Claims
- 1. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a ring system compound present in an amount to provide 100-500 mg of compound per unit dose;wherein the ring system compound has a ring system and a sulphamate group of the formula: wherein each of R1 and R2 is independently selected from II, alkyl, alkenyl, cycloalkyl and aryl, and at least one of R1 and R2 is H; 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 it provides a substrate for a steroid sulphatase enzyme (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° C. it provides a Km value of less than 50 μM.
- 2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a ring system compound present in a pharmaceutically effective amount;wherein the ring system compound has a ring system and a sulphamate group of the formula: wherein each of R1 and R2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl, and at least one of R1 and R2 is II; wherein the ring system has at least three rings, wherein at least two of those rings are fused; 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 it provides a substrate for a steroid sulphatase enzyme (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° C. it provides a Km value of less than 50 μM.
- 3. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a ring system compound present in a pharmaceutically effective amount;wherein the ring system compound has 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, and at least one of R1 and R2 is H; 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 it provides a substrate for a steroid sulphatase enzyme (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° C. it provides a Km value of less than 50 μM.
Priority Claims (1)
Number |
Date |
Country |
Kind |
9118478 |
Aug 1991 |
GB |
|
Parent Case Info
This application is 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(c) 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. 9118578, filed Aug. 29, 1991. U.S. Ser. No. 09/111,927 was also a continuation-in-part of PCT patent application No. 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 No. 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 No. 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.
US Referenced Citations (8)
Foreign Referenced Citations (7)
Number |
Date |
Country |
645975 |
Feb 1994 |
AU |
114806 |
Aug 1975 |
DE |
0 403 185 |
Dec 1990 |
EP |
1398026 |
Jun 1975 |
GB |
WO9730041 |
Aug 1997 |
WO |
WO9732872 |
Sep 1997 |
WO |
WO9824802 |
Jun 1998 |
WO |
Non-Patent Literature Citations (6)
Entry |
Stoler “Animal Experimental Contribution to the Development of Estrogenic Substances”, Dissertation for award of Doctor of Science degree at the Mathematic-Naturwissenschaftlichh-Technischen faculty of Friedrich-Schiller-University Jena, Jul. 1989. |
Clausen Erythrocytes as a drug carrier—Investigations with selected estrogens for loading following oral administration, Natural Science Faculty, Science Council, Martin-Luther Unversitat Halle-Wittenberg, Germany, Aug. 1989. |
Schwarz et al., Pharmazie, vol. 30 (1975), pp. 17-21. |
Howarth et al., J. Med. Chem., vol. 37 (1994), pp. 219-221. |
Zeitschrift Fur Chemie, vol. 14, No. 1, 1974 pp. 15-16. |
Townsley et al., Research Steroids, vol. 5 (1973), pp. 73-78. |
Continuation in Parts (4)
|
Number |
Date |
Country |
Parent |
08/458352 |
Jun 1995 |
US |
Child |
09/111927 |
|
US |
Parent |
PCT/GB97/00600 |
Mar 1997 |
US |
Child |
08/196192 |
|
US |
Parent |
PCT/GB97/00444 |
Feb 1997 |
US |
Child |
PCT/GB97/00600 |
|
US |
Parent |
PCT/GB97/03352 |
Dec 1997 |
US |
Child |
PCT/GB97/00444 |
|
US |