Use of a polymorph of flibanserin for treating disease
AssigneeSprout Pharmaceuticals, Inc.
InventorsCarlo Bombarda, Enrica Dubini, Antoine Ezhaya
Life of this patent
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Abstract
The invention relates to the polymorph A of flibanserin, to a technical process for the preparation thereof, as well as to the use thereof for preparing medicaments.
Claims6
A method of treating a disease, wherein said disease is schizophrenia, Parkinson's, anxiety, sleep disturbances, sexual and mental disorders or age associated memory impairment in a patient, comprising administering to said patient a therapeutically effective amount of a crystalline polymorph of flibanserin 1,
- having an endothermic maximum at about 161° C. which occurs during thermal analysis using Differential Scanning Calorimetry.
A method of treating a disease, wherein said disease is schizophrenia, Parkinson's, anxiety, sleep disturbances, sexual and mental disorders or age associated memory impairment in a patient, comprising administering to said patient a therapeutically effective amount of flibanserin 1,
- having an endothermic maximum at about 161° C. which occurs during thermal analysis using Differential Scanning Calorimetry.
A method of treating a disease, wherein said disease is schizophrenia, Parkinson's, anxiety, sleep disturbances, sexual and mental disorders or age associated memory impairment in a patient, comprising administering to said patient a therapeutically effective amount of a polymorph of flibanserin 1 characterized by the following X-ray powder diffraction pattern:
- Peak
- Back.
- Angle
- d-value
- d-value
- width
- Peak int
- int
- Rel. int
- [°2Θ]
- α1 [Å]
- α2 [Å]
- [°2Θ]
- [counts]
- [counts]
- [%]
- Signif.
- 5.195
- 16.9967
- 17.0390
- 0.960
- 8
- 69
- 0.1
- 1.05
- 9.045
- 9.7689
- 9.7931
- 0.100
- 92
- 96
- 1.3
- 0.97
- 9.335
- 9.4660
- 9.4896
- 0.080
- 114
- 98
- 1.6
- 0.88
- 10.025
- 8.8160
- 8.8379
- 0.140
- 400
- 100
- 5.5
- 7.18
- 10.595
- 8.3430
- 8.3637
- 0.140
- 204
- 102
- 2.8
- 3.46
- 11.290
- 7.8309
- 7.8503
- 0.140
- 467
- 104
- 6.4
- 6.91
- 13.225
- 6.6891
- 6.7058
- 0.180
- 548
- 112
- 7.5
- 13.10
- 14.595
- 6.0642
- 6.0793
- 0.180
- 404
- 121
- 5.5
- 9.17
- 15.460
- 5.7268
- 5.7410
- 0.140
- 4186
- 125
- 57.3
- 23.20
- 16.655
- 5.3185
- 5.3317
- 0.200
- 515
- 130
- 7.0
- 12.38
- 17.085
- 5.1856
- 5.1985
- 0.100
- 1347
- 132
- 18.4
- 2.78
- 17.285
- 5.1260
- 5.1388
- 0.060
- 1399
- 135
- 19.1
- 2.26
- 17.420
- 5.0866
- 5.0992
- 0.100
- 1204
- 135
- 16.5
- 4.71
- 18.140
- 4.8863
- 4.8984
- 0.180
- 1043
- 139
- 14.3
- 13.14
- 18.650
- 4.7538
- 4.7656
- 0.120
- 1063
- 142
- 14.5
- 0.91
- 19.140
- 4.6332
- 4.6447
- 0.140
- 7310
- 144
- 100.0
- 32.77
- 19.820
- 4.4757
- 4.4869
- 0.160
- 3624
- 146
- 49.6
- 9.02
- 20.080
- 4.4184
- 4.4294
- 0.140
- 5402
- 149
- 73.9
- 21.06
- 20.385
- 4.3530
- 4.3638
- 0.160
- 2652
- 149
- 36.3
- 23.25
- 21.215
- 4.1845
- 4.1949
- 0.160
- 369
- 154
- 5.0
- 5.78
- 21.890
- 4.0570
- 4.0670
- 0.200
- 773
- 156
- 10.6
- 3.09
- 22.630
- 3.9259
- 3.9357
- 0.280
- 4277
- 161
- 58.5
- 74.66
- 23.210
- 3.8291
- 3.8386
- 0.120
- 484
- 164
- 6.6
- 3.33
- 24.355
- 3.6516
- 3.6607
- 0.060
- 2725
- 169
- 37.3
- 1.16
- 24.610
- 3.6144
- 3.6234
- 0.140
- 3540
- 172
- 48.4
- 17.08
- 24.995
- 3.5596
- 3.5684
- 0.100
- 529
- 174
- 7.2
- 1.01
- 25.260
- 3.5228
- 3.5316
- 0.120
- 557
- 174
- 7.6
- 3.02
- 26.575
- 3.3514
- 3.3597
- 0.240
- 2421
- 182
- 33.1
- 42.58
- 27.155
- 3.2811
- 3.2893
- 0.140
- 676
- 185
- 9.2
- 1.32
- 27.310
- 3.2629
- 3.2710
- 0.100
- 767
- 185
- 10.5
- 2.75
- 27.865
- 3.1991
- 3.2071
- 0.120
- 420
- 188
- 5.7
- 1.08
- 28.210
- 3.1608
- 3.1686
- 0.100
- 1467
- 190
- 20.1
- 0.79
- 28.325
- 3.1482
- 3.1560
- 0.140
- 1789
- 190
- 24.5
- 4.41
- 28.650
- 3.1132
- 3.1210
- 0.180
- 1204
- 190
- 16.5
- 11.65
- 29.520
- 3.0234
- 3.0309
- 0.220
- 1011
- 196
- 13.8
- 15.74
- 30.250
- 2.9521
- 2.9594
- 0.120
- 159
- 199
- 2.2
- 1.22
- 31.105
- 2.8729
- 2.8800
- 0.360
- 282
- 204
- 3.9
- 8.14
- 31.905
- 2.8026
- 2.8096
- 0.100
- 339
- 207
- 4.6
- 0.96
- 32.350
- 2.7651
- 2.7720
- 0.120
- 237
- 210
- 3.2
- 3.01
- 33.300
- 2.6884
- 2.6950
- 0.180
- 1347
- 216
- 18.4
- 14.06
- 33.640
- 2.6620
- 2.6686
- 0.100
- 404
- 216
- 5.5
- 1.45
- 34.880
- 2.5701
- 2.5765
- 0.200
- 202
- 222
- 2.8
- 1.04
- 35.275
- 2.5422
- 2.5486
- 0.240
- 299
- 225
- 4.1
- 4.84
- 36.055
- 2.4890
- 2.4952
- 0.280
- 202
- 228
- 2.8
- 3.78
- 36.910
- 2.4333
- 2.4393
- 0.320
- 169
- 234
- 2.3
- 0.90
- 37.160
- 2.4175
- 2.4235
- 0.120
- 216
- 234
- 3.0
- 2.14
- 37.680
- 2.3853
- 2.3912
- 0.240
- 240
- 2.37
- 3.3
- 1.58
- 39.435
- 2.2831
- 2.2888
- 0.280
- 449
- 246
- 6.1
- 2.67
- 39.675
- 2.2698
- 2.2755
- 0.080
- 396
- 246
- 5.4
- 0.82
- 40.325
- 2.2347
- 2.2403
- 0.160
- 520
- 250
- 7.1
- 0.95
- 40.930
- 2.2031
- 2.2086
- 0.120
- 480
- 253
- 6.6
- 2.66
- 41.445
- 2.1769
- 2.1823
- 0.240
- 372
- 256
- 5.1
- 2.65
- 41.990
- 2.1499
- 2.1552
- 0.120
- 538
- 259
- 7.4
- 1.31
- 42.670
- 2.1172
- 2.1225
- 0.160
- 428
- 262
- 5.9
- 1.45
- 43.145
- 2.0950
- 2.1002
- 0.120
- 433
- 266
- 5.9
- 1.50
- 44.190
- 2.0478
- 2.0529
- 0.160
- 376
- 269
- 5.1
- 0.89
- 46.095
- 1.9675
- 1.9724
- 0.160
- 279
- 279
- 3.8
- 0.86
- 46.510
- 1.9509
- 1.9558
- 0.240
- 310
- 282
- 4.2
- 0.87
- 48.305
- 1.8826
- 1.8872
- 0.200
- 506
- 292
- 6.9
- 2.06
- 48.900
- 1.8610
- 1.8657
- 0.240
- 615
- 296
- 8.4
- 1.67
- 50.330
- 1.8115
- 1.8160
- 0.160
- 437
- 303
- 6.0
- 1.73
- 51.035
- 1.7881
- 1.7925
- 0.080
- 416
- 306
- 5.7
- 0.93
- 53.550
- 1.7099
- 1.7141
- 0.480
- 177
- 317
- 2.4
- 2.84
- 54.500
- 1.6823
- 1.6865
- 0.400
- 130
- 324
- 1.8
- 1.37
- 55.420
- 1.6565
- 1.6606
- 0.320
- 130
- 328
- 1.8
- 1.72
- 56.220
- 1.6348
- 1.6389
- 0.320
- 121
- 331
- 1.7
- 0.87
- 56.770
- 1.6203
- 1.6243
- 0.240
- 142
- 335
- 1.9
- 1.59
- 57.405
- 1.6039
- 1.6079
- 0.240
- 112
- 339
- 1.5
- 1.19
- 58.500
- 1.5764
- 1.5804
- 0.240
- 67
- 342
- 0.9
- 1.57
A method of treating a disease, wherein said disease is schizophrenia, Parkinson's, anxiety, sleep disturbances, sexual and mental disorders or age associated memory impairment in a patient, comprising administering to said patient a therapeutically effective amount of a polymorph of flibanserin 1 characterized by having an X-ray powder diffraction pattern as shown in FIG. 1.
Dependencies are inferred from the claim text.