Claims
- 1. A composition comprising a compound of Formula (I):
- 2. A composition comprising a compound of Formula (I):
- 3. The composition of claim 2 wherein R1 is a substituent independently selected from the group consisting of hydrogen; hydroxy; halogen; and C1-8alkanyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy.
- 4. The composition of claim 2 wherein R1 is a substituent independently selected from the group consisting of hydrogen; hydroxy; halogen; and C1-8alkanyl.
- 5. The composition of claim 2 wherein R1 is a substituent independently selected from the group consisting of hydrogen; hydroxy; methyl; and chloro.
- 6. The composition of claim 2 wherein R2 is a substituent independently selected from the group consisting of hydrogen; hydroxy; halogen; and C1-8alkanyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy.
- 7. The composition of claim 2 wherein R2 is hydrogen or halogen.
- 8. The composition of claim 2 wherein R2 is hydrogen or chloro.
- 9. The composition of claim 2 wherein R3 is independently selected from the group consisting of hydrogen; hydroxy; fluoro; and chloro.
- 10. The composition of claim 2 wherein R3 is hydrogen.
- 11. The composition of claim 2 wherein L is C1-4alkandiyl optionally substituted with a substituent selected from the group consisting of C1-8alkanyl, C3-8cycloalkanyl and phenyl.
- 12. The composition of claim 2 wherein L is C1-4alkandiyl optionally substituted with a substituent selected from the group consisting of C3-8cycloalkanyl and phenyl.
- 13. The composition of claim 2 wherein L is —CH2— and —CH2CH2— optionally substituted with a substituent selected from the group consisting of C3-8cycloalkanyl and phenyl.
- 14. The composition of claim 2 wherein L is —CH2.
- 15. The composition of claim 2 wherein R4 is hydrogen.
- 16. The composition of claim 2 wherein R5 is hydrogen.
- 17. The composition of claim 2 wherein R6 is selected from the group consisting of phenyl substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, chloro, fluoro, C1-8alkanyloxy, fluorinated alkanyl, and fluorinated alkanyloxy; naphthyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, chloro, fluoro, C1-8alkanyloxy, fluorinated alkanyl, and fluorinated alkanyloxy; and thienyl optionally substituted with one to two substituents selected from the group consisting of C1-8alkanyl, chloro, fluoro, C1-8alkanyloxy, fluorinated alkanyl, and fluorinated alkanyloxy.
- 18. The composition of claim 2 wherein R6 is phenyl substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, chloro, fluoro, C1-8alkanyloxy, fluorinated alkanyl, and fluorinated alkanyloxy.
- 19. The composition of claim 2 wherein R6 is phenyl substituted with one to three substituents independently selected from the group consisting of t-butyl, chloro, fluoro, methoxy, trifluoromethyl, and trifluoromethoxy.
- 20. The composition of claim 2 wherein Z is O.
- 21. A compound of Formula (II):
- 22. The composition of claim 21 wherein R1 is a substituent independently selected from the group consisting of hydrogen; hydroxy; halogen; and C1-8alkanyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy.
- 23. The composition of claim 21 wherein R1 is a substituent independently selected from the group consisting of hydrogen; hydroxy; halogen; and C1-8alkanyl.
- 24. The composition of claim 21 wherein R1 is a substituent independently selected from the group consisting of hydrogen; hydroxy; methyl; and chloro.
- 25. The composition of claim 21 wherein R2 is a substituent independently selected from the group consisting of hydrogen; hydroxy; halogen; and C1-8alkanyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy.
- 26. The composition of claim 21 wherein R2 is hydrogen or halogen.
- 27. The composition of claim 21 wherein R2 is hydrogen or chloro.
- 28. The composition of claim 21 wherein L is C1-4alkandiyl optionally substituted with a substituent selected from the group consisting of C1-8alkanyl, C3-8cycloalkanyl and phenyl.
- 29. The composition of claim 21 wherein L is C1-4alkandiyl optionally substituted with a substituent selected from the group consisting of C3-8cycloalkanyl and phenyl.
- 30. The composition of claim 21 wherein L is —CH2— and —CH2CH2— optionally substituted with a substituent selected from the group consisting of C3-8cycloalkanyl and phenyl.
- 31. The composition of claim 21 wherein L is —CH2—.
- 32. The composition of claim 21 wherein R4 is hydrogen.
- 33. The composition of claim 21 wherein R5 is hydrogen.
- 34. The composition of claim 21 wherein R6 is selected from the group consisting of phenyl substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, chloro, fluoro, C1-8alkanyloxy, fluorinated alkanyl, and fluorinated alkanyloxy; naphthyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, chloro, fluoro, C1-8alkanyloxy, fluorinated alkanyl, and fluorinated alkanyloxy; and thienyl optionally substituted with one to two substituents selected from the group consisting of C1-8alkanyl, chloro, fluoro, C1-8alkanyloxy, fluorinated alkanyl, and fluorinated alkanyloxy.
- 35. The composition of claim 21 wherein R6 is phenyl substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, chloro, fluoro, C1-8alkanyloxy, fluorinated alkanyl, and fluorinated alkanyloxy.
- 36. The composition of claim 21 wherein R6 is phenyl substituted with one to three substituents independently selected from the group consisting of t-butyl, chloro, fluoro, methoxy, trifluoromethyl, and trifluoromethoxy.
- 37. The composition of claim 21 wherein Z is O.
- 38. A compound of Formula (III):
- 39. The composition of claim 38 wherein R1 is a substituent independently selected from the group consisting of hydrogen; hydroxy; halogen; and C1-8alkanyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy.
- 40. The composition of claim 38 wherein R1 is a substituent independently selected from the group consisting of hydrogen; hydroxy; halogen; and C1-8alkanyl.
- 41. The composition of claim 38 wherein R1 is a substituent independently selected from the group consisting of hydrogen; hydroxy; methyl; and chloro.
- 42. The composition of claim 38 wherein R2 is a substituent independently selected from the group consisting of hydrogen; hydroxy; halogen; and C1-8alkanyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy.
- 43. The composition of claim 38 wherein R2 is hydrogen or halogen.
- 44. The composition of claim 38 wherein R2 is hydrogen or chloro.
- 45. The composition of claim 38 wherein L is C1-4alkandiyl optionally substituted with a substituent selected from the group consisting of C1-8alkanyl, C3-8cycloalkanyl and phenyl.
- 46. The composition of claim 38 wherein L is C1-4alkandiyl, optionally substituted with a substituent selected from the group consisting of C3-8cycloalkanyl and phenyl.
- 47. The composition of claim 38 wherein L is —CH2— and —CH2CH2— optionally substituted with a substituent selected from the group consisting of C3-8cycloalkanyl and phenyl.
- 48. The composition of claim 38 wherein L is —CH2—.
- 49. The composition of claim 38 wherein R4 is hydrogen.
- 50. The composition of claim 38 wherein R5 is hydrogen.
- 51. The composition of claim 38 wherein R6 is selected from the group consisting of phenyl substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, chloro, fluoro, C1-8alkanyloxy, fluorinated alkanyl, and fluorinated alkanyloxy; naphthyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, chloro, fluoro, C1-8alkanyloxy, fluorinated alkanyl, and fluorinated alkanyloxy; and thienyl optionally substituted with one to two substituents selected from the group consisting of C1-8alkanyl, chloro, fluoro, C1-8alkanyloxy, fluorinated alkanyl, and fluorinated alkanyloxy.
- 52. The composition of claim 38 wherein R6 is phenyl substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, chloro, fluoro, C1-8alkanyloxy, fluorinated alkanyl, and fluorinated alkanyloxy.
- 53. The composition of claim 38 wherein R6 is phenyl substituted with one to three substituents independently selected from the group consisting of t-butyl, chloro, fluoro, methoxy, trifluoromethyl, and trifluoromethoxy.
- 54. The composition of claim 38 wherein Z is O.
- 55. A composition comprising a compound of Formula (IV):
- 56. The composition of claim 55 wherein R1 is a substituent independently selected from the group consisting of hydrogen; hydroxy; halogen; and C1-8alkanyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy.
- 57. The composition of claim 55 wherein R1 is a substituent independently selected from the group consisting of hydrogen; hydroxy; halogen; and C1-8alkanyl.
- 58. The composition of claim 55 wherein R1 is a substituent independently selected from the group consisting of hydrogen; hydroxy; methyl; and chloro.
- 59. The composition of claim 55 wherein R2 is a substituent independently selected from the group consisting of hydrogen; hydroxy; halogen; and C1-8alkanyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C1-8alkanyloxy.
- 60. The composition of claim 55 wherein R2 is hydrogen or halogen.
- 61. The composition of claim 55 wherein R2 is hydrogen or chloro.
- 62. The composition of claim 55 wherein L is C1-4alkandiyl optionally substituted with a substituent selected from the group consisting of C1-8alkanyl, C3-8cycloalkanyl and phenyl.
- 63. The composition of claim 55 wherein L is C1-4alkandiyl optionally substituted with a substituent selected from the group consisting of C3-8cycloalkanyl and phenyl.
- 64. The composition of claim 55 wherein L is —CH2— and —CH2CH2— optionally substituted with a substituent selected from the group consisting of C3-8cycloalkanyl and phenyl.
- 65. The composition of claim 55 wherein L is —CH2—.
- 66. The composition of claim 55 wherein R4 is hydrogen.
- 67. The composition of claim 55 wherein R5 is hydrogen.
- 68. The composition of claim 55 wherein R6 is selected from the group consisting of phenyl substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, chloro, fluoro, C1-8alkanyloxy, fluorinated alkanyl, and fluorinated alkanyloxy; naphthyl optionally substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, chloro, fluoro, C1-8alkanyloxy, fluorinated alkanyl, and fluorinated alkanyloxy; and thienyl optionally substituted with one to two substituents selected from the group consisting of C1-8alkanyl, chloro, fluoro, C1-8alkanyloxy, fluorinated alkanyl, and fluorinated alkanyloxy.
- 69. The composition of claim 55 wherein R6 is phenyl substituted with one to three substituents independently selected from the group consisting of C1-8alkanyl, chloro, fluoro, C1-8alkanyloxy, fluorinated alkanyl, and fluorinated alkanyloxy.
- 70. The composition of claim 55 wherein R6 is phenyl substituted with one to three substituents independently selected from the group consisting of t-butyl, chloro, fluoro, methoxy, trifluoromethyl, and trifluoromethoxy.
- 71. The composition of claim 55 wherein Z is O.
- 72. The composition of claim 2 wherein R3 is independently selected from the group consisting of hydrogen; hydroxy; fluoro; and chloro.
- 73. The composition of claim 2 wherein R3 is hydrogen.
- 74. A composition comprising a compound of Formula (V):
- 75. The composition according to claim 74 wherein X is N, R1 is hydroxy, and R3 is hydrogen.
- 76. The composition according to claim 74 wherein X is N, R1 is hydroxy; R2, R3, R4, and R5 are hydrogen; R6 is 3,4-di-substituted phenyl, and Z is O.
- 77. The composition according to claim 74 wherein X is N, R1 is hydroxy, R2, R3, R4, and R5 are hydrogen; R6 is 3-trifluoromethyl-4-chlorophenyl, and Z is O.
- 78. A composition comprising a compound of Formula (Ia):
- 79. A composition according to claim 78 wherein the compound is selected from the group consisting of:
a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-CF3)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-OCF3)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-t-Bu)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3-CF3)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3-CF3-4-Cl)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2CH2—, R6 is (3,4-diCl)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3,4-diCl)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (2,4-diCl)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-Cl)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3,5-diCF3)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3,4-diF)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (6-CF3)Pyridin-3-yl, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2CH2—, R6 is Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-t-Bu)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3-CF3-4-Cl)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-OCF3)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2CH2—, R6 is (4-t-Bu)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2CH(—CH2cyclohexyl)-, R6 is (4-OMe)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2CH(—CH2Ph)-, R6 is (4-OMe)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2CH2—, R6 is (4-OCF3)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-CF3)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is C1, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-CF3)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3,4-diCl)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2CH2—, R6 is (3,4-diCl)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is Me, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3,4-diCl)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2CH2—, R6 is (4-CF3)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3-CF3)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-Cl)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is Me, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3-CF3)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2CH2—, R6 is (3-CF3)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2CH2—, R6 is (4-Cl)Ph, X is N, and Y is C; and a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-OMe)Ph, X is N, and Y is C.
- 80. A composition according to claim 78 wherein the compound is selected from the group consisting of:
a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-CF3)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-OCF3)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-t-Bu)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3-CF3)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3-CF3-4-Cl)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2CH2—, R6 is (3,4-diCl)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3,4-diCl)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (2,4-diCl)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-Cl)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3,5-diCF3)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3,4-diF)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-t-Bu)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3-CF3-4-Cl)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-OCF3)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2CH2—, R6 is (4-t-Bu)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2CH(—CH2cyclohexyl)-, R6 is (4-OMe)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H; R3 is H, R4 is H, R5 is H, L is —CH2CH(—CH2Ph)-, R6 is (4-OMe)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2CH2—, R6 is (4-OCF3)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-CF3)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is C1, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-CF3)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3,4-diCl)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2CH2—, R6 is (3,4-diCl)Ph, X is N, and Y is C; and a compound of formula (Ia) wherein R1 is Me, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3,4-diCl)Ph, X is N, and Y is C.
- 81. A composition according to claim 78 wherein the compound is selected from the group consisting of:
a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-CF3)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-OCF3)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-t-Bu)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3-CF3)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3-CF3-4-Cl)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is OH, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2CH2—, R6 is (3,4-diCl)Ph, X is C, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-t-Bu)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (3-CF3-4-Cl)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is Me, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-CF3)Ph, X is N, and Y is C; a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2—, R6 is (4-OCF3)Ph, X is N, and Y is C; and a compound of formula (Ia) wherein R1 is H, R2 is H, R3 is H, R4 is H, R5 is H, L is —CH2CH2—, R6 is (4-t-Bu)Ph, X is N, and Y is C.
- 82. A composition comprising a compound of Formula (II):
- 83. A pharmaceutical composition comprising a compound, salt or solvate according to claim 2 admixed with a pharmaceutically acceptable carrier, excipient or diluent.
- 84. A veterinary composition comprising a compound, salt or solvate according to claim 2 admixed with a veterinarily acceptable carrier, excipient or dilluent.
- 85. A method of treating or preventing a disease or condition in a mammal which disease or condition is affected by the modulation of one or more vanilloid receptors, which method comprises administering to a mammal in need of such treatment or prevention a therapeutically effective amount of a compound, salt or solvate of claim 2.
- 86. A method for preventing or treating a chronic-pain causing disease or condition, an acute-pain causing disease or condition, or a pulmonary dysfunction comprising the step of administering to a mammal in need of such treatment a therapeutically effective amount of a compound, salt or solvate of claim 2.
- 87. A method for preventing or treating a disease or condition, wherein said disease or condition causes inflammatory pain, burning pain, itch urinary incontinence, or chronic obstructive pulmonary disease, said method comprising the step of administering to a mammal in need of such treatment a therapeutically effective amount of a compound, salt or solvate of claim 2.
- 88. A method for preventing or treating a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough, asthma, chronic obstructive pulmonary disease, rhinitis, contact dermatitis/hypersensitivity, itch, eczema, anxiety, panic disorders, pharyngitis, mucositis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, irritable bowel syndrome, inflammatory bowel diseases such as Crohn's Disease and ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstruation, hot flash, cancer, and trauma, said method comprising the step of administering to a mammal in need of such treatment a therapeutically effective amount of a compound, salt or solvate of claim 2.
- 89. The method of claim 88 wherein said therapeutically effective amount comprises a dose range of from about 0.001 mg to about 1,000 mg.
- 90. The method of claim 88 wherein said therapeutically effective amount comprises a dose range of from about 0.1 mg to about 500 mg.
- 91. The method of claim 88 wherein said therapeutically effective amount comprises a dose range of from about 1 mg to about 250 mg.
- 92. A kit comprising in one or more containers an amount of the composition of claim 2 effective to treat or prevent a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough, asthma, chronic obstructive pulmonary disease, rhinitis, contact dermatitis/hypersensitivity, itch, eczema, anxiety, panic disorders, pharyngitis, mucositis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, irritable bowel syndrome, inflammatory bowel diseases such as Crohn's Disease and ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstruation, hot flash, cancer, and trauma.
- 93. A pharmaceutical composition comprising a compound, salt or solvate according to claim 21 admixed with a pharmaceutically acceptable carrier, excipient or diluent.
- 94. A veterinary composition comprising a compound, salt or solvate according to claim 21 admixed with a veterinarily acceptable carrier, excipient or dilluent.
- 95. A method for preventing or treating a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough, asthma, chronic obstructive pulmonary disease, rhinitis, contact dermatitis/hypersensitivity, itch, eczema, anxiety, panic disorders, pharyngitis, mucositis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, irritable bowel syndrome, inflammatory bowel diseases such as Crohn's Disease and ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstruation, hot flash, cancer, and trauma, said method comprising the step of administering to a mammal in need of such treatment a therapeutically effective amount of a compound, salt or solvate of claim 21.
- 96. The method of claim 95 wherein said therapeutically effective amount comprises a dose range of from about 0.001 mg to about 1,000 mg.
- 97. The method of claim 95 wherein said therapeutically effective amount comprises a dose range of from about 0.1 mg to about 500 mg.
- 98. The method of claim 95 wherein said therapeutically effective amount comprises a dose range of from about 1 mg to about 250 mg.
- 99. A kit comprising in one or more containers an amount of the composition of claim 21 effective to treat or prevent a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough, asthma, chronic obstructive pulmonary disease, rhinitis, contact dermatitis/hypersensitivity, itch, eczema, anxiety, panic disorders, pharyngitis, mucositis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, irritable bowel syndrome, inflammatory bowel diseases such as Crohn's Disease and ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstruation, hot flash, cancer, and trauma.
- 100. A pharmaceutical composition comprising a compound, salt or solvate according to claim 38 admixed with a pharmaceutically acceptable carrier, excipient or diluent.
- 101. A veterinary composition comprising a compound, salt or solvate according to claim 38 admixed with a veterinarily acceptable carrier, excipient or dilluent.
- 102. A method for preventing or treating a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough, asthma, chronic obstructive pulmonary disease, rhinitis, contact dermatitis/hypersensitivity, itch, eczema, anxiety, panic disorders, pharyngitis, mucositis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, irritable bowel syndrome, inflammatory bowel diseases such as Crohn's Disease and ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstruation, hot flash, cancer, and trauma, said method comprising the step of administering to a mammal in need of such treatment a therapeutically effective amount of a compound, salt or solvate of claim 38.
- 103. The method of claim 102 wherein said therapeutically effective amount comprises a dose range of from about 0.001 mg to about 1,000 mg.
- 104. The method of claim 102 wherein said therapeutically effective amount comprises a dose range of from about 0.1 mg to about 500 mg.
- 105. The method of claim 102 wherein said therapeutically effective amount comprises a dose range of from about 1 mg to about 250 mg.
- 106. A kit comprising in one or more containers an amount of the composition of claim 38 effective to treat or prevent a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough, asthma, chronic obstructive pulmonary disease, rhinitis, contact dermatitis/hypersensitivity, itch, eczema, anxiety, panic disorders, pharyngitis, mucositis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, irritable bowel syndrome, inflammatory bowel diseases such as Crohn's Disease and ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstruation, hot flash, cancer, and trauma.
- 107. A pharmaceutical composition comprising a compound, salt or solvate according to claim 55 admixed with a pharmaceutically acceptable carrier, excipient or diluent.
- 108. A veterinary composition comprising a compound, salt or solvate according to claim 55 admixed with a veterinarily acceptable carrier, excipient or dilluent.
- 109. A method for preventing or treating a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough, asthma, chronic obstructive pulmonary disease, rhinitis, contact dermatitis/hypersensitivity, itch, eczema, anxiety, panic disorders, pharyngitis, mucositis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, irritable bowel syndrome, inflammatory bowel diseases such as Crohn's Disease and ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstruation, hot flash, cancer, and trauma, said method comprising the step of administering to a mammal in need of such treatment a therapeutically effective amount of a compound, salt or solvate of claim 55.
- 110. The method of claim 109 wherein said therapeutically effective amount comprises a dose range of from about 0.001 mg to about 1,000 mg.
- 111. The method of claim 109 wherein said therapeutically effective amount comprises a dose range of from about 0.1 mg to about 500 mg.
- 112. The method of claim 109 wherein said therapeutically effective amount comprises a dose range of from about 1 mg to about 250 mg.
- 113. A kit comprising in one or more containers an amount of the composition of claim 55 effective to treat or prevent a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough, asthma, chronic obstructive pulmonary disease, rhinitis, contact dermatitis/hypersensitivity, itch, eczema, anxiety, panic disorders, pharyngitis, mucositis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, irritable bowel syndrome, inflammatory bowel diseases such as Crohn's Disease and ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstruation, hot flash, cancer, and trauma.
- 114. A pharmaceutical composition comprising a compound, salt or solvate according to claim 74 admixed with a pharmaceutically acceptable carrier, excipient or diluent.
- 115. A veterinary composition comprising a compound, salt or solvate according to claim 74 admixed with a veterinarily acceptable carrier, excipient or dilluent.
- 116. A method for preventing or treating a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough, asthma, chronic obstructive pulmonary disease, rhinitis, contact dermatitis/hypersensitivity, itch, eczema, anxiety, panic disorders, pharyngitis, mucositis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, irritable bowel syndrome, inflammatory bowel diseases such as Crohn's Disease and ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia; Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstruation, hot flash, cancer, and trauma, said method comprising the step of administering to a mammal in need of such treatment a therapeutically effective amount of a compound, salt or solvate of claim 74.
- 117. The method of claim 116 wherein said therapeutically effective amount comprises a dose range of from about 0.001 mg to about 1,000 mg.
- 118. The method of claim 116 wherein said therapeutically effective amount comprises a dose range of from about 0.1 mg to about 500 mg.
- 119. The method of claim 116 wherein said therapeutically effective amount comprises a dose range of from about 1 mg to about 250 mg.
- 120. A kit comprising in one or more containers an amount of the composition of claim 74 effective to treat or prevent a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough, asthma, chronic obstructive pulmonary disease, rhinitis, contact dermatitis/hypersensitivity, itch, eczema, anxiety, panic disorders, pharyngitis, mucositis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, irritable bowel syndrome, inflammatory bowel diseases such as Crohn's Disease and ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstruation, hot flash, cancer, and trauma.
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application claims priority to U.S. Provisional Patent Application Nos. 60/395,728 and 60/395,951, filed Jul. 12, 2002 and Jul. 15, 2002, respectively, which are hereby incorporated by reference in their entirety.
Provisional Applications (1)
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Number |
Date |
Country |
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60395728 |
Jul 2002 |
US |