Crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra- hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
The present invention relates to a crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease.
1. A method for treating mantle cell lymphoma in a subject, comprising administering to the subject in need thereof a crystalline form of Compound 1,
wherein the crystalline form exhibits an X-ray powder diffraction pattern comprising diffraction peaks having 2θ angle values at 14.8±0.2°, 15.6±0.2°, 16.4±0.2°, and 21.4±0.2°.
2. The method of claim 1 , wherein the crystalline form of Compound 1 is administrated at a dose of 40 mg to 320 mg/day.
3. The method of claim 1 , wherein the crystalline form of Compound 1 is administered at a dose of 160 mg twice a day (BID).
4. The method of claim 1 , wherein the crystalline form of Compound 1 is administered at a dose of 320 mg once a day (QD).
5. The method of claim 1 , wherein the crystalline form is an anhydrate.
6. The method of claim 1 , wherein the crystalline form of Compound 1 has an Enantiomeric Excess value of greater than 97%.
7. The method of claim 1 , wherein the subject has received at least one prior therapy.
8. A method for treating Waldenström's macroglobulinemia in a subject, comprising administering to the subject in need thereof a crystalline form of Compound 1,
wherein the crystalline form exhibits an X-ray powder diffraction pattern comprising diffraction peaks having 2θ angle values at 14.8±0.2°, 15.6±0.2°, 16.4±0.2°, and 21.4±0.2°.
9. The method of claim 8 , wherein the crystalline form of Compound 1 is administrated at a dose of 40 mg to 320 mg/day.
10. The method of claim 8 , wherein the crystalline form of Compound 1 is administered at a dose of 160 mg twice a day (BID).
11. The method of claim 8 , wherein the crystalline form of Compound 1 is administered at a dose of 320 mg once a day (QD).
12. The method of claim 8 , wherein the crystalline form is an anhydrate.
13. The method of claim 8 , wherein the crystalline form of Compound 1 has an Enantiomeric Excess value of greater than 97%.
14. A method for treating marginal zone lymphoma in a subject, comprising administering to the subject in need thereof a crystalline form of Compound 1,
wherein the crystalline form exhibits an X-ray powder diffraction pattern comprising diffraction peaks having 2θ angle values at 14.8±0.2°, 15.6±0.2°, 16.4±0.2°, and 21.4±0.2°.
15. The method of claim 14 , wherein the crystalline form of Compound 1 is administrated at a dose of 40 mg to 320 mg/day.
16. The method of claim 14 , wherein the crystalline form of Compound 1 is administered at a dose of 160 mg twice a day (BID).
17. The method of claim 14 , wherein the crystalline form of Compound 1 is administered at a dose of 320 mg once a day (QD).
18. The method of claim 14 , wherein the crystalline form is an anhydrate.
19. The method of claim 14 , wherein the crystalline form of Compound 1 has an Enantiomeric Excess value of greater than 97%.
20. The method of claim 14 , wherein the subject has received at least one prior therapy.
21. A method for treating chronic lymphocytic leukemia or small lymphocytic lymphoma in a subject, comprising administering to the subject in need thereof a crystalline form of Compound 1,
wherein the crystalline form exhibits an X-ray powder diffraction pattern comprising diffraction peaks having 2θ angle values at 14.8±0.2°, 15.6±0.2°, 16.4±0.2° and 21.4±0.2°.
22. The method of claim 21 , wherein the crystalline form of Compound 1 is administrated at a dose of 40 mg to 320 mg/day.
23. The method of claim 21 , wherein the crystalline form of Compound 1 is administered at a dose of 160 mg twice a day (BID).
24. The method of claim 21 , wherein the crystalline form of Compound 1 is administered at a dose of 320 mg once a day (QD).
25. The method of claim 21 , wherein the crystalline form is an anhydrate.
26. The method of claim 21 , wherein the crystalline form of Compound 1 has an Enantiomeric Excess value of greater than 97%.
27. The method of claim 21 , wherein the subject has received at least one prior therapy.