Abstract:
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
Abstract:
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
Abstract:
The invention provides methods, assays and systems for determining the efficacy of a TEC family kinase inhibitor on a target kinase. The methods, assays and systems relate to determining the occupancy of a target kinase by a TEC family kinase inhibitor (e.g., BTK inhibitors). Such quantitative measurements are used to inform therapeutic treatment and the over-all health care management of a subject. For example, diagnostic kits for diagnosing, prognosing, and monitoring a disease or indication benefitting from treatment with a TEC family kinase inhibitor are provided. In another example, diagnostic kits for identifying responders to TEC family kinase inhibitor therapy, determining therapeutic regimens, and detecting resistance to TEC family kinase inhibitor also are provided.
Abstract:
Described herein are kinase inhibitor compounds, methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate inhibitor of a protein, including a kinase.
Abstract:
Disclosed herein are methods and compounds for inhibiting bone and/or cartilage resorption in an individual. The methods comprise administering to the individual a composition comprising a therapeutically effective amount of a compound that is an irreversible inhibitor of a Bruton's tyrosine kinase (BTK), or a pharmaceutically acceptable salt thereof. Also described are irreversible inhibitors of Btk and methods for the preparation of the compounds. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the inhibition of cancer metastasis, and for inhibition of bone or cartilage resorption in cancer patients.
Abstract:
NOUVEAU SCHEMA D'ADMINISTRATION DU W-HYDROXY-4-{2-[3-(W,W-DIMETHYLAMINOMETHYL)BENZOFU- RAN-2-YLCARBONYLAMINO]ETHOXY} BENZAMIDE /V-hydroxy-4-{2-[3-{/V,/V-diméthylaminométhyl)benzofu- ran-2-ylcarbonylamino]éthoxy} benzamide de formule (I) : ou un de ses sels d'addition à un acide ou à une base pharmaceutiquement acceptable, seul ou en association avec un traitement de chirurgie, de chimiothérapie, d'hormonothérapie ou avec la radiothérapie, pour le traitement du cancer, caractérisé en ce qu'il est administré pendant 4 jours consécutifs, cette période étant suivie de 3 jours consécutifs sans aucune administration du composé de formule (I), étant entendu que le traitement de chimiothérapie n'est pas le FOLFOX.
Abstract:
Described herein are kinase inhibitor compounds, methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate inhibitor of a protein, including a kinase.
Abstract:
Described herein are compositions and methods for treating a subject suffering from a non-localized inflammatory condition (or any symptoms associated with such inflammation), including systemic inflammation, and inflammatory conditions affecting the large portions of or the whole body, or sepsis by administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of a compound that is a pan-HDAC inhibitor. Also described herein are methods for decreasing iNOS and cytokine expression by administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of a compound that is a pan-HDAC inhibitor.
Abstract:
Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the acitivy of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.