56 results about "Antimalarial Agent" patented technology

The invention relates to novel piperazine derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, especially malaria.

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.

Biologically-active, water soluble, 3-substituted trioxanes of the formula wherein R represents a COOH- substituted aryl group, a substituted or unsubstituted heteroaryl group or an alkyl group, and C12-(p-carboxy)benzyloxy trioxanes of formula wherein R represents a substituted or unsubstituted alkyl, alkenyl, aryl or heteroaryl group and methods for their use as antiparasitic agents, particularly for the treatment of malaria.

The invention relates to a C-10 site carbamido substituted artemisinin derivative (I), and relates to a structure, a preparation method and an application of the novel artemisinin 10 site derivative. The structural formula is shown as a formula I, and relates to its pharmaceutically acceptable salt, a solvate, an optical isomer or a polymorphic substance and a pharmaceutical composition which takes the compound as an active component. Being as a new antimalarial agent, an antitumor agent and an antifungal agent, the compound can be used for treating or preventing malaria, fungal infection, malignant tumor and the like. The compound takes substituted carbamide as an initial raw material, and is obtained by reacting with dihydroartemisinin under catalysis of Et2O.BF3.

An antimalarial conjugate according to a non-limiting embodiment of the present invention may include a metallocene, a carbohydrate, and an antimalarial agent. The metallocene may include two cyclopentadienyl rings bound to a central metal atom. The carbohydrate and the antimalarial agent may be appended to at least one of the cyclopentadienyl rings of the metallocene, wherein the antimalarial agent has therapeutic properties directed to treating and / or preventing malaria. The metallocene may be ferrocene, the carbohydrate may be glucose, and the antimalarial agent may be chloroquine.

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 medicine for treating malaria and controlling malaria spreading consists of artemisinin or its derivative, or the mixture of artemisinin or its derivative and antimalarial agent with long or medium half life, or separated packed artemisinin or its derivative and antimalarial agent with long or medium half life, in 1-500 weight portions; and lower dosage of primaqine or its salt in 0.1-1 weight portions. Clinical experiment shows that the medicine has the features of high and fast curative effect, low toxicity, short treating period, convenient taking and fast killing gametophyte to block the spreading of malaria.

The present invention is to provide an antimalarial agent having excellent antimalarial activity with little side effects, in particular, having remarkable antimalarial activity against drug-resistant malaria parasites, and being capable of increasing solubility not only to organic solvent including olive oil, but also to water, and therefore, being usable not only as oral drugs but also as injectable solutions. The antimalarial agent of the present invention contains a compound represented by the following general formula (I) [wherein Z represents an unsubstituted or optionally substituted alicyclic hydrocarbon group, R0 represents a water-soluble functional group, m represents anyone of integers of from 0 to 6, n represents any one of integers of from 0 to 10.].

The invention designs an efficient synthesis method for preparing a compound shown as a general formula (I) and an application of a derivative of the compound to the research and development of an antimalarial active medicament. The method comprises the following steps of: dissolving a reactant into an appropriate solvent; and reacting under the irradiation condition of a high-voltage mercury lamp (ultraviolet lamp). In the method disclosed by the invention, a series of poly-substituted indole lactam compounds taking 3,4,5-trisubstituted indole as a basic framework are efficiently synthesized with a one-pot method under an illumination condition, so that the defects of complex steps, difficulty in operating and low total yield existing in synthesis of the type of compounds under the condition of the prior art are overcome. Derivatives containing different substituted functional groups are obtained only through a four-step reaction, and the type of compounds has potential antimalarial activity, so that necessary material bases are provided for the researches of active screening, acting mechanisms and structure-activity relationships of a large quantity of analogues, and the type of compound can possibly become a new type of antimalarial candidate medicament. The general formula (I) is shown in the specifications.

The present invention relates to a process for the isolation of artemisinin, an antimalarial agent from the herb of the Artemisia annuaplant, comprising of extracting the herb with ethanol, partitioning of thextract between water and hexane, followed by evaporative crystallization of artemisinin from hexane phase to produce substantially pure artemisinin.

Inhibitors of parasitic dihydroorotate dehydrogenase enzyme (DHOD) are candidate therapeutics for treating malaria. Illustrative of such therapeutic agents include the compound:and a triazolopyrimidine class of compounds that conform to Formula IX:and their solvates, stereoisomers, tautomers and pharmaceutically acceptable salts.

The present invention relates to a process for the isolation of artemisinin, an antimalarial agent from the herb of the Artemisia annua plant, comprising of extracting the herb with ethanol, partitioning of the extract between water and hexane, followed by evaporative crystallization of artemisinin from hexane phase to produce substantially pure artemisinin.

The invention relates to novel tetrahydroisoquinoline derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria.

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.

Disclosed herein is the process for the preparation of 1-(4-chlorophenyl)-5-isopropyl-biguanide hydrochloride (Proguanil hydrochloride), Formula-I, an antimalarial agent.

The invention relates to piperazine derivatives of Formula I and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria.

Organometallic compounds comprising a chloroquinoline moiety for use in the prophylaxis and treatment of malaria. The compounds can be manganese or rhenium complexes of a ligand comprising a chloroquinoline moiety.

The present invention provides methods of treating malaria comprising administration of an N3-substituted iminopyrimidinone of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables R1, R2, R3, R4, R5, A, B, L, m, and n are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin V activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

The invention discloses a preparation method for 1, 3-dichloro- 6- trifluoromethyl ¿C 9 - phenanthryl formaldehyde as intermediate of antimalarial agent by 1, 3-dichloro- 6- trifluoromethyl ¿C 9 ¿C phenanthryl carbinol with active manganese bioxide. This method is simple with mild reaction condition, and has high purity and yield.

The present invention relates to spiro 1,2,4-trioxanes of general formula 4. This invention more particularly relates to a process for the preparation of a series of spiro 1,2,4-trioxanes.Wherein, Ar represents aryl groups such as phenyl, 4-biphenyl, 4-chlorophenyl, 4-methoxyphenyl, 4-methylphenyl, 4-cyclohexylphenyl, 1-naphthyl, 2-naphthyl and the like and R represents hydrogen or the alkyl group such as methyl, ethyl and the like. Several of these compounds show high order of antimalarial activity against multidrug-resistant malaria in mice and thus hold promise as antimalarial agents against multidrug-resistant malaria.

Embodiments disclosed herein relate to new imidazolidinedione derivatives, methods of making these compounds, and methods of using the same to prevent, treat, or inhibit malaria in a subject.