Oestrogen derivatives as inhibitors of steroid sulphatase

Details Oestrogen derivatives as inhibitors of steroid sulphatase Oestrogen derivatives as inhibitors of steroid sulphatase

C - Chemistry, Metallurgy

07

J

C07J 41/00 (2006.01) A61K 31/56 (2006.01) C07J 43/00 (2006.01)

Patent

CA 2520142

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 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 a nitrite group, an alcohol, an ester, an ether, an amine and an alkene, provided that when R3 is or comprises an alcohol, L is present; and wherein the A ring of the steroidal ring system is substituted at position 2 or 4 with a group R4, wherein R4 is a hydrocarbyl group.

L'invention concerne un composé comprenant un système cyclique stéroïdien et un groupe facultatif R?1¿ sélectionné parmi -OH, un groupe sulfamate, un groupe phosphonate, un groupe thiophosphonate, un groupe sulfonate ou un groupe sulfamide. Le cycle D du système cyclique stéroïdien est substitué par un groupe R?2¿ de formule -L-R?3¿, dans laquelle L est un groupe de liaison et R?3¿ est sélectionné parmi des groupes qui sont ou qui comprennent un des éléments suivants: groupe nitrite alcool, ester, éther, amine ou alcène, sous réserve que lorsque R?3¿ est ou comprend un alcool, L est présent; et le cycle A du système cyclique stéroïdien est substitué en position 2 ou 4 par un groupe R?4¿, R?4¿ étant un groupe hydrocarbyle.

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