Vortioxetine Pyroglutamate

Patent metadata

Field	Value
Publication number	US-2016368884-A1
Application number	US-201615152902-A
Country	US
Kind code	A1
Filing date	May 12, 2016
Priority date	May 13, 2015
Publication date	Dec 22, 2016
Grant date	—

Abstract

The present invention provides vortioxetine pyroglutamate salt and pharmaceutical compositions comprising said salt.

First claim

1 . Vortioxetine pyroglutamate.

2 . The compound according to claim 1 , wherein the compound is selected from the group consisting of vortioxetine (L)-pyroglutamate, vortioxetine (D)-pyroglutamate and vortioxetine (DL)-pyroglutamate.

3 . The compound according to claim 1 , wherein the compound is vortioxetine (L)-pyroglutamate or vortioxetine (D)-pyroglutamate in crystalline form with XRPD reflections at 10.72, 12.14, 16.22 and 18.59 (° 2θ) (±0.1 ° 2θ).

4 . The compound according to claim 1 , wherein the compound is vortioxetine (DL)-pyroglutamate monohydrate in crystalline form with XRPD reflections at 6.16, 9.25, 17.68 and 18.12 (° 2θ) (±0.1 ° 2θ).

5 . The compound according to claim 1 , wherein the compound is vortioxetine (DL)-pyroglutamate a-form in crystalline form with XRPD reflections at 14.27, 15.75, 17.06 and 18.59 (° 2θ) (±0.1 ° 2θ).

6 . A pharmaceutical composition, comprising the compound of claim 1 together with at least one pharmaceutically acceptable carrier or diluent.

7 . A gelable pharmaceutical composition, comprising the compound of claim 1 and a salt.

8 . A gel, comprising the compound of claim 1 , a salt and water.

9 . A solid pharmaceutical composition for oral administration, comprising the compound of claim 1 and an enteric coating.

10 . A method for preparing a gel, said method comprising mixing the compound of claim 1 , a salt and an aqueous solution.

11 . A method for the treatment of a disease selected from major depressive disorder; major depressive episode; general anxiety disorder; obsessive compulsive disorder (OCD), panic disorder; post traumatic stress disorder; cognitive impairment; mild cognitive impairment (MCI); cognitive impairment associated with Alzheimer's disease, depression, schizophrenia (CIAS); and attention deficit hyperactivity disorder (ADHD), the method comprising the administration of a therapeutically effective amount of the compound of claim 1 to a patient in need thereof.

12 . A method for the treatment of a disease selected from major depressive disorder; major depressive episode; general anxiety disorder; obsessive compulsive disorder (OCD), panic disorder; post traumatic stress disorder; cognitive impairment; mild cognitive impairment (MCI); cognitive impairment associated with Alzheimer's disease, depression, schizophrenia (CIAS); and attention deficit hyperactivity disorder (ADHD), the method comprising the administration of a therapeutically effective amount of a gel comprising the compound of claim 1 , a salt and water, to a patient in need thereof.

13 . A method for the treatment of a disease selected from major depressive disorder; major depressive episode; general anxiety disorder; obsessive compulsive disorder (OCD), panic disorder; post traumatic stress disorder; cognitive impairment; mild cognitive impairment (MCI); cognitive impairment associated with Alzheimer's disease, depression, schizophrenia (CIAS); and attention deficit hyperactivity disorder (ADHD), the method comprising the administration of a therapeutically effective amount of a gel to a patient in need thereof, wherein said gel is prepared by mixing the compound of claim 1 , a salt and water.

Assignees

• H Lundbeck As

Inventors

• De Diego Heidi Lopez
• Christensen Kim Lasse
• Holm Rene
• Kateb Jens

Classifications

• A61P25/18

  Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia · CPC title

• A61P25/22

  Anxiolytics · CPC title

• A61P25/24

  Antidepressants · CPC title

• A61P25/28

  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 title

• A61P25/00

  Drugs for disorders of the nervous system · CPC title