179687-79-7Relevant articles and documents
Novel heteroaryl amide derivatives as MAO-B inhibitors and pharmaceutical compositions for preventing, ameliorating or treating neurodegenerative diseases comprising the same
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Paragraph 0382; 0385-0388, (2021/04/06)
A novel heteroaryl amide derivative compound useful as MAO-B inhibitors. The present invention relates to a compound selected from a pharmaceutically acceptable salt thereof, a hydrate thereof, or a stereoisomer thereof, and a pharmaceutical composition comprising the compound as an active ingredient for preventing, alleviating, or treating neurodegenerative diseases such MAO as B's disease, 's disease, 's disease, and the like.
Synthesis method of pyrotinib intermediate 2-[(2-chloro-4-nitrophenoxy)methyl]pyridine
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Paragraph 0009; 0017-0022, (2020/03/03)
The invention discloses a synthesis method of a pyrotinib intermediate 2-[(2-chloro-4-nitrophenoxy)methyl]pyridine. According to the method, 2-bromomethylpyridine and 2-chloro-4-nitrophenol are subjected to a mild reaction under an alkaline condition to obtain 2-[(2-chloro-4-nitrophenoxy)methyl]pyridine. According to the invention, the method has advantages of mild reaction conditions, simple post-treatment, high product purity (the yield is greater than or equal to 95%) and high yield (the purity is greater than or equal to 99.5%), and is suitable for industrial production.
Design, synthesis and biological study of potent and covalent HER-2 tyrosine kinase inhibitors with low cytotoxicity in vitro
Jin, Shuyu,Sun, Xiuyun,Liu, Dan,Xie, Hua,Rao, Yu
, p. 1333 - 1345 (2019/05/06)
The discovery and development of a novel HER-2 tyrosine kinase inhibitor for the treatment of HER2-positive breast cancer are presented in this article. EGFR family has been recognized as a crucial meditator in the cancer progression; HER-2 tyrosine kinase was one of the members among them. In the effort to explore potent HER-2 inhibitors, a novel series of 4-anilino-3-cyanoquinoline derivatives have been designed, synthesized and evaluated. Most compounds possessed modest proliferation inhibition on SK-BR-3 cell line and HER-2 kinase. Compound 16 appeared to be the most potent compound (HER-2 kinase IC50: 19.4?nM, SK-BR-3 IC50: 94?nM). In the experiment of cellular cytotoxicity assay, compound 16 shows a much lower cytotoxicity than neratinib on Beas-2b cell line (Human bronchial epithelial cells). In conclusion, compound 16 would be a promising lead compound for further anti-breast cancer drug discovery.