Claims
- 1. A method of inhibiting steroid sulphatase activity in a subject in need of same, comprising administering to said subject a steroid sulphatase inhibiting amount of a compound which comprises a ring system and a sulphamate group of the formula: ##STR99## wherein each of R.sub.1 and R.sub.2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl, or together represent alkylene optionally containing one or more hetero atoms or groups in the alkylene chain; and wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (EC 3.1.6.2); and wherein when the sulphamate group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (EC 3.1.6.2) at a pH of 7.4 and 37.degree. C. it provides a K.sub.m value of less than 50 .mu.M.
- 2. A method of inhibiting steroid sulphatase activity in a subject in need of same, comprising administering to said subject a steroid sulphatase inhibiting amount of a compound which comprises a non-steroidal ring system and a sulphamate group of the formula: ##STR100## wherein each of R.sub.1 and R.sub.2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl, or together represent alkylene optionally containing one or more hetero atoms or groups in the alkylene chain; and wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (EC 3.1.6.2); and wherein when the sulphamate group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (EC 3.1.6.2) at a pH of 7.4 and 37.degree. C. it provides a K.sub.m value of less than 50 .mu.M.
- 3. The method according to any one of claims 1 or 2, wherein the compound comprises a six membered ring to which is attached the sulphamate group.
- 4. The method of claim 3 wherein the six membered ring is a six membered carbon ring to which is attached the sulphamate group.
- 5. The method according to any one of claims 1 or 2, wherein at least one of R.sub.1 and R.sub.2 is hydrogen.
- 6. The method according to any one of claims 1 or 2, wherein R.sub.1 and R.sub.2 together represent alkylene optionally containing one or more hetero atoms or groups in the alkylene chain.
Priority Claims (1)
Number |
Date |
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Kind |
9118478 |
Aug 1991 |
GBX |
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RELATED APPLICATIONS
This application is 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, 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. U.S. application Ser. No. 08/196,192 has a .sctn.371 date of Dec. 27, 1994 and a .sctn.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 Kingdon patent application No. 9118478, filed Aug. 29, 1991. This application is also a continuation-in-part of PCT patent application number PCT/GB97/00600, filed March 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. This application is 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. This application is 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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Date |
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0 403 185 |
Dec 1990 |
EPX |
2133484 |
Dec 1972 |
FRX |
1398026 |
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GBX |
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Related Publications (3)
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Number |
Date |
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PCTGB9700600 |
Mar 1997 |
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PCTGB9700444 |
Feb 1997 |
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PCTGB9703352 |
Dec 1997 |
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Divisions (1)
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Date |
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Parent |
196192 |
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Continuation in Parts (1)
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Number |
Date |
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Parent |
458352 |
Jun 1995 |
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