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Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2017 May 03; Vol. 8 (6), pp. 608-613. Date of Electronic Publication: 2017 May 03 (Print Publication: 2017). - Publication Year :
- 2017
-
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.
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 8
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 28626519
- Full Text :
- https://doi.org/10.1021/acsmedchemlett.7b00103