β-secretase inhibitors
View Patent ↗The present invention provides compounds that are inhibitors of the proteolytic activity of the enzyme β-secretase, pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the compounds, processes for making the compounds, and methods of using the compounds to treat Alzheimers disease.
1. A compound of Formula 1 or a pharmaceutically acceptable salt thereof:
wherein:
R 1 is independently selected from the group consisting of: C 1-4 alkyl, cyclic alkyl, arylalkyl, and aryloxyalkyl;
R 2 is independently selected from the group consisting of: hydrogen,
R 3 is independently selected from the group consisting of: C 1-4 alkyl, cycloalkyl, and arylalkyl;
and R 4 is independently selected from the group consisting of: C 1-4 alkyl and arylalkyl.
2. The compound of claim 1 wherein:
R 1 is independently selected from the group consisting of:
3. The compound of claim 1 wherein;
R 3 is independently selected from the group consisting of:
4. The compound of claim 1 wherein:
R 4 is independently selected from the group consisting of:
5. The compound of claim 1 wherein:
R 1 is independently selected from the group consisting of:
R 3 is independently selected from the group consisting of:
and R 4 is independently selected from the group consisting of:
6. A compound of Formula 2 or a pharmaceutically acceptable salt thereof:
wherein:
R 1 is independently selected from the group consisting of: C 1-4 alkyl, cyclic alkyl, arylalkyl, and aryloxyalkyl;
R 2 is independently selected from the group consisting of: hydrogen,
R 3 is independently selected from the group consisting of: C 1-4 alkyl, cycloalkyl, and arylalkyl;
and R 4 is independently selected from the group consisting of: C 1-4 alkyl and arylalkyl.
7. The compound of claim 6 wherein:
R 1 is independently selected from the group consisting of:
8. The compound of claim 6 wherein:
R 3 is independently selected from the group consisting of:
9. The compound of claim 6 wherein:
R 4 is independently selected from the group consisting of:
10. The compound or pharmaceutically acceptable salt thereof of claim 6 wherein:
R 1 is independently selected from the group consisting of:
R 3 is independently selected from the group consisting of:
and R 4 is independently selected from the group consisting of:
11. A compound which is selected from the group consisting of:
or a pharmaceutically acceptable salt thereof.
12. A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
13. A method for the treatment of a person suffering from or prone to Alzheimer's disease comprising administering to that person an effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof.