95 results about "Epidermal growth factor receptor tyrosine kinase" patented technology

The present invention relates to quinazoline containing zinc-binding moiety based derivatives that have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.

Radiolabeled epidermal growth factor receptor tyrosine kinase (EGFR-TK) irreversible inhibitors and their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) and as radiopharmaceuticals for radiotherapy are disclosed.

The invention discloses an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, and the structural formula of the inhibitor is shown as in the formula (I). The invention further discloses an application of any compound shown as in the formula (I) and pharmacy-acceptable salt of the compound. The invention further provides a medicine compound for curing, and the medicine compound comprises the compound shown as in the formula (I) and an EGFR modifier.

The present invention relates to quinazoline containing zinc-binding moiety based derivatives that have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.

Novel epidermal growth factor receptor tyrosine kinase (EGFR-TK) irreversible inhibitors, pharmaceutical compositions including same and their use in the treatment of EGFR-TK related diseases or disorders are disclosed. Novel radiolabeled EGFR-TK irreversible inhibitors as their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) and as radiopharmaceuticals for radiotherapy are further disclosed.

Methods using mass spectral data analysis and a classification algorithm provide an ability to determine whether a head and neck squamous cell carcinoma (HNSCC) patient is likely to benefit from a drug targeting an epidermal growth factor receptor pathway, including small molecule epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) and monoclonal antibody EGFR inhibitors.

Novel epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitors, pharmaceutical compositions including same and their use in the treatment of EGFR-TK related diseases or disorders are disclosed. Novel radiolabeled EGFR-TK inhibitors as their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) and as radiopharmaceuticals for radiotherapy are further disclosed. The disclosed EGFR-TK inhibitors comprise a polyalkylene glycol moiety and / or a hydroxy-containing moiety and are characterized by improved solubility, biostability and bioavailability. Processes of preparing the disclosed EGFR-TK inhibitors and of radiolabeling same, via, for example, one-step radiosyntheses, are also disclosed.

The invention discloses a medicinal composition for resisting non-small cell lung cancer. The active components of the medicinal composition comprise an artemisinin derivative and EGFR-TKI (epidermal growth factor receptor-tyrosine kinase inhibitor), wherein the artemisinin derivative is selected from one of dihydroartemisinin, artesunate, artemether and arteether; and the EGFR-TKI is selected from one of gefitinib, erlotinib, afatinib and osimertinib. The invention also discloses application of the medicinal composition to preparation of medicines for treating and resisting the non-small cell lung cancer. When the medicinal composition provided by the invention is used for treating the non-small cell lung cancer, the medicinal effect which is more excellent than that of the singly used EGFR-TKI can be achieved, the sensitizing effect is achieved, the problem of partial medicine resistance of the non-small cell lung cancer EGFR-TKI is solved, and a scientific basis is provided for the development of new medicines.

Cancer treatment with a combination of an Epidermal Growth Factor Receptor tyrosine kinase inhibitor and an Interleukin-6 inhibitor.

The invention relates to a test method of KRAS gene mutation for screening and assessing therapeutic effects of molecular targeted agents, which is characterized by the following specific steps: acquiring serum or tumor tissue samples of testees, extracting genomic DNA, testing a No.2 exon of the KRAS gene, designing corresponding site-specific primers and adopting experimental schemes, reagents and report generation systems for sequence determination and assessing the effectiveness of EGFR tyrosine kinase inhibitors used for treating cancer individuals by simultaneously testing and analyzingwhether mutation exists on the No.2 exon of the individual KRAS gene. The method has the advantage of being used for application of the EGFR tyrosine kinase inhibitors used for treating cancer individuals.

The invention relates to a medicament composition containing sorafenib, hepatocyte growth factor receptor (cMet) inhibitors and epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors and application thereof in preparing medicaments for treating lung cancer, colon cancer, liver cancer, kidney cancer, stomach cancer, encephaloma, sarcoma, pancreatic cancer, ovarian cancer, breast canceror prostatic cancer. The medicament composition has remarkable synergistic effect, improves the curative effect of the medicament, decreases the administration dosage and reduces the occurrence of side effects.

The invention discloses epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKI) NXGF and NXGH with antineoplastic activity and a preparing method and application thereof, and belongs to the field of biological medicine. The brand new EGFR TKI are obtained by optimizing and improving the chemical structure of Pelitinib and named NXGF (the formula I) and NXGH (the formula II) respectively. It is shown through research that the synthesized EGFR TKI-NXGF and the synthesized EGFR TKI-NXGH can effectively inhibit proliferation of tumor cells, have a higher proliferation inhibiting effect on the mutation EGFR lung cancer cell line HCC827 compared with Pelitinib, and thus can be clinically applied as an antineoplastic agent. The invention further discloses the preparing method of the EGFR TKI NXGF and NXGH with antineoplastic activity. By proposing the EGFR TKI NXGF and NXGH with antineoplastic activity, and the preparing method and application thereof, an effective technical means is provided for treating tumors and especially non-small cell lung cancer.

The present invention relates to quinazoline containing zinc-binding moiety based derivatives of Formula (IV) below.These compounds have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and are useful in the treatment of EGFR-TK related diseases and disorders such as cancer. These compounds may further act as HDAC inhibitors.

The invention discloses epidermal growth factor receptor tyrosin kinase inhibitors IRSF and IRSH with antitumor activity, a preparation method and application thereof. By optimization and improvement of a gefitinib chemical structure, brand-new EGFR TKI (epidermal growth factor receptor tyrosin kinase inhibitors) named as IRSF (shown as formula I) and IRSH (shown as formula II) are obtained. According to researches, the IRSF and IRSH are higher in water solubility and fewer in toxic and side effects and have high inhibition activity on mutant EGFR non-small-cell lung cancer, and the IRSF and IRSH inhibit phosphorylation of cancer cell epidermal growth factor receptor tyrosin kinase to prevent downstream signal path activation so as to promote tumor cell apoptosis. In addition, the invention further discloses a method for preparing the epidermal growth factor receptor tyrosin kinase inhibitors with antitumor activity. The epidermal growth factor receptor tyrosin kinase inhibitors IRSF and IRSH with antitumor activity, the preparation method and application thereof provide effective technical means for tumor treatment, especially treatment of the non-small-cell lung cancer.

Cancer treatment with a combination of an Epidermal Growth Factor Receptor tyrosine kinase inhibitor and an Interleukin-6 inhibitor.

The invention discloses an EGFR (epidermal growth factor receptor) TKI (tyrosine kinase inhibitor) BF3-AZD9291 with anti-tumor activity as well as a preparation method and application thereof, and belongs to the field of biomedicines. By optimizing and improving the chemical structure of AZD9291, a fully new EGFR TKI is obtained, and is named as BF3-AZD9291 (formula I). Proofed by study, the synthesized EGFR TKI BF3-AZD9291 has the advantages that the drug resistance of tumor cells can be effectively inhibited; compared with AZD9291, the stronger drug resistance inhibiting function is realizedfor the mutation EGFR tumor cell line H1975T790M, and the EGFR TKI BF3-AZD9291 can be used as an anti-tumor reagent in clinical application. The invention also discloses the method for preparing theEGFR TKI BF3-AZD9291 with the anti-tumor activity. The EGFR TKI BF3-AZD9291 provides an effective technical method for the treatment of tumors, especially non-small cell lung cancer. (The formula I isshown in the attached figure.).

A purpose of the invention is to solve the problems of drug resistance, high toxic and side effects and the like of epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) in non-smallcell lung cancer (NSCLC) treatment and provide a pharmaceutical composition for targeted therapy of lung cancer, wherein the active ingredients of the pharmaceutical composition are quercetin metal coordination compound and osimertinib or a pharmaceutically acceptable salt thereof, and the quercetin metal coordination compound is selected from quercetin copper, quercetin manganese and quercetin zinc. The pharmaceutical composition provided by the invention has good water solubility, low drug resistance, high curative effect and few side effects.

The present invention relates to a fast screening method for identifying large quantities of new substances which can effectively inhibit the activity of EGFR tyrosine kinase, and comprises attaching an EGFR tyrosine substrate, which is activated by reaction with EGFR tyrosine kinase, to a protein chip and reacting it with a compound pool consisting of EGFR tyrosine kinase, ATP, Mg2+ and a single candidate library, to provide superior and rapid screening for tyrosine kinase inhibitors.

The invention discloses an EGFR degradation agent containing a 2, 8, 9-trisubstituted-9H-purine structure fragment and salt and application of the EGFR degradation agent, and belongs to the technical field of anti-cancer drugs. The compound is novel in structure, has remarkable activity of degrading epidermal growth factor receptor (EGFR) tyrosine kinase, has remarkable inhibitory activity on growth of human lung cancer cells HCC827 (EGFR) single mutation and H1975 (EGFR) double mutation, can be used for treating cancers related to EGFR mutation, and has the advantages of easily available synthetic raw materials and easily realized synthetic method.

The invention discloses an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, and the structural formula of the inhibitor is shown as in the formula (I). The invention further discloses an application of any compound shown as in the formula (I) and pharmacy-acceptable salt of the compound. The invention further provides a medicine compound for curing, and the medicine compound comprises the compound shown as in the formula (I) and an EGFR modifier.

The invention provides a pharmaceutical composition containing small-molecule targeted drug gefitinib and application of the pharmaceutical composition to the preparation of antitumor drugs. The pharmaceutical composition is characterized by comprising active components including ursolic acid and gefitinib. When the mass ratio of ursolic acid to gefitinib is 10-20:1-25, the ursolic acid and gefitinib can be combined and coordinated to resist the proliferation of tumor cells. The pharmaceutical composition has the advantages that due to the fact that the epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitor gefitinib and the efficient and low-toxicity antitumor natural ursolic acid are combined, targeted inhibition of the tumor cells can be achieved, the proliferation of the tumor cells can be inhibited in a coordinated manner, the toxic and side effects of drugs can be reduced, tumor treatment effect can be increased, and the pharmaceutical composition is applicable to the preparation of antitumor drugs.

The invention relates to the field of tumor drug treatment, in particular to application of an autophagy inhibitor for overcoming drug resistance of epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) in treatment of non-small cell lung cancer. The autophagy inhibitor is chloroquine. The EGFR-TKI is erlotinib. The method and application has the beneficial effects that autophagy is involved in development of the EGFR-TKI drug resistance of non-small cell lung cancer, the autophagy inhibitor chloroquine can overcome the drug resistance of the EGFR-TKI by inhibiting autophagy, and combination of the chloroquine and the erlotinib can effectively kill lung cancer cells resistant to the erlotinib inside and outside bodies.

The invention discloses a nano-drug sustained release preparation for treating a malignant tumor and a preparation method thereof. The preparation is formed by an epidermal growth factor receptor tyrosine kinase inhibitor with the tumor growth inhibition effect, a high-molecular polymer and a freeze-drying protective additive. The preparation method is simple, suitable for the large-scale production, and particularly suitable for preparing an antitumor drug nano-preparation with the characteristics of long blood circulation time, biodegradation in vivo, slow release of drugs, and passive targeting. The antitumor nano-drug sustained release preparation prepared by the method is suitable for the management by using modes, such as intravenous injection, intramuscular injection, intratumor injection and peritumoral injection, and applied to the treatment of the malignant solid tumors, such as lung cancer, liver cancer, gastric cancer, intestinal cancer, esophagus cancer, nasopharyngeal cancer, uterus cancer, breast cancer, glioma cancer, ovarian cancer, and prostate cancer, and has the good application prospect.

The invention belongs to the technical field of medicines, and relates to a 4H-thieno[2,3-b]thiapyran-4-ketone compound, a preparation method thereof and application thereof as an epidermal growth factor receptor tyrosine kinase inhibitor. The compound, a prodrug thereof, a pharmaceutically active metabolite thereof and a pharmaceutically acceptable salt thereof have structural formula as shown inthe specification, wherein R is independently selected from hydrogen, halogen, hydroxy, nitro, cyan, C1-C4 alkyl, C1-C4 alkoxy, halogen atoms substituted C1-C4 alkyl, and halogen atoms substituted C1-C4 alkoxy. The formula is shown in the description.