Claims
- 1. A compound comprising a steroidal ring system and a group R1 selected 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 R2 of the formula —L—R3, wherein L is an optional linker group and R3 is an aromatic hydrocarbyl group.
- 2. A compound according to claim 1 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.
- 3. A compound according to claim 1 of Formula I
- 4. A compound according to claim 1 of Formula II
- 5. A compound according to claim 1 of Formula III
- 6. A compound according to claim 1 of Formula IV
- 7. A compound according to claim 1 wherein the A ring of the steroidal ring system is substituted with a group R4, wherein R4 is a hydrocarbyl group.
- 8. A compound according to claim 7 wherein R4 is an oxyhydrocarbyl group.
- 9. A compound according to claim 8 wherein R4 is an alkoxy group.
- 10. A compound according to claim 9 wherein R4 is methoxy.
- 11. A compound according to claim 7 wherein R4 is an hydrocarbon group.
- 12. A compound according to claim 11 wherein R4 is an alkyl group.
- 13. A compound according to claim 12 wherein R4 is ethyl.
- 14. A compound according to claim 7 wherein the A ring is substituted with R1 and R4 is ortho substituted with respect to R1.
- 15. A compound according to claim 7 wherein R4 is at position 2 of the A ring.
- 16. A compound according to claim 1 wherein the compound comprises at least two or more of sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group.
- 17. A compound according to claim 1 wherein the compound comprises at least two sulphamate groups.
- 18. A compound according to claim 1 wherein the compound comprises at least two sulphamate groups, wherein said sulphamate groups are not on the same ring.
- 19. A compound according to claim 1 wherein the A ring comprises at least one sulphamate group and wherein the D ring comprises at least one sulphamate group.
- 20. A compound according to claim 1 wherein R1 is a sulphamate group.
- 21. A compound according to claim 1 wherein R3 is or comprises an aromatic ring.
- 22. A compound according to claim 21 wherein R3 is or comprises a six membered aromatic ring.
- 23. A compound according to claim 22 wherein R3 is or comprises a six membered aromatic ring containing carbon and optionally nitrogen.
- 24. A compound according to claim 21 wherein the aromatic ring is substituted with a group R5.
- 25. A compound according to claim 24 wherein R5 is selected from hydrocarbyl and halogens.
- 26. A compound according to claim 24 wherein R5 is selected from hydrocarbon and halogens.
- 27. A compound according to claim 24 wherein R5 is selected from alkyl and halogens.
- 28. A compound according to claim 24 wherein R5 is selected from C1-10 alkyl, and halogens.
- 29. A compound according to claim 28, wherein R5 is C1-5 alkyl.
- 30. A compound according to claim 1 wherein L is a hydrocarbyl group.
- 31. A compound according to claim 1 wherein L is a hydrocarbon group.
- 32. A compound according to claim 1 wherein L is an alkyl group.
- 33. A compound according to claim 1 wherein L is a C1-10 alkyl preferably C1-5 alkyl, preferably C1 or C2 alkyl.
- 34. A compound according to claim 1 wherein group R2 is selected from
- 35. A compound according to claim 1 wherein group R2 is in an α conformation.
- 36. A compound according to claim 1 wherein group R2 is in an α conformation on the 17 position of the D ring.
- 37. A method comprising (a) performing a steroid sulphatase assay with one or more candidate compounds having the formula as defined in claim 1; (b) determining whether one or more of said candidate compounds is/are capable of modulating STS activity and/or cell cycling and/or cell growth and/or apoptosis; and (c) selecting one or more of said candidate compounds that is/are capable of modulating STS activity and/or cell cycling and/or cell growth and/or apoptosis.
- 38. A method comprising (a) performing a steroid sulphatase assay with one or more candidate compounds having the formula as defined claim 1; (b) determining whether one or more of said candidate compounds is/are capable of inhibiting STS activity; and (c) selecting one or more of said candidate compounds that is/are capable of inhibiting STS activity and/or cell cycling and/or cell growth and/or apoptosis.
- 39. A compound identified by the method according to claim 37.
- 40. A compound identified by the method according to claim 38.
- 41. A compound according to claim 1 for use in medicine.
- 42. A pharmaceutical composition comprising the compound according to claim 1 optionally admixed with a pharmaceutically acceptable carrier, diluent, excipient or adjuvant.
- 43. A method of using a compound according to claim 1 in the manufacture of a medicament for use in the therapy of a condition or disease associated with STS and/or cell cycling and/or apoptosis and/or cell growth.
- 44. A method of using a compound according to claim 1 in the manufacture of a medicament for use in the therapy of a condition or disease associated with adverse STS levels and/or cell cycling and/or apoptosis and/or cell growth.
Priority Claims (1)
Number |
Date |
Country |
Kind |
0020498.2 |
Aug 2000 |
GB |
|
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application is a continuation-in-part of International application PCT/GB01/03692 filed Aug. 17, 2001 designating the U.S. and published as WO 02/16393 on Feb. 28, 2002, which claims priority from UK application 0020498.2 filed Aug. 18, 2000.
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
PCT/GB01/03692 |
Aug 2001 |
US |
Child |
10367622 |
Feb 2003 |
US |