1 research outputs found
Discovery of Potent and Selective Tricyclic Inhibitors of Bruton’s Tyrosine Kinase with Improved Druglike Properties
In our continued effort to discover
and develop best-in-class Bruton’s tyrosine kinase (Btk) inhibitors
for the treatment of B-cell lymphomas, rheumatoid arthritis, and systemic
lupus erythematosus, we devised a series of novel tricyclic compounds
that improved upon the druglike properties of our previous chemical
matter. Compounds exemplified by <b>G-744</b> are highly potent,
selective for Btk, metabolically stable, well tolerated, and efficacious
in an animal model of arthritis