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47 results about "ABL Tyrosine Kinase" patented technology

BCR-ABL tyrosine kinase inhibitors inhibit the enzyme BCR-ABL tyrosine kinase, which is important in the pathogenesis of chronic myelogenous leukemia (CML).

Bcr-abl truncation mutations

Truncation variants of BCR-ABL mRNA that produces BCR-ABL proteins with a truncated C-terminus and its role in resistance to treatment with kinase inhibitors is described. Vectors for expressing the truncated gene products are described as well as recombinant cells that express the truncated gene products from cDNA constructs. Also provided are methods compositions and kits for detecting the BCR-ABL truncation variants. Also provided are methods for determining the prognosis of a patient diagnosed as having myeloproliferative disease, and methods for predicting the likelihood for resistance to a treatment with tyrosine kinase inhibitor in a patient diagnosed as having myeloproliferative disease. Additionally, methods for screening BCR-ABL tyrosine kinase domain inhibitors which rely on the recombinant cells are also disclosed.
Owner:QUEST DIAGNOSTICS INVESTMENTS INC

N-methyl-2-[3-((e)-2-pyridin-2-yl-vinyl)-1h-indazol-6-ylsulfanyl]-benzamid- e for the treatment of chronic myelogenous leukemia

InactiveUS20140288125A1BiocideAnimal repellantsT315i mutationChronic myelogenous leukemia
The present invention relates to a method of treating chronic myelogenous leukemia in a subject comprising administering to the subject a compound, such as N-methyl-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]-benzamide, that inhibits the T315I mutation in BCR-ABL tyrosine kinase, or a pharmaceutically acceptable salt thereof. The present invention also relates to a pharmaceutical composition comprising a compound such as N-methyl-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]-benzamide, that inhibits the T315I mutation in BCR-ABL tyrosine kinase, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent.
Owner:PFIZER INC

Formulation comprising phenylaminopyrimidine derivative as active agent

InactiveUS20130338180A1Easy to useImprove the level ofBiocideOrganic active ingredientsBcr-Abl tyrosine-kinase inhibitorMyeloid leukemia
An oral pharmaceutical formulation containing an effective amount of NRC-AN-019 including its pharmaceutically acceptable salts and polymorphs such as Form I, Form II and Form III thereof to improve the bioavailability intended for self-emulsification upon its contact with the gastro-intestinal fluid. The invention also relates to a process for the preparation of oral solution containing NRC-AN-019 in an effective concentration for the better therapy against Chronic Myeloid Leukemia as BCR-ABL tyrosine kinase inhibitor and against other tumors such as head and neck cancer, prostate cancer and the like.
Owner:NATCO PHARMA LTD

Hydroxyproline peptoid derivative and preparation method and application thereof

InactiveCN109796439AHas inhibitory activityStrong inhibitory activityOrganic chemistryAntineoplastic agentsBcr-Abl tyrosine-kinase inhibitorBcr abl kinase
Disclosed are a hydroxyproline peptoid derivative and a preparation method and application thereof. With biphenyl pyridine as a hinge region binding fragment, by adopting a design strategy of a fragment drug and introducing L-hydroxyproline as a flexible Linker, a peptoid micromolecule-like compound library with kinase inhibition activity is constructed, and through screening of ADP-Glo and otheractivity tests, a peptoid tyrosine-like kinase inhibitor which has Bcr-Abl kinase inhibition activity and prevents the proliferation of tumor cells is found. The compound can be used for preparing anti-tumor drugs and has the activity of inhibiting Bcr-Abl and Bcr-AblT315I kinases and activity of inhibiting the cell proliferation of K562 cells. By introducing the L-hydroxyproline, the structural diversity of the Bcr-Abl inhibitor is expanded, the activity result shows that the introduction of proline has a certain effect on the inhibition activity of the compound, and the proline can serve asa novel pharmacological-effect fragment of the Bcr-Abl tyrosine kinase inhibitor.
Owner:XIAN CENT HOSPITAL

Bcr/Abl tyrosine kinase inhibitor as well as preparation method and application thereof in treating chronic granulocytic leukemia

The invention discloses a Bcr / Abl tyrosine kinase inhibitor capable of treating chronic granulocytic leukemia and a preparation method thereof. The Bcr / Abl tyrosine kinase inhibitor capable of treating chronic granulocytic leukemia obtained by a large number of experimental screenings not only can effectively inhibit Bcr / Abl tyrosine kinase, and still has a good inhibitory effect to mutated Bcr / Abl tyrosine kinase, so that the Bcr / Abl tyrosine kinase inhibitor is a novel Bcr / Abl tyrosine kinase inhibitor for effectively treating chronic granulocytic leukemia.
Owner:WUXI ALLNATURE BIOLOGICAL SCI & TECH CO LTD

Phosphorylation of tau by abl

Methods of diagnosing a tauopathy and predicting whether a subject will develop a tauopathy are provided. Also provided are antibody preparations that specifically bind to tau phosphorylated at tyr394 and / or tyr310. Methods of inhibiting tau phosphorylation in a cell and methods of treating a subject having a tauopathy are additionally provided. Methods of treating a subject at risk for a tauopathy are also provided. Additionally, non-human mammals comprising a transgene encoding an abl tyrosine kinase are provided. Also provided are methods of evaluating whether a compound inhibits development of a tauopathy.
Owner:ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIV

Crystals and structures of c-Abl tyrosine kinase domain

InactiveUS20050107298A1Improve other characteristicInhibitory activityNervous disorderPeptide/protein ingredientsThree Dimensional Molecular StructureABL Tyrosine Kinase
The present invention provides machine readable media embedded with the three-dimensional molecular structure coordinates of AblKD and variants and subsets thereof, including binding pockets, methods of using the structure to identify and design affecters, including inhibitors and activator AblKD crystals and compounds and compositions that affect Abl activity.
Owner:SGX PHARMA INC

Mutations in the BCR-ABL tyrosine kinase associated with resistance to STI-571

The invention described herein relates to novel genes and their encoded proteins, termed Mutants Associated with Resistance to STI-571 (e.g., T315I Bcr-Abl), and to diagnostic and therapeutic methods and compositions useful in the management of various cancers that express MARS. The invention further provides methods for identifying molecules that bind to and / or modulate the functional activity of MARS.
Owner:RGT UNIV OF CALIFORNIA

Use of succinyl hydrazine compounds and compositions thereof in preparation of drug for treating leukemia

InactiveCN1990462AExplore effective waysVerify biological activityOrganic chemistryAmide active ingredientsHydrazine compoundChronic granulocytic leukemia
The invention relates to succinyl hydrazine compounds derivative and medical compound containing them; and the application of it in preparing medicine that resists leukemia. The succinyl hydrazine compounds derivative shows inhibiting action to BCR-Ab1 tyrosine kinase activity through pharmacological test. It is characterized by high effecivity and low toxicity, and can be widly used to prepare medicine that treats chronic granulocytic leukemia (CML) and philadelphia chromosome positive acute lymphoblastic leukemia, especially medicine treating patient that generates drug resistance to Gleevec.
Owner:INST OF HEMATOLOGY & BLOOD HOSPITAL CHINESE ACAD OF MEDICAL SCI

Heteroaryl alkyne compound and use thereof

In the field of pharmaceutical chemistry compounds of general formula I having heteroaryl alkynyl moiety or pharmaceutically acceptable salts, isomers, solvates, crystals or prodrugs thereof, and pharmaceutical compositions including these compounds, as well as uses of these compounds and compositions thereof in the manufacture of a medicament. The compounds have a strong inhibitory effect on BCR-ABL tyrosine kinase and are useful for treating diseases, such as tumors.
Owner:NANJING SANHOME PHARMACEUTICAL CO LTD

Application of substance for inhibiting phosphorylation of 357 tyrosine residue of YAP protein to prevention of atherosclerosis

The invention discloses application of a substance for inhibiting phosphorylation of a 357 tyrosine residue of a YAP protein to prevention of atherosclerosis. The substance for inhibiting phosphorylation of the 357 tyrosine residue of the YAP protein is an Src / c-Abl tyrosine kinase double inhibitor or a c-Abl inhibitor or an Src inhibitor; bosutinib is adopted as the Src / c-Abl tyrosine kinase double inhibitor; and experiments prove that the bosutinib prevents atherosclerosis, treats atherosclerosis, decreases the area of plaques of atherosclerosis, reduces lipid deposition, decreases the collagen content, inhibits forming of the plaques of atherosclerosis, inhibits activation of vascular endothelial cells and inhibits the expression level of adherence factors by inhibiting phosphorylation of the 357 tyrosine residue of the YAP protein. The substance has significant application value.
Owner:TIANJIN MEDICAL UNIV

Therapeutic agent or treatment method for philadelphia chromosome-positive (ph+) acute lymphocytic leukemia (ALL) having ikzf1 mutation

ActiveUS20180243284A1Moderate proliferation inhibitory effectPromote resultsHydroxy compound active ingredientsAntineoplastic agentsBcr-Abl tyrosine-kinase inhibitorPhiladelphia Chromosome Positive
According to the present invention, there is provided a pharmaceutical composition for treating Philadelphia chromosome positive lymphocytic leukemia, including a thalidomide derivative and BCR-ABL tyrosine kinase inhibitor. According to the present invention there is also provided a method of treating Philadelphia chromosome positive lymphocytic leukemia, including administering a thalidomide derivative and a BCR-ABL tyrosine kinase inhibitor to a patient suffering from Philadelphia chromosome positive lymphocytic leukemia.
Owner:UNIVERSITY OF YAMANASHI +1

Compounds targeting and degrading bcr-abl protein and its antitumor application

The present disclosure provides a compound of formula (I) targeting and degrading BCR-ABL protein and its use in the field of antitumor. The compound of formula (I) shows degradation and inhibitory effects on BCR-ABL target protein, which is mainly comprised of four moieties, wherein the first moiety (BCR-ABL-TKIs) is compound moiety with BCR-ABL tyrosine kinase inhibited activity; the second moiety (the LIN) is link units; the third moiety (the ULM) is a small molecule ligand for VHL or CRBN proteases with ubiquitination; and the four moiety (the group A) is carbonyl group that covalently binds to BCR-ABL-TKIs and LIN, and the LIN is further covalently bonded to ULM. A series of compounds designed and synthesized by the present disclosure shows extensive pharmacological effective, which function to degrade BCR-ABL protein and inhibit BCR-ABL effective, and can be utilized for treating relevant tumor.
Owner:SHANGHAI TECH UNIV

Thiazolyl aminobenzoic acid derivative and application thereof

ActiveCN109232467AAvoid or reduce toxic side effectsGood inhibitory effectOrganic active ingredientsOrganic chemistryBcr-Abl tyrosine-kinase inhibitorT315i mutation
The invention discloses a thiazolyl aminobenzoic acid derivative with antineoplastic activity, which can be used for preparing an anticancer drug, in particular as a Bcr-Abl tyrosine kinase inhibitor,especially as a Bcr-Abl tyrosine kinase inhibitor of a T315I mutation.
Owner:NANHUA UNIV

Kit for detecting ABL tyrosine kinase inhibitor based on HPLC-MS/MS method and detection method

The invention discloses a kit for detecting an ABL tyrosine kinase inhibitor based on an HPLC-MS / MS method and a detection method. The ABL tyrosine kinase inhibitor comprises imatinib, dasatinib, nilotinib, panatinib and flumatinib. The kit comprises the following reagents: a sample treatment solution, a standard substance, a quality control substance, an internal standard solution and a mobile phase, wherein the mobile phase comprises a mobile phase A and a mobile phase B; the mobile phase A is a 0.1% formic acid methanol solution; the mobile phase B is a 2 mmol.L <-1 > ammonium acetate and -0.1% formic acid aqueous solution; according to the invention, the concentration of the ABL tyrosine kinase inhibitor in the blood plasma is quantitatively detected based on an HPLC-MS / MS technology; the detection result is not interfered by common drugs and combined drugs, and the accuracy of quantitative detection of the ABL tyrosine kinase inhibitor is greatly improved; the kit is helpful for improving the detection quality of the ABL tyrosine kinase inhibitor and promoting the standardization and normalization of a detection method, so that the blood concentration of the clinical ABL tyrosine kinase inhibitor can be monitored more quickly, accurately and reliably.
Owner:北京陆道培生物技术有限公司

Combination therapy with liposomal antisense oligonucleotides

Provided herein are methods of treating a cancer in a patient comprising administration of an effective amount of a nuclease-resistant polynucleotide that hybridizes to the translation initiation site of a Grb2 nucleic acid in the patient and either a Bcr-Abl tyrosine kinase inhibitor (e.g., dasatinib) or a cytidine analogue (e.g., decitabine or cytarabine). The cancer may be Ph+ and / or Bcr-Abl positive chronic myelogenous leukemia or acute myeloid leukemia or myelodysplastic syndrome.
Owner:BIO PATH HLDG INC

Use of a kinase inhibitor for the treatment of particular resistant tumors

InactiveUS20100022532A1High affinitySignificant inhibitory potencyBiocideMicrobiological testing/measurementDiseaseInhibitory potency
The invention provides low molecular weight compounds, namely 1H-thieno[2,3-c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor-resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.
Owner:NERVIANO MEDICAL SCI

Indazole cyclotriazole compound as well as preparation method and application thereof

The invention discloses an indazole cyclotriazole compound as well as a preparation method and application thereof, a drug design strategy based on fragments is adopted, and a halogenated substituent group is introduced to an end benzene ring while amino acylation is performed on an indazole ring, so that an indazole cyclotriazole compound library with kinase inhibition activity is constructed; the tyrosine kinase inhibitor with Bcr-Abl kinase inhibition activity is found through kinase activity screening, and the tyrosine kinase inhibitor can be used for preparing antitumor drugs, has certain activity of inhibiting Bcr-AblWT and Bcr-AblT315I kinase, and has certain cell proliferation inhibition activity on K562 cells. Meanwhile, an activity test shows that indazoletriazole has an important effect on the inhibition activity of a compound, can improve the affinity between a receptor and the compound, and can be used as a pharmacological fragment of a Bcr-Abl tyrosine kinase inhibitor.
Owner:XI AN JIAOTONG UNIV

Aryne derivatives as protein kinase inhibitors and their medical use

InactiveCN103370324BGood anti-inhibition effectOrganic active ingredientsOrganic chemistryDiseasePTK Inhibitors
The invention discloses a class of protein kinase inhibitor aryne derivatives. The compound is a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, R1, R2, R3, R4, ring A, ring B , L, m, n, p or q are defined in the specification. In addition, the invention also discloses a drug with the compound or its salt as active ingredient, which can be used for treating proliferative diseases such as cancer and inflammatory diseases, especially diseases related to Bcr-Abl tyrosine kinase.
Owner:TIANJIN LONGBOGEN PHARMACEUTICAL CO LTD
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