68 results about "Antimalarial medication" patented technology

Disclosed are inhibitors of the plasmodial surface anion channel (PSAC) inhibitors and the use thereof in treating or preventing malaria in an animal such as a human, comprising administering an effective amount of an inhibitor or a combination of inhibitors. An example of such an inhibitor is a compound of formula I, Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R7 are as described herein.

The present inventors succeeded in isolating GWT1 (PfGWT1), which is one of the enzymes involved in GPI biosynthesis in the malaria parasite P. falciparum. In addition, the inventors revealed that degenerate mutant DNAs, with a lower AT content than the DNA encoding the PfGWT1 protein, can complement the phenotype of GWT1-deficient yeast. Based on the findings, the present invention provides the GWT1 protein of malaria parasites and the use of the protein in methods of screening for antimalarial drugs. The present invention also provides degenerate mutant DNAs encoding proteins involved in GPI biosynthesis, and which have a lower AT content than the original DNAs. The present invention also provides methods of screening for antimalarial drugs which use the degenerate mutant DNAs.

Disclosed are inhibitors of the plasmodial surface anion channel (PSAC) inhibitors and the use thereof in treating or preventing malaria in an animal such as a human, comprising administering an effective amount of an inhibitor or a combination of inhibitors. An example of such an inhibitor is a compound of formula I, Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R7 are as described herein.

Novel substituted 4-aminopiperidine derivatives of the formula I: wherein n, R1, Y, and are as defined in claim 1, and optically pure enantiomers, mixtures of enantiomers, racemates, diastereomers, mixtures of diastereomers, diastereomeric racemates, mixtures of diastereomeric racemates and meso-forms, as well as salts and solvent complexes of such compounds, and morphological forms, that exhibit useful parasite aspartic proteases inhibiting properties and can thus be used in the form of pharmaceutical compositions as antimalarial medicines.

The present invention provides novel processes and methodologies to minimize the bitter or otherwise unpleasant taste, to minimize the tendency to stimulate the cough reflex, or to minimize oropharyngeal deposition of medically-active compounds administered by the pulmonary / inhalation route and to deliver hydroxychloroquine (HCQ) either singularly or in combination with an antimalarial and aminoquinolone by the pulmonary / inhalation route in a sustained release or other formulation that minimizes the bitter or otherwise unpleasant taste of HCQ or any potential to stimulate the cough reflex, and to deliver a dopaminergic compound or its prodrug, including ABT-431 by the pulmonary / inhalation route in a sustained release or other formulation that minimizes the unpleasant taste of the drug or any potential to stimulate the cough reflex, and to deliver a lantibiotic, including duramycin by the pulmonary / inhalation route in a sustained release or other formulation that minimizes the unpleasant taste of the drug or any potential to stimulate throat irritation.

The invention provides pharmaceutical compositions for the treatment and prophylaxis of malaria, comprising artemether and a medium chain triglyceride formulated for transmucosal sublingual, buccal or nasal delivery, especially by a spray. Also provided are delivery devices containing the compositions.

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.].

A three-layer compound antimalarial tablet is composed of an amodiaquine hydrochloride layer, an isolating layer and an artesunate layer. Its preparing process is also disclosed.

The present invention relates to combinations between artemisinin-based potent anti-malarial agents, selected from the group consisting of ART, DHA and ARM, and a further chemotherapeutic drug selected from the group consisting of a camptothecin derivative, or a PARP-1 inhibitor, or an intercalating DNA agent, or an alkylating agent. Such combinations, showed medium to strong synergism in various models of cancer, in particular in NSCL.

The field of the invention relates to stable dosage forms comprising spiro or dispiro 1,2,4-trioxolane antimalarials, or their pharmaceutically acceptable salts, prodrugs and analogues, and processes for their preparation. The water content of the dosage form is not more than 6.5% w / w.

New 4-aminoquinoline derivatives having the general formula (I) wherein R, M, X, Y and T have the meaning described in the specification, as potent antimalarials active also on chloroquine-resistant Plasmodium falciparum malaria strains.

The present invention relates to substituted 4-qinolinemethanols and pharmaceutical compositions thereof and methods of using the same for treating of malaria, tuberculosis, and other infectious diseases.

The invention provides a composition prepared from artemisinin antimalarials and aminoquinoline antimalarials; the composition is suitable for treating the cancers, such as lung cancer, breast cancer and melanoma, has low side effect, and is effective in improving cancer treatment effect and reducing the development and progress of a patient's complications.

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 invention relates to a method for preparing 2, 4-dichlorobenzoic acid from propiconazole 4-H isomer, which comprises the steps of hydrolysis reaction, substitution reaction and the like. According to the preparation method disclosed by the invention, the propiconazole 4-H isomer can be efficiently prepared into the 2, 4-dichlorobenzoic acid. The method can effectively reduce hazardous wastes, change wastes into valuables and reduce the production cost. The 2, 4-dichlorobenzoic acid prepared by the method is an intermediate of a bactericide piperidoxime, is also an intermediate of herbicides bensulfuron and pyrazolate, can be used for production of antimalarial drug altapine hydrochloride and non-mercuric diuretic tachycardia, can also be used as an intermediate of other medicines, dyes and pesticides, and has very wide application. The method provided by the invention can also provide a solution thought for conversion of triazole isomers of other medicines (such as itraconazole and intermediates thereof) or pesticides (such as ethoconazole and penconazole) and the like.

The use of compounds of formula wherein R2, R3, R4, R5, R6 and R7 have several meanings, for the treatment of disorders mediated by protozoan organisms, novel compounds of the above formula and intermediates for the preparation of such compounds, pharmaceutical compositions comprising such novel compounds, a method of treating disorders mediated by protozoan organisms comprising administering such compounds, optionally together with a second drug substance, to a subject in need thereof and the use of such compounds, whenever comprising a photoaffinity label, for the identification of the molecular target(s) of arylamino alcohol antimalarials.

The invention relates to a type of cassane type diterpenoid lactone compounds with activity against plasmodium falciparum, which are prepared by taking seeds of a leguminous medicinal plant of caesalpinia minax hance as raw materials, using a specific solvent for extraction, carrying out a variety of chromatography and finally obtaining three cassane type diterpenoid lactone monomeric compounds, which are 5 alpha, 14 beta-dihydroxy-1 alpha, 6 alpha, 7 beta-triacetyl-13(15), 11(12)-diene-16, 12-lactone (I), 12 alpha-methoxy, 5 alpha, 14 beta-dihydroxy-1 alpha, 6 alpha, 7 beta-triacetyl-13(15)-ene-16, 12-lactone (II) and neocaesalpin L (III) respectively, wherein the compound I and the compound II are new compounds. The first research test of in vitro anti-malarial pharmacodynamics of the three compounds shows that the three compounds have obvious effect of suppressing the plasmodium falciparum and can be used for preparing drugs for treating and / or preventing malaria.

The invention relates to an antimalarial drug taking a protein degradation pathway as a target. Particularly, the invention relates to use of tripterine or derivatives of the tripterine in the preparation of drugs for treating malaria and use of the tripterine or the derivatives of the tripterine in the preparation of drugs for the inhibition of proteasome. The invention further relates to a pharmaceutical composition containing the tripterine or the derivatives of the tripterine.

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

The present invention provides hydroxylated indinavir represented by general formula (12). The present invention further provides a preparation method of hydroxylated indinavir, which employs cheap and widely available indene as the raw material, and comprises the following steps: dihydroxylate and protect the indene, oxidize the benzyl to introduce carbonyl, and then transform the carbonyl into amido, to obtain the required reaction intermediate; prepare the other molecular block from indinavir, carry out hydrolytic reaction, and protect the hydroxyl; then, carry out acidamide condensation with the reaction intermediate, remove the protection, to obtain the target product. The present invention further provides an application of hydroxylated indinavir in preparation of antimalarials, especially combination with chloroquini phosphas to treat malaria. The hydroxylated indinavir provided in the present invention has favorable in-vivo and in-vitro activity in inhibition of malarial parasite; when used in combination with chloroquini phosphas, it can works with chloroquini phosphas to inhibit malarial parasite that is resistant or sensitive to chloroquini phosphas in vitro and in vivo. The hydroxylated indinavir can be used to develop antimalarials and compound antimalarials, sets a basis for reapplying the economical and practical chloroquini phosphas in treatment of malaria, andhas excellent application prospects.

The present invention is related to a use of aminopyrazine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyrazine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.

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 quartan Plasmodium inui animal model which is characterized by infecting a healthy monkey or an immune-deficient monkey through a Plasmodium inui CCTCC No. V201021. The Plasmodium inui belongs to quartan Plasmodium inui which is named as Plasmodium inui-China Huang. The invention also discloses an establishing method of the animal model. The model can be obtained by infecting various kinds of healthy monkeys through Anopheles dirus infection route or blood infection route and can be repeatedly passaged for using for a long time. The invention provides an ideal animal model for researches on physiology, pathology, immunology, pharmacology, molecular biology, etc. of plasmodium, lays a foundation for a deep research on quartan malaria, and provides a reliable basis for designing or screening targeted anti-malarial medicines.

The invention discloses an artesunate heparin derivative as well as a pharmaceutical composition and an application thereof. The derivative is pharmaceutically acceptable salt having a high molecularcompound shown in a general formula (1) or a compound shown in the general formula (1): the formula (1) is shown in the description, in the formula (1), artesunate is bonded with heparin through esterbonds. In the artesunate heparin derivative, the content of the artesunate is 5 percent by mass to 50 percent by mass. The pharmaceutical composition of the artesunate heparin derivative comprises the artesunate heparin derivative or a mixture of the artesunate heparin derivative and a synergist. The derivative is characterized in that the artesunate is bonded with the heparin through the ester bonds, the pharmaceutical composition can be nano-particles which are self-assembled by the artesunate heparin derivative and have the particle size of 10 nanometers to 1000 nanometers, or nano-particles loaded with antimalarial medicines, and is used for preparing medicines for treating or preventing malaria caused by plasmodium.

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.