Method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK)

摘要

The present invention relates to a method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK) and the use of the compounds in the prevention or treatment of disease, including pre-diabetes, type 2 diabetes, syndrome X, metabolic syndrome and obesity.;

主权项

1. Compounds for activating AMPK, wherein an effective amount of at least one compound of formula (I) and/or the pharmaceutically or nutritionally acceptable salts thereof, is administrated to a mammal in need of such treatment and wherein the compounds of formulation (I) is defined below: in which R2 is hydrogen, halogen, hydroxy group, amino group, alkyl group or —NHR group, where R is alkyl, cycloalkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, Whereas “substituted phenyl” refers to phenyl group which is substituted with one to five hydroxy and alkoxy groups, one to five hydroxyl and halogen groups, one to five hydroxyl and alkyl groups as define herein; “substituted benzyl” refers to phenylmethyl group which is substituted with one to five hydroxy and alkoxy groups, one to five hydroxyl and halogen groups, one to five hydroxyl and alkyl groups as define herein; R6 is hydroxy group, amino group, mercapto group or —NHR group, where R is alkyl, cycloalkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, Whereas “substituted phenyl” refers to phenyl group which is substituted with one to five hydroxy and alkoxy groups, one to five hydroxyl and halogen groups, one to five hydroxyl and alkyl groups as define herein; “substituted benzyl” refers to phenylmethyl group which is substituted with one to five hydroxy and alkoxy groups, one to five hydroxyl and halogen groups, one to five hydroxyl and alkyl groups as define herein; The generic substitutes have meanings identical with definition, wherein “hydroxy” refers to the group —OH; “halogen” refers to F, Cl, Br, I; “amino” refers to the group —NH2; “mercapto” refers to the group —SH; “alkyl” refers to linear or branched at most 6 carbons saturated chain; “alkoxy” refers to the group —OR, where R is alkyl as defined herein; “cycloalkyl′ refers to a cyclic or polycyclic alky group containing 3 to 6 carbon; and tautomers, racements, optical isomers or pharmaceutically or nutritionally acceptable salts thereof, including a pharmaceutical carrier.