Tricyclic benzoxaboral compound, method for its production and its application

FIELD: pharmacology.

SUBSTANCE: invention relates to a new tricyclic benzoxaboral compound represented by chemical formula 1, its isomer or a pharmaceutically acceptable salt thereof. Chemical formula 1

Also, methods of preparation of the said compound and a pharmaceutical composition are provided.

EFFECT: new tricyclic benzoxaboral compound has antibiotic activity against gram-negative bacteria, including against gram-negative bacteria with multiple drug resistance.

14 cl, 3 tbl, 12 ex

 



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing compounds of formula where R1a and R1b are selected from H and F and one of R1a and R1b is F, Het is tetrazolyl, optionally substituted with methyl, R2 is selected from benzyl and C1-C6 alkyl, optionally substituted with a halogen or C1-C4 alkyloxy. The present method includes combining compounds and where X is selected from Cl, Br, I and trifluoromethanesulphonate, Y is selected from BF3 and BR3R4, R3 and R4 are selected from OH, C1-C6monoalcohols and C1-C6diatomic alcohols, or where R3 and R4 together with B, to which they are attached, form a cyclic boronate optionally substituted with methyl.

EFFECT: obtaining oxazolidinones.

22 cl, 10 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing carbonyl derivatives of 5,10,15,20-tetraphenylporphyrin of formula I where R is o-carborane or m-carborane, which are obtained by reacting mercaptocarborane with 5,10,15,20-tetra(n-trifluoromethanesulphonylmethyloxyphenyl)porphyrin in palladium catalysis conditions while boiling in anhydrous toluene while stirring in an atmosphere of an inert gas at room temperature. The method includes successively adding diisopropylethylamine (DIPEA), the corresponding mercaptocarborane, 1,1'-bis(diphenyl-phosphino)ferrocene (dppf) and tris(dibenzylideneacetone)dipalladium (Pd2(dba)3), followed by boiling the reaction mixture in an Ar atmosphere for a few hours, separating the finished products using know techniques; 5,10,15,20-tetra(n-trifluoromethanesulphonylmethyloxyphenyl)porphyrin is obtained by reacting 5,10,15,20-tetrahydroxyporphyrin with a trifluoromethanesulphonic acid anhydride in a medium of methylene chloride in an atmosphere of an inert gas.

EFFECT: obtaining novel carbonyl derivatives of 5,10,15,20-tetraphenylporphyrin, which can be used as anti-tumour agents in boron neutron capture therapy and photodynamic therapy of cancerous diseases.

1 dwg, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compound of formula: or its pharmaceutically acceptable salts. Values of radicals are as follows: Ra represents member, selected from CN, C(O)NR1R2, C(O)OR3; R1 and R2 represent H, R3 represents H or unsaturated C1-C10 alkyl; X represents member, selected from N, CH and CRb, Rb represents member, selected from halogen, substituted or non-substituted C1-C10 alkyl, C(O)OR4, OR4, NR4R5, where R4 and R5represent members, independently selected from H, substituted or non-substituted C1-C10 alkyl, substituted or non-substituted C1-C10 heteroalkyl, containing at least 1 heteroatom, where heteroatom represents O or N, and heteroatom can take any internal position in heteroalkyl group or take the position, through which alkyl group is bound to the remaining part of molecule, non-substituted C3-C10 cycloalkyl, pyridyl, substituted with CN group, or independently represents ; and , where alkyl and heteroalkyl substituents are independently selected from the group, including: -R', =O, -CO2R', -OR', -OC(O)R', -NR"C(O)R', -NR'R", -CONR'R", pyridyl, halogen, , 4-methylpiperazinyl, 4-methylpiperidinyl, in quantity from 0 to 3; and where R' and R" are independently selected from the group, including hydrogen, non-substituted phenyl, non-substituted C1-C10 alkyl, C1-C10 alkoxy, on condition that R4 and R5, together with atoms to which they are bound, are optionally combined with formation of 4-8-membered non-substituted heterocycloalkyl ring, containing 1-2 heteroatoms, selected from N and O. Also claimed are pharmaceutical compositions, method of treating state, mediated by phosphodiesterase (FDE), a method of FDE inhibition.

EFFECT: invention makes it possible to obtain compounds, capable of inhibiting phosphodiesterase.

134 cl, 141 dwg, 2 tbl, 29 ex

FIELD: chemistry.

SUBSTANCE: claimed is a method of obtaining oligoborosilazanes by the interaction of oligosilazanes, which do not contain alkyl radicals at a nitrogen atom, with an aminoborane complex, which does not contain alkyl radicals at a nitrogen atom, with the ratio of silazane to a boron-containing modifier from 3 to 18, with carrying out the process at a temperature of 40-140°C in a mixture of toluene with diglyme or benzene with diethyl ether with the molar ratio from 1:1 to 1:33.

EFFECT: method makes it possible to obtain oligoborosilazanes with the given molecular weight with high output, which is reached due to the step-by-step thermal processing of the reaction mixture at an increased temperature.

2 cl, 4 tbl, 13 ex

FIELD: chemistry.

SUBSTANCE: invention relates to porous crystalline materials. A porous crystalline material having a tetrahedral framework comprising the general structure M1-IM-M2, wherein M1 comprises a metal having the first valency, M2 comprises a metal having the second valency different from the first valency, and IM is imidazolate or a substituted imidazolate linking moiety. One or more of the following conditions is met: M1 comprises a monovalent metal, and M2 comprises a trivalent metal; M1 is Li+; and M2 is B3+. Also claimed is a gas adsorption method, a method of separating gas from a fluid stream containing the gas.

EFFECT: adsorbents with an improved gas uptake on a gravimetric basis.

28 cl, 3 dwg, 8 tbl, 3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to method of obtaining hydrochloride of tertbutyl ester of (4-fluoro-3-pyperidin-4-yl-benzyl)-carbamic acid (I). Method includes reduction of tertbutyl ester of (4-fluoro-3-pyridin-4-yl-benzyl) carbamic acid under conditions of reducing hedrogenisation and then HCl processing with output of hydrochloride of tertbutyl esther of (4-fluoro-3-pyperidin-4-yl-benzyl)-carbamic acid. Also claimed are methods of obtaining intermediate products, namely 5-((tert-butoxycarbonyl)aminomethyl)-2-fluorobenzeneboronic acid and tertbutyl ester of (4-fluoro-3-pyridin-4-yl)benzyl-carbamic acid.

EFFECT: invention makes it possible to considerably simplify obtaining hydrochloride of tertbutyl esther of (4-fluoro-3-pyperidin-4-yl-benzyl)-carbamic acid.

30 cl, 1 ex

FIELD: biotechnologies.

SUBSTANCE: invention relates to a method of obtaining of unsubstituted alkyl ammonium and alkyl guanidine 7,8(7,9)-dodeca hydro dicarbo nido undecaborates. The method comprises interaction of unsubstituted o(m)-carboranes with alkylamines and alkyl guanidines in the medium of the lower aliphatic alcohols. Meanwhile the process is performed at combined effect of catalyser and ultrasonic activisation at the temperature 60-80°C in the medium of the lowest aliphatic alcohols or respective water and alcohol mixes. The catalysers are fluorides of alkali metals, ammonium fluorides of or ammonium tetraalkyl fluorides.

EFFECT: invention allows to simplify the named compounds and to increase their yield.

6 cl, 12 ex

FIELD: chemistry.

SUBSTANCE: invention relates to method of obtaining monohalogenderivatives of 1,2-, 1,7-, 1,12-dicarba-closo-dodecarboranes(12). Method includes interaction of o(m,p)-carboranes with halogenating agents. As the latter used are N-halogenimides (amides): N-halogen-succinimides, 1,3-dihalogen-5,5-dimethylhydantoins, trihalogen-isocyanuric acids, N-halogen-arylsulfonamides and their sodium salts, N-halogenphthalimides, where halogen = Cl, Br, I; aryl = phenyl, p-tolyl, in the medium of acidic organic solvent. As solvent applied are monobasic liquid organic acids of aliphatic series R-COOH, where R=H, CnH2n+1, CnF2n+1, n=1-3. The process is carried out with application of ultrasound activation at temperature 60-80°C for 3-5 hours.

EFFECT: invention makes it possible to reduce energy consumption.

15 ex

FIELD: chemistry.

SUBSTANCE: invention relates to method of obtaining of monohalogen-derivatives of 1,2-,1,7-,1,12-dicarba-closo-dodecaboranes(12). Method includes interaction of o(m,p)carboranes with halogenating agents; as halogenating agents used are N-halogenimides (amides): N-halogen-succinimides, 1,3-dihalogen-5,5-dimethylhydantoins, trihalo-isocyanuric acids, N-halogenaryl-sulfonamides and their sodium salts, N-halogenphthalimides, where halogen= Cl, Br, I; aryl = phenyl, p-tolyl, in medium of acidic organic solvent. As solvent applied are liquid organic monobasic acids of aliphatic series R-COOH, where R=H, CnH2n+1, CnF2n+1, n=1-3. the process is carried out with application of ultrasound activation in presence of catalyst, as catalyst used are strong acids: sulfuric (H2SO4), methanesulfonic (CH3SO2OH) and trifluoromethanesulfonic (CF3SO2OH) in amount 0.1-1.0 mol %. The process is carried out at temperature 20-50°C for 2-4 hours.

EFFECT: invention makes it possible to reduce energy consumption.

15 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of obtaining pyridinates of 1-fluoro(chloro)-3-alkyl(aryl)borolanes of general formula (1), where R=Bu, X=F (a); R=Hex, X=F (b); R=Hex, X=Cl (c); R=Bn, X=Cl (d). The method includes the interaction of unsaturated compounds, selected from the group of hex-1-ene, oct-1-ene or allylbenzene, with triethylaluminium (AlEt3) in the presence of a catalyst (Cp2ZrCl2) in a ratio of 10:12:0.5 in hexane in an atmosphere of inert gas with mixing for 7 h, addition of boron trifluoride etherate (BF3·Et2O) or boron chloride (BCl3) and pyridine in a double with respect to AlEt3 amount, following mixing at room temperature for 30-60 min.

EFFECT: obtained compounds can be applied as components of catalytic systems in processes of oligo- and polymerisation of olefin, diene and acetylene hydrocarbons, as well as in fine organic and organometallic synthesis.

1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention deals with application of composition, which includes hydrolysate of pea protein and/or peptide for obtaining composition for treatment and/or prevention of infection Helicobacter pylori (versions), as well as such compositions (versions). Characterised compositions include lipid, protein and carbohydrate component, in which protein component includes protein source, which consists of pea protein hydrolysate, obtained by hydrolysis with protease, different from chymotrypsin, or from peptides, selected from group, which consists of Xaan-Asp-Phe-Leu-Glu-Asp-Ala-Phe-Asn-Val-Asn-Arg-Xaam and Xaan-Glu-Leu-Ala-Phe-Pro-Gly-Ser-Ala-Gln-Glu-Val-Asp-Arg-Xaam, where each Xaa independently can be any amino acid, and n and m are integer numbers, independently varying from 0-10, where peptide is contained in pea protein hydrolysate, or from both.

EFFECT: claimed inventions make it possible to treat or prevent diseases, caused by Helicobacter pylori infection, and/or diseases, associated with infection Helicobacter pylori in mammals.

17 cl, 2 tbl, 1 ex

FIELD: veterinary medicine.

SUBSTANCE: method comprises subcutaneous administration of antibiotic preparation enroxyl 5% at a dose of 0.1 ml/kg daily one time a day for 7 days and intramuscular administration of homeopathic preparation ovarinin at a dose of 1 ml/kg one time for 4 days, 4-fold.

EFFECT: use of the invention enables to increase the efficiency of treatment, to reduce treatment time and to restore reproductive function of dogs.

2 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medicine and describes pharmaceutical composition, including therapeutically effective quantity of compound, which has the following structure: , where compound in pharmaceutical composition is present in quantity, efficient for treatment or prevention of antibacterial infection in mammalian subject. Methods of obtaining and application of said dosed forms or pharmaceutical compositions are also claimed.

EFFECT: obtaining composition for treatment or prevention of antibacterial infection in mammalian subject.

15 cl, 8 tbl, 5 ex, 4 dwg

FIELD: medicine.

SUBSTANCE: group of inventions refers to veterinary science and is applicable for treating bovine mastitis. What is declared is a nosode for producing a preparation for treating bovine mastitis. That involves taking mastitis milk 1 ml with clinical signs of purulent-catarrhal mastitis, filling it 70° alcohol 9 ml to produce a homogenous solution; the produced solution is diluted to "Д6" with 70° alcohol. What is also declared is a preparation for treating bovine mastitis containing an aqueous-alcoholic solution of components. The components are Belladonna, Sulphur, Apis mellifica, Conium, Phytolacca, Silicea and above nosode in the following proportions, wt %: Belladonna - 5, Sulphur - 20, Apis mellifica - 20, Conium - 10, Phytolacca - 10, Silicea - 5, nosode - 15, aqueous-alcoholic solution up to 100%. What is also declared is a method of treating bovine mastitis involving the intracisternal administration of the preparation. The preparation is administered in a dose of 5-10 ml per 1 animal once a day.

EFFECT: declared group of inventions is highly effective in treating bovine mastitis.

3 cl, 5 tbl, 1 ex

Antimicrobial agent // 2556509

FIELD: medicine.

SUBSTANCE: compound 2-(1'-hydroxy-4'-isopropenyl-1'-methylcyclohexyl-2'-thio)-methylethanoate having structural formula I: is applicable as an antimicrobial agent.

EFFECT: using the compound of formula I possessing antimicrobial activity provides treating infectious processes caused by susceptible organisms.

5 tbl

FIELD: medicine.

SUBSTANCE: claimed group of inventions relates to field of veterinary. Claimed are: vaccine, aimed against actinobacillous pleuropneumonia, including lipopolysaccharide in complex with one or more repeats of ApxI, ApxII and ApxIII toxins, separated from bacterial culture and polymyxin to reduce symptoms of endotoxic shock, caused by lipopolysaccharide, method of obtaining such vaccine, application of polymyxin to reduce endotoxic shock symptoms when vaccine is introduced, in which polymixyn is added into vaccine in dose from 2.6 to 60 mcg/ml.

EFFECT: claimed group of inventions provides effective means and methods to reduce endotoxic shock symptoms, caused by lipopolysaccharide, when vaccine against actinobacillous pleuropneumonia is introduced to animal.

14 cl, 4 tbl, 4 ex

FIELD: veterinary medicine.

SUBSTANCE: complex antibacterial agent for animals, containing a compound from the group of fluoroquinolones and auxiliary substances, characterised in that it additionally comprises a compound from the group of pleuromutilins in an effective amount.

EFFECT: invention is effective against vegetative and spore forms of bacteria, it is harmless, has no allergenic properties, has a stimulating effect on the indices of humoral immune response, and is stable during storage.

6 cl, 9 ex

FIELD: veterinary medicine.

SUBSTANCE: agent comprises enrofloxacin and excipients. The agent additionally comprises humates of peat or sapropel, with the following ratio of the components, wt %: enrofloxacin substance - 0.5; alkaline solution of humates (pH=12-13) - 80; succinic acid - to pH 10-11; propylene glycol - the rest. The agent is administered with the liquid feed once a day for three to five days at a dose of from 0.5 to 1.0 ml per 1 kg of body weight.

EFFECT: manifestation of pronounced therapeutic effect.

5 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to method of obtaining 7-hydroxyroyleanon, possessing antimicrobial action. said method includes extraction of crushed roots of salvia officinalis with 96% ethyl alcohol with further extract evaporation, processing with water, alcohol distillation and processing with hydrophobic solvent or extraction of said raw material with chloroform with further extract processing with water and evaporation; after which target product is extracted from organic phase by transfer into water-soluble phenolates, with processing with sodium hydroxide water solution; alkali solution is washed with chloroform; acidified with hydrochloric or sulphuric acid; obtained sediment is filtered; dried and crushed.

EFFECT: invention is characterised by improved process manufacturability and provides obtaining individual substance with higher antimicrobial activity than previously extracted royleanon derivatives from salvia officinalis.

2 tbl, 6 ex

FIELD: biotechnology.

SUBSTANCE: invention relates to a strain of the pathogen of pseudomonosis of pigs of the collection of Federal state budgetary institution "VGNKI", deposited under the name "Pseudomonas aeruginosa No.9" and the registration number "No.9-DEP", intended for production of a vaccine against pseudomonosis of pigs.

EFFECT: invention provides high immunogenic activity and the ability of production of the vaccine against pseudomonosis of pigs.

4 ex, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and describes a pharmaceutical composition of dioctahedral smectite presented in the form of a dispersible tablet, as well as a method for producing it. The dispersible tablet is formed by pressing the granules containing dioctahedral smectite in an amount of 800 to 1,200 mg, as well as excipients and target additives in an amount of no more than 50% from a tablet weight. The produced tablet is water-dispersible for 3 minutes to form a dispersion consisting of particles of less than 710 mcm in size, as well as possesses high stability and physical integrity, good mechanical properties in a combination with fast dispersion ability in aqueous solutions.

EFFECT: specified tablet composition enables providing good stability of the technological process of the dispersible tablet.

2 cl, 2 tbl

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