Production and application of bacterial histamine

FIELD: medicine.

SUBSTANCE: method for selecting a probiotic lactic bacterial strain for use in the local production of histamine in a mammal is provided. A product and composition for the local production of histamine in a mammal containing a lactic acid bacterial strain having an active histidine operon and capable of producing histamine is proposed for use in the treatment and/or prevention of inflammatory conditions.

EFFECT: local production of histamine in a mammal by selecting certain strains of lactic acid bacteria.

13 cl, 9 dwg, 2 tbl, 5 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: chemistry.

SUBSTANCE: invention relates to a method of lyophilisation of a composition, which contains purified antithrombin III (AT III) and a crystallised substance, selected from alanine, mannitol, glycine or NaCl. The claimed method includes freezing the composition at a temperature from -52°C to -60°C for 6-15 hours, annealing the composition at -30°C for 1 hour, re-freezing the composition at a temperature from -52°C to -60°C for 2-15 hours at keeping the product temperature between -48°C and -52.7°C for 4-10 before lyophilisation and drying the composition with obtaining a lyophilised cake. The invention also relates to a pharmaceutical set, which contains the said lyophilised cake and a liquid reagent.

EFFECT: invention provides obtaining the lyophilised composition, containing AT III, which preserves its activity and stability.

14 cl, 24 dwg, 5 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relates to medicine. Described is a composition for the transdermal introduction of medications (M) into a human and animal organism, including cases of urgent drug treatment and prevention of acute pathological conditions. The composition consists of a solution of one or several M in a mixture of at least two solvents: dialkylamide of lower carboxylic acid and (or) alkylpyrrolidone and monoterpenes and (or) monoterpenoids. The total volume concentration of N,N-dialkylamides of lower carboxylic acids or N-alkylpyrrolidones constitutes from 1% to 99% of the mixture volume.

EFFECT: composition makes it possible to realise urgent drug treatment and prevention of acute pathological conditions of a human and animal organism by a simple in implementation, safe and cheap method.

12 cl, 6 dwg, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds or their pharmaceutically acceptable salts which can be applicable for biologically active substances delivery.

EFFECT: invention refers to pharmaceutical formulations containing the above compounds, and to a method for administering the biologically active substances.

17 cl, 10 tbl, 19 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to medicine, namely to pharmacology and describes a histidine-free pharmaceutical composition containing high-purity factor VIII; arginine and saccharose, a surfactant for the prevention or at least the inhibition of a surface adsorption of factor VIII; 0.5 to 10 mM calcium chloride for the specific stabilisation of factor VIII, and sodium citrate or maleic acid as a pH buffer.

EFFECT: invention provides the protective function for preserve high-yield factor VIII over the whole cycle of pharmaceutical processing, long storage and end recovery and administration into the patient.

18 cl, 16 tbl, 8 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to dermatooncology, and can be used in treatment of actinic keratosis. For this purpose foci of disease are identified with further carrying out their US-examination and derma analysis. In case if hypoechogenic zone, occupying from 5% to 30% of entire derma thickness, is present in derma, applications with liquid nitrogen with textile tip are performed. In case if hypoechogenic zone, occupying from 30% to 70% of entire derma thickness, is detected, applications with liquid nitrogen with copper tip or photodynamic therapy with application of photosensitiser are performed. In case if hypoechogenic zone, occupying from 70% to entire derma thickness, is detected, photodynamic therapy with application of photosensitiser is carried out.

EFFECT: method makes it possible to select tactics of treating said pathology in the most accurate way basing not only on clinical manifestations of disease, but also due to taking into account proliferative abilities of cells, which excludes necessity of carrying out tissue biopsy.

3 dwg, 4 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely rheumatology, and is applicable for preventing and treating rheumatoid arthritis in a patient. That is ensured by the oral administration of a therapeutically effective amount of calcitonin in the free form or in the form of a salt or a delivery agent specified in a group specified in N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC), N-(10-[2- hydroxybenzoyl]amino)decanoic acid (SNAD), N-(8-[2-hydroxybenzoyl]amino)caprylic acid (SNAC) and their pharmaceutically acceptable salts.

EFFECT: oral introduction promotes improved absorption, more acceptable pharmacokinetic and pharmacodynamic profile and a smaller degree of calcitonin variability, as compared with the other methods of delivery that provides reduced chondrolysis.

8 cl, 2 dwg, 2 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relates to pharmacy and medicine. Pharmaceutical composition includes mixture of: (a) active macromolecular substance; (b) aromatic alcohol, absoption amplifier, selected from propylgallate, butylated hydroxytotuol (BHT), butylated hydroxyanisole (BHA) and their analogues and derivatives, or their mixtures; and (c) biguanide or its pharmaceutically acceptable salt, capable of increasing solubility of aromatic alcohol, absorption amplifier, in water medium, where aromatic alcohol, absorption amplifier, is present in amount (by weight) greater or equal to amount of active substance. Application in pharmaceutical composition of aromatic alcohol, selected from propylgallate, BHT, BHA and their analogues and derivatives, together with biguanide or its pharmaceutically acceptable salt, capable of increasing solubility of aromatic alcohol in water medium, as amplifier of macromolecule absorption through intestine wall. Method of increasing absorption of active macromolecular substance and method of patient treatment include introduction of claimed composition to patient. Application of active macromolecular substance, selected from insulin, C-peptide, GLP-1 or their mixture; aromatic alcohol, absorption amplifier, selected from propylgallate, butylated hydroxytotuol (BHT), butylated hydroxyanisole (BHA) and their analogues and derivatives, or their mixtures; and biguanide or its pharmaceutically acceptable salt, capable of increasing solubility of aromatic alcohol, absorption amplifier, in water medium, in manufacturing medications for treatment of diabetes, osteoporosis, obesity, cancer, osteoarthritis.

EFFECT: group of inventions ensures facilitation of passage of peptides, proteins and other macromolecular substances through intestinal wall for improvements of their bioavailability.

27 cl, 3 tbl, 11 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to method of obtaining composition, including lyophilised one, containing epoprostenol, which includes obtaining solution of epoprostenol or its salt and arginine and bringing solution pH to more than 12 by addition of potassium hydroxide or sodium hydroxide. Invention also relates to pharmaceutical composition and stable solution for treatment of cardio-vascular diseases, which contain epoprostenol or its salt and arginin and have pH higher than 12. Also described is method of treating patient with cardio-vascular disease, which includes introduction of effective amount of said composition.

EFFECT: invention ensures obtaining hemocompatible, stable to microorganisms and stable epoprostenol compositions.

46 cl, 30 tbl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, namely to pharmaceutical compositions containing a peptide and propylene glycol, to methods of preparing such compositions, and also concerns methods of reducing contamination of injection devices by a peptide composition and reducing sediment formation in the production equipment during manufacturing of the peptide composition. The agonist GLP-1 is used as said peptide in the composition.

EFFECT: reduced contamination of the injection devices during injection.

23 cl, 6 ex, 7 dwg

FIELD: medicine.

SUBSTANCE: offered invention refers to medicine, namely to surgery, and can be used for prevention of inconsistency of anastomoses of hollow organs in gastrointestinal tract surgery. That is ensured by the oral introduction of 5-oxymethyluracil pills of the weight 1.5 g and diameter 7-7.5 mm on the 2nd postoperative day in the following proportions: 5-oxymethyluracil - 0.5 g, 5 % spirit-acetone acetylphthalylcellulose - 3 layers, 10 % hexane solution of low-molecular polyethylene - 1-3 layers, biological adhesive Sulphacrylate - 1-3 layers.

EFFECT: introduction of 5-oxymethyluracil in said dosage form provides stimulation of repair regeneration ensured by selective maximum concentration of the preparation in gastrointestinal segments where the anastomosis has been created, and reduced ischemic disorders.

1 ex, 1 dwg

FIELD: chemistry.

SUBSTANCE: present invention relates to biotechnology and provides a α1,6-glucan-containing compound of Helicobacter pylori. The present invention also discloses a conjugate for inducing immune response against H.pylori, which contains said compound conjugated with a carrier protein. The present invention also discloses an immunogenic composition, use of said composition and a method of inducing immune response against H.pylori using said composition. The present invention also discloses immune serum for neutralising H.pylori in mammals, which is obtained by immunising said mammal with an immunogenic composition containing said immunogenic composition. The present invention discloses an antibody which recognises said α1,6-glucan-containing compound of H.pylori, use of said antibody and a method of inducing complement-mediated bacteriolysis of H.pylori strains which express α1,6-glucan using said antibody.

EFFECT: invention improves the effectiveness of immunogenic compositions against Hpylori.

27 cl, 8 dwg, 21 tbl, 11 ex

Up!