172 results about "Chloroquine" patented technology

This invention discloses compositions of chloroquine-coupled active agents such as therapeutic antibodies or insulin, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the drug is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to a drug directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing the drug for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and antibody or insulin to their site of action.

The present invention provides improved cell delivery compositions. In particular, the invention provides biocompatible endosomolytic agents. In a preferred embodiment, the endosomolytic agents are also biodegradable and can be broken down within cells into components that the cells can either reuse of dispose of. In one aspect, the present invention provides endosomolytic agents capable of effecting the lysis of an endosome in response to a change in pH, and methods for effecting the lysis of an endosome. These inventive endosomolytic agents obviate the need for known agents (i.e., chloroquine, fusogenic peptides, inactivated adenoviruses and polyethyleneimine) that can burst endosomes and have negative effects on cells. In another aspect, the present invention provides cell delivery compositions comprising an endosomolytic component that is capable of effecting the lysis of the endosome in response to a change in pH, and an encapsulating, or packaging, component capable of packaging a therapeutic agent to be delivered to cellular or subcellular components.

This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.

The invention relates to an inhalation spray of antivirus medicines. The inhalation spray comprises the following components in percentage by mass of 0%-30% of antivirus activity agents, 0%-30% of auxiliary agents, 0%-30% of taste masking agents and the balance solvents, wherein the content of the antivirus activity agents and the content of the auxiliary agents are not 0% at the same time. Compared with the prior art, the inhalation spray disclosed by the application has the purpose that during outbreak period of epidemic corona viruses and other viruses, people do not need to occupy medicalresources in short supply and only need to inhale the antivirus medicines into respiratory tracts, medicine administration is accurately targeted, and the objective of preventing virus infection and propagation can be achieved; in addition, through united medication of the antivirus activity agents and the auxiliary agents, besides, various medicines are inhaled into the respiratory tract of a patient, synergistic treatment effects are generated, the viruses are eliminated, and serious respiratory tract and infection and serious pulmonary infection caused by the viruses can be treated; and chloroquine type antivirus medicines and macrocyclic antibiotics are inhaled through spraying for united medication, and the dosage of the medicines can be notably reduced, so that side effects of prolonged QT intervals, Tdp and sudden cardiac death caused by the medicines can be reduced.

The present invention provides methods and compositions for modulating certain metabolic processes and for treating a variety of disorders associated with metabolic syndrome, including insulin related disorders, ischemia, oxidative stress, atherosclerosis, hypertension, obesity, abnormal lipid metabolism, and stroke by administering an effective dose of a chloroquine compound. The invention also provides methods and compositions relating to administering an effective dose of a chloroquine compound in combination with at least a second pharmaceutically active ingredient or compound including an antihyperglycemic diabetes treatment, an antihypertensive agent, an antithrombotic agent, and / or an inhibitor of cholesterol synthesis or absorption.

The invention relates to the novel usage of an antimalarial medicine, in particular to the novel usage of hydroxychloroquine having sensitivity enhancing effect on various chemical anti-multiple myeloma medicaments. The novel usage is characterized in the application of hydroxychloroquine in treatment of multiple myeloma through chemotherapeutic medicaments. The hydroxychloroquine can obviously enhance the killing activity of chemotherapeutic medicines such as doxorubicine, epidoxorubicin, cis-platinum and mitoxantrone to multiple myeloma cells, and the killing activity thereof is realized by inhibiting the myeloma cell autophagy signals by hydroxychloroquine. Hydroxychloroquine can induce the quantity of the autophagy lysosomes of the multiple myeloma cells to be increased and the expression of the autophagy-associated albumen LC3-II to be increased.

Improved methods, reagents, and kits for quantitation of HLA-DR and / or CD11b expression on peripheral blood cells are presented. Inclusion of a lysosomotropic amine, such as chloroquine, during staining stabilizes HLA-DR and CD11b expression. Use of a novel anti-CD14 conjugate, anti-CD14-PerCP / CY5.5, permits the ready discrimination of monocytes. The improved methods, reagents, and kits may be used to assess immune competence, and to direct and monitor immunostimulatory therapies in septic patients exhibiting monocyte deactivation.

The present invention provides methods and compositions for modulating certain metabolic processes and for treating a variety of disorders associated with metabolic syndrome, including insulin related disorders, ischemia, oxidative stress, atherosclerosis, hypertension, obesity, abnormal lipid metabolism, and stroke by administering an effective dose of a chloroquine compound. The invention also provides methods and compositions relating to administering an effective dose of a chloroquine compound in combination with at least a second pharmaceutically active ingredient or compound including an antihyperglycemic diabetes treatment, an antihypertensive agent, an antithrombotic agent, and / or an inhibitor of cholesterol synthesis or absorption.

The invention provides a chloroquine liposome lyophilized powder for injection, comprising (by weight parts) the chloroquine or the salt formed by the chloroquine and acid 1part, phospholipid 2-100 parts, cholesterol 1-35 parts, vitamin E 0.5-5.0 and excipients. The preparation method comprises two steps, including the preparation of blank liposome, and the preparation of drug-carrying liposome through the pH gradient method. The injection has the advantages of reasonable design, wide carrier selection range, high drug entrapment efficiency, and good stability. The preparation method has the advantages of easy operation, low cost, and good controllability and repeatability.

The invention relates to a clinic detection marker of an inflammatory bowel disease, and applications thereof, and concretely relates to a molecular marker-Erbin gene in the inflammatory bowel disease, and an application of an inhibitor chloroquine of a downstream autophagy pathway regulated by the marker. An experiment result shows that the intestinal mucosa damage of DSS induced Erbin<+ / +> and Erbin<- / -> mice injected with chloroquine are substantially reduced, the intestinal mucosa damage of the Erbin<- / -> mice is obviously severer than that of the Erbin<+ / +> mice, and the mice injected with chloroquine have higher intestinal mucosa integrity, substantially lower inflammatory cell infiltration and substantially alleviated inflammatory bowel disease symptoms than mice not injected with the chloroquine, so the autophagy inhibitor chloroquine can improve the integrity of the intestinal mucosa and has a very good IBD inhibition effect, thereby the chloroquine has certain prevention and treatment effects on the inflammatory bowel disease.

The present invention provides methods and compositions for prophylaxis and treatment of a variety of disorders including DNA damage related disorders, cancer, ischemia, oxidative stress, atherosclerosis, and stroke using a chloroquine compound.

The invention provides a micro RNA group related to Th17 differentiation. The micro RNA group comprises micro RNA 4426, micro RNA 3615, micro RNA 106b, micro RNA 590 and micro RNA 573. The micro RNA changes remarkably in the Th17 differentiation process and can be used as Th17 control targets for preparing drugs for treating or preventing Th17-related diseases including lupus erythematosus, dermatomyositis, vasculitis, sicca syndromes, rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, scleroderma, multiple sclerosis, malaria, solar dermatitis, eczema, leucoderma, psoriasis, atopic dermatitis, lichen planus, diabetes, coronary heart diseases, hyperlipemia and the like. The micro RNA group is sensitive to hydroxychloroquine intervention and can serve as a sensitive index for judgment of the clinical effect of hydroxychloroquine, and the micro RNA is convenient to test clinically and can be rapidly used for judging the clinical effect of hydroxychloroquine.

The invention discloses a chloroquine-polymerized nanogel delivery system and a preparation method thereof. The delivery system contains chloroquine-polymerized nanogel particles, and antitumor medicines which are wrapped with the particles, wherein the chloroquine-polymerized nanogel is prepared through hydroxychloroquine and polysaccharide framework which is modified through a hydrophobic side chain. According to the medicine delivery system, malignant tumor and tumor metastasis are treated synchronously; the signal cascade of cancer cells metastasizing to surrounding and distant sides is stopped while cancer cell proliferation is inhibited, and malignant cancer can be effectively treated.

The invention relates to a pesticide, wherein the invention comprises active component, stuff and agent; the active component is formed by methyl acrylate pesticide, triazole pesticide and chloroquine. The invention has 94. 56% protecting effect and 89. 85% treatment effects, with low cost.

The present invention relates to the technical field of biomedicine, and mainly provides new uses of tauroursodeoxycholic acid, wherein the new uses comprise that the tauroursodeoxycholic acid inhibits the virus-entry-host cells adopting endocytosis so as to achieve prevention and treatment of virus infection, anti-injury, and anti-fibrosis. The present invention provides applications of the tauroursodeoxycholic acid in preparation of drugs for treatment of acute lung injury and pulmonary fibrosis, such that the application range of the tauroursodeoxycholic acid is broadened, and the new drug selection is provided for the virus infection patients. According to the present invention, it is confirmed that the tauroursodeoxycholic acid can effectively prevent and treat H5N1 avian influenza virus, human adenovirus and Zaire-type Ebola virus, and it is cleared that the pulmonary fibrosis prevention and control effect of the tauroursodeoxycholic acid is superior to the pulmonary fibrosis prevention and control effect of the chloroquine.

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.

A nose and throat anti-influenza solution is described that decreases the likelihood influenza infection and its spread. The solution's components are readily available and have been used to treat humans for other ailments previously, leading to an easily implemented, scalable, safe, and cost-effective solution. The core components of the solution include: specially denatured alcohol (SDA); Triton x-100; sodium saccharin; 1,8 cineole (eucalyptol); thymol; methyl salicylate; menthol; sorbitol and / or glycerin; sodium benzoate; poloxamer 407; polysorbate 80; and distilled water. Optionally, the solution also includes one or more of the following: citric acid; sambucus nigra agglutinin; a lectin that binds 2,3 sialic acid; nonoxynol-9; sialyllactose; a protease; a protease inhibitor; and / or chloroquine. The solution is applied to the nasal cavity via a pre-moistened cotton swab or a pre-moistened facial tissue and the solution is applied to the back of the throat via a spray, gum, or gargle solution. Further a nebulizer, atomizer, or inhaler can be used to apply the solution to the back of the throat, to the pharynx, and / or to the respiratory tract.

A cell permeable iron chelator, optionally in combination with an autophagy inhibiting agent, is used for treating a solid cancer tumour in a person. A preferred chelator is an alkyl substituted N-(1-pyridine-2-yl-methylidene)-N-(9H-1,3,4,9-tetraaza-fluoren-2-yl)-hydrazine. A preferred autophagy inhibiting agent is chloroquine. Also disclosed is a pharmaceutical composition comprising iron chelator, pharmaceutically acceptable carrier and, optionally, autophagy inhibiting agent; and a method of treating cancer by administering cancer combating-effective amount(s) of the iron chelator or the combination of iron chelator and autophagy inhibiting agent.

This disclosure provides a method of treating a subject infected with a mycobacteria of the M. tuberculosis complex or infected with an atypical mycobacterium. Aspects of the method include administering to a subject in need thereof a therapeutically effective amount of an enantiomerically pure (R)-chloroquine agent. The (R)-chloroquine agent may be an analog or derivate of chloroquine having a particular stereochemistry at the position located alpha to the amino-quinoline core of the chloroquine agent. Also provided are methods of inhibiting mycobacteria of the M. tuberculosis complex or other atypical mycobacteria in a cell. Kits and pharmaceutical compositions for practicing the subject methods are also provided.

The invention discloses a chloroquine and adriamycin co-supported liposome, which is prepared from medicaments, phospholipid, cholesterol compounds, an internal buffer system and a pH value regulator, wherein a weight ratio of the medicaments to the phospholipid to the cholesterol compounds is (1:2)-(100:1)-35, and the medicaments comprises chloroquine medicaments and adriamycin medicaments. The chloroquine and adriamycin common-carried liposome has the characteristics of inhibiting the tolerance of multiple medicaments and reducing medicinal toxicity under the synergistic action of chloroquine and adriamycin. The invention also discloses a preparation method for the chloroquine and adriamycin co-supported liposome, a preparation process is simple, controlled parameters are few, reaction conditions are low, production cost can be reduced conveniently and the chloroquine and adriamycin co-supported liposome is easy to industrially produce.

A pharmaceutical composition or kit of parts comprising at least three ingredients from a HMG-CoA reductase inhibitor, a leukotriene antagonist, a proton pump inhibitor, melatonin or a melatonin receptor agonist, a bioavailable preparation of a curcuminoid, a calciferol derivative, a compound from the group consisting of metformin and phenformin, valproate, minocycline and chloroquine and one or more pharmaceutically acceptable carriers or excipients.

The invention discloses a chloroquine antibacterial disinfectant and application thereof. Chloroquine or a chloroquine derivative with the mass concentration of 0.1-5.0% is used as a main effective component, and the pH value is 4.0-7.0. Furthermore, plant extracts which are derived from natural plants and have a bactericidal effect can be supplemented, and an obvious synergistic effect is achieved on the bacteriostatic and antiviral effects of chloroquine. The liquid medicine has a certain cleaning and killing effect on various bacteria and viruses, especially on spreading and infection of coronavirus, HPV, HIV and other viruses and bacteria, and has a very good effect on prevention of oral cavity, home environment, exposed skin and other bacteria and virus susceptible parts. Moreover, chloroquine is developed into an external disinfection preparation and can be further developed into various sanitary disinfection products and old medicines for new use, compared with similar disinfection products, the external disinfection preparation can be orally taken and is small in harm, people can be more effectively protected against germs and viruses when the external disinfection preparation is sold on the market, and the external disinfection preparation is wide in application prospect.

The invention belongs to the technical field of medicines, and relates to a medicine composition of autophagy inhibitor and lapatinib, and an application thereof. The medicine composition comprises a cell autophagy inhibitor and lapatinib, wherein the cell autophagy inhibitor is one or more selected from 3-MA, wortmannin, LY294002, cycloheximide, bafilomycin A1, NH4Cl, chloroquine and hydroxychloroquine. The medicine composition can inhibit lapatinib-induced tumor cell autophagy, offset an antagonistic effect of tumor for lapatinib caused by cell autophagy and significantly enhance a curative effect of lapatinib on the tumor. The medicine composition provided by the invention can enhance a killing effect of lapatinib on the tumor, enhance the curative effect of lapatinib, and can be used for treating malignant tumor.

The invention provides a pharmaceutical composition for treating viral infection of respiratory system. The pharmaceutical composition contains chloroquine and a sputum-removing drug. The sputum-removing drug is selected from at least one of acetylcysteine, ambroxol or ammonium chloride. The invention provides a preparation method of the pharmaceutical composition for preventing and treating diseases caused by virus infection of a human respiratory system. The medicine composition of the chloroquine and sputum-removing drug is prepared into a spray, an aerosol or an inhalation preparation forpreventing and treating the diseases caused by the virus infection of the human respiratory system.

The invention provides in certain embodiments a therapeutic regimen comprising (a) an anti-cancer combination of vemurafenib and cobimetinib, or a combination of trametinib and dabrafenib, and (b) a secondary agent comprising L-buthionine-[S,R]-sulfoximine (BSO), or phenyl butyric acid (PBA) or a pharmaceutically acceptable salt thereof, and chloroquine or hydrochloroquine (HCQ) for the therapeutic treatment of a hyperproliferative disorder.

The invention relates to application of chloroquine and chlorpromazine to preparation of drugs for treating and preventing lung infection and injuries, in particular to application of the chloroquine, the chlorpromazine, derivatives of the chloroquine and the chlorpromazine, mixture of the chloroquine and the chlorpromazine, and drug compositions containing the chloroquine or the chlorpromazine to the preparation of drugs for treating and / preventing lung infection and injuries caused by influenza viruses to mammals including human.

The invention provides a rapid and simple method for preparing optically active chloroquine, hydroxychloroquine and analogues thereof, which comprises the following steps: reacting racemates of chloroquine, hydroxychloroquine and analogues thereof with an acidic chiral resolution reagent to generate corresponding salts, and separating and purifying to obtain optically pure salts of chloroquine, hydroxychloroquine and analogues thereof, and reacting with alkali to obtain (R)- or (S)- chloroquine with high optical purity and (R)- or (S)- hydroxychloroquine and analogues thereof. The method is simple and convenient to operate and low in cost, the enantiomer purity can reach 99.9% ee, and industrial production of chloroquine, hydroxychloroquine and analogues thereof with single chiral configuration is easy to realize. The invention also provides (R)- or (S)- chloroquine and (R)- or (S)- hydroxychloroquine and analogues thereof, pharmaceutical compositions and uses thereof, optically activechloroquine and hydroxychloroquine and analogues thereof reduce toxic and side effects, and have better treatment effects on coronavirus, influenza virus and autoimmune diseases.

The invention relates to a novel medicine composition capable of synergistically enhancing the capacity of restraining tumor growth. The composition contains tetrandrine and chloroquine. Researches prove that the combined medication of the tetrandrine and the chloroquine with a certain concentration can effectively induce the death of tumor cells; a BALB / c nude mouse is vaccinated with a tumor cell of a person, a tumor is formed, a nude mouse heterograft model is established, and the monitoring on the growth curve of the tumor and the weight of the tumor indicates that the combined medication has the obvious effect of restraining the tumor growth. The invention confirms that the antitumor effect of the medicine combination containing the tetrandrine and the chloroquine is much better than that of the single tetrandrine or the single chloroquine, the medicine combination has an obvious synergistic effect, the basis of clinical combined application of the tetrandrine and the chloroquine for resisting the tumor is provided, and the medicine combination is a potential tumor medicine with high efficiency and low toxicity.

The invention discloses an application of chiral chloroquine, hydroxychloroquine or pharmaceutically acceptable salts of the chiral chloroquine and hydroxychloroquine in preparation of drugs used forpreventing and / or treating coronavirus pneumonia by using a coronavirus key drug target 3CL hydrolase (Mpro) as an action target. The chiral chloroquine and hydroxychloroquine have high bonding strength with the Mpro causing inflammation of the lung and the like; the activity of the Mpro can be significantly inhibited; and the chiral chloroquine and hydroxychloroquine are indicated to have the effect of preventing and treating pneumonia caused by coronaviruses and be able to be used as anti-pneumonia drugs. Through evaluation on the inhibitory activity of an hERG potassium ion channel, the concentration at which the chloroquine, hydroxychloroquine and enantiomers of the chloroquine and hydroxychloroquine are likely to generate cardiotoxicity to the hERG potassium ion channel is provided. The chiral chloroquine and hydroxychloroquine are prepared through chiral high-performance liquid chromatography and chiral synthesis; S-configuration chloroquine, hydroxychloroquine or salts of the chloroquine and hydroxychloroquine can be selected as a drug independently, or form a pharmaceutical composition for treating diseases caused by the coronaviruses; and due to higher activity and low cardiotoxicity of the chloroquine, hydroxychloroquine or salts of the chloroquine and hydroxychloroquine, the administration dosage range is greatly widened.

The invention discloses a chloroquine spray and a preparation method thereof. The spray consists of a powder and a solution, wherein the powder contains chloroquine or a chloroquine derivative, a carrier macromolecular material and a sweetening agent, and the solution is a salt solution containing borneol and / or menthol. The spray containing a chloroquine medicament is developed for the first time, has small toxic and side effects, can be directly used for antibacterial and antiviral protection of the oral and nasopharynx, can be used for clearing the nose and cleaning the pharynx and throat,and has the original clinical treatment application. Meanwhile, the method utilizes the carrier macromolecular material to wrap the chloroquine, prolongs the retention time of the chloroquine spray in the oral mucosa or the nasal mucosa to achieve the effect of slow release and long-acting, and can obviously improve the bacteriostatic disinfection effect of the chloroquine by being supplemented with menthol, borneol and ethanol. The chloroquine spray is mild and non-irritating, has good taste and convenient use, and can provide normal care for healthy people and more effective prevention andtreatment measures for infected or latent people in the aspects of virus protection such as novel coronavirus and the like.