IP Library Granted Patent US 8,476,288
Granted Patent B2
US 8,476,288 · App. 12/784,226 · Granted Jul 2, 2013

Salts 756

Inventors: Nicholas James Bennett (Leicestershire, GB); Thomas McInally (Leicestershire, GB); Austen Pimm (Leicestershire, GB); Yoshiaki Isobe (Osaka, JP)
Assignees: AstraZeneca AB; Dainippon Sumitomo Pharma Co., Ltd.
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Quick Facts
Patent No.
US 8,476,288
App. No.
12/784,226
Granted
Jul 2, 2013
Kind
B2
Abstract

The invention provides salts of 4-(dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate, pharmaceutical compositions containing them and their use in therapy.

Claims (35)

1. Form A of 4-(dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate disaccharin salt, characterised in that said Form A has an X-ray powder diffraction pattern with specific peaks at 2θ about 9.2°, 13.9°, 14.9° or 15.2° when measured using CuKα radiation.

2. Form B of 4-(dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate disaccharin salt, characterised in that said Form B has an X-ray powder diffraction pattern with specific peaks at 2θ about=12.0°, 12.5°, 16.4° or 19.8° when measured using CuKα radiation.

3. 4-(Dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate difumaric acid salt, characterised in that said salt has an X-ray powder diffraction pattern with specific peaks at 2θ about =9.1°, 14.2°, 15.8° or 20.4° when measured using CuKα radiation.

4. 4-(Dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate di-1-hydroxy-2-naphthoic acid salt, characterised in that said salt has an X-ray powder diffraction pattern with specific peaks at 2θ about =8.3°, 16.6°, 19.4° or 23.4° when measured using CuKα radiation.

5. 4-(Dimethylamino)butyl 2-4-((2-amino-4-meth-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate mono-benzoic acid salt, characterised in that said salt has an X-ray powder diffraction pattern with specific peaks at 2θ about =6.3°, 9.3°, 17.8° or 23.8° when measured using CuKα radiation.

6. A pharmaceutical composition comprising a salt as claimed in claim 1 in association with a pharmaceutically acceptable adjuvant, diluent or carrier.

7. The pharmaceutical composition according to claim 6 , which is in a dry powder formulation suitable for inhalation therapy.

8. A dry powder inhaler containing a pharmaceutical composition as claimed in claim 7 .

9. The pharmaceutical composition according to claim 7 , comprising lactose monohydrate as a carrier.

10. The pharmaceutical composition according to claim 9 , wherein the lactose monohydrate is in particle form, wherein the particles have a mass median diameter of 20-1000 μm.

11. Form A of 4-(dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate disaccharin salt according to claim 1 , characterised in that said Form A has an X-ray powder diffraction pattern substantially as shown in FIG. 4 when measured using CuKα radiation.

12. Form B of 4-(dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate disaccharin salt according to claim 2 , characterised in that said Form B has an X-ray powder diffraction pattern substantially as shown in FIG. 5 when measured using CuKα radiation.

13. 4-(Dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate difumaric acid salt according to claim 3 , characterised in that said salt has an X-ray powder diffraction pattern substantially as shown in FIG. 19 when measured using CuKα radiation.

14. 4-(Dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate di-1-hydroxy-2-naphthoic acid salt according to claim 4 , characterised in that said salt has an X-ray powder diffraction pattern substantially as shown in FIG. 2 when measured using CuKα radiation.

15. 4-(Dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate mono-benzoic acid salt according to claim 5 , characterised in that said salt has an X-ray powder diffraction pattern substantially as shown in FIG. 1 when measured using CuKα radiation.

16. A pharmaceutical composition comprising a salt as claimed in claim 2 in association with a pharmaceutically acceptable adjuvant, diluent or carrier.

17. The pharmaceutical composition according to claim 16 , which is in a dry powder formulation suitable for inhalation therapy.

18. A dry powder inhaler containing a pharmaceutical composition as claimed in claim 17 .

19. The pharmaceutical composition according to claim 17 , comprising lactose monohydrate as a carrier.

20. The pharmaceutical composition according to claim 19 , wherein the lactose monohydrate is in particle form wherein the particles have a mass median diameter of 20-1000 μm.

21. A pharmaceutical composition comprising a salt as claimed in claim 3 in association with a pharmaceutically acceptable adjuvant, diluent or carrier.

22. The pharmaceutical composition according to claim 21 , which is a dry powder formulation suitable for inhalation therapy.

23. A dry powder inhaler containing a pharmaceutical composition as claimed in claim 22 .

24. The pharmaceutical composition according to claim 22 , comprising lactose monohydrate as a carrier.

25. The pharmaceutical composition according to claim 24 , wherein the lactose monohydrate is in particle form wherein the particles have a mass median diameter of 20-1000 μm.

26. A pharmaceutical composition comprising a salt as claimed in claim 4 in association with a pharmaceutically acceptable adjuvant, diluent or carrier.

27. The pharmaceutical composition according to claim 26 , which is in a dry powder formulation suitable for inhalation therapy.

28. A dry powder inhaler containing a pharmaceutical composition as claimed in claim 27 .

29. The pharmaceutical composition according to claim 27 , comprising lactose monohydrate as a carrier.

30. The pharmaceutical composition according to claim 29 , wherein the lactose monohydrate is in particle form wherein the particles have a mass median diameter of 20-1000 μm.

31. A pharmaceutical composition comprising a salt as claimed in claim 5 in association with a pharmaceutically acceptable adjuvant, diluent or carrier.

32. The pharmaceutical composition according to claim 31 , which is in a dry powder formulation suitable for inhalation therapy.

33. A dry powder inhaler containing a pharmaceutical composition as claimed in claim 32 .

34. The pharmaceutical composition according to claim 32 , comprising lactose monohydrate as a carrier.

35. The pharmaceutical composition according to claim 34 , wherein the lactose monohydrate is in particle form wherein the particles have a mass median diameter of 20-1000 μm.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 28, 2011
From: BENNETT, NICHOLAS JAMES; MCINALLY, THOMAS; PIMM, AUSTEN; THOM, STEPHEN; ISOBE, YOSHIAKI
To: ASTRAZENECA AB; DAINIPPON SUMITOMO PHARMA CO., LTD.
Reel/Frame 026513/0651 →
Priority Claims (1)
GB 0908772.7 · May 21, 2009 · national
Continuity (1)
Related Publication 20100298364A1 · Nov 25, 2010