Organic chemistry (C07)

C   Chemistry; metallurgy(315514)
C07            Organic chemistry(61593)
C07M - (20)

Salts and crystalline forms of apottosis-inducing agent // 2628560
FIELD: pharmacology.SUBSTANCE: invention relates to a compound having the systematic name 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy) benzamide (compound 1) in the form of a free base crystalline anhydrate, a free base hydrate of crystalline form, a solvate of crystalline form, a hydrochloride salt of crystalline form, or a sulfate salt of crystalline form. The invention also relates to a pharmaceutical composition having an inhibitory activity against anti-apoptotic proteins of the Bcl-2 family comprising a therapeutically effective amount of the compound of the invention and one or more pharmaceutically acceptable excipients.EFFECT: crystalline forms of compound 1 suitable for use as an active pharmaceutical ingredient.21 cl, 14 dwg, 14 tbl, 17 ex
Oral care products, including zinc oxide and trimethylglycine // 2628540
FIELD: pharmacology.SUBSTANCE: group of inventions refers to oral care compositions, consisting of a mixture of zinc oxide and trimethylglycine (TMG), where the TMG is included into the composition in the form of hydrohalogenide, and zinc oxide and TMG form soluble complexes, selected from zinc-TMG-hydrohalogenide complexes, zinc-hydrohalogenide complexes and mixtures, where the hydrohalogenide is selected from hydrofluoride, hydrochloride and hydrobromide, as well as to a method for tooth enamel erosion treatment or mitigation, biofilm and bacterial plaque reduction, gingivitis reduction, tooth decay and cavities formation reduction, dentin hypersensitivity reduction, including application of such composition to the teeth, zinc oxide application together with the TMG in the form of hydrohalogenide during oral care composition production.EFFECT: creation of a complex, capable of yielding a solution which precipitates when diluted.15 cl, 4 ex, 6 tbl

ethod for alcoxyphenol and alcoxyhydroxybenzaldehyde production // 2628525
FIELD: chemistry.SUBSTANCE: method for alkoxyphenol production comprises O-alkylation of at least one hydroxyphenol to form at least one alkoxyphenol, at that, the said reaction is carried out using an O-alkylating agent, an aqueous solvent containing a Bronsted base and an organic solvent with a base/O-alkylating agent ration in the range of 0.5 to 1.5 moles of base per mole of O-alkylating agent, with an O-alkylating agent/hydroxyphenol ratio in the range of 0.5 to 2 moles of O-alkylating agent per mole of hydroxyphenol and with an organic solvent/hydroxyphenol ratio of less than 280 ml, preferably in the range of 10 to 250 ml and more preferably in the range of 50 to 150 ml of an organic solvent per mole of hydroxyphenol. One of the versions of the alkoxyhydroxybenzaldehyde production method comprises preparation of alkoxyphenol from hydroxyphenol by the foregoing method and a reaction of the aldehyde group addition to the resulting alkoxyphenol to obtain the corresponding alkoxyhydroxybenzaldehyde, preferably by condensation reaction between alkoxyphenol and glyoxylic acid, followed by oxidation of the resulting compound.EFFECT: proposed method for alkoxyphenol production allows the desired product to be obtained in good yield and high purity with high conversion of initial hydroxyphenol.11 cl, 3 dwg, 7 ex

ethod of oxidative dehydration with improved regulatibility for obtaining butadiene // 2628519
FIELD: chemistry.SUBSTANCE: one of the process variants comprises the steps of providing a butene-enriched hydrocarbon feed, evaporating and superheating said butene-enriched hydrocarbon feed at a temperature of at least about 345°C (650°F), mixing said butene-rich hydrocarbon feed with superheated steam and oxygen-rich gas to form a reactor feed stream; providing a catalytic bed of oxidative dehydrogenation catalyst pellets, passing mentioned reactor feed stream from the inlet through said catalyst bed and forming a stream of a butadiene-rich product; providing a catalytic bed of oxidative dehydrogenation catalyst pellets, passing mentioned reactor feed stream from the inlet through said catalyst bed and forming a stream of a butadiene-rich product; providing mentioned catalytic oxidative dehydrogenation catalyst bed with a plurality of temperature sensing devices associated therewith for measuring the temperature in the bed in the direction of flow; controlling the inlet conditions of mentioned reactor such that oxidative dehydrogenation reactions initially take place in the layers of mentioned oxidative dehydrogenation catalyst most remote from said inlet, including reacting interaction with reactor feed stream with mentioned catalyst in the reaction zone and forming a butadiene-rich product stream; controlling the temperature over the length of the bed and occasionally increasing the temperature at the inlet so that the reaction zone migrates relative to said inlet in said oxidative dehydrogenation catalytic bed.EFFECT: use of the proposed invention avoids the effects of oxygen leaking into the catalyst.20 cl, 6 tbl, 8 dwg
Process of producing 2,3-dimethoxy-5-methyl-1,4-benzoquinone // 2628457
FIELD: chemistry.SUBSTANCE: invention relates to the method of producing 2,3-dimethoxy-5-methyl-1,4-benzoquinone, a key intermediate in the synthesis of ubiquinones (coenzymes of the Qn series), in particular of coenzyme Q10, widely used in medical practice and cosmetology, as well as its synthetic analogue - idebenone - a drug for the treatment of Alzheimer's disease. The method consists in oxidizing 3,4,5-trimethoxytoluene with hydrogen peroxide in an organic solvent medium. Herewith the acid tetrabutylammonium salts of the vanadium-containing polyoxo-tungstate (C4H9)4N)5-nHn[γ-PV2W10O40], where the number of protons n in the cationic part of the polyox-tungstate varies from 1 to 2, as co-catalyst, HClO4 with respect to the catalyst, 0.5-1 equivalents, as the organic solvent, preferably acetonitrile is used, the process is carried out at the temperature of, at least, 30°C, at the molar ratio of 3,4,5-trimethoxytoluene: the catalyst is not lower than 40 and the concentration of 3,4,5-trimethoxytoluene is not higher than 0.4M, an aqueous solution of hydrogen peroxide with a peroxide content of, at least, 30 wt %, the process is carried out at the molar ratio of hydrogen peroxide: 3,4,5-trimethoxyphenol not less than 2.EFFECT: desired product in high yield without the formation of a large amount of by-products.2 cl, 1 tbl, 23 ex

New pyrimidine inhibitors of human adenovirus replication // 2628456
FIELD: pharmacology.SUBSTANCE: invention relates to new 5-aminouracil derivatives containing 4-(phenoxy) benzyl or ω-(phenoxy)alkyl substituent in the N1 position, corresponding to the general structural formula (I). Compounds represent a new class of anti-adenoviral agents of a non-nucleoside nature. In the general formula (I), X = CH or N; Y=(CH2)2, (CH2)3, (CH2)4 or C6H4; R1= H, R2= C6H or 3,5-Cl2C6H3; R1+R2= morpholino; R3=H, F or Cl.EFFECT: compounds have a selective antiviral effect against human adenoviruses and can be used for treatment of adenoviral infections.1 dwg, 3 tbl, 11 ex

Human antibodies to clostridium difficile toxins // 2628305
FIELD: biotechnology.SUBSTANCE: completely human antibodies that bind either to toxin A, or to toxin B Clostridium difficile, or both to toxin A and toxin B. Formulations containing these antibodies and methods for their application are also described. The antibodies of the present invention are useful for neutralisation of toxins from C. difficile, thus providing agents for treatment of disease and symptoms associated with C. difficile infection, including an agent for treatment of diarrhea or pseudomembranous colitis caused by C. difficile. Antibodies may also limit the severity and/or duration of the underlying disease or limit the amount, duration and/or severity of disease relapse or exacerbation due to the presence of C. difficile.EFFECT: antibodies of this invention may also be suitable for infection diagnosis.34 cl, 5 dwg, 10 tbl, 11 ex
ethod of producing alkoxysilanes // 2628299
FIELD: chemistry.SUBSTANCE: one-step method of producing tri- and tetraalkoxysilanes is proposed, involving direct interaction of silicon with an appropriate aliphatic alcohol containing 1 to 4 carbon atoms, in the presence of a catalyst such as copper or copper chloride at a temperature of 200-300°C, which is carried out in the vibrating bed of milling bodies in the acceleration range of oscillations of 26.6 to 985.9 m/s2.EFFECT: method is chlorine-free process that meets modern environmental requirements, and ensures the production of the desired product in high yield and high conversion of the starting materials.8 cl, 7 ex

ethod and intermediate compounds for pregabaline production // 2628298
FIELD: pharmacology.SUBSTANCE: invention relates to a method for preparation of a compound of the formula and intermediates used to implement the method, as well as a method for pregabalin preparation.EFFECT: method can be implemented on a commercial scale using readily available, safe raw materials and reagents, and without the need for difficult separations.20 cl, 8 tbl, 41 ex
Piperazino[1,2-a]indole-1-ones and [1,4] diazeptino[1,2-a]indole-1-one // 2628126
FIELD: medicine.SUBSTANCE: invention relates to application of compounds of general formula I .EFFECT: new compounds, as well as pharmaceutical compositions based thereon, are obtained, that can be used to treat schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorder, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down's syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, and violations resulting from radiation therapy, chronic stress or abuse of neuroactive drugs, such as alcohol, opiates, methamphetamine, phencyclidine or cocaine.11 cl, 1 tbl, 46 ex

Rsv-specific binding molecules and means for their obtaining // 2628095
FIELD: biotechnology.SUBSTANCE: isolated antibody or a functional part thereof, capable of specifically binding the respiratory syncytial virus (RSV), is proposed. A nucleic acid molecule encoding the antibody is also provided. An expression vector and isolated cells comprising the said nucleic acid molecule for production of said antibody are described. In addition, the invention relates to a method for production of the said antibody, as well as to application of the said antibody in methods for RSV-related disorder treatment or prevention.EFFECT: invention allows to effectively bind RSV and can be used for RSV-related disorders therapy.27 cl, 16 dwg, 2 tbl, 5 ex

Antibodies, capable of specific connecting with her2 // 2628094
FIELD: biotechnology.SUBSTANCE: human epidermal growth factor 2 (HER2) receptor antibody is proposed, as well as pharmaceutical compositions comprising the said antibody for malignant tumour prevention and treatment and for apoptosis induction. In addition, a kit for malignant tumour diagnosing, comprising the said antibody, is provided.EFFECT: invention allows cancer cells destruction with significantly increased cytotoxicity when used in combination with trastuzumab and can be used for cancer therapy.11 cl, 27 dwg, 10 tbl, 15 ex

ethod for the preparation of surfactant peptides // 2628088
FIELD: biotechnology.SUBSTANCE: expression cassette is constructed containing the sequence encoding the SP-C33(Leu) peptide coding a linker with a protease cleavage site and encoding MBP protein, at that, the said sequences are sequentially fused to a polynucleotide and the polynucleotide is operably linked to a promoter sequence suitable for expression in a prokaryotic cell. The expression cassette is used to prepare an expression vector that is introduced into E. coli cells, cultured under conditions allowing fusion protein expression, purification of the aid protein, followed by fusion protein cleavage with an appropriate protease, and isolation of the SP-C33(Leu) peptide.EFFECT: increased efficiency of recombinant peptide production.13 cl, 3 dwg, 1 tbl

Thioesterification of mercaptanes in mixtures of hydrocarbons c4 // 2628085
FIELD: chemistry.SUBSTANCE: invention relates to a method for thioesterificating mercaptans by polyunsaturated hydrocarbons carried out in a reactor by feeding hydrogen using a heterogeneous catalyst and in the presence of 1-butene, characterized in that the molar ratio of hydrogen to polyunsaturated hydrocarbons is in the range of 0.01 to 0.8.EFFECT: increasing economic efficiency of processing the applied raw hydrocarbon feedstock stream.14 cl, 5 dwg, 6 ex, 13 tbl
Pyperidinyl naphthyluxic acids // 2628083
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of formula (I): , as well as to pharmaceutically acceptable salts, pharmaceutical compositions and application thereof.EFFECT: new compounds that are CRTH2 receptor antagonists have been obtained that can be useful for respiratory diseases treatment or prevention.20 cl, 2 tbl, 37 ex
Hinuclidine ethers of 1-azaheterocylic acetic acid as antimuscarine means, method for their production and their drug compositions // 2628082
FIELD: pharmacology.SUBSTANCE: invention relates to formula compounds, where A can be a single bond, a double bond, O, S, NR3, C(R3)R4, CO, C(O)N(R3), N(R3)C(O) and C(R3)-(CH2)-C(R4); m is an integer from 1 to 4; N is 0 or an integer from 1 to 4; R1 is selected from the group consisting of phenyl and 5-member heteroaryl containing one S heteroatom optionally substituted by one or more substituents selected from the group consisting of halogen atoms, (C1-C6)alkyl and (C1-C6)alkoxy; X is a physiologically acceptable anion; R2 is a group of the formula (Y), where p is 0 or an integer from 1 to 4; Q is 0 or an integer from 1 to 4; P is absent or selected from the group consisting of CO, N(R3)C(O) and C(O)N(R3); W is selected from the group consisting of H, (C1-C10)alkoxyl, phenyl, heteroaryl optionally substituted with one or more substituents selected from the group consisting of halogen atoms, OH, oxo (=O), CO2R3, (C1-C6)alkyl, (C1-C6)alkoxyl and phenyl; wherein heteroaryl is a mono- or bicyclic ring system having from 5 to 9 ring atoms and from 1 to 3 heteroatoms selected from N, O and S; R3 and R4 are independently selected from the group consisting of H, halogen atoms, CONH2, (C1-C6)alkyl, (C1-C6)alkanoyl and (C3-C8)cycloalkyl, as selective M3 receptor antagonists, to a method for their preparation, to compositions containing them, and to their therapeutic use for treatment of a respiratory disease such as asthma and chronic obstructive pulmonary disease (COPD).EFFECT: increased composition application efficiency.14 cl, 2 tbl, 34 ex
ethods and intermediate compounds for obtaining macrocyclic inhibitors of protease hcv // 2628081
FIELD: chemistry.SUBSTANCE: invention relates in particular to an improved process of preparation of (1R, 2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II by resolution of racemic 4-oxo-1,2-cyclopentanedicarboxylic acid (V). This method comprises: a) reacting 4-oxo-1,2-cyclopentanedicarboxylic acid (V) with brucine or (1R, 2S)-(-)- ephedrine to give the bis-brucinic or bis- (1R, 2S) -(-)- ephedrine salt of compound (V), and b) selective precipitation of (1R, 2R)-4-oxo-1,2-cyclopentanedicarboxylic acid bis-brucine or bis- (1R, 2S)-(-)- ephedrine salt II. The bis-brucine or bis (1R, 2S)-(-)- ephedrine salt of (1S, 2S)-4-oxo-1,2-cyclopentanedicarboxylic acid remains in solution; C) the release of acid II by removal of brucine or (1R, 2S)-(-)- ephedrine from the precipitated salt obtained in step (b); which is outlined in the following reaction scheme. .EFFECT: methods allow the production of large quantities of the active ingredient based on the methods that provide the product in high yield and with a high degree of purity.22 cl, 41 ex

Obtaining the catalyzer of oligomerization of olefines // 2628078
FIELD: chemistry.SUBSTANCE: catalytic system comprises: a) a composition comprising C3-C25-chromium (III) carboxylate, b) a pyrrole compound; and c) a hydrocarbyl-metal compound. In this case, component (a): i) is characterized by an infrared spectrum taken with KBr plates, with an absorption peak of infrared radiation υasym (CO2) within 110 cm-1 from infrared peak υsym (CO2) and the ratio of the heights of the absorption peaks of infrared radiation for the absorption peak of infrared radiation υasym (CO2) at 1516+15 cm-1 and an absorption peak of infrared radiation located at 700±50 cm-1, greater than or equal to 3:1, or ii) is characterized by an acceptance test value, R2, equal to at least 0.6, to compare the data points of the high-energy X-ray analysis g(r) of the composition containing C3-C25-chromium(III) carboxylate, with the calculated points of the high-energy x-ray diffraction data g (r) for the theoretical model of single-core chromium(III) acetate in the range r from 1.3 to 4 angstroms, or iii) obtained by contacting essentially anhydrous and substantially acid-free conditions 1) a precursor of chromium(III) having the formula CrX3Lℓ, wherein each X is independently a halide, each L is independently a C2-C10 ether, a C2-C10 thioether, a C2-C5 nitrile, a C1-C30 amine or a C3-C30 phosphine or any combination thereof and ℓ nap Is in the range from 0 to 7, 2) C3-C25 carboxylate of the metal of group 1 or 2 groups and 3) of the first solvent.EFFECT: increase in productivity or decrease in the cost of the catalytic system during the polymerization of olefins.53 cl, 23 dwg, 12 tbl, 11 ex

New derivative of 3-(4-(benzyloxy)phenyl)hex-4-ine acid, method for its production and pharmaceutical composition for metabolic disease prevention and treatment including it as effective ingredient // 2628077
FIELD: pharmacology.SUBSTANCE: invention relates to a compound represented by formula 1, its optical isomer or a pharmaceutically acceptable salt thereof: [Formula 1] , as well as to methods for its preparation and a pharmaceutical composition based on it.EFFECT: new connections are obtained, with the ability to activate the GPR40 enzyme, suitable for use for metabolic disease prevention or treatment.10 cl, 7 tbl, 77 ex, 2 dwg

Compounds with groups of oxymic compounds and/or acylic groups // 2628076
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formulas 1 or 2: (Formula 1) or (Formula 2).EFFECT: new compounds are obtained, useful as photoinitiators.25 cl, 16 dwg, 2 tbl, 31 ex
Tricyclic nitrogen-containing derivatives of imidazo[4,5-c]pyridine, having inhibiting activity in response to hystamine 4 receptor (hh4r) // 2628074
FIELD: pharmacology.SUBSTANCE: invention relates to a heterocyclic compound of formula 1 , or to a racemate, isomer, or pharmaceutically acceptable salt thereof, wherein X1 and X2 are C; each of X3 and X4 is independently C or N, provided that one of X3 and X4 is N; R1 is a saturated 4-9 member mono- or bi-heterocyclyl containing 1-2 heteroatoms (where the heteroatoms are N), where R1 is unsubstituted or substituted by 1 to 3 substituents selected from -NR6R7 and R8; or R1 is selected from -NR6R7 and R8; R2, R3, R4 and R5 may be the same or different; and each is independently selected from -H; -C1-C6alkyl; -C1-C6haloalkyl; -C1 -C6perhaloalkyl; -halogen (-F, -Cl, -Br, -I); -CN; -C1-C6talkoxy; -C1-C6haloalkoxy; -C1-C6perhaloalkoxy; C2alkenyl; -C2-C3alkynyl; -amino; -OH; -nitro (-NO2); -C6-C1aryl; and furan; provided that, when X3 is N, R4 is absent; and when X4 is N, R5 is absent, each of Y1, Y2, Y3, Y4 and Y5 is independently C or a heteroatom (preferably a heteroatom independently selected from N, O and S), provided that at least two of Y1, Y2, Y3, Y4 and Y5 are heteroatoms independently selected from N and O; each of Y2 and Y3 can be independently substituted by R9; Y4 may be substituted with -H or -C1-C6alkyl; each of R6 and R7 is independently selected from -H; -C1-C6alkyl; and -carboxyl (-COOH); R8 is -C1-C6alkyl or -C3cycloalkyl; and R9 is selected from -H; -C1-C6alkyl; and -C3cycloalkyl; wherein the alkyl and heterocyclyl may be independently unsubstituted or substituted by one or more substituents (for example, 1 to 3 substituents) selected from the group consisting of -C1-C4alkyl, -C1-C4alkoxy and -OH. The invention also relates to particular compounds and a pharmaceutical composition based on the said compounds.EFFECT: new heterocyclic compounds useful for human histamine receptor 4 inhibition are obtained.13 cl, 13 tbl, 144 ex

ethod of producing alkylbenzol // 2628070
FIELD: chemistry.SUBSTANCE: alkylation and dealkylation processes are carried out in a cascade of alkylation reactors consisting of two reactors connected in series. The entire first olefin, part of the fresh catalyst complex, part of the benzene charge, and part of the polyalkylbenzenes are fed to the comb of the first reactor, in which the alkylation process proceeds predominantly, a recycle catalyst complex is fed to the middle portion of the first alkylation reactor, to the second reactor pool, in which the dealkylation process proceeds, the remaining portions of the fresh catalyst complex, the benzene charge, the polyalkylbenzenes are fed, and separately the reaction mixture is fed from the first reactor to the bottom part of the second reactor.EFFECT: increasing the selectivity of the alkylation reaction and increasing the yield of the desired product.3 cl, 1 dwg, 3 tbl, 2 ex

New cc-1065 analogs and their conjugates // 2628069
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula or a pharmaceutically acceptable salt thereof, wherein DB is a DNA-binding group and is DB6 group ; R1 is chlorine; R2, R2', R3, R3', R4, R4', R12 and R19are H; X2 is selected from C(R14)(R14'), where R14' has the same value as defined for R7' and is independently selected, and R14' and R7' are absent, which gives a double bond between the atoms carrying R7' and R14'; R5, R6 and R7 are independently selected from H, R, where Re are selected from C1Alkyl, and R5'+R6', are absent, which gives a double bond between the atoms carrying R5 and R6, and/or R6 and R7, and/or R7 and R14 respectively; X1 is selected from O; X3 is selected from S, N, and NR15; X4 is selected from N and CR16; X5 is selected from O; X6* is selected from CR11; X7 is selected from CR8, N; X8 is selected from CR9, N; X9* is selected from CR10; X10* is selected from CR20; X11* is selected from C; X7* and X8* have the same values as those defined for X7 and X8 respectively, and are chosen independently; X34 is selected from C; annular atom B in X11* in DB6 is connected to the ring atom of ring A, so that ring A and ring B in DB6 are directly connected through a direct link; fig. implies that the said bond can be a or a non-cumulated direct bond, optionally delocalized, double bond; R8, R9, R10, R11, R15, R16, R20 are each independently selected from H, N(Rh)C(O)Ri, where Rh, Ri are independently selected from H and optionally substituted C6 aryl, one optional substituent in Ri is -OH or -NH2; a is 0 and b is 1. The invention relates to a pharmaceutical composition for tumour treatment or prevention for a mammal, comprising a therapeutically effective amount of formula (I) compound and a pharmaceutically acceptable carrier.EFFECT: DNA-alkylating agent SS-1065 analogues.6 cl, 13 dwg, 1 tbl, 23 ex
ethod for production of alpha-thiocyanated derivatives of beta-dicarbonyl compounds // 2628066
FIELD: chemistry.SUBSTANCE: invention relates to a method for production of α thiocyanated derivatives β- dicarbonyl compounds of general formula , where R = alkyl C1-C6, unsubstituted or substituted benzyl, allyl, CH2)2COOEt, (CH2)2CN; R1 and R2=CH3 or OEt or R+R1=(CH2)4, which can be used as medicinal products (anti-cancer, anti-asthmatic, analgesic, anti-inflammatory, antipyretic) and pesticides. The method includes reacting of α-substituted β-dicarbonyl compounds of general formula , where R, R1 and R2 have the above values, with sodium thiocyanate in the presence of cerium (IV) ammonium nitrate. The process is carried out in an organic solvent at a temperature of 20-25°C and molar ratio α-substituted of β-dicarbonyl compound: sodium thiocyanate: cerium(IV) ammonium nitrate equal to 1:2-4:2-4, respectively.EFFECT: method allows to increase the yield of target products, to shorten the process time, to abandon highly toxic reagents and additional stages, to expand the range of obtained compounds of general formula I.18 ex

9-benzyl-2-biphenylimidazo[1,2-a]benzimidazole and pharmaceutically acceptable salts thereof that express properties of destroyers of transversal cross-links of glycosylated proteins // 2627769
FIELD: pharmacology.SUBSTANCE: invention relates to new 9-benzyl-2-biphenylimidazo[1,2-a]benzimidazole (I) and pharmaceutically acceptable salts thereof.EFFECT: imidazobenzimidazole derivatives having the property of destroyers of transversal cross-links of glycosylated proteins.3 cl, 2 dwg, 1 tbl, 1 ex
ethod for producing alkyl salicylic acid // 2627768
FIELD: chemistry.SUBSTANCE: method for producing alkyl salicylic acid involves alkylation by the reaction of a long chainα-olefin and salicylic acid in a molar ratio of 1:1.05 to 1:1.14 in the presence of a heterogeneous sulphocathionite catalyst having a BET specific surface area of not more than 24 m2/g and not less than 22 m2/g.EFFECT: simplification of the method and increased output of the target product.3 cl, 2 tbl, 2 ex
ethod of producing aromatic amines // 2627765
FIELD: chemistry.SUBSTANCE: method consists in the reduction of aromatic nitro compounds in supercritical isopropyl alcohol as a solvent at a temperature of 270-330°C and pressure of P = 180-200 atm. A feature of the proposed method is the reduction reaction of aromatic nitro compounds in the presence of a heterogeneous zirconia catalyst ZrO2 or titanium dioxide TiO2. Preferably, the process is to be carried out in a flow tube type reactor. As a supercritical solvent, isopropyl alcohol can be used with the addition of supercritical CO2. The method allows to simplify the process by eliminating explosive molecular hydrogen, significantly shortening the process time by increasing the reaction rate, and avoiding the formation of decomposition products.EFFECT: method allows to control the selectivity of target product formation.5 tbl, 5 ex

2-acetyl-6-(2-(2-(4-brombenzylidene)hydrazinyl)thiazol-4-yl)-3,7,9-trihydroxy-8,9b-dimethyldiobenzo[b,d]furan-1(9bh)-oh, with inhibiting action on humen tyrosyl-dna-phosphodiesterase 1 // 2627764
FIELD: biotechnology.SUBSTANCE: compound is 2-acetyl-6-(2-(2-(4-bromobenzylidene)hydrazinyl)thiazol-4-yl)-3,7,9-trihydroxy-8,9b-dimethyldibenzo[b,d]furan-1(9bH)-one of formula . The compound of the invention shows the ability to inhibit the action of the human tyrosyl-DNA-phosphodiesterase 1 (Tdp1) enzyme.EFFECT: derivative of usnic acid as a human tyrosyl-DNA phosphodiesterase 1 enzym inhibitor and an increased inhibitory effect on the Tdp1 enzyme.2 dwg, 3 ex
Compound as wnt signal inhibitor, its compositions and application // 2627712
FIELD: pharmacology.SUBSTANCE: invention relates to a heterocyclic compound of the general formula (I) or an N-oxide thereof, wherein X1, X2, X3 and X4 independently represent CR4 or N, where 0 or 1 of X1-X4 can be N; Y1, Y2 and Y3 are hydrogen; R1 is selected from hydrogen, , C6 aryl, 6-member heterocycloalkyl containing 2 heteroatoms selected from N and O, and 5- or 6-member heteroaryl containing 1-4 heteroatoms selected from N, O and S, wherein each of C6 aryl, 6-member heterocycloalkyl and 5- or 6-member heteroaryl may be optionally substituted with one R4; R2 is selected from hydrogen, halogen, C1-6 alkyl, , C6 aryl and 6-member heteroaryl containing 1 to 2 N atoms, where each of C6 aryl and 6-member heteroaryl may be optionally substituted with one R4. If X5 is N, R2 is selected from halogen, C1-6 alkyl, , C6 aryl and 6-member heteroaryl containing 1 to 2 N atoms, where each of C6 aryl, and 6-member heteroaryl may be optionally substituted with one R4; each R4 Is independently selected from hydrogen, halogen, cyano, oxo, C1-6 alkoxy, -C(O)OR5, -C(O)R5, C1-6 alkyl. Moreover , C1-6 alkyl may be optionally substituted with 1 to 3 substituents selected from halogen and cyano; R5 is C1-6 alkyl; and where the central structure of Formula I, limited by X5, X6, X7 and X8, is: or The invention also relates to particular compounds, a method for inhibiting the secretion of WNT signalling in a cell, use of a compound of formula (I), a method for treatment of a disorder mediated by WNT. .EFFECT: new heterocyclic compounds have been obtained that are useful for treatment of cancer, fibrosis and osteoarthritis.22 cl

Sterines derivatives and their application for treatment of diseases related to transformed astrocytal cells, or for treatment of malignant blood diseases // 2627710
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula having a basic structure of 7 beta-hydroxycholesterol, where A is a group of -(R1)n, where R1 is an amino acid residue of glycine or alanine attached to its C-terminus, and n is 1 or 2. Moreover, R1 are the same or differentt and the N-terminus of the said amino acid is substituted with -C(O)-R2, where R2 is a benzyloxy group or a -(R1)n group, where R1 is an amino acid residue of glycine or alanine, n is 1 or 2, and the N-terminus of the said amino acid is substituted with benzyloxycarbonyl; or -C(O)-R6 group, where R6 is a five-member heterocycle comprising 2 oxygen heteroatoms unsubstituted or substituted with at least one unbranched or branched C1-C6alkyl; B is a -C(O)-R7 group, where R7 is C1-C6alkyl, unbranched or branched; or R7 is OR8, where R8 is C1-C6alkyl unbranched or branched. The invention also relates to individual compounds, a process for the preparation of a formula (I) compound, and a pharmaceutical composition having activity against transformed astrocyte cells.EFFECT: new compounds of the formula are obtained that can be used to treat diseases associated with transformed astrocytes.15 cl, 4 tbl, 16 ex
Derivatives of indolin-2-she as inhibitors of proteinkinas // 2627706
FIELD: pharmacology.SUBSTANCE: invention relates to indoline-2-one derivatives, the formula A, which are protein kinase inhibitors for the treatment of hyperproliferative diseases such as lung cancer, colorectal cancer, liver cancer and acute myelomonocytic leukemia.EFFECT: increased efficiency of treatment.15 cl, 3 dwg, 6 tbl, 1 ex
Gpr40 agonists // 2627703
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula (I), wherein ring A is an optionally substituted phenyl group, wherein the optional substituent is fluorine or methoxy; ring B is an optionally substituted phenyl group, wherein the optional substituent is selected from methoxy, 1 or 2 fluorine atoms, -CH2CN, -O-CH2-C3cycloalkyl, isopropoxy; isoxazole (which may be substituted with 1 or 2 methyl groups), -O-CH2-CN and -O-CH2-C(O)OH; X is a bond or -CH2O-; Y is -CH2O-; Z is a bond or -(CR5R6)-; L is -CO2H; R1 is OR7; R2 is a ring, selected from the group consisting of C3-C12 cycloalkyl, C6aryl-condensedC3-C6 cycloalkyl, and optionally substituted C6 aryl, each possible substituent being selected from methyl, fluoro, methoxy, cyano and methanesulfonyl; each R3, R4, R5 and R6 is independently selected from the group consisting of H, CN, OH, CONH2, C1-C12 alkyl, C2-C12 alkynyl, C6 aryl and optionally substituted C1-C18 heteroaryl selected from isoxazole, wherein the isoxazole may be substituted with 1 or 2 methyl groups, or any two of R3, R4, R5 and R6 together with the atoms to which they are attached, can form an optionally substituted C3 cycloalkyl or a double bond between the atoms to which they are attached; R7 is selected from the group consisting of H, optionally substituted C1-C12 alkyl, where possible substituents are selected from 3 fluorine atoms or -N(CH3)2 or phenyl, C2-C12 alkenyl, C3-C12 cycloalkyl and C6 aryl; r is 1; or a pharmaceutically acceptable salt thereof. The compounds of formula (I) of the invention are intended for manufacture of a pharmaceutical composition or a medicament for diabetes treatment.EFFECT: GPR40 activating connections.30 cl, 3 tbl, 124 ex

Crystalline forms of 1-(3-tret-butyl-1-p-tolyl-1h-pyrazol-5-yl)-3-(5-fluoro-2-(1-(2-hydroxyetil)-1h-indasol-5-yloxy)benzyl) hydrochloride urea // 2627702
FIELD: pharmacology.SUBSTANCE: invention relates to a crystalline polymorphic Form B of the hydrochloride salt of 1-(3-t-butyl-1-p-tolyl-1H-pyrazol-5-yl)-3-(5-fluoro-2-(1-(2-hydroxyethyl)-1H-indazol-5-yloxy)benzyl) urea, which is characterized by the presence of peaked diffraction peaks (degrees 2θ at ± 0.3) at about 12.3, 13.0, 15.9, 16.9 and 17.6 and to a pharmaceutical composition for proliferative disorders treatment comprising the said polymorphic Form B. The invention also relates to a method for proliferative diseases treatment with the claimed pharmaceutical composition, pharmaceutical composition and method application for preparation of the said polymorphic Form B.EFFECT: increased efficiency of treatment.89 cl, 7 dwg, 23 tbl, 10 ex
Sulfonamide compounds and their use as tnap inhibitors // 2627701
FIELD: chemistry.SUBSTANCE: invention relates to compounds of Formula I: wherein: Y1 is a bond and Y2 is -N(R6)-; L1 and L2 are each a bond; X1 is =N- or =C(R2)-; X2 is =N- or =C(R3)-; R1 and R4 are independently selected from the group consisting of -F, -Cl, -Br, -CN, -C(O)N(R7)-R8, -C(O)-O-R9, methyl, -OMe, -OCF3, optionally substituted phenyl and optionally substituted 5- or 6-membered heteroaryl; R2, R3 and R5 are hydrogen; R6 is hydrogen; R7 is hydrogen and R8 is selected from hydrogen, optionally substituted C1-C4 alkyl, optionally substituted C3-C6 cycloalkyl or optionally substituted phenyl; either R7 and R8 together with the nitrogen atom to which they are attached form an optionally substituted heterocycloamino which is an optionally substituted pyrrolidine, an optionally substituted piperidine, an optionally substituted morpholine or an optionally substituted piperazine; R9 is selected from hydrogen, optionally substituted C1-C4 alkyl, optionally substituted C3-C6 cycloalkyl or optionally substituted phenyl; A is selected from the group consisting of -C(O)-N(R7)-R8 or -C(O)-O-R9, or A is , R12 and R13 are independently selected from the group consisting of hydrogen, halogen, -CN, -OH, -C(O)-O-R19, optionally substituted C1-C4 alkyl, optionally substituted C3-C6 cycloalkyl optionally substituted with C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, optionally substituted phenyl and optionally substituted 5- or 6-membered heteroaryl, R19 is selected from the group consisting of hydrogen, optionally substituted C1-C4 lkila, C1-C4 haloalkyl, optionally substituted C3-C6 cycloalkyl and optionally substituted phenyl; and R15 represents hydrogen or C1-C4 alkyl; Wherein the substituted group is substituted by -CO2H, nitrile, hydroxyl, C1-C4 alkyl, C1-C4 alkoxy, phenyl, C3-C6 cycloalkyl or diC1-C4 alkylamine, which modulate TNAP activity.EFFECT: improved properties of compounds.14 cl, 1 tbl, 12 ex

ethod for producing (2s,5r)-7-oxo-6-sulphoxi-2-[((3r)-piperidine-3-carbonyl)hydrazinocarbonyl]-1,6-diazabicyclo[3,2,1]octane // 2627700
FIELD: chemistry.SUBSTANCE: invention relates to method for obtaining compound of Formula , comprising: (a) reaction between compound of Formula and compound of Formula in the presence of water taken as solvent to obtain compound of Formula ; (b) hydrogenolysis of compound of Formula (IV) to obtain compound of Formula ; (c) sulfonation of compound of Formula (V) to obtain compound of Formula ; and (d) conversion of compound of Formula (VI) to compound of Formula (I). The invention also relates to method of producing compound of formula (I).EFFECT: simplicity of operations, safer conditions, high yield of the target product.10 cl, 1 dwg, 2 ex

Sodium salt (2s,5r)-6-benzyloxy-7-oxo-1,6-diaza-bicyclo[3,2,1]octane-2-carbonic acid and its production // 2627698
FIELD: chemistry.SUBSTANCE: invention relates to sodium salt of (2S,5R)-6-benzyloxy-7-oxo-1,6-diaza-bicyclo[3.2.1]octane-2-carboxylic acid of formula , its crystalline form and method for its production.EFFECT: stability of form, useful in synthesis of antibacterial agents.9 cl, 1 dwg, 1 ex
Catalyst on the carrier, its activated form and their production and application // 2627697
FIELD: chemistry.SUBSTANCE: describes the non-activated Renei catalyst on the carrier. The catalyst comprises an organic polymeric carrier material and Renei alloy particles. The Renei alloy particles are supported on a polymeric carrier material, where substantially all the particles are partially embedded in the carrier material. In this case, the particles of the Renei alloy are distributed unevenly in the catalyst and the concentration of particles in the surface portion of this carrier is greater than the concentration of the particles of the Renei alloy in the middle part of this carrier. Activation of the catalyst is carried out by activating a non-activated supported catalyst with a caustic aqueous solution.EFFECT: preparation of Renei catalyst with high activity, good selectivity and easy extraction of metal.17 cl, 2 dwg, 3 tbl, 10 ex

ethod of alkylation of alkyl benzenes // 2627695
FIELD: chemistry.SUBSTANCE: method comprises the following steps: a) feeding the alkyl benzene having the formula (I) and the first stream of the alkylating agent to the first reaction zone, contacting them with the catalyst A to obtain the reaction stream I, wherein at least one alkylating agent is selected from the group, Consisting of methanol, formaldehyde and dimethoxymethane, where the substituents RN, When there are more than one, may be the same or different from each other, each independently selected from the group consisting of C1-4 Linear or branched alkyl, n is the number of substituents R and is an integer of 0, 1 or 2; B) feeding the reaction stream I and the second stream of the alkylating agent to at least one second reaction zone where they are contacted with catalyst B to obtain reaction stream II; and c) feeding the reaction stream II to at least one third reaction zone, where it is contacted with the catalyst C to obtain the reaction stream III containing the alkylate. The reaction temperature in the first reaction zone is lower than the reaction temperature in the third reaction zone, at least one of catalyst A, catalyst B and catalyst C is a molecular sieve ionically exchanged with an alkali metal in accordance with a method comprising the step of carrying out the contacting of molecular sieve with a source of alkali metal ions to effect ion exchange, wherein the molecular sieve is one or more sieves selected from the group consisting of a molecular sieve of the type X and Y type molecular sieve, and the alkali metal is selected from the combination K/Rb, K/C°s combination, Rb/Cs combination or K/Rb/C°s combination, the temperature in the first reaction zone is 320-385°C, the temperature in the second reaction zone is 380-420°C and wherein the alkylate is a compound having the following formula (II) and/or a compound having the following formula (III), and R and n in each formula have the same meaning as for formula (I), respectively.EFFECT: alkylation process can improve the efficiency of using an alkylating agent.19 cl, 1 tbl, 12 ex, 2 dwg

Derivatives of hinoline, visualizing tau protein // 2627694
FIELD: pharmacology.SUBSTANCE: invention relates to a new quinoline derivative of formula (I) or a pharmaceutically acceptable salt thereof, wherein A is or , R1 is halogen or , in which R4 and R5 each independently represents hydrogen, a lower alkyl group, or R4, R5 and the nitrogen atom to which they are attached together form a 6-member nitrogen-containing aliphatic ring (where the nitrogen atom may be substituted by a lower alkyl group), or R4 and the nitrogen atom to which it is attached together with ring A form a 10-membered nitrogen-containing fused bicyclic ring (one carbon atom constituting the nitrogen-containing condensed bicyclic ring can be replaced by the oxygen atom), and R5 is a lower alkyl group where a line crossed by a dashed line means a bond of the above general formula with another structural moiety, R2 or R3 each independently represents NRaRb or -O-lower alkyl group (each alkyl group may be substituted with 1 to 2 substituents selected from halogen, hydroxy groups), ring A is unsubstituted or substituted by R6 (where R6 is one substituent selected from halogen and an -O-lower alkyl group (each alkyl group may be substituted with 1 to 2 substituents selected from halogen, hydroxy, Ra and Rb each represents hydrogen or a lower alkyl group, m and n denote an integer from 0 to 1, wherein at least one of R2, R3 and R6 is an -O-lower alkyl group substituted with one hydroxy group and one halogen. The invention also relates to a pharmaceutical composition, a composition for conformational disease diagnosis, treatment or prevention, a diagnostic kit based on a compound of formula (I), a method of treatment, a method for detection or staining of a protein-layer β-structure, a process for preparation of a compound of formula (I) and intermediates.EFFECT: new compounds are obtained that can be used to diagnose and treat conformational diseases, in particular, a disease having such a cardinal symptom as intracerebral accumulation of tau protein, for example, Alzheimer's disease.17 cl, 29 dwg, 26 tbl, 2 ex
Catalyst with low content of chrome oxide for isobutane dehydrogenation and method for dehydrogenating isobutane using it // 2627667
FIELD: chemistry.SUBSTANCE: catalyst for isobutane dehydrogenation obtained by impregnating nanostructured zirconium oxide with an aqueous solution of CrO3, the catalyst further contains soluble potassium and/or sodium salts, with subsequent drying at 95-120°C and calcination at 600°C, the catalyst is characterised in that the content of chromium oxide in the catalyst is not more than 6 wt % on Cr2O3 basis. A method for isobutane dehydrogenation is also disclosed.EFFECT: catalyst is characterized in high catalytic properties over a wide temperature range with a low chromium oxide content.2 cl, 1 tbl, 2 ex

Dehydrogenation catalyst of light paraffin hydrocarbons and production method of unsaturated hydrocarbons with its use // 2627664
FIELD: chemistry.SUBSTANCE: disclosed the catalyst for the light paraffin hydrocarbons dehydrogenation, which is the chromium oxide, supported on alumina, at that the chromic oxide in the amount of 15-23 wt % is in the dispersed X-ray amorphous state. Also described the method of production the unsaturated hydrocarbons by dehydrogenation the corresponding paraffin hydrocarbons in the flow reactor with the fixed bed catalyst of volume ~ 1 cm3 when the paraffinic hydrocarbon is supplied at the rate of 420 h-1 and the process temperature 570°C, which is realized, using the above described catalyst, and the catalytic cycle is carried out for 31-136 minutes, including the dehydrogenation for 15-120 minutes.EFFECT: increase of the process productivity due to the increase of the dehydrogenation stage time and, correspondingly, the increase in the total yield of the unsaturated hydrocarbon per one dehydrogenation-regeneration-activation cycle.2 cl, 2 dwg, 1 tbl, 9 ex
Compounds of pyridazinamide and their use as synthetic syneckinasis inhibitors (syk) // 2627661
FIELD: chemistry.SUBSTANCE: invention relates to novel pyridazinamides of the formula I , where all variable substituents are defined in the claims, and their pharmaceutically acceptable salts, as well as a pharmaceutical composition based on them.EFFECT: compounds of the formula are SYK inhibitors and are useful for the treatment of autoimmune and inflammatory diseases.10 cl, 1 tbl, 43 ex
Fluoropicolinoyl fluorides and methods of their production // 2627659
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula: in which R is selected from the group consisting of halogen; alkyl; cycloalkyl; alkenyl; alkynyl; alkoxy and aryl substituted with 0 to 5 substituents independently selected from the group consisting of halogen, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy and C1-C4haloalkoxy; m is 0, 1, 2 or 3 and n is 0, 1, 2, 3 or 4; in which the sum of m and n is from 1 to 4, and methods for their production.EFFECT: obtaining method improvement.29 cl, 19 ex
Dicationic ionic liquids with polysiloxane fragment in cation structure as coolants // 2627658
FIELD: chemistry.SUBSTANCE: dicationic ionic liquids with a polysiloxane fragment in a cation structure of general formula where R1 and R2 - methyl or phenyl, R3 - CH2 and (CH2)3, n=3-8, as coolants. The properties of the produced ionic liquids (IL) allow to use them in open outer space as coolants. They also have physico-chemical and thermophysical characteristics (viscosity, density, volatility, heat capacity and thermal conductivity) necessary for their use as coolants.EFFECT: proposed new dicationic ionic liquids with a polysiloxane fragment in the cation structure of general formula I are liquid at normal conditions and have a lower saturated vapor pressure in high temperature region as compared to the prototype and with other known coolants, which ensures their explosion safety and significantly low volatility in the dynamic vacuum.1 tbl, 6 ex

ore energy-efficient way of hydrogenation of c5 // 2627657
FIELD: chemistry.SUBSTANCE: method of selective hydrogenation of acetylenes and dienes in the flow of the C5 hydrocarbons include: hydrogen supply and C5-olefin-containing stream containing the linear pentenes, dienes, acetylenes and cyclopentene, in the reaction system of catalytic distillation; at the same time in the reactor system of catalytic distillation: hydrogenation of acetylenes and dienes; and fractionation C5-olefin-containing stream; removing the head of the faction that contains linear pentenes; removing the side fractions containing cyclopentene; and extract cubic faction. Also the invention relates to method of conversion of linear pentenes in propylene and selective hydrogenation of acetylenes and dienes in a stream of C5 hydrocarbons.EFFECT: lower costs.21 cl, 6 dwg, 2 tbl
Polybacterial drug with advantages for health: with antioxidant effect, decreased cholesterol concentration, anti-inflammatory and immuno-modulating effect, and release of bioactive peptides inhibiting angiotensin-converting enzyme // 2627651
FIELD: biotechnology.SUBSTANCE: group of inventions refers to polybacterial probiotic drug including new strains of lactic acid bacteria Lactobacillus gasseri 7/12 NBIMCC No. 8720, Lactobacillus plantarum F12 NBIMCC No. 8722 and Lactobacillus helveticus A1, NBIMCC No. 8721, which has anti-inflammatory immunomodulatory, hypocholesterolemic, antioxidant and antihypertensive activity. The group of inventions also refers to the use of drug as a probiotic agent, as well as an agent which has anti-inflammatory immunomodulatory, hypocholesterolemic, antioxidant and antihypertensive activity.EFFECT: food additives, food and functional products, pharmaceutical preparations that include this drug, have a beneficial effect on the health of people and animals.9 cl, 8 dwg, 15 tbl
ethod for production of hyperimmune serum containing heterologic immunoglobulines against ebola fever // 2627631
FIELD: pharmacology.SUBSTANCE: method for hyperimmune serum production contains heterologous immunoglobulins against Ebola fever, involves 4-fold immunization of horses with viral preparations that do not contain live Ebola virus, followedantigenic by blood collection from producer animals and hyperimmune serum isolation. As a viral antigenic preparation, a DNA preparation containing the Ebola virus glycoprotein gene and a HPV preparation containing virus-like particles comprising the Ebola virus glycoprotein gene are used, the 3-fold administration of the DNA preparation is performed intramuscularly according to the following scheme: 1st immunization - DNA preparation administration at a dose of 4 mg/animal on day 0, 2nd immunization - DNA preparation administration at a dose of 4 mg/animal on day 21-28 after the first administration of the drug, 3rd immunization - DNA preparation administration at a dose of 4 mg animal on day 21-28 after the second administration of the drug, the fourth immunization performed subcutaneously by HPV preparation administration at a dose× of 3109 HPV/animal on day 56 after the third administration of the DNA preparation, allowing to induce formation of common specific antibodies in titres of at least 1:75,000 and formation of neutralising antibodies to Ebola virus in titres of at least 1:640, and blood sampling for production of a hyperimmune serum containing immunoglobulins is carried out on day 10 -13 after immunization with the HPV preparation. The total time of immunization (from the 1st immunization to blood sampling) is 122 days.EFFECT: simplification of technology for hyperimmune serum obtaining and reduced cost of its production.3 cl, 4 dwg

ethod to obtain chemeric recombinant protein flic:pagn // 2627602
FIELD: biotechnology.SUBSTANCE: to implement the method, a recombinant plasmid pETfliCpagN is constructed, then Escherichia coli BL21 (DE3) cells with the said plasmid and the resulting BL-fliCpagN strain is cultured at a temperature of 37°C. Next, a periplasmic fraction of producer bacteria is prepared by cells treatment with lysozyme in a 20% sucrose solution, followed by centrifugation, the chemeric fliC:pagN by metal chelate, anion exchange, and gel filtration chromatography to obtain a homogeneous final preparation of fliC:pagN protein. The recombinant pETfliCpagN plasmid contains the T7 bacteriophage promoter and carries sequences encoding fliC proteins, including the leader sequence of this protein, and pagN S. typhimurium, combined with a short linker sequence GSVDSSSGGN, and fused at the 3'-end with a synthetic sequence encoding six histidins.EFFECT: method allows to synthesise this protein in soluble form with a native N-terminal amino acid sequence, yielding at least 0,3 g of protein from a litre of bacterial culture with 98 percent purity.7 dwg, 4 ex

ammalian cells expressing cd40l ligand and their application // 2627597
FIELD: biotechnology.SUBSTANCE: co-culturing of a pool of rabbit B cells with BHK or CHO cells expressing CD40L, which are used as a feeder in the presence of IL-2 at a concentration of about 50 U/ml and IL-21 at a concentration of approx. 10 ng/ml to approx. 100 ng/ml.EFFECT: invention allows to obtain high concentrations of IgG in a short time.7 cl, 14 dwg, 16 tbl, 16 ex
4-aryl (hetaril) methyl-substituted 8-cyclopentilamine-5,7-difluor-3,4-dihydro-2h-benzo [1,4] thiazine-1,1-dioxides that hypertensive action // 2627499
FIELD: pharmacology.SUBSTANCE: invention relates to 4-aryl (hetaryl) methyl-substituted 8-cyclopentylamino-5,7-difluoro-3,4-dihydro-2H-benzo [1,4] thiazine-1,1-dioxides 1: .EFFECT: new compounds of formula 1 have been obtained, which can be used as mild hypertensive drugs.1 tbl, 3 ex
 
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