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Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.

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.

SUBMITTER: Wang X

PROVIDER: S-EPMC5467183 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature

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Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.

Wang Xiaojing X Barbosa James J Blomgren Peter P Bremer Meire C MC Chen Jacob J Crawford James J JJ Deng Wei W Dong Liming L Eigenbrot Charles C Gallion Steve S Hau Jonathon J Hu Huiyong H Johnson Adam R AR Katewa Arna A Kropf Jeffrey E JE Lee Seung H SH Liu Lichuan L Lubach Joseph W JW Macaluso Jen J Maciejewski Pat P Mitchell Scott A SA Ortwine Daniel F DF DiPaolo Julie J Reif Karin K Scheerens Heleen H Schmitt Aaron A Wong Harvey H Xiong Jin-Ming JM Xu Jianjun J Zhao Zhongdong Z Zhou Fusheng F Currie Kevin S KS Young Wendy B WB

ACS medicinal chemistry letters 20170503 6

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. ...[more]

PMID: 28626519

Dataset Information

Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.

Publications

Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.

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