RussianPatents.com
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Benzimidazole derivatives, compositions containing said derivatives, production and use thereof. RU patent 2374234. |
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FIELD: chemistry. SUBSTANCE: present invention relates to a compound of formula: which is N-{2-tert-butyl-1-[(4,4-diflurocyclohexyl)methyl]-1H-benzimidazol-5-yl}ethanesulfonamide and its pharmaceutically acceptable salt, their diastereomers, enantiomers or their mixture. The invention also relates to use of this compound in making a medicinal agent with modulator activity of CB1 receptors; to a pharmaceutical composition based on this compound; to a method of modulating CB1 receptors, based on use of effective quantities of this compound, as well as to a method of producing the compound described above. EFFECT: obtaining a new derivative of benzimidazole with useful biological activity. 8 cl, 1 tbl, 28 ex
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Heteroarylalkylcarbamate derivatives, their obtaining and their application as enzyme faah inhibitors / 2364586 Invention relates to novel compounds of general formula (I) , in which A is selected from one or several X and/or Y groups; X represents methylene group; Y represents C2-alkinylene group; n represent integer number from 1 to 5; R1 represents group R2, optionally substituted with one or several R3 and/or R4 groups; R2 represents group selected from pyridinyl, pyrimidinyl, pyridazinyl, imidazolyl, oxazolyl, pyrazolyl, isoxazolyl, oxadiazolyl, naphtyl, chinolinyl, isochinolinyl, dihydroisochinolinyl, 2-oxo-3,4-dihydrochinolinyl, indolyl, benzimidazolyl, pyrrolopyridinyl; R3 represents group selected from halogen atoms, groups C1-6-alkyl, C3-7-Cycloalkyl, C1-6-alkoxy, NR5R6 and phenyl; R4 represents group selected from groups: phenyl, naphtyl, pyridinyl; R4 group or groups can be substituted with one or several R3 groups, similar or different from each other; R5 and R6 independently on each other represent C1-6-alkyl group; R7 represents hydrogen atom or C1-6-alkyl group; R8 represents hydrogen atom or group C1-6-alkyl, C3-7-cycloalkyl, C3-7-Cycloalkyl- C1-3-alkylene; in form of base, acid-additive salt, hydrate or solvate. Invention also relates to methods of obtaining formula (I) compound by any of ii. 1-3, to compounds, determined by general formula (IV), (VII), to pharmaceutical composition, as well as to application of formula (I) compounds by any of ii. 1-3. |
Substituted n-[omega-azol-1-yl)alkyl]benzolsulfamides, methods of obtaining them and their application as antiagregants / 2339625 In substituted N-[ω-azol-1-yl)alkyl]benzolsulfamides , X and Y represent CH-group, n stands for 2 or 4, R - similar or different stand for alkyl group with number of carbon atoms from 1 to 4, perfluoralkyl group with number of carbon atoms from 1 to 4, perfluoralkoxy group with number of carbon atoms from 1 to 4, nitro group, alkoxycarbonyl group with number of carbon atoms from 1 to 4, and their salts, n stands for 3, R - similar or different stand for alkyl group with number of carbon atoms from 2 to 4, perfluoralkyl group with number of carbon atoms from 1 to 4, perfluoralkoxy group with number of carbon atoms from 2 to 4, alkoxycarbonyl group with number of carbon atoms from 1 to 4, and their salts, where X stands for CH-group, Y stands for nitrogen atom, n stands for 2, R - similar or different stand for alkyl group with number of carbon atoms from 2 to 4, perfluoralkyl group with number of carbon atoms from 1 to 4, perfluoralkoxy group with number of carbon atoms from 1 to 4, nitro group, alkoxycarbonyl group with number of carbon atoms from 1 to 4, and their salts, n stands for 3 or 4, R - similar or different stand for alkyl group with number of carbon atoms from 1 to 4, perfluoralkyl group with number of carbon atoms from 1 to 4, perfluoralkoxy group with number of carbon atoms from 1 to 4, nitro group, alkoxycarbonyl group with number of carbon atoms from 1 to 4, and their salts, where X and Y simultaneously are chain C-CH=CH-CH=CH-C constituting together annelated with heterocycle ring, n stands for whole number from 2 to 4, R - similar or different stand for alkyl group with number of carbon atoms from 1 to 4, perfluoralkyl group with number of carbon atoms from 1 to 4, perfluoralkoxy group with number of carbon atoms from 1 to 4, nitro group, alkoxycarbonyl group with number of carbon atoms from 1 to 4, and their salts, methods of their obtaining and application as anti-aggregation preparations. Anti-aggregation activity of N-[ω -azol-1-yl)alkyl]benzolsulfamides, of general formula I, for instance, hydrochloride of N-[4-(1H-triasol-1-yl)butyl]-n-methylbenzolsulfumide (35) is higher than of etalon dazoxyben. |
N3-alkylated benzimidazole derivatives as mek inhibitors / 2300528 Invention relates to N3-alkylated benzimidazole derivatives for preparing a drug used in inhibition of MEK activity. Invention describes benzimidazole compound of the formula (I): and its pharmaceutically acceptable salts and solvates wherein R1, R2, R9 and R10 are chosen independently from hydrogen atom, halogen atom, trifluoromethyl group, difluoromethoxy-, trifluoromethoxy-, azido-group, -OR3, -C(O)R3, -C(O)OR3, -OC(O)R3, (C1-C10)-alkyl, (C3-C10)-cycloalkyl, (C3-C10)-cycloalkylalkyl wherein each alkyl and cycloalkyl moiety is substituted possibly with groups in the amount from one to five and chosen independently from halogen atom, trifluoromethyl group, difluoromethoxy-, trifluoromethoxy-group; R3 is chosen from hydrogen atom, trifluormethyl group, (C1-C10)-alkyl, (C3-C10)-cycloalkyl, (C3-C10)-cycloalkylalkyl wherein each alkyl and cycloalkyl group is substituted possibly with groups in the amount from one to five and chosen independently from halogen atom, trifluoromethyl group, difluoromethoxy-, trifluoromethoxy-group, -C(O)R', -C(O)OR', -OC(O)R' wherein R' is chosen independently from hydrogen atom, lower alkyl; R4 represents independently hydrogen atom or (C1-C6)-alkyl; R6 is chosen from trifluoromethyl group or (C1-C10)-alkyl, (C3-C10)-cycloalkyl wherein each alkyl and cycloalkyl moiety is substituted possibly with groups in the amount from one to five and chosen independently from halogen atom, trifluoromethyl group, difluoromethoxy-, trifluoromethoxy-group, -C(O)R', -C(O)OR', -OC(O)R', -OR'; R7 is chosen from (C1-C10)-alkyl, (C3-C10)-cycloalkyl, (C3-C10)-cycloalkylalkyl wherein each alkyl and cycloalkyl moiety is substituted possibly with groups in the amount from one to five and chosen independently from halogen atom, trifluoromethyl group, difluoromethoxy-, trifluoromethoxy-group, -C(O)R3, -C(O)OR3, -OC(O)R3, -SO2R6, aryl, heteroaryl, arylalkyl, heteroarylalkyl, heterocyclyl and heterocyclylalkyl; W is chosen from -C(O)OR3, -C(O)NR3R4, -C(O)NROR3, -C(O)R4OR3, -C(O)(C3-C10)-cycloalkyl, -C(O)(C1-C10)-alkyl. Also, invention describes compositions used for inhibition of MEK activity, using such compounds for preparing a drug used in inhibition of MEK activity and preparing a drug used in cancer treatment. |
Derivatives of alpha-(n-sulfonamido)acetamide as inhibitors of beta-amyloid / 2300518 Invention relates to novel α-(N-sulfonamido)acetamides of the formula (I) or their optical isomers wherein values R1, R, R2 and R3 are given in the invention claim. Proposed compounds are inhibitors of production of β-amyloid peptide and can be used for inhibition of production of β-amyloid peptide. Also, invention relates to pharmaceutical composition based on these compounds and to a method for inhibition of production of β-amyloid peptide. |
Bicyclic derivatives of guanidine and their therapeutic using / 2282622 Invention relates to compounds of the general formula (I): wherein A means benzene ring optionally substituted with one or more the following groups: -OR2 wherein R2 mean linear or branched (C1-C5)-alkyl; X means -CH=, -CH2-, -N= or -NH-radical; Y means radical -CH2, oxygen or sulfur atom or group -NR7 wherein R7 means hydrogen atom or linear or branched (C1-C5)-alkyl; R1 means hydrogen atom, linear or branched (C1-C5)-alkyl, and to pharmaceutically acceptable salts also. Also, invention relates to a pharmaceutical composition showing anti-diabetic activity. The pharmaceutical composition comprises compound of the general formula (I) as an active component and an inert excipient. Invention provides bicyclic derivatives of guanidine eliciting anti-diabetic activity. |
4-phenylpiperidine derivatives as renin inhibitors / 2374228 Invention relates to new compounds of formula , where R1 is -O-X, where X is -(CH2)m-(CR9R10)p-(CH2)n-Z-(CH2)q-W, where m, n and q are independently equal to zero or assume values from 1 to 5; p equals 0 or 1; R9 and R10 are independently hydrogen, hydroxy, halogen, lower alkyl, lower alkoxy or cycloalkyl; or R9 and R10 together represent alkylene, which together with the carbon atom to which the are bonded, form an aryl; Z is a bond or O, W is aryl; R2 is hydrogen; L is a bond; R3 is hydrogen; R4 is hydrogen; R5 and R6 are independently hydrogen; R7 is hydrogen, halogen, hydroxy, trifluromethyl, lower alkyl, lower alkoxy, alkanoyl, alkyloxyalkoxy, alkanoyloxy, amino, alkylamino, dialkylamino, acylamino, carbamoyl, carboxy, alkoxycarbonyl; or R5 and R6 together represent -(CH2)1-2-; Y is -(CH2)r-, -O-(CH2)r, -(CH2)r-O-, where r equals zero or assumes values from 1 to 3; Q together with atoms to which it is bonded form an aryl, pyridyl, pyrimidinyl, thienyl, furyl, pyrroliyl or indolyl ring; or to its pharmaceutically acceptable salts. The invention also relates to a method of inhibiting rennin activity in mammals, to a pharmaceutical composition, as well as to application. |
Application of glutaric acid derivatives or their pharmaceutically acceptable salts as antiarrhythmic drug / 2373934 There is offered application of glutaric acid derivatives of general formula where R1 = imidazole, indole, R2 = COOH, H, or its pharmaceutically acceptable salt as an antiarrhythmic drug (versions), a medical product, a pharmaceutical composition and method of appropriate prescription. There is presented effectiveness of Nαglutaryl-L-histidine, Nαglutaryl-L-tryptophan in arrhythmia caused by adrenal heart rhythm disorder, in nicotine arrhythmia and acute occlusive myocardium disorder. |
Method for normalisation of thromboplastin formation in patients suffering from arterial hypertension with impaired glucose tolerance / 2373933 Invention refers to medicine, namely to cardiology and endocrinology, and concerns normalisation of thromboplastin formation in patients suffering from arterial hypertension with impaired glucose tolerance. That is ensured by integrated treatment including graduated static and dynamic physical exercises, and also introduction of pioglitazone in a dose 30 mg once in the morning and a lisinopril in a dose 10 mg once a day in the morning during 1.5 months. |
Method for correction of blood microvesicle level in arterial hypertension / 2373932 Invention refers to medicine, namely to haematology and cardiology, and concerns correction of blood microvesicle level in arterial hypertension. That is ensured by introduction of lisinopril in a dose 10 mg once in the morning and amlodipine in a dose 5 mg once in the morning within at least 5 weeks. Introduction of specific preparations throughout empirically specified time of treatment ensures complete normalisation of blood microvesicle level. |
Method for correction of blood microvesicle level in arterial hypertension with impaired glucose tolerance / 2373931 Invention refers to medicine, namely to haematology, cardiology and endocrinology, and concerns correction of blood microvesicle level in arterial hypertension with impaired glucose tolerance. That is ensured by integrated treatment including graduated physical exercises, and introduction of Fosinopril in a dose 10 mg once in the morning and pioglitazone in a dose 30 mg once in the morning. Therapeutic course is at least 7 weeks. |
Method for blood microvesicle correction in arterial hypertension and pancreatic diabetes type ii / 2373930 Invention concerns medicine, namely haematology, cardiology and endocrinology and concerns correction of blood microvesicle level in arterial hypertension (AH) and pancreatic diabetes type II (PD II). That is ensured by integrated therapy involving graduated physical exercises, as well as introduction of lisinopril in a dose 10 mg once in the morning, amlodipine in a dose 5 mg once in the morning and pioglitazone in a dose 30 mg once in the morning for therapeutic course at least 7 weeks. |
Benzofuran derivatives, compositions based on said derivatives and methods of treating cardiac arrhythmia / 2373199 Invention relates to new benzofuran derivatives of formula II or their pharmaceutically acceptable salts, where R1 is H or C1-C10 alkyl; R2 is H or C1-C10 alkyl; n ranges from 0 to 4; p ranges from 0 to 1; R3 and R4 represent H, as well as to pharmaceutical compositions based on said derivatives and methods of treating cardiac arrhythmia using these compositions. |
Application of composition consisting of concentrated cell population representing stem cells and undifferentiated precursors / 2372924 Invention relates to medicine, particularly to cardiology, and concerns treatments of cardiovascular diseases that is ensured by introduction of a composition containing stem cells and undifferentiated precursors prepared of adipose tissue by separating mature adipocytes and connective tissue. |
Hypolipidemic and antiatherosclerotic agent / 2372923 Invention concerns medicine, namely application of sodium thiosulphate as a hypolipidemic and antiatherosclerotic agent for oral introduction to treat dislipoproteinemia and atherosclerosis. |
Pharmaceutical composition with telmisartan sodium salt / 2372918 Invention refers to medical products and concerns a pharmaceutical tablet, contains a therapeutically effective dose of crystalline telmisartan sodium salt of fusion temperature 245±5°C and diuretic hydrochlorothiaside, as well as one or more adjuvants used to prepare medical products. There is also disclosed method for making thereof. According to the invention, the pharmaceutical tablets are storage-stable. |
Methods of treating prostate intraepithelial neoplasia with using herbal compositions / 2373948 Group of inventions refers to medicine, namely oncology and can be used for treating prostate intraepithelial neoplasia. The methods according to the invention involve introduction of a composition containing therapeutically effective amounts of supercritical extracts of rosemary, turmeric, origanum and ginger; and therapeutically effective amounts of water-alcohol extracts of holy basil, ginger, turmeric, Scutellaria baicalensis, rosemary, green tea, Polygonum cuspidatum, Coptis chinensis and barberry. |
Method of treatment tactics optimisation in case of hodgkin's lymphoma in children and teenagers / 2373836 Invention relates to medicine, in particular to oncology, and can be used for optimisation of treatment tactics in case of Hodgkin's lymphoma in children and teenagers. Method is realised in the following way. Such unfavourable prognostic factors as: age over 10 years, IV stage of disease, conglomerate dimensions more than 5 cm and/or value of mediastinal-thoracic index greater than 0.33, number of affected zones more than 4, symptoms of intoxication and biological activity of process. After that three risk groups are determined by the sum of detected unfavourable factors. In the first group, if 0-2 factors are detected, 2 cycles of polychemotherapy in accordance with regimen VBVP are carried out, in the second group, if 3-4 risk factors are detected - 4 cycles in alternating regimen VBVP-ABVD-VBVP-ABVD, in the third group, if 5-6 factors are detected - 6 cycles in alternating regimen VBVP-ABVD-VBVP-ABVD-VBVP-ABVD. Two weeks after carrying out polychemotherapy in all groups irradiation of all earlier affected zones is performed. |
Pyrrolotriazine compounds as kinase inhibitors / 2373209 New pyrrolotriazine derivatives of general formula (I) are described, where R1 is possibly substituted piperidinyl or piperazinyl; R2 is possibly substituted phenyl; R3 is hydrogen; X is -NH-; Y is -CH2-; as well as their pharmaceutically acceptable salts or steroisomers, and pharmaceutical compositions containing said compounds. |
Derivatives of imidazo[1,2-c]pyrimidinyl acetic acid / 2373208 Invention relates to new derivatives of imidazo[1,2-c]pyrimidinyl acetic acid of formula (I) or to its salts: , where R1 is ,, in which n is an integer ranging from 0 to 6; Y is aryl, where the said aryl is optionally substituted at a substitutable position with one or more substitutes selected from a group which consists of halogen or C1-6alkyl, optionally substituted with mono-, di- or trihalogen; R2 is hydrogen; R3 is hydrogen or halogen; and R4 is hydrogen. The invention also relates to derivatives of imidazo[1,2-c]pyrimidinyl acetic acid of formula (I-i) or to its salts, to a drug, to use of compounds in paragraph 1, as well as to a drug in form of a standard single dosage. |
Thermochemoradiation therapy of oesophageal cancer / 2372950 Invention concerns medicine, oncology, and can be used for thermochemoradiation therapy of oesophagus cancer. That is ensured by local transoesophageal hyperthermia, gamma-ray teletherapy and chemotherapy as preoperative actions. Herewith gamma-ray therapy is carried out within 2 weeks in average fractionation mode at 3 Gy 5 times a week to total focal dose 30 Gy. Chemotherapy accompanies the whole course of gamma therapy by daily introduction of fluorouracil dosed 300 mg/m2 to the central vein in continuous infusion mode and daily intravenous introduction of cisplatin dosed 6 mg/m2 daily within 1 hour. Hyperthermia is applied on 4th, 8th and 12th days of gamma therapy immediately before irradiation session at temperature 42-44°C within 60 minutes. |
Agent stimulating human leukaemia cell apoptosis (versions) / 2372919 Invention concerns medical products and covers applications of O- and S-glycosides 5-hydroxy-1,4-naphthoquinone (judlone) derivatives of formula 1 as an agent that stimulates human leukaemia cell apoptosis. Disclosed compounds selectively stimulate human leukemia cell apoptosis as comparrf with a prototype juglone without affecting normal cells of human immune system (neutrophils). |
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