31 results about "Stat3 inhibitor" patented technology

The application discloses application of a pharmaceutical composition in treating cancer, wherein the pharmaceutical composition comprises a BCL-XL inhibitor and a HER2 targeted drug or comprises a BCL-XL inhibitor and a STAT3 inhibitor. The application provides medical use of the pharmaceutical composition according to the application for treating or preventing cancer. The application also provides a method for treating or preventing cancer, and provides a brand-new treatment scheme for the technical field of cancer treatment, and has important scientific significance and clinical application value.

The invention discloses a drug-loaded polymer, an STAT3 inhibitor composite nanoparticle, a preparation method of the STAT3 inhibitor composite nanoparticle and application of the STAT3 inhibitor composite nanoparticle in ophthalmic drugs. The STAT3 inhibitor composite nanoparticle comprises the drug-loaded polymer, an STAT3 inhibitor loaded on the drug-loaded polymer and thermosensitive lipidosome. The drug-loaded polymer is astaxanthin macromolecules, and the astaxanthin macromolecules are prepared by the following steps: in an inert atmosphere, performing condensation polymerization on astaxanthin and HPMDA, and then performing end capping reaction by using mPEG-OH. The compound is used for treating retinal neuron progressive death and ophthalmic diseases caused by axon loss of the retinal neuron progressive death, can show good ROS response and consumption performance, inhibits necrotic apoptosis, apoptosis and pyroptosis of cells, relieves cell death performance, and can show good drug slow release performance.

The invention discloses an application of a dihydroisoflavone derivative. Specifically, the invention provides application of a compound shown as a formula I or pharmaceutically acceptable salt thereof in preparation of an STAT3 inhibitor. The compound and STAT3 protein have high affinity, and the compound shows good activity on human cancer cells, especially on one or more of prostate cancer, head and neck cancer and human tongue squamous cell carcinoma at the cellular level, has the potential of being prepared into novel antitumor drugs and has good market prospects. # imgabs0 #

An exosomal composition is provided that includes a therapeutic agent encapsulated by an exosome. The therapeutic agent can be a phytochemical agent, a chemotherapeutic agent, or a Stat3 inhibitor. Pharmaceutical compositions that contain the exosomal compositions are also provided. Methods for treating an inflammatory disease or a cancer are further provided and include administering an effective amount of an exosomal composition to a subject in need thereof to thereby treat the inflammatory disorder or the cancer.

The invention belongs to the technical field of medicines, and particularly discloses an oral squamous cell carcinoma inhibitor and application thereof. The inhibitor takes rutin as an active component. In-vitro experiments prove that rutin can significantly inhibit proliferation, clone formation, migration and invasion ability of OSCC cells in a dose-dependent manner, and effectively induce cell apoptosis. The action mechanism of the rutin is as follows: the rutin can directly target STAT3 protein and inhibit phosphorylation of the STAT3 protein so as to regulate and control a downstream BCL2 / CASP3 apoptosis pathway, thereby playing a role in treating OSCC. Molecular docking results further show that rutin and STAT3 have strong binding capacity. The invention discloses a new application of rutin as an STAT3 inhibitor in treating oral squamous cell carcinoma, and provides a new strategy and a candidate compound for developing high-efficiency and low-toxicity OSCC treatment medicines.

The application discloses a synthesis method and application of a kind of phenothiazine leuco photo-caged compound, and relates to the application in the field of biological medicine.The compound is formed by using oxygen, sulfur and selenium containing phenothiazine leuco as matrix, connecting different functional groups by amide bond, especially STAT3 inhibitor molecules, forming a photo-controllable release platform that can be activated under near infrared light 650 or 660nm.In addition, the dye has good biocompatibility and low cytotoxicity, and experiments prove that it also has excellent imaging and treatment effect on specific tumor cells.

The invention belongs to the technical field of medicines, and particularly relates to an STAT3 inhibitor, a preparation method, a pharmaceutical composition and application of the STAT3 inhibitor. The compound is a compound as shown in a formula I or pharmaceutically acceptable salt, hydrate, solvate and isotope compound thereof. The compound provided by the invention can be used as a main component of a pharmaceutical composition, the aim of treating tumors is fulfilled by inhibiting the activity of STAT3, and the aim of treatment can be fulfilled by administering one or more compounds or pharmaceutical salts, stereoisomers or tautomers of the compounds of which the treatment or prevention is required to a patient. The structure of the formula I is shown in the specification.

The invention discloses application of an AKT inhibitor or an STAT3 inhibitor in preparation of a medicine for overcoming drug resistance of bladder cancer to an MEK inhibitor, and belongs to the field of biological medicine. Detecting the cell activity through an MTT method; a Western blot experiment is adopted to detect a key target protein or gene expression level, a bladder cancer drug-resistant cell ERK abnormal activation + STAT3 / Akt compensation activation mechanism is defined, p-ERK, p-STAT3 and p-Akt are locked as targets, the drug resistance of bladder cancer to an MEK inhibitor is overcome through an AKT inhibitor or an STAT3 inhibitor, the scheme can accurately inhibit abnormal pathways, reverse drug resistance and improve treatment sensitivity, and the method is safe and suitable for clinical application. A new direction is provided for patients with drug-resistant bladder cancer, and the clinical bottleneck of the MEK inhibitor is helped to be broken through.

Provided herein, in some embodiments, are solid-state forms of a compound represented by Formula (I), as free acid or base, or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions comprising one or more solid-state forms of a compound represented by Formula (I), as free acid or base, or a pharmaceutically acceptable salt or solvate thereof, and methods of use thereof.

Methods of using the small molecule STAT3 inhibitor LLL 12B in the treatment of cancer, such as triple-negative breast cancer (TNBC) and pancreatic cancer, either alone or in combination with additional therapeutic agents, such as PARP inhibitors and CDK inhibitors, are provided.

The application discloses a salicylaldehyde derivative and application thereof. The compound and pharmaceutically acceptable salt and ester thereof can inhibit the combination of STAT3 and phosphorylated polypeptide, and achieve the anti-tumor purpose. The salicylaldehyde derivative can be combined with the SH2 domain of target protein STAT3, and inhibit the combination of the target protein and phosphorylated polypeptide. Compound 25 shows good competitive inhibition activity. In the anti-proliferation activity of pancreatic cancer cells in vitro, the compound 25 has sub-micromolar anti-proliferation activity of pancreatic cancer cells, and can induce cancer cell apoptosis. In addition, the compound 25 can significantly inhibit the phosphorylation of STAT3 705 sites and 727 sites, can inhibit the proliferation of various tumor cells in vitro, and has low toxicity to normal cells. Therefore, the compound can be used for preparing a STAT3 inhibitor, and used for preparing a medicine for preventing and / or treating diseases related to tumors.

The present invention relates to the field of cancer. More specifically, the present invention provides compositions and methods for treating cancer by targeting YAP1 and STAT3 pathways. In a specific embodiment, the present invention provides a method for increasing sensitivity of cancer in a subject to chemotherapy and / or immunotherapy comprising the step of administering to the subject an effective amount of a YAP1 inhibitor and a STAT3 inhibitor.

Provided herein, in some embodiments, are methods of treating a cancer characterized by the presence of a mutant p53 protein in a subject in need thereof, comprising administering to the subject an effective amount of a STAT3 inhibitor.

Provided herein, in certain embodiments, are compounds of Formula I:or a pharmaceutically acceptable salt or a solvate thereof, compositions comprising a compounds of Formula I, or a pharmaceutically acceptable salt or a solvate thereof, and uses thereof such as in treating certain diseases or disorders (e.g., cancer, fibrosis, chronic inflammation).

Provided herein, in some embodiments, are methods of treating a subject diagnosed with a non-viral liver cancer, the method comprising administering to the subject an effective amount of a STAT3 inhibitor.

The invention relates to a Napabucasin derivative with double-target antitumor activity as well as a preparation method and application of the Napabucasin derivative. According to the invention, an STAT3 inhibitor Napabucasin is used as a parent nucleus, active structures such as zinc ion chelating group hydroxamic acid, o-phenylenediamine and alkane hydrazide of an HDAC inhibitor are introduced at the tail end of the STAT3 inhibitor Napabucasin through different Linkers, a series of Napabucasin derivative inhibitors with double-target antitumor activity are successfully obtained, the structural general formula of the Napabucasin derivative inhibitors is shown as (I), and pharmacological experiments show that the Napabucasin derivative inhibitors can be used for preparing antitumor drugs. The compound has high in-vitro anti-tumor activity, so that the compound can be used as an anti-tumor medicine. .

The present invention relates to the discovery and characterization of novel, potent, and efficient STAT3 inhibitors which are two benzothiophene analogs named SIMMPYRA1 (SIM1) and SIMMPYRA2 (SIM2), and the method of their production by an in silico high throughput screening study. The presently disclosed STAT3 inhibitors specifically target STAT3 unregulated or irregular activation as in various STAT3-related diseases such as Triple-negative breast cancer (TNBC), a devastating form of breast cancer with poor life expectancy. The present invention discloses these inhibitors as potential prevention and treatment options for TNBC demonstrated by marked downregulation of several STAT3-dependent targets primarily IL6 and RANTES in TNBC cells, inducing apoptosis and / or downregulating cell growth suppression in multiple TNBC cells, and stimulating cytotoxicity and promoting tumor regression in vivo in a patient-derived xenograft (PDX) mouse model, without causing off-target side effects and preventing STAT3 activation-driven pathogenesis.

The application relates to the technical field of pharmaceutical chemistry, in particular to a STAT3 inhibitor, a PROTAC molecule and a preparation method and application thereof. A novel STAT3 inhibitor is designed and synthesized as a ligand combined with a target protein, thalidomide is used as a ligand of an E3 ligase CRBN, a PROTAC molecule for targeted degradation of STAT3 protein is synthesized by connection of a connection chain Linker, the PROTAC molecule has a good degradation effect on STAT3 protein, and has good proliferation inhibition activity on various malignant tumor cells, for example, lung cancer cells, liver cancer cells and the like, and especially has a good industrial prospect in the application to the preparation of a drug for treating non-small cell lung cancer.

The invention belongs to the field of medicinal chemistry, and relates to a furo-quinoline diketone compound and medical application thereof. Specifically, the invention relates to a compound as shown in a formula (I), a prodrug, a stereoisomer or pharmaceutically acceptable salt, a hydrate or a crystal form thereof, a pharmaceutical composition thereof, a preparation method thereof and medical application thereof.

Provided herein, in some embodiments, are solid-state forms of a compound represented by Formula (I), as free acid or base, or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions comprising one or more solid-state forms of a compound represented by Formula (I), as free acid or base, or a pharmaceutically acceptable salt or solvate thereof, and methods of use thereof.

The present invention relates to a benzamide compound and a preparation method, use and pharmaceutical composition thereof. The benzamide compound represented by formula (I) is a STAT3 inhibitor, and can be used to prevent and / or treat a disease related to STAT3 activity, such as a tumor, autoimmune disease, renal disease, cardiovascular disease, inflammation, metabolic / endocrine dysfunction, and neurological disease.

The present invention relates to a composition for preventing or treating diabetes mellitus using a 4-component mixture of putrescine, glucosamine, nicotinamide, and a STAT3 inhibitor. It has been confirmed that blood glucose is stably regulated when a compound of the 4-component mixture according to the present invention is injected into the caudal vein of a diabetes mellitus-induced mouse. The compound can be practically and usefully used as a therapeutic agent for diabetes mellitus patients and patients exposed to diabetes mellitus risk.

The present invention relates to a solid dispersion including a heterocycle derivative, a method for preparing same, and a pharmaceutical composition including same. The solid dispersion including a heterocycle derivative comprises: as an active ingredient, a compound, which is a STAT3 inhibitor, represented by chemical formula 1, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof; and one polymer among hydroxypropyl cellulose (HPC), hydroxypropyl methylcellulose (HPMC), and a methacrylic acid-methyl methacrylate copolymer.

The invention relates to a compound as well as a composition and application thereof, the compound can be used for preparing an STAT3 inhibitor, and can also be used for preventing or treating diseases related to inhibition of STAT3, including but not limited to cancers, rheumatoid arthritis, Crohn's disease, atherosclerosis or inflammatory bowel disease and the like. The compound has the following structural formula,

The application discloses application of a STAT3 inhibitor combined with oxaliplatin in preparation of a drug for treating solid tumors with p-STAT3 activation or p-STAT3 low expression. The solid tumor with p-STAT3 activation is sensitive colorectal cancer. The solid tumor with p-STAT3 low expression is oxaliplatin-resistant colorectal cancer. The combination of the STAT3 inhibitor and the oxaliplatin has a good synergistic effect on the treatment of the colorectal cancer with p-STAT3 activation. Meanwhile, the combination of the STAT3 inhibitor and the oxaliplatin can increase the sensitivity of the colorectal cancer with p-STAT3 low expression to the oxaliplatin, enhance the role of the oxaliplatin in inhibiting the proliferation, invasion and migration of the CRC, obviously inhibit the growth rate of the CRC tumor in the body, and has a good synergistic effect on the colorectal cancer with p-STAT3 low expression and oxaliplatin resistance.

The invention discloses a JAK-STAT3 degradation agent and a preparation method and application thereof.The structure of the degradation agent is shown in the formula I. The compound can degrade JAK and STAT3 protein at the same time through the molecular glue effect, and compared with existing JAK-STAT3 inhibitors such as tofacitinib or ruxotinib, the degradation agent can directly down-regulate an IL6-JAK-STAT3 signal channel, and the degradation effect is good. According to the present invention, the compound can effectively inhibit the phosphorylation of STAT3, block the proliferation, the survival, the angiogenesis, the invasion, the metastasis and other processes of cancer cells, and reduce the levels of JAK1, JAK2, JAK3, STAT3 and pSTAT3, such that the compound has strong pathway inhibition activity compared with the traditional inhibitor.

The invention discloses an application of a glucaric acid 1, 4-lactone and lenvatinib composition in preparation of an STAT3 phosphorylation inhibitor, the pharmaceutical composition comprises an active component A and an active component B, the active component A is D-glucaric acid-1, 4-lactone, and the active component B is lenvatinib or a pharmaceutically acceptable salt thereof; the mass ratio of the D-glucaric acid-1, 4-lactone to the lenvatinib is 1 to (0.1 to 50). The pharmaceutical composition can be used for preparing STAT3 inhibitors, anti-liver cancer drugs and drugs for inhibiting immune escape of liver cancer cells. According to the pharmaceutical composition, the anti-tumor effect of lenvatinib is enhanced by inhibiting STAT3 phosphorylation and PD-L1 protein expression, and a new scheme is provided for solving the drug resistance problem of lenvatinib.

The invention discloses a screening method of a small molecule STAT3 inhibitor and application of the small molecule STAT3 inhibitor. The screening method comprises the following steps: obtaining an STAT3 protein-small molecule compound crystal structure from a Protein Data Bank database, and carrying out pretreatment on the STAT3 protein-small molecule compound crystal structure; a SiteMap module is adopted to search a protein surface binding pocket, and a pocket at an SH2 structural domain is selected to screen an STAT3 inhibitor; selecting the center of a butt joint box and setting the size of the butt joint box; selecting and downloading a to-be-screened compound library; compound library preprocessing, multi-mode molecular docking and MM / GBSA free energy calculation are performed in sequence in a virtual screening workflow mode, and sorting is performed according to combination free energy values from small to large; and a molecular dynamics simulation method of Binding Pose Metadynamics is adopted for further screening, so that a compound with potential activity is obtained.

The present invention relates to a solid dispersion comprising a heterocyclic derivative, a preparation method thereof, and a pharmaceutical composition comprising the same, wherein the solid dispersion comprising the heterocyclic derivative can comprise a compound represented by Formula 1, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as a STAT3 inhibitor as an active ingredient, and one polymer selected from the group consisting of hydroxypropyl cellulose (HPC), hydroxypropyl methyl cellulose (HPMC), and a methyl methacrylate-methyl methacrylate methyl ester copolymer.

The invention discloses a compound and application thereof, and the compound can be combined with an SH2 structural domain of a target protein STAT3 to inhibit the combination of the target protein and phosphorylated polypeptide so as to achieve the anti-tumor purpose. Pharmacological experiments prove that the compound disclosed by the invention achieves the anti-tumor purpose by inhibiting proliferation of tumor cells and inducing apoptosis of the tumor cells. The compound provided by the invention can be used for preparing STAT3 inhibitors and medicines for preventing and / or treating tumor-related diseases.