invention refers to 6-substituted isoquinoline and isoquinolinone derivatives of formula or to its stereoisomer and/or tautomer forms and/or a pharmaceutically acceptable salt, wherein R1 represents H, OH or NH2; R3 represents H; R4 represents H, a halogen atom, CN or (C1-C6)alkylene-(C6-C10)aryl; R5 represents H, a halogen atom, (C1-C6)alkyl; R7 represents H, a halogen atom, (C1-C6)alkyl, O-(C1-C6)alkyl; R8 represents H; R9 and R6 are absent; R10 represents (C1-C6)alkyl, (C1-C8)heteroalkyl, (C3-C8)cycloalkyl, (C6)hetrocycloalkyl, (C1-C6)alkylene-(C3-C8)cycloalkyl, (C1-C6)alkylene-(C6-C10)aryl, (C1-C6)alkylene-(C6)heterocycloalkyl; R11 represents H; R12 represents (C1-C6)alkyl, (C3-C8)cycloalkyl, (C5)heteroaryl or (C6-C10)aryl; R13 and R14 independently represent H, (C1-C6)alkyl, (C1-C6)alkylene-R'; n is equal to 0; m is equal to 2 or 3; s is equal to 1 or 2; r is equal to 1; L represents O or NH; R' represents (C3-C8)cycloalkyl, (C6-C10)aryl; wherein in the rests, R10, R12-R14 alkyl or alkylene are unsubstituted or optionally substituted by one or more OCH3; wherein in the rests, R10, R12-R14 alkyl or alkylene are unsubstituted or optionally substituted by one or more halogen atoms; wherein (C1-C8)heteroaryl group means (C1-C8)alkyl groups, wherein at least one carbon atom is substituted by O;. (C6)heterocycloalkyl group means a monocyclic carbon ring system containing 6 ring atoms wherein one carbon atom can be substituted by 1 oxygen atom or 1 sulphur atom which can be optionally oxidated; (C5)heteroaryl means a monoring system wherein one or more carbon atoms can be substituted by 1 nitrogen atom or 1 sulphur atom or a combination of various heteroatoms. Also, the invention refers to using the compound of formula (I) and to a therapeutic agent based on the compound of formula (I). |
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2,5-disubstituted arylsulphonamide ccr3 antagonists Invention relates to 2,5 substituted arylsulphonamides of formula (Ia) or to their pharmaceutically acceptable salts, solvates, hydrates, stereoisomers or tautomers, where X represents S, SO or SO2; Y and Z represents (i) Y represents NR5; and Z represents =O, CO2R6 or C1-6alkyl; or (ii) Y represents CH2, CHF, CHCH3, O, S or SO2; and Z represents hydrogen or C1-6alkyl; R1 and R2 each independently represents halogen, C1-6alkyl or C1-6 halogenalkyl; R3 represents CN or NO2; R4 represents hydrogen or C1-6alkyl; R5 represents hydrogen or C1-6alkyl; and R6 represents hydrogen or C1-6alkyl. Invention also relates to compounds of formula (I) and (II), values of radicals of which are given in the invention formula, specific compounds, pharmaceutical composition based on compound of formula |
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Invention refers to medicine, namely to therapy and infectious diseases, and can be used for preventing and treating bronchial asthma, complicating respiratory viral infections and other respiratory inflammatory diseases. That is ensured by a combined inhibition of p-gene of the respiratory syncytial virus (further - RSV) and anti-inflammatory murine il-5 gene; p-gene of the RSV required for the cell replication is inhibited using a created molecule of small interfering RNA (siRNA) - SEQ ID NO 1 (siP1), while anti-inflammatory murine il-5 gene is inhibited using a created molecule of siRNA - SEQ ID NO 15 (siIL4-408). They are used to develop preparations containing therapeutically effective amounts thereof to be used intranasally. |
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Phenylpyrimidone derivatives, pharmaceutical compositions, methods for preparing and using them Present invention refers to new phenylpyrimidone derivatives of formula I possessing the properties of a phosphodiesterase type 5 (PDE5) inhibitor. The compounds of formula I can be used for treating various vascular disorders, such as erectile dysfunction, pulmonary arterial hypertension, etc. In formula each R1 and R2 independently means H; C1-C10alkyl; halogen; CF3; CN; OR5; NR6R7; NHCOR8; aryl; or C1-C4alkyl optionally substituted by OR5; Z means OR3; R3 means C1-C6alkyl or C1-C3alkyl, substituted by C1-C3alkoxy group; R4 means SO2NR6R7; NR9R10, providing NR9R10 is other than NH2; COR11; OR12; or R4 means 5-6-merous heterocyclyl optionally substituted by one or more substitutes specified in a group consisting of OH and C1-C6 alkyl; or R4 means 5- or 6-merous cyclic monosaccharide group; R5 means C1-C6alkyl; C1-C4alkyl optionally substituted by C1-C4alkoxy group; each R6 and R7 independently means H, OH, C1-C6alkyl, C1-C6alkoxy group, C3-C6alkenyl, C3-C6cycloalkyl, adamantyl, C3-C8lactamyl, aryl, Het or (CH2CH2O)jH, wherein j is 1-3; or each R6 and R7 independently means C1-C6alkyl, optionally substituted by OH, C1-C4alkoxy group, SO3H, SO2NR13R14, SO2R16, NR13R14, aryl, Het or 5-6-merous heterocyclyl; or each R6 and R7 independently means 5-6-merous heterocyclyl optionally substituted by one or more substitutes specified in a group consisting of C1-C6 alkyl and C1-C6alkyl substituted by hydroxyl; or R6 and R7 together with a nitrogen atom attached whereto form 5-7-merous heterocyclyl optionally substituted by one or more substitutes specified in a group consisting of OH, COOR8, (CH2CH2O)jH, wherein j is 1-3, C1-C4alkoxy group, Het and C1-C6alkyl substituted by aryl; or R6 and R7 together with a nitrogen atom attached whereto form a glucosyl amino group, an amino acid residue, a residue of an amino acid ester or an amino amide residue. The other radical values are specified in the patent claim. |
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Invention relates to medicine and the pharmaceutical industry and describes a pharmaceutical inhaled medication for treatment of bronchial asthma and chronic obstructive lung disease, containing micronised tiotropium bromide as an active substance, and which contains as a carrier lactose with the average particle size of 120-200 mcm, sodium benzoate, sieved with a bulk density within the range of 0.30-0.50 g/cm3 and sodium benzoate micronised with the average particle size of 0.5-10 mcm with a specified content of components per a dose of medication. |
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Low-molecular polysulphated hyaluronic acid derivative and medicinal agent containing same Invention relates to an agent for preventing and/or treating an allergic disease selected from pollinosis, allergic rhinitis, allergic conjunctivitis, atopic dermatitis and asthma, which is a low-molecular polysulphated hyaluronic acid derivative. |
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Using glucocorticoid composition for treating severe and uncontrolled asthma Invention refers to methods of treating a patient suffering from severe and uncontrolled asthma which involve pulmonary administration of a glucocorticoid in the form of a vapour-phase nebulised aerosol in a combination with oral administration of a glucocorticoid. According to one of the declared methods, the nebulised aerosol is administered by inhalation at no more than 20 l/min rate in the total inhalation volume of at least 0.4 l of the vapour phase; t administration of the nebulised aerosol is preceded by administering no more than 150 ml of aerosol-free air. The glucocorticoid is administered in a daily dose of no more than 40 mg of prednisolone and an equivalent dose of another glucocorticoid. The other method of treating the patient involves pulmonary administration of the glucocorticoid in an amount of 400 to 4,000 mcg with using a nebuliser which is used to administer the glucocorticoid aerosol into the lower portion of the lungs at excessive pressure of 40 mbar or less that leads to deposition of more than 200 mcg of the glucocorticoid in the lower portion of the lungs. What is also declared is a method of treating the patient which involves pulmonary administration of the glucocorticoid in the amount of 400 to 4,000 mcg with the aerosol administered by inhalation consisting of three pre-specified periods wherein after the third period, the patient is advised to stop inhaling and exhale; the presented treatment leads to deposition of more than 200 microgram of the glucocorticoid in the lower portion of the lungs. |
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Invention relates to compounds of general formula or , where Ar1 represents phenyl group, optionally substituted with one or several identical or non-identical halogen atoms; R1 represents hydrogen atom; R4, R5, R6a, R6b represent hydrogen atoms; Y, Z independently represent linear C1-4 alkylene group, optionally substituted with one linear C1-4 alkyl group; Ar2 stands for condensed with benzene 5-membered heterocyclic ring, containing one nitrogen atom and one sulphur atom, substituted with one linear C1-4 alkyl group, or derivative of 5- or 6-membered heterocyclic ring, containing one nitrogen atom and one sulphur atom, condensed with heteroaromatic 6-memebered ring, containing one or two nitrogen atoms, substituted with one linear C1-4 alkyl group, linear C1-4 alkoxygroup or group -NR7R8, where R7 and R8 independently stand for hydrogen atom, linear or branched C1-4 alkyl group, or R7 and R8 together with nitrogen atom form group of general formula , where R2, R3 represent linear C1-4 alkyl groups, A stands for group -CHR12, oxygen atom or group -NR9, where R12 and R9 stand for hydrogen atom or linear C1-4 alkyl group, m has value 1 or 2, n has value 1 or 2, o has value 0 or 1, p has value 0 or 1, Q stands for group -O-, group -N--H or group -N--CO-R10, where R10 stands for linear C1-4 alkyl group or -NH-R11 group, where R11 represents linear C1-4 alkyl group; and to their salts. Invention also relates to methods of obtaining therein and to based on them pharmaceutical composition, possessing antagonistic activity with respect to receptor CCR3. |
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Method of treating bronchial asthma (ba) Invention refers to medicine, particularly to paediatrics, allergology and pulmonology, and can be used for treating bronchial asthma (BA) with persistent cytomegalovirus (CMV) in children. For this purpose after the signs of persistent CMV have been detected in bronchi, including its DNA fragments in expectorations, human immunoglobulin titred by CMV antibody count is immediately prescribed according to the scheme of 1.5 ml intramuscularly every third day within the course of 5 injections. |
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Antiallergic combinations of calcium and lanthanum salts Group of inventions refers to medicine, namely to clinical allergology, and may be used for extracorporeal allergen denaturation. That is ensured by treating a surface of objects with an allergen-denaturing composition. The composition contains calcium chloride or calcium acetate and lanthanum chloride or lanthanum nitrate in certain proportions. |
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P38 kinase-inhibiting isoquinoline derivatives Claimed invention relates to isoquinolinone derivatives of formula (I) or to its pharmaceutically acceptable salt, where R1 represents (C1-C5)alkyl, possibly substituted with 1, 2 or 3 groups, independently selected from groups -(C1-C6)alkyl, -(C1-C6)alkyloxy, -OH or -(C1-C6)alkyl-hydroxy, and where one independent substituent of R1 radical, representing -(C1-C6)alkyl, can be possibly condensed with other independent substituent of R1 radical, representing -(C1-C6)alkyl, with formation of saturated (C3-C4)cycloalkyl; R2 represents H; R3 represents (CH2)d-Y and R3 is independently possibly substituted with one or two groups -(C1-C6)alkyl, -NH2, -HN(C1-C6)alkyl, -N-di-(C1-C6)alkyl, -(C1-C6)alkyl-NH2, -(C1-C6)alkyl-hydroxy; Y us selected from heterocycloalkyl, S-(O)e-heterocycloalkyl, S-(O)e-(C1-C6)alkyl- heterocycloalkyl, -SO2NH-(C1-C6)alkyl; d equal 0, 1 and 2; e equals o, 1 or 2; R4 and R5 are independently selected from (C1-C6)alkyl and halogeno; R6 represents H; heterocycloalkyl represents C- or N-bound 5-7-membered non-aromatic cyclic ring, which, when it is C-bound, contains one NR7 atom, and when it is N-bound, contains one N-atom, or one N-atom and one NR7 atom, R7 represents H or (C1-C6)alkyl. Invention also relates to application of formula (I) compound in treatment of chronic obstructive pulmonary disease (COPD) and asthma. |
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Invention refers to medicine and pharmaceutical industry concerns a dry powder preparation containing formoterol fumarate dihydrate in the microionised form enabling bronchial and pulmonary alveolar penetration and additives, namely mixed lactose and sodium benzoate prepared in a particular way and enabling dosing and disaggregating the active ingredient effectively. |
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Phenoxypyridinylamide derivatives, and their use in treatment of pde4-mediated disease states Invention refers to a compound of formula (I): |
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Biological materials and their use Peptide of DGSVVVNKVSELPAGHGLNVNTLSYGDLAAD structure is used for suppression of allergic inflammation of respiratory passages, for prophylaxis and treatment of arthritis, as well as for pain relief. A peptide is effective as an adjuvant and for stimulation of IL-12 products in a cell. |
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Antagonists of sphingonsine-1-phosphate (s1p) receptor and methods of thereof application Invention relates to substituted benzamides, which can be applied as antagonists of sphingonsine-1-phosphate receptors. |
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Present invention refers to medicine and pharmaceutical industry and describes an inhalation formulation in the form of aerosol for treating bronchial asthma and chronic obstructive pulmonary disease, containing beclomethasone dipropionate, a solvent an adjuvant and a propellant; the solvent is presented by absolute ethyl alcohol, while the adjuvant is an aerosol particle size control consisting of triethyl citrate and perfluorodecaline; the propellant is 1,1,1,4 tetrafluoroethane (HFA-134a) and/or 1,1,1,2,3,3,3-heptafluoropropane (HFA-227ea). The formulation has a higher efficacy. |
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Present invention refers to medicine and pharmaceutical industry and describes an inhalation preparation for treating bronchial asthma and chronic obstructive pulmonary disease, containing micronized budesonide and micronised formoterol fumarate dehydrate as active ingredients, wherein the preparation contains a carrier presented by lactose of average particle diameter 1 to 10 mcm and sodium benzoate of bulk density 0.30-0.50 g/cm3, in the following proportions of the ingredients per a dose of the preparation: budesonide 50 mcg - 800 mcg, formoterol fumarate dehydrate 4.5 mcg - 18 mcg, lactose 5 mg - 50 mg, sodium benzoate 0.01 mg - 5 mg. What is also described is a method for producing the given preparation. |
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Method for reducing and managing bronchial asthma status Invention refers to medicine, namely to emergency medicine, and may be used for reducing and managing the bronchial asthma status. That is ensured by introducing human urotensin 2 (hU) antiserum that is a hormone of the caudal neurosecretory system (CNSS) one a day intracutaneously into a palmar surface of the arm in 2-3 points in a dose of 0.1- 0.2 ml and 25% magnesium sulphate intravenously in a dose of 5-10 ml twice a day in a combination with intravenous glucocorticosteroids and bronchial spasmolytic inhalations. |
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Therapeutic substituted cyclopentanes Invention relates to a novel compound of formula where Y is or or a pharmaceutically acceptable salt thereof. |
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Piperazine compound inhibiting prostaglandin-d-synthase Present invention refers to a piperazine compound presented by formula , wherein R1 represents C1-6 alkyl; R2 represents hydroxy, C1-6 alkyl which can contain a substitute specified in saturated or unsaturated 5-6 member heterocycle with 1-3 heteroatoms specified in oxygen and nitrogen, -(C=O)-N(R3)(R4) or -(C=O)-OR5; R3 and R4 may be identical or different, and each represents hydrogen or C1-6 alkyl which can contain a substitute specified in saturated or unsaturated 5-6 member heterocycle with 1-3 heteroatoms specified in oxygen and nitrogen, or R3 and R4 bound through a nitrogen atom whereto R3 and R4 are attached, can form a saturated heterocyclic group specified in 5-6 member heterocycle with 1-3 heteroatoms specified in oxygen and nitrogen; R5 represents hydrogen or C1-6 alkyl; and n represents 1 or 2; or a salt thereof. Also, the invention refers to a pharmaceutical compositions and an agent exhibiting prostaglandin-D-synthase activity and based on the compound of formula I, as well as to a method of preventing and treating a disease wherein prostaglandin D2 is involved. |
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2,4-pyrimidine diamine compounds and use thereof Invention relates to novel of 2,4-pyrimidine diamine compounds of formula I, which inhibit degranulation of immune cells and can be used in treating cell reactions mediated by FcεRI or FcγRl receptors. In formula (I) each R2 and R4 is independently phenyl substituted with one or more R8 groups or a heteroaryl selected from a group consisting of , where the heteroaryl is optionally substituted with one or more R8 groups and at least one of R2 and R4 is a heteroaryl; R5 is selected from a group consisting of (C1-C6)alkyl, optionally substituted with one or more identical or different R8 groups, -ORd, -SRd, fluorine, (C1-C3)halogenalkyloxy, (C1-C3)perhalogenalkyloxy, -NRcRc, (C1-C3)halogenalkyl, -CN, -NO2, -C(O)Rd, -C(O)ORd, -C(O)NRcRc, -C(NH)NRcRc, -OC(O)Rd, -OC(O)ORd, -OC(O)NRcRc; -OC(NH)NRcRc, - [NHC(O)]nORd, R35 is hydrogen or R8; each Y is independently selected from a group consisting of O, S and NH; each Y1 is independently selected from a group consisting of O, S and NH; each Y2 is independently selected from a group consisting of CH, CH2, S, N, NH and NR37. Other values of radicals are given in the claim. |
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2-s-benzylsubstituted pyrimidines as crth2 antagonists Invention refers to new 2-S-benzylpyrimidine derivatives having CRTH2 receptor antagonist activity. In formula 1: R1 means -CO2H; R4a and R4b mean hydrogen; W means -C(O)NR7-; R2 and R3, each independently mean F; Cl; Br;-NR10R11 or (C1-C6)alkoxy, optionally substituted by 1-3 halogen atoms; R5 means hydrogen; R6 means (C1-C6)alkyl; (C6-C19)aryl or (5-15)-member heteroaryl containing nitrogen, oxygen or sulphur atoms as heteroatoms, wherein above aryl and heteroaryl are optionally substituted by one or more substitutes specified in a group consisting of halogen; (C1-C6)alkyl optionally substituted by 1-3 halogen atoms; and (C1-C6)alkoxy optionally substituted by one, two or three halogen atoms; R7 means hydrogen; R10 and R11, each independently mean (C1-C6)alkyl; or R10 and R11, together with N, whereto attached form a 3-8- member saturated or unsaturated ring optionally containing one or more O or S atoms, or one or more additional N atoms in the ring; k is equal to 0; m is equal to 1. |
![Triazolo[1,5-a]quinolines as ligands of adenosine a3 receptor](http://img.russianpatents.com/img_data/1145/11451521-s.gif)
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Triazolo[1,5-a]quinolines as ligands of adenosine a3 receptor New derivatives of triazolo[1,5-a]quinoline of general formula (I) |
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5-substituted indazole as kinase inhibitors Present invention refers to compounds of formula (I) or pharmaceutically acceptable salts thereof wherein A, R1, R2, R3 and m are specified in the patent claim. The present invention also refers to the number of specific compounds, and to a pharmaceutical composition containing the above compounds effective for inhibition of kinases, such as glycogen synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus kinase (JAK), AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2. |
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New 1,2-dihydroquinoline derivatives possessing glucocorticoid receptor binding activity Present invention refers to organic chemistry, namely to new 1,2-dihydroquinoline derivatives of general formula , or to a pharmaceutically acceptable salt thereof, wherein R1 represents a lower alkyl group; R2 represents a hydrogen atom; each of R3 and R4 represents a lower alkyl group; R5 represents a lower alkyl group; R6 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group; X represents -CO-, -C(O)NR8 - or -S(O)2-; each of R7 and/or R8 may be identical or different, and represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower cycloalkyl group, a phenyl or naphthyl group, a saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, a lower alkoxy group, a phenoxy group; provided R7 and/or R8 represent a lower alkyl group, a lower alkoxy group, the mentioned lower alkyl group and lower alkoxy group may contain one or three groups specified in a halogen atom, a phenyl group, an unsubstituted monocyclic 6-member heterocyclyl with one heteroatom specified in a nitrogen atom, and 5 carbon atoms in a cycle, a lower alkoxy group, and -NRaRb as a substitute (substitutes); provided R7 and/or R8 represent a phenyl group, a saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, a phenoxy group, the mentioned phenyl group, saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, phenoxy group may contain one or two groups specified in a halogen atom, a lower alkyl group, a halogen-substituted lower alkyl group, a phenyl group, a hydroxyl group, a lower alkoxy group, a halogen-substituted lower alkoxy group, a lower alkylthio group, a lower alkylcarbonyl group, a lower alkoxycarbonyl group, a lower alkylcarbonyloxy group, -NRaRb, a nitro group and a cyano group as a substitute (substitutes); Ra and Rb may be identical or different, and each of them represents a hydrogen atom, a lower alkyl group, a lower alkoxycarbonyl group; Y represents a lower alkylene group; Z represents an oxygen atom; p is equal to 2, provided p is equal to 2, R6 may be identical or different. The invention also relates to a pharmaceutical composition and a glucocorticoid receptor modulator of the compound of formula (1). |
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Chemical compounds 637: pyridopyrimidinediones as pde4 inhibitors Invention relates to a compound of formula |
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Pyrazinone derivatives and use thereof in treatment of lung diseases Invention relates to pyrazinone derivatives of formula (I): |
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Substituted benzoylaminoindan-2-carboxylic acids and related compounds Present invention refers to compounds of formula 1a: |
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Present invention relates to a piperidine derivative of general formula (I) |
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Novel 707 compounds and use thereof Invention relates to novel isoquinolinone derivatives of formula (I) , wherein R1 is selected from H, (C1-C6)alkyl, (C2-C6)alkenyl, (CH2)a-X-Ar and (CR101R102)a-X-Ar, where said (C1-C6)alkyl is optionally substituted with 1, 2 or 3 groups independently selected from -(C1-C6)alkoxy, -halogen, -OH, -heterocycloalkyl, (C3-C7)cycloalkyl and -NR8R9; R2 is selected from H and (C1-C6)alkyl; R is selected from H, (C1-C6)alkyl and (CH2)d-Y; provided that when R3 is (CH2)d-Y, R2 is selected from H; R4 and R5 are independently selected from H, (C1-C6)alkyl and halogen; R is (C3-C7)cycloalkyl; R7 is H; Ar is phenyl or heteroaryl, optionally substituted with 1, 2 or 3 groups independently selected from -(C1-C6)alkyl, -(CH2)e-O-(C1-C6)alkyl, -(CH2)e-S(O)f(C1-C6)alkyl, -(CH2)e-N(R10)-(C1-C6)alkyl, -(CH2)e-Z-(C1-C6)alkyl, -halogen, heterocycloalkyl, -C(O)NR8R9, -NR8R9 and -C(O)OH, where (C1-C6)alkyl in each case is independently optionally substituted with 1, 2 or 3 groups, independently selected from -NRI2R13; X is selected from a single bond; Y is NR16R17, where R16 and R17 together with a nitrogen atom with which they are bonded form a 5-7-member ring, optionally containing an additional heteroatom NR27, where said ring is optionally substituted on the carbon atom with 1 or 2 substitutes independently selected from -(C1-C6)alkyl, where said -(C1-C6)alkyl is optionally substituted with -OH; and where R27 is selected from H and (C1-C6)alkyl, where said (C1-C6)alkyl is optionally substituted with -OH; Z is selected from C(O)N(R18); R8 and R9 are independently selected from H and (C1-C6)alkyl, where said (C1-C6)alkyl is optionally substituted with 1, 2 or 3 groups, independently selected from NR19R20; or R8 and R9 together with the nitrogen atom with which they are bonded form a 5-6-member ring, optionally containing an additional heteroatom, selected from NR21; R12 and R13 are independently selected from H and (C1-C6)alkyl, where said (C1-C6)alkyl is optionally substituted with -(C1-C6)alkoxy, -OH; or R12 and R13 together with the nitrogen atom with which they are bonded form a 5-6-member ring optionally containing an additional heteroatom selected from NR24; R10, R18, R19, R20, R21, R22, R23 and R24 are independently selected from H and (C1-C6)alkyl; a is selected from 1, 2, 3, 4, 5 and 6; d equals 0 or 1; e equals 0; f is independently selected from 1 and 2; where the heterocycloalkyl is a 5-6-member non-aromatic cyclic ring bonded at a C atom, having 1-2 NR28 atoms; optionally having one double bond; the heteroaryl is a 6-member aromatic ring containing 1 N atom; R is selected from H, (C1-C6)alkyl and -C(O)O-(C1-C6)alkyl; R101 is (C1-C6)alkyl; R102 is H; or pharmaceutically acceptable salts thereof or N-oxides. The invention also relates to methods of producing said compounds and use thereof as a p38 kinase inhibitor. |
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Use of arsenic compounds for pain management and inflammation treatment Invention refers to chemical-pharmaceutical industry and represents the use of sodium metaarsenite in preparing an oral dosage form of a pharmaceutical composition for inflammation treatment in a mammal. |
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Method and composition for treatment of inflammatory disorders Invention relates to homogenous pharmaceutical composition for treatment of inflammatory disorders, which contains mixture of steroid anti-inflammatory or anti-histamine active ingredient in pharmaceutically acceptable water carrier with liposome. As steroid anti-inflammatory ingredient used is budesonide or fluticasone or their pharmaceutically acceptable salt, and antihistamine preparation is represented by azelastine or its pharmaceutically acceptable salt, concentration of active ingredient in water carrier is, in fact, equal inside and outside liposomic structures and varies ±20% when concentration of active ingredient inside and outside liposomic structures is compared. Polar lipid is swellable in water and represents phospholipid or glycosphingolipid. Invention also relates to method of composition obtaining, which lies in joint mixing of polar lipid, water phase and said active ingredient and mixture homogenising. Invention also relates to method of treating inflammatory disorders, including introduction of claimed composition to individuum, suffering from or sensitive to said disorders. |
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Amine salts of crth2 antagonist Invention relates to method of obtaining said salts, to pharmaceutical composition, containing said salts, and to application of salt for preparation of medication for treatment, prevention or relief of one or several symptoms of disease, mediated by CRTH2, associated with eosinophils, basophils, where disease is selected from asthma, allergic asthma, asthma of physical effort, allergic rhinitis, atopic dermatitis, contact hypersensitivity and hyper IgE syndrome. |
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Invention relates to novel crystalline forms I, II and amorphous form of {4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)benzyl)pyrimidin-5-yl}acetic acid. |
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Pyrimidine hydrazide compounds as pgds inhibitors Invention relates to novel substituted pyrimidine derivatives having PGDS inhibiting properties. In formula (I): (I), R1 denotes phenyl or a 5- or 6-member heteroaryl containing 1-3 heteroatoms selected from N, O and S, each optionally having one or more of the following independent substitutes: halogen, (C1-C6)-alkyl, or (C1-C4)-haloalkyl; R2 denotes hydrogen or (C1-C6)-alkyl, which is optionally substituted with one or more halogens; R3 denotes hydrogen, (C1-C6)-alkyl or phenyl; R4 denotes C6-cycloalkyl, phenyl, a 6-member heterocyclyl containing one N heteroatom, a 6-member heteroaryl containing one N heteroatom, -C(=O)-NY1Y2, -C(=S)-NY1Y2, or -C(=O)-R5, where the phenyl, 6-member heteroaryl or 6-member heterocyclyl group optionally has one or more independent substitutes R6, or R3 and R4 together with a nitrogen atom with which they are bonded form a 5- or 6-member heterocyclyl containing one or two heteroatoms selected from N, O and S, a 6-member heterocyclenyl containing two or three N heteroatoms, a 5-member monocyclic or 9-member bicyclic heteroaryl containing one to three N heteroatoms, phenylheterocyclyl, where the heterocyclyl is 5- or 6-membered and contains one or two heteroatoms selected from N and O, each optionally having one or more independent substitutes R6. Values of R5, R6, Y1, Y2 are given in the claim. The invention also relates to a pharmaceutical composition containing said compounds. |
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Hydantoin derivatives used as mmp inhibitors Invention refers to compounds of formula (I) and their pharmaceutically acceptable salts possessing the properties of a MMP12 inhibitor, a method for preparing them, an intermediate compound of formula (III), a pharmaceutical composition, a method for preparing it, using the compounds of formula (I) and versions of methods of treating with the use of the compounds of formula (I). The compounds may be used for treating the MMP12-mediated diseases, such as chronic obstructive pulmonary disease. In formula (I) and (III) R1 represents H, CH3, CH3CH2, CF3 or cyclopropyl; and R2 represents H or CH3. |
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Method for arrest of cold bronchospasm and mucosal oedema in patients with bronchial asthma Invention refers to medicine, namely to pulmonology, and may be used in treating the patients with cold bronchospasm and mucosal oedema in the patients with cold bronchial asthma. That is ensured by 2-3 inhalations of berodual and simbicort before walking in the open air at temperature (-20°C)-(-45°C). |
Another patent 2551166.