35 results about "Pyrimethamine" patented technology

The invention relates to a medicinal composition and injecta for curing avian toxoplasmosis, and a preparation method thereof. The medicinal composition comprises the following components in percentage by weight: 18 to 36 percent of sulfamonomethoxine, 16 to 65 percent of sulfamethoxazole, 7 to 18 percent of trimethoprim, 4 to 14 percent of pyrimethamine and 6 to 16 percent of nonsteroidal anti-inflammatory medicament. The injecta comprises the following components in percentage by weight: 5 to 10 percent of sulfamonomethoxine, 4 to 20 percent of sulfamethoxazole, 2 to 5 percent of trimethoprim, 1 to 3 percent of pyrimethamine, 1.5 to 4 percent of nonsteroidal anti-inflammatory medicament, 5 to 10 percent of polyethyleneglycol-400, 10 to 30 percent of propylene glycol, 30 to 60 percent of alpha-pyrrolidone, 0.1 to 0.2 percent of antioxidant, 0.01 to 0.02 percent of metal complexing agent and the balance of water for injection. Sulfamonomethoxine, sulfamethoxazole, trimethoprim and pyrimethamine are jointly applied and a long-acting preparation is prepared by adopting composite solvent, so that the medicinal composition and the injecta can prevent the secondary infection of other pathogen at the same time of destroying and expelling toxoplasma so as to relieve different symptoms and complicating diseases caused by the toxoplasma.

The invention relates to a controllable genome-modified plasmodium, a recombinant expression vector and the construction method and application of the controllable genome-modified plasmodium and the recombinant expression vector. The recombinant expression vector comprises a gene targeting long homologous arm, a gene targeting short homologous arm, a tetracycline repression protein gene expression cassette, a pyrimethamine resistance gene expression cassette and a target gene expression cassette, wherein the tetracycline repression protein gene expression cassette, the pyrimethamine resistance gene expression cassette and the target gene expression cassette are located between the gene targeting long homologous arm and the gene targeting short homologous arm, and tetracycline operator gene sequences are inserted in multiple transcriptional start sites of a target gene promoter, so that the recombinant expression vector can be used for conditional research of the functions of a certain functional gene in a plasmodium genome. Furthermore, a functional gene expression sequence, corresponding to a target gene, in the plasmodium genome is knocked out by means of the gene knockout technique; meanwhile, the recombinant expression vector is transfected into a plasmodium with genes knocked out, so that the controllable genome-modified plasmodium is obtained; a new technical scheme is provided for further research of the functions of all functional genes in the plasmodium genome, and application prospects are broad.

The present invention relates to a combination of a signal transducer and activator of transcription 3 (STAT3) activity inhibitor; and an immune checkpoint inhibitor for use in treating or preventing the hyperproliferative disorder in a subject. Preferably, the STA3 activity inhibitor is pyrimethamine or atovaquone, and the immune checkpoint inhibitor is an anti-PD1 antibody. Preferably, the hyperproliferative disorder is a glioma or a glioblastoma.

The present invention relates to a method for preparation of synergistic combination kits of α,β-arteether, sulfadoxin and pyrimethamine for the treatment of severe / multi-drug resistant cerebral malaria.

Compounds of the formula (I) wherein R1 represents a hydrogen atom or a 3-halogen atom, and R2 represents a straight-chain alkyl group containing up to 6 carbon atoms, a straight-chain alkyl group containing up to 3 carbon atoms with unsubstituted or substituted aromatic ring, or alkoxycarbonyl substituent at the end position, or aryloxyalkoxyalkyl group have been found to possess antimalarial activity against Plasmodium falciparum lines, including those resistant against pyrimethamine and other antifolates. The compounds themselves, methods of making these compounds, and methods of using these compounds are all disclosed.

The invention discloses an orally disintegrating tablet for preventing and treating and a preparation process thereof, and belongs to the field of veterinary drug preparations. The orally disintegrating tablet comprises the following components in parts by weight: 0.01-0.2 parts of pyrimethamine, 0.1-0.2 parts of sulfamethoxazole, 0.03-0.04 parts of trimethoprim, 20-30 parts of disintegrating agent, 15-40 parts of filler, 1-2 parts of lubricant, 1-5 parts of flow aid, 2-5 parts of adhesive, 1-2 parts of surfactant, and 1-2 parts of flavoring agent. According to the orally disintegrating tablet, pyrimethamine, sulfamethoxazole and trimethoprim are combined to prepare the orally disintegrating tablet, the principle of drug combination is accorded, the drug synergism can be improved, and the administration times can be reduced. The preparation is an orally disintegrating tablet, has the characteristics of simple production, accurate dosage and high bioavailability, has a key point that the administration means of medicine is changed, and can be used for solving the problem that a pet cat cannot be easily subjected to injection administration and oral tablet administration. The orally disintegrating tablet can be taken without water, does not need swallow, can be disintegrated in the oral cavity when encountering saliva, and can be absorbed by virtue of oral mucosa.

A method of treating a lysosomal storage disease comprises administering a pyrimethamine derivative to a subject in need thereof.

The invention discloses an anti-toxoplasma composition drug and a screening method thereof, and belongs to the field of medicine. According to the anti-toxoplasma composition drug and the screening method thereof, mouse test toxoplasmosis animal models are established, the ten drugs of a sulfadiazine sodium injection, a compound sulfamethoxazole, a lincomycin hydrochloride injection, a sulfamonomethoxine sodium injection, a florfenicol injection, acetylspiramycin, pyrimethamine, roxithromycin, artemisinin and radix sophorae flavescentis are selected out, two compositions which have the best anti-toxoplasma effect are screened out, one composition comprises the sulfamonomethoxine, the pyrimethamine and TMP, and the other composition comprises the compound sulfamethoxazole and the acetylspiramycin; animal models in mice and pigs are established, it is verified that the two compositions are both effective on the treatment of artificially infected toxplasmosis in pigs, and the treatment effect on the pigs is in accordance with that of the mouse models. By means of the anti-toxoplasma composition drug and the screening method thereof, it is proved that the the feasible method is achieved by utilizing the mouse test toxoplasmosis models to evaluate the efficacy of drugs on treating toxplasmosis in pigs, and meanwhile two anti-toxoplasma drug compositions with good effects are provided.

The invention discloses a method for comprehensive prevention and treatment of raspberry palmate wilt, which comprises the following steps: (1) before planting, the seedlings of raspberry palmate are treated with diluted prochloraz or diluted pyrimethanil medicament Soak; (2) eradicate the palm leaf raspberry infected with Fusarium wilt, and alternately use diluted prochloraz and diluted pyrimethanil for other palm leaf raspberries within 5 meters from the palm leaf raspberry infected with Fusarium wilt (3) Before and after the rainy season, use diluted prochloraz and diluted pyrimethanil medicaments to treat palm leaves and raspberry palms every 3 to 8 days. Leaves of raspberry are carried out alternate root irrigation. The comprehensive prevention and control method can well suppress the large-scale outbreak of Fusarium wilt in palmate raspberry orchards, and control the incidence rate below 5%.

The present invention relates to a combination of a signal transducer and activator of transcription 3 (STAT3) activity inhibitor; and an immune checkpoint inhibitor for use in treating or preventing the hyperproliferative disorder in a subject. Preferably, the STA3 activity inhibitor is pyrimethamine or atovaquone, and the immune checkpoint inhibitor is an anti-PD1 antibody. Preferably, the hyperproliferative disorder is a glioma or a glioblastoma.

The invention discloses a method for separation and detection of pyrimethamine, which comprises the following steps: (1) adding acetonitrile to the sample, shaking and mixing, centrifuging, taking the supernatant and drying it with nitrogen, and redissolving the residue with a solvent as The solution to be tested; (2) adding the magnetic molecularly imprinted polymer to the test solution, shaking for 20-120 minutes, magnetically separating the magnetically imprinted polymer; (3) eluting the magnetically imprinted polymer with a certain volume of elution solvent pyrimethamine in the eluate, and collect the eluate; (4) measure the concentration of pyrimethamine in the eluate with HPLC / UV; The functional monomer is prepared. The magnetic molecularly imprinted polymer used in the present invention uses multiple hydrogen bond interactions between template molecules and functional monomers to form an intermolecular interaction matrix, strengthen the interaction between template molecules and functional monomers, and improve the affinity for pyrimethamine and selective.

The invention relates to a controllable genome-modified plasmodium, a recombinant expression vector and the construction method and application of the controllable genome-modified plasmodium and the recombinant expression vector. The recombinant expression vector comprises a gene targeting long homologous arm, a gene targeting short homologous arm, a tetracycline repression protein gene expression cassette, a pyrimethamine resistance gene expression cassette and a target gene expression cassette, wherein the tetracycline repression protein gene expression cassette, the pyrimethamine resistance gene expression cassette and the target gene expression cassette are located between the gene targeting long homologous arm and the gene targeting short homologous arm, and tetracycline operator gene sequences are inserted in multiple transcriptional start sites of a target gene promoter, so that the recombinant expression vector can be used for conditional research of the functions of a certain functional gene in a plasmodium genome. Furthermore, a functional gene expression sequence, corresponding to a target gene, in the plasmodium genome is knocked out by means of the gene knockout technique; meanwhile, the recombinant expression vector is transfected into a plasmodium with genes knocked out, so that the controllable genome-modified plasmodium is obtained; a new technical scheme is provided for further research of the functions of all functional genes in the plasmodium genome, and application prospects are broad.

The invention belongs to the technical field of preparation of functional materials, and discloses a preparation method and application of a pyrimethamine molecularly imprinted composite membrane based on double-sided loading of click chemistry; the preparation steps are as follows: dopamine is used as a bionic modification material, and carbon nanotubes are used as a membrane Loading material, pyrimethamine as template molecule, methacrylic acid as functional monomer, tetrakis(3-mercaptopropionate) pentaerythritol ester as cross-linking agent, dipentaerythritol pentyl- / hexyl-acrylic acid as auxiliary cross-linking agent, combined with double-sided Suction filtration loading means, based on the "click chemistry" polymerization method, prepares a double-sided loaded pyrimethamine molecularly imprinted composite membrane; the double-sided loaded pyrimethamine molecularly imprinted composite membrane prepared by the present invention effectively solves the problem of existing pyrimethamine molecularly imprinted composite membranes. Molecularly imprinted polymers have the disadvantages of difficult recovery and secondary pollution; in addition, they have good specific recognition and adsorption and separation capabilities for pyrimethamine.

The present invention relates to 2,4-diamino-6-ethylpyrimidine derivatives that are inhibitors of wild type and quadruple mutant dihydrofolate reductase (DHFR) of Plasmodium falciparum. They also show in vitro antimalarial activities against Plasmodium falciparum for both wild type and mutant that are comparable to or better than pyrimethamine. In addition, the compounds of the present invention show a good selectivity to Plasmodium falciparum and exhibit lower cytotoxicity than pyrimethamine.

The invention discloses a separation detection method for pyrimethamine. The separation detection method for pyrimethamine comprises the following steps that firstly, a sample is treated, and a solution to be detected is obtained; secondly, a pyrimethamine molecularly-imprinted polymer is added into the solution to be detected and is separated through centrifuging; thirdly, pyrimethamine is eluted with a certain volume of an eluting solvent, and eluant is collected; fourthly, the concentration of pyrimethamine in the eluant is measured with HPLC / UV, pyrimethamine serves as a template of the pyrimethamine molecularly-imprinted polymer, functional monomers silicon dioxide microspheres with grafted double bonds, a sulphydryl cross-linking agent and the like are added, and pyrimethamine is obtained through a sulphydryl-alkenyl click reaction. According to the pyrimethamine molecularly-imprinted polymer, the sulphydryl cross-linking agent is used in the preparing process, the sulphydryl-alkenyl click chemistry is used in combination with the molecular imprinting technology, the reaction conditions are mild, and the adsorption capacity and the selective performance to pyrimethamine are improved by optimizing the reaction conditions of synthesizing the molecularly-imprinted polymer through the sulphydryl-alkenyl click reaction.

The invention discloses a method for treating toxoplasmosis by using an isoflavanoid compound glabridin. The method comprises the following specific steps: step 1, preparing a medicine by using the isoflavanoid compound glabridin; and step 2, resisting invasion of toxoplasma gondii by the prepared medicine. The isoflavanoid compound glabridin has remarkable activity on toxoplasma gondii, can remarkably inhibit invasion and proliferation of the toxoplasma gondii and can be used for treating toxoplasmosis, and the anti-proliferation and anti-invasion effects of the glabridin are even superior to those of an existing clinically used medicine pyrimethamine; and the medicine prepared from the isoflavanoid compound glabridin is effective to acute toxoplasmosis.