Compositions and methods for treatment of chronic inflammation and inflammatory diseases

FIELD: pharmacology.

SUBSTANCE: group of inventions refers to an oral pharmaceutical composition with anti-inflammatory activity, to a method for preparation of the said composition, to application of an oral pharmaceutical composition for manufacture of a medicament for treatment of chronic inflammation, to application of an oral pharmaceutical composition for treatment of chronic inflammation, and to a method for treatment of an individual with chronic inflammation. The pharmaceutical composition comprises: a) a non-steroidal anti-inflammatory drug (NSAID), which is a propionic acid derivative that has a log P value greater than 2.0; b) 0.01-15 vol. % of a pharmaceutically acceptable solvent, wherein the solvent is a pharmaceutically acceptable liquid polyethylene glycol polymer; and c) at least 50 vol. % of a pharmaceutically acceptable hydrophobic lipid adjuvant, wherein the pharmaceutically acceptable hydrophobic lipid adjuvant consists of a fatty acid triglyceride, a fatty acid diglyceride and a fatty acid monoglyceride, wherein the pharmaceutical composition is prepared so as to be in a solid state at a temperature of 15°C or lower and has a melting point of 25°C or higher.

EFFECT: group of inventions allows the delivery of a therapeutic chemical compound with anti-inflammatory activity so that it more effectively inhibits the anti-inflammatory response, which ultimately increases the effectiveness of chronic inflammation treatment.

16 cl, 4 dwg, 7 tbl, 10 ex

 



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to a novel chemical substance - 4,10-bis((±)-5-benzoyl-2,3-dihydro-1H-pyrrolo[1,2-a]pyrrole-1-carbonyl)-2,6,8,12-tetraacetyl-2,4,6,8,10,12-hexaazatetracyclo[5,5,0,03,11,05,9]dodecane The invention also relates to a method of its obtaining, which consists in the acylation of 2,6,8,12-tetraacetyl-2,4,6,8,10,12- hexaazatetracyclo [5,5,0,03,11,05,9]dodecane by chloranhydride 5-benzoyl-2,3-dihydro-1H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid.

EFFECT: novel compound, which has analgetic activity, is obtained.

2 cl, 1 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to novel heterocyclic compounds of general formula (I) or enantiomers, diastereomers or pharmaceutically acceptable salts thereof, where Y is: phenyl or a heteroaryl selected from thiazolyl, pyridyl, pyrimidinyl, 1,3,5-triazinyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl and 1,3,4-thiadiazolyl; wherein the phenyl or heteroaryl is optionally substituted with one substitute selected from fluorine, chlorine, bromine, iodine, C1-4alkyl, trifluoromethyl, C1-4alkoxy, C1-4alkylthio, nitro and cyano; r=1-2; R2 is absent or is an oxo-group; Z is: (a) phenyl substituted with NRaRb; where Ra is: H or C1-4alkyl; where Rb is: C1-4alkyl, cycloalkyl, phenyl, furanylmethyl, or phenyl(C1-2alkyl); and wherein the phenyl or the furanyl are optionally substituted with iodine; alternatively, Ra and Rb are taken together with the nitrogen atom to which they are bonded to form a 5-8 member heterocyclyl, which is optionally condensed to a benzene ring; (b) biphenyl-3-yl or biphenyl-4-yl; where the interior phenyl ring, attached to the carbonyl in formula (I) is optionally substituted with a fluorine atom; and where the terminal phenyl ring is optionally substituted with a substitute selected from trifluoromethyl, C1-4alkoxy, chlorine, dichloro, fluorine, and iodine; (c) phenyl substituted with a substitute selected from C5-8cycloalkyl, -NHC(=O)cyclohexyl, phenyloxy, phenylcarbonyl, phenyl(C1-3)alkyl, phenyl(C1-3)alkoxy, pyrrolyl, pyrazolyl, imidazolyl, isoindol-2-yl-l,3-dione, 2,3-dihydro-isoindol-2-yl; l-(tert- butoxycarbonyl)piperidin-4-yloxy, and 1-(tert-butoxycarbonyl)piperidin-4-yl; (d) phenyl substituted with 1-2 substitutes independently selected from: C1-6alkyl, C1-4alkoxy, iodine, chlorine and nitro; (e) phenyl(C1-2)alkyl; where the phenyl is optionally substituted with 1 or 2 substitutes independently selected from iodine, fluorine, C1-6alkyl, phenyl and NRcRd; where Rc: H or C1-4alkyl; where Rd is: C1-4alkyl or C1-6cycloalkyl(C1-4)alkyl; and where the C1-2alkyl of phenyl(C1-2)alkyl is optionally substituted with phenyl; (f) phenyl(C2-4)alkenyl; where the phenyl is optionally substituted with a substitute selected from C1-4alkyl, C1-4alkoxy, trifluoromethyl, trifluoromethylthio and phenyl; (g) naphthyl; where the naphthyl is optionally substituted with one C1-4alkoxy substitute; (h) fluorenyl or xanthenyl; where the fluorenyl or xanthenyl is optionally substituted with an oxo group; (i) C5-8cycloalkyl; where the C5-8cycloalkyl is optionally substituted with one C1-6alkyl substitute; (j) benzene ring-condensed C5-8cycloalkyl or benzene ring-condensed C5-8cycloalkyl(C1-4)alkyl; where said C5-8cycloalkyl fragment is optionally substituted with 1-4 methyl groups; (k) bicyclo[2.2.2]octyl-1-yl; where the bicyclo[2.2.2]octyl-l-yl is optionally substituted with C1-6alkyl; (1) a heteroaryl or benzene ring-condensed heteroaryl selected from benzooxazolyl, quinolinyl, benzimidazolyl, pyridinyl, indolyl, thienyl, furanyl, pyrazolyl, oxazolyl, benzothienyl and benzofuranyl; where the heteroaryl or benzene ring-condensed heteroaryl is optionally substituted with 1 or 2 substitutes independently selected from C1-4alkyl, trifluoromethyl, C5-8cycloalkyl, phenyl, phenyl(C1-2)alkoxy, phenyl(C2-4)alkynyl and dichlorophenoxy; and where the phenyl substitute in the heteroaryl is further optionally substituted with C1-4alkyl, C1-4alkoxy or trifluoromethyl; (m) l,5-diphenyl-lH-pyrazol-3-yl; where the pyrazol-3-yl is optionally substituted with a methyl group; and where each of the phenyl groups of the 1,5-diphenyl substitutes is also optionally substituted with substitutes selected from chlorine, dichloro or aminosulphonyl; (n) 1,2,3,4-tetrahydroquinolin-6-yl; where the 1,2,3,4-tetrahydroquinolin-6-yl is optionally substituted with phenyl or trifluoromethyl-substituted phenyl; and (o) benzene ring-condensed heterocyclyl(C2-4)alkenyl; where the benzene ring-condensed heterocyclyl is attached to the C2-4alkenyl via the benzene ring; and where benzene ring-condensed heterocyclyl is further optionally substituted with C5-6cycloalkyl; taking into account constraining conditions indicated in claim 1. The invention also relates to a pharmaceutical composition based on the compound of formula (I), a method of producing said pharmaceutical composition, a method of treating said pathological conditions and use of the compound of formula (I).

EFFECT: obtaining novel heterocyclic compounds having MGL inhibiting activity.

21 cl, 5 tbl, 11 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and represents a pharmaceutical composition for control of pain accompanying individual's joint diseases containing hyaluronic acid, which is cross-linked by cycling a double bond in a group of cinnamic acid in partially amidated hyaluronic acid presented by formula (1) to form a cyclobutane cycle, wherein in the above formula, Ar represents a phenyl group, n is equal to an integer 2 or 3; HA represents a carboxy residue of hyaluronic acid, and m represents a relation of amidation of hyaluronic acid to all the carboxyl groups and is equal to 3-50% in relation to all the carboxyl groups, and a pharmaceutically acceptable carrier, wherein the pharmaceutical composition represents a product for injection, wherein the pharmaceutical composition represents the product for injection, wherein the amount of the cross-linked hyaluronic acid makes 1 wt % at the total amount of the product for injection, wherein a single dose of the product for injection makes 2-3 ml, wherein the pharmaceutical composition represents a single-use preparation, which is administered every 13 weeks and more.

EFFECT: invention provides the extremely long analgesic action after the single administration, earlier onset of the analgesic action.

15 cl, 1 dwg, 5 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, namely to a method for preparing a medicinal product possessing choleretic activity. The medicinal product possessing choleretic activity and prepared by extracting an elevated part of Lomatogonium carinthiacum in 96% ethanol twice at room temperature, them in 40% ethanol with an extractant added in an amount equal to a discharged one, twice; the filtered aqueous-alcoholic extracts are combined; the extraction cake is extracted in purified water; the aqueous extract is filtered; the aqueous residues of the aqueous-alcoholic extracts are combined with the aqueous extract, concentrated, dried in a vacuum drying cabinet to produce the dry extract in the certain environment.

EFFECT: medicinal product prepared as described above possesses the evident choleretic activity.

11 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: using a polyphenolic complex produced by extracting milled ash berry in 40% ethanol, condensing the alcohol-water extract, adding 95% ethanol, centrifuging the residue, filtering and condensing the supernatant in the certain environment, as an agent possessing anti-inflammatory action.

EFFECT: polyphenolic complex possesses pronounced anti-inflammatory action.

1 dwg, 9 tbl, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical composition, containing compound of formula or for prevention or treatment of diseases, associated with oxidative stress, selected from group, consisting of MELAS (mitochondrial myopathy, encephalopathy, lactic acidosis and stroke episodes), MERRF syndrome (myoclonic epilepsy with ragged red fibres) or Kearns-Sayre syndrome, arrhythmia, cardioplegia or myocardium infarction. in formula (1) na stands for 1 or 2, Aa represents 5-membered heteroaryl or heterocycle, each of which has 2 heteroatoms, selected from N, O and S, Rla represents R5a-Xa-Ba-X′a-, Ba represents direct bond, Xa and X′a independently on each other represent direct bond or -OC(O)-, R5a represents hydrogen or 6-9-membered monocyclic or condensed cyclic heterocycle or heteroaryl, each of which has from 1 to 3 heteroatoms, selected from N, O and S, and is optionally substituted with oxo or C1-C6-alkyl, R2a represents -(CR8aR9a)pa-Ya-R7a, pa stands for number from 0 or 1, Ya represents direct bond or -O-, R7a represents hydrogen or phenyl, R3a, R8a, R9a, R10a represent hydrogen, R4a represents -(CH2)pa-Da-R10a-, Da represents C5-cycloalkyl or 6-membered heterocycle, which has 1 heteroatom, selected from N, S and O. Radical values for formula (2) are give in invention formula.

EFFECT: obtaining compositions for prevention or treatment of diseases, associated with oxidative stress.

19 dwg, 5 tbl, 3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing 9-aryl-6,8,20-trioxa-13-azapentacyclo-[11.8.0.01,10.02,7.014,19]heneicosa-9,14,16,18-tetraene-11,12,21-triones (IIa-d), which includes reacting 3-aroyl-1H-pyrrolo[2,1-c][1,4]benzoxazine-1,2,4-triones (Ia-d) with 3,4-dihydro-2H-pyran in a medium of an inert aprotic solvent, followed by separation of the end products. In general formula (I) Ar=Ph (a, d), C6H4Br-4 (b), C6H4OMe-4 (c), R=H (a-c), Cl (d).

EFFECT: obtaining 9-aryl-6,8,20-trioxa-13-azapentacyclo-[11,8,0,01,10,02,7,014,19]heneicosa-9,14,16,18-tetraene-11,12,21-triones.

2 cl, 1 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention refers to a new compound, namely to 2-[(2-methylphenyl)imino]-9-oxo-7-phenyl-8-(3-phenyl-2-quinoxalinyl)-1,6-dioxaspiro[4,4]none-3,7-diene-3,4-dicarboxylic acid dimethyl ester of formula possessing antinociceptive activity, and a method for producing it consisting in synthesis of 4-(3-phenylquinoxalin-2-yl)-5-phenylfurane-2,3-dione, acetylene dicarboxylic acid dimethyl ester and o-methylphenylisonitrile.

EFFECT: preparing the new compound.

2 cl, 1 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compound, represented by the following formula

,

or its pharmaceutically acceptable salt. In claimed formula each symbol has values, determined in formula of invention. Versions of formula [I] compound and particular compounds are also objects of invention. In addition, invention relates to pharmaceutical composition, ITK inhibitor and means for treatment or prevention of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection and other diseases and methods of treating said diseases.

EFFECT: claimed compounds inhibit induced T-cellular kinase (ITK).

32 cl, 86 tbl, 387 ex

FIELD: medicine.

SUBSTANCE: application of a compound of the general formula 1 or its spatial isomers as analgesic means is claimed.

EFFECT: compounds have high efficiency, low toxicity, can be applied in medicine.

4 tbl 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and represents a pharmaceutical composition for control of pain accompanying individual's joint diseases containing hyaluronic acid, which is cross-linked by cycling a double bond in a group of cinnamic acid in partially amidated hyaluronic acid presented by formula (1) to form a cyclobutane cycle, wherein in the above formula, Ar represents a phenyl group, n is equal to an integer 2 or 3; HA represents a carboxy residue of hyaluronic acid, and m represents a relation of amidation of hyaluronic acid to all the carboxyl groups and is equal to 3-50% in relation to all the carboxyl groups, and a pharmaceutically acceptable carrier, wherein the pharmaceutical composition represents a product for injection, wherein the pharmaceutical composition represents the product for injection, wherein the amount of the cross-linked hyaluronic acid makes 1 wt % at the total amount of the product for injection, wherein a single dose of the product for injection makes 2-3 ml, wherein the pharmaceutical composition represents a single-use preparation, which is administered every 13 weeks and more.

EFFECT: invention provides the extremely long analgesic action after the single administration, earlier onset of the analgesic action.

15 cl, 1 dwg, 5 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical industry and represents medication, possessing virucidal activity, for preventive and therapeutic treatment of viral infections, caused by virus of herpesviridae family, characterised by the fact that said medication contains pyroxican in carrier substance.

EFFECT: invention provides extension of arsenal of means, possessing virucidal activity.

7 cl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a microbiologically stable pharmaceutical composition containing an active agent specified in prostaglandins, and a carrier. The carrier contains an aqueous electrochemically activated saline containing 1 to 500 mg/l of free chlorine and having an oxidation-reduction potential from +150 to +1350 mV. The active agent is present in a phase separated from the electrochemically activated saline; the electrochemically activated saline is a hypochlorite solution.

EFFECT: invention refers to using the pharmaceutical composition for treating and/or preventing dry eye syndrome and for cleansing contact lenses.

14 cl, 5 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relate to field of pharmaceutics and deal with pharmaceutically stable compositions, which contain human antibody, specifically bound with human interleukine 6 (hIL-6R) receptor, where said human antibody is contained in concentration from 5 to 200 mg/ml and includes variable region of light chain with amino acid succession SEQ ID NO:26, histidine, arginine, sucrose, polysorbate.

EFFECT: group of inventions ensure considerable degree of antibody stability after storing for several months.

22 cl, 8 ex, 28 tbl, 4 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to an injectable therapeutic anti-cancer formulation administered into cancer cells directly. The formulation contains 5-25% (wt/vol) of hydroxychloroquine or hydroxychloroquine sulphate, Lidocaine concentrated 1-2% (wt/vol), Riboflavin concentrated 0.1-0.5% (wt/vol) and physiologic saline.

EFFECT: invention provides the formulation which exhibits cytotoxic effect on the cancer cells without involving normal cells, and which is administered into the cancer cells directly.

2 cl, 3 tbl, 4 dwg, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and represents a pharmaceutical composition in the form of a liquid solution for nasal administration of spray containing naltrexone in an amount of 0.005-0.02 wt/vl %.

EFFECT: invention provides eliminating the undesired side effects with preserving naltrexone activity.

6 cl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medicine. Described is medical form for transmucousal per oral introduction of, at least, one active substance of antispasmodic and/or analgesic action, which contains said active substance in form of base and/or in form of salt, water-alcohol solution, with alcoholic content, at least, 35° of alcohol by weight, with said active substance being present in water-alcohol solution in condition of stable and complete dissolution. Invention also relates to method of said medical form preparation and its application for treating spastic attacks.

EFFECT: medical form makes it possible to realise instantaneous transmucousal per oral introduction.

10 cl

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely represents a method for the therapy of respiratory symptom. The method involves administering a liquid composition containing a gel former and/or a mucoactive polymer, a non-menthol cooling substance; and contacting the oral mucosa with the liquid composition. The invention also describes liquid compositions applicable in the method for the therapy of a respiratory disease.

EFFECT: implementing the method provides improving the cooling properties of the cooling agent N-(4-cyanomethylphenyl)-n-menthane carboxamide in the liquid composition by combining the non-menthol cooling substance with the gel former.

14 cl, 2 tbl, 5 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relates to the field of pharmaceutics and deals with a pharmaceutical composition, which contains feline erythropoietin as an active ingredient, to which two or more polyethyleneglycol molecules with a non-branched chain are attached, with a water-soluble long-chain molecule having the molecular weight, constituting not less than 30 kDa and producing the haemopoietic effect. A haemopoietic medication and a medication for the treatment of anaemia are based on the said composition.

EFFECT: group of inventions provides the haemopoietic effect, which lasts for not less than seven days, when introduced to humans and/or animals.

8 cl, 4 dwg, 2 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: invention represents a composition for preventing and treating allergic conjunctivitis and keratoconjunctivitis, containing cromoglicic acid, boric acid and water-soluble polymers specified in a group of: carbomer, hypromellose, macrogol and polyvinylpyrrolidone with the components of the composition taken in specific relations, g in 1 ml of the mixture.

EFFECT: invention provides the better reduction of the inflammatory process and symptoms of the disease; there are also ensured ease of use with a smaller frequency of administration, prolonged action and no side effects.

5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medicine and represents emulsion for prevention or treatment of syndrome of inflammatory response and other diseases. Emulsion includes oily component and water component, and oily component contains triglycerides of fish oil and medium-chain triglyceride. Said fish oil triglycerides contain omega-3 fatty acids in quantity at least 60% counted per the total weight of fatty acids of fish oil triglycerides with the total quantity of EPA and DHA constitutes at least 45% counted per the total weight of fatty acids of fish oil triglycerides. Versions of emulsion include vegetable oil in quantity to 10% counted per the total weight of oily component.

EFFECT: emulsion is stable, represents concentrated source of energy and calories, and reduces cytotoxicity of medications.

26 cl, 6 tbl

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