379 results about "Anti hbv" patented technology

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 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 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 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.

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 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.

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 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.