Abstract
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 G-744 are highly potent, selective for Btk, metabolically stable, well tolerated, and efficacious in an animal model of arthritis.
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Wang, X., Barbosa, J., Blomgren, P., Bremer, M. C., Chen, J., Crawford, J. J., … Young, W. B. (2017). Discovery of Potent and Selective Tricyclic Inhibitors of Bruton’s Tyrosine Kinase with Improved Druglike Properties. ACS Medicinal Chemistry Letters, 8(6), 608–613. https://doi.org/10.1021/acsmedchemlett.7b00103
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