Sterix Limited

Matthew Paul Leese

Michael John Reed

Barry Victor Lloyd Potter

Atul Purohit

Bertrand Leblond

Fabrice Jourdan

Lok Wai Lawrence Woo

Hatem Hejaz

Simon Paul Newman

Surinder Kuman Chander

Graham Keith Packham

Meriel Kimberley

The present invention involves tetrahydroisoquinoline compounds and their use in the inhibition and/or prevention of tumor growth.

Compound

There is provided a compound of Formula I wherein X is a ring system; Ris any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; Ris any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein when X is a steroidal structure and both of Rand Rare sulphamate groups, the steroidal ring system (X) represents an oestrogen; and wherein said compound is capable of inhibiting steroid sulphatase (STS) activity and/or is capable of acting as a modulator of cell cycling and/or as a modulator of apoptosis and/or as a modulator of cell growth. There is also provided a compound of Formula VIII wherein Ris any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; and wherein said compound is capable of inhibiting steroid sulphatase (STS) activity and/or is capable of acting as a modulator of cell cycling and/or as a modulator of apoptosis and/or as a modulator of cell growth.

Oestrogen-17-sulphamates as inhibitors of steroid sulphatase

The present invention provides a compound comprising a steroidal ring system and an optional group Rselected from any one of &#x2014;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 Rof the formula -L-R, wherein L is an optional linker group and Ris 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 Ris 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 R, wherein Ris a hydrocarbyl group.

Oestrogen derivatives as inhibitors of steroid sulphatase

There is provided use of a compound of Formula XI: wherein Ris a sulphamate group and at least of Ror Ris a thioether group as disclosed by the present specification, capable of inhibiting steroid sulphatase.

Thioether sulphamate steroids as steroid inhibitors and anti-cancer compounds

There is provided a compound comprising a steroidal ring system and a group Rselected from any one of 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 Rof the formula &#x2014;L-R, wherein L is an optional linker group and Ris an aromatic hydrocarbyl group.

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Matthew Paul Leese