The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Feb. 01, 2022

Filed:

Mar. 02, 2021
Applicant:

Actelion Pharmaceuticals Ltd, Allschwil, CH;

Inventors:

Dénes Csonka, Allschwil, CH;

Wassim Fares, Chapel Hill, NC (US);

Hans Hoogkamer, Bubendorf, CH;

Koen Torfs, Kasterlee, BE;

Assignee:
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K 31/506 (2006.01); A61P 9/12 (2006.01); A61K 31/4965 (2006.01); A61K 31/4985 (2006.01);
U.S. Cl.
CPC ...
A61K 31/506 (2013.01); A61K 31/4965 (2013.01); A61K 31/4985 (2013.01); A61P 9/12 (2018.01);
Abstract

The present invention relates to high doses of macitentan, i.e. propylsulfamic acid [5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl]-amide or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof, or of aprocitentan, for use in the treatment and/or prevention of pulmonary arterial hypertension (PAH). Moreover, the present invention relates to the use of high doses of macitentan, or of aprocitentan, for the manufacture of a medicament for the treatment and/or prevention of PAH, as well as to a method for the treatment and/or prevention of PAH comprising high doses of macitentan or of aprocitentan. Further, the present invention relates to a dosage regimen for the treatment and/or prevention of PAH as well as to a combination of macitentan, or of aprocitentan, with one or more phosphodiesterase type 5 (PDE5) inhibitors, prostacyclin analogues, prostacyclin receptor agonists or soluble guanylate cyclase stimulators. Therein, PAH is preferably mild or moderate PAH. Moreover, the present invention relates to a pharmaceutical composition for the treatment of PAH comprising a high dose of macitentan or of aprocitentan.


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