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US 12,234,211 B2Granted
Cycloolefin substituted heteroaromatic compounds and their use
AssigneeHutchison Medipharma Limited
InventorsWei-Guo Su, Guangxiu Dai, Kun Xiao
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I) or a pharmaceutically acceptable salt thereof, and/or solvates racemic mixtures, enantiomers, diasteromers, and tautomers thereof, wherein A, R1, R2, R3, R3′, R4, R4′, R5, R6, R7, R8, m, and n are as defined in the detailed description.
Claims15
A compound of formula (I-1):
- or a pharmaceutically acceptable salt, solvate, racemic mixture, enantiomer, diastereomer, or tautomer thereof, wherein
- R1 is chosen from H, —OH, halo, C1-6 alkyl, C1-6 alkoxyl, —NH2, —NH (C1-4 alkyl), —N(C1-4 alkyl)2, oxo, or C3-8 cycloalkyl;
- each of R2 is independently chosen from H, deuterium, halo, —OH, —NH2, —CN, —SH, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-8 cycloalkyl, oxo, —OR5, —OCOR5, —NHR5, —N(R5) (C1-4 alkyl), —COR5, —NHCOR5, or 3-8 membered heterocyclyl containing one or more heteroatoms independently chosen from N, O, and S;
- in which each of said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl or 3-8 membered heterocyclyl containing one or more heteroatoms independently chosen from N, O, and S is optionally substituted with one or more groups chosen from deuterium, halo, —CN, —OH, —SH, —NH2, —NH (C1-4 alkyl), —N(C1-4 alkyl)2, or C1-6 alkoxyl;
- or two R2, which attach to the same carbon atom, together with the carbon atom they are attached to form a 3-5 membered cycloalkyl which is optionally substituted with one or more halo or deuterium;
- R3′ and R4′ are both H;
- R3 and R4 are independently chosen from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-12 cycloalkyl, 3-12 membered heterocyclyl containing one or more heteroatoms independently chosen from N, O, and S, phenyl, 5-12 membered heteroaryl containing one or more heteroatoms independently chosen from N, O, and S, —C(O)R5, —OR5, or —NHR5, in which each of said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-12 cycloalkyl, 3-12 membered heterocyclyl containing one or more heteroatoms independently chosen from N, O, and S, phenyl, or 5-12 membered heteroaryl containing one or more heteroatoms independently chosen from N, O, and S is optionally substituted with one or more R66;
- provided that R3 and R4 are not H simultaneously;
- provided that when one of R3 and R4 is optionally substituted phenyl or optionally substituted 5-6 membered heteroaryl containing one or more heteroatoms independently chosen from N, O, and S, the other one is —OR5 or —NHR5;
- or R3 and R3′ are independently chosen from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-12 cycloalkyl, 3-12 membered heterocyclyl containing one or more heteroatoms independently chosen from N, O, and S, phenyl, 5-12 membered heteroaryl containing one or more heteroatoms independently chosen from N, O, and S, —C(O)R5, —OR5, or —NHR5, in which each of said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-12 cycloalkyl, 3-12 membered heterocyclyl containing one or more heteroatoms independently chosen from N, O, and S, phenyl, or 5-12 membered heteroaryl containing one or more heteroatoms independently chosen from N, O, and S is optionally substituted with one or more R6;
- R4 and R4′ together with the N atom they are attached to form a 3-8 membered heterocyclic ring containing one or more heteroatoms independently chosen from N, O, and S which is optionally substituted by one or more R6;
- R5 is chosen from C1-6 alkyl or C3-8 cycloalkyl, each of which is optionally substituted with one or more groups independently chosen from halo, —CN, —OH, —SH, —NH2, or C1-6 alkoxyl;
- each of R6 is independently chosen from deuterium, halo, —CN, —OH, —SH, —NH2, C1-6 alkoxyl, C1-6 alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, 3-8 membered heterocyclyl containing one or more heteroatoms independently chosen from N, O, and S, phenyl, or 5-6 membered heteroaryl containing one or more heteroatoms independently chosen from N, O, and S, in which each of said C1-6 alkoxyl, C1-6 alkyl, C3-8 cycloalkyl, 3-8 membered heterocyclyl containing one or more heteroatoms independently chosen from N, O, and S, phenyl, or 5-6 membered heteroaryl containing one or more heteroatoms independently chosen from N, O, and S is optionally substituted with one or more groups independently chosen from halo, —CN, —OH, —SH, —NH2, C1-6 alkoxyl, C2-6 alkynyl, or C1-6 alkyl;
- m is 0, 1, 2, 3, 4, 5, or 6;
- n is 0, 1, or 2.
12 more elements
A compound selected from:
- Compound
- Structure
- 1
- 2
- 3
- 4
- 5
- 6
- 7
- 8
- 9
- 10
- 11
- 12
- 13
- 14
- 15
- 16
- 17
- 18
- 19
- 20
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- 22
- 23
- 24
- 25
- 26
- 27
- 28
- 29
- 30
- 31
- 32
- 33
- 34
- 35
- 36
- 37
- 38
- 39
- 40
- 41
- 42
- 43
- 44
- 45
- 46
- 47
- 48
- 49
- 50
- 51
- 52
- 53
- 55
- 56
- 57
- 59
- 60
- 61
- 62
- 63
- 64
- 65
- 66
- 67
- 68
- 69
- 71
- 72
- 73
- 74
- 75
- 76
- 77
- 78
- 79
- 80
- 81
- 82
- 83
- 84
- 85
- 87
- 89
- 90
- 91
- 92
- 93
- 95 & 96
- 97 & 98
- 99
- 100 & 101
- 102 & 103
- 104 & 105
- 106 & 107
- 108 & 109
- 110 & 111
- 112 & 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 & 151
- 152
- 153
- 154
- 155
- 156
- 157
- 158
- 159
- 160
- 161
- 162
- 163
- 164
- 165
- 166
- 167
- 168
- 169
- 170
- 171
- 172
- 173
- 174
- 175
- 175 & 177
- 178
- 179
- 180
- 181
- 182
- 183
- 184
- 186
- 187
- 188
- 189
- 190
- 191
- 192
- 193
- 194
- 195
- 199
- 200
- 201 & 202
- 203
- 204
- 205
- 206
- 207
- 209
- 212
- 213
- 214
- 215
- 216
- 217
- 218
- 219
- 220
- 221
- 222 & 223
- 224
- 225 & 226
- 227 & 228
- 229
- 230 & 231
- 232 & 233
- 235
- 236 & 237
- 238
- 239
- 240
- 241
- 242
- 243
- 246 & 247
- 251 & 252
- 253 & 254
- 259
- 260
- 261
- 262 & 263
- 264 & 265
- 266, 267, 268, & 269
- 270
- 271
- 272 & 273
- 274
- 275
- 277
- 278
- 279
- 280
- 281
- 282
- 283
- 285 & 286
- 287 & 288
- 289 & 290
- 291 & 292
- 293
- 294
- 295
- 296
- 297
- 298
- 299
- 300
- 301
- or a pharmaceutically acceptable salt thereof.
239 more elements
Dependencies are inferred from the claim text.