1139453-98-7Relevant articles and documents
Design, synthesis and biological evaluation of deuterated nintedanib for improving pharmacokinetic properties
Xu, Ruixue,Zhan, Miao,Peng, Lingling,Pang, Xuehai,Yang, Jun,Zhang, Tao,Jiang, Hongxia,Zhao, Lifeng,Chen, Yuanwei
, p. 308 - 312 (2015)
Nintedanib is a novel triple angiokinase inhibitor that inhibits three growth factors simultaneously. Deuterated derivatives of nintedanib at certain metabolically active sites were prepared and evaluated in vitro and in vivo. In particular, deuterated compound SKLB-C2202 had significantly improved pharmacokinetic properties compared with nintedanib. These efforts lay the foundation for further investigating the druggability of SKLB-C2202. Deuterated derivatives of nintedanib at certain metabolically active sites were prepared and evaluated in vitro and in vivo. Deuterated compound SKLB-C2202 had significantly improved pharmacokinetic properties compared with nintedanib. Further research is underway.
Preparation method of amino intermediate (by machine translation)
-
Paragraph 0023-0031; 0036-0037, (2020/02/20)
Compared with an existing preparation method, the method for preparing. the amine-based (I) intermediate disclosed by the invention comprises the following, steps: carrying (III) out condensation, reduction and the like of the compound of. the formula I to obtain, the target compound (I), and 1 remarkably reducing the, content of the impurities in the obtained compound according to the, invention as compared with the existing preparation. method. (by machine translation)
INDOLINONE DERIVATIVES AS INHIBITORS OF MATERNAL EMBRYONIC LEUCINE ZIPPER KINASE
-
Page/Page column 58, (2018/09/20)
The present disclosure relates to indolinone compounds, compositions, and methods for the inhibition of maternal embryonic leucine zipper kinase (MELK). The present disclosure further relates to indolinone compounds, compositions, and methods for the treatment or prevention of a cancer (for example, triple negative breast cancer).