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New compounds that modulate the activity of FXR (NR1H4)
专利权人:
Gilead Sciences; Inc.
发明人:
KINZEL, Olaf,STEENECK, Christoph,KREMOSER, Claus
申请号:
ES12735100
公开号:
ES2569718T3
申请日:
2012.07.12
申请国别(地区):
ES
年份:
2016
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 groups independently selected from the group group consisting of OH, O-C 1-6 alkyl, O-C 1-6 haloalkyl, 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.Un compuesto de acuerdo con la Fórmula (1), un enantiómero, diastereómero, tautómero, o sal farmacéuticamente aceptable del mismo**Fórmula** en la que R se selecciona del grupo que consiste de COOR6, CONR7R8, tetrazolilo, SO2NR7R8, alquilo C1-6, SO2-alquilo C1- 6 y H, en el que R6 se selecciona independiente
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