Therapeutic application of compounds
SUBSTANCE: invention refers to the application of a compound of formula R1-COOH (I), where R1 is an alkyl group with a main chain of 7-11 carbon atoms, possibly branched in any position of the carbon atom in the main chain, where branching is a side C1-6 alkyl group. The alkyl group of the main chain and/or the side alkyl groups optionally contain one or more heteroatoms. The specified compound is selected from 4-ethyl octanoic acid, 2-butyl octanoic acid, 4-methyl nonanoic acid and 3-methyl undecanoic acid or its pharmaceutically acceptable salt, amide or ester, for treatment or prevention of disease or biomedical state, selected from disorders associated with cramps.
EFFECT: increased efficiency of the composition and treatment method.
2 cl, 9 dwg, 3 tbl
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 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: invention represents a pharmaceutical composition for treating the HIV infection in the form of a solid dosage form, containing at least one HIV protease inhibitor in a therapeutically effective amount specified in a group of nelfinavir, sacvinavir, tipranavir, darunavir, indinavir, ritonavir, lopinavir, palinavir or fosamprenavir, and pharmaceutically acceptable additives differing by the fact that as the pharmaceutically acceptable additives it contains at least one water-insoluble polymer from 0.39 to 28 wt % of the total dosage form, surfactants, excipients up to 100% of the total dosage form, as well as a method of treating the HIV infection.
EFFECT: pharmaceutical composition according to the invention possesses the improved technological properties and improved bioavailability as compared to a prototype therapeutic agent.
10 cl, 4 ex, 1 tbl
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to the pharmaceutical industry, particularly to a composition for treating or preventing the human immunodeficiency virus (HIV) or hepatitis C. The herbal composition used for treating or preventing the patients infected by the HIV or hepatitis C viruses and containing a herbal ingredient with tannin agents and catechin, and a pharmaceutically acceptable carrier; the herbal ingredient is Agrimonia Eupatoria (GAFT) and/or gambier (Uncaria gambir). A method for preparing the herbal composition for treating or preventing the patients infected by the HIV or hepatitis C viruses.
EFFECT: composition is effective for treating or preventing the patients infected by the HIV or hepatitis C viruses.
12 cl, 6 dwg, 2 tbl
SUBSTANCE: invention relates to the field of biotechnology and cell technology. The claimed invention is aimed at the creation of pluripotent, multipotent and/or self-renewing cells, which are able to start differentiating in a culture into various types of cells and are capable of further differentiation in vivo. The claimed invention is also aimed at the creation of populations of the required differentiating cells, which can be transplanted to patients, genetic modification of endogenic cells and treatment of patients, suffering from diseases, intensity of which can be reduced by means of the said methods.
EFFECT: invention also claims methods of prevention, treatment or retardation of a disease, associated with an infection of immunodeficiency virus.
17 cl, 1 dwg, 13 ex
SUBSTANCE: invention refers to medical and molecular genetics. There are described genetic constructs expressing RNA sequences and genes coding proteins possessing the antiviral activity on human immunodeficiency virus. The genetic constructs contain a sequence coding the human TRIM5a modified protein. The invention can be used in scientific investigations.
EFFECT: presented constructs enable providing the higher expression of the modified gene of the human TRIM5a.
40 cl, 4 dwg, 3 tbl, 13 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to a pharmaceutical composition in a tabletted dosage form which contains the first layer containing ritonavir and a polymer in a ratio of 1:1 - 1:6, and the second layer containing darunavir. The first layer is produced by hot extrusion, and the second layer - by direct extrusion or wet granulation. Also, the invention refers to a method for preparing the above pharmaceutical composition, and to a method of treating HIV or AIDS involving administering the above composition.
EFFECT: invention enables overcoming the incompatibility of ritonavir and darunavir, and also provides an optimum dissolution profile of both the active substances.
17 cl, 2 tbl, 2 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to a pharmaceutical composition for HIV-1 replication inhibition containing a compound of Formula
wherein n is equal to 1 or 2; Ar means phenyl substituted by one substitute specified in a group consisting of OH and NO2, or by two substitutes OR, or thienyl; R1 is specified in a group consisting of R6, C(O)N(R6)2, and C1-C6 alkyl substituted by OR; R2 means H or C1-C6 alkyl; R6 is independently in each specific case specified in H and C1-C6 alkyl; each R independently represents C1-C8 alkyl; or its pharmaceutically acceptable salt, or a compound 1G3, or its pharmaceutically acceptable salt. Also, the invention refers to a method of treating an individual either HIV-1 infected or suffering a high risk of HIV-1 infection involving administration of the above composition, to a method for HIV-1 virus replication inhibition.
EFFECT: what is prepared is the new pharmaceutical composition possessing effective biological properties 1G3.
11 cl, 6 tbl, 1 ex
SUBSTANCE: invention relates to improved method of obtaining pyridine compounds (AA),(BB) and (CC) of respective formulas:
said compounds possess inhibiting action with respect to HIV-integrase. method consists in carrying out the following stages: P-1) bromination of compound of formula (I-I) with obtaining bromine-compound of formula (II-II)
where value R represents -CHO, -CH(OH)2, -CH(OH)(OR4), -CH(OH)-CH2OH or -CH(OR5)(OR6); P1 represents benzyl; P3 represents H or protective group of carboxyl; R4 represents lower alkyl; R5 and R6 independently represent lower alkyl or R5 and R6 can represent alkyl and be connected with formation of 5-, 6- or 7-member ring, P-2) formation of side chain of 2,4-di-fluorophenyl-CH2-NH-C(O)- with application of reagents 2,4-di-fluorophenyl-CH2-NH2 and carbon monoxide, stage of formation of Q ring by means of respective amine, selected from 3-amino-butan-1-ol, 2-amino-propan-1-ol and 2-pyrrolidinyl methylamine, and stage of debenzylation with obtaining compound of formula (AA), (BB) or (CC), where said stage P-2 is carried out after formation of Q ring.
EFFECT: method makes it possible to simplify obtaining target compounds due to carrying out regioselective bromination at the first stage.
6 cl, 3 ex, 7 dwg
SUBSTANCE: invention relates to use of nucleoside derivatives - 1,2,5-oxadiazoles of general structural formula I where R1 and R2 are selected from phenylsulphonyl, substituted with one or more halogen atoms, nitro groups, carboxy groups, alkyl halides, CH3, OCH3, OCF3; X is selected from N or N→O; or R1 and R2 form a group, where R', R", R'" and R'''' are independently selected from hydrogen; halogens; nitro groups, hydroxy group, carboxy group, CH3; CH2Br; OCH3; phenylsulphonyl; phenylthio group; or the following groups: R' and R" can also be merged into one of the following common rings for inhibiting human immunodeficiency virus (HIV) replication. The invention also relates to a pharmaceutical composition based on compounds of formula I and a method of inhibiting HIV-1 subtypes A and B integrase, including forms which are resistant to raltegravir.
EFFECT: detecting novel activity in compounds of formula I, which can be used in medicine as HIV replication inhibitors.
3 cl, 5 tbl, 4 ex
SUBSTANCE: invention relates to compounds of general formula or , where Ar1 represents phenyl group, optionally substituted with one or several identical or non-identical halogen atoms; R1 represents hydrogen atom; R4, R5, R6a, R6b represent hydrogen atoms; Y, Z independently represent linear C1-4 alkylene group, optionally substituted with one linear C1-4 alkyl group; Ar2 stands for condensed with benzene 5-membered heterocyclic ring, containing one nitrogen atom and one sulphur atom, substituted with one linear C1-4 alkyl group, or derivative of 5- or 6-membered heterocyclic ring, containing one nitrogen atom and one sulphur atom, condensed with heteroaromatic 6-memebered ring, containing one or two nitrogen atoms, substituted with one linear C1-4 alkyl group, linear C1-4 alkoxygroup or group -NR7R8, where R7 and R8 independently stand for hydrogen atom, linear or branched C1-4 alkyl group, or R7 and R8 together with nitrogen atom form group of general formula , where R2, R3 represent linear C1-4 alkyl groups, A stands for group -CHR12, oxygen atom or group -NR9, where R12 and R9 stand for hydrogen atom or linear C1-4 alkyl group, m has value 1 or 2, n has value 1 or 2, o has value 0 or 1, p has value 0 or 1, Q stands for group -O-, group -N--H or group -N--CO-R10, where R10 stands for linear C1-4 alkyl group or -NH-R11 group, where R11 represents linear C1-4 alkyl group; and to their salts. Invention also relates to methods of obtaining therein and to based on them pharmaceutical composition, possessing antagonistic activity with respect to receptor CCR3.
EFFECT: obtained are novel compounds and based on them pharmaceutical compositions, which can be applied in medicine for obtaining medication, intended for treating asthma, allergic rhinitis, atopic dermatitis, eczema, inflammatory intestinal diseases, ulcerous colitis, Crohn's disease, allergic conjunctivitis, multiple sclerosis or HIV-infection and AIDS-associated diseases.
14 cl, 3 tbl, 26 ex
SUBSTANCE: biologically active peptide is obtained, which has curative effect against Alzheimer disease, and consisting of the amino acid sequence Ala-Trp-Lys-Val-Leu-Ser-Pro-Gln-Gly-Gly-Gly-Pro-Trp-Asp-Ser-Val-Ala.
EFFECT: invention enables to use the resulting peptide to create a drug effective in the therapy of Alzheimer disease.
1 dwg, 2 ex