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Novel FXR (NR1H4) binding and activity modulating compounds
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 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.
Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Recommanded Product: 52409-22-0, you can also check out more blogs about52409-22-0
Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method