62 results about "Dihydroarteannuin" patented technology

A composite medicine for treating the umatoid arthritis and autoimmune disease contains the sweet worm wood herb's extract (dihydroarteannuin, artesumate, artemether, etc).

The present invention discloses the new use of available antimalarial arteannuin and its derivatives dihydro arteannuin, antiannuic methyl ether, antiannuic ethyl ether and antiannuic amber. Arteannuin and its derivatives are used through combination with antibiotic medicine to inhibit bacterial growth and enhance the antibiotic effect of available antibiotic medicine. Especially, antiannuic amber is applied in preventing and treating bacterial infection diseases except being used as antimalarial.

The invention discloses dihydroarteannuin-memantine diad compounds, and a synthesis method and application thereof. The structure of the compounds is disclosed as Formula I. The synthesis method comprises the following steps: reducing arteannuin to obtain dihydroarteannuin, carrying out acetalation reaction on the dihydroarteannuin and 2-bromoethanol under the catalytic action of Lewis acid, and carrying out reaction on the acetalation reaction product and memantine hydrochloride to obtain the dihydroarteannuin-memantine diad compounds. The compounds are reported for the first time, have an therapeutic effect on neurodegenerative diseases, and can be used for preparing drugs for treating neurodegenerative diseases. Compared with other prior arts, the compounds disclosed by the invention have the advantages of simple preparation technique and better curative effect than memantine.

The invention relates to synergistic dihydroarteannuin oxyethylimidazole derivatives and application thereof. The dihydroarteannuin oxyethylimidazole derivatives have the structure disclosed as one of Formulae I-III, and can be used for preparing an antimicrobial synergist for antibiotics. The dihydroarteannuin derivatives can inhibit growth of multidrug-resistant Escherichia coli when being used independently or combined with beta-lactam antibiotics, reverse the drug resistance of the antibacterial drug to bacteria, and enhance the antimicrobial efficacy of antibiotics.

The invention relates to [(10S)-9,10-dihydroartemisinine-10-oxyl]benzaldehyde semicarbazones (sulfur) series substances and provides a structure, a preparation method and application of a novel artemisinine 10-locus derivative. The structural formula of the [(10S)-9,10-dihydroartemisinine-10-oxyl]benzaldehyde semicarbazones (sulfur) series substance is shown in a formula I. The invention also relates to pharmaceutically-acceptable slats, a solvate, an optical isomer or a polymorphic substance of the [(10S)-9,10-dihydroartemisinine-10-oxyl]benzaldehyde semicarbazones (sulfur) series substances and a medicinal composition by taking the compounds as active components. As novel antimalarial agents, anti-tumor agents and antifungal agents, the compounds can be used for treating or preventing malaria, mycotic infection, malignant tumor and the like. The compounds can be prepared by reacting dihydroartemisinine as an initial raw material with trifluoroacetic anhydride/triethylamine to obtain 10(R)-trifluoro-acetoxyl-9,10-dihydroartemisinine, directly reacting the 10(R)-trifluoro-acetoxyl-9,10-dihydroartemisinine with hydroxy benzaldehyde without separation to obtain (10S)-9,10-dihydroartemisinine-10-oxyl]benzaldehyde, and reacting the (10S)-9,10-dihydroartemisinine-10-oxyl]benzaldehyde with the substituted amino (sulfur) urea compounds in acid catalysts and alcohol solvents to obtain target compounds.

The invention provides application of dihydroartemisinin to preparation of a tumor cell autophagy induction medicament. The molecular formula of the dihydroartemisinin is C15H24O5. The medicinal preparation comprises a preparation-allowable medicinal excipient or carrier. The excipient is in the form of a solid preparation. The medicinal preparation provided by the invention can be used as a mitochondrion targeting autophagy inductor, which has a specific anti-tumor effect and can provide a therapeutic medicament for overcoming medicament resistance and improving prognosis for treatment of tumors. The effects and the mechanisms of effective monomer components in a traditional Chinese medicine are research and described under the background of a cell autophagy theory; and an important basis is provided for the development of new theory of the traditional Chinese medicine and new acting target of the medicament, and a new research direction for developing the theory of the traditional Chinese medicine is provided.

This invention comprises compositions containing dihydroartemisinin and dihydroartemisitene dimers with activity as anticancer agents and anti-protozal, including anti-malarial and anti-leishmanial properties. This invention also describes methods of preparation of these compositions and methods of use of such compositions for the treatment of cancer, and protozoal infections, including malaria, or leishmaniasis.

The compounds of this invention represent a potential new class of anti-tumor agents, one that has shown promising activity against solid tumors, and with a pattern of selectivity that suggests a possible new mechanism of action.

The present invention provides an application of dihydroartemisinin in the preparation of the drugs to enhance the anti-tumor efficacy of the chemotherapeutic drugs. The pharmaceutical preparation contains preparation allowable pharmaceutical excipients or carriers. The form of the preparation is solid preparation. The pharmaceutical preparation provided by the present invention can enhance the anti-tumor efficacy of the chemotherapeutic drugs and can be used in the adjuvant therapy during the tumor chemotherapy process. The present invention takes the theory that the angiogenesis inhibitor can change the micro-environment of tumor as the background, studies and clarifies the function and the mechanism that the effective monomer in the traditional Chinese medicine can enhance the anti-tumor efficacy of the chemotherapy drugs, provides a pharmacological basis for the development of the new usages of the artemisinin drugs and provides an important basis for the development of the new clinical values of the angiogenesis inhibitor, so the present invention is a new research direction for the development of the theory of traditional Chinese medicine.

An application of arteannuin and its derivatives (dihydroarteannuin, artemether, arteether and artesunate) in preparing the medicines for preventing and treating the sepsis caused by CpG-ODN and bacteria is disclosed.

The invention relates to a composite of an artemisinin derivative and vinorelbine in the technical field of pharmaceuticals and the application thereof; wherein, the ratio of the artemisinin derivative (including dihydroartemisinin or artesunate) and the vinorelbine is 1:500 to 500:1. The composite can be applied to preparing antineoplastics and made into the dosage forms of injection administration and oral administration by adding pharmaceutically acceptable adjuvant carriers. The two effective components (the artemisinin derivative and the vinorelbine) of the composite not only have obvious synergistic effect and but also can be cooperatively applied so as to reduce the amount of the vinorelbine and lower the production cost. By adding the pharmaceutically acceptable adjuvant carriers to prepare the dosage forms of injection administration and oral administration, the composite can be applied to the anti-tumor field.

The invention provides a tert-butoxycarbonyl dihydroartemisine, which is characterized by that said invention provides its structural formula, and it is made up by using dihydroartemisine as initiation raw material, and making it and double tertiary butyl dicarbonate implement acidation reactino in organic solvent. The invented mecicine composition for resisting parasitic disease contains tert-butoxycarbonyl dihydroartemisine with therapeutic effective dose and pharmaceutically-acceptable carrier. Said invented product is high in therapeutical effect and low in toxicity, can be used for preventing and curing the parasitic diseases of schistosomiasis and malaria, etc.

The invention discloses an application of an artemisinin-typed compound in preparation of a drug for treating and preventing hyperlipidemia. The artemisinin-typed compound is artemisinin, artesunate, dihydroartemisinin or artemether. The artemisinin-typed compound can be prepared into any pharmaceutically-acceptable preparation. The invention develops new medical applications of the artemisinin-typed compound. The application overcomes defect of a drug for treating and preventing the hyperlipidemia in the prior art. The drug can achieve a treatment effect from inflammatory resistance and blood fat reducing. Meanwhile, the artemisinin-typed compound is a drug which is firstly developed in our country, which means that our country is a main producing country, so that the artemisinin-typed compound is wide in sources and is low in price. In addition, the artemisinin-typed compound is strong in pharmacologic action, is high in safety, and provides an economical and safe drug for patients suffered from cardiovascular diseases.

The present invention discloses one kind of fatty artemisinin emulsion and its preparation and application. The fatty artemisinin emulsion includes oil for injection, smulsifier, solubilizer and isotonizer, and has artemisinin or dihydroartemisinin well dissolved in oil and coated in emulsified oil phase, so that it has high stability, strengthened medicinal effect, slow releasing and targeting administration effect, prolonged medicine residence time in blood and raised bioavailability.

The invention relates to a water-soluble arteannuin derivative and a preparation method thereof. The method comprises the following steps of: (1) preparing dihydroarteannuin; (2) preparing tetra-acetyl-mannopyranosyl bromide; and (3) preparing the water-soluble arteannuin derivative. The water-soluble arteannuin derivative is proven to have good water solubility, is easy for preparing preparations and has good pharmaceutical prospect after structural identification and water solubility analysis. The inventive preparation method has the advantages of simple operation, mild reaction conditions, and no need of deprotection step. After initial cell experiments, the water-soluble arteannuin derivative is proven to have no toxic or side effects on normal cells.

A novel one-stage process for preparing 10α-[4′-(S,S-dioxothiomorpholin-1′-yl)]-10-deoxo-10-dihydroartemisinin (1a) by reacting a compound of the formula (1b)

in which X is a halogen atom with thiomorpholine dioxide at a temperature in the range of −30° C. to +20° C. is provided.

The invention discloses an injection dihydroartemisinin emulsion, which is prepared by adjusting the pH value of the mixture consisting of the following raw materials with weight/volume percent based on the total volume of the emulsion: 0.05-0.3 percent of dihydroartemisinin, 5-30 percent of injection oil, 0.5-10 percent of emulsion, 0.1-3 percent of stabilizing agent, 0.5-5 percent of isoosmotic adjustment agent and the rest of injection water; the stabilizing agent consists of one or more of sodium taurocholate, sodium deoxycholate, oleic acid, sodium oleate and cholesterin and glycerol stearate. Freeze-dried emulsion can be made through freeze drying after adding freeze-dried protecting agent into the emulsion. The invention also discloses a method for preparing the emulsion as well as the freeze-dried emulsion. The injection dihydroartemisinin emulsion prepared by the method leads to the stable existence of dihydroartemisinin in the oil phase of the emulsion and has the advantages of good long term stability and curative effect, high bioavailability and accordance with the standards of intravenous injection; and the freeze-dried emulsion is convenient for carrying and storage and can further increase the stability of drugs.

The invention provides a method for recycling mother solution generated in the process of producing artemether. In the conventional method for recycling alpha-artemether, the integral utilization rate of unit artemisinin and the total yield of beta-artemether are low. The method comprises the following steps of: evaporating artemether mother solution generated in the process of producing the artemether to remove methanol, performing concentration pretreatment, extracting by using a solvent, converting part of alpha-artemether and dihydroartemisinin into the beta-artemether in the presence of acid serving as a catalyst, neutralizing, washing, concentrating, and recrystallizing in a methanol-water system to generate the beta-artemether with high purity. The process is simple and high in recycling value and can be used for industrial production.

The invention belongs to the field of new auxiliary materials and new dosage forms for pharmaceutical preparations and relates to design and application of a drug delivery system taking endogenous apolipoprotein E as a target spot, comprising design and synthesis of a carrier structure modifying a hydrophobic material by virtue of a polyethylene glycol (PEG) connecting arm by dihydroartemisinin (DHA). The used carrier material actively customizing apolipoprotein E takes DHA as a target head, PEG as a connecting arm and the hydrophobic material (such as PLGA) as an anchoring part. A nano delivery preparation prepared from the carrier material can encapsulate multiple anti-tumor drugs, and by virtue of interaction of the apolipoprotein combined with DHA on the surface of the nano delivery preparation and low density lipoprotein receptors (LDLr) highly expressed by tumor cells, multiple biological transmission barriers are overcome, and accumulation of nano particles at tumor parts as well as intake and anti-tumor activity in the tumor cells are effectively improved. The nano delivery preparation has good stability, high safety and excellent targeting capability, can be applied to intravenous injection and has a relatively great market application prospect.

The invention discloses dihydroartemisinin oxime-containing phenol derivatives as well as a synthesis method and application thereof, and belongs to the technical field of chemical medicines. The derivatives or racemates, stereoisomers, tautomers and pharmaceutically acceptable salts thereof have the following general formula shown in the specification. The invention also discloses the synthesis method of the derivatives, and the application of the derivatives in antituberculotic, antidiabetic, lipid-lowering and interleukin-17 inhibition drugs.

The invention discloses a dihydroartemisinin-containing carboxy phenol/ester phenol/amido phenol conjugate. The conjugate or a racemate, stereoisomer and tautomer thereof and a pharmaceutically acceptable salt of the conjugate have a structural general formula as shown in a formula I, wherein n is equal to 2 or 3, X is an alkoxyl, a hydroxyl, an amino group or -O(CH2)b-DHA, Y is -H or an alkoxyl,Z is an alkenyl and an alkyl or has no groups, b is equal to 2 or 3, and DHA represents for dihydroartemisinin. The invention further discloses a synthesis method of the dihydroartemisinin-containingcarboxy phenol/ester phenol/amido phenol conjugate and an application of the conjugate as a drug for resisting to tuberculosis and diabetes mellitus, reducing blood fat and inhibiting interleukin-17.

The invention relates to a veterinary compound diminazene aceturate and artemisinin preparation, which is a powder injection comprising the following medicinal components in percentage by mass: 10 to 85 percent of diminazene aceturate, 5 to 60 percent of artemisinin or artemisinin extract, and 2 to 30 percent of beta-cyclodextrin. The preparation is prepared by the following steps of: 1) refining the diminazene aceturate; 2) preparing a water-soluble inclusion complex of the artemisinin or the artemisinin extract; and 3) proportioning, mixing, sterilizing and filling the preparation. The veterinary compound diminazene aceturate and artemisinin preparation has the advantages that the preparation is quick in absorption and high in bioavailability in subcutaneous or intramuscular injection; by combined utilization of the artemisinin and the diminazene aceturate which serve as active Chinese medicinal ingredients, a synergistic effect of Chinese medicaments can be achieved, and the toxic or side effect of the diminazene aceturate is reduced; the artemisinin, particularly the artemisinin extract is cheaper than dihydroartemisinin, artemether and artesunate; and the preparation is suitable to be produced in injection workshops of animal pharmaceutical factories with good manufacturing practice (GMP) conditions, and does not require to update the investment.