Method for treatment of alcoholic cardiomyopathy
SUBSTANCE: method includes introduction of metabolitotropic cardioprotector represented by (S)-2,6-diaminohexanoic acid 3-methyl-1,2,4-triazolyl-5-thioacetate in a dose of 100 mg/kg a day for 30 days. Invention application allows to increase therapeutic efficiency due to cardioprotective activity and low toxicity of (S)-2,6-diaminohexanoic acid 3-methyl-1,2,4-triazolyl-5-thioacetate.
EFFECT: increased efficiency of treatment.
2 tbl,1 ex
SUBSTANCE: invention relates to medicine, namely to cardiovascular surgery and cardiology, and deals with complex correction of immunoinflammatory responses of cardiovascular bed. For this purpose, in case of presence of high level of circulating immune complexes and/or complement in patient, three sessions of plasmapheresis in accordance with conventional methods, and in case of low level of IgG and reduced phagocytic activity of neutrophils and monocytes, as well as in case of confirmed autoimmune process, a course of intravenous infusions of human polyvalent immunoglobulin is carried out in accordance with conventional schemes.
EFFECT: method provides reduction of both hypo- and hyperactive disorders in immune system of patients and resulting increase of efficiency of treatment of cardiovascular system diseases.
SUBSTANCE: limb ischemia is simulated in a male Wistar rat anaesthetised with chloral hydrate in a dose of 250-300 mg/kg by the surgical removal of femoral, popliteal arteries and the front shin artery. That is followed by introducing a prepared mononuclear fraction of the autologous bone marrow in a dose of 4×106 cells in an amount of 200 mcl. The above is introduced into the ischemic limb from two points in an amount of 100 mcl each. One point is found directly under the femoral arch paravasally within the anatomical position of collaterals of the inner iliac artery and its branches. The other point is located in the calf muscle on an anteriolateral surface of the midleg.
EFFECT: more effective experimental treatment ensured by stimulating the collateral blood flow in the ischemic limb and improving the arterial blood flow from the proximal to distal parts of the limb.
1 ex, 1 tbl
SUBSTANCE: early postoperative period involves administering low-molecular heparins and anti-inflammatory agents. Anti-inflammatory therapy requires administering cycloferon according to the schedule: 2 tablets of cycloferon 0.15 mg on the first preoperative day, 2 tablets on the first postoperative day, 2 tablets in the morning on the 2nd, 4th, 6th postoperative day, and further, every third day throughout 1 postoperative month (on the 9th, 12th, 15th, 18th, 21st, 24th, 27th, 30th day).
EFFECT: method provides the effective prevention of postpericardiotomy syndrome with a lower risk of side effects by administering cycloferon according to the developed schedule requiring non-steroidal anti-inflammatory agents and glucocorticosteroids.
2 ex, 3 tbl
SUBSTANCE: group of inventions refers to medicine, and concerns using a human Annexin-1 antibody (Anx-A1), which has the sequence SEQ ID NO: 23 for treating a disease caused by abnormal T-cell activation. The group of inventions also concerns a method of treating a disease caused by abnormal T-cell activation, involving administering a therapeutic amount of the above antibody into an individual in need thereof; using the above antibody for producing a therapeutic agent for treating a disease caused by abnormal T-cell activation.
EFFECT: group of inventions provides treating the disease caused by abnormal T-cell activation.
9 cl, 11 ex, 22 dwg
SUBSTANCE: invention concerns rehabilitation of elderly patients with ischemic heart disease (IHD) accompanied by chronic heart insufficiency (CHI) following myocardial in myocardial infarction (MI). That is ensured by administering Omacor, a preparation of omega-3-polyunsaturated fatty acids in the remote period, 6 or more months after the suffered MI with underlying a standard drug therapy 60 minutes before the graduated walking.
EFFECT: this complex of the drug preparations combined with the graduated physical exercises provides higher tolerance to physical exercises, improving the cardiovascular function and normalising the lipid exchange that in turn leads to reducing a number of unfavourable cardiovascular episodes and delaying CHI.
2 ex, 5 tbl
SUBSTANCE: claimed is the application of N-(2-adamantyl)-hexamethylenimine hydrochloride (himantane) as a medication for treating cerebral circulation disorders and brain traumas. An ability of himantane to reduce animal morbidity and increase cognitive and motor indices in case of its introduction after 3.5 hours after modelling a hematoma in rats and further introduction for 4 days was determined, which testifies to its possessing the neuroprotective potential on the model of the intracerebral post-traumatic hematoma. The technical result consists in the realisation of the claimed purpose: it has been shown that himantane in a dose of 5 mg/kg in case of intravenous introduction causes the increase of cerebral circulation in the rats' brain after ischemic brain affection without changing the level of arterial pressure.
EFFECT: medication did not produce a significant impact on the blood supply of the brain of the intact animals and did not cause a change in the heart rate and respiratory rate.
1 dwg, 6 tbl
SUBSTANCE: group of inventions relates to medicine, namely to neurology, and deals with the treatment of ischemic stroke. For this purpose the introduction of ubidecarenone by injection, mainly intravenous, is carried out.
EFFECT: introduction of the medication provides the reduction of the zone of brain tissue injury and reduction of neurologic deficiency expression due to the accumulation of ubidecarenone, possessing an expressed neuroprotective action, in brain tissues.
7 cl, 4 dwg, 3 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to a compound of formula , which is a methylhydrofumarate (MHF) prodrug. In formula (I), radicals and symbols have the values specified in the patent claim. The invention also refers to a pharmaceutical composition containing the declared methylhydrofumarate drugs, to using the declared methylhydrofumarate drugs and the pharmaceutical composition containing them, for treating diseases, such as psoriasis, asthma, multiple sclerosis, inflammatory intestinal disease and arthritis, and to a method of treating the above diseases.
EFFECT: higher oral bioavailability and plasma MHF, dimethylfumarate and/or other metabolites.
47 cl, 1 tbl, 54 ex
SUBSTANCE: antianginal therapy is accompanied by a primary discrete plasmapheresis in a refrigerate centrifuge PC-6 having a rotating speed of 2,000 rpm for 15 minutes at a temperature of 22°C in number of 5 sessions every second day. One session involves removing the whole blood in an amount of: 2 flexible PVC packages x 450 ml if the patient's body weight index is from 18 to 29.9 kg/m2, 3 flexible PVC packages x 450 ml if the patient's body weight index is over 30 kg/m2. The total volume of the removed plasma makes 600-900 ml. The circulating blood volume is replaced with 0.9% NaCl in an amount of half as much as the removed plasma volume. Once the plasmapheresis course is completed, the blood is exposed to ultraviolet light generated by OVK-3 apparatus for at wave length more than 400 nm in number of 5 procedures every second day.
EFFECT: effective treatment of the given category of the patients by improving the haemorheology, normalising the lipid spectrum without increasing liver enzymes with preserving the hepatic function, decreasing the dyslipidemia level and functional class of angina in the patients with limited use of statins with underlying cholestasis.
2 tbl, 5 ex
SUBSTANCE: urgent surgery on vessels of a lower extremity involves placing an electrode for transoesophageal atrial temporal pacing (TOTP). That is followed by administering a beta adrenergic blocking agent intravenously in a load dose to achieve a decreased heart rate of ≤ 60 beats per minute. The dose of the beta adrenergic blocking agent is reduced to a maintaining one with preserving a sinus decreased heart rate from 72 to 74 beats per minute for the whole surgery and for 2-3 days thereafter as it may be necessary. The surgical repair of coronary arteries is performed at least 3-4 weeks after the surgery on the vessels of the lower extremities.
EFFECT: therapeutic approach provides preventing minor cardiac output syndrome and other cardiovascular adverse effects accompanying the repair surgeries on the arteries of the lower extremities that enables a coronary artery bypass surgery 3-4 weeks later.
2 cl, 2 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to substituted phenylureas and phenylamides of formula in which X stands for CR3 or N, where R3 stands for H; C1-10alkyl, saturated or unsaturated, branched or non-branched, non-substituted; or CF3; A stands for N or CR5b; R1 stands for substructure , which has the formula, given below. The other radicals and symbols have the values, given in the invention formula. The invention also relates to methods of obtaining formula (If) compounds, to pharmaceutical compositions, containing the said compounds, as well as to the application of the said compositions for the preparation of the pharmaceutical compositions.
EFFECT: formula (If) compounds possess activity with respect to the vanilloid receptor of I subtype (receptor VR1/TRPV1).
7 cl, 1 tbl, 147 ex
SUBSTANCE: therapeutic agent contains anastrozole, poly(lactic-co-glycolic acid), polyvinyl alcohol and D-mannitol. The therapeutic agent represents sub-micron particles and can be presented in the form of capsules, granules, powder, as well as a suspension for injections.
EFFECT: using the developed therapeutic agent enables achieving the therapeutic effect with lower therapeutic doses and making the antitumour therapy more comfortable for the patient.
2 cl, 1 tbl, 2 dwg, 3 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to new aminotetraline derivatives of formula (I) and their physiologically tolerable salts. In formula
A means a benzene ring or a ring specified in a group consisting of a 5-merous ring
R means the group R1-W-A1-Q-Y-A2-X1-; R1 means hydrogen, C1-C6-alkyl, C3-C6-cycloalkyl-C1-C4-alkyl, halogenated C1-C6-alkyl, tri-(C1-C4-alkyl)-silyl-C1-C4-alkyl, C1-C6-alkoxy-C1-C4-alkyl, amino-C1-C4-alkyl, C3-C6-cycloalkyl, C2-C6-alkenyl, an optionally substituted phenyl, C1-C6-alkoxy, di-C1-C6-alkylamino, an optionally substituted 5 or 6-merous heterocyclyl containing 1-3 heteroatoms specified in nitrogen and/or oxygen or sulphur; W means a bond; A1 means a bond; Q means -S(O)2- or -C(O)-; Y means -NR9- or a bond; A2 means C1-C4-alkylene, or a bond; X1 means -O-, C1-C4-alkylene, C2-C4-alkynylene; R2 means hydrogen, halogen, or two radicals R2 together with the ring atom to which they are attached form a benzene ring; R3 means hydrogen. The other radical values are specified in the patent claim. The invention also refers to intermediate products for preparing the compounds of formula (I).
EFFECT: compounds possess the properties of glycine transporter inhibitors, particularly GlyT1 and can find application in treating neurological and psychiatric disorders, such as dementia, bipolar disorder, schizophrenia, etc or for managing pain related to glycerinergic or glutamatergic neurotransmission dysfunction.
20 cl, 2 tbl, 326 ex
SUBSTANCE: agent is presented in the form of a tablet, contains isoniazid and a substance which reduces its toxicity; as the substance which reduces the isoniazid toxicity, it contains thiotriazolin. The isoniazid/thiotriazolin ratio makes 4:1.
EFFECT: combined antituberculous drug ensures reducing toxicity as compared to the known ones and increasing its pharmacological activity.
2 cl, 1 ex, 1 tbl
SUBSTANCE: therapeutic agent contains recombinant interferon specified in a group of: recombinant interferon alpha, recombinant interferon beta, recombinant interferon gamma, metronidazole, fluconazole and/or voriconazole, and a pharmaceutically acceptable base in the following proportions, g per 1 ml of the mixture: recombinant interferon, international units 100-10,000,000; metronidazole 0.00001-0.5; fluconazole and/or voriconazole 0.00001-0.5; pharmaceutically acceptable base - the rest. Besides, the therapeutic agent contains boric acid in an amount of 0.00001-0.5 g and hypromellose in an amount of 0.00001-0.5 g. As a pharmaceutically acceptable base, it contains macrogol 400 or macrogol 1500, or macrogol 4000.
EFFECT: higher efficacy of the compound.
2 cl, 5 ex
SUBSTANCE: described is novel biologically active compound 2-methylsulphanyl-6-nitro-7-oxo-1,2,4-triazolo[5,1-c][1,2,4]triazinide L-argininium dehydrate of formula , which has antiviral action, method of its obtaining and application for prevention and treatment of West Nile fever.
EFFECT: increased efficiency of compound application.
3 cl, 2 tbl, 2 ex
SUBSTANCE: invention represents an antifungal preparation in suppositories for children containing recombinant human interferon 2α and fluconazole, wherein lysozyme, Licopid and dimephosphone are additionally introduced.
EFFECT: preparation possesses the high clinical effectiveness in the fungal diseases in children that leads to reducing the length of treatment and prolonging the intercurrent period.
1 tbl, 3 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to medicine, pharmacy and pharmacology. What is presented is using 1-(β-phenylethyl)-4-amino-1,2,4-triazolium bromide (Hypertril) as an active base of drug preparations for correcting dysfunctions of the nitroxydergic system of target organs accompanying homocysteinemia and acute cerebrovascular disorders.
EFFECT: what has been shown is achieving the declared application that is normalising the nitroxydergic function irrespective of whether the NO deficiency or hyperproduction is observed; Hypertril is three times more effective to reduce the homocystein production in comparison to the similar known preparation L-arginine, and has no side effect.
2 tbl, 2 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to compounds of formula 1.0:
where Q represents tetrahydropyridinyl ring substituted. R5, R1 are selected from: (1) pyridyl, substituted with substituent, selected from group, consisting of: -O-CH3, -O-C2H5, -O-CH(CH3)2, and -O-(CH2)2-O-CH3, R2 is selected from group, consisting of: -OCH3 and -SCH3; and R5 is selected from (a) substituted triazolylphenyl-, where triazolyl is substituted with one or two alkyl groups, selected from group, consisting of: -C1-C4alkyl, (b) substituted triazolylpheenyl-, wheretriazolyl is substituted on nitrogen atom with -C1-C4alkyl, (c) substituted triazolylphenyl-, where triazolyl is substituted on nitrogen atom with -C2alkylene-O-C1-C2alkyl, (d) substituted triazolylphenyl-, where triazolyl is substituted on nitrogen atom with -C2-C4alkylene-O-CH3, and (e) substituted triazolylphenyl-, where triazolyl is substituted on nitrogen atom with hydroxy-substituted -C1-C4alkyl, and where phenyl is optionally substituted with from 1 to 3 substituents, independently selected from group, consisting of halogen; and their pharmaceutically acceptable salts and solvates, which are claimed as ERK inhibitors.
EFFECT: obtaining pharmaceutically acceptable salts and solvates, claimed as ERK inhibitors.
15 cl, 2 tbl, 32 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to compounds of formula , wherein A means a six-merous aryl radical or a five-merous heteroaryl radical which contains one heteroatom specified in oxygen and sulphur; one or more hydrogen atoms in the above aryl or heteroaryl radicals can be substituted by substituting groups R1 which are independently specified in a group consisting of: F, Cl, Br, I, (C1-C10)-alkyl-, (C1-C10)-alkoxy-, -NR13R14; B means a radical with mono- or condensed bicyclic rings specified in a group consisting of: six-ten-merous aryl radicals, five-ten-merous heteroaryl radicals and nine-fourteen-merous cycloheteroalkylaryl radicals, wherein cycloheteroalkyl links can be saturated or partially unsaturated, while the heterocyclic groups can contain one or more heteroatoms specified in a group consisting of nitrogen, oxygen and sulphur, one or more hydrogen atoms in the radical groups B can be substituted by substituting groups R5 (as specified in the patent claim), L means a covalent bond, X means the group -O-, R2 is absent or means one or more substitutes specified in F and (C1-C4)-alkyl radical; R3 and R4 independently mean (C1-C10)-alkyl, (C3-C14)-cycloalkyl, (C4-C20)-cycloalkylalkyl, (C2-C19)-cycloheteroalkyl, (C3-C19)-cycloheteroalkylalkyl, (C6-C10)-aryl, (C7-C20)-arylalkyl, (C1-C9)-heteroaryl, (C2-C19)-heteroarylalkyl radicals, or R3 and R4 together with nitrogen attached whereto can form a four-ten-merous saturated, unsaturated or partially unsaturated heterocyclic compound which can additionally contain one or more heteroatoms among -O-, -S(O)n-, =N- and -NR8-; other radicals are such as specified in the patient claim. Also, the invention refers to using the compound of formula I for preparing a drug.
EFFECT: compounds of formula (I) as Na+/H+ metabolism inhibitors NHE3.
22 cl, 27 dwg, 1 tbl, 756 ex
FIELD: organic chemistry, pharmaceutical compositions.
SUBSTANCE: 5-aryl-1H-1,2,4-triazole derivatives of general formula I
, pharmaceutically acceptable salts thereof or pharmaceutical composition containing the same are described. In formula R1 is C1-C6-alkyl, C1-C6-haloalkyl or phenyl; R2 is C3-C8-cycloalkyl; phenyl optionally substituted with one or more substituents selected from C1-C4-alkyl; halogen, hydroxyl, C1-C4-alkoxy, nitro, di-(C1-C4)-alkylamino, C1-C4-alkylsulphonyl, C1-C4- alkylsulphonylamino, and methylenedioxy; phenyl-(C1-C4)-alkyl, wherein phenyl is substituted with C1-C4-alkoxy; or pyridil. New compounds are effective and selective cyclooxygenase-2 (COX-2) inhibitors and useful in treatment of inflammations.
EFFECT: new compounds for inflammation treatment.
10 cl, 36 ex, 1 tbl