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US 11,229,634 B2Granted
Methods for treating gastrointestinal disorders using FXR agonists
AssigneeNovartis AG
InventorsBryan Laffitte, Michael Badman, Jin Chen, Sam Lindgren
Life of this patent
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Abstract
The invention provides methods for modulating the activity of farnesoid X receptors (FXRs) using specific FXR agonists, in particular for treating or preventing liver and gastrointestinal diseases.
Claims16
A method for treating a condition mediated by Farnesoid X receptor (FXR), comprising administering to a subject in need thereof a compound of Formula (I)
- or a stereoisomer, an enantiomer, a pharmaceutically acceptable salt thereof, an amino acid conjugate, or an acyl glucuronide conjugate thereof, at a dose of about 3 μg to about 100 μg;
- wherein said amino acid conjugate or acyl glucuronide conjugate is selected from:
- 2-({2-[(1R,3R,5S)-3-({5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl}methoxy)-8-azabicyclo[3.2.1]octan-8-yl]-4-fluoro-1,3-benzothiazol-6-yl}formamido)acetic acid;
- 2-({2-[(1R,3R,5S)-3-({5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl}methoxy)-8-azabicyclo[3.2.1]octan-8-yl]-4-fluoro-1,3-benzothiazol-6-yl}formamido)ethane-1-sulfonic acid;
- and
- (2S,3S,4S,5R,6S)-6-((2-((1R,3S,5S)-3-((5-cyclopropyl-3-(2-(trifluoromethoxy)phenyl)isoxazol-4-yl)methoxy)-8-azabicyclo[3.2.1]octan-8-yl)-4-fluorobenzo[d]thiazole-6-carbonyl)oxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid;
- and
- wherein said condition mediated by FXR is bile acid diarrhea.
5 more elements
Dependencies are inferred from the claim text.