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1. (WO2019041026) NOUVELLES FORMES CRISTALLINES D'ACALABRUTINIB
Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

What is claimed is:

1 . A crystalline form of Acalabrutinib that is a co-crystal of Acalabrutinib and urea.

2. The co-crystal of claim 1 , wherein the molar ratio of Acalabrutinib to urea is between approximately 1 : 1 and approximately 1 :3.

3. The co-crystal of claim 1 , wherein the molar ratio of Acalabrutinib to urea is approximately 1 :2.

4. A crystalline form of Acalabrutinib that is a co-crystal of Acalabrutinib and urea characterized by a PXRD diffractogram comprising peaks, expressed in degrees 2Θ (± 0.2°), at 5.4°, 7.3° and 10.0°.

5. The co-crystal of claim 4, further comprising at least three peaks, expressed in degrees 2Θ (± 0.2°), selected from the group consisting of: 10.4°, 1 1 .4°, 1 1 .8°, 12.8°, 15.3°, 17.0°, 18.4°, 20.1 °, 20.8° and 21 .3°.

6. The co-crystal of claim 4, further comprising peaks, expressed in degrees

2Θ (± 0.2°), at 10.4°, 1 1 .4°, 1 1 .8°, 12.8°, 15.3°, 17.0°, 18.4°, 20.1 °, 20.8° and 21 .3°.

7. The co-crystal of any one of claims 4 to 6, wherein the molar ratio of Acalabrutinib to urea is approximately 1 :2.

8. A crystalline form of Acalabrutinib that is a co-crystal of Acalabrutinib and nicotinamide.

9. The co-crystal of claim 8, wherein the molar ratio of Acalabrutinib to nicotinamide is between approximately 1 : 1 and approximately 1 :3.

10. The co-crystal of claim 8, wherein the molar ratio of Acalabrutinib to nicotinamide is approximately 1 :2.

1 1 . A crystalline form of Acalabrutinib that is a co-crystal of Acalabrutinib and nicotinamide characterized by a PXRD diffractogram comprising peaks, expressed in degrees 2Θ (± 0.2°), at 5.8°, 7.2° and 14.6°.

12. The co-crystal of claim 1 1 , further comprising at least three peaks, expressed in degrees 2Θ (± 0.2°), selected from the group consisting of: 9.2°,

10.2°, 1 1 .4°, 12.8°, 16.0°, 18.5°, 21 .1 °, 21 .9°, 23.4° and 24.1 °.

13. The co-crystal of claim 1 1 , further comprising peaks, expressed in degrees 2Θ (± 0.2°), at 9.2°, 10.2°, 1 1 .4°, 12.8°, 16.0°, 18.5°, 21 .1 °, 21 .9°, 23.4° and 24.1 °.

14. The co-crystal of any one of claims 1 1 to 13, wherein the molar ratio of

Acalabrutinib to nicotinamide is approximately 1 :2.

15. A crystalline form of Acalabrutinib that is a co-crystal of Acalabrutinib and L-sorbitol.

16. The co-crystal of claim 15, wherein the molar ratio of Acalabrutinib to L-sorbitol is between approximately 1 :0.5 and approximately 1 :2.

17. The co-crystal of claim 15, wherein the molar ratio of Acalabrutinib to L-sorbitol is approximately 1 : 1 .

18. A crystalline form of Acalabrutinib that is a co-crystal of Acalabrutinib and L-sorbitol characterized by a PXRD diffractogram comprising peaks, expressed in degrees 2Θ (± 0.2°), at 8.5°, 10.8° and 12.3°.

19. The co-crystal of claim 18, further comprising at least three peaks, expressed in degrees 2Θ (± 0.2°), selected from the group consisting of: 1 1 .6°, 12.8°, 13.4°, 14.1 °, 16.2°, 17.8° and 20.3°.

20. The co-crystal of claim 18, further comprising peaks, expressed degrees 2Θ (± 0.2°), at 1 1 .6°, 12.8°, 13.4°, 14.1 °, 16.2°, 17.8° and 20.3°.

21 . The co-crystal of any one of claims 18 to 20, wherein the molar ratio of Acalabrutinib to L-sorbitol is approximately 1 : 1.

22. A crystalline form of Acalabrutinib characterized by a PXRD diffractogram comprising peaks, expressed in degrees 2Θ (± 0.2°), at 7.5°, 10.9° and 12.6°.

23. The crystalline form of claim 22, further comprising at least three peaks, expressed in degrees 2Θ (± 0.2°), selected from the group consisting of: 13.9°, 14.8°, 17.2°, 18.1 °, 19.4°, 20.8°, 21 .7°, 22.6° and 24.3°.

24. The crystalline form of claim 22, further comprising peaks, expressed in degrees 2Θ (± 0.2°), at 13.9°, 14.8°, 17.2°, 18.1 °, 19.4°, 20.8°, 21 .7°, 22.6° and 24.3°.

25. A crystalline form of Acalabrutinib that is a co-crystal of Acalabrutinib and urea characterized by a PXRD diffractogram comprising peaks, expressed in degrees 2Θ (± 0.2°), at 5.4°, 6.6° and 1 1 .0°.

26. The co-crystal of claim 25, further comprising at least three peaks, expressed in degrees 2Θ (± 0.2°), selected from the group consisting of: 10.1 °, 13.2°, 15.1 °, 17.3°, 19.9°, 21 .1 ° and 22.2°.

27. The co-crystal of claim 25, further comprising peaks, expressed in degrees 2Θ (± 0.2°), at 10.1 °, 13.2°, 15.1 °, 17.3°, 19.9°, 21 .1 ° and 22.2°.

28. The co-crystal of any one of claims 25 to 27, wherein the molar ratio of Acalabrutinib to urea is approximately 1 :2.

29. The co-crystal of any one of claims 25 to 28, having a weight percentage of water of between approximately 2.0 wt% and approximately 4.0 wt%.

30. A pharmaceutical composition comprising the crystalline form of Acalabrutinib according to any one of claims 1 to 29, and one or more pharmaceutically acceptable excipients.

31 . The pharmaceutical composition of claim 30, wherein the pharmaceutical composition is a capsule.

32. The use of the crystalline form of Acalabrutinib according to any one of claims 1 to 29 in the treatment of a Bruton's Tyrosine Kinase (Btk) mediated disorder.

33. The use of claim 32, wherein the Bruton's Tyrosine Kinase (Btk) mediated disorder is lymphoma or leukemia.

34. The use of claim 33, wherein the lymphoma is mantle cell lymphoma (MCL).