1350708-05-2Relevant academic research and scientific papers
Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors
Jaime-Figueroa, Saul,De Vicente, Javier,Hermann, Johannes,Jahangir, Alam,Jin, Sue,Kuglstatter, Andreas,Lynch, Stephen M.,Menke, John,Niu, Linghao,Patel, Vaishali,Shao, Ada,Soth, Michael,Vu, Minh Diem,Yee, Calvin
supporting information, p. 2522 - 2526 (2013/06/26)
We report the discovery of a novel series of ATP-competitive Janus kinase 3 (JAK3) inhibitors based on the 5H-pyrrolo[2,3-b]pyrazine scaffold. The initial leads in this series, compounds 1a and 1h, showed promising potencies, but a lack of selectivity against other isoforms in the JAK family. Computational and crystallographic analysis suggested that the phenyl ether moiety possessed a favorable vector to achieve selectivity. Exploration of this vector resulted in the identification of 12b and 12d, as potent JAK3 inhibitors, demonstrating improved JAK family and kinase selectivity.
PYRROLO [2, 3 - B] PYRAZINE - 7 - CARBOXAMIDE DERIVATIVES AND THEIR USE AS JAK AND SYK INHIBITORS
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Page/Page column 198-199, (2011/12/04)
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula (I), wherein the variables Q and R, R2, and R3 are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
