27 results about "Etoposide" patented technology

The invention relates to the technical field of antibacterial preparations, and discloses an application of etoposide in an antibacterial preparation and the antibacterial preparation, the antibacterial preparation is a biofilm inhibitor, and etoposide inhibits formation of a biofilm or destroys the formed biofilm by down-regulating gene expression of the bacterial biofilm, so that the antibacterial effect of etoposide is improved. The biofilm is a biofilm of streptococcus mutans ATCC700610, and the biofilm is a biofilm of streptococcus mutans The antibacterial preparation comprises an antibacterial drug, an oral care product, a medical coating and an anti-caries preparation. MIC and MBC determination tests, growth curve tests, crystal violet staining tests, bacterium living / death staining tests and qRT-PCR tests prove that etoposide can effectively down-regulate biofilm related gene expression (such as gtfB, gtfC, gtfD and the like), inhibit formation of a bacterial biofilm or destroy a formed biofilm, and achieve an antibacterial effect.

Disclosed herein are compositions and methods for treating cancer, specifically extensive-stage small-cell lung cancer (ES-SCLC), through the administration of a combination therapy. In some embodiments, the method comprises administering plinabulin, one or more immune checkpoint inhibitors, including but not limited to pembrolizumab, and a regimen of etoposide with a platinum-based agent (EP). The disclosed methods enhance tumor reduction, prolong progression-free survival, and improve overall treatment efficacy compared to traditional therapies.

The invention discloses an application of an ARRB1 inhibitor in preparation of a tumor drug resistance reversal agent or a tumor drug sensitizer. It is found that by reducing ARRB1 expression, the sensitivity of human breast cancer cells to etoposide can be improved, the drug resistance of breast cancer etoposide can be reversed, and an ARRB1 inhibitor can be combined with an anti-tumor drug etoposide for use to improve the treatment effect. The invention provides a new direction for research and development of drugs for overcoming breast cancer treatment drug resistance, and has important clinical application value and development value.

The invention provides a pharmaceutical composition and application thereof in preparation of medicines for treating tumors. The pharmaceutical composition comprises the orbitrazine fumarate, a second active agent and pharmaceutically acceptable auxiliary materials. The second active agent comprises at least one of tamoxifen, irinotecan hydrochloride, sorafenib, cis-platinum, doxorubicin hydrochloride, paclitaxel and etoposide. The scheme provided by the invention has a remarkable synergistic anti-tumor effect, and a combined medication scheme is expected to provide a safer and more effective treatment choice for tumor patients, so that the pharmaceutical composition has an important clinical application value.

The invention belongs to the technical field of protein, and aims to solve the problem that the application range of spider silk particles as a drug carrier is limited due to the fact that the spider silk particles are in negative net charge under a neutral condition and can only load drugs with positive charges or neutral charges at present. The novel recombinant spider silk protein is prepared on the basis of an N connection sequence of araneus ventricosus MaSp1, has positive net charge under a neutral pH value, can load a negatively charged drug, and expands the application range of the spider silk protein as a drug carrier; and a drug release test result shows that the recombinant spider silk protein is superior to MaSp2-based silk protein particles in the aspect of etoposide delivery.

The invention discloses application of deaminotyrosine in improvement or prevention and treatment of muscular atrophy, and relates to the technical field of biological medicines. The invention finds that in the cellular level, DAT can effectively resist C2C12 myoblast senescence induced by etoposide; in a dexamethasone-induced C2C12 myotube atrophy model, DAT not only inhibits myotube diameter reduction from the form, but also down-regulates mRNA expression of key atrophy genes Atrogin-1 and MuRF-1 from the molecular level, and inhibits excessive activation of a ubiquitin-proteasome system; in-vivo animal experiments prove that DAT can reverse aging-related dyskinesia of rapidly-aged SAMP8 mice, and gait parameters of the rapidly-aged SAMP8 mice are all remarkably improved. According to the invention, a complete evidence chain from cells to the whole is constructed, and the DAT is proved to improve the senescent skeletal muscle atrophy through multiple ways of intervening cell senescence, antagonizing protein degradation, improving muscle microenvironment and the like, and shows important potential application value.

The present invention relates to a pharmaceutical composition for preventing or treating cancer, containing 2,6-dichloro-4-(4-(4-hydroxycyclohexylamino)-7H-pyrrolo[2,3-D]pyrimidin-5-yl)phenol as an active ingredient. It has been ascertained that the present invention inhibits the formation of mammospheres in a breast cancer cell line and, when compared to anticancer drugs sorafenib and etoposide, which are topoisomerase inhibitors widely used in lung cancer, ovarian cancer, colon cancer, melanoma and the like, exhibits remarkable effects greater than or equal to those of the anticancer drugs sorafenib and etoposide. In addition, a compound of example 1, according to the present invention, exhibits synergistic anticancer effects when combined with radiotherapy or other anticancer drugs in a breast cancer cell line and a liver cancer cell line, and thus can be developed as an anticancer drug or a food exhibiting excellent effects in the treatment of cancer.

To provide a method for extending progression-free survival (PFS) in a patient with extensive-stage small cell lung cancer (ES-SCLC).SOLUTION: This method comprises treating a patient with extensive-stage small cell lung cancer with a) a human anti-PD-L1 antibody and b) etoposide and a platinum-based therapeutic agent (EP).SELECTED DRAWING: None

The invention discloses a series connection synthesis method of 3, 4, 5-trimethoxy benzaldehyde. The 3, 4, 5-trimethoxybenzaldehyde is an important medicine and fine chemical engineering intermediate, and can be used for synthesizing a sulfanilamide synergist trimethoprim and an anti-cancer drug etoposide. According to the invention, 3, 5-dibromo-4-hydroxybenzaldehyde is taken as a raw material, a sodium methoxide-methanol solution is taken as a methoxylation reagent, dimethyl carbonate is taken as a methylation reagent, and tandem synthesis of 3, 4, 5-trimethoxybenzaldehyde is realized by adding a plurality of catalysts under normal pressure. The method does not need to separate a reaction intermediate or use a high-pressure reaction container, and has the advantages of simplicity, convenience and safety in operation, low reagent toxicity, higher yield, short reaction time and the like.

The present invention relates to a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PCL S-PAC-PEG S) micelle in which osimertinib, etoposide, and docetaxel are encapsulated, and used thereof. Specifically, the present invention relates to a pharmaceutical composition for preventing or treating cancer, wherein osimertinib, which is a target therapeutic agent, and etoposide and docetaxel, which are both anticancer chemotherapeutic drugs, are encapsulated in a Soluplus® polymer to form micelles, whereby anticancer activity can be effectively induced through an improvement in the solubility of the poorly soluble drug in water and a synergistic action between the drugs. The pharmaceutical composition for cancer treatment according to the present invention enables effective solubilization of osimertinib, etoposide, and docetaxel by encapsulating the poorly soluble drugs in micelles formed using the PCL-PVAc-PEG (Soluplus®) polymer, and thus can be advantageously used as an intravenous injection. With the advantage of avoiding first-pass metabolism in the liver, unlike oral dosage forms, intravenous injection can reduce unnecessary loss of drugs and also increase bioavailability compared to oral dosage forms, and thus is an effective administration method capable of expecting a high effect with the same amount of drugs. Therefore, development of such a formulation allows effective administration of osimertinib, etoposide, and docetaxel. In addition, the composition of the present invention can effectively treat non-small cell lung cancer having an EGFR-sensitive mutation while preventing the development of anticancer drug resistance, which can be caused by single drug administration, by using a targeted therapeutic agent and chemotherapy in combination. Furthermore, the composition of the present invention employs a biocompatible polymer as a material of the micelle and thus has an advantage of being safe for the human body. Moreover, by combining osimertinib, etoposide, and docetaxel at a specific molar ratio and encapsulating same in Soluplus® micelles, the composition of the present invention has excellent encapsulation efficiency of three kinds of drugs and has high monodispersibility having a consistent particle size of 50-60 nm. Thus, the composition can maintain consistent product quality and has excellent formulation stability.

The invention provides a novel application of melia diol. The melia diol has a remarkable senescence cell removing capability in a bleomycin induced cell senescence model, an etoposide induced cell senescence model and a replicative cell senescence model; the activity of anti-apoptotic protein Bcl-2 can be obviously inhibited; the neem diol has no obvious liver and kidney toxicity while selectively removing senescent cells; the neem diol has the effects of remarkably lightening wrinkles on the back skin of a photoaged mouse, improving the transdermal moisture loss condition of the back skin of the photoaged mouse, increasing the moisture content of the back skin of the photoaged mouse, reducing the thickness of an epidermal layer and improving the fracture and content of collagenous fibers in a corium layer; the method has a wide application prospect in preparation of anti-aging products.

The present disclosure provides the first asymmetric total synthesis and target identification of the curcusone natural products. The novel convergent synthesis is built upon a cheap and abundant chiral pool molecule (8) and features a thermal [3,3]-sigmatropic rearrangement and an FeCl3-promoted global hydrolysis / adol condensation cascade to rapidly construct the critical cycloheptadienone core. By performing chemoproteomics with the alkyne probe 37, we identified the previously “undruggable” oncogenic protein BRAT1 as a key cellular target of 1d. Furthermore, 1d inhibits BRAT1 in cancer cells, thereby reducing cancer cell migration, increasing susceptibility to DNA damage, and inducing chemosensitization to the approved drug etoposide. Compound 1d is the first known small-molecule inhibitor for BRAT1, a master regulator of the DDR and DNA repair. Composition matters and methods of uses are within the scope of this disclosure.

The present invention relates to a pharmaceutical composition for preventing or treating cancers, which contains 2, 6-dichloro-4 - (4 - (4-hydroxycyclohexylamino) -7H - pynolo [2, 3-D] pyrimidin-5-yl) phenol as an active ingredient.SOLUTION: The present invention inhibits the formation of mammospheres in breast cancer cell lines, and when compared with the anticancer drugs sorafenib and etoposide, which are widely used topoisomerase inhibitors in lung cancer, ovarian cancer, colon cancer, melanoma and the like, it has been found to exhibit an effect more marked than or equal to the anticancer drugs sorafenib and etoposide. In addition, the compound of Example 1, according to the present invention, exhibits synergistic anticancer effects when combined with radiotherapy or other anticancer drugs in breast cancer cell lines and liver cancer cell lines, and thus can be developed as an anticancer drug or food exhibiting excellent effects in the treatment of cancer.SELECTED DRAWING: Figure 12

The invention relates to the technical field of medicines, and particularly discloses a pharmaceutical composition based on an IRF7-PTEN signal axis and application of the pharmaceutical composition in spinal cord injury. According to the application, a plurality of spinal cord injury single cell sequencing data sets are integrated, and the interferon regulatory factor 7, namely IRF7, is screened and verified to be a key hub gene for regulating and controlling apoptosis of astrocytes. Knock-down IRF7 significantly inhibits astrocyte apoptosis induced by etoposide, and rotation IRF7 can reverse the effect. In mechanism, the IRF7 promotes cell apoptosis by negatively regulating a PTEN pathway, and the PTEN inhibitor SF1670 can block the IRF7 overexpression mediated apoptosis promoting effect. On the basis, the invention provides a pharmaceutical composition taking the signal axis as a target spot, and the active ingredient of the pharmaceutical composition can be an IRF7 inhibitor or a PTEN inhibitor; the invention also discloses application of the inhibitor in preparation of drugs for treating spinal cord injury. The application provides a new target spot and an effective intervention strategy for treatment of spinal cord injury.

The invention discloses an application of etoposide in preparation of anti-rabies virus drugs, and proves that the clinical anti-tumor drug etoposide has remarkable anti-rabies virus activity on cell and animal levels for the first time, and plays an antiviral role in vitro and vivo by inhibiting virus replication and reducing virus gene and protein expression. The invention provides a brand-new medical application for etoposide, namely provides a new medicine and a technical scheme for preparing a rabies virus, and has important significance for solving the problem of clinical treatment of rabies.

The invention discloses amine alkoxy cotinine compounds (I), pharmaceutically acceptable salts thereof, a preparation method of the amine alkoxy cotinine compounds, a pharmaceutical composition of the amine alkoxy cotinine compounds and application of the amine alkoxy cotinine compounds in preparation of drugs for treating and / or preventing nervous system diseases. Comprising but not limited to vascular dementia, Alzheimer's disease, frontotemporal dementia, Prion disease, dementia with Lewy bodies, Parkinson's disease, Huntington's disease, HIV-related dementia, multiple sclerosis, amyotrophic lateral sclerosis, neuropathic pain, cerebral arterial thrombosis, hemorrhagic stroke, nerve injury caused by cerebral trauma and other diseases;

The invention discloses an innovative application of pseudo-ginsenoside RT5 in preparation of leukocyte increasing drugs and tumor treatment support drugs. The medicine is used for treating or relieving myelosuppression leucopenia induced by chemotherapeutic medicines (such as etoposide). The invention creatively discovers that the pseudo-ginsenoside RT5 can remarkably improve the level of neutrophil caused by myelosuppression and effectively relieve the side effect of chemotherapy, and experiments prove that the pseudo-ginsenoside RT5 remarkably prolongs the survival time under the influence of chemotherapy drugs. The effectiveness of the method is analyzed based on an etoposide myelosuppression model and survival time of zebrafish fries. As the pseudo-ginsenoside RT5 is derived from a natural component of homology of medicine and food (such as American ginseng), the pseudo-ginsenoside RT5 has the advantages of high safety and suitability for long-term drug combination, the chemotherapy compliance and the curative effect can be remarkably improved, and a novel efficient and low-toxicity support drug is provided for overcoming myelosuppression in tumor chemotherapy.

The present invention relates to new stable oral pharmaceutical formulations of etoposide toniribate, lyophilized composition of etoposide toninbate solutions and methods of treating cancer using said formulations and compositions.

This invention provides a method and apparatus for continuous flow synthesis of the key intermediate MMPE, etocoxib. The method includes the following steps: First, a 4-methanesulfonylphenylacetic acid solution and a first stream of tert-butylmagnesium chloride solution are subjected to a first-step continuous flow synthesis to obtain reaction solution A; then, reaction solution A and a methyl 6-methylnicotinate solution are subjected to a second-step continuous flow synthesis to obtain reaction solution B; next, reaction solution B and a second stream of tert-butylmagnesium chloride solution are combined to obtain the final reaction solution C; the obtained reaction solution C is post-processed to obtain the desired MMPE product. A microreactor is selected as the reactor for the reaction. The method provided by this invention significantly simplifies the preparation process, greatly shortens the reaction time, and achieves excellent yield and purity, while also exhibiting excellent reproducibility.

The present invention provides a new use of cycloeugenol. The cycloeugenol has a significant ability to eliminate senescent cells in a bleomycin-induced cell senescence model, an etoposide-induced cell senescence model, and a replicative cell senescence model; can significantly inhibit the activity of the anti-apoptotic protein Bcl-2; cycloeugenol selectively eliminates senescent cells while having no obvious liver or kidney toxicity; cycloeugenol can significantly reduce the expression levels of aging biomarkers such as P16 and P21 in naturally aged mice, improve the antioxidant capacity of naturally aged mice, restore the abnormal number of immune cells caused by natural aging, and significantly reduce skin wrinkles in naturally aged mice. The cycloeugenol has a clear anti-aging effect and has broad application prospects in the preparation of anti-aging products.

A method for treating cancer, especially small-cell lung cancer with a compound of formula I, e.g. compound A, the pharmaceutically acceptable salt or the solvate thereof, as a focal adhesion kinase inhibitor. A pharmaceutical combination or a kit comprising the compound and a chemotherapy agent, e.g. topotecan, etoposide, or carboplatin.

The application discloses application of Rineterkib combined with a DNA damaging agent in preparation of a SLFN11-deficient tumor treatment drug. Rineterkib can significantly restore the sensitivity of SLFN11-deficient tumor cells to DNA damaging agents (such as 2-fluoroadenine, cisplatin, bleomycin and etoposide). Further research shows that Rineterkib can achieve a synergistic killing effect on SLFN11-deficient tumor cells by blocking DNA damage repair, inducing G2 / M phase arrest and promoting cell apoptosis.

A treatment of lung cancer, particularly small cell lung cancer, in a human subject using an anti-PD-1 antibody and optionally a chemotherapy is provided. In some embodiments, the small cell lung cancer is an advanced (e.g., locally advanced) or diffusive (e.g., stage III or stage IV), non-resectable or metastatic (e.g., with liver, lung or lymph node metastasis, e.g., with 2, 3 or more metastatic sites) lung cancer. In some embodiments, the chemotherapy is carboplatin and / or cis-platinum, and optionally further etoposide. In some embodiments, the SCLC is a small cell carcinoma. In some embodiments, the SCLC is a complex small cell carcinoma. In some embodiments, the treatment is a first-line treatment. In some embodiments, the claimed therapies are effective in the treatment of SCLC. In some embodiments, the human subject is a responder to a treatment by at least one measurement of a response to the treatment.

The invention relates to the technical field of preparation of etocrilene, and discloses a preparation method of etocrilene, which sequentially comprises the steps of condensation reaction, rough preparation, refining, drying and packaging. According to the preparation method of the etocrilene provided by the invention, the vacuum degree and the temperature are synergistically optimized, and the reaction time is shortened and the generation of by-products is inhibited mainly by applying the vacuum degree of-0.088 MPa, controlling the temperature in stages, reducing the reaction activation energy and promoting the full contact of ethyl cyanoacetate and benzophenone. The vacuum environment can timely remove moisture generated by the reaction and push the balance to move towards the positive reaction direction, so that the yield is obviously improved. By optimizing the raw material ratio, the nucleophilic activity of benzophenone can be enhanced by a composite catalytic system of acetic acid and ammonium acetate, so that the raw material conversion rate is greatly improved compared with that of a traditional process. Through the synergistic effect of the processes of all the steps, the problems of low purity and insufficient yield in the prior art are systematically solved.

The invention provides a new application of cyclodecenol. The cyclodecenol has a remarkable senescence cell removing capability in a bleomycin induced cell senescence model, an etoposide induced cell senescence model and a replicative cell senescence model; the activity of anti-apoptotic protein Bcl-2 can be obviously inhibited; cycloeudecenol has no obvious liver and kidney toxicity while selectively removing senescent cells; the cycloeudecenol can obviously reduce the expression level of aging biomarkers such as P16 and P21 in naturally aged mice, improve the antioxidant capacity of the naturally aged mice, recover abnormal immune cell quantity caused by natural aging and obviously reduce skin wrinkles of the naturally aged mice, has a definite aging delaying effect, and can be used for preparing natural aging mice. The method has a wide application prospect in preparation of anti-aging products.

The invention relates to the technical field of drug detection, and discloses a method for detecting beta-lactam compound residues in a drug, which comprises the following steps of: extracting and diluting beta-lactam compounds in the drug through a uniform pretreatment process (adopting 50% acetonitrile) in combination with optimized LC-MS / MS conditions (including specific chromatographic columns, gradient elution procedures and mass spectrum parameters); synchronous quantitative detection of eight beta-lactam compounds (covering cephalosporin and penem) in five raw material medicines (exemestane, etoposide, abiraterone acetate, emtricitinib and cilnimod) with remarkable structural difference is realized, and the limit of quantitation is as low as 0.008 ppm. According to the method, the detection sensitivity is remarkably improved, the trace residue monitoring requirement is met, pretreatment steps are simple and universal, conditions do not need to be adjusted according to different raw material medicines, the detection efficiency and the method applicability are greatly improved, and the problems that the sensitivity is insufficient and the universality is poor in the prior art are effectively solved.

The invention relates to application of a compound for inhibiting SASP in preparation of an anti-aging product, and belongs to the technical field of new application of known medicines. The compound for inhibiting the SASP is pinocembrin, and the pinocembrin is used for inhibiting replicative senescence of cells and cell stress senescence induced by etoposide, adriamycin and H2O2. The invention researches that pinocembrin realizes an anti-aging effect by inhibiting characteristic senescence-related secretion phenotype factors of senescence cells, reducing expression of senescence-related cell cycle arrest marker genes and relieving the senescence condition of the cells, and does not have an effect of eliminating and damaging the cells.