gsk2292767 has been researched along with Respiratory-Tract-Diseases* in 2 studies
2 other study(ies) available for gsk2292767 and Respiratory-Tract-Diseases
| Article | Year |
|---|---|
Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.
A four-step process of high-quality modeling of existing data, deconstruction, identification of replacement cores, and an innovative synthetic regrowth strategy led to the rapid discovery of a novel oral series of PI3Kδ inhibitors with promising selectivity and excellent in vivo characteristics. Topics: Administration, Inhalation; Animals; Biological Availability; Class Ia Phosphatidylinositol 3-Kinase; Dose-Response Relationship, Drug; Male; Models, Molecular; Molecular Structure; Phosphoinositide-3 Kinase Inhibitors; Protein Kinase Inhibitors; Rats; Rats, Sprague-Dawley; Respiratory Tract Diseases; Structure-Activity Relationship | 2016 |
Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease.
Optimization of lead compound 1, through extensive use of structure-based design and a focus on PI3Kδ potency, isoform selectivity, and inhaled PK properties, led to the discovery of clinical candidates 2 (GSK2269557) and 3 (GSK2292767) for the treatment of respiratory indications via inhalation. Compounds 2 and 3 are both highly selective for PI3Kδ over the closely related isoforms and are active in a disease relevant brown Norway rat acute OVA model of Th2-driven lung inflammation. Topics: Administration, Inhalation; Animals; Asthma; Female; Humans; Indazoles; Indoles; Isoenzymes; Male; Microsomes; Molecular Docking Simulation; Ovalbumin; Oxazoles; Phosphoinositide-3 Kinase Inhibitors; Piperazines; Pneumonia; Pulmonary Disease, Chronic Obstructive; Rabbits; Rats; Rats, Sprague-Dawley; Respiratory Tract Diseases; Stereoisomerism; Structure-Activity Relationship; Sulfonamides; Th2 Cells | 2015 |