Claims
- 1. A compound of the formula, or a pharmaceutically acceptable salt thereof: ##STR12## where R is H, alkyl, cycloalkyl, alkenyl or aryl; and the group --O-- polycycle represents the residue of a sterol the sulfate of which is hydrolyzable by an enzyme having steroid sulphatase (E.C. 3.1.6.2) activity excluding cholest-5-en-3-ol(3..beta.-hydrogen phosphonate) and provided R is not methyl.
- 2. A compound according to claim 1, wherein the sterol is a 3-sterol.
- 3. A compound according to claim 1, wherein the sterol is selected from the group consisting of oestrone, a substituted oestrone, dehydroepiandrosterone, oestradiol, substituted oestradiol, oestriol and substituted oestriol.
- 4. A compound according to claim 1 where R is alkyl, cycloalkyl or aryl containing up to 10 carbon atoms.
- 5. A compound according to claim 4, wherein R is C.sub.2 -C.sub.5 alkyl, phenyl or tolyl.
- 6. Oestrone-3-phosphonate.
- 7. Oestrone-3-phenylphosphonate.
- 8. Oestrone-3-ethylphosphonate.
- 9. A pharmaceutical composition comprising in admixture with a pharmaceutically acceptable diluent or carrier a compound of the formula: ##STR13## where R is H, alkyl, cycloalkyl, alkenyl or aryl; and the group --O-- polycycle represents the residue of a sterol the sulfate of which is hydrolyzable by an enzyme having steroid sulphatase (E.C. 3.1.6.2) activity, or a pharmaceutically acceptable salt thereof provided R is not methyl.
- 10. A composition according to claim 9, wherein the sterol is a 3-sterol.
- 11. A composition according to claim 9, wherein the sterol is selected from the group consisting of oestrone, a substituted oestrone, dehydroepiandrosterone, oestradiol, substituted oestradiol, oestriol and substituted oestriol.
- 12. A composition according to claim 9 where R is alkyl, cycloalkyl or aryl containing up to 10 carbon atoms.
- 13. A composition according to claim 12, wherein R is C.sub.2 -C.sub.5 alkyl, phenyl or tolyl.
- 14. The composition according to claim 9 wherein the compound is oestrone-3-phosphonate, oestrone-3-phenylphosphonate or oestrone-3-ethylphosphonate.
Priority Claims (1)
Number |
Date |
Country |
Kind |
9118465 |
Aug 1991 |
GBX |
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Parent Case Info
This is a divisional of application Ser. No. 08/196,191, filed Dec. 27, 1994 now U.S. Pat. No. 5,674,215 which is a continuation of PCT/GB92/01586 filed Aug. 28, 1992.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
4937237 |
Holt et al. |
Jun 1990 |
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5177064 |
Bodor et al. |
Jan 1993 |
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Non-Patent Literature Citations (5)
Entry |
Riess et al, Bulletin de la Societe Chemique de France pp. 933-941 1965. |
CA101:171353, Gibbs et al, 1984. |
RN 1100-39-5, 1967. |
RN 2358-82-9, 1967. |
RN 4281-98-5, 1967. |
Divisions (1)
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Number |
Date |
Country |
Parent |
196191 |
Dec 1994 |
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