| abstract |
The subject invention provides novel calcium channel blockers based upon mibefradil: (I) wherein: X = a bond, (CH2)n, O, S, or O(CH2)n wherein = 1-6; R1 = C1-6 alkyl, optionally substituted with OH or NH2; R2 = F or COOR5, wherein R5 is C1-6 alkyl, optionally substituted with OH or NH2; R3 = CH3 or (CH2)„ - COOR6, wherein n =1-6 and R6 is C1-6 alkyl, optionally substituted with OH or NH2; R4 = (CH2)n - COR7R8 -(CH2)n -R10R11 or (II) R7 = 0, NH, or NR9, R8 = optionally substituted aryl or heterocycle, R9 = C1-6 alkyl, R10 = 0, S, SO, S02, NH, NR12 or N(CH2 )m COOR13 R11 = aryl of heterocyclyl optionally substituted with (CH2)n, COOR14, R12 = C1-6 alkyl, optionally substituted with OH or NH2, R13 = C1-6 alkyl, optionally substituted with OH or NH2, R14 = C1-6 alkyl, optionally substituted with OH or NH2, R15 = (CH2)n COOR16, R16 = C1-6 alkyl, optionally substituted with OH or NH2, R17 = not present or COOR18 wherein R18 is C1-6 alkyl, optionally substituted with OH or NH2, and wherein n =1-6, useful in the treatment of hypertension, angina pectoris, ischemia, arrhythmias and cardiaq, insufficiency. |