Forms of methyl {4,6-diamino-2-[1 (2-fluorobenzyl)-1h-pyrazolo[3-4-b]pyridino-3-yl]pyrimidino-5-yl}methyl carbamate
View Patent ↗This present invention relates to forms of methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridino-3-yl]pyrimidino-5-yl}methylcarbamate comprising its Modification I, Modification II, mono-DMSO solvate, sesqui-DMSO solvate and ¼-ethyl acetate solvate.
1. A compound of the formula (I)
in the form of Modification II or as sesqui-DMSO solvate, wherein
the Modification II is characterized by an X-Ray powder diffractogram comprising peak maxima of the 2 Theta angle of 11.2, 12.6, 12.7, 13.9, 15.2, 17.3, 22.5, 22.8, 25.0, 25.5, and
the sesqui-DMSO solvate is characterized by an X-Ray powder diffractogram comprising peak maxima of the 2 Theta angle of 8.3, 8.4, 13.7, 13.9, 15.7, 17.2, 18.4, 19.6, 21.4, 24.9.
2. The compound of claim 1 in the form of Modification II.
3. The compound of claim 1 as sesqui-DMSO solvate.
4. A pharmaceutical composition comprising the compound of the formula (I)
in the form of Modification II or as sesqui-DMSO solvate, and a pharmaceutically acceptable carrier, wherein
the Modification II is characterized by an X-Ray powder diffractogram comprising peak maxima of the 2 Theta angle of 11.2, 12.6, 12.7, 13.9, 15.2, 17.3, 22.5, 22.8, 25.0, 25.5, and
the sesqui-DMSO solvate is characterized by an X-Ray powder diffractogram comprising peak maxima of the 2 Theta angle of 8.3, 8.4, 13.7, 13.9, 15.7, 17.2, 18.4, 19.6, 21.4, 24.9.
5. The pharmaceutical composition of claim 4 , wherein the pharmaceutical composition comprises a mixture of the compound of the formula (I) in the form of Modification II and as sesqui-DMSO solvate.
6. The pharmaceutical composition of claim 4 , wherein the pharmaceutical composition comprises a mixture of the compound of the formula (I) in the form of Modification II and/or as sesqui-DMSO solvate, and one or more forms of the compound of formula (I) selected from the group consisting of the Modification I, mono-DMSO solvate, ¼ ethyl acetate solvate and the amorphous form, wherein
the Modification I is characterized by an X-Ray powder diffractogram comprising peak maxima of the 2 Theta angle of 6.7, 9.1, 14.3, 14.4, 17.8, 19.8, 20.2, 24.8, 25.6, 27.3,
the mono-DMSO solvate is characterized by an X-Ray powder diffractogram comprising peak maxima of the 2 Theta angle of 9.0, 10.8, 11.1, 11.2, 13.0, 15.5, 15.9, 16.0, 20.7, 25.6,
and
the ¼ ethyl acetate solvate is characterized by an X-Ray powder diffractogram comprising peak maxima of the 2 Theta angle of 6.7, 8.3, 8.7, 12.9, 14.2, 17.8, 19.3, 24.0, 25.1, 26.7.
7. The pharmaceutical composition of claim 4 comprising only one of the forms of the compound of the formula (I) selected from the group consisting of Modification II and sesqui-DMSO solvate.
8. The pharmaceutical composition of claim 4 comprising Modification II of the compound of the formula (I), wherein the pharmaceutical composition does not contain Modification I, mono-DMSO solvate, sesqui-DMSO solvate, or ¼ ethyl acetate solvate forms of the compound of formula (I).
9. The pharmaceutical composition of claim 4 comprising Modification II of the compound of the formula (I) mainly and no significant fractions of another form of the compound of the formula (I).
10. The pharmaceutical composition of claim 4 comprising the sesqui-DMSO solvate of the compound of the formula (I), wherein the pharmaceutical composition does not contain Modification I, mono-DMSO solvate, Modification II, or ¼ ethyl acetate solvate forms of the compound of formula (I).
11. The pharmaceutical composition of claim 4 comprising the sesqui-DMSO solvate of the compound of the formula (I) mainly and no significant fractions of another form of the compound of the formula (I).
12. The pharmaceutical composition of claim 6 comprising the compound of formula (I) in the Modification I and the compound of formula (I) in the Modification II.
13. The pharmaceutical composition of claim 6 comprising the compound of formula (I) in the Modification I and the compound of formula (I) in the Modification II and no other form of the compound of the formula (I).
14. The pharmaceutical composition of claim 6 comprising the compound of formula (I) in the Modification I and the compound of formula (I) as the sesqui-DMSO solvate.
15. The pharmaceutical composition of claim 6 comprising the compound of formula (I) in the Modification I and the compound of formula (I) as the sesqui-DMSO solvate and no other form of the compound of the formula (I).
16. The pharmaceutical composition of claim 4 formulated for oral administration.
17. A method for the treatment and/or prophylaxis of cardiovascular, pulmonary, thromboembolic and fibrotic diseases comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 4 to a patient in need thereof.
18. A method for the treatment and/or prophylaxis of cardiovascular, pulmonary, thromboembolic and fibrotic diseases comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 5 to a patient in need thereof.
19. A method for the treatment and/or prophylaxis of cardiovascular, pulmonary, thromboembolic and fibrotic diseases comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 6 to a patient in need thereof.
20. A method for the treatment and/or prophylaxis of cardiovascular, pulmonary, thromboembolic and fibrotic diseases comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 7 to a patient in need thereof.
21. A method for the treatment and/or prophylaxis of cardiovascular, pulmonary, thromboembolic and fibrotic diseases comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 8 to a patient in need thereof.
22. A method for the treatment and/or prophylaxis of cardiovascular, pulmonary, thromboembolic and fibrotic diseases comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 9 to a patient in need thereof.
23. A method for the treatment and/or prophylaxis of cardiovascular, pulmonary, thromboembolic and fibrotic diseases comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 10 to a patient in need thereof.
24. A method for the treatment and/or prophylaxis of cardiovascular, pulmonary, thromboembolic and fibrotic diseases comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 11 to a patient in need thereof.
25. A method for the treatment and/or prophylaxis of cardiovascular, pulmonary, thromboembolic and fibrotic diseases comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 12 to a patient in need thereof.
26. A method for the treatment and/or prophylaxis of cardiovascular, pulmonary, thromboembolic and fibrotic diseases comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 13 to a patient in need thereof.
27. A method for the treatment and/or prophylaxis of cardiovascular, pulmonary, thromboembolic and fibrotic diseases comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 14 to a patient in need thereof.
28. A method for the treatment and/or prophylaxis of cardiovascular, pulmonary, thromboembolic and fibrotic diseases comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 15 to a patient in need thereof.
29. A method for the treatment and/or prophylaxis of cardiovascular, pulmonary, thromboembolic and fibrotic diseases comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 16 to a patient in need thereof.
30. The method for the treatment and/or prophylaxis of cardiovascular, pulmonary, thromboembolic and fibrotic diseases of any one of claims 17 - 29 , wherein the pharmaceutical composition is administered one or more times per day.