Stable polymorph of flibanserin

• US 7,183,410 B2
• Filed: 08/01/2002
• Issued: 02/27/2007
• Est. Priority Date: 08/02/2001
• Status: Expired due to Term

• Current Assignee: Sprout Pharmaceuticals, Inc. (Sprout2, Inc.)
• Original Assignee: BIDACHEM S.p.A. (C.H. Boehringer Sohn AG & Co. KG)
• Inventors: Ezhaya, Antoine, Schneider, legal representative, Bombarda, Carlo, Dubini, Enrica, Schneider, deceased
• Primary Examiner(s): Page; Thurman K.
• Assistant Examiner(s): NWAONICHA, CHUKWUMA O
• Application Number:
  US10/210,474
• Publication Number:
  US 20030119850A1
• Time in Patent Office: 1,671 Days
• Field of Search: 544/370,295,366 514/253,252.13,254.06
• 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 process for preparing form A of flibanserin 1 having an endothermic maximum at about 161°

C. which occurs during thermal analysis using DSC,

2. A process according to claim 1, wherein the reaction of 2 with 3 is conducted at a temperature of at least 50°

C.

3. A process according to claim 2, wherein heating is conducted for about 10 minutes to about 12 hours.

4. A process for preparing flibanserin 1 comprising form A having an endothermic maximum at about 161°

C. which occurs during thermal analysis using DSC,

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

C.

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