346629-30-9Relevant academic research and scientific papers
Process development and large-scale synthesis of a PDE4 inhibitor
Conlon, David A.,Drahus-Paone, Antoinette,Ho, Guo-Jie,Pipik, Brenda,Helmy, Roy,McNamara, James M.,Shi, Yao-Jun,Williams, J. Michael,Macdonald, Dwight,Deschenes, Denis,Gallant, Michel,Mastracchio, Anthony,Roy, Bruno,Scheigetz, John
, p. 36 - 45 (2012/12/21)
An efficient, scalable synthesis of the PDE4 inhibitor, 6-[1-methyl-1-(methylsulfonyl)ethyl]-8-(3-{(E)-2-(3-methyl-1,2,4-oxadiazol-5-yl) -2-[4-(methylsulfonyl)phenyl]vinyl}phenyl)-quinoline benzenesulfonate (10) is described. The synthesis is highly conve
Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: Structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor
Macdonald, Dwight,Mastracchio, Anthony,Perrier, Helene,Dube, Daniel,Gallant, Michel,Lacombe, Patrick,Deschenes, Denis,Roy, Bruno,Scheigetz, John,Bateman, Kevin,Li, Chun,Trimble, Laird A.,Day, Stephen,Chauret, Nathalie,Nicoll-Griffith, Deborah A.,Silva, Jose M.,Huang, Zheng,Laliberte, France,Liu, Susana,Ethier, Diane,Pon, Doug,Muise, Eric,Boulet, Louise,Chi, Chung Chan,Styhler, Angela,Charleson, Stella,Mancini, Joseph,Masson, Paul,Claveau, David,Nicholson, Donald,Turner, Mervyn,Young, Robert N.,Girard, Yves
, p. 5241 - 5246 (2007/10/03)
The discovery and SAR of a new series of substituted 8-arylquinoline PDE4 inhibitors are herein described. This work has led to the identification of several compounds with excellent in vitro and in vivo profiles, including a good therapeutic window of em
