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Finding and Evaluating Generic and Branded Drug Market Entry Opportunities

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Generated: August 18, 2019

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Claims for Patent: 7,968,559

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Summary for Patent: 7,968,559
Title:Methods of using 4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds
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:12/754,341
Patent Claims: 1. A method of treating irritable bowel syndrome, which comprises administering to a patient in need thereof a therapeutically effective amount of a compound of the formula: ##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 method of claim 1, wherein the compound is of the formula: ##STR00059## 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.

3. The method of claim 1, wherein the compound 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 method of claim 1, wherein the compound is of the formula: ##STR00061## 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.

5. The method of claim 1, wherein the compound 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 p is 1-4.

6. The method of claim 1, wherein the compound is of the formula: ##STR00063## 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.

7. The method of claim 1, wherein the compound 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 q is 1-2.

8. The method of claim 1, wherein the compound is of the formula: ##STR00065## 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.

9. The method of claim 1, wherein R.sub.1 is hydrogen or halogen.

10. The method of claim 1, wherein m is 1.

11. The method of claim 1, wherein R.sub.2 is hydrogen or amino.

12. The method of claim 1, wherein R.sub.3 is hydrogen or lower alkyl.

13. The method of claim 1, wherein R.sub.4 is hydrogen or lower alkyl.

14. A method of treating irritable bowel syndrome, which comprises administering to a patient in need thereof a therapeutically effective amount of a compound of the formula: ##STR00066## or a pharmaceutically acceptable salt thereof, wherein R.sub.4 is hydrogen or lower alkyl.

15. The method of claim 14, wherein R.sub.4 is hydrogen.

16. The method of claim 14, wherein R.sub.4 is ethyl.

17. A method of treating carcinoid syndrome, which comprises administering to a patient in need thereof a therapeutically effective amount of a compound of the formula: ##STR00067## 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.

18. The method of claim 17, wherein the compound 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 n is 1-3.

19. The method of claim 17, wherein the compound is of the formula: ##STR00069## 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.

20. The method of claim 17, wherein the compound 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 n is 1-3.

21. The method of claim 17, wherein the compound is of the formula: ##STR00071## 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.

22. The method of claim 17, wherein the compound 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.

23. The method of claim 17, wherein the compound is of the formula: ##STR00073## 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.

24. The method of claim 17, wherein the compound is of the formula: ##STR00074## 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.

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

26. The method of claim 17, wherein m is 1.

27. The method of claim 17, wherein R.sub.2 is hydrogen or amino.

28. The method of claim 17, wherein R.sub.3 is hydrogen or lower alkyl.

29. The method of claim 17, wherein R.sub.4 is hydrogen or lower alkyl.

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