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US 2012/0232116 A1Published application
Novel fxr (nr1h4) binding and activity modulating compounds
AssigneePhenex Pharmaceuticals AG
InventorsClaus Kremoser, Ulrich Abel, Christoph Steeneck, Olaf Kinzel
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Abstract
The present invention relates to compounds which bind to the NR1 H4 receptor (FXR) and act as agonists of the NR1 H4 receptor (FXR). The invention 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.
Claims15
-15. (canceled)
A compound according to the following formula (1), or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof:
- wherein:
- R is selected from the group consisting of COOR6, CONR7R8, tetrazolyl and H, with R6 independently selected from the group consisting of H and lower alkyl, and R7 and R8 independently from each other selected from the group consisting of H, lower alkyl, C1-6haloalkyl, C1-6 alkylene-R9, and SO2—C1-6 alkyl wherein R9 is selected from the group consisting of COOH, OH, and SO3H;
- A is selected from the group consisting of phenyl, pyridyl, pyrazolyl, indolyl, thienyl, benzothienyl, indazolyl, benzisoxazolyl, benzofuranyl, benzotriazolyl, furanyl, benzothiazolyl, and thiazolyl, each optionally substituted with one or two groups independently selected from the group consisting of OH, lower alkyl, lower cycloalkyl, and halogen;
- Q is selected from the group consisting of phenyl, pyridyl, thiazolyl, thiophenyl, and pyrimidyl, each optionally substituted with one or two groups independently selected from the group consisting of lower alkyl, halogen and CF3;
- and
- wherein:
- X═CH, N, NO;
- R1 is selected from the group consisting of hydrogen, C1-C3 alkyl, C3-C6 cycloalkyl, and C4-C5 alkylcycloalkyl, wherein C1-3 alkyl is optionally substituted with 1 to 3 substituents independently selected from halogen, hydroxy or C1-6 alkoxy;
- and
- R2 and R3 are independently selected from the group consisting of hydrogen, C1-C3 alkyl, C1-C3 haloalkyl, C1-C3 alkoxy, C1-C3 haloalkoxy and halogen.
7 more elements
Dependencies are inferred from the claim text.