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486 LIVER SPECIFIC BILE ACID DERIVATIVES OF THE GLUCOCORTICOID ANTAGONIST RU486

机译:486糖皮质激素拮抗剂RU486的肝特定胆汁酸衍生物

摘要

(Ⅰ); Novel glucocorticoid receptor ligands of the present invention, the gatneunde the general formula (Ⅰ) Here, R represents a hydrogen atom, an aliphatic hydrocarbon, aromatic hydrocarbon, carboxylic acid or their esters, high-flying hydroxy, halogen, or cyano halogen, or the salts cyano, or a pharmaceutically acceptable. W is a methine carbon atom having the R, S or a racemic (racemic) stereochemistry material. X and Z are the same or different conjugates, an amide (-CONR'- or NR'CO-), an amine (-NR'-), an ether (-O-), or a thioether (-S-) R 'is hydrogen atom, an aliphatic hydrocarbon, or an aromatic hydrocarbon. Symbol n, o are the same or different and is an integer from 1 to 6. m is an integer from 0 to 6. Y is a hydroxy group, a carboxylic acid or their esters, tetrazole, acyl sulfonamide (R "is an aliphatic or aromatic hydrocarbon is -CONHSO 2 R" or -SO 2 NHCOR "), or a pharmaceutically acceptable salt thereof a. method for the treatment of diseases that are dependent upon the expression of a disease or a glucocorticoid receptor regulated genes associated with metabolism dysfunction is also provided.
机译:(Ⅰ);本发明的新型糖皮质激素受体配体,其通式为(Ⅰ),式中,R表示氢原子,脂族烃,芳族烃,羧酸或其酯,高空羟基,卤素或氰基卤素,或氰基盐或药学上可接受的盐。 W是具有R,S或外消旋(外消旋)立体化学材料的次甲基碳原子。 X和Z是相同或不同的共轭物,酰胺(-CONR'-或NR'CO-),胺(-NR'-),醚(-O-)或硫醚(-S-)R '是氢原子,脂族烃或芳族烃。符号n,o相同或不同,为1〜6的整数。m为0〜6的整数。Y为羟基,羧酸或其酯,四唑,酰基磺酰胺(R“为脂肪族。或芳族烃是-CONHSO 2 R“或-SO 2 NHCOR”,或其药学上可接受的盐。a。治疗依赖于还提供了与代谢功能障碍相关的疾病或糖皮质激素受体调节基因的表达。

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