Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.

Janus kinases (JAK1, JAK2, JAK3, and TYK2) are involved in the signaling of multiple cytokines important in cellular function. Blockade of the JAK-STAT pathway with a small molecule has been shown to provide therapeutic immunomodulation. Having identified JAK1 as a possible new target for arthritis at Galapagos, the compound library was screened against JAK1, resulting in the identification of a triazolopyridine-based series of inhibitors represented by 3.

Evidence of a green luminescence band related to surface flaws in high purity silica glass.

Using luminescence confocal microscopy under 325 nm laser excitation, we explore the populations of defects existing in or at the vicinity of macroscopic surface flaws in fused silica. We report our luminescence results on two types of surface flaws: laser damage and indentation on fused silica polished surfaces. Luminescence cartographies are made to show the spatial distribution of each kind of defect.