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Claims for Patent: 8,471,025

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Claims for Patent: 8,471,025

Title:Crystalline forms of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide sodium salt
Abstract: The present invention relates to novel crystalline forms of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) thereof. The present invention relates to compositions comprising a crystalline form of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil). Processes for the preparation of the crystalline forms and methods of treating bacterial infections by administering the crystalline forms alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil) are also described.
Inventor(s): Dedhiya; Mahendra G. (Pomona, NY), Bhattacharya; Sisir (Hauppauge, NY), Ducandas; Veronique (Vitry sur Seine, FR), Giuliani; Alexandre (Villecresnes, FR), Ravaux; Valerie (Reyrieux, FR), Bonnet; Alain (Chateau-Thierry, FR), Priour; Alain (Paris, FR), Spargo; Peter Lionel (Deal, GB)
Assignee:
Application Number:12/900,567
Patent Claims: 1. A crystalline form of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide or a pharmaceutically acceptable salt thereof, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 13.0 and about 17.3+/-0.5 degrees 2.theta..

2. The crystalline form according to claim 1, wherein the salt is a sodium salt of (1R,2S,5R)-7-oxo-6-sulphooxy-1,6-diazabicyclo[3.2.1]octane-2-carboxamide.

3. The crystalline form according to claim 2, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 19.9, about 22.0 or about 28.2+/-0.5 degrees 2.theta..

4. The crystalline form according to claim 2, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 16.5+/-0.5 degrees 2.theta..

5. The crystalline form according to claim 2, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 17.5+/-0.5 degrees 2.theta..

6. The crystalline form according to claim 2, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at; about 22.3+/-0.5 degrees 2.theta..

7. The crystalline form according to claim 2, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 19.2; about 19.5+/-0.5 degrees 2.theta. or a combination thereof.

8. The crystalline form according to claim 2, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 19.9; about 22.0; about 25.2; about 28.2+/-0.5 degrees 2.theta. or a combination thereof.

9. The crystalline form according to claim 2, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 23.2; about 30.2; about 30.9; about 36.1+/-0.5 degrees 2.theta. or a combination thereof.

10. The crystalline form according to claim 1, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 13.0; about 17.3; about 19.9; about 22.0; and about 28.2+/-0.5 degrees 2.theta..

11. A crystalline form of trans-7-oxo-6-(sulphooxv)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide or a pharmaceutically acceptable salt thereof, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 13.0; about 16.5; about 17.3; about 17.5; about 19.2; about 19.5; about 19.9; about 22.0; about 22.3; about 23.2; about 25.2; about 28.2; about 30.2; about 30.9 and about 36.1+/-0.5 degrees 2.theta..

12. A crystalline form of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide or a pharmaceutically acceptable salt thereof, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a d-spacing value at about 5.1 and about 6.8+/-0.2 nm.

13. The crystalline form according to claim 12, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a d-spacing value at about 5.4+/-0.2 nm.

14. The crystalline form according to claim 12, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a d-spacing value at about 3.2; about 4.0; about 4.5; +/-0.2 nm or a combination thereof.

15. The crystalline form according to claim 12, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a d-spacing value at about 2.5; about 2.9; about 3.0; about 3.2; about 3.5; about 3.8; about 4.0; about 4.5; about 4.6; about 5.4; +/-0.2 nm or a combination thereof.

16. A crystalline form of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide or a pharmaceutically acceptable salt thereof, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a d-spacing value at about 2.5; about 2.9; about 3.0; about 3.2; about 3.5; about 3.8; about 4.0; about 4.5; about 4.6; about 5.1; about 5.4; and about 6.8+/-0.2 nm.

17. A crystalline form of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide or a pharmaceutically acceptable salt thereof, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 8.7; about 11.3; about 12.5; about 16.3; about 17.5; about 17.8; about 18.6; about 21.0; about 22.3; about 26.2; about 26.6; about 26.9; about 27.6; about 28.7; about 29.8; about 30.4; about 31.2; about 32.9; about 33.4; about 34.4; about 37.1; about 37.3; about 37.6 and about 38.5+/-0.5 degrees 2.theta..

18. A crystalline form of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide or a pharmaceutically acceptable salt thereof, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a d-spacing value at about 2.3; about 2.4; about 2.6; about 2.7; about 2.9; about 3.0; about 3.1; about 3.2; about 3.3; about 3.4; about 4.0; about 4.2; about 4.8; about 5.0; about 5.1; about 5.4; about 7.1; about 7.8 and about 10.1+/-0.2 nm.

19. A crystalline form of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide or a pharmaceutically acceptable salt thereof, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 8.5 and about 24.3+/-0.5degrees 2.theta..

20. The crystalline form according to claim 19, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 18.4; about 18.7; about 24.0; about 25.7; about 27.4; about 28.8; +/-0.5 degrees 2.theta. or a combination thereof.

21. A crystalline form of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide or a pharmaceutically acceptable salt thereof, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 17.8 and about 18.6+/-0.5 degrees 2.theta..

22. The crystalline form according to claim 21, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 8.7; about 11.3; about 12.5; about 16.3; about 21.1; about 27.0; about 26.6; about 28.7 or a combination thereof.

23. A crystalline form of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide or a pharmaceutically acceptable salt thereof, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 17.8 and about 18.6+/-0.5 degrees 2.theta..

24. The crystalline form according to claim 23, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 14.2; about 15.0; about 22.5; about 22.8; about 24.6; about 28.0+/-0.5 degrees 2.theta. or a combination thereof.

25. A crystalline form of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide or a pharmaceutically acceptable salt thereof, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 17.8 and about 18.6+/-0.5 degrees 2.theta..

26. The crystalline form according to claim 25, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a characteristic peak at about 14.4; about 15.5; about 19.3; +/-0.5 degrees 2.theta. or a combination thereof.

27. A crystalline form of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide or a pharmaceutically acceptable salt thereof, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a d-spacing value at about 3.7 and about 10.4+/-0.2 nm.

28. The crystalline form according to claim 27, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a d-spacing value at about 3.1; about 3.3; about 3.5; about 3.7; about 4.7; about 4.8; +/-0.2 nm or a combination thereof.

29. A crystalline form of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide or a pharmaceutically acceptable salt thereof, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a d-spacing value at about 4.8 and about 5.0+/-0.2 nm.

30. The crystalline form according to claim 29, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a d-spacing value at about 3.1; about 3.3; about 3.4; about 4.2; about 5.4; about 7.1; about 7.8; about 10.1+/-0.2 nm or a combination thereof.

31. A crystalline form of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide or a pharmaceutically acceptable salt thereof, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a d-spacing value at about 5.6 and about 9.0+/-0.2 nm.

32. The crystalline form according to claim 31, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a d-spacing value at about 3.2; about 3.6; about 3.9; about 4.0; about 5.9; about 6.2+/-0.2 nm or a combination thereof.

33. A crystalline form of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide or a pharmaceutically acceptable salt thereof, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a d-spacing value at about 4.9 and about 13.6+/-0.2 nm.

34. The crystalline form according to claim 33, wherein the crystalline form has an X-Ray powder diffraction pattern comprising a d-spacing value at about 4.6; about 5.7; about 6.1+/-0.2 nm or a combination thereof.
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