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Claims for Patent: 9,173,881

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Claims for Patent: 9,173,881

Title:Therapeutic compositions containing macitentan
Abstract: The invention relates to a product containing the compound of formula (I) below or a pharmaceutically acceptable salt of this compound, in combination of at least one compound having prostacyclin receptor (IP) agonist properties, or a pharmaceutically acceptable salt thereof. ##STR00001##
Inventor(s): Clozel; Martine (Binningen, CH)
Assignee: ACTELION PHARMACEUTICALS LTD. (Allschwil, CH)
Application Number:14/335,657
Patent Claims: 1. A method for the treatment of a disease selected from hypertension, pulmonary hypertension, diabetic arteriopathy, heart failure, erectile dysfunction, angina pectoris and pulmonary fibrosis, comprising administering an effective amount of the compound of formula (I) ##STR00003## in free or pharmaceutically acceptable salt form, in combination with an effective amount of at least one compound having prostacyclin receptor (IP) agonist properties selected from 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfony- l)acetamide and {4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}acetic acid, in free or pharmaceutically acceptable salt form.

2. The method according to claim 1, wherein the compound having prostacyclin receptor (IP) agonist properties is {4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}acetic acid, in free or pharmaceutically acceptable salt form.

3. The method according to claim 1, wherein the compound having prostacyclin receptor (IP) agonist properties is 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfony- l)acetamide, in free or pharmaceutically acceptable salt form.

4. The method according to claim 1, wherein the compound of formula (I) and the compound having prostacyclin receptor (IP) agonist properties are administered simultaneously, separately or over a period of time.

5. The method according to claim 1, wherein the disease is pulmonary hypertension.

6. The method according to claim 1, wherein the disease is pulmonary arterial hypertension.

7. The method according to claim 6, wherein the compound of formula (I) is in free form.

8. The method according to claim 7, wherein the compound of formula (I) and the compound having prostacyclin receptor (IP) agonist properties are administered simultaneously.

9. The method according to claim 7, wherein the compound of formula (I) and the compound having prostacyclin receptor (IP) agonist properties are administered separately.

10. The method according to claim 7, wherein the compound of formula (I) and the compound having prostacyclin receptor (IP) agonist properties are administered over a period of time.

11. The method according to claim 6, wherein the compound of formula (I) and the prostacyclin receptor (IP) agonist are administered orally.

12. The method according to claim 1, wherein the compound of formula (I) and the prostacyclin receptor (IP) agonist are administered orally.

13. A method for the treatment of pulmonary arterial hypertension comprising administering an effective amount of the compound of formula (I) ##STR00004## in free or pharmaceutically acceptable salt form, in combination with an effective amount of 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfony- l)acetamide, in free or pharmaceutically acceptable salt form.

14. The method according to claim 13, wherein the compound of formula (I) and 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsul- fonyl)acetamide are administered simultaneously.

15. The method according to claim 13, wherein the compound of formula (I) and 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsul- fonyl)acetamide are administered separately.

16. The method according to claim 13, wherein the compound of formula (I) and 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsul- fonyl)acetamide are administered over a period of time.

17. The method according to claim 13, wherein the compound of formula (I) is administered once a day.

18. The method according to claim 13, wherein 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfony- l)acetamide is administered twice a day.

19. The method according to claim 13 wherein the compound of formula (I) and the prostacyclin receptor (IP) agonist are administered orally.
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