16 results about "Imatinib" patented technology

The invention belongs to the technical field of medicines. The invention relates to a plaster, in particular to a plaster containing anilinoprofen and a composition. The invention provides an externally applied medicine containing anilinoprofen or a composition containing anilinoprofen and iguratimod. Pharmacodynamic studies show that the aniline-ibuprofen single-prescription plaster can treat osteoarthritis (OA) and rheumatoid arthritis (RA), can effectively inhibit arthrocele and volume increase, remarkably reduces the level of proinflammatory factors, and improves the pathological score of joint tissue. After the anilinoprofen and the iguratimod are combined for use, the curative effect is further enhanced, multiple indexes are obviously superior to those of a single drug group, and an obvious synergistic interaction effect is shown. The iguratimod and anilinoprofen compound preparation disclosed by the invention is developed in an external form such as a gel plaster for the first time, an external compound system of anilinoprofen and iguratimod is innovatively constructed, a safe, effective and convenient novel local treatment choice is provided for OA / RA patients, especially people with oral taboo or needing long-term treatment, and the iguratimod and anilinoprofen compound preparation has good clinical transformation potential and application value.

The addition of a tyrosine kinase inhibitor, including but not limited to imatinib, in a dosage regimen in combination with tecovirimat provides superior results in the treatment of orthopox infections, including monkeypox infections or monkeypox disease. The unexpected results show that the combined administration of imatinib and tecovirimat provides synergistic reduction of monkeypox spread.

The application discloses a new preparation method of an intermediate of imatinib, and relates to the technical fields of medicines and chemical industry. The intermediate of imatinib, i.e. a-amino-2-methoxy-4-methanesulfonamido-5-phenoxyphenylacetophenone, is synthesized by taking 3-methanesulfonamido-4-phenoxyanisole and chloroacetyl chloride as raw materials, perfluoro-tert-butyl alcohol as a solvent, and D72 strong-acid macroporous resin as a catalyst, and then reacting with ammonia after a-chloro-2-methoxy-4-methanesulfonamido-5-phenoxyphenylacetophenone is synthesized. The application greatly improves the yield and purity, overcomes the shortcomings of the prior art in safety production, environmental protection and clean production, has a simple route, high reaction safety, convenient post-treatment, and effectively reduces the production cost, and is suitable for large-scale production.

The invention discloses a targeted protein degradation agent utilizing a ubiquitin-proteasome pathway as well as a preparation method and application of the targeted protein degradation agent, and belongs to the technical field of biological medicines. On the basis of a PROTAC (protein targeted degradation chimera) strategy and on the basis of imatinib, different Linkers are introduced to be connected with an E3 ubiquitin enzyme ligand Nutlin-3 derivative, a degradation tag is labeled on BCR-ABL cancer protein, and the degradation agent with the Bcr-Abl protein targeting capacity is constructed. A Western blot experiment shows that the targeted protein degradation agent shows a good degradation effect on the Bcr-Abl protein in K562 cells, and the compound WP shows a degradation effect on concentration dependence and time dependence of the Bcr-Abl protein. Tumor cell proliferation experiments show that the compound has certain inhibitory activity on K562 cells. Wherein when the Linker is dodecane-1, 12-diketone, the anti-proliferative activity is the best. An apoptosis experiment and a period experiment show that the targeted protein degradation agent can realize concentration-dependent promotion of cell apoptosis and retard cells in S and G1 / G0 periods.

This invention discloses an enzyme-sensitive PDC-type PROTAC modified with a human leukemia cell-targeting transmembrane peptide, its preparation method, and its applications, belonging to the field of tumor targeted therapy technology. This PDC-type PROTAC is composed of a hypoxia-inducible factor 1α (HIF-1α) protein fragment linked to imatinib via dodecanoic acid, and further modified with the human leukemia cell-targeting transmembrane peptide Cyclo-C9C-R and the cathepsin B-sensitive sequence GFLG. The modified PDC-type PROTAC can release the original drug under the catalysis of cathepsin B, with minimal impact on THP1 cell viability, but effectively inhibits the proliferation of K562 and KU812 cells, degrades target proteins, induces apoptosis, and affects the cell cycle. This gives the PDC-type PROTAC significant advantages in the preparation of anti-tumor drugs, particularly showing promising application prospects in the development of drugs targeting human chronic myeloid leukemia cells and human peripheral blood basophilic leukemia cells, opening up a new field for PROTAC drug development.

The invention provides an osteoarthritis analgesic enteric capsule containing a non-steroidal anti-inflammatory component, and relates to the technical field of pharmaceutical preparations. The osteoarthritis analgesic enteric capsule containing the non-steroidal anti-inflammatory component comprises an enteric capsule shell and a content, and is characterized in that the content comprises iguratimod and celecoxib which serve as active components, and the content is composed of two independent enteric coated pellets: A type pellets, B type pellets, C type pellets and D type pellets, comprising a celecoxib-containing drug-loaded pellet core and an enteric coating layer coating the celecoxib-containing drug-loaded pellet core, the B-type pellet comprises a drug-loaded pellet core containing iguratimod and an enteric coating layer coating the drug-loaded pellet core; the A-type pellets and the B-type pellets are physically mixed according to a certain proportion and then are filled in the same enteric capsule shell. Celecoxib and iguratimod are adopted, Celecoxib provides rapid and powerful pain relief, iguratimod inhibits inflammation pathways from multiple targets and provides cartilage protection, and the combination of Celecoxib and iguratimod realizes the synergistic effect of treating both symptoms and root causes.

The application discloses a method for determining the concentration of sofosbuvir in blood plasma and screening a non-isotope labeled internal standard, wherein anlotinib, imatinib, olaparib, osimertinib and pralsetinib are used as internal standards, quantitative analysis is performed by combining LC-MS / MS with protein precipitation pretreatment. The internal standard screening method is screened from candidate compounds by systematically evaluating four dimensions of protein precipitation compatibility, matrix effect, detection stability and extraction recovery, and an internal standard consistent with the behavior of the measured substance is screened. The application solves the problem of the lack of commercial isotope internal standards for sofosbuvir, and provides a reliable and efficient detection and internal standard screening scheme.

The invention discloses an organic ionic liquid formed by mixing double drugs and application thereof.The organic ionic liquid with different molar ratios is prepared from imatinib (IM) and 3-bromopyruvic acid (BP), and the optimal molar ratio is obtained according to in-vitro toxicity experiments and theoretical calculation on tumor cells; the organic ionic liquid with the proportion is encapsulated into engineered bacterium exosome-liposome hybrid vesicles (IM-BP-coated HV-Pep-PEG), and a double-drug co-delivery system is constructed. And a better synergistic treatment effect is achieved while the dosage is reduced. Meanwhile, the outer membrane vesicle part of the carrier can reverse a tumor immune microenvironment, promote tumor cell immunogenic death, and realize an anti-tumor effect of immunotherapy-assisted double-drug synergistic treatment.

The invention discloses a targeted protein degradation agent utilizing an autophagy-lysosome pathway as well as a preparation method and application of the targeted protein degradation agent, and belongs to the technical field of degradation agent preparation. The preparation method comprises the following steps: carrying out nucleophilic substitution reaction on a GW5074 derivative and a linker arm precursor to obtain a GW5074 derivative-linker arm intermediate, and coupling the GW5074 derivative-linker arm intermediate with demethylated imatinib to obtain the targeted protein degradation agent utilizing the autophagy-lysosome pathway. The protein degradation agent disclosed by the invention is relatively few in preparation steps, easy to synthesize and relatively high in yield, and can be used for preparing medicines for treating cancers, particularly antitumor medicines for treating chronic granulocytic leukemia.

The application belongs to the field of medicine, and particularly relates to a novel quinoline compound containing 6-oxo-1-substituted phenyl-1,6-dihydropyridazine-3-carboxamide and application thereof. The novel quinoline compound containing 6-oxo-1-substituted phenyl-1,6-dihydropyridazine-3-carboxamide has a structure of general formula (I). The application also relates to the compound of general formula (I) having a strong inhibitory effect on c-Met kinase, and further relates to the use of the compound and a pharmaceutically acceptable salt thereof in the preparation of a drug for treating and / or preventing a disease caused by abnormally high expression of c-Met kinase, in particular, in the preparation of a drug for treating and / or preventing cancer. The compound of the application is particularly suitable for preparing a drug for treating and / or preventing gastric cancer, colon cancer, lung cancer, gastrointestinal stromal tumor and imatinib-resistant human gastrointestinal stromal tumor.

This invention discloses an electrochemiluminescence aptamer sensor for imatinib detection, its preparation method, and its detection application. Addressing the problems of cumbersome procedures and insufficient sensitivity in existing detection methods, this invention constructs the sensor through the following steps: first, gold is deposited on the surface of a glassy carbon electrode; then, double-stranded DNA, bovine serum albumin, imatinib solutions of different concentrations, and a carboxyl-modified activated signal probe solution are incubated sequentially to obtain a sensor for imatinib detection. This invention also discloses a method for detecting imatinib using this sensor. This method combines the high sensitivity of electrochemiluminescence technology with the high specificity of aptamers, possessing advantages such as high sensitivity, low detection limit, wide linear range, rapid detection, simple operation, and small sample volume. It has been successfully applied to the detection of clinical blood samples taken with imatinib.

The invention relates to the technical field of pharmaceutical preparations, in particular to Iguratimod tablets with improved dissolution rate and stability and a preparation method of the Iguratimod tablets. The iguratimod tablet comprises iguratimod, a microcrystalline cellulose 101 and 302 mixed filler, polyvinylpolypyrrolidone, a polysorbate 80 and starch sodium octenylsuccinate composite surfactant, an HPMC (Hydroxy Propyl Methyl Cellulose) adhesive, a sodium stearyl fumarate lubricant and L-glutamine. The method comprises a process route of wet granulation, fluidized bed drying, size stabilization, total mixing and tabletting. According to the application, the dissolution rate of Iguratimod in media with different pH values can be remarkably improved, the chemical stability is guaranteed, and the adverse reaction of gastrointestinal tracts is reduced. The Iguratimod tablet with high dissolution rate, high stability and low irritation is constructed by accurately designing the types, proportions and process parameters of auxiliary materials, the technical scheme of the Iguratimod tablet is not obvious, and experiments prove that the Iguratimod tablet is remarkably superior to the prior art in the aspects of dissolution rate, related substance control and gastric mucosa protection.

The invention belongs to the technical field of biological medicines, and particularly relates to application of gambogic acid combined with imatinib in preparation of a medicine for treating gastrointestinal stromal tumor. The gambogic acid and the imatinib are jointly applied to treatment of the gastrointestinal stromal tumor, and compared with an existing single imatinib treatment scheme, the gambogic acid and the imatinib can form a synergistic anti-tumor effect, so that the sensitivity of gastrointestinal stromal tumor cells to the imatinib is effectively improved, the problem that the drug effect is insufficient possibly existing when a single drug is used is solved, and the curative effect of the gastrointestinal stromal tumor is improved. And the overall treatment effect is improved. The gambogic acid and imatinib are combined to further inhibit the activity and proliferation of gastrointestinal stromal tumor cells and induce tumor cell apoptosis, so that the gastrointestinal stromal tumor resisting effect is enhanced. Therefore, the invention provides a new strategy and choice for the drug treatment of gastrointestinal stromal tumor, and has important clinical application value.

The invention discloses a Bcr-Abl protein degradation agent based on a hydrophobic label technology as well as a preparation method and application thereof, and belongs to the technical field of preparation of protein degradation agents. The preparation method comprises the following steps: coupling demethylated imatinib with alpha-bromo-carboxylic acid tert-butyl ester to obtain target protein ligands with connecting arms with different lengths; exposing carboxyl through a protecting group removing reaction to obtain a target protein ligand with carboxyl and a connecting arm; a target protein ligand with carboxyl and a connecting arm and 5-norbornene-2-methylamine are subjected to an amide condensation reaction, and the Bcr-Abl protein degradation agent based on the hydrophobic label technology is obtained. The preparation method of the protein degradation agent is simple, easy to implement and high in yield, and the protein degradation agent can be used for preparing drugs for treating or preventing cancers, especially for preparing anti-tumor drugs taking Bcr-Abl as a target spot.

The invention discloses a novel 4-methyl benzamide compound containing a benzenesulfonyl structure and application thereof, and belongs to the technical field of medicines, the 4-methyl benzamide compound containing the benzenesulfonyl structure has a structure shown in a general formula (I), and can be used for pharmaceutical salt formation by adding acid. Pharmacological activity screening results show that the compound has a remarkable inhibition effect on a human chronic myelogenous leukemia cell strain K562, a human chronic myelogenous leukemia cell imatinib-resistant cell strain K562 / G01, a human gastrointestinal stromal tumor cell strain GIST882 and a human gastrointestinal stromal tumor cell imatinib-resistant cell strain GIST1210, and has a good prospect in development and application of antitumor drugs.

The invention discloses an application of an anti-malarial drug primaquine phosphate in preparation of drugs for treating BCR-ABL positive leukemia and breast cancer and a drug combination composition, and discovers that the anti-malarial drug primaquine phosphate has obvious effects of resisting BCR-ABL + leukemia and breast cancer, and has obvious anti-BCR-ABL + leukemia and breast cancer in the cellular level. The PRQ can significantly inhibit the growth of a BCR-ABL + leukemia cell line and an imatinib drug-resistant BCR-ABL + leukemia cell line, significantly inhibit the growth of breast cancer cells and induce ferroptosis of the breast cancer cells, and further researches find that the PRQ can degrade wild or mutant BCR-ABL proteins in a targeted manner. At the patient level, the PRQ is found to be capable of inhibiting the formation ability of primary cell colonies of wild-type or mutant patients with the BCR-ABL + leukemia, and at the animal level, the PRQ is found to have an obvious inhibiting effect on the progress of the BCR-ABL + leukemia.