1583-66-0Relevant articles and documents
Effect of Substituents at the 5-Position on the First and Second Dissociation Constants of Isophthalic Acid
Gumbley, Stewart J.,Stewart, Ross
, p. 529 - 532 (1984)
The dissociation constants of benzoic acid and 20 of its meta- or para-substituted derivatives and of isophthalic acid and ten of its 5-substituted derivatives have been measured in 50 wtpercent aqueous methanol.The Hammett ρ value for benzoic acid is 1.28; for isophthalic acid the ρ values are 1.21 (pK1) and 1.20 (pK2).The ?meta values for hydroxy and acetoxy are -0.01 and +0.29, respectively, in this system.Values for ?meta for CO2H and CO2- are calculated to be +0.28 and -0.20, respectively; however there are indications that these values are not completely structure-independent.
COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF
-
Page/Page column 55; 60, (2008/06/13)
The present invention provides novel beta-secretase inhibitors of the general formula (I), where the variables A1, A2, L1, L2, L3, R1, R2, R3, R4, R5, R6 and R7 are as defined in the claims, a method for their use in treating Alzheimer's disease, and methods for their use in reducing memapsin 2 catalytic activity.