1147858-83-0Relevant articles and documents
Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties
Wang, Xiaojing,Barbosa, James,Blomgren, Peter,Bremer, Meire C.,Chen, Jacob,Crawford, James J.,Deng, Wei,Dong, Liming,Eigenbrot, Charles,Gallion, Steve,Hau, Jonathon,Hu, Huiyong,Johnson, Adam R.,Katewa, Arna,Kropf, Jeffrey E.,Lee, Seung H.,Liu, Lichuan,Lubach, Joseph W.,Macaluso, Jen,Maciejewski, Pat,Mitchell, Scott A.,Ortwine, Daniel F.,Dipaolo, Julie,Reif, Karin,Scheerens, Heleen,Schmitt, Aaron,Wong, Harvey,Xiong, Jin-Ming,Xu, Jianjun,Zhao, Zhongdong,Zhou, Fusheng,Currie, Kevin S.,Young, Wendy B.
supporting information, p. 608 - 613 (2017/06/13)
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.
PYRIDAZINONES, METHOD OF MAKING, AND METHOD OF USE THEREOF
-
Page/Page column 62, (2012/03/26)
Pyridazinone compounds of Formula (I) including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
INHIBITORS OF BRUTON'S TYROSINE KINASE
-
, (2012/12/13)
This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.