Discovery and Evaluation of Pyrazolo[3,4-d]pyridazinone as a Potent and Orally Active Irreversible BTK Inhibitor
Year: 2019
Type: article
Abstract: 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.
Source: ACS Medicinal Chemistry Letters
Authors: 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
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: green
OpenAlex ID: W2995239697