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191 results about "Vascular Endothelial Growth Factor Receptor" patented technology
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RNA interference mediated inhibition of vascular endothelial growth factor and vascular endothelial growth factor receptor gene expression using short interfering nucleic acid (siNA)
InactiveUS20050171039A1Improves various propertyImprove the immunityBiocideSugar derivativesDiseaseFactor ii
The present invention concerns methods and reagents useful in modulating vascular endothelial growth factor (VEGF, VEGF-A, VEGF-B, VEGF-C, VEGF-D) and / or vascular endothelial growth factor receptor (e.g., VEGFR1, VEGFR2 and / or VEGFr3) gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules capable of mediating RNA interference (RNAi) against VEGF and / or VEGFr gene expression and / or activity. The small nucleic acid molecules are useful in the diagnosis and treatment of cancer, proliferative diseases, and any other disease or condition that responds to modulation of VEGF and / or VEGFr expression or activity.
Owner:SIRNA THERAPEUTICS INC
Inhibitors of type 2 vascular endothelial growth factor receptors
ActiveUS20070148126A1Improve pharmacokineticsIncrease target binding affinityOrganic active ingredientsSenses disorderVascular Endothelial Growth Factor ReceptorDrug biological activity
The present disclosure relates to novel vascular endothelial growth factor receptor (VEGFR)-binding polypeptides and methods for using these polypeptides to inhibit biological activities mediated by vascular endothelial growth factors (VEGFs). The present disclosure also provides various improvements relating to single domain binding polypeptides.
Owner:BRISTOL MYERS SQUIBB CO
Pharmacokinetic modulation and compositions for modified Fn3 polypeptides
ActiveUS20070160533A1Improve continuityReduce the differenceSenses disorderPeptide/protein ingredientsVascular Endothelial Growth Factor ReceptorDrug biological activity
Owner:BRISTOL MYERS SQUIBB CO
Methods
InactiveUS20110044997A1Reduce unwanted side effectPreventing agonism of unnecessary targetsBiocideNervous disorderProgenitorCXCR4
The current invention provides a method for mobilising endothelial progenitor cells (EPC) and / or mesenchymal stem cells (MSC) in a patient, wherein the method comprises the steps of (i) administering a vascular endothelial growth factor receptor (VEGFR) agonist to the patient; and (ii) administering an antagonist of CXCR4 to the patient. Also provided are uses of EPC and MSC harvested using the methods of the invention.
Owner:IMPERIAL INNOVATIONS LTD
Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity and methods of treating a patient
Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.
Owner:DUQUESNE UNIVERSITY
RNA interference mediated inhibition of vascular endothelial growth factor and vascular endothelial growth factor receptor gene expression using short interfering nucleic acid (siNA)
InactiveUS20050148530A1Improves various propertyImprove the immunityBiocideSugar derivativesDiseaseFactor ii
The present invention concerns methods and reagents useful in modulating vascular endothelial growth factor (VEGF, VEGF-A, VEGF-B, VEGF-C, VEGF-D) and / or vascular endothelial growth factor receptor (e.g., VEGFR1, VEGFR2 and / or VEGFr3) gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (mRNA), and short hairpin RNA (shRNA) molecules capable of mediating RNA interference (RNAi) against VEGF and / or VEGFr gene expression and / or activity. The small nucleic acid molecules are useful in the diagnosis and treatment of cancer, proliferative diseases, and any other disease or condition that responds to modulation of VEGF and / or VEGFr expression or activity.
Owner:SIRNA THERAPEUTICS INC
Modified binding proteins inhibiting the VEGF-A receptor interaction
ActiveUS8710187B2Senses disorderPeptide/protein ingredientsAnkyrin Repeat ProteinPolyethylene glycol
The present invention relates to binding proteins specific for Vascular Endothelial Growth Factor A (VEGF-A), in particular to recombinant binding proteins comprising a polyethylene glycol moiety and a binding domain, which inhibits VEGF-Axxx (wherein xxx denotes the amino acid length of the VEGF-A mature protein) binding to Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2). Examples of such recombinant binding proteins are proteins which comprise an ankyrin repeat domain with the desired binding specificity, and a polyethylene glycol moiety. The binding proteins are useful in the treatment of cancer and other pathological conditions, e.g. eye diseases such as age-related macular degeneration.
Owner:MOLECULAR PARTNERS AG
Anti-cancer pharmaceutical compositions and methods for treating patients with cancer
InactiveUS20090028868A1Agent for prophylaxis and treatmentBiocideOrganic chemistryPancreas CancersLiposarcoma
Method of treating persons having carcinoma, sarcoma or hematopoietic cancer by administering (i) a compound of the formula (I)and (ii) an epidermal growth factor receptor (EGFR) inhibitor, a vascular endothelial growth factor receptor (VEGFR) inhibitor and pharmaceutical compositions for use in said method. A method for treating gastric cancer, colon cancer, lung cancer, breast cancer, pancreas cancer, kidney cancer, prostate cancer, medulloblastoma, rhabdomyosarcoma, Ewing sarcoma, liposarcoma, multiple myeloma and leukemia by administering a compound of the formula (I).
Owner:DAIICHI SANKYO CO LTD
High affinity vegf-receptor antagonists
ActiveUS20090246124A1In-vivo radioactive preparationsPeptide/protein ingredientsOligomerNK1 receptor antagonist
A cell-based screen is reported can be used to identify specific receptor-binding compounds in a combinatorial library of peptoids (N-alkylglycine oligomers) displayed on beads. This strategy was applied to the isolation of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2)-binding peptoids, which were optimized to create lead compounds with high affinity for VEGFR2. One of these peptoids was shown to be an antagonist of VEGF-VEGFR2 interaction and receptor function.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST
Human monoclonal antibody neutralizing vascular endothelial growth factor receptor and use thereof
ActiveUS20110065176A1Improve abilitiesBacteriaPeptide/protein ingredientsMonoclonal antibodyAngiogenesis growth factor
The present invention relates to human monoclonal antibodies neutralizing vascular endothelial growth factor receptor and the use thereof. More specifically, relates to human ScFv molecules neutralizing vascular endothelial growth factor receptor, and a composition for inhibiting angiogenesis and a composition for treating cancer, which contain the human ScFv molecules. The disclosed monoclonal antibody neutralizing vascular endothelial growth factor receptor shows excellent neutralizing ability in living cells, compared to that of a commercially available antibody against vascular endothelial growth factor receptor, and shows the ability to neutralize vascular endothelial growth factor receptor not only in humans, but also in mice and rats. Thus, the monoclonal antibody will be useful in anticancer studies and will be highly effective in cancer treatment.
Owner:PHARMABCINE
Venom-derived vascular endothelial growth factor-like protein having binding activity specific to vascular endothelial growth factor receptor type 2 and use thereof
InactiveUS20050181995A1High activityInhibition is effectiveSenses disorderPeptide/protein ingredientsGenus ViperaVascular Endothelial Growth Factor Receptor
An objective of the present invention is to provide a newly isolated vascular endothelial growth factor (VEGF)-like protein having binding activity specific to a vascular endothelial growth factor receptor type 2 (KDR) but exhibiting no binding affinity to a vascular endothelial growth factor receptor type 1 (Flt-1), and thus being excellent in hypotensive effect. There have been newly purified and isolated a VEGF-like protein from a venom of Vipera ammodytes ammodytes: vammin and a VEGF-like protein from a venom of Daboia russelli russelli: VR-1 as the VEGF-like protein having binding activity specific to KDR but exhibiting no binding affinity to Flt-1, and thereby being excellent in hypotensive effect, and the amino acid sequences of these both have been analyzed in the present invention.
Owner:NEC SOLUTION INNOVATORS LTD +1
Anti-cancer pharmaceutical compositions and methods for treating patients with cancer
InactiveUS8263631B2BiocideOrganic chemistryProstate cancerVascular Endothelial Growth Factor Receptor
Owner:DAIICHI SANKYO CO LTD
Soluble VEGFR (Vascular Endothelial Growth Factor Receptor) difunctional chimera receptor VEGFR31-Ig as well as preparation method and application thereof
InactiveCN102134277AInhibit synthesisPeptide/protein ingredientsAntibody ingredientsVascular Endothelial Growth Factor ReceptorMedicinal chemistry
The invention discloses a soluble VEGFR (Vascular Endothelial Growth Factor Receptor) difunctional chimera receptor VEGFR31-Ig as well as a preparation method and application thereof in preparing antineoplastic drugs. The soluble VEGFR difunctional chimera receptor VEGFR31-Ig disclosed by the invention can not only be combined with VEGF-A and VEGF-B, but also be combined with VEGF-C or VEGF-D, and can be used for preparing the antineoplastic drugs.
Owner:SHANGHAI NAT ENG RES CENT OF ANTIBODY MEDICINE
Antibody fusion protein targeting VEGFR2 as well as preparation and use thereof
InactiveCN104628866AEnhanced ADCC effectPeptide/protein ingredientsPeptide preparation methodsAbnormal tissue growthNatural Killer Cell Inhibitory Receptors
The invention belongs to the technical field of genetically engineered antibody, in particular relates to a fusion protein of tumor vascular endothelial growth factor receptor 2 (VEGFR2 / KDR3) antibody and MICA as well as a preparation method and use thereof. In the invention, a full-length antibody of VEGFR2 is linked with a ligand MHC I molecule associated protein A (MICA) of activated receptor of NK cell (NKG2D) through a flexible linker and expressed by CHO cells by utilizing the genetic engineering technology, and the formed fusion protein can act on VEGFR on the surface of a tumor cell to inhibit or kill tumor and inhibit or destroy tumor angiogenesis, and on the other hand, the formed fusion protein can increase the level of MICA on the surface of the tumor cell and stimulate the NK cells to kill tumor cells through identification of NKG2D on the surfaces of the NK cells, thereby reestablishing the immunological surveillance of an body activated by the NKG2D pathway, and enhancing effects of antibody-dependent cell-mediated cytotoxicity (ADCC) and the like mediated by the Fc region of the antibody to kill tumor cells.
Owner:CHINA PHARM UNIV
Purification method of recombinant human vascular endothelial growth factor receptor-antibody fusion protein
ActiveCN105175548AEasy to removeFor the purpose of purificationPeptide preparation methodsHybrid peptidesPurification methodsProtein target
The invention relates to production of a genetic engineering drug by a recombinant DNA technology, belongs to the biotechnical field, and particularly relates to a purification method of a recombinant human vascular endothelial growth factor receptor-antibody fusion protein, that is to say, a cell supernatant containing the recombinant human vascular endothelial growth factor receptor-antibody fusion protein is successively subjected to affinity chromatography, anion exchange chromatography, cation exchange chromatography, hydrophobic chromatography and desalination chromatography to obtain the high-quality recombinant human vascular endothelial growth factor receptor-antibody fusion protein. The purification method has the characteristics of low cost, high purity of the target protein, easily controlled technological process, easily large-scale enlarged production and the like.
Owner:QILU PHARMA CO LTD
Whole human source anti-vascular endothelial cell growth factor receptor 2 single chain antibody
InactiveCN101863980AImmunoglobulins against cell receptors/antigens/surface-determinantsMaterial analysisSingle-Chain AntibodiesVascular endothelium
The invention belongs to the technical field of genetic engineering antibodies and particularly relates to a whole human source single chain antibody which is designed and expressed by genetic engineering and has specific affinity towards human vascular endothelial growth factor receptor 2 (VEGFR-2). The invention also provides a nucleotide sequence of heavy chain variable region and light chain variable region immunoglobulin molecules, a nucleotide sequence which comprises the heavy chain variable region and light chain variable region immunoglobulin molecules, an amino acid sequence which comprises variable heavy chain and variable light chain immunoglobulin molecules, and a sequence which corresponds to CDR1, CDR2 and CDR3 of a complementary determining region. The invention also provides a method for generating and expressing the anti-VEGFR-2 single chain antibody, by cycling operations of gathering-elution-gathering, an antibody which has specific affinity towards the human vascular endothelial growth factor is screened, and then the single chain antibody is obtained through a prokaryotic cell secretion and expression system and an affinity purification system. The antibody can be coupled with a detectable substance and therapeutic agent.
Owner:CHINA PHARM UNIV
Improved anti-VEGFR (vascular endothelial growth factor receptor)-2 monoclonal antibody
ActiveCN106674349AHigh affinityInhibit bindingSenses disorderAntibody mimetics/scaffoldsAbnormal tissue growthDisease
The invention relates to the technical field of biomedicine, in particular to an improved anti-VEGFR (vascular endothelial growth factor receptor)-2 monoclonal antibody and application. On the basis of the original research, a new phage antibody library is designed by computer-aided simulation by taking two of them with the highest affinity as templates, and improved heavy chain variable region and light chain variable region amino acid sequences are obtained by multi-round screening; the affinity and biological activity of the anti-VEGFR 2 monoclonal antibody are higher than those of the original antibody. The anti-VEGFR 2 monoclonal antibody obtained by the invention has relatively high affinity, can inhibit the binding of VEGFR-2 and a ligand VEGF thereof in vitro and has good biological activity, and can be used for the treatment of tumors, macular degeneration and other diseases caused by neovascularization.
Owner:BEIJING DONGFANG BIOTECH
Anti-VEGFR (vascular endothelial growth factor receptor) 2 monoclonal antibody and application thereof
ActiveCN106892980AIncrease calcium ion concentrationImmunoglobulins against cell receptors/antigens/surface-determinantsAntibody ingredientsAntiendomysial antibodiesVascular proliferation
The invention belongs to the field of antibody drug, and discloses a full human-derived anti-human VEGFR2 monoclonal antibody screened by a phage antibody base technology and prepared by a gene engineering method, and further discloses a carrier including polynucleotide for encoding the monoclonal antibody, a host cell and an application. Through combining with VEGFR2, the monoclonal antibody stops the combination of VEGF with VEGR2, and does not induce receptor dimerization, cause the following tyrosine residue phosphorylation in intracellular tyrosine kinase structure and activate downstream signal access including activation of phospholipase C and increase of calcium ion concentration in the cell and others; the antibody drug triggers endothelial proliferation, survival, cytoskeleton rearrangement, cell migration, gene expression and others, and finally stops the vascular proliferation caused by combination of VEGF and VEGFR2 and induction of dimerization. The monoclonal antibody can be used for treating diseases caused by tumor angiogenesis.
Owner:CHANGCHUN GENESCIENCE PHARM CO LTD
Lactobacillus plantarum with colorectal cancer inhibition function and application of Lactobacillus plantarum
ActiveCN107629987AGood resistance to gastric acid and bile saltsAchieve inhibitionMilk preparationBacteriaMicroorganismGut flora
Owner:JIANGNAN UNIV
Methods and compositions for diagnosis and prognosis of renal injury and renal failure
ActiveUS20170248613A1Eliminate needDisease diagnosisBiological testingInterleukin 1 receptor, type IVascular Endothelial Growth Factor Receptor
Owner:ASTUTE MEDICAL
Thienopyrimidine and furopyrimidine derivative, its preparation method and application in medicines
ActiveCN103087077ANovel structureStrong inhibitory activityOrganic active ingredientsOrganic chemistryDiseaseTyrosine-kinase inhibitor
The invention discloses a thienopyrimidine and furopyrimidine derivative, its preparation method and its application in medicines. The derivative is a compound shown as general formula I, general formula II, general formula III or general formula IV. The thienopyrimidine and furopyrimidine pyrimidine derivative provided in the invention has an obvious EGFR (epidermal growth factor receptor) inhibitory activity, and some of the compounds also have an obvious inhibitory activity on VEGFR (vascular endothelial growth factor receptor), so that the thienopyrimidine and furopyrimidine pyrimidine derivative can be expected to be developed into tyrosine kinase EGFR or / and VEGFR inhibitors, which can be used for preparation of drugs preventing or treating diseases related to EGFR and / or VEGFR. Therefore, the derivative provided in the invention provides a new development direction and approach for developing novel tyrosine kinase inhibitor drugs that have low resistance or can alleviate early inhibitor resistance, and has wide application prospect and medicinal value.
Owner:JIANGSU DESANO PHARMA
Isoquinolinone derivatives, and preparation method and medical purpose thereof
The invention relates to the fields of pharmaceutical chemistry and organic chemistry, in particular to isoquinolinone derivatives. The compounds can be used for treating various medical indications associated with postmenopausal symptoms, uterine fiber lesions and arterial smooth muscle cell proliferation, particularly ER-(+) breast cancer by inhibiting alpha-estrogen receptor subtype (ER alpha) and through vascular endothelial growth factor receptor (VEGFR-2) bi-target. Meanwhile, the compounds have an obvious inhibiting effect on tumor metastasis, and have a general formula I.
Owner:CHINA PHARM UNIV
Nanocrystalline eye drop, and preparation method and application thereof
ActiveCN110664757AAvoid exclusionGood biocompatibilitySenses disorderNanomedicinePotocytosisTherapeutic effect
The present invention relates to the field of eye drops and particularly relates to a nanocrystalline eye drop, and a preparation method and an application thereof. The nanocrystalline eye drop comprises double-soluble macromolecules, single-soluble macromolecules and targeted drugs acting on vascular endothelial growth factor receptors and / or platelet growth factor receptors. The double-soluble macromolecules and the single-soluble macromolecules interact to encapsulate the targeted drugs to form nanocrystallines and maintain stability of the nanocrystallines. The eye drop can quickly penetrate a blood-eye barrier and enter a vitreous body through a special intercellular space penetration and / or pinocytosis method, an effective therapeutic effect is achieved through passive targeting andattachment, and at the same time, the drug is convenient to use.
Owner:CHENGDU RUIMU BIO PHARM TECH CO LTD
Charles ketone oxime and its composition , preparation method and uses
InactiveCN1807405AImprove solubilityInhibition of in vitro growthOximes preparationAmine active ingredientsSolubilityPhosphorylation
The related chalketoxime shown as the formula (1) is prepared by heating and reflux reacting the 2', 4'-dihydroxy -6'-methoxyl-3', 5'-dimethylchalcone and hydroxylamine hydrochloride in pyridine, which has well solvability, fit to direct inject for drug, restrains obviously all of the activity of blood vessel endothelium growth factor receptor, HER2 receptor and Tyr kinase as PDGFR receptor, the external growth of cells for breast cancer and liver cancer, and the phosphorylation of KDR in ECV304 cell, HER2 in MDA-MB-453 cell and PDGFR receptor in C6 cell, and benefit to treat tumor.
Owner:SOUTH CHINA BOTANICAL GARDEN CHINESE ACADEMY OF SCI +1
VEGF receptor antagonists
ActiveUS20050196396A1Shorten the progressSlow proliferationPeptide/protein ingredientsAntibody mimetics/scaffoldsOncologyPolynucleotide
Owner:ORBIS HEALTH SOLUTIONS
Drug composition preparation for recombining human vascular endothelial growth factor receptor-antibody fusion protein
ActiveCN108671229AInhibition of aggregation and precipitationAvoid hydrolysisPeptide/protein ingredientsAntibody ingredientsFreeze thawingBuffering agent
The invention relates to a drug composition preparation for recombining human vascular endothelial growth factor receptor-antibody fusion protein and preparation thereof. The drug composition preparation specifically comprises recombination fusion protein, a buffering agent, a stabilizing agent, a surfactant and sterilize injection water. The drug composition preparation is capable of effectivelyinhibiting fusion protein accumulating and depositing, hydrolyzing, oxidizing, decarboxamidation and other side reaction, and meanwhile, the stability of the product in pressurizing (high temperature,strong light irradiating, freeze thawing, and the like), accelerating and long-term frozen storing conditions can be effectively improved; and the safety in clinical use can be improved.
Owner:HUABO BIOPHARM
Human VEGFR-1 (Vascular Endothelial Growth Factor Receptor-1) targeting genetically engineered lymphocyte as well as preparation method and application thereof
ActiveCN102584999AHigh activitySuppress generationPolypeptide with localisation/targeting motifImmunoglobulin superfamilySingle-Chain AntibodiesPlasmid Vector
The invention relates to the field of gene engineering, and particularly relates to an anti-VEGFR-1 (Vascular Endothelial Growth Factor Receptor-1) mosaic type antigen receptor and lymphocyte capable of expressing the antigen receptor, and aims at providing a new and effective choice for the technical field of antitumor. The technical scheme for solving the technical problems is as follows: a single-chain antibody ScFv is provided, the single-chain antibody can recognize VEGFR-1, the single-chain antibody is prepared into the mosaic type antigen receptor which has a structure of (ScFv-V)-(IgG1-Fc)-(CD4-TM)-(CD3-z), the encoding gene of the antigen receptor is transformed into a plasmid vector, and the plasmid vector is transfected to lymphocyte, so that the lymphocyte has antitumor action, thereby providing the new and effective choice for the field.
Owner:SICHUAN UNIV +1
Epitope peptides derived from vascular endothelial growth factor receptor 1 and vaccines containing these peptides
ActiveUS20090214581A1High cytotoxic T cell inducibilityGrowth inhibitionSenses disorderPeptide/protein ingredientsImmunogenic peptideVascular Endothelial Growth Factor Receptor
The present invention provides immunogenic peptides comprising the amino acid sequence of SEQ ID NO: 1, 2, 13, 32, and peptides comprising the above-mentioned amino acid sequences in which 1, 2, or several amino acids are substituted or added, and having cytotoxic T cell inducibility, and also provides drugs for treating or preventing tumors comprising these peptides. The peptides of this invention can be used as vaccines.
Owner:ONCOTHERAPY SCI INC
Quinazolinyl aryl urea derivatives and preparation method and application thereof
ActiveCN102532103AStrong enzyme inhibitionLow toxicityOrganic active ingredientsOrganic chemistryDiseaseUrea derivatives
The invention relates to quinazolinyl aryl urea derivatives with a general formula I and a preparation method and application thereof, wherein R1, R2 and R3 respectively have meanings limited in a specification. The invention further relates to the preparation method of the derivatives, and a physiologically-acceptable salt formed by the derivatives and an inorganic acid or an organic acid includes a medicinal combination of the derivatives. The compounds have a valuable pharmacologic property, particularly have an inhibition effect on the signal transduction caused by a tyrosine kinase, particularly have higher inhibition activity on mutant VEGFR-2 (Vascular Endothelial Growth Factor Receptor-2), and furthermore, have lower toxicity. The invention further relates to the application of the quinazolinyl aryl urea derivatives in the treatment of diseases, particularly tumor diseases, and the preparation method of the quinazolinyl aryl urea derivatives.
Owner:天津天诚新药评价有限公司
Recombinant Adenovirus Having Anti-Angiogenesis Activity
InactiveUS20130101557A1Inhibit angiogenesisCancer treatment is limitedSenses disorderVirusesDiseaseNucleotide
The present disclosure relates to a recombinant adenovirus with improved angiogenesis inhibition activity and a pharmaceutical composition for inhibiting angiogenesis. The recombinant adenovirus includes: (a) an inverted terminal repeat (ITR) nucleotide sequence of an adenovirus; and (b) a nucleotide sequence coding for a chimeric decoy receptor containing (i) an extracellular domain of vascular endothelial growth factor receptor 1 (VEGFR-1) and (ii) an extracellular domain of vascular endothelial growth factor receptor 2 (VEGFR-2). The recombinant adenovirus according the present disclosure which expresses the chimeric decoy receptor inhibits angiogenesis very effectively and can be used for gene therapy for various angiogenesis-related diseases. Particularly, the recombinant adenovirus of the present disclosure has superior oncolytic activity.
Owner:IUCF HYU (IND UNIV COOP FOUND HANYANG UNIV)
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