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Composition for injections based on crystalline β-modification of 7-brom-1,3-dihydro-5-(2-chlorphenyl)-2h-1,4-benzodiazepin-2-one exhibiting tranquilising action and method for preparing it. RU patent 2440120. |
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FIELD: medicine, pharmaceutics. SUBSTANCE: group of inventions relates to medicine, in particular to pharmacy. A composition for injections exhibiting tranquilising action contains the ingredients in the following proportions, wt %: crystalline β-modification of 7-brom-1,3-dihydro-5-(2-chlorphenyl)-2H-1,4-benzodiazepin-2-one - 0.05-0.15, polyvinylpyrrolidone - 0.50-1.20, "Tween-80" - 2.00-10.00, glycerine - 5.00-15.00, sodium pyrosulphite - 0.30-1.20, sodium hydrate solution - to pH 6.0-7.5, water - the rest. A method for preparing the composition consist in the fact that "Tween-80" and glycerine are mixed, heated to 70-90°C, and crystalline β-modification of 7-brom-1,3-dihydro-5-(2-chlorphenyl)-2H-1,4-benzodiazepin-2-one is dissolved. The prepared mixture is poured in the mixed aqueous solution of sodium pyrosulphite and polyvinylpyrrolidone heated to 40-90°C, cooled to room temperature, filtered, reduced to pH 6.0-7.5 with sodium hydrate solution, bottled and sterilised. EFFECT: presented group of inventions provide a composition exhibiting improved anxiolytic action and decreased sedation in comparison with the composition based on pharmacopoeial phenazepam. 2 cl, 2 tbl, 4 ex
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Mglur5 modulators / 2439068 Described are novel compounds of general formula I: |
Agent showing serotonin 5-ht3-receptor antagonist properties / 2438669 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. |
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. |
Valganciclovir powder / 2440118 Declared invention refers to chemical-pharmaceutical industry, and concerns new solid pharmaceutical dosage forms of valganciclovir hydrochloride for oral administration after reduced in water. These new pharmaceutical dosage forms are applicable for treating or controlling viruses, such as herpes virus or cytomegalovirus. |
Drug stimulating production of granulocyte-macrophage colony-forming factor in cells of mononuclear phagocyte system / 2438676 Invention refers to medicine, particularly immunology, namely immunocorrection drugs, and can be used as an inducer of a granulocyte-macrophage colony-forming factor in cells of a mononuclear phagocyte system in vitro and for efferent therapy in pathological conditions accompanied by decrease in cell-mediated immunity. The drug represents oxidised dextrane of average molecular weight 35 - 65 kDa. The drug can be presented in the form of a solution or a nanoliposomal emulsion of the concentration of oxidised dextrane 1-5 wt %. The drug is applied by introduction in a cell culture of the mononuclear phagocyte system in an amount containing oxidised dextrane 125-250 mcg per culture medium 1 ml. |
Prolonged release injection solvent for preparing agents used in treating oncological gynaecopathies / 2438653 Invention refers to chemical-pharmaceutical industry and medicine, and concerns a composition of solvent ingredients for producing an injection solution, it can be used for preparing injection dosage forms for treating oncological gynaecopathies. The offered agent contains water for injections, low-molecular polyethylene, emulsifier T-2, lutrol F-127, Cremophor RH-40, oil olive in the following proportions, wt %: waters for injections - 1.841; LMPE - 67.114; emulsifier T-2 - 16.778; Lutrol F-127 - 1.677; Cremophor RH-40 - 2.520; oil olive-10.070. |
Drug for human papilloma virus associated diseases of uterine neck, presented in form of solution for vaginal irrigations, kit and method for preparing / 2438652 Invention refers to medicine and pharmaceutical industry, namely to gynaecology and can find application for treating the pre-cancer diseases of uterine neck. A drug presented in the form of a solution for vaginal irrigations, characterised by the fact that it contains a recombinant composition of proteins E7 of HPV type 16 and 18 types linked to an amino acid sequence of heat-shock proteins of m. w. 70 kDa from M. tuberculosis in the form of a lyophilised powder, chitosan of a degree of acetylation 86%, a preserving agent, carboxymethyl cellulose sodium salt of molecular weight 250000, a foaming agent selected from glycyrrhizic acid and its pharmaceutically acceptable salts, purified water. Also, there is offered a kit and method for preparing it. |
Method of local prolonged chemical-therapeutic treatment of locally spread unresectable glandular cancer of pelvis minor organs / 2437660 Claimed invention relates to field of medicine. Claimed is method of chemical-therapeutic treatment of locally spread unresectable glandular cancer of pelvis minor organs. Introduction of medication, containing 5-fluorouracil, metronidazole water for injections, low molecular polyethylene, emulsifier T-2, olive oil, lutrol F127 and cremofor RH40 is performed in dose 1 ml into cellular spaces, surrounding organ, ligaments and under serous membrane of organs in area of cancer tumour. Single introduction must not exceed 5.0 g of chemical preparation. |
Pharmaceutic composition, possessing antibacterial, antiviral and antifungal action / 2437647 Invention relates to pharmaceutical industry, namely to medications, intended for antiseptic processing and disinfection of wounds, burned surfaces, skin cracks, injured mucous membranes and insect bites. Composition contains active substances with specified quantitative component ratio, as such chlorhexidine gluconate and benzoxonium chloride, solvent and shape-forming agent - purified water - are used. |
Dalargin-containing intranasal composition and its application for treating diseases / 2436588 There are offered a dalargin-containing intranasal composition suspended or dissolved in a liquid propellant, containing stabilising and suspending agents and/or cosolvents, and its application for treating the diseases (particularly, gastric ulcer, duodenal ulcer, pancreatitis, pancreatonecrosis). |
Oral composition containing 3-{5-[4-(cyclopentloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl}propionic acid or its salt / 2436576 Oral composition contains 3-{5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl}propionic acid or its salt, polyvinylpyrrolidone and an alkaline compound, solution 5 % wt/vl of which has pH 10 or more. The preferential alkaline compound is L-arginine of potassium carbonate or sodium hydroxide. The oral composition can be presented in the form of a solid form or in the form of a water solution. |
Self-preserved water pharmaceutical compositions / 2436568 Invention relates to medicine, in particular to ophthalmology. Self-preserved compositions are preserved effectively by means of a balanced buffer system containing zinc ions in the concentration 0.04-0.9 mm, preferentially 0.04-0.4 mm. One aspect of the balanced buffer system is the limited amount of buffering anions to the concentration 15 mM or less, preferentially 5 mM or less. In one version, the compositions contain borate or one or more borate/polyol complexes. Application of propylene glycol as polyol in such complexes is especially preferential. The limited amount of the bivalent metals different from zinc, and the amount of the present ionised salts, is important to maximise antimicrobial activity of the balanced buffer systems. |
Compound for local anesthesia and treatment of inflammatory diseases of oral mucosa / 2435603 Invention refers to dentistry, and can be used for treatment of inflammatory damages of an oral mucosa, and for local anaesthesia in dental practice for instrument interventions in treating teeth and gums (stomatitis, gingivitis, etc.) The compound for local anaesthesia and treatment of inflammatory diseases of the oral mucosa contains lidocaine hydrochloride, glycerin, water, rhubarb extract, salicylic acid, ethanol, carbomer, sodium alginate, sodium saccharinate and triethanol amine in the following proportions, wt %. |
Method for metabolic syndrome correction in schizophrenic patients / 2432162 Invention refers to medicine, namely to psychiatry, and concerns treating metabolic syndrome in schizophrenic patients. That is ensured by integrated treatment including rhythmic motions for an hour 3 times a week throughout 6 months combined with introduction of neuroleptics. The second generation neuroleptics are replaced by first generation neuroleptics according to the developed scheme with considering prevailing semiology in a specific patient. |
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