379 results about "Anti hbv" patented technology

The invention relates to an enantiomorphic amine alkyl sesquiterpene alcohol and glucoside and the medicated salt or solvent thereof, as well as the effect and activity of the composed medicine combination, mainly relating to the medical use in reducing HBV-DNA replication activity. And it has considerably strong inhibiting effect on HBsAG screted by HepG2.2.15 and HBV-DNA replication as compared with positive contrast Lamivudine; and it has obvious inhibition activity to HBV-DNA replication at large dosage (100 mug / mL) and medium dosage(20 mug / mL) as contrasted with Lamivudine, and can be expected to apply to preparing medicines for curing HB virus infection disease.

The invention involves A 1- beta-keto-5, 11(13)-diene eudesmane-12-acidum who has the structure as formula (1) shows and its medical salt, or solvate and its drug combinations and its medical usage in reducing hepatitis B surface antgien and inhibiting replication activity of aethyl- hepatovirus HBV-DNA medicinal. The invention compounds has strong inhibitory action in hepatitis B surface antgien (HBsAg) externalized by HepG2.2.15 cells and replication of aethyl- hepatovirus deoxyribonucleotide (HBV-DNA) in vitro, its inhibiting ability against HBsAg surpasses that of positive control Lamivudine in the same dose; it has obvious inhibiting ability against replication of aethyl- hepatovirus HBV-DNA under the concentration of 100 mu g / mL,20 mug / mL and 4 mug / mL DNA, it belongs to anti- aethyl- hepatovirus natural products of superactive non-nucleoside, can be expected for producing drugs for treating aethyl- hepatovirus infected disease.

The invention relates to a hemiterpene derivant 2-Hydroxyilicic acid, as formula (1) 2beta-hydroxy-5alphaH-eudesmane-11(13)-allyl-12-acid and relative compounds which can be used to prepare the drug treating hepatitis B disease. The inventive compound can restrain the copy of hepatitis B surface antigen (HBsAg) and the hepatitis B deoxyribonucleic acid (HBV-DNA), while its HBsAg restrain ability is higher than positive contrast difuradin; in the density as 100mug / ml, 20mug / ml, and 4mug / ml, it can restrain the copy of hepatitis B virus HBV-DNA.

The present invention relates to an eudesmane type sesquiterpene derivative 1 beta-hydroxyilicic acid, namely 1 beta-hydroxy-5 alpha H-eudesmane-11 (13)-ethylene-12-acid, its medicineal salt or solvent compound and its medicine composition and medicinal application for preparing medicine capable of curing hepatitis B virus infective disease and resisting hepatitis B virus. Said invention also provides its chemical structure formula.

The invention relates to a sesterterpane as formula (1) and relative medical drug or solvent, and relative drug compound, which can reduce hepatitis B surface antigen and restrain hepatitis B HBVDNA copy activity. Wherein, said invention has strong restrain on hepatitis B surface antigen (HBsAg) generated by HepG2.2.15 cell and the copy of hepatitis B deoxyribonucleic acid (HBV-DNA), while it restrain ability is higher than positive contrast difuradin; and the copy restrain activity at large amount (100 mug / mL) and middle amount (20 mug / mL) on the hepatitis B HBV-DNA are both higher then difuradin.

The invention discloses a eudesmane typed sesquiterpene acid compound named 5alphaH-eudesmane-11 (13)-alkylene-12 acid, which is characterized by the following: inhibiting the replication of HBsAg and HBV-DNA; fitting for preparing prevention drug of virus B hepatitis; reducing the application in the hepatitis B surface antigen drug.

The invention provides therapeutic or diagnostic antibodies with modified N— or C-terminal sequences that are enriched with lysine or tyrosine residues. These lysine or tyfosine residues can be used to couple radioisotopes, cytotoxic agents, or detectable labels. The increased stoichiometric ratios of these agents in the antibody conjugates lead to improved therapeutic efficacy or enhanced detection sensitivity. Non-limiting examples of antibodies suitable for the present invention include anti-CD22, anti-ErbB2, anti-VEGF, anti-EGFR, anti-VEGFR, anti-Her-3, anti-Her-4, anti-CEA, anti-CTLA-4, anti-CD4, anti-CD3, anti-CD20, anti-TNF-a, anti-CD11a, anti-Lewis Y antigen, anti-TrailR, anti-IL2R, anti-CD30, anti-CD146, anti-CD147, anti-alpha V integrin beta, anti-CD19, anti-GD2, anti-3H11, anti-EBV, anti-HIV, anti-HBV, anti-HCV, and other disease-specific antibodies.

This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-β-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2′-deoxy-β-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.

The invention relates to application of ring A dioxane flavonolignan in preparing medicaments for resisting hepatitis B viruses (HBV), in particular to application of ring A dioxane coupling type flavone lignan or a pharmaceutically acceptable salt thereof in preparing medicaments for clearing away hepatitis B e antigen (HBeAg), suppressing the HBV DNA replication and treating HBV infection diseases. The flavonolignan has certain activity on resisting the HBeAg, and the intensity of the flavonolignan for clearing away the HBeAg is higher than that of Lamivudine which is a positive control and close to that of 10,000 units / milliliter of alpha-interferon. Meanwhile, the suppression ratio of the compound to the HBV DNA replication is higher than 80 percent in the presence of a concentration of 100 micrograms / milliliter. The pharmacodynamical results indicate that the flavonolignan or the pharmaceutically acceptable salt thereof can be expected to be used for preparing the medicaments for clearing away the HBeAg, suppressing the HBV DNA replication and treating the HBV infection diseases.

The invention relates to an anti-hepatitis B virus tertiary amine oxide and preparation method and uses for manufacturing drugs, wherein the tertiary amine oxidate has a structure represented by general formula (I) and (II), its preparing process comprises the compound having general formula (I) is prepared through condensation of derivatives of amine with acidamide and further oxidation, the compound having general formula (II) is prepared through the condensation between mono-hydrocarbyl piperazidine with carboxylic acid or carboxylic acid derivatives, or through alkylation of piperazine amidos and further oxidization. The compound can be used for preparing medicament for preventing or treating hepatitis B virus related diseases.

The present invention discloses non-enantioselective preparation process of emtricitabine. The preparation process includes condensation of glyoxalic acid as the initial material and 2, 5-dihydroxy-1, 4-dithiane under the asymmetric induction of optically active alcohol ester to obtain trans-5-hydroxy-1, 3-oxythiacyclopentane-2-carboxylate; halogenating and coupling with silylated 5-flucytosine, and reducing to obtain initial product; reaction with salicylic acid to form salt, purification and separation to obtain optically pure emtricitabine. The present invention has mild reaction condition, simple operation, low cost, less environmental pollution and high product purity reaching medicinal standard, and is suitable for industrial production. The product is used in treating hepatitis B and AIDS.

The invention discloses a new use of phenanthridine biologic alcali of general formula I containing coumarone and its derivant in preparing anti-hepatitis b virus medicament.The biologic alcali has tumor cell apoptosis inducing effect, has strong inhibiting activity against to such pathogen, has antiviral effect, and is expected for treating liver cancer, wherein R1 to R10, R12 and R13 is hydrogen, hydroxy, carbon chain or naphthenic base with 1-12 carbon atoms, alkoxyl or acyloxy group, benzyloxy, chlorine and other halogen atoms, amino group, methylol, aldehyde group, carbonyl, acetonyl, carboxy, sulacyloxy, 4-methyl-benzenesulfonyloxyl, arylsulfonyloxy, diphenylphosphonoxyl and -OCONH2; R11 is hydrogen, methyl or oxygen atom; R14 and R15 are respectively hydrogen or methyl.

The invention relates to the field of chemical and biological sciences, in particular to LQC-X structural formula I, and synthesis and application of intermediate of LQC-X, wherein a maximum dosage of LQC-X6 given to an mouse is 2000 mg / kg once in one day; the mouse is continuously observed for 7 days; no toxic reaction appears, and the medicine is proven to have quite high safety; and it is proved through pharmacodynamics experiments that LQC-X compounds have obvious anti-hepatitis B virus action and liver protecting and transaminase lowering action. The compounds can be used for preparing medicines for preventing and treating diseases of hepatitis B, chronic liver cirrhosis and the like. The structural formula I of LQC-X is shown in the description.

The invention relates to a novel method for preparing tenofovir, in particular to a method for preparing a tenofovir compound, in particular the monohydrate of the tenofovir for resisting hepatitis B viruses and human immunodeficiency viruses. The method comprises the following steps of: using (substituted) triphenylchloromethane XIII to protect hydroxy in the end position of (R)-1,2-propanediol,condensing the obtained product with dialkyl sulfonyloxy methyl phosphonate V to obtain XV, hydrolyzing the XV in the aqueous solution of an organic acid to remove the protective group of the hydroxyl at the end position of XV to obtain an intermediate XI, condensing sulfonate XII of the intermediate XI with adenine to obtain an intermediate VII, transforming the intermediate VII into the corresponding trimethylsilyl phosphonate VIII by trimethylsilyl bromide (TMSBr), and hydrolyzing the VIII to obtain the target product. The method has the advantages of short process route, convenient operation, low cost and easy access of raw materials and favorability for large scale production.

The invention discloses the medical application of a 15-methylene replaced andrographolide derivant as shown in general formula 1, more particularly relates to the application thereof in preparing anti-hepatitis B virus drugs, pertaining to the pharmaceutical chemistry field. HepG2.2.15 cells are used for detecting the secretory volumes of HBsAg and HBeAg and the HBV DNA level related to viral particles in the supernatant liquid of a nutrient solution, and the result shows that the 15-methylene replaced andrographolide derivant has good in-vitro anti-HBV effect. The 15-methylene replaced andrographolide derivant has better development and application prospect by being applied in preparing drugs used for treating and preventing Hepatitis B.

The invention provides a synthetic method of anti-hepatitis B virus medicine Adefovir dipivoxil, including the steps: (1) preparing chloroethyl chloromethylether; (2) preparing chloroethyl methylether; (3) preparing 2-[bis(trifluoroethyl)-phosphoryl methoxyl] ethyl chloride; (4) preparing 9-[bis(trifluoroethoxyl)-phosphoryl methoxyl ethyl]-adenine; (5) preparing PMEA; (6) preparing 9-[bis[(isopentanoyl)methoxyl]phosphinyl]-methoxyl]adenine; it has the characters of process easy to apply, environmental protection and higher yield.

This invention provides substituted benzimidazole compounds shown in common formula (I) and their pharmacologically permitted salts. The definitions of R1, R2, R3, R4 and n in common formula (I) are mentioned in the instruction. Pharmacological experiments show that, this kind of compounds and their pharmacologically permitted salts or their solvates or hydrates perform excellent anti-hepatitis B virus (anti-HBV) activities and are especially inhibitory to DNA replication of HBV. They are thus promising as anti-HBV drugs. This invention also provides a method to prepare this kind of compounds.

The invention relates to an anti-hepatitis B virus composition taken from fresh dandelion and an application of the anti-hepatitis B virus composition in preparation of an anti-hepatitis B virus drug and belongs to the field of traditional Chinese medicines. The anti-hepatitis B virus composition provided by the invention comprises a fresh dandelion polysaccharide component, a phenolic acid component and a flavone component and is characterized in that the weight ratio of the fresh dandelion polysaccharide component to the phenolic acid component to the flavone component is (2-40): (3-70): (2-50). According to an optimized scheme, the phenolic acid component takes caffeic acid, chlorogenic acid and isochlorogenic acid A as typical ingredients; the flavone component takes galuteolin, quercetin and luteolin as typical ingredients; and the weight ratio of the caffeic acid to the chlorogenic acid to the isochlorogenic acid A to the galuteolin to the quercetin to the luteolin is (0.25-10): (2-40): (0.25-20): (0.5-20): (0-10): (1.5-20). According to the invention, the fresh dandelion is taken as raw material, effective ingredients are separated, purified and enriched by macroporous resin, the effective ingredients are mixed to obtain the fresh dandelion anti-hepatitis B virus composition, a process is simple and convenient, related diseases caused by hepatitis B viruses can be effectively treated, cost is low, and mass production can be achieved.

This invention discloses a method for preparing entecavir acid-addition salts, entecavir magnesium salt and entecavir barium salt. The entecavir acid-addition salts are prepared from entecavir and inorganic or organic acids, and are preferential entecavir hydrochloride, entecavir bromate, entecavir sulfate, entecavir phosphate, entecavir sulfonate, and entecavir benzenesulfonate. The entecavir slats are stable, and have higher water solubility than entecavir itself, thus are more suitable to manufacture anti-HBV drugs.

The invention relates to a series of novel compounds and a preparation method thereof, particularly to a series of benzoxazolone derivatives and a preparation method thereof, and solves the problem that the prior benzoxazolone compounds have no 4-substituted derivatives and have anti-HBV activity and anti-HIV activity. The general structural formula of the derivatives is shown in the figure, wherein R is C3-C6 fatty acid ester group, benzoate group / substituted benzoate group, benzene sulfonate group / substituted benzene sulfonate group, amino acid ester group, or heterocyclic acid ester group / substituted heterocyclic acid ester group. The invention obtains a series of 4-substituted benzoxazolone derivatives with proven anti-HBV activity and anti-HIV activity, opens new preparation paths of the above three drugs, and brings new breakthrough in pharmaceutical and pesticide fields. In addition, the synthetic method has the advantages of easy operation, mild reaction conditions, single reaction product, and applicability to large scale production.

The invention relates to a novel anti-hepatitis B virus drug represented in a formula I, and a nontoxic pharmaceutically acceptable salt and a hydrate thereof: (img file= 'DSA00000804267600011.TIF' wi= '739' he= '766' / ), wherein R1 is alkyl or naphthenic base, of which the carbon number is 1-6, and R2 is H or alkyl of which the carbon number is 1-6.

An application of 6-methoxy dideoxyguanosine in preparing the medicine to prevent and treat hepatitis B and liver cancers. It has high resistance to hepatitis B virus and its mutation strain.

The invention relates to a sulphoxide and sulphone containing novel thiazolyldihydropyrimidine applicable to acting against hepatitis B virus (HBV) infection and a composition of the same and other antiviral agents.

The invention provides a prodrug of a hepatitis b virus resistant drug with a liver targeting action and a preparation method for the same. The prodrug is a prodrug of Adefovir or Tenofovir. Higher fatty acid, glyceride, cholic acid compounds or the base groups of derivatives thereof with the liver targeting action are connected with Adefovir or Tenofovir to prepare the prodrug. After being taken into a human body, the prodrug is concentrated in the liver and then is decomposed, thereby having the effects of reducing the dosage, improving the curative effect, reducing the drug concentration in a kidney and reducing the toxic and side effect. The invention also provides a method for synthesizing the prodrug.

The invention relates to wormwood leaf volatile oil which is prepared by adopting a method comprising the steps of: carrying out steam distillation on wormwood leaves subjected to soaking with water, and collecting distillate; and after standing and cooling and demixing the distillate, taking an oil layer at the upper layer of the distillate to obtain the wormwood leaf volatile oil. The wormwood leaf volatile oil is simple in an extraction method; and proved by in vitro cell tests, the wormwood leaf volatile oil has strong anti-hepatitis B virus activity, and can be used for preparing the anti-hepatitis B virus medicines.

The invention relates to the technical field of gene engineering, in particular to an immune enhanced gene vaccine of a hepatitis B virus core antigen (HBcAg). The vaccine is an immune stimulating complex (ISCOM) vaccine consisting of HBcAg and OX40 ligand (OX40L) dual-gene co-expression recombinant eukaryotic vector, saponin Quil A, cholesterol and lecithin. The vaccine can promote immune response of specific T cells of the HBcAg and efficiently induce the anti-virus replication capacity of immune cells, and has good application prospect in the field of hepatitis B virus infection resistance. The invention also relates to a preparation method for the vaccine with simple and convenient operation and low cost.

The invention relates to application of stephanine and hydrochloride thereof in the field of medicine, namely the stephanine or cepharanthine hydrochlofide is taken as an effective ingredient to prepare an anti-hepatitis B virus drug. The research shows that: the median toxic concentration (TC50) of the CH to cells is 2.09mu g.ml; and the CH can inhibit the synthesis of HBV DNA in the cells (P is less than 0.01) and is dose-dependent, the inhibition ratio of the CH to the HBV DNA in supernatant fluids of the cells is more than 50 percent when the dose is more than 0.5mu g.mL, IC50 of the CH is 0.324mu g.mL, the therapeutic index TI is equal to 6.45 (the TI is more than 2.0 and less than 10.0), and the CH has stronger effect of inhibiting the synthesis of the HBV DNA and is an effective low-toxicity drug. The invention develops novel pharmaceutical application of the stephanine and the hydrochloride of the stephanine, has the advantages of rich source of preparation raw materials, low cost, small toxic side effect, and simple preparation technology, can be prepared into oral dosage forms, injection dosage forms, tablets and the like, and has convenient use.

The invention discloses a siRNA interference-based anti-HBV gene-based drug mediated by complex carriers. Based on the characteristic of HBV and expression products thereof, active epitope protein in HBsAg expressed by HBV is biologically linked with cationic liposome and specially binds with hepatic cell surface receptors with the help of the epitope protein in the HBsAg to induce RNAi to enter hepatic cells; meanwhile, the meltability of bilayers of the cationic liposome and the cytolipin is used for increasing the efficiency of an siRNA expressed carrier entering into the hepatic cells. The drug of the invention can improve the effectiveness of the siRNA, biological stability in the human body, safety and effective targeting delivery and can be used in the clinical treatment.

The present invention pertains to the pharmaceutical field and relates to an antiviral compound drug, in particular to an entecavir drug composition and the anti-HBV usage. The present invention is composed of entecavir, (1s-(1 Alpha, 3 Alpha, 4 Beta))-2-amino-1, 9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purine-6-ketone, monocase compound which is extracted from one or more traditional Chinese medicines and the pharmaceutical excipients. The results of the in vitro and the duck hepatitis B animal model tests show that the present invention has obvious anti-HBV efficacy; at the same time, the present invention also has good hepatoprotective effect. The entecavir drug composition becomes the more safe and effective drug for treating hepatitis B and thus having very broad application prospect and far-reaching social benefits.