36760-19-7Relevant articles and documents
FUSED RING DERIVATIVE AS A2A RECEPTOR INHIBITOR
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Paragraph 0138-0141, (2020/08/09)
Disclosed are a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, and an application of the compound or slat in preparation of drugs for treating diseases related to an A2A receptor.
SODIUM CHANNEL BLOCKERS
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Page/Page column 46-47, (2016/09/22)
The present invention relates to a compound having a blocking effect against sodium ion channels, particularly Nav 1.7, a preparation method thereof and use thereof. The compound represented by the Formula 1 or a pharmaceutically acceptable salt, hydrate,
Design and synthesis of pyridine-pyrazolopyridine-based inhibitors of protein kinase B/Akt
Zhu, Gui-Dong,Gong, Jianchun,Gandhi, Viraj B.,Woods, Keith,Luo, Yan,Liu, Xuesong,Guan, Ran,Klinghofer, Vered,Johnson, Eric F.,Stoll, Vincent S.,Mamo, Mulugeta,Li, Qun,Rosenberg, Saul H.,Giranda, Vincent L.
, p. 2441 - 2452 (2007/10/03)
Thr-211 is one of three different amino acid residues in the kinase domain of protein kinase B/Akt as compared to protein kinase A (PKA), a closely related analog in the same AGC family. In an attempt to improve the potency and selectivity of our indazole-pyridine series of Akt inhibitors over PKA, efforts have focused on the incorporation of a chemical functionality to interact with the hydroxy group of Thr-211. Several substituents including an oxygen anion, amino, and nitro groups have been introduced at the C-6 position of the indazole scaffold, leading to a significant drop in Akt potency. Incorporation of a nitrogen atom into the phenyl ring at the same position (i.e., 9f) maintained the Akt activity and, in some cases, improved the selectivity over PKA. The structure-activity relationships of the new pyridine-pyrazolopyridine series of Akt inhibitors and their structural features when bound to PKA are also discussed.