Claims for Patent: 11,970,500

Summary for Patent: 11,970,500

Title:	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
Abstract:	The present invention relates to a crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetr a-hydropyrazolo[1,5-a]pyrimi dine-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.
Inventor(s):	Zhiwei Wang, Yunhang Guo, Gongyin Shi, Lai Wang
Assignee:	BeiGene Switzerland GmbH
Application Number:	US18/526,535
Patent Claims:	1. A method for treating a B-cell proliferative disease in a subject, comprising administering to the subject in need thereof Compound 1, wherein the B-cell proliferative disease is selected from a group consisting of chronic lymphocytic leukemia, small lymphocytic lymphoma, mantle cell lymphoma, Waldenstrom's macroglobulinemia, marginal zone lymphoma, and follicular lymphoma; and Compound 1 is administrated at a dose of 320 mg once a day (QD). 2. The method of claim 1, wherein Compound 1 has a purity of at least 99.3%. 3. The method of claim 1, wherein Compound 1 has a purity of at least 99.5%. 4. The method of claim 3, wherein the B-cell proliferative disease is mantle cell lymphoma. 5. The method of claim 4, wherein the subject has received at least one prior therapy. 6. The method of claim 3, wherein the B-cell proliferative disease is Waldenström's macroglobulinemia. 7. The method of claim 3, wherein the B-cell proliferative disease is marginal zone lymphoma. 8. The method of claim 7, wherein the subject has received at least one prior therapy. 9. The method of claim 8, wherein the marginal zone lymphoma is relapsed or refractory marginal zone lymphoma. 10. The method of claim 3, wherein the B-cell proliferative disease is chronic lymphocytic leukemia. 11. The method of claim 3, wherein the B-cell proliferative disease is small lymphocytic lymphoma. 12. The method of claim 3, wherein the B-cell proliferative disease is follicular lymphoma. 13. The method of claim 3, wherein an amorphous form or a crystalline form of Compound 1 is administered. 14. The method of claim 13, wherein a crystalline form of Compound 1 is administered. 15. The method of claim 14, wherein the crystalline form exhibits an X-ray powder diffraction pattern comprising diffraction peaks having 20 angle values at 14.8±0.2°, 16.4±0.2° and 21.4±0.2°. 16. The method of claim 15, wherein the crystalline form exhibits an X-ray powder diffraction pattern comprising diffraction peaks having 20 angle values at 14.8±0.2°, 15.6±0.2°, 16.4±0.2° and 21.4±0.2°. 17. The method of claim 16, wherein the B-cell proliferative disease is mantle cell lymphoma, wherein the subject has received at least one prior therapy. 18. The method of claim 16, wherein the B-cell proliferative disease is Waldenström's macroglobulinemia. 19. The method of claim 16, wherein the B-cell proliferative disease is relapsed or refractory marginal zone lymphoma, wherein the subject has received at least one prior therapy. 20. The method of claim 16, wherein the B-cell proliferative disease is chronic lymphocytic leukemia or small lymphocytic lymphoma. 21. The method of claim 13, wherein an amorphous form of Compound 1 is administered. 22. The method of claim 21, wherein the amorphous form of Compound 1 has a mid-point temperature of a glass transition temperature at 79.7° C. 23. The method of claim 22, wherein the amorphous form has an enantiomeric excess value of at least 97%. 24. The method of claim 23, wherein the B-cell proliferative disease is mantle cell lymphoma, wherein the subject has received at least one prior therapy. 25. The method of claim 23, wherein the B-cell proliferative disease is Waldenström's macroglobulinemia. 26. The method of claim 23, wherein the B-cell proliferative disease is relapsed or refractory marginal zone lymphoma, wherein the subject has received at least one prior therapy. 27. The method of claim 23, wherein the B-cell proliferative disease is chronic lymphocytic leukemia or small lymphocytic lymphoma. 28. The method of claim 3, wherein Compound 1 is administered orally.