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Last Updated: March 29, 2024

Details for Patent: 9,139,530


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Title:Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide
Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.
Inventor(s): Hurter; Patricia (Harvard, MA), Rowe; William (Medford, MA), Young; Christopher R. (Waltham, MA), Costache; Adriana (Cambridge, MA), Connelly; Patrick R. (Harvard, MA), Krawiec; Mariusz (Marlborough, MA), Gong; Yuchuan (Waukegan, IL), Feng; Yushi (Zionsville, IN), Trudeau; Martin (Shannon, CA)
Assignee: Vertex Pharmaceuticals Incorporated (Boston, MA)
Filing Date:May 08, 2014
Application Number:14/272,692
Claims:1. A crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide, characterized as Form A, wherein the Form A is characterized by one or more peaks at 5.0 and 15.6 degrees in an X-ray powder diffraction pattern obtained using Cu K alpha radiation.

2. Form A of claim 1, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 7.8.

3. Form A of claim 2, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 8.5.

4. Form A of claim 3, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 9.2.

5. Form A of claim 4, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 9.9.

6. Form A of claim 5, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 11.9.

7. Form A of claim 6, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 12.6.

8. Form A of claim 7, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 13.9.

9. Form A of claim 8, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 14.9.

10. Form A of claim 9, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 16.5.

11. Form A of claim 10, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 18.1.

12. Form A of claim 11, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 18.5.

13. Form A of claim 12, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 20.7.

14. Form A of claim 13, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 22.0.

15. Form A of claim 14, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 23.5.

16. Form A of claim 15, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 25.3.

17. Form A of claim 16, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 28.0.

18. Form A of claim 17, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 29.4.

19. Form A of claim 18, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak 30.9.

20. A pharmaceutical composition comprising the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide according to claim 1, and a pharmaceutically acceptable adjuvant or carrier.

21. A process for preparing Form A of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide according to claim 1, wherein said process comprises the step of heating N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide to about 250.degree. C. and cooling to room temperature.

22. A method for treating a disease in a mammal comprising administering Form A of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-ox- oquinoline-3-carboxamide according to claim 1, wherein said disease is selected from cystic fibrosis, hereditary emphysema, COPD, and dry-eye disease.

23. The method of claim 22, wherein the Form A of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is in a pharmaceutical composition.

24. The method according to claim 22, wherein the method comprises administering an additional therapeutic agent.

25. A pharmaceutical pack or kit comprising Form A of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide according to claim 1 and a pharmaceutically acceptable carrier.

26. The method according to claim 22, wherein said disease is cystic fibrosis.

27. Form A of claim 1, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peaks: 9.9, 14.9, 18.1, and 28.0.

28. Form A of claim 27, wherein the crystal form of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide is further characterized by the following peak: 30.9.

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