XU, JIANJUN,KROPF, JEFFREY E.,GEGE, CHRISTIAN,CURRIE, KEVIN S.,BLOMGREN, PETER A.
申请号：
ARP170101593
公开号：
AR108709A1
申请日:
2017.06.09
申请国别(地区):
AR
年份:
2018
代理人:
摘要：
The compounds referred to in this table are combined with n1h1h4 receiver (FXRs) and act as FXRs activators. It also refers to the combination of compounds with nuclear receivers, the use of compounds in the development of drugs for the treatment of diseases and / or conditions, and the procedures for the synthesis of these compounds. Claim 1: a compound calculated according to formula (1),where: Q is phenylene or pyridylene, each of which is optionally substituted with one or two substituents independently selected from halogen, methyl, C₁₋₄ alkoxy,halo-alkoxy-C₁₋₄,-CH₂F, -CHF₂ and -CF₃；Y is N or CH； A is pyridylene or phenylene, each of which is optionally substituted with one or two groups independently selected from halogen, alkoxy-C₁₋₄,halo-alkoxy-C₁₋₄,C-alkyl and halo-C₁₋₄ alkyl；Z is isoxazol, replaced by R1 or pirazol, replaced by R1；R¹ is C-alkyl or cycloalkyl-C₃₋₆,a. On a voluntary basis, one to three substitutes selected independently from among fluorination, hydroxyl group, alcox-c8321 and fluorination-alcoxi-c83218331 were used to replace the asphalt-c83318324；and said C ciclo cycloalkyl is optionally substituted with 1 to 3 substituents independently selected from fluoro, hydroxyl, C-alkyl,Fluorination asphalt c8321e-83318323；a. Alcox-c83217c83331-83223 and fluorination alcox-c83218c83331；R2 and R3 are selected independently among hydrogen, halogen and methoxy-cf8323；-CHF₂,-CH F -OCH F -OCHF-Keywords ocf8323 and methyl； rs8308es-coc222； r83090 O-C (o) n8309； r8310；R830909 is hydrogen, hydrocarbon-c83218331-832626；or halo-C₁₋₆-alkyl；and R⁶ is hydrogen or C-alkyl,wherein said C--alkyl is optionally substituted with 1 to 6 substituents independently selected from halogen, -SO₃H and -CO₂H； or a pharmaceutically acceptable salt, a stereoisomer, a mixture of stereoisomers, or a tautomer thereof.La presente se refiere a compuestos que se unen al receptor NR1H4 (FXR) y actúan como agonistas de FXR. Se refiere además al uso de los compuestos para la preparación
