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US 10,329,286 B2Granted
FXR (NR1H4) modulating compounds
AssigneeGilead Sciences, Inc.
InventorsPeter A. Blomgren, Kevin S. Currie, Julie Farand, Christian Gege, Jeffrey E. Kropf, Jianjun Xu
Life of this patent
Estimating the term…
Abstract
The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
Claims7
A compound according to Formula (I):
- wherein:
- Q is phenylene optionally substituted with one or two substituents selected from halogen, methyl, —CH2F, —CHF2, and —CF3;
- Z is:
- L is a bond;
- X is CH or C—CH3;
- R1 is C1-4-alkyl or C3-6-cycloalkyl;
- R3 is halogen, C1-4-alkyl, halo-C1-4-alkyl, C1-4-alkoxy, or halo-C1-4-alkoxy;
- R4 is hydroxyl, C1-6-alkoxy, halo-C1-6-alkoxy, or NR5R6;
- R5 is hydrogen, C1-6-alkyl, or halo-C1-6-alkyl;
- R6 is hydrogen or C1-6-alkyl, wherein said C1-6-alkyl is optionally substituted with 1 to 6 substituents independently selected from halogen, —SO3H, and —CO2H;
- R7 and R8 are independently selected from halogen, C1-3-alkoxy, and fluoro-C1-3-alkoxy;
- and
- n is 0 or 1;
- or a pharmaceutically acceptable salt, a stereoisomer, a mixture of stereoisomers, or a tautomer thereof.
11 more elements
A compound selected from the group consisting of:
- or a pharmaceutically acceptable salt, a stereoisomer, a mixture of stereoisomers, or a tautomer thereof.
Dependencies are inferred from the claim text.