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Last Updated: April 19, 2024

Details for Patent: 8,809,334


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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 with 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)
Filing Date:Aug 12, 2009
Application Number:13/058,639
Claims:1. A product containing macitentan or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having prostacyclin receptor (IP) agonist properties, or a pharmaceutically acceptable salt thereof selected from 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfony- l)acetamide and its pharmaceutically acceptable salts, and {4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}acetic acid and its pharmaceutically acceptable salts.

2. A product according to claim 1, wherein the compound having prostacyclin receptor (IP) agonist properties or a pharmaceutically acceptable salt thereof is {4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}acetic acid and its pharmaceutically acceptable salts.

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

4. A method for the treatment of a disease wherein endothelin is involved, is selected from hypertension, pulmonary hypertension, diabetic arteriopathy, heart failure, erectile dysfunction, angina pectoris and pulmonary fibrosis comprising administering an effective amount of a product of claim 1.

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

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

7. The method according to claim 4, wherein the disease wherein endothelin is involved is pulmonary arterial hypertension.

8. The method according to claim 4, wherein the disease wherein endothelin is involved is pulmonary hypertension.

9. A pharmaceutical composition containing, as active principles, macitentan, or a pharmaceutically acceptable salt thereof, in combination with at least one compound having prostacyclin receptor (IP) agonist properties, or a pharmaceutically acceptable salt thereof selected from 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfony- l)acetamide and its pharmaceutically acceptable salts, and {4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}acetic acid and its pharmaceutically acceptable salts, as well as at least one pharmaceutically acceptable excipient.

10. A pharmaceutical composition according to claim 9, wherein the compound having prostacyclin receptor (IP) agonist properties or pharmaceutically acceptable salt thereof is 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfony- l)acetamide or a pharmaceutically acceptable salt thereof.

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