gsk-2126458 and Cough

Two applications claim the use of the closely related, broad spectrum phosphatidylinositol 3-kinase inhibitors 2,4-difluoro-N-{2-(methoxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl}benzenesulfonamide (GSK-2126458) and 2,4-difluoro-N-{2-(methoxy)-5-[4-(4-morpholino)-6-quinazolinyl]-3-pyridinyl}benzenesulfonamide for the treatment of idiopathic pulmonary fibrosis and cough, respectively. Some in vitro data are presented in support of these claimed utilities. Since the filing of these applications, GSK-2126458 has commenced a dose-finding Phase I study in patients with idiopathic pulmonary fibrosis.

Topics: Cough; Drug Discovery; Fibroblasts; Humans; Patents as Topic; Phosphoinositide-3 Kinase Inhibitors; Phosphorylation; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-akt; Pulmonary Fibrosis; Pyridazines; Quinolines; Sulfonamides