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81 results about "Bruton's tyrosine kinase" patented technology

Bruton's tyrosine kinase (abbreviated Btk or BTK), also known as tyrosine-protein kinase BTK, is an enzyme that in humans is encoded by the BTK gene. BTK is a kinase that plays a crucial role in B-cell development.

Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton's tyrosine kinase by such compounds

Compounds of Formula I-a and all pharmaceutically-acceptable forms thereof, are described herein. The variables R1, R2, R3, Z1, Q, and A shown in Formula I-a are defined herein. Pharmaceutical compositions containing one or more compounds of Formula I-a, or a pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein. Methods of treating patients suffering from certain diseases responsive to inhibition of tyrosine kinase activity are also given. In certain embodiments the diseases are responsive to inhibition of Btk activity and / or B-cell proliferation. Such methods comprise administering to such patients an amount of a compound of Formula I-a effective to reduce signs or symptoms of the disease. These diseases include cancer, an autoimmune and / or inflammatory disease, or an acute inflammatory reaction. Thus methods of treatment include administering a sufficient amount of a compound or salt as provided herein to decrease the symptoms or slow the progression of these diseases. Other embodiments include methods of treating other animals, including livestock and domesticated companion animals, suffering from a disease responsive to inhibition of kinase activity. Methods of treatment include administering a compound of Formula I-a as a single active agent or administering a compound of Formula I-a in combination with one or more other therapeutic agent. A method for determining the presence of Btk in a sample, comprising contacting the sample with a compound or form thereof of Formula I-a under conditions that permit detection of Btk activity, detecting a level of Btk activity in the sample, and therefrom determining the presence or absence of Btk in the sample.
Owner:GILEAD CONNENTICUT INC

Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds

Compounds of Formula Iand all pharmaceutically acceptable forms thereof, are described herein.The variables R1, R2, R3, Z2, and Q, shown in Formula I are defined herein.Pharmaceutical compositions containing one or more compounds of Formula I, or a pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein.Methods of treating patients suffering from certain diseases responsive to inhibition of tyrosine kinase activity are also given. In certain embodiments the diseases are responsive to inhibition of Btk activity and / or B-cell proliferation. Such methods comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These diseases include cancer, an autoimmune and / or inflammatory disease, or an acute inflammatory reaction. Thus methods of treatment include administering a sufficient amount of a compound or salt as provided herein to decrease the symptoms or slow the progression of these diseases.Other embodiments include methods of treating other animals, including livestock and domesticated companion animals, suffering from a disease responsive to inhibition of kinase activity.Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with one or more other therapeutic agent.A method for determining the presence of Btk in a sample, comprising contacting the sample with a compound or form thereof of Formula I under conditions that permit detection of Btk activity, detecting a level of Btk activity in the sample, and therefrom determining the presence or absence of Btk in the sample.
Owner:GILEAD CONNENTICUT INC

Compositions and Methods for the Production of Pyrimidine and Pyridine Compounds with BTK Inhibitory Activity

ActiveUS20140162983A1Lowering of ground state energyReduction in rate in rate-limiting bond breakageBiocideNervous disorderBruton's tyrosine kinaseSystemic lupus erythematosus
The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.
Owner:MERCK PATENT GMBH

Compound for inhibiting activity of BTK and/or JAK3

The invention relates to a compound for inhibiting the activity of BTK (Bruton's Tyrosine Kinase) and / or JAK3 (Janus Tyrosine Kinase 3), a medicinal composition of the compound, a use of the compound in the pharmacy, a method for inhibiting the activity of BTK and / or JAK3 by using the compound, and a method for treating and / or preventing BTK and / or JAK3 mediated diseases or illnesses in mammals (especially human beings) by using the compound. The compound is represented by structural formula I shown in the specification.
Owner:BEIJING HANMI PHARMA CO LTD

Compound for inhibiting kinase activity of BTK and/or JAK3

The invention relates to a compound for inhibiting kinase activity of BTK and / or JAK3, as well as a pharmaceutical composition of the compound use of the compound in pharmaceuticals, a method for inhibiting the activity of BTK and / or JAK3 by virtue of the compound and a method for treating and / or preventing BTK and / or JAK3 mediated diseases or symptoms of mammals (particularly human) by virtue of the compound. The compound has a structural formula I shown in the specification.
Owner:BEIJING HANMI PHARMA CO LTD

Optimized medicine combination and application thereof for treating cancers and autoimmune diseases

The invention provides a series of new multi-fluorine-substituted pyrazolopyrimidine type compounds or salts. The compounds are Bruton's tyrosine kinase (BTK) inhibitors, and can have better kinase inhibition selectivity and pharmacokinetic property. The invention discloses a preparation method of the compounds and also discloses medicine combination containing the compounds with other target medicine compositions or other medicines. The optimized medicine combination has a synergistic effect, can greatly inhibit the existence of tumors as compared with a single target medicine, and can completely eliminate certain tumors. The optimized medicine combination can greatly treat the medicine resistance of the tumors and prevent the cancer recurrence as compared with the single target medicine, and the treatment period is shorter. The invention further relates to combined compounds and medicine preparations using the compounds as active elements, and at a lower dosage, the compounds are safer and have the curative effect of the synergistic effect. The invention further comprises methods for treating and inhibiting the autoimmune diseases or symptoms, heterogeneous immune diseases or symptoms, inflammatory diseases and cancer or symptoms by using the compounds and preparations of the compounds.
Owner:ZHEJIANG DTRM BIOPHARMA +1

Bruton's kinase inhibitor

Provided are a 2-phenyl-isoquinoline-1-ketone derivative having a structure of formula (I), and uses thereof. The compound has good inhibitory effect on Bruton's tyrosine kinase activity, and the median inhibition concentration of the compound is generally below 10-7 mol.L-1. The compound having the structure of formula (I) and prepared in an embodiment of the present invention has clear anti-inflammatory activity on different animal models.
Owner:HAINAN SIMCERE PHARMA CO LTD

Pyrazolopyrimidine derivative, preparation method, pharmaceutical composition and application

The invention discloses a pyrazolopyrimidine derivative, a preparation method, a pharmaceutical composition and application. The invention provides the pyrazolopyrimidine derivative as shown in a formula I and stereoisomer or solvate or pharmaceutically acceptable salts or active metabolite or prodrug thereof. The pyrazolopyrimidine derivative as shown in the formula I has good inhibitory activity on Bruton's tyrosine kinase (Btk) and particularly has good in vitro and in vivo inhibitory activity on growth of tumor cells, and a good marketization prospect is achieved. Please see the formula I in the description.
Owner:ARROMAX PHARMATECH

Bruton's tyrosine kinase inhibitor

ActiveCN109422696AInhibits Bruton's tyrosine kinase activityOrganic active ingredientsOrganic chemistryImmunologic disordersDisease
The invention discloses a compound with a general formula (I), wherein the compound is capable of inhibiting Btk, and the groups are disclosed in the invention. The compound can be used for treating autoimmune diseases, heterologous immunization diseases, cancers, or thromboembolism diseases. The invention also discloses a pharmaceutical composition containing the compound represented by formula (I). The Bruton's tyrosine kinase inhibitor is capable of inhibiting the activity of Bruton's tyrosine kinas through covalent binding such as a covalent reversible mode.
Owner:BEIJING RECIPROCAPHARM

Novel compounds

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

Thiazolyl-containing compounds for treating proliferative diseases

The present disclosure provides thiazolyl-containing compounds of Formula (I), (II), or (III). The compounds described herein may be able to inhibit protein kinases (e.g., Src family kinases (e.g., hemopoietic cell kinase (HCK)), Bruton's tyrosine kinase (BTK)) and may be useful in treating and / or preventing proliferative diseases (e.g., myelodysplasia, leukemia, lymphoma (e.g., Waldenstrom's macroglobulinemia)) and in inducing apoptosis in a cell (e.g., malignant blood cell). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.
Owner:DANA FARBER CANCER INST INC

Compositions and methods for quantitatively monitoring lipids

Provided herein are fluorescent lipid binding proteins (FLBPs). The FLBPs comprise a lipid binding domain linked to a fluorophore, whrereby the fluorophore's fluorescence emission undergoes a spectral change upon lipid binding. the fluorophore is selected from the group consisting of 2-dimethylamino-6-acyl-naphthalene (DAN) and RED fluorophore and the lipid binding protein is selected from the group consisting of ENTH domain of epsin 1, C2 domain of bovine lactadherin, C 1B domain of protein kinase C-gamma, C2 domain of cytosolic phospholipase A2-beta, and PH domain of Bruton's tyrosine kinase PH.
Owner:THE BOARD OF TRUSTEES OF THE UNIV OF ILLINOIS

Dosage form compositions comprising an inhibitor of bruton's tyrosine kinase

The invention relates generally to pharmaceutical tablet compositions comprising fumaric acid and the compound (S)-2-(3′-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4′-bipyridin]-2′-yl)-7,7-dimethyl-2,3,4,6,7,8-hexahydro-1H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one free base that is an inhibitor of Bruton's tyrosine kinase. The invention further relates to amorphous solid dispersions comprising at least one polymer and the Bruton's kinase inhibitor free base compound. The invention further relates to crystalline mesylate salts, crystalline chloride salts and crystalline sulfate salts of the Bruton's kinase inhibitor free base compound. In some aspects, the crystalline salts are single polymorphs.
Owner:GENENTECH INC

Crystal form of acp-196, preparation method therefor and pharmaceutical composition thereof

Crystalline forms of ACP-196, preparation methods, pharmaceutical compositions and uses thereof in the preparation of drugs for treatment and / or prevention of Bruton's tyrosine kinase (BTK)-mediated disorders such as autoimmune diseases or disorders, heteroimmune diseases or disorders, cancers including lymphoma and inflammatory diseases or disorders. As compared with the known solid form of ACP-196, the crystalline forms of the present invention have advantages in crystallinity.
Owner:SOLIPHARMA

4-Aminopyrimidine compound, and preparation method and medicinal use thereof

ActiveCN107043366AOrganic active ingredientsOrganic chemistryWaldenstrom macroglobulinemiaChemical compound
The invention belongs to the field of medicines, and concretely relates to a 4-aminopyrimidine compound having a structural represented by formula (I), or pharmaceutically acceptable salts thereof, a preparation method of the compound, and a use of the compound and the salts as a Bruton tyrosine kinase (BTK) inhibitor. A result of experiments shows that the compound has a significant inhibition effect on the BTK, and can be used for treating thromboembolism, inflammatory disorders, autoimmune diseases, Waldenstrom macroglobulinemia, B cell lymphomas and other diseases.
Owner:CHINA PHARM UNIV
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