56 results about "Tyrosine kinase 2" patented technology

There are provided compounds of formula I,wherein R, R1, Ra, Rb, Q, X and Y have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

This disclosure concerns novel quinazoline compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful anticancer agents, especially in inhibiting the function of the EGF receptor tyrosine kinases, HERl tyrosine kinase, and HER2 tyrosine kinase. Thus, the disclosure also concerns a method of treating hyperproliferative diseases or conditions, such as various cancers and benign prostate hyperplasia (BPH), by use of these novel compounds or a composition comprising such novel compounds.

Compounds of formula (I):wherein R1, R2, J, Q, V, X, Y and Z are defined herein are disclosed. The compounds are inhibitors of the family of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha sub-type thereof, and of Syk kinase and the Src family of tyrosine kinases. The compounds may be used in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, in particular inflammatory diseases of the lung, such as asthma and COPD, as well as those of the gastrointestinal tract, such as ulcerative colitis and Crohn's disease and of the eye, such as uveitis.

3-pyrrolo[b]cyclohexylene-2-dihydro-indolinone derivatives of formula (I) or their pharmaceutically acceptable salts and uses thereof. The intermediates of formula (II) for preparing the above compounds. The bioassay shows that the above compounds and their pharmaceutically acceptable salts can modulate the activity of protein kinases (PKs), inhibit the activity of tyrosine kinases (PTKs) and inhibit many kinds of tumor cells as well as.

Compounds of formula (I):wherein R1, R2, J, Q, V, X, Y and Z are defined herein are disclosed. The compounds are inhibitors of the family of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha sub-type thereof, and of Syk kinase and the Src family of tyrosine kinases. The compounds may be used in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, in particular inflammatory diseases of the lung, such as asthma and COPD, as well as those of the gastrointestinal tract, such as ulcerative colitis and Crohn's disease and of the eye, such as uveitis.

Novel compounds of the formula Iin whichR, X and n are as defined herein,are inhibitors of tyrosine kinase and can be employed for the treatment of tumours, for neuroprotection and for protection of the stress proteins of the skin.

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.

The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate Pim kinase activity and / or FMS-like tyrosine kinase (Flt) activity. The invention also relates in part to methods for using such molecules.

The present invention provides methods of treating, stabilizing or lessening the severity or progression of a disease or disorder associated with BTK.

Provided are methods and compositions for a combination therapy for liver disorders such as hepatocellular carcinoma. Also provided is a method for determining the effectiveness of therapy involving tyrosine kinase inhibitors such as sorafenib. The method comprises determining the status of PD-1 on T cells, and based on a change in the level of PD-1 on certain cells, a determination of the effectiveness of the tyrosine kinase, and an indication for a combination therapy comprising a lower dose of tyrosine kinase inhibitor and a PD-1 inhibitor can be made.

The present invention relates to compounds which inhibit, regulate and / or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

The invention relates to pyrido[2,3-b]pyrazine compounds of formulae (Ia) and (Ib) which have activity to the modulation of misdirected cellular signal transduction processes such as tyrosine kinases, serine / threonine kinases and / or lipid kinases, their preparation and use as medicaments, especially for the treatment of malignant disorders and other disorders based on pathological cell proliferations:

The present invention relates to novel amidoheteroaryl aroyl hydrazide ethynes as tyrosine kinase inhibitors, process of preparation thereof, and use of the compounds for preparation of pharmaceutical compositions in the therapeutic treatment of disorders related to tyrosine kinases in humans.

The present invention relates to novel amidoheteroaryl aroyl hydrazide ethynes as tyrosine kinase inhibitors, process of preparation thereof, and use of the compounds for preparation of pharmaceutical compositions in the therapeutic treatment of disorders related to tyrosine kinases in humans.

Novel compounds of the formula Iin whichR, X, n and m are as defined herein are inhibitors of tyrosine kinase and can be employed for the treatment of tumours, for neuroprotection and for protection of the stress proteins of the skin.

The present invention relates to derivatives of benzimidazoles of formula (I) as disclosed herein as well as pharmaceutical compositions comprising said derivatives. The derivates according to the present invention are serine / threonine and tyrosine kinase-inhibitors, particularly of PIM1-3- and DYRK1A-kinases and may particularly be used in the treatment of diseases linked to these kinases, such as e.g. leukemias, lymphomas, solid tumors and autoimmune disorders.

The present invention relates to a tyrosine kinase-inducible domain (pKID) and uses thereof. An isolated polypeptide comprising the pKID, and an isolated polynucleotide comprising a nucleic acid sequence encoding the pKID are provided. Also provided are methods for determining tyrosine kinase and / or phosphatase activity in a sample and for identifying an agent that inhibits a tyrosine kinase or phosphatase using a polypeptide comprising the pKID.

The invention relates to a heterocyclic compound suitable for inhibiting or regulating Janus family kinase (JAK), in particular tyrosine kinase 2 (TYK2), a preparation method of the heterocyclic compound and application of the heterocyclic compound in medicine. Specifically, the present invention relates to a compound represented by a general formula (I), a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt thereof, and a method of using the compound or the pharmaceutically acceptable salt thereof to treat and / or prevent Janus kinase-mediated related diseases, especially autoimmune diseases, inflammatory diseases and cancers and a method for preparing the compound or pharmaceutically acceptable salt thereof. The invention also relates to application of the compound or the pharmaceutically acceptable salt thereof or the pharmaceutical composition containing the compound or the pharmaceutically acceptablesalt thereof in preparation of drugs for treating and / or preventing Janus kinase mediated related diseases, especially autoimmune diseases, inflammatory diseases and cancers. Each substituent of thegeneral formula (I) is as defined in the specification.