发明名称 NOVEL FXR (NR1H4) BINDING AND ACTIVITY MODULATING COMPOUNDS
摘要 The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of 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.
申请公布号 US2014221659(A1) 申请公布日期 2014.08.07
申请号 US201214232118 申请日期 2012.07.12
申请人 Kinzel Olaf;Steeneck Christoph;Kremoser Claus 发明人 Kinzel Olaf;Steeneck Christoph;Kremoser Claus
分类号 C07D261/08;C07D413/14;C07D413/12 主分类号 C07D261/08
代理机构 代理人
主权项 1. A compound according to the following Formula (1), an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof wherein R is selected from the group consisting of COOR6, CONR7R8, tetrazolyl, SO2NR7R8, C1-6 alkyl, SO2—C1-6 alkyl and H, with R6 independently selected from the group consisting of H or C1-6 alkyl, and R7 and R8 independently from each other selected from the group consisting of H, C1-6 alkyl, halo-C1-6 alkyl, C1-6 alkylene-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, benzisoxazolyl, benzofuranyl, benzotriazolyl, furanyl, benzothiazolyl, thiazolyl, oxadiazolyl, each optionally substituted with one or two groups independently selected from the group consisting of OH, O—C1-6 alkyl, O-halo-C1-6 alkyl, C1-6 alkyl, halo-C1-6 alkyl, C3-6 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, halo-C1-6 alkyl, halogen and CF3; Y is selected from N or CH; Z is selected from wherein X═CH, N, NO; R1 is selected from the group consisting of hydrogen, C1-3 alkyl, C3-6 cylcoalkyl, C4-5 alkylcycloalkyl, wherein C1-3 alkyl is optionally substituted with 1 to 3 substituents independently selected from halogen, hydroxy or C1-6 alkoxy; 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.
地址 Heidelberg DE