Complex connection of 5-hydroxy-3,6-dimethyluracyl with succinic acid exhibiting membrane-stabilizing activity and method of its production
SUBSTANCE: complex compound is produced by mixing equimolar amounts of 5-hydroxy-3,6-dimethyluracil with succinic acid in an organic solvent, followed by heating the reaction mixture for 1 hour at 70°C, cooling the reaction mixture and filtering the precipitated crystals. .
EFFECT: having membrane-stabilizing and anti-radical activity, reduced toxicity in comparison with the known compounds of identical purpose.
2 cl, 3 tbl, 4 ex
SUBSTANCE: invention relates to a novel complex of 5-hydroxy-6-methyluracil with 5-aminosalicylic acid of formula . The compound has anti-inflammatory activity and can be used as a basic active substance when producing novel medicinal preparations having anti-inflammatory action. The invention also relates to a method of obtaining said complex. The method includes reacting 5-hydroxy-6-methyluracil with 5-aminosalicylic acid in equimolar amounts in an aqueous medium at room temperature for 24 hours, followed by removal of water from the reaction mixture and obtaining the product.
EFFECT: wider range of pharmacological preparations with low toxicity, having higher anti-inflammatory activity.
2 cl, 1 tbl, 1 ex
SUBSTANCE: preparation shows an antitoxic activity, and can be used as an antidote for nitrite and nitrate poisoning. A complex compound of 5-hydroxy-6-methyluracil with ascorbic acid (5-hydroxy-6-methyluracil ascorbate) is described by formula: The preparation contains the complex compound in an amount of 0.3-0.4 wt %, and ascorbic acid - the rest. The method for producing the preparation consists in a reaction of 5-hydroxy-6-methyluracil and ascorbic acid taken in the relation of ascorbic acid: 5-hydroxy-6-methyluracil equal to 1:(0.0015-0.0022), in water as a solvent at a temperature of 20-40°C for 30-60 minutes. The complex compound is produced as shown by infra-red and NMR spectra. The antitoxic activity of 5-hydroxy-6-methyluracil on nitrite has been unknown before.
EFFECT: water removal from the reaction mixture under low pressure.
2 cl, 2 tbl, 1 ex
SUBSTANCE: invention relates to a novel complex of 5-hydroxy-6-methyluracil with sodium succinate (5-hydroxy-6-methyluracil succinate) of formula: , which exhibits antihypoxic activity. The disclosed compound widens the range of pharmacologically active compounds with low toxicity and high antihypoxic activity, which increase body resistance to certain types of hypoxia and in conditions influenced by other extreme environmental factors. The invention also relates to a method of producing the complex. The method involves mixing 5-hydroxy-6-methyluracil and sodium succinate in ratio of 1:10 in distilled water and then mixing the reaction mixture until dissolution of 5-hydroxy-6-methyluracil, removing the solvent from the reaction mixture and extracting the product.
EFFECT: output of the end product reaches 98%.
3 cl, 2 tbl, 4 ex
SUBSTANCE: invention refers to new biologically active high-immunotropic compound -N,N'-(sulphonyldi-1,4-phenylene)bis[(N",N'"-dimethyl)methyliminomethane]1,2,3,4-tetrahydro-6-methyl-2,4-dioxo-5-pyrimidinesulphonate of formula stated below to be used in treatment of, e.g., patients suffering from leprosy, allergic dermatosis, dermatitis herpetiformis. .
EFFECT: new compound is characterised with useful biological activity.
2 tbl, 1 ex
SUBSTANCE: invention relates to the new complex compound of 1,3-bis(2-hydroxyethyl)-5-hydroxy-6-methyluracil with fumaric acid of the formula which can be used in medicine as the substance capable of raising the survival rate in conditions under the influence of extreme environmental factors, particularly hypoxia. The new complex compound 1,3-bis(2-hydroxyethyl)-5-hydroxy-6-methyluracil with fumaric acid is obtained with 94% output by mixing equimolar quantities of 1,3-bis(2-hydroxyethyl)-5-hydroxy-6-methyluracil with fumaric acid in organic solvent with the subsequent heating of the reaction mixture for 2-3 hours, preferably at a temperature of 60-70°, removal of the solvent from the reaction mixture and the isolation of the product.
EFFECT: it makes it possible to increase the survival rate in harsh environmental conditions.
3 cl, 3 tbl, 5 ex
FIELD: organic chemistry, chemical technology.
SUBSTANCE: invention relates to the improved method for preparing 4,6-dimethoxy-2-(methylsulfonyl)-1,3-pyrimidine. Method involves reaction of 4,6-dichloro-2-(methylthio)-1,3-pyrimidine with alkaline metal methoxide in inert organic solvent, transfer of prepared 4,6-dimethoxy-2-(methylthio)-1,3-pyrimidine in aqueous acid medium and the following oxidation of this compound in the presence of catalyst if necessary, preferably, with an interphase catalyst, such as tricaprylmethylammonium chloride. Then method involves carrying out the purification stage wherein pH value of the aqueous acid reaction mixture is brought about to the value from 5 to 8 with aqueous base, such as alkaline metal hydroxide, for example, sodium hydroxide at temperature 10-90°C and stirring in the presence of absence of organic solvent, for example, aromatic hydrocarbon, such as benzene, toluene or isomeric xylenes, or alcohol, such as methanol or ethanol. Also, invention relates to using the prepared compound as an intermediate substance for synthesis of herbicide, in particular, 7-[(4,6-dimethoxypyrimidin-2-yl)thio]-3-methylphthalide by reaction of 7-mercapto-3-methylphthalide of compound in preparing herbicides, for example, 7-[(4,6-dimethoxypyrimidin-2-yl)thio]-3-methylphthalide.
EFFECT: improved preparing method.
24 cl, 2 sch, 1 ex
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to 4,4'-sulfonyl-bis-(N,N'-dimethylammoniomethyleneaniline)-chloride, 6-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonate of the formula (I) eliciting antibacterial, antimycobacterial and immunotropic activities. Also, invention describes a pharmaceutical composition based on compound of the formula (I).
EFFECT: valuable medicinal properties of compounds and composition.
3 cl, 7 tbl, 2 ex
FIELD: organic chemistry, biochemistry, pharmacy.
SUBSTANCE: invention relates to new heterocyclylsulfonyl alkylcarboxylic acids and their derivatives of the general formula (1): or their pharmaceutically acceptable salts, N-oxides or hydrates possessing the inhibitory effect on kinase activity and to the focused library for search of active leader-compounds comprising at least abovementioned compound. In the general formula 91) W represents optionally substituted heterocyclic radical, among them: pyrrole-3-yl, thiophene-2-yl, isooxazole-4-yl, pyrazole-4-yl, imidazole-4-yl, pyridine-3-yl, 1H-2,4-dioxopyrimidine-5-yl, 2,3-dihydro-1H-indole-5-yl, 2,3-dihydro-1H-indole-7-yl, 1,3-dihydro-2-oxoindole-5-yl, 2,3-dioxo-1H-indole-5-yl, 2-oxo-3H-benzoxazole-6-yl, benzothiazole-6-yl, 1H-benzimidazole-5-yl, benzo[1,2,5]oxadiazole-4-yl, benzo[1,2,5]thiadiazole-4-yl, 1,2,3,4-tetrahydroquinoline-6-yl, 3,4-dihydro-2-oxo-1H-quinoline-6-yl, quinoline-8-yl, 1,4-dihydro-2,3-dioxoquinoxaline-6-yl, 3-oxo-4H-benzo[1,4]oxazine-7-yl, 3-oxo-4H-benzo[1,4]thiazine-7-yl, 2,4-dioxo-1H-quinazoline-6-yl, 2,4-dioxo-1,5-dihydrobenzo[b][1,4]diazepine-7-yl or 2,5-dioxo-3,4-dihydrobenzo[b][1,4]diazepine-7-yl; Y represents optionally substituted methylene group; R1 represents chlorine atom, optionally substituted hydroxyl group, optionally substituted amino-group, optionally substituted azaheterocyclyl; n = 1, 2 or 3; or Yn represents carbon atom of optionally substituted (C3-C7)-cycloalkyl or optionally substituted (C4-C7)-heterocyclyl. Also, invention relates to a pharmaceutical composition in form of tablets, capsules or injections placed into pharmaceutically acceptable package.
EFFECT: valuable properties of compounds.
5 cl, 3 sch, 5 tbl, 6 ex
< / BR>where R denotes cyclopropyl, cyclobutyl, cyclohexyl, phenyl, unsubstituted or mono -, di - or tizamidine group selected from hydroxy, C1-C4of alkyl, C1-C4alkoxy, halogen, trifloromethyl, ceanography and amino groups; 1-or 2-naphthyl, 9-anthracene; 2-anthrachinone, Persil, unsubstituted or substituted group selected from1-C4of alkyl, C1-C4alkoxy, ceanography and halogen; 2-, 3 - or 4-chinoline, oxiranyl, 1-benzotriazolyl, 2-benzoxazolyl, furanyl, substituted C1-C4alkoxycarbonyl; C1-C4alkylsulphonyl or benzoyl; R1denotes halogen or1-C4alkyl, R2and R3independently represent hydrogen or C1-C4alkyl; X denotes an oxygen atom and Y represents an oxygen atom, a sulfur atom or a carbonyl, or their pharmaceutically acceptable salts, method of production thereof and pharmaceutical composition having antiviral activity, containing antiviruse-effective amount of compounds of General formula I
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to pharmaceutical industry, namely to selenium nanocomposites of natural hepatotrophic galactose-containing polysaccharide matrixes, representing water-soluble orange-red powders containing zerovalent selenium (Se0) nanoparticles sized 1-100 nm in the quantitative content of 0.5 - 60 wt %, possessing antioxidant activity for treating and preventing redox-related pathologies, particularly for treating toxic liver damage, to a method for producing and to an antioxidant agent containing the above nanocomposites.
EFFECT: invention provides the targeted agent delivery to liver cells, as well as higher agent accessibility and lower toxic action of selenium.
7 cl, 11 ex, 4 tbl
SUBSTANCE: method involves chelation of ferric (III) ions both in vivo, and in vitro with using 2-ethyl-6-methyl-3-hydroxypyridine succinate (Mexidol) to produce a stable stained complex having a high molecular weight and a complex (organic-inorganic) composition not identified among the known compounds.
EFFECT: high effectiveness of the chelation process and low toxicity of Mexidol that makes it promising for biomedical application.
4 dwg, 3 tbl, 3 ex
SUBSTANCE: invention relates to field of organic chemistry, namely to novel compound - 5(6)-nitro-1-(thietanyl-3)-2-ethoxybenzimidazole, inhibiting peroxidation of lipids.
EFFECT: novel compound, possessing useful biological properties, has been obtained.
2 cl, 1 dwg, 2 ex
SUBSTANCE: invention represents a mixture of two structural isomers: 2,6-di(1,7,7-trimethylbicyclo[2.2.1]hept-2-yl)-4-methylphenol and its diastereomers, and 2-(1,7,7-trimethylbicyclo[2.2.1]hept-2-yl)-6-(2,2,1-trimethylbicyclo[2.2.1]hept-5-yl)-4-methylphenol, and their diastereomers with the ratio of the first and second structural isomer isomers from 60:40 wt % to 95:5 wt %.
EFFECT: extension of the arsenal of means, possessing simultaneously haemorheological, anti-aggregate, anti-thrombogenic, retinoprotecting, endothelium-protecting, neuroprotecting, anti-arrhythmia and anti-ischemic activity, enhancing the cerebral blood flow.
4 dwg, 20 tbl, 6 ex
SUBSTANCE: what is presented is using Histochrom (same as echinochrome A or pentahydroxyethyl naphthoquinone) as an agent able to prevent pulmonary fibrosis developed under cytostatic agents. The invention can be used for the pharmacological prevention and correction of the pulmonary tissue disorders caused by administering the cytostatic agents.
EFFECT: preventing hypertrophy of interalveolar connective tissue in the lungs associated with administering bleomycin.
4 dwg, 1 tbl
SUBSTANCE: drops possessing antiviral and immunomodulatory effects characterised by the fact that they represent a 95% ethanol infusion of wild strawberry leaves and fruit specified in: red raspberry fruit, mountain ash fruit, bilberry fruit, blood-red hawthorn fruit, cinnamon rose fruit; 15-25 mg of the substance in 1 ml of the infusion.
EFFECT: drops possess pronounced antiviral and immunomodulatory effects.
15 tbl, 5 ex
SUBSTANCE: melanin having water-solubility of at least 80% and an paramagnetic centre concentration of at least 8·1017 spin/g is administered orally into the animals having been exposed to the radiation in a dose high enough to cause a spinal radiation injury; melanin is administered after dissolved in distilled water in the effective concentration. Melanin water is used as drinking water for the mice having been exposed to single and fractionated acute radiation, which is able to cause acute radiation disease. Melanin water is taken from the 1st to 30th day following the single radiation, or from the 1st day of the fractionated radiation to the 30th day on completion of the radiation.
EFFECT: higher survival rate, faster recovered haemopoiesis, body weight and orientation and motion activity.
7 tbl, 5 ex
SUBSTANCE: invention provides a composition having antioxidant properties in the form of a tablet, comprising an active agent based on nicotinamide adenine dinucleotide in reduced form (NADH) and inert filling agents, characterised by that the active ingredient is a complex which is a mixture of 10 wt % NADH with 63 wt % vegetable fats, 17 wt % beeswax and 10 wt % chlorophyll, and the inert filling agents are in the form of microcrystalline cellulose, Macrogol 6000, intense sweetener and a food flavourant.
EFFECT: invention provides a new tablet form of NADH.
SUBSTANCE: invention refers to a pharmaceutical composition with anti-ischemic and antioxidant activity in the form of tablets or capsules, and a method for preparing it. The composition contains 4-((3-oxo-3-ethoxypropanoyl)amino)benzoic acid in an amount of 40 to 80 wt %, an amino-containing compound and pharmaceutically acceptable excipients. The amino-containing compound is specified in a group of trometamol, methyl glucamine and L-lysine; 1 mole of 4-((3-oxo-3-ethoxypropanoyl)amino)benzoic acid is accounted for 0.05 to 0.25 mole of the above amino-containing compound. The composition also contains lactose, microcrystalline cellulose, calcium stearate and other pharmaceutically acceptable excipients. According to the method for preparing the composition, taking 4-((3-oxo-3-ethoxypropanoyl)amino)benzoic acid and amino-containing compound in molar ratio 1:0.05 to 1:0.25, pre-mixing, moisturising with a aqueous or alcohol solution of a binding agent, adding pharmaceutically acceptable excipients in such an amount to provide the content of 4-((3-oxo-3-ethoxypropanoyl)amino)benzoic acid from 40 to 80 wt %, granulating the mixture, drying and producing tablets or capsules according to the known technique.
EFFECT: implementing the above application.
6 cl, 7 tbl, 4 ex
SUBSTANCE: claimed is the application of 5(6)-nitro-1-(1,1-dioxothietanyl-3)-2-chlorobenzimidazole of formula (I) , earlier known as the means with broncholytic and spasmolytic activity, as the means, inhibiting peroxide oxidation of lipids.
EFFECT: realisation of the claimed purpose.
SUBSTANCE: what is presented is a method for acute exposure to organophosphates with pronounced non-anticholinesterase mode of toxicity. A method consists in preventive administration of β-oestradiol 100 mg/kg 20-60 min prior to application of the toxic agent organophosphate.
EFFECT: reducing the manifestations of first signs of the exposure, developing convulsions and complete elimination of animals' death experimentally, administering β-oestradiol 5 days or 1 day before the exposure has not been producing such an effect.