Derivatives of 7-oxo-1,6-diazabicyclo[3.2.1]oct-3-ene, useful for bacterial infections treatment

FIELD: chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, namely a heterocyclic compound of formula (Ia), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, where R1 is -CONR'R'' or -CN; R2 and R3 are independently selected from H, C1-C6alkyl, C3-C6cycloalkyl; where alkyl in the definition of R2 or R3 independently and optionally substituted with -OH, C1-C3alkoxy, -NR'R'', -C(O)NR'R'' or -NR'C(O)R''; and each of R' and R'' is independently selected from hydrogen, C1-C6alkyl, 6-membered saturated heterocyclyl containing one heteroatom N; wherein each alkyl and heterocyclyl are optionally and independently substituted with -C(O)(C1-C6alkoxy) or -NH2; provided that R2 and R3 are not both hydrogen. Invention also relates to particular compounds, a pharmaceutical composition based on a compound of formula (Ia), its use and method of treating a bacterial infection based on the use of a compound of formula (Ia). .

EFFECT: technical result: new diazabicyclooctene derivatives, useful in the treatment of bacterial infection, were obtained.

15 cl, 31 ex

 



 

Same patents:

FIELD: medicine.

SUBSTANCE: invention relates to a method of treatment or relieving the severity of cystic fibrosis in a patient, where the patient has the cystic fibrosis transmembrane receptor (CFTR) with R117H mutation, including a stage of introduction to the said patient of an effective quantity of N-(5-hydroxy-2,4-ditert-butyl-phenyl)-N-methyl-4-oxo-1H-quinoline-3-carboxamide.

EFFECT: elaborated is the method of treating cystic fibrosis, based on the application of N-(5-hydroxy-2,4-ditert-butyl-phenyl)-N-methyl-4-oxo-1H-quinoline-3-carboxamide.

3 cl, 4 tbl, 30 ex

FIELD: chemistry.

SUBSTANCE: second amines are N-alkylated by cis-2,3-dichlormethyl-hem-dichlorcyclopropane in the presence of the phase transfer catalyst triethylbenzylammonium chloride at 75°C for 8 hours in the presence of the following components, wt %: diethylamine 4.7; cis-2,3-dichloromethyl-hem-dichlorcyclopropane 6.7; dimethylsulphoxide 87.8; triethylbenzyl ammonium chloride 0.26; potassium hydroxide 0.54; a dibutylamine reaction is carried out in the following proportions, wt %: dibutylamine 8; -2,3-dichloromethyl-hem-dichlorcyclopropane 6.45; dimethylsulphoxide 84.8; ammonium chloride 0.25; potassium hydroxide 0.5.

EFFECT: higher target product yield and higher quality.

2 cl, 1 tbl, 1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to field of organic chemistry, namely to method of obtaining N,N'-di(1-adamantyl)bispidin-9-ones, where R=R'=methyl (1a), R=R'=ethyl (1b), R=R'=propyl (1c), R=methyl and R'=1-adamantylaminomethyl (2), R=R'=1-adamantylaminomethyl (3). Method is realised by two-stage condensation, at the first stage condensed is 1-aminoadamantane with formaldehyde, at the second stage formed product is condensed with ketones in the same reactor with heating in butanol or other alcohols. Obtained products are extracted after condensing reaction mass under vacuum with hot toluene and re-crystallised from toluene.

EFFECT: N,N'-di(1-adamantyl)bispidin-9-ones, which can be used as substances for medications and as initial substances for obtaining novel derivatives of N,N'-di(1-adamantyl)bispidine .

5 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a biologically active analgesic with non-opioid action 2-[3'-(6'-chloropyridyl)]-7-azabicyclo[2.2.1]-haptane, and specifically to a method of producing an exo-isomer thereof via isomerisation of an endo-isomer in the presence of strong bases in an aprotic solvent solution at room temperature. The disclosed method is easily implemented in industrial conditions and enables to obtain 2-exo-[3'-(6'-chloropyridyl)]-7-azabicyclo[2.2.1]-haptane with high output.

EFFECT: high output.

4 cl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: compounds can find application for preventing or treating cancer, lung cancer, non-small cells lung cancer, small-cell lung cancer, EML4-ALK hybrid polynucleotide-positive cancer, EML4-ALK hybrid polynucleotide-positive lung cancer or EML4-ALK hybrid polynucleotide-positive non-small cells lung cancer. In formula (I) -X-: group of formula , A represents chlorine, ethyl or isopropyl; R1 represents phenyl wherein carbon in the 4th position is substituted by the group -W-Y-Z, and carbon in the 3rd position can be substituted by a group specified in a group consisting of halogen, R00 and -O-R00; R00: lower alkyl which can be substituted by one or more halogen atoms; -W-: a bond, piperidine-1,4-diyl or piperazine-1,4-diyl; -Y- represents a bond; Z represents a monovalent 3-10-membered monocyclic non-aromatic heterocyclic ring which contains 1 to 4 heteroatoms specified in a group consisting of nitrogen, oxygen and sulphur, which can be substituted by one or more substitutes R00; R2 represents (i) an optionally bridged saturated C3-10cycloalkyl which can be substituted by one or more groups specified in -N(lower alkyl)2, lower alkyl, -COO-lower alkyl, -OH, -COOH, -CONH-RZB and morpholinyl, or (ii) a monovalent 3-10-membered monocyclic non-aromatic heterocyclic ring which contains 1 to 4 heteroatoms specified in a group consisting of nitrogen, oxygen and sulphur, which can be substituted by one or more groups specified in a group consisting of lower alkyl, -CO-lower alkyl, oxo, -CO-RZB and benzene; and RZB: phenyl which can be substituted by a group consisting of halogen and -O-lower alkyl; R3 represents -H.

EFFECT: invention refers to new compounds of formula or their pharmaceutically acceptable salts possessing the properties of a selective inhibitor of EML4-ALK hybrid protein kinase activity.

16 cl, 201 tbl, 582 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to novel compounds of formula I: where n has values 0 or 1, and Cy represents a heteroaryl group, selected from such groups as 2-furanyl, 3-furanyl, 2-oxazolyl, 4-oxazolyl, 5-oxazolyl, 3-isoxazolyl, 4-isoxazolyl, 5-isoxazolyl and 4-pyridinyl, where heteroaryl groups are optionally substituted by up to 3 substituents, different from hydrogen, independently selected fromC1-6alkyl, C2-6alkenyl, C2-6alkinyl, C3-8cycloalkyl, substituted phenyl, furyl, halogen, -OR', -CF3, -CN, -NO2, -SO2R', -SO2NR'R″, -R'SO2R″, where R' and R″ are independently selected from hydrogen, C1-6alkyl, where the term "substituted", applicable with respect to substituted phenyl, relates to substitution with one or several halogens, and their pharmaceutically acceptable salts, as well as to pharmaceutical compositions based on the said compounds.

EFFECT: application of the said compounds for treatment and/or prevention of wide spectrum of CNS diseases and disorders.

13 cl, 2 dwg, 1 tbl, 11 ex

FIELD: biotechnologies.

SUBSTANCE: invention refers to new positively charged NSAIA prodrugs of a common formula (1, 2a, 2b, 2c or 2d) of "1, 2a, 2b, 2c or 2d structure"

Structure 1, Structure 2a,

Structure 2b, Structure 2c, Structure 2d. Values of R, R1, R2, R3, R4, R5, Ary, X radicals are presented in Claims 1,2.

EFFECT: increasing agent penetration speed.

22 cl, 14 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula

,

where: A is CA1; E is CE1; W is (CH2)n; Y is (CH2)P; n and p are independently equal to 0 or 1; R1 is a phenyl which is substituted with a phenyl {which is optionally substituted with a halogen, hydroxy, CH(O), CO2H, C1-4alkyl, C1-4alkyl-(N(C1-4alkyl)2), C1-4alkyl(NH2), C1-4alkyl(NH(C1-4alkyl)), C1-4hydroxyalkyl, CF3, C1-4alkylthio, C1-4alkyl(heterocyclyl) or C1-4alkylNHC(O)O(C1-4alkyl)} or a heterocyclyl; and the heterocyclyl is optionally substituted with C1-6alkyl; R2 is NHC(O)R3; and R3 is C1-4alkyl {substituted with NR7R8 or a heterocyclyl}, C3-7cycloalkyl (optionally substituted with a NR43R44 group) or a heteroaryl; where R7, R8, R43 and R44 are as defined in claim 1; wherein the heteroaryl is optionally substituted with a halogen, C1-4alkyl, CF3, C1-4alkoxy, OCF3, heterocyclyl or an amino(C1-4alkyl) group; R7 and R8 are independently C1-6alkyl; A1, E1 and G1 are independently hydrogen or halogen; unless otherwise stated, the heterocyclyl is optionally substituted with C1-6alkyl; R25 is C1-6alkyl; R50 is hydrogen or C1-6alkyl (optionally substituted with a NR51R52 group); R30, R36, R40, R42 or R44 is independently hydrogen, C1-6alkyl(optionally substituted with hydroxy, C1-6alkoxy, C1-6alkylthio, C3-7cycloalkyl (which is optionally substituted with hydroxy) or NR45R46), C3-7cycloalkyl (optionally substituted with a hydroxy(C1-6alkyl) group) or a heterocyclyl (optionally substituted with C1-6alkyl); R29, R35, R39, R41, R43, R45, R46 and R51 are independently hydrogen or C1-6alkyl; where the heterocyclyl is a non-aromatic 5- or 6-member ring containing one or two heteroatoms selected from a group comprising nitrogen and oxygen; and where the aryl is phenyl or naphthyl; and where the heteroaryl is an aromatic 5- or 6-member ring, optionally condensed with another ring (which can be carbocyclic and aromatic or non-aromatic), having one or two heteroatoms selected from a group comprising nitrogen, or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition based on said compounds.

EFFECT: obtaining novel compounds and a pharmaceutical composition based on said compounds, which can be used in medicine to treat a PDE4-mediated disease state.

10 cl, 81 dwg, 15 tbl, 375 ex

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to 1,5-bis[(tert-butylamino)methyl]-N,N'-di-tert-butylbispidin-9-one and a method for production thereof. 1,5-bis[(tert-butylamino)methyl]-N,N'-di-tert-butylbispidin-9-one is obtained by condensation of acetone with 1,3,5-tri-(tert-butyl)-1,3,5-triazacyclohexane while heating in an alcohol in the presence of acetic acid. The reaction is carried out while heating in ethanol or another alcohol. The obtained product is extracted after condensation of the reaction mass in a vacuum with hot toluene and recrystallised from ethyl alcohol.

EFFECT: obtaining a novel compound which can be used as a starting substance when producing bispidine and 1,3-diazaadamantane derivatives.

2 cl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds in the form of a free base or a pharmaceutically acceptable acid addition salt specified in a group including: (4S,5R)-4-[5-(1H-indol-5-yl)-pyrimidin-2-yloxy]-1-azabicyclo[3.3.1]nonane, 5-{2-[(4S,5R)-(1-azabicyclo[3.3.1]non-4-yl)oxy]-pyrimidin-5-yl}-1,3-dihydroindol-2-one, (4S,5R)-4-[6-(1H-indol-5-yl)-pyridin-3-yloxy]-1-azabicyclo[3.3.1]nonane, (4S,5R)-4-[5-(1H-indol-5-yl)-pyridin-2-yloxy]-1-azabicyclo[3.3.1]nonane, (4S,5R)-4-[6-(1H-indol-5-yl)-pyridazin-3-yloxy]-1-azabicyclo[1.3.1]nonane and 5-{6-[(4S,5R)-(1-azabicyclo[3,3,1]non-4-yl)oxy]-pyridazin-3-yl}-1,3-dihydroindol-2-one, possess nAChR α7 agonist activity.

EFFECT: using them in pharmaceutical compositions and for preparing a drug applicable for preventing and treating a memory disorder.

21 cl, 2 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 relates to pharmaceutical industry, namely to pharmaceutical composition in form of dry, free-flowing, compressible powder, which contains (a) rapamycin and mixture of (b) hydrophobic polyoxyethylene and polyoxypropylene block-copolymer and (c) hydrophilic polyoxyethylene and polyoxypropylene block-copolymer with weight proportions b:c equal from 1:3 to 1:9.

EFFECT: invention provides increase of powder compressibility and increase of rapamycin stability and bioavailability.

15 cl, 8 ex, 5 tbl

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