Pesticide compositions and related methods
SUBSTANCE: invention relates to a compound of formula one, two or three: Formula 1 Formula 2 Formula 3, where Ar1 is a substituted phenyl, containing one substitute independently selected from C1-C6 halogenalkyl with C1-C6 halogenalkoxy; Het denotes a 5-member unsaturated heterocyclic ring containing two or three heteroatoms selected from nitrogen; Ar2 is phenyl. Invention also relates to a method of pest control.
EFFECT: obtaining novel compounds which can be used in agriculture against pests.
8 cl, 5 tbl, 22 ex
SUBSTANCE: disclosed is a method of producing polyfluoroaryl(trimethyl)silanes of formula (I): ArFSi(CH3)3, where R = F, H, Si(CH3)3, CH3, by reacting fluorinated aromatic acids with trimethylchlorosilane to obtain corresponding silyl esters and then heating said esters with alkali metal halides in polar aprotic solvents to obtain fluoroaryl(trimethyl)silanes and extraction thereof using known methods.
EFFECT: method is easy to carry out and enables to obtain various said compounds with high output from affordable industrially manufactured raw materials.
3 cl, 1 tbl, 18 ex
SUBSTANCE: invention relates to novel substituted 3-(4-methylcarbamoyl-3-fluorophenylamino)tetrahydrofuran-3-ene carboxylic acid or esters thereof of general formula 1 and stereoisomers. The compounds of formula 1 are intermediate products in synthesis of androgen receptor inhibitors of formula A1, A2, A3, which are of interest as anticancer drugs. The invention also relates to methods of producing compounds of formula 1 and compounds of formulae A1, A2, A3. In general formula 1 R1=H, C1-C4alkyl; R2=H, CH2OCH2CH2Si(CH3)3. The method of producing compounds of formula (1) involves reacting compounds of general formula 2 with compounds 3(1) or 3(2) in dimethylformamide, K2CO3 while simultaneously adding copper iodide, water and triethylamine to the reaction mass. 2: By reacting compounds of formula 1, obtained using said method, with 4-isothiocyanato-2-trifluoromethylbenzonitrile in a mixture of dimethyl sulphoxide and ethyl acetate in ratio of 1:2 and at high temperature, compounds A1, A2, A3, whose structure is given in the claim, are obtained, respectively.
EFFECT: use of novel intermediate products improves output and stereoselectivity of the method of producing compounds A1, A2, A3.
4 cl, 6 ex
SUBSTANCE: invention refers to a method for obtaining a compound of formula 682, which is in a crystalline form, where the above method involves the following: (i) treatment of the compound of formula 682-9 with palmitic anhydride mixed with H2O/dioxane so that the compound of formula 682 is formed; (ii) treatment of the product obtained at stage (i) with methanol so that the compound of formula 682 is obtained in the form of solvate with methanol (Form K); (iii) extraction of the compound of formula 682, which has been obtained at stage (ii) in the form of solvate with methanol (Form K); (iv) optional cleaning of the product of stage (iii) by recrystallisation. Besides, the invention proposes a method for obtaining the compound of formula 682-4, where the above method involves the following: (i) conversion of the compound of formula 682-1 to the compound of formula 682-2' by treatment of the above compound of formula 682-1 with 1,3-dichloro-1,1,4,4-tetraisopropyldisiloxane (CIPS) in pyridine; (ii) conversion of the above compound of formula 682-2' to the compound of formula 682-3 by treatment of the above compound of formula 682-2' with acetic anhydride to EtOH; and (iii) conversion of the above compound of formula 682-3 to the compound of formula 682-4 by treatment of the above compound of formula 682-3 with an oxidiser, preferably with free radical 2,2,6,6-tetramethylpiperidinyloxy (TEMPO) and NaOCl. Further aspects of the invention refer to use of the above methods for obtaining 2'-cyano-2'-deoxy-N4-palmitoyl-1-β-D-arabinofuranosylcytosine, pyrimidine nucleoside, and are suitable for treatment and/or prevention of cancer.
EFFECT: improvement of compounds.
22 cl, 1 tbl, 1 ex
SUBSTANCE: invention relates to a method of producing fluorine-containing aromatic silanes. Disclosed is a method of producing polyfluoroaryl(trimethyl)silanes of formula ArF-Si (CH3)3 (I), where by reacting polyfluoroaromatic acids with potassium hydroxide solution to form corresponding potassium or dipotassium salts, followed by reacting the separated salts with trimethylchlorosilane in polar aprotic solvents such as DMF, DMAA, N-methylpyrrolidone, sulpholane, at temperature of 70-130°C. The obtained polyfluoroaryl(trimethyl)silanes are separated using existing methods. Output of desired products is 73-86% with respect to the acid.
EFFECT: disclosed method is simple from the technical perspective and enables to obtain various polyfluoroaryl(trimethyl)silanes with high output from readily available off-the-shelf reactants.
3 cl, 1 tbl, 14 ex
SUBSTANCE: invention relates to substituted 4-aminocyclohexane derivatives of general formula I: where: R1 and R2 independently denote C1-3-alkyl, H or R1 and R2 together with an N tom form a (CH2)3, (CH2)4 ring; R3 optionally denotes a phenyl or thienyl linked through a C1-3-alkyl chain, each unsubstituted; or an unsubstituted C1-6-alkyl; R4 denotes indole, pyrrolo[2,3-b]pyridine, pyrrolo[2,3-c]pyridine, pyrrolo[3,2-c]pyridine, pyrrolo[3,2-b]pyridine, optionally mono- or multi-substituted with a substitute selected from a group comprising F, CI, Br, CN, CH3, C2H5,' NH2, tert-butyl, Si(ethyl)3, Si(methyl)2(tert-butyl), SO2CH3, SO2-phenyl, C(O)CH3, NO2, SH, CF3, OCF3, OH, OCH3, OC2H5, N(CH3)2; in form of a racemate; enantiomers, diastereomers, mixtures of enantiomers or diastereomers or separately an enantiomer or diastereomers; bases and/or salts of physiologically compatible acids or cations; as well as a drug based on compounds I for treating neuropathic pain.
EFFECT: improved properties.
14 cl, 73 ex
SUBSTANCE: asymmetric organomodified disiloxane surfactant having the formula: MM' wherein M contains branched hydrocarbon substitutes and M' contains a cationic, anionic or zwitterionic substitute and a polyether substitute which may be combined as one fragment. Aqueous and non-aqueous emulsions contain said surfactant.
EFFECT: invention increases hydrolysis resistance of the surfactant in the pH range from 3 to 12.
25 cl, 4 tbl, 4 ex
SUBSTANCE: invention relates to a method of producing glycidyloxyalkyl alkoxysilanes by hydrosilylation of olefin-glycide ether in the presence of a catalyst. Disclosed is a method of producing glycidyloxyalkyl alkoxysilanes of general formula (R")O-CnH2nSi(OR)3, wherein groups R independently denote a linear or branched alkyl with 1-4 carbon atoms, n is a number equal to 1, 2, 3, 4, 5, 6, 7 or 8, R'' denotes a group H2C(O)CH- or H2C(O)CHCH2-, by reacting (i) a functionalised alkene of general formula (R")OCnH2n-1 wherein R" denotes a group H2C(O)CH- or H2C(O)CHCH2-, and n is a number equal to 1, 2, 3, 4, 5, 6, 7 or 8, (ii) with at least one hydrogen alkoxysilane of general formula HSi(OR)3, wherein groups R independently denote a linear or branched alkyl with 1-4 carbon atoms, in the presence of (iii) at least one homogeneous catalyst selected from a group comprising Spayer catalysts and Karstedt catalysts, (iv) at least one solvent and/or at least one diluent and (v)at least one acid promoter from a group of mono- and dicarboxylic acids, wherein: components (i) alkene and (ii) hydrogen alkoxysilane, used in molar ratio of 1.8-1.0:1.0; catalyst (iii) is used in molar ratio to alkene (i) ranging from 1:1000000 to 1:25000; catalyst (iii) and promoter (v) are used in molar ratio from 1:250 to 1:25000 and the catalyst (iii) and promoter (v) are used together in a solvent and/or diluent in diluted form.
EFFECT: disclosed method enables to achieve high output of the end product compared with existing methods.
12 cl, 1 ex
SUBSTANCE: invention refers to polymers on the base of poly(ferrocenyl)sylane used in photon semiconductor matrixes. The invention proposes celled polymer on the base of poly(ferrocenyl)sylane including repeating blocks with three types of structures, way of its manufacturing based on spatial crossing of basic polymer and binding agent and the film including the substrate and connected to it celled polymer on the base of poly(ferrocenyl)sylane.
EFFECT: proposed celled polymers have 3D structures and are produced using technological method that does not require special multistage cleaning of precursors.
12 cl, 1 dwg, 1 ex
SUBSTANCE: invention discloses a method of producing 1-alkyl-2-(trimethylsilyl)cyclopropane by reacting 1-alkyl-2-(trimethylsilyl)acetylenes with triisobutylaluminium in the presence of diidomethane in an argon atmosphere at temperature 20-22°C and atmospheric pressure in dichloromethane for 3-5 hours, followed by hydrolysis of the reaction mass.
EFFECT: disclosed method enables to obtain compounds in mild conditions with high output using industrially available reagents.
1 cl, 1 tbl, 1 ex
SUBSTANCE: in order to simplify the process of producing alkyl silanes and their further purification, synthesis of alkylchloro silanes is carried out in the medium of aromatic hydrocarbons in the presence of a catalyst - tetrakis(diethylamido)-phosphonium salts, more preferably bromides and chlorides, at temperature ranging from 20°C to 250°C. The activator is used in amount of 0.005-1 mol, more preferably 0.01-0.05 mol for each substituted halogen atom in the initial alkylchloro silane.
EFFECT: disclosed method enables to obtain the end product with high purity and high output.
3 cl, 1 tbl, 8 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to 2-(3-amino-1-(2,4-difluorophenyl)-1H-1,2,4-triazol-5-yl)-N-methyl-4,5-dihydrobenzo[b]thieno[2,3-d]oxepin-8-carboxamide. As well as to a pharmaceutical composition containing the above compound, to the use thereof and a set for treating.
EFFECT: 2-(3-amino-1-(2,4-difluorophenyl)-1H-1,2,4-triazol-5-yl)-N-methyl-4,5-dihydrobenzo[b]thieno[2,3-d]oxepin-8-carboxamide inhibiting PI3 kinase (PI3K).
6 cl, 15 dwg, 1 tbl, 610 ex
SUBSTANCE: method includes reacting 2,4-difluoro-5-nitro-1-chlorobenzene (2) with a compound of formula (3) to obtain a compound of formula (4) , reducing the compound of formula (4) with sodium dithionite in a suitable solvent to obtain a compound of formula (5) , ring closure of the compound of formula (5) to form a compound of formula (6) , crystallising a compound of formula (7) from the compound of formula (6), reacting said compound of formula (7) with an amino derivative of a compound of formula (9)
EFFECT: high degree of purity.
10 cl, 4 dwg, 4 ex
SUBSTANCE: invention relates to novel choline salt of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid, corresponding to formula and to its crystalline form. Crystalline form of salt (A) has characteristic peaks at diffraction angles (2θ(E)) 7.1, 11.5, 19.4, 20.3, 21.5, 22.0, 22.6, 23.5 and 26.2 in diagram of powder diffraction of X-rays, characteristic peaks of values of chemical shifts (δ(ppm)) 155.8, 149.8, 145.3, 118.0, 113.7, 111.6, 110.3, 98.1, 69.8, 58.7, 57.1 and 55.5 in solid-state 13C NMR spectrum and characteristic peaks of values of chemical shifts (δ(ppm)) -131.6, -145, and -151.8 in solid-state 19F NMR spectrum, as well as endothermic peak about 213°C in diagram of differential-thermal analysis.
EFFECT: compound has excellent solubility and stability in storage.
5 cl, 5 dwg, 3 tbl, 8 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to compound of structural formula
which can be applied for treatment, prevention or carrying out treatment of neurological disorder. In formula (Iva) m is equal 0; n is equal 1; R1 and R2 are, each independently, hydrogen, C1-C4alkyl or C3-C6cycloalkyl; R3 and R4 are, each independently, hydrogen or C1-C4alkyl; R5 is hydrogen and R6 and R7 are, each independently hydrogen, halogen, C1-C4alkyl, C6-C10aryl, 5-10-membered heteroaryl, which contains one O atom, one S atom and/or 1-4 N atom(s), 3-8-membered heterocyclyl, containing 1-2 heteroatoms, selected from O, S and N, C1-C4alcoxyl or aminoC1-C4alkyl.
EFFECT: invention relates to pharmaceutical industry, which contains claimed compound, and to method of treatment, prevention or carrying out of treatment of neurological disorder such as psychosis or schizophrenia.
54 cl, 2 tbl
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to 5,5-condensed heteroarylene compounds IIIB, where U2, V1, V2 and W1 are selected from O, N, NH, S or CR3a; U1, W2, X1 and X2 represent C or N; R1 and R2 represents hydrogen, -C(O)CH(NR1bR1c)R1a, -C(O)CH(N(R1c)C(O)OR1b)R1a or -C(O)OR1a; R3a represents hydrogen or R3; R3 represents halogen or -C(O)OR1a; L1 and L2 are such as given in invention formula, each Z1 and Z2 represents bond or -O-; each Rla, R1b and R1c represents hydrogen, C1-6 alkyl or C6-14 aryl; or Rlb and Rlc together with N atom, which they are bound to, form 5-6-membered heterocyclyl; q, r, s, t and u equal 1. Invention also relates to pharmaceutical compositions, containing 5,5-condensed heteroarylene compounds, and methods of treating or preventing HCV infection.
EFFECT: 5,5-condensed heteroarylene derivatives, possessing inhibiting activity with respect to hepatitis C virus.
43 cl, 42 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to a compound of formula , wherein Y and Z are independently specified in a group of a) or b) so that one of Y or Z is specified in the group a), and another one - in the group b); the group a) represents i) substituted C6-10aryl; ii) C3-8cycloalkyl; iii) trifluoromethyl or iv) heteroaryl specified in a group consisting of thienyl, furanyl, thiazolyl, isothiazolyl, oxazolyl, pyrrolyl, pyridinyl, isoxazolyl, imidazolyl, furasan-3-yl, benzothienyl, thieno[3,2-b]thiophen-2-yl, pyrazolyl, triazolyl, tetrazolyl and [1,2,3]thiadiazolyl; the group b) represents i) C6-10aryl; ii) heteroaryl specified in a group consisting of thiazolyl, pyridinyl, indolyl, pyrrolyl, benzoxazolyl, benzothiazolyl, benzothienyl, benzofuranyl, imidazo[1,2-a]pyridin-2-yl, furo[2,3-b]pyridinyl, pyrrolo[2,3-b]pyridinyl, pyrrolo[3,2-b]pyridinyl, thieno[2,3-b]pyridinyl, quinolinyl, quinazolinyl, thienyl and benzimidazolyl; iii) benzofused heterocyclyl attached through a carbon atom, and when a heterocyclyl component contains a nitrogen atom, the carbon atom is optionally substituted by one substitute specified in a group consisting of C3-7cycloalkylcarbonyl; C3-7cycloalkylsulphonyl; phenyl; phenylcarbonyl; pyrrolylcarbonyl; phenylsulphonyl; phenyl(C1-4)alkyl; C1-6alkylcarbonyl; C1-6alkylsulphonyl; pyrimidinyl and pyridinyl; C3-7cycloalkylcarbonyl, phenyl, phenylcarbonyl, phenyl(C1-4)alkyl and phenylsulphonyl are optionally substituted by trifluoromethyl, or by one or two fluor-substitutes; iv) phenoxatiynyl; vi) fluoren-9-on-2-yl; vii) 9,9-dimethyl-9H-fluorenyl; viii) 1-chlornaphtho[2,1-b]thiophen-2-yl; ix) xanthen-9-on-3-yl; x) 9-methyl-9H-carbazol-3-yl; xi) 6,7,8,9-tetrahydro-5H-carbazol-3-yl; xiii) 3-methyl-2-phenyl-4-oxochromen-8-yl; or xiv) 1,3-dihydrobenzimidazol-2-on-5-yl optionally substituted by 1-phenyl, 1-(2,2,2-trifluoroethyl), 1-(3,3,3-trifluoropropyl) or 1-(4,4-difluorocyclohexyl); 1-phenyl is optionally substituted by one or more fluor-substitutes or trifluoromethyl; or xv) 4-(3-chlorophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl; R1 represents C6-10aryl, C1-3alkyl, benzyloxymethyl, hydroxy(C1-3)alkyl, aminocarbonyl, carboxy, trifluoromethyl, spirofused cyclopropyl, 3-oxo or aryl(C1-3)alkyl; or when s is equal to 2 and R1 represents C1-3alkyl, the substitutes C1-3akyl is taken with a piperazine ring to form 3,8-diazabicyclo[3.2.1]octanyl or 2,5-diazabicyclo[2.2.2]octanyl ring system, and its pharmaceutical compositions.
EFFECT: preparing the new pharmaceutical compositions.
20 cl, 7 tbl, 72 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to new compounds of formula IV, VIII-A and X, and to their pharmaceutical acceptable salts possessing the inhibitory activity on PI3-kinase (phosphoinositide-3-kinase). In compounds of formula IV and IX and Wd is specified in a group consisting of, , , and each of which can be substituted. In formula VIII-A, the group Wd represents the group or , wherein Ra is hydrogen, R11 is amino; in compound IV, Wa 2 represents CR5; Wa 3 represents CR6; Wa 4 represents N or CR7; in compound IX, Wa 1 and Wa 2 independently represent CR5, N or NR4, and Wa 4 independently represents CR7 or S, wherein no more than two neighbouring atoms in a ring represent atom or sulphur; Wb 5 represents N; B represents a grouping of formula II, as well as in case of compound IV, B means C1-C10alkyl, C3-C10cycloalkyl, C3-C10heterocycloalkyl having one to six ring heteroatoms specified in N, O and S; in case of compound IX, B also means C1-C10alkyl, C3-C10cycloalkyl or 6-merous heterocycloalkyl having nitrogen atom; Wc represents C6-C10aryl or 5-18-merous heteroaryl having one or more ring heteroatoms specified in N, O and S, or phenyl or 6-merous heteroaryl respectively is equal to an integer of 0, 1, 2, 3 or 4; X is absent or represents -(CH(R9))z-, respectively; z is equal to 1; Y is absent. The other radical values are specified in the patent claim.
EFFECT: compounds can be used for treating such diseases, as cancer, bone disorders, an inflammatory or immune disease, diseases of the nervous system, metabolic disorders, respiratory diseases, thrombosis or cardiac diseases mediated by PI3-kinase.
68 cl, 11 dwg, 7 tbl, 55 ex
SUBSTANCE: invention relates to a compound of formula wherein each of R1 and R2 is independently selected from a group consisting of a hydrogen atom, nitro and NR6R7; R3 is C1-C8alkyl; each of R4 and R5 is independently selected from a group consisting of C1-C8alkoxy, phenoxy and phenyl(C1-C8alkylene)oxy; each of R6 and R7 is independently selected from a group consisting of a hydrogen atom, C1-C8alkyl, C(O)R8 and SO2R8;R8 is selected from a group consisting of a hydrogen atom, C1-C8alkyl, halogen-substituted C1-C8-alkyl, C1-C8-alkyl, substituted (C1-C8-alkylsubstituted amino), C1-C8-alkyl, substituted with piperidine and C1-C8-alkyl, substituted with morpholine.
EFFECT: reduced PDE4 enzyme activity and treating PDE4 enzyme mediated diseases or conditions.
21 cl, 2 tbl, 32 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to organic chemistry, namely to a compound of formula and to its pharmaceutically acceptable salt and its enantiomers, wherein D means pyridyl, which is substituted by 1-2 independently specified groups R38; M means , wherein * means an attachment position to D; and † means an attachment position to Z; Z means -O-; Ar means phenyl, which is optionally substituted by 0-4 groups R2; and G means ; wherein each R38 means -C0-C6-alkyl-(substituted by one group containing heterocyclyl, which means a monocyclic structure, and contains 5 to 7 atoms, wherein 1 or 2 atoms are independently specified in a group containing N, O and S optionally substituted by one or more oxo groups); in each specific case R2 is independently specified in -H and halogen; each R13 means -H; Q means cyclopropyl. The invention also refers to a pharmaceutical composition based on the composition of formula (I), a method for inhibiting the activity of protein kinase of the growth factor receptors and a method of treating choroidal neovascularisation.
EFFECT: there are prepared new compounds possessing the activity on protein kinase inhibitors.
7 cl, 8 tbl, 27 ex
SUBSTANCE: invention relates to an improved method of obtaining compounds of formula . The compounds of formula 6 are intermediate products for obtaining dihydrothieno[3,2-d]pyrimidines, which produce an impact on the cardiovascular system, possess sedative action, or can be applied in treatment of inflammatory diseases of joints, skin, eyes or diseases of the peripheral or central nervous system, respiratory or gastrointestinal disorders. The method includes the following stages: a) interaction of reagents of formulas HS-CH2-CO2Ra and CHR5=CR4-CO2Ra with obtaining an intermediate product of formula ; and b) cyclisation of the intermediate product of formula 7 in a solvent in the presence of TiCl2(O-iPr)2, TiCl(O-iPr)3, TiCl3(O-iPr) and in the presence of a base-amine, with obtaining a product of formula 6. Ra stands for alkyl, R4 and R5 are independently selected from a group, including H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkinyl, C6-C10-aryl, C6-C10-aryl-C1-C6-alkylene, C5-C10-heteroaryl-C1-C6-alkylene, C3-C10-heterocycle and C5-C10-heteroaryl, -O-C1-C6-alkyl, -O-C6-C10-aryl, -O-C3-C10-heterocycle and -O-C5-C10-heteroaryl, -NR'R", fluorine, C1-C6-fluoroalkyl and C1-C6-fluoroalkoxygroup, where R' and R" are independently selected from a group, including H and C1-C6-alkyl, and where in each case the group can be optionally substituted with one or more groups, selected from a group, including OH, oxogroup, halogen, C1-C6-alkyl and O-C1-C6-alkyl. The method makes it possible to obtain the intermediate products 6, which do not require carrying out distillation and chromatographic purification between stages in realisation of processes suitable for wide-scale synthesis of dihydrothieno[3,2-d]pyrimidines.
EFFECT: invention results in higher total output of the final products as compared to that in realisation of methods of preceding level of technology.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to compound, represented by the following formula
or its pharmaceutically acceptable salt. In claimed formula each symbol has values, determined in formula of invention. Versions of formula [I] compound and particular compounds are also objects of invention. In addition, invention relates to pharmaceutical composition, ITK inhibitor and means for treatment or prevention of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection and other diseases and methods of treating said diseases.
EFFECT: claimed compounds inhibit induced T-cellular kinase (ITK).
32 cl, 86 tbl, 387 ex