19064-67-6Relevant articles and documents
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Taft et al.
, p. 605 (1961)
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NOVEL HYDRAZONE DERIVATIVE WITH ARYL OR HETEROARYL GROUP SUBSTITUTED AT TERMINAL AMINE GROUP THEREOF AND USE THEREOF
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Paragraph 0396, (2021/11/04)
The present invention relates to novel hydrazone derivatives in which a terminal amine group is substituted with an aryl group or a heteroaryl group, and uses thereof.
Pyridazine hydrazone derivative and preparation method and application thereof
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Paragraph 0035-0039, (2020/05/14)
The invention relates to a pyridazine hydrazone derivative shown as a chemical structural formula I and a pharmaceutically acceptable salt thereof, a pharmaceutical composition and application thereofin preparation of an influenza virus neuraminidase inhibitor, wherein Y is selected from the group consisting of: hydroxyl, dihydroxyl, 2-hydroxyl-3-methoxy, 2-hydroxyl-4-methoxy, 2-hydroxyl-5-methoxy, 2-hydroxyl-6-methoxy, 3-hydroxyl-2-methoxy, 3-hydroxyl-4-methoxy, 3-hydroxyl-5-methoxy, 3-hydroxyl-6-methoxy, 4-hydroxyl-2-methoxy, 4-hydroxyl-3-methoxy, 4-hydroxyl-3, 5-dimethoxy, 2-hydroxyl-3-ethoxy, 2-hydroxy-4-ethyoxyl, 2-hydroxy-5-ethyoxyl, 2-hydroxy-6-ethyoxyl, 3-hydroxy-2-ethyoxyl, 3-hydroxy-4-ethyoxyl, 3-hydroxy-5-ethyoxyl, 3-hydroxy-6-ethyoxyl, 4-hydroxy-2-ethyoxyl, 4-hydroxy-3-ethyoxyl, 4-hydroxy-3, 5-diethyoxyl, trihydroxy or 4-hydroxy-3, 5-dimethyl.
Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor
Zhuang, Linghang,Tice, Colin M.,Xu, Zhenrong,Zhao, Wei,Cacatian, Salvacion,Ye, Yuan-Jie,Singh, Suresh B.,Lindblom, Peter,McKeever, Brian M.,Krosky, Paula M.,Zhao, Yi,Lala, Deepak,Kruk, Barbara A.,Meng, Shi,Howard, Lamont,Johnson, Judith A.,Bukhtiyarov, Yuri,Panemangalore, Reshma,Guo, Joan,Guo, Rong,Himmelsbach, Frank,Hamilton, Bradford,Schuler-Metz, Annette,Schauerte, Heike,Gregg, Richard,McGeehan, Gerard M.,Leftheris, Katerina,Claremon, David A.
supporting information, p. 3649 - 3657 (2017/06/13)
A potent, in vivo efficacious 11β hydroxysteroid dehydrogenase type 1 (11β HSD1) inhibitor (11j) has been identified. Compound 11j inhibited 11β HSD1 activity in human adipocytes with an IC50 of 4.3?nM and in primary human adipose tissue with an IC80 of 53?nM. Oral administration of 11j to cynomolgus monkey inhibited 11β HSD1 activity in adipose tissue. Compound 11j exhibited >1000× selectivity over other hydroxysteroid dehydrogenases, displays desirable pharmacodynamic properties and entered human clinical trials in 2011.