33 results about "ERBB Family" patented technology

Ditosylate salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorde4rs characterized by aberrant erbB family PTK activity.

Antibodies which bind to activated members of the erbB, TNF, and IgSF family of receptors and pharmaceutical compositions comprising the same are disclosed. Peptides and mimetics of erbB, TNF, and IgSF receptors and pharmaceutical compositions comprising the same are also described. Methods of using such antibodies, peptides, and mimetics in tumor therapeutic, prophylactic, imaging and diagnostic applications are disclosed.

The present invention relates to pyrimidine derivatives for the treatment of cancer. Specifically, the present invention relates to anilino-pyrimidine compounds of Formula (I), Formula (II), Formula (III) and Formula (IV) and pharmaceutically acceptable salts thereof; wherein the compound or the salts thereof can be used for the treatment or prevention of diseases or disorders by modulating certain mutated forms of epidermal growth factor receptors. The present invention also relates to pharmaceutical compositions comprising said compounds or salts thereof, and methods of using said compoundsand salts thereof in the treatment of a variety of diseases mediated by EGFR, HER2 and / or HER4 in the ErbB family.

Pancreatic ductal adenocarcinoma (PDAC) is one of the most lethal types of tumor amongst all human cancers due to late diagnosis and resistant to treatment with chemotherapy and radiation. Preclinical and clinical studies have revealed that ErbB family for example epidermal growth factor receptor (EGFR) is a validated molecular target for pancreatic cancer prevention and therapy. The ErbB signaling cascade is regulated by a member of the ADAM (a disintegrin and metalloprotease) family, namely ADAM17, by enzymatic cleavage of precursor ligands into soluble cytokines and growth factors. Mouse genetic studies have demonstrated that ADAM17 is required for PDAC development. In this study, we evaluated the anti-tumor effects of A9(B8) IgG—the first specific ‘human and mouse cross-reactive’ ADAM17 inhibitory antibody on pancreatic malignant transformation. We found that inhibition of ADAM17 with A9(B8) IgG efficiently suppressed the shedding of ADAM17 substrates both in vivo and in vitro. Furthermore, we demonstrated that administration of A9(B8) IgG significantly suppressed motility in human pancreatic cancer cells and also significantly delayed tumorigenesis in the Pdx1Cre;KrasG12D;Trp53fl / + PDAC mouse model. Inhibition of ADAM17 with A9(B8) IgG particularly affected the progression of pre-invasive pancreatic lesions to advanced PDAC in mice. Taken together, the preclinical data presented here will provide a starting point for clinical applications of ADAM17 targeted therapy.

The present invention relates to a substituted aminoquinazoline compound, and a pharmaceutical composition and a use thereof. The aminoquinazoline compound is a compound represented by formula (I), or a pharmaceutically acceptable salt thereof, a prodrug, a hydrate or a solvent compound, a crystal form, a stereoisomer or an isotope variant. The compound and the composition can be used for treating and / or preventing ErbB family tyrosine kinase mediated diseases.

The present invention relates to a quinoline or a quinazoline derivative having the structure of formula (I), a pharmaceutical composition containing the compound of formula (I), and the preparation of the compound for preventing or treating human epidermal growth factor receptor Her / erbB family related diseases Use of a medicament, particularly for the prevention or treatment of tumors associated with protein tyrosine kinases. wherein each substituent in the formula (I) is the same as defined in the specification.

The invention belongs to the technical field of medicinal chemistry, and relates to quinazoline derivatives of general formula (I) and their preparation methods, and their physiologically acceptable salts formed with inorganic or organic acids or bases, and pharmaceutical compositions containing them , and its application in the preparation of medicines for treating diseases, especially the medicines for diseases characterized by abnormal erbB family PTK activity. Said compounds have valuable pharmacological properties, in particular an inhibitory effect on signal transduction caused by tyrosine kinases.

The invention belongs to the technical field of pharmaceutical chemistry, and relates to 4-substituted p-methyl sulfonamide anilino-quinazoline derivatives with a general formula (I), wherein R1 and R2 respectively have meanings limited in the specifications. The invention also relates to a preparation method of the derivatives, physiologically acceptable salt composed of the derivatives and inorganic or organic acid or alkali, and a pharmaceutical composition containing the same. The compound has valuable pharmacological properties, has an inhibitory effect on signal transduction caused by PTK (Protein Tyrosine Kinase), and especially has higher inhibitory activity on a mutant EGFR (Epidermal Growth Factor Receptor) (L858R / T790M) and an HER2 (Human Epidermal Growth Factor Receptor 2). The invention also relates to a method for treating diseases, especially diseases characterized by abnormal erbB family PTK activity, by using the derivatives.

Heterocycle amino alkyloxy substituted quinazoline derivatives as represented by the structural Formula (I) and pharmaceutically acceptable salts thereof, capable of inhibiting the activity of receptor tyrosine kinase EGFR, and being used to treat cancers related to the expression of the receptor tyrosine kinase of the ErbB family are provided.

The invention belongs to the technical field of pharmaceutical chemistry and discloses quinazoline derivatives as shown in a general formula (I), wherein the R1 and R2 are defined by the specification. The invention also discloses a preparation method for the derivatives, physiologically acceptable salts formed by the derivatives and inorganic or organic acid or alkali as well as a pharmaceutical composition containing the derivatives and the physiologically acceptable salts. The compounds have the valuable pharmacological properties, especially the inhibitory effect on the signal transduction caused by tyrosine kinase. The invention also discloses a method for treating diseases, especially treating diseases which have the characteristic of abnormal erbB family protein tyrosine kinase (PTK) activity.