48 results about "Egfr tyrosine kinase" patented technology

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.

Provided are an arylamino pyramidine compound having an inhibiting effect on EGFR tyrosine kinases, and pharmaceutically acceptable salt, stereoisomer, solvent compound, or prodrug of said arylamino pyramidine compound; also provided are pharmaceutical compositions and pharmaceutically acceptable compositions containing the arylamino pyramidine compound, and applications thereof.

The present invention provides a class of 2,4-substituted phenylene-1,5-diamine derivatives, having an inhibiting effect on EGFR tyrosine kinases, and pharmaceutically acceptable salt, stereoisomer, solvate or prodrug of said derivatives. See the description for the definition of each group in the formula. In addition, the present invention also discloses pharmaceutical compositions, pharmaceutically acceptable compositions and applications thereof.

Belonging to the technical field of medicine, the invention in particular relates to a zinc binding group-containing irreversible EGFR (epidermal growth factor receptor) tyrosine kinase inhibitor shown as general formula (I), its deuterated compounds, pharmaceutically acceptable salts or stereoisomers, wherein R1, R2, R3, R4, R5, R6, R7, W, X, L, T, and n are defined as the specification. The invention also relates to a preparation method of the compounds, pharmaceutical preparations containing the compounds, and application of the compounds in preparation of drugs treating and/or preventing tumors. (formula I).

The invention provides a 2-aminoimidazopyridine derivative shown as a formula I, a formula II, a formula III or a formula IV and further provides a preparation method and application of the 2-aminoimidazopyridine derivative. An experiment shows that the 2-aminoimidazopyridine derivative has a remarkable proliferation inhibition effect on tumor cells (including an over-expressed wild type EGFR (Epidermal Growth Factor Receptor) human epidermal carcinoma cell line A431 and a Gefitinib drug-resisting human lung adenocarcinoma cell line H1975) related to the activity of EGFR tyrosine kinase in the aspect of a cell level, especially has a relatively good inhibition effect on the drug-resisting cell line H1975, has relatively weak inhibition activity on a low-expression EGFR human colon cancer cell line SW620 and can be applied to preparation of corresponding anti-tumor cell medicines. A general formula is shown in the description.

The invention provides 2-arylamine pyrimidine derivatives containing hydroxamic acid fragments shown in the formulas I and II. 2-arylamine pyrimidine containing carboxyl fragments is mainly used as a parent nucleus and is subjected to single-step condensation and related modification with hydroxylamine protected by THP to obtain a target compound. An experiment proves that the derivatives has the remarkable anti-proliferative effect on tumor cells (an overexpression EGFR human epidermal carcinoma cell line A431 and a human pulmonary carcinoma cell line H1975 resisting Gefitinib) related to EGFR tyrosine kinase activity on the cellular level, and tumor cells (a human cervical carcinoma cell line Hela, a human hepatoma cell line HepG2, a human promyelocytic acute leukemia cell line HL60, a human oral epidermoid carcinoma cell line KB, a human colon cancer cell line SW620) related to the HDAC histone acetylase activity, and the corresponding medicine for resisting cancer cells can be prepared. The general structural formula is shown in the description.

The present disclosure relates to compounds that are capable penetrating to the blood brain barrier to modulate the activity of EGFR tyrosine kinase. The disclosure further relates to methods of treating glioblastoma and other EGFR mediated cancers. The disclosure further relates to methods of treating glioblastoma and other EGFR mediated cancers that have been determined to have altered glucose metabolism in the presence of inhibitors. The present disclosure also provides methods of administering to a subject a glucose metabolism inhibitor and a cytoplasmic p53 stabilizer.

The present invention relates to a method and assay kit for BRAF gene mutations which relates to the effect of molecule-targeting anti-tumor drug. Particularly, the present invention relates to a fluorescent quantitative PCR method and kit for detecting mutations at hotspots of BRAF gene, together with the use thereof. The present invention detects the mutations at specific sites of BRAF gene, and can predict the therapeutic efficacy of anti-EGFR tyrosine kinase inhibitors, an anti-tumor drug. Therefore, the present invention can provide a guidance to individualized treatments for cancer patients.

The subject invention concerns peptide molecules that specifically inhibit the enzymatic function of tyrosine kinases, including the JAK and EGF receptor (EGFR) family of kinases, to autophosphorylate, i.e., to transfer a phosphate group from ATP to an amino acid in the kinase. Phosphorylation of proteins is the most fundamental method for signal transduction among proteins in a cell. Inhibition of tyrosine kinase autophosphorylation activities inhibits the enzyme's signaling and shuts down the functioning pathways originating from the enzyme. The JAK2 and EGFR tyrosine kinases are involved in both inflammatory disorders and cancer. In these disorders, the tyrosine kinases can often be activated in an uncontrolled fashion. The subject application also concerns antibodies that bind to a tyrosine kinase autophosphorylation site. The subject invention also concerns pharmaceutically acceptable formulations of the subject peptides and antibodies, and methods for treating inflammatory and oncological disorders by inhibiting tyrosine kinase signaling in these situations by administering a peptide or antibody of the present invention.

The present invention provides compounds of Formula (I) or a subgeneric structure or species thereof, or a pharmaceutically acceptable salt, ester, solvate, and/or prodrug thereof, and methods and compositions for treating or ameliorating abnormal cell proliferative disorders, such as cancer, wherein A, R², R³, R¹⁰, E¹, E², E³, Y, and Z are as defined herein.

Disclosed are a quinazoline derivative, a preparation method therefor, and a pharmaceutical composition and an application thereof. The present invention provides a compound represented by general formula I, a stereoisomer thereof and a pharmaceutical acceptable salt or a solvate thereof. The quinazoline derivative of the present invention has a unique chemical structure, is characterized by irreversibly inhibiting EGFR tyrosine kinase, has high biological activity, apparently improves the inhibiting effect on the EGFR tyrosine kinase, has quite strong tumor inhibiting effect on tumor cells and a transplantation tumor pathological model of animal tumors, and has good market developing prospects.

The invention provides quinazoline derivatives containing hydroxamic acid side chains, 4-arylamido quinazoline is used as a mother nucleus, and a target compound is obtained by one-step condensation of a special connecting group and hydroxylamine which is protected by THP as well as subsequent deprotection. Experiments prove that the product has substantial proliferation inhibition effects for EGFR tyrosine kinase activity related tumor cells (an epidermal carcinoma cancer cell line A431 with EGFR overexpression and human lung adenocarcinoma cell H1975 with drug resistance for Gefitinib) on the cell level, especially has good inhibition effects for H1975 with drug resistance, and at the same time the product has good inhibition effects for Hela, HepG2 and other tumor cells; the product is used for preparing corresponding medicaments for resisting tumor cells. The structural general formula is as follows.

The invention discloses an adamantyl quinazoline compound, a composition and application of the adamantyl quinazoline compound and the composition. The compound shown in a formula (I) and all possible isomers or pharmaceutically acceptable salts or hydrates or compositions are used to treat diseases caused by EGFR (Epidermal Growth Factor Receptor) tyrosine kinase, and are particularly used to treat non-small cell lung cancer, small cell lung cancer, squamous-cell carcinoma, breast cancer and gastric carcinoma.

The invention discloses a 4-methoxyphenyl-1, 3-diamine derivative containing a 1-methyl-1H-indole structure and an application of the 4-methoxyphenyl-1, 3-diamine derivative containing the 1-methyl-1H-indole structure. The compound has a structural general formula as shown in (I). The 4-methoxyphenyl-1, 3-diamine derivative containing the 1-methyl-1H-indole structure and the pharmaceutically acceptable salt of the 4-methoxyphenyl-1, 3-diamine derivative are reversible inhibitors of EGFR (epidermal growth factor receptor) kinases, are compounds with inhibition effects on tumor cells with mutational EGFR tyrosine kinases, and can be used for treatment, combined treatment or prevention of various cancers.

The invention belongs to the field of medicines and relates to a new application of total glucosides of paeony as an EGFR (epidermal growth factor receptor) tyrosine kinase inhibitor. The content of paeoniflorin (C23H28O11) in the total glucosides of paeony is not less than 34.6%. Compared with the traditional EGFR tyrosine kinase inhibitor gefitinib, the total glucosides of paeony have the advantages that the total glucosides of paeony have high safety, can obviously reduce the expression quantity and activation quantity of EGFR tyrosine kinase, are low in price and have abundant resources, thereby providing a new choice for medicine development.

The invention discloses an EGFR-TK (epidermal growth factor receptor tyrosine kinase) inhibitor BF3-AZD9291 with antitumor activity as well as a preparation method and an application of the EGFR-TK inhibitor BF3-AZD9291, and belongs to the field of biomedicine. Brand-new EGFRTKI is obtained by optimizing and improving chemical structure of AZD9291 and named BF3-AZD9291 shown as formula I in the description. Research proves that the synthesized EGFR TKI BF3-AZD9291 can effectively inhibit drug resistance of tumor cells, has stronger drug resistance habitation effect on a mutant EGFR lung cancer cell line H1975T790M than AZD9291 and can be clinically applied as an antitumor agent accordingly. Besides, the invention discloses the preparation method of the EGFR-TK inhibitor BF3-AZD9291 with antitumor activity. With provision of the invention, an effective technological means for tumor treatment, especially treatment of non-small-cell lung cancer.

The invention provides 2,4-diarylamine pyrimidine derivatives containing hydroxamic acid fragments shown in formulas I and II. 2,4-diarylamine pyrimidine containing carboxyl fragments is mainly used as a parent nucleus and is subjected to single-step condensation and related modification with hydroxylamine protected by THP to obtain a target compound. An experiment proves that the remarkable anti-proliferative effect is achieved for tumor cells (a human lung adenocarcinoma cell line H1975 and an overexpression EGFR human epidermal carcinoma cell line A431) related to EGFR tyrosine kinase activity on the cellular level, and a human cervical carcinoma cell line Hela, a human oral epidermoid carcinoma cell line KB, a human promyelocytic acute leukemia cell line HL60, a human hepatoma cell line HepG2, a human colon cancer cell line SW620 and other tumor cells related to the HDAC histone acetylase activity, and the corresponding medicine for resisting cancer cells can be prepared. The general structural formula is shown in the description.

The invention belongs to the technical field of medicin and specifically relates to a quinolyl EGFR tyrosine kinase inhibitor containing a zinc binding group and a deuterated material, a pharmaceutically acceptable salt or stereoisomer thereof. The inhibitor is represented by a general formula (I) which is described in the specification; and in the general formula (I), R1, R2, R2', R3, R4, R5, R6, R7, W, X, L, T and n are as defined in the specification. The invention further relates to a preparation method for the inhibitor, a medicinal preparation containing the inhibitor and application of the inhibitor in preparation of drugs used for treating and/or preventing tumors.