Dauh-Rurng Wu

TL;DR: Different enantioselective chromatography techniques are reviewed here, with particular emphasis on the most widespread high performance liquid Chromatography (HPLC) and the rapidly emerging supercritical fluid chromatography (SFC) techniques.

TL;DR: The structure-activity relationships (SAR) leading to a novel series of highly potent and selective carbazole and tetrahydrocarbazole based, reversible inhibitors of BTK are detailed, resulting in enhanced potency and selectivity as well as a reduction in safety liabilities.

TL;DR: Structure-activity relationships in a series of (2-oxo-1,4-benzodiazepin-3-yl)-succinamides identified highly potent inhibitors of γ-secretase mediated signaling of Notch1/2/3/4 receptors selected as a candidate for clinical evaluation.

TL;DR: A new phenyl (3-phenylpyrrolidin-3-yl)sulfone series of RORγt inverse agonists was discovered utilizing the binding conformation of previously reported bicyclic sulfonamide 1 to achieve high selectivity against PXR, LXRα, and LXRβ.

TL;DR: The optimization of a high throughput screening hit to yield benzothiazine and tetrahydroquinoline sulfonamides as potent RORγt inverse agonists showed potent activity against pregnane X receptor (PXR) and modest activity against liver X receptor α (XRα).