Solid forms of an epidermal growth factor receptor kinase inhibitor
The present invention provides a solid form and compositions thereof, which are useful as an inhibitor of EGFR kinases and which exhibit desirable characteristics for the same.
1. A method of treating a proliferative disorder comprising administering to a patient in need thereof a solid form of Compound 1:
or a composition thereof.
2. The method of claim 1 , wherein the proliferative disorder is a cancer associated with a solid tumor.
3. The method of claim 2 , wherein the cancer associated with a solid tumor is selected from breast cancer, glioblastoma, lung cancer, cancer of the head and neck, colorectal cancer, bladder cancer, squamous cell carcinoma, salivary gland carcinoma, ovarian carcinoma, or pancreatic cancer.
4. The method of claim 2 , wherein the cancer associated with a solid tumor is a mutant EGFR-mediated cancer.
5. The method of claim 3 , wherein the cancer associated with a solid tumor is lung cancer.
6. The method of claim 5 , wherein the lung cancer is non-small cell lung cancer.
7. The method according to claim 1 , wherein the solid form of Compound 1 is crystalline.
8. The method according to claim 7 , wherein the solid form of Compound 1 is unsolvated.
9. The method according to claim 8 , wherein the solid form of Compound 1 is characterized by one or more peaks in its X-ray powder diffraction pattern selected from those at about 6.73, about 18.30, about 18.96 and about 25.48 degrees 2-theta.
10. The method according to claim 9 , wherein the solid form of Compound 1 is Form A.
11. The method according to claim 8 , wherein the solid form of Compound 1 is characterized by one or more peaks in its X-ray powder diffraction pattern selected from those at about 10.67, about 12.21, about 18.11, about 19.24 and about 21.53 degrees 2-theta.
12. The method according to claim 11 , wherein the solid form of Compound 1 is Form B.
13. The method according to claim 7 , wherein the solid form of Compound 1 is a dimethylformamide solvate.
14. The method according to claim 13 , wherein the solid form of Compound 1 is characterized by one or more peaks in its X-ray powder diffraction pattern selected from those at about 16.32, about 18.82, about 20.26, about 22.58 and about 25.36 degrees 2-theta.
15. The method according to claim 14 , wherein the solid form of Compound 1 is Form C.
16. The method according to claim 7 , wherein the solid form of Compound 1 is a 1,4-dioxane solvate.
17. The method according to claim 16 , wherein the solid form of Compound 1 is characterized by one or more peaks in its X-ray powder diffraction pattern selected from those at about 18.40, about 19.31, about 20.14, about 20.53 and about 25.25 degrees 2-theta.
18. The method according to claim 17 , wherein the solid form of Compound 1 is Form D.
19. The method according to claim 7 , wherein the solid form of Compound 1 is a methyl ethyl ketone solvate.
20. The method according to claim 19 , wherein the solid form of Compound 1 is characterized by one or more peaks in its X-ray powder diffraction pattern selected from those at about 5.78, about 12.57, about 15.34, about 19.10 and about 24.80 degrees 2-theta.
21. The method according to claim 20 , wherein the solid form of Compound 1 is Form E.
22. The method according to claim 7 , wherein the solid form of Compound 1 is a N-methyl-2-pyrrolidone solvate.
23. The method according to claim 22 , wherein the solid form of Compound 1 is characterized by one or more peaks in its X-ray powder diffraction pattern selected from those at about 15.51, about 16.86, about 18.80, about 20.97 and about 23.32 degrees 2-theta.
24. The method according to claim 23 , wherein the solid form of Compound 1 is Form F.
25. The method according to claim 22 , wherein the solid form of Compound 1 is characterized by one or more peaks in its X-ray powder diffraction pattern selected from those at about 6.79, about 17.86, about 19.43, about 19.98 and about 22.35 degrees 2-theta.
26. The method according to claim 25 , wherein the solid form of Compound 1 is Form G.
27. The method according to claim 7 , wherein the solid form of Compound 1 is a hydrate.
28. The method according to claim 27 , wherein the solid form of Compound 1 is characterized by one or more peaks in its X-ray powder diffraction pattern selected from those at about 10.82, about 11.08, about 18.45, about 22.85 and about 25.06 degrees 2-theta.
29. The method according to claim 28 , wherein the solid form of Compound 1 is Form H.
30. The method according to claim 27 , wherein the solid form of Compound 1 is characterized by one or more peaks in its X-ray powder diffraction pattern selected from those at about 6.13, about 12.22, about 15.91, about 18.35, about 18.88, and about 21.90 degrees 2-theta.
31. The method according to claim 30 , wherein the solid form of Compound 1 is Form I.