INHIBITORS OF BRUTON'S TYROSINE KINASE
Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.
1 - 100 . (canceled)
101 . An irreversible Bruton's tyrosine kinase (BTK) inhibitor having the structure:
wherein
is a substituted moiety that binds to the active site ATP binding pocket of BTK, provided that
is not
where each squiggle represents a substitution other than H, and
wherein R 1 is L 2 -substituted aryl, wherein L 2 is a bond.
102 . The irreversible BTK inhibitor of claim 1 , wherein R 1 is a substituted phenyl.