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Agent possessing antiarrhythmic and hepatoprotective properties. RU patent 2469720. |
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FIELD: medicine. SUBSTANCE: invention refers to the use of 9-(2-diethylaminomethyl)-2-(3,4-dioxyphenyl)imidazo[1,2-a]benzimidazole dihydrobromide of formula I: as an agent possessing antiarrhythmic and hepatoprotective properties. The invention also refers to the use of 9-(2-diethylaminomethyl)-2-(3,4-dioxyphenyl)imidazo[1,2-a]benzimidazole dihydrobromide for preparing pharmaceutical compositions. EFFECT: higher antiarrhythmic and hepatoprotective activity. 2 cl, 11 tbl, 4 ex
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Method for detection of genetic predisposition to developing myocarial infarction in individuals with no clinical implications of ischemic heart disease / 2469096 Invention refers to a method for detection of genetic predisposition in an individual with no clinical implications of ischemic heart disease (IHD) to developing myocardial infarction (MI). The invention may be used in cardiology for detection of genetic predisposition to developing myocardial infarction (MI). A combination of two pathogenetically MI-related polymorphisms representing single nucleotide substitutes C1019T in connexin-37 (Cx37) gene and G894T in endothelial NO-CHHTa3bi.(eNOS) gene are examined. A high degree of risk of developing MI in an individual being examined is stated by a combination of homozygous genotype TT in C1019T polymorphism of Cx37 gene and homozygous genotype GG in G894T polymorphism of eNOS gene. |
Substituted dihydropyrazolones for treating cardiovascular and haematologic diseases / 2469031 Present invention relates to dihydropyrazolone derivatives or of formula (I), where R1 denotes a heteroaryl group of formulae given below, where * denotes the linkage point with the dihydropyrazolone ring, A in each individual occurrence denotes C-R4 or N, wherein at most two ring members A represent N at the same time, E denotes O or S, R2, R3 and R4 are as defined in the claim. The invention also relates to a method of producing said compounds. |
Substance showing combined antiagregant, anticoagulant and vasodilator activities, n,n'-substituted piperazines and method for preparing them (versions) / 2469029 Invention refers to medicine, namely new organic compounds, namely N,N'-substituted piperazines of general formula (I), wherein R1, R2: linear or branched alkoxy (C1÷C4), CH3C(=O)O; n=1-5; m=0-3; Z: C=O, SO2; X:C(=NH)NH2, C(=NH)NHC(-NH)NH2, G is low-molecular organic or mineral acid, sodium, potassium, ammonium cations or water influences the haemostasis system, showing antiagregant, anticoagulant and vasodilator properties, and to a method for preparing N,N'-substituted piperazines of formula 1 by reaction of N-substituted piperazines of general formula wherein R1, R2; linear or branched alkoxy (C1÷C4), CH3C(=O)O; n=1-5; m=0-3; Z: C=O, SO2; and 1H-pyrazole-1-carboxamidine, dicyane diamide and their salts in organic solvents or water at temperature 10-50°C in the presence of bases. |
Substance showing combined antiagregant, anticoagulant and vasodilator activities, n,n'-substituted piperazines and method for preparing them (versions) / 2469029 Invention refers to medicine, namely new organic compounds, namely N,N'-substituted piperazines of general formula (I), wherein R1, R2: linear or branched alkoxy (C1÷C4), CH3C(=O)O; n=1-5; m=0-3; Z: C=O, SO2; X:C(=NH)NH2, C(=NH)NHC(-NH)NH2, G is low-molecular organic or mineral acid, sodium, potassium, ammonium cations or water influences the haemostasis system, showing antiagregant, anticoagulant and vasodilator properties, and to a method for preparing N,N'-substituted piperazines of formula 1 by reaction of N-substituted piperazines of general formula wherein R1, R2; linear or branched alkoxy (C1÷C4), CH3C(=O)O; n=1-5; m=0-3; Z: C=O, SO2; and 1H-pyrazole-1-carboxamidine, dicyane diamide and their salts in organic solvents or water at temperature 10-50°C in the presence of bases. |
Medication for prevention and treatment of atheroslerosis / 2468789 Invention relates to chemical-pharmaceutical industry, medicine, pharmacology and represents medication for prevention and treatment of atherosclerotic lesion of blood vessels, as well as pre- and thrombotic states, which possesses hypolipidemic and anticoagulant and antithrombotic activity, and is made in dosed drug form in form of coated tablets, consisting of core, which contains active substance and auxiliary substances, characterised by the fact that core contains substance of sulfated arabinogalactan potassium salt as active ingredient, and ludipress, aerosol and sodium stearate as auxiliary substances, components in medication being in definite ratio in wt %. |
Purinyl derivatives and use thereof as potassium channel modulators / 2468026 Present invention relates to novel purinyl derivatives of formula or , a stereoisomer thereof or a mixture of stereoisomers thereof, or a pharmaceutically acceptable salt thereof, where n equals 0, 1, 2 or 3; X is O, S or NR', where R' is hydrogen or methyl; Y is cycloalkyl, phenyl, benzo[1,3]dioxolyl or pyridyl, where the cycloalkyl, phenyl, benzo[1,3]dioxolyl and pyridyl are possibly substituted with one substitute selected from a group consisting of halogen, trifluoromethyl, cyano, nitro and amine; R1 is hydrogen, alkyl or alkoxy-alkyl; and Het is a pyrazolyl group which is substituted twice or more with substitutes selected from a group consisting of alkyl, hydroxy-alkyl, halogen, trifluoromethyl, alkoxy-carbonyl and phenyl. The invention also relates to pharmaceutical compositions which are useful for treating or relieving symptoms of diseases and disorders associated with activity of potassium channels. |
Condensed bicyclic compound / 2468017 Invention relates to condensed bicyclic compounds, having affinity with mineralocorticoid receptor (VR) of formula [I] and formula [ii], as well as to pharmaceutical compositions on their basis. In general formula [I[ and [ii] ring A represents benzene ring, which has substituent R1, condensed with adjacent 6-membered heterocyclic ring, and said benzene ring additionally optionally is substituted with one or two substituent(s), selected from halogen atom and C1-8-alkyl group, R1 represents C1-8-alkylsulfonyl amino group or C1-8-alkyl aminosulfonyl group, R2 and R3 (a) are similar or different and represent group, selected from hydrogen atom, C1-8-alkyl group, and from 6- to 10-membered monocyclic or bicyclic aryl group (said aryl group is optionally substituted with halogen atom), (b) are combined with each other with formation of oxogroup or (c) are combined with each other on their ends together with adjacent carbon atom with formation of C3-10-cycloalkyl group, X represents the following group =N-, =C(R4)- or -CH(R4)-, R4 represents hydrogen atom, cyanogroup, halogen atom, C1-6-alkyl group, C2-6-alkenyl group, C3-10-dicloalkyl group, C1-7-alkanoyl group, carbamoyl group or C3-8cycloalkenyl group, Ar represents from 6- to 10-membered monocyclic or bicyclic aryl group, optionally containing one or several heteroatom(s), selected from sulphur atom, oxygen atom and nitrogen atom (said aryl group is optionally substituted with similar or different, one or two substituent(s), selected from halogen atom, cyanogroup, C1-8-alkyl group, trihalogen- C1-8-alkyl group and C1-8alkoxygroup), and dotted line represents presence or absence of double bond, Xa represents the following group =N- or =C(CN)-, RZ represents hydrogen atom or halogen atom, R25 and R35 represent alkyl group, and Ar3 represents phenyl group, optionally substituted with one or two group(s), which is(are) selected from halogen atom and trihalogenalkyl group. |
Cycloalkylamine-substituted isoquinoline and isoquinolinone derivatives / 2468011 Present invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of formula or stereoisomer and/or tautomer forms thereof, and/or pharmaceutically acceptable salts thereof, where R1 is H or OH; R2 is R', (C7-C8)alkyl, (C1-C6)alkylene-R', (C2-C6)alkenyl; or R2 is (C1-C6)alkyl, under the condition that in said alkyl residue, at least one hydrogen is substituted with OH or OCH3; or R2 is (C1-C6)alkylene, bonded with cycloalkylamine, where (C1-C4)alkylene forms a second bond with another carbon atom of the cycloalkylamine ring and, together with carbon atoms of the cycloalkyalmine, forms a second 5-8-member ring; R3, R5 and R8 denote H; R4 is H, (C1-C6)alkyl or (C1-C6)alkylene-R'; R6 and R6' independently denote H, (C1-C8)alkyl, (C1-C6)alkylene-R' or C(O)O-(C1-C6)alkyl; R7 is H, halogen or (C1-C6)alkyl; n equals 1; m equals 3 or 5; r equals 0 or 1 and L is O(CH2)p, where p=0; where R' is (C3-C8)cycloalkyl, (C6)aryl; where in residues R2-R8 (C6)aryl is unsubstituted or substituted with one or more suitable groups independently selected from halogen, (C1-C6)alkyl, O-(C1-C6)alkyl, where the alkyl group can be substituted with 1-3 halogen atoms. The invention also relates to use of the compound of formula (I) and a medicinal agent based on the compound of formula (I). |
Cycloalkylamine-substituted isoquinoline and isoquinolinone derivatives / 2468011 Present invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of formula or stereoisomer and/or tautomer forms thereof, and/or pharmaceutically acceptable salts thereof, where R1 is H or OH; R2 is R', (C7-C8)alkyl, (C1-C6)alkylene-R', (C2-C6)alkenyl; or R2 is (C1-C6)alkyl, under the condition that in said alkyl residue, at least one hydrogen is substituted with OH or OCH3; or R2 is (C1-C6)alkylene, bonded with cycloalkylamine, where (C1-C4)alkylene forms a second bond with another carbon atom of the cycloalkylamine ring and, together with carbon atoms of the cycloalkyalmine, forms a second 5-8-member ring; R3, R5 and R8 denote H; R4 is H, (C1-C6)alkyl or (C1-C6)alkylene-R'; R6 and R6' independently denote H, (C1-C8)alkyl, (C1-C6)alkylene-R' or C(O)O-(C1-C6)alkyl; R7 is H, halogen or (C1-C6)alkyl; n equals 1; m equals 3 or 5; r equals 0 or 1 and L is O(CH2)p, where p=0; where R' is (C3-C8)cycloalkyl, (C6)aryl; where in residues R2-R8 (C6)aryl is unsubstituted or substituted with one or more suitable groups independently selected from halogen, (C1-C6)alkyl, O-(C1-C6)alkyl, where the alkyl group can be substituted with 1-3 halogen atoms. The invention also relates to use of the compound of formula (I) and a medicinal agent based on the compound of formula (I). |
1-substituted tetrahydroisoquinoline derivative, based on them pharmaceutical composition and methods of their application / 2468010 Claimed invention relates to specific compounds of 1-substituted 3,4-tetrahydroisoquinoline derivative. Invention also relates to pharmaceutical composition based on claimed compounds, to blocker of N-type Ca2+- channel based on claimed compounds, to application of claimed compounds, as well as to method of prevention or treatment of some pathologic conditions. |
Use of polydatine for treating hepatic diseases and polydatine pharmaceutical composition / 2468803 There are presented the use of polydatine for treating toxic (including drug-induced) and alcoholic hepatic diseases, as well as based oral compositions. What is shown is reduction of a degree of hepatocyte adipose degeneration in sub-acute alcoholisation, reduction of glycemia and lactate-acidosis. Polydactine promoted reduction of synthesis and accumulation of glycosaminoglycans. |
Method of preventing chronic toxic hepatopathy / 2468446 In order to prevent chronic toxic hepatopathy melaxen is introduced to animals in experiment one time per day in dose 10 mg/ml through probe into stomach. Simultaneously intragastric introduction of cobalt chloride solution in dose 2 mg/kg, in terms of metal, is performed daily, to create cobalt intoxication in organism. |
Method for preparing agent showing cholagogue action / 2465000 Invention refers to pharmaceutical industry, specifically to an agent showing cholagogue action. A method for preparing the agent showing cholagogue action consisting in the fact that ground sandy everlasting blossom, nosebleed herb and peppermint leaves are mixed with coriander fruit, extracted in 40% ethanol by multistage counterflow extraction, settled, filtered, condensed under certain conditions. |
Quinazoline derivative and pharmaceutical preparation / 2464263 Invention relates to a quinazoline derivative of general formula [1], or a pharmaceutically acceptable salt thereof [1], where R1-R6 assume values given claim 1, except compounds in which R5 is hydrogen and R6 is -NH2. The invention also relates to a pharmaceutical composition having the activity of an antipruritic agent, containing as an active ingredient said quinazoline derivative or pharmaceutically acceptable salt thereof. |
Agent of saussurea ds plants possessing hepatoprotective action / 2464036 Invention refers to pharmaceutical industry, particularly to an agent possessing hepatoprotective activity and an ability to normalise the hepatic function. The use of a ground elevated part of Saussurea plants or an aqueous or aqueous-alcoholic or supercritical fluid extract of the elevated part of Saussurea plants as the agent possessing hepatoprotective activity and the ability to normalise the hepatic function. |
Use of modified cyclosporines / 2463071 Group of inventions refers to medicine, particularly the use of non-immunosuppressive cyclophilin-binding cyclosporine for preventing or treating transplantation-related cirrhosis wherein cyclosporine (I) binds to human recombinant cyclophilin with a binding constant (BR) making less than 0.7 wherein BR represents a common logarithm of IC50 cyclosporine to IC50 cyclosporine A relation in concurrent experiment when evaluating by ELISA procedure; and (II) has activity in lymphocyte assay in the mixed culture making no more than 5% as compared with cyclosporine A activity (cl. 1) of the patent claim. There are also disclosed a pharmaceutical composition and a pharmaceutical combination containing cyclosporine under cl. 1. |
Phospholipid nanoform for oral application (sachet) and method for preparing it (versions) / 2463057 Invention refers to medicine, pharmacology and concerns an oral granulated dosage form in sachets containing phospholipids in the form of particles of small (20-30 nm) diameter, glycyrrhizic acid and its salt (including sodium glycerrhizinate), as well as carbohydrate (including maltose) and excipients (granulation, anti-clotting and powder), as well as to a method for preparing it by mixing fat and water phases of herbal phospholipids and acceptable carbohydrate to prepare an emulsion, cooling to 50°C and passing through a microfluidiser for 4-5 cycles under pressure 2000 atm. |
Agent showing hepatoprotective action, and method for preparing it / 2462259 Invention refers to pharmaceutical industry, specifically to an agent showing hepatoprotective action. The agent showing hepatoprotective action of a herbal polyphenol extract of Amur maackia heartwood (Maxar) which represents an aqueous solution of Maxar in the molecular-capsulated form in the form of a water-soluble associated with a surfactant having a specific hydrophilic-lipophilic balance. A method for preparing the agent showing hepatoprotective action by Maxar homogenisation in the melt surfactant under certain conditions to produce the molecular-capsulated form of the end product. |
Method of treating patients with chronic liver diseases in stage of latency and degree i manifested stage of hepatic encephalopathy / 2462251 Invention refers to medicine and aims at treating the patients with chronic liver diseases (CLD) in the stage of latency and degree I manifested stage of hepatic encephalopathy. The preparation Essentiale forte N is used. It is combined with prescribing the preparation Mucofalk. The course is 28-30 days. |
Method of treating chronic viral hepatitis c / 2459629 Invention refers to medicine, namely hepatology and may be applicable in treating chronic viral hepatitis C. That is ensured by introducing short-lived interferon-alpha (IFN) and the nucleoside analogue Ribamidil in the patient with an initial average week dosage specified in the range of 10.5 to 21.0 mil. IU depending on the level of native patient's interferon-alpha. Interferon-alpha is introduced with at least twice gradually increase of the average week dose to 21.0 to 84 mil. IU. Over the whole period of introducing IFN, the patient is prescribed with additional antiviral preparations - an interferon inducer, as well as an amantadin preparation or a glycyrrhizic acid preparation. It is combined with a support therapy involving the introduction of T-cell immunity stimulators and preparations for correction of side effects. The presence of blood viral ribonucleic acid is occasionally controlled and the introduction of Ribamidil is started in a daily dose of 800-1200 mg from the third month from the beginning of treatment if observing the presence of ribonucleic acid or from the tenth month if observing the absence. The treatment is continued until at least a 12-month aviremia period is achieved. |
Compositions for activation of lipoprotein lipase containing benzene derivatives / 2466725 Invention refers to an agent for activation of lipoprotein lipase containing a benzene derivative of general formula (1) which is used for preventing and treating hyperlipidemia and obesity. The invention also refers to the benzene derivatives of general formula (1a). |
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