180 results about "Antineoplastic Drugs" patented technology

The invention discloses an anti-tumor drug tablet stability prediction method based on multi-source data fusion, and particularly relates to the field of pharmaceutical preparation stability prediction, and the method comprises the following steps: S1, data acquisition; s2, extracting multi-dimensional characteristic parameters; s3, constructing a stability prediction reference model; s4, calculating a real-time attenuation index; s5, determining a deviation threshold range; s6, analyzing a stability deviation index; s7, dynamically updating a prediction result; according to the method, accurate prediction of content attenuation, related substance growth and disintegration time limit change indexes is realized through integration of multi-source data, construction of a stability prediction reference model, simple trend analysis not limited to a single factor, key influence factor marking, critical threshold setting and theoretical attenuation curve fitting; the accuracy and timeliness of stability prediction of antitumor drug tablets are effectively improved, and a scientific basis is provided for drug validity period evaluation and quality risk management and control.

The invention discloses a naphthyridine mycin compound generated by streptomyces as well as a preparation method and application thereof, and belongs to the field of medicines. The naphthyridine mycin compound and the analogue of the naphthyridine mycin compound are prepared by fermenting, extracting, separating and purifying streptomyces lageri W307 (the preservation number of the strain is CGMCC (China General Microbiological Culture Collection Center) No.32721). The invention further discloses a preparation method of the naphthyridine mycin compound and the analogue of the naphthyridine mycin compound. The invention further provides application of the eight naphthyridine mycin compounds in preparation of anti-tumor drugs and application of the eight naphthyridine mycin compounds in preparation of antibacterial drugs, and potential anti-tumor drugs and antibacterial drugs are provided clinically.

The invention discloses an embolism microsphere and a preparation method thereof.The embolism microsphere is prepared through the following steps that a polycarboxylate microsphere is prepared by combining a free radical polymerization method and an emulsion polymerization method, and the polycarboxylate microsphere is obtained; and saponifying and hydrolyzing the polycarboxylate microspheres to hydrolyze the polycarboxylate microspheres to obtain hydroxyl polymer microspheres, and introducing an acidic group onto the hydroxyl polymer microspheres to obtain the embolism microspheres containing both the hydroxyl group and the acidic group. The embolism microsphere disclosed by the invention realizes high loading capacity and controllable release of the anti-tumor drug, realizes accurate embolism in blood flow, and improves the treatment effect of the drug.

The invention relates to the field of antitumor drugs, in particular to a thiophene acetyl tetrahydro-beta-carboline compound and application thereof. The thiophene acetyl tetrahydro-beta-carboline compound or the pharmaceutically acceptable salt thereof, and the pharmaceutical composition containing the compound can be used for preparing medicines for preventing and / or treating various cancers. The cancer is at least one of breast cancer, lung cancer, osteosarcoma, melanoma, gastric cancer, pancreatic cancer, kidney cancer, glioma and ovarian cancer. Activity screening is carried out on various compounds, it is found for the first time that the 12 compounds provided by the invention have remarkable broad-spectrum inhibitory activity on various human cancer cell lines, and key candidate compounds are provided for developing novel anti-cancer drugs.

A closed, gravity-fed burette for intravenous (IV) fluid delivery and flush system supporting multiple input combinations for simplicity and standardization. Able to handle both hazardous and non-hazardous drugs, this system may incorporate plastic and elastomeric materials that are resistant to the effects of antineoplastic materials in conjunction with a hazardous air filter module while still integration compatible with electronic peristaltic pumps for finer control of flow rate and when the IV infusion recipient's physical position is not compatible with a gravity-fed flow. The buoyant-activated shuttle valve enables the AutoStart function providing steady flush of the IV line to the patient for optimized vein patency from the Primary IV fluid feed. This Primary line works in conjunction with a Secondary IV fluid feed and a needleless connector Drug Port for multiple feed and flush conditions directed by way of a monoblock design supporting combinations of rotary, toggle, and check valves.

The application belongs to the technical field of antitumor drugs, and discloses an iron complex as well as a preparation method and application thereof.The preparation steps of the iron complex are as follows: 1, reacting 2-hydrazinylbenzothiazole, a ketone compound and a solvent to obtain a ligand; and 2, reacting the ligand, ferric chloride and a solvent, and then cooling and crystallizing to obtain the iron complex.The obtained iron complex can effectively induce cancer cell ferroptosis, can effectively inhibit the growth of breast cancer, lung cancer, liver cancer or glioma, has high selectivity, has small toxicity to normal cell strains, and has better treatment effect compared with existing clinical drugs, such as cisplatin.

The application discloses an 8-hydroxyquinoline anticancer zinc (II) complex and a synthesis method and application thereof. The 8-hydroxyquinoline anticancer zinc (II) complex is synthesized by taking 5,7-diiodo-8-hydroxyquinoline, 5,7-dichloro-8-hydroxyquinoline, 5-chloro-7-iodo-8-hydroxyquinoline, 5,7-dibromo-8-hydroxyquinoline and 5-chloro-8-hydroxyquinoline as a first ligand and taking 4,4'-dimethoxy-2,2'-bipyridine, 4,4-di-tert-butyl-2,2-bipyridine, 5,5'-dimethyl-2,2-bipyridine, 2,2-bipyridine and 4,4'-dimethyl-2,2'-bipyridine as auxiliary ligands. The 8-hydroxyquinoline anticancer zinc (II) complex has good inhibiting effect on SK-OV-3CR cells of an ovarian cancer drug-resistant strain, is higher than that of cisplatin drugs, overcomes drug resistance of clinical drugs, has potential medicinal value and can be used for preparation of various antitumor drugs.

The application discloses oripramine derivatives, a preparation method and pharmaceutical compositions and application thereof, wherein the oripramine derivative is a compound with the shown structure or a medicinal salt thereof, wherein R is selected from any one of hydrogen, deuterium and substituted or unsubstituted alkyl, alkenyl, alkynyl, heteroalkyl, heteroalkenyl, heteroalkynyl, cycloalkyl, heterocyclyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl or heterocyclylalkyl. Experiments prove that the oripramine derivative has higher anti-inflammatory activity and lower toxicity compared with existing oripramine, can be applied as an active ingredient in the preparation of an anti-inflammatory disease, a nervous system disease or an antitumor drug, provides a new thought and method for preparing a novel oripramine derivative drug with better curative effect and lower toxicity, and has a wide application prospect.

The present invention discloses an antitumor pharmaceutical composition based on immune checkpoint blockade and its application, which comprises paroxetine hydrochloride and a T cell enhancer, which is at least one of vitamin E and thymosin. Through a series of in vitro and in vivo experiments, the present invention has first discovered that cannabidiol and paroxetine hydrochloride can effectively reduce the expression of PD-L1 on the surface of tumor cells, block the PD-1 / PD-L1 signaling pathway, and enhance the tumor cell killing effect of T cells. Based on this, the addition of a T cell enhancer can further increase the number and activity of T cells, significantly enhancing the killing ability of T cells after immunosuppression is released, thereby significantly enhancing the antitumor effect of the drug. The components of the pharmaceutical composition of the present invention, cannabidiol, paroxetine hydrochloride, vitamin E, and thymosin, exert a synergistic effect, improving the antitumor effect.

The invention discloses a 5-bromoindole-2-carboxylic acid methyl ester derivative as well as a preparation method and application thereof in a protein inhibitor, and relates to the technical field of synthesis and preparation of inhibitors. According to the 5-bromoindole-2-carboxylic acid methyl ester derivative, compared with a contrast product, the synthetic route steps of the prepared 5-bromoindole-2-carboxylic acid methyl ester derivative are simpler and more convenient, structural modification and preparation are easier, the application range of a substrate is widened, the yield of the product is increased, and the yield of the product is increased. The differentiated requirements on the molecular structure novelty in the field of kinase inhibitors can be met. An epidermal growth factor receptor (EGFR) inhibitor prepared from the 5-bromoindole-2-carboxylic acid methyl ester derivative is higher in inhibition efficiency on biological activity, the physiological solubility is improved more remarkably, a more excellent and stable target binding result can be shown, and the EGFR inhibitor can be used for preparing an epidermal growth factor receptor (EGFR) inhibitor. The application effect of the compound in scenes such as antitumor drug development and the like is favorably improved.

The invention relates to the technical field of anti-cancer chemical drugs, in particular to a thiadiazole tetranuclear copper complex with anti-tumor and antibacterial activity and a preparation method and application of the thiadiazole tetranuclear copper complex. The chemical formula of the complex is [Cu4 (C3H3S2N2) 2 (C3H4S2N2) 4], the complex is synthesized from ligand thiadiazole and CuX, X is I or Br, and copper in the obtained complex is + 1 valence. The complex shows a good cytotoxic effect on breast cancer cells MCF-7, is likely to play a toxic effect by inducing apoptosis, ferroptosis, copper death and other ways, has a good antibacterial effect, has potential medicinal value, and is expected to be developed into a new generation of anti-tumor drugs with antibacterial properties.

To provide a type I receptor tyrosine kinase inhibitor.SOLUTION: Or a pharmaceutically acceptable salt thereof. Specific examples thereof include N - (4 - ([1,2,4] triazolo [1, 5-c] pyrimidin-7-yloxy) - 3-methylphenyl) - 5 - (3 - (dimethylamino) azetidin-1-yl) - 6-methoxyquinazolin-4-amine.SELECTED DRAWING: None

The application belongs to the technical field of antitumor drugs, and particularly relates to an AuNRs@L / D-Ag2S QDs complex, a preparation method and application thereof. Sodium polystyrene sulfonate is electrostatically adsorbed on AuNRs to obtain 1-PSS-AuNRs; polyallylamine hydrochloride is electrostatically adsorbed on 1-PSS-AuNRs to obtain 2-PAH-AuNRs; polyallylamine hydrochloride is electrostatically adsorbed on 2-PAH-AuNRs to obtain a non-chiral nanomaterial; and the non-chiral nanomaterial is covalently crosslinked with L / D-Ag2S QDs to obtain the AuNRs@L / D-Ag2S QDs complex. The application combines the efficient photo-thermal conversion characteristics of AuNRs with the chiral-dependent targeting and potential fluorescence imaging ability of chiral Ag2S quantum dots by constructing a complex structure, so that a novel nanodiagnostic and therapeutic agent with efficient photo-thermal performance and chiral selectivity is obtained.

The invention discloses a phenoxazine skeleton-containing drug small molecule and application thereof, and belongs to the technical field of synthesis of heterocyclic compounds and antitumor drugs, the phenoxazine skeleton-containing drug small molecule has an inhibition effect on HepG2 and A549, a phenoxazine derivative 7c with the third site connected with a methoxy group at the tail end of a phenoxazine structure benzene ring has a better overall effect, and the phenoxazine skeleton-containing drug small molecule can be applied to preparation of antitumor drugs. The inhibition rates of the compound on HepG2 and A549 are respectively 87.67% and 94.23%. 7g of the phenoxazine derivative of which the methyl ester structure is connected to the third site of the phenoxazine structure only has an obvious effect on A549, and the inhibition rate in A549 cells is 96.00%.

The application discloses a porphyrin-eugenol derivative with antitumor activity, uses DPBF to detect the yield of singlet oxygen, and in-vitro antitumor activity test shows that the compound has good activity. The porphyrin-coumarin compound can realize the synergistic treatment of phototherapy and chemotherapy, in addition, the insertion of metal Zn in the porphyrin can also enhance the antitumor activity of the compound. Thus, the compound can be used as an active ingredient of an antitumor drug, and has good development and application prospect.

The application belongs to the technical field of medicine, and relates to a use of minocycline in preparation of an antitumor synergist. The minocycline, as the antitumor synergist, has a synergistic effect with 5-fluorouracil and gemcitabine, significantly enhances the curative effect of an antitumor drug, reduces the dosage of the antitumor drug, and reduces side effects of the antitumor drug on the body or damage of the antitumor drug to normal tissue cells.

The invention belongs to the technical field of medicines, and relates to an amide compound based on a hydrophobic labeling technology and preparation and application thereof. The structural general formula H of the target product is shown in the specification, or pharmaceutically acceptable salts, solvent compounds or hydrates of the target product. The compound provided by the invention has dual mechanisms of inhibiting polymerization and degradation of tubulin, has an effect of inhibiting tumor proliferation, and has a good prospect in the aspect of development of antitumor drugs.

The invention relates to the technical field of drug monitoring, and mainly relates to a method for detecting multiple antitumor drugs and metabolites in human plasma through liquid chromatography-tandem mass spectrometry and application of the method. The medicine to be detected is prepared from cevaltinib, loratinib, vomitinib, amitinib, sovantinib, anlotinib, glutamitinib, emtricitinib, N-demethylated vomitinib and N-demethylated emtricitinib; s2, preparing a calibration product and a quality control product, and preparing a working curve concentration table; s3, carrying out pretreatment on the calibration product and the quality control product obtained in the step S2; s4, carrying out liquid chromatography-tandem mass spectrometry detection on the pretreated liquid; and S5, performing methodological verification on the detection method. The detection method has the advantages of high sensitivity, good detection result accuracy, simple and rapid detection process, short analysis time and the like, and is suitable for detection of large-flux samples.

The application discloses a high-activity 8-hydroxyquinoline rhodium complex in vivo and in vitro and a synthesis method and application thereof. The 5,7-dichloro-8-hydroxy-2-methylquinoline, dichloro (pentamethylcyclopentadienyl) rhodium (III) dimer, methanol, dimethyl sulfoxide and triethylamine are taken, and under a closed condition, the reaction is carried out at 80 DEG C for 3 days; after being cooled to 37 DEG C, filtration and drying are carried out, and the 5-chloro-8-hydroxyquinoline rhodium complex is obtained. The 5-chloro-8-hydroxyquinoline rhodium complex has obvious inhibiting effect on SK-OV-3 and SK-OV-3 / DDP cancer cells, shows superior antitumor activity, and has small toxicity to normal HL-7702 cells; the 5-chloro-8-hydroxyquinoline rhodium complex has potential medicinal value and is expected to be used for preparation of various antitumor drugs.

This invention discloses a hyaluronic acid-phenylboronic acid-methotrexate antitumor conjugate and its preparation method in the field of drug preparation technology. First, hyaluronic acid is activated with carboxylic acid, then subjected to an amidation reaction with 3-aminophenylboronic acid to obtain a hyaluronic acid-phenylboronic acid conjugate. Next, methotrexate is activated and added to the hyaluronic acid-phenylboronic acid mixture, followed by stirring to obtain the hyaluronic acid-phenylboronic acid-methotrexate antitumor conjugate. The preparation method of this invention is simple. While the three drugs exert their respective effects, the introduction of phenylboronic acid enhances the targeted antitumor effect of the drug. The combined use of hyaluronic acid and phenylboronic acid further reduces the toxic side effects of methotrexate and improves the biocompatibility, bioavailability, and degradability of the resulting drug, making it suitable for application in the preparation of antitumor drugs.

The present application relates to a kind of 3-(2H-benzopyran-3-yl)-5-phenyl-1,2,4-oxadiazole derivative purposes, 3-(2H-benzopyran-3-yl)-5-phenyl-1,2,4-oxadiazole derivative structure as shown in formula I, this 3-(2H-benzopyran-3-yl)-5-phenyl-1,2,4-oxadiazole derivative has the potential to be developed as anti-radiation drug and antitumor drug.

The invention relates to diarylamine compounds containing a dimethyl phosphine oxide structure as well as a preparation method and application of the diarylamine compounds. The compounds have a structural formula as shown in a general formula (I). The invention relates to a compound shown in a general formula (I), which has a strong effect of inhibiting L858R / T790M / C797S drug-resistant mutant EGFR kinase, and also relates to application of the compound and pharmaceutically acceptable salt thereof in preparation of drugs for treating and / or preventing diseases caused by drug-resistant mutation of EGFR kinase, the invention particularly relates to application in preparation of medicines for treating and / or preventing cancers. The invention also provides a preparation method of the compounds, a pharmaceutical composition containing the compounds and application of the pharmaceutical composition. The compound is especially used for preparing drugs for treating and / or preventing lung cancer, and has good antitumor drug development and application prospects.

The application discloses a 2,2'-biquinoline-4,4'-dicarboxylic aliphatic amino acid derivative, and a preparation and application thereof, and belongs to the technical field of medicines.The structure of the 2,2'-biquinoline-4,4'-dicarboxylic aliphatic amino acid derivative is shown in the following formula: wherein RNH is selected from the group consisting of structures that are stable, have low toxicity, have antitumor activity, and can be used as effective components of antitumor drugs for antitumor treatment.The preparation process of the 2,2'-biquinoline-4,4'-dicarboxylic aliphatic amino acid derivative is simple, and the 2,2'-biquinoline-4,4'-dicarboxylic aliphatic amino acid derivative is easy to be industrialized when being used for preparing antitumor drugs.

The invention discloses application of a small molecule compound in targeting TOPBP1 protein, and belongs to the technical field of biological medicine. The application verifies that various small molecular compounds, namely diclofenac sodium, zaltoprofen, quinine and adamantine acetic acid, can be combined with the BRCT 7-8 structural domain of the TOPBP1, so as to target the TOPBP1 protein, and the dissociation equilibrium constant of the combination is between 100 and 250 mu M. And through AI model prediction, X-ray crystallography technology and the like, the combined action mechanism is disclosed. The application proves that diclofenac sodium, zaltoprofen, quinine and adamantane acetic acid as a class of small molecular compounds have the potential of serving as candidate molecules of antitumor drugs.

The application relates to an amphiphilic block copolymer and a preparation method and application thereof, the amphiphilic block copolymer has a general structure formula as shown in (I), the amphiphilic block copolymer provided by the application is terminated by Boc-phenylalanine for polymer terminal hydroxyl groups, the stability of the micelles formed is obviously improved in and out of the body, the amphiphilic block copolymer can be made into a drug loading system together with an antitumor drug and a pharmaceutically acceptable auxiliary material, and has a higher application prospect.

The application relates to application of C-methylated high isoflavone compounds in preparation of antitumor drugs and belongs to the technical field of drug application. In order to solve the problem that the existing antitumor activity is not much reported, the application of C-methylated high isoflavone compounds in preparation of antitumor drugs is provided, the C-methylated high isoflavone compounds are selected from compounds shown in the following formula 1 or formula 2: the C-methylated high isoflavone compounds or pharmaceutically acceptable salts thereof are used as active ingredients for preparation of antitumor drugs for preventing and / or treating adrenal pheochromocytoma (PC-12) and / or human brain astrocytoma (U-87MG). The C-methylated high isoflavone compounds have the advantages of high activity and high inhibition capacity, can be extracted from polygonatum sibiricum and have good drug safety.

Disclosed are methods of treating cancer with a tri-agent therapy. The methods include a cancer treatment regimen with two or three different antineoplastic medications, including tamoxifen, gefitinib, and vinorelbine (TGV). The cancer treatment regimen can include sequential and / or concurrent administration of tamoxifen, gefitinib, and vinorelbine. The cancer treatment regimen can include sequential and / or concurrent administration of tamoxifen and gefitinib as adjuvants to a prescribed treatment. The cancer treatment regimen can be cyclical or can be a continuous metronomic treatment with metronomic dosing. The cancer treatment regimen can be cyclical and then can be followed by a continuous metronomic treatment with metronomic dosing.

The invention belongs to the field of medicines, and particularly relates to a triazole compound as well as a preparation method and application thereof, the triazole compound is a compound shown in a formula (I) or pharmaceutically acceptable salt, and the triazole compound is novel in structure. Cell activity tests prove that the compound has a good potential antitumor drug application value, and a brand new drug choice can be provided for development of antitumor and anti-inflammatory drugs.

The application belongs to the technical field of medicine, and specifically discloses a glycyrrhetinic acid injectable hydrogel as well as a preparation method and application thereof. The preparation method of the glycyrrhetinic acid injectable hydrogel comprises the following steps: glycyrrhetinic acid and choline hydroxide are added into pure water, heated and stirred to fully react, and a mixed solution is obtained; the mixed solution is first spin-evaporated and then vacuum-dried to obtain glycyrrhetinic acid-choline; the glycyrrhetinic acid-choline is added into pure water, heated to completely dissolve and cooled at room temperature to form an injectable hydrogel. The hydrogel is used for preparing an antitumor drug in an injectable dosage form. In the application, the glycyrrhetinic acid and the choline hydroxide are self-assembled into a hydrogel with a three-dimensional network microstructure by losing one molecule of water without adding any cross-linking agent and organic solvent. The hydrogel can quickly recover to the original gel state after injection, and the problems of low drug loading, low bioavailability and difficult degradation existing in the prior art are solved.