2-SUBSTITUTED ESTROGEN SULPHAMATES FOR INHIBITION OF STEROID SULPHATASE

摘要

The present invention provides a compound comprising a steroidal ring system and an optional group R¹ selected from any one of -OH, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the A ring of the steroidal ring system is optionally substituted at position 2 or 4 with a group R⁴ which may be a suitable subtituent wherein the D ring of the steroidal ring system is substituted by a group R² of the formula -L-R³, wherein L is an optional linker group and R³ is selected from groups which are or which comprise one of (i) -S0₂R⁵, wherein R⁵ is H, a hydrocarbyl group or a bond or group attached to the D ring; (ii) -NO₂; (iii) -SOR⁶, wherein R⁶ is H or a hydrocarbyl group; (iv) -R⁷, wherein R⁷ is a halogen; (v) - alkyl; (vi) -C(=O)R⁸, wherein R⁸ is H or hydrocarbyl; (vii) -C=CR⁹, wherein R⁹ is H or hydrocarbyl; (viii) -OC(=O)NR¹⁰R¹¹ wherein R¹⁰ and R¹¹ are independently selected from H and hydrocarbyl; (ix), (x), (xi), (xii) and (xiii) are formulae wherein when R³ is -alkyl, R⁴ is present as a hydrocarbon group, when R³ is -NO₂ R⁴ is present and/or R¹ is present as a sulphamate group, and when R³ is -C(=O)R⁸ R⁴ is present and R¹ is present as a sulphamate group.