.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 9,139,530

« Back to Dashboard

Details for Patent: 9,139,530

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.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc