| abstract |
The invention concerns compounds of formula (I), wherein R1 and R2 independently are hydrogen, acyl, alkoxycarbonyl or alkyl; either the sulfamoyloxy side chain is bound to the 6 position; R3 is alkyl; alkenyl; alkinyl; a cycloalkyl moiety optionally substituted by alkyl, alkoxy or halogen; arylalkyl; arylalkenyl; arylalkinyl; acyl; cycloalkylalkyl; 3-oxo-2-oxacamphanyl; 6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl; a heteroaryl moiety optionally substituted by alkyl, alkoxy or halogen; or is heteroarylalkyl; and R4 is hydrogen; alkyl; hydroxy; or alkoxy; or the sulfamoyloxy side chain is bound to the 7 position; R3 has the significance indicated above for R4; and R4 has the significance indicated above for R3; X is O or S; and the symbol --- is a single or a double bond; in free form or salt form. They can be prepared by sulfamoylation of corresponding hydroxylated compounds, by reduction and/or by N-substitution. They are indicated for use as pharmaceuticals, particularly in the prophylactic or curative treatment of illnesses responsive to steroid sulfatase inhibition. |