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Last Updated: March 29, 2024

Claims for Patent: 7,553,840


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Summary for Patent: 7,553,840
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:11/954,000
Patent Claims: 1. A compound of formula I: ##STR00058## or a pharmaceutically acceptable salt thereof, wherein: A.sub.1 is optionally substituted heterocycle; each R.sub.1 is independently halogen, hydrogen, C(O)R.sub.A, OR.sub.A, NR.sub.BR.sub.C, S(O.sub.2)R.sub.A, or optionally substituted alkyl, alkyl-aryl or alkyl-heterocycle; R.sub.2 is independently halogen, hydrogen, C(O)R.sub.A, OR.sub.A, NR.sub.BR.sub.C, S(O.sub.2)R.sub.A, or optionally substituted alkyl, alkyl-aryl or alkyl-heterocycle; R.sub.3 is hydrogen, C(O)R.sub.A, C(O)OR.sub.A, or optionally substituted alkyl, alkyl-aryl, alkyl-heterocycle, aryl, or heterocycle; R.sub.4 is hydrogen or optionally substituted alkyl, alkyl-aryl, alkyl-heterocycle, aryl, or heterocycle; each R.sub.A is independently hydrogen or optionally substituted alkyl, alkyl-aryl or alkyl-heterocycle; each R.sub.B is independently hydrogen or optionally substituted alkyl, alkyl-aryl or alkyl-heterocycle; each R.sub.C is independently hydrogen or optionally substituted alkyl, alkyl-aryl or alkyl-heterocycle; and m is 1-4.

2. The compound of claim 1, which is of the formula: ##STR00059##

3. The compound of claim 1, which is of the formula: ##STR00060## wherein: each R.sub.5 is independently halogen, hydrogen, C(O)R.sub.A, OR.sub.A, NR.sub.BR.sub.C, S(O.sub.2)R.sub.A, or optionally substituted alkyl, alkyl-aryl or alkyl-heterocycle; and n is 1-3.

4. The compound of claim 3, which is of the formula: ##STR00061##

5. The compound of claim 1, which is of the formula: ##STR00062## wherein: each R.sub.5 is independently halogen, hydrogen, C(O)R.sub.A, OR.sub.A, NR.sub.BR.sub.C, S(O.sub.2)R.sub.A, or optionally substituted alkyl, alkyl-aryl or alkyl-heterocycle; and n is 1-3.

6. The compound of claim 5, which is of the formula: ##STR00063##

7. The compound of claim 1, which is of the formula: ##STR00064## wherein: each R.sub.5 is independently halogen, hydrogen, C(O)R.sub.A, OR.sub.A, NR.sub.BR.sub.C, S(O.sub.2)R.sub.A, or optionally substituted alkyl, alkyl-aryl or alkyl-heterocycle; and n is 1-3.

8. The compound of claim 7, which is of the formula: ##STR00065##

9. The compound of claim 1, which is of the formula: ##STR00066## wherein: each R.sub.5 is independently halogen, hydrogen, C(O)R.sub.A, OR.sub.A, NR.sub.BR.sub.C, S(O.sub.2)R.sub.A, or optionally substituted alkyl, alkyl-aryl or alkyl-heterocycle; and p is 1-4.

10. The compound of claim 9, which is of the formula: ##STR00067##

11. The compound of claim 1, which is of the formula: ##STR00068## wherein: each R.sub.5 is independently halogen, hydrogen, C(O)R.sub.A, OR.sub.A, NR.sub.BR.sub.C, S(O.sub.2)R.sub.A, or optionally substituted alkyl, alkyl-aryl or alkyl-heterocycle; and q is 1-2.

12. The compound of claim 11, which is of the formula: ##STR00069##

13. The compound of claim 1, which is of the formula: ##STR00070## wherein: each R.sub.5 is independently halogen, hydrogen, C(O)R.sub.A, OR.sub.A, NR.sub.BR.sub.C, S(O.sub.2)R.sub.A, or optionally substituted alkyl, alkyl-aryl or alkyl-heterocycle; and q is 1-2.

14. The compound of claim 13, which is of the formula: ##STR00071##

15. The compound of claim 1, which is of the formula: ##STR00072## wherein: each R.sub.5 is independently halogen, hydrogen, C(O)R.sub.A, OR.sub.A, NR.sub.BR.sub.C, S(O.sub.2)R.sub.A, or optionally substituted alkyl, alkyl-aryl or alkyl-heterocycle; and q is 1-2.

16. The compound of claim 15, which is of the formula: ##STR00073##

17. The compound of claim 1, wherein R.sub.1 is hydrogen or halogen.

18. The compound of claim 1, wherein m is 1.

19. The compound of claim 1, wherein R.sub.2 is hydrogen or amino.

20. The compound of claim 1, wherein R.sub.3 is hydrogen or lower alkyl.

21. The compound of claim 1, wherein R.sub.3 is C(O)OR.sub.A and R.sub.A is alkyl.

22. The compound of claim 1, wherein R.sub.4 is hydrogen or lower alkyl.

23. A composition comprising a compound of claim 1 and a pharmaceutically acceptable excipient or diluent.

24. A single unit dosage form comprising the composition of claim 23.

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