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57 results about "Tyrosine Protein Kinases" patented technology
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3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders
Owner:JANSSEN PHARMA NV
Methods of modulating c-kit tyrosine protein kinase function with indolinone compounds
Owner:SUGEN INC
Quinoline derivative, preparation method and medical use thereof
InactiveCN101012224AImprove function and effectOrganic active ingredientsOrganic chemistryTyrosine Protein KinasesDisease
The invention discloses a making method of compound I and drug composition and application to treat tumour, which is 3-nitrile quinoline derivant (I) as dual-inhibitor protein kinase of tyrosine and nitric oxide synthase, wherein G1, G2, G3, G4, X, Z and n are defined as instruction.
Owner:CHINA PHARM UNIV
Protein tyrosine kinase modulators and methods of use
InactiveCN105377835AOrganic active ingredientsOrganic chemistryKinase activityTyrosine Protein Kinases
Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and / or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative,and methods of treatment for diseases associated with protein kinase enzymatic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed.
Owner:BETTA PHARM CO LTD
Application of indazole bi-aryl urea compound serving as protein kinase inhibitor
The invention relates to application of a series of indazole bi-aryl urea compounds and pharmaceutically acceptable salts thereof serving as protein kinase inhibitors to preparation of medicaments for treating diseases relevant to protein kinase activity, including tumors, inflammations, diseases relevant to autoimmunity reaction and diseases relevant to stem cells. As proved by experimental study, the indazole bi-aryl urea compounds and the pharmaceutically acceptable salts thereof play important roles in medical treatment and adjusting the activities of kinases such as KIT, PDGF (Platelet Derivation Growth Factor)-alpha, PDGF-beta, CSF1R (Colony Stimulating Factor 1 Receptor), DDR1and FLT3 of an original and / or mutative receptor tyrosine kinase (RTK) family and / or CDK8 (Cyclin-Dependent Kinase 8), CDK11 and HIPK4 (Homeodomain Interacting Protein Kinase 4) and the like of a CDK family. Preferred protein kinases are Kit, PDGF-alpha, PDGF-beta and FLT3 of the RTK family as well as CDK8 and CDK11 of the CDK family.
Owner:JINAN HAILE MEDICAL TECH DEV
Heteroaryl imidazolone derivatives as JAK inhibitors
New heteroaryl imidazolone derivatives having the chemical structure of formula (I) disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
Owner:ALMIRALL
Process for preparing N-phenyl-2-pyrimidyl amine derivative
The present invention relates to new organic compound, and is especially the preparation process of N-(2-methyl-5-nitro) phenyl-4-(3-pyridyl) pyrimidiyl-2-amine as the key intermediate for imatinib, which is tyrosine protein kinase inhibitor for treating chronic myeloid leukemia and other diseases, and its analog N- phenyl-pyrimidiyl-2-amine derivative. The target product may be prepared through condensation of 4-aromatic heterocycle-2-halogenated pyrimidine and substituted aniline in the presence of catalyst. The preparation process has low material cost, scientific synthesis path, high product yield and other advantages.
Owner:ZHEJIANG ACAD OF MEDICAL SCI
Phenyl urazan nitrogen nitric oxide donor 2-aniline pyrimidine derivatives, preparation method, compound containing the same and use thereof
ActiveCN101225085AAdvantagesHas inhibitory effectOrganic active ingredientsOrganic chemistryTyrosine Protein KinasesDisease
The invention discloses a compound used as a general formula (I) of protein kinase inhibitor, the salt accepted pharmaceutically and the preparation method; wherein, X is -(CH2)m-COO-; m is equal to 1 to 5 or direct bond; Y is -(CH2)n-O- or -(CH2)n-PhO-; n is equal to1 to 10 or direct bond; the preparation method comprises a step which uses N-(5-amino-2- methyl-phenyl)-4- (3-pyridyl)-2-pyrimidinamine and general formula (II) compound as raw material synthesis. The invention also discloses the preparation method of the compound, comprising the compound and the treatment of being used as tyrosine protein kinase inhibitor in diseases such as cancer relative to tyrosine in particular to Bcr-Abl.
Owner:JIANGSU TASLY DIYI PHARMA CO LTD
Application of 5,6,7,4'-tetrahydroxyflavone and derivatives thereof as JAK tyrosine protein kinase inhibitor
The invention relates to the field of medicines, discloses application of 5,6,7,4'-tetrahydroxyflavone and derivatives thereof as a JAK tyrosine protein kinase inhibitor, and especially relates to application of 5,6,7,4'-tetrahydroxyflavone and derivatives thereof as a JAK tyrosine protein kinase inhibitor in preparing medicines for treating diseases related to JAK / STAT signal transduction pathway abnormity. The 5,6,7,4'-tetrahydroxyflavone and derivatives thereof provided in the invention have a strong inhibition effect on JAK tyrosine protein kinase and an enzymological binding characteristic of competitive inhibition; the 5,6,7,4'-tetrahydroxyflavone and derivatives thereof further can penetrate cell membranes and effectively intercept activation of a JAK / STAT signal transduction pathway, thereby inhibiting lymphocytes from secreting cytokines such as interferon to peripheral tissue. According to pharmacological research, the 5,6,7,4'-tetrahydroxyflavone and derivatives thereof have an obvious effect in relaxing vessels; therefore, it is indicated that the 5,6,7,4'-tetrahydroxyflavone and derivatives thereof have a critical clinical application value.
Owner:KPC PHARM INC
Translocation and mutant ros kinase in human non-small cell lung carcinoma
ActiveCN101528921AOrganic active ingredientsAntibody mimetics/scaffoldsProto-Oncogene Tyrosine-Protein Kinase ROSNucleotide
In accordance with the invention, a novel gene translocation, (4p15, 6q22), in human non-small cell lung carcinoma (NSCLC) that results in a fusion proteins combining part of Sodium-dependent Phosphate Transporter lsoform NaPi-3b protein (SLC34A2) with Proto- oncogene Tyrosine Protein Kinase ROS Precursor (ROS) kinase has now been identified. The SLC34A2-ROS fusion protein is anticipated to drive the proliferation and survival of a subgroup of NSCLC tumors. The invention therefore provides, in part, isolated polynucleotides and vectors encoding the disclosed mutant ROS kinase polypeptides, probes for detecting it, isolated mutant polypeptides, recombinant polypeptides, and reagents for detecting the fusion and truncated polypeptides. The disclosed identification of the new fusion protein enables new methods for determining the presence of these mutant ROS kinase polypeptides in a biological sample, methods for screening for compounds that inhibit the proteins, and methods for inhibiting the progression of a cancer characterized by the mutant polynucleotides or polypeptides, which are also provided by the invention.
Owner:CELL SIGNALING TECHNOLOGY
Application of 4', 5, 7-genistein in preparing rotavirus resisting medicine
InactiveCN103462977APoor resolutionSolve the problem of large toxic side effectsOrganic active ingredientsDigestive systemRotavirus RNABiological activation
The invention discloses application of 4', 5, 7-genistein in preparing rotavirus resisting medicine. The genistein can restrain damage of tyrosine protein kinase to cell junction by restraining activation, caused by rotavirus infection, of tyrosine protein kinase of intestinal epithelial cells, so that the intestinal epithelial cells are prevented from being damaged by rotavirus, the completeness of intestinal mucosa is protected, the symptom of rotavirus diarrhea is obviously reduced, and the lethality is reduced. Thus, when the genistein is used as a main active ingredient, high-efficient and low-toxicity specificity rotavirus diarrhea resisting medicine can be researched and developed hopefully.
Owner:ARMY MEDICAL UNIV
Novel compounds
InactiveUS20190210996A1Organic active ingredientsOrganic chemistryProtein-Tyrosine KinasesBruton's tyrosine kinase
A method of treating disorders associated with aberrant kinase activity, wherein the kinase is. Adaptor-associated protein kinase 1 (AAK1), Aurora Kinase A (AURKA), Aurora Kinase B (AURKB), Bruton's Tyrosine Kinase (BTK), Interleukin-1 receptor-associated kinase 3 (IRAK3), Protein tyrosine kinase 2 beta (PTK2B), Tyrosine-protein kinase Tec (TEC), Serine / threonine-protein kinase Wee1 (WEE1), Cyclin G-associated kinase (GAK), Large Tumour suppressor 1 Kinase (LATS1), Focal Adhesion Kinase (PTK2), Ribosomal protein S6 kinase alpha-1 (RPS6KA1) said method comprising degrading said kinase.
Owner:GLAXOSMITHKLINE INTPROP DEV LTD
Quinazoline derivatives and quinazoline complex protein kinase inhibitor for inhibiting multiplicaiton of tumor cells and preparation method thereof
ActiveUS20130225811A1Strong inhibitory activityEnhanced inhibitory effectRuthenium organic compoundsGroup 4/14 element organic compoundsProstate cancer cellPTK Inhibitors
Quinazoline derivatives represented by general formula (1) and quinazoline complexes as protein kinase inhibitors, and their preparation methods are provided. Wherein, in general formula (1), at least one of R and R′ is a group containing an atom capable of coordinating with noble metals, m and n are either the same or different and are integers from 0 to 5. Said quinazoline complex as protein kinase inhibitor is formed by coordination compound containing noble metal and said quinazoline derivative ligand capable of coordinating with noble metal in the coordination compound. Used as tyrosine protein kinase inhibitors, Quinazoline derivatives and quinazoline complexes as protein kinase inhibitors provided by the present invention have exhibited good inhibitory effect on proliferation of various tumor cells including human breast cancer cells line (drug-resistant) MCF-7 / A, human breast cancer cell line (sensitive) MCF-7 / S, prostate cancer cell PC-3, keratinocytes Colo-16, human non-small cell lung cancer cell line A549, etc.
Owner:INST OF CHEM CHINESE ACAD OF SCI
Application of NRG1 (neuregulin1)-ERBB4 complex in preparing medicaments for treating myocardial ischemia
InactiveCN104922153AImprove survival rateImprove enduranceUnknown materialsCardiovascular disorderEndurance capacityOxygen deficient
The invention provides an application a complex (NRG1-ERBB4 complex) of NRG1 (neuregulin1) and a tyrosine kinase receptor ERBB4 thereof in preparing medicaments for treating myocardial ischemia. The invention provides a medicament for treating the myocardial ischemia by using the NRG1-ERBB4 complex as a target. Preferably, the medicament is mesenchymal stem cells (MSC) modified by ERBB4 genes. ERBB4 is over-expressed in the MSC by lentivirus, and therefore, the expression of a ligand NRG1 of the ERBB4 is up-regulated in a feedback manner so as to form a medicament having an NRG1-ERBB4-NRG1 self-feedback channel, so that not only is the endurance capacity of the MSCC on an oxygen-deficient environment improved, but also the concentration of high-level NRG1 is kept by means of the NRG1-ERBB4-NRG1 self-feedback channel, a protection role of the MSC on myocardial cells is improved and enhanced, and a curative effect of the medicament for treating the myocardial ischemia is improved.
Owner:连祺周
5,8-disubstituted-1,6-naphthyridine-7-carbonyl amide compounds, dimer compounds of 5,8-disubstituted-1,6-naphthyridine-7-carbonyl amide compounds, and preparation method and use of 5,8-disubstituted-1,6-naphthyridine-7-carbonyl amide compounds and dimer compounds of 5,8-disubstituted-1,6-naphthyridine-7-carbonyl amide compounds
InactiveCN102558172ABroaden the structure typeStrong inhibitory activityOrganic active ingredientsOrganic chemistryTyrosine Protein KinasesProtein-Tyrosine Kinases
The invention discloses 5,8-disubstituted-1,6-naphthyridine-7-carbonyl amide compounds, dimer compounds of the 5,8-disubstituted-1,6-naphthyridine-7-carbonyl amide compounds, a preparation method and use of the 5,8-disubstituted-1,6-naphthyridine-7-carbonyl amide compounds and the dimer compounds of the 5,8-disubstituted-1,6-naphthyridine-7-carbonyl amide compounds, and pharmaceutical compositions containing the 5,8-disubstituted-1,6-naphthyridine-7-carbonyl amide compounds. More specifically, the invention discloses the 5,8-disubstituted-1,6-naphthyridine-7-carbonyl amide compounds expressed by structural formulae I and II or III, the dimer compounds of the 5,8-disubstituted-1,6-naphthyridine-7-carbonyl amide compounds and the preparation method of the 5,8-disubstituted-1,6-naphthyridine-7-carbonyl amide compounds and the dimer compounds of the 5,8-disubstituted-1,6-naphthyridine-7-carbonyl amide compounds, and provides the use of the 5,8-disubstituted-1,6-naphthyridine-7-carbonyl amide compounds and the pharmaceutical compositions containing the 5,8-disubstituted-1,6-naphthyridine-7-carbonyl amide compounds in the treatment of diseases related to protein tyrosine kinase, in particular to c-Src, such as tumor diseases, by serving as a multi-target spot protein tyrosine kinase inhibitor.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Porcine anti-porcine reproductive and respiratory syndrome related SNP label in tyrosine protein kinase JAK2 gene and application thereof
InactiveCN104046621ASpeed up the breeding processPrecise screeningMicrobiological testing/measurementDNA/RNA fragmentationNucleotideScreening method
The invention relates to a porcine anti-porcine reproductive and respiratory syndrome (PRRS) related SNP label in a tyrosine protein kinase JAK2 gene and application thereof. The porcine anti-porcine reproductive and respiratory syndrome related SNP label is located on the porcine tyrosine protein kinase JAK2 gene. The nucleotide sequence of the SNP label is shown as SEQ ID NO.1, wherein a to-be-tested pig with 81bp, 115bp, 151bp and 264bp basic groups respectively as T, A, G and A at the sequence belongs to a PRRS susceptible pig variety, and a to-be-tested pig with the four basic groups respectively as C, G, A and T belongs to an anti-PRRS pig variety. The molecular genetic label provided by the invention is not restricted by porcine age, gender and the like, can be used for early breeding of the anti-PRRS pig variety, and even can realize accurate screening of newborn pigs, thus greatly accelerating the breeding process of anti-PRRS pigs. The screening method is accurate, and has the advantages of simple operation, low cost, and high efficiency.
Owner:CHINA AGRI UNIV
Method for the recombinant production and purification of protein kinases
A method for the recombinant production and purification of a protein kinase selected from the group consisting of tyrosine protein kinases and serine / threonine kinases by expressing a nucleic acid encoding said kinase in a microbial host cell, forming inclusion bodies containing said kinase, isolating, solubilizing, naturing, and purifying said kinase wherein said purification is performed by hydrophobic interaction with an hydrophobic adsorbent under conditions whereby at least 70% of said protein kinase are not bound to said adsorbent and the protein kinase not bound to said adsorbent is recovered.
Owner:F HOFFMANN LA ROCHE & CO AG
Methods and compositions for diagnosis and prognosis of renal injury and renal failure
ActiveUS20180209990A1Eliminate needEasy to adaptDisease diagnosisBiological testingTyrosine Protein KinasesAssay
The present invention relates to methods and compositions for monitoring, diagnosis, prognosis, and determination of treatment regimens in subjects suffering from or suspected of having a renal injury. In particular, the invention relates to using assays that detect one or more of C-C motif chemokine 16, C-C motif chemokine 14, and Tyrosine-protein kinase receptor UFO as diagnostic and prognostic biomarker assays in renal injuries.
Owner:ASTUTE MEDICAL
Protein tyrosine kinase modulators salt, crystallographic forms, and uses thereof
InactiveCN109311845AOrganic active ingredientsAntipyreticTyrosine Protein KinasesProtein-Tyrosine Kinases
The invention relates to N-(5-(5-chloro-4-(2-(2-(dimethylamino)-2-oxoacetyl)phenylamino) pyrimidin-2-ylamino)-4-methoxy-2-(4-methylpiperazin-1-yl)phenyl) acrylamide succinate (the compound of FormulaI) and new crystalline forms thereof, processes for their preparation, their uses in therapy and the pharmaceutical compositions containing them.
Owner:BETTA PHARM CO LTD
Application of pharmaceutical composition in preparation of Chinese herba preparation for treating functional dyspepsia
InactiveCN107362220AIncrease contentReduce contentDigestive systemPlant ingredientsSide effectVasoactive intestinal peptide
The invention provides an application of a pharmaceutical composition in preparing a traditional Chinese medicine preparation for treating functional dyspepsia. The pharmaceutical composition comprises fenugreek, bran-fried citrus aurantium and red ginseng. The pharmaceutical composition is used for controlling body weight change caused by functional dyspepsia; for reducing the content of nitric oxide in serum; for regulating plasma gastrin, motilin, somatostatin and vasoactive intestinal peptide ; for enhancing the expression of tyrosine protein kinase receptor C-kit and mammary gland-related peptide TFF1 in gastric mucosa. The present invention utilizes a reasonable preparation method and combines the synergistic effects of fragrant tea vegetables, bran-fried citrus aurantium and red ginseng, and can effectively treat functional dyspepsia with little side effect.
Owner:HANGZHOU HUQINGYUTANG PHARM CO LTD
Process for preparing N-phenyl-2-pyrimidyl amine derivative
Owner:ZHEJIANG ACAD OF MEDICAL SCI
Methods of modulating c-kit tyrosine protein kinase function with indolinone compounds
InactiveUS20050288353A1Prevent and alleviate and ameliorate symptomImprove survivalBiocideSenses disorderTyrosine Protein KinasesKinase activity
Owner:SUGEN INC
Quinoline derivative, preparation method and medical use thereof
InactiveCN100540551CImprove function and effectOrganic active ingredientsOrganic chemistryDiseaseTyrosine Protein Kinases
The present invention relates to the field of medicinal chemistry, in particular to a class of 3-cyanoquinoline derivatives (I), a dual inhibitor of tyrosine protein kinase and nitric oxide synthase, wherein G1, G2, G3, G4, X, Z, See the specification for the definition of n. The invention also discloses a preparation method of compound I, a pharmaceutical composition containing it, and an application for treating tumor diseases.
Owner:CHINA PHARM UNIV
Bruton's tyrosine protein kinase inhibitor and application thereof
PendingCN114085207AHigh selectivityReduce off-target effectsOrganic active ingredientsOrganic chemistryImmunologic disordersAutoimmune condition
The invention relates to a compound as shown in a formula (I), and an isomer, a deuterated substance, an active metabolite, a solvate or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition containing the compound or the isomer, the deuterated substance, the active metabolite, the solvate or the pharmaceutically acceptable salt thereof, and a Bruton's tyrosine protein kinase (BTK) inhibitor. The invention also provides application of the substances in treatment of tumors, autoimmune diseases, allergic diseases, inflammation and other diseases caused by BTK abnormality.
Owner:GUANGZHOU BIOTING PHARM TECH CO LTD
Phenyl urazan nitrogen nitric oxide donor 2-aniline pyrimidine derivatives, preparation method, compound containing the same and use thereof
ActiveCN101225085BAdvantagesHas inhibitory effectOrganic active ingredientsOrganic chemistryTyrosine Protein KinasesPTK Inhibitors
The present invention discloses a compound used as a general formula (I) of protein kinase inhibitor, the salt accepted pharmaceutically and the preparation method; wherein, X is -(CH2)m-COO-; m is equal to 1 to 5 or direct bond; Y is -(CH2)n-O- or -(CH2)n-PhO-; n is equal to1 to 10 or direct bond; the preparation method comprises a step which uses N-(5-amino-2- methyl-phenyl)-4- (3-pyridyl)-2-pyrimidinamine and general formula (II) compound as raw material synthesis. The present invention also discloses the preparation method of the compound, comprising the compound and the treatment of being used as tyrosine protein kinase inhibitor in diseases such as cancer relative to tyrosine in particular to Bcr-Abl.
Owner:JIANGSU TASLY DIYI PHARMA CO LTD
Novel tyrosine protein kinase inhibitor
The invention provides a novel and effective tyrosine protein kinase inhibitor, its isomer, pharmaceutically acceptable salts and chemical protection form, and pharmaceutical composition of the novel tyrosine protein kinase inhibitor and a pharmaceutical carrier or a diluent. The novel tyrosine protein kinase inhibitor can effectively treat protein kinase abnormity-caused diseases, and can effectively inhibit c-Met or c-Met mutant, and ALK or ALK fusion protein.
Owner:NANJING SANHOME PHARMACEUTICAL CO LTD
Kit for detecting mRNA (messenger ribonucleic acid) expression quantity of U BCR fusion gene
ActiveCN102925557AStrong specificityImprove accuracyMicrobiological testing/measurementFluorescence/phosphorescencePositive controlFluorescence
The invention discloses a kit for detecting the mRNA (messenger ribonucleic acid) expression quantity of U BCR fusion gene, belonging to the field of biotechnology. The kit comprises a detection primer, a fluorescent probe, a cDNA (complementary deoxyribonucleic acid) first strand synthesis reagent, fluorescent quantitative PCR (polymerase chain reaction) mixed solution, a negative control and a positive control, wherein the detection primer and the fluorescent probe comprise a U BCR fusion gene primer, an internal reference gene ABL primer and a Taqman fluorescent probe. The U BCR fusion gene is mainly found in chronic neutrophilic leukaemia with Ph+, and the gene code is high in the activity of tyrosine protein kinase, so that cells perform excessive multiplication and differentiation in case of no independence on cell factors, and normal cell apoptosis is inhibited. The mRNA level of the U BCR fusion gene is detected by adopting fluorescent quantitative PCR, and the specificity and the sensitivity of the detection result are remarkably improved. Via the kit, a novel rapid, simple and convenient gene diagnosis technology is provided for diagnosis, prediction and prognosis, and chemotherapy for chronic neutrophilic leukaemia.
Owner:HUAXIN SCI & TECH PANYU CITY
Application of 5,6,7,4'-tetrahydroxyflavone and its derivatives in the preparation of jak tyrosine protein kinase inhibitors
Owner:KPC PHARM INC
Method for extracting quantitative information relating to an influence on a cellular response
InactiveUS8058008B2New informationHigh selectivitySugar derivativesMicrobiological testing/measurementDiseaseSTAT5
Cells are genetically modified to express a luminophore, e.g., a modified (F64L, S65T, Y66H) Green Fluorescent Protein (GFP, EGFP) coupled to a component of an intracellular signalling pathway such as a transcription factor, a cGMP- or cAMP-dependent protein kinase, a cyclin-, calmodulin- or phospholipid-dependent or mitogen-activated serine / threonin protein kinase, a tyrosine protein kinase, or a protein phosphatase (e.g. PKA, PKC, Erk, Smad, VASP, actin, p38, Jnk1, PKG, IkappaB, CDK2, Grk5, Zap70, p85, protein-tyrosine phosphatase 1C, Stat5, NFAT, NFkappaB, RhoA, PKB). An influence modulates the intracellular signalling pathway in such a way that the luminophore is being redistributed or translocated with the component in living cells in a manner experimentally determined to be correlated to the degree of the influence. Measurement of redistribution is performed by recording of light intensity, fluorescence lifetime, polarization, wavelength shift, resonance energy transfer, or other properties by an apparatus consisting of e.g. a fluorescence microscope and a CCD camera. Data stored as digital images are processed to numbers representing the degree of redistribution. The method can be used as a screening program for identifying a compound that modulates a component and is capable of treating a disease related to the function of the component.
Owner:FISHER BIOIMAGE
Anti-tie2 antibody and use thereof
The present invention relates to an antibody, which specifically binds to tyrosine-protein kinase receptor TIE-2 (TIE2) so as to possess functions of blood vessel normalization and stabilization through receptor phosphorylation, and relates to: an anti-TIE2 antibody; a nucleic acid encoding same; a vector comprising the nucleic acid; a cell transformed with the vector; a method for preparing the antibody; an agent for stabilizing blood vessels and a composition for treating angiogenesis-associated diseases, both of which comprise the antibody; and a composition for co-administration with a pharmaceutical composition for tumor or cancer treatment and with a composition other than an antibody binding to TIE2.
Owner:PHARMABCINE
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