51 results about "Viral neuraminidase" patented technology

The invention relates to a multimeric compound or a pharmaceutically acceptable salt or derivative thereof which comprises three or more neuraminidase-binding groups attached to a spacer or linking group, in which the neuraminidase-binding group is a compound which binds to the active site of influenza virus neuraminidase, but is not cleaved by the neuraminidase. The invention also relates to processes for the preparation of the multimeric compound defined above, pharmaceutical compositions containing them or methods for the treatment and/or prophylaxis of a viral infection involving them.

The invention belongs to the field of marine medicines, and relates to a fucosan sulphate, a preparation method thereof and application of the fucosan sulphate in preparing an anti-influenza virus medicine. Polysaccharide with a main chain taking alpha-1,2-D-mannose and beta-1,4-D-glucuronic acid as repetitive units, and with a branched chain of alpha-1,3-L-fucosan sulphate is obtained by virtue of hot-water extraction, calcium chloride precipitation and DEAE-Cellulose chromatographic column purification. The fucosan sulphate prepared by the invention is high in inhibition effect on the influenza virus neuraminidase activities of A H1N1, H5N1 and H3N2, and obvious in protection effect on the dog kidney epithelial cells infected by A H1N1. The fucosan sulphate provided by the invention has the advantages of being rich in raw material source, simple in preparation process, easy to industrialize, high in product water solubility, high in stability, free from toxic and side effects, and the like, and has the prospect of being developed to the anti-influenza virus medicine.

The invention relates to 3-[[2-(benzylamino) thiazole-5-yl]-methyl] quinolone-2(1H)-ketone as shown in chemical structural formulas I and II or a salt thereof. In the chemical structural formulas, R, X<1> and X<2> are selected from hydrogen, deuterium, C1-C2 alkyl, C3-C4 linear-chain alkyl or branched-chain alkyl; X<3> is selected from hydroxyl, methoxyl and ethyoxyl; is selected from hydrogen, deuterium, C1-C2 alkyl, fluorine, fluorine or bromine; X4 and X6 are selected from hydrogen, deuterium, C1-C2 alkyl, fluorine, fluorine, bromine or nitryl; X5 and X7 are selected from hydrogen, deuterium and C1-C2 alkyl. The invention also provides an application of the 3-[[2-(benzylamino) thiazole-5-yl]-methyl] quinolone-2(1H)-ketone in preparation of an influenza virus neuraminidase inhibitor.

The invention provides a compound expressed by a general formula I, or its pharmaceutically acceptable salt, and an analyzed enantiomer and a purified diastereomer, wherein R<1>is H or C1-12 alkyl groups; R<2> is H, -C(O)R<1a>, -C(O)OR<1a> or -S(O)2R<1b>, wherein R<1a> is H or C1-6 alkyl groups, R<1b> is selected from H or C1-6 alkyl groups halogenated hydrocarbon, phenyl or aryl group; R<3> is selected from C1-4 alkyl groups substituted amino, halogen, hydroxyl, sulfydryl, guanidyl, nitryl or cyano group; and R<4> is -(CH2)nCO2H, -(CH2)nP(O)(OH)2, -(CH2)nCO2R<1a> and -(CH2)nP(O)(OR<1a>)2, wherein R<1a> is H or C1-6 alkyl groups, n is an integer between 0 and 4, or a salt of the above groups. The invention also provides a preparation method of the cyclohexene compound expressed by the general formula I, and an application of the cyclohexene compound taken as an influenza virus neuraminidase inhibitor for preparing the medicines to prevent or treat the influenza diseases.

The invention belongs to the technical field of biology and particularly relates to a rapid detection method of an influenza virus neuraminidase antibody. The detection method comprises the following steps of: coning the influenza virus neuraminidase gene and then transfecting eukaryotic cells so that influenza virus neuraminidase protein is in recombination expression on the surface of eukaryotic cells, combining with the influenza virus neuraminidase antibody in a sample to be detected, performing agglutination reaction and judging whether the influenza virus neuraminidase antibody exists in the sample to be detected according to whether the agglutination reaction happens or not. The method is simple, rapid, stable and highly sensitive, and has wide application value.

The invention discloses use of 4-alkyl-6-aryl-5-acetyl-1,3-thiazine represented by a chemical structural formula I and 4-alkyl-6-aryl-5-acetyl-2-amino-1,3-thiazine salts, or 4-alkyl-6-aryl-5-acetyl-2-amido-1,3-thiazine represented by a chemical structural formula II and 4-alkyl-6-aryl-5-acetyl-2-amido-1,3-thiazine salts for preparing a neuraminidase inhibitor of influenza viruses.

Methods for preparing viral neuraminidase inhibitors including antiviral peptides by specifically chemically modifying disulfide bonds in precursor molecules. A method of inhibiting viral neuraminidases by administering a viral neuraminidase inhibitor comprising an antiviral peptide prepared by the above methods and inhibiting the viral neuraminidase. Therapeutics for inhibiting viral neuraminidases, including effective amounts of viral neuraminidase inhibitors including antiviral peptides derived from selectively chemically modified disulfide bonds in precursor molecules, and present in a pharmaceutically acceptable carriers.

Methods and compositions for detection of drug resistant pathogens and treatment against infections thereof are provided. Methods for detection of oseltamivir-resistant influenza viruses by competitive binding assays utilizing non-oseltamivir influenza virus neuraminidase inhibitors and oseltamivir carboxylate are provided. Influenza virus neuraminidase inhibitors coupled to sensors and useful for employment in the methods of the invention are disclosed. Novel phosphonate compounds active as neuraminidase inhibitors against wild-type and oseltamivir-resistant influenza strains of H1N1, H5N1 and H3N2 viruses are disclosed. An enantioselective synthetic route to preparation of these phosphonate compounds via sialic acid is provided.

The invention provides influenza A-type influenza virus neuraminidase (NA), a gene and a preparation method thereof as well as a construction method of a screening model of an influenza virus neuraminidase inhibitor. Particularly, influenza A-type influenza virus H1N1 subtype neuraminidase is secretly expressed by pichia pastoris to obtain the neuraminidase with biological activity, and particularly, the truncated neuraminidases of 82 amino acids at N end of an NA full-length sequence is removed, so that an operation process of the NA prepared by totivirus, which is complicated, consumes time and has a safety problem, is avoided. According to the invention, the A-type influenza virus H1N1 subtype neuraminidase inhibitor screening model is also constructed by utilizing the neuraminidase; and the influenza virus H1N1 subtype neuraminidase has the advantages of definite mechanism of drug action, less material consumption, quick screening speed, high sensitivity, easy realization of high throughput screening and the like.

Novel dual-targeted, bifunctional anti-influenza drugs formed by conjugation with anti-inflammatory agents are disclosed. Exemplary drugs according to the invention include caffeic acid (CA)-bearing zanamivir (ZA) conjugates ZA-7-CA (1), ZA-7-CA-amide (7) and ZA-7-Nap (43) for simultaneous inhibition of influenza virus neuraminidase and suppression of proinflammatory cytokines. Synthetic methods for preparation of these enhanced anti-influenza conjugate drugs are provided. The synthetic bifunctional ZA conjugates act synergistically towards protection of mice lethally infected by H1N1 or H5N1 influenza viruses. The efficacy of ZA-7-CA, ZA-7-CA-amide and ZA-7-Nap conjugates is much greater than the combination therapy of ZA with anti-inflammatory agents.

The invention relates to a baicalin injection with anti-influenza virus effect, which is prepared from baicalin weighed according to required volume and set concentration, 0.6g of sodium dihydrogen phosphate, 2.16g of disodium hydrogen phosphate and 100ml of injection water through high-temperature high-pressure sterilization, wherein the pH value of sodium hydroxide is regulated to 7.0. The medicine has a remarkable advantages of in-vivo and in-vitro anti-influenza virus activity, high bioavailability, small side effect and adverse response and the like, has the effect of inhibiting neuraminidase activity to stop virus release, has unique advantages and wide development prospect in the field of preventing and treating influenza virus.

The invention relates to the field of biological medicines, particularly to an MASA (multi-analyte suspension array) detection kit for influenza virus H5N1 and H7N9 subtypes, and provides a primer pair and a probe for detecting influenza virus surface hemagglutinin antigen H5 and H7 subtypes, a primer pair and a probe for detecting influenza virus neuraminidase antigen N1 and N9 subtypes as well as a kit comprising the primer pairs and the probes and a usage method of the kit. The kit is good in sensitivity, accuracy and specificity and simple, convenient and quick to use, and detection of to-be-detected samples can be finished within four hours. Tests prove that no false positive result exists when the kit is used for detecting negative samples; the detection rate of 100% is realized when the kit is used for detecting samples containing H7N9 subtype viruses and H5N1 subtype viruses only; the H7N9 and H5N1 subtype viruses contained in samples can be completely detected when the kit is used for detecting the samples containing both the H5N1 subtype viruses and the H7N9 subtype viruses. Besides, the kit can be used for effectively detecting to-be-detected samples containing more than 10 copies.

The invention belongs to the technical field of antiviral drugs in natural active matters, and particularly relates to an application of baicalin which has the activity of inhibiting AIV (avian influenza virus) H7N9 NA (neuraminidase). The baicalin has the activity of inhibiting the AIV H7N9 NA. Researches show that the baicalin has the obvious activity of inhibiting wild type and oseltamivir-resistant AIV H7N9 NA and has the application of preparation of drugs for resisting AIVs. The AIV NA is the wild type and oseltamivir-resistant AIV A/Anhui/1/2013 (H7N9) NA recombined and expressed in CHO-K1 cells. Research results show that the baicalin has the application of preparation of the drugs for resisting the AIV H7N9.

Certain cyclic compounds are presented as well as their use for inhibiting paramyxovirus neuraminidase. The compounds are represented by the following formulas:

The invention relates to applications of N-[5-(1,2,4-triazole-1-yl)thiazole-2-yl]benzamide represented by chemical structural formula I in preparing influenza neuraminidase inhibitors. According to the chemical structural formula I, R is selected from C1-C2 alkyl, and C3-C4 linear or branched alkyl; R1 and R5 are selected from hydrogen, deuterium, methyl, ethyl, hydroxyl, methoxyl, ethyoxyl, fluorine, chlorine, bromine, nitryl, or trifluoromethyl; R2 and R4 are selected from hydrogen, deuterium, methyl, ethyl, hydroxyl, methoxyl, ethyoxyl, fluorine, chlorine, bromine, nitryl, trifluoromethyl, amino, or acetamido; and R3 is selected from hydrogen, deuterium, methyl, ethyl, hydroxyl, methoxyl, ethyoxyl, fluorine, chlorine, bromine, nitryl, trifluoromethyl, cyanogroup, amino, or acetamido.

Two universally conserved sequences from influenza type A neuraminidases were identified by large scale sequence analysis then chemically modified and conjugated to carrier proteins to generate mono-specific and monoclonal antibodies. The two antibodies, one targeting the N-terminus of the type A neuraminidase and the other sequence close to enzymatic active site, were capable of binding to all 9 subtypes of neuraminidase while demonstrating remarkable specificity against the viral neuraminidase sequences since no cross-reactivity against allantoic proteins was observed. Quantitative analyses of NA using slot blot suggest that the antibodies can be used for NA antigen quantitation in vaccines. These represent the first time the antibody-based immunoassay can be used for NA quantitative determination.

Disclosed are 4,5-diamino-3-halo-2-hydroxybenzoic acid derivatives and manufactures thereof. The 4,5-diamino-3-halo-2-hydroxybenzoic acid derivatives are presented by formula (I):

wherein R₁ group is H, CH₃, or C₂H₅; R₂ group is H, or Br; R₃ group is CH₃, or C₃H₇; and R₄ group is H, or C(═NH)—NH₂. 4,5-diamino-3-halo-2-hydroxybenzoic acid derivatives provided here were non-toxic to MDCK cells, particularly compounds 6a, 6b, 6c, 6e, 6f, 7a, 7b and 8 had better anti-H1N1 activity. In the future, these compounds can be used to focus on viral neuraminidases as targets to develop effective anti-influenza drugs.