Stable polymorph of flibanserin

• US 20070032654A1
• Filed: 10/12/2006
• Published: 02/08/2007
• Est. Priority Date: 08/02/2001
• Status: Abandoned Application

• Current Assignee: Sprout Pharmaceuticals, Inc. (Sprout2, Inc.)
• Original Assignee: BIDACHEM S.p.A. (C.H. Boehringer Sohn AG & Co. KG)
• Inventors: Schneider, Heinrich, Ezhaya, Antoine, Bombarda, Carlo, Dubini, Enrica, Schneider, Margarete
• Application Number:
  US11/546,303
• Publication Number:
  US 20070032654A1
• Time in Patent Office: Days
• US Class Current: 544/370
• CPC Class Codes: A61K 31/496 Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: A61P 25/22 Anxiolytics
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: C07D 233/26 Radicals substituted by carbon atoms having three bonds to hetero atoms
• CPC Class Codes: C07D 235/26 Oxygen atoms
• CPC Class Codes: C07D 403/06 linked by a carbon chain containing only aliphatic carbon atoms

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.

Claims

1. ) A crystalline polymorph, designated form A, of flibanserin 1,

2. ) Flibanserin 1 comprising form A according to claim 1.

3. ) A process for preparing form A of flibanserin 1 according to claim 1,

4. ) A process according to claim 3, wherein the reaction of 2 with 3 is conducted at a temperature of at least 50°

C.

5. ) A process according to claim 4, wherein heating is conducted for about 10 minutes to about 12 hours.

6. ) A process for preparing flibanserin 1 according to claim 2,

7. ) A process according to claim 6, wherein the reaction of 2 with 3 is conducted at a temperature of at least 50°

C.

8. ) A process according to claim 7, wherein heating is conducted for about 10 minutes to about 12 hours.

9. ) Form A of flibanserin 1 obtained by the process according to claim 3.

10. ) Filbanserin 1 obtained by the process according to claim 6.

13. ) A method for treating a disease that is treatable with a compound having an affinity for the 5-HT_1A or 5-HT₂-receptors in a patient, comprising administering to said patient a therapeutically effective amount of form A according to claim 1.

14. ) A method for treating a disease that is treatable with a compound having an affinity for the 5-HT_1A or 5-HT₂-receptors in a patient, comprising administering to said patient a therapeutically effective amount of flibanserin 1 according to claim 2.

17. ) A method for treating a disease selected from depression, schizophrenia, Parkinson'"'"'s, anxiety, sleep disturbances, sexual and mental disorders and age associated memory impairment in a patient, comprising administering to said patient a therapeutically effective amount of form A according to claim 1.

18. ) A method for treating a disease selected from depression, schizophrenia, Parkinson'"'"'s, anxiety, sleep disturbances, sexual and mental disorders and age associated memory impairment in a patient, comprising administering to said patient a therapeutically effective amount of flibanserin I according to claim 2.

21. ) A pharmaceutical composition comprising form A according to claim 1, optionally in admixture with one or more pharmaceutical carriers, diluents or excipients.

22. ) A pharmaceutical composition comprising flibanserin 1 according to claim 2, optionally in admixture with one or more pharmaceutical carriers, diluents or excipients.

11. ) A polymorph of flibanserin 1 characterized by the following X-ray powder diffraction pattern:

15. ) A method for treating a disease that is treatable with a compound having an affinity for the 5-HT_1A or 5-HT₂-receptors in a patient, comprising administering to said patient a therapeutically effective amount of a polymorph of flibanserin 1 according to claim 11.

19. ) A method for treating a disease selected from depression, schizophrenia, Parkinson'"'"'s, anxiety, sleep disturbances, sexual and mental disorders and age associated memory impairment in a patient, comprising administering to said patient a therapeutically effective amount of a polymorph of flibanserin 1 according to claim 11.

23. ) A pharmaceutical composition comprising a polymorph of flibanserin 1 according to claim 11, optionally in admixture with one or more pharmaceutical carriers, diluents or excipients.

12. ) A polymorph of flibanserin 1 characterized by having an X-ray powder diffraction pattern as shown in FIG. 1.

16. ) A method for treating a disease that is treatable with a compound having an affinity for the 5-HT_1A or 5-HT₂-receptors in a patient, comprising administering to said patient a therapeutically effective amount of a polymorph of flibanserin 1 according to claim 12.

20. ) A method for treating a disease selected from depression, schizophrenia, Parkinson'"'"'s, anxiety, sleep disturbances, sexual and mental disorders and age associated memory impairment in a patient, comprising administering to said patient a therapeutically effective amount of a polymorph of flibanserin 1 according to claim 12.

24. ) A pharmaceutical composition comprising a polymorph of flibanserin 1 according to claim 12, optionally in admixture with one or more pharmaceutical carriers, diluents or excipients.