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33 results about "ERBB Family" patented technology
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Quinazoline ditosylate salt compounds
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.
Owner:NOVARTIS AG
Monoclonal antibodies to activated erbB family members and methods of use thereof
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.
Owner:THE TRUSTEES OF THE UNIV OF PENNSYLVANIA
Quinazoline ditosylate salt compounds
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.
Owner:NOVARTIS AG
Pharmaceutical Compounds
InactiveUS20100004232A1Reduce morbidityPatient compliance is goodBiocideSenses disorderDiseaseImatinib resistant
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 R0′, R1, R1′, R2′, R3′, R4′, A′, X′, E, A and M are as defined in the claims.
Owner:ASTEX THERAPEUTICS LTD
Thienopyrimidine compounds as protein tyrosine kinase inhibitors
InactiveUS20050009845A1Undesirable side-effectMinimizing potential side-effectsBiocideOrganic active ingredientsDiseaseProtein-Tyrosine Kinases
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.
Owner:SMITHKLINE BECKMAN CORP
Monoclonal antibodies to activated erbB family members and methods of use thereof
InactiveUS20060073140A1Peptide/protein ingredientsTransferasesAbnormal tissue growthMonoclonal antibody
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.
Owner:THE TRUSTEES OF THE UNIV OF PENNSYLVANIA
Heterocyclic amino and alkoxy-replaced quinazoline derivative and application thereof
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.
Owner:SHANGHAI FENGHUA PHARMA CO LTD
Compositions Comprising Quinazoline Derivatives, Preparation Methods and Uses Thereof
ActiveUS20110111059A1Improve securityGood treatment effectBiocideOrganic active ingredientsDiseaseBULK ACTIVE INGREDIENT
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.
Owner:SHANGHAI ALLIST PHARM CO LTD
6-substituted quinazoline derivative, preparation method and application thereof
InactiveCN102079759AStrong inhibitory effect on cell proliferationOrganic active ingredientsGroup 5/15 element organic compoundsDiseaseOrganic acid
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.
Owner:TIANJIN INSTITUTE OF PHARMA RESEARCH
Novel photoimmunoconjugates for use in photodynamic therapy
ActiveUS20150140022A1Strong specificityImprove efficacySugar derivativesEnergy modified materialsDNA alkyltransferaseO6-alkylguanine-DNA alkyltransferase
A compound comprisinga photosensitizer covalently coupled toa protein selected from the group consisting ofantibodies or their derivatives or fragments thereof, synthetic peptides such as scFv, mimotopeswhich bind CD antigens, cytokine receptors, interleukin receptors, hormone receptors, growth factor receptors, more particularly tyrosine kinase growth factor receptor of the ErbB family, whereinthe photosensitizer is coupled to the binding protein via O6-alkylguanine-DNA alkyltransferase (hAGTm), a modified human DNA repair protein.
Owner:UNIVERSITY OF CAPE TOWN
Pharmaceutical composition
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.
Owner:NOVARTIS AG
Predictive biomarker(s) of treatment with erb antibodies
InactiveUS20170306417A1Improved prognosisMicrobiological testing/measurementImmunoglobulins against cell receptors/antigens/surface-determinantsAntiendomysial antibodiesPredictive biomarker
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.
Owner:CONSORTIUM FOR CLINICAL DIAGNOSTICS
Human epidermal growth factor receptor inhibitor and preparation method and application thereof
ActiveCN110577514ASignificant metabolic stability advantageGood medicineOrganic active ingredientsOrganic chemistryDiseaseProtein-Tyrosine Kinases
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.
Owner:JIANGSU VCARE PHARMATECH
Modulation of epidermal growth factor heterodimer activity
InactiveUS20100015124A1Growth of tumor is suppressedGrowth inhibitionCompound screeningApoptosis detectionAbnormal tissue growthBiology
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.
Owner:THE UNIV OF NORTH CAROLINA AT CHAPEL HILL
Aza aromatic ring amide derivatives for use in treatment of cancer
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.
Owner:SHENZHEN FORWARD PHARMA LTD CO
Pharmaceutical Composition
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.
Owner:NOVARTIS AG
Combination therapies
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.
Owner:MIRATI THERAPEUTICS INC
Quinazoline Salt Compounds
InactiveUS20110245496A1Good water solubilityOrganic active ingredientsOrganic chemistryCombinatorial chemistryQuinazoline
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.
Owner:SMITHKLINE BEECHAM (CORK) LTD
Substituted amino quinazoline compound and pharmaceutical composition and application thereof
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.
Owner:SHENZHEN TARGETRX INC
Neuregulin/erbb signaling and integrin
InactiveUS20110212108A1Inhibit cell proliferationOrganic active ingredientsPeptide/protein ingredientsNeuregulinCancer cell
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.
Owner:RGT UNIV OF CALIFORNIA
4-substituted p-methyl sulfonamide anilino-quinazoline derivatives and preparation method and application thereof
InactiveCN102558160AStrong enzyme inhibitionOrganic active ingredientsOrganic chemistryDiseaseProtein-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.
Owner:天津天诚新药评价有限公司
Quinazoline derivative as well as preparation method and use thereof
InactiveCN103554091AImprove pharmacological activityGood choiceOrganic active ingredientsOrganic chemistryDiseaseOrganic acid
The invention belongs to the technical field of medicinal chemistry, and relates to a quinazoline derivative of a general formula (I) and a preparation method thereof, physiologically acceptable salts formed by inorganic or organic acid or alkaline thereof, pharmaceutical compositions containing the salts, and application thereof in preparing medicaments for treating diseases, especially medicaments for treating the diseases with the characteristic of abnormal erbB-family PTK (Protein Tyrosine Kinase) activity. The compound has valuable pharmacological properties, and has an inhibitory effect for signal transduction caused by tyrosine kinase.
Owner:SHENYANG POLYTECHNIC UNIV
Method of treatment for pancreatic cancer by administering a human-mouse cross-reactive ADAM 17 antibody
ActiveUS10858441B2Immunoglobulins against cell receptors/antigens/surface-determinantsAntibody ingredientsAntiendomysial antibodiesCytokine
Owner:UNIVERSITY OF MACAU
Substituted aminoquinazoline compounds, pharmaceutical compositions and uses thereof
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.
Owner:SHENZHEN TARGETRX INC
Human epidermal growth factor receptor inhibitor and preparation method and application thereof
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.
Owner:JIANGSU VCARE PHARMATECH
Quinazoline derivatives and their preparation and use
InactiveCN103554091BImprove pharmacological activityGood choiceOrganic active ingredientsOrganic chemistryDiseaseOrganic acid
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.
Owner:SHENYANG POLYTECHNIC UNIV
Chemical compounds
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.
Owner:SMITHKLINE BECKMAN CORP
4-substituted p-methylsulfonamidoanilino-quinazoline derivatives and their preparation methods and uses
InactiveCN102558160BStrong enzyme inhibitionOrganic active ingredientsOrganic chemistryDiseaseOrganic acid
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.
Owner:天津天诚新药评价有限公司
Heterocyclic amino and alkoxy-replaced quinazoline derivative and application thereof
Owner:SHANGHAI FENGHUA PHARMA CO LTD
6-substituted quinazoline derivative, preparation method and application thereof
InactiveCN102079759BStrong inhibitory effect on cell proliferationOrganic active ingredientsGroup 5/15 element organic compoundsOrganic acidDisease
Owner:TIANJIN INSTITUTE OF PHARMA RESEARCH
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