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Novel FXR (NR1H4) binding and activity modulating compounds
专利权人:
フェネックス ファーマシューティカルス アーゲー
发明人:
キンツェル オーラフ,シュティーネック クリストフ,クレモザー クラウス
申请号:
JP2014519453
公开号:
JP2014520823A
申请日:
2012.07.12
申请国别(地区):
JP
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.本発明は、NR1H4レセプター(FXR)に結合し、FXRの作動薬として作用する化合物に関する。本発明は更に、前記化合物による前記核レセプターの結合を介する疾患および/または状態の治療のための薬剤の調製を目的とする化合物の使用にも関する。Zは、(a)、(b)、(c)または(d)から選択される。
来源网站:
中国工程科技知识中心
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