19228-91-2Relevant articles and documents
A Scaffold-Hopping Strategy toward the Identification of Inhibitors of Cyclin G Associated Kinase
Wouters, Randy,Tian, Junjun,Herdewijn, Piet,De Jonghe, Steven
, p. 237 - 254 (2019/01/08)
We recently reported the discovery of isothiazolo[4,3-b]pyridine-based inhibitors of cyclin G associated kinase (GAK) displaying low nanomolar binding affinity for GAK and demonstrating broad-spectrum antiviral activity. To come up with novel core structures that act as GAK inhibitors, a scaffold-hopping approach was applied starting from two different isothiazolo[4,3-b]pyridines. In total, 13 novel 5,6- and 6,6-fused bicyclic heteroaromatic scaffolds were synthesized. Four of them displayed GAK affinity with Kd values in the low micromolar range that can serve as chemical starting points for the discovery of GAK inhibitors based on a different scaffold.
Efficient and Mild Ullmann-Type N-Arylation of Amides, Carbamates, and Azoles in Water
Bollenbach, Maud,Aquino, Pedro G. V.,de Araújo-Júnior, Jo?o Xavier,Bourguignon, Jean-Jacques,Bihel, Frédéric,Salomé, Christophe,Wagner, Patrick,Schmitt, Martine
supporting information, p. 13676 - 13683 (2017/10/10)
A simple, sustainable, efficient, mild, and low-cost protocol was developed for d-glucose-assisted Cu-catalyzed Ullmann reactions in water for amides, carbamates, and nitrogen-containing heterocycles. The reaction was compatible with diverse aryl/heteroaryl iodides, giving highly substituted pyridine, indole, or indazole rings. This method offers an attractive alternative to existing protocols, because the reaction proceeds in aqueous media, occurs at or near ambient temperature, and provides the N-arylated products in good to high yields.
N-Unsubstituted thienoisoindigos: preparation, molecular packing and ambipolar organic field-effect transistors
Yoo, Dongho,Hasegawa, Tsukasa,Ashizawa, Minoru,Kawamoto, Tadashi,Masunaga, Hiroyasu,Hikima, Takaaki,Matsumoto, Hidetoshi,Mori, Takehiko
supporting information, p. 2509 - 2512 (2017/03/17)
N-Unsubstituted thienoisoindigo (TIIG) and its diphenyl derivative (dph-TIIG) are synthesized by using a tert-butoxy carbonyl (t-Boc) group as a protecting group. TIIG has a stacking structure analogous to isoindigo, and dph-TIIG is a hybrid of brickwork
Substituted 1,2,3,4-tetrahydrobenzo[C][2,7] naphthyridines and derivatives thereof as kinase inhibitors
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Page/Page column 45-56, (2016/03/06)
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
PYRROLOTRIAZINE INHIBITORS OF IRAK4 ACTIVITY
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Page/Page column 40, (2016/09/26)
The present invention relates to pyrrolotriazine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
PYRAZOLOPYRIMIDINE INHIBITORS OF IRAK4 ACTIVITY
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Page/Page column 61, (2016/09/26)
The present invention relates to pyrazolopyrimidine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
THIENOPYRAZINE INHIBITORS OF IRAK4 ACTIVITY
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Page/Page column 34; 35, (2016/09/26)
The present invention relates to thienopyrazine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
PYRROLOPYRIDAZINE INHIBITORS OF IRAK4 ACTIVITY
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Page/Page column 38, (2016/09/26)
The present invention relates to pyrrolopyridazine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
Ligandless copper-catalyzed coupling of heteroaryl bromides with gaseous ammonia
Fantasia, Serena,Windisch, Johannes,Scalone, Michelangelo
supporting information, p. 627 - 631 (2013/04/11)
A range of different N- and S-containing heterocyclic bromides can be efficiently coupled with gaseous ammonia in the presence of copper(II) acetylacetonate [Cu(acac)2] as catalyst and in the absence of additional ligands. Unstable aminothiophenes and aminobenzothiophenes can be further reacted in situ to afford functionalized derivatives. Copyright
Palladium-catalyzed amidation of aryl halides using 2-dialkylphosphino- 2′-alkoxyl-1,1′-binaphthyl as ligands
Ma, Fangfang,Xie, Xiaomin,Zhang, Lei,Peng, Zhiyong,Ding, Lina,Fu, Lei,Zhang, Zhaoguo
experimental part, p. 5279 - 5285 (2012/08/07)
Palladium-catalyzed intermolecular C-N bond-forming reactions between aryl halides and amides are described using 2-dialkylphosphino-2′-alkoxyl-1, 1′-binaphthyl, which is both bulky and electron-rich, as the ligand. A variety of amides, including aliphatic and aromatic primary amides, lactams, and carbamates, were viable substrates for the amidation, which exhibited good functional group compatibility. By tuning the substituents at the 2,2′-position of 1,1′-binaphthyl of the ligand, the palladium-catalyzed amidation of bulky aryl halides was realized and this coupling reaction was used to synthesize 2-amino-2′-methoxy-1,1′- binaphthyl in high yield.
