RussianPatents.com
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Anxiolytic and cerebroprotective agent reducing inclination to alcohol. RU patent 2393855. |
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FIELD: medicine, pharmaceutics. SUBSTANCE: invention refers to medicine, particularly to pharmacology and concerns application of derivatives of gamma-aminobutyric acid in the form of 4-amino-3-phenyl butane acid salts of general formula as an anxiolytic and cerebroprotective agent reducing inclination to alcohol. EFFECT: preparation of the agent with reduced by-effects. 2 cl, 10 tbl, 14 ex
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Agent and alcohol-free drink for prophylactics of consequences and reduction of manifestations of acute alcohol intoxication / 2393721 Method for prophylactics of consequences and reduction of acute alcohol intoxication manifestations contains biologically active compounds of dry extract of haws. The latter includes procyanidins (from monomers to hexamers with average extent of polymerisation from 1.1 to 5.5) from 1.0-50.0 mg/g of extract dry weight equivalent to cyanidin chloride), epicatechins, chlorogenic acid and flavonoids, represented by hyperoside, rutin, quercitin, glycosides of vitexin, vitexin, isovitexin, orientin, isoorientin, apigenin, with total concentration of phenol compounds of at least 10 mg/g of extarct dry weight equivalent to gallic acid. Alcohol-free drink for prophylactics of consequences and reduction of unfavorable manifestations of acute alcohol intoxication contains above-specified dry extract of haws in concentration from 1.0 to 60.0% as an active substance. It makes it possible to increase latent period of narcotic dream and to reduce its duration. |
Derivatives of aminopiperidine, their production and use in therapy / 2376303 Invention is related to new compounds of formula (I): , in which: Ra and Ra', identical or different, mean atom of hydrogen or alkyl, R1 means atom of hydrogen or alkyl, cycloalkyl, heterocycloalkyl or aryl, R2 means group of formula -(CH2)x-(CO)y-Y or -(CO)y-(CH2)x-Y, in which, x = 0, 1, 2, 3 or 4, y = 0 or 1, Y means atom of hydrogen or the following group: hydroxyl, alkyl, cycloalkyl, alkyloxyl, aryl, heteroaryl or -NR11R12, besides, Y is not an atom of hydrogen, when x=y=0, R11 and R12, identical or different, mean atom of hydrogen or the following group: alkyl, cycloalkyl, alkyloxyl or -NR13R14, or R11 and R12 together with atom of nitrogen, to which they are connected, create mono- or bicyclic structure, which contains 4-10 links and unnecessarily contain additionally 1-3 heteroatoms and/or 1-3 ethylene unsaturated links, besides this cycle is not necessarily substituted in any of positions with 1-3 groups, selected from atoms of halogen and hydroxyl, alkyl, cycloalkyl and alkyloxygroups; R13 and R14, identical or different, mean atom of hydrogen or alkyl, R3 means 1-3 groups, identical or different, available in any position of cyclic structure, to which they are connected, and selected from atoms of halogen; R5 means atom of hydrogen, R4 is selected from groups of formulae (a), (b), (c), which are not necessarily substituted with aryl group, described below: (a), (b), (c), in which p=0,1,2 or 3; m=0,1 or 2, and either a) X means link -N(R10)-, in which R10 is selected from: -CO-alkyl, -CO-cycloalkyl, -CO-heterocycloalkyl, -CO-aryl, -CO-heteroaryl, - or R10 with atom of nitrogen, with which it is connected, and with atom of carbon, available in any position of cyclic structure of formula (a), but not with neighboring to mentioned atom of nitrogen, creates bridge, containing 3-5 links, or, b) X means link -C(R6)(R7)-, where R6 is selected from the following: atom of hydrogen, atom of halogen, group -(CH2)x-OR8, -(CH2)x-NR8R9, -(CH2)x-CO-NR8R9 or -(CH2)x-NR8-COR9, in which x=0,1,2,3 or 4, alkyl, cycloalkyl, heterocycloalkyl, aryl, heterocycloalkyl, condensed with aryl, besides, alkyl, cycloalkyl or aryl groups are not necessarily substituted with 1 or several groups, selected from groups: R, R', -OR, -NRR', -COR; R7 is selected from atoms of hydrogen and halogen and the following groups: alkyls, -OR, -NRR', -NR-CO-R', -NR-COOR', -R8 and R9 are selected, independently from each other, from atom of hydrogen and the following groups: alkyls, cycloalkyls, aryls, -CO-alkyls, besides, alkyls and aryls are unnecessarily substituted with one or several groups, selected from groups: R, R', -OR, or R8 and R9 together create heterocycloalkyl,- R and R' mean, independently from each other, atom of hydrogen or alkyl, cycloalkyl, besides, mentioned hetero aryl groups represent aromatic groups, including from 5 to 10 links and including from 1 to 4 heteroatoms, such as atom of nitrogen, oxygen and/or sulfur; besides mentioned heterocycloalkyl groups represent cycloalkyl groups, including from 5 to 6 links and including from 1 to 4 heteroatoms, such as atom of nitrogen, oxygen or sulfur; in the form of base or acid-additive salt, and also in the form of hydrate or solvate. Invention is also related to medicinal agent, to pharmaceutical composition, to application, to method of production, and also to compounds of formulas (VI), (XVIII), (XIX). |
Derivatives of oxopiperidine, their production and use in therapy / 2376298 Invention is related to new compounds that comply with formula (I) , where: n is equal to 1, Ra, Ra', Rb, Rb', identical or different, mean atom of hydrogen or alkyl or cycloalkyl group, besides, Rb and Rb' may create carbon bridge having 4 links together with hydrogen atoms of cycle, to which they are connected, R1 means cyclohexyl group, R2 means 1,2,4-triazolyl group, R3 means 1-3 groups, selected from atoms of halogen, available in any position of cycle, to which they are connected, R5 means atom of hydrogen, R4 is selected from groups of formulas (a), (b) and (c), given below, mono- or polysubstituted with aryl group: (a), (b), (c), in which: p=0, 1, 2 or 3, m=0, 1 or 2, and either a) X means link -N(R10)-, where R10 is selected from: groups -CO-NR8R9, -COOR8, -(CH2)x-OR8, -(CH2)x-COOR8, -(CH2)x-COR8, in which x=1, 2, 3 or 4, heterocycloalkyl group, condensed with aryl group, cycloalkyl, aryl, heteroaryl, alkylaryl, -CO-alkyl, -CO-cycloalkyl, -CO-heterocycloalkyl, -CO-aryl, -CO-heteroaryl, -CO-alkylaryl, -SO2-alkyl, -SO2-cycloalkyl, -SO2-aryl, besides, alkyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl groups are unnecessarly substituted with one or several groups selected from atoms of halogen and groups R, R', OR, NRR', -CN, -COOR, COR; or R10 together with atom of nitrogen, to which it is connected, and with atom of carbon, available in any position of cyclic structure of formula (a), but not in neighboring position to mentioned atom of nitrogen, creates a bridge that contains 3-5 links, R8 and R9 are selected, independently from each other, from atom of hydrogen and alkyl or cycloalkyl groups; R and R' mean, independently from each other, atom of hydrogen or alkyl, cycloalkyl, aryl groups; or b) X means link - C(R6)(R7)-, where R6 is selected from the following: atom of hydrogen, atom of halogen, groups -(CH2)x-OR8, -(CH2)x-COOR8, -(CH2)x-NR8R9, -(CH2)x-CO-NR8R9 or -(CH2)x-NR8-COR9, in which x=0, 1, 2, 3 or 4, alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, alkylaryl, alkylheteroaryl group, heterocycloalkyl group, condensed or non-condensed, available in spiro-position to cycle of formula (a), to which it is connected, heterocycloalkyl group, condensed with aryl group, besides, alkyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl groups are unnecessarily substituted with one or several groups selected from atoms of halogen and groups R, R', OR, NRR', -CO-NRR', -CN, -COOR, OCOR, COR, NRCOOR'; and heterocycloalkyl groups are unnecessarily condensed with aryl group; R7 is selected from atoms of hydrogen and halogen and alkyl, cycloalkyl, aryl, heteroaryl, alkylaryl, alkylheteroaryl groups, -OR, -O-aryl, -O-alkylaryl, -O-alkylheteroaryl, groups -NRR', -CO-NRR', -NR-CO-R', -NR-CO-NRR', -NR-COOR', -NO2, -CN and -COOR, R8 and R9 are selected, independently from each other, from atom of hydrogen and alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, alkylaryl, alkylheteroaryl groups, -CO-alkyl, -CO-cycloalkyl, -CO-aryl, -(CH2)x-OR, where x=0, 1, 2, 3 or 4, besides, alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl groups are unnecessarily substituted with one or several groups selected from atoms of halogen and groups R, R', OR, NRR', -CO-NRR', -CN, -COOR, OCOR, COR, NRCOOR'; or R8 and R9 create together cycloalkyl or heterocycloalkyl; R and R' mean, independently from each other, atom of hydrogen or alkyl, cycloalkyl, heterocycloalkyl, aryl, or may together create cycloalkyl or heterocycloalkyl; besides heteroaryl group represents aromatic group that contains from 5 to 10 atoms and from 1 to 4 heteroatoms, selected from nitrogen, oxygen or sulfur; heterocycloalkyl group represents cycloalkyl group, which contains from 5 to 10 atoms and contains from 1 to 4 heteroatoms selected from nitrogen, oxygen or sulfur; in the form of base or acid-additive salt, and also in the form of hydrate or solvate. Invention is also related to medicinal agent, to pharmaceutical composition, to application, to method of production, and also to compounds of formulas (IV) , (V), (VI), (XXVIII), (XXIX), (II). |
Agent for reduction of alcohol intoxication period / 2376027 Invention is related to chemical-pharmaceutical industry, namely to agents on vegetal basis, intended for intake together with food or drinks to facilitate consequences and reduce period of alcoholic intoxication of human body (withdrawal syndrome). Agent for reduction of alcoholic intoxication period contains active and auxiliary substances, besides active substances used are dry extracts of ginger, eleutherococcus, ginseng, paullinia and holly at the following ratio of components, wt %: dry extract of ginger 40-60; dry extract of eleutherococcus 14-28; dry extract of ginseng 2.0-6.0; dry extract of paullinia 5.0-9.0; dry extract of holly 0.5-2.5; auxiliary substances - the rest. Auxiliary substances used are mainly represented by citric acid, succinic acid, dry extract of licorice. |
Method for reduction of morbid attraction to ethanol in postabstinent period / 2373927 Invention refers to medicine, particularly to experimental narcology, and concerns reduction of morbid attraction to ethanol in postabstinent period. That is ensured by daily introduction of vinpocetine in a dose 10 mg/kg combined with isonitrosin in a dose 20 mg/kg within 14-20 days. |
Alpha-lipoic (thioctic) acid composition, method for making thereof and therapy / 2372904 Invention refers to medicine and pharmacology and presents a pharmaceutical composition based on alpha-lipoic acid as an aqueous solution for injections, for treatment and/or prevention of a disease chosen from group including alcoholic and/or diabetic polyneuropathy, coronary atherosclerosis, hyperlipidemia, hyperlipoproteinemia, mild and moderate viral hepatitis type A, hepatic cirrhosis, heavy metal salts poisoning, intoxications of various aetiologies, differing that it contains ethylenediamine, propylene glycol, solubiliser presented with plasdone, water for injection or 0.9% NaCI solution for injection in a certain relation components in the composition. |
Compositions with prolonged action based on naltrexone and methods of their application / 2370257 Invention relates to medicine, namely to addictology and can be applied for treating people from alcohol dependence. Method by invention includes stage of parenteral introducing of composition of prolonged action, which contains naltrexone, value of AUC for naltrexone in serum being, at least, twice larger, than corresponding value, achieved by introduction of 50 mg/day perorally. |
Monoaminooxidase inhibitors, therapeutic agent and pharmaceutical composition / 2366430 Invention refers to therapeutic agents and concerns a therapeutic agents used for treatment of the patients suffering from diseases caused by monoaminooxidase overactivity and representing polyprenols of formula (1). The content of polyprenols of formula (1) where n=8-20 in the specified agent is 0.1 to 80%. Also there is disclosed method for treatment of the patients suffering from diseases caused by monoaminooxidase overactivity, characterised that a patient takes one or more doses of polyprenols of formula (1) in amount 1 to 150 mg a day (1). |
Antiwithdrawal agent, biologically active additive, pharmaceutical composition, medical product and method of producing / 2358723 New agent is characterised with antiwithdrawal action, containing L-serine and fructose as an active components and additionally tianin, at mass ratio of L-serine, tianin and fructose (12-18):(0.8-1.2):(40-60) respectively. It is preferentially to use L-tianin at mass ratio of L-serine, L-tianin and fructose as 15:1:50. Said agent can be used as the biological food additive. The invention also concerns a pharmaceutical composition, method of producing and a medical product based on the agent or pharmaceutical composition as tablets, capsules or injections in pharmaceutically acceptable package. The agent allows relieving the alcohol withdrawal caused by overuse, e.g. of products containing ethyl alcohol. |
Method of alcoholic toxicoses treatment / 2350336 Invention concerns medicine, namely to narcology and can be used at treatment of the abstinent syndrome bound to abusing of alcohol both complicated exo- and endointoxications. For this purpose indirect electrochemical oxidation of blood of the patient is spent by intravenous introduction 0.06% solutions of sodium hypochlorite. The solution is administered two times a day with the 12-sentry an interval in volume not more than 600 ml a day. In addition enter ECOFLOR enterosorbent in a dose not more than 1 g of dry matter on 1 kg of body weight of the patient in a day into 3 receptions. |
Substituted 2-amino-3-sulfonyl-tetrahydro-pyrazolo[1,5-a]pyrido-pyrimidines-antagonists of serotonin 5-ht6 receptors, methods of producing and using said compounds / 2384581 Invention relates to novel antagonists of serotonin 5-HT6 receptors - substituted 2-amino-3-sulfonyl-6,7,8,9-tetrahydro-pyrazolo[1,5-a]pyrido[3,4-e]pyrimidines of general formula 1 and substituted 2-amino-3-sulfonyl-5,6,7,8-tetrahydro-pyrazolo[1,5-a]pyrido[4,3-d]pyrimidines of general formula 2 or their pharmaceutically acceptable salts and/or hydrates, method of producing said compounds and pharmaceutical compositions, medicinal agents and treatment method. In compounds of formula 1 and general formula 2 , Ar is phenyl which is possibly substituted with halogen atoms, or a 6-member nitrogen-containing heteroaryl; R1 is a hydrogen atom, C1-C3alkyl which is possibly substituted with phenyl, C1-C5alkoxycarbonyl; R2 is a hydrogen atom, halogen or C1-C3alkyl; R1 3 and R2 3 are optionally identical substitutes selected from a hydrogen atom, optionally substituted C1-C3alkyl or R1 3 and R2 3 together with the nitrogen atom with which they are bonded form a nitrogen-containing 6-member saturated heteroaryl optionally substituted with C1-C5alkoxycarbonyl, where the said heteroaryl has 1-2 heteroatoms selected from nitrogen. |
4-(sulphanilpyrimidine-4-ylmethyl)morpholine derivatives as gaba-receptor ligands for treating anxiety, depression and epilepsy / 2382033 Invention refers to compound of formula I wherein X represents -S- or -NH-; R1 represents C1-12alkyl, C2-12alkenyl, phenyl C1-12alkel, phenyl C2-12alkenyl or phenyl-O-C1-12alkyl and wherein said phenyl groups are optionally substituted with one or two assistants chosen from the group consisting of lower C1-7alkyl, C C1-7alkoxy and halogen C1-7alkyl; R2 represents hydrogen, lower C1-7alkyl or C3-6cycloalkyl; R3/R4 together with N-atom whereto attached, form nonaromatic 5,6-members heterocyclic ring system which optionally contains in addition to N-atom one additional heteroatom chosen from the group, consisting of O or N and where the ring system is optionally substituted group lower C1-7alkyl, lower C1-7alkoxy, -NR2, -CONR2; or R3/R4 together with N-atom whereto attached, can form heterocyclic ring system which contains at least two rings and which optionally contains one or two additional heteroatoms chosen from group, consisting of N and O; R represents hydrogen or lower C1-7alkyl; R5 represents hydrogen or lower C1-7alkyl; or to pharmaceutically acceptable additive salts with acid of this compound. The invention also concerns a medical product. |
Quinoline as allosteric enhencer of gaba-b receptors / 2378256 Present invention relates to compounds of formula (I) , where R1 is hydrogen, C1-C7 alkyl; R2 is C1-C7 alkyl, aryl, C1-C7 haloalkyl or C3-C8 cycloalkyl; R3, R4 each independently represents hydrogen, halogen, C1-C7 alkoxy, C1-C7 alkylsuphonyl; R5 is hydrogen, halogen, C1-C7 alkyl, C1-C7 haloalkoxy, or aryloxy, or is -NR7R8, where R7 and R8 represent C1-C7 alkyls, or R7 and R8 together with the nitrogen atom to which they are bonded can form a 4-7-member heterocycloalkyl group, which can be substituted with one or more substitutes selected from a group consisting of halogen, C1-C7 alkyl, C1-C7 alkoxy, hydroxyl, phenyl and di(C1-C7)alkylamino; R6 is hydrogen or together with R5 can form a 5- or 6-member heterocycloalkyl group which can be substituted with one or more halogens; and their pharmaceutically acceptable salts of acid compound, except the range of compounds given in paragraph 1 of the formula of invention. The invention also relates to medicine based on said compounds, with activity of allosteric enhancer of GABA-B receptors and use of compounds of the formula to prepare medicines used in treating central nervous system disorders, including anxiety and depression. |
Pharmaceutical composition based on ladasten / 2376986 Invention relates to field of medicine, in particular to pharmaceutics, and concerns pharmaceutical compositions, which contain as active substance therapeutically effective quantity of ladasten, and as target additives - starch, stearic acid and/or its salt or ludipress and stearic acid and/or its salt with definite ratio of said components. Composition is made in form of pills, contains optimal quantity of target additives, which allows to obtain easy swallowed pills. Pills meet all requirements of State Pharmacopoeia XI edition. |
Substituted 3,5-diamino-4-sulfonyl-pyrazoles and 2-amino-3-sulfonyl-pyrazolo-[1,5-a]pyrimidines-antagonists of serotonin 5-ht6 receptors, methods for their production and use / 2376291 Invention is related to antagonists of serotonin 5-HT6 receptors of common formula 1 and their pharmaceutically acceptable salts and/or hydrates, pharmaceutical compositions, dosage forms and methods of production. Invention also includes new compounds of formula 1.1. In formulae 1 and 1.1 , Ar represents aryl, selected from unnecessarily substituted phenyl or unnecessarily substituted 5-6-member heteroaryl, which contains atom of nitrogen or atom of sulfur and heteroatom; R1 represents atom of hydrogen, unnecessarily substituted C1-C5 alkyl; Ar represents aryl, selected from unnecessarily substituted phenyl or unnecessarily substituted 5-6-member heteroaryl, which contains atom of nitrogen or atom of sulfur as heteroatom; R1 represents atom of hydrogen, which is unnecessarily substituted C1-C5 alkyl; R2 1,R2 2, R3 1, R3 2 independently from each other represent atom of hydrogen or substituent of aminogroup, selected from unnecessarily substituted C1-C4 alkyl, unnecessarily substituted phenyl, or R3 1 and R3 2 together with atom of nitrogen, to which they are bound, create unnecessarily substituted saturated 6-member heterocycle, possibly containing atom of nitrogen in cycle; or R1 together with atom of nitrogen, to which it is bound, and R2 1 and R2 2 together with atom of nitrogen, to which they are bound, create substituted pyrimidine cycle. In formula 1.1 R4, R5 and R6 independently from each other represent atom of hydrogen, unnecessarily substituted C1-C3 alkyl or phenyl. |
Benzimidazole derivatives, compositions containing said derivatives, production and use thereof / 2374234 Present invention relates to a compound of formula: which is N-{2-tert-butyl-1-[(4,4-diflurocyclohexyl)methyl]-1H-benzimidazol-5-yl}ethanesulfonamide and its pharmaceutically acceptable salt, their diastereomers, enantiomers or their mixture. The invention also relates to use of this compound in making a medicinal agent with modulator activity of CB1 receptors; to a pharmaceutical composition based on this compound; to a method of modulating CB1 receptors, based on use of effective quantities of this compound, as well as to a method of producing the compound described above. |
Gindarine composition / 2372912 Invention refers to chemical-pharmaceutical industry and medicine, namely to an oral gindarine tranquiliser. There is offered composition for capsule containing as an active substance, gindarine in the form of gindarine hydrochloride, and an adjuvant chemically inert to the active substance and physiologically acceptable or number of adjuvants enabling prolonged release of gindarine hydrochloride. The composition represents granules, or mixed powders, or mixed granules and powder, or liquid, or soft form. As adjuvants, the composition contains an excipient, alone or combined with a disintegrant, or an antifriction substance, or a binding substance, or mixture thereof. The composition representing the liquid form - suspension, or the soft form - gel, as adjuvant contains a liquid base, alone or mixed with a thickener or a preservative, or mixture thereof. |
Method of obtaining pharmaceutical composition for oral introduction possessing improved bioaccessibility of biologically active effective medicinal substance, and pharmaceutical composition obtained by said method / 2370268 Method of obtaining tablets containing crystalline-form-free alprazolam, includes at preliminary stage of granulation operation obtaining alprazolam solution in pharmacologically acceptable solvent together with crystallisation-inhibiting agent, formed by mixture of binding substance and from 20 to 60% wt of total amount of lubricating substance, impregnation with obtained solution of mixture of diluent and 25% reticular carboxymethylcellulose as disintegrating agent until homogeneous granulated mass is obtained and grinding of obtained granulated mass, preliminarily dried, until grinded granulometrically homogeneous mass is obtained. At the second stage of granulation operation, 100% of remaining lubricating agent and remaining reticular carboxymethylcellulose and aromatising additives are added to dried and grinded mass, obtained at preliminary stage of granulation operation; aromatised mass is finally mixed and pressed. Non-crystalline state of alprazolam improves its solvability and bioaccessibility. |
Imidazole iii derivatives / 2360911 In general formula I R1 stands for haloid, lower alkyl; R2 stands for lower alkyl or C3-C6-cycloalkyl; R3 stands for lower alkyl, C3-C6-cycloalkyl, -(CH2)n-C3-C6-cycloalkyl, (CH2)n-CN or -(CH2)n-O-(lower)alkyl, (lower)alkoxyaryl, Fn-R5, where R5 is lower alkyl or lower alkenyl; n takes values 1, 2 or 3; R4 is hydrogen or CH2R5, where R5 is hydrogen, C1-C6-alkyl, C3-C12-cycloalkyl; as well as its pharmaceutically acceptable salts. Invention also relates to methods of obtaining formula I compounds, medication based on formula I compound and its application. |
Oral gindarine medicine and production method / 2360675 Invention refers to chemical-pharmaceutical industry and medicine, namely to oral gindarine medicine characterised as a tranquilizer. Said medicine contains gindarine hydrochloride as an active material and auxiliary components and represents a solid gelatinous capsule. Gindarine is included as a compound of the mass filling capsules as mixed powders of gindarine and auxiliary components or as a granulated material. As the auxiliary components, the medicine contains bulking agent either alone, or combined with a disintegrant or antifriction material or with their mixture. There is also provided method of production of specified oral medicine. |
Method for prophylactics of mycotoxicosis in farm animals and birds / 2391975 Invention relates to livestock farming. Method includes addition of betaine into mixed fodders contaminated with mycotoxins at the level of 0.18% of fodder weight. |
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