192 results about "Multiple drug resistance" patented technology

Systems and methods for treating inflammatory and proliferative diseases, and wounds, using as a pharmacon a fatty acid metabolism inhibitor, a glycolytic inhibitor, and / or an agent able to alter cellular production of reactive oxygen, or combination thereof, optionally in combination with one or more chemotherpeutic agents. In preferred embodiments, the invention combines an oxirane carboxylic acid, represented by etomoxir, with a 2-deoxyglucose compound, represented by 2-deoxy-D-glucose, and / or an antibody against UCP and / or Fas antigen. The systems and methods of the invention can be used to treat drug-resistant or multi-drug resistant cancers.

This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.

The present invention relates to certain substituted phenyl piperazinyl oxazolidinones, for example, to those having the structure of Formula I with the variables as defined within, and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacterioides spp. and Clostridia spp. species, and acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.

This invention relates to certain 5-arylpyrimidine compounds or a pharmaceutically acceptable salt thereof, and compositions containing said compounds or a pharmaceutically acceptable salt thereof, wherein said compounds are anti-cancer agents useful for the treatment of cancer in mammals. This invention further relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal and further provides a method for the treatment or prevention of cancerous tumors that express multiple drug resistance (MDR) or are resistant because of MDR, in a mammal in need thereof which method comprises administering to said mammal an effective amount of said compounds or a pharmaceutically acceptable salt thereof.More specifically, the present invention relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof by promotion of microtubule polymerization which comprises administering to said mammal an effective amount of said compounds and pharmaceutically acceptable salts thereof.

Described herein are methods and compositions using chitosan derivatives to treat and / or inhibit acquisition of multiple drug resistance (MDR). Also described herein are methods and compositions using chitosan derivatives in combination with an antibacterial agent to treat a bacterial infection and / or inhibit growth of bacteria, for example, resulting in a synergistic or sensitizing effect.

One embodiment of the present invention is a method of treating a subject with a multi-drug resistant cancer. The method comprises administering to the subject an effective amount of a compound represented by Structural Formula (I):Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group, or, Y, taken together with both >C═Z groups to which it is bonded, is a substituted or unsubstituted aromatic group.R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and / or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. Preferably R1 and R2 are the same and R3 and R4 are the same.R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group.Z is ═O or ═S.

The invention discloses blank mixed micelle, and a preparation method and applications thereof. The blank mixed micelle comprises an amphiphilic copolymer and ginsenoside represented by formula I, ishigh in efficiency, is safe, is stable, is high in targeting performance, is excellent in homogeneity, is stable in quality, is convention in preparation technology, can be used for coating one or a plurality of active substances in drugs or cosmetics and health care substances, and is capable of forming mixed micelle containing loaded active substances. Compared with conventional nanometer micelle, the blank mixed micelle possesses following advantages: the mixed micelle loaded with active substances is excellent in drug forming performance, multiple drug resistance, stability, homogeneity, and safety performance, and is small in particle size; and the curative effect of loaded active drugs on drug resistant cells is better.

An encapsulated delivery system, and, in particular, a nanoparticulate delivery system representing a qualitatively different approach to overcoming multi-drug resistance while simultaneously administering the chosen drug treatment to a patient, e.g., in a site-specific manner, is disclosed. A composition according to the invention includes a therapeutically effective amount of one or more multi-drug resistance reversing agents selected from the group consisting of ceramide and ceramide modulators; and a therapeutically effective amount of a therapeutic agent, wherein the therapeutic agent is different from the one or more multi-drug resistance reversing agents, and the one or more multi-drug resistance reversing agents and the therapeutic agent are encapsulated, preferably co-encapsulated, in a biocompatible, biodegradable delivery vehicle for delivery to a patient in need of treatment, for example, for specific localization at, or higher probability of delivery to, a treatment site in a patient administered the composition. Preferably, the one or more multi-drug resistance reversing agents are ceramide, paclitaxel or tamoxifen.

This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.

The present invention discloses methods, primer, probes, and kits for genotyping various mutations or disease-causing agent. In one embodiment, the present invention is applied to detecting the presence of multidrug-resistant Mycobacterium tuberculosis, HBV, beta-globin mutations, mutations related to thrombophilia, or the presence of sexually transmitted diseases in a subject.

Compositions and methods for using nordihydroguaiaretic acid (NDGA) derivatives for preventing the expression of MDR-1 gene and the synthesis of PgP protein or reversing multiple drug resistance in cells, and for using NDGA derivatives in combination with additional chemotherapeutic agents to treat drug resistant cancer and infections.

The present invention relates to an improved method for the preparation of Artemether. Artemether prepared from the process is useful for the treatment of uncomplicated, severe complicated and multi drug resistant malaria.

Use of 2-bromo-isovanillin in the preparation of an anticancer medicament and / or radio- and chemotherapy sensitizing medicament is disclosed. The medicament for the treatment of cancers and / or for radio- and chemotherapy sensitization comprising 2-bromo-isovanillin as active ingredient provided herein has the following features: (1) low toxicity, without evident adverse effects; (2) significant therapeutic effect, with remarkable proliferation inhibiting and pro-apoptotic effects in tumor cells; (3) a broad-spectrum anticancer activity; (4) suitable to be used in combination with antimetabolites, to enhance the effects and meanwhile lower the toxicity, and also to reduce multi-drug resistance; (5) convenient and safe administration, the main route being oral.

This invention relates to certain 6-[(substituted)phenyl]triazolopyrimidine compounds or pharmaceutically acceptable salts thereof, and compositions containing said compounds or pharmaceutically acceptable salts thereof, wherein said compounds are anti-cancer agents useful for the treatment of cancer in mammals. This invention further relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal and further provides a method for the treatment or prevention of cancerous tumors that express multiple drug resistance (MDR) or are resistant because of MDR, in a mammal in need thereof which method comprises administering to said mammal an effective amount of said compounds or pharmaceutically acceptable salts thereof. The present invention relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof by promotion of microtubule polymerization which comprises administering to said mammal an effective amount of said compounds and pharmaceutically acceptable salts thereof.

The invention relates to a tree-like polymer nanometer drug delivery carrier targeting doxorubicin. The structural general formula of the targeting doxorubicin is PEG-b-PAMAM-hydrozone-(DOX)n. A tree-like polymer nanometer drug delivery carrier targeting doxorubicin of liquid tumors representative to myeloma is provided in the invention. The acidic environment (pH of 5.5) of myeloma makes a hydrogen bond connecting a carrier with doxorubicin be broken, so complete doxorubicin molecules are released. The release is only carried out under the acidic condition of the myeloma, so the treatment pertinence of the drug is greatly improved. P-glycoprotein will diffuse to doxorubicin monomer elimination cells in cells, so tumor cells generate multiple drug resistances. The carrier drug can avoid the medicine efflux phenomenon caused by the p-glycoprotein and can also avoid the multiple drug resistances.

Embodiments of the invention provide a method and composition for treating or reducing multiple drug resistance in cancers. Embodiments of the invention also provide for a xanthene compound to inhibit multidrug resistance protein 1.

The invention belongs to the technical field of medicines and in particular relates to application of an indol-ethylene substituted quinoline derivative in preparing drug-resistance bacterium medicines. The invention provides application of the indol-ethylene substituted quinoline derivative of formula (I) as shown in the specification in preparing drug-resistance bacterium medicines. The indol-ethylene substituted quinoline derivative provided by the invention has a remarkable inhibition function upon multiple drug-resistance bacteria, and is capable of remarkably inhibiting growth and propagation of vancomycin-resistant enterococcus, drug-resistant escherichia coli and methicillin-resistant staphylococcus aureus. Deep structure and function study shows that the indol-ethylene substitutedquinoline derivative provided by the invention has an action target of a bacterium split protein FtsZ, because of differences of FtsZ and human micro-tube protein sequences, drug-resistance bacteriummedicines which can selectively act upon bacteria FtsZ without interfering host cells can be designed, and the derivative is good in antibacterial activity, is capable of reducing amounts of single medicines, then reducing toxic and side effects and reducing drug resistance, and has the prospect of being developed into novel antibiotic medicines.

The invention discloses applications of pharmorubicin and quercetin to preparation of an anti-tumor combined medicament. The invention further discloses a combined medicament. The pharmorubicin is taken as an anti-tumor medicament; the quercetin is taken as an MDR (Multiple Drug Resistance) reversal agent of the pharmorubicin; PLGA (Poly(Lactic-Co-Glycolic Acid)) is taken as nanoparticle copolymer material; compound nanoparticles of pharmorubicin and quercetin are entrapped during preparation, so that a certain entrapment efficiency and medicament loading amount are achieved; various indexes of the nanoparticles are used for evaluating the property of the medicament; and an in-vitro cell test is used for evaluating the reversed multi-medicament resistance effect of the medicament. EPI-QC (Epichlorohydrin-QC) compound nanoparticles are prepared by adopting an emulsified solvent evaporation method; and according to research on a comparison system, the EPI-QC compound nanoparticles can be used for reverting the medicament tolerance of tumor cells in a certain degree, and the toxicity on normal cells is lowered.

The present invention provides gene targets, constructs and methods for the genetic control of plant disease caused by multiple plant viruses. The present invention relates to achieving a plant protective effect through the identification of target coding sequences and the use of recombinant DNA technologies for post-transcriptionally repressing or inhibiting expression of the target coding sequences of plant-parasitic viruses. Protein-expression based approaches may also be utilized to augment phenotype resistance. Thus, transcription of a single transgenic event comprising one or more plant expression cassettes can allow for broad spectrum resistance of a plant to multiple plant viral strains and species among the geminiviruses, tospoviruses, and potexviruses.

The invention belongs to the field of biotechnology, and discloses an alkaline antibacterial peptide as well as targeting design and application thereof. The alkaline antibacterial peptide is composed of at least one alkaline amino acid and one or two hydrophobic amino acids; the alkaline antibacterial peptide includes 12-24 amino acids, wherein the proportion of the alkaline antibacterial peptide is more than 33.3%, and the alkaline antibacterial peptide has a broad-spectrum bacteriostatic action on escherichia coli, pseudomonas aeruginosa, staphylococcus aureus, multi-drug resistance staphylococcus aureus, saccharomyces cerevisiae and the like; the alkaline antibacterial peptide is prepared as a targeted antibacterial peptide, and the efficiency of the antibacterial peptide in killing lung cancer cells at 0.1mM reaches 100.3%; the antibacterial peptide or the targeted antibacterial peptide disclosed by the invention is applicable to bacterium inhabitation and cancer resistance, and can be widely applied to the fields of medicine, agriculture, food preservative and the like.

The present invention relates to 2,4,5-trisulbstituted imidazole compounds and their preparation process and their application in preparing medicines for reversing multiple drug resistance of tumor cell mediated by P-glucoprotein, multiple drug resistance relative protein, lung multiple drug resistance relative protein and other membrane transport proteins and restoring the sensitivity of tumor cells with multiple drug resistance to anticancer medicines.

The invention discloses phage lytic enzymes as well as a gene recombinant expression vector and application thereof. The phage lytic enzyme expression gene is a nucleotide sequence shown as SEQ ID NO:1, and the nucleotide sequence can express phage lytic enzymes in a host cell by constructing a recombinant vector. The phage lytic enzymes obtained through purification have relatively high in-vitroand in-vivo bactericidal activity, acts quickly, is safe and harmless to organisms, can well treat multi-drug-resistance shigella infection, and also has a certain inhibition effect on staphylococcusaureus, vibrio parahaemolyticus and other pathogenic bacteria. The phage lytic enzymes have good lytic thallus activity within the range of 28-42 DEG C, and due to the characteristics, the phage lytic enzymes have a wide prospect in the aspect of preparing drug-resistant infectious disease medicaments and can be used as a substitute or supplement of conventional antibiotics.

The invention relates to dendritic cell (DC) tumor vaccine in which a multi-medicine resistance tumor stem cell antigen composition is loaded. The antigen composition loaded in the DC tumor vaccine derives from tumor tissues, and is mainly used for tumor stem cells; and specifically, the tumor tissues are subjected to tumor stem cell primary separation and culture so as to obtain the tumor stem cells, the tumor stem cells are screened by a flow cytometry so as to obtain tumor stem cells with multi-medicine resistance, and finally full cell antigens are prepared.

The invention relates to novel anti-tumor cytarabine prodrug derivatives through chemically modifying the N4 and O5 positions of cytarabine to prevent N4 amino being metabolized to lose efficacies and result in toxicity and let O5 hydroxy be easily phosphorylated for activation and introducing multifunctional groups of aspirins to the prodrug modules of the cytarabine to increase the drug functions for improving the anti-solid tumor activities. The invention also provides multiple synthesis routes of the cytarabine prodrug derivatives, a cytarabine prodrug derivative preparation and a preparation method thereof in detail and proves the purposes of the cytarabine prodrug derivatives at the aspect of resisting cancers and tumors through a great amount of experimental data. The cytarabine prodrug derivatives have a multi-targeting function and the advantages of increasing bioavailability, reducing multiple drug resistance and increasing solubility and ester dissolution.

Methods and compositions are provided for treating a subject having or at risk of developing a hematologic malignancy and / or multiple drug resistance.

The invention belongs to the biomedical test field, and relates to a microbial molecular biological detection method, in particular to a kit for rapidly testing the multi-drug resistance of mycobacterium tuberculosis. The kit comprises a multiple PCR system simultaneously amplifying four kinds of drug resistance related genes of noddle, and a probe hybrid system simultaneously detecting corresponding point mutation in the drug resistance related genes. The kit can simultaneously detect the mutation of a plurality of drug resistance related genes of noddle through one-time operation, thereby being rapid and time saving, and only needing one working day for the entire process. The kit which has relatively low cost is not required to be provided with an expensive chip reading machine, thereby being easy for implementation and promotion in grass-root medical institutions.

There is described a composition comprising a therapeutically active imidazole, or a derivative thereof, and disulfiram, or a derivative thereof, for treating an infection contributed to or caused by multi-drug resistant bacterial species.

This invention relates to multi-drug resistance (MDR) in cells, and the use of certain xanthene compounds for determining drug resistance in cells and the effect of test compounds on cell membrane transport by the membrane transporters MDR1, MRP and BCRP. Processes and kits for making these determinations and measuring these effects are described and provided.