92 results about "Anti-malarials" patented technology

A chimeric, carboxy-terminal truncated hepatitis B virus nucleocapsid protein (HBc) is disclosed that contains an immunogen for inducing the production of antibodies to malarial proteins. An immunogenic malarial epitope is expressed between residues 78 and 79 of the HBc immunogenic loop sequence. The chimer preferably contains a malaria-specific T cell epitope and is preferably engineered for both enhanced stability of self-assembled particles and enhanced yield of those chimeric particles. Methods of making and using the chimers are also disclosed.

The present invention includes methods of treating or preventing malaria by administering an anti-malarial effective amount of 6-substituted uridine derivatives to a subject need thereof. The invention also includes new 6-substituted uridine derivatives for use as therapeutics, in particular to treat malaria.

The invention pertains to methods for protecting against malaria infection by vaccination. The method of the invention involves priming an anti-malaria immune response with a DNA-based vaccine and boosting that response with a protein-based a vaccine. The method of the invention also relates to broadening the resulting immune response by boosting with a protein-based vaccine.

The present invention provides tricyclic compounds, arylamide compounds, and other compounds, and compositions comprising the same, for treating malaria, and methods of treating malaria comprising administering such compounds to an animal.

A chimeric, carboxy-terminal truncated hepatitis B virus nucleocapsid protein (HBc) is disclosed that contains an immunogen for inducing the production of antibodies to malarial proteins. An immunogenic malarial epitope is expressed between residues 78 and 79 of the HBc immunogenic loop sequence. The chimer preferably contains a malaria-specific T cell epitope and is preferably engineered for both enhanced stability of self-assembled particles and enhanced yield of those chimeric particles. Methods of making and using the chimers are also disclosed.

The present application discloses the use of the anti-malarial drug lumefantrine and related compounds in the treatment of cancer.

The invention relates to a preparation method of new preparation of erythrocin, which is characterized in that an endothelin core of erythrocin is prepared, and then an isolating layer, a protective layer, a second isolating layer and an improved enteric-coating material layer are applied one by one. In this way, new preparation of the erythrocin which has certain feature of releasing (dissolving) in acid solution (hydrochloric acid solution 9 to 1000) can be formed. The technology of the new preparation can also be widely applied to drugs which, like erythrocin, when being taken orally by a patient, cause the patient to suffer the side effects of stimulation, sickness and the like after degradation in the stomach of the patient or contact with the stomach of the patient, and drugs which the patient needs to take orally to let the blood concentration to reach the peak value in a short time. Such drugs include macrolides of azithromycin, metronidazole of nitroimidazoles, tinidazole, acyclovir as an antiviral drug, ammonium chloride as a phlegm eliminating drug, bromhexine, chloroquine as an antimalarial, nitroquine, artemisinin, dihydroartemisinin, artesunate, primaquine, pyrimethamine, carbarsone and emetine amebicides and so on.

The invention discloses a method for asymmetric catalytic synthesis of a spirocyclic tetrahydrocarbazoline compound, comprising the steps: by taking 3-alkenyl indole and isatin derived ketimine as raw materials, a complex formed by chiral amine oxide and nickel trifluoromethane sulfonate as a catalyst and dichloromethane as a solvent, performing reaction on the raw materials at (-30) DEG C to (-10) DEG C at the normal pressure for 96-192h; then adding 6.0M HCl(solution) and performing reaction at 30 DEG C for 4-48h to obtain the chiral spirocyclic tetrahydro carbazoline compound, wherein the yield of the chiral spirocyclic tetrahydro carbazoline compound can reach up to 95%, and the enantioselectivity can reach up to 99%. According to the method provided by the invention, the catalytic reaction conforms with the green chemistry atom economy and has a good prospect in industrial application, thereby providing a new path for asymmetric synthesis of compounds with high anti-malarial activity (NITD609).

The invention relates to eucalyptus sesquiterpene compounds as well as a pharmaceutical composition, a preparation method and application thereof and belongs to the field of natural pharmaceutical chemistry. The pharmaceutical composition takes the compounds in formulas (1)-(IX) as an active ingredient; the preparation method of the eucalyptus sesquiterpene compounds comprises the following steps: taking roots or a rhizomes or whole plants of dobinea plants of anacardiaceae, directly performing cold immersion or thermal reflux or ultrasonic or microwave assisted extraction with organic solvent petroleum ether or chloroform or ethyl acetate or acetone or methanol or ethanol or water or then extracting with the ethyl acetate to obtain a total extract after cold immersion or thermal reflux or ultrasonic or microwave assisted extraction with the organic solvent or the water; obtaining the compounds after the total extract is subjected to repeated chromatography. The anti-malarial pharmaceutical composition takes the compounds as the active ingredient. The compounds provided by the invention are applied to the preparation of anti-malarial agents.

Novel substituted 1,2,4-trioxanes and 1,2,4-trioxepanes useful as anti-malarial and / or anticancer agents, and an improved method for their preparation, preferably involving a thiol-olefin co-oxygenation (TOCO) reaction between an allylic alcohol and a ketone.

The invention relates to a thermally-stable sweet wormwood solid dispersion composition and a preparation method thereof. The invention is characterized in that the composition contains at least one kind of an effective amount of the sweet wormwood anti-malaria medicaments, an anti-oxidant and a solid dispersion material, wherein a ratio of the sweet wormwood derivatives and the solid dispersion accessory is 1 : 0.5 to 1 : 10, the anti-oxidant is thiourea, and a metal chelating agent is randomly added. The solid dispersion composition is high in stability, and can be transported and stored at places with relatively high temperature.

The invention discloses a high-efficiency preparation method of anti-malarial medicine artemisinin. The method comprises the following steps of: preparing dihydroartemisinic acid from artemisinin under the action of reducing agent sodium borohydride / nickel chloride or hydrogen / metal catalyst; oxidizing the dihydroartemisinic acid by peroxide in the existence of the catalyst to obtain oxidized dihydroartemisinic acid; and preparing the target product artemisinin with high yield under catalysis of acid and the action of oxygen. Compared with the prior art, the method has the advantages of low price and easy availability of reagents, short synthetic route, high reaction selectivity, environmentally-friendly preparation process, simplicity in operation and post-treatment and high total yield, and is suitable for industrial production.

The present invention provides a novel combination comprising artemisinin in the form of tablets and related dosage forms for pediatric use, such as granules, suppository, suspension syrup and dry powder, for the treatment of human malarias including multiple-resistant subtertian malaria, tertian malaria and quartan malaria. Said combination is comprised of artemisinin, piperaquine and primaquine. Clinical tests in Southeast Asia countries where malaria is epidemic demonstrate that, apart from having high and rapid therapeutic effect possessed by the most excellent domestic and foreign artemisinin-type anti-malarial drugs, the present combination is also featured with shorter course of treatment, less side effect, lower material cost, and more convenience for administration, and its ability of rapidly killing gametophyte and cutting off infection source thereby blocking spreading of malaria is a further improvement.

The invention relates to a method for synthesizing chiral spiro-oxindole constructed by three-step relay catalysis. The target product chiral spiro-oxindole is synthesized by sequentially conducting a catalyst IA catalyzed nitro-reduction reaction, a catalyst IB catalyzed imine formation reaction and a catalyst IC catalyzed asymmetric catalysis reaction by using a nitro-compound as a raw material. The method adopts a reaction system of one-pot method and three-step relay catalysis which are serially connected, and starts from simple raw materials by means of simple operations, so that separation purification of intermediate can be avoided, and thus the chiral spiro-oxindole compound with high yield and high enantioselectivity is synthesized. The chiral spiro-oxindole has a structure as shown in a formula (3), and has excellent anti-malarial drug activity.

The present invention provides a novel combination comprising artemisinin in the form of tablets and related dosage forms for pediatric use, such as granules, suppository, suspension syrup and dry powder, for the treatment of human malarias including multiple-resistant subtertian malaria, tertian malaria and quartan malaria. The combination is comprised of artemisinin, piperaquine and primaquine. Clinical tests in Southeast Asia countries where malaria is epidemic demonstrate that, apart from having high and rapid therapeutic effect possessed by the most excellent domestic and foreign artemisinin-type anti-malarial drugs, the present combination is also featured with shorter course of treatment, less side effect, lower material cost, and more convenience for administration, and its ability of rapidly killing gametophyte and cutting off infection source thereby blocking spreading of malaria is a further improvement.

The invention relates to application of a dobinea plant extract to the preparation of an anti-malarial product and belongs to the pharmaceutical fields of traditional Chinese medicines and natural medicines. The medicine composition is an anti-malarial medicine with the extract as an active ingredient. The application of the dobinea plant extract, provided by the invention, has the benefits that the indication of a dobinea plant medicinal material is expanded, and the medicinal value of the dobinea plant medicinal material is improved.

A combination kit for the treatment of malaria caused by Plasmodium vivax (P. vivax) having individual doses of an anti-malarial agent, 3-[1-[[4-[(6-methoxy-8-quinolinyl)amino]pentyl]amino]ethylidene]-dihydro-2(3H)-furanone (I) in the form of capsules; individual doses of the anti-malarial agent, chloroquine in the form of tablets; and instruction material for the administration of the two anti-malarial drugs. The combination kit is particularly suited for a 6 days treatment regimen where the treatment is rendered by five tablets containing 500 mg of chloroquine phosphate (equivalent to 300 mg base), three to be taken on day one and one each on days two and three; and five capsules containing 25 mg of 3-[1-[[4-[(6-methoxy-8-quinolinyl)amino]pentyl]amino]ethylidene]-dihydro-2(3H)-furanone (I), one each to be taken on days two to six.

The present invention is directed to a method for treating inflammatory bowel disease in a patient comprising administering to said patient a pharmaceutical composition comprising a pharmaceutically effective amount of an anti-malarial compound in association with a pharmaceutically acceptable carrier and / or excipient that delays and targets the release of the anti-malarial compound in the gastrointestinal tract of the patient. It is also directed to the pharmaceutical composition comprising a pharmaceutically effective amount of the anti-malarial compound in association with a pharmaceutically acceptable carrier or excipient that delays and target the release of the anti-malarial compound in the gastrointestinal tract.

The present invention is directed to a method of protecting an animal against against malaria caused by Plasmodium which undergoes more than one stage in its life cycle or undergoes more than one infectious cycle, the method comprising: a) administering to the animal a live vaccine containing sufficient Plasmodium sporozites that are low in pathogenicity and sensitive to one or more anti-malarial drugs to develop an immunological response in the animal; b) maintaining the animal free from anti-malarial drugs effective against Plasmodium for a period of time corresponding to about one life cycle or infectious cycle of the Plasmodium; and c) thereafter administering to the animal a anti-malarial drugs effective against Plasmodium for a period of time corresponding to at least one life cycle or infectious cycle of the Plasmodium.

The invention discloses a preparation method of a graphene-based adsorption material. The preparation method comprises the steps: first adopting artemisinin medicine as a reducing agent and a protective agent of nano silver to reduce the nano silver, then soaking a single layer of graphene oxide powder in a nano silver aqueous solution, ultrasonically drying, placing under ultraviolet rays to perform irradiation, and repeating the process of extraction, ultrasonic drying and ultraviolet reduction for 3 to 5 times to finally obtain the graphen-based adsorption material. The preparation method adopts artemisinin medicine as the reducing agent and protective agent of the nano silver and has the characteristics of simple process, wide source of raw materials, moderate reaction, environmental friendliness and the like; and the prepared nano silver simultaneously has double effects of antibiosis and anti-malarial. The method adopting ultraviolet to reduce the graphene is environmentally-friendly, high efficient and cheap, so that the use of a toxic reducing agent such as hydrazine or sodium borohydride is avoided. The process of soaking, ultrasonic drying and ultraviolet reduction is repeated for 3 to 5 times, so that the nano silver is uniformly distributed and stably attached on the graphene and is unlikely to fall off. The prepared graphene-based adsorption material has a promising application prospect in the fields of sewage treatment and air purification.

The invention discloses a chalcone derivative (E)-1-(7-hydroxyl-2-methyl-2-(4-methylpentan-1-ol-3-alkene-1-base)-2H-benzopyran-8-base)-3-(6-picoline-3-base) acrylic-2-alkene-1-ketone with anti-malariaactivity and a process for synthesizing the chalcone derivative. The chalcone derivative (E)-1-(7-hydroxyl-2-methyl-2-(4-methylpentan-1-ol-3-alkene-1-base)-2H-benzopyran-8-base)-3-(6-picoline-3-base)acrylic-2-alkene-1-ketone and the process have the advantages that the chalcone derivative is excellent in anti-malaria activity; the chalcone derivative which is a compound can be prepared by the aid of the process which is easy to operate and short in production cycle on a large scale.

The invention provides anazepineindole alkaloid and a preparation method and an anti-malarial application thereof.The preparation method utilizes tryptamine and split ring strychnine as initial raw materials to obtain two diastereoisomers after being catalyzed and chemically modified by strictosidinesynthetase and phosphoric acid.According to the method, two diastereoisomers of the azepineindole alkaloid are synthesized through a simple enzymatic chemical reaction and a purification method, a research shows that compounds and pharmaceutical salts thereof have outstanding anti-malarial activityand can be applied to the preparation of anti-malarial drugs.The structural formula of the two compounds is shown in the description.

The invention provides an application of anthocyanin in preparation of a medicine for treating malaria. The anthocyanin has a structural formula shown in the description. The invention also provides a medicinal composition containing the anthocyanin, a salt compound thereof and a pharmaceutically acceptable carrier. The weight percentage of the active ingredient namely the anthocyanin in the medicinal composition is 5-95%. By virtue of in vitro anti-malarial activity determination, a result shows that the anthocyanin and the salt compound thereof have good in vitro anti-malarial protozoan activity. Therefore, the anthocyanin can be used for preparing the medicine for treating malaria, and has a great clinical application value.

The invention belongs to the technical field of natural medicine chemistry, relates to the technical field of extraction and separation of natural plant active components and particularly relates to apreparation method and application of vernonia amygdalina saponin. Vernonia amygdalina is also named as bitter leaf or South Africa leaf and has the effects of expelling parasite, resisting malaria and promoting excretion. The research shows the saponin separated from vernonia amygdalina has the functions of resisting malaria, relieving pain and relieving fever and is regarded as a main active component of vernonia amygdalina. The invention discloses an industrial extraction and separation process of vernonia amygdalina total saponin; through adoption of the process, the yield of the vernoniaamygdalina total saponin is about 4.2%; the content is greater than 90%.

The invention discloses a benflumetol fat emulsion injection preparation which contains 0.03 to 35 wt% of benflumetol, 10.0 to 30.0 wt% of oil for injection, 0.6 to 30.0 wt% of an emulsifier, 0 to 10 wt% of a solubilizer, 0 to 5 wt% of a co-emulsifier, 2.25 to 7 wt% of an isotonic agent and 0.002 to 0.075 wt% of an anti-oxidant, with the balance being injection water. The invention also discloses a preparation method and pharmacodynamic and safety evaluation for the benflumetol fat emulsion injection preparation. The benflumetol fat emulsion provided by the invention has the characteristics of good biocompatibility, high physical stability, convenient preparation, good security, high drug loading capacity and the like, has a particle size of less than 200 mu m and is suitable for injection, e.g, intravenous injection and intramuscular injection. According to the invention, the characteristic that a soybean oil fat emulsion inhibits growth of plasmodium falciparum is utilized to enhance anti-malarial effects of drugs, to improve bioavailability of the drugs and to reduce toxic and side effects of the drugs; nutrients needed by the body of a patient with malaria can be provided, the activity of lymphocytes of the patient is improved, which assists the patient in resisting malaria and recovering.

A non-naturally occurring variant of a C-terminal fragment of a Plasmodium merozoite surface protein-1 (MSP-1) wherein said variant has (i) a reduced affinity, compared with a naturally occurring Plasmodium MSP-119, for at least one first antibody capable of blocking the binding of a second antibody, which second antibody inhibits the proteolytic cleavage of Plasmodium MSP-142 and (ii) substantially the same affinity for at least one third antibody compared with said naturally occurring Plasmodium MSP-119. which third antibody inhibits the proteolytic cleavage of Plasmodium MSP-142 is provided for use in an anti-malarial vaccine.

The invention relates to orixine hydrochloride as well as a preparation method and medical application thereof. In particular, through pumping hydrochloric acid gas into an ethanol solution of radix dichroa total alkaloids, the orixine hydrochloride of which the stability and water solubility are both increased in comparison with orixine is obtained, the anti-malarial activity of the orixine hydrochloride is enhanced and the orixine hydrochloride can be used as novel anti-malarial drugs.

The present invention relates to methods of combating malaria infection by vaccination. The methods of the present invention involve the use of a DNA-based vaccine to elicit an anti-malarial immune response and the use of a protein-based vaccine to boost that response. The methods of the invention also involve broadening the resulting immune response by boosting with a protein-based vaccine.

The present invention is concerned with the development of novel 8-aminoquinoline analogs in the treatment and prevention of malaria and the said compound has broad spectrum of activity against the blood as well as tissue stages of the human malaria parasites makes these compounds very attractive in the cure and prevention of malaria caused by drug-sensitive and multidrug resistant strains and also it is expected that development of these compounds as ideal antimalarial agents may lead to suppression as well as radical cure of the malaria infection with single drug therapy.

The invention relates to a pyrimidone derivative and application thereof. The pyrimidone derivative is a compound shown as a formula I or pharmaceutically-acceptable salt thereof. An activity inhibition experiment discovers that the pyrimidone derivative provided by the invention has a significant activity inhibition effect on dihydroorotate dehydrogenase of plasmodium falciparum. The invention lays a foundation for the preparation of a novel anti-malarial drug. In the formula I, R1 is a straight chain and a branched chain of C1-C6 or cyclic alkyl or amino; and A is a 5 to 6-membered saturatedor unsaturated carbocyclic group.