New pyrimidine inhibitors of human adenovirus replication
SUBSTANCE: invention relates to new 5-aminouracil derivatives containing 4-(phenoxy) benzyl or ω-(phenoxy)alkyl substituent in the N1 position, corresponding to the general structural formula (I). Compounds represent a new class of anti-adenoviral agents of a non-nucleoside nature. In the general formula (I), X = CH or N; Y=(CH2)2, (CH2)3, (CH2)4 or C6H4; R1= H, R2= C6H or 3,5-Cl2C6H3; R1+R2= morpholino; R3=H, F or Cl.
EFFECT: compounds have a selective antiviral effect against human adenoviruses and can be used for treatment of adenoviral infections.
1 dwg, 3 tbl, 11 ex
SUBSTANCE: preparation can be applied for elimination of fungi and in treatment of diseases, caused by fungi, as well as for the prevention of damage by fungi to different materials and agricultural products. The fungicidal preparation represents an associate of 5-[3,5-dichloro-2-hydroxybenzylidine)amino]-4-hydroxy-1H-pyrimidine-2-one with 1,2,3,4,5-pentahydroxy-6-methylaminohexane and corresponds to the following formula: . Compounds were obtained in the crystalline form, and their structure is proved by spectra of proton magnetic resonance in dimethylsulphoxide.
EFFECT: preparation has a wide spectrum of action and high solubility, which increases efficiency of its application in the form of solutions.
2 tbl, 6 ex
SUBSTANCE: novel chemical compound - L-ascorbate of 1-(2-hydroxyethyl)-4,6-dimethyl-1,2-dihydropyrimidin-2-one has the formula: According to tests conducted in multiple (course) application conditions in a dose of 20 mg/kg with an intraperitoneal administration method, data which indicate stimulation of physical performance of white laboratory rats were obtained.
EFFECT: high physical performance in sports medicine, labour environment and sports.
2 cl, 1 tbl
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to a compound - 6-(4-benzylpiperazino)-1,3-dimethyluracyl dihydrochloride of formula I showing antispasmodic and bronchial spasmolytic activity.
EFFECT: invention extends the range of antispasmodic and bronchial spasmolytic low-toxic agents.
3 cl, 3 tbl
SUBSTANCE: invention relates to a novel broad-action fungicidal agent which is a salt of 2,4-dioxo-5-(2-hydroxy-3,5-dichlorobenzylidene)amino-1,3-pyrimidine of general formula: or dimer thereof: , where X is selected from: Na+, K+, Li+, NH4 +.
EFFECT: agent can be used to treat fungal diseases, as well as prevent damage to different materials and agricultural products by fungi.
SUBSTANCE: invention relates to an improved method of producing 5-amino-6-methyluracil of formula: , by reacting 5-bromo-6-methyluracil with aqueous ammonia in preferable molar ratio of reagents of 1:11 and temperature 110-140°C for 16-20 hours followed by extraction of the product.
EFFECT: simple process and high cost effectiveness while maintaining high output of the product.
FIELD: organic chemistry, microbiology.
SUBSTANCE: invention relates to new synthetic biologically active derivatives of pyrimidine, namely to 2,4-dioxo-5-(2-hydroxy-3,5-dichlorobenzylidene)imino-1,3-pyrimidine potassium, sodium or ammonium salt of the general formula: wherein X is taken among the group: Na+, K+, NH+ 4. The claimed substance shows expressed antibacterial activity directed mainly against different fungi, bacteria, protozoan and viruses.
EFFECT: valuable biological properties of compounds.
13 tbl, 13 ex
SUBSTANCE: claimed invention relates to the field of veterinary and is intended for fighting porcine reproductive and respiratory syndrome (PRRS). The method includes the vaccination of pigs with PRRS with the provision of a reduction of hyperthermia duration and protection of lung integrity. The vaccine is obtained by a method, including mixing a live vaccine, prepared for immediate introduction, with an adjuvant-diluent (AD). The said adjuvant-diluent represents an "oil-in water" type emulsion, which contains per 100% of its weight: from 99 to 50 wt % of water and from 1 to 50 wt % of an oil adjuvant. The oil adjuvant contains per 100 % of its weight: from 1 to 95 wt % of at least one mineral oil and from 1 to 80 wt % of at least one SAS. The mineral oil represents oil of a Marcol or Draekol type. SAS represents an ester, obtained by the condensation of a fatty acid with sorbitol or mannitol.
EFFECT: obtaining the preparation for fighting reproductive and respiratory syndrome.
7 cl, 9 tbl, 1 ex
SUBSTANCE: present invention relates to a novel (2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-ylmethyl aryl phosphoramidate of general formula I or a stereoisomer or a pharmaceutically acceptable salt thereof, having properties of nucleoside inihibitors of RNA polymerase NS5B of the hepatitis C virus. The invention also relates to a method of producing compounds, pharmaceutical compositions and a medicinal agent based on said compounds. In general formula 1 , R1 is hydrogen, (CH3)2[(CH3)3C]Si, C2-C6acyl, optionally substituted with a benzyloxy group, NR5R6 group, wherein R5 and R6 are independently hydrogen or C1-C4alkyl; 1-pyrrol-2-ylcarbonyl, piperidin-3-ylcarbonyl or piperidin-4-ylcarbonyl; R2 and R3 are F or R2 is F or OH and R3 is CH3; R4 is hydrogen or methyl; Ar is phenyl, pyridyl or naphthyl, where the phenyl, pyridyl or naphthyl is optionally substituted with at least one of C1-3alkyl, C2-4alkenyl, C2-4alkynyl, C1-3alkoxy, F, Cl, Br, I, nitro, cyano, -N(C1-3alkyl)2; Pm is 2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl or 4-(4-amino-2-oxo-2H-pyrimidin-1-yl), wherein the amino group is optionally substituted with 1-pyrrol-2-ylcarbonyl, piperidin-3-ylcarbonyl, piperidin-4-ylcarbonyl or a C(O)R8 radical, where R8 is C1-C4alkyl, optionally substituted with a NR6R7 group, where R6 and R7 are independently hydrogen or C1-C4alkyl; C1-3alkoxy, optionally substituted with a phenyl; X is O or N-R9, where R9 is C1-C4alkyl, optionally substituted with OH or OCH3; n=1, 2 or 3.
EFFECT: compounds can be used to prevent and treat viral infections, including hepatitis C.
12 cl, 1 tbl, 11 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to compounds intended for treatment of hepatitis C of formula
its stereoisomeric forms, pharmaceutically acceptable salts or solvates, where R1 represents hydrogen; R2 represents hydrogen, napthyl or phenyl, optionally substituted with 1, 2 or 3 substituents, selected from halogen and C1-C6alkyl; R3 and R4 represent hydrogen or C1-C6alkyl; R5 represents C1-C10alkyl, optionally substituted with C1-C6alkoxygroup, C3-C7cycloalkyl or benzyl; R8 represents hydrogen.
EFFECT: claimed are novel compounds and composition on their base, effective against hepatitis C.
12 cl, 4 ex, 1 tbl
SUBSTANCE: antiviral agent of poly-N1-hydrazino(imino)methyl-1,6-hexane diamine-amino(imino)methyl-1,6-hexanediamine of general formula: wherein: HX is an acid, n=3-20, m=4-20, possessing an activity on simple and complex RNA- and DNA-containing viruses of humans, animals, plants, bacteria and fungi.
EFFECT: what is created is the broad-spectrum antiviral agent possessing the activity on viruses found both intra-, and extracellularly.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to organic chemistry, namely to bis-benzimidazole derivatives of formula I and their optional stereoisomers, pharmaceutically acceptable salts and solvates, wherein R and R' are independently specified in -CR1R2R3, phenyl substituted by 1 substitute specified in halogen; and tetrahydrofuranyl, wherein R1 is specified in C1-4alkyl optionally substituted by methoxy, hydroxyl or dimethylamino; C3-6cycloalkyl; phenyl optionally substituted by 1, 2 or 3 substitutes optionally specified in halogen, C1-4alkoxy, trifluoromethoxy, or 2 substitutes on adjoining atoms of the ring form 1,3-dioxolane group; benzyl substituted by halogen or methoxy; pyridinyl; indolyl; pyridinylmethyl or indolylmethyl; R2 is specified in hydrogen, hydroxyl, di-C1-4alkylamino, (C3-6cycloalkyl) (C1-4alkyl)amino, C1-4alkylcarbonylamino, phenylamino, C1-4alkyloxycarbonylamino, (C1-4alkyloxycarbonyl)(C1-4alkyl)amino, C1-4alkylaminocarbonylamino, tetrahydro-2-oxo-1(2H)-pyrimidinyl, pyrrolidin-1-yl, piperidin-1-yl, 3,3-difluoropiperidin-1-yl, morpholin-1-yl, 7-azabicyclo[2.2.1]hept-7-yl and imidazol-1-yl; and R3 represents hydrogen or C1-4alkyl or CR2R3 together form carbonyl; or CR1R3 form cyclopropyl group. The invention also refers to a pharmaceutical composition based on a compound of formula I.
EFFECT: there are prepared bis-benzimidazole derivatives possessing the inhibitory activity on hepatitis C virus.
9 cl, 4 tbl, 3 ex
SUBSTANCE: invention refers to biotechnology and immunology. There are described antibodies and their functional equivalents specifically binding to RSV. Also, the invention refers to nucleotide sequences coding the above antibody, as well as to the cells producing antibodies, and to methods for producing the above antibodies.
EFFECT: invention can be used in medicine.
23 cl, 4 dwg, 3 tbl, 4 ex
SUBSTANCE: invention relates to heterocyclic compounds of general formula I
or to pharmaceutically acceptable salts or solvates or stereoisomers thereof, where R and R* are each independently -CR1R2R3, C1-4alkylamino, benzylamino, C6-10arylamino, heteroC4-7cycloalkyl containing 1 heteroatom selected from O; where R1 is selected from C1-4alkyl; phenyl, optionally substituted with 1, 2 or 3 substitutes independently selected from halogen, C1-4alkyl, C1-4alkoxy, trifluoromethoxy or 2 substitutes at neighbouring ring atoms, which form a 1,3-dixolane group; benzyl, optionally substituted with a halogen or methoxy; phenylsulphonylmethyl; C3-5heteroaryl containing 1 to 2 heteroatoms independently selected from N and O; C3-5heteroarylmethyl containing 1 to 2 heteroatoms selected from N and C3-6cycloalkyl; R2 is selected from hydrogen, hydroxyl, di-C1-4alkylamino, C1-4alkylcarbonylamino, C1-4alkyloxycarbonylamino, C1-4alkylaminocarbonylamino, piperidin-1-yl or imidazol-1-yl; R3 is hydrogen or, alternatively, R2 and R3 together form an oxo group; or R1 and R3 together form cyclopropyl; under the condition that if one of R and R* is -CH(C6H5)N(CH3)2, the other cannot be -CH(C6H5)NHC(=O)OCH3; and if R and R* are identical, R1 is not phenyl, when R2 is hydroxyl, acetylamino, methoxycarbonylamino or tert-butoxycarbonylamino, and R3 is hydrogen; and R1 is not C1-4alkyl, when R2 is C1-4alkyloxycarbonylamino, and R3 is hydrogen. The invention also relates to a pharmaceutical composition based a compound of formula I and use thereof.
EFFECT: obtaining novel compounds which are useful in preventing or treating HCV infection.
9 cl, 2 tbl, 3 ex
SUBSTANCE: invention relates to a sodium salt of formula I compound in the solid amorphous form. The sodium salt of formula (I) compound is obtained by (a) the preparation of a mixture of the formula I compound in a non-aqueous solvent and a water solution of sodium hydroxide; and (b) drying by spraying of the mixture (a) in a spray-drying device. The stage (a) includes mixing the sodium hydroxide solution with the said solvent and further addition of the formula I compound. The solvent is represented by halogen-containing hydrocarbon. The invention also relates to a pharmaceutical composition, possessing HCV inhibiting properties, including sodium salt of the formula I compound in the amorphous form, and a pharmaceutically acceptable carrier.
EFFECT: sodium salt of the formula (I) compound for application as HCV inhibitor and medication for HCV treatment.
10 cl, 7 dwg, 3 ex
SUBSTANCE: invention relates to novel polyheterocyclic compounds of formulas Ia or Ib, given below, stereoisomers, pharmaceutically acceptable salts or their mixture, where m=0.1 or 2; n=0.1 or 2; p=0.1 or 2; q=0.1 or 2; r=0. 1, 2 or 3; stands for a single bond or a double bond; and stands for a double bond in a macrocyclic internal combination with cyclopropyl formyl; stands for a single bond in a cycle D, E, E1 and G, where D and G independently stand for oxygen, E and E1 independently stand for C(Ra)(Rb); R10 stands for hydrogen; Ra, Rb and Rc independently on each other stand for hydrogen; when r=0 E is absent, D and E1 are directly bound; L stands for methylene (CRbRc); T stands for nitrogen (N) or CH; U stands for carbon (C); W stands for oxygen; X stands for oxygen; Y stands for nitrogen (N) or CH; Z stands for OH; C1-C20 alkyl-sulphonylamido, C3-C20-cycloalkyl-sulphonylamido; R1 and R2 independently stand for C1-C20-alkyl, C3-C20 cycloalkyl, C6-C12 arylamine, C1-C20 alkoxycarbonyl-amino, C2-C20 heterocyclic sulphonylamide ring; R3, R4, R5, R6 - independently stand for H; R7, R8 and R9 independently stand for H. The compounds inhibit replication of protease NS3 of the hepatitis C virus.
EFFECT: improved properties of the compounds.
7 cl, 1 tbl, 11 dwg, 118 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to medicine, namely to pharmacology and virology, and deals with the creation of medications, possessing an anti-retroviral activity.
EFFECT: claimed is a pharmaceutical composition, containing an activated-potentiated form of antibodies to the HIV protein or peptide.
13 cl, 2 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to novel compounds of general formula (I) or their pharmaceutically acceptable salts, which possess properties of RNA-polymerase inhibitor, in particular HCV inhibitor. Such disease can be hepatitis C. In formula (I)
is selected from the group, including simple carbon-carbon bond and double carbon-carbon bond; R1 represents hydrogen atom; R2 represents hydrogen atom; R3 represents hydrogen atom; R4 is selected from the group, including
R5 is selected from the group, including hydrogen atom, C1-C6alkyl and C1-C6alkyloxy; R6 is selected from the group, including hydrogen atom, C1-C6alkyl and C1-C6alkyloxy; R7 is selected from the group, including hydrogen atom, phenyl, 5-membered heterocycle, carbocycle with 2 condensed cycles, where 5-membered heterocycle contains at least 1 heteroatom, selected from the group, consisting of N, O and S, and where phenyl, heterocycle and carbocycle with 2 condensed cycles are optionally substituted with at least one of RJ and RK.
EFFECT: compounds can be used for treatment of disease, which can be treated by HCV inhibition.
21 cl, 2 tbl, 7 ex
SUBSTANCE: as the substance, possessing the arcaricidal action, applied is N,N'-(sulphonyldi-p-phenylene)bis-N",N"-dimethylformamidine.
EFFECT: application of the claimed substance assists to deal with ticks and mites in an efficient and safe way.
6 dwg, 8 tbl, 6 ex