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Last Updated: April 20, 2024

Claims for Patent: 7,709,493


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Summary for Patent: 7,709,493
Title:4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds and methods of their use
Abstract: 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: ##STR00001##
Inventor(s): Devasagayaraj; Arokiasamy (Plainsboro, NJ), Jin; Haihong (Manalapan, NJ), Shi; Zhi-Cai (Monmouth Junction, NJ), Tunoori; Ashok (Princeton, NJ), Wang; Ying (Plainsboro, NJ), Zhang; Chengmin (Morristown, NJ)
Assignee: Lexicon Pharmaceuticals, Inc. (The Woodlands, TX)
Application Number:12/468,974
Patent Claims: 1. A compound of the formula: ##STR00058## or a pharmaceutically acceptable salt thereof, wherein R.sub.4 is hydrogen or lower alkyl.

2. The compound of claim 1, wherein R.sub.4 is hydrogen.

3. The compound of claim 1, wherein R.sub.4 is lower alkyl.

4. The compound of claim 3, wherein R.sub.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)-phen- yl]-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: ##STR00059## or a pharmaceutically acceptable salt thereof, wherein R.sub.4 is hydrogen or lower alkyl.

17. The method of claim 16, wherein R.sub.4 is hydrogen.

18. The method of claim 16, wherein R.sub.4 is lower alkyl.

19. The method of claim 18, wherein R.sub.4 is ethyl.

20. The method of claim 16, wherein the administration is oral.

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