Discovery of ( R )-4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1 H -pyrazolo[4,3- c ]quinoline (ELND006) and ( R )-4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2 H -pyrazolo[4,3- c ]quinoline (ELND007): Metabolically Stable γ-Secretase Inhibitors that Selectively Inhibit the Production of Amyloid-β over Notch

✍ Scribed by Probst, Gary; Aubele, Danielle L.; Bowers, Simeon; Dressen, Darren; Garofalo, Albert W.; Hom, Roy K.; Konradi, Andrei W.; Marugg, Jennifer L.; Mattson, Matthew N.; Neitzel, Martin L.; Semko, Chris M.; Sham, Hing L.; Smith, Jenifer; Sun, Minghua; Truong, Anh P.; Ye, Xiaocong M.; Xu, Ying-zi; Dappen, Michael S.; Jagodzinski, Jacek J.; Keim, Pamela S.; Peterson, Brian; Latimer, Lee H.; Quincy, David; Wu, Jing; Goldbach, Erich; Ness, Daniel K.; Quinn, Kevin P.; Sauer, John-Michael; Wong, Karina; Zhang, Hongbin; Zmolek, Wes; Brigham, Elizabeth F.; Kholodenko, Dora; Hu, Kang; Kwong, Grace T.; Lee, Michael; Liao, Anna; Motter, Ruth N.; Sacayon, Patricia; Santiago, Pamela; Willits, Christopher; Bard, Frédérique; Bova, Michael P.; Hemphill, Susanna S.; Nguyen, Lam; Ruslim, Lany; Tanaka, Kevin; Tanaka, Pearl; Wallace, William; Yednock, Ted A.; Basi, Guriqbal S.

• Book ID: 120469102
• Publisher: American Chemical Society
• Year: 2013
• Tongue: English
• Weight: 964 KB
• Volume: 56
• Category: Article
• ISSN: 0022-2623
• DOI: 10.1021/jm301741t