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Last Updated: April 25, 2024

Claims for Patent: 10,154,990


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Summary for Patent: 10,154,990
Title:Medicaments for the treatment or prevention of fibrotic diseases
Abstract: The present invention relates to the use of indolinones of general formula ##STR00001## substituted in the 6 position, wherein R.sub.1 to R.sub.5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.
Inventor(s): Park; John Edward (Warthausen, DE), Roth; Gerald Juergen (Biberach, DE), Heckel; Armin (Biberach, DE), Chaudhary; Nveed (Southampton, GB), Brandl; Trixi (Allschwil, CH), Dahmann; Georg (Warthausen-Birkenhard, DE), Grauert; Matthias (Biberach an der Riss, DE)
Assignee: Boehringer Ingelheim International GmbH (Ingelheim am Rhein, DE)
Application Number:14/982,179
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 10,154,990
Patent Claims: 1. A method for treating systemic scleroderma, which comprises administering to a patient in need thereof a therapeutically effective amount of 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methy- l-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone, or a salt thereof.

2. The method as recited in claim 1 wherein 3-Z- [1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anili- no)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone is in the form of the monoethanesulfonate salt.

3. The method as recited in claim 1 further comprising administering an additional pharmacologically active substance selected from the group consisting of anticholinergic agents, beta-2 mimetics, steroids, PDE-IV inhibitors, p38 MAP kinase inhibitors, NK.sub.1 antagonists, LTD4 antagonists, EGFR inhibitors and endothelin-antagonists in combination with the 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl- -amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone, or salt thereof.

4. The method of claim 3, wherein the 3-Z-[1-(4-(N-((4 -methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl- -methylene]-6-methoxycarbonyl-2-indolinone, or salt thereof, and the additional pharmacologically active substance together comprise a pharmaceutical composition that further comprises one or more pharmaceutically acceptable carriers or excipients.

5. A method for treating systemic scleroderma comprising administering a therapeutically effective amount of 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-a- nilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone in the form of the monoethanesulfonate salt, to a patient in need thereof.

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