Macrocyclic acyl guanidines as beta-secretase inhibitors

Details Macrocyclic acyl guanidines as beta-secretase inhibitors Macrocyclic acyl guanidines as beta-secretase inhibitors

2008-04-08

2010-06-08

Kifle, Bruck (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C514S373000, C514S379000, C540S456000

Reexamination Certificate

active

07732434

ABSTRACT:
There is provided a series of heterocyclic-containing macrocyclic acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof,wherein R1, R2, R3, R4, R5, n and X as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

REFERENCES:
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