Claims
- 1. A compound of the formula:
- 2. The compound of claim 1, wherein
R1 is H, OH, F, or Cl; R2 is phenyl optionally p-substituted with lower alkoxy, OH, CN, F, Cl, Br, I, NO2, NH2, C(O)NH2, CO2H, or CO2R′; R3 is H; R4 is N-oxy p-pyridyl or p-pyridyl optionally substituted with F, Cl, Br, or I; and X is CH2.
- 3. The compound of claim 1, wherein
R1 is H, OH, F, or Cl; R2 is phenyl optionally p-substituted with lower alkoxy, OH, CN, F, Cl, Br, I, NO2, NH2, C(O)NH2, CO2H, or CO2R′; R3 is H; R4 is o-pyridyl optionally substituted with F, Cl, Br, or I; and X is CH2.
- 4. The compound of claim 1, wherein
R1 is H, OH, F, or Cl; R2 is phenyl optionally p-substituted with lower alkoxy, OH, CN, F, Cl, Br, I, NO2, NH2, C(O)NH2, CO2H, or CO2R′; R3 is H; R4 is m-pyridyl optionally substituted with F, Cl, Br, or I; and X is CH2.
- 5. The compound of claim 2, wherein R1 is H.
- 6. The compound of claim 2, wherein R1 is OH.
- 7. The compound of claim 2, wherein R1 is F.
- 8. The compound of claim 3, wherein R1 is H.
- 9. The compound of claim 4, wherein R1 is H.
- 10. The compound of claim 4, wherein R1 is OH or F.
- 11. The compound of claim 5, wherein R2 is phenyl p-substituted with CN, F, or Cl.
- 12. The compound of claim 6, wherein R2 is phenyl p-substituted with F.
- 13. The compound of claim 7, wherein R2 is phenyl p-substituted with F or OH.
- 14. The compound of claim 8, wherein R2 is phenyl p-substituted with CN and R4 is pyridyl.
- 15. The compound of claim 8, wherein R2 is phenyl or phenyl p-substituted with Cl or F.
- 16. The compound of claim 9, wherein R2 is phenyl or phenyl p-substituted with CN, F, Cl, NO2, NH2, or C(O)NH2.
- 17. The compound of claim 10, wherein R2 is phenyl or phenyl p-substituted with CN, F, Cl, NO2, NH2, or C(O)NH2.
- 18. The compound of claim 11, wherein R4 is pyridyl di-substituted with Cl at 2- and 6-positions.
- 19. The compound of claim 12, wherein R4 is pyridyl di-substituted with Cl at 2- and 6-positions.
- 20. A pharmaceutical composition comprising
a compound of the formula: 12wherein R1 is H, lower alkyl, lower alkoxy, OH, F, Cl, Br, I, NO2, or CN; R2 is alkyl optionally substituted with lower alkoxy, OH, CN, F, Cl, Br, I, NO2, NH2, C(O)NH2, CO2H, or CO2R′; or aryl optionally substituted with lower alkyl, lower alkoxy, OH, CN, F, Cl, Br, I, NO2, NH2, C(O)NH2, CO2H, or CO2R′; R3 is H or lower alkyl; R4 is N-oxy pyridyl or pyridyl optionally substituted with F, Cl, Br, or I; and X is C(R′R″), N(R′), O, S, S(O), S(O)2, C(O), C(O)—N(R′), N(R′)—C(O), or deleted; in which each of R′ and R″, independently, is H, or alkyl optionally substituted with lower alkoxy, OH, CN, F, Cl, Br, I, NO2, NH2, or C(O)NH2; and a pharmaceutically acceptable carrier.
- 21. The composition of claim 20, wherein
R1 is H, OH, F, or Cl; R2 is phenyl optionally p-substituted with lower alkoxy, OH, CN, F, Cl, Br, I, NO2, NH2, C(O)NH2, CO2H, or CO2R′; R3 is H; R4 is N-oxy p-pyridyl or p-pyridyl optionally substituted with F, Cl, Br, or I; and X is CH2.
- 22. The composition of claim 20, wherein
R1 is H, OH, F, or Cl; R2 is phenyl optionally p-substituted with lower alkoxy, OH, CN, F, Cl, Br, I, NO2, NH2, C(O)NH2, CO2H, or CO2R′; R3 is H; R4 is o-pyridyl optionally substituted with F, Cl, Br, or I; and X is CH2.
- 23. The composition of claim 20, wherein
R1 is H, OH, F, or Cl; R2 is phenyl optionally p-substituted with lower alkoxy, OH, CN, F, Cl, Br, I, NO2, NH2, C(O)NH2, CO2H, or CO2R′; R3 is H; R4 is m-pyridyl optionally substituted with F, Cl, Br, or I; and X is CH2.
- 24. The composition of claim 21, wherein R1 is H and R2 is phenyl p-substituted with CN, F, or Cl.
- 25. The composition of claim 21, wherein R1 is OH and R2 is phenyl p-substituted with F.
- 26. The composition of claim 22, wherein R1 is H; R2 is phenyl or phenyl p-substituted with CN; and R4 is pyridyl.
- 27. The composition of claim 23, wherein R1 is H; R2 is phenyl p-substituted with CN, F, Cl, NO2, NH2, or C(O)NH2; and R4 is pyridyl.
- 28. A method for treating an inflammatory disorder, comprising administering to a subject in need thereof an effective amount of the compound of the formula:
- 29. The method of claim 28, wherein
R1 is H, OH, F, or Cl; R2 is phenyl optionally p-substituted with lower alkoxy, OH, CN, F, Cl, Br, I, NO2, NH2, C(O)NH2, CO2H, or CO2R′; R3 is H; R4 is N-oxy p-pyridyl or p-pyridyl optionally substituted with F, Cl, Br, or I; and X is CH2.
- 30. The method of claim 28, wherein
R1 is H, OH, F, or Cl; R2 is phenyl optionally p-substituted with lower alkoxy, OH, CN, F, Cl, Br, I, NO2, NH2, C(O)NH2, CO2H, or CO2R′; R3 is H; R4 is o-pyridyl optionally substituted with F, Cl, Br, or I; and X is CH2.
- 31. The method of claim 28, wherein
R1 is H, OH, or Cl; R2 is phenyl optionally p-substituted with lower alkoxy, OH, CN, F, Cl, Br, I, NO2, NH2, C(O)NH2, CO2H, or CO2R′; R3 is H; R4 is m-pyridyl optionally substituted with F, Cl, Br, or I; and X is CH2.
- 32. The method of claim 29, wherein R is —H and R2 is phenyl p-substituted with CN, F, or Cl.
- 33. The method of claim 29, wherein R is OH and R2 is phenyl p-substituted with F.
- 34. The method of claim 30, wherein R1 is H; R2 is phenyl or phenyl p-substituted with CN; and R4 is pyridyl.
- 35. The method of claim 31, wherein R1 is —H; R2 is phenyl p-substituted with CN, F, Cl, NO2, NH2, or C(O)NH2; and R4 is pyridyl.
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This application claims the benefit of U.S. Utility application Ser. No. 10/244,088, filed Aug. 27, 2002, which, in turn, claims the benefit of U.S. Provisional Application Serial No. 60/322,020, filed Sep. 13, 2001.