55 results about "Antimalarial medication" patented technology

The invention belongs to the technical field of biomedicine, and particularly relates to application of GABA (gamma-aminobutyric acid) driven by lactobacillus rhamnosus to treatment of cerebral malaria of mice. According to the invention, the obviously enriched lactobacillus muricatum is found, and the lactobacillus muricatum is proved to be capable of generating GABA (gamma-aminobutyric acid). Afterwards, on the mouse cerebral malaria model, under the condition that the lactobacillus rhamnosus and the GABA are independently used or auxiliary dihydroartemisinin is used, the effect of the lactobacillus rhamnosus and the GABA on improving and treating the mouse cerebral malaria is evaluated. Results show that the strain and the metabolite GABA thereof can effectively improve behavioristics of mice and immune pathological injuries of all organs, reduce protozoemia and prolong the lifetime of the mice whether the strain is independently used or combined with dihydroartemisinin, and can effectively treat cerebral malaria of the mice compared with the strain which is independently used with drugs. The invention provides a brand-new solution for treating severe malaria, especially human brain malaria, caused by malignant malaria from the perspective that the probiotics drive metabolites of the probiotics to assist the anti-malarial drug in treating rat brain malaria.

Methods of treating malaria comprising administration of compounds of Formula (I′) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. It also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin X, plasmepsin IX or plasmepsin X and IX 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.

Provided are methods of treating malaria comprising administration of compounds of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. Also provided are uses of the compounds of Formula (I), as defined herein, 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 present invention provides methods of treating malaria comprising administration of compounds of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for the possible inhibition of plasmepsin X, plasmepsin IX or plasmepsin X and IX 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 relates to application of a mir-331-3p inhibitor in preparation of a medicine for inhibiting malaria mosquito transmission, and belongs to the technical field of biological medicine. Aiming at the technical problems that the existing anti-malarial drug mainly acts on the later stage of plasmodium development and is lack of an effective propagation blocker, the invention provides the miR-331-3p inhibitor which is used for blocking the formation of plasmodium oocysts by inhibiting the interaction between microRNA and a mosquito target gene spetzle. Experiments show that the inhibitor can reduce the mosquito infection rate by about 50%, and has the characteristics of high targeting property, simplicity in operation and the like. The invention provides a novel drug development target for blocking malaria transmission, can effectively supplement the prevention and control blind area of the existing anti-malarial drug, and has important application value in the field of mosquito-borne infectious disease control.

The present disclosure generally relates to substituted heteroaromatic compounds. The invention relates to novel substituted 4-heteroatom-isoquinolone compounds, and isomers, derivatives, analogues and / or salt forms thereof of formula I; and its process of preparation thereof. Furtherore, the present invention relates to a process of preparation of various drugs / APIs / alkaloids e.g. Ampikin APIs such as CX-614, CX-554, DRF-2655, ITF-296, ITF-1129, Raititrexed, Deoxyvasicinone family of quinazolinone alkaloids, etc. using said formula I compound as starting material. The compound of formula I acts as antimalarial agent, anticancer agent, neuroprotective agent and so on. Formula I

Compound for use in a method of treating a coronavirus infection, wherein the compound comprises Artemether, Atazanavir, Efavirenz, Fosamprenavir or Saquinavir, and wherein the method includes administering to a subject in need of the treatment an effective amount of the compound; wherein the term “compound” is inclusive of pharmaceutically acceptable salts of the compound; and wherein the coronavirus infection is an infection by a human coronavirus (e.g. SARS-CoV-2). Also claimed for use are the same compounds for use in a method of treating a coronavirus infection, or for use in a prophylaxis method to prevent Covid-19 infection. Further claimed, is compounds for use in a method of treating a coronavirus infection, wherein the compounds comprise: (A) Atazanavir, Efavirenz, Fosamprenavir, Saquinavir or Remdesivir (GS-5734); and (B) an antimalarial drug, an anti-hypertensive drug, an immunomodulatory drug, a neuroprotective drug, or an anti-inflammatory drug, each of which is as defined herein; wherein the method includes administering to a subject in need of the treatment or prophylaxis an effective amount of the compounds.

To provide a new antimalarial agent that achieves a balance between strong antimalarial activity and low cytotoxicity.SOLUTION: An antimalarial agent comprising an ethanol extract and / or a methanol extract of at least one plant selected from the group consisting of Ficus hispida, Streblus asper, Boerhavia repens, Clerodendrum viscosum, Amaranthus spinosus, and Mussaenda corymbosa.SELECTED DRAWING: None

This invention provides the application of Pulsatilla saponin B4 in the preparation of antimalarial drugs, which can significantly improve weight loss, peripheral blood parasitemia, and survival rate in mice infected with lethal Plasmodium. Its mechanism of action is not to directly kill Plasmodium, but to regulate the host immune system, including activating T / B cell immune responses, upregulating pro-inflammatory factors and interferon signaling pathways, and downregulating Arg1 expression. At the same time, Pulsatilla saponin B4 can alleviate immunopathological damage to organs such as the spleen and liver, restore the homeostasis of the spleen's immune microenvironment, and protect the normal structure of tissues. As a natural product, this compound has the characteristics of multiple targets and low toxicity, and has the dual advantages of anti-infection and immune homeostasis regulation, showing good prospects for clinical application and translation.

Disclosed herein are methods and compositions for treating and / or preventing Plasmodium falciparum malaria by administering a compound that mimics the binding of anti-Plasmodium falciparum Glutamic Acid Rich Protein (PfGARP).

The present application relates to a preparation of a 7,7'-epoxy lignan compound and its application in preparing anti-malaria products, and belongs to the field of traditional Chinese medicine and natural medicine pharmacy. The anti-malaria medicine with the compound as an active ingredient. The present application expands the medicinal value of 7,7'-epoxy lignan compounds in Rhodiola henryi.

The present invention discloses a functionalized isoquinolone and quinolone compounds and an efficient transition-metal-free approach for the synthesis of the same. The invention provides a highly functionalized isoquinolones from the reaction of dimethyl-2-((phenylamino)methylene) malonate with aryne precursors under mild. The reaction proceeds through insertion of aryne into the C−C σ-bond, which offers a novel and practical entry to access a wide range of isoquinolones with enhanced yields. The substrate scope is broad as the process can stands a variety of functional groups and the application of the developed process has been demonstrated in the total synthesis of antimalarial agent SJ000101247. Also, the highly functionalized quinolones are also useful in the synthesis of floxacins based compounds and derivatives e.g. ciprofloxacin, norfloxacin, G003967, etc.

The use of the combination of living plasmodium vivax and an antimalarial drug in the preparation of a product for activating CIK cells. It is found in the present application that maintaining the number of plasmodium vivax at a low density level by administering a low-dose antimalarial drug can activate CIK cells in a human body, thereby improving the tumor killing ability of CIK cells. The present invention is expected to be used in the preparation of a product for activating CIK cells and for killing tumor cells, and has the advantages of good safety, low toxicity and side effects, etc.

The present invention relates to the technical field of drug application. Disclosed are patchouli alcohol, a patchouli alcohol compound antimalarial composition, and a use in preparation of an anti-plasmodial drug. The antimalarial pharmaceutical composition is a composition of artesunate and patchouli alcohol. By compounding patchouli alcohol and artesunate, synergistic antimalarial activity can be produced; and by reducing the plasmodium infection rate in red blood cells, patchouli alcohol and the compound antimalarial composition alleviate edema and inflammation in the liver and the spleen caused by malaria, and decrease haemozoin deposition in the liver and the spleen, having minimal toxic and side effects on the liver while exerting the antimalarial activity. The antimalarial effect of patchouli alcohol is obviously superior to that of patchouli oil, the antimalarial effect of the composition of artesunate and patchouli alcohol is obviously superior to that of artesunate or patchouli alcohol used alone, and patchouli alcohol and the composition of artesunate and patchouli alcohol especially have a more obvious inhibitory effect on artesunate-resistant plasmodium.

The present invention belongs to the technical field of synthesis of small molecule compounds containing 4-aminoquinoline, and specifically relates to a method for preparing 4-aminoquinoline derivatives by coordinated catalytic oxidative aromatization of palladium and copper, which is applied to the synthesis of small molecule compounds containing 4-aminoquinoline and the synthesis of the core skeleton of antimalarial drugs. The present invention uses palladium acetate and copper acetate as catalysts, 4,4'-dimethoxybipyridine and the like as ligands, and oxygen as a green oxidant, and amination dehydrogenation aromatization occurs under the action of acid to prepare 4-aminoquinoline derivatives.

The present invention belongs to the field of biomedical technology, and specifically relates to the application of Lactobacillus murinus driving GABA in the treatment of cerebral malaria in mice. The present invention found significantly enriched Lactobacillus murinus and confirmed that Lactobacillus murinus can produce GABA. Subsequently, in a mouse cerebral malaria model, the effects of Lactobacillus murinus and GABA on improving and treating mouse cerebral malaria were evaluated when Lactobacillus murinus and GABA were used alone or in conjunction with dihydroartemisinin. The results showed that whether used alone or in combination with dihydroartemisinin, the bacteria and its metabolite GABA can effectively improve mouse behavior, immune pathological damage to various organs, reduce parasitemia, and prolong mouse survival. Compared with the use of drugs alone, it can effectively treat mouse cerebral malaria. From the perspective of using probiotics to drive their metabolites to assist antimalarial drugs in the treatment of mouse cerebral malaria, the present invention provides a new solution for the treatment of severe malaria caused by falciparum malaria, especially human cerebral malaria.

The invention discloses an artemisinin compound containing a piperazine side chain or a pharmaceutical salt thereof, and the structural general formula is shown in the specification. The artemisinin compound containing the piperazine side chain and the pharmaceutical salt thereof provided by the invention have a brand-new skeleton structure and better anti-malaria and anti-tumor activity, can be used as an anti-tumor drug and an anti-malarial drug, and can be used as an anti-malarial drug. And more choices can be provided for clinical treatment.

The invention belongs to the field of compound synthesis, and discloses an epsilon-caprolactam compound containing a guanidyl structural unit and preparation and application of the epsilon-caprolactam compound, the chemical structure of the epsilon-caprolactam compound is shown in the specification, and the epsilon-caprolactam compound containing the guanidyl structural unit has good anti-malarial activity and is expected to become a novel drug intermediate. The compound is used for preparing antimalarial drugs. The invention also discloses a preparation method of the epsilon-caprolactam compound containing the guanidyl structural unit. The preparation method of the epsilon-caprolactam compound containing the guanidyl structural unit has the advantages that the raw materials and the catalyst are cheap and easy to obtain; reaction conditions are mild, and operation is simple and convenient; and the method has the advantages of wide substrate universality, high yield for a series of epsilon-caprolactam products containing guanidyl structural units, and the like.

The invention discloses application of a naturally-sourced small molecule compound and a pharmaceutical composition thereof in preparation of antimalarial drugs, and belongs to the technical field of biological medicines. The small molecule compound is PHPP, the CAS number of the small molecule compound is 252205-23-5, and the structure of the small molecule compound is shown in the specification. According to the invention, the small molecule compound PHPP, which is a specific monomer component, is screened from natural products for the first time and is proved to have remarkable anti-malarial activity, and the cognitive blank of the anti-malarial application of the small molecule compound is filled up; the compound not only has an excellent in-vitro anti-malarial effect, but also has no obvious cytotoxicity under an effective concentration and is high in safety; more importantly, when the compound is combined with artemisinin, a remarkable synergistic effect can be generated, a brand new solution is provided for solving the problem of severe artemisinin drug resistance, and candidate lead compounds and combination schemes with wide prospects are provided for developing new-generation antimalarial drugs.

The present invention provides a method of treating malaria, comprising administering to a subject in need of such treatment a compound of formula (I) or a pharma- ceutically acceptable salt thereof, wherein the variables are as defined herein. The present invention further provides the use of a compound of formula (I) as defined herein for inhibiting the activity of plasmepsin X, plasmepsin IX or plasmepsin X and IX, for treating a malaria parasite infection, and for treating malaria. Also provided are methods of treatment further comprising administering one or more additional antimalarial compounds. [Formula 1] TIFF2024545498000356.tif52134

The invention provides a compound containing an artemisinin similar structure and a preparation method and application of the compound, the structural formula of the compound is shown in the formula I. The compound has excellent histone deacetylase inhibitory activity and anti-tumor and anti-malarial activity and can be used for preparing anti-tumor and anti-malarial drugs.

The present invention is related to the telotristat ethyl compound for use in the treatment of malaria and / or the prevention and treatment of the complications thereof. The present invention also concerns a combination of the telotristat ethyl compound and of at least one antimalarial drug conventionally used for treatment of the subject with malaria, and a kit comprising the telotristat ethyl compound inside a container, and one or more antimalarial drugs in one or more containers. Furthermore, the present invention is related to a process for the preparation of the telotristat ethyl.

The synthesis and characterization of a series of derivatives and analogs based on the 9-aminoacridine scaffold shared by antimalarial drugs quinacrine and pyronaridine are described. Also described is the structure-activity relationship of these compounds against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the virus that causes the coronavirus disease of 2019 (COVID-19). Several compounds displayed potent in vitro activity, with 50% inhibitory concentrations below 1 micromolar.

The invention discloses an artemisinin compound containing a 10-bit ether side chain or a pharmaceutical salt thereof, the structural general formula is one of the following structures: the artemisinin compound containing the 10-bit ether side chain provided by the invention has a relatively obvious proliferation inhibition effect on liver cancer HepG2, lung cancer A549, intestinal cancer HCT116, hematologic tumors MV-4-11 and HL-60; the anti-tumor activity of part of the compounds is higher than that of commercially available drugs SAHA and belinostat, and the compounds are expected to be developed into novel anti-tumor drugs. In addition, the performance of a plurality of compounds is superior to the in-vitro antimalarial activity of artemisinin, and the compounds are expected to be developed into novel antimalarial drugs.

The present invention recognizes that there is a need for the prophylaxis or treatment of COVID and COVID-19. A first aspect of the present invention generally relates to methods of prophylaxis or treatment of COVID or COVID-19 using various pharmaceutical compositions. A second aspect of the present invention generally relates to methods of prophylaxis or treatment of COVID or COVID-19 using combinations of antimalarial drugs and antiviral drugs. A third aspect of the present invention generally relates to methods of prophylaxis or treatment of COVID or COVID-19 using nanoparticle formulations that include pharmaceutical compositions. A fourth aspect of the present invention generally relates to methods of prophylaxis or treatment of COVID or COVID-19 using combinations of various pharmaceutical compositions. A fifth aspect of the present invention generally relates to methods of prophylaxis or treatment of COVID or COVID-19 using a polio vaccine and pharmaceutical compositions.

The present invention relates to dosing regimen of a new antimalarial drug, as monotherapy or combination therapy.

The invention discloses a method for inducing polarization of macrophages by AKK and / or outer membrane vesicles thereof and application of AKK and / or outer membrane vesicles thereof in preparation of drugs for promoting phagocytosis and infection of erythrocytes by macrophages, and belongs to the technical field of biological medicines. According to the invention, after macrophages are induced by AKK bacteria or OMVs thereof, an M1 polarization phenomenon occurs. Macrophages polarized by M1 generate proinflammatory factors, and meanwhile, erythrocytes infected by plasmodium are subjected to more phagocytosis. Compared with macrophages not polarized by M1, the macrophages polarized by M1 induced by AKK bacteria or AKK-OMVs can swallow more erythrocytes infected by plasmodium under the condition of not using the existing anti-malarial drugs, so that the resistance of plasmodium to the anti-malarial drugs due to long-term use of the anti-malarial drugs is effectively avoided; and a new scheme is provided for clinical malaria treatment.

The invention provides a nano preparation acting on plasmodium in a targeting manner and a preparation method of the nano preparation. The preparation comprises a hydrophobic antimalarial drug dihydroartemisinin and a high-selectivity PI3K inhibitor delalisib, and the nano carrier comprises polyethylene glycol-polycaprolactone (mPEG2000-PCL1140), a high molecular polymer (polydopamine), and glucosamine. The preparation method comprises the following steps: co-entrapping dihydroartemisinin and delalisib in a cavity of a polyethylene glycol-polycaprolactone copolymer, forming polydopamine from a dopamine monomer through a self-polymerization reaction under an alkaline condition, and uniformly coating the surfaces of nanoparticles with the polydopamine; the glucosamine and catecholamine of the polydopamine are subjected to a Michael addition and / or Schiff base reaction and are covalently coupled with the nanoparticles to be adsorbed on the surface of a polydopamine shell layer, and finally the anti-malarial nano-drug is obtained. The pharmaceutical composition can greatly enhance the anti-malarial effect and realize reverse drug resistance. Meanwhile, glucosamine on the surfaces of the nanoparticles has targeting property and can be specifically combined with an erythrocyte membrane glucose transporter 1 and a plasmodium hexose transporter, so that a better treatment effect is achieved.