 Patent Application Title |
Patent App Num. |
Date |
| Anti-cytomegalovirus activity of artemisinin-derived dimers | 20130109654 | 20130502 |
 Artemisinin-derived monomers and artemisinin dimers are shown to exhibit in-vitro anti-cytomegalovirus (CMV) activity. Artemisinin dimers effectively inhibited CMV replication in human foreskin fibroblasts and human embryonic lung fibroblasts with no cytotoxicity at concentrations required for complete CMV inhibition. Artemisinin dimers were found to be potent and non-cytotoxic inhibitors of CMV replication, which indicates their use as therapeutic agents for the treatment of CMV infection in humans.
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| Artemisinin with berberine compositions and methods of making | 20130102625 | 20130425 |
 An all-natural herbal composition and methods of preparing the same are provided. The novel Artemisinin Combination Therapy (ACT) consists of artemisinin and its derivatives and berberine, the two active substances mixed with various selected excipient compounds to form a single pill, tablet or capsule for treatment and prevention of malaria, dengue fever, yellow fever, dysentery, Lyme disease, babesiosis, progressive multifocal leukoencephalopathy, Helicobacter Pylori, and colitis, in adults and children. A tablet or pill for children is formulated to be chewable.
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| Combinations of berberine, artemisinin, loperamide and their derivatives to treat malaria, diarrhea, travelers' diarrhea, dysentery, dengue fever, parasites, cholera and viruses | 20130071474 | 20130321 |
 This invention relates to compositions and methods of combining berberine, artemisinin and loperamide or their derivatives in a therapeutic product for mammals suffering from malaria, diarrhea, travelers' diarrhea, dysentery, dengue fever, parasites, cholera and viruses by administration of a therapeutically effective amount of the composition.
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| Combinations of berberine, artemisinin, loperamide and their derivatives to treat malaria, diarrhea, travelers' diarrhea, dysentery, dengue fever, parasites, cholera and viruses | 20130072513 | 20130321 |
 This invention relates to compositions and methods of combining berberine, artemisinin and loperamide or their derivatives in a therapeutic product for mammals suffering from malaria, diarrhea, travelers' diarrhea, dysentery, dengue fever, parasites, cholera and viruses by administration of a therapeutically effective amount of the composition.
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| Combined use of ribonuclease and artemisinin | 20130052181 | 20130228 |
 The invention discloses a kit which comprises a formulation containing artemisinin or the derivatives thereof, a formulation containing ribonuclease, and a specification.
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| New series of artemisinin derivatives and process for preparation thereof | 20130030044 | 20130131 |
| This invention relates to the synthesis of certain novel Baylis-Hillman adducts of artremisinin derived aldehyde 2[10′β-deoxoartemisininyl]-ethanal. The capabilities of introduction of three functional groups into a molecule in one step using Baylis-Hillman reaction encouraged us to synthesize some highly functionalized derivatives of artemisinin. These highly functionalized artemisinin derivatives embodied in this document are found to be active against various cancer cell-lines
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| Association between ferroquine and an artemisinine derivative for treating malaria | 20120258945 | 20121011 |
| This invention is directed to methods for the treatment and prevention of malaria comprising administering a combination of ferroquine, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and an artemisinin derivative, and to pharmaceutical compositions comprising such combination.
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| Artemisinin derivatives with natural amino acids, peptides, and amino sugars for skin imperfections and infection in mammals | 20120189567 | 20120726 |
| The present invention discloses certain derivatives of artemisinin and the active principles contained in Artemisia annua extracts with amino acids, peptides, and amino sugars and salts thereof (formula I). The compounds of the present invention possess wide-spectrum antibacterial and antifungal biological activity suitable for topical or oral application for the treatment of infections and topical ailments in mammals, including acne, rosacea, topical wounds, infections, dandruff, skin disfigurements caused by infection, skin discoloration, age spots, wrinkles, excess facial oil, and veterinary problems including canine infections;
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| Compositions comprising thalidomide and artemisinin for the treatment of cancer | 20120190646 | 20120726 |
| The present invention relates to pharmaceutical compositions for the treatment of cancer and especially for the treatment of hematological malignancies such as multiple myeloma. Specifically, the present invention relates to pharmaceutical composition for the treatment of cancer comprising: thalidomide, or a derivative thereof, or salts or solvates thereof; one or more artemisinin compounds, or salts or solvates thereof; and one or more pharmaceutically acceptable carriers and/or excipients.
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| Combination therapy and uses thereof for treatment and prevention of parasitic infection and disease | 20120101151 | 20120426 |
| The invention relates to compounds, methods, uses, compositions, combinations, kits and packages for the prevention and/or treatment of parasite infection (e.g., Plasmodium parasites) and/or disease (e.g., malaria) based on uses of (a) cystamine, cysteamine, and analogs, derivatives, prodrugs, precursors thereof; an agent capable of inducing their production; and/or salts thereof, and (b) artemisinin and functional derivative, analog, conjugate, metabolite, prodrug or precursor thereof, and/or salts thereof.
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| Use of artemisinin derivatives for the treatment of asthma and chronic obstructive pulmonary disease (copd) | 20120015922 | 20120119 |
| Artesunate is a derivative of artemisinin isolated from a Chinese herb Artemisia annua L. It is used clinically for the treatment of malaria. We investigated potential anti-inflammatory actions of artemisinin derivatives. artemisinin derivatives significantly inhibited OVA-induced signs, symptoms and parameter of airway disorders Taken together, our results clearly demonstrate anti-inflammatory effects of artemisinin derivatives. Artemisinin derivatives can be used to complement or to replace oral steroids during asthma exacerbation treatment. Further artemisinin derivatives can be used as an anti-inflammatory agent for controlling airway disorders.
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| Use of artemisinin for treating tumors induced by oncogenic viruses and for treating viral infections | 20120010278 | 20120112 |
| In certain aspects, the invention relates to methods of treating proliferative cervical disorders (such as cervical cancer and cervical dysplasia) and treating virus infection by administering artemisinin-related compounds. In certain aspects, the invention relates to methods of treating a tumor induced by an oncogenic virus, methods of killing or inhibiting a squamous cell carcinoma, and methods of inhibiting the replication of a virus, by administering artemisinin-related compounds.
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| Pharmaceutical composition for treating malaria | 20110008410 | 20110113 |
| The invention relates to a pharmaceutical composition in the form of rectal capsules, comprising a combination, effective against malaria parasites, of artemisinine or a derivative of artemisinine, particularly artesunate, with piperaquine or a pharmaceutically acceptable salt thereof, particularly piperaquine tetraphosphate, and having high activity against Plasmodium such as, for example, Plasmodium falciparum.
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| Process for manufacturing artemisinin | 20100331553 | 20101230 |
| Disclosed is a process for manufacturing crude Artemisinin comprising the extraction of Artemisia annua from plant material with carbon dioxide or water in a critical physical state such that after extraction, the solvent evaporates completely from the resulting extract.
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| Nucleotide sequence encoding artemisinic aldehyde double bond reductase, artemisinic aldehyde double bond reductase and uses thereof | 20100299778 | 20101125 |
| An isolated nucleic acid molecule cloned from Artemisia annua encodes an artemisinic aldehyde double bond reductase. Artemisinic aldehyde double bond reductase enzymatically reduces artemisinic aldehyde to (11R)-dihydroartemisinic aldehyde. The nucleic acid molecule, and the enzyme encoded thereby, may be used in processes to produce dihydroartemsinic aldehyde and/or dihydroartemisinic acid in a host cell. Dihydroartemisinic acid is a late precursor to the antimalarial compound artemisinin.
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| Colorimetric test for antimalarial artemesin derivatives | 20100297775 | 20101125 |
| A process for testing a composition as containing an artemisinin derivative is provided that includes contacting the composition with a reagent made up of a hydrogen bonding polar organic solvent and an acid having a pK value of less than 3.8 at 25° Celsius and capable of acid catalyzing a decomposition reaction of the artemisinin derivative so as to provide a reaction mixture. The reaction mixture is allowed sufficient time at a reaction temperature for the artemisinin derivative to decompose to yield a colored decomposition product discerned by a normal unaided human eye. A kit for testing a composition for an artemisinin derivative according to the process is provided together with instructions for contacting the solvent and the acid with the composition to decompose the artemisinin... |
| Increasing the in vivo biological activity of biologically active compounds | 20100286393 | 20101111 |
| covalently linked at the 1 or the 2 position to a compound with a biological activity thereby increasing the biological activity of said compound or a pharmaceutically acceptable salt thereof.
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| Use of artemisinin and its derivatives in cancer therapy | 20100279976 | 20101104 |
| A method for treating cancer in a mammal includes administering to the mammal in need thereof a therapeutically effective amount of artemisinin (ART) or its derivative, such as dihydroartemisinin (DHA), artemether (ARM), or artesunate (ARS) alone or in combination with a chemotherapeutic agent, such as gemcitabine and carboplatin. A method for inhibiting tumor cell proliferation includes contacting a tumor cell with ART or its derivative, such as DHA, ARM, and ARS, in an amount effective to inhibit tumor cell proliferation or in combination with a chemotherapeutic agent, such as gemcitabine and carboplatin.
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| Dimeric derivatives of artemisinin and application in anticancer therapy | 20100266570 | 20101021 |
| The present invention relates to dimeric derivatives of 10-trifluoromethylated artemisinin of formula (I): or a pharmaceutically acceptable salt thereof with B1 and B2 selected from C═O, CHOH and CH2, as well as to their use in treating cancer and to their preparation method.
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| Artemisinin derivatives for the treatment of melanoma | 20100216869 | 20100826 |
| wherein A and B are as defined in the specification. Compounds (I) have proved able to inhibit cell proliferation, in particular of uveal melanoma cells, and can therefore be used, either alone or in association with other antitumoral drugs, for the preparation of medicaments intended for the treatment of malignant melanoma.
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| Artemisinin derivatives | 20100093651 | 20100415 |
| This disclosure provides improved derivatives of artemisinin; pharamaceutical compositions containing these compounds; methods for preparing these compounds and compositions; methods of using these compounds and compositions for preventing, controlling or treating infectious diseases including but not limited to parasitic infectious diseases such as T. gondii infection, trypanosome parasite infection, plasmodia parasite infection, and cryptosporidium parasite infection; methods for preventing, controlling or treating toxoplasma infection; and methods for treating psychiatric disorders associated with toxoplasma infection including but not limited to schizophrenia using the disclosed compounds and compositions alone or in combination with one or more antipsychotic drugs.
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| Composition for skin whitening comprising artemisinine | 20100061948 | 20100311 |
| The present invention relates to a skin-whitening composition comprising artemisinine. Artemsinine according to the present invention suppresses melanin synthesis and tyrosinase activity to inhibit pigmentation, and has excellent whitening effect and safety without side effects, thereby being used for improving melasma or freckles, and whitening skin.
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| Anti-parasitic compositions | 20100015233 | 20100121 |
| The present invention relates to nanodisperse antiparasitics and provides a composition comprising at least one water insoluble anti-parasitic drug and a water-soluble carrier material, wherein the water-insoluble anti-parasitic drug (preferably an Artemisinin-type drug or a quinine type drug) is dispersed through the carrier material in nano-disperse form having a peak diameter of the nano-disperse form below 1000 nm. The invention further provides an aqueous dispersion of a water insoluble anti-parasitic drug and a water-soluble carrier material, wherein the anti-parasitic drug is in nano-disperse form having a peak diameter of the nano-disperse form below 1000 nm, the invention further subsists in a process for preparing an anti-parasitic composition comprising a water insoluble anti-parasitic agent and a water-soluble carrier, which comprises the steps of either: a) providing an... |
| Artemisinins in the clinical and veterinary management of kinetoplastid infections | 20090317499 | 20091224 |
| The invention relates to the treatment of kintoplastid infections by administering a pharmaceutical composition containing an extract from the plant Artemisia annua. The invention also relates to isolated, semi-synthetic and synthetic artemisinins that show improved efficacy in treating kinetoplastid infections. This invention also relates to a method of treating kintoplastid infections with artelinic acid and artemisinins and where Artelinic acid is administered orally.
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| Antimalarial therapy using a combination of synthetic artemisinin derivative and bisquinoline derivative | 20090306091 | 20091210 |
| The technical field of the present invention relates to antimalarial therapy using a synthetic artemisinin derivative and bisquinoline derivative.
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| Water-soluble artemisinin derivatives, their preparation methods, the pharmaceutical compositions and the use thereof | 20090298881 | 20091203 |
| Water-soluble artemisinin derivatives, their preparation methods, the pharmaceutical compositions containing the same derivatives and the use thereof are disclosed. The artemisinin derivatives have following formula I. It has been proved by pharmacological tests that these compounds and compositions have evident immuno-suppressive activities, and may be used in the preparation of novel immuno-suppressants for treating the diseases caused by hyperfunction of human immunity (e.g. the auto-immune diseases such as lupus erythematosus, rheumatoid arthritis, multiple sclerosis and the like), and for inhibiting the graft rejection after cell or organ transplantation.
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| Nucleotide sequences encoding enzymes in biosynthesis of dihydroartemisinic acid | 20090265804 | 20091022 |
| Isolated nucleic acid molecules cloned from Artemisia annua encode artemisinic aldehyde double bond reductase and artemisinic/dihydroartemisinic aldehyde dehydrogenase. Artemisinic aldehyde double bond reductase enzymatically reduces artemisinic aldehyde to dihydroartemisinic aldehyde. Artemisinic/dihydroartemisinic aldehyde dehydrogenase enzymatically oxidizes dihydroartemisinic aldehyde to dihydroartemisinic acid and artemisinic aldehyde to artemisinic acid. The nucleic acid molecules, and the enzymes encoded thereby, may be used in processes to produce dihydroartemsinic aldehyde, dihydroartemisinic acid or artemisinic acid in a host cell. Dihydroartemisinic acid is a late precursor to the a antimalarial compound artemisinin.
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| Dimers of artemisinin derivatives, preparation thereof and therapeutic use thereof | 20090082426 | 20090326 |
| The present invention relates to dimers of artemisinin derivatives, to processes for the preparation of such dimers, to methods of treatment comprising administration of such dimers, and to intermediates to such dimers.
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| Suppression and prevention of tumors | 20090042845 | 20090212 |
| Combinations of betaine and vitamin C are used to suppress or prevent malignant tumors, e.g., by combining the two ingredients in a product consumed by a human, dog, or cat, such as an aqueous liquid such as grape juice, the ingredients being provided in containers with instructions for use, or in finished products, especially with support of tests demonstrating the effectiveness of the treatment for, e.g., preventing tumors in populations known to be at risk of developing tumors, or, treating existing cancers in combination with other cancer drugs such as anastrozole and/or fulvestrant and/or artemisinin either concurrently or sequentially to prevent the cancer from growing when the cancer drug is not being used, the combination of betaine and Vitamin C optionally being supplemented or replaced by... |
| derivatives of artemisinin, and their uses in the treatment of malaria | 20080287433 | 20081120 |
| R4 is H or OH. The invention also relates to the process by which they are obtained, and their uses in pharmaceutical compositions intended for the treatment of malaria.
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| Anticancer and antiprotozoal dihydroartemisinene and dihydroartemisitene dimers with desirable chemical functionalities | 20080275106 | 20081106 |
| This invention comprises compositions containing dihydroartemisinin- and dihydroartemisitene-dimers with activity as anticancer or anticancer metastasis 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 or prevention of cancer metastasis, and protozoal infections, including malaria, or leishmaniasis. The compounds of this invention represent a potential new class of anti-tumor or anti-metastasis agents, one that has shown promising activity against solid tumors.
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| Treatment and prevention of benign pigmented moles (naevi) using artemisinine and the derivatives thereof | 20080255223 | 20081016 |
| A method of treating a benign pigmented mole or a dermatomycosis. The method comprises locally applying to a subject in need thereof artemisinine and/or one or more structurally related compounds. Also disclosed is a plaster which comprises a topical formulation comprising artemisinine and/or one or more structurally related compounds.
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| Artemisinic epoxide and methods for producing same | 20080187983 | 20080807 |
| The present invention provides artemisinic epoxide, and methods of synthesizing artemisinic epoxide in a genetically modified host cell. The present invention further provides methods for producing artemisinin. The present invention further provides variant enzymes that catalyze the oxidation of amorpha-4,11-diene to artemisinic epoxide; nucleic acids encoding the variant enzymes; as well as recombinant vectors and host cells comprising the nucleic acids.
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| Artemisinins in the clinical and veterinary management of kinetoplastid infections | 20080152729 | 20080626 |
| The invention relates to the treatment of kintoplastid infections by administering a pharmaceutical composition containing an extract from the plant Artemisia annua. The invention also relates to isolated, semi-synthetic and synthetic artemisinins that show improved efficacy in treating kinetoplastid infections. This invention also relates to a method of treating kintoplastid infections with artelinic acid and artemisinins and where Artelinic acid is administered orally.
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| Artemisinin (qinghaosu) derivatives, their preparation methods and their use, and pharmaceutical compositions containing the same | 20080139642 | 20080612 |
| The invention provides a type of artemisinin derivatives having following structure I, its preparation method and use, as well as a pharmaceutical composition containing such artemisinin derivatives and its use. The artemisinin derivatives of the present invention and their pharmaceutical composition containing the artemisinin derivatives. have immunosuppressive activities and can be used more safely. The composition which comprises the artemisinin derivatives can be formulated into long-term dosage forms such as tablet, pellet and the like, and have wider productive and use value.
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| Dispiro 1,2,4-trioxolane antimalarials | 20080125411 | 20080529 |
| A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the invention unexpectedly provide a single-dose cure for malaria, as well as prophylactic activity against the same. The compounds are also active against schistosomiasis and cancer.
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| Spiro and dispiro 1,2,4-trioxolane antimalarials | 20080125441 | 20080529 |
| A means and method for treating malaria, schistosomiasis, and cancer using a Spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably substituted at the 4-position. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.
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| Methods of using artemisinin-like compounds to prevent or delay the appearance of cancer | 20080119542 | 20080522 |
| The invention provides methods for preventing or delaying the development of cancer by administering free radical-generating agents to a subject. Representative free radical-generating agents include endoperoxide compounds, such as endoperoxides bearing sesquiterpene compounds such as artemisinin and its analogs, arteflene and its analogs, 1,2,4-trioxanes and 1,2,4,5-tetraoxanes. Intracellular iron concentrations may be enhanced by the administration of iron salts or complexes.
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| Conjugates of artemisinin-related endoperoxides and hydrazone derivatives for the treatment of cancer | 20080103192 | 20080501 |
| Compounds having an artemisinin-related endoperoxide moiety covalently coupled to a hydrazone moiety through a linker. Compositions and methods for treating cancer using the compounds.
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| Skin condition improvement including acne, rosacea, and topical wounds by artemisia annua extract via iron siderophore trojan horse delivery system | 20070269537 | 20071122 |
| This invention relates to certain extracts of Artemisia annua plant, both in their crude and refined forms, and certain refined forms of Artemisia annua plant extracts composed substantially of Artemisinin and its analogs, which are chemically classified as sesquiterpenes with an endo-peroxide group [FIG. 1]. These are suitable for compositions comprising topical application, and for the treatment or improvement of skin condition including acne, rosacea, topical wounds, age spots, wrinkles, excess facial oil, and darkened skin.
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| Process for one pot conversion of artemisinin into artelinic acid | 20070270598 | 20071122 |
| The present invention relates to an improved process for one pot conversion of artemisinin into artelinic acid, which reduces the three step (three pot) conversion of artemisinin to artelinic acid in one step (one pot). The process of preparation of artelinic acid involves stirring of artemisinin with sodium borohydride, catalyst, polyhydroxy compound or chlorotrimethylsilane or amberlyst-15 resin and methyl p-(hydroxymethyl) benzoate, filtration of undissolved, unwanted reaction products and finally stirring of the filtrate with alcoholic or aqueous alkali hydroxide.
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| Antiparasitic artemisinin derivatives (endoperoxides) | 20070191354 | 20070816 |
| This invention relates to the use of certain C-10 substituted derivatives of artemisinin of general formula (I) in the treatment and/or prophylaxis of diseases caused by infection with a parasite, certain novel C-10 substitued derivatives of artemisinin, processes for their preparation and pharmaceutical compositions containing such C-10 substituted derivatives. The compounds are particularly effective in the treatment of malaria, neosporosis and coccidiosis.
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| Use of artemisinin for treating tumors induced by oncogenic viruses and for treating viral infections | 20070142459 | 20070621 |
| In certain aspects, the invention relates to methods of treating proliferative cervical disorders (such as cervical cancer and cervical dysplasia) and treating virus infections by administering artemisinin-related compounds. In certain aspects, the invention relates to methods of treating a tumor induced by an oncogenic virus, methods of killing or inhibiting a squamous cell carcinoma, and methods of inhibiting the replication of a virus, by administering artemisinin-related compounds.
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| Antimalarial drug containing synergistic combination of curcumin and artemisinin | 20070105945 | 20070510 |
| A pharmaceutical composition for the treatment of malaria in mammals is disclosed. The composition comprises of a synergistic combination of curcumin and artemisinin.
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| High artemisinin yielding plant genotype 'cim-arogya' | 20070089211 | 20070419 |
| The present invention is related to the development of a novel, distinct high herb and artemisinin yielding genotype of Artemisia annua obtained through systematic marker assisted breeding followed by selection of uniform population in a methodical way wherein the genotype is distinct, uniform and stably maintainable by continuous rouging of off types in the population using DNA marker at early seedling stage from nursery itself and suitable for commercial cultivation.
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| Transgenic amorpha-4, 11-diene synthesis | 20070031947 | 20070208 |
| The present invention relates to an isolated DNA sequence encoding a polypeptide having the biological activity of amorpha-4,11-diene synthase. This DNA sequence can be used for the transformation of bacteria, yeasts and plants for the production of amorpha-4,11-diene, a specific precursor in the synthesis of artemisinin, in the respective organisms. The invention also relates to these organisms.
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| Antiparasitic artemisinin derivatives (endoperoxides) | 20070021409 | 20070125 |
| This invention relates to the use of certain C-10 substituted derivatives of artemisinin of general formula (I) in the treatment and/or prophylaxis of diseases caused by infection with a parasite, certain novel C-10 substitued derivatives of artemisinin, processes for their preparation and pharmaceutical compositions containing such C-10 substituted derivatives. The compounds are particularly effective in the treatment of malaria, neosporosis and coccidiosis.
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| Antiparasitic artemisinin derivatives (endoperoxides) | 20060287305 | 20061221 |
| This invention relates to the use of certain C-10 substituted derivatives of artemisinin of general formula (I) in the treatment and/or prophylaxis of diseases caused by infection with a parasite, certain novel C-10 substitued derivatives of artemisinin, processes for their preparation and pharmaceutical compositions containing such C-10 substituted derivatives. The compounds are particularly effective in the treatment of malaria, neosporosis and coccidiosis.
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| Compound artemisinin | 20060281785 | 20061214 |
| 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... |
| Conversion of amorpha-4,11-diene to artemisinin and artemisinin precursors | 20060270863 | 20061130 |
| The present invention relates to methods for the conversion of amorpha-4,11-diene to artemisinin and various artemisinin precursors.
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| Herbal remedy for treating lyme disease | 20060233895 | 20061019 |
| The present invention is directed to a composition for the treatment of Lyme disease, comprising: Uncaria tomentosa (Cat's Claw); Pau d'arco; Scutellaria baicalensis (Baikal Scullcap); Artemisinin; and Sambucus nigra (Elderberry).
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| Artemisinins with improved stability and bioavailability for therapeutic drug development and application | 20060229279 | 20061012 |
| A stable form of artemisinin wherein an artelinic acid or artesunic acid is complexed with cyclodextrin analogs, preferably, β-cyclodextrin. The complexed cyclodextrin artemisinin formulation shields the peroxide portion of the artemisinin backbone from hydrolytic decomposition rendering it stable in solution. Artelinic acid and cyclodextrin are placed into contact with one another to yield a 2:1 molecular species. Artesunic acid and cyclodextrin yield a 1:1 molecular species. The complexed cyclodextrin artemisinin formulation is effective for the treatment of malaria and is stable in solution for long periods of time.
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| Orally active, antimalarial, anticancer, artemisinin-derived trioxane dimers with high selectively, stability and efficacy and methods of making the same | 20060142377 | 20060629 |
| In only two steps and in 65% overall yield, natural trioxane artemisinin (I) was converted on gram scale into C-10-carba trioxane dimer (3). This new, very stable dimer was then transformed easily in one additional step into four different dimers (4-7). Alcohol and diol dimers (4 and 5) and ketone dimer (7) are 10 times more antimalarially potent in vitro than artemisinin (1), and alcohol and diol dimers (4 and 5) are strongly inhibitory but not cytotoxic toward several human cancer cell lines. Water-soluble carboxylic acid derivatives (8a-10c and 12) were easily prepared from dimers (4-6); they are thermally stable even at 60° C. for 24 hours, are more orally efficacious as antimalarials than either artelinic acid or sodium artesunate, and have potent and selective anticancer... |
| Deoxoartemisinin analogs, process for their preparation, and anticancer agent comprising them | 20060074251 | 20060406 |
| The present invention relates to a new deoxoartemisinin dimer and trimer, which have excellent anticancer activity and lower toxicity and are stable to acids, to a new deoxoartemisinin monomer of intermediate thereof, to preparations thereof, and to anticancer agents comprising the deoxoartemisinin dimer or trimer.
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