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Use of quartenary pyridinium compounds for vasoprotection and/or hepatoprotection. RU patent 2477132. |
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FIELD: medicine, pharmaceutics. SUBSTANCE: invention refers to using a compound of formula (I): wherein R represents a hydrogen atom or CH3, and X represents a physiologically acceptable counter ion for preparing a hepatoprotective agent for treating or preventing a liver injury. The invention also refers to a method for treating or preventing the liver injury which involves a therapeutically or preventive effective amount of said compound of formula (I). EFFECT: declared group of inventions provides hepatoprotective activity ensured by an ability of the compounds of formula (I) to improve an endothelium function to release endogenic prostacyclin. 14 cl, 7 dwg, 3 tbl, 5 ex
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Capsule and drug preparation for preventing cardiovascular diseases / 2477123 Invention refers to pharmaceutical industry, particularly a drug preparation for preventing the development of cardiovascular diseases in individuals of a high-risk group. A capsule for preventing the development of cardiovascular diseases in individuals of a high-risk group which contains acetylsalicylic acid tablets coated by partially hydrolised polyvinyl alcohol (PVA), tablets of simvastatin and pravastatin coated by hydroxypropyl methylcellulose (HPMC) and tablets of lisinopril, ramipril or perindopril coated by partially hydrolised polyvinyl chloride. Using the capsule in producing the drug preparation for preventing the development of cardiovascular diseases in individuals of a high-risk group. |
4-dimethyl aminobutyric acid derivatives / 2474573 Disclosed are novel 4-dimethyl aminobutyric acid derivatives of formula (I) (pharmaceutically acceptable salts thereof), where values of A1, A2, R1, m and n are given in the claim, which inhibit activity of carnitine palmitoyltransferase (CPT), and more specifically CPT2. |
Substituted 4-aryl-1,4-dihydro-1,6-naphthyridine amides and use thereof / 2470932 Invention relates to novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridine-3-carboxamides, method for production thereof, use thereof to produce a medicinal agent which inhibits MR activity. |
Cycloalkylamine-substituted isoquinoline and isoquinolinone derivatives / 2468011 Present invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of formula or stereoisomer and/or tautomer forms thereof, and/or pharmaceutically acceptable salts thereof, where R1 is H or OH; R2 is R', (C7-C8)alkyl, (C1-C6)alkylene-R', (C2-C6)alkenyl; or R2 is (C1-C6)alkyl, under the condition that in said alkyl residue, at least one hydrogen is substituted with OH or OCH3; or R2 is (C1-C6)alkylene, bonded with cycloalkylamine, where (C1-C4)alkylene forms a second bond with another carbon atom of the cycloalkylamine ring and, together with carbon atoms of the cycloalkyalmine, forms a second 5-8-member ring; R3, R5 and R8 denote H; R4 is H, (C1-C6)alkyl or (C1-C6)alkylene-R'; R6 and R6' independently denote H, (C1-C8)alkyl, (C1-C6)alkylene-R' or C(O)O-(C1-C6)alkyl; R7 is H, halogen or (C1-C6)alkyl; n equals 1; m equals 3 or 5; r equals 0 or 1 and L is O(CH2)p, where p=0; where R' is (C3-C8)cycloalkyl, (C6)aryl; where in residues R2-R8 (C6)aryl is unsubstituted or substituted with one or more suitable groups independently selected from halogen, (C1-C6)alkyl, O-(C1-C6)alkyl, where the alkyl group can be substituted with 1-3 halogen atoms. The invention also relates to use of the compound of formula (I) and a medicinal agent based on the compound of formula (I). |
3-(2,2,2-trimethylhydrazinium) propionate derivative - 3-(2,2,2-trimethylhydrazinium) potassium propionate 5-bromnicotinate exhibiting endothelioprotective activity / 2467745 Invention refers to pharmaceutics and medicine, more specifically to a new 3-(2,2,2-trimethylhydrazinium)propionate derivative, 3-(2,2,2-trimethylhydrazinium)potassium propionate 5-bromnicotinate (CH3)3N+HCH2CH2COOKRCOO- wherein . |
3-(2,2,2-trimethylhydrazinium) propionate derivative - 3-(2,2,2-trimethylhydrazinium) potassium propionate 5-nicotinate hydroxide exhibiting endothelioprotective activity / 2467744 Invention refers to pharmaceutics and medicine, more specifically to a new chemical compound, a 3-(2,2,2-trimethylhydrazinium)propionate derivative, namely 3-(2,2,2-trimethylhydrazinium)potassium propionate 5-nicotinate hydroxide showing endothelioprotective activity. |
Crystalline forms of aliskiren hemifumarate / 2466982 Crystalline form of aliskiren hemifumarate is characterized by the picture of X-ray diffraction in powder demonstrating the following main peaks, given at degrees 2 Teta+/- 0.3 degree: 3.8, 6.5, 7.7, 8.0, 15.6 and 17.4. said form is obtained from solution with weight ratio (weight/weight) acetonyl : ethanol, being in the interval from 90:10 to 75:25 (for instance, 80:20) at suitable temperature in the interval from 15 to 40°C, for instance, by cooling from 37°C to 35°C and especially after dimming - by further cooling to 20°C, ensuring aliskiren hemifumarate crystallisation, filtered and dried under vacuum, for instance, at 10 mbar and 40°C. Crystalline form of aliskiren hemifumarate is applied for obtaining pharmaceutical composition, suitable for treating disease in warm-blooded animal, modulated by rennin inhibition. |
Irbesartan-containing pharmaceutical compositions / 2465900 Pharmaceutical composition by invention possesses antagonistic activity with respect to angiotensin II. Pharmaceutical composition contains 30-80 wt % of inrbesartan or its pharmaceutically acceptable salt as active ingredient and more than 10 wt % of loosening agent in terms of complete composition weight. Pharmaceutical composition does not contain silicon-containing antiadhesive. Pharmaceutical composition of irbesartan is made in form of tablet with film coating. Also described is method of irbesartan tablet manufacturing. |
Sustained-action pharmaceutical composition for treating heart diseases / 2464018 Present invention refers to a pharmaceutical composition for treating cardiovascular diseases which contains a therapeutically effective amount of metoprolol succinate as an active substance, and excipients - a combination of hypromellose type 2910 and hypromellose type 2208 taken in the relation of 1:(0.18-472.5), a filler, a glidant, a lubricant. Said pharmaceutical composition is presented in the form of a coated tablet. |
Method of treating chronic obstructive pulmonary disease accompanied by bronchiectasia / 2464017 Invention refers to medicine, namely pulmonology, and concerns treating chronic obstructive pulmonary disease accompanied by bronchiectasia. That is ensured by the endotracheal introduction of berodual 2 ml, 0.25% novocaine 5 ml, 1% diphenylhydramine 1 ml, and 1% dioxidine 15 ml; the procedure is performed for 15-20 min; the therapeutic course makes 10-15 daily instillations. |
Method of early postoperative drug-induced correction of central hemodynamic disorders in oncological patients / 2477128 Invention refers to medicine, namely anaesthesiology, and concerns the early postoperative drug-induced correction of central hemodynamic disorders in oncological patients. That is ensured by measuring a cardiac index (CI), an impact index (II), a LV filling pressure (LVFP), a total peripheral vascular resistance (TPVR), a LV mechanical work index (LVMWI), a systolic blood pressure (SBP); the derived relations of these values in a patient are used to prescribe an individual drug-induced therapy. |
Capsule and drug preparation for preventing cardiovascular diseases / 2477123 Invention refers to pharmaceutical industry, particularly a drug preparation for preventing the development of cardiovascular diseases in individuals of a high-risk group. A capsule for preventing the development of cardiovascular diseases in individuals of a high-risk group which contains acetylsalicylic acid tablets coated by partially hydrolised polyvinyl alcohol (PVA), tablets of simvastatin and pravastatin coated by hydroxypropyl methylcellulose (HPMC) and tablets of lisinopril, ramipril or perindopril coated by partially hydrolised polyvinyl chloride. Using the capsule in producing the drug preparation for preventing the development of cardiovascular diseases in individuals of a high-risk group. |
Novel tetrahydroisoquinoline derivative, pharmaceutical composition based thereon, use thereof and method of treating and/or preventing disease / 2474575 Invention relates to novel tetrahydroisoquinoline derivatives of general formula (I) or pharmacologically acceptable salts thereof, where R1 is a phenyl aminocarbonyl group which can be substituted with 1-3 groups independently selected from a substituting group A, a heteroaryl aminocarbonyl group, where the heteroaryl is pyridine, pyrazine, thiazole, pyrazole or isoxazole, which can be substituted with 1 group selected from a substituting group A, benzoxazol-2-yl group, which can be substituted with 1 group selected from a substituting group A, benzothiazol-2-yl group, (C1-C6 alkyl which can be monosubstituted with a C3-C6 cycloalkyl group), aminocarbonyl group, (C3-C6 cycloalkyl)aminocarbonyl group or adamantyl aminocarbonyl group; R2 independently represents a C1-C6 alkyl group; R3 is a heterocyclic group, where the heterocycle is oxazole, oxadiazole, pyrazole, isoxazole or tetrazole, which can be substituted with 1 group selected from a substituting group A, a group of formula -C(=O)-O-R4, or a group of formula -C(=O)-N(R5)R6; R4 is a hydrogen atom, a C1-C6 alkyl group which can be substituted with 1-2 groups independently selected from a substituting group B; R5 is a hydrogen atom, a C1-C6 alkyl group which can be substituted with 1 group selected from a substituting group B, a C3-C6 cycloalkyl group which is monosubstituted with a carboxyl group, or a heterocyclic group, where the heterocycle is tetrazole, which can be substituted with 1 group selected from a substituting group A; R6 is a hydrogen atom or a C1-C6 alkyl group; in those cases when both R5 and R6 represent a C1-C6 alkyl group, which can be substituted with 1 group selected from a substituting group B, their carbon atoms can be bonded to each other to form a 5-member saturated ring; X is an oxygen atom, a methylene group, a group of formula -NH-, a methylene group which is monosubstituted with a C1-C6 alkyl group, or a group of formula -N(R7)-; R7 is a C1-C6 alkyl group; L is a single bond, a methylene group, a 1,1-dimethylmethylene group, an ethylene group, a group of formula - CH=, or a methylene group which is monosubstituted with a C1-C6 alkyl group; … denotes a single bond or a double bond (however, … denotes a single bond when L is a group of formula -CH=); m equals 1 or 2; n equals 0 or 1; substituting group A is a group of substitutes selected from a halogen atom, a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, a C1-C6 alkoxy group, a C1-C6 halogenated alkoxy group, a C1-C6 alkylthio group, a carboxyl group, a di-(C1-C6 alkyl)amino group, a cyano group, a hydroxy group, a C1-C6 alkylthionyl group and an oxo group; and substituting group B is a group of substitutes selected from a carboxyl group and a hydroxy group. The invention also relates to a pharmaceutical composition based on the compound of formula (I), use of the compound of formula (I) and a method of treating and/or preventing a disease. |
4-dimethyl aminobutyric acid derivatives / 2474573 Disclosed are novel 4-dimethyl aminobutyric acid derivatives of formula (I) (pharmaceutically acceptable salts thereof), where values of A1, A2, R1, m and n are given in the claim, which inhibit activity of carnitine palmitoyltransferase (CPT), and more specifically CPT2. |
Pyridinone pyridazinone derivatives as inhibitors of poly(adp-ribose) polymerase (parp) / 2472782 Invention relates to compounds of formula (IX) wherein radicals and symbols have values given in the claim, and pharmaceutically acceptable salts or tautomers thereof. Said compounds are inhibitors of poly(ADP-ribose)polymerase (PARP) and can be used to treat cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitisers for cancer treatment. The invention also relates to a pharmaceutical composition containing said compounds, use of said compounds and a method of treating said diseases. |
Gel polysaccharide compositions and methods for prolonged drug delivery / 2472487 Invention refers to pharmaceutical industry and represents a biologically compatible polysaccharide gel composition possessing the properties of prolonged release and containing triamcinolone acetonide engrafted to hyaluronic acid by covalent binding of triamcinolone acetonide and hyaluronic acid. |
Lyophilised dna compounds for increased plasmid dna expression / 2470995 Invention refers to a lyophilised DNA compound to be applied for treating an ischemic disease and to a method of treating an ischemic disease in an individual. The lyophilised DNA compound contains plasmid DNA, salt and carbohydrate wherein said plasmid DNA contains HGF gene, or its version, and wherein said HGF gene, or its version is specified in a group consisting of flHGF, dHGF, NK1, NK2, NK4 or their mixture. The method of treating an ischemic disease in a human or a mammal involves the introduction of a composition recovered from the lyophilised DNA compound by direct injection. |
Substituted 4-aryl-1,4-dihydro-1,6-naphthyridine amides and use thereof / 2470932 Invention relates to novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridine-3-carboxamides, method for production thereof, use thereof to produce a medicinal agent which inhibits MR activity. |
Derivatives with nitrogen-containing six-member aromatic ring and pharmaceutical products containing said derivatives / 2470927 Invention relates to novel pyrimidine derivatives of general formula (I-a), having the capacity to simulate axonal growth coupled with the capacity to stimulate angiogenesis and can be used in treating spinal chord damage, damage to the central nervous system as a result of head injuries, ischaemic stroke, ischemic heart disease, peripheral arterial occlusive disease, vascular dementia, cerebrovascular dementia or senile dementia. In the compound of formula (I-a): R0 is a group where R3 and R4 denote a hydrogen atom; R1 is a methyl group; R2 is a methyl group; R5 is a hydrogen atom; R6 is a hydrogen atom; R7 is a methyl group; E is an oxygen atom; is a benzyl group, a cyclohexyl methyl group, an isobutyl group, a cyclohexane carbonyl group, an acetyl group, a phenylsulphonyl group, a cyclohexyl group, a piperidine-1-carbonyl group, a methylbenzyl group, a phenyl group, a fluorobenzyl group, a methoxybenzyl group or a trifluorobenzyl group; or a pharmaceutically acceptable salt thereof. |
Drug preparation for treating haemorrhagic and ischemic stroke and method for producing it / 2470650 Invention refers to pharmaceutical industry, namely a preparation for treating ischemic and haemorrhagic stroke. The preparation for treating ischemic and haemorrhagic stroke recovered from swine brains with simulated haemorrhagic hemispheric stroke after common carotid arterial occlusive disease on the same side (ischemic stroke). A method for producing the preparation for treating ischemic and haemorrhagic stroke involves grinding of swine brains with pre-simulated haemorrhagic hemispheric stroke after common carotid arterial occlusive disease on the same side (ischemic stroke), homogenisation in a buffer at pH 7.3-7.6, separation of insoluble fragments from the homogenate, extraction of mixed lipid components; cleaning and sterilising filtration of the product frozen at temperature -30°C and lyophilisation. |
Novel tetrahydroisoquinoline derivative, pharmaceutical composition based thereon, use thereof and method of treating and/or preventing disease / 2474575 Invention relates to novel tetrahydroisoquinoline derivatives of general formula (I) or pharmacologically acceptable salts thereof, where R1 is a phenyl aminocarbonyl group which can be substituted with 1-3 groups independently selected from a substituting group A, a heteroaryl aminocarbonyl group, where the heteroaryl is pyridine, pyrazine, thiazole, pyrazole or isoxazole, which can be substituted with 1 group selected from a substituting group A, benzoxazol-2-yl group, which can be substituted with 1 group selected from a substituting group A, benzothiazol-2-yl group, (C1-C6 alkyl which can be monosubstituted with a C3-C6 cycloalkyl group), aminocarbonyl group, (C3-C6 cycloalkyl)aminocarbonyl group or adamantyl aminocarbonyl group; R2 independently represents a C1-C6 alkyl group; R3 is a heterocyclic group, where the heterocycle is oxazole, oxadiazole, pyrazole, isoxazole or tetrazole, which can be substituted with 1 group selected from a substituting group A, a group of formula -C(=O)-O-R4, or a group of formula -C(=O)-N(R5)R6; R4 is a hydrogen atom, a C1-C6 alkyl group which can be substituted with 1-2 groups independently selected from a substituting group B; R5 is a hydrogen atom, a C1-C6 alkyl group which can be substituted with 1 group selected from a substituting group B, a C3-C6 cycloalkyl group which is monosubstituted with a carboxyl group, or a heterocyclic group, where the heterocycle is tetrazole, which can be substituted with 1 group selected from a substituting group A; R6 is a hydrogen atom or a C1-C6 alkyl group; in those cases when both R5 and R6 represent a C1-C6 alkyl group, which can be substituted with 1 group selected from a substituting group B, their carbon atoms can be bonded to each other to form a 5-member saturated ring; X is an oxygen atom, a methylene group, a group of formula -NH-, a methylene group which is monosubstituted with a C1-C6 alkyl group, or a group of formula -N(R7)-; R7 is a C1-C6 alkyl group; L is a single bond, a methylene group, a 1,1-dimethylmethylene group, an ethylene group, a group of formula - CH=, or a methylene group which is monosubstituted with a C1-C6 alkyl group; … denotes a single bond or a double bond (however, … denotes a single bond when L is a group of formula -CH=); m equals 1 or 2; n equals 0 or 1; substituting group A is a group of substitutes selected from a halogen atom, a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, a C1-C6 alkoxy group, a C1-C6 halogenated alkoxy group, a C1-C6 alkylthio group, a carboxyl group, a di-(C1-C6 alkyl)amino group, a cyano group, a hydroxy group, a C1-C6 alkylthionyl group and an oxo group; and substituting group B is a group of substitutes selected from a carboxyl group and a hydroxy group. The invention also relates to a pharmaceutical composition based on the compound of formula (I), use of the compound of formula (I) and a method of treating and/or preventing a disease. |
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