945761-06-8Relevant articles and documents
Discovery and Evaluation of Pyrazolo[3,4-d]pyridazinone as a Potent and Orally Active Irreversible BTK Inhibitor
Zhang, Xuejun,Sheng, Xijun,Shen, Jie,Zhang, Shoubo,Sun, Wenjie,Shen, Chunli,Li, Yi,Wang, Jun,Lv, Huqiang,Cui, Minghui,Zhu, Yuchuan,Huang, Lei,Hao, Dongling,Qi, Zhibo,Sun, Guanglong,Mao, Weifeng,Pan, Yan,Shen, Liang,Li, Xin,Hu, Guoping,Gong, Zhen,Han, Shuhua,Li, Jian,Chen, Shuhui,Tu, Ronghua,Wang, Xuehai,Wu, Chengde
, p. 1863 - 1868 (2020)
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.
BTK INHIBITOR
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Paragraph 1561-1562, (2017/11/16)
Provided are a series of BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or prodrug thereof represented by formula (I), (II), (III) or (IV).
Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors
Lee, Ki-Ho,Park, Chun-Eung,Min, Kyung-Hyun,Shin, Yong-Je,Chung, Coo-Min,Kim, Hui-Ho,Yoon, Hae-Jeoung,Won-Kim,Ryu, Eun-Ju,Shin, Yu-Jin,Nam, Hyun-Sik,Cho, Jeong-Woo,Lee, Hee-Yoon
scheme or table, p. 5567 - 5571 (2010/12/29)
A series of 3-aryl-3-azolylpropan-1-amines was prepared and screened for its capability of inhibiting monoamine reuptake. Analogs with nanomolar potency, good human in vitro microsomal stability, and low drug-drug interaction potential were described. In
