Christine Chabot

TL;DR: Biological studies with one 6,7-dihydro-5H-cyclopenta[d]pyrimidine compound, 28 (GDC-0068), demonstrate good oral exposure resulting in dose-dependent pharmacodynamic effects on downstream biomarkers and a robust antitumor response in xenograft models in which the phosphatidylinositol 3-kinase-Akt-mammalian target of rapamycin pathway is activated.

TL;DR: A tandem Mitsunobu/3,3-sigmatropic rearrangement of allylic azides on a chiral auxiliary system that favors one regioisomer thanks to its exceptional steric bias is described.

TL;DR: The discovery of novel, potent, and selective PI3Kδ inhibitors are reported and a structural hypothesis for isoform (α, β, γ) selectivity gained from interactions in the affinity pocket is described.

TL;DR: A series of potent and selective benzimidazole-based inhibitors of PI3Kδ are identified using a structure-based design approach and the pharmacokinetic properties and the ability of compound 5 to inhibit the function of B-cells in vivo are described.

TL;DR: In this article, the present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof.