Selective inhibitors of human corticosteroid synthases

摘要

The invention relates to compounds for selectively inhibiting human corticosteroid synthases CYP1 1 B1 and CYP1 1 B2, and to the production and use thereof for treating hypercortisolism, diabetes mellitus, hyperaldosteronism, cardiac insufficiency, myocardial fibrosis, depression, age-related cognitive decline and metabolic syndrome.

主权项

1. A method of treating hyperaldosteronism, heart failure, myocardial fibrosis, hypercortisolism, diabetes mellitus, depression, age-related cognitive decline or metabolic syndrome in a patient comprising, administering to said patient a therapeutically effective amount of a compound having a structure of formula (Ia) wherein R1 or R2 is hydrogen and the other of substituents R1 or R2 is selected from H and O—C1-6 alkyl; wherein R3 is selected from oxazolyl, pyridyl, imidazolyl and pyrimidyl, which selection can be substituted with one R12 residue; wherein R5 and R6 are independently selected from H, fluorine, chlorine and bromine; R8 and R9 are H; and R12 is selected from H, halogen, hydroxy, CN, C1-3 alkyl and C1-3 alkoxy; or a pharmaceutically acceptable salt thereof.