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Claims for Patent: 8,546,428

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Claims for Patent: 8,546,428

Title:Fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-- beta-phenyl-3-quinolineethanol
Abstract: The present invention relates to the fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-- beta-phenyl-3-quinolineethanol, pharmaceutical compositions comprising as active ingredient said salt and to processes for their preparation.
Inventor(s): Hegyi; Jean Francois Alexandre Lucas (Diest, BE), Aelterman; Wim Albert Alex (Gierle, BE), Lang; Yolande Lydia (Vosselaar, BE), Stokbroekx; Sigrid Carl Maria (Beerse, BE), Leys; Carina (Stabroek, BE), Van Remoortere; Peter Jozef Maria (Kapellen, BE), Faure; Anne (Vosselaar, BE)
Assignee: Janssen Pharmaceutica NV (Beerse, BE)
Application Number:12/515,986
Patent Claims: 1. A solid pharmaceutical composition comprising a pharmaceutically acceptable carrier and as active ingredient a therapeutically effective amount of the Fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-- beta-phenyl-3-quinolineethanol, and further comprising a wetting agent, said wetting agent being a polyethylene glycol sorbitan fatty acid ester.

2. A pharmaceutical composition according to claim 1 wherein the composition is suitable for oral administration.

3. A pharmaceutical composition according to claim 1 comprising by weight based on the total weight of the composition: (a) from 5 to 50% of active ingredient; (b) from 0.01 to 5% of a said wetting agent; (c) from 40 to 92% of a diluent; (d) from 0.1 to 5% of a glidant.

4. A pharmaceutical composition according to claim 1 wherein the composition is in the form of a tablet.

5. A pharmaceutical composition according to claim 4 comprising by weight based on the total weight of the tablet core (a) from 5 to 50% of active ingredient; (b) from 0.01 to 5% of a wetting agent; (c) from 40 to 92% of a diluent; (d) from 0 to 10% of a polymer; (e) from 2 to 10% of a disintegrant; (f) from 0.1 to 5% of a glidant; (g) from 0.1 to 1.5% of a lubricant.

6. A pharmaceutical composition according to claim 5 having the following composition TABLE-US-00003 Active ingredient 120.89 mg (i.e. 100 mg base equivalent) Lactose monohydrate (200 mesh) 152.91 mg Maize starch 66 mg Hypromellose 2910 15 mPa s 8 mg Polysorbate 20 1 mg Microcrystalline cellulose 82.2 mg Croscarmellose sodium 23 mg Colloidal silicon dioxide 1.4 mg Magnesium stearate 4.6 mg.

7. A pharmaceutical composition according to claim 4 which is film-coated.

8. A process for preparing a pharmaceutical composition according to claim 4 comprising the following steps: (i) dry blending the active ingredient and part of the diluent; (ii) preparing a binder solution by dissolving the binder and the wetting agent in the binder solution solvent; (iii) spraying the binder solution obtained in step (ii) on the mixture obtained in step (i); (iv) drying the wet powder obtained in step (iii) followed by sieving and optionally mixing; (v) mixing the remaining part of the diluent, the disintegrant and the optional glidant in the mixture obtained in step (iv); (vi) optionally adding the lubricant to the mixture obtained in step (v); (vii) compressing the mixture obtained in step (vi) into a tablet; (viii) optionally film-coating the tablet obtained in step (vii).

9. A process for preparing a pharmaceutical composition according to claim 4 comprising the following steps: (i) dry blending the active ingredient and part of the diluent; (ii) preparing a granulation solution optionally containing the binder and wetting agent; (iii) spraying the granulation solution obtained in step (ii) on the mixture obtained in step (i); (iv) drying the wet granulate obtained in step (iii) followed by sieving and optionally mixing; (v) mixing the remaining part of the diluent, the disintegrant, the optional glidant and optionally the binder and wetting agent in the mixture obtained in step (iv); (vi) optionally adding the lubricant to the mixture obtained in step (v); (vii) compressing the mixture obtained in step (vi) into a tablet; (viii) optionally film-coating the tablet obtained in step (vii).

10. Process for the preparation of a compound as claimed in claim 1 characterized by reacting the corresponding free base with fumaric acid in the presence of a suitable solvent.

11. A method for treating a patient suffering from a mycobacterial infection, said method comprising administering to said patient a therapeutically effective amount of the composition of claim 1.

12. The method of claim 11 wherein the Patient is suffering from tuberculosis.
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