Claims
- 1. A purified compound of the formula wherein each of R1 and R2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl; wherein at least one of R1 and R2 is H; and wherein the group Polycycle is a ring system comprising at least four rings, at least three of which are fused; wherein the compound is an inhibitor of an enzyme having steroid sulphatase activity (E.C.3.1.6.2); wherein if the sulphamate group on the compound were to be replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (E.C.3.1.6.2) at a pH 7.4 and 37° C. it would provide a Km value of less than 50 μM.
- 2. A purified compound comprising a steroidal ring structure and a sulphamate group of the formula wherein each of R1 and R2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl; wherein at least one of R1 and R2 is H; and wherein the compound is an inhibitor of an enzyme having steroid sulphatase activity (E.C.3.1.6.2); wherein if the sulphamate group on the compound were to be replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (E.C.3.1.6.2) at a pH 7.4 and 37° C. it would provide a Km value of less than 50 μM.
- 3. A purified compound according to claim 2, wherein the steroidal ring structure is a residue of a 3-sterol.
- 4. A purified compound according to claim 3, wherein the sterol is selected from the group consisting of oestrone, dehydroepiandrosterones, substituted oestrones and substituted dehydroepiandrosterones.
- 5. A purified compound according to claim 1 wherein R1 and R2 are independently selected from H, or a C1-C10 alkyl; wherein at least one of R1 and R2 is H.
- 6. A purified compound according to claim 2 wherein R1 and R2 are independently selected from H, or a C1-C10 alkyl; wherein at least one of R1 and R2 is H.
- 7. A purified compound according to claim 1 wherein R1 and R2 are independently selected from H, or a C1-C5 alkyl; wherein at least one of R1 and R2 is H.
- 8. A purified compound according to claim 2 wherein R1 and R2 are independently selected from H, or a C1-C5 alkyl; wherein at least one of R1 and R2 is H.
- 9. A purified compound according to claim 1 wherein R1 and R2 are independently selected from H or methyl; wherein at least one of R1 and R2 is H.
- 10. A purified compound according to claim 2 wherein R1 and R2 are independently selected from H or methyl; wherein at least one of R1 and R2 is H.
- 11. A purified compound according to claim 1 wherein R1 is H and R2 is H.
- 12. A purified compound according to claim 2 wherein R1 is H and R2 is H.
- 13. A purified compound according to claim 1 wherein the compound is any one of oestrone-3-sulphamate, oestrone-3-N-monomethylsulphamate.
- 14. A purified compound according to claim 3 wherein the compound is any one of oestrone-3-sulphamate, oestrone-3-N-monomethylsulphamate.
- 15. A purified compound according to claim 1 wherein the group Polycycle represents the residue of a sterol.
- 16. A purified compound according to claim 15 wherein the sterol is a 3-sterol.
- 17. A purified compound according to claim 2 wherein the compound is a compound of the formula wherein the group Polycycle represents the residue of a 3-sterol, and wherein R1 and R2 are H.
- 18. A purified compound according to claim 1 or 2 wherein the compound is Oestrone 3-sulphamate.
- 19. A purified compound according to claim 1 or 2 wherein the compound is Oestrone-3-N-monomethylsulphamate.
Priority Claims (1)
Number |
Date |
Country |
Kind |
9118478 |
Aug 1991 |
GB |
|
RELATED APPLICATIONS
This application is a division of U.S. application Ser. No. 09/238,345, filed Jan. 27, 1999, now U.S. Pat. No. 6,187,766, which in turn was a division of U.S. application Ser. No. 09/111,927, filed Jul. 8, 1998, incorporated herein by reference and now U.S. Pat. No. 6,011,024, which in turn was a continuation-in-part of U.S. application Ser. No. 08/458,352, filed Jun. 2, 1995, now U.S. Pat. No. 5,830,886, which was a division of U.S. application Ser. No. 08/196,192, filed (§102(e) date of) Dec. 27, 1994, now U.S. Pat. No. 5,616,574. U.S. application Ser. No. 08/196,192 was the U.S. National Phase of PCT/GB92/01587, filed Aug. 28, 1992 and designating the U.S. and incorporated herein by reference. U.S. application Ser. No. 08/196,192 has a §371 date of Dec. 27, 1994 and a §102(e) date of Dec. 27, 1994. PCT/GB92/01587 was published as WO93/05064, has a publication date of Mar. 18, 1993, and claims priority from United Kingdom patent application No. 9118478, filed Aug. 29, 1991. U.S. Ser. No. 09/111,927 was also a continuation-in-part of PCT patent application number PCT/GB97/00600, filed Mar. 4, 1997, designating the U.S., and claiming priority from United Kingdom patent applications 9604709.7 and 9605725.2, filed Mar. 5 and 19, 1996, respectively. PCT/GB97/00600 was published as WO 97/32872 on Sep. 12, 1997. U.S. Ser. No. 09/111,927 was also a continuation-in-part of PCT patent application number PCT/GB97/00444, filed Feb. 17, 1997, designating the U.S., and claiming priority from United Kingdom patent application 9603325.3, filed Feb. 16, 1996. PCT/GB97/00444 was published as WO 97/30041 on Aug. 21, 1997. U.S. Ser. No. 09/111,927 was also a continuation-in-part of PCT patent application number PCT/GB97/03352, filed Dec. 4, 1997, designating the U.S., and claiming priority from United Kingdom patent application 9625334.9, filed Dec. 5, 1996. PCT/GB97/03352 was published as WO 98/24802 on Jun. 11, 1998. Each of PCT/GB97/00600 (WO 97/32872), PCT/GB97/00444 (WO 97/30041), and PCT/GB97/03352 (WO 98/24802) is hereby incorporated herein by reference.
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Continuation in Parts (4)
|
Number |
Date |
Country |
Parent |
08/458352 |
Jun 1995 |
US |
Child |
09/111927 |
|
US |
Parent |
PCT/GB97/03352 |
Dec 1997 |
US |
Child |
09/111927 |
|
US |
Parent |
PCT/GB97/00600 |
Mar 1997 |
US |
Child |
PCT/GB97/03352 |
|
US |
Parent |
PCT/GB97/00444 |
Feb 1997 |
US |
Child |
PCT/GB97/00600 |
|
US |