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81 results about "Protein Tyrosine Kinase Inhibitors" patented technology

A tyrosine kinase inhibitor (TKI) is a pharmaceutical drug that inhibits tyrosine kinases. Tyrosine kinases are enzymes responsible for the activation of many proteins by signal transduction cascades. The proteins are activated by adding a phosphate group to the protein (phosphorylation), a step that TKIs inhibit.

Method for designing protein kinase inhibitors

The present invention provides a method for identifying inhibitors of protein kinases. Methods are also provided for inhibiting protein kinase activity. Specific non-peptide protein tyrosine kinase inhibitor are provided. The protein kinases produced using the method of the present invention may be used to treat a number of conditions in patients, including cancer, psoriasis, arthrosclerosis, or immune system activity.
Owner:THE RES FOUND OF STATE UNIV OF NEW YORK

Identification of polynucleotides for predicting activity of compounds that interact with and/or modulate protein tyrosine kinases and/or protein tyrosine kinase pathways in lung cancer cells

The present invention describes polynucleotides that have been discovered to correlate to the relative intrinsic sensitivity or resistance of cells, e.g., lung cell lines, to treatment with compounds that interact with and modulate, e.g., inhibit, protein tyrosine kinases, such as, for example, members of the Src family of tyrosine kinases, e.g., Src, Fgr, Fyn, Yes, Blk, Hck, Lck and Lyn, as well as other protein tyrosine kinases, including, Bcr-abl, Jak, PDGFR, c-kit and Ephr. These polynucleotides have been shown, through a weighted voting cross validation program, to have utility in predicting the resistance and sensitivity of lung cell lines to the compounds. The expression level of some polynucleotides is regulated by treatment with a particular protein tyrosine kinase inhibitor compound, thus indicating that these polynucleotides are involved in the protein tyrosine kinase signal transduction pathway, e.g., Src tyrosine kinase. Such polynucleotides, whose expression levels correlate highly with drug sensitivity or resistance and which are modulated by treatment with the compounds, comprise polynucleotide predictor or marker sets useful in methods of predicting drug response, and as prognostic or diagnostic indicators in disease management, particularly in those disease areas, e.g., lung cancer, in which signaling through the protein tyrosine kinase pathway, such as the Src tyrosine kinase pathway, is involved with the disease process.
Owner:BRISTOL MYERS SQUIBB CO

Small molecule thienopyrimidine-based protein tyrosine kinase inhibitors

Various thienopyrimidine-based analog compounds are able to selectively inhibit the Src family of tyrosine kinases. These compounds are useful in the treatment of various diseases including hyperproliferative diseases, hematologic diseases, osteoporosis, neurological diseases, autoimmune diseases, allergic / immunological diseases, or viral infections.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST

EGFR inhibitor and preparing method and application thereof

The invention discloses an EGFR inhibitor. The EGFR inhibitor is of the structure shown in the formula (I) and is a compound including alpha, beta-unsaturated carboxylic acid amides. Meanwhile, the invention discloses a preparing method of the compound and the application of the compound serving as a protein tyrosine kinase inhibitor, especially the inhibiting function on T790M variant EGFR as the EGFR inhibitor, and the application on treating diseases such as the kidney cancer, the ling cancer, the prostate cancer, the pancreatic cancer the breast cancer and the spongiocytoma which are related to EGFR over expression. The structure is shown in the specification.
Owner:NANJING LEIKEXING BIOTECH CO LTD

Dicoumarol compound, as well as preparation method and application thereof

The invention relates to a dicoumarol compound shown in a general formula I, wherein definition of each substituent is described in the specification. The invention also relates to a preparation method of the dicoumarol compound, and application of the dicoumarol compound serving as protein tyrosine kinase inhibitor in the field of tumor resistance.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI

Medical devices comprising a protein-tyrosine kinase inhibitor to inhibit restonosis

Implantable medical devices having an anti-restenotic coatings are disclosed. Specifically, implantable medical devices having coatings of proteintyrosine kinase inhibitors are disclosed. The anti-restenotic protein-tyrosine kinase inhibitor is 4+4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2pyrimidinyl]amino]-phenyl]benzamide methanesulfonate and pharmaceutically acceptable derivatives thereof (imatinib mesylate). The anti-restenotic medial devices include stents, catheters, micro-particles, probes and vascular grafts. The medical devices can be coated using any method known in the art including compounding the protein-tyrosine kinase inhibitor with a biocompatible polymer prior to applying the coating. Moreover, medical devices composed entirely of biocompatible polymer-protein-tyrosine kinase inhibitor blends are disclosed. Additionally, medical devices having a coating comprising at least one proteintyrosine kinase inhibitor in combination with at least one additional therapeutic agent are also disclosed. Furthermore, related methods of using and making the antirestenotic implantable devices are also disclosed.
Owner:MEDTRONIC VASCULAR INC

Method of treatment of philadelphia chromosome positive leukaemia

InactiveUS20120244116A1Organic active ingredientsPeptide/protein ingredientsBcr-Abl tyrosine-kinase inhibitorLestaurtinib
The invention provides a method for the treatment of Ph+ leukemia in a patient comprising administering to the patient (i) a BCR-ABL tyrosine kinase inhibitor, and (ii) an agent which selectively binds to a cell surface receptor expressed on Ph+ leukemic stem cells. The invention further provides for the use of (i) and (ii) in, or in the manufacture of a medicament for, the treatment of Ph+ leukemia in a patient; and a composition for the treatment of Ph+ leukemia in a patient comprising (i) and (ii); and kits comprising (i) and (ii). In some embodiments, the tyrosine kinase inhibitor is or is not imatinib; or is selected from the group consisting of dasatinib, nilotinib, bosutinib, axitinib, cediranib, crizotinib, damnacanthal, gefitinib, lapatinib, lestaurtinib, neratinib, semaxanib, sunitinib, toceranib, tyrphostins, vandetanib, vatalanib, INNO-406, AP24534, XL228, PHA-739358, MK-0457, SGX393 and DC2036; or is selected from the group consisting of dasatinib and nilotinib. In some embodiments, the agent binds to a receptor involved in signalling by at least one of IL-3, G-CSF and GM-CSF. In some embodiments, the agent is a mutein selected from the group consisting of IL-3 muteins, G-CSF muteins and GM-CSF muteins. In some embodiments, the mutein is an IL-3 mutein. In some embodiments, the agent is a soluble receptor which is capable of binding to IL-3.
Owner:CSL LTD

Series of quinazoline sugar derivatives used as protein tyrosine kinase inhibitor, preparation method and application thereof

InactiveCN101857618ASolve the problem of low activity of inhibiting tyrosine kinaseGood water solubilityOrganic active ingredientsSugar derivativesSolubilityProtein-Tyrosine Kinases
The invention provides a quinazoline sugar derivative and a preparation method and application thereof, which can solve the problem of low activity of inhibiting tyrosine kinase in the prior art. The prepared quinazoline sugar derivative has high water solubility and high activity of inhibiting human skin cancer cells A431, and can be used for preparing medicaments for preventing or treating tumors. The quinazoline sugar derivative provided by the invention is a kind of compounds which have novel structures and comprise abundant glycosyl group segments at a 6-bit side chain of a quinazoline parent ring, wherein the raw materials adopted in a method for performing glycosylation on quinazoline rings are readily available; the synthesis method is simple; the purification mode is simple and convenient and quick; and the quinazoline sugar derivative has high water solubility, high biological activity, particularly obvious activity of selectively inhibiting an EGFR, and obvious anti-tumor effect, so the kind of compounds has a wide application prospect in medicaments for preventing or curing tumors. The quinazoline sugar derivative comprises the following structural formula.
Owner:OCEAN UNIV OF CHINA

Method for reducing hypertension and heart failure

A method is provided for reducing hypertension and / or heart failure in a mammal. Preferably, the method is used to treat or prevent tissue damage to a human heart. The method includes administering an effective amount of a Jak2 inhibitor, preferably a tyrphostin, such as AG490.
Owner:THE RES FOUND OF STATE UNIV OF NEW YORK

Protection against and treatment of hearing loss

The present invention provides a method for protecting against or treating hearing loss in a subject. This method involves administering an effective amount of a protein tyrosine kinase inhibitor to the subject to protect against or to treat hearing loss.
Owner:THE RES FOUND OF STATE UNIV OF NEW YORK +1

c-KIT Phosphorylation in Cancer

An antibody is disclosed for the detection of phosphorylated c-KIT. A method of diagnosing and monitoring cancers responsive to treatment using an anti-phospho-c-KIT antibody are also disclosed. A diagnostic kit is also provided for the detection and monitoring of cancers responsive to tyrosine phosphorylation inhibitor treatment.
Owner:APOCELL

Oligomer-Protein Tyrosine Kinase Inhibitor Conjugates

The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water soluble, non peptidic oligomer.
Owner:NEKTAR THERAPEUTICS INC

Non-myeloablative tolerogenic treatment with tyrphostins

InactiveUS20040197335A1Compounds screening/testingNervous disorderTolerogenic therapyTolerability
A method of inducing immune tolerance in a first mammal to antigens of a second, non-syngeneic, mammal, is disclosed. The method is utilized to minimize graft rejection and / or reduce graft-versus-host diseases in transplantation procedures and to produce hematopoietic mixed chimeras. Methods of determining the activity of tyrphostins and the optimal concentration thereof in this method are also disclosed.
Owner:YISSUM RES DEV CO OF THE HEBREWUNIVERSITY OF JERUSALEM LTD +1

Diarylurea derivatives and application thereof used for preparing anti-neoplastic medicament

The invention belongs to the field of medical technology, which relates to diarylurea derivatives or salts accepted in medicine shown in formula I, wherein substituents of Ar1, Ar2, X and n have definitions given in an instruction. The derivatives shown in the formula I can be used for preparing receptor protein-tyrosine kinase inhibitor (RPTKI), and medicaments used for treating and / or preventingcancer or other proliferative diseases. The derivatives or salts accepted in medicine can be taken as active ingredients for preparing composition or different preparations used in clinical requirement mixed together with different carriers or excipient in medicine so as to be used for treating and / or preventing from various cancers.
Owner:SHENYANG PHARMA UNIVERSITY

Quinazoline and quinoline derivatives as irreversible protein tyrosine kinase inhibitors

A compound of formula (I), a pharmaceutically acceptable salt, or hydrate thereof, and a method of preparing the same. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase activity in a mammal comprising administering to said mammal a pharmaceutical composition comprising a compound of formula (I).
Owner:TIANJIN HEMAY ONCOLOGY PHARMA CO LTD

Anti-vascular and anti-proliferation methods, therapies, and combinations employing specific tyrosine kinase inhibitors

This invention is directed to potent inhibitors of protein tyrosine kinase alone or in synergistic combination with antiangiogenic or chemotherapeutic agents for the abrogation of mature vasculature within chemotherapeutic refractory tumors, pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders / conditions involving cell proliferation, and particularly treatment of brain cancer, ovarian cancer, pancreatic cancer prostate cancer, and human leukemias, such as CML, AML or ALL.
Owner:AVENTIS PHARMA SA (US)

Oligomer-protein tyrosine kinase inhibitor conjugates

The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water-soluble, non-peptidic oligomer.
Owner:NEKTAR THERAPEUTICS INC

Methods and agents for inhibiting dynamin-dependent endocytosis

There are disclosed methods for inhibiting dynamin-dependent endocytosis in cells comprising treating the cells with an effective amount of a compound of formula (I), or a dimeric tyrphostin, physiologically acceptable salt, or prodrug thereof. Compounds useful in the methods described are also provided. The inhibition of dynamin-dependent endocytosis of cells is applicable to the treatment of epilepsy and neurological disorders and conditions.
Owner:UNIV OF NEWCASTLE RES ASSOCS +1

Novel protein kinase modulators and therapeutic uses thereof

The present invention provides new tyrphostin derivatives acting as protein tyrosine kinase (PTK) inhibitors and receptor tyrosine kinase (RTK) inhibitors, and / or which directly or indirectly affect proteins in the PTK-mediated signal transduction pathway, methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for preventions and treatments of PTK and RTK related disorders such as metabolic, fibrotic, and cell proliferative disorders, in particular psoriasis and cancer.
Owner:NOVOTYR THERAPEUTICS LTD

Quinazoline and quinoline derivatives as irreversibe protein tyrosine kinase inhibitors

A compound of formula (I),a pharmaceutically acceptable salt, or hydrate thereof, and a method of preparing the same. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase activity in a mammal comprising administering to said mammal a pharmaceutical composition comprising a compound of formula (I).
Owner:TIANJIN HEMAY ONCOLOGY PHARMA CO LTD
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