| Autor: |
Xuejun, Zhang, Xijun, Sheng, Jie, Shen, Shoubo, Zhang, Wenjie, Sun, Chunli, Shen, Yi, Li, Jun, Wang, Huqiang, Lv, Minghui, Cui, Yuchuan, Zhu, Lei, Huang, Dongling, Hao, Zhibo, Qi, Guanglong, Sun, Weifeng, Mao, Yan, Pan, Liang, Shen, Xin, Li, Guoping, Hu, Zhen, Gong, Shuhua, Han, Jian, Li, Shuhui, Chen, Ronghua, Tu, Xuehai, Wang, Chengde, Wu |
| Rok vydání: |
2019 |
| Zdroj: |
ACS Med Chem Lett |
| ISSN: |
1948-5875 |
| Popis: |
[Image: see text] The identification and lead optimization of a series of pyrazolo[3,4-d]pyridazinone derivatives are described as a novel class of potent irreversible BTK inhibitors, resulting in the discovery of compound 8. Compound 8 exhibited high potency against BTK kinase and acceptable PK profile. Furthermore, compound 8 demonstrated significant in vivo efficacy in a mouse-collagen-induced arthritis (CIA) model. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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