compound, pharmaceutical composition, methods for treating a condition, inhibiting and validating kinase activity, modulating the b-catenin pathway and the tgfb / bmp path in a cell, to modulate stat1 and hif-1 activity alpha in a cell to increase bim expression and to prepare a compound, mutant and protein

摘要

provided herein are compounds of formula (a), (b), (c), (d) and (e), (a), (c) (b), (d), (e) pharmaceutically acceptable salts, salts of quaternary amines and n-oxides thereof and pharmaceutically acceptable pharmaceutical compositions thereof. The compounds of formula (a), (b), (c), (d) and (e) are considered useful as therapeutics for treating a wide variety of conditions, for example, including, but not limited to, associated conditions. with angiogenesis and cdk8 and / or cdk19 kinase activity. methods of inhibiting cdk8 and / or cdk19 kinase activity, methods of modulating the ß-catenin pathway, methods of modulating stat1 activity, methods of modulating tgfß / bmp pathway, methods of modulating hyph activity, are still provided. -1-alpha in a cell and methods of increasing bim expression to induce apoptosis using a compound of the formula (a), (b), (c), (d) or (e). cdk8 and cdk19 point mutants and methods of their use are also provided.