IP Library › Granted Patent US 10,154,990
Granted Patent B2
US 10,154,990 · App. 14/982,179 · Granted Dec 18, 2018

Medicaments for the treatment or prevention of fibrotic diseases

Inventors: John Edward Park (Warthausen, DE); Gerald Juergen Roth (Biberach, DE); Armin Heckel (Biberach, DE); Nveed Chaudhary (Southampton, GB); Trixi Brandl (Allschwil, CH); Georg Dahmann (Warthausen-Birkenhard, DE); Matthias Grauert (Biberach an der Riss, DE)
Assignee: Boehringer Ingelheim International GmbH
A61K31/4045A61K31/404A61K31/4178A61K31/44A61K31/445A61K31/454A61K31/495A61K31/496A61K31/5377A61K31/551A61K45/06C07D209/34C07D295/155C07D295/215C07D401/12C07D403/12
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Quick Facts
Patent No.
US 10,154,990
App. No.
14/982,179
Granted
Dec 18, 2018
Kind
B2
Abstract

The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R 1 to R 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.

Claims (5)

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-methyl-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)-anilino)-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 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)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone in the form of the monoethanesulfonate salt, to a patient in need thereof.

Priority Claims (1)
EP 04030770 · Dec 24, 2004 · regional
Continuity (4)
Continuation 14184821 · Feb 20, 2014
Continuation 12645151 · Dec 22, 2009
Continuation 11275223 · Dec 20, 2005
Related Publication 20160136133A1 · May 19, 2016
Cited By (2)
US 12,539,294 US 12,605,341