Heterocyclic analgesic compounds and methods of use thereof
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Abstract
One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.
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Citations
204 Claims
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1. A compound represented by A:
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204)
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2. The compound of claim 1, wherein X is C(R3)2, O, NR2, or C═
- O.
-
3. The compound of claim 1, wherein X is C(R3)2, O, or NR2.
-
4. The compound of claim 1, wherein X is C(R3)2.
-
5. The compound of claim 1, wherein m is 2 or 3.
-
6. The compound of claim 1, wherein n is 1.
-
7. The compound of claim 1, wherein y is 1.
-
8. The compound of claim 1, wherein R1 represents aryl or heteroaryl.
-
9. The compound of claim 1, wherein R2 represents independently for each occurrence alkyl.
-
10. The compound of claim 1, wherein R3 represents independently for each occurrence H or alkyl.
-
11. The compound of claim 1, wherein R4 represents cycloalkyl, aryl, or heteroaryl.
-
12. The compound of claim 1, wherein R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
-
13. The compound of claim 1, wherein R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
-
14. The compound of claim 1, wherein X is C(R3)2, O, NR2, or C═
- O; and
n is 1.
- O; and
-
15. The compound of claim 1, wherein X is C(R3)2, O, or NR2;
- and n is 1.
-
16. The compound of claim 1, wherein X is C(R3)2;
- and n is 1.
-
17. The compound of claim 1, wherein X is C(R3)2, O, NR2, or C═
- O; and
y is 1.
- O; and
-
18. The compound of claim 1, wherein X is C(R3)2, O, or NR2;
- and y is 1.
-
19. The compound of claim 1, wherein X is C(R3)2;
- and y is 1.
-
20. The compound of claim 1, wherein X is C(R3)2, O, NR2, or C═
- O; and
R1 represents aryl or heteroaryl.
- O; and
-
21. The compound of claim 1, wherein X is C(R3)2, O, or NR2;
- and R1 represents aryl or heteroaryl.
-
22. The compound of claim 1, wherein X is C(R3)2;
- and R1 represents aryl or heteroaryl.
-
23. The compound of claim 1, wherein X is C(R3)2, O, NR2, or C═
- O; and
R2 represents independently for each occurrence alkyl.
- O; and
-
24. The compound of claim 1, wherein X is C(R3)2, O, or NR2;
- and R2 represents independently for each occurrence alkyl.
-
25. The compound of claim 1, wherein X is C(R3)2;
- and R2 represents independently for each occurrence alkyl.
-
26. The compound of claim 1, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1; and
R1 represents aryl or heteroaryl.
- O;
-
27. The compound of claim 1, wherein X is C(R3)2, O, or NR2;
- n is 1; and
R1 represents aryl or heteroaryl.
- n is 1; and
-
28. The compound of claim 1, wherein X is C(R3)2;
- n is 1; and
R1 represents aryl or heteroaryl.
- n is 1; and
-
29. The compound of claim 1, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1;
R1 represents aryl or heteroaryl; and
R2 represents independently for each occurrence alkyl.
- O;
-
30. The compound of claim 1, wherein X is C(R3)2, O, or NR2;
- n is 1;
R1 represents aryl or heteroaryl; and
R2 represents independently for each occurrence alkyl.
- n is 1;
-
31. The compound of claim 1, wherein X is C(R3)2;
- n is 1;
R1 represents aryl or heteroaryl; and
R2 represents independently for each occurrence alkyl.
- n is 1;
-
32. The compound of claim 1, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl; and
R3 represents independently for each occurrence H or alkyl.
- O;
-
33. The compound of claim 1, wherein X is C(R3)2, O, or NR2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl; and
R3 represents independently for each occurrence H or alkyl.
- n is 1;
-
34. The compound of claim 1, wherein X is C(R3)2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl; and
R3 represents independently for each occurrence H or alkyl.
- n is 1;
-
35. The compound of claim 1, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl; and
R4 represents cycloalkyl, aryl, or heteroaryl.
- O;
-
36. The compound of claim 1, wherein X is C(R3)2, O, or NR2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl; and
R4 represents cycloalkyl, aryl, or heteroaryl.
- n is 1;
-
37. The compound of claim 1, wherein X is C(R3)2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl; and
R4 represents cycloalkyl, aryl, or heteroaryl.
- n is 1;
-
38. The compound of claim 1, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl; and
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- O;
-
39. The compound of claim 1, wherein X is C(R3)2, O, or NR2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl; and
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- n is 1;
-
40. The compound of claim 1, wherein X is C(R3)2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl; and
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- n is 1;
-
41. The compound of claim 1, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl;
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F; and
R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- O;
-
42. The compound of claim 1, wherein X is C(R3)2, O, or NR2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl;
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F; and
R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- n is 1;
-
43. The compound of claim 1, wherein X is C(R3)2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl;
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F; and
R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- n is 1;
-
44. The compound of claim 1, wherein X is C(R3)2;
- m is 2;
n is 1;
R1 represents aryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H;
R4 represents aryl;
R5 represents independently for each occurrence H or alkyl; and
R6 represents independently for each occurrence H or alkyl.
- m is 2;
-
187. The compound of claim 1, 84, 112, or 151, wherein said compound is a single stereoisomer.
-
188. A formulation, comprising a compound of claim 1, 45, 84, 98, 112, or 151;
- and a pharmaceutically acceptable excipient.
-
189. The compound of claim 1, 45, 84, 98, 112, or 151, wherein said compound is a ligand for a cellular receptor.
-
190. The compound of claim 189, wherein said compound is a ligand for a G-protein-coupled receptor.
-
191. The compound of claim 189, wherein said compound is a ligand for an opioid receptor.
-
192. The compound of claim 190, wherein said compound is an agonist of a G-protein-coupled receptor.
-
193. The compound of claim 190, wherein said compound is an antagonist of a G-protein-coupled receptor.
-
194. The compound of claim 191, wherein said compound is an agonist of an opioid receptor.
-
195. The compound of claim 191, wherein said compound is an antagonist of an opioid receptor.
-
196. The compound of claim 190, wherein said compound is a ligand which is selective for a subclass of G-protein-coupled receptor.
-
197. The compound of claim 191, wherein said compound is a ligand which is selective for a subclass of opioid receptor.
-
198. A method of treating pain, drug addiction, or tinnitus in a mammal, comprising the step of:
administering to a mammal with pain, drug addiction, or tinnitus an effective amount of a formulation of claim 188.
-
199. The method of claim 198, wherein said mammal is a primate, equine, canine or feline.
-
200. The method claim 198, wherein said mammal is a human.
-
201. The method of claim 198, wherein said formulation is administered orally.
-
202. The method of claim 198, wherein said formulation is administered intravenously.
-
203. The method of claim 198, wherein said formulation is administered sublingually.
-
204. The method of claim 198, wherein said formulation is administered ocularly.
-
2. The compound of claim 1, wherein X is C(R3)2, O, NR2, or C═
-
45. A compound represented by B:
- View Dependent Claims (46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83)
-
46. The compound of claim 45, wherein X is C(R3)2, O, NR2, or C═
- O.
-
47. The compound of claim 45, wherein X is C(R3)2, O, or NR2.
-
48. The compound of claim 45, wherein X is C(R3)2.
-
49. The compound of claim 45, wherein m is 2 or 3.
-
50. The compound of claim 45, wherein n is 1.
-
51. The compound of claim 45, wherein R1 represents aryl or heteroaryl.
-
52. The compound of claim 45, wherein R2 represents independently for each occurrence alkyl.
-
53. The compound of claim 45, wherein R3 represents independently for each occurrence H or alkyl.
-
54. The compound of claim 45, wherein R4 represents cycloalkyl, aryl, or heteroaryl.
-
55. The compound of claim 45, wherein R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
-
56. The compound of claim 45, wherein R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
-
57. The compound of claim 45, wherein X is C(R3)2, O, NR2, or C═
- O; and
n is 1.
- O; and
-
58. The compound of claim 45, wherein X is C(R3)2, O, or NR2;
- and n is 1.
-
59. The compound of claim 45, wherein X is C(R3)2;
- and n is 1.
-
60. The compound of claim 45, wherein X is C(R3)2, O, NR2, or C═
- O; and
R1 represents aryl or heteroaryl.
- O; and
-
61. The compound of claim 45, wherein X is C(R3)2, O, or NR2;
- and R1 represents aryl or heteroaryl.
-
62. The compound of claim 45, wherein X is C(R3)2;
- and R1 represents aryl or heteroaryl.
-
63. The compound of claim 45, wherein X is C(R3)2, O, NR2, or C═
- O; and
R2 represents independently for each occurrence alkyl.
- O; and
-
64. The compound of claim 45, wherein X is C(R3)2, O, or NR2;
- and R2 represents independently for each occurrence alkyl.
-
65. The compound of claim 45, wherein X is C(R3)2;
- and R2 represents independently for each occurrence alkyl.
-
66. The compound of claim 45, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1; and
R1 represents aryl or heteroaryl.
- O;
-
67. The compound of claim 45, wherein X is C(R3)2, O, or NR2;
- n is 1; and
R1 represents aryl or heteroaryl.
- n is 1; and
-
68. The compound of claim 45, wherein X is C(R3)2;
- n is 1; and
R1 represents aryl or heteroaryl.
- n is 1; and
-
69. The compound of claim 45, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1;
R1 represents aryl or heteroaryl; and
R2 represents independently for each occurrence alkyl.
- O;
-
70. The compound of claim 45, wherein X is C(R3)2, O, or NR2;
- n is 1;
R1 represents aryl or heteroaryl; and
R2 represents independently for each occurrence alkyl.
- n is 1;
-
71. The compound of claim 45, wherein X is C(R3)2;
- n is 1;
R1 represents aryl or heteroaryl; and
R2 represents independently for each occurrence alkyl.
- n is 1;
-
72. The compound of claim 45, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl; and
R3 represents independently for each occurrence H or alkyl.
- O;
-
73. The compound of claim 45, wherein X is C(R3)2, O, or NR2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl; and
R3 represents independently for each occurrence H or alkyl.
- n is 1;
-
74. The compound of claim 45, wherein X is C(R3)2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl; and
R3 represents independently for each occurrence H or alkyl.
- n is 1;
-
75. The compound of claim 45, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl; and
R4 represents cycloalkyl, aryl, or heteroaryl.
- O;
-
76. The compound of claim 45, wherein X is C(R3)2, O, or NR2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl; and
R4 represents cycloalkyl, aryl, or heteroaryl.
- n is 1;
-
77. The compound of claim 45, wherein X is C(R3)2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl; and
R4 represents cycloalkyl, aryl, or heteroaryl.
- n is 1;
-
78. The compound of claim 45, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl; and
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- O;
-
79. The compound of claim 45, wherein X is C(R3)2, O, or NR2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl; and
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- n is 1;
-
80. The compound of claim 45, wherein X is C(R3)2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl; and
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- n is 1;
-
81. The compound of claim 45, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl;
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F; and
R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- O;
-
82. The compound of claim 45, wherein X is C(R3)2, O, or NR2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl;
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F; and
R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- n is 1;
-
83. The compound of claim 45, wherein X is C(R3)2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl;
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F; and
R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- n is 1;
-
46. The compound of claim 45, wherein X is C(R3)2, O, NR2, or C═
-
84. A compound represented by C:
- View Dependent Claims (85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97)
-
85. The compound of claim 84, wherein m is 2 or 3.
-
86. The compound of claim 84, wherein y is 1.
-
87. The compound of claim 84, wherein R1 represents aryl or heteroaryl.
-
88. The compound of claim 84, wherein R2 represents independently for each occurrence alkyl.
-
89. The compound of claim 84, wherein R3 represents independently for each occurrence H or alkyl.
-
90. The compound of claim 84, wherein R4 represents cycloalkyl, aryl, or heteroaryl.
-
91. The compound of claim 84, wherein R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
-
92. The compound of claim 84, wherein R1 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
-
93. The compound of claim 84, wherein R1 represents aryl or heteroaryl;
- and R2 represents independently for each occurrence alkyl.
-
94. The compound of claim 84, wherein R1 represents aryl or heteroaryl;
- R2 represents independently for each occurrence alkyl; and
R3 represents independently for each occurrence H or alkyl.
- R2 represents independently for each occurrence alkyl; and
-
95. The compound of claim 84, wherein R1 represents aryl or heteroaryl;
- R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl; and
R4 represents cycloalkyl, aryl, or heteroaryl.
- R2 represents independently for each occurrence alkyl;
-
96. The compound of claim 84, wherein R1 represents aryl or heteroaryl;
- R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl; and
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- R2 represents independently for each occurrence alkyl;
-
97. The compound of claim 84, wherein R1 represents aryl or heteroaryl;
- R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl;
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F; and
R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- R2 represents independently for each occurrence alkyl;
-
85. The compound of claim 84, wherein m is 2 or 3.
-
98. A compound represented by D:
- View Dependent Claims (99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111)
-
99. The compound of claim 98, wherein m is 2 or 3.
-
100. The compound of claim 98, wherein y is 1.
-
101. The compound of claim 98, wherein R1 represents aryl or heteroaryl.
-
102. The compound of claim 98, wherein R2 represents independently for each occurrence alkyl.
-
103. The compound of claim 98, wherein R3 represents independently for each occurrence H or alkyl.
-
104. The compound of claim 98, wherein R4 represents cycloalkyl, aryl, or heteroaryl.
-
105. The compound of claim 98, wherein R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
-
106. The compound of claim 98, wherein R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
-
107. The compound of claim 98, wherein R1 represents aryl or heteroaryl;
- and R2 represents independently for each occurrence alkyl.
-
108. The compound of claim 98, wherein R1 represents aryl or heteroaryl;
- R2 represents independently for each occurrence alkyl; and
R3 represents independently for each occurrence H or alkyl.
- R2 represents independently for each occurrence alkyl; and
-
109. The compound of claim 98, wherein R1 represents aryl or heteroaryl;
- R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl; and
R4 represents cycloalkyl, aryl, or heteroaryl.
- R2 represents independently for each occurrence alkyl;
-
110. The compound of claim 98, wherein R1 represents aryl or heteroaryl;
- R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl; and
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- R2 represents independently for each occurrence alkyl;
-
111. The compound of claim 98, wherein R1 represents aryl or heteroaryl;
- R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl;
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F; and
R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- R2 represents independently for each occurrence alkyl;
-
99. The compound of claim 98, wherein m is 2 or 3.
-
112. A compound represented by E:
- View Dependent Claims (113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150)
-
113. The compound of claim 112, wherein X is C(R3)2, O, NR2, or C═
- O.
-
114. The compound of claim 112, wherein X is C(R3)2, O, or NR2.
-
115. The compound of claim 112, wherein X is C(R3)2.
-
116. The compound of claim 112, wherein m is 2 or 3.
-
117. The compound of claim 112, wherein n is 1.
-
118. The compound of claim 112, wherein R1 represents aryl or heteroaryl.
-
119. The compound of claim 112, wherein R2 represents independently for each occurrence alkyl.
-
120. The compound of claim 112, wherein R3 represents independently for each occurrence H or alkyl.
-
121. The compound of claim 112, wherein R4 represents cycloalkyl, aryl, or heteroaryl.
-
122. The compound of claim 112, wherein R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
-
123. The compound of claim 112, wherein R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
-
124. The compound of claim 112, wherein X is C(R3)2, O, NR2, or C═
- O; and
n is 1.
- O; and
-
125. The compound of claim 112, wherein X is C(R3)2, O, or NR2;
- and n is 1.
-
126. The compound of claim 112, wherein X is C(R3)2;
- and n is 1.
-
127. The compound of claim 112, wherein X is C(R3)2, O, NR2, or C═
- O; and
R1 represents aryl or heteroaryl.
- O; and
-
128. The compound of claim 112, wherein X is C(R3)2, O, or NR2;
- and R1 represents aryl or heteroaryl.
-
129. The compound of claim 112, wherein X is C(R3)2;
- and R1 represents aryl or heteroaryl.
-
130. The compound of claim 112, wherein X is C(R3)2, O, NR2, or C═
- O; and
R2 represents independently for each occurrence alkyl.
- O; and
-
131. The compound of claim 112, wherein X is C(R3)2, O, or NR2;
- and R2 represents independently for each occurrence alkyl.
-
132. The compound of claim 112, wherein X is C(R3)2;
- and R2 represents independently for each occurrence alkyl.
-
133. The compound of claim 112, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1; and
R1 represents aryl or heteroaryl.
- O;
-
134. The compound of claim 112, wherein X is C(R3)2, O, or NR2;
- n is 1; and
R1 represents aryl or heteroaryl.
- n is 1; and
-
135. The compound of claim 112, wherein X is C(R3)2;
- n is 1; and
R1 represents aryl or heteroaryl.
- n is 1; and
-
136. The compound of claim 112, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1;
R1 represents aryl or heteroaryl; and
R2 represents independently for each occurrence alkyl.
- O;
-
137. The compound of claim 112, wherein X is C(R3)2, O, or NR2;
- n is 1;
R1 represents aryl or heteroaryl; and
R2 represents independently for each occurrence alkyl.
- n is 1;
-
138. The compound of claim 112, wherein X is C(R3)2;
- n is 1;
R1 represents aryl or heteroaryl; and
R2 represents independently for each occurrence alkyl.
- n is 1;
-
139. The compound of claim 112, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl; and
R3 represents independently for each occurrence H or alkyl.
- O;
-
140. The compound of claim 112, wherein X is C(R3)2, O, or NR2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl; and
R3 represents independently for each occurrence H or alkyl.
- n is 1;
-
141. The compound of claim 112, wherein X is C(R3)2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl; and
R3 represents independently for each occurrence H or alkyl.
- n is 1;
-
142. The compound of claim 112, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl; and
R4 represents cycloalkyl, aryl, or heteroaryl.
- O;
-
143. The compound of claim 112, wherein X is C(R3)2, or NR2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl; and
R4 represents cycloalkyl, aryl, or heteroaryl.
- n is 1;
-
144. The compound of claim 112, wherein X is C(R3)2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl; and
R4 represents cycloalkyl, aryl, or heteroaryl.
- n is 1;
-
145. The compound of claim 112, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl; and
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- O;
-
146. The compound of claim 112, wherein X is C(R3)2, O, or NR2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl; and
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- n is 1;
-
147. The compound of claim 112, wherein X is C(R3)2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl; and
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- n is 1;
-
148. The compound of claim 112, wherein X is C(R3)2, O, NR2, or C═
- O;
n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl;
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F; and
R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- O;
-
149. The compound of claim 112, wherein X is C(R3)2, O, or NR2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl;
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F; and
R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- n is 1;
-
150. The compound of claim 112, wherein X is C(R3)2;
- n is 1;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl;
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F; and
R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- n is 1;
-
113. The compound of claim 112, wherein X is C(R3)2, O, NR2, or C═
-
151. A compound represented by F:
- View Dependent Claims (152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186)
-
152. The compound of claim 151, wherein X is O, NR2, or C═
- O.
-
153. The compound of claim 151, wherein X is O or NR2.
-
154. The compound of claim 151, wherein X is NR2.
-
155. The compound of claim 151, wherein m is 2 or 3.
-
156. The compound of claim 151, wherein y is 1.
-
157. The compound of claim 151, wherein R1 represents aryl or heteroaryl.
-
158. The compound of claim 151, wherein R2 represents independently for each occurrence alkyl.
-
159. The compound of claim 151, wherein R3 represents independently for each occurrence H or alkyl.
-
160. The compound of claim 151, wherein R4 represents cycloalkyl, aryl, or heteroaryl.
-
161. The compound of claim 151, wherein R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
-
162. The compound of claim 151, wherein R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
-
163. The compound of claim 151, wherein X is O, NR2, or C═
- O; and
y is 1.
- O; and
-
164. The compound of claim 151, wherein X is O or NR2;
- and y is 1.
-
165. The compound of claim 151, wherein X is NR2;
- and y is 1.
-
166. The compound of claim 151, wherein X is O, NR2, or C═
- O; and
R1 represents aryl or heteroaryl.
- O; and
-
167. The compound of claim 151, wherein X is O or NR2;
- and R1 represents aryl or heteroaryl.
-
168. The compound of claim 151, wherein X is NR2;
- and R1 represents aryl or heteroaryl.
-
169. The compound of claim 151, wherein X is O, NR2, or C═
- O; and
R2 represents independently for each occurrence alkyl.
- O; and
-
170. The compound of claim 151, wherein X is O or NR2;
- and R2 represents independently for each occurrence alkyl.
-
171. The compound of claim 151, wherein X is NR2;
- and R2 represents independently for each occurrence alkyl.
-
172. The compound of claim 151, wherein X is O, NR2, or C═
- O;
R1 represents aryl or heteroaryl; and
R2 represents independently for each occurrence allyl.
- O;
-
173. The compound of claim 151, wherein X is O or NR2;
- R1 represents aryl or heteroaryl; and
R2 represents independently for each occurrence alkyl.
- R1 represents aryl or heteroaryl; and
-
174. The compound of claim 151, wherein X is NR2;
- R1 represents aryl or heteroaryl; and
R2 represents independently for each occurrence alkyl.
- R1 represents aryl or heteroaryl; and
-
175. The compound of claim 151, wherein X is O, NR2, or C═
- O;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl; and
R3 represents independently for each occurrence H or alkyl.
- O;
-
176. The compound of claim 151, wherein X is O or NR2;
- R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence allyl; and
R3 represents independently for each occurrence H or allyl.
- R1 represents aryl or heteroaryl;
-
177. The compound of claim 151, wherein X is NR2;
- R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence allyl; and
R3 represents independently for each occurrence H or alkyl.
- R1 represents aryl or heteroaryl;
-
178. The compound of claim 151, wherein X is O, NR2, or C═
- O;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl; and
R4 represents cycloalkyl, aryl, or heteroaryl.
- O;
-
179. The compound of claim 151, wherein X is O or NR2;
- R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl; and
R4 represents cycloalkyl, aryl, or heteroaryl.
- R1 represents aryl or heteroaryl;
-
180. The compound of claim 151, wherein X is NR2;
- R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl; and
R4 represents cycloalkyl, aryl, or heteroaryl.
- R1 represents aryl or heteroaryl;
-
181. The compound of claim 151, wherein X is O, NR2, or C═
- O;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl; and
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- O;
-
182. The compound of claim 151, wherein X is O or NR2;
- R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl; and
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- R1 represents aryl or heteroaryl;
-
183. The compound of claim 151, wherein X is NR2;
- R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl; and
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- R1 represents aryl or heteroaryl;
-
184. The compound of claim 151, wherein X is O, NR2, or C═
- O;
R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl;
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F; and
R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- O;
-
185. The compound of claim 151, wherein X is O or NR2;
- R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl;
R5 represents independently for each occurrence H, alkyl aryl, heteroaryl, or F; and
R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- R1 represents aryl or heteroaryl;
-
186. The compound of claim 151, wherein X is NR2;
- R1 represents aryl or heteroaryl;
R2 represents independently for each occurrence alkyl;
R3 represents independently for each occurrence H or alkyl;
R4 represents cycloalkyl, aryl, or heteroaryl;
R5 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F; and
R6 represents independently for each occurrence H, alkyl, aryl, heteroaryl, or F.
- R1 represents aryl or heteroaryl;
-
152. The compound of claim 151, wherein X is O, NR2, or C═
Specification
- Resources
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Current AssigneeBrian M. Aquila, Fengjiang Wang, Gregory D. Cuny, James R. Hauske, Liming Shao, Michele L.R. Heffernan, Thomas D. Bannister, Xinhe Wu
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Original AssigneeBrian M. Aquila, Fengjiang Wang, Gregory D. Cuny, James R. Hauske, Liming Shao, Michele L.R. Heffernan, Thomas D. Bannister, Xinhe Wu
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InventorsHeffernan, Michele L.R., Cuny, Gregory D., Hauske, James R., Aquila, Brian M., Bannister, Thomas D., Shao, Liming, Wu, Xinhe, Wang, Fengjiang
-
Granted Patent
-
Time in Patent OfficeDays
-
Field of Search
-
US Class Current514/89
-
CPC Class CodesA61K 31/397 having four-membered rings,...A61K 31/438 The ring being spiro-conden...A61K 31/4523 containing further heterocy...A61K 31/495 having six-membered rings w...A61K 31/5375 1,4-Oxazines, e.g. morpholineA61K 31/551 having two nitrogen atoms, ...A61K 31/553 having at least one nitroge...A61P 25/00 Drugs for disorders of the ...C07D 205/04 having no double bonds betw...C07D 211/26 with hydrocarbon radicals, ...C07D 211/42 attached in position 3 or 5C07D 211/56 Nitrogen atoms nitro radica...C07D 211/60 Carbon atoms having three b...C07D 211/70 with only hydrogen atoms, h...C07D 221/04 Ortho- or peri-condensed ri...C07D 223/04 with only hydrogen atoms, h...C07D 223/10 attached in position 2C07D 241/04 having no double bonds betw...C07D 243/08 not condensed with other ringsC07D 265/30 not condensed with other ringsC07D 267/10 : not condensed with other ringsC07D 333/38 : Carbon atoms having three b...C07D 401/06 : linked by a carbon chain co...C07D 401/12 : linked by a chain containin...C07D 405/12 : linked by a chain containin...C07D 405/14 : containing three or more he...C07D 409/06 : linked by a carbon chain co...C07D 409/12 : linked by a chain containin...C07D 491/10 : Spiro-condensed systems