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1. WO2021044327 - SOLID FORMS OF FILGOTINIB MALEATE AND PROCESSES THEREOF

Note: Text based on automatic Optical Character Recognition processes. Please use the PDF version for legal matters

[ EN ]

Claims

1. A crystalline Form FM1 of Filgotinib maleate, characterized by X-ray powder diffraction pattern comprising the peaks at 8.68, 16.84, 17.27, 19.51, 21.62, 23.27, 25.14 and 27.16 ± 0.2° 2Q.

2. The crystalline Form FM1 of Filgotinib maleate of claim 1, characterized by additional peaks at 17.82 and 18.77° 2Q.

3. The crystalline Form FM1 of claim 1, characterized by X-ray powder diffraction pattern as depicted in Figure 1.

4. A crystalline Form FM2 of Filgotinib maleate, characterized by X-ray powder diffraction pattern comprising the peaks at 9.31, 17.56, 26.33 ± 0.2° 2Q.

5. The crystalline Form FM2 of claim 4, characterized by additional peaks at 3.90, 7.86, 16.27 and 17.97° 2Q.

6. The crystalline Form FM2 of claim 4, characterized by X-ray powder diffraction pattern as depicted in Figure 2 or 4 or 6.

7. A crystalline Form FM3 of Filgotinib maleate, characterized by X-ray powder diffraction pattern comprising the peaks at 8.60, 16.68, 17.00, 19.37, 21.50, 23.57, 25.04 and 27.18 ± 0.2° 20.

8. The crystalline Form FM3 of claim 7, characterized by additional peaks at about 9.57, 17.86, 20.96 and 18.76° 20.

9. The crystalline Form FM3 of claim 7, characterized by X-ray powder diffraction pattern as depicted in Figure 3.

10. A process for the preparation of crystalline Form FM1 of Filgotinib maleate of claim 1, comprising the steps of combining Filgotinib with maleic acid in the presence of 1,4-dioxane and isolating crystalline Form FM1.

11. A process for the preparation of crystalline Form FM2 of Filgotinib maleate of claim 4, comprising the step of heating crystalline Form FM1 of Filgotinib maleate.

12. A process for the preparation of crystalline Form FM3 of Filgotinib maleate of claim 7, comprising the steps of combining Filgotinib maleate with anisole and isolating crystalline Form FM3.

13. A process for the preparation of crystalline Form FM2 of Filgotinib maleate of claim 4, comprising the step of heating crystalline Form FM3 of Filgotinib maleate.

14. A process for the preparation of pharmaceutical compositions comprising the step of using crystalline Filgotinib maleate selected from the group consisting of FM1, FM2, FM3 and mixtures thereof.