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Claims for Patent: 8,536,206

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Claims for Patent: 8,536,206

Title:Process for the preparation of roflumilast
Abstract: The invention relates to novel processes for the preparation of high-purity roflumilast.
Inventor(s): Kohl; Bernhard (Constance, DE), Mueller; Bernd (Constance, DE), Palosch; Walter (Rielasingen, DE)
Assignee: Takeda GmbH (Konstanz, DE)
Application Number:13/547,945
Patent Claims: 1. A method for the treatment of chronic obstructive pulmonary disease, comprising: administering to a patient suffering from chronic obstructive pulmonary disease N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide and a therapeutically effective amount of roflumilast.

2. The method of claim 1, wherein said roflumilast has a purity of greater than or equal to 99% by weight.

3. The method of claim 2, wherein said roflumilast has a purity of greater than or equal to 99.8% by weight.

4. The method of claim 1, wherein said N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide is present (relative to roflumilast) in an amount greater than zero and less than 0.1% by weight.

5. The method of claim 4, wherein said N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide is present (relative to roflumilast) in an amount greater than zero and less than 0.05% by weight.

6. A method for the treatment of chronic obstructive pulmonary disease, comprising: administering to a patient suffering from chronic obstructive pulmonary disease, a therapeutically effective amount of roflumilast having a purity of greater than or equal to 99% by weight, and N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide present (relative to roflumilast) in an amount greater than zero and less than 0.1% by weight.

7. The method of claim 6 wherein said roflumilast has a purity of greater than or equal to 99.8% by weight.

8. The method of claim 6, wherein said N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide is present (relative to roflumilast) in an amount greater than zero and less than 0.05% by weight.

9. A method for the treatment of chronic obstructive pulmonary disease, comprising: administering to a patient suffering from chronic obstructive pulmonary disease a therapeutically effective amount of a pharmaceutical composition, comprising: roflumilast; N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide; and pharmaceutically acceptable auxiliaries and/or excipients.

10. The method of claim 9, wherein said roflumilast has a purity of greater than or equal to 99% by weight.

11. The method of claim 10, wherein said roflumilast has a purity of greater than or equal to 99.8% by weight.

12. The method of claim 9, wherein said N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide is present (relative to roflumilast) in an amount greater than zero and less than 0.1% by weight.

13. The method of claim 12, wherein said N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide is present (relative to roflumilast) in an amount greater than zero and less than 0.05% by weight.

14. A method for the treatment of chronic obstructive pulmonary disease, comprising: administering to a patient suffering from chronic obstructive pulmonary disease, a therapeutically effective amount of a pharmaceutical composition, comprising: roflumilast having a purity of greater than or equal to 99% by weight; N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide present (relative to roflumilast) in an amount greater than zero and less than 0.1% by weight; and pharmaceutically acceptable auxiliaries and/or excipients.

15. The method of claim 14, wherein said roflumilast has a purity of greater than or equal to 99.8% by weight.

16. The method of claim 14, wherein said N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide is present (relative to roflumilast) in an amount greater than zero and less than 0.05% by weight.

17. A method for the treatment of chronic obstructive pulmonary disease, comprising: administering to a patient suffering from chronic obstructive pulmonary disease, a therapeutically effective amount of a pharmaceutical dosage form, comprising: roflumilast having a purity of greater than or equal to 99% by weight; N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide present (relative to roflumilast) in an amount greater than zero and less than 0.1% by weight; and pharmaceutically acceptable auxiliaries and/or excipients.

18. The method of claim 17, wherein said roflumilast has a purity of greater than or equal to 99.8% by weight.

19. The method of claim 17, wherein said N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide is present (relative to roflumilast) in an amount greater than zero and less than 0.05% by weight.

20. The method of claim 17, wherein said pharmaceutical dosage form is selected from the group consisting of tablets, coated tablets, capsules, caplets, suppositories, emulsions, suspensions, gels and solutions.

21. The method of claim 17, wherein said pharmaceutical dosage form includes from between 0.1% and 95% roflumilast.

22. The method of claim 17, wherein the pharmaceutical dosage form is an oral dosage form.

23. The method of claim 17, wherein the pharmaceutical dosage form contains from 0.05 mg to 2.5 mg of roflumilast.

24. The method of claim 23, wherein the pharmaceutical dosage form contains from 0.1 to 0.5 mg of roflumilast.

25. The method of claim 24, wherein the pharmaceutical dosage form contains 0.25 mg of roflumilast.

26. The method of claim 24, wherein the pharmaceutical dosage form contains 0.5 mg of roflumilast.

27. A method for the treatment of chronic obstructive pulmonary disease, comprising: administering to a patient suffering from chronic obstructive pulmonary disease, a therapeutically effective amount of a pharmaceutical tablet, comprising: 0.5 mg of roflumilast having a purity of greater than or equal to 99% by weight; N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide present (relative to roflumilast) in an amount less than 0.1% by weight; and pharmaceutically acceptable auxiliaries and/or excipients.

28. The method of claim 27, wherein said roflumilast has a purity of greater than or equal to 99.8% by weight.

29. The method of claim 27, wherein said N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide is present (relative to roflumilast) in an amount greater than zero and less than 0.05% by weight.
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