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42 results about "VEGFR Inhibitor" patented technology

Biomarkers for response to tyrosine kinase pathway inhibitors in cancer

Copy number gains detected in tumors and associated with drug sensitivity and resistance in vivo and in vitro can be used as biomarkers to select, predict and monitor drug treatment outcomes in cancer patients treated with tyrosine kinase inhibitors. Methods to identify patients with NSCLC or other malignancies who are more likely to benefit from tyrosine kinase inhibitors such as VEGF or VEGFR inhibitors when used either as monotherapy or in combination with other therapies such as chemotherapy or EGFR inhibitors, and who are in the advanced stages of disease and / or who have undergone adjuvant therapy are also provided herein.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST

Thienopyrimidine and furopyrimidine derivative, its preparation method and application in medicines

The invention discloses a thienopyrimidine and furopyrimidine derivative, its preparation method and its application in medicines. The derivative is a compound shown as general formula I, general formula II, general formula III or general formula IV. The thienopyrimidine and furopyrimidine pyrimidine derivative provided in the invention has an obvious EGFR (epidermal growth factor receptor) inhibitory activity, and some of the compounds also have an obvious inhibitory activity on VEGFR (vascular endothelial growth factor receptor), so that the thienopyrimidine and furopyrimidine pyrimidine derivative can be expected to be developed into tyrosine kinase EGFR or / and VEGFR inhibitors, which can be used for preparation of drugs preventing or treating diseases related to EGFR and / or VEGFR. Therefore, the derivative provided in the invention provides a new development direction and approach for developing novel tyrosine kinase inhibitor drugs that have low resistance or can alleviate early inhibitor resistance, and has wide application prospect and medicinal value.
Owner:JIANGSU DESANO PHARMA

Application of VEGFR inhibitor in preparation of anti-Alzheimer's disease medicine

The invention discloses an application of a VEGFR inhibitor in preparation of an anti-Alzheimer's disease medicine. The VEGFR inhibitor is axitinib and an analogue thereof. It is found that axitinib has an unexpected curative effect on Alzheimer's disease, and Alzheimer's disease model animal in-vivo experiments prove that after administration of axitinib, beta-amyloid protein deposition in the brain of a model animal is significantly reduced, the content of acetylcholin esterase is reduced, the oxidative stress level and inflammatory response of the lesion part of the model animal are relieved, the learning and memory ability and learning and memory behaviors of the model animal on space and direction are improved, and the curative effect is obviously higher than that of a clinical first-line treatment drug donepezil. The axitinib and the analogue thereof provide a new means for clinical treatment of the Alzheimer's disease, and the axitinib and the analogue thereof are high in human body safety, low in price and easy to prepare. According to the invention, non-intracranial administration mode is adopted, safety is high, administration is convenient and fast, and patient compliance is high. The application of a VEGFR inhibitor in preparation of an anti-Alzheimer's disease medicine has wide market prospects and great social significance.
Owner:ZHEJIANG UNIV

Nano-drug taking irinotecan as carrier as well as preparation method and application of nano-drug

The invention discloses a nano-drug taking irinotecan as a carrier and a preparation method of the nano-drug. The metabolic toxicity of the irinotecan is reduced; and meanwhile, the application range of the irinotecan as a small molecular carrier is expanded. The nano-drug is mainly composed of the irinotecan, a COX-2 inhibitor or a VEGFR inhibitor and a dispersing agent. The COX-2 inhibitor, the VEGFR inhibitor and the irinotecan can be prepared into the nano-drug through a pi-pi accumulation effect, a hydrophobic effect, an electrostatic effect, a hydrogen bond effect and the like under the assistance of a proper dispersing agent. Based on physical forces, such as pi-pi accumulation, the COX-2 inhibitor or the VEGFR inhibitor exerts efficacy as a prototype drug. The nano-drug is prepared through a solvent conversion method; the method is simple; the quality is controllable; the drug loading capacity is high; proliferation of metastatic colorectal cancer cells is effectively inhibited; angiogenesis is reduced; and the microenvironment is improved.
Owner:CHINA PHARM UNIV

Combination of antibody-drug conjugate and kinase inhibitor

A pharmaceutical composition wherein an antibody-drug conjugate in which a drug-linker of the represented formula (wherein A represents a connecting position to an antibody) is conjugated to the antibody via a thioether bond and a kinase inhibitor (at least one selected from the group consisting of a CDK4 / 6 inhibitor, an mTOR inhibitor, a PI3K inhibitor, an AKT inhibitor, an ERK inhibitor, an MEK inhibitor, an RAF inhibitor, a CDK1 inhibitor, a CDK2 inhibitor, a CHK1 inhibitor, a WEE1 inhibitor, a PLK1 inhibitor, an Aurora kinase inhibitor, a Bcr-Abl inhibitor, an Src inhibitor, an EPH inhibitor, a VEGFR inhibitor, a KIT inhibitor, an RET inhibitor, a PDGFR inhibitor, an FGFR inhibitor, a BTK inhibitor, an FLT3 inhibitor, an ALK inhibitor, a JAK inhibitor, an MET inhibitor, a CSF-1R inhibitor, an NTRK inhibitor, an EGFR inhibitor, and an HER2 inhibitor) are administered in combination, and / or a method of treatment.
Owner:DAIICHI SANKYO CO LTD

Preparation method of VEGFR inhibitor tevozanib

The invention relates to a preparation method of a VEGFR (vascular endothelial growth factor receptor) inhibitor tevozanib. Compared with the prior art, according to the preparation method, the compound shown in the formula 1 and the compound shown in the formula 2 are selected to react, the reaction reagent compound shown in the formula 3 is prepared firstly, then the reaction reagent compound shown in the formula 3 and the hydroxyl of the compound shown in the formula 4 are subjected to the substitution reaction, the reaction site of the reaction is single, the yield is excellent, and reaction purification is convenient; the method provided by the invention has the advantages of simple operation process, low purification cost and high overall yield, and is suitable for industrial large-scale production of bulk pharmaceutical chemicals, and the process steps for synthesizing and preparing the tevozanib are simplified.
Owner:武汉九州钰民医药科技有限公司
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