Stable polymorph of flibanserin

• US 7,420,057 B2
• Filed: 10/12/2006
• Issued: 09/02/2008
• Est. Priority Date: 08/02/2001
• Status: Expired due to Term

• Current Assignee: Sprout Pharmaceuticals, Inc. (Sprout2, Inc.)
• Original Assignee: Boehringer Ingelheim Pharmaceuticals Incorporated (C.H. Boehringer Sohn AG & Co. KG)
• Inventors: Bombarda, Carlo, Schneider, Heinrich, Ezhaya, Antoine, Schneider, legal representative, Dubini, Enrica
• Primary Examiner(s): Eyler; Yvonne
• Assistant Examiner(s): Nwaonicha; Chukwuma O
• Application Number:
  US11/546,304
• Publication Number:
  US 20070032655A1
• Time in Patent Office: 691 Days
• Field of Search: 514/254.06,253 544/370,366,295
• 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,

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.

2. A polymorph, designated form A, of flibanserin 1, characterized by the following X-ray powder diffraction pattern:

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

6. A pharmaceutical composition comprising form A of flibanserin 1

7. A polymorph, designated form A, of flibanserin 1,

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.

8. A polymorph, designated form A, of flibanserin 1,

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.

9. A polymorph, designated form A, of flibanserin 1,

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.

10. A polymorph, designated form A, of flibanserin 1,

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.