1249463-71-5Relevant articles and documents
Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model
Truong, Anh P.,Tóth, Gergley,Probst, Gary D.,Sealy, Jennifer M.,Bowers, Simeon,Wone, David W.G.,Dressen, Darren,Hom, Roy K.,Konradi, Andrei W.,Sham, Hing L.,Wu, Jing,Peterson, Brian T.,Ruslim, Lany,Bova, Michael P.,Kholodenko, Dora,Motter, Ruth N.,Bard, Frédérique,Santiago, Pamela,Ni, Huifang,Chian, David,Soriano, Ferdie,Cole, Tracy,Brigham, Elizabeth F.,Wong, Karina,Zmolek, Wes,Goldbach, Erich,Samant, Bhushan,Chen, Linda,Zhang, Hongbing,Nakamura, David F.,Quinn, Kevin P.,Yednock, Ted A.,Sauer, John-Michael
, p. 6231 - 6236 (2010)
In this Letter, we describe our efforts to design HEA BACE-1 inhibitors that are highly permeable coupled with negligible levels of permeability- glycoprotein activity. These efforts culminate in producing 16 which lowers Αβ by 28% and 32% in the cortex and CSF, respectively, in the preclinical wild type Hartley guinea pig animal model when dosed orally at 30 mpk BID for 2.5 days.
Palladium-Catalyzed α-Arylation of Carboxylic Acids and Secondary Amides via a Traceless Protecting Strategy
He, Zhi-Tao,Hartwig, John F.
supporting information, p. 11749 - 11753 (2019/08/26)
A novel traceless protecting strategy is presented for the long-standing challenge of conducting the palladium-catalyzed α-arylation of carboxylic aids and secondary amides with aryl halides. Both of the presented coupling processes occur with a variety of carboxylic acids and amides and with a variety of aryl bromides containing a broad range of functional groups, including base-sensitive functionality like acyl, alkoxycarbonyl, nitro, cyano, and even hydroxyl groups. Five commercial drugs were prepared through this method in one step in 81-96% yield. Gram-scale synthesis of medication Naproxen and Flurbiprofen with low palladium loading further highlights the practical value of this method.
Amine Substituted Methanesulfonamide Derivatives as Vanilloid Receptor Ligands
-
, (2013/04/10)
The invention relates to amine substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
