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Claims for Patent: 7,420,057

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Claims for Patent: 7,420,057

Title:Stable polymorph of flibanserin
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.
Inventor(s): Bombarda; Carlo (Chester, VA), Dubini; Enrica (Milan, IT), Ezhaya; Antoine (Milan, IT), Schneider, legal representative; Margarete (Ingelheim, DE), Schneider; Heinrich (Ingelheim, DE)
Assignee: Boehringer Ingelheim Pharma KG (Ingelheim, DE)
Application Number:11/546,304
Patent Claims: 1. A crystalline polymorph, designated form A, of flibanserin 1, ##STR00003## having an endothermic maximum at about 161.degree. C. which occurs during thermal analysis using DSC.

2. A polymorph, designated form A, of flibanserin 1, characterized by the following X-ray powder diffraction pattern: TABLE-US-00003 d- d- Peak Peak Back. Rel. Angle value value width int int int [.degree.2.THETA.] .alpha.1 [.ANG.] .alpha.2 [.ANG.] [.degree.2.THETA.] [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 0.240 240 237 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.

3. A pharmaceutical composition comprising form A according to claim 1, optionally in admixture with one or more pharmaceutical carriers, diluents or excipients, wherein the polymorph is present in crystalline form.

4. A pharmaceutical composition comprising a polymorph, designated form A, of flibanserin 1 according to claim 2, optionally in admixture with one or more pharmaceutical carriers, diluents or excipients, wherein the polymorph is present in crystalline form.

5. Form A of flibanserin 1 ##STR00004## having an endothermic maximum at about 161.degree. C. which occurs during thermal analysis using DSC, and obtained by the process comprising: (a) reacting a benzimidazolone 2 ##STR00005## wherein R denotes a suitable amino protecting group, with a piperazine 3 ##STR00006## wherein X is a leaving group selected from chlorine, bromine, iodine, methanesulphonate, trifluoromethansulphonate and para-toluenesulphonate, in a suitable solvent selected from water, alcohols, mixtures of water with alcohols, polar aprotic solvents and mixtures of polar aprotic solvents with water, in the presence of a suitable base, and (b) cleaving the amino protecting group R under suitable cleaving conditions.

6. A pharmaceutical composition comprising form A of flibanserin 1 ##STR00007## having an endothermic maximum at about 161.degree. C. which occurs during thermal analysis using DSC, and obtained by the process-comprising: (a) reacting a benzimidazolone 2 ##STR00008## wherein R denotes a suitable amino protecting group, with a piperazine 3 ##STR00009## wherein X is a leaving group selected from chlorine, bromine, iodine, methanesulphonate, trifluoromethansulphonate and para-toluenesulphonate, in a suitable solvent selected from water, alcohols, mixtures of water with alcohols, polar aprotic solvents and mixtures of polar aprotic solvents with water, in the presence of a suitable base, and (b) cleaving the amino protecting group R under suitable cleaving conditions.

7. A polymorph, designated form A, of flibanserin 1, ##STR00010## having an endothermic maximum at about 161.degree. C. which occurs during thermal analysis using DSC, and characterized by an X-ray powder diffraction pattern comprising peaks (.degree.2.THETA.) at 15.460, 19.140, 19.820, 20.080, 22.630, 24.610, 24.355, 26.575, 28.210 and 28.325.

8. A polymorph, designated form A, of flibanserin 1, ##STR00011## characterized by a powder X-ray diffraction patent comprising peaks (.degree.20.THETA.) at 15.460, 19.140, 19.820, 20.080, 22.630, 24.610, 24.355, 26.575, 28.210 and 28.325.

9. A polymorph, designated form A, of flibanserin 1, ##STR00012## having an endothermic maximum at about 161.degree. C. which occurs during thermal analysis using DSC, and characterized by an X-ray powder diffraction pattern comprising peaks(.degree.20.THETA.) at 5.195, 9.045, 9.335, 10.025, 10.595, 11.290, 13.225, 14.595, 15.460, 16.655, 17.085, 17.285, 17.420, 18.140, 18.650, 19.140, 19.820, 20.080, 20.385, 21.215, 21.890, 22.630, 23.210, 24.355, 24.610, 25.995, 25.260, 26.575, 27.155, 27.310, 27.865, 28.210, 28.325, 28.650, 29.520, 30.250, 31.105, 31.905, 32.350, 33.300, 33.640, 34.880, 35.275, 36.055, 36.910, 37.160, 37.680 39.435, 39.675, 40.325, 40.930, 41.445, 41.990, 42.670, 43.145, 44.190, 46.095, 46.510, 48.305, 48.900, 50.330, 51.035, 53.550, 54.500, 55.420, 56.220, 56.770, 57.405, and 58.500.

10. A polymorph, designated form A, of flibanserin 1, ##STR00013## characterized by an X-ray powder diffraction pattern comprising peaks (.degree.2.THETA.) at 5.195, 9.045, 9.335, 10.025, 10.595, 11.290, 13.225, 14.595, 15.460, 16.655, 17.085, 17.285, 17.420, 18.140, 18.650, 19.140, 19.820, 20.080, 20.385, 21.215, 21.890, 22.630, 23.210, 24.355, 24.610, 25.995, 25.260, 26.575, 27.155, 27.310, 27.865, 28.210, 28.325, 28.650, 29.520, 30.250, 31.105, 31.905, 32.350, 33.300, 33.640, 34.880, 35.275, 36.055, 36.910, 37.160, 37.680 39.435, 39.675, 40.325, 40.930, 41.445, 41.990, 42.670, 43.145, 44.190, 46.095, 46.510, 48.305, 48.900, 50.330, 51.035, 53.550, 54.500, 55.420, 56.220, 56.770, 57.405, and 58.500.

11. A pharmaceutical composition comprising a polymorph designated form A, of flibanserin 1 according to claim 7, optionally in admixture with one or more pharmaceutical carriers, diluents or excipients, wherein the polymorph is present in crystalline form.

12. A pharmaceutical composition comprising a polymorph, designated form A, of flibanserin 1 according to claim 8, optionally in admixture with one or more pharmaceutical carriers, diluents or excipients, wherein the polymorph is present in crystalline form.

13. A pharmaceutical composition comprising a polymorph, designated form A, of flibanserin 1 according to claim 9, optionally in admixture with one or more pharmaceutical carriers, diluents or excipients, wherein the polymorph is present in crystalline form.

14. A pharmaceutical composition comprising a polymorph, designated form A, of flibanserin 1 according to claim 10, optionally in admixture with one or more pharmaceutical carriers, diluents or excipients, wherein the polymorph is present in crystalline form.

15. A polymorph, designated form A, of flibanserin 1 characterized by having an X-ray powder diffraction pattern as shown in FIG. 1.

16. A pharmaceutical composition comprising a polymorph, designated form A, of flibanserin 1 according to claim 15, optionally in admixture with one or more pharmaceutical carriers, diluents or excipients, wherein the polymorph is present in crystalline form.
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