4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds and methods of their use
View Patent ↗Compounds of formula I are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and/or manage diseases and disorders:
1. A compound of the formula:
or a pharmaceutically acceptable salt thereof, wherein R 4 is hydrogen or lower alkyl.
2. The compound of claim 1 , wherein R 4 is hydrogen.
3. The compound of claim 1 , wherein R 4 is lower alkyl.
4. The compound of claim 3 , wherein R 4 is ethyl.
5. A composition comprising the compound of claim 1 and a pharmaceutically acceptable excipient or diluent.
6. A dosage form suitable for administration to a patient comprising the composition of claim 5 .
7. The dosage form of claim 6 , which is suitable for oral administration.
8. The dosage form of claim 7 , which is a tablet.
9. The dosage form of claim 7 , which is a capsule.
10. A compound, which is (S)-2-amino-3-[4-(2-amino-6-{R-1-[4-chloro-2-(3-methyl-pyrazol-1-yl)-phenyl]-2,2,2-trifluoro-ethoxy}-pyrimidin-4-yl)-phenyl]-propionic acid ethyl ester or a pharmaceutically acceptable salt thereof.
11. A tablet comprising the compound of claim 10 and a pharmaceutically acceptable excipient.
12. A capsule comprising the compound of claim 10 and a pharmaceutically acceptable excipient.
13. A compound, which is (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid or a pharmaceutically acceptable salt thereof.
14. A tablet comprising the compound of claim 13 and a pharmaceutically acceptable excipient.
15. A capsule comprising the compound of claim 13 and a pharmaceutically acceptable excipient.
16. A method of treating or managing carcinoid syndrome, which comprises administering to a patient in need thereof a therapeutically effective amount of a compound of the formula:
or a pharmaceutically acceptable salt thereof, wherein R 4 is hydrogen or lower alkyl.
17. The method of claim 16 , wherein R 4 is hydrogen.
18. The method of claim 16 , wherein R 4 is lower alkyl.
19. The method of claim 18 , wherein R 4 is ethyl.
20. The method of claim 16 , wherein the administration is oral.