33 results about "ERBB Family" patented technology

The use of a compound for the manufacture of a medicament for the prophylaxis or treatment of: A. a disease state or condition mediated by a kinase which is BCR-abl, VEGFR, PDGFR, EGFR, Flt3, JAK (e.g. JAK2 or JAK3), C-abl, PDK1, Chk (e.g. Cbk1 or Chk2), FGFR (e.g. FGFR3), Ret, Eph (e.g. EphB2 or EphB4), or Src (e.g. cSrc); or B. a cancer in which the cancer cells thereof contain a drug resistant kinase mutation which is: (a) a threonine gatekeeper mutation; or (b) a drug-resistant gatekeeper mutation; or (c) an imatinib resistant mutation; or (d) a nilotinib resistant mutation; or (e) a dasatinib resistant mutation; or (f) a T670I mutation in KIT; or (g) a T674I mutation in PDGFR; or (h) T790M mutation in EGFR; or (i) a T315I mutation in abl; or C. a cancer which expresses a mutated molecular target which is a mutated form of BCRabl, c-kit, PDGF, EGF receptor or ErbB2; or D. a disease mediated by a kinase containing a mutation in a region of the protein that binds to or interacts with other cancer agents but does not bind to or interact with the compounds of formula (I) or (I′), for example a mutated kinase selected from c-abl, c-kit, PDGFR including PDGFR-beta and PDGFR-alpha, and ErbB family members such as EGFR (ErbB1), HER2 (ErbB2), ErbB3, and ErbB4, members of the Ephrin receptor family including EphA1, EphA2, EphA3, EphA4, EphA5, EphA8, EphA10, EphB1, EphB2, EphB3, EphB5, EphB6, c-Src and kinases of the JAK family such as TYK2; wherein the compound is a compound of the formula (I or I′): or a salt, solvate, tautomer or N-oxide thereof wherein R^0′, R¹, R^1′, R^2′, R^3′, R^4′, A′, X′, E, A and M are as defined in the claims.

The present invention relates to thienopyrmidine compounds of formula (I) (one of A¹ and A² is S and the other is CH), salts thereof, as well as use and preparation of the same. These compounds are inhibitors of various protein tyrosine kinases (PTKs) of the ErbB family and consequently are useful in the treatment of disorders mediated by aberrant activity of such kinases.

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 invention discloses a heterocyclic amino and alkoxy-replaced quinazoline derivative and a pharmaceutically acceptable salt. The derivative inhibits the activity of a receptor tyrosine kinase epidermal growth factor receptor (EGFR) and can be used for treating cancers related to the receptor tyrosine kinase expression of an ErbB family.

The present invention provides a pharmaceutical composition, useful for the treatment of diseases characterized by abnormal PTKs activity of erbB family in a mammal, comprising pharmaceutically acceptable salts of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]quinazolin-6-yl}-acrylamide, optionally a pharmaceutically applicable carrier or diluent, and a stabilizer having a dispersing and/or protective effect on the active ingredient. The present invention further provides a pharmaceutical formulation comprising said composition, methods for preparation of said composition and said formulation, as well as use of said composition and said formulation for treating diseases characterized by abnormal PTKs activity of erbB family in a mammal.

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.

A compound comprising

• • a photosensitizer covalently coupled to
  • a protein selected from the group consisting of
    • antibodies or their derivatives or fragments thereof, synthetic peptides such as scFv, mimotopes
  • which bind CD antigens, cytokine receptors, interleukin receptors, hormone receptors, growth factor receptors, more particularly tyrosine kinase growth factor receptor of the ErbB family, wherein
  • the photosensitizer is coupled to the binding protein via O6-alkylguanine-DNA alkyltransferase (hAGTm), a modified human DNA repair protein.

The present disclosure includes methods for the prediction of outcome in breast cancer where EGFR/ErbB family members are over expressed and the benefit of treatment with an anti-ErbB antibody. More specifically, the present invention relates the use of the mRNA expression level of a C8A, OR56A1, or PRR20C biomarker compared to a reference expression level for providing information regarding the benefit of treatment with a HER2 antibody, such as trastuzumab, in HER2+ breast cancer.

The invention relates to a quinoline or quinazoline derivative with a structure as shown in a formula (I), a pharmaceutical composition containing the compound as shown in the formula (I) and application of the compound in preparation of drugs for preventing or treating human epidermal growth factor receptor Her/erbB family related diseases, and particularly relates to application of the compoundsfor preventing or treating tumors associated with protein tyrosine kinase, wherein each substituent in the formula (I) is the same as the definition in the specification.

Provided is a method for screening a plurality of compounds for an ability to bind to a heterodimer of EGFR and another ERBB family member. Also provided are compounds that bind to heterodimers of EGFR and another ERBB family member; and methods of using the identified compounds to suppress the growth of a tumor associated with EGFR heterodimer activity in a subject.

Oral pharmaceutical formulations containing ditosylate salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorders characterized by aberrant erbB family PTK activity.

The present invention relates to combination therapies for treating KRas G12C cancers. In particular, the present invention relates to methods of treating cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a combination of a pan ErbB family inhibitor and a KRAS G12C inhibitor of Formula (I), Formula (I-A) or Formula (I-B), pharmaceutical compositions comprising a therapeutically effective amounts of the inhibitors, kits comprising the compositions and methods of use therefor.

The invention provides a substituted amino quinazoline compound and a pharmaceutical composition and application thereof. The substituted amino quinazoline compound refers to a compound shown as a formula (I), or a pharmaceutically acceptable salt of the compound, a prodrug, a hydrate or a solvate, a crystal form, a stereoisomer or an isotope variant. The compound and the composition can be used for treatment and/or prevention of ErbB family tyrosine kinase mediated diseases.

The present invention resides in the discovery that the specific interaction between neuregulin 1 (NRG1) and integrin is important for ErbB signaling, which in turn plays an important role in cellular signaling in various physiological processes such as cell proliferation, especially in cancer cells overexpressing ErbB family members. Thus, this invention provides for a novel method for inhibiting ErbB signaling by using an inhibitor of NRG1-integrin binding. A method for identifying inhibitors of NRG1-integrin binding is also described. Further disclosed are polypeptides, nucleic acids, and corresponding compositions for inhibiting ErbB signaling.

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.

The present invention discloses pyrimidine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such pyrimidine derivatives are useful in the treatment of diseases associated with inappropriate ErbB family kinase.