abstract |
Compounds of the formula (I), (R1 is one of a wide range of substituents; R2 = H, halogen and R3 = H, hydroxymethyl or CR2R3 = cyclopropyl ring; CR4R5 is one of formula (II), formula (III) and formula (IV) Ra and Rb are a bond between carbons 9 and 11 or an -O-, -S-, -CH2- or -CF2- bridge; R6 is H, alkyl, -CH2ORx, -CH2SRx, -CH2SO-alkyl, -CH2SO2-alkyl, -CH2NHRx, -CH2N(alkyl)(Rx), -C(=O)O-alkyl, -C(=O)-alkyl, -C(=O)NHRx or -C(=O)N(alkyl)(Rx); R7 = R8 = H or CR7R8 is a cyclopropyl ring; R9 and R9’ are H, halogen, alkyl or alkoxycarbonyl or a bond between carbons 22 and 23; R10 is H or -C(=O)ORx; Rx is H, alkyl or acyl; Ry is H, alkyl; Rz is H, alkyl) are provided. They are aldosterone receptor antagonists, useful for the treatment of aldosteronism including hypertension, cardiovascular disease, renal dysfunction, edema, cerebrovascular disease and insulinopathies. |