445003-61-2Relevant academic research and scientific papers
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
scheme or table, p. 6231 - 6236 (2010/12/18)
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.
METHODS OF TREATING AMYLOIDOSIS USING ARYL-CYCLOPROPYL DERIVATIVE ASPARTYL PROTEASE INHIBITORS
-
Page/Page column 86, (2010/11/27)
The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta prote
Carboxylic acid amides having antithrombotic activity
-
, (2008/06/13)
Compounds with antithrombotic activity and factor Xa-inhibiting activity of the general formula: Exemplary are: (1) (L)-2-(5-carbamimidoyl-2-hydroxy-phenyl)-N-[3-methyl-4-(2-aminocarbonyl-pyrrolidin-1-yl-carbonyl)-phenyl]-acetamide, (2) 2-(5-carbamimidoyl
