Some content of this application is unavailable at the moment.
If this situation persist, please contact us atFeedback&Contact
1. (WO2018224594) COCRYSTALS OF VORTIOXETINE HYDROBROMIDE AND RESORCINOL
Note: Text based on automatic Optical Character Recognition processes. Please use the PDF version for legal matters

Claims

1 . A cocrystal of vortioxetine hydrobromide and resorcinol.

2. The cocrystal according to claim 1 , which is characterized by having an X-ray diffractogram that comprises peaks at 9.0 and 17.9 degrees 2 theta at a Cu-KQ radiation, λ = 1.5406 A.

3. The cocrystal according to claim 2, which is characterized by having an X-ray diffractogram that comprises peaks at approximately 12.1 , 19.1 and 23.6 degrees 2 theta at a Cu-Ka radiation, λ = 1.5406 A.

4. The cocrystal according to claim 3, which is characterized by having an X-ray diffractogram that comprises peaks at approximately 14.0, 14.5, 18.1 , 18.3, 19.3, 21.4, 21.9, 24.2, 24.4, 24.7, 25.9, 26.4, and 27.0 degrees 2 theta at a Cu-KQ radiation, λ = 1 .5406 A.

5. The cocrystal according to any of the claims 2-4, which is characterized by having a DSC analysis which shows an endothermic event with an onset at about 201 °C.

6. The cocrystal according to any of the claims 1 -5, wherein the molar ratio vortioxetine hydrobromide: resorcinol is about 2:1.

7. A cocrystal of vortioxetine hydrobromide and resorcinol as defined in any of the claims 1 -6, for use as a medicament.

8. A cocrystal of vortioxetine hydrobromide and resorcinol as defined in any of the claims 1 -6, for use in the prevention and/or treatment of major depressive disorder.

9. A pharmaceutical composition comprising a cocrystal of vortioxetine hydrobromide and resorcinol as defined in any of the claims 1 -6, together with appropriate amounts of pharmaceutical excipients or carriers.

10. A process for the preparation of a cocrystal of vortioxetine hydrobromide and resorcinol cocrystal as defined in any of the claims 1 -6, which comprises slurrying a mixture of vortioxetine hydrobromide form β and resorcinol in water at room temperature for the necessary period of time to form the cocrystal; and subsequently isolating the compound thus obtained.

1 1 . The process according to claim 10, wherein the isolation of the cocrystal comprises filtering the product thus obtained and drying it at room temperature under vacuum.

12. The process according to any of the claims 10-1 1 , wherein the cocrystal of vortioxetine hydrobromide and resorcinol is the Form I as defined in any of the claims 3-6, and the process comprises using 2 moles of resorcinol per mol of vortioxetine

hydrobromide.

13. A process for the preparation of a cocrystal of vortioxetine hydrobromide and resorcinol Form I, as defined in any of the claims 1 -6, which comprises its crystallization from a solution of vortioxetine hydrobromide and resorcinol in a solvent selected from the group consisting of water, isopropanol, and a mixture thereof; and subsequently isolating the compound thus obtained.