62 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.

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 relates to novel derivatives of Andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The novel derivatives of Andrographolide have the general formula (I)The andrographolide derivatives represented by general formula (I) are useful for treating cancer, HSV, HIV, psoriasis, restonosis, atherosclerosis, other cardiovascular disorders, and can be used as antiviral, antimalarial, antibacterial, hepatoprotective, and immunomodulating agents and for treatment of other metabolic disorders.

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.

This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQR and CQS malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQR reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQR or CQS Plasmodium sp. (such as P. falciparum).

The invention relates to a compound antimalarial composition. Particularly, the invention relates to a compound antimalarial composition containing artesunate and febrifugine, particularly to a compound antimalarial ethosome composition containing artesunate ethosomes and febrifugine ethosomes, and a compound antimalarial ethosome gel cataplasm, as well as the preparation method and usage thereof. The compound antimalarial ethosome gel cataplasm is composed of a gel substrate, artesunate ethosomes, febrifugine ethosomes, a backing and an anti-sticking layer. According to the compound antimalarial composition provided by the invention, carriers of the ethosomes are used for promoting percolation properties, the release and the skin penetration of the antimalarial are improved, and the anti-malarial effect of the antimalarial is enhanced; in addition, the ethosome gel cataplasm provided by the invention is simple in preparation process, high temperature heating is not required during the preparation process, and the use of a harmful organic solvent can be avoided.

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 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 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 amberis applied in preventing and treating bacterial infection diseases except being used as antimalarial.

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.

The invention relates to an anti-malarial medicine capsule and a preparation method thereof. The anti-malarial medicine comprises the following ingredients in parts by mass: 20-30 parts of verbena, 17-25 parts of ching-chieh, 8-13 parts of the root of red-rooted salvia, 4-10 parts of curcuma zedoary, 10-15 parts of centella asiatica, 7-13 parts of radix paeoniae rubra, 8-12 parts of angelica sinensis, 3-8 parts of carthamus tinctorius, 4-9 parts of folium mori, 1-6 parts of grevllia, 25-44 parts of starch, 5.8-10 parts of sodium carboxymethyl starch and 1.2-2 parts of magnesium stearate. The anti-malarial medicine provided by the invention is capable of treating symptoms such as blood heat, vital energy deficiency, meridian symptom acerbity, stasis and impassability, numbness of limbs, skin ulcer caused by muscle heat, and body pain and fatigue, and as the medicine is prepared into capsules, the oral bioavailability can be improved.