发现具有改善类药性质的布鲁顿酪氨酸激酶强效和选择性三环抑制剂。
Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.
作者信息
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
机构信息
Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.
Gilead Sciences (formerly CGI Pharmaceuticals), 199 East Blaine Street, Seattle, Washington 98102, United States.
出版信息
ACS Med Chem Lett. 2017 May 3;8(6):608-613. doi: 10.1021/acsmedchemlett.7b00103. eCollection 2017 Jun 8.
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 are highly potent, selective for Btk, metabolically stable, well tolerated, and efficacious in an animal model of arthritis.
为了持续致力于发现和开发一流的布鲁顿酪氨酸激酶（Btk）抑制剂，用于治疗B细胞淋巴瘤、类风湿性关节炎和系统性红斑狼疮，我们设计了一系列新型三环化合物，这些化合物在类药性质方面比我们之前的化学物质有所改进。以 为例的化合物具有高效、对Btk有选择性、代谢稳定、耐受性良好且在关节炎动物模型中有效的特点。
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