Process for the preparation of roflumilast
View Patent ↗A method for the treatment of chronic obstructive pulmonary disease (COPD), including administering to a patient suffering from COPD, 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.
1. A method for the treatment of an acute or chronic airway disorder comprising: administering to a patient suffering from an acute or chronic airway disorder, 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.
2. The method of claim 1 , wherein said roflumilast has a purity of greater than or equal to 99.8% by weight.
3. 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 0.05% by weight.
4. A method for the treatment of an acute or chronic airway disorder comprising: administering to a patient suffering from an acute or chronic airway disorder, 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.
5. The method of claim 4 , wherein said roflumilast has a purity of greater than or equal to 99.8% by weight.
6. 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.
7. A method for the treatment of an acute or chronic airway disorder comprising: administering to a patient suffering from an acute or chronic airway disorder, 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.
8. The method of claim 7 , wherein said roflumilast has a purity of greater than or equal to 99.8% by weight.
9. The method of claim 7 , 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.
10. The method of claim 7 , wherein said pharmaceutical dosage form is selected from the group consisting of tablets, coated tablets, capsules, caplets, suppositories, emulsions, suspensions, gels and solutions.
11. The method of claim 7 , wherein said pharmaceutical dosage form includes from between 0.1% and 95% roflumilast.
12. The method of claim 7 , wherein the pharmaceutical dosage form is an oral dosage form.
13. The method of claim 7 , wherein the pharmaceutical dosage form contains from 0.05 mg to 2.5 mg of roflumilast.
14. The method of claim 13 , wherein the pharmaceutical dosage form contains from 0.1 to 0.5 mg of roflumilast.
15. The method of claim 14 , wherein the pharmaceutical dosage form contains 0.25 mg of roflumilast.
16. The method of claim 14 , wherein the pharmaceutical dosage form contains 0.5 mg of roflumilast.
17. A method for the treatment of an acute or chronic airway disorder comprising: administering to a patient suffering from an acute or chronic airway disorder, 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.
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 1 , wherein said disorder is selected from the group consisting of asthma, bronchitis, allergic rhinitis, emphysema and chronic obstructive pulmonary disease.
21. The method of claim 4 , wherein said disorder is selected from the group consisting of asthma, bronchitis, allergic rhinitis, emphysema and chronic obstructive pulmonary disease.
22. The method of claim 7 , wherein said disorder is selected from the group consisting of asthma, bronchitis, allergic rhinitis, emphysema and chronic obstructive pulmonary disease.
23. The method of claim 17 , wherein said disorder is selected from the group consisting of asthma, bronchitis, allergic rhinitis, emphysema and chronic obstructive pulmonary disease.