1094070-77-5Relevant articles and documents
SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS
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Page/Page column 64-65, (2021/04/10)
Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein X, Y, A, G, R1, and R5 are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
(NHC)Cu-Catalyzed Mild C-H Amidation of (Hetero)arenes with Deprotectable Carbamates: Scope and Mechanistic Studies
Xie, Weilong,Yoon, Jung Hee,Chang, Sukbok
, p. 12605 - 12614 (2016/10/07)
Primary arylamines are an important unit broadly found in synthetic, biological, and materials science. Herein we describe the development of a (NHC)Cu system that mediates a direct C-H amidation of (hetero)arenes by using N-chlorocarbamates or their sodio derivatives as the practical amino sources. A facile stoichiometric reaction of reactive copper-aryl intermediates with the amidating reagent led us to isolate key copper arylcarbamate species with the formation of a C-N bond. The use of tBuONa base made this transformation catalytic under mild conditions. The present (NHC)Cu-catalyzed C-H amidation works efficiently and selectively on a large scale over a range of arenes including polyfluorobenzenes, azoles, and quinoline N-oxides. Deprotection of the newly installed carbamate groups such as Boc and Cbz was readily performed to afford the corresponding primary arylamines.
Azole-based inhibitors of AKT/PKB for the treatment of cancer
Zeng, Qingping,Allen, John G.,Bourbeau, Matthew P.,Wang, Xianghong,Yao, Guomin,Tadesse, Seifu,Rider, James T.,Yuan, Chester C.,Hong, Fang-Tsao,Lee, Matthew R.,Zhang, Shiwen,Lofgren, Julie A.,Freeman, Daniel J.,Yang, Suijin,Li, Chun,Tominey, Elizabeth,Huang, Xin,Hoffman, Douglas,Yamane, Harvey K.,Fotsch, Christopher,Dominguez, Celia,Hungate, Randall,Zhang, Xiaoling
scheme or table, p. 1559 - 1564 (2010/06/16)
Through a combination of screening and structure-based rational design, we have discovered a series of N1-(5-(heterocyclyl)-thiazol-2-yl)-3-(4-trifluoromethylphenyl)-1,2-propanediamines that were developed into potent ATP competitive inhibitors of AKT. Studies of linker strand-binding adenine isosteres identified SAR trends in potency and selectivity that were consistent with binding interactions observed in structures of the inhibitors bound to AKT1 and to the counter-screening target PKA. One compound was shown to have acceptable pharmacokinetic properties and to be a potent inhibitor of AKT signaling and of in vivo xenograft tumor growth in a preclinical model of glioblastoma.