Macrocyclic acyl guanidines as beta-secretase inhibitors
AssigneeBristol-Myers Squibb Company
InventorsShuhao Shi, Samuel Gerritz, Shirong Zhu
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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.
Claims5
A compound of the Formula (I);
- or a stereoisomer thereof
- wherein
- represents a single or double bond;
- R1 and R2 are independently hydrogen, halogen, C1-4alkyl or CF3;
- R3 is hydrogen, C1-4alkyl, fluoro C1-4alkyl, CF3 or benzyl;
- R4 is hydrogen, C1-4alkyl or phenyl in which each is optionally substituted with halogen, C1-4alkyl or C1-4alkoxy;
- R5 is hydrogen, halogen, CF3, OH, NH2, C1-4alkyl or C1-4alkoxy;
- n is an integer of 1, 2, 3 or 4;
- and
- X is O or S;
- or a nontoxic pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.