108results about How to "Overcome drug resistance" patented technology

The invention is directed to novel prodrug compounds, compositions comprising the prodrug compounds, methods of making the prodrug compounds and methods of using the prodrug compounds. The prodrug compounds comprise a biologically active entity linked to a masking moiety via a linking moiety. The prodrug compounds are selectively activated at or near target cells and display lower toxicity and possibly a longer in vivo or serum half-life than the corresponding naked biologically active entity.

The invention discloses a 5,8-dioxo-pyrimido[4,5-e][1,4]diazepine compound of a structural formula (1) or a pharmaceutically acceptable salt or stereoisomer or prodrug molecule thereof. The 5,8-dioxo-pyrimido[4,5-e][1,4]diazepine compound has the effects of effectively inhibiting the growth of various tumor cells and the generation of the EGFR (epidermal growth factor receptor), can be used for preparing anticancer medicaments and can overcome the resistance of the existing medicaments including the gefitinib, the erlotinib and the like.

Prodrugs based on gemcitabine structure shown in formula (I) as well as their synthetic method and application are disclosed in the present invention, wherein the definitions for the groups of a, b, c, d, E, Z and V are described in the specification. By modifying the N⁴ group, the solubility, the bioavailability and the organ specificity of the prodrugs are improved. Therefore, the fast metabolism problem is overcome for the produced prodrugs compounds. Intestinal toxicity induced by gemcitabine is decreased. Thereby, the prodrugs can be delivered by oral administration in clinics and further improve their anti-tumor, anti-cancer, anti-infection and diffusion preventing capability, and can also specifically act on liver or colon. The synthetic method is simple and adapted to industrial production.

The invention provides therapeutically effective compounds for the prevention and treatment of cancer and pharmaceutical compositions containing these compounds as well as methods of using and administering these compounds. The invention also includes methods of activating a prodrug of these therapeutically effective compounds by the administration of a peptide-directed targeting construct that delivers a prodrug-activating enzyme to a target activation site.

The invention relates to a 2-aminopyrimidine compound and application thereof. The structure of the 2-aminopyrimidine compound is shown as I. The compound can effectively inhibit the activity of EGFRprotein kinase resistance mutants (such as EGFRT790M and EGFRT790M/C797S), and can overcome clinical drug resistance of tumor patients such as patients suffering from non-small cell lung cancer induced by an existing third-generation selective EGFRT790M small molecule inhibitors Osimertinib (AZD9291), Olmutinib (HM6171), Rocketinib (CO-1686) and the like.

The invention relates to the technical field of biological medicines, in particular to a kit for quantum dot nucleic acid detection of urinary tract infection-causing pathogens. The kit comprises a detection membrane strip, a fluorescent detection solution and reaction solutions, wherein the detection membrane strip comprises a nylon membrane and a capture probe fixed to the nylon membrane; the fluorescent detection solution comprises quantum dots for marking the capture probe and coupled with streptavidin on the surfaces; the reaction solutions include a reaction solution I, a reaction solution II, a reaction solution III and a reaction solution IV. The kit has the beneficial effects as follows: the high-throughput, high-sensitivity and high-specificity kit for the quantum dot nucleic acid detection of the urinary tract infection-causing pathogens is provided; the kit has fewer steps and obviously shorter detection time than the existing colorimetric gene chip, has lower equipment cost than an organic fluorescent gene chip, and is conducive to clinical popularization.

The invention discloses a composite plant disinfectant and a preparation method thereof. The composite plant disinfectant comprises the main raw materials including lonicera, Chinese atractylodes, scutellaria, crataegus, dandelion, phellodendron, lithospermum and the like, and the raw materials are crushed, immersed in distilled water, boiled, cooled, subjected to standing, filtered, added with chitosan and separately packed, so as to obtain the composite plant disinfectant. The composite plant disinfectant, disclosed by the invention, combines a variety of traditional Chinese medicine extracts for internal use, has good antibacterial function, can well sterilize golden staphylococci, colibacillus and salmonella, prevents microorganism from generating medicine resistance, does not pollute the environment, and is a disinfectant which is relevant to food sterilization, safe, innoxious, residue-free, high in action speed, stable in property and efficient.

The invention discloses pyrimidotricyclic compounds or pyrimidotetracyclic compounds having a structure represented by the formula (I), (II) or (III), pharmaceutically-acceptable salts, stereoisomers, or prodrug molecules. The compounds can inhibit various tumor cells, and especially, the compounds can selectively act on lung cancer cells of EGFR L858R/T790 and EGFR E745 A750/T790M. Compared to wild type cancer cells, the IC50 of the compounds is 10 times, 100 times or even 1000 times higher. The compounds are a novel protein kinase inhibitor, which can overcome the drug resistance of EGFR-TKI and has selectivity.

Advancements in solid tumor (e.g., renal cell carcinoma) treatments and imaging are described. The advancements are based on nanoformulations that: (i) overcome deliverability issues associated with anti-cancer compounds; (ii) have increased targeted delivery to tumors, and hypoxic cores of tumors due to the presence of targeting ligands; (iii) have increased delivery to the hypoxic cores of tumors due to engineered shapes; (iv) provide synergistic treatment combinations; and/or (v) overcome cancer cell resistance to therapeutic treatments.

The invention relates to the technical field of biological medicines, specifically to a kit for detecting quantum dot nucleic acid of a bloodstream infection pathogen. The kit comprises a detecting membrane strip, a fluorescence detecting solution and a reaction solution, wherein the detecting membrane strip comprises a nylon membrane and a capture probe fixed to the nylon membrane; the fluorescence detecting solution comprises quantum dots for marking streptavidin which is coupled on the surface of the capture probe; the reaction solution comprises a reaction solution I, a reaction solution II, a reaction solution III and a reaction solution IV. The kit has the beneficial effects of being high in throughput, flexibility and specificity; the steps are fewer than the steps of the conventional color-developing gene chip; the detection time is obviously shortened; the cost is less than that of an organic fluorescence gene chip device; the kit is beneficial for clinical popularization.

The present invention provides a broad-spectrum malassezia-resistant natural product composition. The broad-spectrum malassezia-resistant natural product composition consists of tropolone, cinnamaldehyde and nisin. In-vitro drug sensitivity experiments prove that the tropolone, cinnamaldehyde and nisin have an obvious inhibition effect on malassezia, besides, the three materials have synergistic or addition effects, so that compounding of the three materials can reduce drug dosage, enhance a sterilization effect and prevent drug resistance. The composition can be made into drugs and daily chemical products which can be used for treating skin diseases caused by malassezia, such as seborrheic dermatitis, dandruff, etc. Compared with synthetic drugs, the natural product composition is strongin micro-organism-inhibiting ability, natural and free of toxicity, stable in property, small in damages to the environment, low in stimulation, obvious in effects, etc., and has wide application prospects.

The invention provides an N2-carbamylaryl-2-aminopyrimidine derivative and a medical application thereof. The N2-carbamylaryl-2-aminopyrimidine derivative provided by the invention comprises an optical isomer of the N2-carbamylaryl-2-aminopyrimidine derivative and pharmaceutically acceptable salt thereof. Pharmacodynamic research shows that the traditional Chinese medicine composition has no toxicor side effect, the compound has an FLT3 inhibitory activity. The proliferation inhibition activity is realized on various leukemia cell strains; a medium inhibition effect is achieved on breast cancer cells; moreover, the polypeptide is effective for multiple mutations of AML, such as internal tandem repeat mutation of a near-membrane structural domain and D835 point mutation of an activated ring in a kinase structural domain, almost has no inhibition effect on c-KIT, can overcome drug resistance brought by clinical point mutation, can reduce toxic and side effects of bone marrow inhibition,and can be applied to preparation of antitumor drugs. The structures of the general formulas Ia and Ib of the N2-carbamylaryl-2-aminopyrimidine derivative are shown in the specification,

The invention discloses a compound used as an estrogen-related receptor regulator and an application of the compound. The compound is a 1-hydrogen-1, 2, 3-triazole compound with a structure as shown in formula (I) as well as pharmaceutical acceptable salt or prodrug molecule. The compound as well as pharmaceutical acceptable salt or prodrug molecule can be used for preparing drugs for adjusting activity of estrogen relevant receptor (ERR), preventing and treating breast cancer (comprising diseases which are free of influence of an anti-estrogen method), prostatic cancer or metabolic diseases. The formula (I) is as shown in the specification.

The invention provides an application of a laetiporus sulphureus extract to preparation of a medicine for resisting hepatitis b virus. The laetiporus sulphureus extract is an extract obtained throughperforming refluxing on a laetiporus sulphureus fruiting body or mycelium with an alcohol solvent, wherein the alcohol solvent comprises ethanol, and the concentration of the ethanol is 95% and above.The laetiporus sulphureus and components thereof can prevent hepatitis b infection, treat hepatitis b infectious hepatitis, prevent liver cancer, treat hepatitis b relevance liver cancer, and preventrecurrence. The laetiporus sulphureus extract has positive effects in the overall process of pathological changes. The laetiporus sulphureus extract has important significance on solving the difficult problem of clinical treatment of hepatitis b infection and particularly solving the difficult problem of a hepatitis b relevance liver cancer technique.

The invention discloses an application of a compound Hu-17 alone or in combination with platinum drugs in preparing drugs for treating ovarian cancer and provides a new treatment protocol for patients with ovarian cancer, especially for those who relapse due to drug resistance. By adopting the treatment protocol, drug resistance of the patients carrying a P53 mutation or having P53 deletion to platinum drugs can be overcome. The pharmacologic mechanism is clear, implementation feasibility is high, and the application on which new hopes of curing patients who have ovarian cancer and relapse due to drug resistance will arise has great social significance and application value.