Pharmaceutical compositions for the treatment and/or prevention of depression

• US 20060211685A1
• Filed: 02/28/2006
• Published: 09/21/2006
• Est. Priority Date: 03/04/2005
• Status: Abandoned Application

• Current Assignee: Boehringer Ingelheim International GmbH (C.H. Boehringer Sohn AG & Co. KG)
• Original Assignee: Boehringer Ingelheim International GmbH (C.H. Boehringer Sohn AG & Co. KG)
• Inventors: Ceci, Angelo, Pyke, Robert
• Application Number:
  US11/364,153
• Publication Number:
  US 20060211685A1
• Time in Patent Office: Days
• US Class Current: 514/220
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 31/138 Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine atenolol A61K31/165; pindolol A61K31/404; timolol A61K31/5377
• CPC Class Codes: A61K 31/343 condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
• CPC Class Codes: A61K 31/381 having five-membered rings
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 31/496 Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• CPC Class Codes: A61K 31/551 having two nitrogen atoms, e.g. dilazep
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 25/24 Antidepressants

Abstract

The invention relates to new pharmaceutical compositions for the treatment and/or prevention of depression and methods for the preparation thereof. In a preferred embodiment, the instant invention is directed to pharmaceutical combinations comprising flibanserin as one active ingredient in combination with at least one additional active ingredient for the treatment and/or prevention of depression and methods for the preparation thereof.

Claims

1. ) A pharmaceutical composition comprising a therapeutically effective amount of flibanserin, in the form of a free base or a pharmacologically acceptable acid addition salt, in combination with a therapeutically effective amount of an additional antidepressant.

2. ) The pharmaceutical composition according to claim 1, wherein the additional antidepressant is selected from the group consisting of 5-HTlA agonists, 5-HT reuptake inhibitors, D2/D3 antagonists, NE reuptake inhibitors, Chloride channel modulators, MAO-A inhibitors, MAO-B inhibitors, 5-HT_1B antagonist, 5-HT2 antagonists, 5-HT_2C antagonists, NK1 antagonists, 5-HT_1D antgonists, alpha 2 adrenoreceptor antagonists and NK 3 antagonists.

3. ) The pharmaceutical composition according to claim 1, wherein the additional antidepressant is selected from the group consisting of mirtazepine, mianserin, fluoxetine, escitalopram, paroxetine, citalopram, sertraline, fluvoxamine, duloxetine, milnacipran, venlafaxine, tianeptine, trazodone, mirtazapine (Org-3770), reboxetine, opipramol, amisulpride, bupropion, moclobemide (RO-111163), olanzapine, selegiline, agomelatine (S-20098), SR-5861 1, mifepristone, desvenlafaxine (DVS-233), vilazodone, OPC-14523, eizasonan, Org-24448, SLV-308, Org-34517, POL-240 (1H-indole-3-pyruvic acid), saredutant (SR-48968), nemifitide (INN-00835), DOV-21947, nivazole, emapunil, SSR-146977, SA-4503, E 6006, delucemine, SSR-149415, gepirone, nefazodone, radafaxine (GW-353162) and (+)-didesmethylsibutramine ((R)-DDMS).

4. ) The pharmaceutical composition according to claim 1, wherein the additional antidepressant is selected from the group consisting of duloxetine and bupropion.

5. ) The pharmaceutical composition according to claim 1, wherein flibanserin, in the form of a free base or a pharmacologically acceptable acid addition salt, and the additional antidepressant are together in one dosage form.

6. ) The pharmaceutical composition according to claim 1, wherein flibanserin, in the form of a free base or a pharmacologically acceptable acid addition salt, and the additional antidepressant are separate, each in one dosage form.

7. ) The pharmaceutical composition of claim 1, wherein flibanserin, in the form of a free base or a pharmacologically acceptable acid addition salt, is a hydrate and/or a solvate.

8. ) The pharmaceutical composition of claim 1, wherein the additional antidepressant is in the form of a pharmaceutically acceptable acid addition salt.

9. ) The pharmaceutical composition of claim 1, wherein the additional antidepressant is a hydrate and/or a solvate.

10. ) The pharmaceutical composition of claim 1, wherein the additional antidepressant is an individual optical isomer, a mixture of individual enantiomers or racemates thereof.

11. ) A method for the treatment and/or prevention of depression, comprising the administration of a therapeutically effective amount of flibanserin, in the form of a free base or a pharmacologically acceptable acid addition salt, in combination with a therapeutically effective amount of an additional antidepressant, wherein the flibanserin, in the form of a free base or a pharmacologically acceptable acid addition salt, and the additional antidepressant are administered separately, each in one dosage form, or together, within one dosage form.

12. ) The method according to claim 11, wherein the depression is major depressive disorder.

13. ) The method according to claim 11, wherein the depression is childhood depression.

14. ) The method according to claim 11, wherein the depression is dysthymia.

15. ) The method according to claim 11, wherein the depression is seasonal affective disorder.

16. ) The method according to claim 11, wherein the depression is dysthymic disorder.

17. ) The method according to claim 11, wherein the depression is minor depressive disorder.

18. ) The method according to claim 11, wherein the additional antidepressant is selected from the group consisting of 5-HTlA agonists, 5-HT reuptake inhibitors, D2/D3 antagonists, NE reuptake inhibitors, Chloride channel modulators, MAO-A inhibitors, MAO-B inhibitors, 5-HT_1B antagonist, 5-HT2 antagonists, 5-HT_2C antagonists, NK1 antagonists, 5-HT_1D antgonists, alpha 2 adrenoreceptor antagonists and NK 3 antagonists.

19. ) The method according to claim 11, wherein the additional antidepressant is selected from the group consisting of mirtazepine, mianserin, fluoxetine, escitalopram, paroxetine, citalopram, sertraline, fluvoxamine, duloxetine, milnacipran, venlafaxine, tianeptine, trazodone, mirtazapine (Org-3770), reboxetine, opipramol, amisulpride, bupropion, moclobemide (RO-111163), olanzapine, selegiline, agomelatine (S-20098), SR-5861 1, mifepristone, desvenlafaxine (DVS-233), vilazodone, OPC-14523, elzasonan, Org-24448, SLV-308, Org-34517, POL-240 (1H-indole-3-pyruvic acid), saredutant (SR-48968), nemifitide (INN-00835), DOV-21947, nivazole, emapunil, SSR-146977, SA-4503, E 6006, delucemine, SSR-149415, gepirone, nefazodone, radafaxine (GW-353162) and (+)-didesmethylsibutramine ((R)-DDMS).

20. ) The method according to claim 11, wherein the additional antidepressant is selected from the group consisting of duloxetine and bupropion.