77 results about "Epidermal Growth Factor Receptor Inhibitors" patented technology

The invention concerns genes and gene sets and methods useful in the prediction of the response of a cancer patient to treatment with an epidermal growth factor receptor (EGFR) inhibitor.

Disclosed are biomarkers, methods and assay kits for the identification of cancer patients who are predicted to benefit, or not to benefit, from the therapeutic administration of an epidermal growth factor receptor (EGFR) inhibitor. The biomarkers of the present invention include detection of EGFR and HER 2 gene amplification and polysomy, EGFR protein expression, EGFR mutations, phosphorylated Akt protein expression, and various combinations of such biomarkers, as well as the combination of these biomarkers with mutations in the tyrosine kinase domain of the EGFR gene. Increased EGFR gene copy number, increased HER2 gene copy number, increased EGFR, protein expression, activated AKT protein expression (phosphorylated AKT) and EGFR mutations are all associated with better outcome for cancer patients treated with EGFR inhibitors. The invention provides a diagnostic paradigm based on each of these tests and combinations of these tests to select cancer patients who will benefit from EGFR inhibitor therapy, as well as a diagnostic paradigm to select cancer patients who will not benefit from EGFR inhibitor therapy.

The purpose of this invention is to provide an agent useful for prevention and / or treatment of psychosis, schizophrenia and cognitive impairments. To solve this problem, this invention provides epidermal growth factor receptor inhibitors as therapeutic agents for psychosis, schizophrenia and cognitive impairments.

The invention discloses an EGFR inhibitor. The EGFR inhibitor is of the structure shown in the formula (I) and is a compound including alpha, beta-unsaturated carboxylic acid amides. Meanwhile, the invention discloses a preparing method of the compound and the application of the compound serving as a protein tyrosine kinase inhibitor, especially the inhibiting function on T790M variant EGFR as the EGFR inhibitor, and the application on treating diseases such as the kidney cancer, the ling cancer, the prostate cancer, the pancreatic cancer the breast cancer and the spongiocytoma which are related to EGFR over expression. The structure is shown in the specification.

The invention discloses 3-methoxymethyl-2,3-dihydro-[1,4]dioxano[2,3-f]quinazoline-10-amine compound and a preparation method thereof, and application of the compound as an epidermal growth factor receptor inhibitor for treating cancers, belonging to the field of biology. The compound is an N-substituted phenyl-5-substituted alkoxy-3-methoxymethyl-2,3-dihydro-[1,4]dioxano[2,3-f]quinazoline-10-amine compound as shown in a formula (I) which is described in the specification, or a pharmaceutically acceptable salt or a prodrug molecule thereof. In the formula (I), R<1> is selected from a group consisting of -H, C1-5 straight-chain or branched-chain alkyl groups, alkyloxy groups, alkyloxy-substituted C1-5 straight-chain or branched-chain alkyl groups, etc.; R<2> is selected from a group consisting of -H, halogen, aromatic alkyloxy groups, C1-3 alkyl groups, and C1-3 straight-chain or branched-chain alkoxy groups; and R<3> is selected from a group consisting of -H, halogen, C1-4 unsaturated alkyl groups, nitro groups, cyano groups and C1-3 straight-chain or branched-chain alkoxy groups. The compound provided by the invention can be applied to treatment or prevention a variety of cancers.

The invention relates to phosphate of a compound as shown in the formula (I) which is described in the specification, and a crystal form and a preparation method thereof. The phosphate of the compound has a stable crystal form; the crystal form has favorable performance like good solubility, low hygroscopicity and process developability; and the preparation method is simple and has low cost, so the method has an important value to optimization and development of the phosphate of the compound as a drug in the future.

Epidermal growth factor receptor (EGFR) inhibitors are provided. In particular, 4-substituted-2-(N-(5-substituted allyl amide)phenyl)amino)pyrimidine derivatives of formula (I), a preparation method and use thereof as an EGFR inhibitor are provided. The 4-substituted-2-(N-(5-substituted allyl amide)phenyl)amino)pyrimidine derivatives of formula (I) have inhibitory activity against the L858R EGFR mutant, the T790M EGFR mutant and the exon 19 deletion activating mutant, and can be used to treat diseases mediated alone or in part by EGFR mutant activity. The derivatives of formula (I) can be used to treat and / or prevent cancers, particularly non-small cell lung cancer.

The present invention pertains to a method for treating cancer, such as lung cancer, multiple myeloma, lymphoma, and epithelial ovarian cancer, comprising the administration to a patient in need thereof a first amount or dose of a histone deacetylase (HDAC) inhibitor, such as PXD-101, and a second amount or dose of another chemotherapeutic agent, such as dexamethasone or 5-fluorouracil, or an epidermal growth factor receptor (EGFR) inhibitor, such as TarcevaÚ, wherein the first and second amounts or doses together comprise a therapeutically effective amount.

The present invention relates generally to methods of preventing or treating toxicities of the skin, hair, and / or nails, which are associated with administration of one or more epidermal growth factor receptor inhibitors, with light-emitting diode photomodulation treatment, either alone or in combination with other agents.

Disclosed is the use of a combination of histone deacetylase inhibitors and epidermal growth factor receptor (EGFR) inhibitors to treat cancer.

The present invention relates to a method for the treatment, prevention and / or diagnosis of metastatic prostate cancer. More specifically inhibitors of Epidermal Growth Factor Receptor (EGFR) are used in the preparation of a pharmaceutical composition for treating or preventing metastatic prostate cancer. The EGFR inhibitors can for instance be EGFR inhibitors, EGFR signaling inhibitors and / or inhibitors of kinases downstream of EGFR kinases. The EGFR inhibitors can also be used in detection, screening, prediction and treatment monitoring methods for metastatic prostate cancer.

The invention provides a novel epidermal growth factor receptor inhibitor and an application thereof. The novel epidermal growth factor receptor inhibitor can be used as a T790M variation induced drug-resistant inhibitor.

The invention belongs to the technical field of medical chemistry, and specifically relates to a novel epidermal growth factor receptor inhibitor, a pharmaceutical composition containing the novel epidermal growth factor receptor inhibitor and use of the novel epidermal growth factor receptor inhibitor or the pharmaceutical composition as a cancer prevention and / or treatment medicament. The compounds exhibit excellent EGFR (Epidermal Growth Factor Receptor) inhibition activity, especially for mutative EGFR, and is expected to become a pharmaceutical with a special treatment effect and smaller side effect on resisting pharmaceutical-resistant tumors caused by EGFR mutation.

The invention specifically relates to an indazole-substituted EGFR inhibitor, a pharmaceutical composition containing the inhibitor, and application of the inhibitor or the pharmaceutical composition as a drug for prevention and / or treatment of cancers, belonging to the field of medical chemistry. The inhibitor presents good EGFR inhibitory activity, especially good inhibitory effect on mutant EGFR, and is expected to become a drug with specific curative effect and small side effect on treatment of tumors resistant to drugs due to EGFR mutation.

Provided herein are compounds that inhibit a binding interaction between an epidermal growth factor receptor (EGFR) and a heat shock protein 90 (HSP90), as well as compositions, e.g., pharmaceutical compositions, comprising the same, and related kits. In some embodiments, the compound is an antibody or antibody analog, and, in other embodiments, the compound is a peptide or peptide analog. Also provided are methods of using the compounds, including methods of increasing degradation of an EGFR, methods of treating cancer, and methods of sensitizing tumors to radiation therapy.

We identify markers capable of guiding the decision to incorporate epidermal growth factor receptor (EGFR) inhibitors, in particular EGFR tyrosine kinase inhibitors (TKIs), into chemotherapeutic regimens. Mitogen-inducible gene 6 (Mig6), a negative regulator of EGFR, is selectively upregulated during the development of resistance to the EGFR tyrosine kinase inhibitor (TKI) erlotinib, resulting in decreased EGFR phosphorylation. The ratio of Mig6 / EGFR expression highly correlates with erlotinib sensitivity. A low Mig6 / EGFR ratio correlates with a high response rate to gefitinib and a marked increase in progression-free survival for patients. The ratio of Mig6 to EGFR is a major predictor of biologic and clinical responses to EGFR inhibitors.

The invention relates to a kit for forecasting the treatment effect of an epidermal growth factor receptor inhibitor, in particular to a specific primer and a probe for detecting the polymorphism of a nineteenth exon of an epidermal growth factor receptor gene by a PCR method, application of the same in preparing a reagent for detecting the polymorphism of the nineteenth exon of the epidermal growth factor receptor gene through a PCR amplified biological nucleic acid sample, a kit for detecting the polymorphism of the nineteenth exon of the epidermal growth factor receptor gene and application of the kit, and belongs to the field of medicaments.

The invention relates to a specific primer and a probe for detecting the polymorphism of a twenty-first exon L861Q of an epidermal growth factor receptor gene by a PCR method, application of the same in preparing a reagent for detecting the polymorphism of the twenty-first exon L861Q of the epidermal growth factor receptor gene through a PCR amplified biological nucleic acid sample, a kit for detecting the polymorphism of the twenty-first exon L861Q of the epidermal growth factor receptor gene and application of the kit, and belongs to the field of medicine.

The invention relates to the technical field of medicament, in particular to application of an EGFR (Epidermal Growth Factor Receptor) inhibitor in preparation of medicine for treating JE (Japanese Encephalitis). According to the application of the EGFR inhibitor in preparation of the medicine for treating JE, provided by the invention, an important function of the EGFR in JEV (Japanese Encephalitis Virus) infection is discovered, and the EGFR inhibitor has the characteristic of inhibiting the JEV infection; furthermore, the situation that the EGFR inhibitor is capable of influencing the JEV infection through inhibiting phosphorylation of the EGFR is discovered. According to the application of the EGFR inhibitor in preparation of the medicine for treating JE, provided by the invention, the novel medicine is provided for preventing and treating JE, and the market value and a clinic application prospect are better.

The invention provides a traditional Chinese medicinal composition for external use for treating rash. The traditional Chinese medicinal composition is prepared from the following raw medicines: 10 to 50 weight parts of radix scutellariae, 10 to 60 weight parts of herba portulacae, 10 to 60 weight parts of cortex dictamni, 10 to 50 weight parts of radix sophorae flavescentis, and 10 to 60 weight parts of herba taraxaci. The traditional Chinese medicinal composition disclosed by the invention has a remarkable effect on the aspect of improving acne-like rash and itch degree related to EGFRIs (Epidermal Growth Factor Receptor Inhibitors); moreover, an obvious adverse effect is avoided.

The invention relates to a specific primer and a probe for detecting the polymorphism of a twenty-first exon L858R of an epidermal growth factor receptor gene by a PCR method, application of the same in preparing a reagent for detecting the polymorphism of the twenty-first exon L858R of the epidermal growth factor receptor gene through a PCR amplified biological nucleic acid sample, a kit for detecting the polymorphism of the twenty-first exon L858R of the epidermal growth factor receptor gene and application of the kit, and belongs to the field of medicine.

The invention provides application of a rhinoceros horn and rehmannia glutinosa composition in preparation of a medicine for preventing and treating related rash caused by an epidermal growth factor receptor inhibitor. The rhinoceros horn and rehmannia glutinosa composition includes rhinoceros horns, radix paeoniae rubra, radix rehmanniae and cortex moutan serving as effective ingredients. The medicine composition prepared by rhinoceros horn and rehmannia glutinosa decoction for treating severe hepatitis, hepatic coma, uremia, allergic purpura, acute leukemia, sepsis syndrome and other symptoms is creatively used for preventing and treating the rash caused by the epidermal growth factor receptor inhibitor, is better in clinical curative effect and low in toxicity and can be taken for a long time.

It is an object to provide a culture method which is capable of maintaining and / or culturing iPS cell-derived intestinal stem cells, while maintaining the properties of intestinal stem cells. The induced pluripotent stem cell-derived intestinal stem cell-like cells are cultured in the presence of a GSK-3β inhibitor, a histone deacetylation inhibitor, and a serum replacement, or in the presence of a GSK-3β inhibitor and a serum replacement. Preferably, the culture is carried out under conditions in which one or more compounds selected from the group consisting of an epidermal growth factor, a TGFβ receptor inhibitor and a fibroblast growth factor are further present.

The invention provides a traditional Chinese medicine composition for externally treating skin rash. The traditional Chinese medicine composition comprises the following raw herbal materials in part by weight: 10-50 parts of radix scutellariae, 10-60 parts of purslane, 10-60 parts of cortex dictamni, 10-50 parts of sophora flavescens, 10-60 parts of dandelion, 5-30 parts of red peony root and 1-10 parts of mechanism. The traditional Chinese medicine composition has an obvious effect of improving EGFRIs (epidermal growth factor receptor inhibitors) relevant acneiform rash and itch degree, and untoward effects do not exist.

The invention provides an external traditional Chinese medicine composition for treating tetter. The traditional Chinese medicine composition is prepared from the following active pharmaceutical ingredients in parts by weight: 10 to 50 parts of radix scutellariae, 10 to 60 parts of herba portulacae, 10 to 60 parts of cortex dictamni, 10 to 50 parts of radix sophorae flavescentis and 10 to 60 partsof herba taraxaci. The traditional Chinese medicine composition has the obvious effect in aspects of relieving EGFRIs ((epidermal growth factor receptor inhibitors) relevant acne-like tetter and thepruritus degree; no obvious untoward effects exist.

Epidermal growth factor receptor (EGFR) inhibitors are provided. In particular, 4-substituted-2-(N-(5-substituted ally amide)phenyl)amino)pyrimidine derivatives of formula (I), a preparation method and use thereof as an EGFR inhibitor are provided. The 4-substituted-2-(N-(5-substituted ally amide)phenyl)amino)pyrimidine derivatives of formula (I) have inhibitory activity against the L858R EGFR mutant, the T790M EGFR mutant and the exon 19 deletion activating mutant, and can be used to treat diseases mediated alone or in part by EGFR mutant activity. The derivatives of formula (I) can be used to treat and / or prevent cancers, particularly non-small cell lung cancer.

The invention relates to a kit for forecasting the treatment effect of an epidermal growth factor receptor inhibitor, in particular to a specific primer and a probe for detecting the G719S polymorphism locus of an eighteenth exon of an epidermal growth factor receptor gene by a PCR method, application of the same in preparing a reagent for detecting the G719S polymorphism locus of the eighteenth exon of the epidermal growth factor receptor gene through a PCR amplified biological sample, a kit for detecting the G719S polymorphism of the eighteenth exon of the epidermal growth factor receptor gene and application of the kit, and belongs to the field of medicaments.