Selective antibacterial agents, represented by 3-(azol-1-yl)-6-amino-substituted 1,2,4,5-tetrazines

FIELD: pharmacology.

SUBSTANCE: invention relates to 3-(azol-1-yl)-6-amino substituted 1,2,4,5-tetrazines of the formula: , where Het = imidazol-1-yl, NHR = allylamino (Ia); Het = 4-methylimidazol-1-yl, NHR = allylamino (Ib); Het = benzimidazol-1-yl, NHR = allylamino (Ic); Het = indazol-1-yl, NHR = allylamino (Id); Het = imidazol-1-yl, NHR = propargylamino (Ie); Het = 4-methylimidazol-1-yl, NHR = propargylamino (If); Het = benzimidazol-1-yl, NHR = propargylamino (Ig); Het = indazol-1-yl, NHR = propargylamino (Ih). The invention also relates to antibacterial agents.

EFFECT: new compounds of formula I, active against gram-negative bacteria Neisseria gonorrhoeae and clinically relevant pathogenic and opportunistic microorganisms, are obtained.

2 cl, 2 tbl, 8 ex

 



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to organic chemistry, namely to benzimidazole-4-carboxamide derivatives of formula , wherein X means an alkenyl group C2-C7 substituted by two methyls, nitro-radical mono-substituted thienyl, unsubstituted quinolinyl, unsubstituted indolyl, unsubstituted pyridazinyl, unsubstituted piperazinyl, C1-C6-alkyl disubstituted piperazinyl, unsubstituted piperidinyl, unsubstituted pyrazinyl, unsubstituted imidazolyl, unsubstituted pyrimidinyl, phenyl monosubstituted pyrimidinyl, pyrimidinyl disubstituted by an amine radical and a radical specified in a group containing -F, -Cl, -Br or -I, hydroxyl trisubstituted phenyl, methoxy-radical trisubstituted phenyl, hydroxyl and methoxy-radical disubstituted phenyl, pyrazolyl disubstituted by a radical specified in a group containing a C1-C6-alkyl, and by a radical specified in a group containing -F, -C1, -Br or -I; Y means aminophenyl monosubstituted by a radical of -F, -O, -Br or -I phenyl, hydroxyethyl disubstituted by hydroxymethyl or C1-C6-alkyl and phenyl monosubstituted by a nitro group, an amino group or a halogen atom; Y also means unsubstituted piperazinyl, unsubstituted pyridyl, unsubstituted pyrazinyl, C1-C6-alkyl monosubstituted thiazol, unsubstituted pyrimidinyl, unsubstituted purinyl. The invention also refers to a pharmaceutical composition based on the compound of formula (I), using the compound of formula (I), a method for producing the compound of formula (I).

EFFECT: there are prepared new benzimidazol-4-carboxamide derivatives possessing antiviral activity.

5 cl, 6 dwg, 4 tbl, 688 ex

FIELD: chemistry.

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

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

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to a novel compound of formula

(I)

or its pharmaceutically acceptable salt, possessing properties of the IKKβ and TNFα inhibitor. The compound can be used with an additional therapeutic agent, selected from vincristine, camptothecin hydrochloride (CPT-11), lefunomid, dexamethasone and TNFα. Preferable are compounds of formula (I), corresponding to 2-{5-chloro-2-[(1R,2R)-2-hydroxycyclopentylamino]pyrimidin-4-yl}-N-cyclopropyl-1H-indole-4-carboxamide and 2-{5-chloro-2-[(1R,2S)-2-hydroxycyclopentylamino]pyrimidin-4-yl}-N-cyclopropyl-1H-indole-4-carboxamide.

EFFECT: compound can be applied in the treatment of inflammatory diseases such as rheumatoid arthritis, chronic obstructive lung disease, bronchial asthma, multiple sclerosis and intestinal inflammatory diseases, or cancer diseases, such as multiple myeloma, colon cancer, pancreas cancer and ovary cancer, by IKKβ inhibition.

30 cl, 4 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula (I) such as below, or to their pharmaceutically acceptable salts, wherein R1 means H, C1-8alkyl morpholinyl, haloC1-8alkylamino, C1-8alkyloxadiazolyl, hydroxyl, halopyrrolidinyl, azetidinyl, C1-8alkylamino, amino, cyano C1-8alkylamino, halophenylC1-8alkylamino or cyanoC3-8cycloalkylamino; R2, R3, R4, R5 and R6 independently mean H, C1-8alkyl, haloC1-8alkyl, hydroxyC1-8alkyl, C1-8alkoxy, haloC1-8alkyloxy, halogen, hydroxyl, cyanopyrazinyloxy, halogen, hydroxyl, cyanopyrazinyloxy, pyrazolyl, C1-8alkylpyrazolyl, imidazolyl, benzimidazolyl, 6-oxo-6H-piridazinyl, C1-8alkyl-6-oxo-6H-pyridazinyl, piperazinyl, N-C1-8alkylpiperazinyl, piperidinyl, difluoropyrrolidinyl, phenylimidazolyl, oxo-pyrrolidinyl, oxo-oxazolidinyl, morpholinyl, oxo-morpholinyl, oxo-pyridinyl, 2-oxo-2H-pyrazinyl, difluoropiperidinyl, haloC1-8alkylpiperidinyl, piperidinylC1-8alkoxy, oxetanyloxy, C1-8alkylpyrazolyl, halopyridinyl, C1-8alkylpyridinyl, C3-8cycloalkyl, C3-8 cycloalkylC1-8alkyl, halophanyl, C1-8alkylcarbonylamino-C3-8-cycloalkyl-C1-8alkyl, haloC1-8alkylpiperazinyl, C1-8alkylamino, C1-8alkoxy-C1-8alkylpiperazinyl, C3-8cycloalkylpiperazinyl, hexahydropyrrolo[1,2-a]pyrazinyl, 5,6-dihydro-8H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl, C1-8alkylimidazolyl, azetidinyl, C3-8cycloalkylpiperazinyl, C1-8alkylimidazolyl, C1-8alkoxy C1-8alkoxy, imidazo[4,5-c]pyridinyl, C1-8alkylpiperazinyl, hexahydro-pyrrolo[1,2-a]pyrazinyl, haloazetidinyl, pyrimidinyl and C2-8alkenyloxy; A1 means -CH2-, carbonyl, -C(O)O- or is absence; A2 means N, CR7; A3 means N, CR8; A4 means N, CR9; R7 means H, C1-8alkyl, haloC1-8alkyl, halogen, hydroxyl, haloC1-8alkylaminocarbonyl; halophenylC1-8alkylaminocarbonyl, phenyl-C3-8-cycloalkylaminocarbonyl, haloC1-8alkylphenylC1-8alkylaminocarbonyl, halophenylC3-8 cycloalkylaminocarbonyl, halophenylC3-8cycloalkylC1-8alkylaminocarbonyl; R8 means H, C1-8alkyl, haloC1-8alkyl, halogen or hydroxyl; or R7 and R8 together with a carbon atom they are attached to, form C3-8cycloalkyl or substituted pyrrolidine, wherein substituted pyrrolidine represents pyrrolidine, N-substituted haloC1-8alkyl or formyl; R9 means H, C1-8alkyl, haloC1-8alkyl, halogen or nitro; or R8 and R9 together with a carbon atom they are attached to, form C3-8cycloalkyl; or its pharmaceutically acceptable salt

EFFECT: compounds inhibit the enzyme catepsin that enables using them in pharmaceutical compositions.

27 cl, 8 dwg, 1 tbl, 88 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a chemical compound of formula wherein R=benzyl and to an antituberculous therapeutic agent representing a composition of imidazo[1,2-b][1,2,4,5]tetrazine derivative of formula I, wherein R=benzyl, isopropyl or phenyl and the known antituberculous preparation pyrazinamide with the ingredients in mole ratio 1:1.

EFFECT: there are prepared new antituberculous therapeutic agents.

2 cl, 2 tbl, 6 ex

Antiviral compounds // 2541571

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula I, such as below, or its pharmaceutically acceptable salts. What is described is a method for preparing them.

,

wherein: A independently from B means phenyl,

, or ,

and B independently from A means phenyl,

, or ,

and the values Z, Y, D, L1, L2, L3, Z1, Z2 are presented in the patent claim.

EFFECT: compounds are effective for hepatitis C virus (HCV) replication inhibition.

17 cl, 3 tbl, 8 dwg, 177 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula , wherein A represents CRaRb or -CH2-CH2-; R1 represents hydrogen or alkyl; R2 represents hydrogen or alkyl; R3 represents alkyl, cycloalkyl, cycloalkylalkyl, aryl, substituted aryl, 1H-pyrazolyl or substituted 1H-pyrazolyl, wherein substituted aryl represents aryl substituted by 1-3 substitutes independently specified in alkyl, halogen and halogenalkyl, and wherein substituted 1H-pyrazolyl represents 1H-pyrazolyl substituted by 1-3 substitutes independently specified in alkyl and aryl; Ra represents hydrogen or methyl; Rb represents hydrogen or methyl; or Ra and Rb together with a carbon atom, to which they are attached, form cyclopropyl, cyclobutyl or cyclopentyl; provided Ra and Rb both represent hydrogen, or both represent methyl simultaneously, R3 represents (1-methylcyclopropyl)methyl, which possess the inhibitory action on 11b-HSD1.

EFFECT: preparing the compounds, which possess the inhibitory action on 11b-HSD1.

15 cl, 1 tbl, 32 ex

FIELD: chemistry.

SUBSTANCE: invention relates to application of 2-R1-4-R2-6-polynitromethyl-1,3,5-triazines of general formula: , where n=0, X=NO2, Cl, Br, R1=R2=OR3, OAr (R3=CH3, C2H5, CH2(CH2)6CH3, CH2CH2Cl, Ar=metha-C6H4CH3), R1=OR3, OAr, R2=N(C2H5)2; n=1, X=Cl, R1=OR3, R2=NH(CH2)2NH2, N(CH2CH2)2NCH3 as compounds, which possess antibacterial activity.

EFFECT: identification of compounds based on 1,3,5-triazine derivatives, which possess high antibacterial activity.

3 tbl, 7 ex

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, namely to mixture of E- and Z-isomers of (4-bromophenyl)ethylidene hydrazide of 2-[6-methyl-1-(thiethan-3-yl)uracyl-3-yl]acetic acid in molar ratio 3.5:1 of general formula: .

EFFECT: obtained is novel mixture of isomers, demonstrating hypotensive activity.

2 cl, 4 tbl, 4 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 a chemical compound of formula wherein R=benzyl and to an antituberculous therapeutic agent representing a composition of imidazo[1,2-b][1,2,4,5]tetrazine derivative of formula I, wherein R=benzyl, isopropyl or phenyl and the known antituberculous preparation pyrazinamide with the ingredients in mole ratio 1:1.

EFFECT: there are prepared new antituberculous therapeutic agents.

2 cl, 2 tbl, 6 ex

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