1234616-25-1Relevant academic research and scientific papers
HPK1 ANTAGONISTS AND USES THEREOF
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Paragraph 1202; 1203, (2021/03/19)
The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.
Diversification of Heteroaryl-Aryl Ether via Ligand-Free, Copper-Catalyzed O-Arylation Under Microwave Heating
Byeon, Jeong Seob,Choi, Sung Min,Yum, Eul Kgun
, (2020/08/12)
Diverse O-arylated pyrrolo[2,3-d]pyrimidine and pyrrolo[2,3-b]pyridine were obtained using relatively low amounts of Cu catalyst with ligand-free conditions under microwave heating. The O-arylation reaction could be applied to less oxidative heteroaryl-chlorides. The microwave-assisted Cu-catalyzed O-aryaltion would be useful for preparing potent bioactive compounds for drug discovery while reducing waste, time, and saving energy.
ARYL-BIPYRIDINE AMINE DERIVATIVES AS PHOSPHATIDYLINOSITOL PHOSPHATE KINASE INHIBITORS
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Paragraph 0490, (2019/07/13)
The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula (I): wherein A, X, Y, Z, Q, R1, R2, R3, R4, R5, and n are described herein.
Palladium-catalyzed aminocarbonylation of halo-substituted 7-azaindoles and other heteroarenes using chloroform as a carbon monoxide source
Kannaboina, Prakash,Raina, Gaurav,Anil Kumar,Das, Parthasarathi
supporting information, p. 9446 - 9449 (2017/09/01)
A palladium-catalyzed aminocarbonylation of halo-substituted 7-azaindoles utilizing CHCl3 as the carbonyl source has been developed for the straightforward incorporation of an amide functional group. The protocol was extended to other heteroarenes such as pyrazolopyridines and indazoles. The substrate scope of the reaction with respect to heteroarenes and the amine component is reported. This method offers an alternative avenue for aminocarbonylation of pharmaceutically important heterocycles.
Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR)
Tsou, Hwei-Ru,MacEwan, Gloria,Birnberg, Gary,Grosu, George,Bursavich, Matthew G.,Bard, Joel,Brooijmans, Natasja,Toral-Barza, Lourdes,Hollander, Irwin,Mansour, Tarek S.,Ayral-Kaloustian, Semiramis,Yu, Ker
scheme or table, p. 2321 - 2325 (2010/08/22)
We discovered 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR). Since phenolic OH groups pose metabolic liability, one of th
