Antiseptic drug

FIELD: pharmacology.

SUBSTANCE: invention relates to the organic heterocyclic compounds chemistry, namely a new quaternary ammonium salt containing a fragment of a vitamin B6 derivative of formula I , which exhibits antibacterial, antimycotic, antiviral and antiprotozoal properties.

EFFECT: compound can be used in medicine and veterinary medicine.

2 cl, 2 dwg, 16 tbl

 



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to synthetic biologically active heterocyclic substances having antagonist activity on purinoreceptors and which are products of modifying pyridoxin, particularly n-(1,5-dihydro-3-R-8-methyl-9-hydroxy-[1,3]dioxepino[5,6-c]pyridinyl-6-azo)phenyl sulphonic acid and salt forms thereof of general formula I , where is selected from: a hydrogen atom, ethyl, heptyl or octyl.

EFFECT: compounds of the given formula have high antagonist activity on purinoreceptors and can be used in medicine and veterinary.

2 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention relates to use of synthetic biologically active heterocyclic substances as purinoreceptor antagonists, said substances having antagonist activity on purinoreceptors and being a product of modifying pyridoxin, particularly n-(1,5-dihydro-3-R1-3-R2-8-methyl-9-hydroxy-[1,3]dioxepino[5,6-c]pyridinyl-6-azo)phenyl sulphonic acid and salt forms thereof of general formula I , where R1 is a hydrogen atom or methyl, R2 is methyl, isopropyl.

EFFECT: compounds of the given formula have high antagonist activity on purinoreceptors and can be used in medicine and veterinary.

2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to synthetic biologically active substances of the heterocyclic series, having anticholinesterase activity, and is a product of modification of pyrodoxine acetals, specifically 1,5-dihydro-3-R1-3-R2-7,8-dimethyl-9-dimethylcarbamoyloxy-[1,3]dioxepino[5,6-c]pyridinium bromide of general formula I, where R1 is a hydrogen atom or a methyl, R2 is selected from: methyl, ethyl, propyl, iso-propyl, tert-butyl, heptyl, octyl or (1-methyldecyl). The compounds of formula (I) have high anticholinesterase activity and can be used in medicine and veterinary.

EFFECT: high activity of the compounds.

2 tbl, 11 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula and their pharmaceutically acceptable salts possessing antibacterial properties, as well as to a based pharmaceutical composition. In formula (I) R1 represents an alkoxy group; each of U and V represents CH, and W represents N, or U represents N, V represents CH and W represents CH or N, or each of U and V represents N, and W represents CH; R2 represents hydrogen or fluorine, if W represents CH, or R2 represents hydrogen, if W represents N; A represents O or CH2; Y represents CH or N; Q represents O or S; and n represents 0 or 1.

EFFECT: preparing the pharmaceutically acceptable salts possessing the antibacterial properties.

23 cl, 3 tbl, 15 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel polyheterocyclic compounds of formulas Ia or Ib, given below, stereoisomers, pharmaceutically acceptable salts or their mixture, where m=0.1 or 2; n=0.1 or 2; p=0.1 or 2; q=0.1 or 2; r=0. 1, 2 or 3; stands for a single bond or a double bond; and stands for a double bond in a macrocyclic internal combination with cyclopropyl formyl; stands for a single bond in a cycle D, E, E1 and G, where D and G independently stand for oxygen, E and E1 independently stand for C(Ra)(Rb); R10 stands for hydrogen; Ra, Rb and Rc independently on each other stand for hydrogen; when r=0 E is absent, D and E1 are directly bound; L stands for methylene (CRbRc); T stands for nitrogen (N) or CH; U stands for carbon (C); W stands for oxygen; X stands for oxygen; Y stands for nitrogen (N) or CH; Z stands for OH; C1-C20 alkyl-sulphonylamido, C3-C20-cycloalkyl-sulphonylamido; R1 and R2 independently stand for C1-C20-alkyl, C3-C20 cycloalkyl, C6-C12 arylamine, C1-C20 alkoxycarbonyl-amino, C2-C20 heterocyclic sulphonylamide ring; R3, R4, R5, R6 - independently stand for H; R7, R8 and R9 independently stand for H. The compounds inhibit replication of protease NS3 of the hepatitis C virus.

EFFECT: improved properties of the compounds.

7 cl, 1 tbl, 11 dwg, 118 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel derivatives of 1-(2-chloroquinolin-3-yl)-4-dimethylamino-2-(naphthalen-1-yl)-1-phenylbutan-2-ol of general formula I or their pharmaceutically acceptable salts with acids, where R1 denotes H, R2+R3 denotes -O-(CH2)n-O-, where n=1-2, which forms additional dioxane and 1,3-dioxolane rings. The invention also relates to a method of producing a compound of formula I and to use of the compound of formula I in treating infectious mycobacterial diseases.

EFFECT: obtaining novel compounds with useful biological activity.

4 cl, 2 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to quinazolinone compounds of formula (I) and its pharmaceutically acceptable salts, wherein n is equal to 0 to 3, and R1 is defined as stated in the patent claim. The above compounds are prolyl hydroxylase inhibitors and can be used in pharmaceutical compositions and methods of treating pathological conditions, disorders and conditions mediated by prolyl hydroxylase activity.

EFFECT: compounds can be administered into the patient for treating, eg anaemia, vascular diseases, metabolic disorders, as well as for wound healing.

22 cl, 2 tbl, 211 ex

FIELD: chemistry.

SUBSTANCE: invention relates to antibacterial compounds of formula

,

where R1 is an alkoxy group; R2 is H or F; each of R3, R4, R5 and R6 is independently H or D; V is CH and W is CH or N, or V is N and W is CH; Y is CH or N; Z is O, S or CH2 and A is CH2, CH2CH2 or CD2CD2; or a salt of said compound. The invention also describes a antibacterial pharmaceutical composition which contains the compound of formula (I) as a basic component, and use of the compound of formula (I).

EFFECT: obtaining novel compounds possessing useful biological properties.

25 cl, 2 tbl, 24 ex

FIELD: chemistry.

SUBSTANCE: invention relates to pyridoxine derivatives general formula I, where: when R2+R3=-C(CH3)2- or -CH(CH3)-; , when R1=H; R2=H; , when R1=H; R3=H; , .

EFFECT: pyridoxine derivatives, having high anti-inflammatory activity and low toxicity.

2 cl, 2 dwg, 6 ex

FIELD: chemistry.

SUBSTANCE: invention relates to pyridoxine derivatives of general formula

,

where R1-is a hydrogen atom or methyl, R2 is a hydrogen atom, methyl, linear, branched or cyclic alkyl or R1 and R2 together form a cyclic alkyl capable of powder second-harmonic generation (SHG).

EFFECT: invention can be used in laser technology and communication equipment.

1 cl, 1 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 compounds of formula A-I, where G1 stands for hydrogen atom or R'; G2 stands for halogen atom, CN, CF3, isopropyl or phenyl, where said isopropyl or phenyl is optionally substituted with up to three substituents, independently selected from WRW; G3 stands for isopropyl or (C3-C10)cycloaliphatic ring, where said G3 is optionally substituted with up to three substituents, independently selected from WRW; W stands for bond or (C1-C6)alkylidene chain, where up to two methylene groups of W residue are optionally and independently substituted for -CO2- or -O-; RW stands for R'; and R' is independently selected from hydrogen atom or (C1-C8)alkyl group. Invention also relates to method of obtaining compound of formula FF (stands for bromine atom, fluorine atom or tret-butyl; G3 stands for tret-butyl) by hydrogenation of respective nitrocompound in presence of palladium catalyst and to methods of obtaining C-9 and 433 compounds, which include stage of hydrogenation of respective nitrocompound in presence of palladium catalyst as intermediate stage.

EFFECT: formula A-I compounds, which are intermediate for synthesis of modulators of ATP-binding cassette ("ABC") transporters.

35 cl, 4 tbl, 80 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates for composition for treatment or prevention of disorders, associated with reduced level of defensins. Composition contains from 0.005 to 1000 mg of Lactobacillus johnsonii Lal (NCC533, No CNCM 1-1225) per a daily dose, with at least 90% of L. johnsonii Lal (NCC533, No CNCM 1-1225) being transferred into state in which they become non-replicating at temperature110-140°C for 5-30 s.

EFFECT: invention provides enhancement of expression of defensin hBD1 mRNA.

5 cl, 2 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relates to field of pharmaceutics and medicine and deals with composition, possessing property to stimulate antimicrobial defence by increasing expression of endogenous β-defensins, containing strain B. longum NCC 2705, depositary number CNCM 1-2618, with said strain being brought, at least, partially into non-replicable condition by thermal inactivation, processing , at least, about 70°C. Method of stimulating endogenous antimicrobial activity of mammal by increasing expression of endogenous β-defensins, includes introduction of claimed composition.

EFFECT: group of inventions provides increase of efficiency in comparison with live strains.

12 cl, 2 dwg

FIELD: chemistry.

SUBSTANCE: group of inventions relates to biotechnology. Claimed is a strain of Bacillus subtilis Maseca-1, producing a peptide, which has the antimicrobial activity against Micrococcus luteus, Bacillus cereus and Aspergillus flavus. The strain is deposited in ATCC under number PTA-8831. The strain was isolated from pericarp of nixtamalised corn. Also claimed is a method of inhibiting Micrococcus luteus, Bacillus cereus and Aspergillus flavus in a material, containing or subjected to the action of the said microorganisms. The method includes the impact of an effective quantity of the said strain on the material.

EFFECT: group of inventions provides the effective inhibition of the growth of pathogenic microorganisms Micrococcus luteus, Bacillus cereus and Aspergillus flavus.

5 cl, 13 dwg, 7 tbl

FIELD: chemistry.

SUBSTANCE: method includes treating crushed Echinacea purpurea (L.) Moench roots and rhizome with steam, extraction with ethyl alcohol, then steeping, stirring, steeping, draining a portion of the extract which is equal to the amount of the loaded Echinacea purpurea (L.) Moench roots and rhizome, after draining a portion of the extract, adding ethyl alcohol to the treated material, draining the whole extract; extracting crushed Echinacea purpurea (L.) Moench herbs with ethyl alcohol, steeping, then stirring, steeping, draining a portion of the extract which is equal to the amount of the loaded Echinacea purpurea (L.) Moench herbs, after draining a portion of the extract, adding ethyl alcohol to the treated herbs, draining the whole extract; all obtained extracts are mixed, cooled and filtered under certain conditions. An Echinacea purpurea (L.) Moench tincture. Use of the method to obtain an Echinacea purpurea (L.) Moench tincture.

EFFECT: method preserves the biological activity of components of the tincture and medicinal properties.

3 cl

FIELD: biotechnologies.

SUBSTANCE: method of obtaining of a complex of antimicrobic peptides of an insect includes infecting of adipose body of an insect at a larval instar with Micrococcus luteus A270 and Escherichia coli D31 bacteria with the subsequent extraction of adipose body of an insect at a larval instar. The adipose body of an insect is placed into a nutrient medium containing water solution of sugars, inorganic salts and the antibiotic meropenem in pre-set ratio and incubated during a day with the subsequent elution of the complex of antimicrobic peptides of an insect from cultural liquid by the method of reverse-phase chromatography on the column Vydac C18 at the linear gradient of acetonitrile from 0% up to 50%.

EFFECT: invention allows to simplify a method of obtaining antimicrobic peptides.

5 dwg, 4 ex

FIELD: chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, namely to the field of obtaining 5,9-eicosadienoic acid of formula (1), demonstrating an inhibiting effect on human topoisomerase (5Z,9Z)-5,9- The essence of the method consists in the following: tetrahydropyran ether of 5,6-heptadien-1-ol (4) and 1,2-tridecadiene (5) interact with the Grignard reagent RMgX (R=Me, Et, Pr, Bu, Oct; X=Cl, Br, I) in diethyl ether in the presence of metal Mg (powder) and the catalyst titanocenedichloride Cp2TiCl2, with the molar ratio of (4):5): RMgX:Mg:Cp2TiCl2=10:12:(30-50):32:(0.4-0.6), in an argon atmosphere at a temperature of 0-35°C and atmospheric pressure for 6-10 h, after which the reaction mass is processed with a 5% water HCl solution with obtaining 2-[(5Z,9Z)-5,9-eicosadien-1-yloxy]tetrahydro-2H-pyrane (6), which is oxidised with the Jones reagent.

EFFECT: eicosadienic acid is promising as the medication, possessing anti-tumour, antiviral and antibacterial action.

2 cl, 1 tbl, 1 dwg, 15 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of formula , wherein A and V independently represents H or a halogen; Q is absent; R4 independently represents H, a C1-C6 alkyl or C3-C6 cycloalkyl; R7 represents H; and R8 represents a C1-C10 alkyl substituted by OH or C1-C6 alkoxy; or C1-4 alkyl substituted by a 5-6-merous aromatic heterocyclic ring containing 1-2 heteroatoms specified in N and S, wherein the above aromatic heterocyclic ring is optionally substituted by a C1-C10 alkyl; or in -NR7R8, R7 and R8 together with N can form an optionally substituted azacyclic ring containing where applicable an additional heteroatom specified in H, O and S, as a cycle member, optionally substituted by a C1-C10 alkyl, which is substituted by a C1-C6 alkoxy; m is equal to 0; n is equal to 0. The invention also refers to a compound of formula (wherein the substitutes are those as specified in the patient claim), to a pharmaceutical composition containing a therapeutically effective amount of the compounds of formula (VIII), and to a method of treating or relieving a cell-proliferative disorder.

EFFECT: compound of formula (VIII) inhibiting cell proliferation or cell apoptosis.

12 cl, 1 dwg, 14 tbl, 55 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to the strain Lactobacillus rhamnosus CNCM I-3690 and to a dairy food product containing the above strain. The presented strain possesses the mannose-specific adhesive properties. The strain possesses the antimicrobial properties in relation to, e.g. Escherichia coli, Salmonella enteritidis and Lysteria monocytogenes.

EFFECT: strain possesses the immunomodulatory properties, particularly possesses an ability to inhibit an inflammatory reaction of HT-29 epithelial cells.

2 cl, 2 dwg, 5 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to 2-(3-amino-1-(2,4-difluorophenyl)-1H-1,2,4-triazol-5-yl)-N-methyl-4,5-dihydrobenzo[b]thieno[2,3-d]oxepin-8-carboxamide. As well as to a pharmaceutical composition containing the above compound, to the use thereof and a set for treating.

EFFECT: 2-(3-amino-1-(2,4-difluorophenyl)-1H-1,2,4-triazol-5-yl)-N-methyl-4,5-dihydrobenzo[b]thieno[2,3-d]oxepin-8-carboxamide inhibiting PI3 kinase (PI3K).

6 cl, 15 dwg, 1 tbl, 610 ex

Up!