RussianPatents.com
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Agent showing serotonin 5-ht3-receptor antagonist properties. RU patent 2438669. |
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FIELD: medicine, pharmaceutics. SUBSTANCE: what is offered is a biologically active substance showing 5-HT3-serotonin receptor antagonist properties, 1-piperidinopropyl-2-(4-fluorophenyl)imidazo[1,2-a]benzimidazole of formula I. The compound has been known as a local anaesthetic. There are shown evident 5-HT3-antagonist properties of the compound in the macromolar concentration equal to the reference preparation ondansetron with the compound of formula I being safer. EFFECT: new properties of the compound can be used for creating the effective agents exhibiting antiemetic, anxiolytic and analgesic activities. 2 cl, 2 tbl
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Method of pharmacological correction of ischemic tissues survival rate in reduced blood circulation environment / 2438190 For tissue ischemia correction, in the reduced blood circulation environment an isolated pedicle skin flap is simulated in a laboratory animal. On the first, third and fifth experimental days, recombinant erythropoietin 50 IU/kg is injected subcutaneously. |
Dihydropyrazolopyrimidinone derivatives / 2437885 Invention describes a compound of general formula where A1 is selected from the following formula R1c denotes a hydrogen atom, a lower alkenyl group or a -Q3-A3(R1d)R1e group; A3 denotes a methane or lower alkyl group; Q3 denotes a single bond; R1d and R1e independently denote a hydrogen atom, hydroxyl group, lower alkyl group or hydroxyl-containing lower alkyl group, or together form a lower alkylene group in which one or two or more methylene groups constituting the lower alkylene group can be independently substituted with an oxygen atom; R1 denotes a lower alkenyl group or a lower alkynyl group; R2 denotes a phenyl, pyridyl or thienyl group, which can contain a -Q4-A4(R1g)R1h group; A4 denotes a nitrogen atom, a lower alkyl group optionally substituted with a hydroxy-lower alkyl group, or a methane group optionally substituted with a halogen atom, a hydroxyl group, a lower alkyl group or a hydroxy-lower alkyl group; Q denotes a single bond or a lower alkylene group in which one or two or more methylene groups constituting the lower alkylene group can be independently substituted with an oxygen atom; R1g and R1h independently denote a hydrogen atom, a lower alkyl group or a lower alkylsulphonyl group; R5 and R6 independently denote a hydrogen atom, a lower alkyl group or a hydroxyl-containing lower alkyl group, or a pharmaceutically acceptable salt thereof. The invention also describes a pharmaceutical composition based on compounds of formula I, having anti-cancer activity, an anticancer agent, a codrug, as well as an exposure sensitising agent containing the pharmaceutical composition. |
Method of obtaining medication, possessing adaptogenic activity / 2437674 Invention relates to pharmaceutic industry, in particular to method of obtaining medication, possessing adaptogenic activity. Method obtaining medication, possessing adaptogenic activity, by extraction of milled natural raw material, which contains seeds of elettaria, rhizome of elecampane, rhizome of Zingiber oficinale, wood of Caragana jubata with 40% ethanol at room temperature with the following filtration, under defined conditions. |
Method of reducing level of increased vomiting reflex at dental appointment / 2437670 Invention relates to medicine, namely to dentistry, and namely to method of reducing increased vomiting reflex level of patient at dental appointment. Method of reducing increased vomiting reflex level of patient at dentist appointment, consists in the fact, that immediately before carrying out therapeutic manipulations, patient during 2-3 minutes rinses oral cavity with 20% alcohol tincture (1:10), obtained from collection of medicinal plants, taken in the following weight fractions: rhizome with roots of Rhaponticum carthamoides -2, rhizome of erect cinquefoil - 1, leaves of peppermint - 1. |
Application of alpha-1-antitrypsin for preparing drug for treating chronic fatigue syndrome / 2436590 Application of alpha-1-antitrypsin (AAT) for preparing a drug for treating chronic fatigue syndrome (CFS) is offered. It is shown: AAT inhibited intracellular elastase activity of mononuclear cells of peripheral blood of the CFS patients, prevented degradation RNAase L 83 kDa with formation of the overactive RNAase L 37 kDa form. After treating with the preparation AAT, elastase activity in the specified blood cells decreased from approximately 1459 U/mg to 134 U/mg; the patient showed obvious clinical improvements, decreased cognitive disorders cognitive infringements, has went back to work. Particularly, the invention refers to the application of plasma or other therapeutic forms containing alpha-1-antitrypsin sufficient for produce a dosage of alpha-1-antitrypsin equal to 6 mg or more per one kg of body weight with frequency 1 to 31 days. |
Compositions containing polyunsaturated fatty acids (pufa), and methods of application thereof / 2436571 Invention refers to medicine, namely to neurology, and can be used for increasing a level of synaptic proteins in a nerve cell or a brain cell in a subject. That is ensured by introduction a combination of agents to the specified subject, namely omega-3 fatty acid and/or omega-6 fatty acid in a combination with uridine or choline salts. |
Pleurotus 1137 preparation for drug hypersensitivity correction in integrated therapy of pulmonary tuberculosis / 2435600 Invention refers to pharmaceutical industry, particularly to a preparation for drug hypersensitivity correction in integrated therapy of pulmonary tuberculosis. Application of biologically active substances with antimicrobial activity recovered from Pleurotus 1137 fungus mycelium (Russian National Collection of Industrial Microorganisms, F-819), as a preparation for drug hypersensitivity correction in integrated therapy of pulmonary tuberculosis. |
Preparation-4-hydroxy-17r-methylincisterol affecting tissue exchange and application of pleurotus 1137 fungus strain for making it / 2435599 Invention refers to medicine and biotechnology and concerns a preparation of 4-hydroxy - 17R - methylincisterol affecting tissue exchange and exhibiting anticancer and hypolipidemic activities and a producer of a biologically active substance of sterol 4-hydroxy - 17R - methylincisterol derivative. Substance of the invention involves submerged Pleurotus ostreatus 1137 (Russian National Collection of Industrial Microorganisms, F-819) fungus cultivation followed by mycelium separation from a culture fluid and recovery from the mycelium by extraction in ethanol at acid value pH of a medium of low-molecular 100 to 500 Da biologically active substances and recovery of sterol 4-hydroxy - 17R - methylincisterol derivative with preset molecular weight, gross formula and structural formula by dichloromethane. The invention also concerns application of Pleurotus ostreatus 1137 (Russian National Collection of Industrial Microorganisms, F-819) strain as a producer of the biologically active substance of sterol 4 - hydroxy - 17R - methylincisterol derivative. |
Preparation potentiating radiation therapy / 2435587 Invention relates to potentiating preparation for radiation therapy, which as effective component contains uracyl derivative, represented by formula (1) where R1 represents halogen atom or cyanogroup; and R2 represents (4-8)-member heterocyclic group, which has from 1 to 3 nitrogen atoms and optinally has as substituent C1-C4 alkyl group, iminogroup, hydroxyl group, hydroxymethyl group, methansulphonyloxy group or aminogroup; amidinothiogroup, in which hydrogen atom, bound to nitrogen atom, can be substituted by C1-C4 alkyl group; guanidinogroup, in which hydrogen atom, bound to nitrogen atom, can be substituted by C1-C4 alkyl group or cyanogroup; C1-C4 alkylamidinogroup; or 1-pyrrolidinylmethyl group or its pharmaceutically acceptable salt. Invention also relates to method of radiation therapy potentiation, and to method of cancer treatment, which include introduction of described above uracyl derivative of formula (1) to patient who needs it. |
Method of selecting tactics of treatment of acute inflammatory diseases of orbit / 2435555 Invention relates to medicine, namely to ophthalmology, ophthalmic surgery, physiotherapy. In case of localization of inflammatory focus in orbit without involvement into the process of paraorbital areas hospitalisation of patient into ophthalmology department of hospital is carried out. Orbitotomy in one or more quadrants is performed. Traditional intensive therapy is carried out. In case of intraorbital complications second stage of treatment is carried out. 1% solution of nicotinic acid is introduced intravenously in dose 2 ml on the first day, with daily 0.5-1.0 ml increase on the following days until maximal therapeutic efficiency is achieved, after that, successively dose is daily reduced by 0.5-1.0 ml to initial dose. Additionally after each injection of nicotinic acid, intravenous drip infusion of 2% pentoxifylline 5 ml on physiological solution in dose 100-200 ml is carried out during 7-15 days. Parabulbarly dexason 0.4% in dose 0.5 ml is introduced. Intramuscularly introduced are lidase in dose 64 U, actovegin in dose 2 ml and proserin 0.05% in dose 1 ml daily during 10 days. Electrophoresis with 0.05% proserin is carried out alternately with 0.5% hydrocortosone emulsion endonasally in case of optic nerve neuritis and bath method - in case of affection of eye-moving muscles with course of 10-15 procedures. If inflammatory process spreads into orbit from anatomically adjacent regions hospitalisation into otolaryngology department or into department of maxillofacial surgery, or neurosurgery or septic department of hospital is carried out. Sanitation of primary focuses of purulent infection is carried out. Traditional intensive therapy, which includes antibacterial, detoxication, desensibilising, immunologic and vitamin therapy, is performed. In case of intraorbital complications second stage of treatment is carried out in ophthalmology department of hospital. |
Medication possessing antidepressive, anxiolytic and nootropic action / 2437659 Invention relates to pharmaceutical industry and medicine. Claimed is application of N-carbamoyl-4-(n-methoxyphenyl)-2-pyrrolidone of structural formula as means possessing antidepressive, anxiolytic and nootropic action. This low-toxic compound (LD50 2263.88 mg/kg) possesses high antidepressive, anxiolytic and nootropic activity, affect of which is not accompanied by hypnosedative phenomena, or reduction of mental and physical work ability. |
Thiophenyl and pyrrolyl azepines as serotonin 5ht2c receptor ligands and use thereof / 2434872 Invention relates to compounds of formula , where X denotes S; R1 and R2 taken together with atoms to which they are bonded form a 5-member carbocycle, substituted with up to two substitutes selected from alkyl and CF3; R3 is selected from a group consisting of a hydrogen atom and C1-8-alkyl; R3a denotes a hydrogen atom; R4 denotes a hydrogen atom; R4a denotes a hydrogen atom; R5 denotes a hydrogen atom; R5a denotes a hydrogen atom; R6 denotes a hydrogen atom; R6a denotes a hydrogen atom; R7 denotes a hydrogen atom; or pharmaceutically acceptable salts thereof. The invention also relates to compounds of the given formula, compounds selected from the group, as well as a pharmaceutical composition. |
Crystalline beta-modification of 7-bromo-1,3-dihydro-5-(2-chlorophenyl)-2h-1,4-benzodiazepin-2-one and synthesis method thereof / 2430094 Described is a novel crystalline β-modification of 7-bromo-1,3-dihydro-5-(2-chlorophenyl)-2H-1,4-benzodiazepin-2-one (phenazepam) and synthesis method thereof, which can be used in pharmaceutical industry and medicine as a tranquilliser. Said novel crystalline β-modification of 7-bromo-1,3-dihydro-5-(2-chlorophenyl)-2H-1,4-benzodiazepin-2-one is characterised by certain interplanar spacing (A0) and corresponding intensity and parameters of the crystal lattice, given in the claims. |
S-adenosylmethionine compositions for peroral application / 2427376 Claimed are dietary and/or nutriceutic pharmaceutical composition for peroral application which contains S-adenosylmethi-onine-para-toluolsulfonate (SAMe) in combination with inositol and/or ino-sitol-1-phosphate and pharmaceutically acceptable excipients, in which at least one of and pharmaceutically acceptable excipients represents magnesium oxide in concentration from approximately 1.0 to approximately 10.0% of composition weight (versions), method of its obtaining, method of stabilisation of hard food and/or nutriceutic pharmaceutical composition based on SAMe-para-toluolsulfonate by application of inositol and/or inositol-1-phosphate, application of SAMe-para-toluolsulfonate in combination with inositol and/or inositol-1-phosphate for obtaining composition for treatment of depressive states and panic syndromes. |
Alkyl sulphonamide quinolines with affinity to nk-3 receptors / 2421447 Compound is ((S)-1-phenyl-propyl)-amide 3-(methane sulphonyl amino)-2-phenyl- quinoline-4-carboxylic acid, stereoisomer, enantiomer or pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition based on the disclosed compound. |
Polymorphic modification in n-{5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-2-fluoro-phenyl}-n-methyl-acetamide (versions), containing it pharmaceutical composition (versions), medication, method of obtaining said polymorphic modification (versions) and method of treatment and/or prevention of nervous disorders / 2413729 Claimed invention describes novel polymorphic modification N-{5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-2-fluoro-phenyl}-N-methyl-acetamide, methods of its obtaining, its application as medication, its application for preparation of medication and pharmaceutical compositions, including novel polymorphic modification. |
Anti-vomit nk-1 antagonist metabolites / 2404969 Invention relates to compounds of general formula (I) , where R is methyl and R1 is 4-methyl-oxy-piperazin-1-yl; or R is CH2OH and R1 is 4-methyl-piperzin-1-yl or 4-methyl-4-oxy-piperazin-1-yl; and to pharmaceutically acceptable acid addition salts thereof, as well as to a medicinal agent based on said compounds, having NK-1 receptor antagonist activity and to use of said compounds in treating NK-1 receptor associated diseases. |
Substituted 8-sulphonyl-2,3,4,5-tetrahydro-1h-gamma-carbolines, ligands, pharmaceutical composition, synthesis method and use thereof / 2404180 Invention relates to novel substituted 8-sulphonyl-2,3,4,5-tetrahydro-1H-γ-carbolines of general formula 1 or pharmaceutically acceptable salts thereof, which are ligands with a wider range of simultaneous activity towards alpha adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors, sigma receptors, norepiniphrine receptors and serotonin receptors. In compounds of general formula 1 R1 is an amino group substitute selected from hydrogen; C1-C3alkyl optionally substituted with phenyl; C1-C4alkyloxycarbonyl; R2 is a cyclic system substitute selected from hydrogen, C1-C3alkyl optionally substituted with phenyl, pyridin-(3- or 4-yl), (6-methylpyridin-3-yl); C1-C3alkenyl substituted with phenyl; or optionally substituted phenylsulphonyl; R3 is an optionally halogen-substituted phenyl, six member aromatic azaheterocycle, mono- or di-C1-C3alkylamino group, phenylamino group which is optionally substituted with halogen atoms on the phenyl ring, or a substituted six member azaheterocycle containing an additional nitrogen atom, substituted with C1-C3alkyl. |
Diarylmetyhylpyperazine derivatives, their obtaining and application / 2404172 There are described compound of formula, its pharmaceutically acceptable salt or their mixture, enentiomerically pure 4-{(R)-(3-aminophenyl)[4-(4-fluorobenzyl)pyperazin-1-yl]-N,N-diethylbenzamide or its pharmaceutically acceptable salt. Also described are method of anxiety therapy, method of pain therapy and method of depression therapy in animal. |
Substituted 4-phenyltetrahydroisoquinolines, preparation method, application as medicinal agents, and also medicinal agents containing them / 2398766 Invention refers to new compounds of formula I , where: R1, R2, R3 and R4 independently from each other mean hydrogen, F, CI, Br, I; R5 designates hydrogen, alkyl with 1, 2, 3, 4, 5 or 6 C atoms, or cycloalkyl with 3, 4, 5 or 6 C atoms; R6 designates hydrogen; R7 and R8 independently from each other mean hydrogen, W means CrH2r or CsH2S-2; and one or more CH2-groups in C2H2r and CsH2s-2 can be substituted with NR17, oxygen or S; R17 means hydrogen, alkyl with 1, 2, 3 or 4 C atoms; r means 1, 2, 3, 4, 5 or 6; s means 2, 3 or 4; X designates-with C(O)- or -S(O)2-; Z means -C(O)- or a bond; and also to their pharmaceutically acceptable salts and trifluoroacetates. The invention also concerns application of the compounds of formula I, and also to a pharmaceutical composition. |
Method of preventing post-operation nausea and vomiting in children in otolaryngological surgery / 2426541 Invention relates to field of medicine, and can be used for prevention of post-operation nausea and vomiting in children in otolayngologic (ENT) surgery. Premedication is performed. Dexametazone is introduced in dose 0.2 mg/kg i/v, 8 mg maximum. Propofol is introduced in dose 2-3 mg/kg i/v, fentanyl 4-5 mcg/kg i/v with anesthesia induction. Anesthesia is performed with nitrous oxide - oxygen mixture N2O+O2 with ratio 2:1. Propofol 2.5-3.5 mg/kg/hour i/v, fentanyl 3-4 mcg/kg/hour in micro-jet manner in basis-anesthesia. When operation is over, metoclopromide is introduced in dose 0.2 mg/kg i/v not more than 10 mg. After extubation oxygenation with oxygen through facial mask in dose 3-4 l/min is carried out for 3-5 minutes. |
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