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Claims for Patent: 6,890,927

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Claims for Patent: 6,890,927

Title: Tartrate salts of 5,8, 14-triazateracyclo[10.3.1.02,11 04.9]-hexadeca-2(11),3,5,7,9-pentaene and pharmaceutical compositions thereof
Abstract:The present invention is directed to the tartrate salts of 5,8,14-triazatetracyclo[10.3.1.0.sup.2,11.0.sup.4,9 ]-hexadeca-2(11),3,5,7,9-pentaene: ##STR1## and pharmaceutical compositions thereof. The present invention in particular is directed to the L-tartrate salt, and further to the various polymorphs of the L-tartrate salt, including two distinct anhydrous polymorphs (referred to herein as Forms A and B) and a hydrate polymorph (referred to herein as Form C). In addition, the present invention is also directed to the D-tartrate salt of 5,8,14-triazatetracyclo[10.3.1.0.sup.2,11.0.sup.4,9 ]-hexadeca-2(11),3,5,7,9-pentaene and the various polymorphs thereof; as well as the D,L-tartrate salt thereof and its polymorphs, and the meso-tartrate salt thereof and its polymorphs.
Inventor(s): Bogle; David E. (Jewett City, CT), Rose; Peter R. (Ledyard, CT), Williams; Glenn R. (East Aurora, NY)
Assignee: Pfizer Inc (New York, NY)
Application Number:10/139,730
Patent Claims: 1. The tartrate salt of 5,8,14-triazatetracyclo[10.3.1.0.sup.2,11.0.sup.4,9 ]-hexadeca -2(11),3,5,7,9-pentaene.

2. A compound according to claim 1 which is the L-tartrate salt.

3. A compound according to claim 2 which is anhydrous.

4. A compound according to claim 1 which is the D,L-tartrate salt.

5. A compound according to claim 4 which is anhydrous.

6. A compound according to claim 1 which is D-tartrate salt.

7. A compound according to claim 6 which is anhydrous.

8. A compound according to claim 6 which is a hydrate.

9. A compound according to claim 1 which is the meso-tartrate salt.

10. The L-tartrate salt of claim 2 that is a hydrate.

11. A compound according to claim 10 where the hydrate is a monohydrate.

12. A D,L-tartrate of claim 4 which is a hydrate.

13. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound according to any of claims 1, 2, 6 or 9.

14. A method of treatment for nicotine dependency, addiction and withdrawal comprising the administration of a compound according to any of claims 1, 2, 6 or 9 to a subject in need thereof.

15. A process for the preparation of a compound according to claim 1 comprising the steps of (i) contacting 5,8,14-triazatetracyclo[10.3.1.0.sup.2,11.0.sup.4,9 ]-hexadeca-2(11),3,5,7,9-pentaene in a suitable solvent with between about 1 and about 2 equivalents of L-tartaric acid; and (ii) collecting the crystals formed.

16. A process according to claim 15 wherein 1.1 equivalents of L-tartaric acid are employed and the tartaric acid is added to a solution containing the free base.

17. A process according to claim 15 wherein the contacting step is allowed to proceed above 45.degree. C.

18. A process according to claim 15 wherein the contacting step is allowed to proceed for less than 2 hours.

19. A process according to claim 15 wherein the suitable solvent is selected from the group consisting of an (C.sub.1 -C.sub.6)alkyl alcohol, an (C.sub.1 -C.sub.6)alkyl ketone, an (C.sub.1 -C.sub.6)alkyl ether, acetonitrile and an (C.sub.1 -C.sub.6)alkyl ester.

20. A process according to claim 15 wherein the suitable solvent is ethanol or methanol.

21. A process for the preparation of a compound according to claim 1 comprising the steps of (i) contacting 5,8,14-triazatetracyclo[10.3.1.0.sup.2,11.0.sup.4,9 ]-hexadeca-2(11),3,5,7,9-pentaene in a suitable solvent with between about 1 and about 2.3 equivalents of L-tartaric acid; and (ii) collecting the crystals formed.

22. A process according to claim 21 wherein 1.1 equivalents of L-tartaric acid are employed and the free base in solution is added to a solution containing L-tartaric acid.

23. A process according to claim 21 wherein the contact step is allowed to proceed for at least 2 hours.

24. A process according to claim 21 wherein the contact step is allowed to proceed for at least 12 hours.

25. A process according to claim 21 wherein the suitable solvent is selected from the group consisting of an (C.sub.1 -C.sub.6)alkyl alcohol, an (C.sub.1 -C.sub.6)alkyl ketone, an (C.sub.1 -C.sub.6)alkyl ether, acetonitrile and an (C.sub.1 -C.sub.6)alkyl ester.

26. A process according to claim 21 wherein the suitable solvent is methanol or ethanol.

27. A process according to claim 21 wherein the suitable solvent is methanol.

28. A process for the preparation of a compound according to claim 16 comprising the steps of (i) contacting an anhydrous L-tartrate salt of 5,8,14-triazatetracyclo[10.3.1.0.sup.2,11.0.sup.4,9 ]-hexadeca-2(11),3,5,7,9-pentaene with water; and (ii) collecting the crystals formed.

29. A process according to claim 28 wherein the contacting of step (i) comprises exposing the anhydrous L-tartrate salt to greater than 70% humidity.

30. A process according to claim 28 wherein the contacting of step (i) comprises slurrying the anhydrous L-tartrate salt with water.

31. A process according to claim 28 wherein step (i) comprises the addition of an organic solvent.

32. A process according to claim 28 wherein step (i) comprises the addition of methanol, ethanol or acetonitrile.

33. A process for the preparation of a compound according to claim 25 comprising the steps of (i) contacting 5,8,14-triazatetracyclo[10.3.1.0.sup.2,11.0.sup.4,9 ]-hexadeca-2(11),3,5,7,9-pentaene in a suitable solvent with about 1 to about 2.3 equivalents of D,L-tartaric acid; and (ii) collecting the crystals formed.

34. A process according to claim 33 wherein about 2.2 equivalents of D,L-tartaric acid is employed and the free base in solution is added to a solution containing D,L-tartaric acid.

35. A process according to claim 33 wherein the contact step is allowed to proceed for at least 24 hours.

36. A process according to claim 33 wherein the suitable solvent is anhydrous ethanol.

37. A process for the preparation of a compound according to claim 12 comprising the steps of (i) contacting 5,8,14-triazatetracyclo[10.3.1.0.sup.2,11.0.sup.4,9 ]-hexadeca-2(11),3,5,7,9-pentaene in a suitable solvent with about 1 to about 2.3 equivalents of D,L-tartaric acid; and (ii) collecting the crystals formed.

38. A process according to claim 37 wherein about 2.2 equivalents of D,L-tartaric acid is employed and the free base in solution is added to a solution containing D,L-tartaric acid.

39. A process according to claim 37 wherein the contact step is allowed to proceed for at least 24 hours.

40. A process according to claim 37 wherein the suitable solvent is 20% aqueous ethanol.
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