Organic chemistry (C07)

C   Chemistry; metallurgy(311501)
C07            Organic chemistry(60703)
C07M - (20)
Novel pyrrole compounds, synthesis method thereof and pharmaceutical compositions containing same // 2607788
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula (I) possessing inhibitory activity on Bcl-2 family proteins. In formula (I) (I) A1 is hydrogen, (C1-C6)polyhaloalkyl group or (C1-C6)alkyl group, A2 is hydrogen, (C1-C6)polyhaloalkyl group, (C1-C6)alkyl group or cycloalkyl group, T denotes a hydrogen atom, (C1-C6)alkyl group, optionally substituted with one-three halogen atoms, group (C1-C4)alkyl-NR1R2 or group (C1-C4)alkyl-OR6, R1 and R2 each independently from each other is a hydrogen atom or (C1-C6)alkyl group, or R1 and R2 form with a nitrogen atom bearing them, heterocycloalkyl, R3 is (C1-C6)alkyl group, cycloalkyl group, heterocycloalkyl group, aryl group or heteroaryl group, wherein one or more carbon atoms of previous groups or their possible substitutes can be deuterated, R4 is an aryl group or heteroaryl group, wherein one or more carbon atoms of previous groups or their possible substitutes can be deuterated, R5 is hydrogen or halogen atom, R6 is a hydrogen atom or a linear or branched (C1-C6)alkyl group, Ra, Rb, Rc and Rd each independently from other represents hydrogen, linear or branched (C1-C6)alkyl, halogen atom, a linear or branched (C1-C6)alkoxy group, hydroxy group, R7-CO-NH-(C0-C6)alkyl-, R7-SO2-NH-(C0-C6)alkyl-, R7-NH-CO-NH-(C0-C6)alkyl-, R7-O-CO-NH-(C0-C6)alkyl-, or substitutes of pair (Rb, Rc) form together with carbon atoms carrying them, a ring consisting of 5–6 ring members, which may contain 1–2 oxygen atoms, R7 is hydrogen, linear or branched (C1-C6)alkyl, aryl or heteroaryl. Invention also relates to methods of producing compounds of formula (I), to a pharmaceutical composition, use of a pharmaceutical composition for preparing a drug, use of compound of formula (I) for preparing a drug.EFFECT: obtaining novel compounds of formula (I) possessing inhibitory activity on Bcl-2 family proteins.37 cl, 2 tbl, 473 ex
Improved solvent for extraction of maleic anhydride from gas stream // 2607762
FIELD: chemistry.SUBSTANCE: invention relates to methods of producing raw maleic anhydride. In particular, method includes steps where: reactor output stream, containing maleic anhydride, is fed into bottom part of absorption column, where it comes into contact with a non-cyclic solvent, that is fed close to its upper part and is a diester, having a boiling point under normal conditions between 250 °C and 350 °C, solubility of fumaric acid at least 0.06 wt% at temperature of 60 °C, solubility of maleic anhydride at least 10 wt% at temperature of 60 °C, water solubility not higher than 100 mg/l, density, different from water density at least to 0.020 g/ml, and a water-soluble hydrolysis product with molecular weight not higher than that of pentanol, with transfer of maleic anhydride of outlet stream of reactor into a solvent, wherein gas stream to be extracted is blown off from absorption column, and enriched solvent, containing maleic anhydride, is removed from absorption column near bottom of absorber and directed into flash tower near its middle part, untreated maleic anhydride is removed from stripping column near its middle or upper part.EFFECT: methods make it possible to use cheaper solvent than phthalates.11 cl, 1 dwg, 1 tbl
ethod of producing aromatic thiol derivatives during hydrogenation of disulphides // 2607636
FIELD: chemistry.SUBSTANCE: invention relates to methods of producing thiophenols during reaction of corresponding disulphide with hydrogen in presence of a heterogeneous hydrogenation catalyst based on a transition metal. In particular, method of producing a compound of formula (I') involves reaction of a compound of formula (II'), wherein R is H or with H2 in presence of a heterogeneous hydrogenation catalyst based on a transition metal, where heterogeneous hydrogenation catalyst based on a transition metal is a Raney catalyst, Pd/C, Pd(OH)2/C, nanoparticles of palladium (0), micro-encapsulated in a polyurea matrix, Au/TiO2, Rh/C, Ru/Al2O3, Ir/CaCO3, Pt/C or mixture thereof. When reaction is carried out in presence of an acylating reagent, such as anhydride or halide of carboxylic acid, acylated thiophenol is obtained.EFFECT: pharmaceutically active compound S-[2-[1-(2-ethylbutyl)cyclohexylcarbonylamino]-phenyl]-2-methylthiopropionate is obtained during said method.20 cl, 16 ex, 1 tbl
N-9-substituted purine compounds, compositions and methods of use // 2607635
FIELD: chemistry.SUBSTANCE: present invention relates to novel compounds of formula I-A, having properties of inhibitors of kinase of phosphoinositide-3-kinase family mTOR and PI3K, for use in treating cancer, as well as for preparing drugs for treating cancer. In compounds of formula I-A R1 is selected from a group comprising cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, pyrrolidin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, oxetan-2-yl, oxetan-3-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl and tetrahydropyran-4-yl, oxepan-2-yl, oxepan-3-yl, oxepan-4-yl, phenyl pyrrol-2-yl, pyrrol-3-yl, pyrazol-3-yl, pyrazol-4-yl, pyrazol-5-yl, furan-2-yl, furan-3-yl, thien-2-yl, thien-3-yl, thiazol-2-yl, thiazol-3-yl, thiazol-4-yl, imidazol-1-yl, imidazol-4-yl, pyrid-2-yl, pyrid-3-yl, pyrid-4-yl, pyrimidin-1-yl, pyrimidin-2-yl, pyrimidin-3-yl, pyrazin-2-yl, pyridazin-2-yl, pyridazin-3-yl and triazin-2-yl, where R1 substituted by 0-3 substitutes RR1, selected from a group consisting of halogen, F, Cl, Br, I, -ORa, -C(O)Ra, -Rc; where Ra is selected from hydrogen or C1-6alkyl, Rc is C1-6alkyl; R2 is selected from a group comprising hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl; R3 is a morpholine-4-yl, where group R3 is substituted with 0–3 substitutes RR3, selected from a group consisting of -Ri, halogen, where Ri is selected from C1-6alkyl, C1-6haloalkyl; D is -NR4C(O)NR5R6 or -NR5R6, where R4 and R5 each denotes hydrogen and R6 is C1-6alkyl, C1-6haloalkyl oxetan-3-yl and pyridyl-on.EFFECT: treatment of cancer.11 cl, 1 tbl, 26 ex
Romidepsin solid forms and use thereof // 2607634
FIELD: chemistry.SUBSTANCE: invention relates to novel crystalline form C of romidepsin, a pharmaceutical composition containing form C of romidepsin.EFFECT: treatment of skin T-cell lymphoma.3 cl, 12 dwg, 19 tbl, 16 ex
oulded catalyst for converting methanol into aromatic hydrocarbons and method of producing said catalyst // 2607633
FIELD: chemistry.SUBSTANCE: invention relates to a catalyst for converting methanol into aromatic hydrocarbons, method of producing said catalyst and method of converting methanol into aromatic hydrocarbons. Catalyst contains 85 to 99 parts by weight of zeolite ZSM-5, from 0.1 to 15 parts by weight of element M1, which is least one element selected from a group consisting of Ag, Zn and Ga, and from 0 to 5 parts by weight of element M2, which is at least one element selected from a group consisting of Mo, Cu, La, Ce and P, Co, wherein total specific surface area of catalyst is in range of 350–500 m2/g, and specific surface area of micro pores is within range of 200–350 m2/g. Method involves following steps: step I: mixing template agent I, an inorganic acid, silicon source, aluminium source, water, soluble compound of element M1 and, optionally, soluble compound of element M2 to obtain a mixture, converting mixture into gel with subsequent holding and drying of gel to obtain amorphous mixed silicon-aluminium mixed oxide precursor; step II: mixing silicon-aluminium mixed oxide precursor obtained at step I, with a crystal seed and binding agent, moulding and drying mixture to produce a moulded semi-finished product; and step III: crystallisation followed by calcination of moulded semi-finished product obtained at step (II), to obtain said catalyst. Catalyst is characterised by high values of total specific surface area, specific surface area of micro pores and micropore volume.EFFECT: results of reaction for synthesis of aromatic hydrocarbons from methanol using a catalyst, provided in present invention, demonstrated good catalytic activity.14 cl, 3 tbl, 25 ex
ethod for production of liquefied hydrocarbon gases // 2607631
FIELD: gas industry.SUBSTANCE: invention relates to production of liquefied hydrocarbon gases, including adsorption purification of a broad fraction of light hydrocarbons from sulphur compounds and methanol. Method is characterized by that adsorption purification of liquefied hydrocarbon is implemented in multilayer adsorbers, in which each layer of adsorbent is series-selective in relation to a specific type of extracted impurities, temperature regeneration and subsequent cooling of adsorbents is carried out with a methane fraction, purified from impurities, similar to extracted impurities, and supplied on side, at final stage of cooling of adsorbents, adsorbers are blown with dry high-pressure nitrogen prior to feeding broad fraction of light hydrocarbons into adsorber with regenerated adsorbents, and purified broad fraction of light hydrocarbons undergoes distillation to produce liquefied narrow fractions of light hydrocarbons in system, at least two full rectification columns.EFFECT: use of present method simplifies and provides universalisation of process diagram of production of liquefied hydrocarbon gases at stage of purification of liquefied gases independently from combination of extracted impurities, reduced power consumption of process and flexible variability of process with formation of a range of final product depending on marketing requirements.14 cl, 1 tbl, 3 dwg
Aromatic derivatives of sulfanilamides carbonic anhydrase ii (ca ii) inhibitors, methods for production and use thereof // 2607630
FIELD: chemistry.SUBSTANCE: present invention relates to novel aromatic sulphonamide derivatives, general formula 1 and pharmaceutically acceptable salts thereof, which are selective inhibitors of carbonic anhydrase II (CA II). Substituted sulphonamides correspond to general formula 1 ,where A is phenyl or thiophene; R1 is C1-C5alkyl, C-3C6cycloalkyl, -C(O)R3; provided that R1 is not methyl, when A is phenyl, R2 represents hydrogen; R3 is a 5-6 member heterocyclyl with one or two heteroatoms, selected from nitrogen or oxygen atoms; R2 is C1-C3alkyl, C1-C3alkoxy. Invention also relates to a method of producing compounds of general formula 1. Method involves two stages: a) sulphochlorination of corresponding oxazole derivative of general formula 5 (a-o) or 6 (a-j) with a mixture chlorosulphonic acid and thionyl chloride to produce intermediate sulphochlorides of formula 7 (a-o) or 8 (a-j), respectively, and b) with subsequent conversion of obtained sulphochlorides into primary sulphamides of formula 9 (b-o) or 10 (a-j) by reacting with ammonia according to following scheme ,where ,where R1 is C1-C5alkyl, C3-C6cycloalkyl; NR'Rʺ is a morpholine or pyrrolidine.EFFECT: compounds can be used for treating glaucoma, in particular, open-angle glaucoma, and other diseases caused by high intraocular pressure, age-related macular degeneration, diabetic macular edema, diabetic retinopathy, hypertensive retinopathy and retinal vasculopathy mediated by activity of carbonic anhydrase II.11 cl, 2 dwg, 2 tbl, 57 ex
N-alkylsubstituted benzo- and (pyrido[2,3-b]thieno)pyrrolo[1,2-a][1,4]diazepin-6-ones - antidotes of herbicide of hormonal action 2,4-dichlorophenoxyacetic acid on sunflower // 2607629
FIELD: chemistry.SUBSTANCE: invention relates to novel synthetic, biologically active chemical substances from series of heterocyclic compounds of formula 1 EFFECT: technical result is synthesis of novel compounds in a series of condensed pyrrolo[1,2-a][1,4]benzodiazepines of formula 1a-d in order to expand range of biologically active substances, obtained synthetically, for use in agriculture as antidotes of herbicide of hormonal action 2,4-D.1 cl, 3 tbl, 6 ex
Sodium salt of 2-methylthio-6-cyano-1,2,4-triazolo[5,1-c]-1,2,4-triazin-7(4h)-one, trihydrate // 2607628
FIELD: chemistry.SUBSTANCE: invention relates to a sodium salt of 2-methylthio-6-cyano-1,2,4-triazolo[5,1-c]-1,2,4-triazin-7(4H)-one, trihydrate, which exhibits antiviral action on influenza .EFFECT: obtaining a novel compound having antiviral activity.1 cl, 1 dwg, 2 tbl, 4 ex
ethod of propylene production by recycling of heavy fractions // 2607626
FIELD: manufacturing technology.SUBSTANCE: invention relates to two versions of method of propylene production. One of versions includes: metathesis reaction of raw supply stream consisting of mixture of n-butene with ethylene in presence of metathesis catalyst to form fraction containing propylene, ethylene, butene and C5+ olefins, 2-pentene and 3-hexene; extraction of propylene from ethylene, butene and C5+ olefins from fraction of metathesis products; and recirculation of at least part of C5+ olefins for metathesis reaction recycled C5+ olefins are converted into propylene and butene, wherein ethylene is introduced into metathesis reaction at ratio, which is sufficient for maintaining reaction, where C4+ ratio for reaction with metathesis catalyst ranges from 0.3:1 to 3:1 and at least 5 % of C5+ olefins return into metathesis reaction.EFFECT: use of recycling of C5+ olefin gasoline increases efficiency of method with low total flow through metathesis reactor.11 cl, 3 dwg
Compositions and methods for treating and diagnosing asthma // 2607569
FIELD: biotechnology.SUBSTANCE: invention relates to biotechnology, immunology and medicine. Application of antibody binding to IL-13 is disclosed as medicinal agent for treating asthma in humans. Wherein patient has high expression levels of POSTN in relation to average or median level of POSTN expression. Method of treating asthma subtype using such antibodies is also described.EFFECT: disclosed group of inventions can be used in medicine.23 cl, 49 dwg, 13 tbl, 9 ex
Quaternary ammonium salts based on derivatives of vitamin b6 // 2607522
FIELD: medicine.SUBSTANCE: invention relates to novel derivatives of vitamin B6 of general formula (I) with high antibacterial activity. ,where at R1=R4=N+(CH3)2C8H17, R2+R3=-C(CH3)2O-, R5=H, n=2, m=0; at R1=R4=N+(CH3)2C12H25, R2+R3=-C(CH3)2O-, R5=H, n=2, m=0; at R1=R4=N+(CH3)2C18H37, R2+R3=-C(CH3)2O-, R5=H, n=2, m=0; at R1=R4=N+(CH3)2C8H17, R2=R5=H, R3=OH, n=2, m=1; at R1=R4=N+(CH3)2C12H25, R2=R5=H, R3=OH, n=2, m=1; at R1=R4=N+(CH3)2C18H37, R2=R5=H, R3=OH, n=2, m=1; at R1=R5=H, R2+R3=-CH(C2H5)O-, R4=N+(CH3)2C18H37, n=1, m=0; at R1=R5=H, R2+R3=-CH(C3H7)O-, R4=N+(CH3)2C18H37, n=1, m=0; at R1=R5=H, R2+R3=-CH(C4H9)O-, R4=N+(CH3)2C18H37, n=1, m=0; at R1=R5=H, R2+R3=-CH(C(CH3)3)O-, R4=N+(CH3)2C18H37, n=1, m=0; at R1=R5=H, R2+R3=-CH(C8H17)O-, R4=N+(CH3)2C18H37, n=1, m=0; at R1=R5=H, R2+R3=-CH(CH2CH(CH3)C9H19)O-, R4=N+(CH3)2C18H37, n=1, m=0; at R1=R5=H, R2+R3=-CH2O-, R4=N+(CH3)2C18H37, n=1, m=0; at R1=R5=H, R2+R3=-C(cycle-C4H8)O-, R4=N+(CH3)2C18H37, n=1, m=0; at R1=R5=H, R2+R3=-CH(C3H7)O-, R4=N+(CH3)2C8H17, n=1, m=0; at R1=R5=H, R2+R3=-CH(C3H7)O-, R4=N+(CH3)2C12H25, n=1, m=0; at R1=R5=H, R2+R3=-CH2O-, R4=N+(CH3)2C8H17, n=1, m=0; at R1=R5=H, R2+R3=-CH2O-, R4=N+(CH3)2C12H25, n=1, m=0; at R1=R5=H, R2+R3=-C(CH3)2O-, R4=N+(CH3)2C12H25, n=1, m=0; at R1=R2=R5=H, R3=OH, R4=N+(CH3)2C12H25, n=1, m=1; at R1=R3=R5=H, R2=C(O)CH3, R4=N+(CH3)2C8H17, n=1, m=0; at R1=R3=R5=H, R2=C(O)CH3, R4=N+(CH3)2C12H25, n=1, m=0; at R1=R3=R5=H, R2=C(O)CH3, R4=N+(CH3)2C18H37, n=1, m=0; at R1=R2=R3=R5=H, R4=N+(CH3)2C8H17, n=1, m=1; at R1=R2=R3=R5=H, R4=N+(CH3)2C12H25, n=1, m=1; at R1=R2=R3=R5=H, R4=N+(CH3)2C18H37, n=1, m=1; at R1=N+(CH3)2C8H17, R2+R3=-C(CH3)2O-, R4+R5=-OC(CH3)2OCH2-, n=1, m=0; at R1=N+(CH3)2C18H37, R2+R3=-C(CH3)2O-, R4+R5=-OC(CH3)2OCH2-, n=1, m=0; at R1=N+(CH3)2C8H17, R2+R3=-C(CH3)2O-, R4=OH, R5=CH2OH, n=1, m=1; at R1=N+(CH3)2C18H37, R2=H, R3=R4=OH, R5=CH2OH, n=1, m=1.EFFECT: invention can be used in medicine and veterinary science.1 cl, 2 tbl, 30 ex
ethod of producing 2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazatetracyclo[5,5,0,03,11,05,9]dodecane // 2607517
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, more specifically to a method of producing 2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazatetracyclo[5,5,0,03,11,05,9]dodecane, used as highly efficient explosive. Disclosed method involves nitration of 2,6,8,12-tetraacetyl-2,4,6,8,10,12-hexaazatetracyclo[5,5,0,03,11,05,9]dodecane with a sulphuric-nitric mixture and is characterised by that 2,6,8,12-tetraacetyl-2,4,6,8,10,12-hexaazatetracyclo[5,5,0,03,11,05,9]dodecane is nitrated in crystalline form or in form of its aqueous-acetic solution of anhydrous sulphuric-nitric mixture containing free sulphuric anhydride. During nitration in crystalline form anhydrous sulphuric-nitric mixture containing free sulphuric anhydride in amount of 0.1–6.0 % is used, and during nitration in form of aqueous-acetic solution – anhydrous sulphuric-nitric mixture containing free sulphuric anhydride in amount of 6.0–15.0 %.EFFECT: method enables to obtain an end product with high output and purity.1 cl, 4 ex
ethod of producing molecular complex [1,2,5]oxadiazolo[3,4-e][1,2,3,4]-tetrazine-4,6-di-n-oxide with 2,4-dinitro-2,4-diazapentane // 2607516
FIELD: chemistry.SUBSTANCE: invention relates to a method of producing molecular complex [1,2,5]oxadiazolo[3,4-e][1,2,3,4]-tetrazine-4,6-di-N-oxide with 2,4-dinitro-2,4-diazapentane (FTDO-DNP), involving preparation of a solution of [1,2,5]oxadiazolo[3,4-e][1,2,3,4]-tetrazine-4,6-di-N-oxide using a mixture of polar halogen-derivative aprotic solvents, adding to obtained solution 2,4-dinitro-2,4-diazapentane, mixing at a temperature of 11–15 °C, and then adding a non-polar hydrocarbon precipitator.EFFECT: safe and efficient method of producing molecular complex FTDO-DNP which enables to increase output of end product.3 cl, 6 ex
Crystalline form of sodium salt of 4-tert-butyl-n-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]-benzenesulfonamide // 2607515
FIELD: chemistry.SUBSTANCE: invention relates to a novel crystalline form of a sodium salt of 4-tert-butyl-N-[4-chloro-2-(1- oxy-pyridine-4-carbonyl)-phenyl]-benzenesulphonamide.EFFECT: said crystalline form can be used in treating inflammatory bowel disease.19 cl, 10 dwg, 2 tbl, 3 ex
Polymorphic forms of sodium salt of 4-tert-butyl-n-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]-benzenesulphonamide // 2607514
FIELD: chemistry.SUBSTANCE: invention relates to novel polymorphic trihydrated forms of sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl] benzenesulphonamide.EFFECT: disclosed polymorphic forms can be used for treating inflammatory bowel disease.10 cl, 8 dwg, 2 tbl, 3 ex
Pyrazolopyrimidines and related heterocycles as ck2 inhibitors // 2607453
FIELD: chemistry.SUBSTANCE: invention relates to novel compounds of formula (II) or (II') or pharmaceutically acceptable salts thereof. Compounds inhibit activity of protein kinase CK2 (casein kinase II) or PIM kinase and can be used for treating proliferative diseases selected from cancer of various cell lines, such as breast cancer, lung, skin cancer etc, angiogenesis, as well as other kinase related conditions, including inflammation, vascular diseases, pathogenic infections, neurodegenerative diseases, some immunological diseases. In compounds of formula (II) or (II') or Z3 denotes N and Z4 denotes CR5; or Z3 denotes CR5 and Z4 denotes N; or Z3 and Z4 both denote N; each R5 is independently selected from halo, -CN and -R, where each R is independently selected from H and optionally substituted C1-C4 alkyl; each R2, R3 and R4 is independently selected from H and optionally substituted C1-C10 alkyl; X denotes S or NR2; Y is O or S; Z is O or S; L is a bond, -CR7=CR8-, -C≡C- or -(CR7R8)m-, and W is optionally substituted C1-C10alkyl, optionally substituted with 1-10-member heteroalkyl, optionally substituted C6-C12aryl, Optionally substituted 5-12-member heteroaryl, -NR7R8, -OR7, -S(O)nR7, -CONR7R8, optionally substituted 3-10-member heterocyclyl, optionally substituted with C3-C10carbocyclyl, optionally substituted C2-C10alkenyl, optionally substituted C2-C10alkynyl or -CR7R8R9; or L is a bond, -NR7-, -O-, -S(O)n-, -(CR7R8)m- or -(CR7R8)m-NR7-; and W is selected from optionally substituted C6-C12aryl, optionally substituted 5-12-member heteroaryl and -NR7R8; where each R7 and R8 and R9 is independently selected from H, optionally substituted C1-C10alkyl, optionally substituted 1-10-member heteroalkyl, optionally substituted C3-C10carbocyclyl, optionally substituted 3-10-member heterocyclyl, optionally substituted C3-C10carbocyclylalkyl, optionally substituted 3-10-member heterocyclylC1-C8-alkyl, optionally substituted C6-C12aryl, optionally substituted C7-C12arylalkyl, optionally substituted 5-12-member heteroaryl and optionally substituted 5-12-member heteroarylC1-C8alkyl; or R8 and R9, taken together with carbon atom to which they are bonded form =O(oxo); or R7 and R8, taken together and arranged on one carbon atom or on adjacent bonded atoms (CR7R8)m, either alone, or as part of another group, form a 3-8-member carbocyclic ring or a heterocyclic ring; or R7 and R8, taken together with a nitrogen atom to which they are bonded, form an optionally substituted 5-10-member heterocyclic or heteroaryl ring, which optionally contains one or more additional ring heteroatoms selected from N, O and S; provided that no more than one group from R7 and R8 in -NR7R8 is selected from a group consisting of alkoxy, alkylamino, dialkylamino and heterocyclyl; each n is independently equal to 0, 1 or 2; each m is independently equal to 1, 2, 3 or 4; and R1A is selected from H, optionally substituted C1-C10alkyl; and R1B each is independently selected from H, optionally substituted C1-C10alkyl, optionally substituted 3-10-member heterocyclyl, optionally substituted C3-C10carbocyclyl, optionally substituted C3-C10carbocyclylalkyl, optionally substituted 3-10-member heterocyclyl-C1-C8alkyl, optionally substituted C6-C12aryl, optionally substituted C7-C12arylalkyl, optionally substituted 5-12-member heteroaryl or optionally substituted 5-12-member heteroaryl-C1-C8alkyl.EFFECT: substitutes for saturated and unsaturated carbon atoms are selected from corresponding groups specified in patent claim.58 cl, 14 dwg, 113 tbl, 299 ex
ethods of producing viral particles with simplified surface proteins' glycosylation // 2607452
FIELD: biotechnology.SUBSTANCE: present invention relates to biotechnology. Method for production of influenza virus with monoglycosylated hemagglutinin-antigen (HA-antigen) is disclosed. Method involves cultivation of influenza virus, containing hemagglutinin-antigen in specific pathogen free (SPF) chicken egg with embryo with an effective amount of mannosidase inhibitor, concentration of which is sufficient for inhibiting of α-mannosidase I in the path of N-glycosylation followed by extraction of produced influenza virus. Further contact of extracted influenza virus with endoglycosidase (EndoH) leads to production of influenza virus, having monoglycosylated influenza virus HA-antigen.EFFECT: disclosed method enables to obtain influenza virus with monoglycosylated hemagglutinin-antigen (HA-antigen) with high yield using specific pathogen free (SPF) chicken eggs with embryo, and can be used for producing monoglycosylated hemagglutinin-antigen in production of vaccines.19 cl, 4 dwg, 4 ex
Imine derivatives of camphor, containing aromatic or heteroaromatic fragment - inhibitors of reproduction of flu virus (strain a/california/07/09(h1n1)pdm09) // 2607451
FIELD: medicine.SUBSTANCE: invention relates to medicine and pharmaceutics, namely to use of camphor imine derivatives of general formula I, where n=0, 1, 2; X=CH or N, R – hydroxy, alkoxy group, as inhibitors of reproduction of flu virus (strain A/California/07/09(H1N1)pdm09).EFFECT: said imine compounds exhibit evident antiviral activity along with low toxicity.1 cl, 1 tbl, 10 ex
ethod for stabilization of gas condensate // 2607394
FIELD: gas industry.SUBSTANCE: invention relates to methods of preparing gas condensate for single-phase transfer and can be used in gas industry. Method for stabilization of gas condensate comprises separation of reduced unstable condensate, which is carried out in one stage in a film column, consisting of a cooled reflux and a heated stripping sections and a feed zone, located between them. As cooling medium reflux section is supplied with reduced unstable condensate, and then it is directed into supply zone. From reflux section top hydrocarbon gas is discharged, and from stripping section bottom condensate is discharged, which is divided into two parts. One part of condensate is heated and separated with formation of separation gas, which is directed to the bottom of the stripping section as a stripping agent, and a separation residue, which is mixed with another part of condensate, supplied as heat carrier into stripping section and discharged as commercial condensate. Hydrocarbon gas is compressed, cooled down and separated under dephlegmation conditions and reflux stabilization to produce propane-butane fraction and gas weathering.EFFECT: technical result is increased output and wider range of commercial products, reducing amount of weathering gas and power saving.1 cl, 1 dwg
Cancer antigen // 2607379
FIELD: biotechnology.SUBSTANCE: invention relates to biotechnology, specifically to antigen expression induction on cancer cells, and can be used in medicine. Treatment of cancer cells with agent selected from Mycobacterium w, cisplatin, paclitaxel, Gemcitabine and combinations thereof, obtaining cancer antigens: protein 45 kDa, expressed by pancreatic cancer cells, and protein 36 kDa, expressed by melanoma cells.EFFECT: invention enables to obtain tumor-specific antigen expressed by cancer cells treated by said agent, capable of immune response inducing on homologous and heterogeneous cancer cells, originating from same tissue/same organ.5 cl, 4 dwg, 1 tbl, 8 ex
New antibody to c-met // 2607377
FIELD: biochemistry.SUBSTANCE: invention relates to biochemistry, namely to monoclonal antibody, which is capable of inhibiting dimerization of c-Met. Composition for preventing and treating cancer, associated with c-Met, containing said antibody is also disclosed. Application of said antibody and composition is disclosed for preparing therapeutic agent against cancer, associated with c-Met.EFFECT: invention is capable of total inhibiting dimerization of c-Met, which enables effective treatment of cancer, characterized by ligand-independent c-Met activation.19 cl, 39 dwg, 4 tbl, 20 ex
Versions of albumin // 2607374
FIELD: biotechnology.SUBSTANCE: present invention relates to biotechnology, namely to production of versions of albumin with changed half-life period in plasma in comparison with initial albumin, and can be used in medicine. Version of albumin is obtained, containing one or more substitutes relative to SEQ ID NO: 2, selected from following: 1) E492A, C, D, F, G, H, I, K, L, M, N, Q, R; 2) K500I, R; 3) N503H; 4) E505Q; 5) H510D; 6) D550E, H, I, M, N, R, S, W; 7) K573A, C, D, F, G, H, I, L, M, N, P, R, S, V, W, Y; 8) K574D, F, G, H, I, L, M, P, R, S, T, V, W, Y; 9) A578F; 10) S579C; 11) Q580I, K, M, R, V; or 12) G584D.EFFECT: invention enables to obtain version of albumin or its fragment, capable to bind with FcRn, or chimeric polypeptide, including said version of albumin or its fragment, with longer half-life period in plasma or increased binding affinity with FcRn in comparison with initial albumin, its fragment or chimeric polypeptide.10 cl, 32 dwg, 22 tbl, 22 ex
odification of group 6 poaceae (bluegrass) allergens with low allergenic capacity due to mutagenesis of proline residues // 2607373
FIELD: biotechnology.SUBSTANCE: present invention relates to biotechnology, namely to recombinant modifications of group 6 Poaceae (bluegrass) allergens, and can be used in medicine for preventing or treating type 1 allergies, in initiation of which group 6 bluegrass allergens are involved. Recombinant allergen Phl p 6 is obtained, in which prolines, corresponding in linearized form to prolines in positions 29, 30, 57 and 79 of amino acid sequence of wild type protein Phl p 6 in compliance with SEQ ID NO: 2, are mutated separately or in combination by point mutations, selected from deletions and substitutions of amino acids.EFFECT: present invention enables to obtain recombinant allergen Phl p 6 with low IgE reactivity, compared to existing non-mutated allergens, and with substantially preserved T-lymphocytes reactivity at the same time.12 cl, 20 dwg, 2 tbl, 3 ex
Substituted n2-(4-amino-2-methoxyphenyl)-n4-[2-(dimethylphosphoryl)-phenyl]-5-chloro-pyrimidine-2,4-diamines as modulators of alk and egfr, applicable for treating cancer // 2607371
FIELD: chemistry.SUBSTANCE: invention relates to novel substituted N2-(4-amino-2-methoxyphenyl)-N4-[2-(dimethylphosphoryl)-phenyl]-5-chloro-pyrimidine-2,4-diamines of general formula 1 and their stereoisomers, N4-[2-(dimethylphosphoryl)-phenyl]-N2-{4-[4-(1-methyl-1,8-diaza-spiro[4.5]dec-8-yl)-piperidin-1-yl]-2-methoxyphenyl}-5-chloro-pyrimidine-2,4-diamine and their pharmaceutically acceptable salts. Compounds have anti-cancer effect and can be used for preparing a drug for preventing or treating cancer, in particular, non-small cell lung cancer (NSCLC), including with metastases in brain. In compounds of general formula 1 1, R denotes a substitute, selected from a series (a)-(o): (a)-(c), (e)-(i), (k)-(l), (m)-(o), in which R2, R3, R4 and R5 are optionally identical C1-C4alkyls; n is an optionally identical number 1 or 2; arrow indicates binding point of substitute. Invention also relates to a method of producing compounds of formula 1.EFFECT: method comprises reacting compounds of general formula 2, 1_1(17) where R is a substitute selected from corresponding substitutes given above, with N-[2-(dimethylphosphoryl)phenyl]-2,5-dichloro-pyrimidine-4-amine of formula 1_1(17).12 cl, 2 tbl, 4 ex
Pharmaceutical composition for treatment and/or prevention of cancer // 2607366
FIELD: biochemistry.SUBSTANCE: invention relates to biochemistry, particularly to an antibody which specifically binds with CAPRIN-1 protein and having immunological reactivity with respect to a partial polypeptide of CAPRIN-1 protein, wherein said antibody has cytotoxic activity against a cancer cell expressing CAPRIN-1 protein, as well as a medicinal agent containing same. Invention also relates to a method of treating or preventing CAPRIN-1 expressing cancer using said antibody or composition.EFFECT: invention provides effective treatment or prevention of CAPRIN-1 expressing cancer.17 cl, 3 dwg, 6 ex
Conjugate, containing oxyntomodulin and fragment of immunoglobulin, and use thereof // 2607365
FIELD: biotechnology.SUBSTANCE: invention relates to biotechnology, namely to conjugates of oxyntomodulin with immunoglobulin Fc-region, and can be used in medicine for treating obesity. Conjugate, capable of activating receptor CLP-1 (glucagon-like peptide-1), and glucagon receptor, are obtained, which contains derivative of oxyntomodulin with SEQ ID NO: 23, 24, 25, 32, 33 or 34, covalently bound with Fc-region of immunoglobulin by polyethylene glycol.EFFECT: invention enables to obtain conjugate of oxyntomodulin, which reduces food consumption, suppresses gastric emptying and promotes lipolysis without side effects in contrast to native oxyntomodulin and also shows excellent receptor-activating effects and long-term stability as compared to native oxyntomodulin.18 cl, 13 dwg, 4 tbl, 18 ex
ethod of producing 2,3-diamino-1,4-naphthoquinones // 2607192
FIELD: chemistry.SUBSTANCE: invention relates to a novel method of producing 2,3-diamino-1,4-naphthoquinones of general formula given below, which can be used for producing anticancer, antiviral compounds or herbicides. 2,3-diamino-1.4-naphthoquinones correspond to general formula , where R = H, CH3, C2H5 and other residues of saturated hydrocarbons, such as butyl and isobutyl. Method consists in that 2-(R-amino)-3-nitro-1,4-naphthoquinone is reduced in a solution consisting of ethanol, water and sodium dithionite to end products according to following scheme: . Method enables to obtain in a single step 2,3-diamino-1,4-naphthoquinone and expand range of compounds.EFFECT: wherein products are produced with higher output (up to 61–84 %).1 cl, 5 ex
Polymorphic forms of sodium salt of 4-tert-butyl-n-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]-benzenesulphonamide // 2607191
FIELD: chemistry.SUBSTANCE: invention relates to novel polymorphic solvated and desolvated forms of sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]-benzenesulphonamide.EFFECT: said polymorphs can be used for treating inflammatory bowel disease.20 cl, 18 dwg, 5 tbl, 6 ex
ethod of controlling process control and list of produced oil products during oil refining (versions) // 2607089
FIELD: oil industry.SUBSTANCE: invention relates to a method of controlling process and list of produced oil products during oil refining. Method comprises the most complete physical separation into fractions and is characterised by that to increase output of most valuable light fractions, oil is subjected to cryolysis at temperature not higher than -15 °C for not less than 20 hours with preliminary addition of a donor additive (water) in amount of not less than 1 % at different processing steps: before fractionation, instead of vacuum distillation at oil fields, where simultaneously with increase in content of fuel fractions in oil fractions there is its dewatering and desalination (partial or complete), as well as in various combinations of processing steps, for example before fractionation and instead of vacuum distillation or at oil fields and instead of vacuum distillation.EFFECT: use of disclosed method makes it possible to increase number of extracted fuel fractions.1 cl, 1 dwg, 5 tbl
Crystals of 6,7-unsaturated-7-carbamoyl morphinane derivative, and method for producing same // 2607084
FIELD: chemistry.SUBSTANCE: invention relates to salts of p-toluenesulphonic acid compound of formula (IA) or hydrate thereof, including crystalline forms thereof. Invention relates to form I of crystals of hydrate of salt of p-toluenesulphonic acid compound of formula (IA), where X-ray diffraction spectrum of powder of crystalline has peaks, corresponding to diffraction angles (2θ): 12.9°±0.2°, 17.6°±0.2°, 22.4°±0.2°, 25.4°±0.2° and 28.7°±0.2°. Invention also relates to form II of crystals of hydrate of salt of p-toluenesulphonic acid compound of formula (IA), where X-ray diffraction spectrum of powder of crystalline has peaks, corresponding to diffraction angles (2θ): 8.8°±0.2°, 17.5°±0.2°, 21.9°±0.2°, 23.7°±0.2° and 26.1°±0.2°. Crystalline forms of salts of p-toluenesulphonic acid compound of formula (IA) and hydrates thereof are intended for preparing a pharmaceutical composition, exhibiting agonistic activity with respect to opioid receptor. Crystalline form of salt of p-toluenesulphonic acid compound of formula (IA) or crystalline forms of hydrate of said salt of p-toluenesulphonic acid is obtained by adding p-toluenesulphonic acid to a compound of formula (IA) and crystallisation of salt of p-toluenesulphonic acid or hydrate thereof in a solvent. Method of producing crystalline form or crystalline form of hydrates of said salt of p-toluenesulphonic acid of formula (IA) can also be performed in following steps: 1) treating with a base compound of formula (IIE), where R1a is hydrogen or protecting hydroxyl group, which can be removed by a base selected from a group, consisting of acetyl, formyl, benzoyl, chloroacetyl, pivaloyl, methyl carbonate, isobutyl carbonate, benzyl carbonate, vinyl carbonate, phenyl carbamate, mesyl and tosyl, 2) adding p-toluenesulphonic acid and 3) crystallisation of salt of p-toluenesulphonic acid in a solvent.EFFECT: technical result is stable form of 6,7-unsaturated-7-carbamoyl morphinane.14 cl, 19 tbl, 26 ex ,
High-purity cyclopeptide crystal as well as preparation method and use thereof // 2607083
FIELD: chemistry.SUBSTANCE: invention relates to a cyclopeptide crystal of formula I, methods for preparing and use thereof for producing a compound, having antifungal activity. Cyclopeptide crystal has high purity and stability.EFFECT: method of production enables to obtain a cyclopeptide crystal of formula I with high output and acceptable for large-scale production.26 cl, 2 tbl, 14 dwg
Chemical compounds // 2607082
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula (I) and formula (II), where R1 and R2, independently from each other, are selected from aliphatic hydrocarbons, containing from 1 carbon atom to 30 carbon atoms, provided that at least one of R1 and R2 is selected from aliphatic hydrocarbons containing at least 8 carbon atoms, and A is a halogen as a hydrophobicity-providing agent, such as adhesive for making paper.EFFECT: invention discloses chemical compounds.9 cl, 2 tbl, 6 ex
Sulfonamide derivative and medicinal use thereof // 2607081
FIELD: chemistry; pharmaceutics.SUBSTANCE: invention relates to novel sulfonamide derivatives of general formula (1) or pharmaceutically acceptable salts thereof, possessing the properties of inhibition integrin α4β7. In general formula (1) (1), A means a group presented by general formula (2-1) or (2-2) , where Arm is a 5- or 6-member aromatic ring, containing 0, 1 or 2 heteroatoms, selected from nitrogen atoms, R1 and R11, each, independently, represents any substitute selected from a hydrogen atom, halogen atom, lower alkyl group, lower alkoxy group, mono- or di-lower alkylamino group, R12, R13 and R14, each, independently, represents any substitute selected from a hydrogen atom, lower alkyl group, lower alkoxy group, amino group, lower alkylamino group, low di(alkyl)amino group or (lower alkylamino)lower alkyl group, R2 and R3, each, independently, represents any substitute selected from a hydrogen atom, lower alkyl group or lower alkoxy group, B is represents any substitute selected from lower alkoxy group, optionally substituted by hydroxyl group, lower alkyl group, mono- or di-lower alkylamino group; C3-C6cyclic alkoxy group and/or 6-member(s) heterocyclic(s) group (groups) with an oxygen atom, sulphur atom or a nitrogen atom as heteroatom, hydroxyl group, R41 is represents a hydrogen atom or lower alkyl group, a, b, c and d, each, independently, represents C-R31, C-R32, C-R33 and C-R34 respectively, but one or two of a, b, c and d, each, can be a nitrogen atom, R31, R32, R33 and R34, each, independently, represents any substitute selected from a hydrogen atom, halogen atom, lower alkyl group, lower alkoxy group, provided that any R31, R32, R33 and R34 represents a halogen atom or lower alkyl group, e, f, g and h, each, independently, represents C-R35, C-R36, C-R37 and C-R38 respectively, however, one or two of e, f, g and h, each, can be a nitrogen atom, R35, R36, R37 and R38, each, independently, represents any substitute selected from a hydrogen atom, lower alkyl group or lower alkoxy group, D represents a phenyl group or a 5 -or 6-member aromatic heterocyclic group, containing a nitrogen atom, an oxygen atom or sulphur atom, optionally containing a substitute(s), selected from a group consisting of hydroxyl groups, lower alkyl groups, lower alkoxy groups, E is a 5- or 6-member heterocyclic group with 1-4 heteroatoms, selected from nitrogen atoms, an oxygen atom and sulphur atom in the cycle, optionally containing a substitute(s), selected from a group consisting of halogen atoms, hydroxyl groups, lower alkyl groups, lower alkoxy groups, amino groups, 4- or 6-member cyclic amino groups, carboxyl groups and lower alkoxy-carbonyl groups; aminocarbonyl group, optionally containing a substitute(s) selected from the group, consisting of hydroxyl groups, lower alkyl groups, lower alkoxy groups, 5- or 6-member heterocyclic groups, containing 1, 2, 3 or 4 heteroatoms, selected from a group consisting of oxygen atoms, sulphur atoms and nitrogen atoms as a component(s) ring atom(s), and substituted by heterocycle of lower alkyl groups, where heterocycle means a 5- or 6-member heterocyclic groups, containing 1, 2, 3 or 4 heteroatoms, selected from group consisting of oxygen atoms, sulphur atoms and nitrogen atoms as a component(s) ring atom(s); hydrogen atom, hydroxyl group, lower alkyl group, lower alkoxy group, amino group, lower alkyl-carbonyl group, lower alkyloxy-carbonyl group or a lower alkylaminoalkilen group, and provided that the lowest alkyl-carbonyl group and the lowest alkyloxycarbonil group can be, each of which, are connected to a phenyl group, presented D, to form condensed ring.EFFECT: compounds can be used for treating or preventing an inflammatory disease, in which the pathological condition associated with indirect by integrins α4β7 adhesion process.15 cl, 2 tbl, 258 ex
Spiro-condensed cyclohexane derivatives as inhibitors of hsl, effective for diabetes treatment // 2607080
FIELD: pharmaceutics.SUBSTANCE: present invention relates to novel compounds of formula (I), as well as to their pharmaceutically acceptable salts possessing activity of HSL inhibitors, to pharmaceutical composition, method of inhibiting of enzyme HSL lipase, as well as to use of disclosed compounds for preparing a drug. Values R1, R2, R3, Ca and Cb are given in the claim.EFFECT: invention discloses spiro-condensed cyclohexane derivatives as inhibitors of HSL, effective for diabetes treatment.24 cl, 377 ex
Benzylamine derivatives as inhibitors of plasma kallikrein // 2607045
FIELD: chemistry.SUBSTANCE: present invention relates to compounds of formula (I), compositions containing such compounds; use of such compounds in therapy for treating or preventing diseases or conditions, involving plasma kallikrein activity; and methods of treating patients with using said compounds; where R1 is selected from H, alkyl, -COalkyl, -COaryl, -COheteroaryl, -(CH2)aOH, -(CH2)bCOOR10, -(CH2)cCONH2, -SO2alkyl, -SO2aryl, -SO2(CH2)hR13, -CO(CH2)iR14, -COcycloalkyl, -COCH=CHR15, -CO(CH2)jNHCO(CH2)kR16 and -CONR17R18; R2 is selected from H and alkyl; R3 is selected from alkyl, -(CH2)daryl, -(CH2)eheteroaryl, (CH2)fcycloalkyl, -CH(cycloalkyl)2 and -(CH2)laryl-O-(CH2)m-aryl; R4 and R6 are independently selected from H and alkyl; R5 is selected from H and OH; or R4 and R5, together with atoms to which they are bonded, can be bonded to form a 5- or 6-member azacycloalkyl structure; R7 is selected from H and halogen; R8 is selected from H, alkyl, halogen and CF3; R9 represents aryl or heteroaryl; R10 represents H or alkyl; a, b, c, d, e, f, g, h, i, j, l and m independently represent 1, 2 or 3; k is equal to 0, 1, 2 or 3; *1 and *2 denote chiral centres.EFFECT: novel compounds.19 cl, 2 dwg, 15 tbl, 201 ex
Antigen-binding proteins // 2607038
FIELD: medicine.SUBSTANCE: invention relates to immunology. Method of producing antigen-binding protein and host cell for its production are proposed. Antigen-binding protein obtained using present invention includes: a) two modified heavy chains of antibody, in which VH of each heavy chain has been replaced for VL of said antibody and which are linked to each other via their CH3-domains of Fc-part; and b) two modified heavy chains of antibody, in which CH1 of each heavy chain has been replaced for CL of above antibody and which are linked to each other via their CH3-domains of Fc-part; wherein VL-domains of heavy chains a) are linked to VH domains of heavy chains b), and CH1-domains of heavy chains a) are linked to CL-domains of heavy chains b).EFFECT: obtained antigen-binding protein shows increased antibody-dependent cell mediated cytotoxicity (ADCC).14 cl, 12 dwg, 5 tbl, 10 ex
Nd2 peptides and methods of treating neurological disease // 2607033
FIELD: biotechnology.SUBSTANCE: invention relates to biotechnology, specifically to identifying a core region of ND2 responsible for interacting with Src, and can be used in medicine. Peptides are obtained, no more than 20 amino acid residues ND2 region, containing residues 310-321.EFFECT: invention enables to obtain peptides inhibiting interaction ND2 with Src, that can be used for effective therapy of stroke and pain.15 cl, 23 dwg, 9 ex
Antibody fc variants // 2607014
FIELD: biochemistry.SUBSTANCE: invention relates to biochemistry, in particular, to modified polypeptides containing Fc variants and their uses. Disclosed a polypeptide, having reduced affinity to Fc-receptors and containing modified Fc region of human IgG1 of wild type. Modified Fc region comprises replacement of R329G, L234A and L235A in accordance with a system of EU index at Kabat. Polypeptide is used for treat a disease, in which it is desirable to reduce effector function mediated by polypeptide.EFFECT: invention allows to reduce the effector function of polypeptide containing modified Fc region of human IgG1, in order to reduce undesirable toxicity and side effects in treating the patients said polypeptide.12 cl, 16 dwg, 4 tbl, 8 ex
Process for maximum distillate production from fluid catalytic cracking units (fccu) // 2606971
FIELD: chemistry.SUBSTANCE: invention relates to a method for increasing middle distillate production and quality from a hydrocarbon feed. Method includes: a) delivering a partially-regenerated catalyst or a fully- regenerated catalyst, having MAT activity (MAT - microactivity) from 30 wt% to 65 wt%, to a first riser reactor and fully- regenerated catalyst having MAT activity from 50 wt% to 80 wt%, to a second riser reactor; b) cracking first feed in first riser reactor, where catalyst has carbon content on regenerated catalyst (CRC) of 0.2 wt% to 0.5 wt%, to obtain a first cracked product and spent catalyst; c) separating said first cracked product including a middle distillate from said spent catalyst in a single reactor vessel; d) recovering said first cracked product including said middle distillate and separating uncracked bottoms from said first cracked product; e) cracking second feed containing uncracked bottoms from step (d) in second riser reactor to produce a second cracked product; f) separating second cracked product including LHG and middle distillate from spent catalyst in said single reactor vessel; and g) passing spent catalyst from first and second riser reactors to a single two-stage catalyst regenerator device, where spent catalyst is partially regenerated in first stage of said two-stage catalyst regenerator to obtain said partially regenerated catalyst and part of said partially regenerated catalyst is fed into second regeneration stage of said two-stage catalyst regenerator to obtain fully regenerated catalyst, said catalyst regeneration device provides said partially regenerated catalyst and said fully regenerated catalyst, having a different MAT activity. Invention also relates to a system.EFFECT: use of present method enables to maximise production required product.32 cl, 6 dwg
ethod of inhibiting undesirable radical polymerization of acrylic acid available in liquid phase p // 2606953
FIELD: technological processes.SUBSTANCE: present invention relates to a method of inhibiting undesirable radical polymerization of acrylic acid in liquid phase P in storage or process operation, content of acrylic acid which is at least 10 wt %, and which, in terms of weight contained in it of acrylic acid, additionally contains 100 ppm by weight to ≤ 5 wt% propionic acid and from 100 ppm by weight to ≤ 5 wt% of glyoxal. According to the invention to liquid phase p is added at least one chemical compound of copper element, and at least one chemical compound containing copper in one of degrees of oxidation +2, +1, added in amount which provides content of added copper in liquid phase P in terms of the molar amount of acrylic acid contained therein, in the amount of 0.01 mole ppm to 5 mole per cent, the liquid phase P is subjected to thermal separation different from crystallization.EFFECT: effective prevention of undesirable radical polymerization of acrylic acid.16 cl, 2 ex
Dichloroacetates of substituted n4-[2-(dimethylphosphoryl)phenyl]-n2-(2-methoxy-4-piperidin-1-ylphenyl)-5-chloropyrimidine-2,4-diamines as modulators of alk and egfr, intended for treating cancer // 2606951
FIELD: chemistry.SUBSTANCE: invention relates to novel compounds – dichloroacetates of substituted N4-[2-(dimethylphosphoryl)phenyl]-N2-(2-methoxy-4-piperidin-1-ylphenyl)-5-chloropyrimidine-2,4-diamine of general formula 1, which are modulators of ALK and EGFR and can be used for preventing and/or treating cancer, in particular for treating non-small cell lung cancer (NSCLC), including with metastases in brain. In formula 1 R represents dimethylamine group or 4-methylpiperazin-1-yl fragment, and k is a number 1, 2 or 3. Invention also relates to a pharmaceutical composition, containing said compound as an active component in therapeutically effective amount in combination with pharmaceutically acceptable diluent and/or carrier. Composition can be made in form of tablets, capsules or injections, placed in a pharmaceutically acceptable packaging.EFFECT: invention also relates to a method of producing a compound of formula 1 by reacting a compound of general formula 2, where R is a dimethylamine group or 4-methylpiperazin-1-yl fragment, with 1, 2 or 3 equivalents of 2,2-dichloroacetic acid.11 cl, 2 tbl, 10 ex
Substituted n-{3-[4-(1-methyl-1h-indol-3-yl)pyrimidin-2-ylamino]-4-methoxyphenyl}-amides as modulators of egfr, applicable for treating cancer // 2606949
FIELD: chemistry.SUBSTANCE: invention relates to novel substituted N-{3-[4-(1-methyl-1H-indol-3-yl)pyrimidin-2-ylamino]-4-methoxyphenyl}-amides of general formula 1 and pharmaceutically acceptable salts thereof, having properties of modulators of EGFR and suitable for treating cancer, for example small cell lung cancer. In general formula 1 R1 represents CH2=C(R3)-, R3CH=CH-; R2 is (2-dimethylaminoethyl)-methylamino, 3-dimethylaminopiperidin-1-yl; R3 is fluorine, trifluoromethyl, dimethylcarbamoyl; or R2 is 3-dimethylaminopiperidin-1-yl; R3 is H; or mesylate compound 1, where R1 is C(CH3)≡C-, R2 is (2-dimethylaminoethyl)-methylamino. Preferable compounds are N-{2-[(2-dimethylaminoethyl)-methylamino]-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenyl}-2-fluoro-acrylamide (1.2); N-{2-[(2-dimethylaminoethyl)-methylamino]-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenyl}-4,4,4-trifluorobut-2-enamide (1.6); (E)-3-{2-[(2-dimethylaminoethyl)-methylamino]-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenylcarbamoyl}-N,N-dimethylacrylamide (1.8); N-{2-(3-dimethylaminopiperidin-1-yl)-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenyl}-acrylamide (1.11); mesylate N-{2-[(2-dimethylaminoethyl)-methylamino]-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenyl}-2-butynamide (1.14⋅CH3SO3H) or mesylate N-{2-(3-dimethylaminopiperidin-1-yl)-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenyl}-acrylamide (1.11⋅CH3SO3H). Invention also relates to a method of producing compounds of formula 1.EFFECT: method involves reacting a compound of formula 2 or its salt with activated derivative of corresponding organic acid, such as an acid, ester or organic acid anhydride.15 cl, 2 tbl, 14 ex
Boron-containing small molecules // 2606947
FIELD: pharmaceutics.SUBSTANCE: invention relates to boron-containing compounds, namely to the compound which represents 5-fluoro-1,3-dihydro-1-hydroxy-3-methyl-2,1-benzoxaborole, 6-fluoro-1-hydroxy-1,2,3,4-tetrahydro-2,1-benzoxaborine, 5-cyano-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 1,3-dihydro-1-hydroxy-5-methyl-2,1-benzoxaborole, 1,3-dihydro-1-hydroxy-5-hydroxymethyl-2,1-benzoxaborole, 7-hydroxy-2,1-oxaborolano[5,4-cl]pyridine, 3-benzyl-1,3-dihydro-1-hydroxy-3-methyl-2,1-benzoxaborole, 3-benzyl-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 6-phenoxy-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 5-(N-methyl-N-phenyl sulfanilamide)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 6-(4-methoxyphenyl sulfonyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 6-(4- methoxyphenyl sulfonyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole or 4-(4-cyano-phenoxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole or its pharmaceutically acceptable salt. Invention also discloses the compound and its pharmaceutically acceptable salt of formula (IIb), pharmaceutical compositions, use of compounds and pharmaceutical compositions.EFFECT: invention enables to obtain compounds applicable for treating or preventing infection.84 cl, 12 dwg, 6 tbl, 20 ex
Short biologically active peptides for accelerating wound healing // 2606753
FIELD: biotechnology.SUBSTANCE: invention relates to biotechnology, namely to cell technologies, and can be used for skin care or for treating skin wounds or mucous membrane tissue of mammal. Following peptides are obtained: EKMG, MGRN and KMGRN – short fragments of peptide HB-107 (MPKEKVFLKIEKMGRNIRN), which itself is fragment of antimicrobial protein cecropin B and exhibits properties of cell migration stimulation. Peptides can be amidated at C-end or lipidized at N-end.EFFECT: present invention enables to obtain peptide with improved activity in human skin fibroblasts stimulation compared to peptide HB107 – cecropin B fragment.16 cl, 3 tbl, 4 ex
Pesticide compositions // 2606641
FIELD: chemistry.SUBSTANCE: invention relates to a compound of Formula One, where R10 is substituted pyridine of formula (a), R1 is selected from H, F, Cl, Br, I or substituted or unsubstituted C1-C6 alkyl, where each R1, which is substituted, has one or more substitutes selected from F, Cl, Br or I; R2 is H, F, Cl, Br, I or a substituted or unsubstituted C1-C6 alkyl, where each R2, which is substituted, has one or more substitutes selected from F, Cl, Br or I; R3 is H or unsubstituted C1-C6 alkyl; R4 is O, S; R5 is (C1-C12 alkyl)S(O)n(C1-C12 alkyl), R7 is H, F, Cl, Br, I or a substituted or unsubstituted C1-C6 alkyl, where each R7, which is substituted, has one or more substitutes selected from F, Cl, Br or I; R8 is H, F, Cl, Br, I or a substituted or unsubstituted C1-C6 alkyl, where each R8, which is substituted, has one or more substitutes selected from F, Cl, Br or I; and n is (each independently) 0, 1 or 2. Compounds of Formula One are intended for pest control, performed by applying compound on a surface in an amount, sufficient for control.EFFECT: technical result is compound for pest control.3 cl, 4 tbl, 47 ex , (а)
Sulphonic acid salts of heterocyclylamide-substituted imidazoles // 2606639
FIELD: chemistry.SUBSTANCE: invention relates to a salt of a compound of formula wherein R1 denotes methyl, ethyl, butyl or cyclopropylmethyl, R2 denotes phenyl, where phenyl contains a substitute selected from a group, including trifluoromethoxy group and difluoromethoxy group, and R3 denotes hydrogen, methyl, chloro, methoxy group or trifluoromethyl, with organic sulphonic acid or its solvate, or hydrate, their solvates and hydrates and their use as antiviral agents.EFFECT: novel compounds.14 cl, 1 dwg, 4 tbl, 1 ex
Novel compound having parp inhibitory activity // 2606635
FIELD: chemistry.SUBSTANCE: invention relates to novel compounds of general formula 1 or pharmaceutically acceptable salts thereof, which posses PARP (poly(ADP-ribose)polymerase) inhibitor properties. Compounds can be used for prevention or therapy of posterior eye diseases. In formula (1) R1 is a halogen atom; R2 and R3 represent a hydrogen atom; R4 and R5 represent a hydrogen atom or a deuterium atom, or R4 and R5 can form an oxo group; Ra is a hydrogen atom or lower alkyl group, and Rb is a phenyl group or lower alkyl group, substituted with di-(lower alkyl) amino group, or 5-6-member heterocyclic group containing 1-2 heteroatoms in ring, selected from nitrogen atoms or nitrogen atom and an oxygen atom or a phenyl group, or 6-member nitrogen-containing heteroaryl group; Ra and Rb can be bonded with each other to form a 5-7-member nitrogen-containing heterocyclic ring, which can contain an additional nitrogen atom, optionally condensed with a benzene ring and optionally substituted with a group, selected from lower alkyl group, lower haloalkyl group, lower cycloalkyl group, lower cycloalkylcarbonyl group, lower alkoxycarbonyl group, low-cycloalkyl-lower alkyl group, di-(lower alkyl) amino group, di-(lower alkyl) amino-lower alkoxy group; phenyl group or phenyl-lower alkyl group, in each of which phenyl group can be substituted with 1–2 halogen atoms, hydroxy group, lower alkyl group, lower haloalkyl group, lower alkoxy group, C1-C2alkylenedioxy group; 5-6-member heterocyclic group, containing 1–2 heteroatoms in ring, selected from nitrogen atom, oxygen atom and sulphur atom, and/or nitrogen atom and oxygen atom, optionally substituted with a halogen atom and optionally condensed with a benzene ring or pyridine ring; ring A is a benzene ring or thiophenyl ring; and m is 0 or 1.EFFECT: obtaining novel compounds.12 cl, 61 tbl, 7 ex
ethod for capturing and recycling iron catalyst used in production of haloalkane compounds // 2606633
FIELD: chemistry.SUBSTANCE: invention relates to a method for capturing and recycling iron catalyst used in production of haloalkane compounds from carbon tetrachloride and alkene using iron catalyst and one or more trialkyl phosphate compounds as a cocatalyst, using an electromagnetic separation unit (EMSU). Upon activation, electromagnetic separation unit acts to remove iron particles from a stream exiting reactor; When electromagnetic separation unit is deactivated, captured iron particles can be separated back into reactor for repeated use in continuous production of haloalkane compounds. Present invention can be used in methods of producing haloalkane compounds, selected from a group consisting of 1,1,1,3,3-pentachloropropane (HCC-240fa), 1, 1,1,3-tetrachloropropane (HCC-250) and 1,1,1,3,3-pentachlorobutane (HCC-360).EFFECT: technical result is iron catalyst can be captured and sent back into reactor.10 cl, 1 dwg
 
2551106.
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