FXR (NR1H4) modulating compounds
AssigneeGilead Sciences, Inc.
InventorsPeter A. Blomgren, Kevin S. Currie, Christian Gege, Jeffrey E. Kropf, Jianjun Xu
Life of this patent
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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.
Claims17
A method of treating a patient suffering from Primary Biliary Cirrhosis (PBC) or Primary Sclerosing Cholangitis (PSC) comprising administering to the patient a compound having the structure of Formula (Ia):
- wherein:
- Q is phenylene substituted with one chloro;
- Y is N;
- R1 is cyclopropyl or methyl;
- R2 and R3 are chloro;
- R4-A is:
- wherein the pyridylene is optionally substituted with one or two groups independently selected from halogen, C1-4-alkoxy, halo-C1-4-alkoxy, C1-4-alkyl, and halo-C1-4-alkyl, and R4 is —CO2R5 or —C(O)NR5R6;
- R5 is hydrogen;
- and
- R6 is C1-2-alkyl optionally substituted with —CO2H or —SO3H;
- or a pharmaceutically acceptable salt, a stereoisomer, a mixture of stereoisomers, or a tautomer thereof.
A method of treating a patient suffering from Primary Biliary Cirrhosis (PBC) or Primary Sclerosing Cholangitis (PSC) comprising administering to the patient a compound having the structure of Formula (Ia):
- wherein:
- Q is phenylene substituted with one chloro;
- Y is N;
- R1 is cyclopropyl or methyl;
- R2 and R3 are chloro;
- R4-A is:
- wherein the pyridylene is optionally substituted with one or two groups independently selected from halogen, C1-4-alkoxy, halo-C1-4-alkoxy, C1-4-alkyl, and halo-C1-4-alkyl, and R4 is —CO2R5 or —C(O)NR5R6;
- R5 is hydrogen;
- and
- R6 is C1-2-alkyl optionally substituted with —CO2H or —SO3H;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.