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New compounds that modulate the binding and activity of FXR (NR1H4)
专利权人:
GILEAD SCIENCES; INC.
发明人:
Kinzel, Olaf,Steeneck, Christoph,Kremoser, Claus
申请号:
ES15002478
公开号:
ES2632492T3
申请日:
2012.07.12
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound according to Formula (1), an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt thereof ** Formula ** wherein R is selected from the group consisting of COOR6, CONR7R8, tetrazolyl, SO2NR7R8, C1 alkyl -6, SO2-C1-6 alkyl and H, wherein R6 is independently selected from the group consisting of H or C1-6 alkyl, and R7 and R8 independently selected from each other from the group consisting of H, C1-6 alkyl , C1-6 haloalkyl, C1-6 alkyl-R9, 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, pyrimidyl, pyrazolyl, indolyl, thienyl, benzothienyl, indazolyl, bencisoxazolyl, benzofuranyl, benzotriazolyl, furanyl, benzothiazolyl, thiazolyl, oxadiazolyl, each optionally substituted with one or two independently selected groups group consisting of OH, O-C 1-6 alkyl, O-C 1-6 haloalkyl, C 1-6 alkyl, C 1-6 haloalkyl, C 3-6 cycloalkyl and halogen; Q is selected from the group consisting of phenyl, pyridyl, thiazolyl, thiophenyl, pyrimidyl, each optionally substituted with one or two groups independently selected from the group consisting of C1-6 alkyl, C1-6 haloalkyl, halogen and CF3; Y is selected from N or CH; Z is selected from ** Formula ** in which X>; = CH, N, NO; R1 is selected from the group consisting of hydrogen, C1-3 alkyl, C3-6 cycloalkyl, C4-5 alkylcycloalkyl, wherein C1-3 alkyl is optionally substituted with 1 to 3 substituents independently selected from halogen, hydroxy or C1 alkoxy -6; R2 and R3 are independently selected from the group consisting of hydrogen, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy and halogen. for use in the prophylaxis and / or treatment of chronic diseases selected from the group consisting of primary biliary cirrhosis (PBC) and primary sclerosing cholangitis (PSC).Un compuesto de acuerdo con la Fórmula (1), un enantiómero, diastereómero, tautómero, o sal farmacéuticamente aceptable del mismo**Fórmula**
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