The tool inactivation of coronaviruses
(57) Abstract:Proposed: a new tool inactivation of coronaviruses. A tool is a Miramistin (aka ministerocomunicazione chloride), formerly known as antiseptic, antifungal, antimicrobial action, is also effective against viruses, HIV, influenza and herpes). The invention expands the Arsenal of tools for a specified purpose and allows to treat and prevent caused by a coronavirus, respiratory disease (which also applies SARS) and gastroenteritis. 3 table. The invention relates to the field of medicine and pharmaceutical industries and can be used in the creation, production and application of therapeutic and preventive medicines.Known use as a means for inactivation of coronaviruses of lipid solvents, detergents, antiseptics (L. J. Sekstinska, A. Century of Rebadow // Coronaviruses human and animal. - M.: Medicine, 1977. -S. 221; public and private Virology /edited by C. M. Zhdanov, S. Y., Russian. - M.: Medicine, 1982, T. 2, S. 316-339; A. I. Korotyaev, S. A. Babichev // Medical Microbiology, Virology and immunology. - SPb.: Special literature, 1998. - S. 273).Proposed chloride, formerly known as prophylaxis traditional venereal diseases “Miramistin” (A. C. 1832496): syphilis, trichomoniasis, gonorrhea, and also used as an antiseptic eye (RF Patent 2164135) with purulent-inflammatory diseases of the cornea.The proposed solution allows you to expand the Arsenal of tools for the prevention and treatment of diseases caused by coronaviruses.The inactivating effect of the proposed drug is illustrated by the following examples (for the sake of simplicity, hereinafter used the name Miramistin).Example 1: Determination of minimum inhibitory concentrations (MICS) Miramistin in relation to the test culture of coronaviruses (fcov person OS) in vitro culture of kidney cells of a human embryo was carried out according to the following scheme:It was delivered in three series of experiments in four dilutions of the drug, and then calculated its IPC against coronaviruses. The results of the experiments are presented in table.1.As can be seen from the data presented in table.1, Miramistin exceeds the effect of inactivation of coronaviruses known and currently used antiseptic.Just been delivered 3 series of experiments in 4 concentrations of 6 animals each. Virus infectivity was expressed in lg50for mice-suckers. The average results of the experiments are presented in table.2.Analysis of the obtained data shows that the Miramistin in a concentration of 0.0001% reduces infectious activity of coronavirus man almost twice, and at a concentration of 0.005 and above fully counteract it.Example 3. The influence of Miramistin on hemagglutinin activity of coronavirus AS determined by the setting reaction of haemagglutination (DSA) with chicken erythrocytes.To the culture fluid containing the coronavirus AS with hemagglutinins the titre not less than 1:512, solution was added Miramistin in concentrations of from 0.000001 to 0.001%. The mixture is incubated for 30 min, was added 25% fetal cow serum to neutralize Miramistin, kept for 10-20 min and then put DSA with chicken erythrocytes. Just spent 4 series of experiments in four concentrations on three experiences at each. The average results of the experiments are presented in table.3.The results of the experiments show that the Miramistin begins to act on the hemagglutinin of coronavirus AS, obespechivaya (0,0001%).The given examples show that the proposed solution allows to use the connection ministerocomunicazione chloride (“Miramistin”) as a means of inactivation of coronaviruses and on its basis to create new preventive and therapeutic drugs to combat diseases caused by coronaviruses. Application ministerocomunicazione chloride (“Miramistin”) as a means of inactivation of coronaviruses.
< / BR>where R3represents (1-6C)alkyl or halogen; Q is aryl or heteroaryl, which optionally carries 1, 2, 3, or 4 substituent selected from hydroxy, halogen, cyano, nitro, amino, carboxy, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)quinil, (1-6C)alkoxy, (1-3C)alkylenedioxy, (1-6C)alkylamino and so on; R2- (1-6C)alkyl, (2-6C)alkenyl, (2-6C)quinil, (1-6C)alkoxy, (1-6C)alkylamino or di-[(1-6C)alkyl]amino; p is 0, 1 or 2; q = 0, 1, 2, 3 or 4; R4- aryl, aryl-(1-6C)alkoxy, aryloxy, arylamino, cycloalkyl or heteroaryl and R4optionally carries 1, 2, 3, or 4 substituent selected from halogen, cyano, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)quinil, (1-6C)alkoxy, (1-6C)alkylamino and so on, or its pharmaceutically acceptable salt, or cleaved in vivo ester
< / BR>where R3represents (1-6C)alkyl or halogen; m is 0, 1, 2 or 3; R1represents hydroxy, halogen, trifluoromethyl, nitro, amino, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)quinil, (1-6C)alkoxy, (1-6C)alkylamino, di-[(1-6C)alkyl] amino, amino-(2-6C)alkylamino, (1-6C)alkylamino-(2-6C)alkylamino etc
FIELD: organic chemistry, pharmacology.
SUBSTANCE: invention relates to compounds of formula I ,
where R(1), R(2), R(3), R(4), R(5), R(6), R(7), R(8), R(30), and R(31) are disclosed in claims. Compound of present invention are particularly useful as new antiarrythmia bioactive substances, in particular for treatment and prophylaxis of atrial arrhythmia (e.g., atrial fibrillation or auricular flutter).
EFFECT: higher efficiency.
13 cl, 18 ex, 1 tbl
FIELD: medicine, cardiology, pharmacy.
SUBSTANCE: invention relates to pharmaceutical composition comprising atenolol as an active component and additives - starch, magnesium basic carbonate, polyvinylpyrrolidone and/or starch glycolate sodium salt, gelatin and stearate; or starch, polyvinylpyrrolidone, stearate, aerosil and microcrystalline cellulose. Composition shows improved physical-mechanical properties.
EFFECT: improved pharmaceutical properties of composition.
14 cl, 1 tbl, 5 ex
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to derivatives of N-desacetylthiocolchicine of the formula (I):
wherein n represents a whole number from 0 to 8; Y represents group CH2 or if n = 1 then can mean group NH also. These compounds elicit an anti-proliferative activity. Also, invention describes pharmaceutical composition based on compounds of the formula (I).
EFFECT: valuable medicinal properties of derivatives.
4 cl, 1 tbl, 4 ex
FIELD: neurological diseases.
SUBSTANCE: composition contains therapeutically effective amount of anticonvulsant agent dissolved or dispersed in aqueous carrier containing 10-80 vol % aliphatic alcohol, 10-80 vol % ethylene glycol, and 0.1-5 vol % bile acid salt or lecithin. Indicated carrier ensures increased access of anticonvulsant agent (such as benzodiazepin, in particular diazepam, clonazepam, phoenitoin, mephoenitoin, ethotoin, phenobarbital, carbamazepin, ethosuccinamide, valproic acid, gabapentine, trimethadion, lamotrigin) into blood and rapid pharmacological response when using nasal administration.
EFFECT: accelerated anticonvulsant effect.
11 cl, 9 dwg, 10 tbl, 13 ex
FIELD: organic chemistry, analytical chemistry, bioorganic chemistry, biochemistry, applied medicine, labeled compounds.
SUBSTANCE: invention proposes labeled analogue of physiologically active compound, namely, tritium high-labeled [3H]-(E)-N-[(4-hydroxy-3-methoxyphenyl)methyl]-8-methyl-6-noneneamide of the formula:
Invention provides expanding the assortment of labeled analogues of physiologically active compounds.
EFFECT: valuable properties of compounds.
SUBSTANCE: method involves administering fixed 3% Prospidine ointment applications applied to the uterine cervix on the immune correction treatment background at the second menstrual cycle half. The uterine cervix is treated with Myramistin solution.
EFFECT: reduced risk of complications.