162 results about "Fibroblast growth factor receptor" patented technology

Molecules comprising the antigen-binding portion of antibodies that block constitutive and/or ligand-dependent activation of a receptor protein tyrosine kinase, such as fibroblast growth factor receptor 3 (FGFR3), are found through screening methods, where a soluble dimeric form of a receptor protein tyrosine kinase is used as target for screening a library of antibody fragments displayed on the surface of bacteriophage. The molecules of the present invention which block constitutive activation can be administered to treat or inhibit skeletal dysplasia, craniosynostosis disorders, cell proliferative diseases or disorders, or tumor progression associated with the constitutive activation of a receptor protein tyrosine kinase.

A composition is provided that contains a polypeptide and a modulator or a cell comprising the polypeptide and a modulator, where the modulator specifically interferes with the activity of the polypeptide, and the polypeptide is either FGFR3 or FGFR4, inclusive of all polymorphic forms and variants thereof. The modulator can be an antibody or active fragments thereof, a small molecule drug, an RNAi molecule, an antisense molecule or a ribozyme. A method of treatment of tumors in a subject is also provided where an antagonist of FGFR3 or FGFR4 is administered to the subject.

Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.

The present invention relates to a therapeutic agent represented by the General formula (I), or a pharmacologically acceptable salt thereof, or a solvate of the compound or the salt thereof:

The therapeutic agent comprises a substance having the activity of inhibiting kinase activity of fibroblast growth factor receptor 2 (“FGFR2”). The therapeutic agent can be used for treating undifferentiated gastric cancer, and can also be used to treat organisms comprising a cell overexpressing FGFR2 or a cell expressing mutant FGFR2, or both. The present invention further relates to a pharmaceutical composition comprising an FGFR2 inhibitory and methods of treatment therewith. The present invention also relates to a method for predicting the effect of an FGFR2 inhibitory substance on a patient.

Fibroblast growth factor receptor (FGFR) extracellular domain (ECD) acidic region muteins that have been engineered to exhibit decreased tissue binding by increasing the number of acidic amino acid residues within the D1-D2 linker region are provided. Polynucleotides encoding FGFR ECD acidic region muteins are also provided. Methods of making FGFR ECD acidic region muteins, and methods of using such molecules to treat proliferative disorders, including cancers, disorders of angiogenesis, and macular degeneration, are also provided.

The invention provides synthetic heparin-binding growth factor analogs having at least one peptide chain that binds a heparin-binding growth factor receptor, covalently bound to a hydrophobic linker, which is in turn covalently bound to a non-signaling peptide that includes a heparin-binding domain. The synthetic heparin-binding growth factor analogs are useful as soluble biologics or as surface coatings for medical devices.

The invention provides synthetic heparin-binding growth factor analogs of formulas I or II as given in the specification, having two peptide chains branched from a dipeptide branch moiety composed of at least one and preferably two trifunctional amino acid residues, which peptide chain or chains bind a heparin-binding growth factor receptor. The synthetic heparin-binding growth factor analogs are useful as pharmaceutical agents, soluble biologics or as surface coatings for medical devices.

The present invention is directed toward a monoclonal antibody to fibroblast growth factor receptor 2, a pharmaceutical composition comprising same, and methods of treatment comprising administering such a pharmaceutical composition to a patient.

The present invention relates to the use of Fibroblast Growth Factor Receptor I (FGFR1) extracellular domain (ECD) polypeptides for treatment of cancers characterized by ligand dependent activating mutations in Fibroblast Growth Factor Receptor 2 (FGFR2). For example, the present invention relates to the treatment of endometrial cancers and other cancers wherein tumor cells express FGFR2 mutants in the IgII-IgIII hinge region or IgIII domain of the protein, such as at amino acid positions 252 and/or 253.

The invention belongs to the field of medicinal chemistry and particularly relates to 2,4,5-trisubstituted pyrimidine compounds taking FGFRs (fibroblast growth factor receptors) as targets as well as preparation methods and an application of the 2,4,5-trisubstituted pyrimidine compounds. The compounds can selectively inhibit phosphorylation of FGFR kinase so as to be used for treating malignant tumors closely related with the kinase, and can reduce adverse reactions; the compounds can be used for treating tumors related with the FGFR kinase or relevant diseases. The general formula of the 2,4,5-trisubstituted pyrimidine compounds is shown in the specification, wherein R<1>, R<2> and R<3> can be selected from multiple substituents and can be combined randomly. The 2,4,5-trisubstituted pyrimidine compounds taking the FGFRs as the targets have a good inhibition function on the FGFR1 kinase, have an anti-proliferation function on FGFR1-dependent tumor cell line KG1 cells, can be used for preparing antitumor drugs and have better antitumor effects.

The invention relates to a preparation method and application of an electrochemical sensor for achondroplasia prenatal diagnosis gene-fibroblast growth factor receptor 3 (FGFR3) gene polymorphism detection, belonging to the technical field of electrochemical detection. The preparation method is characterized by comprising the following steps: synthesizing a Hemin-MOFs composite material, reducing platinum nanoparticles onto the Hemin-MOFs composite material, and mixing a single-strand DNA signal probe with the composite material to obtain a biological signal probe; and carrying out layer-by-layer self-assembly by using reducible graphene oxide tetraethylenepentamine, nano gold and avidin to fix the biotinylated DNA capture probe, thereby preparing the electrochemical sensor for FGFR3-1138G>A gene polymorphism detection. The sensor is successfully used for detecting FGFR3-gene single base mutation. The sensor has the advantages of high sensitivity and high specificity, and is quick and convenient for detection. The invention provides a new detection method for prenatal noninvasive diagnosis of achondroplasia.

Isolated fibroblast growth factor receptor 5 (FGFR5) polypeptides are provided, together with polynucleotides encoding such polypeptides. Also provided are modulators of FGFR5 gene expression and binding molecules that specifically bind to, and agonize or antagonize, FGFR5 polypeptide function. Binding molecules include antibodies, and functional fragments thereof, as well as scFv and Camelidae heavy chain IgG that specifically bind to FGFR5 thereby modulating the activity of FGFR5. Such binding agents and modulators of FGFR5 gene expression may be employed for the treatment of disorders including: osteopontin-mediated diseases; autoimmune diseases, such as systemic lupus erythematosus; bone disorders such as osteoporosis and osteopetrosis; and cancers, including cellular carcinomas such as hepatocellular carcinomas.

Isolated fibroblast growth factor receptor 5 (FGFR5) polypeptides are provided, together with polynucleotides encoding such polypeptides. Also provided are modulators of FGFR5 gene expression and binding molecules that specifically bind to, and agonize or antagonize, FGFR5 polypeptide function. Binding molecules include antibodies, and functional fragments thereof, as well as scFv and Camelidae heavy chain IgG that specifically bind to FGFR5 thereby modulating the activity of FGFR5. Such binding agents and modulators of FGFR5 gene expression may be employed for the treatment of disorders including: osteopontin-mediated diseases; autoimmune diseases, such as systemic lupus erythematosus; bone disorders such as osteoporosis and osteopetrosis; and cancers, including cellular carcinomas such as hepatocellular carcinomas.

The present invention relates to general formula (I) spiroheterocyclic compound, its stereoisomer, enantiomer, tautomer or its mixture, or its pharmaceutically acceptable salt, solvate or prodrug, wherein ( II, k, j, P, Q, R1, R2 and R3) are as defined herein, which are useful for the treatment and/or prevention of diseases or conditions mediated by fibroblast growth factors and their receptor signaling pathways, such as cancer . Also disclosed are pharmaceutical compositions comprising the compounds and methods of using the compounds.

The invention belongs to the technical field of medicine, and specifically relates to the application of the following 11 compounds in the preparation of fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor drugs: 3,5-bis(2,4-dichlorophenylene) Methyl)piperidin-4-one; 3,5-bis(2-chlorobenzylidene)piperidin-4-one; 3,5-bis(2-bromobenzylidene)piperidin-4- Ketone; 3,5-bis(3,4-difluorobenzylidene)piperidin-4-one; 3,5-bis(3-fluorobenzylidene)piperidin-4-one; 3,5 - Bis(3,4-dihydroxybenzylidene)piperidin-4-one; 3,5-bis(3,4-dihydroxybenzylidene)-1-methylpiperidin-4-one; 3,5-bis(3,4-dihydroxybenzylidene)-tetrahydropyran-4-one; 3,5-bis(3,4-dihydroxybenzylidene)-tetrahydrothiopyran- 4-keto; 3,5-bis(3,4-difluorobenzylidene)-tetrahydropyran-4-one; 3,5-bis(bis(2-chloroethyl)aminobenzylidene )-tetrahydrothiopyran-4-one.

The invention discloses nitrogen-containing fused ring compounds as well as a preparation method and application thereof. The nitrogen-containing fused ring compounds have a structure represented by aformula (I) shown in the description, wherein each group is defined in the description. The nitrogen-containing fused ring compounds provided by the invention belong to novel irreversible inhibitorsof specific fibroblast growth factor receptor (FGFR) kinase, and can be used for treating related diseases such as tumors caused by abnormal FGFR kinase.