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Organic chemistry (C07)

C
Chemistry; metallurgy
(64305)
C07
Organic chemistry
(12286)

C07B - General methods of organic chemistry; apparatus therefor (preparation of carboxylic acid esters by telomerisation c07c0067470000; processes for preparing macromolecular compounds, e.g. telomerisation c08f, c08g)
(152)
C07C - Acyclic or carbocyclic compounds (macromolecular compounds c08; production of organic compounds by electrolysis or electrophoresis c25b0003000000, c25b0007000000)
(4644)
C07D - Heterocyclic compounds (macromolecular compounds c08)
(5349)
C07F - Acyclic, carbocyclic, or heterocyclic compounds containing elements other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur, selenium or tellurium (metal-containing porphyrins c07d0487220000; macromolecular compounds c08)
(936)
C07G - Compounds of unknown constitution (sulfonated fats, oils or waxes of undetermined constution c07c0309620000)
(18)
C07H - Sugars; derivatives thereof; nucleosides; nucleotides; nucleic acids (derivatives of aldonic or saccharic acids c07c, c07d; aldonic acids, saccharic acids c07c0059105000, c07c0059285000; cyanohydrins c07c0255160000; glycals c07d; compounds of unknown constitution c07g; polysaccharides, derivatives thereof c08b; dna or rna concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification c12n0015000000; sugar industry c13)
(384)
C07J - Steroids (seco-steroids c07c)
(220)
C07K - Peptides (peptides containing -lactam rings c07d; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, c07d; ergot alkaloids of the cyclic peptide type c07d0519020000; genetic engineering processes for obtaining peptides c12n0015000000)
(1698)

Bispecific antibodies

Bispecific antibodies

Invention relates to field of biotechnology and immunology and represents method for production of bispecific antibody, which contains: a) heavy chain and light chain of first full length antibody, which specifically binds with first antigen; and b) heavy chain and light chain of second full length antibody, which specifically binds with second antigen, where N-end of heavy chain is bound with C-end of light chain via peptide linker, with each of CH3-domain of heavy chain of full length antibody a) and CH3-domain of heavy chain of full length antibody b) being found on contact surface, which includes changes in initial contact surface of CH3-domains of antibody; wherein changes in CH3- domains of heavy chains represent changes of "key-lock" type; wherein said method includes the following stages: a) transformation of host-cell with vectors, containing nucleic acid molecules, coding said molecule of bispecific antibody; b) cultivation of host cell under conditions, providing synthesis of said molecule of bispecific antibody; and c) isolation of said molecule of bispecific antibody from said culture.

Conjugated factor viii molecules

Conjugated factor viii molecules

Invention relates to field of biotechnology, namely to obtaining B-domain truncated factor VIII molecule and covalently conjugated with hydrophilic polymer, which has altered half-life in bloodstream, and can be used in medicine to treat haemophilia. Molecule of precursor of B-domain truncated factor VII, where B-domain corresponds to amino acids 741-761 from SEQ ID NO 2, is obtained. Said molecule is covalently conjugated with PEG or polysaccharide with size 10-80 kDa by means of O-linked oligosaccharide at serine residue in truncated B-domain, which corresponds to amino acid 750 in SEQ ID NO 2.

Polyvinyl chloride plasticiser

Polyvinyl chloride plasticiser

Invention relates to preparation of a polyvinyl chloride plasticiser, which contains as the basic component phthalates - benzyloxypropylbenzyl phthalates of formula given below.

Conversion of glycolaldehyde with amination agent

Conversion of glycolaldehyde with amination agent

Invention relates to improved method for converting glycolaldehyde with amination agent in presence of hydrogen, catalyst and solvent. Catalyst is activated by reduction of catalyst precursor or by reduction of passivated catalyst and glycolaldehyde is brought in contact with activated catalyst. To carry out the process activated catalyst is used during and after reduction before bringing into contact with glycolaldehyde under inert conditions. Catalyst contains less than 0.4 mol % of atoms of noble metal, selected from the group, consisting of ruthenium, rhodium, palladium, silver, rhenium, osmium, platinum, gold and mercury. As catalytically active components catalyst precursor contains one or several oxides of metals Ni, Co and/or Cu. Conversion is carried out at temperature from 15 to 350°C under pressure from 10 to 350 bar. Tetrahydrofurane or water is a preferable solvent. Activated catalyst, possessing reduction degree of 30% or higher, is usually used for the process. Activated catalyst, obtained by reduction of passivated catalyst, after activation possesses reduction degree, at least by 2% higher than reduction degree of passivated catalyst.

Isoindolinone-based phosphatidylinositol-3-kinase inhibitors

Isoindolinone-based phosphatidylinositol-3-kinase inhibitors

Invention refers to pharmaceutically acceptable compositions containing the above compounds, and to methods for using the compositions for treating various diseases, conditions or disorders.

Method for obtaining terephthalic acid

Method for obtaining terephthalic acid

Invention relates to method for obtaining terephthalic acid, which includes obtaining flow of virtually pure p-toluic acid, containing 80 wt % or more of p-toluic acid; contact of flow of virtually pure p-toluic acid, solvent, containing more than 5 wt % of ionic liquid, boron source, catalyst and oxidiser to obtain product, which contains terephthalic acid.

Method and system for obtaining petrol or dimethyl ether

Method and system for obtaining petrol or dimethyl ether

System for obtaining petrol or dimethyl ether from natural gas with intermediate methanol synthesis includes: device (10) for steam natural gas reforming for obtaining reforming gas; heat exchanger (17) of flue gas-steam type for obtaining steam or heat, used in system, by recovery of heat of flue gas, formed in combustion zone (12) of steam reforming device (10); methanol synthesis device (20) from reforming gas, obtained in device for steam reforming; heat exchanger (19) of reforming gas-steam type, intended for obtaining steam or heat, used in system, by recovery of reforming gas heat before supply of reforming gas into methanol synthesis device (20); device (30) for synthesis of petrol or dimethyl ether from methanol, synthesised in methanol synthesis device, and device, selected from the group, and a series of heat exchanges as shown in the invention formula. Signs, effecting total energy balance of system, are formulated for system.

Method for obtaining olefin c<sub>3</sub> in installation for fluid catalystical cracking

Method for obtaining olefin c3 in installation for fluid catalystical cracking

Method includes the following stages: (a) cracking of hydrocarbon raw material in riser, which works in temperature range from 500°C to 625°C in presence of fluidised solid microspheric cracking catalyst to obtain hydrocarbon products; (b) separation of coke-loaded waste catalyst from hydrocarbon products and its stripping in stripping column to remove hydrocarbons, trapped inside catalyst pores; (c) burning coke sediments on waste catalyst in regenerator; (d) recirculation of part of hot regenerated catalyst in stripping column with support of temperature in stripping column in the range from 550°C to 650°C and recirculation of remaining part of hot regenerated catalyst into lower part of riser; (e) pumping hydrocarbon fraction C4, separated from cracking products, by selection with external stream of hydrocarbon C4 into stripping column, with coke on circulating catalyst in stripping column constituting from 0.3 to 1 wt %, and WHSV value of WHSV being in the range from 5 to 50 hour-1. Application of claimed invention increases activity of catalyst inside stripping column. Direct pumping of regenerated catalyst into stripping column in addition to increase of propylene output increases stripping efficiency, which leads to increase of extraction of hydrocarbons removed by stripping.

Arylethinyl derivatives

Arylethinyl derivatives

Invention refers to a new ethinyl derivative of formula I in the form of a racemic mixture or respective enanthiomer and/or optic isomer and/or stereoisomer or to a pharmaceutically acceptable salt of the above compounds formed by acid addition. The compounds are allosteric modulators of metabotropic glutamate receptor subtype 5 (mGluR5) and can find application in treating diseases mediated by mGluR5 action, wherein a disease is schizophrenia, cognitive disorders, fragile X syndrome or autism. In formula I

Carbodiimide-based adhesion promoter, adhesion promoter-containing water resorcinol-formaldehyde latex dispersion, fibres with improved adhesion, adhesion promoter compositions, methods of obtaining and application thereof

Carbodiimide-based adhesion promoter, adhesion promoter-containing water resorcinol-formaldehyde latex dispersion, fibres with improved adhesion, adhesion promoter compositions, methods of obtaining and application thereof

Invention relates to adhesion promoter based on carbodiimides, adhesion promoter-containing water resorcinol-formaldehyde latex dispersion, fibres with improved adhesion, compositions of adhesion promoter, methods of obtaining and application thereof for improvement of adhesion in tyres. Carbodiimide is selected from group of formula and/or compounds, where R stands for C1-C18-alkylene, C5-C18-cycloalkylene, arylene and/or C7-C18-aralkylene and j inside molecule are similar or different and have value from 1 to 5, and p stands for 0-500, which is superficially deactivated by exchange reaction with at least one amine, selected from group, including multifunctional primary and secondary amines.

Method of obtaining product from gaseous reagent in suspended layer

Method of obtaining product from gaseous reagent in suspended layer

Method includes feeding a gaseous reagent as gaseous raw material or portion of gaseous raw material with reduced gas flow rate at the input of at least 0.5 m/s into a vessel containing an extended suspended layer of solid catalyst particles, which are suspended in a suspension liquid, such that the gaseous reagent can bubble upwards through the suspended layer, wherein the suspended layer contains a catalyst charge which makes up at least 20 vol % evacuated suspension, catalytic reaction of the gaseous reagent at a pressure higher than atmospheric pressure as bubbles of the gaseous reagent bubble upwards through the suspended layer to form a product, and removing the product and the unreacted gaseous reagent from the vessel.

Peptide produced of human lactoferrin applicable as antigen masking agent

Peptide produced of human lactoferrin applicable as antigen masking agent

Invention refers to biochemistry, particularly to using a peptide produced of human lactoferrin as a masking agent. What is also disclosed is a method for producing a pharmaceutical composition.

Production of pellets containing one or several complexing agent salts

Production of pellets containing one or several complexing agent salts

Invention relates to production of pellets. The latter contain one or several complexing agent salts of general formula (I) from initial water solution. The latter includes one or several complexing agent salts in concentration of 10-80 wt % per total weight of said initial water solution. Claimed process is implemented in the vortex appliance. Central or one or several gaseous jets directed from bottom to top in the area of the appliance of central axis develop the inner loop-like motion to create a vortex zone. Flowing zone adjoins the end of aforesaid the aforesaid zone to change over to reverse motion zone in the area of vortex appliance walls. The latter changes over in its lower zone into vortex zone whereto the initial water solution id injected into one or several gaseous flowing jets. Here, it is dried to get the pellets to be discharged from said appliance. R′ in formula (I) stands for hydrogen atom or one groups or . Note also that R′′ stands for hydrogen atom, alkyl residue with 1-12 atoms of carbon or residue -(CH2)q-COOM, where q = 1-5, n and m are integer equal to 0-5. UR'′′ stands for hydrogen atom or alkyl residue with 1-12 carbon atoms, or olefin residue with 2-12 carbon atoms that can contain up to 5 hydroxyl groups as substituent, or one of groups -(CH2)0-CO2M or wherein o and p are integers equal to 0-5, M stand for hydrogen atom, alkaline metal, alkali-earth metal, ammonium ion and substituted ammonium ion in appropriate stoichiometric amounts.

New octahydrothienoquinoline derivative, pharmaceutical composition containing derivative, and using them

New octahydrothienoquinoline derivative, pharmaceutical composition containing derivative, and using them

Invention refers to compounds presented by general formula (I) and their pharmaceutically acceptable salts. The compounds of the invention possess activity of D2 receptor agonist. In general formula (I) R1 represents a cyano group; each R2 and R3 independently represents a hydrogen atom, C1-6alkyl group, C1-7acyl group or (C1-6alkoxy)-C(O)-; R4 represents a hydrogen atom, C1-6alkyl group or halogen-C1-6alkyl group; the other radicals are presented in the patent claim. The invention also refers to individual compounds and pharmaceutical compositions containing an effective amount of the compound of the invention.

Novel naphthyridine derivatives and thereof application as kinase inhibitors

Novel naphthyridine derivatives and thereof application as kinase inhibitors

Invention relates to naphthyridine derivatives of general formula I in which R1-R6 substituents have the following values: R1 represents NR7R8, R2 represents hydrogen, and R3 represents hydrogen, where R7 represents hydrogen, and R8 can represent -C(Y)NR9R10, where Y represents O, S, and R9 hydrogen and R10 can represent (i) non-substituted saturated C1-6-alkyl, possibly substituted with non-substituted C6-aryl, (ii) non-substituted C6-aryl, R4 represents hydrogen, R5 can represent (i) C6-aryl, substituted with saturated C1-6-alkoxy or hydroxyl, (ii) C5-heteroaryl, containing 2 nitrogen atoms, substituted with saturated C1-6-alkyl, (iii) NR15R16, where R15 represents hydrogen, and R16 represents C6-aryl, substituted with saturated C1-6-alkoxy, and R6 represents hydrogen; and their physiologically acceptable salts, which are kinase modulators.

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods for producing and using them

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods for producing and using them

Invention refers to a prodrug composition for treating diseases, disorders or conditions mediated by opioid binding to opioid receptors, containing a conjugate representing 3,6-diaspirin-hydromorphone in a pharmaceutically effective amount, and a biologically acceptable carrier. The invention also refers to a method of treating a patient suffering a disease, disorder or condition mediated by opioid binding to opioid receptors.

Stable aqueous acrylamide solution

Invention relates to an aqueous acrylamide solution for producing an acrylamide polymer, which contains acetaldehyde in concentration of 1.5 mg/kg acrylamide to 4 mg/kg acrylamide for stabilising the aqueous acrylamide solution. The invention also relates to a stabilised aqueous acrylamide solution and a method of stabilising an aqueous acrylamide solution.

Novel polymorphs and salts

Novel polymorphs and salts

Invention relates to novel crystalline polymorph (form II) of 1-(3′,4′-dichloro-2-fluorobiphenyl-4-yl)cyclopropanecarboxylic acid, which is characterised by X-ray powder diffraction pattern, including characteristic peaks, expressed by the following values of angle 2-theta ± 0.2: (°2Θ) 17.22, 19.14, 19.23, 20.34, 24.17 and 25.02; or to crystalline polymorph (form II) of 1-(3′,4′-dichloro-2-fluorobiphenyl-4-yl)cyclopropanecarboxylic acid, which is characterised by X-ray powder diffraction pattern, which includes characteristic peaks, expressed by the following values of angle 2-theta ± 0.2: (°2Θ) 16.41, 17.09, 17.22, 17.78, 19.14, 19.23, 20.34, 24.17, 24.76, 25.02, 28.88, 26.11, 28.00, 28.52, 28.95, 29.21, 29.99 and 30.82. Invention also relates to salt of 1-(3′,4′-dichloro-2-fluorobiphenyl-4-yl)cyclopropanecarboxylic acid, selected from the group, consisting of salts of L-arginine, D-arginine and L-lysine, and to application of said crystalline polymorph and salt for prevention or treatment of Alzheimer's disease.

Crystalline forms of 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-{ 6-[4-(4-ethylpiperazin-1-yl)-phenylamino]-pyrimidin-4-yl} -1-methylurea and its fractions

Crystalline forms of 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-{ 6-[4-(4-ethylpiperazin-1-yl)-phenylamino]-pyrimidin-4-yl} -1-methylurea and its fractions

Invention relates to novel hydrated and anhydrous crystalline forms, as well as to amorphous form of 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-{6-[4-(4-ethylpiperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methylurea of formula (I) and its monophosphoric and hydrochloride salt. Compounds possess properties of inhibitors of activity of kinase, selected from the group, including FGFR1, FGFR2, FGFR3, FGFR4, KDR, HER1, HER2, Bcr-Abl, Tie2 and Ret, and can be used in treatment of diseases, mediated by activity of said kinases. Diseases are selected from the group, including carcinoma of kidneys, liver, adrenal glands, urinary bladder, mammary gland, stomach, ovaries, large intestine, rectum, prostate, pancreas, lungs, vagina or thyroid gland; sarcoma, glioblastoma, leukaemia; tumours of head or neck; psoriasis; prostate gland hyperplasia or neoplasia In particular invention relates to anhydrous crystalline form of formula (I) compound and its monohydrate; to salt of phosphoric acid of formula (I) compound, its anhydrous crystalline forms A and B and its amorphous form; crystalline hydrochloride dehydrate. Crystalline form s are characterised by respective data of powder radiograph, indices of thermogram of differential scanning calorimetry, characteristic peaks of Raman scattering Invention also relates to method for obtaining anhydrous crystalline form A of monophosphoric acid salt.

Process for acetic acid production

Process for acetic acid production

Invention relates to method of obtaining acetic acid, which includes stages: (a) methanol carbonylation in presence of catalyst in reaction zone with obtaining reaction mixture (A), which contains acetic acid, methylacetate, methyliodide, catalyst and water; (b) separation of , at least, part of reaction mixture (A) in stripping zone to obtain catalyst-containing liquid flow (BL) and steam flow (BV), which contains acetic acid, methylacetate, methyliodide and water, and output of steam flow (BV) from stripping zone; (c) separation of steam flow in fractioning zone to obtain product flow (CP), which contains acetic acid and insignificant quantity of water, and main distillate (CO), which contains acetic acid, methylacetate, methyliodide and water; (d) condensation of main distillate (CO) and formation of liquid mixture (D) with content of water not higher than 10 wt %, content of acetic acid, at least, 10 wt %, which also contains methyliodide, at least 20 wt %, and methylacetate, at least, 5 wt %, (e) separation of liquid mixture (D) in separation zone to obtain acetic acid and water of light water phase (DA) and heavy organic phase (DO), which contains methyliodide and methylacetate. Reduction of separation time at reduction of liquid mixture temperature to level from 0 to 35°C is realized, and at correction of weight ratio of methyliodide to methylacetate to weight ratio of methyliodide and methylacetate, at least, 1.5:1. Invention also relates to acceleration of separation of liquid mixture phases, which contains, at least, 10 wt % of acetic acid, at least 5 wt % of methylacetate, at least, 20 wt % of methyliodide and not more than 10 wt % of water, where said acceleration is realised due to the following stages: (a) reduction of temperate of liquid mixture to level from 0 to 35°C and (b) correction of weight ratio of methyliodide to methylacetate in liquid mixture to weight ratio of methyliodide to methylacetate, at least, 1.5:1.

Derivatives of (4-methylsulphonylaminophenyl)-quinoline, useful in treatment of hepatitis c

Derivatives of (4-methylsulphonylaminophenyl)-quinoline, useful in treatment of hepatitis c

Invention relates to field of organic chemistry, namely to compound, selected from the group of N-{4-[7-tert-butyl-8-methoxy-5-(2-oxo-1,2-dihydro-pyridin-3-yl)-quinolin-2-yl]phenyl}-methanesulphonamide; N-{4-[7-tert-butyl-8-methoxy-5-(6-methyl-2-oxo-1,2-dihydro-pyridin-3-yl)-quinolin-2-yl]-phenyl}- methanesulphonamide; and N-{4-[7-tert-butyl-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-8-methoxy-quinolin-2-yl]-phenyl}- methanesulphonamide; or to its pharmaceutically acceptable salt. The invention also relates to application of said compound for treatment or prevention of infection with hepatitis C virus (HCV) and for manufacturing thereof based medication.

Method for depolymerisation of polysulphides and obtaining bismercaptodiethers

Method for depolymerisation of polysulphides and obtaining bismercaptodiethers

Invention relates to method for obtaining bismercaptodiether of formula HS-R1-O-C(R2)H-O-R1-SH, in which R1 represents linear, branched or cyclic alkylene group, containing from 1 to 6 carbon atoms, or arylene group and R2 represents hydrogen atom, linear, branched or cyclic alkyl group, containing from 1 to 6 carbon atoms, or aryl group by interaction of polysulphide with the following structure: R3-S-[S-R1-O-C(R2)H-O-R1-S]n-S-R3 , in which each R3 is independently selected from alkyl groups, etheralkyl, aryl ad alkaryl groups, containing from 1 to 6 carbon atoms and having terminal -SH and -OH groups, and n is in the interval from 1 to 100, with monothiol of formula R4-SH, in which R4 represents linear or branched alkyl, aryl or alkaryl group, optionally substituted with heteroatoms, in presence of base, where base has pKa index higher than monothiol pKa index, as determined in water solution at 25°C, as well as to method for polysulphide obtaining.

Method of synthesising nucleic acids, modified by phosphorus atom

Method of synthesising nucleic acids, modified by phosphorus atom

Invention relates to a method of synthesising nucleic acid, containing a chiral X-phosphonate constituent, which can be used in the pharmaceutical industry. The claimed method includes the reaction of a molecule, which contains an achiral H-phosphonate constituent, a chiral agent, a condensing reagent, which activates the molecule, containing the achiral H-phosphonate constituent for the reaction with the said chiral reagent, and nucleoside, containing a 5'-OH constituent, with obtaining a condensed intermediate compound, and conversion of the said condensed intermediate compound into nucleic acid, which contains the chiral X-phosphonate constituent.

Novel crystalline acid-addition salts of tricyclic derivative or their hydrates and method for thereof obtaining

Novel crystalline acid-addition salts of tricyclic derivative or their hydrates and method for thereof obtaining

Invention relates to novel crystalline acid-addition salt of tricyclic derivative in form of its hydrate, represented by the following chemical formula 2: , method for thereof obtaining, and based on its pharmaceutical composition for prevention and treatment of diseases, caused by PARP overactivity.

Tetrahydrocarboline derivative

Tetrahydrocarboline derivative

Claimed invention relates to field of organic chemistry, namely to novel heterocyclic compounds of general formula (I) and to its pharmaceutically acceptable salt or its solvate, where R1 represents halogen atom, C1-4 alkyl group, C1-4 alkoxygroup, C1-4 halogenalkyl group, cyanogroup, carbamoyl group, R2 represents hydrogen atom, R3 represents C1-4 alkyl group, R4 represents hydrogen atom or C1-4 alkyl group, ring A represents (i) C3-6 monocyclic carbon ring, including phenyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cyclohexene, (iii) 5-6-membered monocyclic heterocyclic ring, containing one-two heteroatoms, selected from oxygen atom, nitrogen atom and sulphur atom, including thiophene, furan, isoxazole, imidazole, pyrazole, thiazole, pyridine or (iv) 9-membered bicycic heterocyclic ring, including indole, X represents nitrogen atom or carbon atom, T represents bond or linear C1-4 alkylene group, C2-4 alkenylene group or C2-4 alkinylene group, optionally substituted with two R5 (where R5 represents C1-4 alkyl group or aminogroup), U represents (i) methylene group, (ii)oxygen atom, (iii) -NR6- (where R6 represents hydrogen atom or methyl group) or (iv) 3-6-membered monocycle, including cyclobutane, cyclopentane, cyclohexane, phenyl, thiophene, pyrrolidine, pyrazole, imidazole, triazole, oxazole, piperazine, piperidine, tetrahydropyridine C7-8 bridge carbon ting, including bicyclooctane, bicycloheptane and imidazolidine, optionally substituted with one-three R7 (where R7 represents halogen atom, C1-4 alkyl group; hydroxygroup, C1-4 alkoxygroup or benzyloxy group), Y represents (i) bond or (ii) linear C1-3 alkylene group, optionally substituted with one or two R8 (where R8 represents methyl group), W represents bond or linear C1-3 alkylene group; Z represents methylene group, oxygen atom or sulphur atom, q represents integer number 1, r represents integer number from 0 to 5, and t represents integer number from 0 to 2, on condition that groups, represented by set R1, R2, R3, R5, R7 and R8, can be similar or different, respectively, and two R3 or R5, bound with one and the same carbon atom, can be taken together with carbon atom with formation of C3cycloalkyl, respectively. Invention also relates to pharmaceutical composition, pharmaceutical preparation and ENPP2 inhibitor, based on formula (I) compound.

Cycloalkyl-substituted imidazole derivative, possessing inhibiting activity with respect to tafia

Cycloalkyl-substituted imidazole derivative, possessing inhibiting activity with respect to tafia

Invention relates to field of organic chemistry, namely to novel imidazole derivative of general formula , or to its pharmacologically acceptable salt, where A represents group: , where * represents position for substitution; R1, R2 and R3, each represents hydrogen atom; R4 represents hydrogen atom or prodrug group; and Y represents group: -CH2-CHR5-CH2-NHR6 (where R5 represents hydrogen atom or C1-C6alkyl group, and R6 represents hydrogen atom or prodrug group), -O-CHR7-CH2-NHR8 (where R7 represents hydrogen atom C1-C6alkyl group, and R8 represents hydrogen atom) or , (where R9 represents hydrogen atom, and * represents position for substitution); where prodrug group, represented by R4, represents [(isopropoxycarbonyl)oxy]ethyl group or C1-C6alkyl group, which is substituted with one phenyl group; and where prodrug group, represented by R6, represents C1-C6alkanoyl group, which is substituted with one or two similar or different groups, selected from aminogroup and phenyl group; (C1-C6alcoxy)carbonyl group; substituted with one group, selected from C2-C6alkanoyloxy group and (C3-C6cycloalkyl)carbonyloxy group; or 1,3-dioxol-methoxycarbonyl group, substituted with two different groups, selected from oxogroup and C1-C6alkyl group. Invention also relates to particular compounds and salts, TAFIa inhibitor, fibrinolysis promoter, pharmaceutical composition and preventive or therapeutic medication based on formula (I) compound, as well as to intermediate compounds of formulae , and .

Method for obtaining linoleic acid

Method for obtaining linoleic acid

Invention relates to field of chemistry and can be applied in medicine as marker in research of liver and myocardium metabolism. Method for obtaining linoleic acid includes obtaining 7-chloroheptanoic acid methyl ether or 7-iodineheptanoic acid methyl ether, condensation of 1-chloroundecaine-2,5 with 7-chlorheptanoic acid methyl ether or with 7-iodineheptanoic acid methyl ether, and hydration of obtained methyl ether of octadiin-9,12-oic-1 acid with further saponification of obtained octadiin-9,12-oic-1 acid methyl ether to octadecadien-9,12-oic-1 acid (linoleic acid), with stages of reaction of obtaining methyl ethers, reaction of condensation in presence of magnesium and reaction of hydration in presence of palladium catalyst being carried out in field of ultrasonic radiation with power 300 W and frequency 22 kHz.

Method of producing palladium catalyst for hydrogenating acetylene

Method of producing palladium catalyst for hydrogenating acetylene

Catalyst is produced by dissolving a palladium catalyst in supercritical carbon dioxide in the temperature interval of 305-353 K, followed by deposition on an alumina substrate. The palladium complex used is palladium hexafluoroacetylacetonate and dissolution thereof in supercritical carbon dioxide is carried out at pressure of 8-8.5 MPa.

Method of producing carboxy-substituted glycopeptides of glycyrrhizic acid

Method of producing carboxy-substituted glycopeptides of glycyrrhizic acid

Invention relates to a method of producing glycyrrhizic acid derivatives of formula I: , which are suitable for use in chemical industry. In the disclosed method, compounds of general formula I are obtained by treating glycyrrhizic acid (GA) with N-hydroxybenzotriaozole (HOBt), carbodiimide and an amine component (AC) with molar ratio of reactants GA/HOBt/AC/carbodiimide, equal to 1/3.5-4.0/3.5-4.0/3.5-4.0 mmol at room temperature in N,N′-dimethyl formamide in the presence of N-ethyl morpholine, wherein the carbodiimide used is 1-(3-dimethylaminopropyl)-3-ethyl carbodiimide hydrochloride, the amine component is hydrochlorides of amino acid esters of formula R1NH2·HCl, where R1=C6H5CH2CH(COOCH3)-, HOC6H4CH2CH(COOCH3)-, (CH3)2CHCH2CH(COOCH3)-, CH3CH2CH(CH3)CH(COOCH3)-, (CH3)2CHCH(COOCH3)-, CH3SCH2CH2CH(COOCH3)-, C6H5CH2SCH2CH(COOC(CH3)3-, where the process takes place in a single step for 10-12 hours.

Indium oxoalkoxides for obtaining indium oxide-containing layers

Indium oxoalkoxides for obtaining indium oxide-containing layers

Invention relates to halogen-containing indium oxoalkoxide of general formula In7O2(OH)(OR)12X4(ROH)x, in which R stands for alkyl with 1-15 carbon atoms, X stands for fluorine, bromine, iodine and x stands for number from 0 to 10 Also method of obtaining halogen-containing indium oxoalkoxide and thereof application are claimed.

Steam system

Steam system

Set of inventions relates to the steam system to be used in production of olefins. The steam system comprises low-pressure feed water degasifier (16). Its working pressure first level (P1) is higher than barometric pressure P1>1 bar. The working pressure of the system low-pressure steam line (22) features the second pressure level (P2). Note here that the second pressure level is higher than the first one P2>P1. The steam system comprises also high-pressure steam line (38) with working pressure featuring the third pressure level P3. Note here that the third pressure level is higher than the second one P3>P2. Claimed system comprises between the high pressure steam line (38) and the degasifier (16) at least one steam turbine (40) to expand the steam of the high pressure steam line (38) from (P3) to (P1).

Method for alkylaromatic compound oxidation

Method for alkylaromatic compound oxidation

Invention refers to a method for alkylaromatic compound oxidation involving alkylaromatic compound oxidation for producing a first oxidation product; contacting a portion of the first oxidation product, a solvent containing ionic liquid and carboxylic acid, wherein the ionic liquid content makes more than 5 wt %, a catalytic promoter containing a bromine source, a catalyst and an oxidising agent, for producing a second oxidation product containing at least one of the following compounds: aromatic alcohol, aromatic aldehyde, aromatic ketone and aromatic carboxylic acid.

Inhibitors of catechol-o-methyltransferase and thereof application in treatment of psychic disorders

Inhibitors of catechol-o-methyltransferase and thereof application in treatment of psychic disorders

Claimed invention relates to novel compounds of 4-pyrimidinone of structural formula I and II, which possess properties of catechol-O-methyltransferase (COMT) inhibitor. Compounds can be applied in treatment and prevention of neurological, psychic disorders and diseases, which COMT fragment is involved in, such as negative and positive symptoms of schizophrenia, depression, depressive phase of bipolar disorder, diseases, associated with DA deficiency, such as ADD/ADHD, and addiction, such as opiate, drug and tobacco-addiction, as well as against growth of weight/sense of hunger, associated with cessation of smoking of use of antipsychotics. In formula and compounds A represents hydrogen or C1-6alkyl; X represents hydrogen or halogen; R1 represents phenyl or heterocyclyl, selected from 6-membered unsaturated heterocyclyl with one nitrogen atom in cycle, where said phenyl and heterocyclyl is substituted with 1-3 groups Ra; R2 represents C1-6alkyl, N(CH3)2, (CH2)nC5-10heterocyclyl, (CH2)nC6-10aryl, where said aryl and heterocyclyl is optionally substituted with 1-2 groups Ra; Ra represents halogen, C2-4alkinyl, (CH2)nCF3, CN, NHSO2R2, OR2, (CH2)nC5-10heterocyclyl, containing 1-2 nitrogen atoms and possibly additionally oxygen or sulphur atom in ring, (CH2)nC6aryl, O(CH2)nC6aryl, where said aryl represents phenyl, where said alkinyl, heterocyclyl and aryl is optionally substituted with 1-3 groups Rb; Rb represents C1-6alkyl, OC1-6alkyl, halogen, CHF2, OCHF2, -O-, (CH2)nC6aryl, (CH2)nC5heterocyclyl, containing 3 heteroatoms in cycle, selected from nitrogen and oxygen, OR2, (CH2)nCF3, where said heterocycle is optionally substituted with 1 or several C1-6alkyls; and n equals 0-1.

Peptide

Invention refers to peptides specified in FSY or FTY for treating or preventing a condition, in which angiotensin converting enzyme (ACE) inhibition is effective, and their pharmaceutical compositions.

Kibdelos porangium extracts as antibacterial agents

Kibdelos porangium extracts as antibacterial agents

Invention refers to an antibacterial composition containing one or more refined compounds specified in compounds of formula:

Crystalline ingenol mebutate

Crystalline ingenol mebutate

Invention relates to novel crystalline form of ingenol mebutate, characterised by FTIR-ATR spectrum, demonstrating peaks in spectrum of frustrated total internal reflection with frequencies at 3535, 2951, 1712, 1456, 1378, 1246, 1133, 1028 and/or 956 cm-1 (±3 cm-1), and curve of which, obtained by means of differential scanning calorimetry, demonstrates jump at temperature 153±5°C, as well as to methods of its obtaining and its application for treatment of skin lesions.

Novel heterocycles

Novel heterocycles

Invention relates to application of formula (I) compound, for preparation of medication, used for treatment of chronic obstructive pulmonary disease. In compound (I) A represents aryl group, selected from phenyl; B represents aryl group, selected from phenyl or pyridyl; X represents carbon atom or nitrogen atom; R represents substituted or non-substituted groups, selected from heteroaryl groups, including pyridyl, thienyl, furyl, pyrrolyl, pyrazolyl, oxazolyl, thiazolyl, imidazolyl, thiadiazolyl, triazolyl, tetrazolyl, pyrimidinyl and pyrazinyl, and heterocyclic groups, including morpholine, thiomorpholine, piperazine, piperidine, piperidin-4-one, pyrrolidine, pyrrole-2,5-dione, thiazolidine, 1-oxido-thiazolidine and 1,1-dioxido-1,3-thiazolidine; where heterocyclic group is optionally substituted with substituents, independently selected from substituted or non-substituted (C6)aryl, -CH2-C6aryl, -CH2-heteroaryl, CO-C6aryl, -CO-heteroaryl, -CS-heteroaryl, -CO-C3-6cycloalkyl, cyano(C1-4)alkyl, -O-methyloxime, -SO2Cl, formyl, or other substituted or non-substituted heterocyclic group, selected from pyridyl, pyrimidinyl and piperidinyl; where binding of heterocyclic group to pyrimidine ring takes place through carbon or nitrogen atom; and where group R or substituent of heterocyclic group R are optionally substituted. Other substituents are given in invention formula.

Phenyloxadiazole derivatives as pgds inhibitors

Phenyloxadiazole derivatives as pgds inhibitors

Invention relates to compounds of formula (I), where R1 is hydrogen or C1-C6alkyl; R2 is hydrogen and R3 is hydroxy(C1-C6)alkyl; or pharmaceutically acceptable salts thereof. The invention also relates to methods of producing compounds of formula (I), intermediate compounds given in paragraphs 14-19 of the claim, and a method of producing an intermediate compound according to paragraph 17 of the claim.

Substituted pyridine compound

Substituted pyridine compound

Invention relates to compound of general formula

Spatially hindered amines

Spatially hindered amines

Invention relates to compound of formula stabilised composition with thereof application, method for stabilisation of natural or synthetic organic polymer against destruction, caused by light, heating or oxidation, as well as to application of formula (A) compound for stabilisation of natural or synthetic organic polymer against thermal, oxidative or light destruction. In formula (A) R1 independently on each other represent methyl, ethyl or n-propyl, and X represents C2-C8alkylene or C2-C8alkylene, containing sulphur atom in chain.

Method for separation by absorption of pyrolysis gas produced from lower olefin hydrocarbons

Method for separation by absorption of pyrolysis gas produced from lower olefin hydrocarbons

Invention is referred to method for separation by absorption of pyrolysis gas produced from lower olefin hydrocarbons, wherein primary and secondary absorbing agents are supplied to demethaniser in order to separate by absorption raw material of demethaniser by conunterflow contacting at moderate temperature and pressure, at that the above raw material is supplied to the medium or lower part of demethaniser, the above primary absorbing agent is supplied only to the medium part of demethaniser or to the medium and lower part of demethaniser simultaneously, the above secondary absorbing agent is supplied only to the upper part of demethaniser. At that the above primary absorbing agent and secondary absorbing agent are supplied to demethaniser with ratio of total flow rate of the first agent to the second one in the range from 10 to 1.05, thus obtaining top fraction containing mainly hydrogen and methane, and bottom fraction containing mainly absorbents and fraction C2+, at that the primary absorbing agent represents in essence mixed up fraction Cn or Cn+, the secondary absorbing agent represents in essence Cn' fraction of alkane or mixed up fraction Cn' or Cn'+, at that n and n' are equal to 3, 4 or 5 independently provided that when secondary absorbing agent represents mixed up fraction n' is not equal to 3.

Method for oxidation of alkylaromatic compounds

Method for oxidation of alkylaromatic compounds

Method includes the following stages: oxidation of alkylaromatic compound to obtain first oxidation product, contact of part of first oxidation product, solvent, which contains ionic liquid, source of bromine, catalyst and oxidant to obtain second product, which contains mother liquor and of compounds: aromatic alcohol, aromatic aldehyde, aromatic ketone and aromatic carbonic acid; addition of part of mother liquor at stage of contact; contact of part of second product; second solvent, which contains second ionic liquid, second bromine source, second catalyst and second oxidant to obtain third product, which contains second mother liquor; and addition of part of mother liquor at one or both stages of contact.

Method for separation of at least one oligomerised output flow

Method for separation of at least one oligomerised output flow

Invention relates to method for separation of at least one oligomerised output flow. Method includes the following stages at which: A) water-washed raw material flow, containing water and C3 and C4 hydrocarbons, is divided into flow, containing water and C3 hydrocarbons and flow, containing C4 hydrocarbons; B) said flow, containing water and C3 hydrocarbons, is dried in drier to remove water and obtain water-depleted flow, containing C3 hydrocarbons; C) said water-depleted flow, containing C3 hydrocarbons, is introduced into first zone of liquid-phase oligomerisation to obtain first output flow, containing C9 hydrocarbons, C12 hydrocarbons, or their combination; D) said flow, containing C4 hydrocarbons, is introduced into second zone of liquid-phase oligomerisation to obtain second output flow, containing C8 hydrocarbons, C12 hydrocarbons, or their combination, with recirculating flow of C8+ hydrocarbons being introduced into second zone of liquid-phase oligomerisation; E) at least part of said first output flow and/or said second output flow is supplied into separation zone; and F) at least one flow from said separation zone is supplied into hydroprocessing zone.

Therapeutic agents based on diglycylyl ether derivatives and methods for using them

Therapeutic agents based on diglycylyl ether derivatives and methods for using them

Invention refers to a method for inhibiting androgen receptor (AR) activity, which involves administering a therapeutically effective amount of a compound having a structure of formula

Anti-cancer steroid lactones unsaturated in position 7(8)

Anti-cancer steroid lactones unsaturated in position 7(8)

Invention refers to a compound of general formula and its pharmaceutically acceptable salts and stereoisomers possessing anti-cancer activity, a based pharmaceutical composition, using them and a method of treating cancer with using them. In general formula I R1 and R2 are specified in hydrogen and halogen; R3, R5, R6, R7, R11, R12, R14 and R15 mean hydrogen; R4 means -OH; R8, R9 and R17 mean unsubstituted C1-C6 alkyl; R10 is specified in hydrogen, =O and ORb, wherein Rb means unsubstituted C1-C6 alkyl; R13 is specified in unsubstituted C1-C6 alkyl, OH-substituted C1-C6 alkyl and COH; R16 means -OH; and the line ----- represents either a bond, or an epoxy group.

N-[(1h-pyrazol-1-yl) aryl]-1h-indole or 1h-indazole-3-carboxamide derivatives, producing and using them as p2y12 antagonists

N-[(1h-pyrazol-1-yl) aryl]-1h-indole or 1h-indazole-3-carboxamide derivatives, producing and using them as p2y12 antagonists

Present invention refers to compounds characterised by general formula (I), wherein A represents an aromatic diradical specified in groups having formulas such as below whereas the other radical and groups have values presented in the patent claim.

Mean for intracellular delivery of nucleic acids to cells of mammals

Mean for intracellular delivery of nucleic acids to cells of mammals

Invention relates to creation of low-toxic cation dendrimer peptide with structural formula (Arg)8(Lys)4(Lys)2LysAlaCys-NH2 (Fig. 1). The said dendrimer peptide is used as the mean for intracellular delivery of nucleic acids to cells of mammals. At ratio of number of positive charges to number of negative phosphate groups of the nucleic acids from 24 to 96 the dendrimer peptide can effectively penetrate in different types of cells of the mammals and completely interact with the plasmid DNA. At LD50 for 0.8-1.5 mg/ml the mean for intracellular delivery of nucleic acids to cells of mammals is low toxic.

Antiviral heterocyclic compounds

Antiviral heterocyclic compounds

Invention refers to new compounds of formula (I), which possess the properties of HCV NS5B RNA-polymerase inhibitor. The compounds may be used for treating or preventing an infection caused by hepatitis C virus (HCV). In formula (I), X represents CH or N, R1 is specified in a group consisting of R1a, R1c : wherein R1a is optionally substituted by C1-6alkyl, C1-6alkoxy or hydroxy, and wherein R1c is optionally substituted by C1-6alkyl; R2 represents (a) aryl specified in phenyl, or (b) NRaRb, wherein the above aryl is optionally substituted by (CH2)nNRcRd; Ra and Rb together with a nitrogen atom, to which they are attached, represent 5-merous heterocyclic amine substituted by (CH2)nNRcRd group, wherein n means a number from zero to two; Rc and Rd independently represent hydrogen, O2SR4, wherein R4 represents C16alkyl; R3 represents CR4aR4bR4c, wherein: 1) R4a, R4b and R4c are independently specified in C1-3alkyl.

Method for obtaining dimethyl ether

Method for obtaining dimethyl ether

Claimed invention relates to method for obtaining dimethyl ether. Method includes the following stages: a) provision of methanol-containing initial raw material; b) introduction of initial raw material into reaction zone inside gas-cooled reactor for obtaining dimethyl ether and passing of initial raw material through reaction zone; c) introduction of cooling gas flow into cooled space inside gas-cooled reactor for obtaining dimethyl ether; d) reaction of initial raw material in reaction zone in presence of catalyst, active with respect to dehydration of methanol to dimethyl ether, with obtaining reactor-leaving flow, which contains dimethyl ether; e) passing of cooling gas flow through cooled space under conditions of indirect heat exchange with initial raw material in reaction zone, with cooling gas flow being concurrent to direction of initial raw material flow in reaction zone.

Novel dihydro-oxazolobenzodiazepine compounds, method of obtaining thereof and thereof-containing pharmaceutical compositions

Novel dihydro-oxazolobenzodiazepine compounds, method of obtaining thereof and thereof-containing pharmaceutical compositions

Invention relates to compounds of formula (I) or their pharmaceutically acceptable acid addition salts, where R1 represents hydrogen atom or linear or branched (C1-C4)alkyl group; R2 represents linear or branched (C1-C4)alkyl group; R3 represents aryl or heteroaryl group; where aryl group represents naphthyl group, optionally substituted with one or several identical or different groups, selected from halogen atoms; linear or branched (C1-C6)alkyl group, which is non-substituted or is substituted with one or several halogen atoms; linear or branched (C1-C6)alkoxygroup; cyanogroup; or aminogroup, which is non-substituted or is substituted with one or two linear or branched (C1-C6)alkyl groups; and heteroaryl group represents bicyclic or tricyclic group, in which at least one of rings is aromatic, which contains from 1 to 3, identical or different, heteroatoms, selected from nitrogen, oxygen and sulphur, optionally substituted with one or several identical or different groups, selected from halogen atoms; linear or branched (C1-C6)alkyl group, which is non-substituted or is substituted with one or several halogen atoms; linear or branched (C1-C6)alkoxygroup; cyanogroup; or aminogroup, which is non-substituted or is substituted with one or two linear or branched (C1-C6)alkyl groups. Invention also relates to method of obtaining formula (I) compounds, pharmaceutical composition, containing formula (I) compound as active ingredient, and application of formula (I) compounds for preparation of medications.

Another patent 2550852.

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