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Last Updated: April 25, 2024

Claims for Patent: 10,385,078


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Summary for Patent: 10,385,078
Title:Crystalline forms of 5-chloro-N4-[-2-(dimethylphosphoryl)phenyl]-N2-{2-methoxy-4-[4-(4-methylp- iperazin-1-YL) piperidin-1-YL]phenyl}pyrimidine-2,4-diamine
Abstract: Crystalline forms of brigatinib, pharmaceutical compositions comprising the same, and methods of their preparation and use of the same are disclosed herein.
Inventor(s): Rozamus; Leonard W. (Andover, MA), Sharma; Pradeep (Westford, MA)
Assignee: ARIAD PHARMACEUTICALS, INC. (Cambridge, MA)
Application Number:15/520,694
Patent Claims: 1. Crystalline form A of brigatinib having the structure: ##STR00033## wherein the crystalline form has an x-ray powder diffraction pattern with peaks at 9.6, 17.2, 19.4, 20.1, 23.1, and 27.7.degree.2.theta., with a variance of .+-.0.2.degree.2.theta..

2. The crystalline form of claim 1, having an x-ray powder diffraction pattern as shown in FIG. 2.

3. The crystalline form of claim 1, having an x-ray powder diffraction pattern with peaks at 6.1, 8.6, 9.6, 10.8, 11.3, 13.5, 14.3, 15.9, 17.2, 18.9, 19.4, 20.1, 21.8, 22.6, 23.1, 23.9, and 27.7.degree.2.theta., with a variance of .+-.0.2.degree.2.theta..

4. A pharmaceutical composition comprising the crystalline form of brigatinib of claim 1 and at least one component chosen from pharmaceutically acceptable carriers, pharmaceutically acceptable vehicles, and pharmaceutically acceptable excipients.

5. A method for treating non-small cell lung cancer in a subject in need thereof comprising administering to the subject the crystalline form of brigatinib of claim 1.

6. The method of claim 5, wherein the non-small cell lung cancer is ALK-positive non-small cell lung cancer.

7. The method of claim 6, wherein the non-small cell lung cancer is ALK-positive metastatic non-small cell lung cancer.

8. The method of claim 7, wherein the subject has been previously treated with crizotinib.

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