Truong A.P.,Elan Pharmaceuticals Inc. |
Toth G.,Elan Pharmaceuticals Inc. |
Probst G.D.,Elan Pharmaceuticals Inc. |
Sealy J.M.,Elan Pharmaceuticals Inc. |
And 29 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 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. © 2010 Elsevier Ltd. All rights reserved.