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Claims for Patent: 7,265,124

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Claims for Patent: 7,265,124

Title:Cristalline and amorphous form of a triazolo (4,5-D) pyridimine compound
Abstract: The invention provides new forms of a chemical compound of formula (I). The invention relates to forms of a chemical compound (I), in particular to crystalline and amorphous forms, more particularly four crystalline forms and an amorphous form. The invention further relates to processes for the preparation of such forms, to pharmaceutical compositions comprising the compound in crystalline and/or amorphous form and to therapeutic use of such forms.
Inventor(s): Bohlin; Martin (Sodertalje, SE), Cosgrove; Steve (Loughborough, GB), Lassen; Bo (Sodertalje, SE)
Assignee: AstraZeneca AB (Sodertalje, SE)
Application Number:11/240,801
Patent Claims: 1. A compound of formula (I): ##STR00002## selected from: a compound of formula (I) characterised by an X-ray powder diffraction pattern containing specific peaks of high intensity at 5.3.degree. (.+-.0.1.degree.), 20.1.degree. (.+-.0.1.degree.), 20.7.degree. (.+-.0.1.degree.), 21.0.degree. (.+-.0.1.degree. ) and 21.3.degree. (.+-.0.1.degree.) 2.theta.; a compound of formula (I) characterised by an X-ray powder diffraction pattern containing specific peaks of high intensity at 5.5.degree. (.+-.0.1.degree.), 13.5.degree. (.+-.0.1.degree.), 18.3.degree. (.+-.0.1.degree.), 22.7.degree. (.+-.0.1.degree.) and 24.3.degree. (.+-.0.1.degree.) 2.theta.; a compound of formula (I) characterised by an X-ray powder diffraction pattern containing specific peaks of high intensity at 14.0.degree. (.+-.0.1.degree.), 17.4.degree. (.+-.0.1.degree.), 18.4.degree. (.+-.0.1.degree.), 21.4.degree. (.+-.0.1.degree.) and 24.1.degree. (.+-.0.1.degree.) 2.theta.; and a compound of formula (I) characterised by an X-ray powder diffraction pattern containing specific peaks of high intensity at 4.9.degree. (.+-.0.1.degree.), 9.2.degree. (.+-.0.1.degree.), 11.6.degree. (.+-.0.1.degree.), 15.6.degree. (.+-.0.1.degree.) and 16.4.degree. (.+-.0.1.degree.) 2.theta..

2. A compound of formula (I) as claimed in claim 1 that exists in an anhydrous form.

3. A compound of formula (I) as claimed in claim 1 characterised by an X-ray powder diffraction pattern containing specific peaks at 5.3.degree. (.+-.0.1.degree.), 8.0.degree. (.+-.0.1.degree.), 9.6.degree. (.+-.0.1.degree.), 13.9.degree. (.+-.0.1.degree.), 15.3.degree. (.+-.0.1.degree.), 20.1.degree. (.+-.0.1.degree.), 20.7.degree. (.+-.0.1.degree.), 21.0.degree. (0.1.degree.), 21.3.degree. (.+-.0.1.degree.), 26.2.degree. (.+-.0.1.degree.) and 27.5.degree. (.+-.0.1.degree.) 2.theta..

4. A compound of formula (I) as claimed in claim 1 characterised by a differential scanning calorimetry curve to have an onset of melting which is in the range 146-152.degree. C.

5. A compound of formula (I) as claimed in claim 1 characterised by an X-ray powder diffraction pattern containing specific peaks at 5.5.degree. (.+-.0.1.degree.), 6.8.degree. (.+-.0.1.degree.), 10.6.degree. (.+-.0.1.degree.), 13.5.degree. (.+-.0.1.degree.), 14.9.degree. (.+-.0.1.degree.), 18.3.degree. (.+-.0.1.degree.), 19.2.degree. (.+-.0.1.degree.), 22.7.degree. (.+-.0.1.degree.), 24.3.degree. (.+-.0.1.degree.) and 27.1.degree. (0.1.degree.) 2.theta..

6. A compound of formula (I) as claimed in claim 1 characterised by a differential scanning calorimetry curve to have an onset of melting which is in the range of 136-139.degree. C.

7. A compound of formula (I) as claimed in claim 1 characterised by an X-ray powder diffraction pattern containing specific peaks at 5.6.degree. (.+-.0.1.degree.), 12.5.degree. (.+-.0.1.degree.), 14.0.degree. (.+-.0.1.degree.), 17.4.degree. (.+-.0.1.degree.), 18.4.degree. (.+-.0.1.degree.), 21.4.degree. (.+-.0.1.degree.), 22.2.degree. (.+-.0.1.degree.), 22.9.degree. (.+-.0.1.degree.), 24.1.degree. (.+-.0.1.degree.) and 24.5.degree. (.+-.0.1.degree.) 2.theta..

8. A compound of formula (I) as claimed in claim 1 characterised by a differential scanning calorimetry curve to have an onset of melting which is in the range 127-132.degree. C.

9. A compound of formula (I) as claimed in claim 1 characterised by an X-ray powder diffraction pattern containing specific peaks at 4.9.degree. (.+-.0.1.degree.), 6.0.degree. (.+-.0.1.degree.), 9.2.degree. (.+-.0.1.degree.), 11.6.degree. (.+-.0.1.degree.), 12.8.degree. (.+-.0.1.degree.), 15.6.degree. (.+-.0.1.degree.), 16.4.degree. (.+-.0.1.degree.), 17.2.degree. (.+-.0.1.degree.) and 18.1.degree. (.+-.0.1.degree.) 2.theta..

10. A compound of formula (I) as claimed in claim 1 characterised by a differential scanning calorimetry curve to have an onset of melting which at approximately 139.degree. C.

11. A process for the preparation of a compound as claimed in claim 1, comprising crystallizing a compound of formula (I) from a solvent selected from the group consisting of a lower alkyl acetate, a lower alkyl alcohol, an aliphatic hydrocarbon, an aromatic hydrocarbon, a dialkyl ether, a dialkyl ketone, acetonitrile, water, and a mixture thereof.

12. A process as claimed in claim 11, wherein the solvent in selected from the group consisting of ethanol, ethyl acetate, iso-propanol, iso-octane, acetonitrile, water, and a mixture thereof.

13. A process as claimed in claim 12 wherein the solvent is selected from the group consisting of a mixture of methanol and water, ethanol, ethyl acetate, a mixture of ethanol and water, a mixture of iso-propanol and water, a mixture of ethyl acetate and iso-octane, and acetonitrile.

14. A process for the production of a compound of formula (I) as claimed in claim 1, characterised by an X-ray powder diffraction pattern containing specific peaks at 5.3.degree. (.+-.0.1.degree.), 20.1.degree. (.+-.0.1.degree.), 20.7.degree. (.+-.0.1.degree.), 21.0.degree. (.+-.0.1.degree.) and 21.3.degree. (.+-.0.1.degree.) 2.theta., comprising crystallizing the compound of formula (I) from a mixture of methanol and water.

15. A process as claimed in claim 14 which includes the step of using a seed.

16. A process according to claim 15 in which the seed is prepared by melting a compound of formula (I): ##STR00003## characterised by an X-ray powder diffraction pattern containing specific peaks of high intensity at 5.3.degree. (.+-.0.1.degree.), 8.0.degree. (0.1.degree.), 9.6.degree. (.+-.0.1.degree.), 13.9.degree. (.+-.0.1.degree.), 15.3.degree. (.+-.0.1.degree.), 20.1.degree. (.+-.0.1.degree.), 20.7.degree. (.+-.0.1.degree.), 21.0.degree. (.+-.0.1.degree.), 21.3.degree. (.+-.0.1.degree.), 26.2.degree. (.+-.0.1.degree.) and 27.5.degree. (.+-.0.1.degree.) 2.theta..

17. A process for the production of a compound of formula (I) as claimed in claim 1, characterised by an X-ray powder diffraction pattern containing specific peaks of high intensity at 14.0.degree. (.+-.0.1.degree.), 17.4.degree. (.+-.0.1.degree.), 18.4.degree. (.+-.0.1.degree.), 21.4.degree. (.+-.0.1.degree.) and 24.1.degree. (.+-.0.1.degree.) 2.theta., comprising crystallizing the compound of formula (I) from an alcohol.

18. A process for the production of a compound of formula (I) as claimed in claim 1, characterised by an X-ray powder diffraction pattern containing specific peaks of high intensity at 5.5.degree. (.+-.0.1.degree.), 13.5.degree. (.+-.0.1.degree.), 18.3.degree. (.+-.0.1.degree.), 22.7.degree. (.+-.0.1.degree.) and 24.3.degree.(.+-.0.1.degree.) 2.theta., comprising crystallizing the compound of formula (I) from a solvent selected from the group consisting of ethyl acetate and chloroform.

19. A process for the production of a compound of formula (I) as claimed in claim 1, characterised by an X-ray powder diffraction pattern containing specific peaks of high intensity at 14.0.degree. (.+-.0.1.degree.), 17.4.degree.(.+-.0.1.degree.), 18.4.degree. (.+-.0.1.degree.), 21.4.degree. (.+-.0.1.degree.) and 24.1.degree.(.+-.0.1.degree.) 2.theta., comprising slurrying a compound of formula (I) in an IPA/water solvent system at a temperature of 5 to 65.degree. C.

20. A process for the production of a compound of formula (I) as claimed in claim 1, characterised by an X-ray powder diffraction pattern containing specific peaks of high intensity at 4.9.degree. (.+-.0.1.degree.), 9.2.degree. (.+-.0.1.degree.), 11.6.degree. (.+-.0.1.degree.), 15.6.degree. (.+-.0.1.degree.) and 16.4.degree. (.+-.0.1.degree.) 2.theta., comprising crystallizing the compound of formula (I) from acetonitrile.

21. A pharmaceutical composition comprising a compound as claimed in claim 1 in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier.

22. A method of treatment of arterial thrombotic complications selected from the group consisting of unstable angina, thrombotic or embolic stroke, transient ischaemic attacks, peripheral vascular disease and myocardial infarction in patients with coronary artery, cerebrovascular or peripheral vascular disease, which comprises administering to a person suffering from such a disorder a therapeutically effective amount of a compound as claimed in claim 1.

23. A method of treatment of arterial thrombotic complications selected from the group consisting of unstable angina, thrombotic or embolic stroke, transient ischaemic attacks, peripheral vascular disease and myocardial infarction in patients with coronary artery, cerebrovascular or peripheral vascular disease, which comprises administering to a person suffering from such a disorder a therapeutically effective amount of a compound as claimed in claim 3.

24. A method of treatment of arterial thrombotic complications selected from the group consisting of unstable angina, thrombotic or embolic stroke, transient ischaemic attacks, peripheral vascular disease and myocardial infarction in patents with coronary artery, cerebrovascular or peripheral vascular disease, which comprises administering to a person suffering from such a disorder a therapeutically effective amount of a compound as claimed in claim 5.

25. A method of treatment of arterial thrombotic complications selected from the group consisting of unstable angina, thrombotic or embolic stroke, transient ischaemic attacks, peripheral vascular disease and myocardial infarction in patients with coronary artery, cerebrovascular or peripheral vascular disease, which comprises administering to a person suffering from such a disorder a therapeutically effective amount of a compound as claimed in claim 7.

26. A method of treatment of arterial thrombotic complications selected from the group consisting of unstable angina, thrombotic or embolic stroke, transient ischaemic attacks, peripheral vascular disease and myocardial infarction in patients with coronary artery, cerebrovascular or peripheral vascular disease, which comprises administering to a person suffering from such a disorder a therapeutically effective amount of a compound as claimed in claim 9.

27. A method of treatment of an arterial thrombotic complication in a patient with coronary artery, cerebrovascular or peripheral vascular disease, which comprises administering to a person suffering from such a disorder a therapeutically effective amount of a compound as claimed in claim 1, wherein the arterial thrombotic complication is an arterial complication due to angioplasty, endarterectomy, stent placement, vascular graft surgery and thrombotic complications of surgical or mechanical damage.

28. A method of treatment of an arterial thrombotic complication in a patient with coronary artery, cerebrovascular or peripheral vascular disease, which comprises administering to a person suffering from such a disorder a therapeutically effective amount of a compound as claimed in claim 3, wherein the arterial thrombotic complication is an arterial complication due to angioplasty, endarterectomy, stent placement, vascular graft surgery and thrombotic complications of surgical or mechanical damage.

29. A method of treatment of an arterial thrombotic complication in a patient with coronary artery, cerebrovascular or peripheral vascular disease, which comprises administering to a person suffering from such a disorder a therapeutically effective amount of a compound as claimed in claim 5, wherein the arterial thrombotic complication is an arterial complication due to angioplasty, endarterectomy, stent placement, vascular graft surgery and thrombotic complications of surgical or mechanical damage.

30. A method of treatment of an arterial thrombotic complication in a patient with coronary artery, cerebrovascular or peripheral vascular disease, which comprises administering to a person suffering from such a disorder a therapeutically effective amount of a compound as claimed in claim 7, wherein the arterial thrombotic complication is an arterial complication due to angioplasty, endarterectomy, stent placement, vascular graft surgery and thrombotic complications of surgical or mechanical damage.

31. A method of treatment of an arterial thrombotic complication in a patient with coronary artery, cerebrovascular or peripheral vascular disease, which comprises administering to a person suffering from such a disorder a therapeutically effective amount of a compound as claimed in claim 9, wherein the arterial thrombotic complication is an arterial complication due to angioplasty, endarterectomy, stent placement, vascular graft surgery and thrombotic complications of surgical or mechanical damage.
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