The In Vitro Pharmacology of GS-5759 , A Novel Bifunctional Phosphodiesterase 4 Inhibitor and Long Acting b 2-Adrenoceptor Agonist

@inproceedings{Tannheimer2014TheIV,
  title={The In Vitro Pharmacology of GS-5759 , A Novel Bifunctional Phosphodiesterase 4 Inhibitor and Long Acting b 2-Adrenoceptor Agonist},
  author={Stacey L. Tannheimer and Eric A. Sorensen and Zhi-Hua Cui and Musong Kim and Leena B. Patel and William R. Baker and Gary B. Phillips and Clifford D. Wright and Michael Salmon},
  year={2014}
}
Inhaled long-acting b2-adrenoceptor agonists (LABA) that act as bronchodilators and the oral anti-inflammatory phosphodiesterase 4 (PDE4) inhibitor roflumilast are both approved therapies for chronic obstructive pulmonary disease (COPD). Here we describe the activity of a novel, inhaled, bifunctional, small molecule (R)-6-[(3{[4-(5-{[2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl) ethyl]amino}pent-1-yn-1-yl)phenyl]carbamoyl}phenyl)sulfonyl]4-[(3-methoxyphenyl)amino]-8-methylquinoline-3… CONTINUE READING