US 11,629,171 B2 · Beta-hairpin peptidomimetics

Abstract

Beta-hairpin peptidomimetics of the general formula (I), and pharmaceutically acceptable salts thereof, with P, X, Q., and optionally L being elements as defined in the description and the claims, have Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as Klebsiella pneumoniae and/or Acinetobacter baumannii and/or Escherichia coli and/or Pseudomonas aeruginosa and/or Enterobacter cloacae. They can be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

A β-hairpin peptidomimetic selected from the group consisting of Ex. 1 to 385, the sequences of which are shown in the following Table below:

Ex.
No.
Sequence
Ex. 1
Ex. 2
Ex. 3
Ex. 4
Ex. 5
Ex. 6
Ex. 7
Ex. 8
Ex. 9
Ex. 10
Ex. 11
Ex. 12
Ex. 13
Ex. 14
Ex. 15
Ex. 16
Ex. 17
Ex. 18
Ex. 19
Ex. 20
Ex. 21
Ex. 22
Ex. 23
Ex. 24
Ex. 25
Ex. 26
Ex. 27
Ex. 28
Ex. 29
Ex. 30
Ex. 31
Ex. 32
Ex. 33
Ex. 34
Ex. 35
Ex. 36
Ex. 37
Ex. 38
Ex. 39
Ex. 40
Ex. 41
Ex. 42
Ex. 43
Ex. 44
Ex. 45
Ex. 46
Ex. 47
Ex. 48
Ex. 49
Ex. 50
Ex. 51
Ex. 52
Ex. 53
Ex. 54
Ex. 55
Ex. 56
Ex. 57
Ex. 58
Ex. 59
Ex. 60
Ex. 61
Ex. 62
Ex. 63
Ex. 64
Ex. 65
Ex. 66
Ex. 67
Ex. 68
Ex. 69
Ex. 70
Ex. 71
Ex. 72
Ex. 73
Ex. 74
Ex. 75
Ex. 76
Ex. 77
Ex. 78
Ex. 79
Ex. 80
Ex. 81
Ex. 82
Ex. 83
Ex. 84
Ex. 85
Ex. 86
Ex. 87
Ex. 88
Ex. 89
Ex. 90
Ex. 91
Ex. 92
Ex. 93
Ex. 94
Ex. 95
Ex. 96
Ex. 97
Ex. 98
Ex. 99
Ex. 100
Ex. 101
Ex. 102
Ex. 103
Ex. 104
Ex. 105
Ex. 106
Ex. 107
Ex. 108
Ex. 109
Ex. 110
Ex. 111
Ex. 112
Ex. 113
Ex. 114
Ex. 115
Ex. 116
Ex. 117
Ex. 119
Ex. 120
Ex. 121
Ex. 122
Ex. 123
Ex. 124
Ex. 125
Ex. 126
Ex. 127
Ex. 128
Ex. 129
Ex. 130
Ex. 131
Ex. 132
Ex. 133
Ex. 134
Ex. 135
Ex. 136
Ex. 137
Ex. 138
Ex. 139
Ex. 140
Ex. 141
Ex. 142
Ex. 143
Ex. 144
Ex. 145
Ex. 146
Ex. 147
Ex. 148
Ex. 149
Ex. 150
Ex. 151
Ex. 152
Ex. 153
Ex. 154
Ex. 155
Ex. 156
Ex. 157
Ex. 158
Ex. 159
Ex. 160
Ex. 161
Ex. 162
Ex. 163
Ex. 164
Ex. 165
Ex. 166
Ex. 167
Ex. 168
Ex. 169
Ex. 170
Ex. 171
Ex. 172
Ex. 173
Ex. 174
Ex. 175
Ex. 176
Ex. 177
Ex. 178
Ex. 179
Ex. 180
Ex. 181
Ex. 182
Ex. 183
Ex. 184
Ex. 185
Ex. 186
Ex. 187
Ex. 188
Ex. 189
Ex. 190
Ex. 191
Ex. 192
Ex. 193
Ex. 194
Ex. 195
Ex. 196
Ex. 197
Ex. 198
Ex. 199
Ex. 200
Ex. 201
Ex. 202
Ex. 203
Ex. 204
Ex. 205
Ex. 206
Ex. 207
Ex. 208
Ex. 209
Ex. 210
Ex. 211
Ex. 212
Ex. 213
Ex. 214
Ex. 215
Ex. 216
Ex. 217
Ex. 218
Ex. 219
Ex. 220
Ex. 221
Ex. 222
Ex. 223
Ex. 224
Ex. 225
Ex. 226
Ex. 227
Ex. 228
Ex. 229
Ex. 230
Ex. 232
Ex. 233
Ex. 234
Ex. 235
Ex. 236
Ex. 237
Ex. 238
Ex. 239
Ex. 240
Ex. 241
Ex. 242
Ex. 243
Ex. 244
Ex. 245
Ex. 246
Ex. 247
Ex. 248
Ex. 249
Ex. 250
Ex. 251
Ex. 252
Ex. 253
Ex. 254
Ex. 255
Ex. 256
Ex. 257
Ex. 258
Ex. 259
Ex. 260
Ex. 261
Ex. 262
Ex. 263
Ex. 264
Ex. 265
Ex. 266
Ex. 267
Ex. 268
Ex. 269
Ex. 270
Ex. 271
Ex. 272
Ex. 273
Ex. 274
Ex. 275
Ex. 276
Ex. 277
Ex. 278
Ex. 279
Ex. 280
Ex. 281
Ex. 282
Ex. 283
Ex. 284
Ex. 285
Ex. 286
Ex. 287
Ex. 288
Ex. 289
Ex. 290
Ex. 291
Ex. 292
Ex. 293
Ex. 294
Ex. 295
Ex. 296
Ex. 297
Ex. 298
Ex. 299
Ex. 300
Ex. 301
Ex. 302
Ex. 303
Ex. 304
Ex. 305
Ex. 306
Ex. 307
Ex. 308
Ex. 309
Ex. 310
Ex. 311
Ex. 312
Ex. 313
Ex. 314
Ex. 315
Ex. 316
Ex. 317
Ex. 318
Ex. 319
Ex. 320
Ex. 321
Ex. 322
Ex. 323
Ex. 324
Ex. 325
Ex. 326
Ex. 327
Ex. 328
Ex. 329
Ex. 330
Ex. 331
Ex. 332
Ex. 333
Ex. 334
Ex. 335
Ex. 336
Ex. 337
Ex. 338
Ex. 339
Ex. 340
Ex. 341
Ex. 342
Ex. 343
Ex. 344
Ex. 345
Ex. 346
Ex. 347
Ex. 348
Ex. 349
Ex. 350
Ex. 351
Ex. 352
Ex. 353
Ex. 354
Ex. 355
Ex. 356
Ex. 357
Ex. 358
Ex. 359
Ex. 360
Ex. 361
Ex. 362
Ex. 363
Ex. 364
Ex. 365
Ex. 366
Ex. 367
Ex. 368
Ex. 369
Ex. 370
Ex. 371
Ex. 372
Ex. 373
Ex. 374
Ex. 375
Ex. 376
Ex. 377
Ex. 378
Ex. 379
Ex. 380
Ex. 381
Ex. 382
Ex. 383
Ex. 384
Ex. 385
or a pharmaceutically acceptable salt thereof.

384 more elements

Beta-hairpin peptidomimetics

Life of this patent

Beta-hairpin peptidomimetics

Life of this patent

Abstract

Claims3