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NOUVEAUX COMPOSÉS MODULANT L'ACTIVITÉ DE FXR (NR1H4) ET S'Y LIANT
专利权人:
Phenex Pharmaceuticals AG
发明人:
申请号:
EP12735100.5
公开号:
EP2731676A1
申请日:
2012.07.12
申请国别(地区):
EP
年份:
2014
代理人:
摘要:
The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (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. wherein R is selected from the group consisting of COOR 6 , CONR 7 R 8 , tetrazolyl, SO 2 NR 7 R 8 , C 1-6 alkyl, SO 2 -C 1-6 alkyl and H, with R 6 independently selected from the group consisting of H or C 1-6 alkyl, and R 7 and R 8 independently from each other selected from the group consisting of H, C 1-6 alkyl, halo-C 1-6 alkyl, C 1-6 alkylene-R 9 , SO 2 -C 1-6 alkyl, wherein R 9 is selected from the group consisting of COOH, OH and SO 3 H; 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-C 1-6 alkyl, O-halo-C 1-6 alkyl, C 1-6 alkyl, halo-C 1-6 alkyl, 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 C 1-6 alkyl, halo-C 1-6 alkyl, halogen and CF 3 ; Y is selected from N or CH; Z is selected from wherein X= CH, N, NO.La présente invention concerne des composés qui se lient au récepteur NR1H4 (FXR) et qui agissent comme des agonistes de FXR. L'invention concerne en outre l'utilisation des composés pour la préparation d'un médicament destiné au traitement de maladies et/ou de conditions par la liaison dudit récepteur nucléaire par lesdits composés et un procédé de synthèse desdits composés (1). Z est
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